isotretinoin

Action and Spectrum

Actions and Spectrum: 

isotretinoin is a medication used primarily for the treatment of severe nodular acne. Its actions and spectrum include: 

• Anti-inflammatory action: isotretinoin reduces the inflammation associated with severe acne by suppressing the production of inflammatory cytokines. 
• Anti-seborrheic action: isotretinoin decreases sebum production, a natural oil produced by the sebaceous glands in the skin, which can contribute to developing acne. 
• Keratolytic action: isotretinoin promotes the shedding of dead skin cells and the formation of new skin cells, which can help to prevent the formation of comedones (blackheads and whiteheads). 
• Spectrum: It treats other skin disorders, such as rosacea and keratosis pilaris. 

Drug Interaction

Adverse Reaction

Frequency Defined 

>10% 

Cheilitis  

Xerostomia 

Xerosis 

Dry nose 

Conjunctivitis 

Thinning of hair  

Epistaxis 

Pruritus 

Palmoplantar desquamation 

Rash  

Hypertriglyceridemia  

Bone or joint pain 

 Skin fragility 

Skin infections  

Decreased HDLs  

Increased LFTs  

Generalized muscle ache 

Arthralgia 

Increased CPK  

1-10% 

Premature closure of epiphysis  

Decreased bone mineral density  

Frequency not Defined 

Lethargy 

Vomiting 

Headache 

Fatigue 

Nausea 

Anorexia 

Thirst  

Increased appetite 

Black Box Warning

Black Box Warning: 

isotretinoin is entirely unsafe for pregnant females. It causes embryofetal toxicity in them. 

A high rate of congenital disabilities is also seen.  

Contraindication / Caution

Contraindication/Caution: 

isotretinoin is a powerful medication that is associated with several contraindications and precautions, including: 

• Pregnancy: isotretinoin is contraindicated because it can cause severe congenital disabilities. Women of childbearing age must use highly effective contraception for at least one month before starting isotretinoin and at least one month after stopping treatment. 
• Liver disease: isotretinoin can cause liver damage, so it should not be used in patients with severe liver disease or abnormal liver function tests. 
• High blood lipid levels: isotretinoin can increase blood lipid levels, leading to pancreatitis. Patients with pre-existing high blood lipid levels should be monitored closely during the treatment. 
• Hypersensitivity: isotretinoin should not be used in patients with a known hypersensitivity to the medication or its components. 
• Depression: isotretinoin has been associated with an increased risk of depression and suicidal ideation. Patients with a history of depression or other psychiatric disorders should be closely monitored during treatment. 
• Children: isotretinoin is not recommended for use in children under the age of 12 years. 
• Other medications: isotretinoin can interact with other medications, including vitamin A supplements, tetracycline antibiotics, and corticosteroids. Patients should inform their healthcare provider of all medications before starting isotretinoin. 

Pregnancy / Lactation

Pregnancy consideration:  

isotretinoin is not allowed during pregnancy. 

Breastfeeding warnings:  

Do not breastfeed 8 days before the last dose of isotretinoin. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

isotretinoin is a retinoid, which is a derivative of vitamin A. It works by regulating the growth and differentiation of skin cells, decreasing the production of sebum (oil) from sebaceous glands, and reducing inflammation in the skin.  

isotretinoin: 

• Inhibits sebaceous gland activity: isotretinoin reduces the size and activity of the sebaceous glands, which leads to a decrease in the production of sebum. This helps to prevent the formation of comedones (blackheads and whiteheads) and acne lesions. 
• Reduces inflammation: isotretinoin suppresses the production of inflammatory cytokines, which helps to reduce the inflammation associated with severe acne. 
• Modifies keratinization: isotretinoin promotes normal keratinization (the process of skin cell turnover and shedding) and helps to prevent the formation of abnormal keratin plugs that can contribute to acne. 
• Alters gene expression: isotretinoin has been shown to alter gene expression in cell differentiation, proliferation, and apoptosis (cell death). These changes can help to improve acne symptoms. 

Adminstartion

Administration: 

isotretinoin is administered as capsules or tablets. The medication should be taken with food to improve absorption and reduce the risk of gastrointestinal side effects. 

The recommended dose of isotretinoin varies depending on the patient’s weight and the severity of their acne. Typically, patients start with a low dose and gradually increase the dose over several weeks to reach the target dose. The duration of treatment is usually 4-6 months. 

It is essential to take isotretinoin precisely as prescribed by the healthcare provider. Patients should not take more or less of the medication than prescribed or stop taking it without consulting their healthcare provider. 

Patients should avoid taking vitamin A supplements during treatment with isotretinoin, as this can increase the risk of toxicity. Patients should also avoid donating blood during treatment and at least one month after stopping treatment, as the medication can cause congenital disabilities. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: isotretinoin 

Pronounced: i-so-tre-tin-oin 

Why do we use isotretinoin? 

isotretinoin is considered a “last resort” treatment for severe acne due to its powerful effects and potential side effects. 

isotretinoin is effective in treating acne because it addresses several underlying causes of the condition, including: 

• Excess sebum production: isotretinoin reduces the production of sebum, which can contribute to the formation of acne. 
• Abnormal skin cell turnover: isotretinoin helps promote average skin cell turnover, preventing the formation of comedones (blackheads and whiteheads) and acne lesions. 
• Inflammation: isotretinoin has anti-inflammatory properties, which can reduce the inflammation associated with severe acne. 

In addition to treating severe acne, isotretinoin is also used in treating other skin disorders, such as rosacea and keratosis pilaris.