Comparative Pharmacology
Head-to-head clinical analysis: ACCUTANE versus TARGRETIN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ACCUTANE versus TARGRETIN.
ACCUTANE vs TARGRETIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Retinoid that reduces sebum production, normalizes follicular keratinization, and decreases Propionibacterium acnes growth by binding to nuclear retinoic acid receptors, altering gene expression.
Selective retinoid X receptor (RXR) agonist that modulates gene expression involved in cell differentiation, proliferation, and apoptosis.
Isotretinoin 0.5-1 mg/kg/day orally in 2 divided doses for 15-20 weeks.
300 mg/m2 orally once daily.
None Documented
None Documented
Terminal elimination half-life of isotretinoin is 10-20 hours. The half-life of the major metabolite, 4-oxo-isotretinoin, is 11-50 hours. The long half-life of the metabolite may contribute to sustained clinical effects.
Terminal elimination half-life is approximately 7 hours (range 3–10 hours) for the parent drug. The active metabolite (bexarotene glucuronide) has a half-life of about 9 hours. Clinically, steady state is reached within 3–5 days.
Renal and biliary: approximately equal amounts of metabolites are excreted in urine and feces. Unchanged drug is not excreted. Major metabolites: 4-oxo-isotretinoin, tretinoin, 4-oxo-tretinoin. Renal excretion of metabolites accounts for ~65-83% of the dose; fecal excretion accounts for the remainder.
Primarily metabolized in the liver via CYP3A4; elimination is mainly through hepatobiliary excretion into feces. Renal excretion is minimal (<3% as unchanged drug).
Category C
Category C
Retinoid
Retinoid