Cyproheptadine HCI
Indications
Cyproheptadine HCI is used for:
Rash, pruritus in a variety of condition, appetite stimulation, anorexia nervosa, cushing's syndrome, Nelson's syndrome, acromegaly, hyperprolactinemia, migraine, antidepressant-induced inorgasmia
Adult Dose
Oral
Allergic conditions
Adult: Initially, 4 mg tid, adjusted as necessary. Usual: 12-16 mg daily in 3-4 divided doses. Max: 32 mg/day.
Treatment and prophylaxis of migraine and other vascular headaches
Adult: 4 mg may be repeated after 30 min. Not to exceed 8 mg w/in a 4- to 6-hr period. Maintenance: 4 mg 4-6 hrly.
Child Dose
Oral
Allergic conditions
Child: 2-6 yr 2 mg bid or tid. Max: 12 mg daily;
7-14 yr 4 mg bid or tid. Max: 16 mg daily.
Migraine
Prophylaxis
< 3 years: Safety and efficacy not established
>3 years and adolescents: 0.2-0.4 mg/kg/day PO divided BID; not to exceed 0.5 mg/kg/day
Renal Dose
Administration
May be taken with or without food. May be taken w/ meals to reduce GI discomfort.
Contra Indications
Narrow-angle glaucoma; acute asthmatic attack; bladder neck obstruction; stenosing peptic ulcer; GIT obstruction; MAOIs therapy; hypersensitivity; neonates, lactation.
Precautions
Elderly; epilepsy; tasks requiring mental alertness; symptomatic prostate hypertrophy; epilepsy; alcoholism; pregnancy.
Lactation: Excretion in milk unknown; contraindicated
Pregnancy-Lactation
Pregnancy category: B
Lactation: Excretion in milk unknown; contraindicated
Interactions
May have additive effects w/ CNS depressants e.g. hypnotics, sedatives, tranquilizers, antianxiety agents.
Potentially Fatal: MAOIs prolong and intensify the anticholinergic effects of antihistamines.
Adverse Effects
Side effects of Cyproheptadine HCI :
Psychiatric/neurologic: CNS depression, drowsiness, sedation ranging from mild drowsiness to deep sleep (most frequent), dizziness, lassitude, disturbed coordination; less commonly, restlessness, insomnia, tremors, euphoria, nervousness, irritability, delirium, seizures, toxic psychosis, paresthesia
Muscular: Weakness
Cardiovascular: Palpitation, tachycardia, palpitation, ECG changes (eg, widened QRS), arrhythmias (eg, extrasystole, heart block), hypotension, hypertension, dizziness, sedation, hypotension
GI: Epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation
Hepatic: Cholestasis, hepatitis, hepatic failure, hepatic function abnormality, jaundice (rare)
Skin: Eczema, pruritus, inflammation, papular rash, erythema on exposed skin
Sensory: Visual disturbances, blurred vision, diplopia, tinnitus, acute labyrinthitis
Renal: Dysuria, urinary retention
Respiratory: Thickening of bronchial secretions, wheezing, nasal stuffiness
Other: Vertigo, sweating, chills, early menses, headache, impotence, dryness of mouth, nose, and throat, facial dyskinesia, tightness of chest, faintness
Mechanism of Action
Cyproheptadine is a sedating antihistamine w/ antimuscarinic, serotonin antagonist and Ca channel blocking properties. It competes w/ histamine for H1-receptor sites on effector cells in the GI tract, blood vessels and resp tract.