drug-information.ru

|Alitretinoin

Alitretinoin

Trade Names:
Panretin
- Gel 0.1%

Mechanism of Action

Pharmacology

Binds to and activates all known intracellular retinoid receptor substrates. Once activated, these receptors function as transcription factors that regulate the expression of genes that control the process of cellular differentiation and proliferation of both normal and neoplastic cells.

Pharmacokinetics

Absorption

Indirect evidence indicates that absorption is not extensive. Plasma levels are similar to circulating, naturally occurring 9-cis-retinoic acid levels.

Indications and Usage

Topical treatment of cutaneous lesions of AIDS-related Kaposi sarcoma (KS).

Contraindications

Hypersensitivity to retinoids or any component of the product.

Dosage and Administration

Topical Start with twice-daily application to KS lesions. Application can be gradually increased to 3 or 4 times daily or reduced according to individual lesion tolerance or application site toxicity. If severe irritation occurs, application of drug can be temporarily stopped for a few days until symptoms subside. Apply a sufficient amount of gel to cover the lesion with a generous coating. Allow to dry for 3 to 5 min before covering with clothing. A response to KS lesions may be seen as soon as 2 wk; however, some patients have required over 14 wk.

General Advice

• Do not apply gel on or near mucosal surfaces or on healthy skin surrounding lesion(s).
• Do not allow patient to shower, bathe, or swim for at least 3 h following application of gel.
• Do not cover with occlusive dressings.

Storage/Stability

Store gel at controlled room temperature (59° to 86°F). Keep tube tightly capped.

Drug Interactions

Avoid concurrent use of products containing DEET (a common component of insect repellents).

Laboratory Test Interactions

None well documented.

Adverse Reactions

Dermatologic

Rash (77%); pain (34%); pruritus (11%); exfoliative dermatitis (9%); edema, skin disorder (including excoriation, cracking, scab, crusting, drainage, eschar, fissure, oozing [8%]); paresthesia (3%).

Precautions

Pregnancy

Category D . Could cause fetal harm if absorption were to occur in pregnant women.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Photosensitivity

May occur with this class of agent; avoid excessive sunlight and ultraviolet light.

Coadministration of topical products

Do not apply other topical products unless advised by health care provider. Assess the skin and identify areas where medication is to be applied and areas that should be avoided (eg, healthy skin).

Systemic

Do not use gel on patient who requires systemic anti-KS therapy (eg, more than 10 new KS lesions in prior month, symptomatic pulmonary KS, symptomatic visceral involvement).

Patient Information

• Advise patient that gel will not work immediately but to expect a slow improvement over several wk.
• Advise patient to apply gel to skin lesion(s) 2 to 4 times daily as directed by health care provider.
• Caution patient not to apply gel on or near mucosal surfaces (eg, eyes, nostrils, mouth, lips, vagina, tip of penis, rectum, anus) or on healthy skin surrounding lesion(s).
• Caution patient that gel contains alcohol and is flammable and to keep away from open flame.
• Teach patient or caregiver proper technique for applying gel: wash hands; apply sufficient gel to generously coat lesion(s); wash hands after applying gel; allow gel to dry for 3 to 5 min before covering with clothing.
• Caution patient not to scratch or cover treated areas with bandages, dressings, or wraps and not to swim, bathe, or shower for at least 3 h after application.
• Advise patient not to stop treatment after lesion(s) have improved and that daily application of gel will be required to maintain the improvement.
• Advise patient that application site reactions occur commonly and to notify health care provider if swelling, blistering, oozing, drainage, pain, or intense redness or itching occurs.
• Advise patient that medication does not prevent the appearance of new KS lesions or increased growth of KS lesions not being treated, nor does the medication treat lung or intestinal KS.
• Instruct patient to avoid use of other topical products on treated lesion(s) except for mineral oil, which may be used 2 h before or after alitretinoin applications to help prevent excessive dryness and itching.
• Advise patient that if gel comes in contact with the eyes to wash eyes with large amounts of cool water and to contact health care provider if eye irritation persists.
• Advise patient to talk to health care provider before using any other topical agents (eg, medicated soaps, astringents, cosmetics) on treated skin.
• Caution patient that medication can increase sensitivity to ultraviolet light and to avoid use of sun lamps and unnecessary exposure to sunlight while undergoing treatment.
• Caution patient not to use insect repellants containing DEET while using alitretinoin. Advise patient that toxicity from DEET may occur if applied together.
• Advise patient that follow-up visits to monitor KS disease will be necessary and to keep appointments.