GEMCITABINE HYDROCHLORIDE
| GEMCITABINE HYDROCHLORIDE (gem-ci'ta-been) Gemzar Classifications: antineoplastic agent; antimetabolite, pyrimidine; Therapeutic: antineoplastic; antimetabolite Prototype: Fluorouracil Pregnancy Category: D |
Availability
20 mg/mL injection
Action
Pyrimidine analog with cell phase specificity by affecting rapidly dividing cells in S phase (DNA synthesis). It also blocks the progression of cells from G1 phase to S phase of cell cycle. Gemcitabine interferes with DNA synthesis by inhibiting ribonucleotide reductase, which results in a reduction in the concentration of deoxynucleotides. In addition, if gemcitabine is incorporated into the DNA strand, it inhibits further growth of the DNA strand.
Therapeutic Effect
Gemcitabine induces DNA fragmentation in dividing cells, resulting in the cell death of tumor cells.
Uses
Locally advanced or metastatic adenocarcinoma of the pancreas, non-small cell lung cancer, breast cancer.
Contraindications
Hypersensitivity to gemcitabine, severe thrombocytopenia, acute infection, pregnancy (category D), lactation.
Cautious Use
Myelosuppression, renal or hepatic dysfunction, older adults; neutropenia; history of bleeding disorders, infection, previous cytotoxic or radiation treatment. Safety and effectiveness in children are not established.
Route & Dosage
| Pancreatic Cancer Adult: IV 1000 mg/m2 once weekly for up to 7 wk, followed by 1 wk rest from treatment; may repeat once weekly for 3 of every 4 wk Non-Small Cell Lung Cancer Adult: IV 1000 mg/m2 on days 1, 8, 15 of 28-d cycle OR 1250 mg/m2 on days 1 and 8 of 21 d cycle. Given with cisplatin. Breast Cancer Adult: IV 1250 mg/m2 on days 1 and 8 of 21 d cycle. Given with paclitaxel. |
Administration
| Intravenous PREPARE: IV Infusion: ??Dilute with NS without preservatives by adding 5 mL or 25 mL to the 200 mg or 1 g vial, respectively, to yield 38 mg/mL.??Shake to dissolve.??Dilute further if necessary with NS to concentrations as low as 0.1 mg/mL. ADMINISTER: IV Infusion: Infuse over 30 min. Infusion time >60 min is associated with increased toxicity. INCOMPATIBILITIES Y-site: Acyclovir, amphotericin B, cefoperazone, cefotaxime, furosemide, ganciclovir, imipenem/cilastatin, irinotecan, methotrexate, methylprednisolone, mitomycin, piperacillin, piperacillin/tazobactam, prochlorperazine. |
- Store reconstituted solutions unrefrigerated at 20°–25° C (68°–77° F). Use within 24 h of reconstitution.
Adverse Effects (≥1%)
CNS: Fever, flu-like syndrome (anorexia, headache, cough, chills, myalgia), paresthesias. GI: Nausea, vomiting, diarrhea, stomatitis, transient elevations of liver transaminases. Hematologic: Myelosuppression (anemia, leukopenia, neutropenia, thrombocytopenia). Skin: Bullous skin eruption, desquamation. Urogenital: Mild proteinuria and hematuria. Other: Dyspnea, edema, peripheral edema, infection, elevated liver function tests.Interactions
Drug: May increase effect of warfarin or oral anticoagulants.Pharmacokinetics
Peak: Peak concentrations reached 30 min after infusion; lower clearance in women and older adult results in higher concentrations at any given dose. Distribution: Crosses placenta, distributed into breast milk. Metabolism: Intracellularly by nucleoside kinases to active diphosphate and triphosphate nucleosides. Elimination: 92–98% recovered in urine within 1 wk. Half-Life: 32–94 min.Nursing Implications
Assessment & Drug Effects
- Lab tests: Monitor CBC with differential and platelet count prior to each dose. Monitor baseline and periodic renal and hepatic function.
Patient & Family Education
- Learn about common adverse effects and measures to control or minimize when possible. Notify physician immediately of any distressing adverse effects.
- Note: Fever with flu-like symptoms, rash, and GI distress are very common.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug