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

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