Gemcitabine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IV Locally advanced or metastatic pancreatic cancer 1,000 mg/m2 once wkly over 30 min for 7 wk followed by 1 wk rest, then once wkly for 3 consecutive wk out of every 4 wk cycle. Locally advanced or metastatic non-small cell lung cancer Monotherapy: 1,000 mg/m2 once wkly over 30 min for 3 wk followed by 1 wk rest; then 4-wk cycle is repeated. Combination therapy w/ cisplatin: 1,000 mg/m2 over 30 min on days 1, 8, and 15 of a 28-day cycle. Alternatively, 1,250 mg/m2 over 30 min on days 1 and 8 of a 21-day cycle. Locally advanced or metastatic bladder cancer Combination therapy w/ cisplatin: 1,000 mg/m2 over 30 min on days 1, 8 and 15 of a 28-day cycle; then 4-wk cycle is repeated. Locally advanced or metastatic epithelial ovarian cancer Combination therapy w/ carboplatin: 1,000 mg/m2 over 30 min on days 1 and 8 of a 21-day cycle. Unresectable, locally recurrent, or metastatic breast cancer Combination therapy w/ paclitaxel: 1,250 mg/m2 over 30 min on days 1 and 8 of a 21-day cycle. All dosage may reduce w/ each cycle or w/in a cycle based on toxicity.
Dosage Details
Intravenous
Cancer, pancreatic
Adult: Patient w/ locally advanced or metastatic cases: 1,000 mg/m2 once wkly via infusion over 30 min for 7 wk followed by 1 wk rest, then once wkly for 3 consecutive wk out of every 4 wk cycle. Dosage may reduce w/ each cycle or w/in a cycle based on toxicity.

Intravenous
Breast cancer
Adult: Patient w/ unresectable, locally recurrent, or metastatic cases: Combination therapy w/ paclitaxel: 1,250 mg/m2 via infusion over 30 min on days 1 and 8 of a 21-day cycle. Dosage may reduce w/ each cycle or w/in a cycle based on toxicity. Patients should have absolute granulocyte count of ≥1,500 x 106/L prior to initiation of therapy.

Intravenous
Bladder cancer
Adult: Patient w/ locally advanced or metastatic cases: Combination therapy w/ cisplatin: 1,000 mg/m2 via infusion over 30 min on days 1, 8 and 15 of a 28-day cycle. This 4-wk cycle is then repeated. Dosage may reduce w/ each cycle or w/in a cycle based on toxicity.

Intravenous
Non-small cell lung cancer
Adult: Patient w/ locally advanced or metastatic cases: Monotherapy: 1,000 mg/m2 once wkly via infusion over 30 min for 3 wk followed by 1 wk rest for locally advanced or metastatic cases. This 4-wk cycle is then repeated. Combination therapy w/ cisplatin: 1,000 mg/m2 via infusion over 30 min on days 1, 8, and 15 of a 28-day cycle. Alternatively, 1,250 mg/m2 via infusion over 30 min on days 1 and 8 of a 21-day cycle. Dosage may reduce w/ each cycle or w/in a cycle based on toxicity.

Intravenous
Ovarian cancer
Adult: Patient w/ locally advanced or metastatic epithelial cases: Combination therapy w/ carboplatin: 1,000 mg/m2 via infusion over 30 min on days 1 and 8 of a 21-day cycle. Dosage may reduce w/ each cycle or w/in a cycle based on toxicity.
Reconstitution
Add 5 or 25 mL of NaCl 0.9% inj in a vial labelled as containing 200 or 1,000 mg respectively, to provide a soln containing 38 mg/mL.
Contraindications
Admin of yellow fever and other live attenuated vaccines.
Special Precautions
Patient w/ history of cirrhosis, hepatitis, alcoholism, CV events. Patients on radiotherapy. Hepatic (e.g. hepatic metastases) and renal impairment. Pregnancy. Prolonged infusion duration of >60 min or more frequent than wkly dosing may increase toxicity.
Adverse Reactions
Significant: Bone marrow suppression manifested by neutropenia, thrombocytopaenia, and anaemia; capillary leak syndrome, posterior reversible encephalopathy syndrome (PRES).
Nervous: Somnolence, flu-like symptoms, paraesthesia.
CV: Peripheral oedema.
GI: Nausea, vomiting, diarrhoea, stomatitis, constipation.
Resp: Dyspnoea.
Hepatic: Transient liver enzyme elevations (e.g. AST, ALT, bilirubin, alkaline phosphatase).
Genitourinary: Haematuria, proteinuria, increased BUN.
Haematologic: Haemorrhage.
Musculoskeletal: Myalgia.
Dermatologic: Rash, pruritus, oedema, thrombocytopenic purpura, alopecia, peripheral vasculitis, gangrene.
Immunologic: Infection.
Others: Pain, fever, extravasation, injection site reaction.
Potentially Fatal: Severe hepatotoxicity (e.g. liver failure), pulmonary toxicity (e.g. pulmonary oedema, pulmonary fibrosis, interstitial pneumonitis, adult resp distress syndrome), ischaemic colitis w/ necrosis. Rarely, haemolytic uremic syndrome leading to renal failure.
IV/Parenteral: D
Patient Counseling Information
This drug may cause somnolence, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor CBC w/ differential and platelet count prior to each dose. Monitor pulmonary, hepatic, and renal function; electrolytes (i.e. K, Mg, Ca) when in combination therapy w/ cisplatin. Monitor for signs and symptoms of capillary leak syndrome and PRES.
Overdosage
Symptoms: Myelosuppression, severe rash, paraesthesia. Management: Supportive treatment. Monitor CBC.
Drug Interactions
May cause pulmonary toxicity w/ concurrent use of bleomycin. May enhance anticoagulant effect of warfarin.
Potentially Fatal: Admin of yellow fever and other live attenuated vaccines may increase risk of systemic disease esp in immunosuppressed patients.
Action
Description: Gemcitabine, a synthetic pyrimidine nucleoside and cytarabine analogue, inhibits DNA synthesis by blocking DNA polymerase and ribonucleotide reductase. It is cell-cycle specific acting mainly on the S-phase, but may also block cellular progression at the G1-S border.
Pharmacokinetics:
Distribution: Widely distributed into tissues; present in ascitic fluid. Volume of distribution: 50 L/m2 (<70 min infusion time); 370 L/m2 (70-285 min infusion time).
Metabolism: Rapidly metabolised in the liver, kidney, blood, and other tissues by cytidine deaminase to the inactive metabolite 2’-deoxy-2’,2’-difluorouridine (dFdU); undergoes intracellular metabolism by nucleoside kinases to the active metabolites, gemcitabine diphosphate and triphosphate nucleosides.
Excretion: Mainly via urine (92-98% mainly as dFdU; <10% as unchanged drug) and faeces (<1%). Elimination half-life: Gemcitabine: Approx 42-94 min (≤70 min infusion time); 4-10.5 hr (3-4 hr infusion time). Gemcitabine triphosphate: 1.7-19.4 hr.
Chemical Structure

Chemical Structure Image
Gemcitabine

Source: National Center for Biotechnology Information. PubChem Database. Gemcitabine, CID=60750, https://pubchem.ncbi.nlm.nih.gov/compound/Gemcitabine (accessed on Jan. 22, 2020)

Storage
Concentrate soln for infusion: Store between 2-8°C. Powder for soln for infusion: Store between 20-25°C.
Avoid inhalation and contact w/ skin or mucous membranes by wearing gloves and protective equipment. Wash hands before and after handling. Any unused portions should be disposed of in accordance w/ local requirements. Pregnant staff should not handle this product.
ATC Classification
L01BC05 - gemcitabine ; Belongs to the class of antimetabolites, pyrimidine analogues. Used in the treatment of cancer.
References
Anon. Gemcitabine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 26/05/2017.

Buckingham R (ed). Gemcitabine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/05/2017.

Gemcitabine Hydrochloride Injection, Powder, Lyophilized, for Soln (Accord Healthcare Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 26/05/2017.

Joint Formulary Committee. Gemcitabine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/05/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Gemcitabine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 26/05/2017.

Disclaimer: This information is independently developed by MIMS based on Gemcitabine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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