gemcitabine (jem-site-a-been) Gemzar

 Indications

Pancreatic cancer (locally advanced or metastatic). Inoperable

locally advanced/metastatic non–small-cell

lung cancer (with cisplatin). Metastatic breast cancer

(with paclitaxel). Advanced ovarian cancer that has relapsed

6 mo after completion of platinum-based therapy

(with carboplatin).

Action

Interferes with DNA synthesis (cell-cycle phase–specific).

Therapeutic Effects: Death of rapidly replicating

cells, particularly malignant ones.

Pharmacokinetics

Absorption: IV administration results in complete

bioavailability.

Distribution: Unknown.

Metabolism and Excretion: Converted in cells to

active diphosphate and triphosphate metabolites; these

are excreted primarily by the kidneys.

Half-life: 32–94 min.

TIME/ACTION PROFILE (effect on blood

counts)

ROUTE ONSET PEAK DURATION

IV unknown unknown unknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity; OB: Can

cause fetal malformation; Lactation: Can expose infant

to serious adverse effects. Bottle-feed if gemcitabine

therapy is necessary.

Use Cautiously in: History of cardiovascular disease;

Impaired hepatic or renal function (qrisk of toxicity);

Other chronic debilitating illness; Rep: Patients

with childbearing potential.

Adverse Reactions/Side Effects

CNS: POSTERIOR REVERSIBLE ENCEPHALOPATHY SYNDROME

(PRES). Resp: PULMONARY TOXICITY, dyspnea,

bronchospasm. CV: ARRHYTHMIAS, CAPILLARY LEAK SYNDROME,

CEREBROVASCULAR ACCIDENT, MI, edema, hypertension.

GI: HEPATOTOXICITY, diarrhea,qliver enzymes,

nausea, stomatitis, vomiting. GU: HEMOLYTIC UREMIC

SYNDROME, hematuria, proteinuria. Derm: alopecia,

rash. Hemat: anemia, leukopenia, thrombocytopenia.

Local: injection site reactions. Neuro: paresthesias.

Misc: flu-like symptoms, fever, anaphylactoid reactions.

Interactions

Drug-Drug:qbone marrow depression with other

antineoplastics or radiation therapy. Maypantibody

response to live virus vaccines andqrisk of adverse

reactions.

Route/Dosage

Other regimens are used.

Pancreatic Cancer

IV (Adults): 1000 mg/m2 once weekly for 7 wk, followed

by a wk of rest. May be followed by cycles of

once-weekly administration for 3 wk followed by a wk

of rest.

Non–Small-Cell Lung Cancer (with Cisplatin)

IV (Adults): 1000 mg/m2 on days 1, 8, and 15 of each

28-day cycle (cisplatin is also given on day 1) or 1250

mg/m2 on days 1 and 8 of each 21-day cycle (cisplatin

is also given on day 1).

Breast Cancer

IV (Adults): 1250 mg/m2 on days 1 and 8 of each 21-

day cycle (paclitaxel is also given on day 1).

Ovarian Cancer

IV (Adults): 1000 mg/m2 on days 1 and 8 of each 21-

day cycle.

Availability (generic available)

Powder for injection: 200 mg/vial, 1 g/vial, 2 g/

vial.