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Trade Names:
Cyproheptadine Hydrochloride
- Tablets 4 mg
- Syrup 2 mg per 5 mL

Mechanism of Action

Pharmacology

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

Pharmacokinetics

Metabolism

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

Elimination

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.

Indications and Usage

Symptomatic relief of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis; amelioration of allergic reactions to blood or plasma; management of allergic pruritic symptoms, mild skin manifestations of uncomplicated urticaria and angioedema, and cold urticaria; dermographism; adjunctive anaphylactic therapy.

Unlabeled Uses

Prophylactic treatment of pediatric migraines; suppression of vascular headaches; appetite stimulation.

Contraindications

Hypersensitivity to antihistamines; newborn or premature infants; breast-feeding mothers; narrow-angle glaucoma; stenosing peptic ulcer; symptomatic prostatic hypertrophy; bladder neck obstruction; pyloroduodenal obstruction; elderly, debilitated patients; MAO therapy.

Dosage and Administration

PO Starting dose, 4 mg every 8 h. Usual dose, 4 to 20 mg/day; not to exceed 0.5 mg/kg/day.

PO 4 mg bid or three times daily (max, 16 mg/day).

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.

Storage/Stability

Store tablets and syrup at controlled room temperature (59° to 86°F). Keep container tightly closed.

Drug Interactions

May cause additive CNS depressant effects.

Anticholinergic effects of cyproheptadine may increase.

Effects of serotonin reuptake inhibitors may be reversed.

Laboratory Test Interactions

In skin testing procedures, antihistamines may prevent or diminish otherwise positive reaction to dermal reactivity indicators.

Adverse Reactions

Cardiovascular

Orthostatic hypotension; palpitations; tachycardia; reflex tachycardia; extrasystoles; faintness.

CNS

Drowsiness (often transient); sedation; dizziness; faintness; disturbed coordination; confusion; restlessness; excitement; nervous tremor; paresthesias; convulsions; hallucinations; headache; fatigue; nervousness; irritability; insomnia; neuritis; euphoria; hysteria.

Dermatologic

Excessive perspiration; photosensitivity; rash; urticaria.

EENT

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

GI

Epigastric distress; nausea; vomiting; diarrhea; anorexia; constipation; change in bowel habits.

Genitourinary

Urinary frequency; difficult urination; urinary retention; early menses.

Hematologic

Hemolytic anemia; leukopenia; thrombocytopenia; agranulocytosis.

Hepatic

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

Metabolic

Increased weight.

Respiratory

Thickening of bronchial secretions; chest tightness; wheezing; nasal stuffiness; respiratory depression.

Miscellaneous

Anaphylactic shock; chills; edema; increased appetite.

Precautions

Pregnancy

Category B .

Lactation

Undetermined. Contraindicated in breast-feeding women.

Children

Safety and efficacy in children younger than 2 yr of age not established.

Elderly

Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Hepatic Function

Use drug with caution in patients with cirrhosis or other liver disease.

Special Risk Patients

Use drug with caution in patients with predisposition to urinary retention, history of bronchial asthma, increased IOP, hyperthyroidism, CV disease, or hypertension.

Respiratory disease

Generally not recommended for treatment of lower respiratory tract symptoms, including asthma.

Sedatives/CNS depressants

Avoid in patients with history of sleep apnea.

Overdosage

Symptoms

CNS depression, CV collapse, CV stimulation, seizures, hypotension, anticholinergic effects (eg, dilated pupils, dry mouth, flushing), hyperthermia (especially in children), dystonic reactions, dizziness, ataxia, blurred vision.

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 a dose is missed to take the missed dose as soon as possible unless it is nearing time for the next scheduled dose. Then, skip the missed dose and take the next dose at the regularly scheduled time. Caution patient not to double the dose to catch up.
• 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.
• If patient is to have allergy skin testing, advise not to take the medication for at least 4 days before the skin testing.