PHBP | Part 2 & 3 Flashcards
The enzymatic or biochemical transformation of the drug substance to (usually less toxic) metabolic products, which may be eliminated more readily from the body
METABOLISM
Principal site of metabolism
Both synthesizing and eliminating organ
LIVER
Basic unit of liver
Liver Lobule
A network of interconnected lymph and blood vessels
PARENCHYMAL CELLS
Perfused blood in the liver
Hepatic artery
Carries oxygen in the liver
Hepatic artery
Collects blood from various segments of GIT that perfuse in the liver
Hepatic Portal Vein
Carries nutrient to the liver
HEPATIC PORTAL VEIN
Large vascular capilaries
SINUSOIDS
Facilitates drug and nutrient removal before the blood enters the general circulation
SINUSOIDS
Endothelial lining of the sinusoids
Part of the Reticulo Endothelial system
Kupffer cells
Phagocytic macrophages
Kupffer cells
secreted by the liver
Bile Acids
3 Major Components of a drug biotransformation
Reactant (Drug/Xenobiotics)
Product (Metabolite)
Reaction catalyst (Enzymes)
5 Types of Metabolites
Inactive Metabolite
Retain Similar Activity
Altered Activity
Bioactivated Metabolite
Reactive Metabolite
Birth
Sulfation
1st Week
Reduction. Oxidation
1 month
Acetylation
2 months
Glucoronidation
3 months
Glycine, Glutathione, Cysteine Conjugation
Presystemic metabolism
First Pass Effect
Initial Biotransformation of an active drug BEFORE reaching the systemic circulation
FIRST PASS EFFECT
the final LOSS of the drug substance or its metabolites from the body
EXCRETION
Are excreted mainly by renal excretion, into the urine
NONVOLATILE DRUGS
Gaseous anesthetics, or drugs with high volatility, are excreted via lungs into expired air
VOLATILE DRUGS
Excretion Pathway
Anion, cations, non-ionized molecules with lipophilic polar groups & those with MW > 500
Biliary Excretion
Excretion Pathway
For drugs poorly absorbed in the intestines
Biliary Excretion