Drug Metabolism-phase 1 And 2 Flashcards
What are the functional groups that are added or unmasked in during phase 1 of drug metabolism
OH, SH, COOH, NH2
The reactions that occur during phase 1 reaction of drug metabolism are ?
Key(5 reactions)
Oxidative, reductive, hydrolytic, cyclisation and decyclisation
The endogenous substrate groups that are conjugated to the drug during phase 2 of drug metabolism are?
Key(5 groups)
Glucoronide, amino acid, acetate, sulfate, glycine
The microsomal enzymes in drug metabolism are?
Key(4 of them in the slide)
Epoxide hydroxylases, cytochrome p450, ugt, monooxygenases
5 drugs that induce microsomal enzymes activity
Rifampicin, phenytoin, phenobarbital, ethanol, carbamazepine
Microsomal enzymes are found in?
The smooth endoplasmic reticulum of liver, lungs, kidney and GI mucosa
Non microsomal enzymes are found in?
The cytoplasm and mitochondria of hepatic cells and other tissues like blood
Two groups of non microsomal enzymes
Esterases, amidases
What does the enzymes of the cytochrome p450 system contain?
And where in the cell are they found ?
Heme containing protein
Bound to the membrane
The CYP has how many families?
Subfamilies?
Genes?
18
44
57
What CYP is involved in a larger number of drug metabolism compared to other enzymes ?
CYP3A4
MAOI means?
Monoamine oxidase inhibitors
CYP inhibitors examples
Monoamine oxidase inhibitors, cimetidine, isoniazid
High level of a certain drug causes grey baby syndrome. What is this drug ?
Chloramphenicol
Grape juice inhibits what drug ?
Felodipine
First pass effects lead to ?
The amount of drug absorbed being lesser than the amount of drug reaching the systemic circulation
Which method of drug administration provides the highest bioavailability for drugs ?
Intravenous administration
Four drugs with very high first pass effect ?
Lidocaine, morphine, propranolol, nitroglycerin
CYP inducers
Key (4 in the slide)
Carbamazepine, barbiturates, rifampin, cyclophosphamide
The major and most important organ in the excretion of drugs is ?
Kidney
The two drugs excreted via the bile/large intestine according to the slide are ?
Vancomycin and vincristine
Drugs excreted via the saliva
Key (5+1)
Diazepam, lithium, caffeine,theophylline, phenytoin
Alcohol is also an honorary mention
For drugs to be excreted via the eyes, three conditions must be met. What are they ?
Non protein bound, unionised and lipophilic
The skin excretes what drugs
Key( 7 of them)
Cocaine, alcohol, lead, mercury, salicylic acid, benzoic acid and antipyrine
