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Medication Safety Issues
Sound-alike/look-alike issues:
Cyproheptadine may be confused with cyclobenzaprine
Periactin may be confused with Perative®, Percodan®, Persantine®
Pronunciation
(si proe HEP ta deen)
Index Terms
Generic Available
Yes
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria
Use: Unlabeled/Investigational
Appetite stimulation, blepharospasm, cluster headaches, migraine headaches, Nelson's syndrome, pruritus, schizophrenia, spinal cord damage associated spasticity, and tardive dyskinesia
Pregnancy Risk Factor
B
Lactation
Excretion in breast milk unknown/contraindicated
Contraindications
Hypersensitivity to cyproheptadine or any component of the formulation; narrow-angle glaucoma; bladder neck obstruction; symptomatic prostatic hyperplasia; acute asthmatic attack; stenosing peptic ulcer; GI tract obstruction; concurrent use of MAO inhibitors; avoid use in premature and term newborns due to potential association with SIDS
Warnings/Precautions
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:
• Anorexic adults: In case reports, cyproheptadine has promoted weight gain in anorexic adults, though it has not been specifically studied in the elderly. All cases of weight loss or decreased appetite should be adequately assessed.
• Elderly: Use with caution in the elderly; may be more sensitive to adverse effects.
• Pediatrics: Antihistamines may cause excitation in young children. Safety and efficacy have not been established in children <2 years of age.
Adverse Reactions
>10%:
Central nervous system: Slight-to-moderate drowsiness
Respiratory: Thickening of bronchial secretions
1% to 10%:
Central nervous system: Dizziness, fatigue, headache, nervousness
Gastrointestinal: Abdominal pain, appetitie stimulation, diarrhea, nausea, xerostomia
Neuromuscular & skeletal: Arthralgia
Respiratory: Pharyngitis
<1%: Allergic reaction, angioedema, bronchospasm, CNS stimulation, depression, edema, epistaxis, hemolytic anemia, hepatitis, leukopenia, myalgia, palpitation, paresthesia, photosensitivity, rash, sedation, seizure, tachycardia, thrombocytopenia
Drug 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: Paliperidone. Risk C: Monitor therapy
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. 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
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may increase CNS sedation).
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
Excretion: Urine (>50% primarily as metabolites); feces (?25%)
Dosage
Oral:
Children:
Allergic conditions: 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 headaches: 4 mg 2-3 times/day
Children ?12 years and Adults: Spasticity associated with spinal cord damage: 4 mg at bedtime; increase by a 4 mg dose every 3-4 days; average daily dose: 16 mg in divided doses; not to exceed 36 mg/day
Children >13 years and Adults: Appetite stimulation (anorexia nervosa): 2 mg 4 times/day; may be increased gradually over a 3-week period to 8 mg 4 times/day
Adults:
Allergic conditions: 4-20 mg/day divided every 8 hours (not to exceed 0.5 mg/kg/day)
Cluster headaches: 4 mg 4 times/day
Migraine headaches: 4-8 mg 3 times/day
Dosage adjustment in hepatic impairment: Reduce dosage in patients with significant hepatic dysfunction
Test Interactions
Diagnostic antigen skin test results may be suppressed; false positive serum TCA screen
Patient Education
Take as directed; do not exceed recommended dose. Avoid use of other depressants, alcohol, or sleep-inducing medications unless approved by prescriber. You may experience drowsiness or dizziness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth, nausea, or abdominal pain (small frequent meals, frequent mouth care, chewing gum, or sucking hard candy may help). Report persistent sedation, confusion, or agitation; changes in urinary pattern; blurred vision; chest pain or palpitations; sore throat respiratory difficulty or expectorating (thick secretions); significant change in weight; or lack of improvement or worsening or condition. Breast-feeding precaution: Do not breast-feed.
Geriatric Considerations
In case reports, cyproheptadine has promoted weight gain in anorexic adults, though it has not been specifically studied in the elderly. All cases of weight loss or decreased appetite should be adequately assessed. Cyproheptadine may cause less sedation than diphenhydramine or hydroxyzine and, therefore, may be useful for pruritus in elderly; however, elderly may not tolerate anticholinergic effects.
Additional Information
May stimulate appetite. In case reports, cyproheptadine has promoted weight gain in anorexic adults.
Anesthesia and Critical Care Concerns/Other Considerations
May stimulate appetite; in case reports, cyproheptadine has promoted weight gain in anorexic adults.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation)
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness is common; may cause nervousness or depression
Mental Health: Effects on Psychiatric Treatment
Contraindicated with MAO inhibitors; concurrent use with psychotropic may produce additive sedation
Nursing: Physical Assessment/Monitoring
Assess effectiveness and interactions of other medications patient may be taking. Monitor weight periodically. Monitor effectiveness of therapy and adverse reactions (eg, excess anticholinergic effects) at beginning of therapy and periodically with long-term use. Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse symptoms to report.
Oncology: Emetic Potential
Very low (<10%)
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Syrup, as hydrochloride: 2 mg/5 mL (473 mL) [contains alcohol 5%; mint flavor]
Tablet, as hydrochloride: 4 mg
Pricing: U.S. (www.drugstore.com)
Syrup (Cyproheptadine HCl)
2 mg/5 mL (120): $14.99
Tablets (Cyproheptadine HCl)
4 mg (30): $11.99
References
Carlton MC, Kunkel DB, and Curry SC, “Ergotism Treated With Cyproheptadine,” Clin Toxicol, 1995, 33(5):552.
Craven JL and Rodin GM, “Cyproheptadine Dependence Associated With an Atypical Somatoform Disorder,” Can J Psychiatry, 1987, 32(2):143-5.
Herzog DB and Copeland PM, “Eating Disorders,” N Engl J Med, 1985, 313(5):295-303.
Lappin RI and Auchincloss EL, “Treatment of the Serotonin Syndrome With Cyproheptadine,” N Engl J Med, 1994, 331(15):1021-2.
Wians FH, Norton JT, and Wirebaugh, “False-Positive Serum Tricyclic Antidepressant Screen With Cyproheptadine,” Clin Chem, 1993, 39(6):1355-6.
International Brand Names
Lexi-Comp.com
Last full review/revision August 2008
Content last modified August 2008
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