TEMOZOLOMIDE (tem-o-zol'o-mide)
Temodar Classifications: antineoplastic; alkylating agent; Therapeutic: antineoplastic Prototype: Cyclophosphamide Pregnancy Category: D
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Availability
5 mg, 20 mg, 100 mg, 140 mg, 180 mg, 250 mg capsules
Action
Cytotoxic agent with alkylating properties structurally similar to dacarbazine. Effects are cell cycle nonspecific. Interferes
with purine (e.g., guanine) metabolism and thus protein synthesis in rapidly proliferating cells.
Therapeutic Effect
Effectiveness is indicated by objective evidence of tumor regression.
Uses
Adult patients with refractory anaplastic astrocytoma, glioblastoma multiforme with radiotherapy.
Contraindications
Hypersensitivity to temozolomide, DTIC, or dacarbazine; severe bone marrow suppression; children <3 y; pregnancy (category
D), lactation.
Cautious Use
Bacterial or viral infection; older adults; severe hepatic or renal impairment; myelosuppression; prior radiotherapy or
chemotherapy.
Route & Dosage
Astrocytoma Adult: PO 150 mg/m2 daily for 5 consecutive days per 28 d treatment cycle; subsequent doses are based on absolute neutrophil count on day 21
or at least 48 h before next scheduled cycle (see prescribing information for dosage adjustments based on neutrophil count)
Glioblastoma Multiforme Adult: PO 75 mg/m2 daily for 42 d with focal radiotherapy; after 4 wk, maintenance phase of 150 mg/m2
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Administration
Oral
- Give consistently with regard to food.
- Do not administer unless absolute neutrophil count >1500 per microliter and platelet count >100,000 per microliter.
- Do not open capsules. Avoid inhalation or contact with skin or mucous membranes, if accidentally opened/damaged.
- Store at room temperature, 15°30° C (59°86° F).
Adverse Effects (≥1%)
Body as a Whole: Headache, fatigue, asthenia, fever, back pain, myalgia, weight gain; viral
infection.
CNS: Convulsions, hemiparesis, dizziness, abnormal coordination, amnesia, insomnia, paresthesia, somnolence, paresis, ataxia, dysphasia, abnormal gait, confusion, anxiety,
depression.
CV: Peripheral edema. GI: Nausea, vomiting, constipation, diarrhea, abdominal pain, anorexia.
Hematologic: Anemia,
neutropenia, thrombocytopenia, leukopenia, lymphopenia.
Respiratory: Upper respiratory tract
infection, pharyngitis,
sinusitis, cough.
Skin: Rash, pruritus.
Metabolic: Adrenal hypercorticism.
Urogenital: Urinary incontinence.
Special Senses: Diplopia, abnormal vision.
Interactions
Drug: Valproic acid may decrease
temozolomide levels.
Pharmacokinetics
Absorption: Rapidly.
Peak: 1 h.
Metabolism: Spontaneously metabolized to active
metabolite MTIC.
Elimination: Primarily in urine.
Half-Life: 1.8 h.
Nursing Implications
Assessment & Drug Effects
- Monitor for S&S of toxicity: Infection, bleeding episodes, jaundice, rash, CNS disturbances.
- Lab tests: CBC with differential on day 22 and weekly until absolute neutrophil count (ANC) >1500 per microliter and platelet
count >100,000 per microliter; periodic LFT and routine serum chemistry, including serum calcium.
Patient & Family Education
- Take consistently with respect to meals.
- Report to physician signs of infection, bleeding, discoloration of skin or skin rash, dizziness, lack of balance, or other
bothersome side effects promptly.
- Exercise caution with hazardous activities until response to drug is known.
- Use effective methods of contraception; avoid pregnancy.