Order Retin-A (Tretinoin) over the counter (otc)

Pharmacological action

Retinoid. Structurally close to vitamin A, is a natural metabolite of retinol. When taken orally, it inhibits the differentiation and growth of a clone of altered blood cells, including human myeloleukemic cells. The mechanism of action in acute promyelocytic leukemia is probably due to damage caused by the binding of tretinoin to nuclear receptors of retinoic acid.

When applied externally, it enhances cell proliferation in the papillary layer of the skin, reduces the adhesion of cells involved in the formation of acne vulgaris. When treating open acne, it helps to smooth the skin surface without signs of inflammation. When treating closed acne, it promotes their transition to open acne or papules, which then heal without scarring after removing the keratin plug. Prevents the formation of new acne.

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Pharmacokinetics

Tretinoin is a natural metabolite of retinol, which is normally present in plasma. After oral administration, tretinoin is absorbed from the gastrointestinal tract. Plasma concentration returns to the initial endogenous level 7-12 hours after a single dose of 40 mg.

Plasma protein binding is high. Does not accumulate.

T1/2 is 0.7 hours. After oral administration of radiolabeled tretinoin, about 60% is excreted in the urine and about 30% in the feces. Metabolites are formed by oxidation and glucuronidation.

With prolonged use of tretinoin, a decrease in its concentration in the plasma is observed, which may be due to the induction of CYP isoenzymes.

Indications for use

Acne vulgaris (including comedones, papules, pustules), confluent acne. Favre-Racouchot disease (nodular cystic elastosis of the skin with comedones).

Contraindications

Hypersensitivity, pregnancy, lactation, children under 12 years of age (for all indications), under 18 years of age (for treatment of adverse effects of sunlight), over 50 years of age (for treatment of adverse effects of sunlight). With caution. Seborrheic dermatitis, eczema, sunburn, liver failure, pancreatitis, chronic renal failure, chronic intoxication (including alcohol intoxication), diabetes mellitus.

Method of administration and dosage

Externally, apply to the affected areas in a very thin layer once a day in the evening before bedtime, leave on the skin for 6 hours, then wash with running water; if necessary, increase the frequency of application to 2 times a day.

For people with light and dry skin, the exposure time of the drug at the beginning of treatment is 30 minutes, then it can be gradually increased. During the treatment, it is allowed to carefully remove completely softened comedones and pustules.

The duration of treatment depends on the type of pathology: in the treatment of acne vulgaris, the therapeutic effect occurs after 2-3 weeks, in most cases - after 6-7 weeks; the best clinical result is achieved after 3 months of therapy; in the treatment of adverse effects from exposure to sunlight - after 4-24 weeks.

For preventive purposes - 1 time per week, after a warm bath.

Treatment of flat warts begins with weak concentrations of tretinoin, in the absence of a clinical effect, both the concentration of the drug and the frequency of its use are increased (in the absence of skin irritation).

Side effects

Local reactions: allergic reactions (from moderate to severe) - tingling, hyperemia, burning, swelling at the site of application of the drug, photosensitivity; hypopigmentation of the skin, peeling and dryness of the skin, blistering or crusting; rarely - hyperpigmentation of the skin.

Special instructions

When applied externally, avoid contact with eyes, mouth, mucous membranes (if contact occurs, rinse immediately with water).

During the treatment period, it is recommended to avoid exposure to the sun. Patients with a tan can begin treatment after the tan has weakened.

After 1 week of therapy, the appearance of acne may increase, which is associated with the effect of the drug on deep acne, which were not visible before the start of treatment.

It should not be prescribed simultaneously with drugs that cause desquamation of the epithelium, as well as with cosmetics and hygiene products that cause dryness and irritation of the skin.

Sometimes, for the treatment of acne vulgaris, it is recommended to simultaneously prescribe oral isotretinoin and a local form of tretinoin, in which case, if adverse effects occur, either reduce the dose of one of the retinoids or cancel it until the adverse effects disappear.

In the treatment of follicular keratosis, irritation symptoms can be reduced by simultaneously prescribing local GCS.

Do not use a water-oil based cream to treat acne vulgaris.

It should be borne in mind that tretinoin as a monotherapy is used to treat acne vulgaris of I and II degrees of severity. In more severe cases, a combination of tretinoin with antibiotics (local and systemic) or benzoyl peroxide is recommended to enhance the therapeutic effect.

Efficacy and safety in the treatment of photochemical dermatosis and skin tumors have not been established.

Tretinoin should not be used in cases of deep wrinkles, yellowing of the skin, telangiectasias, "sluggish" skin, melanocytic atypia, skin elastosis.

Interaction

Concomitant use of tretinoin with topical antibiotics (clindamycin, erythromycin), benzoyl peroxide, resorcinol, salicylic acid, astringents, aftershave lotions, products containing peeling agents, sulfur, ethanol, cosmetics, soaps and hair care products that cause dry skin, substances containing lemon or having an abrasive effect, can cause increased irritation and dryness of the skin (requires either a reduction in the dose of tretinoin or temporary cessation of treatment until the disappearance of adverse effects).

Increases the rate and systemic absorption of minoxidil (topical forms), which promotes hair growth and increases the risk of skin irritation (simultaneous use is not recommended).

Simultaneous use with drugs that increase photosensitivity (including fluoroquinolones, phenothiazines, sulfonamides, thiazide diuretics) increases the risk of photosensitivity (especially in the first months of treatment), which requires either a reduction in the dose of tretinoin or a temporary cessation of its use until the adverse effects disappear.

When used simultaneously with other retinoids (acitretin, etretinate, isotretinoin, oral tretinoin), dryness and irritation of the skin increases.

Storage conditions for Retin-A®

At a temperature of 15-25 °C.

Keep out of the reach of children.

Shelf life of Retin-A®

3 years.

Do not use after the expiry date stated on the package.

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