gimeracil

Action and Spectrum

Actions and Spectrum 

gimeracil is a dihydropyrimidine dehydrogenase (DPD) inhibitor, which prevents the enzyme from degrading and inactivating the chemotherapeutic medication 5-fluorouracil (5-FU).  

gimeracil works better to destroy cancer cells that divide quickly by increasing the content of active 5-FU inside cancer cells by inhibiting DPD. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Sore mouth 

Fatigue 

Loss of appetite  

Constipation  

Brittle nails 

Drowsiness  

Change in taste  

Diarrhea  

Rash 

Headaches 

Photosensitivity  

Confusion 

Insomnia 

Black Box Warning

Black Box Warning 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• gimeracil should not be used in individuals with a known hypersensitivity to gimeracil or any of the other components of the medication. 

Caution: 

• Patients with severe gastrointestinal disorders may require caution when using gimeracil-based therapy due to potential gastrointestinal adverse effects. 
• Caution should be needed in patients with a history of cardiovascular disease. 

Pregnancy / Lactation

Pregnancy consideration: 

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

The pharmacological action of gimeracil is to block the activity of the enzyme dihydropyrimidine dehydrogenase (DPD).  

It oversees the body’s ability to break down the chemotherapeutic medication 5-fluorouracil (5-FU). 

Pharmacodynamics 

Increased levels of active 5-FU are seen in cancer cells because of gimeracil’s suppression of DPD.  

A cytotoxic antimetabolite called 5-FU disrupts DNA synthesis and function, which ultimately causes cell death. 

Pharmacokinetics 

Absorption   

gimeracil is absorbed from the gastrointestinal tract and enters the bloodstream.  

Distribution 

gimeracil is distributed throughout the body. 

Metabolism 

gimeracil undergoes metabolic processes in the liver. 

Elimination and excretion 

gimeracil is primarily excreted through the renal route. 

Adminstartion

Administration 

gimeracil is administered orally and it is available in tablet and capsule form.

Patient Information Leaflet

Patient information leaflet 

Generic Name: gimeracil 

Why do we use gimeracil? 

gimeracil is used as part of combination therapy for the treatment of Resectable gastric carcinoma. gimeracil is used in combination with tegafur and oteracil as a chemotherapy for various gastrointestinal cancers including Colorectal cancer and Pancreatic cancer.