Erin's Pharm Exam 1; preop Flashcards
Drug effect relates to ____
number of bound receptors
Agonists bind through three types of bonds
ion, hydrogen, van der waals
and covalent (some do this but we dont like it because we want reversible bonds)
How does competitive antagonism shift the dose response curve?
Shift dose response curves to the right
Increasing amounts of this progressively inhibits the agonist
Competitive antagonism
Non-competitive antagonism
Even high concentrations of the agonist can not cause the agonist effect
Inverse agonist drugs (6)
LMNCPP
Loratadine, metoprolol, naloxone, cetirizine, prazosin, propanolol
This type of agonists causes less response than the agonist even at supramaximal doses
Partial agonist
Inverse agonist
compete for the same site as the agonist but produce the opposite effect; were categorized as agonists
Does the number of receptors stay the same?
No! It can increase or decrease depending on age, disease state, comorbidity, drug therapy, etc.
What are 4 examples of the number of receptors changing?
-Tachyphylaxis
-Albuterol treatment for asthma (down regulation of receptors due to repetition)
-Pheochromocytoma (decreased beta receptors in response to catecholamines)
-Ephedrine
How are receptor types classified?
By location!
Receptor locations (3)
-Lipid bilayer
-Intracellular proteins
-Circulating proteins
This receptor location is common for anesthesia drugs, opioids, benzos, beta blockers, catecholamines and NMBD (B-BACON)
Lipid bilayer
This receptor location is common for insulin, steroids and milrinone (SIM)
intracellular proteins
This receptor location is common for anticoagulants to bind to
circulating proteins
What the body does to the drug
pharmacokinetics (ADME)
What type of drugs bind primarily to albumin?
acidic drugs
What do alkalotic drugs primarily bind to?
Alpha 1-acid glycoprotein
What do you call it when only “free” (unbound) drugs can cross cell membranes?
distribution
What do you call it when only a free drug can determine concentration available to receptor?
Potency
What can cause decreased plasma proteins?
age, hepatic disease, renal failure, pregnancy
Drugs that are plasma protein bound ____% or greater can be impacted by abnormal plasma protein concentration
90
If a normal free fraction of a drug is 2% and we lose 50% of proteins, then the free fraction of drugs is __%
4%
This drug is highly bound to plasma proteins and has a small volume of distribution
warfarin