ThalidomideRx

Trade Names: Thalomid

Drug Class: Immunomodulator

Preparations: Capsule: 50-, 100-, 150-, 200 mg

Dose: 100–300 mg daily in divided doses; must only be administered in compliance with the REMS program

Indications: Erythema nodosum leprosum, myeloma, small, mostly uncontrolled reports have suggested possible benefit in severe recurrent refractory apthous stomatitis including ulcers associated with HIV and Behçet’s disease, and pyoderma gangrenosum and other refractory dermatological conditions

Mechanism of Action: Unknown; may inhibit angiogenesis and TNF

Contraindications: Pregnancy, hypersensitivity to thalidomide, childbearing potential and noncompliance with contraception, neutropenia

Precautions: May only be prescribed by physicians registered in the Thalidomid REMS  program (formerly System for Thalidomide Education and Prescribing Safety (STEPS) program (see www.celgeneriskmanagement.com). If possible, avoid in women of childbearing potential; if not possible, ensure contraception for 4 weeks before and 4 weeks after therapy and a negative pregnancy test within 10-14 days and again within 24 hours of beginning treatment.

Monitoring: Monthly pregnancy tests, monthly assessment for peripheral neuropathy for 3  months and  then periodically, consider electrophysiologic testing to monitor for neuropathy, monitor CBC periodically

Pregnancy Risk: X, highly teratogenic

Adverse Effects
Common: Peripheral neuropathy that may be permanent; this can occur after short-term use. Postural hypotension, dizziness, sleepiness. If used during pregnancy, causes birth defects such as phocomelia
Less common: Neutropenia, hypersensitivity including Stevens-Johnson syndrome, seizures, edema, rash, deep vein thrombosis, bradycardia, myocardial infarction and stroke

Drug Interactions: Increased sedation with sedatives and increased risk of bradycardia and peripheral neuropathy with drugs that cause those

Patient Instructions: Do not share the medication. Use two forms of contraception if a women and a latex condom if a man. This drug causes birth defects; do not become pregnant. Report changes in sensation in your hands and feet. Can cause sleepiness and dizziness on standing. Do not donate blood or sperm. Increased risk of blood  clots.

Comments: Has limited potential for long-term use owing to frequent side effects, teratogenicity, lack of proven efficacy in rheumatic diseases, and the relapse of disease after discontinuation. Strategies to prevent fetal exposure to thalidomide are outlined in the REMS  program; can only be prescribed by program-approved physicians.

Clinical Pharmacology: Peak concentrations at 4 hours; elimination half-life is 5 hours, largely through nonenzymatic hydrolysis

Cost: $$$$$

BIBLIOGRAPHY

Hello M, Barbarot S, Bastuji-Garin S, Revuz J, Chosidow O. Use of thalidomide for severe recurrent aphthous stomatitis: a multicenter cohort analysis. Medicine 2010;89:176-82.PMID: 20453604.