bexarotene

Contraindicated in:

Hypersensitivity;
Concurrent use of gemfibrozil;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Hepatic impairment;
Renal impairment;
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may be more sensitive to drug effects.

Adv. Reactions/Side Effects ⬆ ⬇

Oral

CV: peripheral edema

Derm: dry skin, rash, alopecia, exfoliative dermatitis, photosensitivity

EENT: new/worsening cataracts

Endo: hyperlipidemia, hypothyroidism, hypercholesterolemia

GI: abdominal pain, nausea, ↑liver enzymes, anorexia, diarrhea, PANCREATITIS, vomiting

Hemat: anemia, leukopenia

Neuro: headache, weakness, insomnia

Misc: flu-like syndrome

Topical

CV: edema

Derm: pruritus, skin disorder, rash

Endo: hyperlipidemia

Hemat: leukopenia

Misc: lymphadenopathy

Interactions ⬆ ⬇

Drug-drug:

Interactions are noted for oral use, but may occur with topical use especially with high dose/prolonged treatment.
↑levels and risk of toxicity with gemfibrozil; concurrent use not recommended.
Combination regimen of paclitaxel and carboplatin↑ levels.
May ↓ levels and effectiveness of CYP3A4 substrates, including atorvastatin, tamoxifen, paclitaxel, and hormonal contraceptives.
Vitamin A may ↑ risk of toxicity (limit supplementation to <15,000 units/day).
Concurrent use of insulin, sulfonylureas, or thiazolidinediones in patients with may ↑ risk of hypoglycemia.
Topical: Concurrent use with DEET (N,N-diethyl-m-toluamide)-containing insect repellents may ↑ risk of DEET toxicity and should be avoided.

Availability ⬆ ⬇

(Generic available)

Capsules: 75 mg
Topical gel: 1% (contains dehydrated alcohol and propylene glycol)

Route/Dosage ⬆ ⬇

PO (Adults ): 300 mg/m² once daily; dosage to be adjusted based on tolerance/toxicity.
(Adults ): Apply once every other day for 1 wk; increase at weekly interval to once daily, then twice daily, then 3 times daily, and finally 4 times daily as tolerated; continued as long as benefit is derived.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Binds and inactivates selected retinoid X receptors that are ultimately responsible for cellular differentiation and proliferation. Inhibits growth of some tumor cell lines including lines of hematopoietic and squamous cell origin.

Therapeutic effects:

Decreased spread of cutaneous T-cell lymphoma.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: retinoids

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration; absorption is enhance by a fat-containing meal. Some systemic absorption follows topical application.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Mostly metabolized by the liver, mainly by the CYP3A4 isoenzyme; some metabolites may be pharmacologically active. Excreted almost entirely via hepatobiliary elimination;, <1% excreted in urine.

Half-Life: 7 hr.

Time/Action Profile ⬆ ⬇

(improvement in lesions)

ROUTE	ONSET	PEAK	DURATION
PO, Top	within 4 wk‡	unknown	unknown

‡Some responses took longer.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take or apply bexarotene as directed. Take missed doses as soon as remembered unless close to time for next dose; do not double doses.
Advise patient to avoid touching broken or leaking capsules and notify pharmacist. If contents get on skin, immediately wash area with soap and water and notify health care professional. Do not use capsules after expiration date.
Advise patient to notify health care professional immediately if signs and symptoms of pancreatitis (persistent nausea, vomiting, and abdominal or back pain) occur.
Caution patient to wear protective clothing and avoid sunlight and artificial ultraviolet light to prevent photosensitivity reactions.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially vitamin A.
Rep: May cause fetal harm. Pregnancy tests will be taken before starting and monthly during therapy. Effective contraception must be used 1 mo before beginning therapy, during, and 1 mo following therapy. Two forms of contraception are recommended, with at least 1 being condom, diaphragm, cervical cap, IUD, or spermacide. Patients should not breastfeed during therapy. Male patients whose partner is pregnant or capable of becoming pregnant must use a condom during and for at least 1 mo after completion of therapy and should discuss precautions with health care professional.
Explain need for regular blood tests to patient.
Topical Advise patient to avoid showering, bathing, or swimming for at least 3 hr after application. Avoid insect repellent containing DEET or other products containing DEET during therapy. Keep gel away from flame; contains alcohol.
Inform patient that redness, itching, burning, irritation, and scaling at application area may occur; notify health care professional if they become troublesome.

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Indications ⬇

Contraind./Precautions ⬆ ⬇