PERIACTINE

Cyproheptadine is a potent competitive antagonist of both serotonin and histamine receptors.

It is used primarily to treat allergic symptoms, though it is perhaps more notable for its use in appetite stimulation and its off-label use in the treatment of serotonin syndrome.

In the

US, prescription cyproheptadine is indicated for the treatment of various allergic symptomatologies.

• including dermatographia, rhinitis, conjunctivitis, and urticaria.

• as well as adjunctive therapy in the management of anaphylaxis following treatment with epinephrine.

In Canada, cyproheptadine is available over-the-counter and is indicated for the treatment of pruritus and for appetite stimulation.

In Australia, cyproheptadine is additionally indicated for the treatment vascular headaches.

Cyproheptadine is also used off-label for the treatment of serotonin syndrome.

Cyproheptadine has been observed to antagonize several pharmacodynamic effects of serotonin in laboratory animals, including bronchoconstriction and vasodepression, and has demonstrated similar efficacy in antagonizing histamine-mediated effects.

The reason for its efficacy in preventing anaphylactic shock has not been elucidated, but appears to be related to its anti-serotonergic effects.

H1 receptor Antagonist 5-hydroxytryptamine receptor 2A Antagonist 5-hydroxytryptamine receptor 2C Antagonist + 1 more target.

A single study examining the difference in absorption of Oral administered versus sublingually administered cyproheptadine in five healthy males demonstrated a mean C max of 30.0 mcg/L and 4.0 mcg/L, respectively, and a mean AUC of 209 mcg.h/L and 25 mcg.h/L, respectively.

The T max of

Oral and sublingually administered cyproheptadine was 4 hours and 9.6 hours, respectively.

The principal metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine.

Hover over products below to view reaction partners Cyproheptadine Cyproheptadine N-glucuronide.

Approximately 2-20% of the radioactivity from an Oral administered radio-labeled dose of cyproheptadine is excreted in the feces, of which approximately 34% is unchanged parent drug (less than 5.7% of the total dose).

At least 40% of radioactivity is recovered in the urine.

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Overdosage with cyproheptadine is likely to result in significant sedation.

• although paradoxical stimulation has been noted in pediatric patients.

• and anticholinergic adverse effects such as dry mouth and flushing.

Most patients appear to recover without incident, as a review of cyproheptadine overdose cases in Hong Kong found the majority of patients had no or mild symptoms following intentional overdose.

In the event of overdosage with cyproheptadine, prescribing information recommends the induction of vomiting (if it has not occurred spontaneously) using syrup of ipecac.

Gastric lavage and activated charcoal may also be considered.

Vasopressors may be used to treat hypotension and intravenous physostigmine salicylate may be considered for the treatment of significant CNS symptoms depending on the clinical picture.

• Overdosage of antihistamines, particularly in infants and children, may produce hallucinations, central nervous system depression, convulsions, and death.

Antihistamines may diminish mental alertness conversely particularly in the young child they may occasionally produce excitation.

• Antihistamines may have additive effects with alcohol and other CNS depressants, e.g., hypnotics, sedatives, tranquilizers, antianxiety agents.

• Patients should be warned about engaging in activities requiring mental alertness and motor coordination, such as driving a car or operating machinery.

Antihistamines are more likely to cause dizziness, sedation and hypotension in elderly patients.

This drug should not be used in newborn or premature infants.

Because of the higher risk of antihistamines for infants generally, and for newborns and prematures in particular, antihistamine therapy is contraindicated in nursing mothers.

Hypersensitivity to cyproheptadine and other drugs of similar chemical structure.

Monoamine oxidase inhibitor therapy.

Angle-closure glaucoma.

Stenosing peptic ulcer.

Symptomatic prostatic hypertrophy.

Bladder neck obstruction.

Pyloroduodenal obstruction, elderly, debilitated patients.

The total daily dosage for children may be calculated on the basis of body weight or body area using approximately 0.25 mg/kg/day (0.11 mg/lb/day) or 8 mg per square meter of body surface (8 mg/m 2 ).

In small children for whom the calculation of the dosage based upon body size is important, it may be necessary to use cyproheptadine syrup to permit accurate dosage.

Age to 6 years: The usual dose is 2 mg (1/2 tablet) two or three times a day, adjusted as necessary to the size and response of the patient.

The dose is not to exceed 12 mg a day. Age to 14 years: The usual dose is 4 mg (1 tablet) two or three times a day, adjusted as necessary to the size and response of the patient.

The dose is not to exceed 16 mg a day. Adults: The total daily dose for adults should not exceed 0.5 mg/kg/day (0.23 mg/lb/day).

The therapeutic range is to 20 mg a day, with the majority of patients requiring to 16 mg, a day. An occasional patient may require as much as 32 mg a day for adequate relief.

It is suggested that dosage be initiated with 4 mg (1 tablet) three times a day and adjusted according to the size and response of the patient.

Each tablet contains 4 mg of cyproheptadine hydrochloride, are white to off-white, round, flat faced, beveled edge tablets debossed with “CE 73” on one side and a score on other side.

They are supplied as follows: bottles of 90 count, NDC 62135-236-90.

Dispense in tight containers as defined by the USP/NF.

Federal law prohibits dispensing without prescription.

KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.

Manufactured for

Chartwell RX, LLC Congers, NY 10920 Telephone Number-1-845-232-1683 L70791 Rev. 01/2023.

Reproduction studies have been performed in rabbits, mice, and rats at oral or subcutaneous doses up to 32 times the maximum recommended human oral dose and have revealed no evidence of impaired fertility or harm to the fetus due to cyproheptadine.

Cyproheptadine has been shown to be fetotoxic in rats when given by intraperitoneal injection in doses four times the maximum recommended human oral dose.

Two studies in pregnant women, however, have not shown that cyproheptadine increases the risk of abnormalities when administered during the first, second and third trimesters of pregnancy.

No teratogenic effects were observed in any of the newborns.

Nevertheless, because the studies in humans cannot rule out the possibility of harm, cyproheptadine should be used during pregnancy only if clearly needed.

It is not known whether this drug is excreted in human milk.

Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants from cyproheptadine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother See CONTRAINDICATIONS.

Safety and effectiveness in children below the age of two years have not been established. See CONTRAINDICATIONS, Newborn or Premature infants, and WARNINGS, Children..