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Alitretinoin (Topical)

Medically reviewed on August 12, 2018

Pronunciation

(a li TRET i noyn)

Index Terms

  • 9-cis-retinoic acid

Dosage Forms

Information with regard to form, strength, and availability of products uniquely available in Canada but currently not available in the US.

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

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

Absorption

Not extensive

Use: Labeled Indications

Kaposi sarcoma: Topical treatment of cutaneous lesions in AIDS-related Kaposi sarcoma.

Limitations of use: Alitretinoin is not indicated when systemic therapy is necessary (eg, >10 new Kaposi sarcoma lesions in previous month, symptomatic visceral involvement, symptomatic pulmonary Kaposi sarcoma, symptomatic lymphedema). There is no experience in using alitretinoin (topical) in combination with systemic treatment for Kaposi sarcoma.

Contraindications

Known hypersensitivity to alitretinoin, other retinoids, or any component of the formulation

Dosing: Adult

Kaposi sarcoma: Topical: Initial: Apply gel twice daily to cutaneous lesions; may gradually increase application frequency to 3 or 4 times daily based on lesion tolerance. Continue as long as deriving clinical benefit; response may be observed within 2 weeks of initiation, but typically a longer period is required (>14 weeks); 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

Application site irritation: May reduce the frequency of administration if application site toxicity occurs.

Grades 0, 1, or 2 dermal irritation: No dosage adjustment necessary (Walmsley 1999).

Grade 3 dermal irritation: Reduce dosing frequency to once daily (Bodsworth 2001) or reduce frequency or withhold treatment for up to 2 weeks and restart when irritation improves to grade 1 or lower (Walmsley 1999).

Grade 4 dermal irritation: Discontinue treatment until irritation improves to grade 1 or lower within 2 weeks and then restart at less than once daily for 2 weeks before increasing application frequency. If grade 4 irritation occurs less than once daily, do not restart treatment (Walmsley 1999).

Administration

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

Storage

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

Drug Interactions

Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Avoid combination

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

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

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

Progestins (Contraceptive): Retinoic Acid Derivatives may diminish the therapeutic effect of Progestins (Contraceptive). Retinoic Acid Derivatives may decrease the serum concentration of Progestins (Contraceptive). 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

Tetracyclines: 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:

• Dermal irritation: Application site irritation and pain have been reported, including grade 3 dermal irritation; may require dosage reduction.

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

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Other warnings/precautions:

• Products containing DEET: Do not use concurrently with topical products containing DEET (eg, insect repellant); an increase in DEET toxicity has been observed.

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 female who is pregnant. Females of reproductive 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.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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