Pharmacokinetics
If a drug saturates enzymes, what order of kinetics will the enzyme follow?
Zero Order Kinetics (constant amount of drug eliminated / time)
Measure of the intrinsic ability of a drug to elicit a given clinical effect
Efficacy
Potency is the dose required to achieve a given clinical effect
What herb is commonly used for headaches and rheumatoid arthritis but inhibits platelet activity and reduces bioavailability of iron?
Feverfew
-D/t platelet activity inhibition, avoid with pts on heparin, warfarin, NSAID, aspirin, and vitamin E
Type of metabolizer that has 1 normal allele and 1 reduced allele OR 2 reduced alleles
What are intermediate metabolizer?
Three types of phase 1 metabolism
Oxidation, Reduction, Hydrolysis
The process in which a polar, water-soluble substrate is added to a molecule
Conjugation (phase 2 metabolism): produces a water-soluble, inactive molecule for excretion
Ex of substrates: glucuronic acid, glycine, acetic acid, sulfuric acid, methyl groups
Phase 1: Oxidation (removes electrons), reduction (adds electrons), hydrolysis (adds water to split it apart)
Ration between LD50 and ED50
St Johns Wort
Genetic variability occurs in which CYP?
CYP2D6
Fully elimination usually occurs after this many half lifes
4-5 half lifes to get to 95% drug elimination
What route of administration has the lowest bioavailability?
Intrathecal intentionally because you act on nerves
What type of bond do noncompetitive drugs use to bind between antagonist and receptor site?
Covalent
Echinacea
-Immunosuppressive actions of corticosteroids and cyclosporine may antagonized echinacea
-Inhibition of enzymes: avoid rifampin, phenytoin, and phenobarbital
Mutation in RYR1 leads to this condition..
Malignant Hyperthermia
Two conditions that increase a1 acid glycoprotein
Inflammatory disease
Malignancy
Base Drugs are more bound to which type of protein?
a1-acid glycoprotein
Beta globulin
(Bonus Q: Acid drugs are more bound to which type of protein?)
Competitive
-Ketamine is a type of noncompetitive antagonist
3 Herbs that potentiate sedative effects
Kava Kava, Valarian, St Johns Wort
Red heads need more anesthesia due to a mutation in this gene
Melanocortin-1 Receptor
what drug displaces unconjugated bilirubin from albumin in neonates leading to bilirubin encephalopathy?
5 Drug characteristics of transdermal administration
Water and lipid solubility
Smaller molecular weight
pH 5-9
Absence of histamine releasing effects
Daily dose < 10 mg
4 drugs that do not interact with receptors
Antacids, chelating drugs, iodine, sodium bicarbonate
4 herbs that contribute to bleeding
Garlic, ginger, ginkgo biloba, and willow bark
"Gee Whiz, Look at all that Bleeding"
Pseudocholinesterase metabolizes which three drugs
Succinylcholine, mivacurium, and ester local anesthesia
6 highly bound protein drugs