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Adapalene | apollo +9191 46 950 950

Adapalene | apollo +9191 46 950 950

Adapalene

CAS Number : 106685-40-9

Molecular Weight : 412.52 g/mol

Molecular Formula : C28H28O3

Systematic (IUPAC) : 6-[3-(adamantan-1-yl)-4-methoxyphenyl]

naphthalene-2-carboxylic acid

Type : small molecule

Description : Adapalene is a topical retinoid primarily used in the treatment of acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions. It is currently marketed by Galderma under the trade

names Differin in some countries, and Adaferin in India.

Categories : Dermatologic Agents

Taxonomy

Kingdom : Organic

Classes : Retinoids

Substructures

Hydroxy Compounds

Benzyl Alcohols and Derivatives

Naphthalenes

Acetates

Benzoates

Phenols and Derivatives

Ethers

Benzene and Derivatives

Biphenyl and Derivatives

Carboxylic Acids and Derivatives

Adamantanes

Aromatic compounds

Anisoles

Benzoyl Derivatives

Retinoids

Cyclooctane and Derivatives

Phenyl Esters

Pharmacology

Indication : For the topical treatment of comedo, papular and pustular acne (acne vulgaris) of the face,

chest or back.

Pharmacodynamics : Adapalene is a chemically stable retinoid-like compound. Biochemical and

pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation,

keratinization, and inflammatory processes all of which represent important features in the pathology of acne

vulgaris.

Mechanism of action : Mechanistically, adapalene binds to specific retinoic acid nuclear receptors (gamma and beta) and retinoid X receptors but does not bind to the cytosolic receptor protein. Although the exact mode of action of adapalene is unknown, it is suggested that topical adapalene may normalize the differentiation of

follicular epithelial cells resulting in decreased microcomedone formation.

Absorption : Absorption of adapalene through human skin is low. Only trace amounts (<0.25 ng/mL) of parent

substance have been found in the plasma of acne patients following chronic topical application of

adapalene in controlled clinical trials

Metabolism : Metabolized mainly by O-demethylation, hydroxylation and conjugation, and excretion is

primarily by the biliary route.

Route of elimination : Excretion appears to be primarily by the biliary route.

Toxicity : The acute oral toxicity of adapalene in mice and rats is greater than 10 mL/kg. Chronic ingestion of the drug may lead to the same side effects as those associated with excessive oral intake of Vitamin A.

Affected organisms : Humans and other mammals

Dosing

Wash and dry the affected areas. Apply a thin layer of gel to the affected areas once daily at bedtime. Avoid the eyes, lips and nose. There may be a worsening of acne during the first few weeks of therapy because adapalene promotes the growth of pimples that have begun to form but are not yet visible. Therefore, treatment should not be stopped if acne appears to be worsening. Beneficial

effects should be seen by 8 to 12 weeks.

Uses

This medication is used to treat acne. It may decrease the number and severity of acne pimples and promote quick healing of pimples that do develop. Adapalene belongs to a class of medications called retinoids. It works by affecting the growth of cells and decreasing

swelling and inflammation.

How To Use?

Wash your hands before applying this medication. Gently clean the affected skin with a mild or soapless

cleanser and pat dry. Use your fingertips to apply a small amount of medication in a thin layer, usually once daily at bedtime, or as directed by your doctor. A gauze pad or cotton swab can be used to apply the solution.Use this medication on the skin only. Do not apply to the inner lip area or inside the nose/mouth. Do not apply to cut, scraped, sunburned, or eczema-affected skin.Avoid

getting this medication in your eyes. If this medication gets into your eyes, flush with large amounts of water. Call your doctor if eye irritation develops. Wash your hands after using the medication to avoid accidentally

getting it in your eyes.During the first few weeks of using adapalene, your acne might appear worse because the medication is working on pimples forming inside the

skin. It may take up to 8-12 weeks to notice results from this medication.Use it regularly in order to get the most benefit from it. To help you remember, use it at the same time each day. Do not use a larger amount or use it more

frequently than recommended. Your skin will not improve any faster, and it will increase the risk of

developing redness, peeling and pain.This medication is available in different strengths and forms (e.g., gel,

cream, solution). The best type of medication for you to

use will depend on the condition of your skin and your response to therapy. Inform your doctor if your

condition persists or worsens.

Why is this medication prescribed?

Adapalene is used to treat acne. Adapalene is in a class of medications called retinoid-like compounds. It works by stopping pimples from forming under the surface of

the skin.

How should this medicine be used?

Adapalene comes as a gel, a solution (liquid), and a cream to apply to the skin. The solution comes in a glass

bottle with an applicator and as individual pledgets (medicated wipes for one time use). It is usually applied once a day at bedtime. Follow the directions on your prescription label carefully, and ask your doctor or

pharmacist to explain any part you do not understand. Apply adapalene exactly as directed. Do not apply more or less of it or apply it more often than prescribed by your doctor. Applying more adapalene or applying

adaplene more often than recommended will not speed up or improve results, but it may irritate your skin.

Adapalene controls acne but does not cure it. Your acne may get worse during the first few weeks of treatment, and it may take 8-12 weeks or longer before you feel the full benefit of adapalene. Pimples can take 6-8 weeks to form under the skin, and during the first weeks of your treatment, adapalene may bring these pimples to the skin surface. Continue to use adapalene even if your acne worsens or you do not see much improvement at first. Do not stop using adapalene without talking to

your doctor.

Do not apply adapalene to skin that is sunburned, broken, or covered with eczema (a skin disease). If you

have any of these conditions, do not apply adapalene until your skin has healed.

Be careful not to get adapalene in your eyes, nose, or mouth. If you do get adapalene in your eyes, wash them with plenty of water and call your doctor. Your eyes may

become irritated, swollen, or infected.

To use the cream, gel, or solution, follow these steps:

Gently wash the affected skin with a mild soap or soapless cleanser and pat dry with a soft towel. Do not use harsh or abrasive cleansers, and do not scrub your

skin vigorously. Ask your doctor or pharmacist to recommend a gentle cleanser.

If you are using the gel or cream, use your fingers to spread a thin film of medication over the affected area. If you are using a pledget, remove it from the foil pouch

and gently wipe the entire affected area. If you are using the glass bottle of solution, apply a thin layer to the

affected area using the applicator provided.

You may feel a slight warmth or stinging in the place where you applied adapalene. This feeling is normal and

should go away by itself in a short time.

If you used a pledget, throw it away after use. Do not save it to use again.

Other uses for this medicine

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

What special precautions should I follow?

Before taking adapalene,

tell your doctor and pharmacist if you are allergic to adapalene or any other medications.

tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or

using. Be sure to mention all skin care products including soaps, cleansers, moisturizers, and cosmetics. Many skin care products can irritate your skin if you use them with adapalene. This is especially likely if you use products that are harsh, dry out the skin, or contain alcohol, spices, lime rind, sulfur, resorcinol, salicylic

acid, or alpha hydroxy acid. If you have been using these products, your doctor may want you to wait for your skin to return to normal before you begin using adapalene.

tell your doctor if you have or have ever had eczema or cancer.

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

while using adapalene, call your doctor.

plan to avoid unnecessary or prolonged exposure to real and artificial sunlight and to wear protective clothing, sunglasses, and sunscreen with an SPF of 15 or higher, especially if you sunburn easily. Also avoid prolonged exposure to cold or wind. Adapalene may make your

skin sensitive to sunlight or extreme weather.

do not use hot wax to remove unwanted hair during your treatment with adapalene.

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?

Apply 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 apply a double dose to make up for a missed one.

What side effects can this medication cause?

Adapalene may cause side effects. The following symptoms are likely to affect your skin during the first 2-4 weeks of treatment. Tell your doctor if any of these

symptoms are severe or do not go away:

redness

scaling

dryness

burning or stinging

itching

Medications that are similar to adapalene have caused tumors in laboratory animals who were given the

medications and exposed to real or artificial sunlight. It is not known whether adapalene increases the risk of tumors in humans. Protect yourself from sunlight and sunlamps while taking adapalene, and talk to your doctor about the risks of taking this medication.

Adapalene may cause other side effects. Call your doctor if you have any unusual problems while 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). If you are using a bottle of

adapalene solution, be sure to store it upright. 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 use 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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