Adult: As 1st-line treatment in newly diagnosed patients who are ineligible for high dose chemotherapy: In combination with melphalan and prednisone: 200 mg once daily at bedtime for a 42-day (6-week) cycle. Max treatment duration: 12 cycles. Alternatively, in combination with dexamethasone: 200 mg once daily at bedtime in 28-day treatment cycles. Thromboprophylaxis (e.g. LMWH, warfarin) is recommended for at least the 1st 5 months of therapy (particularly in patients with additional thrombotic risk factors). Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline). Elderly: >75 years As 1st-line treatment in newly diagnosed patients who are ineligible for high dose chemotherapy in combination with melphalan and prednisone: 100 mg once daily at bedtime for a 42-day (6-week) cycle. Max treatment duration: 12 cycles. Thromboprophylaxis (e.g. LMWH, warfarin) is recommended for at least the 1st 5 months of therapy (particularly in patients with additional thrombotic risk factors). Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline).
Oral Erythema nodosum leprosum
Adult: For the acute treatment of moderate to severe cases: 100-300 mg once daily, preferably at bedtime. In patients weighing <50 kg: Initiate at the low end of the dose range. If moderate to severe neuritis is present, consider concomitant use with corticosteroid until neuritis improves. In severe cases or in patients who previously required higher doses to control the reaction: May be initiated at up to 400 mg once daily at bedtime or in divided doses. Continue treatment until signs and symptoms of active reaction have subsided (usually approx 2 weeks) then taper off in 50 mg decrements every 2-4 weeks. Maintenance treatment for the prevention and suppression of cutaneous manifestations of recurrent cases: Maintain on the minimum dosage needed to control the reaction; tapering off must be attempted every 3-6 months in decrements of 50 mg every 2-4 weeks. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline).
Should be taken on an empty stomach. Take at least 1 hr after a meal, w/ a full glass of water.
Absolute neutrophil count (ANC) of <750/mm3. Pregnancy, women of childbearing potential who are not using stringent contraceptive measures; lactation.
Patient with risk factors for thromboembolism (e.g. previous thrombosis, hypertension, hyperlipidaemia, smoking), pre-existing liver disorder or peripheral neuropathy; high tumour burden (before treatment); HIV. Patient who may not tolerate transient hypotensive episodes. Patients must not donate blood or sperm (in men) during therapy, including dose interruptions for 4 weeks after discontinuation of therapy. Severe renal and hepatic impairment. Elderly. Concomitant use with erythropoietic agents or other agents (e.g. hormone replacement therapy).
Significant: Menstrual disorders (e.g. amenorrhoea), venous thromboembolism (e.g. DVT, pulmonary embolism), arterial thromboembolism (e.g. MI, cerebrovascular event), hypothyroidism, severe and irreversible peripheral neuropathy, neutropenia, leucopenia, febrile neutropenia, pancytopenia, thrombocytopenia (including grade 3 or 4 cases), anaemia, tumour lysis syndrome, hepatic disorders (e.g. abnormal LFTs, cholestatic jaundice, hepatitis), constipation, hypersensitivity reactions (including angioedema and anaphylactic reaction), somnolence, viral reactivation (serious cases of herpes zoster or hepatitis B virus reactivation), increased viral load, secondary malignancy (e.g. acute myeloid leukaemia, myelodysplastic syndromes), bradycardia, orthostatic hypotension, seizures (including grand mal convulsions). Blood and lymphatic system disorders: Lymphopenia. Cardiac disorders: Cardiac failure. Ear and labyrinth disorders: Hearing impaired or deafness. Gastrointestinal disorders: Dry mouth, vomiting. General disorders and administration site conditions: Peripheral oedema, asthenia, malaise, pyrexia. Nervous system disorders: Dizziness, paraesthesia, dysaesthesia, tremor, abnormal coordination, posterior reversible encephalopathy syndrome. Psychiatric disorders: Confusional state, depression. Renal and urinary disorders: Renal failure. Respiratory, thoracic and mediastinal disorders: Pneumonia, interstitial lung disease, bronchopneumopathy, dyspnoea. Skin and subcutaneous tissue disorders: Dry skin, rash. Potentially Fatal: Severe cutaneous reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms); pulmonary hypertension; severe birth defects or embryo foetal death.
Patient Counseling Information
Women of childbearing potential must use 2 proven forms of contraceptive methods for at least 4 weeks prior to start, during (even during dose interruption), and until at least 4 weeks after therapy. Men with partners of child-bearing potential (even after successful vasectomy) must use condoms during therapy and dose interruption, and for up to 28 days after stopping treatment; do not donate semen or sperm. This drug may cause tiredness, dizziness, and drowsiness; if affected, do not drive or operate machinery.
Perform pregnancy tests (minimum sensitivity of 25 mIU/mL) in women of childbearing potential 10-14 days and within 24 hours before initiating treatment, weekly during the 1st 4 weeks, then repeated every 4 weeks thereafter (every 2 weeks for women with irregular menstrual cycles), including 4 weeks after the end of therapy (except in cases of confirmed tubal sterilisation). Screen for hepatitis B virus with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to treatment initiation. Monitor CBC with differential, platelet counts; thyroid function (at baseline and during treatment), LFTs (periodically). Observe for signs and symptoms of thromboembolic events; peripheral neuropathy (monthly for the 1st 3 months then periodically during treatment); severe skin reactions, bradycardia, syncope, atrioventricular block, somnolence, neutropenia, and thrombocytopenia. Consider electrophysiological testing (consisting of measurement of sensory nerve action potential amplitudes) at baseline and every 6 months thereafter. Obtain viral load in HIV-infected patients following the 1st and 3rd months of therapy, then every 3 months thereafter.
Symptoms: Drowsiness, irritability, headache. Rarely, abnormal plantar response. Management: Supportive treatment. Monitor vital signs. Maintain blood pressure and respiratory status as necessary.
May enhance the sedative effects of anxiolytics, hypnotics, H1 antihistamines, antipsychotics, opioids, and barbiturates; avoid concomitant use. May cause additive bradycardic effect with β-blockers, Ca channel blockers, digoxin, lithium, TCAs, H2 blockers (e.g. famotidine, cimetidine), or neuromuscular blockers (e.g. succinylcholine). Increased risk of peripheral neuropathy with drugs known to cause the condition (e.g. vincristine, bortezomib, amiodarone, cisplatin, phenytoin, disulfiram, metronidazole). May increase the risk of venous thromboembolic disease with erythropoietic agents or other drugs (e.g. estrogen-containing contraceptive).
May enhance the sedative effects of alcohol; avoid concomitant use.
Description: Thalidomide has immunomodulatory, anti-inflammatory, and antiangiogenic activities. The mechanism of action is not fully understood, however, in vitro studies suggest that its immunomodulatory effect may be related to the inhibition of excessive tumour necrosis factor-α (TNF-α) production and down-regulation of selected cell surface adhesion molecules associated in leucocyte migration. In multiple myeloma, it is associated with the increase in number of natural killer cells, and interleukin-2 and interferon γ plasma levels. Pharmacokinetics: Absorption: Slowly absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1-5 hours. Distribution: Present in semen. Crosses the placenta. Volume of distribution: 1.1 L/kg. Plasma protein binding: 55-66%. Metabolism: Almost exclusively metabolised by non-enzymatic hydrolysis. Excretion: Via urine (approx 92%; <4% as unchanged drug); faeces (<2%). Elimination half-life: 5.5-7.3 hours.
Store between 15-30°C. Protect from light. Follow applicable procedures for receiving, handling, administration, and disposal.