cyproheptadine (Rx)

Brand and Other Names:
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 4mg

oral solution

  • 2mg/5mL
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Hypersensitivity Reaction

4 mg PO q8hr initially; maintenance: 4-20 mg/day, up to 32 mg/day divided q8hr in some patients; not to exceed 0.5 mg/kg/day  

Spasticity Associated With Spinal Cord (Off-label)

2-4 mg PO q8hr initially; not to exceed 24 mg/day

Migraine Headache Prophylaxis (Off-Label)

2 mg PO q12hr with or without propanol

Decreased Appetite Secondary to Chronic Disease (Off-label)

2 mg PO q6hr for one week; THEN 4 mg PO q6hr

Drug-Induced Sexual Dysfunction (Off-label)

4-12 mg PO 1-2 hours before anticipated coitus or 1-16 mg/day

Serotonin Syndrome (Off-Label)

12 mg initially PO, followed by 2 mg q2hr or 4-8 mg PO q6hr as needed to control symptoms

Dosing Modifications

Nonanticholinergic antihistamines should be considered first when treating allergic reactions (Beers Criteria)

Advanced age is associated with reduced clearance and greater risk of confusion, dry mouth, constipation, and other anticholinergic effects and toxicity; use lower end of dosage range (4 mg PO q12hr) for elderly patients, or administer less frequently

Renal impairment: Elimination is reduced in renal insufficiency; administer lower doses, and monitor closely

Dosage Forms & Strengths

tablet

  • 4mg

oral solution

  • 2mg/5mL
more...

Hypersensitivity Reaction

<2 years old: Safety and efficacy not established

2-6 years old: 2 mg PO q8-12hr; not to exceed 12 mg/day

7-14 years old: 4 mg PO q8-12hr; not to exceed 16 mg/day

Alternatively, total daily dose of 0.25 mg/kg or 8 mg/m²

Migraine

Prophylaxis

< 3 years: Safety and efficacy not established

>3 years and adolescents: 0.2-0.4 mg/kg/day PO divided BID; not to exceed 0.5 mg/kg/day

Loss of Appetite (Including Anorexia Nervosa; Off-label)

Stimulation of appetite

<13 years: Safety and efficacy not established

>13 years: 2 mg PO q6hr initially; increased to up to 8 mg q6hr over 3 weeks

Dosing Modifications

Renal impairment: Elimination is reduced in renal insufficiency; administer lower doses, and monitor closely

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Interactions

Interaction Checker

and cyproheptadine

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    Interactions Found

    Contraindicated

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            Adverse Effects

            Frequency Not Defined

            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

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            Warnings

            Contraindications

            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

            Cautions

            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

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            Pregnancy & Lactation

            Pregnancy category: B

            Lactation: Excretion in milk unknown; contraindicated

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Serotonin and histamine antagonist; competitively inhibits H1 receptor, mediating bronchial constriction, smooth-muscle contraction, edema, hypotension, CNS depression, and cardiac arrhythmias; prevents histamine release in blood vessels and is more effective in preventing histamine response than in reversing it; may be useful in patients with syndromes sustained by histamine-producing tumors

            Moderate anticholinergic activity with low sedative effect

            May have anti-5HT2 effects

            May have some calcium-channel blocking activity

            Absorption

            Peak plasma time: 6-9 hr

            Metabolism

            Metabolized by glucuronidation via UGT1A

            Metabolites: Quaternary ammonium glucuronide conjugate

            Elimination

            Excretion: Urine (40%), feces (2-20%)

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.