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Pronunciation
(si proe HEP ta deen)
Generic Available (U.S.)
Yes
Index Terms
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria
Use: Unlabeled
Migraine headache prophylaxis, pruritus, spasticity associated with spinal cord damage
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; 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
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: Avoid use of this potent anticholinergic agent due to increased risk of confusion, dry mouth, constipation, and other anticholinergic effects; clearance decreases in patients of advanced age (Beers Criteria).
• Pediatrics: Antihistamines may cause excitation in young children.
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
Metabolism/Transport Effects
None known.
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: 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
Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving antihistamines (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
Metyrosine: CNS Depressants may enhance the sedative effect of Metyrosine. 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: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
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
Metabolism: Primarily by hepatic glucuronidation via UGT1A (Walker, 1996)
Half-life elimination: Metabolites: ~16 hours (Paton, 1985)
Time to peak, plasma: 6-9 hours (Paton, 1985)
Excretion: Urine (~40% primarily as metabolites); feces (2% to 20%)
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 headache prophylaxis (unlabeled use): 4 mg every 8-12 hours
Adults:
Allergic conditions: 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): Initial: 2-4 mg every 8 hours; maximum: 8 mg every 8 hours (Barbeau, 1982; Wainberg, 1990)
Elderly: Initiate therapy at the lower end of the dosage range
Test Interactions
Diagnostic antigen skin test results may be suppressed; false positive serum TCA screen
Patient Education
Avoid use of alcohol. You may experience drowsiness, dizziness, dry mouth, nausea, or abdominal pain. Report persistent sedation, confusion, agitation, blurred vision, respiratory difficulty, or lack of improvement or worsening of condition.
Geriatric Considerations
Elderly patients may not tolerate the anticholinergic effects of cyproheptadine.
This medication is considered to be potentially inappropriate in this patient population (Beers Criteria: Quality of evidence - moderate; Strength of recommendation - strong).
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
Monitor weight periodically. Monitor for excess anticholinergic effects at beginning of therapy and periodically throughout.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Syrup, oral, as hydrochloride: 2 mg/5 mL (473 mL, 480 mL)
Tablet, oral, as hydrochloride: 4 mg
References
"American Geriatrics Society Updated Beers Criteria for Potentially Inappropriate Medication Use in Older Adults," J Am Geriatr Soc, 2012 [epub ahead of print].
Barbeau H, Richards CL, and Bedard PJ, “Action of Cyproheptadine in Spastic Paraparetic Patients,” J Neurol Neurosurg Psychiatry, 1982, 45(10):926-6.
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.
Gracies JM, Nance P, Elovic E, et al, “Traditional Pharmacological Treatments for Spasticity. Part II: General and Regional Treatments,” Muscle Nerve Suppl, 1997, 6:S92-120.
Hintze KL, Wold JS, and Fischer LJ, “Disposition of Cyproheptadine in Rats, Mice, and Humans and Identification of a Stable Epoxide Metabolite,” Drug Metab Dispos, 1975, 3(1):1-9.
Lappin RI and Auchincloss EL, “Treatment of the Serotonin Syndrome With Cyproheptadine,” N Engl J Med, 1994, 331(15):1021-2.
Paton DM and Webster DR, "Clinical Pharmacokinetics of H1-Receptor Antagonists (The Antihistamines)," Clin Pharmacokinet, 1985, 10(6):477-97.
Wainberg M, Barbeau H, and Gauthier S, “The Effects of Cyproheptadine on Locomotion and on Spasticity in Patients With Spinal Cord Injuries,” J Neurol Neurosurg Psychiatry, 1990, 53(9):754-63.
Walker RB and Kanfer I, "Pharmacokinetics of Cyclizine Following Intravenous Administration to Human Volunteers," Eur J Pharm Sci, 1996, 4(5):301-6.
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 April 2012
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