Class: First Generation Antihistamines
ATC Class: R06AX02
VA Class: AH107
Chemical Name: 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride
Molecular Formula: C21H21N•HCl
CAS Number: 41354-29-4
Uses for Cyproheptadine Hydrochloride
Has been effective in some patients for the treatment of Cushing’s syndrome† secondary to pituitary disorders;14 15 16 17 18 19 20 21 48 52 53 63 however, in most patients, other therapy (e.g., surgery, radiation therapy) is preferred.21 39 48
Has been effective for the management of inhibited male or female orgasm† (anorgasmy) induced by tricyclic antidepressants,55 57 58 66 MAO inhibitors,54 56 fluoxetine,68 or antipsychotic agents.56 However, consider the potential for interactions between these drugs and cyproheptadine.5 66 (See Interactions.)
Has been shown to stimulate appetite and weight gain in children32 33 and adults;34 35 36 however, few indications for clinical use.40 May be of some value in the treatment of anorexia nervosa†;37 38 41 46 47 59 60 may be more effective in nonbulimic patients than in those who are bulimic.59
Reportedly has been effective in some patients for the management of vascular headaches† (e.g., migraine).30 31 43 44 71 Efficacy for prophylaxis of migraine not established in randomized controlled studies, but some experts consider the drug to be effective based on consensus and clinical experience.71
Cyproheptadine Hydrochloride Dosage and Administration
Children 2–6 years of age: Usual dosage is 2 mg 2 or 3 times daily; adjust as needed based on the size and response of the patient, up to maximum of 12 mg daily.5 74 75 (See Pediatric Use under Cautions.)
Adolescents ≥15 years of age: Initially, 4 mg 3 times daily; adjust based on the size and response of the patient, up to 0.5 mg/kg daily.74 75 Dosage range: 4–20 mg daily; most patients require 12–16 mg daily.74 75
Cautions for Cyproheptadine Hydrochloride
Because of anticholinergic effects, use with caution in patients with increased intraocular pressure, active or history of respiratory disease (e.g., bronchial asthma), hyperthyroidism, or cardiovascular disease (e.g., hypertension).74 75 c (See Contraindications.) Use of antihistamines generally not recommended in asthmatics who previously experienced a serious antihistamine-induced adverse bronchopulmonary effect.
Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection.72 73 Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established.72 Therefore, FDA recommended not to use such preparations in children <2 years of age; safety and efficacy in older children currently under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 years of age”). FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.
Possible paradoxical excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures), especially in young children.74 75 c Central anticholinergic syndrome (e.g., hallucinations, agitation, confusion) has occurred.
Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults; clinical experience has not revealed age-related differences.5 74 Select dosage with caution (usually starting at low end of dosage range) because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.5 74
Common Adverse Effects
Interactions for Cyproheptadine Hydrochloride
Specific Drugs and Laboratory Tests
CNS depressants (e.g., alcohol, hypnotics, sedatives, tranquilizers)
Use caution to avoid overdosage;c advise patient to avoid alcohol
Test, antigen or histamine
Inhalation-challenge testing with histamine or antigen: Possible suppression of test response
Antigen skin testing: Possible suppression of wheal and flare reactions
Cyproheptadine Hydrochloride Pharmacokinetics
Distribution into human body tissues and fluids has not been characterized.7
Tightly closed container at 15–30°C.74
Advice to Patients
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Many prescription cough, cold, and allergy preparations commercially available in the US have not been approved by FDA.500 Because of the potentially serious health risks associated with unapproved preparations, FDA announced on March 3, 2011, that it would take enforcement action (e.g., seizure, injunction, other judicial or administrative proceeding) against any currently marketed and listed unapproved cough, cold, and allergy preparation manufactured on or after June 1, 2011 or shipped on or after August 30, 2011.500 For additional information and for a complete list of unapproved cough, cold, and allergy preparations affected by this FDA notice, see FDA website ().
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
2 mg/5 mL*
Cyproheptadine Hydrochloride Syrup
Cyproheptadine Hydrochloride Tablets
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Cyproheptadine HCl 2MG/5ML Syrup (ACTAVIS MID ATLANTIC): 120/$24.38 or 360/$50.02
Cyproheptadine HCl 4MG Tablets (CYPRESS PHARMACEUTICAL): 30/$13.99 or 60/$19.98
AHFS DI Essentials. © Copyright, 2004-2016, Selected Revisions January 11, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
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