P - Contraindicated in pregnancy
L - Contraindicated in lactation
FI - Food *
Isotretinoin is a medication used for the treatment of moderate to severe acne. It was first developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more. It is still used in the treatment of these cancers to this day because of its ability to kill rapidly dividing cells. The effects of the medication are systemic and non-selective. In some cases, it is used to treat Harlequin type ichthyosis, a usually lethal skin deformation in which sufferers develop armor plated-like skin and usually die soon after birth. It is a retinoid, meaning it derives from vitamin A and is found in small quantities naturally in the body. Oral isotretinoin is marketed under various trade names, most commonly Roaccutane (Hoffman-La Roche; simply Accutane before July 2009), Amnesteem (Mylan), Claravis (Barr), Clarus (PremPharm), Decutan (Actavis), Isotane (Pacific Pharmaceuticals), Izotek (BlauFarma), Oratane (Genepharm Australasia), or Sotret (Ranbaxy), while topical isotretinoin is most commonly marketed under the trade names Isotrex or Isotrexin (Stiefel).
Isotretinoin is a synthetic retinoid which reduces sebaceous gland size and sebum production. It also regulates cell proliferation and differentiation.
Low oral bioavailability. Peak plasma concentrations in 1-4 hours (oral).
Protein-binding: 99.9%, mainly to albumin.
Hepatic, via CYP450 isoenzyme pathway.
Via urine and faeces.
Information Not Available
Dryness of mucous membranes, dryness of skin with scaling, fragility, erythema, cheilitis, pruritus, epistaxis, conjunctivitis, dry sore mouth and palmo-plantar exfoliation. Corneal opacities, dry eyes, visual disturbances, skeletal hyperostosis and musculoskeletal symptoms. Elevation of serum triglycerides, LFTs, ESR and blood glucose. Hair thinning, photosensitivity, changes in skin pigmentation, paronychia. GI disturbances, hepatitis. Headache, drowsiness, sweating, mood changes, psychotic symptoms, depression, suicidal tendencies, benign intracranial hypertension, seizures. Vasculitis, hypersensitivity reactions, IBS.
Potentially Fatal: Anaphylaxis. Haemorrhagic pancreatitis.
Special prescribing requirements
Because of isotretinoin's teratogenicity, and to minimize fetal exposure, isotretinoin is approved for marketing only under a restricted distribution program, called iPLEDGE, approved by the FDA. Isotretinoin must be prescribed by prescribers and dispensed by pharmacies registered and activated with the iPLEDGE program, and must only be dispensed to patients who are registered and meet all the requirements of iPLEDGE.
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; obtain pretreatment and follow-up lipids during fasting conditions; monitor liver function weekly or biweekly until isotretinoin response has been established; periodically determine blood glucose.
Preexisting or predisposition to hypertriglyceridaemia (e.g. DM, obesity or increased alcohol intake). Monitor triglyceride levels. Monitor blood lipids and LFTs at wkly or bi-wkly intervals. Monitor blood glucose in known or suspected DM patients. Genetic predisposition for age-related osteoporosis, history of childhood osteoporosis, osteomalacia or other bone metabolism disorders. Anorexia nervosa. History of psychiatric disorder. May impair night vision. Avoid wax epilation and skin resurfacing procedures for at least 6 mth. Avoid prolonged exposure to UV light or sunlight. Discontinue if hearing impairment, abdominal pain, rectal bleeding, severe diarrhoea or adverse ocular effects occur. Patient should not donate blood during therapy and for at least 1 mth following drug discontinuation.
Additive toxicity with vitamin A or its derivatives. Decreased efficacy of microdosed progesterone (use 2 forms of contraception). May increase risk of bone loss with phenytoin. May increase risk of osteoporosis with systemic corticosteroids. Reduces plasma levels of carbamazepine.
Potentially Fatal: Increased risk of pseudotumor cerebri with tetracyclines.
Avoid or limit ethanol intake. Avoid dong quai, St John's wort.
Adult: Initially, 0.5-1 mg/kg daily in 2 divided doses. Usual duration of treatment: 15-20 weeks; may be discontinued if number of cysts is reduced by >70% (whichever is sooner). Patients intolerant to initial dose: Continue treatment at a lower dose. Patients with very severe acne or acne evident on the body instead of face: Up to 2 mg/kg daily. There should be a 2-mth drug-free interval if a 2nd course is necessary.
Renal impairment: Dose reduction may be needed.
Hepatic impairment: Dose reduction may be needed.
Adult: As 0.05% gel: Apply sparingly once or twice daily. Effect may not be evident for 6-8 weeks.
Should be taken with food
Contraindicated in pregnancy
Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Contraindicated in lactation
Safety and efficacy not established in children younger than 12 years of age. Use with caution in children 12 to 17 years of age, especially in those with known metabolic or structural bone disease.
Clinical studies did not include sufficient numbers of subjects aged 65 years and older to determine whether they respond differently from younger subjects.
Store at 15-30°C (59-86°F)
Store below 25°C (77°F)
Store at 15-30°C (59-86°F)
Store below 25°C (77°F)