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76 Cards in this Set
- Front
- Back
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which adrenergic blocker binds to alpha 2 receptors?
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a-methyldopa
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what is reserpine used for?
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hypertension --> decline in BP and HR
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what is guanethidine used for?
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used to be used for hypertension
AEs: excessive sympathetoplegia interferes with male sexual function, orthostatic hypotension |
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what is pargyline used for?
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MAOI:
parkinsons & depression |
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what is entacapone used for?
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parkinsons
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which transporters does cocaine block?
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DA, and NE
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what are cocaine's effects?
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stimulates CNS and cardiovascular system
- euphoria, addiction, tolerance - HTM, coronary vasospasm --> MI |
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what is imipramine used for?
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same mech as cocaine
- one of the first TCA |
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which receptor types can epi activate?
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all
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what is epi used for?
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bronchospasm, anaphylaxis, anesthetics, glaucoma
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which receptor types can NE activate?
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all, but weak B2 effect
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what is NE used for?
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sometimes as a pressor for shock, although DA is better
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which receptor types can DA activate?
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all.
primary actions in basal ganglia and kidney |
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where do you find the cell bodies of sympathetic neurons?
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intermediolateral column of spinal cord, from T1 to L3
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where do you find the cell bodies of parasympathetic neurons?
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nuclei of cranial nerves (II, VII, IX, X) and S2-4 nerve rootes
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draw the sympathetic and parasymathetic schema with NTs
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sympathetic: ACh --> ganglia far from end point --> adrenergic NT
parasympathetic: ACh --> ganglia close to end point --> mACh |
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where are nACh receptors found?
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motor end plate
autonomic ganglia |
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what does bugarotoxin do?
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antagonizes the nAChR at the motor end plate
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explain ganglionic transmission
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there are many factors affecting trasnmission
- initial nicotinic effect leads to an increase in Na conductance and fast EPSP. - this is modulated by M1 (slow EPSP) and M2/adrenergic (IPSP) |
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give the relative potencies of adrenergic agonists
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a: E > NE > phenylephrine>> isoproterenol
B: isoproterenol> E> NE > phenylephrine |
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define: tachyphylaxis
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certain drugs (e.g ephedrine) release stores of NE. After repeated dosing, the NT may be exhausted
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define: receptor down regulation
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decrease in number of available receptors or decrease in ligand affinity for the receptor.
e.g. decrease in B1 receptors in myocardium of patients with CHF |
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define: desensitization
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reversible uncoupling of receptor occupancy and cellular response by receptor phosphorylation, then internalization by enodcytosis
(e.g. B adrenergic receptor) |
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where are M1 receptors found?
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ganglia, depolarize
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where are M2 receptors found?
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Heart, hyperpolarize
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where are M3 receptors found?
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smooth muscle, depolarize
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what is the relative NT potency at B receptors?
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iso > Epi > NE
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what is uptake1?
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the transporter for NE (aka NET)
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how do you decrease adrenergic transmission?
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attack uptake 1
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how do you decrease cholinergic transmission?
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attack acetylcholinesterase
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where does DA act at high concentrations?
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alpha receptors
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where does DA act at low concentrations?
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beta receptors
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what happens with DA binds D1 and D2 receptors?
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vasodilation of renal and mesenteric vasculature
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why do you use DA for shock?
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raises BP by B1 stimulation and aviods kidney shutdown by D1,D2 activation
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phenylephrine
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a1> a2.
direct a agonist nasal decongestant (from vasoconstriction), raises BP |
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methoxamine
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a1
overcome hypotension brought on by anesthetics also used in supraventricular Tach |
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clonidine
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a2
lowers BP in essential HTN by acting at CNS |
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isoproterenol
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b1, b2
rarely used as a bronchodilator for asthma |
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dobutamine
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b1
increase CO in CHF. DOES NOT INCREASE HR significantly- minimal impact on O2 demand |
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terbutaline
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B2
used in asthma as bronchodilator. reduce uterine contractions in premature labor (ritodrine more commonly used now) |
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why should you not use B2 agonists during shock?
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decrease BP!
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phenoxybenzamine
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a1, a2 antagonist (covalent)
pheochromocytoma treatment |
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phentolamine
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a1, a2 antagonist (competitive)
diagnosis of pheochromocytoma |
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prazosin
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a1 antagonist (competitive)
decrease BP increase urinary sphincter relaxiation in patients with BPH |
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Propanolol
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B1, B2
HTN, glaucoma, hyperthyroidism, angina, protective against MI AD: bronchoconstriction, arrhthia, increased risk of hypoglycemia (makss tachycardia and other signs of insulin reaction) |
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Pindolol
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partial agonist at B1 and B2
HTN who have bradycardia - doesn't lower heart rate that much more |
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metoprolol
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b1 blocker
HTN with impaired pulmonary function, diabetic HTN recieving hypoglycemics |
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amphetamine
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causes release of vesicles from presynaptic terminal, and reversal of DAT, NET, 5HTT
used in depression, narcolepsy, appetite controle |
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ephedrine
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1. release of presynaptic vesicles
2. direct action on a and b receptors Uses: asthma, BP elevation, nasal decongestant |
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list 3 MAOIs
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isocarboxazid
pargyline tranylcypromine |
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what is the danger of tyramine?
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when there's too much in a patient given MAOIs for depression, you can cause a hypertensive crisis
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tell me more about MAOIs and hypertension
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can cause a false transmitter octopamine. diminishes the vascular and cardiac responses
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hemicholinum
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blocks uptake of choline
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vesamicol
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blocks vesicular uptake of acetylcholine
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alpha-latrotoxin
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black widow toxin: oligomerizes to form membrane pores and stimulates large release of NT
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what is a nicotinic antagonist?
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succinylcholine
used as a FAST onset muscle relaxnat during surgery caveat: pseudocholinesterase deficiency |
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pancuronium
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non-depolarizing musle relaxant binds to nAChR without activating --> paralysis
used as muscle relaxant in surgery avoids fasciuclations (can cause soreness) of succinylcholine, but doesn't work as fast |
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cis-atracurium
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non-depolarizing muscle relaxant
can cause histamine release |
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D-turbocurarine
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same as pancuronium
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a-bungarotoxin
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nondepolarizing nicotinic blocker. found in snake venom
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hexamethonium
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blocks nAChR at autonomic ganglia
used for initial control of BP with acute dissectin aortic aneurysm reduces BP and prevents sympathetic reflexes, reducing the pressure rise near the tear |
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trimethaphan
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same as hexamethonium
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muscarine
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found in mushrooms. activate mAChR
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methacholine
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analog of ACH. less susceptible to AChE
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Carbachol
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analog of Ach
resistant to AChE used to reduce intraocular pressure in eye (causes pupillary contraction |
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pilocarpine
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analog of Ah
stable against AChE used in emergency reduction of IOP in both kinds of glaucoma |
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atropine
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competitive inhibitor at mAChR
antidote for cholinergic agonists as well as AChE inhibitors antisecretory drug to prevent pulmonary secretions |
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scopolamine
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similar to atropine but enters CNS more readily
used in motion sickness |
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physostigmine
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when AChE tries to hydorlyze this alkaloid, it's trapped at an intermediate with a long half life
prolongs the effects of ACh used for potentiating parasympathetic effects: increases intestinal and bladder motility used in glaucoma to cause miosis--> relieves pressure |
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neostigmine
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same mechanims oas physostigmine, but is more polar so it doesn't cross the BBB
used to treat myasthenia gravis |
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parathion
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found in insecticides
traps AChE in phosphorylated form are toxic! |
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malathion
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found in insecticides
traps AChE in phosphorylated form are toxic! |
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soman
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nerve gas
more potent organophosphate than parathion and malathion antidotes exist: atropine, pralidoxime |
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echothiophate
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less potent organophoslate used clinically
prolonged relieve of pressure in glaucoma |
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pralidoxime (2-PAM)
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regenerates AChE after phosphorylation
organophsophate poisoning antidote |
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atropine
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counters muscarinic side effect but doesn't revers teh skeletal musc fasiculations/paralysis
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