Pharmacology lecture 6 0.0 / 5 ? BiologyDrug metabolism and eliminationUniversityNone Created by: willmiddlehamCreated on: 27-03-15 16:19 What is enterohepatic recirculation? Where drugs hat have been eliminated in the bile can be reabsorbed in the GI tract 1 of 27 Drugs with.................... and/or........... degree of................ to.......... .............. will tend to stay in systemic circulation high Mr, high, binding, plasma proteins 2 of 27 What are the two main binding proteins? Albumin, Alpha 1 acid glycoprotein 3 of 27 Where is albumin produced? Liver 4 of 27 What does albumin bind? acidic drugs 5 of 27 What does albumin cause? DECREASE in malnutrition and cirrhosis 6 of 27 What are the normal ranges of albumin in the blood? 3.5-5 g/dL 7 of 27 Where is alpha 1 acid glycoprotein produced? Liver 8 of 27 What does alpha 1 acid glycoprotein bind? Basic drugs 9 of 27 What are the normal ranges of alpha 1 acid glycoprotein in the blood? 0.4-1.1 mg/ml 10 of 27 If there are LARGE amounts of drug binding proteins in the blood... LOWER DISTRIBUTION because more protein bound to drug 11 of 27 If there are SMALL amounts of drug binding proteins in the blood... more DRUG to TISSUE because less bound to protein 12 of 27 What are the Phase I drug metabolising enzymes? Cytochrome P450 family 13 of 27 What are the Phase II drug metabolising enzymes? UDP-glucuronosyltransferases 14 of 27 What is the goal of drug metabolising enzymes? Make a drug more water-soluble to be excreted in the urine (metabolite) 15 of 27 What do prodrugs contain? They contain an ester group which are hydrolysed in vivo 16 of 27 How do you calculate volume of distribution? Vd = total amount of drug in body/ drug blood plasma concentration (time 0) 17 of 27 Ke = gradient of the log-transformed concentration-time profile (elimination rate constant) 18 of 27 How do you eliminate volatile gases? Exhalation 19 of 27 How do you eliminate water-soluble drugs? Urine/bile 20 of 27 How do you eliminate lipid-soluble drugs? change to water-soluble then out via urine/bile 21 of 27 What is the half-life? time it takes for concentration of a compound to reach 50% of its current value 22 of 27 Half life = 0.693/Ke 23 of 27 How do you calculate total clearance? Total Cl = Hepatic Cl + Renal Cl + other Cl 24 of 27 What is clearance? volume of plasma cleared of compound per unit of time 25 of 27 Clearance: IV dosing Cl= IV dose/IV AUC 26 of 27 Clearance Cl = Dose x F / Oral AUC 27 of 27
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