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ASSIGNMENT on Toxicity Concern of Combination of Paracetamol and Caffeine

ASSIGNMENT on Toxicity Concern of Combination of Paracetamol and Caffeine

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Published by Rinta Moon
METABOLISM OF PARACETAMOL AND CAFFEINE IN THE BODY
TOXITIES AND OTHER PROBLEMS OF CAFFEINE RELATED PARACETAMOL: HEPATOTOXICITY; NEPHROTOXICITY; PREGNANCY RELATED PROBLEMS; and REBOUND HEADACHE
METABOLISM OF PARACETAMOL AND CAFFEINE IN THE BODY
TOXITIES AND OTHER PROBLEMS OF CAFFEINE RELATED PARACETAMOL: HEPATOTOXICITY; NEPHROTOXICITY; PREGNANCY RELATED PROBLEMS; and REBOUND HEADACHE

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Published by: Rinta Moon on Feb 08, 2014
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ASSIGNMENT ON
Toxicity concern of combination of paracetamol and caffeine
Course name: Medicinal Chemistry II Course code: PHRM 304 Section 1 Semester: Fall 2012 SUBMITTED TO: Apurba Sarker Apu Senior Lecturer Department of Pharmacy East West University SUBMITTED BY: Joynab Akhter Jolly (ID: 2010-1-70-016) Bushra Rahman (ID: 2010-1-70-017) Zenifar Karim (ID: 2010-1-70-042) Jannat Mahal Rume (ID: 2010-1-70-048) Samiya Khondaker Rinta (ID: 2010-3-70-048) Submission date: 15th November, 2012
 
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INTRODUCTION
Paracetamol is the most widely used drug. It has mild analgesic (pain relieving) and antipyretic (fever reducing) properties. It is also known as acetaminophen and
 N 
 -acetyl-p-aminophenol (APAP). It produces analgesic action by elevation of the pain threshold and antipyresis through action on the hypothalamic heat regulating center of the brain. Caffeine is an alkaloid which is a theophylline - like xanthine derivative. By intermolecular association with paracetamol, caffeine increases the solubility and transmembrane permeation of paracetamol. It enhances the pain relieving effects of paracetamol (Square Pharmaceuticals, 2012). It has also an intrinsic power to raise vessel tone in the cranial of the brain, which provides another benefit to treat migraine and headache. So it is often combined with paracetamol in over-the-counter and prescription analgesics (Frey, 2003). This combination is used to treat mild to moderate pain including headache, migraine, neuralgia, toothache and dysmenorrhoea pains. It is also used for symptomatic relief of sprains and strains, rheumatic pain, fibrosis, muscular aches and pains, influenza, feverishness and feverish colds (Square Pharmaceuticals, 2012). However, according to the Chemical Research in Toxicology study of USA it has been recently found out that this combination increases the risk of paracetamol toxicity (BBC News, 2007).
METABOLISM OF PARACETAMOL AND CAFFEINE IN THE BODY
Paracetamol is metabolized primarily in the liver, where its major metabolites include inactive sulfate and glucuronide conjugates, which are excreted by the kidneys. A minor metabolite is  produced in minute amounts by cytochrome P450 isoenzymes in the liver and kidney. Cytochromes P450 2E1 (CYP2E1) and 3A4 (CYP3A4) convert paracetamol to a highly-reactive intermediate metabolite, N-acetyl-p-benzo-quinoneimine (NAPQI). Under normal conditions,  NAPQI is detoxified by conjugation with glutathione as shown in Figure 1.
 
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Caffeine is metabolized in the liver  by the cytochrome P450 oxidase enzyme system into three metabolic dimethylxanthines as shown in Figure 2. Each of these metabolites is further metabolized and then excreted in the urine (Dyson and May, 1959). Figure 1: Safe and unsafe metabolic pathways of paracetamol

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