Drug information of Isotretinoin

Mechanism of effect

Reduces sebum secretion and sebaceous gland size, and inhibits sebaceous gland differentiation.

Pharmacodynamic

Isotretinoin, a retinoid, is indicated in the treatment of severe recalcitrant nodular acne.

Pharmacokinetics

The T max is approximately 3 h (fasted); 5 h (fed). Absorption increases with food or milk. More than 99.9% bound to protein, primarily albumin. The major metabolite is 4-oxo-isotretinoin. CYP2C8, CYP2C9, CYP3A4, and CYP2B6 involved in isotretinoin metabolism. The mean t ½ is 21 h (isotretinoin) and 24 h (4-oxo-isotretinoin). 65% to 83% is excreted equally via the urine and feces.

Drug indications

Acute Nonlymphocytic Leukemia , Acne , Melanoma - Metastatic , Granuloma Annulare

Dosage

Usual Adult Dose for Acne Severe recalcitrant nodular acne: 0.5 to 1 mg/kg/day orally in 2 divided doses; patients whose disease is very severe with scarring or is primarily manifested on the trunk may require up to 2 mg/kg/day.

Drug contraindications

Pregnancy , hypersensitivity to drug or its components. , Hypersensitivity to parabens

Side effects

Headache , insomnia , Tachycardia , dizziness , fatigue , Hepatic dysfunction , allergic reaction , Depression , urticaria , anemia , palpitations , respiratory tract infection , malaise , conjunctivitis , bronchospasm , syncope , Cataracts , vascular access thrombosis , sweating , hepatitis , Photosensitivity , lethargy

Interactions

Tetracycline , Doxycycline , Minocycline , Vitamin A , Vitamin A+E+C , Benzoyl Peroxide , teriflunomide , Mequinol , meglitol , triparanol , Azelaic acid , Demeclocycline , aminolevulinic acid oral , Aminolevulinic acid topical , Salicylic acid , Methyl aminolevulinate , Cannabidiol , Blonanserin , Sarecycline , sirukumab , Omadacycline

Alerts

1-Isotretinoin must not be used by females who are or may become pregnant. 2-Impaired hearing has been reported in patients taking isotretinoin. 3-Obtain 2 negative urine or serum pregnancy tests prior to receiving initial isotretinoin prescription and negative result for urine or serum pregnancy test each month. 4-obtain pretreatment and follow-up lipids during fasting conditions. 5-monitor liver function weekly or biweekly until isotretinoin response has been established. 6- periodically determine blood glucose.

Points of recommendation

1-Caution patient against use of vitamin A, even in multivitamins, to avoid additive toxicity. 2-Advise patient to take medication with meals. 3-Suggest use of lubricant (eg, petroleum jelly) on lips to prevent cheilitis. 4-Inform patient to avoid wax epilation and skin resurfacing procedures (eg, dermabrasion, laser) during therapy and for at least 6 mo thereafter because of possible scarring. 5-Advise patient to control weight, decrease dietary fat, and restrict alcohol intake 36 h before lipid determinations to avoid elevation in serum triglycerides. 6-Instruct patient to discontinue any other acne medications (including OTC topical preparations) before starting therapy.

Pregnancy level

X

Related drugs

Bexarotene