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Cyproheptadine
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(si proe HEP ta deen)

U.S. Brand Names
Periactin®

Generic Available

Yes


Canadian Brand Names
PMS-Cyproheptadine

Synonyms
Cyproheptadine Hydrochloride

Pharmacological Index

Antihistamine


Use

Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to cyproheptadine or any component; narrow-angle glaucoma, bladder neck obstruction, acute asthmatic attack, stenosing peptic ulcer, GI tract obstruction, those on MAO inhibitors; avoid use in premature and term newborns due to potential association with SIDS


Warnings/Precautions

Do not use in neonates, safety and efficacy have not been established in children <2 years of age; symptomatic prostate hypertrophy; antihistamines are more likely to cause dizziness, excessive sedation, syncope, toxic confusion states, and hypotension in the elderly. 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.


Adverse Reactions

>10%:

Central nervous system: Slight to moderate drowsiness

Respiratory: Thickening of bronchial secretions

1% to 10%:

Central nervous system: Headache, fatigue, nervousness, dizziness

Gastrointestinal: Appetite stimulation, nausea, diarrhea, abdominal pain, xerostomia

Neuromuscular & skeletal: Arthralgia

Respiratory: Pharyngitis

<1%: Tachycardia, palpitations, edema, sedation, CNS stimulation, seizures, depression, photosensitivity, rash, angioedema, hemolytic anemia, leukopenia, thrombocytopenia, hepatitis, myalgia, paresthesia, bronchospasm, epistaxis, allergic reactions


Overdosage/Toxicology

Symptoms of overdose include CNS depression or stimulation, dry mouth, flushed skin, fixed and dilated pupils, apnea

There is no specific treatment for an antihistamine overdose, however, most of its clinical toxicity is due to anticholinergic effects. Anticholinesterase inhibitors may be useful by reducing acetylcholinesterase. Anticholinesterase inhibitors include physostigmine, neostigmine, pyridostigmine, and edrophonium. For anticholinergic overdose with severe life-threatening symptoms, physostigmine 1-2 mg (0.5 mg or 0.02 mg/kg for children) I.V., slowly may be given to reverse these effects.


Drug Interactions

Increased toxicity: MAO inhibitors hallucinations


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: Almost completely

Elimination: >50% excreted in urine (primarily as metabolites); ~25% excreted in feces


Usual Dosage

Oral:

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)

Adults: 4-20 mg/day divided every 8 hours (not to exceed 0.5 mg/kg/day)

Dosing adjustment in hepatic impairment: Dosage should be reduced in patients with significant hepatic dysfunction


Dietary Considerations

Alcohol: Additive CNS effects, avoid use


Test Interactions

Diagnostic antigen skin tests, amylases (S), fasting glucose (S)


Mental Health: Effects on Mental Status

Drowsiness is common; may cause nervousness or depression


Mental Health: Effects on Psychiatric Treatment

Contraindicated with MAOIs; concurrent use with psychotropic may produce additive sedation


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

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 (frequent small 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 difficulty breathing or expectorating (thick secretions); or lack of improvement or worsening or condition. Breast-feeding precautions: Do not breast-feed.


Nursing Implications

Raise bed rails, institute safety measures, assist with ambulation


Dosage Forms

Syrup, as hydrochloride: 2 mg/5 mL with alcohol 5% (473 mL)

Tablet, as hydrochloride: 4 mg


References

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.


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