pharm part1 Flashcards
what is the pKa
pH at which the ionized and unionized concentrations are equal
if pH < pKa, what is favored: the protonated or the unprotonated form
protonated
if pH > pKa, what is favored: the protonated or the unprotonated form
unprotonated
what is the therapeutic index formula
TD50/ED50
bond strength is directly proportional to specificity. true/false?
false. it is indirectly proportional
flux is directly proportional to specificity. true/false?
true
Kd is directly proportional to drug binding
affinity. true/false?
false. it is indirectly proportional
drug safety is directly proportional to drug therapeutic index. true/false?
true
Volume of Distribution (Vd) is directly
proportional to the concentration of drug
outside of the systemic circulation. true/false?
true
what is the definition of volume of distribution
apparent volume of a drug
what is clearance
predicts rate of elimination in relation to drug concentration
in first order elimination, which value is constant
clearance
in zero order elimination, which value is constant
rate of elimination
what 3 meds use zero order elimination
ethanol
phenytoin
aspirin
what 4 parameters affect passive diffusion
molecular weight
pKa
lipid solubility
plasma protein binding
4 basic mechanisms for transmembrane signaling
lipid soluble diffusion to intracellular receptor
ligand binding to RTK
ligand gated ion channel
GPCR
how many trans-membrane alpha helixes does a GPCR have
7
what are the 3 major drug efflux transporters in the ABC family
B, C, G
what is the major site of exclusion in the blood-brain barrier
vascular epithelium
what enzyme is majorly implicated in phase 1 of metabolism
cytochrome P450
if a drug X enhances synthesis of CYP450, and the enzyme deactivates another drug Z, what happens to the effect of drug Z
decreased drug effect
if a drug X enhances synthesis of CYP450, and the enzyme activates another drug Z, what happens to the effect of drug Z
increased drug effect
what is pharmacokinetics
the effects of the body on a drug
what is pharmacodynamics
the effects of the drug on the body
what is pharmacogenomics
the primary reason patients respond differently to the same drug
what is pharmacology
the study of the effects of drugs on the body
what are the 6 neurotransmitter classes
esters - acetylcholine
monoamines - norepinephrine
amino acids- glutamate
purines - adenosine
peptides - substance P
inorganic gases - nitric oxide
where is the location of the ganglia of the sympathetic ANS
close to the spinal cord
where is the location of the ganglia of the parasympathetic ANS
in the visceral effector organs
what enzymes does alpha-1 receptor activate
phospholipase C
what enzymes does beta-1 receptor activate
adenylyl cyclase
what enzymes does beta-2 receptor activate
adenylyl cyclase
the gut has its own nervous system called the
enteric nervous system
alpha1 receptor activation leads to smooth muscle contraction. what are the second messengers produced by agonist binding to alpha-1 receptors
DAG
IP3
give an example of indirect acting adrenergic agonist
amphetamine
give 2 examples of adrenergic antagonist drugs
phentolamine
prazosin
labetalol
what is the important thing to note about phenoxybenzamine (adrenoceptor antagonist drug)
forms irreversible covalent bonds
what effect does beta agonists have on the blood vessels
opposes beta2-mediated vasodilation
which beta blocker is ultra short acting
esmolol
which betablocker is safer in COPD and diabetic patients
metoprolol
atenolol
what is the effect of cholinomimetics on the eye
miosis
increase intraocular drainage
what is the effect of cholinomimetics on the CV
vasodilation
reduction in PVR
bradycardia if given in large doses
what indirect acting cholinomimetic is a simple alcohol
edrophonium
give 2 major uses of indirect acting cholinomimetics
eye disease
GI/Urinary tract
NMJ
atropine overdose
what are the s/s of organophosphate exposure
SLUDGE-M
what are the s/s of poisonous mushroom exposure
SLUDGE-M
what are the s/s of atropine overdose
BRAND
blind, red, absent bowel sounds, nuts, dry