Drug Metabolism Flashcards
Biotransformation?
Converting lipophilic drugs into hydrophilic drugs - so they can be e created by the kidney in the urine
Give an example of a active drug into an active metabolite?
Heroin to morphine - through hydrolysis
Hepatic vs extrahepatic sites of drug metabolism?
Hepatic:
• liver
Extrahepatic:
• lungs
• kidneys
• skin
• placenta
• bacterial flora
Which main enzyme is used in phase 1
CYP450
What happens during an oxidation reaction?
• gain of oxygen
• loss of hydrogen
• loss of electro.
What happens during a reduction reaction
• loss of oxygen
• gain of hydrogen
• gain of electron
What happens during a hydrolysis reaction?
Water breaks chemical bonds
Phase II - converts xenobiotics or phase I metabolites into conjugated products.
Conjugated products are?
• less toxic
• more water soluble
• polar
• biologically inactive
Examples of conjugation reactions?
• glucuronic acid
• glutathione
• methylation
• sulphate
• amino acid
these reactions are careless by transferase enzymes
What is the conjugation reaction for Aspirin
Glucuronic acid
What are the 2 conjugation reaction for Paracetamol
Glucuronic Acid & Sulphate
Neonates & young children have a decreased glucuronidation
capacity - due low levels
of these transferase enzymes
Which conjugation reaction occurs for paracetamol
Sulphate conjugation
