Pharmacology Flashcards
How does Km relate to affinity
inversely related
What is the formula for half life?
0.7Vd/CL
Reduction, oxidation, hydrolysis with P450- what kind of metabolism
Phase I
Glucoronidation, Acetylation, sulfation- what kind of metabolism
Phase II
What type of metabolism is defective in geriactric patients?
phase I
Efficacy vs potency
Efficacy- maximal effect a drug can produce
potency- amount of drug needed for a given effect
What type of receptor is a nicotinic Ach receptor?
ligand-gated Na/K channel
What type of receptor is a muscarinic ACh receptor?
GPCR
What type of neurotransmitter is released on postsynaptic, 2nd neuron for parasymp?
ACh M
What type of neurotransmitter is released on postsynaptic, 2nd neuron for sympathetic, sweat glands?
AChM
What type of neurotransmitter is released on postsynaptic, 2nd neuron for sympathetic, cardiac?
NEab
What type of neurotransmitter is released on postsynaptic skeletal muscle?
AChN
What type of neurotransmitter is released on postsynaptic, 2nd neuron for sympathetic, renal vasculature and smooth muscle?
D
What type of neurotransmitter is released on adrenal medulla?
ACh N
What are the two types of nicotinic receptors? where are they found?
NN- autonomic ganglia
NM- NMJ
What autonomic receptors are Gi (3)
M2, a2, D2
What autonomic receptors are Gq (5)
H1, a1, V1, M1, M3
What does dopamine do to renal vascular smooth muscle?
relaxes
What muscarinic/adrenergic receptors are found on the heart? what is the effect?
M2
decr heart rate and atrial contractility
B1/B2
incr HR, contractility
What receptors affect pupillary contraction?
a1- contraction of dilator muscles (mydriasis)
M3- pupillary sphincter muscle contraction (Miosis)
Where are the vasopressin receptors found?
V1- vascular smooth muscle contraction
V2- incr H2O permeability and reabsorption of kidneys
What adrenergic receptor promotes renin release?
B2
What adrenergic receptor affects aqueous humour production?
B2- incr production
What adrenergic receptors are found on the uterus?
B2- decr tone
a1- incr contraction
What receptors are on vascular smooth muscle?
a1- contraction
V1- contraction
Bethanechol
direct cholinomimetic agonist
ileus and urinary retenthion
Pilocarpine
direct cholinomimetic agonist
glaucoma, pupillary constriction, relief intraoc pressure
Methacholine
direct cholinomimetic agonist
asthma challenge test
Neostigmine
anticholinesterase
long-acting, quarternary (not lipid sol)
reversal NMJ blockade, myasthenia gravis, postop ileus, urinary retention
Pyridostigmine
anticholinesterase
Myasthenia gravis
doesnt penetrate CNS
Donepezil
anticholinesterase
Alzheimers (incr ACh)
lipid sol- ternary amine
Edrophonium
anticholinesterase
short acting
used to diagnose myasthenia gravis
What is the antidote for organophosphate poisoning?
atropine- competitive inhib (does not prevent muscle paralysis- nicotinic)
praloxidime- needs to be given early
Diarrhea, urination, miosis, bronchospasm, bradychardia, lacrimation, sweating, salivation, muscle and CNS excitation
organophosphate poisoning
irreversibly inhibits AChE
Atropine
muscarinic antagonist (treats bradychardia and opthalmic)
Benzotropine
muscarinic antagonist
used to treat parkinson, acts on CNS
Scopolamine
muscarininc antag
motion sickness
Ipratropium
muscarinic antag
respiratory aplications
oxybutynin
muscarinic antag
decr urgency, bladder spasm
darifenacin
muscarinic antag
decr urgency, bladder spasm
Glycopyrrolate
musarinic antag
reduce airway secretion, drooling, peptic ulcer
What is the toxicity of atropine?
Hot as a hare dry as a bone Red as a beet Blind as a bat Mad as a hatter
Epinephrine
Can stim all 4, depends on dose Low dose: b>a Med does: b1, b2, a1 high dose: a1 anaphlaxis
Norepinephrine
a1, a2, b1 (no b2)
treats hypotension
Dobutamine
B1>B2, a
used to treat heart failure, stress test
Phenylephrine
a1>a2
hypotension, decongestion, mydriasis
Albuterol
B2>b1
asthma
Salmeterol
B2>b1
asthma- long acting
Terbutaline
b2>b1
prevent uterine contractions
isoproterenol
b1=b2
Norepinephrine vs isoproterenol effect on HR, BP
NE: incr BP, reflex bradycardia
Iso: decr BP, incr PP, incr BP
Clonidine
a2 agnoist
hypertensive urgency
a-methyldopa
a2 agnoist
hypertension in pregnancy
phenoxybenzamine
a blocker (irreversible) Pheo-preop
phentolamine
a blocker (reversible) give to patients on MAO inh
Prazosin
a1 selective blocker (all ending osin)
BPH, PTSD, hypertension
Mirtazapine
a2-selective blocker
depression
What are the toxicities of mirtazapine
sedation, incr serum cholesterol, incr appetite
What effect does epinephrine have on BP before and after a block?
before- incr BP
after- decr BP
carvedilol
nonselective a and b antag
labetalol
nonselective a and b antag
nebivolol
b1 blockade of heart
b3 stim- activate NO synthase vasculature
acebutolol
b1 selective, partial agonist
atenolol
b1 selective antag
pindolol
nonselective b, partial agonist
propanolol
nonselective b antagonist
What b blockers decr mortality after MI?
metoprolol, carvedilol, bisoprolol
betaxolol
b1 selective antag
What b blockers are class II antiarrythmics?
metoprolol, esmolol
What b blockers are used to treat glaucoma
timolol (decr aq hum)
What population should avoid b blockers?
cocaine users (unopposed a agonist)