Cyproheptadine | apollo +9191 46 950 950

Cyproheptadine | apollo +9191 46 950 950

Cyproheptadine

CAS Number : 129-03-3

Molecular Formula : C21H21N

Molecular Weight : 287.398 g/mol

Systematic (IUPAC) : 1-methyl-4-{tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-

heptaen-2-ylidene}piperidine

Type : small molecule

Description

A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for

the post-gastrectomy dumping syndrome, etc.

Categories

Serotonin Antagonists

Antipruritics

Gastrointestinal Agents

Anti-Allergic Agents

Histamine H1 Antagonists

Antihistamine derivatives

Taxonomy

Kingdom : Organic

Classes

Dibenzocycloheptenes

Substructures

Benzene and Derivatives

Aliphatic and Aryl Amines

Heterocyclic compounds

Aromatic compounds

Piperidines

Dibenzocycloheptenes

Pharmacology

Indication : For 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, and

as therapy for anaphylactic reactions adjunctive to epinephrine.

Pharmacodynamics : Cyproheptadine is a piperidine antihistamine. Unlike other antihistamines, this drug

also antagonizes serotonin receptors. This action makes Cyproheptadine useful in conditions such as vascular headache and anorexia. Cyproheptadine does not

prevent the release of histamine but rather competes with free histamine for binding at HA-receptor sites.

Cyproheptadine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large

blood vessels, and bronchial smooth muscle. Most antihistamines possess significant anticholinergic properties, but Cyproheptadine exerts only weak

anticholinergic actions. Blockade of central muscarinic receptors appears to account for Cyproheptadine's antiemetic effects, although the exact mechanism is

unknown. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite

center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite.

Cyproheptadine also has been used to counter vascular headaches, which many believe are caused by changes in

serotonin activity, however it is unclear how Cyproheptadine exerts a beneficial effect on this

condition.

Mechanism of action : Cyproheptadine competes with free histamine for binding at HA-receptor sites.

This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor

binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite

center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite.

Absorption : Well absorbed after oral administration.

Protein binding : 96 to 99%

Metabolism : Hepatic (cytochrome P-450 system) and

some renal.

Route of elimination : After a single 4 mg oral dose of14C-labelled cyproheptadine HCl in normal subjects,

given as tablets 2% to 20% of the radioactivity was excreted in the stools. At least 40% of the administered

radioactivity was excreted in the urine.

Affected organisms : Humans and other mammals

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 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), and sexual function problems caused by certain drugs.

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.

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.

Why is this medication prescribed?

Cyproheptadine relieves red, irritated, itchy, watery eyes; sneezing; and runny nose caused by allergies,

irritants in the air, and hay fever. It may also be used to relieve the itching of allergic skin conditions, and to

treat hives, including hives caused by exposure to cold temperatures and by rubbing the skin. Cyproheptadine

is also sometimes used to treat allergic reactions in people who have received blood products as part of

medical treatment and to treat life-threatening allergic reactions after the symptoms have been brought under control with other medications. Cyproheptadine will help relieve symptoms but will not treat the cause of symptoms or speed recovery. Cyproheptadine is in a

class of medications called antihistamines. It works by blocking the action of histamine, a substance in the body

that causes allergic symptoms.

How should this medicine be used?

Cyproheptadine comes as a tablet and a solution (liquid) to take by mouth. It is usually taken two or three times a day. Take cyproheptadine at around the same time(s) every day. Follow the directions on your prescription

label carefully, and ask your doctor or pharmacist to explain any part you do not understand. 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.

Other uses for this medicine

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.Talk to your doctor about the possible risks of using this

medication for your condition.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

What special precautions should I follow?

Before taking cyproheptadine,

tell your doctor and pharmacist if you are allergic to cyproheptadine, other antihistamines, or any other

medications.

tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional

supplements, and herbal products you are taking or plan to take. 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; and tranquilizers. Your doctor may need to change the

doses of your medications or monitor you carefully for side effects.

tell your doctor if you have or have ever had asthma, glaucoma (a condition in which increased pressure in

the eye can lead to gradual loss of vision), ulcers, difficulty urinating (due to an enlarged prostate gland),

heart disease, high blood pressure, seizures, or an overactive thyroid gland.

tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant

while taking cyproheptadine, call your doctor.

talk to your doctor about the risks and benefits of taking cyproheptadine if you are 65 years of age or older. Older adults should not usually take cyproheptadine because it is not as safe or effective as other medications that can

be used to treat the same condition.

if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking cyproheptadine.

you should know that this medication may make you drowsy. Do not drive a car or operate machinery until

you know how this medication affects you.

talk to your doctor about the safe use of alcohol while you are taking this medication. Alcohol can make the

side effects of cyproheptadine worse.

What special dietary instructions should I

follow?

Unless your doctor tells you otherwise, continue your normal diet.

What should I do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the

missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

What side effects can this medication cause?

Cyproheptadine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

dry mouth, nose, and throat

drowsiness

dizziness

nausea

chest congestion

headache

excitement (especially in children)

muscle weakness

Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately:

difficulty urinating

vision problems

nervousness

Cyproheptadine may cause other side effects. Call your doctor if you have any unusual problems while you are

taking this medication.

What storage conditions are needed for this

medicine?

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture

(not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist

about the proper disposal of your medication.

What other information should I know?

Keep all appointments with your doctor.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your

prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such

as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of

emergencies.

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