ACOTIN 10 CAPSULES (Each soft gel contains Isotrelinum 10 mg)

Indications

• Severe acne vulgaris
• Nodular acne
• Acne conglobata
• Acne fulminans

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations based on age and weight.

Adults: Refer to the relevant prescribing guidelines for specific dosing information based on individual patient circumstances.

Mechanism of action

Isotretinoin exerts its effects by binding to retinoic acid receptors (RARs) and retinoid X receptors (RXRs), which are nuclear receptors that regulate gene expression. This binding leads to altered transcription of genes involved in cell growth, differentiation, and apoptosis. Isotretinoin decreases the size and activity of sebaceous glands, reduces sebum production, and promotes the turnover of epithelial cells in the hair follicles, preventing the clogging that leads to acne formation.

Pharmacodynamics

Isotretinoin has a profound effect on the skin and sebaceous glands. It reduces the size of sebaceous glands and the volume of sebum they produce, leading to a decrease in the number of acne lesions. The drug also exhibits anti-inflammatory effects, which help decrease the redness and swelling associated with acne. Furthermore, it alters keratinization, promoting normal skin cell turnover and preventing clogged pores.

Pharmacokinetics

Isotretinoin is well absorbed from the gastrointestinal tract, with peak plasma concentrations typically occurring 1-4 hours after oral administration. It is highly lipophilic and is extensively bound to plasma proteins. The drug undergoes hepatic metabolism, primarily via cytochrome P450 enzymes, and is converted to its active metabolites, including 4-oxo-isotretinoin. The elimination half-life of isotretinoin is approximately 10-20 hours, and it is primarily excreted in urine as metabolites.

Contra-indications

• Hypersensitivity to isotretionin or any excipients
• Pregnancy
• Severe hepatic impairment
• Hypervitaminosis A
• Concurrent use of tetracyclines

Adverse effects

• Dry skin
• Chapped lips
• Nosebleeds
• Headaches
• Muscle and joint pain
• Increased liver enzymes
• Elevated triglycerides
• Mood changes
• Visual disturbances

Interactions

• Tetracyclines - increased risk of intracranial hypertension
• Vitamin A supplements - risk of hypervitaminosis A
• St. John's Wort - potential for reduced efficacy of isotretionin

Precautions

• Regular monitoring of liver function tests and lipid levels
• Use caution in patients with a history of mental health disorders
• Avoid concurrent use of other retinoids
• Patients should be advised to avoid sun exposure and use sunscreen

Pregnancy

Isotretionin is highly teratogenic. It is contraindicated in pregnancy due to the risk of severe birth defects.

Breast-feeding

Isotretionin is contraindicated during breastfeeding as it may be excreted in breast milk and could harm the nursing infant.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Capsules
• Topical gel
• Topical cream