Alitretinoin: Dose, Frequency, ROA, MOA, PK, PD, Usage & More

Alitretinoin is a retinoid derivative used in the treatment of severe chronic hand eczema (CHE) that has not responded to topical corticosteroids. It belongs to the class of medications known as retinoids, which are derivatives of vitamin A. Alitretinoin works by regulating epidermal cell proliferation and differentiation, reducing inflammation, and promoting skin healing.

Recommended Dose and Dosage Regimen

The recommended dose of alitretinoin for the treatment of severe chronic hand eczema is typically 30 milligrams (mg) administered once daily with food. Treatment duration may vary depending on individual patient response and the severity of the condition. Patients should adhere to the prescribed dosing regimen and follow up with their healthcare provider regularly to assess treatment efficacy and safety.

Frequency of Administration

Alitretinoin is administered orally once daily with food to maximize absorption and reduce the risk of gastrointestinal side effects. The dosing frequency is fixed, and doses should be taken at the same time each day to maintain consistent drug levels in the bloodstream. Patients should avoid missing doses and contact their healthcare provider if they have any questions or concerns about adherence to the dosing schedule.

Route of Administration

Alitretinoin is administered orally as capsules, which should be swallowed whole with a full glass of water to facilitate proper absorption. The capsules should not be chewed, crushed, or opened, as this may affect the drug’s efficacy and increase the risk of adverse effects. Alitretinoin capsules are available in various strengths, and patients should follow their healthcare provider’s instructions regarding the prescribed dosage.

Mechanism of Action (MOA)

The exact mechanism of action of alitretinoin in the treatment of severe chronic hand eczema is not fully understood. However, it is believed to exert its therapeutic effects by binding to and activating retinoic acid receptors (RARs) and retinoid X receptors (RXRs) in the skin. This leads to the regulation of gene expression involved in epidermal differentiation, keratinization, and inflammation, ultimately promoting skin repair and reducing eczematous lesions.

Pharmacokinetics (PK)

Following oral administration, alitretinoin is well absorbed from the gastrointestinal tract, with peak plasma concentrations reached within 2 to 4 hours. It undergoes extensive metabolism in the liver via cytochrome P450 enzymes, primarily CYP2C9 and CYP3A4, to form pharmacologically active metabolites. The elimination half-life of alitretinoin and its metabolites is approximately 9 to 40 hours. Dosage adjustments may be necessary in patients with hepatic impairment or concomitant use of medications that affect its metabolism.

Pharmacodynamics (PD)

The pharmacodynamic effects of alitretinoin in the treatment of severe chronic hand eczema include the normalization of epidermal differentiation and keratinization, reduction of inflammatory cytokines, and inhibition of immune-mediated responses. Alitretinoin promotes the resolution of eczematous lesions, reduces pruritus, and improves overall skin barrier function. The onset of therapeutic effects may vary among individuals, with noticeable improvement typically observed within weeks to months of treatment initiation.

Primary Indications

Alitretinoin is indicated for the treatment of severe chronic hand eczema (CHE) in adult patients who have not responded to topical corticosteroids or for whom these treatments are not suitable. Severe CHE is characterized by persistent, disabling hand eczema that significantly impairs daily functioning and quality of life. Alitretinoin is considered a second-line therapy for severe CHE and should be initiated under the supervision of a dermatologist or healthcare provider experienced in managing dermatological conditions.

Contraindications

Alitretinoin is contraindicated in pregnant women due to the risk of teratogenicity and fetal harm. It is also contraindicated in patients with a known hypersensitivity to retinoids or any component of the formulation. Alitretinoin should not be used in patients with severe hepatic impairment or pre-existing hyperlipidemia. Female patients of childbearing potential should undergo pregnancy testing before starting alitretinoin therapy and use effective contraception during treatment and for at least one month after discontinuation.

Purpose of Taking Medication

The primary purpose of taking alitretinoin is to alleviate the symptoms of severe chronic hand eczema (CHE) and improve the quality of life in affected patients. Alitretinoin promotes skin healing, reduces inflammation, and restores the integrity of the skin barrier, leading to resolution of eczematous lesions and relief of pruritus. Treatment with alitretinoin may help patients regain functional use of their hands and improve psychosocial well-being.

Usage Instructions

Patients should take alitretinoin capsules orally once daily with food to enhance absorption and minimize gastrointestinal side effects. The capsules should be swallowed whole and not chewed, crushed, or opened. Patients should adhere to the prescribed dosing regimen and follow up with their healthcare provider regularly for monitoring of treatment efficacy and safety. It is essential to avoid exposure to sunlight and ultraviolet (UV) light during alitretinoin therapy, as this may increase the risk of photosensitivity reactions.

Precautions and Care

Patients receiving alitretinoin should be monitored regularly for signs of adverse effects, including elevated serum lipids, hepatic dysfunction, and teratogenicity. Female patients of childbearing potential should undergo pregnancy testing before starting treatment and use effective contraception throughout therapy. Patients should avoid excessive alcohol consumption, as it may exacerbate the risk of hepatotoxicity. Healthcare providers should counsel patients on the importance of sun protection and skin moisturization during alitretinoin therapy.

Dietary Considerations

There are no specific dietary restrictions associated with alitretinoin therapy. However, patients are encouraged to maintain a balanced diet rich in fruits, vegetables, and whole grains to support overall health and well-being. Patients should stay well-hydrated and avoid excessive intake of vitamin A supplements, as this may increase the risk of vitamin A toxicity when combined with alitretinoin.

Possible Side Effects

Common side effects of alitretinoin may include headache, nausea, fatigue, dry skin, and mucocutaneous dryness. Other adverse effects may include elevated serum triglycerides, liver enzyme abnormalities, and musculoskeletal symptoms. Serious adverse reactions, such as hepatotoxicity, pancreatitis, depression, and pseudotumor cerebri, may occur rarely. Patients should report any new or worsening symptoms to their healthcare provider promptly.

Storage and Disposal

Alitretinoin capsules should be stored at room temperature (20°C to 25°C; 68°F to 77°F) in a dry place away from moisture and heat. Keep the medication out of reach of children and pets. Unused medication and expired capsules should be disposed of properly according to local regulations or guidelines for pharmaceutical waste disposal.

Conclusion

Alitretinoin is an oral retinoid medication indicated for the treatment of severe chronic hand eczema (CHE) in adult patients who have not responded to topical corticosteroids. By regulating epidermal cell proliferation and differentiation, reducing inflammation, and promoting skin healing, alitretinoin helps alleviate the symptoms of severe CHE and improve the quality of life in affected individuals. Healthcare providers should educate patients about the proper use of alitretinoin and monitor them regularly for adverse effects to ensure safe and effective treatment outcomes.

Important Note: Always consult with a healthcare professional for personalized medical advice and guidance regarding the use of given drug, especially regarding dosing, administration, and potential side effects. Your healthcare provider can provide tailored recommendations based on your individual medical history, current medications, and specific treatment needs. Never self-adjust your given drug regimen or discontinue treatment without first consulting your healthcare provider. If you have any questions or concerns about given drug or its use, talk to your doctor or pharmacist for further information and assistance.