Cyproheptadine HCl is an antihistaminic and antiserotonergic agent.

Cyproheptadine hydrochloride is a white to slightly yellowish, crystalline solid, which is soluble in water, freely soluble in methanol, sparingly soluble in ethanol, soluble in chloroform, and practically insoluble in ether. It is the sesquihydrate of 4-(5H-dibenzo[a,d] cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride. The molecular and structural formula of the anhydrous salt is:

C₂₁H₂₁N•HCl..................MW: 350.89

Cyproheptadine HCl is available in tablets for oral administration containing 4 mg of cyproheptadine hydrochloride. Each tablet also contains the following inactive ingredients: dibasic calcium phosphate dihydrate, magnesium stearate, microcrystalline cellulose, polyoxyl (40) stearate, purified water, sodium starch glycolate, and stearic acid.

Last updated on RxList: 4/3/2009

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 and other standard measures after the acute manifestations have been controlled.

DOSAGE SHOULD BE INDIVIDUALIZED ACCORDING TO THE NEEDS AND THE RESPONSE OF THE PATIENT.

Each Cyproheptadine HCl Tablet contains 4 mg of cyproheptadine hydrochloride.

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 necessry 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.

Adults

The total daily dose for adults should not exceed 0.5 mg/kg/day.

The therapeutic range is 4 mg to 20 mg a day, with the majority of patients requiring 12 mg 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.

Cyproheptadine Hydrochloride Tablets 4 mg are white, round, scored, compressed tablets, debossed "Par 043" on one side. They are available in bottles of 100 (NDC 49884-043-01), and 1000 (NDC 49884-043-10). Store at controlled room temperature, 15° to 30°C (59° to 86°F), in a well-closed container.

Manufactured by: Par Pharmaceutical Companies, Inc. Spring Valley, NY 10977. Revised: 04/08.

Last updated on RxList: 4/3/2009

Adverse reactions which have been reported with the use of antihistamines are as follows:

Central Nervous System: Sedation and sleepiness (often transient), dizziness, disturbed coordination, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, paresthesias, neuritis, convulsions, euphoria, hallucination, hysteria, faintness.

Integumentary: Allergic manifestation of rash and edema, excessive perspiration, urticaria, photosensitivity.

Special Senses: Acute labyrinthitis, blurred vision, diplopia, vertigo, tinnitus.

Cardiovascular: Hypotension, palpitation, tachycardia, extrasystoles, anaphylactic shock.

Hematologic: Hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia.

Digestive System: Cholestasis, heptatic failure, hepatitis, hepatic function abnormality, dryness of mouth, epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation, jaundice.

Genitourinary:Urinary frequency, difficult urination, urinary retention, early menses.

Respiratory: Dryness of nose and throat, thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness.

Miscellaneous: Fatigue, chills, headache, increased appetite/weight gain.

MAO Inhibitors prolong and intensify the anticholinergic effects of antihistamines.

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

Last updated on RxList: 4/3/2009

Pediatric Patients

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.

CNS Depressants

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

Activities Requiring Mental Alertness

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 (see PRECAUTIONS, Geriatric Use).

General

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

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term carcinogenic studies have not been done with cyproheptadine.

Cyproheptadine had no effect on fertility in a two-litter study in rats or a two generation study in mice at about 10 times the human dose.

Cyproheptadine did not produce chromosome damage in human lymphocytes or fibroblasts in-vitro; high doses (10^-4M) were cytotoxic. Cyproheptadine did not have any mutagenic effect in the Ames microbial mutagen test; concentrations of above 500 mcg/plate inhibited bacterial growth.

Pregnancy

Pregnancy Category B: 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.

Nursing Mothers

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).

Pediatric Use

Safety and effectiveness in pediatric patients below the age of two have not been established (see CONTRAINDICATIONS, Newborn or Premature Infants,and WARNINGS, Pediatric Patients).

Geriatric Use

Clinical studies of Cyproheptadine HCl Tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy (see WARNINGS, Activities Requiring Mental Alertness).

Last updated on RxList: 4/3/2009

Antihistamine overdosage reactions may vary from 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.

If vomiting has not occurred spontaneously the patient should be induced to vomit with syrup of ipecac. If the patient is unable to vomit, perform gastric lavage followed by activated charcoal. Isotonic or 1/2 isotonic saline is the lavage of choice. Precautions against aspiration must be taken especially in infants and children.

When life threatening CNS signs and symptoms are present, intravenous physostigmine salicylate may be considered. Dosage and frequency of administration are dependent on age, clinical response, and recurrence after response. (See package circulars for physostigmine products.)

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.

The oral LD₅₀ of cyproheptadine is 123 mg/kg, and 295 mg/kg in the mouse and rat, respectively.

Newborn or Premature Infants

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

Nursing Mothers

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

Other Conditions

Hypersensitivity to cyproheptadine and other drugs of similar chemical structure:

Monoamine oxidase inhibitor therapy (see PRECAUTIONS: DRUG INTERACTIONS)
Angle-closure glaucoma
Stenosing peptic ulcer
Symptomatic prostatic hypertrophy
Bladder neck obstruction
Pyloroduodenal obstruction
Elderly, debilitated patients

Last updated on RxList: 4/3/2009

Cyproheptadine is a serotonin and histamine antagonist with anticholinergic and sedative effects. Antiserotonin and antihistamine drugs appear to compete with serotonin and histamine, respectively, for receptor sites.

Pharmacokinetics and Metabolism

After a single 4 mg oral dose of ¹⁴C-labelled cyproheptadine HCl in normal subjects, given as tablets 2% to 20% of the radioactivity was excreted in the stools. Only about 34% of the stool radioactivity was unchanged drug, corresponding to less than 5.7% of the dose. At least 40% of the administered radioactivity was excreted in the urine. No detectable amounts of unchanged drug were present in the urine of patients on chronic 12-20 mg daily doses. The principal metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine. Elimination is diminished in renal insufficiency.

Last updated on RxList: 4/3/2009

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

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

Last updated on RxList: 4/3/2009

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

CYPROHEPTADINE - ORAL

(sigh-pro-HEP-tah-deen)

USES: This medication relieves seasonal and year-round allergy symptoms such as watery/itchy eyes, runny nose, and sneezing. It is also used to relieve itching and hives caused by some skin conditions. Cyproheptadine belongs to a class of drugs known as antihistamines. It works by blocking the action of certain natural substances in the body (histamine and serotonin).

Do not use this medication in children younger than 2 years unless specifically directed by the doctor. To decrease the risk for serious side effects, carefully follow all of the doctor's dosage directions. Do not give other cough and cold medication that might contain the same or similar ingredients (see also Drug Interactions section). Ask your doctor or pharmacist about other ways to relieve cough and cold symptoms (e.g., saline nose drops/spray, using a humidifier or infant nasal suction bulb).

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

This medication may also be used to treat a type of hormone disorder (Cushing's syndrome caused by a pituitary gland problem), sexual function problems caused by certain drugs, and a type of eating disorder (anorexia nervosa).

HOW TO USE: Take this medication by mouth, usually 2 to 3 times a day or as directed by your doctor. You may take this drug with food to minimize stomach upset. When using the syrup, measure the dose out carefully with a medication spoon/cup.

The dosage is based on your medical condition and response to therapy. In children, the dosage is also based on weight. Children 2 to 6 years of age should not take more than 12 milligrams per day unless directed by the doctor. Children 7 to 14 years of age should not take more than 16 milligrams per day unless directed by the doctor. Adults should not take more than 32 milligrams per day.

Do not increase your dose or take this medication more often than directed.

Do not take this medication for several days before allergy testing since test results can be affected. Consult your doctor or pharmacist for more information.

Inform your doctor if your condition does not improve or if it worsens.

SIDE EFFECTS: Drowsiness, dizziness, blurred vision, loss of coordination, upset stomach, constipation, increased appetite, weight gain, thickening of mucus in the nose/throat, or dry mouth/throat/nose may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: mental/mood changes (e.g., unusual excitement, confusion, hallucinations), fast/pounding/irregular heartbeat, difficulty urinating, seizures.

Tell your doctor immediately if any of these rare but very serious side effects occur: stomach/abdominal pain, persistent nausea/vomiting, yellowing eyes/skin, dark urine, unusual tiredness.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking cyproheptadine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: glaucoma (narrow-angle), stomach problems (e.g., peptic ulcer, stomach/intestinal obstruction), urinary problems (e.g., enlarged prostate, bladder obstruction).

Before using this medication, tell your doctor or pharmacist your medical history, especially of: asthma, glaucoma, overactive thyroid, heart disease, high blood pressure, seizure disorder, kidney problems.

This drug may make you dizzy or drowsy; use caution while engaging in activities requiring alertness such as driving or using machinery. Limit alcoholic beverages.

To minimize dizziness, get up slowly when rising from a seated or lying position.

The elderly may be more sensitive to the side effects of this drug, especially drowsiness and dizziness.

Do not use this drug in newborn or premature infants. Children may be more sensitive to the side effects of this drug, especially unusual excitement and seizures.

This medication should be used only when clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

It is not known if this medication passes into breast milk. Due to the potential risk to the nursing infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription products you may use, especially of: anticholinergic drugs (e.g., atropine, scopolamine), antispasmodic drugs (e.g., belladonna alkaloids, dicyclomine, oxybutynin), certain drugs for Parkinson's disease (e.g., benztropine, trihexyphenidyl), MAO inhibitors (e.g., furazolidone, isocarboxazid, linezolid, moclobemide, phenelzine, procarbazine, rasagiline, selegiline, tranylcypromine), SSRI antidepressants (e.g., fluoxetine, citalopram).

Tell your doctor or pharmacist if you also take drugs that cause drowsiness such as: anti-seizure drugs (e.g., carbamazepine), medicine for sleep or anxiety (e.g., alprazolam, diazepam, zolpidem), muscle relaxants, narcotic pain relievers (e.g., codeine), psychiatric medicines (e.g., chlorpromazine, risperidone, amitriptyline, trazodone).

Check the labels on all your medicines (e.g., cough-and-cold products) because they may contain drowsiness-causing ingredients (e.g., other antihistamines such as diphenhydramine). Ask your pharmacist about the safe use of those products.

This medication can affect the results of certain lab tests (pituitary-adrenal response). Make sure laboratory personnel and your doctors know you use this drug.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. Symptoms of overdose in children may include mental/mood changes, unusual excitement, or seizures. Symptoms of overdose in adults may include severe drowsiness or loss of consciousness, which may be followed by unusual excitement or seizures.

NOTES: Do not share this medication with others.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture. Do not freeze the oral solution. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For enrollment information call MedicAlert at 1-800-854-1166 (USA) or 1-800-668-1507 (Canada).

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.