Cyproheptadine

What is Cyproheptadine?

• Cyproheptadine (Periactin) is an antihistaminic and antiserotonergic agent, used in the treatment of allergic rhinitis and urticaria and as an appetite stimulant.

Cyproheptadine

Cyproheptadine3

Cyproheptadine-3D-ball-model 3

What are the uses of this medicine?

Cyproheptadine (Periactin) is used in the treatment of:

• Perennial and seasonal allergic rhinitis
• Vasomotor rhinitis
• Allergic conjunctivitis due to inhalant allergens and foods
• Mild, uncomplicated allergic skin manifestations of urticaria and angioedema
• Amelioration of allergic reactions to blood or plasma
• Cold urticaria
• Dermatographism
• As therapy for anaphylactic reactions adjunctive to epinephrine

Other uses:

• Cyproheptadine also is used for the treatment of Cushing's Syndrome (an abnormal condition that is caused by excess hormones [[[corticosteroids]]]) and to treat certain types of headache such as migraine.

How does this medicine work?

• The hydrochloride salt of a synthetic methyl-piperidine derivative with antihistaminic and anti-serotoninergic properties.
• Cyproheptadine competes with free histamine (HA) for binding at HA-receptor sites, thereby competitively antagonizing histamine stimulation of HA-receptors in the gastrointestinal tract, large blood vessels, and bronchial smooth muscle.
• This agent also competes with free serotonin for binding at serotonin receptor sites.
• Cyproheptadine exhibits anticholinergic and sedative properties and has been shown to stimulate appetite and weight gain.

Who Should Not Use this medicine ?

This medicine cannot be used:

• in newborn or premature infants.
• in nursing mothers.
• In patients with hypersensitivity to cyproheptadine.
• with Monoamine oxidase inhibitor therapy.

In patients with fallowing conditions:

• Angle-closure glaucoma
• Stenosing peptic ulcer
• Symptomatic prostatic hypertrophy
• Bladder neck obstruction
• Pyloroduodenal obstruction
• Elderly, debilitated patients

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• other medications for allergies or colds
• medications for anxiety, depression, or seizures
• muscle relaxants
• narcotic medications for pain
• sedatives
• sleeping pills
• tranquilizers
• MAO inhibitors

Is this medicine FDA approved?

• It was patented in 1959 and came into medical use in 1961.

How should this medicine be used?

Recommended dosage:

In Pediatric Patients: Age 2 to 6 years:

• The total daily dosage for pediatric patients may be calculated on the basis of body weight or body area using approximately 0.25 mg/kg/day or 8 mg per square meter of body surface (8 mg/m2).
• 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 7 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.

In Adults:

• The total daily dose for adults should not exceed 0.5 mg/kg/day.
• The therapeutic range is 4 to 20 mg a day, with the majority of patients requiring 12 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 three times a day and adjusted according to the size and response of the patient.

Administration:

• Cyproheptadine comes as a tablet and a solution to take by mouth.
• It is usually taken two or three times a day.
• Take cyproheptadine at around the same times every day.
• Take cyproheptadine exactly as directed.
• Do not take more or less of it or take it more often than prescribed by your doctor.
• If you are using the solution, do not use a household spoon to measure your dose.
• Use the measuring cup or spoon that came with the medication or use a spoon that is made especially for measuring medication.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a tablet and a solution

This medicine is available in fallowing brand namesː

• Periactin

What side effects can this medication cause?

The most common side effects of this medicine include:

• sedation, impairment of motor function, confusion, dizziness, blurred vision, dry mouth and throat, palpitations, tachycardia, abdominal distress, constipation and headache.

Antihistamines can worsen urinary retention and glaucoma.

• Periactin

What special precautions should I follow?

• Overdosage of antihistamines, particularly in infants and young children, may produce hallucinations, central nervous system depression, convulsions, respiratory and cardiac arrest, 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.

Cyproheptadine has an atropine-like action and, therefore, should be used with caution in patients with:

• History of bronchial asthma
• Increased intraocular pressure
• Hyperthyroidism
• Cardiovascular disease
• Hypertension

• It is not known whether this drug is excreted in human milk. Because of the higher risk of antihistamines for infants generally and for newborns and prematures in particular, antihistamine therapy is contraindicated in nursing mothers.
• Cyproheptadine has been linked to rare instances of clinically apparent liver injury.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• central nervous system depression to stimulation especially in pediatric patients.
• Also, atropine-like signs and symptoms (dry-mouth; fixed, dilated pupils; flushing etc.) as well as gastrointestinal symptoms may occur.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• If vomiting has not occurred spontaneously, the patient should be induced to vomit with syrup of ipecac.
• If patient is unable to vomit, perform gastric lavage followed by activated charcoal.
• lsotonic or ½ isotonic saline is the lavage of choice.
• When life threatening CNS signs and symptoms are present, intravenous physostigmine salicylate may be considered.
• Saline cathartics, as milk of magnesia, by osmosis draw water into the bowel and, therefore, are valuable, for their action in rapid dilution of bowel content.
• Stimulants should not be used.
• Vasopressors may be used to treat hypotension.

Can this medicine be used in pregnancy?

• Pregnancy Category B.
• Cyproheptadine should be used during pregnancy only if clearly needed.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients below the age of two have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• CYPROHEPTADINE HYDROCHLORIDE

Inactive ingredients:

• microcrystalline cellulose
• lactose monohydrate
• magnesium stearate
• SODIUM STARCH GLYCOLATE TYPE A POTATO

Who manufactures and distributes this medicine?

Manufactured by:

• Stason Pharmaceuticals, Inc.
• Irvine, CA

Distributed by:

• Breckenridge Pharmaceutical, Inc.
• Berlin, CT

What should I know about storage and disposal of this medication?

• Store at 20° - 25°C (68° - 77°F) excursions permitted to 15° - 30°C (59° - 86°F).
• Dispense in a well-closed container as defined in the USP.
• Use child-resistant closure.

First Generation Antihistamines

• Brompheniramine
• Carbinoxamine
• Chlorcyclizine
• Chlorpheniramine
• Clemastine
• Cyclizine
• Cyproheptadine
• Dexbrompheniramine
• Dexchlorpheniramine
• Dimenhydrinate
• Diphenhydramine
• Doxylamine
• Hydroxyzine
• Meclizine
• Phenyltoloxamine
• Promethazine
• Triprolidine

Second Generation Antihistamines

• Acrivastine
• Cetirizine
• Fexofenadine
• Levocetirizine
• Loratadine
• Desloratadine

• Dailymed label info on Cyproheptadine
• FDA Cyproheptadine

Cyproheptadine Resources
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First Generation Antihistamines

• Brompheniramine
• Carbinoxamine
• Chlorcyclizine
• Chlorpheniramine
• Clemastine
• Cyclizine
• Cyproheptadine
• Dexbrompheniramine
• Dexchlorpheniramine
• Dimenhydrinate
• Diphenhydramine
• Doxylamine
• Hydroxyzine
• Meclizine
• Phenyltoloxamine
• Promethazine
• Triprolidine

Second Generation Antihistamines

• Acrivastine
• Cetirizine
• Fexofenadine
• Levocetirizine
• Loratadine
• Desloratadine

Sedatives and Hypnotics

• Antihistamines
• Diphenhydramine
• Doxylamine
• Hydroxyzine

• Barbiturates
  • Amobarbital
  • Butabarbital
  • Phenobarbital
  • Secobarbital

• Benzodiazepines
  • Diazepam
  • Estazolam
  • Flurazepam
  • Quazepam
  • Temazepam
  • Triazolam

• Benzodiazepine Receptor Agonists
  • Eszopiclone
  • Zaleplon
  • Zolpidem

• Herbals
  • Chamomile (Matricaria recutita)
  • Hops (Humulus lupulus)
  • Lavender (Lavandula angustifolia)
  • Passionflower (Passiflora incarnata)
  • Valerian (Valeriana officinalis)

• Melatonin and its Analogues
  • Melatonin
  • Ramelteon
  • Tasimelteon

Miscellaneous Agents

• • Buspirone
  • Chloral hydrate
  • Doxepin
  • Meprobamate
  • Sodium Oxybate (Narcolepsy Agent)
  • Suvorexant