Thalidomide

Indications
 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.
Oral
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.
Contraindications
 Pregnancy and lactation.
Warnings / Precautions
 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.
Adverse Reactions
 Severe and irreversible peripheral neuropathy, constipation, dizziness, orthostatic hypotension, drowsiness, somnolence, bradycardia, increase of viral load in HIV-infected patients, hypersensitivity reaction.
Potentially Fatal: Stevens-Johnson syndrome, toxic epidermal necrolysis and blood dyscrasias.
Drug Interactions
 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.
See Below for More thalidomide Drug Interactions
Mechanism of Actions
 Thalidomide is a synthetic glutamic acid derivative immunomodulator with anti-inflammatory, antiangiogenetic, sedative and hypnotic activity.
Absorption: Slowly absorbed from GI tract. Peak plasma concentrations: 3 to 6 hr. Food may delay but does not significantly affect extent of absorption of thalidomide.
Distribution: Crosses the placenta, distributed into the semen. Elimination half-life: 5-7 hr.
Metabolism: Exact metabolic fate unknown, it appears to undergo non-enzymatic hydrolysis in plasma.
Administration
 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.)
ATC Classification
 L04AX02 - thalidomide ; Belongs to the class of other immunosuppressive agents.
Available As
  • Thalidomide 100 mg
  • Thalidomide 50 mg

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