Thalidomide

Thalidomide is used for: Multiple myeloma, Erythema nodosum leprosum

Oral Erythema nodosum leprosum (Type 2) Adult: 100-300 mg once daily at bedtime, reduced gradually by 50 mg every 2-4 wk once a satisfactory reponse is achieved. Not for monotherapy if moderate or severe neuritis present. Max: 400 mg/day. Patients < 50 kg: Initially, 100 mg daily. Multiple myeloma Adult: Initial dose of 200 mg once daily, increased by 100 mg at wkly intervals according to patient tolerance. Max: 800 mg daily.

Should be taken on an empty stomach. Take on an empty stomach at least 1 hr after a meal, w/ a full glass of water.

Hypersensitivity. Pregnancy and lactation.

All females of childbearing potential must use 2 reliable forms of contraception simultaneously 4 wk before starting therapy, during and 4 wk after therapy is discontinued. Therapy to be stopped immediately if pregnancy occurs. Male: Use of barrier methods of contraception if partner is of child-bearing potential. Do not donate blood or sperm during therapy. Patient should not drive or operate machinery. Discontinue therapy if any skin rash develops. Do not resume therapy if the rash is exfoliative, purpuric, or bullous, or if Stevens-Johnson syndrome or toxic epidermal necrolysis suspected. Lactation: not known if excreted in breast milk, not recommended

Pregnancy Potent teratogen; contraindicated during pregnancy (see Black Box Warnings; Contraindications, Cautions) Based on the mechanism of action, human and animal data, thalidomide can cause embryo-fetal harm when administered to pregnant female It is a powerful human teratogen, inducing a high frequency of severe and life-threatening birth defects, even after a single dose Mortality at or shortly after birth reported in ~40% of infants If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential risk to a fetus If pregnancy occurs during treatment, discontinue the drug immediately Contraception Females Females must commit either to abstain continuously from heterosexual sexual intercourse or to use 2 methods of reliable birth control, beginning 4 weeks before initiating treatment, during therapy, during dose interruptions, and continuing for 4 weeks following therapy discontinuation 2 negative pregnancy tests must be obtained before initiating; the first test should be performed within 10-14 days and the second test within 24 hr before prescribing therapy and then weekly during the first month, then monthly thereafter in females with regular menstrual cycles or q2week in females with irregular menstrual cycles Males Thalidomide is present in the semen of patients; therefore, males must always use a latex or synthetic condom during any sexual contact with females of reproductive potential while taking thalidomide and for up to 4 weeks after discontinuing, even if they have undergone a successful vasectomy Male patients taking thalidomide must not donate sperm Lactation There is no information regarding presence of thalidomide in human milk; effects of thalidomide on breastfed infant, or effects of thalidomide on milk production Because many drugs are excreted in human milk and because of potential for adverse reactions in breastfed infants from thalidomide advise women not to breastfeed during therapy

Thalidomide enhances sedative activity of barbiturates, alcohol, chlorpromazine and reserpine. Avoid use of other drugs that have the potential to cause peripheral neuropathy. Increased risk of thromboembolic events with darbepoetin-alfa and doxorubicin. Potentially Fatal: Increased risk of bone marrow supression with peg interferon alfa.

Side effects of Thalidomide : >10% Somnolence (37%), Rash (21%), Edema (57%), Hypotension (16%), Leukopenia (17-35%), Neutropenia (31%), Increased bilirubin (14%), Myalgia (17%), Arthralgia (13%), Hematuria (11%), Thrombosis/embolism (23%), Headache (12%), Dyspnea (42%) 1-10% Asthenia (8%), General pain (8%), Impotence (8%), Malaise (8%), Pruritus (8%), Xerostomia (8%), Flatulence (8%), Tooth pain (4%), Impotence (3-8%), Vertigo (8%), Constipation (4%), Diarrhea (4%), Neck rigidity (4%) Frequency Not Defined Photosensitivity, Bradycardia, Hypo/hypertension, Peripheral neuropathy, Neutropenia Potentially Fatal: Stevens-Johnson syndrome, toxic epidermal necrolysis and blood dyscrasias.

Thalidomide is a synthetic glutamic acid derivative immunomodulator with anti-inflammatory, antiangiogenetic, sedative and hypnotic activity.