Problemset 1-1

# Problemset 1-1 - kg adult Vd = 130 L Clearance = 36 L hr...

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1) Estimate the behavior of this drug in the body during: a) Oral absorption b) Liver passage (potential phase I + II reactions) a) Good (drug is generally lipophilic) b) Phase I: a. Ester hydrolysis b. Oxidation c. Demethylation Phase II: a. Glucoronidation b. Sulfation 2) Which drug has the higher efficacy? Both drugs have the same efficacy (they achieve the same maximal response), however, drug A has the higher potency (less drug is required to achieve maximal efficacy).

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A 35 kg child in an ER on an i.v. infusion requires immediate treatment with the antiarrhythmic drug procainamide. The textbook lists the following pharmakokinetic values for procainamide in a 70
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Unformatted text preview: kg adult: Vd = 130 L Clearance = 36 L / hr Oral availability = 83% Therapeutic concentration = 5 mg/L 1. What iv loading dose should be administered? 2. What constant infusion rate is required to maintain the therapeutic concentration? 3. What is the predicted half-life of the drug in the child? Answers: The patient is half the weight of the average adult => Vd and clearance witll be ~ one half the given values. Drug is given i.v. => oral availability irrelevant: 1. Loading dose = Vd x Cp = 130L/2 x 5 mg/mL = 325 mg 2. Infusion rate = Cl x Cp = (36 L / hr)/2 x 5 mg/mL = 90 mg/hr 3. T1/2 = ln2 x Vd/Cl = 0.693 x 130 L / 36 L/hr = 2.5 hrs...
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## This note was uploaded on 04/13/2010 for the course BIMM BIMM118 taught by Professor David during the Winter '09 term at UCSD.

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Problemset 1-1 - kg adult Vd = 130 L Clearance = 36 L hr...

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