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Cyproheptadine Hydrochloride


Pronunciation: SYE-proe-HEP-ta-deen HYE-droe-KLOR-ide
Class: Piperidine, nonselective

Trade Names

Cyproheptadine Hydrochloride
- Tablets 4 mg
- Syrup 2 mg per 5 mL


Competitively antagonizes histamine at H 1 receptor sites. Also exhibits antiserotonin activity.

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The principal metabolite found in the urine is the quaternary ammonium glucuronide conjugate of cyproheptadine.


2% to 20% is excreted in the feces, of which 34% (5.7% of the dose) is unchanged drug. At least 40% is excreted in the urine.

Special Populations

Renal Function Impairment

Elimination is diminished in renal insufficiency.

Indications and Usage

Symptomatic relief of perennial and seasonal allergic rhinitis; vasomotor rhinitis; allergic conjunctivitis due to inhalant allergens and foods; amelioration of allergic reactions to blood or plasma; mild skin manifestations of uncomplicated urticaria and angioedema; cold urticaria; dermatographism; adjunctive anaphylactic therapy.

Unlabeled Uses

Appetite stimulation; migraines; nightmares; suppression of vascular headaches.


Newborn or premature infants; breast-feeding mothers; angle-closure glaucoma; stenosing peptic ulcer; symptomatic prostatic hypertrophy; bladder neck obstruction; pyloroduodenal obstruction; elderly, debilitated patients; MAOI therapy; hypersensitivity to cyproheptadine and other drugs of similar structure.

Dosage and Administration


PO Starting dosage, 4 mg 3 times daily. Usual dosage, 4 to 20 mg/day; not to exceed 0.5 mg/kg/day.

Children 7 to 14 yr of age

PO 4 mg 2 or 3 times daily (max, 16 mg/day).

Children 2 to 6 yr of age

PO 2 mg 2 or 3 times daily (max, 12 mg/day). ( PO Total daily dosage 0.25 mg/kg or 8 mg/m 2 .)

General Advice

  • Administer without regard to meals. Administer with food if GI upset occurs.
  • Measure and administer prescribed dose of syrup using dosing syringe, dosing spoon, or dosing cup.


Store at 59° to 86°F. Keep container tightly closed.

Drug Interactions

Alcohol, CNS depressants

May cause additive CNS depressant effects.


Anticholinergic effects of cyproheptadine may increase. Concurrent use is contraindicated.

Laboratory Test Interactions

None known.

Adverse Reactions


Extrasystoles; hypotension; palpitations; tachycardia.


Confusion; convulsions; disturbed coordination; dizziness; euphoria; excitation; faintness; fatigue; hallucinations; headache; hysteria; insomnia; irritability; nervousness; neuritis; paresthesias; restlessness; sedation and sleepiness (often transient); tremor.


Excessive perspiration; photosensitivity; rash; urticaria.


Acute labyrinthitis; blurred vision; diplopia; dry mouth, nose, and throat; tinnitus; vertigo.


Anorexia; constipation; diarrhea; epigastric distress; nausea; vomiting.


Difficult urination; early menses; urinary frequency; urinary retention.


Agranulocytosis; hemolytic anemia; leukopenia; thrombocytopenia.


Abnormal hepatic function; cholestasis; hepatic failure; hepatitis; jaundice.


Increased appetite; weight gain.


Chest tightness; nasal stuffiness; thickening of bronchial secretions; wheezing.


Anaphylactic shock; chills; edema.



When used for treatment of allergy symptoms, assess allergy symptoms (eg, cough; rhinitis; nasal congestion; sneezing; watery eyes; itching nose, throat, or eyes) before starting therapy and periodically during therapy.

Monitor patient for dizziness and excessive drowsiness. If noted, hold therapy.

Ensure that therapy is periodically reviewed to determine if therapy needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated.


Category B .


Undetermined. Contraindicated in breast-feeding women.


Safety and efficacy in children younger than 2 yr of age not established. Contraindicated in newborn or premature infants.


Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy; more likely to cause dizziness, sedation, and hypotension. Contraindicated in elderly, debilitated patients.

Special Risk Patients

Use drug with caution in patients with a history of bronchial asthma, increased IOP, hyperthyroidism, CV disease, or hypertension.



May vary from CNS depression to stimulation (especially in children), seizures, GI symptoms, hallucinations, respiratory and cardiac arrest, anticholinergic effects (eg, dilated pupils, dry mouth, flushing).

Patient Information

  • Advise patient that medication is usually started at a low dose and then gradually increased until max benefit is obtained.
  • Advise patient to take dose 2 to 3 times daily as prescribed and not to stop taking or change the dose unless advised by health care provider.
  • Advise patient to take each dose without regard to meals but to take with food if stomach upset occurs.
  • Advise patient or caregiver using syrup to measure and administer prescribed dose using dosing syringe, dosing spoon, or dosing cup.
  • Advise patient that if allergy symptoms are not controlled not to increase the dose of medication or frequency of use but to inform their health care provider. Caution patient that larger doses or more frequent dosing does not increase effectiveness and may cause excessive drowsiness or other adverse reactions.
  • Instruct patient to stop taking drug and immediately report any of these symptoms to health care provider: persistent dizziness; excessive drowsiness; severe dry mouth, nose, or throat; flushing; unexplained shortness of breath or difficulty breathing; unusual tiredness or weakness; sore throat, fever, or other signs of infection; bleeding or unusual bruising; fast or irregular heartbeat; excitability, confusion, or changes in thinking or behavior; chest tightness; difficulty with urination.
  • Caution patient not to take any OTC antihistamines while taking this medication unless advised by health care provider.
  • Caution patient that alcohol and other CNS depressants (eg, sedatives) will have additional sedative effects if taken with cyproheptadine.
  • Caution patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
  • Advise patient that medication may cause sensitivity to sunlight and to avoid unnecessary exposure to UV light (sunlight, tanning booths), use sunscreen, and wear protective clothing until tolerance is determined.
  • Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
  • Advise breast-feeding mothers not to breast-feed their children while taking this medicine.

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