Dosing

Dosing: Adult
Allergic conditions: Oral: 4-20 mg/day divided every 8 hours (not to exceed 0.5 mg/kg/day); some patients may require up to 32 mg/day for adequate control of symptoms
Spasticity associated with spinal cord damage (unlabeled use): Oral: Initial: 2-4 mg every 8 hours; maximum: 8 mg every 8 hours (Barbeau, 1982; Wainberg, 1990)

Dosing: Pediatric
Allergic conditions: Oral: Children: 0.25 mg/kg/day or 8 mg/m2/day in 2-3 divided doses or
2-6 years: 2 mg every 8-12 hours (not to exceed 12 mg/day)
7-14 years: 4 mg every 8-12 hours (not to exceed 16 mg/day)
Migraine headache prophylaxis (unlabeled use): Oral: 4 mg every 8-12 hours

Dosing: Geriatric
Initiate therapy at the lower end of the dosage range.

Use

Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria
Use - Unlabeled/Investigational
Migraine headache prophylaxis, pruritus, spasticity associated with spinal cord damage

Adverse Reactions

Frequency not defined.
Cardiovascular: Extrasystoles, hypotension, palpitation, tachycardia
Central nervous system: Confusion, coordination disturbed, dizziness, excitation, euphoria, faintness, hallucinations, headache, hysteria, insomnia, irritability, nervousness, neuritis, restlessness, sedation, seizure, sleepiness, tremor, vertigo
Dermatologic: Angioedema, photosensitivity, rash, urticaria
Gastrointestinal: Abdominal pain, anorexia, appetite increased, constipation, diarrhea, nausea, vomiting, xerostomia
Genitourinary: Difficult urination, urinary frequency, urinary retention
Hematologic: Agranulocytosis, hemolytic anemia, leukopenia, thrombocytopenia
Hepatic: Cholestasis, hepatic failure, hepatitis, jaundice
Neuromuscular & skeletal: Paresthesia
Ocular: Blurred vision, diplopia
Otic: Labyrinthitis (acute), tinnitus
Respiratory: Bronchial secretions (thickening), nasal congestion, pharyngitis
Miscellaneous: Allergic reactions, anaphylactic shock, chills, diaphoresis, fatigue

Contraindications

Hypersensitivity to cyproheptadine or any component of the formulation; narrow-angle glaucoma; bladder neck obstruction; pyloroduodenal obstruction; symptomatic prostatic hyperplasia; stenosing peptic ulcer; concurrent use of MAO inhibitors; use in debilitated elderly patients; use in premature and term newborns due to potential association with SIDS; breast-feeding

Warnings / Precautions Drug

Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease).
• Increased intraocular pressure: Use with caution in patients with increased intraocular pressure.
• Respiratory disease: Use with caution in patients with asthma or other chronic breathing disorders.
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Elderly: May be inappropriate in this age group due to potent anticholinergic effects (Beers Criteria).
• Pediatrics: Antihistamines may cause excitation in young children.

Interactions

Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: Cyproheptadine may diminish the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Risk C: Monitor therapy

Pregnancy

B

Lactation

Excretion in breast milk unknown/contraindicated

Mechanism of Action

A potent antihistamine and serotonin antagonist, competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract

Pharmacodynamics / Kinetics

Absorption: Completely
Metabolism: Almost completely hepatic
Time to peak, plasma: 6-9 hours (Hintze, 1975)
Excretion: Urine (~40% primarily as metabolites); feces (2% to 20%)