Pharmacokinetics

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WSUPharmacy2015 Plus on June 2, 2012

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Pharmacokinetics

Side Chain Oxidation
Microsomal Oxidation: CYP450
Addition of a hydroxyl to a non-terminal carbon
Ex. Pentobarbital (Sedative)
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Definitions

Side Chain Oxidation Microsomal Oxidation: CYP450
Addition of a hydroxyl to a non-terminal carbon
Ex. Pentobarbital (Sedative)
Aromatic Hydroxylation Microsomal Oxidation: CYP450
Addition of a hydroxyl to a aromatic ring
Ex. Tylenol (Anti-pyretic)
N-oxidation Microsomal Oxidation: CYP450
Addition of a ketone to an amine
Ex. Trimethylamine (Tricyclic anti-depressant)
Sulfoxidation Microsomal Oxidation: CYP450
Addition of a ketone to a sulfur
Ex.Chlorpromazine (Anti-psychotic)
N-dealkylation Microsomal Oxidation: CYP450
Replacement of a group with a hydrogen atom
**NEXT to a hetero N atom**
Ex. Aminopyrine (Anti-pyretic)
O-dealkylation Microsomal Oxidation: CYP450
Replacement of a group with a hydrogen atom
**NEXT to a hetero O atom**
Ex. Acetophenetidin (Anti-pyretic)
S-dealkylation Microsomal Oxidation: CYP450
Replacement of a group with a hydrogen atom
**NEXT to a hetero S atom**
Ex. 6-methyl thiopurine (Anti-cancer)
Deamination Microsomal Oxidation: CYP450
Replacement of an amine group with a ketone
**NEXT to a hetero amine group**
Ex. Amphetamine (Stimulant)
N-hydroxylation Microsomal Oxidation: CYP450
Changing a H atom to a hydroxyl group on a N atom
Desulfuration Microsomal Oxidation: CYP450
Replacing a double bonded S atom with a ketone
Ex. Parathion (Organophosphate insecticide)
Alcohol Oxidation Non-Microsomal Oxidation: CYP450
Changing of a hydroxyl group to a aldehyde
Ex. p-nitrobenzyl alcohol (Food Preservative)
Aromatization Non-Microsomal Oxidation: CYP450
Aromatizing a ring
Ex. Androgenic>>>Estrogenic (A-ring cholesterol conversion)
Nitroreductase Reduction: CYP450
Replacement of a nitro with an amine
Ex. Chloramphenicol
Azoreductase Reduction: CYP450
Splitting of an azo group
Ex. Protonsil
Alcohol Dehydrogenase Reduction: CYP450
Replacement of a hydroxyl with a H atom
Ex. Chloral hydrate (Sedative Hypnotic)
Hydrolysis Hydrolysis:
Splitting off a chain from an O atom
Ex. Procaine (Local anesthetic)
Glucuronide Synthesis (Glucuronidation) Microsomal: ONE OF THE MOST COMMON
Addition of a glucose molecule
Ex.
Oxygen: Lorazepam
Nitrogen: Meprobromate
Carbon: Phenylbutazone
Acetylation Conjugation
Acetyl CoA splits with an addition of an amine
Ex. Isoniazid, Hydralazine
Conjugation with Glycine Addition of a glycine molecule
1st drug metabolism reaction
Ex. Benzoic acid to Hippuric acid
Conjugation with Sulfate Addition of a sulfate group
Ex. Acetaminophen
Conjugation with glutathione Addition of glutathione to a drug
**MOST important for prevention of drug toxicity**
O- S- and N-methylation Addition of a methyl group to a heteroatom

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