Skip to Content

Alitretinoin (Topical)

Pronunciation

(a li TRET i noyn)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Gel, External:

Panretin: 0.1% (60 g)

Brand Names: U.S.

  • Panretin

Pharmacologic Category

  • Antineoplastic Agent, Retinoic Acid Derivative

Pharmacology

Naturally occurring endogenous retinoid that binds to and activates intracellular retinoid receptors (RAR and RXR); this results in altered expression of the genes controlling cellular differentiation and proliferation in normal and neoplastic cells, inhibiting the growth of Kaposi’s sarcoma

Absorption

Not extensive

Use: Labeled Indications

Topical treatment of cutaneous lesions in AIDS-related Kaposi's sarcoma. Not indicated when systemic therapy is necessary (eg, >10 new lesions in previous month, symptomatic visceral involvement, symptomatic pulmonary Kaposi’s sarcoma, symptomatic lymphedema)

Contraindications

Hypersensitivity to alitretinoin, other retinoids, or any component of the formulation

Dosing: Adult

Kaposi's sarcoma: Topical: Initial: Apply gel twice daily to cutaneous lesions; may gradually increase application frequency to 3-4 times daily based on lesion tolerance. Response may be observed within 2 weeks of initiation, but typically a longer period is required (some patients have required >14 weeks). Continue therapy for as long as patients derives benefit (in clinical trials, therapy lasted up to 96 weeks).

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer's labeling; however, systemic absorption is not extensive making the need for a dose adjustment appear unlikely.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer's labeling; however, systemic absorption is not extensive making the need for a dose adjustment appear unlikely.

Dosing: Adjustment for Toxicity

Reduce application frequency for application site toxicity; for severe reactions, temporarily discontinue therapy until symptoms resolve.

Administration

Apply sufficient gel to cover lesion(s) with a generous coating; allow gel to dry 3-5 minutes after application before covering with clothing. Do not use occlusive dressings. Avoid applying gel to normal skin surrounding lesions. Do not apply to any lesions on or near mucosal surfaces.

Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).

Storage

Store at 25°C (77°F); excursions permitted between 15°C to 30°C (59°F to 86°F).

Drug Interactions

Aminolevulinic Acid: Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid. Monitor therapy

Contraceptives (Estrogens): Retinoic Acid Derivatives may diminish the therapeutic effect of Contraceptives (Estrogens). Two forms of contraception are recommended in females of child-bearing potential during retinoic acid derivative therapy. Monitor therapy

Contraceptives (Progestins): Retinoic Acid Derivatives may diminish the therapeutic effect of Contraceptives (Progestins). Retinoic Acid Derivatives may decrease the serum concentration of Contraceptives (Progestins). Management: Two forms of effective contraception should be used in patients receiving retinoic acid derivatives. Particularly, microdosed progesterone-only preparations may be inadequately effective. Consider therapy modification

Multivitamins/Fluoride (with ADE): May enhance the adverse/toxic effect of Retinoic Acid Derivatives. Avoid combination

Multivitamins/Minerals (with ADEK, Folate, Iron): May enhance the adverse/toxic effect of Retinoic Acid Derivatives. Avoid combination

Multivitamins/Minerals (with AE, No Iron): May enhance the adverse/toxic effect of Retinoic Acid Derivatives. Avoid combination

Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy

Tetracycline Derivatives: May enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Avoid combination

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy

Adverse Reactions

>10%:

Central nervous system: Pain (≤34%), paresthesia (3% to 22%)

Dermatologic: Skin rash (25% to 77%), pruritus (8% to 11%)

1% to 10%:

Cardiovascular: Edema (3% to 8%)

Dermatologic: Exfoliative dermatitis (3% to 9%), dermatological disease (≤8%)

Warnings/Precautions

Concerns related to adverse effects:

• Photosensitivity: May be photosensitizing (based on experience with other retinoids); minimize sun or other UV exposure of treated areas.

Concurrent drug therapy issues:

• Products containing DEET: Do not use concurrently with topical products containing DEET (eg, insect repellant).

Special populations:

• Pregnancy: May cause fetal harm if significant absorption occurs in a woman who is pregnant.

Special handling:

• Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).

Pregnancy Risk Factor

D

Pregnancy Considerations

Adverse events were observed in animal reproduction studies using an oral preparation; studies have not been conducted using the topical product. Alitretinoin may cause fetal harm if significant absorption occurs in a woman who is pregnant. Women of childbearing potential should avoid becoming pregnant.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Have patient report immediately to prescriber burning or numbness feeling, edema, or severe skin irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

Hide