Principles Of Pharmacokinetics: 3 Questions Answered

821 words - 4 pages

Unit 2 C. Principles of Pharmacokinetics
Objective 1: Define bioavailability and describe factors that can alter absorption.
Bioavailability is the fraction of the dosage form that reaches systemic circulation after any route of administration. In this particular study, acetaminophen was administered orally, intravenously, and rectally in healthy men aged 18 to 45 and the pharmacokinetic parameters were compared for each route. The study assumed IV bioavailability to be 100%. The bioavailability of the oral dose was 89% and 72% for the rectal dose. Drug interactions, intestinal motility, gastric pH, and stomach emptying can all alter absorption. In this study, there were key exclusion ...view middle of the document...

In this study, the half-life for IV administration was 2.17 hours, 2.53 hours for oral administration, and 3 hours when given rectally. The clearances were 20.7, 24.6, and 32.5 L/hr, respectively. These numbers makes sense in terms of the routes of administration. When drugs are administered orally and rectally, they cannot begin to get eliminated until they are absorbed. IV administration skips the absorption part because the drug is delivered right to systemic circulation, so it can essentially begin to get eliminated right away and therefore have the shortest half-life, while the other routes cannot. Since IV drugs can be eliminated right away, they will have smaller clearances because there is less time to clear half the amount of drug from the plasma. Rectally administered acetaminophen had the longest half-life, which again makes sense because it takes the longest for a drug to be absorbed via that route. In the rectum, there is potential for increased mucosal lining and a decreased number of blood vessels, making it harder for drugs to be absorbed.
Objective 3: Identify key enzymes involved in metabolism and their role in drug-drug interactions.
Metabolism refers to the body’s ability to break down a chemical substance and convert it to something that is more able to be excreted, usually by making it more polar. For acetaminophen (referred to as paracetamol in this study), the major site of its metabolism is the liver. Paracetamol is metabolized to paracetamol glucuronide and paracetamol sulphate, which are both inactive metabolites that get...

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