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Tretinoin - Uses, Dosage, Side Effects, Drug Warnings, and Precautions

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Tretinoin is a drug utilized for the treatment of acne and pigmentation of the skin. Refer to this article to know more in detail.

Medically reviewed by

Dr. Dhepe Snehal Madhav

Published At May 24, 2023
Reviewed AtMay 24, 2023

Overview:

Tretinoin is also called all-trans retinoic acid. Tretinoin belongs to a class of medications that are prescribed for the treatment of acne and pigmentation of the skin. Tretinoin is used as a topical ointment and also as an oral drug. Tretinoin acts by promoting the detachment of cornified cells (these are highly insoluble tough structures formed during the differentiation of keratinocytes), and thus it increases the pace of cell shedding. Tretinoin increases mitotic activity, and thus it leads to increased turnover of corneocytes that are loosely adherent; the older skin cells get replaced by the new ones. Tretinoin also plays an important role in protecting the skin from harmful ultraviolet rays (UV-rays). The Food and Drug Administration (FDA) approved Tretinoin on December 24, 1998.

Uses of the Drug Tretinoin:

Tretinoin is available as a topical ointment and also as an oral drug. Tretinoin in the form of Isotretinoin is used as an oral medication. Topical forms of this drug are prescribed in the form of gels and creams; it is used for the treatment of skin disorders like acne and hyperpigmentation. Tretinoin, as an oral medication, is used for the treatment of conditions such as disfiguring nodular acne. The prescription of this drug is based on the age of the individual, the systemic medical conditions they are suffering from, and the response of the body to this drug treatment.

Dosage and Administration:

The commonest prescribed dosage of Tretinoin is 0.05 percent and 0.02 percent.

A pea-sized amount of the drug Tretinoin is prescribed to be applied over the affected area of the skin once a day, and for the best result, it should be applied during bedtime at night.

The following precautions should be taken while applying the drug Tretinoin:

  • Patients are advised to wash their face with a mild soap and pat dry approximately 20 to 30 minutes before the drug application.

  • Few patients may experience a sense of warmth at the drug application site. This is a normal phenomenon that occurs secondary to drug application. Discontinuation of drugs due to the occurrence of such a sensation is not required.

  • Patients should not abruptly stop the application of the medication. Evident signs of retinoid treatment effect on wrinkle reduction are sometimes noticed six months after the regular application of the Tretinoin drug.

Dosage Forms and Strengths:

Tretinoin is available in the following forms:

  • Cream-based Tretinoin ointment.

  • Gel-based Tretinoin ointment.

Both gel and cream forms of T-tretinoin ointment are available in various strengths.

Cream-based Tretinoin ointments are available in the following strengths:

  • Cream 0.1 percent.

  • Cream 0.5 percent.

  • Cream 0.23 percent.

Gel-based tretinoin ointments are available in the following strengths:

  • Gel 0.025 percent.

  • Gel 0.01 percent.

Dosage and Modifications:

Tretinoin, on application, produces warmth and a stinging sensation at the site.

  • Few patients may experience severe warmth and stinging experience; in such cases, the drug should be temporarily stopped. In some cases, the doctors advise reducing the frequency of the drug application until the patient can tolerate the medication.

Warnings and Precautions:

  • Clinical trials have reported a few cases of urticaria (extensively itchy rashes caused due to an allergic reaction), facial edema (swelling of the face), and exfoliative skin disease associated with individuals applying Tretinoin for the management of acne and hyperpigmentation of the skin. The medication should be immediately discontinued in individuals with severe hypersensitivity symptoms, and emergency management protocols should be followed. Alternative drugs should be prescribed when an allergic reaction to Tretinoin gets established to protect the individual from the life-threatening hypersensitivity reactions associated with Tretinoin.

  • The safety and efficacy of the drug ointment Tretinoin for treating acne and other skin disorders have not yet been established for children younger than 12 years of age. So, the drug should be used only after the doctor's recommendations.

  • The safety and efficacy of the drug ointment Tretinoin for treating fine lines and wrinkles in children younger than 18 years of age have not yet been established. So, the drug should be used only after the doctor's recommendations.

  • Over-application of the drug should not be done as it may lead to pilling and caking.

  • The sensation of warmth and stinging may occur at the drug application site.

  • During the first week of treatment, an acute exacerbation of acne may occur. Still, the drug application should not be stopped as the acne is noted to reduce after regular drug application.

  • Patients who experience severe stinging and warmth after applying cream-based Tretinoin ointments are advised to use gel-based Tretinoin.

Contraindications:

It is contraindicated in patients having the following conditions:

  • Allergy: Clinical trials have reported a few cases of urticaria (extensively itchy rashes caused due to an allergic reaction), facial edema (swelling of the face), and exfoliative skin disease associated with individuals applying Tretinoin for the management of acne and hyperpigmentation of the skin. The medication should be immediately discontinued in individuals with severe hypersensitivity symptoms, and emergency management protocols should be followed. Alternative drugs should be prescribed when an allergic reaction to Tretinoin gets established to protect the individual from the life-threatening hypersensitivity reactions associated with Tretinoin.

  • Eczema: The usage of the drug Tretinoin is not recommended in individuals suffering from eczema as it may worsen the symptoms of eczema.

  • Pregnancy: The safety of Tretinoin ointment has not yet been established for the usage in first-trimester .

Drug Interactions:

Tretinoin is noted to interact with drugs like topical aminolevulinic acid, topical benzoyl peroxide, Isotretinoin, Methoxsalen, and topical methyl aminolevulinic acid.

Adverse Reactions Associated With Peramivir:

Adverse reactions include unexpected or dangerous reactions associated with a particular drug.

  • Exfoliative dermatitis and rashes are noted as hypersensitivity reactions with the drug Tretinoin. The medication should be immediately discontinued in individuals with severe hypersensitivity symptoms, and emergency management protocols should be followed. Alternative drugs should be prescribed when an allergic reaction to Tretinoin gets established to protect the individual from the life-threatening hypersensitivity reactions associated with Tretinoin.

For Patients:

What Is Acne?

It is an inflammatory disorder affecting the skin. It generally occurs when the hair follicle in the skin gets plugged with oil and dirt. It is most commonly seen in young adults and teenagers. In common terms, acne is called pimples. Acne on the skin is aesthetically unappealing, thus individuals suffering from acne are concerned about its treatment. Acne appears as red bumps of 0.5 millimeters to 1 millimeter in diameter; sometimes, it may also be pus-filled, and these lesions are noted to be tender on palpation.

What Is Tretinoin?

Tretinoin is also called all-trans retinoic acid. Tretinoin belongs to a class of medications that are prescribed for the treatment of acne and pigmentation of the skin. Tretinoin is used as a topical ointment and also as an oral drug. Tretinoin increase mitotic activity, and thus it leads to increased turnover of corneocytes that are loosely adherent; the older skin cells get replaced by the new ones. Tretinoin also plays an important role in protecting the skin from harmful UV rays. The commonest prescribed dosage of Tretinoin is 0.05 percent and 0.02 percent.

A pea-sized amount of the drug tretinoin is prescribed to be applied over the affected area of the skin once a day, and for the best result, it should be applied during bedtime at night.

What Is the Most Significant Information That Should Be Known about Tretinoin?

The drug should be judiciously prescribed.

  • Exfoliative dermatitis and rashes are noted as hypersensitivity reactions with the drug Tretinoin. The medication should be immediately discontinued in individuals with severe hypersensitivity symptoms, and emergency management protocols should be followed. Alternative drugs should be prescribed when an allergic reaction to Tretinoin gets established to protect the individual from the life-threatening hypersensitivity reactions associated with Tretinoin.

  • The safety of Tretinoin ointment has not yet been established for usage in First-trimester.

  • The usage of the drug Tretinoin is not recommended in individuals suffering from eczema as it may worsen the symptoms of eczema.

  • The safety and efficacy of the drug ointment Tretinoin for treating acne and other skin disorders have not yet been established for children younger than 12 years . So, the drug should be used only after the doctor's recommendations.

What Is to Be Done in Case of a Missed Dose and an Overdose of Tretinoin?

The commonest prescribed dosage of Tretinoin is 0.05 percent and 0.02 percent.

A pea-sized amount of the drug tretinoin is prescribed to be applied over the affected area of the skin once a day, and for the best result, it should be applied during bedtime at night.

  • Missed Dose: In case the individual forgets to apply the prescribed dose of the ointment, or in any case, the amount is omitted, then the Tretinoin ointment should be taken as soon as they remember, or if it is time for the second dose application, then the individual can skip the first dose.

  • Overdose: Over-application of the drug should not be done as it may lead to pilling and caking.

What Things to Inform the Doctor before Starting the Treatment With Tretinoin?

Whenever an individual visits a doctor for the management of skin disorders, the following pieces of information should be given to the doctor:

  • Family History: The patient should inform the doctor if any family members, like their parents, are suffering from diabetes mellitus (increased blood glucose levels), hypertension (increased blood pressure), hypotension, or renal and hepatic disorder. They should also disclose if their siblings or other family member has any history of underlying medical conditions. This information helps the doctors know the disorder's hereditary pattern and the common signs and symptoms that run in the individual's family. Family history of the disease guides the doctor in planning a better management and treatment protocol.

  • Personal History: Personal history includes altered symptoms that an individual faces, like excessive weight gain or weight loss, drowsiness, lethargy, swollen legs, increased heart rate, increased thirst, increased urge to eat food, and increased or reduced urination.

  • Other Systemic Disorders: The patient should always inform the doctors if they are suffering from other underlying diseases like kidney disorders or liver dysfunction. Doctors prescribe medications keeping in consideration the other underlying systemic conditions.

  • Allergy: Known allergies to fish products containing medications should be informed to the doctor.

For Doctors:

Pharmacology:

Tretinoin acts by promoting the detachment of cornified cells (these are highly insoluble tough structures formed during the differentiation of keratinocytes), and thus it increases the pace of cell shedding. Tretinoin increases mitotic activity, and thus it leads to increased turnover of corneocytes that are loosely adherent; the older skin cells get replaced by the new ones.

Mechanism of Action:

Tretinoin binds the retinoic receptors alpha, beta, and gamma with retinoid X receptors. This results in reduced inflammatory response as the inflammatory mediator's activity gets blocked.

Absorption:

Tretinoin, when applied topically, gets around 1 to 31 percent absorbed.

Excretion:

Renal excretion of retinol takes place. Metabolites are formed by the process of oxidation and glucuronidation. 30 percent of the metabolites get excreted in the feces.

Clinical Studies:

Various clinical studies are carried world wide to establish the usage and application of the drug Tretinoin in all population groups. Various studies have shown that application of tretinoin in gel form is more effective and reduces the pigmentation more effectively in comparison to tretinoin creams. Various researches have shown that during the first week of treatment, an acute exacerbation of acne may occur. Still, the drug application should not be stopped as the acne is noted to reduce after regular drug application.Tretinoin for treating acne and other skin disorders have not yet been established for children younger than 12 years . So, the drug should be used only after the doctor's recommendations.

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Dr. Dhepe Snehal Madhav
Dr. Dhepe Snehal Madhav

Venereology

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