No

Immunosuppressant Agent

Treatment of erythema nodosum leprosum

Investigational: Treatment or prevention of graft-versus-host reactions after bone marrow transplantation; in aphthous ulceration in HIV-positive patients; Langerhans cell histiocytosis, Behçet's syndrome; hypnotic agent; also may be effective in rheumatoid arthritis, discoid lupus, and erythema multiforme; useful in type 2 lepra reactions, but not type 1; can assist in healing mouth ulcers in AIDS patients; Crohn's disease, renal cell carcinoma, multiple myeloma, myeloma, Waldenström's macroglobulinemia

Thalidomide is approved for marketing only under a special distribution program. This program, called the "System for Thalidomide Education and Prescribing Safety" (STEPS), has been approved by the FDA. Prescribing and dispensing of thalidomide is restricted to prescribers and pharmacists registered with the program.

X

Embryotoxic with limb defects noted from the 27th to 40th gestational day of exposure; all cases of phocomelia occur from the 27th to 42nd gestational day; fetal cardiac, gastrointestinal, and genitourinary tract abnormalities have also been described

Pregnancy or women in childbearing years, neuropathy (peripheral), thalidomide hypersensitivity

Liver, hepatic, neurological disorders, constipation, congestive heart failure, hypertension

Percentage unknown: Tachycardia, sinus tachycardia, dizziness, headache, irritability, lethargy, fever, edema, alopecia, pruritus, amenorrhea, sexual dysfunction, nausea, vomiting, xerostomia, constipation, leukopenia, sensory neuropathy (peripheral) (after prolonged therapy due to neuronal degeneration), clonus, myoclonus

Other medications known to cause peripheral neuropathy should be used with caution in patients receiving thalidomide; thalidomide may enhance the sedative activity of other drugs such as ethanol, barbiturates, reserpine, and chlorpromazine

A derivative of glutethimide; mode of action for immunosuppression is unclear; inhibition of neutrophil chemotaxis and decreased monocyte phagocytosis may occur; may cause 50% to 80% reduction of tumor necrosis factor - alpha

Distribution: V_d: 120 L

Metabolism: Hepatic

Half-life: 8.7 hours

Peak plasma levels: 2-6 hours

Leprosy: Up to 400 mg/day; usual maintenance dose: 50-100 mg/day

Behçet's syndrome: 100-400 mg/day

Graft-vs-host reactions:

Children: 3 mg/kg 4 times/day

Adults: 100-1600 mg/day; usual initial dose: 200 mg 4 times/day for use up to 700 days

AIDS-related aphthous stomatitis: 200 mg twice daily for 5 days, then 200 mg/day for up to 8 weeks

Discoid lupus erythematosus: 100-400 mg/day; maintenance dose: 25-50 mg

Therapeutic plasma thalidomide levels in graft-vs-host reactions are 5-8 mg/mL, although it has been suggested that lower plasma levels (0.5-1.5 mg/mL) may be therapeutic; peak serum thalidomide level after a 200 mg dose: 1.2 mg/mL

Sedation is common; may cause dizziness, nervousness, insomnia or agitation

May cause leukopenia; use caution with clozapine and carbamazepine; concurrent use with other psychotropics may produce additive sedation

No information available to require special precautions

1% to 10% of patients may experience moniliasis, tooth pain; in HIV-seropositive patients, oral moniliasis was seen in 6.3% to 11.1% of patients; aphthous stomatitis has been reported

You will be given oral and written instructions about the necessity of using two methods of contraception and and the necessity of keeping return visits for pregnancy testing. You may experience sleepiness, dizziness, lack of concentration (use caution when driving, climbing stairs, or engaging in tasks requiring alertness until response to drug is known); nausea or vomiting or loss of appetite (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); constipation or diarrhea; oral thrush (frequent mouth care is necessary); sexual dysfunction (reversible). Report any of the above if persistent or severe. Report chest pain or palpitations or swelling of extremities; back, neck, or muscle pain or stiffness; skin rash or eruptions; increased nervousness, anxiety, or insomnia; or any other symptom of adverse reactions. Pregnancy/breast-feeding precautions: Do not get pregnant. Breast-feeding is not recommended.

Capsule: 50 mg (boxes contain 6 prescription packs of 14 capsules each)

Beckman DA and Brent RL, "Mechanism of Known Environmental Teratogens: Drugs and Chemicals," Clin Perinatol, 1986, 13(3):649-87.

Gunzler V, "Thalidomide in Human Immunodeficiency Virus (HIV) Patients. A Review of Safety Considerations," Drug Saf, 1992, 7(2):116-34.

Hamuryudan V, Mat C, Saip S, et al, "Thalidomide in the Treatment of the Mucocutaneous Lesions of the Behçet Syndrome. A Randomized, Double-Blind, Placebo-Controlled Trial," Ann Intern Med, 1998, 128(6):443-50.

Jacobson JM, Greenspan JS, Spritzler J, et al, "Thalidomide for the Treatment of Oral Aphthous Ulcers in Patients With Human Immunodeficiency Virus Infection. National Institute of Allergy and Infectious Diseases AIDS Clinical Trials Group," N Engl J Med, 1997, 336(21):1487-93.

Schuler U and Ehninger G, "Thalidomide: Rationale for Renewed Use in Immunological Disorders," Drug Saf, 1995, 12(6):364-9.

"Thalidomide," Med Lett Drugs Ther, 1998, 40(1038):103-4.