Drug information of Isotretinoin
Isotretinoin is a form of vitamin A. It reduces the amount of oil released by oil glands in your skin, and helps your skin renew itself more quickly. Isotretinoin is used to treat severe nodular acne that has not responded to other treatments, including antibiotics.
Mechanism of effect
Reduces sebum secretion and sebaceous gland size, and inhibits sebaceous gland differentiation.
Isotretinoin, a retinoid, is indicated in the treatment of severe recalcitrant nodular acne.
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 indicationsAcute Nonlymphocytic Leukemia , Acne , Melanoma - Metastatic , Granuloma Annulare
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 contraindicationsPregnancy , hypersensitivity to drug or its components. , Hypersensitivity to parabens
Side effectsHeadache , 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
InteractionsTetracycline , 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
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.
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