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Pharmacology Group I presentation

Pharmacology Group I presentation. Topic: Cisplatin. Drug background. was first synthesized in 1845 Alkylating agent an inorganic complex formed by an atom of platinum surrounded by chlorine and ammonia atoms in the cis position of a horizontal plane. Drug usage.

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Pharmacology Group I presentation

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  1. PharmacologyGroup I presentation Topic: Cisplatin

  2. Drug background • was first synthesized in 1845 • Alkylating agent • an inorganic complex formed by an atom of platinum surrounded by chlorine and ammonia atoms in the cis position of a horizontal plane

  3. Drug usage • This medication is used to treat: • metastatic testicular tumors • metastatic ovarian tumors • advanced bladder carcinoma • also used to treat other kinds of cancer

  4. Clinical trials Clinical trials which cisplatin have been involved in include:

  5. Clinical trials • Cisplatin has also been involved in clinical trials to determine its toxicity. • Omidvari et al., 2004 concluded their study by advising that cisplatin should be added to a list of agents causing hypokalemic paralysis. However clinical trials which have regulated the dose of cisplatin between 75 – 80mg/m² have shown that this helps minimise toxicity • Future clinical trials involving Cisplatin: • Cancer research in the UK are currently recruiting people for clinical trials involving cisplatin. These include: • Irinotecan & cisplatin for the treatment of ca of the penis • Cisplatin & temozolomide for children diagnosed with glioma • Cisplatin & 5-fluorouracil to prevent recurrence of anal cancer

  6. Pharmacokinetics • Vd = 0.17-1.47 L/kg • Route of Entry • Mainly by intravenous • Distribution organ • Kidney • Also high concentration of drug can be found in liver, intestine • Target • DNA synthesis • Little effect on protein and RNA synthesis • Elimination • By renal clearance • 15 to 30% of drugs will eliminate at first 2-4 hr • 20 to 80% of drugs will recoverd at the first 24hr

  7. Pharmacodynamics

  8. Factor affecting kinetics • Chemical factors • Lipophilicity • water soluble • Chirality • cis isomer provided relief and inhibited several forms of cancer • trans isomer is inactive • slowly changes from the cis to the trans form in aqueous solution • Protein binding capacity • rapidly bound to tissue and plasma proteins • protein-bound drug (nonfilterable): elimination rate declines rapidly, prolonged excretory phase

  9. Factors affecting kinetics • Biological factors • Dose • saturation of plasma-protein binding sites may lead to significance rise in the plasma concentration of free compound • increase toxicity • Age • Children are more sensitive to the effects of cisplatin • Disease • terminal half life of total platinum • 8.1 to 49 minutes (normal renal function) • 1 to 240 hours (patient with severe renal failure)

  10. Contraindications • A factor that renders the administration of a drug or the carrying out of a medical procedure inadvisable: • A previous allergic reaction to penicillin is a contraindication to the future use of that drug. • Because cisplatin is used to treat life-threatening malignancies,contraindications to its use are only relative and must be placed in the context of the patient's overall well-being.

  11. Contraindications • Include: • Renal failure • Severe bone marrow suppression • Peripheral neuropathy • Pregnancy • Hearing disorders • Allergic or anaphylactic-like reactions to platinum containing compounds.

  12. Toxicology Data • The principal target organ for cisplatin toxicity is the kidney: • This toxicity is manifested by reduced renal function and leads to serum electrolyte changes and pathological changes in the urine analysis. • Doses of cisplatin which produce changes in renal function may cause no histopathological changes. • Higher doses of the drug lead to interstitial nephritis. • Nephrotoxicity characterised by oliguria, azotaemia, renal tubular acidosis and acute renal failure may occur. • Electrolyte disturbances, particularly hypomagnesaemia and hypocalcaemia, may occur as a result of renal toxicity • Cisplatin also causes bone marrow hypoplasia and is ototoxic. Bone marrow depression may be severe, with decreased leucocyte and platelet counts.

  13. Toxicology Data • Neurotoxicity is also commonly seen with cisplatin: • Neurotoxicity includes peripheral neuropathy with numbness,tingling and decreased vibratory sensation.Autonomic neuropathy may also occur with gait difficulties, involuntary movements and loss of deep tendon reflexes. • Central nervous system toxicity includes confusion, extrapyramidal effects and focal convulsions progressing to grand mal convulsions. • Other reported effects of cisplatin neurotoxicity include tachycardia, acute respiratory failure, metabolic acidosis, transient elevation of alkaline phosphatase, and serum bilirubin • Prevention of cisplatin toxicity: • Hydration is considered important for the prevention of cisplatin toxicity. • Severe nausea and vomiting may be managed with antiemetics

  14. Reference • IPCSINTOX-Data bank • http://www.intox.org/databank/documents/pharm/cisplat/ukpid21.htm • BC Cancer Agency • http://www.bccancer.bc.ca/HPI/DrugDatabase/DrugIndexPro/Cisplatin.htm

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