Pharmacokinetics Flashcards
(26 cards)
How can you tell if drugs are weak acids?
Paired with a positive ion -
Ex: Na, Mag, Ca
How can you tell if drugs are weak bases?
Chloride or sulfate
What are the three plasma proteins? What do they bind to?
Albumin - primarily acids but can do any
a1-acid glycoprotein - basic
beta-globulin - basic
What conditions reduce serum albumin concentration?
-liver disease
-renal disease
-old age
-malnutrition
-pregnancy
What conditions INCREASE a1-acid glycoprotein?
surgical stress
MI
chronic pain
RA
advanced age
What conditions decrease a1-acid glycoprotein?
neonates
pregnancy
How does an increase or decrease in protein binding affect drug concentration?
decreased binding - increased drug
increased binding-decreased drug
What are 5 substrates of conjugation?
glycine
acetic acid
sulfuric acid
methyl group
glucuronic acid
What are two drugs that have enterohepatic transformation? what is it?
Reactivated by the intestine after undergoing conjugation
-diazepam
-warfarin
What is capacity dependent elimination?
dependent on liver enzymes
-Enzyme induction increases clearance
-Enzyme inhibition decreases clearance
What has a greater affect on a drug with a low hepatic extraction ratio, prolonged hypotension or cyp inhibition
CYP inhibition
Drugs with low and intermediate hepatic ER
Paralytics
Benzo’s
Barbiturates
Methadone
Alfentatnil
Drugs with high hepatic ER
Narcs except alfentanil and methadone
ketamine
locals
Do you need more or less of a drug with enzyme inducers?
More drugs because it decreases the drug concentration
Do you need more or less of a drug with enzyme inhibitors?
less because there is an increase in the drug in the plasma concentration
Examples of enzyme inhibitors?
grapefruit juice
SSRI
Erythromycin
Ketoconazole
Isoniazid
Omeprazole
Types of drugs that metabolized by pseudocholinesterase’s?
Succ + mivacurium
Ester type locals (one i )
Drugs that undergo non specific plasma esterase metabolization?
Clevidipne
Esmolol
Remi
Remi
Etomidate
Atracurium
What drug undergoes alkaline phosphatase hydroloysis?
Fospropofol
What is potency and how is it measured?
The dose required to achieve a desired clinical effect?
On the dose response curve, if a drug is more to the left, is more or less potent
More potent which has a increased receptor affinity and requires less of a drug
What is efficacy ?
a measure of the intrinisc ability of a drug to produce a clinical effect
On the dose response curve, if a drug has a higher plateau, does it have a higher or lower efficacy?
higher so less drug is needed
What does the slope tell you on the dose response curve?
steeper slope= means a small change in the medication can have a great effect
