Tofranil-PM

Generic Name: imipramine (im IP ra meen)

Brand Names: Tofranil, Tofranil-PM

What is Tofranil-PM (imipramine)?

Imipramine is in a group of drugs called tricyclic antidepressants. Imipramine affects chemicals in the brain that may become unbalanced.

Imipramine is used to treat symptoms of depression.

Imipramine may also be used for purposes other than those listed in this medication guide.

What is the most important information I should know about Tofranil-PM (imipramine)?

Do not use imipramine if you have recently had a heart attack, or if you have used an MAO inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam), or tranylcypromine (Parnate) within the past 14 days.

You may have thoughts about suicide when you first start taking an antidepressant, especially if you are younger than 24 years old. Your doctor will need to check you at regular visits for at least the first 12 weeks of treatment.

Video: Treatment for Depression

Treatments for depression are getting better everyday and there are things you can start doing right away.

Call your doctor at once if you have any new or worsening symptoms such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself.

What should I discuss with my healthcare provider before taking Tofranil-PM (imipramine)?

Do not use this medication if you are allergic to imipramine, or if you have recently had a heart attack. Do not use imipramine if you have used an MAO inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam), or tranylcypromine (Parnate) within the past 14 days. Serious, life-threatening side effects can occur if you take imipramine before the MAO inhibitor has cleared from your body.

Before taking imipramine, tell your doctor if you are allergic to any drugs, or if you have:

• 
  

  heart disease;

  
  


• 
  

  a history of heart attack, stroke, or seizures;

  
  


• 
  

  bipolar disorder (manic-depression);

  
  


• kidney or liver disease;


• 
  

  overactive thyroid;

  
  


• 
  

  diabetes (imipramine may raise or lower blood sugar);

  
  


• 
  

  adrenal gland tumor (pheochromocytoma);

  
  


• 
  

  glaucoma; or

  
  


• 
  

  problems with urination.

  
  

If you have any of these conditions, you may not be able to use imipramine, or you may need a dosage adjustment or special tests during treatment.

You may have thoughts about suicide when you first start taking an antidepressant, especially if you are younger than 24 years old. Tell your doctor if you have worsening symptoms of depression or suicidal thoughts during the first several weeks of treatment, or whenever your dose is changed.

Your family or other caregivers should also be alert to changes in your mood or symptoms. Your doctor will need to check you at regular visits for at least the first 12 weeks of treatment.

This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Imipramine can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not give this medication to anyone younger than 18 years old without the advice of a doctor.

How should I take Tofranil-PM (imipramine)?

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Your doctor may occasionally change your dose to make sure you get the best results from this medication. Follow the directions on your prescription label.

If you need to have any type of surgery, tell the surgeon ahead of time that you are taking imipramine. You may need to stop using the medicine for a short time.

Do not stop using imipramine without first talking to your doctor. You may need to use less and less before you stop the medication completely. Stopping this medication suddenly could cause you to have unpleasant side effects. It may take up to 3 weeks of using this medicine before your symptoms improve. For best results, keep using the medication as directed. Talk with your doctor if your symptoms do not improve after 3 weeks of treatment. Store imipramine at room temperature away from moisture and heat.

What happens if I miss a dose?

Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at the next regularly scheduled time. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine. An overdose of imipramine can be fatal.

Symptoms of an imipramine overdose may include uneven heartbeats, extreme drowsiness, agitation, vomiting, blurred vision, sweating, muscle stiffness, swelling, shortness of breath, blue lips or fingernails, feeling light-headed, fainting, seizure (convulsions), or coma.

What should I avoid while taking Tofranil-PM (imipramine)?

Avoid drinking alcohol. It can cause dangerous side effects when taken together with imipramine.

Avoid using other medicines that make you sleepy (such as cold medicine, pain medication, muscle relaxers, medicine for seizures, or other antidepressants). They can add to sleepiness caused by imipramine.

Grapefruit and grapefruit juice may interact with imipramine. Discuss the use of grapefruit products with your doctor before increasing or decreasing the amount of grapefruit products in your diet.

Imipramine can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert. Avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). Imipramine can make your skin more sensitive to sunlight and sunburn may result. Use a sunscreen (minimum SPF 15) and wear protective clothing if you must be out in the sun.

Tofranil-PM (imipramine) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any new or worsening symptoms such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself.

Call your doctor at once if you have any of these serious side effects:

• 
  

  fast, pounding, or uneven heart rate;

  
  


• 
  

  chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;

  
  


• 
  

  sudden numbness or weakness, especially on one side of the body;

  
  


• 
  

  sudden headache, confusion, problems with vision, speech, or balance;

  
  


• 
  

  feeling short of breath, even with mild exertion;

  
  


• 
  

  swelling, rapid weight gain;

  
  


• 
  

  confusion, hallucinations, or seizure (convulsions);

  
  


• 
  

  easy bruising or bleeding, unusual weakness;

  
  


• 
  

  restless muscle movements in your eyes, tongue, jaw, or neck;

  
  


• 
  

  urinating more or less than usual;

  
  


• 
  

  extreme thirst with headache, nausea, vomiting, and weakness;

  
  


• 
  

  skin rash, bruising, severe tingling, numbness, pain, or muscle weakness.

  
  

Less serious side effects may be more likely to occur, such as:

• 
  

  nausea, vomiting, stomach pain, loss of appetite;

  
  


• 
  

  constipation or diarrhea;

  
  


• 
  

  dry mouth, unpleasant taste;

  
  


• 
  

  weight changes;

  
  


• 
  

  weakness, lack of coordination;

  
  


• 
  

  feeling dizzy, drowsy, or tired;

  
  


• 
  

  nightmares;

  
  


• 
  

  blurred vision, headache, ringing in your ears;

  
  


• 
  

  breast swelling (in men or women); or

  
  


• 
  

  decreased sex drive, impotence, or difficulty having an orgasm.

  
  

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Tofranil-PM (imipramine)?

Before taking imipramine, tell your doctor if you have used an "SSRI" antidepressant in the past 5 weeks, such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), or sertraline (Zoloft).

Before taking imipramine, tell your doctor if you are currently using any of the following drugs:

• 
  

  cimetidine (Tagamet);

  
  


• 
  

  clonidine (Catapres);

  
  


• 
  

  guanethidine (Ismelin);

  
  


• 
  

  methylphenidate (Concerta, Ritalin, Daytrana); or

  
  


• 
  

  heart rhythm medications such as flecainide (Tambocor), propafenone (Rhythmol), or quinidine (Cardioquin, Quinidex, Quinaglute).

  
  

If you are using any of these drugs, you may not be able to use imipramine, or you may need dosage adjustments or special tests during treatment.

There are many other medicines that can interact with imipramine. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.

More Tofranil-PM resources

• Tofranil-PM Side Effects (in more detail)
• Tofranil-PM Use in Pregnancy & Breastfeeding
• Drug Images
• Tofranil-PM Drug Interactions
• Tofranil-PM Support Group
• 0 Reviews for Tofranil-PM - Add your own review/rating

• Tofranil-PM Prescribing Information (FDA)


• Tofranil-PM Advanced Consumer (Micromedex) - Includes Dosage Information


• Tofranil-PM MedFacts Consumer Leaflet (Wolters Kluwer)


• Imipramine Prescribing Information (FDA)


• Imipramine MedFacts Consumer Leaflet (Wolters Kluwer)


• Imipramine Professional Patient Advice (Wolters Kluwer)


• Imipramine Hydrochloride Monograph (AHFS DI)


• Tofranil Prescribing Information (FDA)

Compare Tofranil-PM with other medications

• ADHD
• Depression
• Interstitial Cystitis
• Night Terrors
• Pain
• Panic Disorder
• Primary Nocturnal Enuresis

Where can I get more information?

• Your pharmacist has information about imipramine written for health professionals that you may read.

See also: Tofranil-PM side effects (in more detail)

Trimethoprim

Class: Urinary Anti-infectives
VA Class: AM900
CAS Number: 738-70-5
Brands: Primsol, Proloprim

Introduction

Antibacterial; folate-antagonist anti-infective.^b Commercially available alone or in fixed combination with sulfamethoxazole.^b For information on the fixed combination, see Co-trimoxazole (Systemic).

Uses for Trimethoprim

Acute Otitis Media (AOM)

Treatment of AOM caused by Streptococcus pneumoniae and Haemophilus influenzae.¹²⁴

Consider use of an alternative anti-infective if Moraxella catarrhalis is suspected; this organism is resistant to trimethoprim.¹²⁴

Do not use for AOM in adults or in children <6 months of age.¹²⁴

Do not use for prophylaxis of AOM or for prolonged periods in any age group.¹²⁴

Urinary Tract Infections (UTIs)

Treatment of initial episodes of acute, uncomplicated UTIs caused by susceptible Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Enterobacter, or coagulase-negative Staphylococcus (including S. saprophyticus).^{106 124}

Has been used for treatment of chronic and recurrent UTIs†, but is less effective than other anti-infectives (e.g., co-trimoxazole) for these infections.^b

Pneumocystis jiroveci (Pneumocystis carinii) Pneumonia

Used in conjunction with dapsone as an alternative to co-trimoxazole for treatment of initial episodes of mild to moderate Pneumocystis jiroveci (formerly Pneumocystis carinii) pneumonia† (PCP) in HIV-infected adults.^{102 110 115 119 120 121 125}

Should not be used alone for treatment of PCP.^b

Travelers’ Diarrhea

Has been used for treatment and prevention of travelers’ diarrhea†.^{111 112 113 114 115 116 117}

Fluoroquinolones (ciprofloxacin, levofloxacin, norfloxacin, ofloxacin) usually drugs of choice when anti-infective treatment or prevention of travelers’ diarrhea is indicated; co-trimoxazole is an alternative for treatment when fluoroquinolones cannot be used (e.g., in children).^{114 123}

Trimethoprim Dosage and Administration

Administration

Oral Administration

Administer orally.^{106 124}

Dosage

Pediatric Patients

Acute Otitis Media (AOM)

Oral

Children ≥6 months of age: 10 mg/kg daily in 2 divided doses every 12 hours given for 10 days.¹²⁴

Adults

Urinary Tract Infections (UTIs)

Acute, Uncomplicated UTIs

Oral

100 mg every 12 hours or 200 mg once daily for 10–14 days.^{106 124 b}

Pneumocystis jiroveci (Pneumocystis carinii) Pneumonia†

Treatment of PCP†

Oral

5 mg/kg 3 times daily for 21 days; used in conjunction with dapsone (100 mg once daily for 21 days).^{110 115 119 125}

Special Populations

Renal Impairment

Urinary Tract Infections (UTIs)

Acute, Uncomplicated UTIs

Oral

Doses and/or frequency of administration must be modified in response to the degree of renal impairment.^{106 124 b}

50 mg every 12 hours in adults with Cl_cr 15–30 mL/minute.^{106 124}

Manufacturers recommend the drug not be used in patients with Cl_cr <15 mL/minute;^{106 124} some clinicians suggest the drug can be used in reduced dosages in these patients.^b

Geriatric Patients

Cautious dosage selection because of age-related decreases in renal, hepatic, and/or cardiac function.¹⁰⁶ Initiate therapy at the lower end of the dosing range.¹⁰⁶ (See Geriatric Precautions under Cautions.)

Cautions for Trimethoprim

Contraindications

• 
  

  Hypersensitivity to trimethoprim.^{106 124}

  
  


• 
  

  Documented megaloblastic anemia secondary to folate deficiency.^{106 124}

  
  

Warnings/Precautions

Warnings

Hematologic Effects

Hematologic toxicity (as the result of trimethoprim-induced inhibition of dihydrofolate reductase) has resulted in thrombocytopenia, neutropenia, megaloblastic anemia, and methemoglobinemia.^b

Hematologic toxicity occurs most frequently in folate-depleted patients including geriatric, malnourished, alcoholic, pregnant, or debilitated patients; in patients receiving folate antimetabolites (e.g., phenytoin); in patients with hemolysis or impaired renal function; and in patients receiving high trimethoprim dosage for prolonged periods (e.g., >6 months).^b

Clinical signs such as sore throat, fever, pallor, or purpura may be early indications of serious blood disorders.^{106 124} If such signs occur, perform CBC; discontinue trimethoprim if a clinically important decrease in any formed blood element occurs.^{106 124}

Use caution in patients with possible folate deficiency.^{106 124}

Folic acid may be administered during trimethoprim therapy and will not interfere with the drug’s antibacterial effect.^{124 b} Leucovorin (folinic acid) should be administered if bone marrow depression occurs.^b Hematologic abnormalities usually resolve following administration of leucovorin (3–15 mg daily for 3 days or until normal hematopoiesis is restored).^b

Sensitivity Reactions

Hypersensitivity Reactions

Most frequent adverse reactions are rash and pruritus.¹⁰⁶

Serious hypersensitivity reactions reported rarely, including anaphylaxis,¹⁰⁶ exfoliative dermatitis,¹⁰⁶ toxic epidermal necrolysis,^{106 107 108} erythema multiforme,¹⁰⁶ and Stevens-Johnson syndrome.^{106 105 106 107 108}

Photosensitivity

Photosensitivity (e.g., erythematous phototoxic eruptions with subsequent hyperpigmentation of sun-exposed skin) has been reported.^{105 106}

General Precautions

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of trimethoprim and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.¹⁰⁶

Specific Populations

Pregnancy

Category C.^{106 124}

Because trimethoprim may interfere with folic acid metabolism, use during pregnancy only if potential benefits justify risk to the fetus.^{106 124}

Lactation

Distributed into milk.^{106 124} Because trimethoprim may interfere with folic acid metabolism, use caution in nursing women.^{106 124}

Pediatric Use

Safety and efficacy not established in infants <2 months of age.^{106 124}

Efficacy for treatment of AOM not established in children <6 months of age.¹²⁴

It has been suggested that trimethoprim be used with caution in children who have the fragile X chromosome associated with mental retardation, because folate depletion may worsen the psychomotor regression associated with the disorder.^b

Geriatric Use

Experience in those ≥65 years of age insufficient to determine whether they respond differently than younger adults.¹⁰⁶

Hyperkalemia reported in geriatric patients receiving fixed combination of trimethoprim and sulfamethoxazole (co-trimoxazole).¹⁰⁶

Substantially eliminated by kidneys; risk of adverse effects increased in patients with renal impairment.¹⁰⁶ Consider monitoring potassium concentrations and renal function (e.g., Cl_cr) since geriatric patients more likely to have decreased renal function.¹⁰⁶

Caution advised; start at the lower end of the dosing range due to greater frequency of decreased renal, hepatic, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly.¹⁰⁶

Hepatic Impairment

Use with caution.¹⁰⁶

Renal Impairment

Use with caution.¹⁰⁶

Manufacturers recommend trimethoprim not be used in patients with Cl_cr <15 mL/minute.^{106 124}

Common Adverse Effects

Hypersensitivity (rash, pruritus), GI effects (epigastric discomfort, nausea, diarrhea, vomiting, glossitis, abnormal taste sensation).^{106 b 124}

Interactions for Trimethoprim

Specific Drugs and Laboratory Tests

Drug or Test	Interaction	Comments
Phenytoin	May inhibit phenytoin metabolism resulting in increased half-life and decreased clearance of phenytoin104 106 124	Monitor closely for signs of phenytoin toxicity;106 124 reduce phenytoin dosage if necessaryb
Tests for creatinine	Possible interference with Jaffe alkaline picrate assay resulting in falsely elevated creatinine concentrations106 124
Tests for methotrexate	Possible interference with serum methotrexate assays if competitive binding protein technique (CBPA) is used with a bacterial dihydrofolate reductase as the binding protein;106 124 interference does not occur if methotrexate is measured using radioimmunoassay (RIA)106 124

Trimethoprim Pharmacokinetics

Absorption

Bioavailability

Rapidly^{106 124 b} and almost completely absorbed from GI tract.^b

Steady-state concentrations attained within 2–3 days.¹²⁴ Peak serum concentrations attained within 1–4 hours after a dose.^{106 124 b}

Distribution

Extent

Widely distributed into body tissues and fluids, including aqueous humor, middle ear fluid, saliva, lung tissue, sputum, seminal fluid, prostatic tissue and fluid, vaginal secretions, bile, and bone.^{106 124 b}

Distributed into CSF.^b In patients with uninflamed meninges receiving oral trimethoprim, CSF concentrations are approximately 13–34% of concurrent serum concentrations.^b CSF concentrations somewhat higher if meninges are inflamed.^b

Readily crosses the placenta;^{106 124 b} amniotic fluid concentrations are 80% of concurrent maternal serum concentrations.^b

Distributed into milk^{106 124 b} in concentrations approximately 125% those of concurrent maternal serum concentrations.^b

Plasma Protein Binding

42–46% bound to plasma proteins.^{106 124 b}

Elimination

Metabolism

10–20%¹⁰⁶ of a dose is metabolized in the liver to oxide and hydroxylated metabolites.^{106 124 b}

Elimination Route

Eliminated in urine via glomerular filtration and tubular secretion.^{106 124 b} Only small amounts excreted in feces via biliary elimination.^b

In adults with normal renal function, approximately 50–60 and 56–70% of an oral dose is excreted in urine within 24 and 72 hours, respectively.^{106 b} Approximately 80% of the amount recovered in urine is unchanged drug.^{106 124 b}

Hemodialysis is only moderately effective in removing trimethoprim; not removed by peritoneal dialysis.¹⁰⁶

Half-life

8–11 hours in adults with normal renal function.^{106 b}

7.7 hours in children <1 year of age and 5.5 hours in children 1–10 years of age.^b

Special Populations

Half-life is prolonged in patients with renal impairment.^{124 b} Half-life is 15 hours in adults with Cl_cr 10–30 mL/minute and may increase to >26 hours in those with Cl_cr ≤10 mL/minute.^b

Stability

Storage

Oral

Solution

15–25°C in tight, light-resistant container.¹²⁴

Tablets

15–25°C in tight, light-resistant container in a dry place.¹⁰⁶

Actions and SpectrumActions

• 
  

  A folate antagonist that inhibits formation of tetrahydrofolic acid (the metabolically active form of folic acid) in susceptible bacteria.^{106 124 b}

  
  


• 
  

  Inhibits reduction of dihydrofolic acid to tetrahydrofolic acid by binding to the enzyme dihydrofolate reductase^{106 124} and inhibits bacterial thymidine synthesis.^b

  
  


• 
  

  Usually slowly bactericidal.^b

  
  


• 
  

  Spectrum of activity includes some gram-positive aerobes and some gram-negative aerobes, including some Enterobacteriaceae.^{106 b} Inactive against most anaerobes and inactive against Mycobacterium and Chlamydia.^b

  
  


• 
  

  Gram-positive aerobes: Active against coagulase-negative staphylococci (including Staphylococcus saprophyticus)^{106 124} and Streptococcus pyogenes (group A β-hemolytic streptococci),^b and S. pneumoniae (penicillin-susceptible strains).¹²⁴ May be active against some, but not all, strains of Enterococcus faecalis.^b

  
  


• 
  

  Gram-negative aerobes: Active against Acinetobacter, Citrobacter, Enterobacter,^{106 124} Escherichia coli,^{106 124} Haemophilus influenzae (except β-lactamase-negative, ampicillin-resistant strains),¹²⁴ Klebsiella pneumoniae,^{106 124} Proteus mirabilis,^{106 124} Salmonella, and Shigella. Also active against some, but not all, strains of Providencia and Serratia.^b Inactive against Moraxella catarrhalis¹²⁴ and Pseudomonas aeruginosa.^{106 b}

  
  


• 
  

  Resistant strains of Enterobacteriaceae, especially E. coli, Klebsiella, and Proteus, have developed during trimethoprim therapy.^b

  
  

Advice to Patients

• 
  

  Importance of completing full course of therapy, even if feeling better after a few days.

  
  


• 
  

  Importance of reporting clinical signs that may be early indications of serious blood disorders (e.g., sore throat, fever, pallor, purpura).¹⁰⁶

  
  


• 
  

  Importance of discontinuing use and contacting clinician if signs or symptoms of sensitization occur.¹⁰⁶

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  
  


• 
  

  Importance of informing patients of other important precautionary information. (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Trimethoprim

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	100 mg*	Proloprim (scored)	Monarch
			Trimethoprim Tablets	Teva, Watson

Trimethoprim Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Solution	50 mg (of trimethoprim per 5 mL)	Primsol	FSC

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Trimethoprim 100MG Tablets (WATSON LABS): 30/$19.99 or 90/$40.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions July 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. Gross RJ, Threlfall EJ, Ward LR et al. Drug resistance in Shigella dysenteriae, S. flexneri and S. boydii in England and Wales: increasing incidence of resistance to trimethoprim. BMJ. 1984; 288:784-6. [IDIS 183288] [PubMed 6423079]

101. Ling J, Chin PY. Plasmids mediating resistance to chloramphenicol, trimethoprim, and ampicillin in Salmonella typhi strains isolated in the Southeast Asian region. J Infect Dis. 1984; 149:652. [IDIS 184846] [PubMed 6725997]

102. Leoung GS, Mills J, Hopewell PC et al. Dapsone-trimethoprim for Pneumocystis carinii pneumonia in the acquired immunodeficiency syndrome. Ann Intern Med. 1986; 105:45-8. [IDIS 217842] [PubMed 2940954]

103. Hughes WT, Smith BL. Efficacy of diaminodiphenylsulfone and other drugs in murine Pneumocystis carinii pneumonitis. Antimicrob Agents Chemother. 1984; 26:436-40. [PubMed 6335017]

104. Hansen JM, Kampmann JP, Siersbaek-Nielsen K et al. The effect of different sulfonamides on phenytoin metabolism in man. Acta Med Scand Suppl. 1979; 624:106-10. [PubMed 284708]

105. Chandler MJ. Recurrence of phototoxic skin eruptions due to trimethoprim. J Infect Dis. 1986; 153:1001. [IDIS 215212] [PubMed 2939152]

106. Monarch. Proloprim (trimethoprim) tablets prescribing information. Bristol, TN; 2003 Feb.

107. Nwokolo C, Byrne L, Misch KJ. Toxic epidermal necrolysis occurring during treatment with trimethoprim alone. BMJ. 1988; 296:970. [IDIS 240187] [PubMed 3129113]

108. Das G, Bailey MJ, Wickham JEA. Toxic epidermal necrolysis and trimethoprim. BMJ. 1988; 296:1604-5. [IDIS 242513] [PubMed 3135031]

109. Hedlund J, Aurelius E, Andersson J. Recurrent encephalitis due to trimethoprim intake. Scand J Infect Dis. 1990; 22:109-12. [PubMed 2320959]

110. Fishman JA. Treatment of infection due to Pneumocystis carinii. Antimicrob Agents Chemother. 1998; 42:1309-14. [IDIS 408066] [PubMed 9624465]

111. DuPont HL, Reves RR, Galindo E et al. Treatment of travelers’ diarrhea with trimethoprim/sulfamethoxazole and with trimethoprim alone. N Engl J Med. 1982; 307:841-4. [IDIS 157110] [PubMed 7050714]

112. National Institutes of Health Office of Medical Applications of Research. Consensus conference: travelers’ diarrhea. JAMA. 1985; 253:2700-4. [PubMed 2985834]

113. DuPont HL. Ericsson CD, Johnson PC. Chemotherapy and chemoprophylaxis of travelers’ diarrhea. Ann Intern Med. 1985; 102:260-1. [IDIS 195784] [PubMed 3966763]

114. Centers for Disease Control and Prevention. Health information for international travel, 2003–2004. Atlanta, GA: US Department of Health and Human Services; 2003:184-91. Updates available from CDC website ().

115. Safrin S, Finkelstein DM, Feinberg J et al. Comparison of three regimens for treatment of mild to moderate Pneumocystis carinii pneumonia in patients with AIDS: a double-blind, randomized trial of oral trimethoprim—sulfamethoxazole, dapsone—trimethoprim, and clindamycin-primaquine. Ann Intern Med. 1996; 124:792-802. [IDIS 364834] [PubMed 8610948]

116. DuPont HL, Ericsson CD, Reves RR et al. Antimicrobial therapy for travelers’ diarrhea. Rev Infect Dis. 1986; 8(Suppl 2):S217-S222. [IDIS 217199] [PubMed 3523718]

117. DuPont HL, Ericsson CD, Galindo E et al. Antimicrobial therapy of travelers’ diarrhea. Scand J Gastroenterol. 1983; 18(Suppl 84):99-105.

118. DuPont HL, Galindo E, Evans DG et al. Prevention of travelers’ diarrhea with trimethoprim-sulfamethoxazole and trimethoprim alone. Gastroenterology. 1983; 84:75-80. [IDIS 164584] [PubMed 6336616]

119. Anon. Drugs for parasitic infections. Med Lett Drugs Ther. Aug 2004. From the Medical Letter website ().

120. Smith GH. Treatment of infections in the patient with acquired immunodeficiency syndrome. Arch Intern Med. 1994; 154:959-73.

121. National Institutes of Health Combined Clinical Staff Conference. Consensus conference: recent advances in the management of AIDS-related opportunistic infections. Ann Intern Med. 1994; 120:945-55. [IDIS 330618] [PubMed 7909657]

122. National Committee for Clinical Laboratory Standards. Performance standards for antimicrobial susceptibility testing: eleventh informational supplement. NCCLS document M100-S12. Wayne, PA; NCCLS: 2002 Jan.

123. Anon. Advice for travelers. Med Lett Treat Guid. 2004; 2:33-40.

124. FSC Laboratories. Primsol (trimethoprim) solution prescribing information. Charlotte, NC; 2005 Apr.

125. Centers for Disease Control and Prevention. Treating opportunistic infections among HIV-infected adults and adolescents: recommendations from CDC, the National Institutes of Health, and the HIV Medicine Association/Infectious Diseases Society of America. MMWR Morb Mortal Wkly Rep. 2004; 53(No. RR-15):1-112.

b. AHFS Drug Information 2004. McEvoy GK, ed. Trimethoprim. Bethesda, MD: American Society of Health-System Pharmacists; 2004:872-4.

More Trimethoprim resources

• Trimethoprim Side Effects (in more detail)
• Trimethoprim Dosage
• Trimethoprim Use in Pregnancy & Breastfeeding
• Drug Images
• Trimethoprim Drug Interactions
• Trimethoprim Support Group
• 0 Reviews for Trimethoprim - Add your own review/rating

• Trimethoprim Prescribing Information (FDA)


• Trimethoprim MedFacts Consumer Leaflet (Wolters Kluwer)


• trimethoprim Concise Consumer Information (Cerner Multum)


• trimethoprim Advanced Consumer (Micromedex) - Includes Dosage Information


• Primsol Solution MedFacts Consumer Leaflet (Wolters Kluwer)


• Proloprim Prescribing Information (FDA)

Compare Trimethoprim with other medications

• Bladder Infection
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Sodium hyaluronate injection

Generic Name: sodium hyaluronate (injection) (SO dee um HYE al yoo RON ate)

Brand Names: Euflexxa, Hyalgan, Supartz

What is sodium hyaluronate?

Sodium hyaluronate is similar to the fluid that surrounds the joints in your body. This fluid acts as a lubricant and shock absorber for the joints.

Sodium hyaluronate is used to treat knee pain caused by osteoarthritis.

Sodium hyaluronate is usually given after other arthritis medications have been tried without successful treatment of symptoms.

Sodium hyaluronate may also be used for purposes not listed in this medication guide.

What is the most important information I should know about sodium hyaluronate?

You should not receive sodium hyaluronate if you are allergic to it, or if you have an infection in your knee or in the skin around your knee.

Before you receive a sodium hyaluronate injection, tell your doctor if you have blood clots or circulation problems in your legs, or an allergy to birds, feathers, or egg products.

For at least 48 hours after your injection, avoid jogging, strenuous activity, high-impact sports, or standing for longer than 1 hour at a time.

Call your doctor at once if you have severe pain or swelling around the knee after the injection.

What should I discuss with my health care provider before receiving sodium hyaluronate?

You should not receive sodium hyaluronate if you are allergic to it, or if you have an infection in your knee or in the skin around your knee.

To make sure you can safely receive sodium hyaluronate, tell your doctor if you have:

• 
  

  blood clots or circulation problems in your legs; or

  
  


• 
  

  an allergy to birds, feathers, or egg products.

  
  

It is not known whether sodium hyaluronate will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication. It is not known whether sodium hyaluronate passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How is sodium hyaluronate given?

Sodium hyaluronate is injected directly into your knee joint. A healthcare provider will give you this injection.

Sodium hyaluronate is usually given once every week for 3 to 5 weeks. Follow your doctor's dosing instructions very carefully.

To prevent pain and swelling, your doctor may recommend resting your knee or applying ice for a short time after your injection.

What happens if I miss a dose?

Call your doctor for instructions if you miss an appointment for your sodium hyaluronate injection.

What happens if I overdose?

Since this medication is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.

What should I avoid after receiving sodium hyaluronate?

For at least 48 hours after your injection, avoid jogging, strenuous activity, or high-impact sports such as soccer or tennis. Also avoid weight-bearing activity or standing for longer than 1 hour at a time. Ask your doctor how long to wait before you resume these activities.

Sodium hyaluronate side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:

• 
  

  severe pain or swelling around the knee after the injection;

  
  


• 
  

  fast heart rate, sweating, chills or shaking; or

  
  


• 
  

  heavy feeling, anxiety, confusion.

  
  

Less serious side effects may include:

• 
  

  warmth, pain, stiffness, swelling, or puffiness where the medicine was injected;

  
  


• 
  

  nausea, stomach pain;

  
  


• 
  

  headache;

  
  


• 
  

  back pain;

  
  


• 
  

  numbness or tingly feeling;

  
  


• 
  

  cold symptoms such as stuffy nose, sneezing, sore throat;

  
  


• 
  

  tired feeling; or

  
  


• 
  

  itching or skin irritation around the knee.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Sodium hyaluronate Dosing Information

Usual Adult Dose for Osteoarthritis:

Hyalgan(R): 2 mL by intra-articular injection into the knee once weekly for 5 weeks
Supartz(TM): 2.5 mL by intra-articular injection into the knee once weekly for 5 weeks

What other drugs will affect sodium hyaluronate?

There may be other drugs that can interact with sodium hyaluronate. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

More sodium hyaluronate resources

• Sodium hyaluronate Use in Pregnancy & Breastfeeding
• Sodium hyaluronate Drug Interactions
• Sodium hyaluronate Support Group
• 28 Reviews for Sodium hyaluronate - Add your own review/rating

Compare sodium hyaluronate with other medications

• Osteoarthritis

Where can I get more information?

• Your doctor can provide more information about sodium hyaluronate.

Trelstar Depot

Pronunciation: TRIP-toe-REL-in
Generic Name: Triptorelin
Brand Name: Examples include Trelstar Depot and Trelstar LA

Trelstar Depot is used for:

Treating symptoms of advanced prostate cancer. It may be used for other conditions as determined by your doctor.

Trelstar Depot is a synthetic analogue of gonadotropin-releasing hormone (GnRH) agonist. It works by decreasing the production of certain hormones, which reduces testosterone levels in the body.

Do NOT use Trelstar Depot if:

• you are allergic to any ingredient in Trelstar Depot, to GnRH, or to another GnRH agonist (eg, goserelin)


• you are pregnant, may become pregnant, or are breast-feeding

Contact your doctor or health care provider right away if any of these apply to you.

Before using Trelstar Depot:

Some medical conditions may interact with Trelstar Depot. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have a history or urinary problems (eg, blockage of the bladder or ureters), spinal cord problems, abnormal growths on or near the spine or spinal cord, heart problems, blood vessel problems, a stroke, diabetes, or high blood sugar

Some MEDICINES MAY INTERACT with Trelstar Depot. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Medicines that increase prolactin levels in the blood (eg, promethazine) because the effectiveness of Trelstar Depot may be decreased

This may not be a complete list of all interactions that may occur. Ask your health care provider if Trelstar Depot may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Trelstar Depot:

Use Trelstar Depot as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Trelstar Depot is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Trelstar Depot at home, a health care provider will teach you how to use it. Be sure you understand how to use Trelstar Depot. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.


• Trelstar Depot is injected into the muscle.


• Rotate the injection site. Do not inject into an area of skin that is red, hard, or bruised, or has scars or stretch marks.


• Do not use Trelstar Depot if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.


• Keep this product, as well as syringes and needles, out of the reach of children and pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Ask your doctor, nurse, or pharmacist to explain local regulations for selecting an appropriate container and properly disposing of the container when full.


• If you miss a dose of Trelstar Depot, contact your doctor right away.

Ask your health care provider any questions you may have about how to use Trelstar Depot.

Important safety information:

• Trelstar Depot may cause dizziness or vision changes. These effects may be worse if you take it with alcohol or certain medicines. Use Trelstar Depot with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Certain hormone levels may increase during the first few weeks of treatment with Trelstar Depot. This may cause you to experience worsening symptoms or onset of new symptoms (eg, bone pain; blood in the urine; difficulty urinating; burning, numbness, or tingling) during the first few weeks of treatment. Patients with growths on or near the spine or spinal cord, or blockage of the bladder or ureters may be at greater risk of developing serious and sometimes fatal complications. Contact your doctor if any new or worsened symptoms occur while using Trelstar Depot.


• Trelstar Depot lowers the amount of certain hormones in your body. This may cause certain expected side effects to occur, such as breast enlargement, soreness, or tenderness; testicular changes, pain, or soreness; decreased sexual ability; hot flashes; or night sweats. Contact your doctor if you have questions or concerns or if you experience any of these side effects.


• A slight increase in the risk of stroke or serious and sometimes fatal heart problems has been reported with the use of GnRH agonists in men. Although the risk appears to be low, seek immediate medical attention if you experience chest, jaw, or left arm pain; confusion; fainting; numbness of an arm or leg; one-sided weakness; slurred speech; sudden, severe headache or vomiting; or vision changes. Discuss any questions or concerns with your doctor.


• Trelstar Depot may raise your blood sugar. High blood sugar may make you feel confused, drowsy, or thirsty. It can also make you flush, breathe faster, or have a fruit-like breath odor. If these symptoms occur, tell your doctor right away.


• Diabetes patients - Check blood sugar levels closely. Ask your doctor before you change the dose of your diabetes medicine.


• Rarely, a serious pituitary gland problem (pituitary apoplexy) may occur after you use Trelstar Depot. This serious problem usually occurs shortly after you begin to use Trelstar Depot. Contact your doctor immediately if you experience a sudden headache, vomiting, fainting, eye weakness, inability to move your eyes, mental status changes, or vision changes.


• Trelstar Depot may interfere with certain lab tests, including certain hormone and pituitary gland function tests. Be sure your doctor and lab personnel know you are using Trelstar Depot.


• Lab tests, including testosterone,prostate specific antigen (PSA) levels, hemoglobin A_1c, or blood glucose, may be performed while you use Trelstar Depot. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.


• Use Trelstar Depot with extreme caution in CHILDREN; safety and effectiveness in children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: Trelstar Depot may cause harm to the fetus. Do not become pregnant while you are using it. If you think you may be pregnant, contact your doctor right away. You will need to discuss the benefits and risks of using Trelstar Depot while you are pregnant. It is not known if Trelstar Depot is found in breast milk. Do not breast-feed while using Trelstar Depot.

Possible side effects of Trelstar Depot:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Change in breast size; constipation; decreased sexual desire or ability; diarrhea; dizziness; headache; hot flashes; itching, pain, redness, or swelling at the injection site; loss of appetite; nausea; sleeplessness; stomach discomfort; tiredness or weakness; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); back pain; blood in the urine or dark urine; bone pain; breast pain; burning, numbness, or tingling; calf or leg pain or tenderness; fainting; fast or irregular heartbeat; fever, chills, or persistent sore throat; mood or mental changes (eg, depression); painful urination; severe or persistent headache, drowsiness, or dizziness; severe or persistent joint, muscle, or back pain; severe or persistent leg cramps; shortness of breath; sudden, unusual weight gain; swelling of the hands, ankles, feet or legs; symptoms of heart attack (eg, chest, jaw, or left arm pain; numbness of an arm or leg; sudden, severe headache or vomiting); symptoms of high blood sugar (eg, drowsiness; fast breathing; flushing; fruit-like breath odor; increased thirst, hunger, or urination); symptoms of stroke (eg, confusion, one-sided weakness, slurred speech); trouble urinating or inability to urinate; unusual tiredness or weakness; vision changes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Trelstar Depot side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.

Proper storage of Trelstar Depot:

Store Trelstar Depot at room temperature between 68 and 77 degrees F (20 and 25 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Do not freeze. Discard any medicine not used immediately after mixing. Keep Trelstar Depot, as well as needles and syringes, out of the reach of children and away from pets.

General information:

• If you have any questions about Trelstar Depot, please talk with your doctor, pharmacist, or other health care provider.


• Trelstar Depot is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Trelstar Depot. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Trelstar Depot resources

• Trelstar Depot Side Effects (in more detail)
• Trelstar Depot Use in Pregnancy & Breastfeeding
• Trelstar Depot Drug Interactions
• Trelstar Depot Support Group
• 0 Reviews for Trelstar Depot - Add your own review/rating

• Trelstar Depot Prescribing Information (FDA)


• Trelstar Depot Advanced Consumer (Micromedex) - Includes Dosage Information


• Trelstar Depot Concise Consumer Information (Cerner Multum)


• Trelstar LA Prescribing Information (FDA)


• Triptorelin Pamoate Monograph (AHFS DI)

Compare Trelstar Depot with other medications

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Saline Spray

Pronunciation: SAY-leen
Generic Name: Saline
Brand Name: Examples include Rhino-Mist and Salinex

Saline Spray is used for:

Treating dry or irritated nasal passages caused by colds, allergies, low humidity, or overuse of decongestant nose spray.

Saline Spray is a salt solution. It works by rinsing and moisturizing the nostrils.

Do NOT use Saline Spray if:

• you are allergic to any ingredient in Saline Spray

Contact your doctor or health care provider right away if any of these apply to you.

Before using Saline Spray:

Some medical conditions may interact with Saline Spray. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances

Some MEDICINES MAY INTERACT with Saline Spray. However, no specific interactions are known at this time.

This may not be a complete list of all interactions that may occur. Ask your health care provider if Saline Spray may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Saline Spray:

Use Saline Spray as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• To use a nose spray, gently blow your nose. Sit down and tilt your head back slightly. Place the tip of the spray container into the nose. Using a finger from your other hand, press against the opposite nostril to close it off. Breathe gently through the open nostril and squeeze the spray container. If you are using more than 1 spray, wait for 1 to 2 minutes between sprays. After using the medicine, rinse the tip of the spray unit in hot water and dry with a clean tissue to prevent contamination.


• If you miss a dose of Saline Spray, use the dose when you remember and continue to use Saline Spray as directed by your doctor or the package labeling.

Ask your health care provider any questions you may have about how to use Saline Spray.

Important safety information:

• If your symptoms do not improve or if they become worse, check with your doctor.


• PREGNANCY and BREAST-FEEDING: If you become pregnant while taking Saline Spray, discuss with your doctor the benefits and risks of using Saline Spray during pregnancy. If you are or will be breast-feeding while you are using Saline Spray, check with your doctor or pharmacist to discuss the risks to your baby.

Possible side effects of Saline Spray:

All medicines may cause side effects, but many people have no, or minor, side effects. No COMMON side effects have been reported with the proper use of Saline Spray. Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue).

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center ( http://www.aapcc.org), or emergency room immediately.

Proper storage of Saline Spray:

Store Saline Spray at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Saline Spray out of the reach of children and away from pets.

General information:

• If you have any questions about Saline Spray, please talk with your doctor, pharmacist, or other health care provider.


• Saline Spray is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Saline Spray. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Saline resources

• Saline Use in Pregnancy & Breastfeeding
• Saline Support Group
• 0 Reviews for Saline - Add your own review/rating

Compare Saline with other medications

• Nasal Congestion

Stalevo 100

Generic Name: carbidopa, entacapone, and levodopa (Oral route)

lee-voe-DOE-pa, kar-bi-DOE-pa, en-TAK-a-pone

Commonly used brand name(s)

In the U.S.

• Stalevo 100


• Stalevo 125


• Stalevo 150


• Stalevo 50


• Stalevo 75

Available Dosage Forms:

• Tablet

Therapeutic Class: Antiparkinsonian

Pharmacologic Class: Dopamine Precursor

Uses For Stalevo 100

Carbidopa, entacapone, and levodopa combination is used to treat Parkinson's disease, sometimes called shaking palsy. Parkinson's disease is a disorder of the central nervous system (brain and spinal cord).

Dopamine is a naturally occurring substance in the brain that helps provide control of movement and activities such as walking and talking. In patients with Parkinson's disease, there is not enough dopamine in some parts of the brain. Levodopa (a component of this medicine) enters the brain and helps replace the missing dopamine, which allows people to function better. By increasing the amount of dopamine in the brain, levodopa helps control symptoms and helps you to perform daily activities such as dressing, walking, and handling utensils.

This medicine is a combination of three different medicines. This medicine is known as a levodopa therapy. The difference between this medicine and other levodopa treatments is that this medicine contains entacapone. Entacapone helps levodopa last longer by blocking a substance called COMT enzyme. This enzyme breaks down levodopa before it reaches the brain. When less levodopa is broken down, more is available to the brain. Increased availability of levodopa may lead to smoother and steadier levels of dopamine in the brain, which may provide better symptom control for longer periods each day. This may lead to improvement in daily activities.

This medicine is available only with your doctor's prescription.

Before Using Stalevo 100

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of carbidopa, entacapone, and levodopa combination in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date in elderly patients up to age 75 years have not demonstrated geriatrics-specific problems that would limit the usefulness of carbidopa, entacapone, and levodopa combination in the elderly. However, elderly patients are more likely to have age-related kidney, liver, and cardiovascular insufficiency, which may require extra caution.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Clorgyline


• Iproniazid


• Isocarboxazid


• Linezolid


• Nialamide


• Pargyline


• Phenelzine


• Procarbazine


• Selegiline


• Toloxatone


• Tranylcypromine

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Apomorphine


• Bitolterol


• Desipramine


• Dobutamine


• Dopamine


• Epinephrine


• Iproniazid


• Isocarboxazid


• Isoetharine


• Isoniazid


• Isoproterenol


• Linezolid


• Methyldopa


• Moclobemide


• Nialamide


• Norepinephrine


• Pargyline


• Phenelzine


• Procarbazine


• Tranylcypromine


• Venlafaxine

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Bromperidol


• Bupropion


• Droperidol


• Ferric Ammonium Citrate


• Fosphenytoin


• Indinavir


• Iron


• Kava


• Metoclopramide


• Phenylalanine


• Phenytoin


• Spiramycin


• Tyrosine

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• High Protein Food

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Asthma or


• Biliary obstruction or blockage or


• Colitis (inflammation of the colon) or


• Depression, history of or


• Dyskinesia (abnormal muscle movements) or


• Endocrine or metabolic disease or


• Heart attack, history of or


• Heart or blood vessel disease, severe or


• Heart rhythm problems (e.g., ventricular tachycardia) or


• Hypotension (low blood pressure) or


• Kidney disease or


• Liver disease or


• Lung disease, severe or


• Psychosis (mental disorder), or history of or


• Wide-angle glaucoma (eye pressure problem)—Use with caution. May make these conditions worse.

• Melanoma (skin tumor), history of or


• Narrow–angle glaucoma (eye pressure problem) or


• Skin lesions, undiagnosed (rashes that involve changes in color or texture of the skin)—Should not be used in patients with these conditions.

• Peptic ulcer, history of—May increase risk of stomach or bowel hemorrhage.

Proper Use of carbidopa, entacapone, and levodopa

This section provides information on the proper use of a number of products that contain carbidopa, entacapone, and levodopa. It may not be specific to Stalevo 100. Please read with care.

Take this medicine exactly as directed, and every time that you are supposed to take it. It is important that you do not stop taking your medicine unless ordered by your doctor. It is also important to not start taking other medicines for your Parkinson's disease without first talking with your doctor.

Since protein may interfere with the body's response to levodopa, high protein diets should be avoided. Intake of normal amounts of protein should be spaced equally throughout the day, or taken as directed by your doctor.

You may experience a “wearing-off” effect towards the end of the dosing interval. You should tell your doctor if you have problems with this that affect your every day life. Your doctor may want to adjust your dose.

This medicine begins to release its ingredients 30 minutes after you take it.

If you are taking multivitamin tablets or plan to start taking them, discuss this first with your doctor. Iron salts (in vitamins) may keep this medicine from working properly.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage forms (capsules or tablets):
  
  • For Parkinson's disease:
    
    • Adults—The starting dose is usually the same as the current dose you are taking. If you are starting this medicine for the first time, your doctor may want to start you on a carbidopa and levodopa combination with entacapone and gradually switch you over to this combination.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using Stalevo 100

It is very important that your doctor check your progress at regular visits to allow changes in your dose and to check for any unwanted effects.

Do not take this medicine if you have taken a monoamine oxidase (MAO) inhibitor (e.g. phenelzine [Nardil®] or tranylcypromine [Parnate®]) in the past 2 weeks.

Do not stop taking this medicine without first checking with your doctor. Your doctor may want you to gradually reduce the amount you are taking before stopping completely.

Check with your doctor right away if you are having convulsions (seizures); difficulty with breathing; a fast heartbeat; a high fever; high or low blood pressure; increased sweating; loss of bladder control; severe muscle stiffness; unusually pale skin; or tiredness. These could be symptoms of a serious condition called neuroleptic malignant syndrome (NMS).

This medicine may cause dizziness, trouble in controlling movements, or trouble in concentrating or seeing clearly. Make sure you know how you react to this medicine before you drive, use machines, or do other jobs that require you to be alert, well-coordinated, or able to think or see well.

Dizziness, lightheadedness, or fainting may occur with this medicine, especially when you get up from a lying or sitting position suddenly. These symptoms are more likely to occur when you begin taking this medicine, or when the dose is increased. Getting up slowly may also help. If this problem continues or gets worse, check with your doctor.

This medicine may cause diarrhea, and in some cases it can be severe. It can occur months after starting this medicine. Do not take any medicine to treat diarrhea without first checking with your doctor. Diarrhea medicines may make the diarrhea worse or make it last longer. If you have any questions about this or if mild diarrhea continues or gets worse, check with your doctor.

If you develop any unusual or strange thoughts and behavior while receiving this medicine, be sure to discuss it with your doctor. Other changes might be confusion, worsening of depression, visual hallucinations (seeing things that are not there), suicidal thoughts, and unusual excitement, nervousness, or irritability.

Check with your doctor right away if you have dark-colored urine, fever, muscle cramps or spasms, muscle pain or stiffness, or unusual tiredness or weakness. These may be symptoms of a condition called rhabdomyolysis.

Stop using this medicine and check with your doctor right away if you are having shortness of breath, chest tightness, or any type of breathing problem while being treated with this medicine.

It is important that your doctor check your skin regularly for signs of a skin cancer called melanoma. If you notice any unusual red, brown, or black spots on your skin, talk to your doctor right away.

It is possible that a dark color (red, brown, or black) may appear in saliva, urine, or sweat after taking this medicine. The color may cause some of your garments to become discolored. This is normal and nothing to worry about.

It is possible that you may become nauseous, especially when you are first starting your medicine.

Some people who have used this medicine had unusual changes in their behavior. Talk with your doctor right away if you start having problems with gambling or an increased interest in sex while using this medicine.

Before you have any medical tests, tell the medical doctor in charge that you are taking this medicine. The results of some tests may be affected by this medicine.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Stalevo 100 Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common-Entacapone

• Twitching, twisting, or uncontrolled repetitive movements of the tongue, lips, face, arms, or legs

Incidence not known-Carbidopa and Levodopa and/or Levodopa alone

• Bleeding gums


• bloody or black, tarry stools


• bloody or cloudy urine


• change in size, shape, or color of an existing mole


• changes in skin color


• chest pain, discomfort, or tightness


• constipation


• constricted pupil


• convulsions


• cough


• difficult or labored breathing


• difficulty with speaking


• drooling


• drooping eyelid (ptosis)


• facial dryness


• fast, irregular, or pounding heartbeat


• fever with or without chills


• general feeling of illness


• hallucinations (seeing, hearing, or feeling things that are not there)


• hoarseness


• high or low blood pressure


• large, flat, blue, or purplish patches in the skin


• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs


• loss of appetite


• loss of bladder control


• lower abdominal or stomach pain


• lower back or side pain


• mole that leaks fluid or bleeds


• muscle cramps or spasms


• muscle pain or stiffness


• muscle trembling, jerking, or stiffness


• nausea


• pain


• painful or difficult urination


• pinpoint red spots on the skin


• raised red swellings on the skin, the buttocks, legs, or ankles


• restlessness


• seizures


• severe mental changes


• shakiness and unsteady walk


• shuffling walk


• sore throat


• sores, ulcers, or white spots on the lips or in the mouth


• sweating


• swollen glands


• trembling, or other problems with muscle control or coordination


• unusual bleeding or bruising


• unusual tiredness or weakness


• vomiting

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common-Entacapone

• Absence of or decrease in body movement


• diarrhea


• dizziness


• urine discoloration

Less common-Entacapone

• Acid or sour stomach


• anxiety


• belching


• bitter, sour, or unusual taste in the mouth


• bloated


• burning feeling in the chest or stomach


• dry mouth


• excess air or gas in the stomach or intestines


• fear


• full feeling


• heartburn


• hyperventilation


• increased sweating


• indigestion


• irritability


• lack or loss of strength


• nervousness


• passing gas


• restlessness


• sleepiness or unusual drowsiness


• stomach discomfort or upset


• swollen mouth and tongue


• tenderness in the stomach area


• trouble sleeping


• urge to have bowel movement


• wheezing

Incidence not known-Carbidopa and Levodopa and/or Levodopa alone

• Being forgetful


• bladder pain


• blurred vision


• body aches or pain


• burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings


• burning and upper abdominal or stomach pain


• burning sensation of the tongue


• clenching, gnashing, or grinding teeth


• confusion about identity, place, and time


• dark saliva


• dark sweat


• decreased mental acuity


• difficulty swallowing


• discouragement


• double vision


• ear congestion


• enlarged pupils


• excessive watering of the mouth


• fainting


• false or unusual sense of well-being


• feeling like you will pass out


• feeling of warmth


• feeling sad or empty


• flushing


• hair loss


• headache


• hiccups


• hives or welts


• increased blinking


• increased interest in sexual ability, desire, drive, or performance


• increased interest in sexual intercourse


• lack of appetite


• large, hard skin blisters


• leg pain


• loss of voice


• muscle spasm, especially of the neck and back


• nasal congestion


• nightmares


• numbness


• pain in the chest below the breastbone


• painful or prolonged erection of the penis


• pharyngeal pain


• pounding in the ears


• problems with memory or speech


• redness of the face, neck, arms, and occasionally upper chest


• runny nose


• sense of stimulation


• skin rash


• sleeplessness


• slow movement


• slow or fast heartbeat


• slow reflexes


• sneezing


• swelling


• tremor, increased


• trouble concentrating


• trouble recognizing objects


• trouble thinking and planning


• urinary frequency


• urinary retention


• weight gain


• weight loss

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Stalevo00 side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Stalevo 100 resources

• Stalevo 100 Side Effects (in more detail)
• Stalevo 100 Use in Pregnancy & Breastfeeding
• Drug Images
• Stalevo 100 Drug Interactions
• Stalevo 100 Support Group
• 0 Reviews for Stalevo00 - Add your own review/rating

• Stalevo 100 Concise Consumer Information (Cerner Multum)


• Carbidopa/Entacapone/Levodopa MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Stalevo 100 with other medications

• Parkinson's Disease

Tigan

Generic Name: Trimethobenzamide Hydrochloride
Class: Antihistamines
VA Class: GA700
Chemical Name: N-(p-[2-(Dimethylamino)ethoxy]benzyl)-3,4,5,-trimethoxybenzamide monohydrochloride
CAS Number: 554-92-7

Introduction

Antiemetic agent.^{100 101 a}

Uses for Tigan

Nausea and Vomiting

Control of nausea and vomiting,^a including treatment of postoperative nausea and vomiting.^{100 101 a}

Treatment of nausea associated with gastroenteritis.^{100 101 a}

Less effective than phenothiazines, but may be associated with fewer adverse effects.^a

Tigan Dosage and Administration

Administration

Administer orally or by IM injection.^{100 101 a}

Not recommended for IV administration.^{100 101 a}

Preparation for rectal administration^c is no longer commercially available in the US;^{102 103} FDA has withdrawn approval of the new drug application (NDA) for the rectal suppositories because of lack of substantial evidence of efficacy.^{102 103} (See Preparations.)

IM Administration

Minimize local adverse effects by injecting deep into the upper outer quadrant of the gluteus maximus; avoid local infiltration of the solution along the needle track.^{100 101 a}

Dosage

Available as trimethobenzamide hydrochloride; dosage expressed in terms of the salt.^{100 101 a}

Pediatric Patients

Nausea and Vomiting

Oral

Children weighing 13.6–45 kg: 100 or 200 mg 3 or 4 times daily; alternatively, children may receive 15–20 mg/kg daily given in 3 or 4 divided doses.^a However, suitable oral dosage forms are no longer commercially available in the US.^a

Adults

Nausea and Vomiting

Oral

Usual dosage: 300 mg 3 or 4 times daily.^{100 a} Adjust dosage according to indication for use, severity of symptoms, and patient response.¹⁰⁰

IM

Usual dosage: 200 mg 3 or 4 times daily.^{100 101 a} Adjust dosage according to indication for use, severity of symptoms, and patient response.^{100 101}

Special Populations

No special population dosage recommendations at this time.^{100 101}

Cautions for Tigan

Contraindications

• 
  

  Known hypersensitivity to trimethobenzamide.^{100 101 a c}

  
  


• 
  

  Injection contraindicated in children.^{100 101 a}

  
  

Warnings/Precautions

Warnings

CNS Depression

May impair ability to perform activities requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle); avoid concomitant use with alcohol.^{100 101 a c}

Neurologic Effects

Possible neurologic reactions (e.g., opisthotonos, seizures, coma, extrapyramidal reactions); may be similar to CNS signs and symptoms accompanying certain disorders (e.g., acute febrile illness, encephalitis, Reye’s syndrome, encephalopathy, gastroenteritis, dehydration, electrolyte imbalance), especially in children and in geriatric or debilitated patients.^{100 101 a c} Diagnosis of these disorders may be obscured or the disease-associated signs and symptoms may be incorrectly diagnosed as drug induced.^{100 101 a c}

Use with caution in patients with such disorders, particularly in those who have recently received other CNS drugs (e.g., phenothiazines, barbiturates, belladonna derivatives).^{100 101 a c} (See Specific Drugs under Interactions.)

Avoid use in pediatric patients with signs and symptoms suggestive of Reye’s syndrome.^{100 101 a c} (See Pediatric Use under Cautions.)

Discontinue drug if CNS symptoms occur.^{100 101 a c}

Sensitivity Reactions

Hypersensitivity Reactions

Hypersensitivity reactions including allergic skin reactions have been reported; discontinue at the first sign of sensitization.^{100 101 a c}

General Precautions

Hepatic Effects

Jaundice reported; discontinue drug if jaundice occurs.^{100 101 a c}

Potential hepatotoxic effects may unfavorably alter the course of Reye’s syndrome.^{100 101 a c} (See Pediatric Use under Cautions.)

Hematologic Effects

Blood dyscrasias reported; discontinue drug if blood dyscrasia occurs.^{100 101 a c}

GI Effects

Antiemetic effect may mask signs of overdosage of other drugs or may obscure the cause of vomiting in various disorders (e.g., appendicitis).^{100 101 a c}

Discontinue drug if exaggeration of preexisting nausea occurs.^{100 101 a c}

Specific Populations

Pregnancy

Category C.^e

Lactation

Not known whether trimethobenzamide is distributed into milk.^{a e} Safety not established.^{100 101 a c}

Pediatric Use

Injection contraindicated in children.^{100 101 a} Suitable oral dosage forms and rectal suppositories for pediatric use no longer are commercially available in the US.^{102 103 a c} (See Preparations.)

Use trimethobenzamide with caution in children.^{a c} Not recommended for treatment of uncomplicated vomiting in children; limit use to treatment of prolonged vomiting of known etiology.^{100 101 c} Avoid use in pediatric patients with signs and symptoms suggestive of Reye’s syndrome.^{100 101 a c}

Extrapyramidal effects of trimethobenzamide may obscure the diagnosis of or be confused with CNS manifestations of Reye’s syndrome or other encephalopathies.^{100 101 a c} (See Neurologic Effects under Cautions.)

Potential hepatotoxic effects of trimethobenzamide may unfavorably alter the course of Reye’s syndrome.^{100 101 a c}

Children with acute febrile illnesses, encephalitides, gastroenteritis, dehydration, or electrolyte imbalance may be at increased risk for adverse CNS effects (e.g., extrapyramidal reactions, opisthotonos, seizures, coma).^{100 101 a c} Use with caution in such children, especially those who recently have received other CNS agents.^{100 101 a c}

Geriatric Use

Geriatric and debilitated patients with acute febrile illnesses, encephalitides, gastroenteritis, dehydration, or electrolyte imbalance may be at increased risk for adverse CNS effects (e.g., extrapyramidal reactions, opisthotonos, seizures, coma).^{100 101 a c} Use with caution in such individuals, especially those who recently have received other CNS agents.^{100 101 a c}

Common Adverse Effects

Adverse effects may include blurred vision,^{100 101 a c} depression,^{100 101 a c} disorientation,^{100 101 a c} dizziness,^{100 101 a c} drowsiness,^{100 101 a c} headache,^{100 101 a c} extrapyramidal symptoms,^{100 101 a c} diarrhea,^{100 a c} opisthotonos,^{100 101 a c} and muscle cramps.^{100 101 a c} In addition, injection site reactions (pain,^{100 101 a} stinging,^{100 101 a} redness,^{100 101 a} swelling^{100 101 a} ) and hypotension^{100 101 a} may occur following IM injection.

Interactions for Tigan

Specific Drugs

Drug	Interaction	Comments
Alcohol	Impaired mental alertness/physical coordination100 101 a	Avoid concomitant usea
CNS drugs (e.g., barbiturates, belladonna derivatives, phenothiazines)	Possible increased risk of CNS reactions100 101 a c	Use with cautiona

Tigan Pharmacokinetics

Absorption

Bioavailability

Relative bioavailability of oral capsule compared with IM injection is 100%.^{100 101 a} Peak plasma concentration attained within 30 minutes after IM injection or 45 minutes after oral dose.^{100 101}

Onset

10–40 minutes after oral administration; 15–35 minutes after IM injection.^a

Duration

3–4 hours after oral administration; 2–3 hours after IM injection.^a

Plasma Concentrations

300-mg oral dose equivalent to a 200-mg IM dose.^{100 101 a}

Distribution

Extent

Distribution into human body tissues and fluids has not been determined.^a Drug and metabolites are distributed mainly into liver, kidneys, and lungs in animals.^a

Elimination

Elimination Route

30–50% of a single dose excreted in urine as unchanged drug within 48–72 hours following administration.^a

Half-life

7–9 hours.^{100 101 a}

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).^{100 c}

Parenteral

Injection

20–25°C.^{100 101}

ActionsActions

• 
  

  Appears to directly affect the medullary chemoreceptor trigger zone (CTZ) by inhibiting stimuli at the CTZ.^{100 101 a c}

  
  


• 
  

  Inhibits the emetic effect of apomorphine in animals; however, does not appear to inhibit direct impulses to the vomiting center in the lateral reticular formation and does not act peripherally to decrease the sensitivity of visceral nerves that transmit afferent impulses from the GI tract to the vomiting center.^{100 101 a c}

  
  


• 
  

  Structurally related to the substituted ethanolamine antihistamines (e.g., diphenhydramine) but exhibits only weak antihistaminic activity.^a

  
  

Advice to Patients

• 
  

  Potential for drug to impair mental alertness or physical coordination; use caution when driving or operating machinery until effects on individual are known.^{100 101 a c} Avoid concomitant use of alcohol.^{100 a}

  
  


• 
  

  Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^{100 101 a c}

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{100 101 a c}

  
  


• 
  

  Importance of informing patients of other important precautionary information.^{100 101 a e} (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

In April 2007, FDA announced that the agency was withdrawing approval of the NDA for trimethobenzamide hydrochloride (Tigan) suppositories because of lack of substantial evidence of efficacy.^{102 103} FDA also announced that it would take enforcement action against all firms attempting to manufacture or distribute trimethobenzamide-containing suppositories after May 9, 2007, without an approved application.^{102 103} Any firm seeking to market this formulation must obtain an approved NDA prior to marketing.^{102 103}

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Trimethobenzamide Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	300 mg*	Tigan	Monarch
			Trimethobenzamide Hydrochloride Capsules	Amide
Parenteral	Injection, for IM use only	100 mg/mL*	Tigan (with phenol in multiple-dose vials and preservative-free in single-dose vials)	Monarch
			Trimethobenzamide Hydrochloride Injection Carpuject (with phenol)	Hospira

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Tigan 300MG Capsules (MONARCH PHARMACEUTICALS): 30/$60.99 or 90/$174.97

Trimethobenzamide HCl 300MG Capsules (MUTUAL PHARMACEUTICAL): 30/$50.99 or 90/$129.98

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions February 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

100. Monarch Pharmaceuticals, Inc. Tigan (trimethobenzamide hydrochloride) capsules and injection prescribing information. Bristol, TN; 2006 Jul.

101. Hospira, Inc. Trimethobenzamide hydrochloride injection prescribing information. Lake Forest, IL; 2004 Oct.

102. US Food and Drug Administration. FDA announces that companies must stop marketing suppository products containing trimethobenzamide. Rockville, MD; 2007 Apr 6. Press release No. P07-58.

103. Food and Drug Administration. Trimethobenzamide hydrochloride suppositories; withdrawal of approval. Notice. [Docket No. 1978N-0224 (formerly Docket No. 78N-0224); DESI 11853]. Fed Regist. 2007; 72:17556-8.

a. AHFS drug information 2007. McEvoy GK, ed. Trimethobenzamide hydrochloride. Bethesda, MD: American Society of Health-Systems Pharmacists; 2007:2938-40.

c. G & W Labs, Inc. Trimethobenzamide HCI suppositories with benzocaine prescribing information. South Plainfield, NJ; 2001 Jun.

e. Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 7th ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005:1631-2.

More Tigan resources

• Tigan Side Effects (in more detail)
• Tigan Use in Pregnancy & Breastfeeding
• Drug Images
• Tigan Drug Interactions
• Tigan Support Group
• 0 Reviews for Tigan - Add your own review/rating

• Tigan Prescribing Information (FDA)


• Tigan Concise Consumer Information (Cerner Multum)


• Tigan Advanced Consumer (Micromedex) - Includes Dosage Information


• Tigan MedFacts Consumer Leaflet (Wolters Kluwer)


• Trimethobenzamide Prescribing Information (FDA)


• Benzacot Advanced Consumer (Micromedex) - Includes Dosage Information

Compare Tigan with other medications

• Nausea/Vomiting