Alitretinoin

Name: Alitretinoin

Uses of Alitretinoin

Alitretinoin is a prescription medication used to treat skin lesions associated with Kaposi's sarcoma.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.
 

Alitretinoin Drug Class

Alitretinoin is part of the drug class:

  • Agents for dermatitis, excluding corticosteroids

Side Effects of Alitretinoin

Common side effects include the following:

  • warmth or slight stinging of the skin
  • lightening or darkening of the skin
  • red, scaling skin
  • rash
  • swelling, blistering, or crusting of the skin
  • pain at site of application
  • itching

This is not a complete list of this medication’s side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Alitretinoin Precautions

  • Do not apply gel on or near mucosal surfaces of the body such as eyes, nostrils, mouth, lips, vagina, tip of the penis, rectum or anus.
  • Do not use insect repellents containing DEET (N,N-diethyl-m-toluamide) or other products containing DEET while using this medication.
  • Product contains alcohol and should be kept away from open flame.
  • Do not use alitretinoin if you are pregnant or breastfeeding. Precautions should be taken to avoid becoming pregnant while taking alitretinoin. If you are pregnant, thinking of becoming pregnant, or breastfeeding, speak with your health care provider for more information.
  • Do not use if you are allergic to alitretinoin or any of its inactive ingredients.
  • Alitretinoin may make your skin sensitive to sunlight.
  • Topical alitretinoin gel does not treat lung or intestinal Kaposi's sarcoma.
  • Topical alitretinoin gel does not prevent the appearance of new KS lesions or the
  • increased growth of KS lesions not treated with alitretinoin gel.
  • Topical alitretinoin gel does not treat extremity swelling associated with KS. It is important to understand that KS lesions can appear and affect other parts of your body, including internal organs (e.g., lungs and intestines). You should regularly consult your health care provider about the status of your KS disease, especially if you note changes.

Alitretinoin Food Interactions

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of this medication, there are no specific foods that you must exclude from your diet.

Uses for Alitretinoin

AIDS-related Kaposi’s Sarcoma

Treatment of cutaneous lesions associated with AIDS-related Kaposi’s sarcoma.1 3 4 9 10 11 14 15 16 17 18

Not recommended for treatment of systemic AIDS-related Kaposi’s sarcoma, characterized by ≥10 new lesions in the prior month, symptomatic lymphedema, symptomatic pulmonary Kaposi’s sarcoma, or symptomatic visceral disease.1

No clinical experience to date in patients receiving systemic therapy for Kaposi’s sarcoma.1

Cautions for Alitretinoin

Contraindications

  • Known hypersensitivity to retinoids or any ingredient in the formulation.1

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenicity and embryotoxicity demonstrated in animals receiving oral alitretinoin.1 No reproduction studies in animals with topical alitretinoin.1 12

No adequate and well-controlled studies in humans.1 Avoid pregnancy during therapy.1 If used during pregnancy, apprise of potential hazard to the fetus.1

Sensitivity Reactions

Photosensitivity

Retinoids associated with photosensitivity; in vitro data indicate alitretinoin may have weak photosensitizing effect.1

Minimize exposure of treated areas to natural or artificial (e.g., sunlamps) sunlight.1

Major Toxicities

Dermatologic Effects

Possible severe local skin reactions (e.g., intense erythema, edema, vesiculation).1 Patients with cutaneous T-cell lymphoma exhibit less tolerance to these effects than those with Kaposi’s sarcoma.1

Specific Populations

Pregnancy

Category D.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Not known whether alitretinoin or its metabolites are distributed into milk; discontinue nursing due to risk in nursing infants.1

Pediatric Use

Safety and efficacy not established in children <18 years of age.1

Geriatric Use

Insufficient clinical experience in patients ≥65 years of age to determine whether they respond differently than younger adults.1

Common Adverse Effects

Rash,1 pruritus,1 exfoliative dermatitis,1 skin disorders (excoriation,1 cracking,1 scabbing,1 crusting,1 drainage,1 eschar,1 fissure,1 oozing1 ), pain,1 paresthesia,1 edema.1

Alitretinoin Pharmacokinetics

Absorption

Bioavailability

Not substantially absorbed systemically following topical application.1 9 17

Following repeated, multiple-daily-dose topical applications of alitretinoin (9-cis-retinoic acid) in patients with cutaneous lesions associated with Kaposi’s sarcoma, plasma concentrations of 9-cis-retinoic acid were similar to those of naturally occurring 9-cis-retinoic acid found in healthy untreated patients.1 9 17

Distribution

Extent

Not known whether alitretinoin or its metabolites are distributed into milk.1

Elimination

Metabolism

Alitretinoin metabolized to 4-hydroxy-9-cis-retinoic acid and 4-oxo-9-cis-retinoic acid by CYP2C9, CYP3A4, CYP1A1, and CYP1A2 in vitro; major circulating metabolite in vivo following oral alitretinoin is 4-oxo-9-cis-retinoic acid.1

Elimination Route

Principally by metabolism; no unchanged drug excreted in urine.b

Half-life

1.3–2.4 hours following oral administration.b

What should i avoid while using alitretinoin topical (panretin)?

Avoid prolonged exposure to sunlight. Alitretinoin topical may increase the sensitivity of the skin to sunlight. Use a sunscreen and wear protective clothing when exposure to the sun is unavoidable.

Do not use products that contain DEET (N, N-diethyl-m-toluamide), a common component of insect repellent products, while using alitretinoin topical. There is an increased risk of harmful effects from DEET when it is used with alitretinoin topical.

Do not cover the treated lesions with any type of occlusive dressing (a dressing that does not allow air to circulate to the area).

Precautions

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

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