ARAZLO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ARAZLO (ARAZLO).
ARAZLO (tazarotene) is a retinoid prodrug that is converted to its active metabolite, tazarotenic acid, which binds to retinoic acid receptors (RARs), specifically RAR-β and RAR-γ, modulating gene expression to normalize epidermal differentiation, reduce keratinocyte proliferation, and decrease inflammation.
| Metabolism | Tazarotene is rapidly metabolized via ester hydrolysis to its active metabolite, tazarotenic acid, primarily by esterases in plasma and liver. Tazarotenic acid is further metabolized by oxidation (CYP2C8, CYP3A4) and conjugation (glucuronidation) to inactive metabolites. |
| Excretion | Primarily fecal excretion of unchanged drug (≥90%) and biliary elimination; renal excretion accounts for <2%. |
| Half-life | Terminal half-life approximately 29 hours, supporting once-weekly topical application. |
| Protein binding | >99% bound to plasma proteins (albumin and lipoproteins). |
| Volume of Distribution | Not reported for topical ARAZLO; systemic absorption minimal. For oral tazarotene, Vd is approximately 1.8 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Systemic bioavailability is <1% after topical application; negligible compared to oral administration. |
| Onset of Action | Onset of action within 2 weeks of topical application; visible improvement may be seen at 4 weeks. |
| Duration of Action | Duration of action is sustained over the 7-day dosing interval; continuous treatment required for maintenance. |
Topical: Apply 0.045% gel once daily to affected areas of the face.
| Dosage form | LOTION |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Not approved for use in pediatric patients below 9 years of age. For patients 9 years and older, same as adult dose. |
| Geriatric use | No specific geriatric dose adjustment; use caution due to potential increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ARAZLO (ARAZLO).
| Breastfeeding | Contraindicated during breastfeeding. Tazarotene is excreted in animal milk; no human data available. M/P ratio not determined. Risk of infant exposure outweighs benefits. |
| Teratogenic Risk | FDA Pregnancy Category X. Contraindicated in pregnancy due to high risk of severe fetal malformations including CNS, cardiovascular, and craniofacial defects, as well as increased risk of spontaneous abortion. All trimesters are affected; no safe period exists. |
| Fetal Monitoring |
■ FDA Black Box Warning
ARAZLO is contraindicated in women who are or may become pregnant. Tazarotene is a teratogen and can cause fetal harm when administered to a pregnant woman. If the patient becomes pregnant while using this drug, treatment should be discontinued immediately and the patient apprised of the potential hazard to the fetus.
| Serious Effects |
["Pregnancy or women planning pregnancy","History of hypersensitivity to tazarotene or any component of the formulation","Nursing mothers (due to potential for transfer to infant)"]
| Precautions | ["Pregnancy category X, contraindicated in women of childbearing potential unless using adequate contraception","Avoid exposure to UV light (sunlight, tanning lamps) due to increased phototoxicity risk","Transient local skin reactions (burning, stinging, erythema, peeling) may occur; reduce frequency or concentration if irritation is severe","Use with caution in patients with eczema or other concurrent skin conditions due to potential irritation","Not recommended for use on broken, eczematous, or sunburned skin"] |
| Food/Dietary |
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| Monitor for signs of teratogenicity if inadvertent exposure occurs. Pregnancy test required before initiation and monthly during therapy. Use two forms of contraception. Discontinue immediately if pregnancy occurs. |
| Fertility Effects | Tazarotene showed no impairment of fertility in animal studies at topical doses. No human data on fertility effects; however, due to teratogenicity, fertility preservation strategies are not applicable given contraindication in pregnancy. |
| No clinically significant food interactions reported. Alcohol may exacerbate skin dryness and irritation; limit consumption. |
| Clinical Pearls | ARAZLO (tazarotene) lotion 0.045% is a retinoid approved for acne vulgaris. Apply a pea-sized amount to entire face after cleansing and drying. Avoid contact with eyes, mouth, and mucous membranes. Use with caution in patients with eczema or sunburn. Photosensitivity occurs; strict sunscreen use required. Women of childbearing potential must use effective contraception and have negative pregnancy test before starting. Avoid concurrent use of other retinoids, resorcinol, or sulfur products to prevent excessive irritation. |
| Patient Advice | Apply a thin layer to clean, dry skin once daily in the evening. · Use only pea-sized amount for entire face to avoid irritation. · Wash hands immediately after application. · Expect initial worsening of acne and skin peeling; improvement over 12 weeks. · Avoid sun exposure; use broad-spectrum SPF 30+ sunscreen daily. · Do not use if pregnant, planning pregnancy, or breastfeeding. · Stop use and consult doctor if severe redness, blistering, or oozing occurs. · Do not apply to broken or eczematous skin. · Avoid waxing, depilatories, or chemical peels during treatment. |