Dosing and uses of Gemzar (gemcitabine)
Adult dosage forms and strengths
powder for injection
- 200mg/vial
- 1g/vial
Pancreatic Cancer
Indicated as first-line treatment for locally advanced (nonresectable Stage II or Stage III) or metastatic (Stage IV) adenocarcinoma of the pancreas
1000 mg/m² IV infusion over 30 minutes once/week x7 weeks; rest 1 week, THEn
1000 mg/m² IV on Days 1, 8, and 15 of each 28-day cycle
Various regimens exist including monotherapy and in combination with other chemotherapy agents (eg, erlotinib, paclitaxel protein bound, capecitabine)
Non-small Cell Lung Cancer
1000 mg/m² IV infusion over 30 minutes on days 1, 8, and 15 of each 28-day cycle, Or
1250 mg/m² IV infusion over 30 minutes on days 1 and 8 of each 21-day cycle
Administer cisplatin 100 mg/m² IV after gemcitabine on day 1
Breast Cancer
1250 mg/m² IV infusion over 30 minutes on Days 1 and 8 of each 21-day cycle
With paclitaxel 175 mg/m² on Day 1 as a 3 hr infusion before gemcitabine
Ovarian Cancer
1000 mg/m² IV infusion over 30 minutes on Days 1 and 8 of each 21-day cycle
With carboplatin AUC 4 on Day 1 after gemcitabine
Dosing Considerations
Monitor: CBC before each dose; renal/hepatic function; (with cisplatin): serum creatinine, electrolytes
Bladder Cancer (Off-label)
May be considered for muscle-invasive bladder cancer in combination with cisplatin
Cholangiocarcinoma (Orphan)
Orphan designation for treatment of cholangiocarcinoma
Sponsor
- InnoPharmax, Inc; 9F, No. 22, Lane 478, Rueiguang Road; Taipei
Pediatric dosage forms and strengths
Not recommended
Gemzar (gemcitabine) adverse (side) effects
>10%
N/V (69%)
Anemia (65%)
Elev LFTs (68%)
Neutropenia (63%)
Leukopenia (62%)
Pain (48%)
Proteinuria (45%)
Fever (41%)
Hematuria (35%)
Rash (30%)
Thrombocytopenia (24%)
Dyspnea (23%)
Constipation (23%)
Diarrhea (19%)
Flu-like syndrome (19%)
Hemorrhage (17%)
BUN increased (16%)
Infection (16%)
Alopecia (15%)
Edema (13%)
Elev bilirubin (13%)
1-10%
Paresthesia (2-10%)
Creatinine increased (2-8%)
Inj site reactions (4%)
Bronchospasm (2%)
Postmarketing Reports
Cardiovascular: CHF, MI, arrhythmias, supraventricular arrhythmias
Vascular disorders: Peripheral vasculitis, gangrene, capillary leak syndrome
Skin: Cellulitis, severe skin reactions, including desquamation and bullous skin eruptions
Hepatic: Hepatic failure, hepatic veno-occlusive disease
Pulmonary: Interstitial pneumonitis, pulmonary fibrosis, pulmonary edema, ARDs
Warnings
Contraindications
Hypersensitivity
Cautions
Myelosuppression reported
In combination with carboplatin or paclitaxel: patients should have ANC >1.5 x 10^6/mL and platelet count >10^8/mL prior to each cycle
Capillary leak syndrome reported with severe consequences; discontinue if symptoms occur
Pulmonary toxicity, including interstitial pneumonitis, pulmonary fibrosis, pulmonary edema, and ARDS reported
Hemolytic uremic syndrome reported, including fatalities
Drug-induced liver injury reported, including liver failure and death
Not indicated for use with radiation therapy; know to exacerbate radiation toxicity, including life-threatening mucositis, especially esophagitis and pneumonitis
Infusions longer than 60 minutes or more frequently than qWk increase the incidence of clinically significant hypotension, severe flu-like symptoms, myelosuppression, and asthenia; gemcitabine half-life is influenced by the length of the infusion
Posterior reversible encephalopathy syndrome (PRES) reported; PRES can present with headache, seizure, lethargy, hypertension, confusion, blindness, and other visual and neurologic disturbances; discontinue if PRES develops
Pregnancy and lactation
Pregnancy category: d
Lactation: not known if excreted in breast milk; do not nurse
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Gemzar (gemcitabine)
Mechanism of action
Pyrimidine analog; kills cells in S-phase (undergoing DNA synthesis)
Pharmacokinetics
Vd: 50 L/sq.meter (short infusions); 370 L/m² (long infusions)
Metabolites: diphosphate (dFdCDP), triphosphate (dFdCTP)
Half-Life: 42-94 min (short infusions); 245-638 min (long infusions)
Clearance: 40-92 L/hr/sq.meter
Excretion: urine
Administration
IV Incompatibilities
Y-site: acyclovir, amphotericin B, cefoperazone, cefotaxime, furosemide, ganciclovir, imipenem/cilastatin, irinotecan, methotrexate, methylprednisolone sodium succinate, mitomycin, piperacillin, piperacillin/tazobactam, prochlorperazine
IV Compatibilities
Y-site (partial list): ampicillin, carboplatin, cefazolin, chlorproazine, cimetidine, clindamycin, cytarabine, diphenhydramine, dopamine, etoposide, heparin, linezolid, metoclopramide, morphine, paclitaxel, KCl, NaHCO3, topotecan, vancomycin, zidovudine
IV Preparation
Reconstitute 200 mg vial with 5 mL 0.9% NaCl OR 1000 mg vial with 25 mL 0.9% NaCL
Resulting solution is approximately 38 mg/mL, but is variable
Reconstituted soln stable for 24 hr at room temp (20-25°C).
Do NOT refrigerate
The appropriate dose may be further diluted with NS to concentrations as low as 0.1 mg/mL
IV Administration
For IV infusion only
Concentrated injection (10 mg/mL) must be diluted to 2 mg/mL prior to administration
Infuse over 30 min
Avoid rapid infusions
Storage
Store intact vials at 25°C (77°F)
