Drug Interaction

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Drug Interactions

DR dra I A ALIT WIDHIARTINI, Apt., M.Si


Objective
• Identifiy the priciples of drug interaction
• List of several categories of the drug interaction
Definition
• An interaction is said to occur when the effects of
one drug are changed by the presence of another
drug, herbal medicine, food, drink or by some
environmental chemical agent.
DRUG INTERACTION

Pharmaceutics

Pharmacokinetics
•ADME
•Effects
•Duration of action
Pharmacodynamic
Drug Absorption Ix
Effects of changes in
gastrointestinal pH: ionization,
polarity
Adsorption, chelation and other
complexing mechanisms
Changes in gastrointestinal
motility

Induction or inhibition of drug


transporter proteins

Malabsorption caused by drugs


The pathway drug use to enter the circulation
Drug distribution Ix

Protein-binding
interactions

Induction or inhibition of
drug transport proteins
Drug metabolism (biotransformation) Ix
Changes in first-pass metabolism

• Changes in blood flow through the liver


• Inhibition or induction of first-pass metabolism

Enzyme induction

Enzyme inhibition

Genetic factors in drug


metabolism
Cytochrome P450 isoenzymes and
predicting drug
Drug excretion Ix

Changes in urinary pH

Changes in active renal tubular


excretion
Changes in renal blood flow
Biliary excretion and the entero-
hepatic shunt
• Enterohepatic recirculation
• Drug transporters (P –glycoprotein)
Ix due to changes in renal transport
Inhibitors and Inducers of P glycoprotein

• Inhibitors
– Atorvastatin
– Clarithromycin, Erythromycin
– Dypiridamole
– Itraconazole, Ketoconazole
– Propafenone
– Quinidine
– Valspodar
– Verapamil
• Inducers
– Rifampicn
– St John wort (Hypericum perforatum) 6
Pharmacodynamic Ix

Additive or synergistic
interactions

Antagonistic or opposing
interactions

Drug or neurotransmitter
uptake interactions
Drug-herb interactions

• St John’s Wort (Hypericum perforatum: serotonergic


• Induce CYP 450 isoenzyme CYP3A4 and Pglycoprotein
• <ciclosporin & digoxin
Drug-food interactions

• Cruciferous vegetables and charcoal-broiled meats


• Grapefruit juice processed
• > level Ca channel blocker: Felodipine
• Fexofenadine
Effect Exercise to the PK Drugs

• Orally given drugs – No substantial effects


• I.M., S.C, transdermal, and inhalation sites : alters
physiological parameters : CO, blood flow to active
skeletal muscle
Summary
• If maintainaing the plasma concentration of a
drug at a certain level is important:
Consider the alternative drugs and physical activity for
patients safety

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