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Cyproheptadine

    DEA Class; OTC, Rx

    Common Brand Names; Periactin

    • Antihistamines, 1st Generation

    Oral piperidine antihistamine (H1-blocker) that also antagonizes serotonin receptors
    Has sedative and anticholinergic effects
    Primarily used to treat perennial and seasonal allergic rhinitis, vasomotor rhinitis, urticaria, and allergic conditions in adults and children as young as 2 years

    Indicated for

    • Hypersensitivity Reaction
    • Spasticity Associated With Spinal Cord (Off-label)
    • Migraine Headache Prophylaxis (Off-Label)
    • Decreased Appetite Secondary to Chronic Disease (Off-label)
    • Drug-Induced Sexual Dysfunction (Off-label)
    • Serotonin Syndrome (Off-Label)

    Documented hypersensitivity

    Premature infants and neonates

    Nursing women

    Concomitant monoamine oxidase inhibitor therapy

    Narrow-angle glaucoma

    Stenosing peptic ulcer, pyloroduodenal obstruction

    Symptomatic prostatic hypertrophy

    Bladder neck obstruction

    Elderly, debilitated patients

    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

    Elimination reduced in renal insufficiency

    Use with caution in cardiovascular disease, including hypertension

    Elderly patients: Avoid use in elderly because of high incidence of anticholinergic effects; may exacerbate existing lower urinary conditions or benign prostatic hyperplasia; if used, administer at low end of dosage range

    May cause CNS depression, which may impair mental abilities; use caution when operating heavy machinery

    Use caution in cardiovascular disease, including hypertension and ischemic heart disease

    Use with caution in patients with increased intraocular pressure, history of asthma or other chornic breathing disorders, or thyroid dysfunction

    Nonanticholinergic antihistamines should be considered first for treatment of allergic reaction in the elderly (Beers criteria)

    Antihistamines may cause excitation in young children

    Pregnancy category: B

    Lactation: Excretion in milk unknown; contraindicated

    Adults

    0.5 mg/kg/day PO or 32 mg/day PO, whichever is less.

    Geriatric

    0.5 mg/kg/day PO or 32 mg/day PO, whichever is less.

    Adolescents

    15 to 17 years: 0.5 mg/kg/day PO or 32 mg/day PO, whichever is less.
    13 to 14 years: 16 mg/day PO.

    Children

    7 to 12 years: 16 mg/day PO.
    2 to 6 years: 12 mg/day PO.
    Less than 2 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Use is contraindicated.

    Cyproheptadine hydrochloride

    tablet

    • 4mg

    oral solution

    • 2mg/5mL