Description

Simple

A chemotherapy medication used with other medications to treat advanced stages of ovarian and breast cancer, a certain type of lung cancer, and used alone to treat pancreatic cancer.

Clinical

A nucleoside metabolic inhibitor used as adjunct therapy in the treatment of certain types of ovarian cancer, non-small cell lung carcinoma, metastatic breast cancer, and as a single agent for pancreatic cancer.

Overview

Gemcitabine is a nucleoside analog used as chemotherapy. It is marketed as Gemzar® by Eli Lilly and Company. As with fluorouracil and other analogues of pyrimidines, the drug replaces one of the building blocks of nucleic acids, in this case cytidine, during DNA replication. The process arrests tumor growth, as new nucleosides cannot be attached to the "faulty" nucleoside, resulting in apoptosis (cellular "suicide").

Gemcitabine is used in various carcinomas: non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. It is being investigated for use in oesophageal cancer, and is used experimentally in lymphomas and various other tumor types.

Pharmacology

Indication

Gemcitabine is indicated for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy; metastatic ovarian cancer; inoperable, locally advanced (Stage IIIA or IIIB), or metastatic (Stage IV) non-small cell lung cancer; and locally advance... Read more

Pharmacodynamic

Gemcitabine is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (or DNA synthesis phase of the cell cycle), stopping normal development... Read more

Mechanism of action

Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occurs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate by deoxycitidine kinase. Gemcitabine... Read more

Absorption

The pharmacokinetics of gemcitabine are described by a 2-compartment model.

Protein binding

Plasma protein binding is negligible (

Volume of distribution

50 L/m^2 [infusions lasting

Clearance

92.2 L/hr/m2 [Men 29 yrs]75.7 L/hr/m2 [Men 45 yrs]55.1 L/hr/m2 [Men 65 yrs]40.7 L/hr/m2 [Men 79 yrs]69.4 L/hr/m2 [Women 29 yrs]57 L/hr/m2 [Women 45 yrs]41.5 L/hr/m2 [Women 65 yrs]30.7 L/hr/m2 [Women 79 yrs]

Half life

Gemcitabine half-life for short infusions ranged from 42 to 94 minutes, and the value for long infusions varied from 245 to 638 minutes, depending on age and gender, reflecting a greatly increased volume of distribution with longer infusions.

Route of elimination

Within one (1) week, 92% to 98% of the dose was recovered, almost entirely in the urine. Gemcitabine (

Toxicity

Myelosuppression, paresthesias, and severe rash were the principal toxicities, LD50=500 mg/kg (orally in mice and rats)

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The therapeutic efficacy of (R)-warfarin can be increased when used in combination with Gemcitabine.
(S)-Warfarin
The therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Gemcitabine.
2-Methoxyethanol
The risk or severity of adverse effects can be increased when Gemcitabine is combined with 2-Methoxyethanol.
4-hydroxycoumarin
The therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Gemcitabine.
5-fluorouridine
The serum concentration of 5-fluorouridine can be increased when it is combined with Gemcitabine.
9-(N-methyl-L-isoleucine)-cyclosporin A
The risk or severity of adverse effects can be increased when Gemcitabine is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Abacavir
Gemcitabine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The risk or severity of adverse effects can be increased when Gemcitabine is combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Gemcitabine.
Abetimus
The risk or severity of adverse effects can be increased when Gemcitabine is combined with Abetimus.
Acarbose
Acarbose may decrease the excretion rate of Gemcitabine which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Gemcitabine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Gemcitabine which could result in a higher serum level.
Acenocoumarol
The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Gemcitabine.
Acetaminophen
Acetaminophen may decrease the excretion rate of Gemcitabine which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Gemcitabine which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Gemcitabine which could result in a higher serum level.
Aclidinium
Gemcitabine may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine
Gemcitabine may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acteoside
The risk or severity of adverse effects can be increased when Gemcitabine is combined with Acteoside.