Tretinoin
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Tretinoin (all-trans retinoic acid, ATRA)
Retin-A, Renova, Atralin, Avita, Tretin-X, Refissa, Altreno; Vesanoid (oral, APL)
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Summary
Common uses
Acne vulgaris (topical)0, Photoaging0, Acute promyelocytic leukemia (oral ATRA, with arsenic trioxide or anthracycline)0
Pharmacy
Starting dose
Topical: pea-sized amount to dry face at bedtime, building from 2-3×/week to nightly as tolerated; oral APL: 45 mg/m²/d in divided doses
Preparations
Topical 0.01-0.1% creams, gels, micropsheres, lotions; oral 10 mg capsules (Vesanoid)
US FDA Max
Topical: nightly; oral APL: 45 mg/m²/d
Pharmacology
Routes
Topical, oral (APL only)
Onset
Topical: irritation within days; acne improvement 6-12 weeks; oral APL response within days
Duration
N/A
Half-life
~0.5-2 hours (oral)[1]
Bioavailability
Topical: minimal systemic absorption with normal skin; oral: variable, induced metabolism with repeated dosing[1]
Pregnancy
Oral tretinoin is teratogenic (Category D historically; APL exception treated under strict pregnancy avoidance); topical tretinoin in pregnancy has lower (but not zero) concern and is generally avoided.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Tretinoin is all-trans retinoic acid, the active metabolite of vitamin A; it binds nuclear retinoic acid receptors (RAR α/β/γ), regulating transcription of genes governing epithelial differentiation, proliferation, and inflammation.0 In acne, normalizes follicular keratinization and reduces comedone formation. In APL, the PML-RARα fusion oncoprotein responds to pharmacologic ATRA by resuming terminal granulocytic differentiation — one of the first successful examples of differentiation therapy in oncology, transforming APL from highly fatal to highly curable. Differentiation syndrome (capillary leak, hyperleukocytosis, dyspnea) is the major adverse effect of oral APL induction[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Vesanoid (tretinoin), Roche, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/020438s004lbl.pdf