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Tretinoin, Discover, Action, Best Uses, Side effects, Dosage and 6 Brands

Tretinoin, Discover, Action, Best Uses, Side effects, Dosage and 6 Brands

  • May 11, 2024
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Introduction

Tretinoin, also known as all-trans retinoic acid, is a topical medication derived from vitamin A. It belongs to a class of drugs called retinoids, which are known for their ability to regulate cell growth and differentiation. It is widely used in dermatology for the treatment of acne, as well as for improving the appearance of photodamaged skin.

Tretinoin is a medication used to treat acne and other skin conditions. It belongs to a class of medications called retinoids and works by affecting the growth of skin cells. It decreases the number and severity of acne pimples and promotes quick healing of pimples that do develop. It is considered a better alternative to retinol for reducing the appearance of fine lines and wrinkles.

Discovery

Tretinoin’s discovery is traced back to the mid-20th century. In the late 1930s and early 1940s, researchers were investigating the effects of vitamin A derivatives on various physiological processes. In the 1950s, scientists discovered that certain vitamin A derivatives had beneficial effects on skin conditions, such as acne.

The specific compound known as tretinoin was first synthesized by researchers at the University of Pennsylvania in the early 1960s. Dr. Albert M. Kligman, along with his colleague Dr. James Fulton, synthesized tretinoin as a modification of vitamin A with the aim of creating a more effective treatment for acne.

Their research led to the development of Retin-A, the first topical formulation of tretinoin, which was approved by the U.S. Food and Drug Administration (FDA) in 1971 for the treatment of acne. Retin-A revolutionized the treatment of acne by offering a more effective and targeted approach compared to existing treatments at the time.

Following its approval for acne, researchers and clinicians began to explore the potential uses of tretinoin beyond acne treatment. It was soon discovered that tretinoin had beneficial effects on other skin conditions, such as photoaging, hyperpigmentation, and rough skin texture.

Mechanism of Action

The mechanism of action of tretinoin primarily involves its interaction with specific receptors in skin cells called retinoic acid receptors (RARs). These receptors are part of the nuclear receptor superfamily and are involved in regulating gene expression.

When tretinoin is applied topically to the skin, it penetrates into the epidermis and dermis layers. Once inside the skin cells, tretinoin binds to and activates RARs, particularly RAR-β and RAR-γ isoforms. This binding leads to conformational changes in the receptor complexes and subsequent recruitment of coactivator proteins.

The activated RARs, in complex with coactivators, then bind to specific DNA sequences known as retinoic acid response elements (RAREs) within the promoter regions of target genes. This binding initiates the transcription of target genes involved in various cellular processes.

The key effects of tretinoin mediated through this mechanism include:

  1. Cellular Differentiation: Tretinoin promotes the differentiation of keratinocytes (the predominant cells in the epidermis) and regulates the formation of mature, functional skin cells. This process helps to prevent the formation of microcomedones (the precursors of acne lesions) and promotes the shedding of dead skin cells, which can contribute to acne and other skin conditions.
  2. Cellular Proliferation: Tretinoin inhibits the proliferation of keratinocytes and sebocytes (oil-producing cells in the skin). By reducing the excessive proliferation of these cells, tretinoin helps to prevent the formation of acne lesions and reduces the risk of pore blockage.
  3. Inflammation: Tretinoin has anti-inflammatory properties and can suppress the production of pro-inflammatory mediators within the skin. By reducing inflammation, tretinoin helps to alleviate the redness, swelling, and discomfort associated with acne and other inflammatory skin conditions.
  4. Collagen Synthesis: Tretinoin stimulates the production of collagen and other extracellular matrix components in the skin. Collagen is a structural protein that provides strength and elasticity to the skin. By promoting collagen synthesis, tretinoin helps to improve skin texture, reduce the appearance of fine lines and wrinkles, and enhance overall skin firmness and resilience.

Tretinoin Uses

Tretinoin has several uses in dermatology due to its ability to influence various cellular processes in the skin. Some uses include:

Acne Treatment

Tretinoin is widely used as a first-line treatment for acne vulgaris. It helps to unclog pores, reduce inflammation, and prevent the formation of new acne lesions. It is particularly effective in treating comedonal acne (blackheads and whiteheads) and can also be beneficial for inflammatory acne lesions.

Anti-aging Treatment

It is also used to improve the appearance of aging skin. It can reduce the appearance of fine lines, wrinkles, and hyperpigmentation, leading to smoother, more youthful-looking skin. It promotes collagen synthesis and increases skin cell turnover, which helps to rejuvenate the skin and diminish the signs of aging.

Hyperpigmentation

Tretinoin helps lighten dark spots and uneven skin tone caused by sun damage, melasma, or post-inflammatory hyperpigmentation. By promoting exfoliation and increasing cell turnover, tretinoin can gradually fade hyperpigmented areas and promote a more even complexion.

Rough Skin Texture

It improves the texture and overall quality of the skin by promoting cell turnover and collagen production. It helps to smooth rough patches, refine pores, and create a more even skin surface.

Keratosis Pilaris

Tretinoin is also used to treat keratosis pilaris, a common skin condition characterized by rough, bumpy skin, usually on the upper arms, thighs, or buttocks. It helps to exfoliate the skin and reduce the buildup of keratin within the hair follicles, improving the appearance of keratosis pilaris over time.

Dosage

The general dosage guidelines for the tretinoin:

For Acne Vulgaris

Start with a low concentration (e.g., 0.025% cream or gel) applied once daily at bedtime.
Depending on the response and tolerance, the concentration and frequency of application may be adjusted by your healthcare provider.

For Anti-aging (Fine Lines and Wrinkles)

Start with a low to moderate concentration (e.g., 0.025% to 0.05% cream or gel) applied once daily at bedtime.
Higher concentrations are used as tolerated, but they should be introduced gradually to minimize skin irritation.

For Hyperpigmentation and Rough Skin Texture

Similar to acne and anti-aging treatments, start with a low to moderate concentration applied once daily at bedtime.
Higher concentrations are necessary for more stubborn cases of hyperpigmentation, but caution should be exercised to avoid irritation.

Side Effects

Tretinoin, like any medication, causes side effects, especially during the initial stages of treatment. Common side effects include:

Skin Irritation

Tretinoin can cause redness, itching, burning, or stinging sensation on the skin, particularly during the first few weeks of treatment. This irritation is usually mild to moderate and tends to diminish as the skin adjusts to the medication.

Dryness and Peeling

It causes dryness and flakiness of the skin, leading to peeling or scaling. This is a result of increased cell turnover and exfoliation induced by the medication. Using a moisturizer can help alleviate dryness and minimize peeling.

Increased Sensitivity to Sunlight

It makes the skin more sensitive to sunlight, increasing the risk of sunburn and other sun-related damage. It’s essential to use sunscreen with a high SPF and to avoid prolonged sun exposure while using tretinoin.

Temporary Worsening of Acne

Some individuals experience a temporary worsening of acne lesions when starting tretinoin treatment. This is often referred to as the “retinoid purge” and is thought to result from the rapid turnover of skin cells and the initial release of trapped debris from the pores. This worsening typically improves with continued use of the medication.

Skin Discoloration

Tretinoin causes temporary hyperpigmentation or hypopigmentation of the skin, particularly in individuals with darker skin tones. This usually resolves once the skin adjusts to the medication, but it’s essential to use sunscreen to prevent further pigmentation changes.

Skin Sensitivity

Some individuals experience increased sensitivity or allergic reactions to tretinoin, leading to additional skin irritation or rash. If you develop severe or persistent skin reactions, it’s important to discontinue use and consult your healthcare provider.

Tretinoin Brands

Tretinoin is a common ingredient in many skincare products, and it’s often used to treat acne, improve skin texture, and reduce the appearance of wrinkles. Some tretinoin creams available in Pakistan are:

Skin A

Skin A is manufactured by various companies, including but not limited to Pharma Health Pakistan Ltd. or Elixir Pharma. This brand could offer products with tretinoin for acne treatment, anti-aging, or skin renewal purposes.

Lazma

Lazma Cream is produced by reputable manufacturers like U&I Pharmaceuticals or other local pharmaceutical companies. While it does not directly contain tretinoin, it includes other skin-lightening agents alongside or in combination with tretinoin for treating hyperpigmentation issues.

Clycin-T

Manufactured by Ranbaxy Laboratories, Clycin-T is a brand that contains tretinoin among its active ingredients. It is commonly used for treating acne and improving overall skin texture.

Acdermin

Manufactured by Atco Pharmaceutical Company. Acdermin is another brand that incorporates tretinoin in its formulations. It’s often utilized for acne treatment and skin rejuvenation.

Cleret Gel

Cleret Gel is manufactured by companies like Hilton Pharma or Martin Dow Pharmaceuticals. it contains tretinoin and is formulated for treating acne or other dermatological conditions.

Hyderquin

Manufactured by reputable pharmaceutical companies such as GSK or others, Hyderquin contains tretinoin among its active ingredients. It is used for treating conditions like melasma or hyperpigmentation.

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