Dextromethorphan | apollo +9191 46 950 950

Dextromethorphan | apollo +9191 46 950 950

Dextromethorphan

CAS Number : 125-71-3

Molecular Formula : C18H25NO

Molecular Weight : 271.39 g/mol

Systematic (IUPAC) : (1R,9R,10R)-4-methoxy-17-methyl-17-

azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2,4,6-triene

Type : small molecule

Description

The d-isomer of the codeine analog of levorphanol. Dextromethorphan shows high affinity binding to

several regions of the brain, including the medullary cough center. This compound is an NMDA receptor

antagonist (receptors, N-methyl-D-aspartate) and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity.

Categories

Analgesics, Opioid

Antitussive Agents

Excitatory Amino Acid Antagonists

Pharmacology

Indication : For treatment and relief of dry cough.

Pharmacodynamics : Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high affinity binding to several regions of the brain, including

the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-

competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of

glutamate receptors in neurotoxicity.

Mechanism of action : Dextromethorphan is an opioid-like drug that binds to and acts as antagonist to the NMDA glutamatergic receptor, it is an agonist to the

opioid sigma 1 and sigma 2 receptors, it is also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump. Dextromethorphan is

rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolized into an active metabolite of dextromethorphan, dextrorphan,

the 3-hydroxy derivative of dextromethorphan.

Absorption : Rapidly absorbed from the

gastrointestinal tract.

Metabolism : Hepatic. Rapidly and extensively

metabolized to dextrorphan (active metabolite). One well known metabolic catalyst involved is a specific

cytochrome P450 enzyme known as 2D6, or CYP2D6.

Half life : 3-6 hours

Affected organisms : Humans and other mammals

What is dextromethorphan?

Dextromethorphan is a cough suppressant. It affects the signals in the brain that trigger cough reflex.

Dextromethorphan is used to treat a cough.

Dextromethorphan will not treat a cough that is caused by smoking, asthma, or emphysema.

Uses

This combination medication is used to treat symptoms caused by the common cold, flu, allergies, hay fever, or other breathing illnesses (e.g., sinusitis, bronchitis).

Dextromethorphan is a cough suppressant that affects a certain part of the brain (cough center), reducing the urge to cough. Decongestants help relieve stuffy nose symptoms. Antihistamines relieve watery eyes, itchy

eyes/nose/throat, runny nose, and sneezing.Cough-and-cold products have not been shown to be safe or effective in children younger than 6 years. Therefore, do not use this product to treat cold symptoms in children younger than 6 years unless specifically directed by the doctor. Some products (such as long-acting tablets/capsules) are not recommended for use in children younger than 12 years. Ask your doctor or pharmacist for more details about using your product safely.These products do not cure or shorten the length of the common cold and may

cause serious side effects. To decrease the risk for serious side effects, carefully follow all dosage

directions. Do not use this product to make a child sleepy. Do not give other cough-and-cold medication that might contain the same or similar ingredients (see

also Drug Interactions section). Ask the doctor or pharmacist about other ways to relieve cough and cold symptoms (such as drinking enough fluids, using a

humidifier or saline nose drops/spray).

How To Use?

If you are taking the over-the-counter product, read all directions on the product package before taking this medication. If you have any questions, consult your

pharmacist. If your doctor has prescribed this

medication, take it as directed.Take this medication by mouth with or without food with a full glass of water (8 ounces or 240 milliliters) or as directed by your doctor.

This medication may be taken with food or milk if stomach upset occurs.If you are using the liquid form, use a medication measuring device to carefully measure the prescribed dose. Do not use a household spoon. If your liquid form is a suspension, shake the bottle well before each dose.If you are using sustained-release

tablets or capsules, swallow the medication whole. Do not crush, chew, or break the tablets or capsules. Doing

so can destroy the long action of the drug and may increase side effects.Chewable forms of this medication should be chewed thoroughly before swallowing.If you are taking the powder, mix it thoroughly in the proper amount of liquid and stir well. Drink all of the liquid

immediately. Do not prepare a supply for future use.The dosage is based on your age, medical condition and

response to therapy. If you are taking this medication for allergy or hay fever symptoms, take it regularly in order

to get the most benefit from it.Improper use of this medication (abuse) may result in serious harm (e.g., brain damage, seizure, death). Do not increase your

dose, take it more frequently, or use it for a longer time than directed.Inform your doctor if your condition

persists or worsens.

Drug interactions

If you are taking this medication under your doctor's direction, your doctor or pharmacist may already be aware of any possible drug interactions and may be

monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your

doctor or pharmacist first.This product should not be used with the following medications because very serious (rarely fatal) interactions may occur: MAO

inhibitors (e.g., furazolidone, isocarboxazid, linezolid, moclobemide, phenelzine, procarbazine, rasagiline, selegiline, tranylcypromine), sibutramine.If you are currently using any of these medications listed above, tell your doctor or pharmacist before starting this

medication. Avoid taking MAO inhibitors within 2 weeks of starting or stopping this medication.Before using this

product, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially: antispasmodics (e.g., atropine,

belladonna alkaloids), beta blockers (e.g., metoprolol, atenolol), drugs for Parkinson's disease (e.g.,

anticholinergics such as benztropine, trihexyphenidyl), guanethidine, certain inhaled anesthetics (e.g., halothane), memantine, methyldopa, reserpine, scopolamine, tricyclic antidepressants (e.g.,

amitriptyline, desipramine).Tell your doctor or pharmacist if you also take drugs that cause drowsiness such as: certain antihistamines (e.g., diphenhydramine), 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, diet aids)

because they may contain ingredients that could affect your heart rate/blood pressure or cause drowsiness. Ask

your pharmacist about the safe use of those products.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?

Dextromethorphan is used to temporarily relieve cough caused by the common cold, the flu, or other conditions. Dextromethorphan will relieve a cough but will not treat

the cause of the cough or speed recovery. Dextromethorphan is in a class of medications called

antitussives. It works by decreasing activity in the part of the brain that causes coughing.

How should this medicine be used?

Dextromethorphan comes as a liquid-filled capsule, a chewable tablet, a dissolving strip, a solution (liquid), an extended-release (long-acting) suspension (liquid), and a lozenge to take by mouth. It is usually taken every 4 to 12 hours as needed. Follow the directions on the package or prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.

Dextromethorphan should only be used according to the label or package directions. Do not take more than the recommended amount of dextromethorphan in a 24-

hour period. Refer to the package or prescription label to determine the amount contained in each dose. Taking dextromethorphan in large amounts can cause serious

side effects or death.

Dextromethorphan comes alone and in combination with antihistamines, cough suppressants, and

decongestants. Ask your doctor or pharmacist for advice on which product is best for your symptoms. Check

nonprescription cough and cold product labels carefully before using 2 or more products at the same time. These

products may contain the same active ingredient(s) and taking them together could cause you to receive an overdose. This is especially important if you will be

giving cough and cold medications to a child.

Nonprescription cough and cold combination products, including products that contain dextromethorphan, can cause serious side effects or death in young children. Do not give these products to children younger than 4 years of age. If you give these products to children 4-11 years of age, use caution and follow the package directions

carefully.

If you are giving dextromethorphan or a combination product that contains dextromethorphan to a child, read the package label carefully to be sure that it is the right

product for a child of that age. Do not give dextromethorphan products that are made for adults to

children.

Before you give a dextromethorphan product to a child, check the package label to find out how much

medication the child should receive. Give the dose that matches the child's age on the chart. Ask the child's

doctor if you don't know how much medication to give the child.

If you are taking the liquid, do not use a household spoon to measure your dose. Use the measuring spoon or cup that came with the medication or use a spoon

made especially for measuring medication.

If you are using the dissolving strips, place them on your tongue and swallow after they melt.

If you are taking the chewable tablets you can allow them to melt in your mouth or you can chew them

before swallowing.

If you are taking the extended-release suspension, shake the bottle well before each use to mix the medication

evenly.

If you are taking the lozenges, allow them to slowly melt in your mouth.

Stop taking dextromethorphan and call your doctor if your cough does not get better within 7 days, if your cough goes away and comes back, or if your cough

occurs with a fever, rash, or headache.

Other uses for this medicine

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

What special precautions should I follow?

Before taking dextromethorphan,

tell your doctor and pharmacist if you are allergic to dextromethorphan, any other medications, or any of the ingredients in the product you plan to take. Check the

package label for a list of the ingredients.

do not take dextromethorphan if you are taking a monoamine oxidase (MAO) inhibitor such as

isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), and tranylcypromine (Parnate), or if you have stopped taking an MAO

inhibitor within the past 2 weeks.

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

supplements, and herbal products you are taking or plan to take.

tell your doctor if you smoke, if you have a cough that occurs with a large amount of phlegm (mucus), or if you

have or have ever had breathing problems such as asthma, emphysema, or chronic bronchitis.

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

while taking dextromethorphan, call your doctor.

if you have phenylketonuria (PKU, an inherited condition in which a special diet must be followed to

prevent mental retardation), you should know that some brands of chewable tablets that contain

dextromethorphan may be sweetened with aspartame, a source of phenylalanine.

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?

Dextromethorphan is usually taken as needed. If your doctor has told you to take dextromethorphan regularly,

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?

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

away:

dizziness

lightheadedness

drowsiness

nervousness

restlessness

nausea

vomiting

stomach pain

If you experience any of the following symptoms, call your doctor immediately:

rash

Dextromethorphan may cause other side effects. Call your doctor if you experience 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.

Symptoms of overdose may include:

nausea

vomiting

drowsiness

dizziness

unsteadiness

changes in vision

difficulty breathing

fast heartbeat

hallucinating (seeing things or hearing voices that do not exist)

seizures

coma (loss of consciousness for a period of time)

What other information should I know?

Ask your pharmacist any questions you have about dextromethorphan.

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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