antineoplastic drugs 4,5.pptx h jnnnnnnm

Introduction to antineoplastics

1. Plant products ETOPOSIDE Pharmacodynamics Mechanism of action Etoposide is a etopoisomerase ii inhibitor. Etopoisomerase ii is an enzyme that is responsible for relaxing and unwinding of DNA, which is necessary for DNA replication and transcription. Etoposide therefore works by preventing the action of the enzyme causing DNA to be tangled and broken. This damage prevents the cell from dividing or replicating, which can lead to cell death.

2. SIDE EFFECTS ADVERSE EFFECTS CONTRAINDICATION DRUG INTERACTION Nausea and vomiting fatique Myelosuppression Alopecia Mouth sores Risk of infection infertility Pregnancy Breastfeeding Hypersensitivity to etoposide Severe liver disease Warfarin Phenobarbitol , phenytoin, valproic acid. grapefruit ABSORPTION DISTRIBUTION HALF LIFE METABOLISM EXCRETION Absorbed slowly and incompletely from the GIT Widely distributed throughout the body 4-8 hours In the liver via gluconiridation Primarily via urine with about 40% unchanged

3. VINBLASTINE Mechanism of action it works by interfering with the formation of microtubules. Microtubules are composed of tubulin dimers. Vinblastine binds to tubulin dimers and prevents formation of microtubules which in turn prevents formation of spindle fibers, which is necessary for chromosome separation during cell division. As a result, vinblastine arrests cells in metaphase and eventually leads to cell death.

4. SIDE EFFECTS ADVERSE EFFECTS CONTRAINDICATION DRUG INTERACTION Nausea Vomiting Constipation Jaw pain Neurotoxicity Alopecia Myelosuppression Oral ulcers Hypersensitivity to vinblastine Pregnancy Breastfeeding Severe liver disease Warfarin Phenobarbital and phenytoin Grape fruit Live attenuated vaccines ABSORPTION DISTRIBUTION HALF LIFE METABOLISM EXCRETION Poorly absorbed from GIT Widely distributed throughout the body 24-48 hrs In liver via CYP3A4 enzyme mediated glucuronidation Via bile and faeces with 30% unchanged

5. Miscellaneous drugs CISPLATIN Mechanism of action I t works by interfering with DNA replication and repair leading to cell death. Once inside cell, it undergoes equation, losing its chloride ligands forming hydrated platinum complexes. These bind to DNA bases, forming crosslinks, which interfere with DNA replication and processes leading to DNA damage.

6. SIDE EFFECTS ADVERSE EFFECTS CONTRAINDICATION DRUG INTERACTION Nausea Vomiting Fatique Allergic reaction Kidney damage Myelosuppression Alopecia Oral sores Hypersensitivity to cisplatin Live attenuated vaccine Severe liver disease Pregnancy breastfeeding Warfarin Phenobarbital and phenytoin Valproic acid Grape fruit furosemide ABSORPTION DISTRIBUTION HALF LIFE METABOLISM EXCRETION Poorly absorbed from GIT Widely distributed 24-48 hrs Primarily in kidney via hydrolysis Via urine Bile and faeces