Comparative Pharmacology
Head-to-head clinical analysis: ISOTRETINOIN versus TARGRETIN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ISOTRETINOIN versus TARGRETIN.
ISOTRETINOIN vs TARGRETIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Reduces sebum production, inhibits sebaceous gland activity, and induces apoptosis in sebocytes. Binds to retinoic acid receptors (RARs) and retinoid X receptors (RXRs) to regulate gene expression.
Selective retinoid X receptor (RXR) agonist that modulates gene expression involved in cell differentiation, proliferation, and apoptosis.
0.5-1 mg/kg/day orally in two divided doses for 15-20 weeks; cumulative dose 120-150 mg/kg.
300 mg/m2 orally once daily.
None Documented
None Documented
Terminal elimination half-life is approximately 20 hours (range 10-30 hours) for the parent drug. Clinical significance: steady-state achieved in ~5 days with repeated dosing; prolongation in renal impairment is minimal.
Clinical Note
moderateIsotretinoin + Estrone sulfate
"The therapeutic efficacy of Estrone sulfate can be decreased when used in combination with Isotretinoin."
Clinical Note
moderateIsotretinoin + Estramustine
"The therapeutic efficacy of Estramustine can be decreased when used in combination with Isotretinoin."
Clinical Note
moderateIsotretinoin + Dienogest
"The therapeutic efficacy of Dienogest can be decreased when used in combination with Isotretinoin."
Clinical Note
moderateIsotretinoin + Medroxyprogesterone acetate
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.
Primarily hepatic metabolism; metabolites excreted in urine (65-80%) and feces (15-35%). Less than 1% excreted unchanged in urine.
Primarily metabolized in the liver via CYP3A4; elimination is mainly through hepatobiliary excretion into feces. Renal excretion is minimal (<3% as unchanged drug).
Category D/X
Category C
Retinoid
Retinoid
"The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Isotretinoin."