DrugInfoSys

Tazarotene

Drug #2230

Tazarotene is a pro-drug of the more water soluble tazarotenic acid and member of the acetylenic class of retinoids; represented by chemical formula: C21H21NO2S. Its chemical name is Ethyl 6-[(4,4-dimethylthiochroman-6-yl)ethynyl]nicotinate. Tazarotene is a a receptor-selective and binds to RAR-beta and RAR-gama and weakly to RAR-alpha.Tazarotenic acid does not interconvert to any other retinoids that could potentially activate other retinoid receptors. In psoriasis, tazarotene normalizes keratinocyte differentiation, reverses keratinocyte hyperproliferation and has anti-inflammatory effects. In acne vulgaris, the abnormal desquamation of the follicular epithelium is normalized.

Primary Characteristics

It belongs to acetylenic class of retinoids.

It is classified in Anti Acne , Antipsoriatics , Antipsoriatics pharmacological group.

Molecular Weight: 351.46 · pKa: 1.5 · Non-proprietary name: Tazarotene.

Molecular structure of Tazarotene

Pharmacokinetics

Distribution: Tazarotene has a plasma protein binding is greater than 99% for tazarotenic acid.

Elimination: it is metabolised via to sulfoxides, sulfones& polar metabolites, plasma half-life is 18 hours, renal excretion is through urinary and fecal pathway..

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Indications

Tazarotene is primarily indicated in conditions like Acne vulgaris, Psoriasis vulgaris.

Contraindications

Tazarotene is contraindicated in conditions like Pregnancy, Hypersensitivity to the drug.

Dosage

Tazarotene's dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
0 – 0Every 24htopicalCleanse the face gently. After the skin is dry, apply a thin film of tazarotene 0.1% (2 mg/cm²) once a day, in the evening, to the skin where lesions appear. Apply to no more than 20% of body surface area. If a bath or shower is taken prior to application, the skin should be dry before applying the gel. If emollients are used, they should be applied at least an hour before its application.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

The signs and symptoms that are produced after acute overdosage of Tazarotene are Hypervitaminosis , Redness.

Tazarotene is known to cause more or less tolerable side effects which are usually transient. These include Burning, Desquamation , Dry skin, Erythema, Irritation, Pruritus , Skin discoloration, Stinging.

Warnings / Precautions

Women of child-bearing potential should be warned of the potential risk and use adequate birth-control measures when it is used. The possibility that a woman of childbearing potential is pregnant at the time of institution of therapy should be considered. A negative result for pregnancy test having a sensitivity down to at least 50 mIU/mL for hCG should be obtained within 2 weeks prior toTazarotene therapy, which should begin during a normal menstrual period. Apply only to the affected areas. For external use only. Avoid contact with eyes, eyelids, and mouth. If contact with eyes occurs, rinse thoroughly with water. The safety of use of Tazarotene over more than 20% of body surface area has not been established in psoriasis or acne. Retinoids should not be used on eczematous skin, as they may cause severe irritation. Avoide sunlight. Use sunscreens (minimum SPF of 15) and protective clothing when using it. Patients who may have considerable sun exposure due to their occupation and those patients with inherent sensitivity to sunlight should exercise particular caution when using it. It should be administered with caution if the patient is also taking drugs known to be photosensitizers (e.g., thiazides, tetracyclines, fluoroquinolones, phenothiazines, sulfonamides) because of the increased possibility of augmented photosensitivity.

Available Brands

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Single Ingredient

Storage Conditions

Tazarotene should be stored .

Drug Classification

  1. 1.13.5.1Antiacne preparations
  2. 2.13.9Anti-psoriatics

Manufacturers

Manufacturers of Tazarotene in Pakistan: