[Posted 10/09/2008] FDA notified healthcare professionals and consumers that the Consumer Healthcare Products Association (CHPA) is voluntarily modifying the product labels for consumers of over the counter (OTC) cough and cold medicines to state “do not use” in children under 4 years of age. FDA supports CHPA members to help prevent and reduce misuse and to better inform consumers about the safe and effective use of these products for children. FDA continues to assess the safety and efficacy of these products and to revise its OTC list of approved ingredients and amounts for these medicines. Parents and care givers should adhere to the dosage instructions and warnings on the label that accompanies OTC cough and cold medications before giving the product to children, and should consult their healthcare professionals if they have any questions or concerns. For more information visit the FDA website at: [Web] and [Web].
Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.
Management of allergic conjunctivitis caused by foods or inhaled allergens.
Management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.
Treatment of dermatographism.
Amelioration of allergic reactions to blood or plasma.
Adjunct to epinephrine and other standard measures for management of anaphylactic reactions after acute manifestations have been controlled.
Cushing’s Syndrome
Has been effective in some patients for the treatment of Cushing’s syndrome† secondary to pituitary disorders; however, in most patients, other therapy (e.g., surgery, radiation therapy) is preferred.
Sexual Dysfunction
Has been effective for the management of inhibited male or female orgasm† (anorgasmy) induced by tricyclic antidepressants, MAO inhibitors, fluoxetine, or antipsychotic agents. However, consider the potential for interactions between these drugs and cyproheptadine. (See Interactions.)
Anorexia Nervosa
Has been shown to stimulate appetite and weight gain in children and adults; however, few indications for clinical use. May be of some value in the treatment of anorexia nervosa†; may be more effective in nonbulimic patients than in those who are bulimic.
Headache
Reportedly has been effective in some patients for the management of vascular headaches† (e.g., migraine). Efficacy for prophylaxis of migraine not established in randomized controlled studies, but some experts consider the drug to be effective based on consensus and clinical experience.
Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.
Allergic Conditions
Oral
Children 2–6 years of age: Usual dosage is 2 mg 2 or 3 times daily; adjust as needed based on the size and response of the patient, up to maximum of 12 mg daily. (See Pediatric Use under Cautions.)
Children 7–14 years of age: Usual dosage is 4 mg 2 or 3 times daily; adjust as needed based on the size and response of the patient, up to maximum of 16 mg daily.
Adolescents ≥15 years of age: Initially, 4 mg 3 times daily; adjust based on the size and response of the patient, up to 0.5 mg/kg daily. Dosage range: 4–20 mg daily; most patients require 12–16 mg daily.
Alternatively, children ≥2 years of age may receive 0.25 mg/kg or 8 mg/m2 daily in divided doses.
Anorexia Nervosa
Oral
Adolescents ≥13 years of age: Dosage of 2 mg 4 times daily, increased gradually over a 3-week period to up to 8 mg 4 times daily, has been used.†
Adults
Allergic Conditions
Oral
Initially, 4 mg 3 times daily; adjust as needed based on the size and response of the patient, up to 0.5 mg/kg daily.
Dosage range: 4–20 mg daily; most patients require 12–16 mg daily. Some patients may require up to 32 mg daily.
Cushing’s Syndrome
Oral
Initially, 8 mg daily in divided doses; gradually increase dosage to up to 24 mg daily in divided doses.†
Anorexia Nervosa
Oral
Dosage of 2 mg 4 times daily, increased gradually over a 3-week period to up to 8 mg 4 times daily, has been used.†
Prescribing Limits
Pediatric Patients
Allergic Conditions
Oral
Children 2–6 years of age: Maximum 12 mg daily.
Children 7–14 years of age: Maximum 16 mg daily.
Adolescents ≥15 years of age: Maximum 0.5 mg/kg daily.
Anorexia Nervosa
Oral
Adolescents ≥13 years of age: Maximum 32 mg daily.†
Adults
Allergic Conditions
Oral
Maximum 0.5 mg/kg daily.
Cushing’s Syndrome
Oral
Maximum 24 mg daily.†
Anorexia Nervosa
Oral
Maximum 32 mg daily.†
Special Populations
Geriatric Patients
Select dosage with caution, starting at the lower end of the usual dosage range. (See Geriatric Use under Cautions.)
Risk of marked drowsiness. Caution required when performing hazardous activities requiring mental alertness and motor coordination (e.g., driving a motor vehicle, operating machinery).
Possible excitability (especially in children). (See Pediatric Use under Cautions.)
Concurrent use of other CNS depressants may have additive CNS depressant effects. (See Interactions.)
General Precautions
Concomitant Diseases
Because of anticholinergic effects, use with caution in patients with increased intraocular pressure, active or history of respiratory disease (e.g., bronchial asthma), hyperthyroidism, or cardiovascular disease (e.g., hypertension). (See Contraindications.) Use of antihistamines generally not recommended in asthmatics who previously experienced a serious antihistamine-induced adverse bronchopulmonary effect.
Specific Populations
Pregnancy
Category B.
Lactation
Not known whether cyproheptadine is distributed into milk.
Because of potential for serious adverse effects in nursing infants, discontinue nursing or the drug. (See Pediatric Use under Cautions.)
Pediatric Use
Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.
Contraindicated in neonates and premature infants.
Safety and efficacy of cyproheptadine not established in children <2 years of age.
Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established. Therefore, FDA recommended not to use such preparations in children <2 years of age; safety and efficacy in older children currently under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 years of age”). FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.
Cyproheptadine overdosage, particularly in infants and young children, may produce hallucinations, CNS depression, seizures, respiratory and cardiac arrest, and death.
Possible paradoxical excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures), especially in young children. Central anticholinergic syndrome (e.g., hallucinations, agitation, confusion) has occurred.
Geriatric Use
Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults; clinical experience has not revealed age-related differences. Select dosage with caution (usually starting at low end of dosage range) because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.
Possible increased risk of dizziness, sedation, and hypotension in geriatric patients.
Contraindicated in debilitated geriatric patients.
Reversal of fluoxetine's antidepressant effects reported in limited number of patients, possibly due to inhibition of fluoxetine's serotonergic effects
MAO inhibitors
MAO inhibitors prolong and intensify anticholinergic effects of antihistamines
Inhalation-challenge testing with histamine or antigen: Possible suppression of test response
Antigen skin testing: Possible suppression of wheal and flare reactions
Pharmacokinetics
Absorption
Bioavailability
Well absorbed following oral administration.
Distribution
Extent
Distribution into human body tissues and fluids has not been characterized.
Elimination
Metabolism
Appears to be almost completely metabolized, principally to the quaternary ammonium glucuronide conjugate.
Elimination Route
Principally in urine, as conjugates; also in feces following oral administration.
Special Populations
Elimination is reduced in renal insufficiency.
Stability
Storage
Oral
Solution
15–30°C.
Tablets
Tightly closed container at 15–30°C.
Actions
Has potent antihistaminic and serotonin antagonist properties; also has anticholinergic and sedative effects and reportedly has calcium-channel blocking activity.
Advice to Patients
Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.
Risk of drowsiness; avoid alcohol and use caution when engaging in activities requiring mental alertness and motor coordination (e.g., driving a motor vehicle, operating machinery).
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 09/2009. For the most current and up-to-date pricing information, please visit www.drugstore.com. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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