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BASIC PROCESSES OF DRUG THERAPY

R. G. ALVERO, MD., MSc, PSECP 2012 - 2013

PROCESS INVOLVED IN DRUG THERAPY


1. Pharmaceutical Process 2. Pharmacokinetic Process 3. Pharmacodynamic Process 4. Therapeutic Process

PHARMACEUTICAL PROCESS
Is the drug getting from the formulation into the patient?

PHARMACEUTICAL PROCESS

Is the drug getting to its site of action?

PHARMACODYNAMIC PROCESS

Is the drug producing required pharmacological effect?

THERAPEUTIC PROCESS
Is the drug pharmacological effect being translated into a therapeutic effect?

PHARMACEUTICAL PROCESS

What can determine whether a drug is absorbed from the gut or not?

PHARMACOKINETIC PROCESS
relationship between the dose & the concentration of unbound drug based on the abstract mathematical modelling of the fine course of drug concentrations in theoretical compartments Physiologically based approach?

PHARMACOKINETIC PROCESS
Fundamental Parameters:
Clearance

Volume of Distribution

PHARMACOKINETIC PROCESS

If the total body clearance, VD & the fraction excreted unchanged are known, the rest can be predicted

PHARMACOKINETIC PROCESS
Drug A Parameters Total Clearance (L/hr) 80 VD (L) 500 Fraction excreted unchanged 0.1 Liver Blood Flow (L/hr) 9.0

PHARMACOKINETIC PROCESS
Predicted Renal Clearance (L/hr) Hepatic Clearance (L/hr) Hepatic Extraction Ratio Max Oral Bioavailability Affected by Liver Enzymes when given PO Affected by Liver BF when given IV Dose in Liver Disease Dose in Renal Disease Half Life Dosing Schedule Time to Reach SS ___ ___ ___ ___ ___

___ ___ ___ ___ ___ ___

PHARMACOKINETIC PROCESS
Predicted
Renal Clearance (L/hr) *fraction excreted unchanged = renal Cl total Cl
Renal Cl = fraction excreted unchange x total CL = 0.1 x 80 = 80

PHARMACOKINETIC PROCESS
Predicted
Hepatic Clearance (L/hr)
* fraction excreted unchanged = (1 fe) (1 - 0.1) = 0.9

* fraction metabolized = hepatic Cl total Cl


Hepatic Cl = 0.9 (80) = 72 L/hr

PHARMACOKINETIC PROCESS
Predicted Hepatic Extraction Ratio * Hepatic Extraction Ratio = hepatic Cl hepatic BF

= 72/90 = 0.8

PHARMACOKINETIC PROCESS
Predicted
Max Oral Bioavailability * fn = (1-E4) = 1 0.8 = 0.2 = (fg) (fn) = 1 x 0.2 = 20%

*F

PHARMACOKINETIC PROCESSES
Predicted Renal Clearance (L/hr) Hepatic Clearance (L/hr) Hepatic Extraction Ratio Max Oral Bioavailability Affected by Liver Enzymes when given PO Affected by Liver BF when given IV Dose in Liver Disease Dose in Renal Disease Half Life Dosing Schedule Time to Reach SS 8 72 0.8 20 Yes Yes Yes No 4 6 20

PHARMACOKINETIC PROCESS
Ask the following question to predict clinical situations likely to require care: 1. It is mainly metabolized? Or mainly excreted? 2. If metabolized, does it have high or low hepatic Cl? 3. What is the t 4. Are there complicating factors such as active metabolites?

PHARMACODYNAMIC PROCESS

How do drugs produce effects?

PHARMACODYNAMIC PROCESS
Types of Pharmacological Actions of Drugs 1. Direct effect on a receptor 2. Indirect alteration of the effect of an endogenous agonist 3. Inhibition of transport process 4. Enzyme inhibition 5. Enzyme activation 6. Misc.

THERAPEUTIC PROCESS

Translation of pharmacological effect therapeutic effect

If a patient appears not to be responding to treatment with a particular drug analyze the processes if drug therapy

Thank you for your attention!!!

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