Thalidomide
- Atc Codes:L04AX02
- CAS Codes:50-35-1
- PHARMGKB ID:50-35-1
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Thalidomide; Cyprus: Thalidomide; Czech Republic: Thalidomide; Denmark: Thalidomide; Estonia: Thalidomide; Finland: Thalidomide; France: Thalidomide; Germany: Thalidomide; Greece: Thalidomide; Hungary: Thalidomide; Ireland: Thalidomide; Italy: Thalidomide; Latvia: Thalidomide; Lithuania: Thalidomide; Luxembourg: Thalidomide; Malta: Thalidomide; Netherlands: Thalidomide; Poland: Thalidomide; Portugal: Thalidomide; Romania: Thalidomide; Slovakia: Thalidomide; Slovenia: Thalidomide; Sweden: Thalidomide; UK: Thalidomide.
North America
USA: Thalomid.
Latin America
Mexico: Inmunoprin, Talizer.
Drug combinations
Thalidomide and Docetaxel
Chemistry
Thalidomide: C~13~H~10~N~2~O~4~. Mw: 258.23. (1) 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-, (±)-; (2)(±)-N-(2,6-Dioxo-3-piperidyl)phthalimide; (3) α-(N-Phthalimido)glutarimide. CAS-50-35-1 (1961).
Pharmacologic Category
Biologic Response Modifiers. Angiogenesis Inhibitor. Systemic Immunomodulator. Tumor Necrosis Factor Blocking Agent. (ATC-Code: L04AX02).
Mechanism of action
Has immunomodulatory and antiangiogenic characteristics. May suppress excessive TNF-α production in erythema nodosum leprous (ENL). May increase plasma TNF-α levels in HIV-positive patients. In multiple myeloma, thalidomide is associated with an increase in natural killer cells and increased levels of IL-2 and IFN-γ. Other proposed mechanisms of action include suppression of angiogenesis, prevention of free-radical-mediated DNA damage, and increased cell-mediated cytotoxic effects.
Therapeutic use
Treatment of multiple myeloma. Treatment and maintenance of cutaneous manifestations of ENL.
Pregnancy and lactiation implications
Thalidomide is a known teratogen. Due to potential for serious adverse reactions in infant, drug should not be used during pregnancy or in nursing women. Thalidomide must be discontinued immediately if pregnancy occurs during treatment.
Unlabeled use
Treatment of Crohn’s disease. Graft vs host reactions after bone marrow transplantation. AIDS-related aphthous stomatitis. Behçet’s syndrome. Waldenström’s macroglobulinemia. Langerhans cell histiocytosis. May be effective in rheumatoid arthritis, discoid lupus erythematosus, and erythema multiforme.
Contraindications
Hypersensitivity to thalidomide or any component of the formulation. Neuropathy (peripheral). Women of childbearing potential unless alternative therapies are inappropriate and adequate precautions taken to avoid pregnancy. Pregnancy.
Warnings and precautions
Hazardous agent. May cause bradycardia (use with caution in cardiovascular disease). Hypersensitivity, Stevens-Johnson syndrome, and toxic epidermal necrolysis reported. May cause neutropenia. May cause orthostatic hypotension. Use associated with development of peripheral neuropathy, which may be irreversible (caution with other medications which may cause peripheral neuropathy). May cause sedation, or seizures (use caution in history of seizures, concurrent therapy with drugs which alter seizure threshold, or conditions which predispose to seizures). Thrombotic events reported, generally in other risk factors for thrombosis (neoplastic disease, inflammatory disease, or concurrent therapy with combination chemotherapy). Use in combination with dexamethasone associated with increased risk for deep vein thrombosis and pulmonary embolism. Use with caution in cardiovascular disease, constipation, hepatic impairment, renal impairment or neurological disorders, including seizure disorder; also with drugs which may decrease efficacy of hormonal contraceptives, and in HIV infection (associated with increased viral loads). Thalidomide is a known teratogen. Effective contraception must be used for at least 4 weeks before initiating therapy, during therapy, and for 4 weeks following discontinuation of thalidomide for women of childbearing potential.