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L3 Hepatic Metabolism / Renal Excretion Dose - 1st Pass - Excretion -…
L3 Hepatic Metabolism / Renal Excretion
Dose - 1st Pass - Excretion - Metab = Plasma Conc
Metabolism
Heptaic Clearance (CLH)
Renal Excretoin (CLR)
Pathways
Phase 1
Non-synthetic
[O], [OH], [H]
Phase 2
Synthetic
e.g. conjugations
glucuronic acid
sulphate
glutathione
Total Drug Clearance (CLT)
Definition
: Conversion of
lipid soluble
drug
into polar metabolites
for excretion
Usually inactive
Drug Metabolizing Enzymes
Microsomal Mixed Functoin Oxidase (MFO)
Found in SER of Hepatocytes
Microsomal
Gucuronyl transferase
Glucuronidation mostly in liver
Enzyme found in
many places
Non-microsomal
Conjugating Enzymes
Hepatic Metabolism Factors
Pharmacological
Inhibition
Induction
Physiological
Age
Neonates
Metabolize faster
Children
Elderly
Metabolize slower
Pathological
Liver disease
Renal Excretion Factors
Overdose
Paracetamol
1. Sulfate Conj
2. Glucuronic Acid Conj
N-OH-Paracetamol > NAPQI
3. Glutathione Conj
Mercapturic Acid Conj
Excreted in urine
4. Nucleophilic cell
Hepatic Necrosis
OD / Poisoning
N-acetylcysteine within 8 - 16h