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266 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Where are SNS PRE cell bodies located?
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thoracic and lumbar segments (lateral horn)
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Where do SNS PRE synapse?
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paravertebral chains of sympathetic ganglia (SHORT PRE)
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Where are PNS PRE cell bodies located?
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cranial N. 3, 7, 9, 10
sacral outflow - nervi erigentes |
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areas with only SNS inn. (5)
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1 = adrenal medulla
2 = kidney 3 = sweat glands 4 = blood vessels 5 = pilomotor mm. |
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is BP controlled by SNS or PNS?
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SNS
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areas with only PNS inn. (2)
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1 = ciliary mm. of eye
2 = bronchial constrictor tone |
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denervation supersensitivity
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nerve is cut --> structure supplied by it becomes supersensitive to transmitter substance released by its terminals
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NANC transmitters (4)
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non-adrenergic, non-cholinergic
1 = nitric oxide 2 = VIP 3 = ATP 4 = neuropeptide Y |
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SNS functions:
(1) HR and BP (2) blood flow to skeletal mm./heart (3) blood flow from skin (4) pupils (5) bronchi (6) GI motility |
1 = increases
2 = increases 3 = decreases (diverts) 4 = dilates 5 = bronchodilation 6 = decreases |
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PNS functions:
(1) HR and contractility (2) GI mm. motility (3) bladder (4) bronchi (5) pupils (6) ciliary mm. |
1 = decreases
2 = increases 3 = contraction 4 = bronchoconstriction 5 = constricts 6 = accomodation for near vision |
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hemicholinium
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inhibits choline transport into cytoplasm of neuron
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botulinum toxin
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blocks fusion of synaptic vesicles -> prevents transmitter release
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black widow toxin
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causes release of all stored Ach
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butylcholinesterase aka (1) is found in (2)
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1 = pseudocholinesterase
2 = plasma |
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heximethonium
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selectively blocks nicotinic ganglionic R.
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tubocurarine
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blocks the Ach-R at NMJ
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membrane response at N-AchR at the NMJ
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excitatory = increased Na+/K+ permeability
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membrane response at N-AchR at autonomic ganglia
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excitatory = increased Na+/K+ permeability
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membrane response at N-AchR in CNS
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can be either excitatory (increased Na+/K+ perm. ) OR excitatory (increased perm. of Ca2+)
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which muscarinic R. are coupled to Gq?
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M1, M3, M5
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which muscarinic R. are coupled to Gi?
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M2 and M4
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Where are M1-R located? (2)
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1 = CNS
2 = gastric parietal cells |
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Where are M2-R located? (2)
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1 = cardiac atrial cells
2 = CNS |
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Where are M3-R located? (3)
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1 = bladder
2 = exocrine glands 3 = smooth muscle |
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What are the non-selective muscarinic agonists? (5) hint: ACOMT
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1 = Ach
2 = Carbachol 3 = oxotremorine 4 = McNA343 5 = Talsaclidine |
1 = Ach
2 = Carbachol 3 = oxotremorine 4 = McNA343 5 = Talsaclidine |
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Which antagonists are selective for M1-R? (2)
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pirenzipine
mamba toxin MT7 |
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Which antagonist is selective for M2-R?
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gallamine
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Which antagonist is selective for M3-R?
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darifenacin
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Which antagonists are selective for M4-R?
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ipratropium
mamba toxin MT3 |
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Darifenacin is used for Tx of ?
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1 = overactive bladder
(selective M3-R antagonist) |
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vesamicol
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blocks accumulation of Ach in vesicles
--> dependent on H+ gradient between intracellular organelles and cytoplasm |
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presynaptic modulation at POST PNS endings?
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M2-R bind Ach and cause autoinhibition of Ach release
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at NMJ, presynaptic nAchR's (1) Ach release
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1 = facilitate
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muscarinic agonists mimic (1)
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PNS
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actions of muscarinic agonists
(1) HR, CO and BP (2) on blood vessels? (3) smooth muscle (4) GI motility (5) bladder/bronchial mm (6) secretions (7) eye |
1 = decrease
2 = vasodilation 3 = contract (other than BVs) 4 = increase 5 = contract 6 = increase endocrine secretions 7 = constrict pupil and accomodate for near vision |
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pilocarpine is used for Tx of
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glaucoma
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bethanechol is used for Tx of
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bladder emptying OR stimuation of GI motility
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bethanecol is selective for (1) receptors with no (2) actions; is not hydrolyzed by (3)
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1 = muscarinic
2 = nicotinic 3 = acetylcholinesterase |
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main actions of bethanecol (2)
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1 = increased intestinal motility
2 = increased contraction of bladder |
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bethanecol is used to Tx (3)
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1 = atonic bladder
2 = urinary retention 3 = megacolon |
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Carbachol
acts on (1) R. mainly in (2) and (3) main action = (4) Tx = (5) contains 4 N, therefore does not (6) |
1 = nicotinic AND muscarinic R.
2 = CNS 3 = GI tract * if used locally does not have systemic penetration 4 = miosis 5 = glaucoma |
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Pilocarpine
- is a (1) amine, therefore (2) - has (3) R. activity - main actions = (4) and (5) Tx = (6) |
1 = tertiary
2 = can cross BBB 3 = muscarinic R. agonist 4 = miosis 5 = spasm of acomodation 6 = drug of choice for emerg. decrease in intraocular P. (glaucome) |
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Which drug opposes action of pilocarpine?
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atropine
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What drug is the most potent stimulant of secretions?
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pilocarpine
- may be used for patients with xerostomia |
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muscarinic antagonists are (1)
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parasympatholytics
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effects of muscarinic antagonists
- (1) secretion = (2) - (2b) heart rate - (3), (4) and (5) in eyes - (6) GI motility - (7) smooth muscle - (8) CNS - (9) extrapyramidal system |
1 - decrease secretions
2 - dry mouth and skin 2b - increase 3 - mydriasis (dilated pupils) 4 - failure of accomodation 5 - increased intraocular P. 6 = inhibit 7 = relax smooth mm 8 = excitatory in CNS 9 = reduce involuntary movement |
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what is the antidote for muscarinic antagonists?
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physostigmine
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atropine is used for Tx of
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sinus bradycardia
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scopolamine is used for Tx of
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motion sickness
facilitates endoscopy |
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atropine methonitrate
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derivative of atropine, that is excluded from BBB --> lacks central actions
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cyclopentolate
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muscarinic antagonist
- used to dilate pupils |
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tropicamide
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muscarinic antagonist
- used to dilate pupils |
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pirenzipine
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selective M1-R antagonist
--> prevents gastric acid secretion --> Tx of peptic ulcer |
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oxybutynin
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selective M3-R antagonist
--> Tx urinary incontinence |
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tolterodine
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selective M3-R antagonist
--> Tx urinary incontinence |
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darifenacin
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selective M3-R antagonist
--> Tx urinary incontinence |
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atropine is a (1) amine with high affinity for (2) R.
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1 = tertiary amine
- > cross BBB 2 = muscarinic R. |
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atropine effects in EYE (3)
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1 = persistent mydriasis (dilate)
2 = no response to light 3 = cycloplegia (inability to focus for near vision) |
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atropine effects in GI (1)
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anti-spasmodic
--> does not affect HCl release |
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atropine effects on urinary system
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decreases hypermotility states of bladder
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atropine effects on CARDIO (low dose vs. high dose)
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low dose = decreases HR (Pre M1R)
high dose = increases HR (M2-R SA node) toxic doses = dilates cutaneous vasculature |
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atropine effects on SECRETIONS
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prevents secretions
--> dry mouth --> no sweat = increased body temp |
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adverse effects of atropine (6)
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1 = dry mouth
2 = blurred vision 3 = sandy eyes 4 = tachycardia 5 = constipation 6 = excitatory CNS effects |
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2 uses of scopolamine
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Tx of motion sickness and blocks short term memory
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adverse effect of scopolamine
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sedation --> high doses produces excitement/euphoria (abuse)
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ipratropium is a (1) amine, acts on (2) to cause (3)
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1 = quaternary
2 = muscarinic antagonist (M3) |
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ipratropium is used for Tx of
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COPD and asthma (inhaled) in ppl who cannot take adrenergic agonists
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examples of ganglionic sitmulants (3)
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nicotine
lobeline demethylphenylpiperazinum |
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first anti-hypertensive drug
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hexamethonium
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trimethaphan
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ganglionic blocker
-> used to lower BP in surgery (Rarely used) |
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mecamylamine
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competitive ganglionic blocker
--> used to lower BP in emergency situations |
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effects of ganglionic blockers
- block (1) - (2) in BP due to (3) causes (4) and (5) |
1 = sympathetic ganglia
2 = fall/drop 3 = arteriolar vasodilation 4 = postural hypotension 5 = postexercise hypotension |
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Examples of NMJ Non Depolarizing blockers? (7)
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1 = tubocurarine
2 = pancuronium 3 = vecuronium 4 = atracurium 5 = cisatracurium 6 = metocurine 7 = doxacurium |
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tubocurarine
low dose (1) high dose (2) |
1 = prevents binding of Ach to R. = prevents mm. contraction - can be overcome by increase Ach conc. in synapse
2 = blocks ion channels on end plate -> cannot be overcome |
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3 non-depolarizing NMJ blockers that also release histamine
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1 = tubocurarine
2 = mevicurium 3 = atracurium |
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non depolarizing competitive blockers are used for (2)
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1 = adjuvant to anesthesia to relax skeletal mm.
2 = facilitate intubation |
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tubucurarine and the like are (1) amines and thus (2) and (3
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1 = quaternary
2 = penetrate mbs. poorly 3 = excreted unchanged in urine |
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atracurarium is degraded (1) and metabolized by (2) which (3)
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1 = in plasma
2= laudanosine 3 = provokes seizures |
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metabolism of vecuronium/recuronium
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deacetylated in liver, excreted in bile
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interaction of tubocurarine with cholinesterase inhibitots
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i.e. physostigmine, neostigmine
--> these overcome the block, but with increased dose cause depolarizing block |
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nteraction of tubocurarine with halogenated anesthetics
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i.e. halothane
--> enhance NMJ blockade |
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interaction of tubocurarine with aminoglycoside antibiotics
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i.e. gentamycin, tobramycin
--> inhibit Ach release by competing with Ca2+ ions (synergize) |
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interaction of tubocurarine with Ca2+ channel blockers
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increases neuromuscular block
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side effects of tubocurarine (2)
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1 = hypotension (ganglion block + histamine)
2 = bronchoconstriction (histamine) |
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side effects of pancuronium
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slight tachycardia
no hypotension |
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examples of depolarizing blocking agents at NMJ (2)
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1 = decamethonium
2 = succinylcholine |
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Two phases of action of depolarizing NMJ blockers
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phase 1 = bind N-AchR and open Na+ ion channel -> cause depolarization = mm. fasciculations
phase 2 = continuous depol leads to repol --> flaccid paralysis |
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succinylcholine is broken down by (1)
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plasma cholinesterase only
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uses of succinylcholine
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rapid endotracheal intubation
electroconvulsive shock therapy |
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adverse effects of succinylcholine (7)
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1 = bradycardia
2 = hyperkalemia 3 = increased intraocular pressure 4 = prolonged paralysis 5 = malignant hyperthermia (if given with halothane) 6 = post-op mm. pain 7 = apnea (paralysis of diaphragm) |
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effect of aminoglycoside antibiotics on neurotransmission
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inhibit Ca2+ entry into cell, thus inhibiting Ach vesicle release
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which drug is used for diagnosis of myasthenia gravis?
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edrophonium (inhibitor of cholinesterase)
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which cholinesterase inhibitor has the shortest duration of action?
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edrophonium
--> too short to be used clinically |
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actions of edrophonium
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1 = DDx of myastenia gravis
2 = antagonist for curare-like block |
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physostigmine is a (1) amine and is a (2); acts by (3)
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1 = tertiary amine (can cross BBB)
2 = indirect acting cholinergic agonist 3 = inhibiting Achesterase activity |
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physostigmine is used for (3)
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1 = to increase intestinal/bladder motility
2 = miosis/spasm of accomodation, decrease intraocular pressure 3 = overdose with drugs with anticholinergic activity |
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side effects of physostigmine
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convulsions with high doses
decreased HR and CO too much Ach = skeletal mm. paralysis |
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physostigmine used for Tx of
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glaucoma
--> eye drops |
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neostigmine is a (1) amine with greater activity on skeletal mm. than (2); its actions are to stimulate (3)
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1 = quaternary (does not enter BBB)
2 = physostigmine 3 = bladder and GI tract |
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neostigmine is used for Tx of (1) or as an antidote for (2)
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1 = chronic myasthenia gravis
2 = tubocurarine |
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side effects of neostigmine (indirect acting cholinergic agonist)
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salivation
flushing decreased BP nausea abdominal cramps diarrhea bronchospasm |
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pyridostigmine
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Achesterase inhibitor
--> used for Tx of chronic myasthenia gravis |
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ambenomium
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Achesterase inhibitor
--> used for Tx of chronic myasthenia gravis |
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demecarium is a (1) amine used as a (2) drug
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1 = quaternary
2 = indirect cholinergic agonist |
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demecarium is used for Tx of (1) and diagnosis (2)
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1 = chronic open angle glaucoma
2 = accomodative estropia |
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indirect acting cholinergic agonists used for treatment of Alzheimers (4)
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tacrine
donepezil rivastigmine galantamine |
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effects of anticholinesterase drugs
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PARASYMPATHOMIMETIC
- increase secretions - increased peristalsis - bronchoconstriction - low HR and low BP - pupillary constriction - decrease intraocular pressure |
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organophosphates cause
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peripheral nerve demyelination leading to progressive weakness and sensory loss
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pralidoxime
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cholinesterase reactivation
--> but ONLY before aging and cannot enter CNS |
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examples of indirect IRREVERSIBLE cholinergic agonists
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nerve gas -> organophosphates
insecticides -> parathion |
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ecothiophate
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indirect cholinergic agonist --> IRREVERSIBLE
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action of ecothiophate (3)
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1 = cholinergic stimulation
2 = paralysis of motor fxn and convulsion 3 = intense miosis |
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ecothiophate used for Tx of (1)
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open angle glaucoma (not first line)
-> may cause cataracts |
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main actions of alpha-1 adrenoR
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- vasoconstriction
- mydriasis - relaxation of GI sm. mm - contraction of all other sm. mm - bronchoconstriction - salivary secretion - hepatic glycogenolysis |
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main actions of alpha-2 adrenoR
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- inhibit NE and Ach release from ANS nerve endings
- inhibit insulin release - platelet aggregation - contraction of vascular sm. mm |
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main actions of beta-1 adrenoR
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- increased HR
- increased force of contraction - increased renin release - salivary amylase secretion |
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main actions of beta-2 adrenoR
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- vasodilation
- bronchodilation - increased mm and liver glycogenolysis - increased release of glucagon - relaxation of visceral sm. mm - muscle tremor |
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main actions of beta-2 adrenoR
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lipolysis and thermogenesis
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desensitization
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prolonged exposure to catecholamines reduces the receptor response to them
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agonist potencies for alpha adrenoreceptor
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E > NE >> ISO
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agonist potencies for beta adrenoreceptors
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ISO > E > NE
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tyrosine hydroxylase converts (1) to (2), is found in (3) and is inhibited by (4) and (5)
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1 = L-tyrosine
2 = DOPA 3 = only in catecholamine producing cells 4 = NE (end product) 5 = a-methyltyrosine (synthetic analogue) |
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dopa decarboxylase converts (1) to (2) and is found (3)
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1 = L dopa
2 = dopamine 3 = cytosolic enzyme not confined to catecholamine cells |
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dopamine beta hydroxylase converts (1) to (2), is found in (3) specifically located in (4), not degraded therefore is an index of (5); inhibited by (6) and (7)
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1 = dopamine
2 = NE 3 = only catecholamine cells 4 = synaptic vesicles 5 = index of SNS activity 6 = copper chelating agents 7 = disulfuram |
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PNMT catalyzes (1) of (2) to (3) and is located in (4)
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1 = n-methylation
2 = NE 3 = E 4 - adrenal medulla A cells |
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vesicular monoamine transporter
- function (1) - blocked by (2) |
1 = conc. NE into vesicles
2 = reserpine |
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uptake 1 -> responsible for (1) of NE uptake, via (2) transporter; this is a (3) affinity system, with a (4) max rate of uptake
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1 = 75%
2 = NET 3 = high affinity 4 = low max uptake rate |
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uptake 1 is blocked by (1) and (2)
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1 = TCAs (imipramine)
2 = cocaine |
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uptake 2 --> responsible for (1) of NE uptake, via (2) transporter; this is a (3) affinity system, with a (4) max rate of uptake
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1 = 25% (into cells in vicinity)
2 = VMAT 3 = low affinity 4 = high max uptake rate |
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monoamine oxidase
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- converts catecholamines into corresponding aldehydes
- converts NE, DA and E - within cells, bound to mitochondria |
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MAO controls
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the releasable store of NE
--> if inhibited, the store of NE increases |
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catechol-O-methyl transferase
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- methylation of one catechol hydroxyl groups to a methoxy derivative
- absent from NE neurons, only in adrenal medulla |
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adrenergic agonist drugs are derivatives of
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B-phenylethylamine
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what are the 4 catecholamines
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NE
E DA isoproterenol |
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what are examples of non-catecholamines
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phenylephrine
ephedrine amphetamine |
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3 characteristics of catecholamines
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1 = highest potency in activating R
2 = rapid inactivation by COMT and MAO 3 = poor CNS penetration (polar) |
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affinity for beta-R (1) as group on amine N. gets (2)
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1 = increases
2 = larger |
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Epinephrine
low doses (1) effects predominate high doses (2) effects predominate |
1 = beta = vasodilation
2 = alpha = vasoconstriction |
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epinephrine effects on CARDIO
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increases HR and force of contraction (B1-R)
decreases renal blood flow increases systolic BP, decreases diastolic BP |
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epinephrine effects on RESP
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bronchodilation (B2)
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epinephrine effects on HYPERGLYCEMIA
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increaes glycogenolysis in liver (B2)
increases glucagon release (B2) decreases release of insulin (a2) |
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therapeutic uses of Epinephrine
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open glaucoma --> decreases intraocular pressure by decreasing prod. of aqueous humor
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epinephrine is the drug of choice for
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acute asthma attacks
anaphylactic shock |
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epinephrine + local anesthetics
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E produces vasoconstriction at site of injection = increases the duration of action of local anesthetic
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pts. with hyperthyroidism and cocaine users + epinephrine
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increased cardiovascular actions
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pts. with diabetes + epinephrine use
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increase blood glucose (may need insulin)
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pts. taking B-blockers + epinephrine use
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alpha-R stimulation is unopposed = large increase in BP
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main therapeutic actions of NE (1)
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1 = increase in TPR = vasoconstriction (alpha 1)
--> causes reflex bradycardia |
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NE is used to Tx (1)
but is NEVER used in (2) or (3) |
1 = shock
2 = asthma 3 = with local anesthetics |
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NE acts mainly on (1) receptors
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alpha adrenoreceptors
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isoproterenol stimulates (1) and (2) receptors
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1 = beta 1
2 = beta 2 |
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main actions of isoproterenol are (3)
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1 = increases HR/force of contraction = increased CO
2 = dilates arterioles of skeletal mm (decrease TPR, decrease BP) 3 = rapid bronchodilation |
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therapeutic uses of isoproterenol
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in emergency situations to stimulate the heart
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dopamine
at low doses acts on (1) adrenoreceptors and at high doses acts on (3) adrenoreceptors |
1 = B1 -R (inotropic, chronotropic)
2 = A1-R (vasoconstriction) |
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aside from adrenoreceptors, dopamine also acts on (1) in the (2) which causes (3)
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1 = D1/D2- R
2 = peripheral mesenteric/renal vascular beds 3 = vasodilation |
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dopamine is the drug of choice for Tx of
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shock
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dobutamine is a selective (1) receptor agonist with effects of (2)
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B1-R agonist
increasing CO |
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dobutamine is used for Tx of
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cardiogenic shock and congestive heart failure
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dobutamine should be used with caution with (1)
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1 = atrial fibrillation -> bc it increases AV nodal conduction
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oxymetazoline stimulates (1) receptors
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alpha 1 and alpha 2 R.
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oxymetazoline is used for Tx of
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locally in eye/nose as vasoconstriction
--> found in OTC nasal and eye sprays |
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phenylephrine favors (1) receptors, is considered a (2) and therefore, is not degraded by (3)
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1 = alpha 1 >> alpha 2
2 = non catecholamine 3 = COMT |
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main action of phenylephrine is (1) which causes (2)
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1 = vasoconstriction = increased BP
2 = reflex bradycardia |
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phenylephrine is used clinically as...
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topically on nasal mucous mbs.
opthalmic solutions - mydriasis to terminate SVT |
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large doses of phenylephrine can cause (2)
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hypertensive headaches
cardiac arrythmias |
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methoxamine is similar to (1)
-> favors (2) receptors -> increases (3) by (4) -> relieves (5) |
1 = phenylephrine
2 = alpha 1>> alpha 2 3 = BP 4 = vasoconstriction 5 = paroxysmal SVT (without triggering arrythmias) |
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What receptor does clonidine act on?
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alpha 2 receptor agonist
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Clinical uses of clonidine (4)
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1 = essential hypertension
2 = decreases intraocular pressure 3 = minimizes withdrawl from opiates/benzo's 4 = decreases migraines |
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What receptor does metaproterenol act on?
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B2-R agonist
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main action of metaproterenol
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bronchodilation
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what are the short acting B2 agonists? (3)
what are they used for? |
1 = albuterol
2 = pirbuterol 3 = terbutaline --> used as bronchodilators (metered dose inhalers) |
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what are the long lasting B2 agonist? (2)
what are they used for? |
1 = salmeterol
2 = formoterol --> primary choice for Tx of nocturnal asthma --> not used in monotherapy usually, but in conjunction with corticosteroids |
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what does amphetamine do?
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blocks reuptake of NE
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clinically, amphetamine is used for Tx of (3)
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1 = narcolepsy
2 = hyperactivity in children 3 = appetite control |
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cocaine blocks
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reuptake of NE
--> causes increase in BP |
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non selective alpha blockers (2)
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1 = phenoxybenzamine
2 = phentolamine |
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phenoxybenzamine is an (1), (2) alpha blocker;
--> main action is (3) with (4) |
1 = irreversible
2 = non competitive 3 = decreased BP 4 = reflex tachycardia |
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main use of phenoxybenzamine
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prevents hypertensive crisis in pheochromocytoma patients undergoing surgery
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adverse effects of phenoxybenzamine (4)
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1 = postural hypotension
2 = nasal stuffiness 3 = nausea/vomiting 4 = inhibits ejaculation |
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phentolamine is a (1) alpha blocker
---> main action is (2) and (3) --> produces (4). (5), (6) and (7) |
1 = competitive
2 = decrease BP 3 = reflex tachycardia 4 = postural hypotension 5 = E reversal 6 = angina 7 = arrythmias |
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phenotalamine is (1) lasting than phenoxybenzamine
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1 = shorter acting -> binds reversibly
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phentolamine is used for Tx of
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pheochromocytoma
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what are the 5 main alpha-1 selective adrenoreceptor antagonists?
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1 = prazosin
2 = doxazosin 3 = terazosin 4 = tamsulosin 5= alfuzosin |
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alpha-1 selective blockers used for Tx of hypertension?
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prazosin
doxazosin terazosin -> less reflex tachycardia bc they do not act on NE release by alpha 2 R |
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alpha-1 selective blockers used for Tx of BPH?
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tamsulosin
alfuzosin |
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tamsulosin
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specifically inhibits alpha 1a R
--> found in smooth mm. of prostate --> relaxes bladder and inhibits hypertrophy of tissues |
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adverse effects of alpha-1 selective blockers (2)
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postural hypotension
impotence |
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yohimbine
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alpha 2 R. antagonist
--> sexual stimulant --> not used clinically |
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pseudoephedrine is used for Tx of
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nasal congestion
--> illegally converted to methamphetamine |
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functions of ephedrine (4)
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1 = vasoconstriction and cardiac stimulation = increased BP
2 = bronchodilation (prophylactic Tx of asthma) 3 = increased motor fxn in myasthenia gravis 4 = mild stimulation of CNS |
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mixed alpha and beta blocker drugs (2)
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labetalol
carvedilol |
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propanolol blocks (1) receptors
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B2 and B1 receptors
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propanolol is used to Tx (2)
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angina
SVT arrythmias |
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unwanted effect of propanolol
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bronchoconstriction
--> respiratory crisis in asthmatics and COPD pts |
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propanolol should be combined with a (1) drug
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diuretic drug
decreased BP = decreased renal perfusion = increased Na+ and H20 retention |
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timolol
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Tx of chronic glaucoma
decreases intraocular pressure |
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B blockers mainly used for
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hypertension
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selective B1 antagonists (4)
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acebutolol
atenolol metoprolol esmolol |
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actions of B1 antagonists
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at low doses, they decrease BP and angina during exercise
--> little effect on pulmonary fxn, TPR or carb metabolism good for ppl with asthma or diabetes |
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B blockers with partial agonist activity (2)
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pindolol
acebutolol |
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ISA
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intrinsic sympathomimetic activity
--> B blockers with partial agonist activity --> stimulate B-R but inhibit stimulation by more potent NE/E |
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B blockers with partial agonist activity used to Tx
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hypertension in ppl. with mild bradycardia (Do not slow heart rate down)
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labetolol used in Tx of (2)
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hypertension during pregnancy
IV dose for emergency hypertension |
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carvedilol used in Tx of
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hypertension in ELDERLY and BLACK ppl where increased TPR is undesirable
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mixed antagonists cause
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orthostatic hypotension
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a-methyltyrosine
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inhibits tyrosine hydroxylase
--> Tx of pheochromocytoma |
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carbidopa
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inhibits dopa decarboxylase
--> Tx of parkinsons |
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methyldopa
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Tx of hypertension in pregnancy
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side effects of methyldopa (3)
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1 = sedation
2 = immune hemolytic reactions 3 = liver toxicity |
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6-hydroxydopamine
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trojan horse neurotoxin
--> taken up selectively by NE nerve terminals, destroys nerve terminal |
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reserpine
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blocks VMAT
--> blocks transport of catecholamines into synaptic vesicles |
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drugs directly blocking NE release (4)
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guanethidine
bretylium bethanidine debrisoquin |
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guanethedine function (2)
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blocks release of stored NE
displaces NE from storage vesicles |
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uptake 2 is inhibited by (2)
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1 = phenoxybenzamine
2 = corticosteroids |
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C3a
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anaphylatoxin
--> stimulates mast cells to secrete chemical mediators and directly stimulates smooth mm |
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C3b
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opsonin
--> attaches to surface of microbes, facilitates ingestion of WBCs |
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the complement system is initiated by ...
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endotoxins
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C5a
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releases mediators from mast cells
powerful chemoattractant and activator of WBCs |
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mast cell membrane has receptors for (1) and (2)
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1 = IgE
2 = C3a/C5a |
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mast cells release
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histamine
heparin leukotriene PGD2 PAF NGF interleukins |
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which leukocytes are involved in late phase of asthma
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eosinophils
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what are the first leukocytes to enter an inflamed area
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neutrophils
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which cells contribute to first phase of asthma
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platelets
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What do platelets generate? (3)
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TXA2
PAF free radicals |
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CD4+ T helper cells are class (1) MHC
CD8+ T cells are class (2) MHC |
1 =2
2 = 1 |
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when activated, T cells acquire (1) receptors and generated (2) which gives rise to (3) cells
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1 = IL2- R
2 = IL2 3 = To cells (clone cells) |
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Th1 cells
- what kind of response? (1) - what IL favors Th1? (2) |
1 = macrophage initiated cell mediated response
2 = IL-12 |
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Th2 cells
- what kind of response? (1) - what IL favors Th2 ? (2) |
1 = antibody mediated response
2 = IL-4 |
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Th1 mediated disease (6)
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DM1
multiple sclerosis H.pylori peptic ulcer aplastic anemia rheumatoid arthritis allograft rejection |
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Th2 mediated disease (2)
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1 = allergic conditions (asthma)
2 = AIDS |
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cyclosporine
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immunosuppressant drug
--> inhibits proliferation of B and T cells |
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Type 1 Hypersensitivity Reaction
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immediate/anaphylactic
--> Th2 response - allergens provoke prod. of IgE - subsequent exposure releases histamine, PAF, eicosanoids and cytokines |
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Type 2 Hypersensitivity Reaction
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antibody dependent cytotoxic
--> response is directed against cells that are foreign to host - triggers complement and NK cell activation - autoimmune |
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Type 3 Hypersensitivity Reaction
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complex mediated
--> antibodies react with soluble antigens, activate complement - SLE |
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serum sickness
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antigen persists in blood after sensitization causing a severe Type 3 reaction
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Type 4 Hypersensitivity Reaction
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cell mediated
--> aka. tuberculin reaction OR delayed hypersensitivty - basis of measles, mumps, insect bites, skin reactions ex. rheumatoid arthritis, DM1 |
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histamine
- located in high conc. in (1) - found mainly in these cells (2) , (3) |
1 = skin, lungs, GI tract
2 = mast cells 3 = basophils |
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agents that (1) cAMP, inhibit histamine secretion ex. (2)
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1 = increase
2 = B-adrenergic agonists |
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actions of H2-R stimulation (2)
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1 = stimulation of gastric acid secretion
2 = increased HR and CO |
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actions of H1-R stimulation (4)
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1 = contraction of sm. mm
2 = dilates blood vessels 3 = increased vascular permeability 4 = itching |
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histamine is implicated in which type of hypersensitivty reaction?
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TYPE 1 - anaphylactic
ex. allergic rhinitis, uritcaria |
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"triple response"
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reddening
weal flare --> characteristic when histamine is injected intradermally |
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mepyramine
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H1-R antihistamine
used to treat inflammation |
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thioperamide
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H3-R antagonist
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PGE2 and PGI2 are generated by (2)
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1 = local tissues
2 = blood vessels |
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PGD2 is released by (1)
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mast cells
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prostanoids (1) the effects of histamine and bradykinin
results in: (2), (3), (4) and (5) |
1 = potentiate
2 = vasodilation 3 = increased permeability 4 = sensation of pain 5 = pyrogenic |
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main actions of PGD2 (4)
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1 = vasodilation
2 = bronchoconstriction 3 = inhibition of platelet aggregation 4 = relaxation of GI /uterine mm |
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main action of PGF2
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myometrial contraction in humans
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PGI1 is found predominantly in (1)
main actions are (4) |
1 = vascular endothelium
1 = vasodilation 2 = inhibits platelet aggregation 3 = rennin release 4 = natriuresis |
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TXA2 is found in (1)
3 main actions |
1 = platelets
1 = vasoconstriction 2 = platelet aggregation 3 = bronchoconstriction |
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PGE2 actions of EP1-R (1)
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contraction of bronchial and GI smooth mm
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PGE2 actions at EP2-R (4)
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1 = bronchodilation
2 = vasodilatio 3 = intestinal fluid secretion 4 = relaxation of GI smooth mm |
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PGE2 actions at EP3-R (4)
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1 = contraction of intestinal sm. mm
2 = inhibition of gastric secretion 3 = inhibition of lipolysis 4 = inhibition of nt. release |
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gemeprost
|
prostanoid drug
- termination of pregnancy |
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misoprostol (2)
|
prostanoid drug
- induction of labour - prevention of Ulcer with NSAID use |
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carbropost
|
prostanoid drug
- post partum hemorrhage |
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alprostadil
|
prostanoid drug
- maintains patent ductus arteriosus |
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epoprosterenol (2)
|
prostanoid drug
1 = inhibits platelet aggregation during hemodialysis 2 = primary pulmonary hypertension |
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latanoprost
|
prostanoid drug
- open angle glaucoma |
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where are leukotrienes found? (4)
|
lungs
platelets mast cells WBCs |
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cysteinyl leukotrienes include (4) and make up the (5)
|
1 = LTC4
2 = LTD4 3 = LTE4 4 = LTF4 5 - slow reacting substance of anaphylaxis |
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actions of cysteinyl leukotrienes (4)
|
1 = contraction of bronchial mm
2 = increase mucus secretion 3 = reduce specific airway conductance 4 = rapid short lived fall in BP |
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given topically, LTD4 increases (2)
|
1 = nasal blood flow
2 = local vascular permeability |
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zafirlukast
|
CysLT receptor antagonist
- used for Tx of asthma |
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montelukast
|
CysLT receptor antagonist
- used for Tx of asthma |
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