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Term 2 Flash Cards > physio pharmacology midterm > Flashcards

physio pharmacology midterm Flashcards

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0
Q

Hemicholinium

A

Prevents choline reuptake

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1
Q

Sildenafil

A

Viagra! Blocks cGMP phosphodiesterase from breaking down cGMP to 3,5’ GMP -> prolonged relaxation of BVs for erection

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2
Q

Vesamicol

A

Prevents vesicular storage of ACh

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3
Q

Botulinum toxin

A

Degrades synaptobrevin (SNARE) and prevents vesicle fusion/exocytosis. Clinically in cases with increased skeletal muscle tone, Lambert-Eaton syndrome, focal dystonias

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4
Q

AChE inhibitors

A

Elevate synaptic concentrations of ACh, therefore enhancing the postsynaptic effects of ACh (parasympathomimetics)

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5
Q

Edrophonium

A

AChE inhibitor/anticholinesterase. Simple alcohol. Short duration of action. Useful for dx’ing myasthenia gravis and Lambert-Eaton syndrome

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6
Q

Neostigmine and physostigmine

A

AChE inhibitor/anticholinesterase. Carbamic acid derivatives. Longer duration of action. Useful for tx’ing MG; reversal of neuromuscular blockers. (Physostigmine crosses BBB - good for CNS eg atropine poisoning.) Hydrolyzed by AChE so that covalent bond forms increasing half life of AChE inhibition

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7
Q

Parathion

A

AChE inhibitor/anticholinesterase. Organophosphate. Irreversible, toxic, commonly used in pesticides. Hydrolyzed by AChE to form an extremely stable complex. Only new recs can facilitate AChR activity and that can take weeks

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8
Q

Myasthenia Gravis

A

Autoimmune dz against Nm subtype (rec internalized), reduces NMJ transmission

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9
Q

Lambert-Eaton syndrome

A

Autoimmune dz against presynaptic Ca2+ channels. Reduces ACh release. Also used in dx

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10
Q

AChE inhibitor uses

A
  1. Increase neuromuscular transmission - MG, LE syndrome
  2. Increase parasympathetic tone (parasympathomimetic) - decrease glaucoma pressure via increased aq humor outflow, increase GI tract motility
  3. Increase central cholinergic neurotransmission in dementia (rivastigmine). Must titrate. Drugs delay development of cognitive and fxn’l impairment by 6 months.
  4. Reversal of paralysis from non-depolarizing neuromuscular blockers - increase ACh levels reverse the competitive block from these blockers
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11
Q

Negative SE’s of AChE inhibitors

A
  1. Excessive muscarinic stim - salivation, lacrimation, miosis, diarrhea, brachycardia
  2. Excessive nicotinic stim - muscle wkness and paralysis
  3. Chemical warfare - used as nerve gases - sx’s include mm wkness and paralysis
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12
Q

Dz using muscarinic agonists as txt: eye; GIT, bladder, urinary tract; salivary glands

A

Eye: glaucoma - contract circular m -> miosis -> aq humor outflow -> decreased intraocular pressure

GIT, bladder, urinary tract: restore GIT and UT motility after anesthesia/surgery

Salivary glands: xerostemia - increase salivation

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13
Q

Rivastigmine

A

AChE inhibitor. Improve dementia and Alzheimer’s dz cognitive sx’s. Requires titration phase. Drugs delay development of cognitive and fxn’l impairment by six months

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14
Q

Carbachol

A

MR agonist. Derivative of ACh. Differs in pharmacokinetic properties, resistance to ChEsterase and its affinity to both Nm and musc recs. Can’t be used systemically because of overall effects

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15
Q

Pilocarpine

A

MR agonist. Alkaloid similar to muscarine. Until recently the only alkaloid MR agonist to be used clinically. Used to tx dry mouth in Sjogrens syndrome

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16
Q

Methacholine

A

MR agonist. 3x more resistant to hydrolysis by AChE. Little affinity for nicotinic recs. used to dx asthma. Asthmatics are more sens to bronchial secreting actions of methacholine

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17
Q

Bethanecol

A

MR agonist. Almost completely selective for muscarinic recs. Choice drug for promoting GI and urinary tract motility. Particularly post-op, post-partum, and drug-related urine retention

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18
Q

Parasympatholytics

A

MR antagonists. Bind MRs and prevent ACh from exerting its effects. Competitive antagonists. Allow sympathetic responses to predominate.

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19
Q

Parasympatholytic prototype

A

Atropine. Actions: pupil dilation, tachycardia, decreased secretions (salivary, bronchial, GIT). Sympathetic response by antagonizing the parasympathetic

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20
Q

Clinical uses of atropine

A
  1. Produce mydriasis for opthalmological exam (applied topically)
  2. Reverse sinus brachycardia caused by excessive vagal tone
  3. Inhibit excessive salivation and mucus secretion during anesthesia and surgery
  4. Counteract the effects of muscarine poisoning AND poisoning with anticholinesterases
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21
Q

Scopolamine

A

MR antagonist. Significant CNS. Txt of nausea and motion sickness, intestinal cramp. As a general depressant and adjunct to narcotic painkillers. Truth drug in 50s and 60s

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22
Q

Pirenzepine

A

MR antagonist. Txt of peptic ulcers, an alternative to H2 histamine rec antagonists

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23
Q

Ipratropium

A

MR antagonist. Relatively selective for M3. Reduces bronchial secretions - used in COPD. Used in asthma where the bronchoconstrictive component is mediated by increased cholinergic neural tone

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24
Succinylcholine
Nicotinic rec depolarizing neuromuscular blocker. Causes excessive activation of Nm rec leading tie widespread muscle fasciculations. Eventual desensitization of Nm rec leading to muscle paralysis. Uses: short term paralysis, ie during intubation. Short duration bc of merabolism by pseudocholinesterases (BuChE) SE's and adverse rxns: brachycardia (M2), K+ release (from prolonged depolarization), prolonged paralysis (genetic variants of pseudocholinesterase), malignant hyperthermia
25
Nicotinic rec antagonists: non-depolarizing neuromuscular blockers
Uses: paralyze skeletal muscles during surgery Mode of action: occupy Nm recs on skeletal muscle. Have no intrinsic activity. Prevent the action of ACh. Muscle can't contract. Flaccid paralysis Competitive antagonists: therefore, effects are overcome by increasing ACh levels. Reversal achieved by AChE inhibitor
26
D-tubocurarine
Non-depolarizing (competitive) neuromuscular blocker. Plant alkaloid ("arrow poison")
27
Pancuronium
Non-depolarizing (competitive) neuromuscular blocker. Long acting
28
Vecuronium
Non-depolarizing (competitive) neuromuscular blocker. Intermediate duration
29
Mivacurium
Nicotinic rec antagonist Non-depolarizing (competitive) neuromuscular blocker. Short acting
30
Uses and SE's of nicotinic rec antagonist non-depolarizing (competitive) neuromuscular blockers
More selective on Nm rec than Nn rec (ganglia)!!! Uses: induction of neuromuscular blockade in surgery SE's: hypertension, apnea, bronchospasm, salivation, flushing, and resp failure
31
Oxymetaxoline
a1 agonist, partial a2 agonist. Nasal decongestant. Tx Ophthalmic hyperaemia (too much bloodflow to eye).
32
Phenoxybenzamine
a1 and a2 antagonist. Irreversible. Tx pheochromocytoma
33
Phentolamine
Alpha antagonist. Reversible antagonist. Tx pheochromocytoma
34
Phenylephrine
Alpha 1 agonist. Used as nasal decongestant. Can also be used for treatment of shock SE's: hypertension
35
Prazosin
Alpha 1 antagonist. Used for txt of hypertension and BPH. SE's: postural orthostatic/hypotension related to 1st dose phenomena
36
Tamsulosin
Alpha 1 antagonist. Used for BPH. More selective for genitourinary smooth muscle receptor subtype (a1A). Less postural/orthostatic hypotension
37
Clonidine
Alpha 2 agonist. Used to tx hypertension (decreased peripheral sympathetic outflow - CNS effect) and opioid withdrawal SE's: brachycardia and hypotension
38
Yohimbine
Alpha 2 antagonist. Previously used for male impotence (psychogenic). SE's: increased sympathetic outflow - hypertension
39
Isoproterenol
Nonselective B receptor agonist. Emergency arrhythmias and bronchospasm. More selective agonists available. SE's: hypertension, palpitations, tremor
40
Dobutamine
Selective B1 receptor agonist. Has prominent inotropic effects resulting in increased contractility and cardiac output. Short half-life due to COMT metabolism. Used in the ACUTE management of heart failure (Note more than just B1 activity). Increased contractility but NOT heart rate - no change in peripheral resistance
41
Albuterol
Selective B2 receptor agonist. Used as asthma reliever. Rapid action (15 minutes), relative short duration (4-6 hours)
42
Salmeterol
Selective B2 receptor agonist. Long-acting beta agonist (LABA's). Have lipophilic side chains that resist degradation. Enhanced duration (12-24 hours), used for prevention of bronchoconstriction
43
B adrenergic antagonists: clinical uses
Reduce chronotropic and inotropic actions of endogenous catecholamines at cardiac B1 receptors, resulting in decreased heart rate and myocardial contractility. Blockade of B1 recs in kidney to reduce renin secretion to reduce fluid overload and vasomotor tone. Are first line drugs in txt of hypertension. Blockade of B2 receptors is clinically undesirable
44
Propranolol
Non-selective B adrenoreceptor antagonist. Used for hypertension, angina SE's include sedation (central effect) and dyspnea
45
Atenolol
B1 selective adrenergic antagonist. Used to tx hypertension and angina. Improves life expectancy in patients with heart failure (via volume reduction (decreased afterload) via decreased renin production. Contraindications
46
Pindolol
Partial B1 agonist. Tx hypertension in patients with brachycardia or low cardiac reserve
47
Carvedilol
Nonselective B and a1 antagonist. a1 receptor blockade results in vasodilation; the B1 blockade prevents a reflex sympathetic increase in heart rate. These effects combine to decrease blood pressure. Also used in txt of heart failure. Contraindicated in severe HF Clinical benefit in HF through volume reduction (decreased afterload) via decreased renin production and vasodilation (decreased preload)
48
Cocaine
Inhibitor of NE reuptake by inhibiting NE transporter
49
Tricyclic antidepressants (TCA's)
Inhibitor of NE reuptake. Inhibit NE transporter
50
Imipramine
Inhibitor of NE reuptake. TCA. Inhibits NE transporter. Used for treating mild depression SE's: postural hypotension and tachycardia
51
Reserpine
Inhibitor of NE storage. Blocks VMAT
52
Tyramine
Inhibits NE storage. Transported VMAT and displaces vesicular NE
53
MAO inhibitor uses
Txt of mild depression
54
Phenelzine
Inhibitor of NE metabolism. Non-selective MAO inhibitor. Implicated in elevated tyramine leading to hypertensive crisis
55
Selegiline
Inhibitor of NE metabolism. Selective MAO B inhibitor. Safer with respect to dietary restriction. Also useful for Parkinson's
56
Iproniazide
MAO inhibitor
57
Possible acute complications of MAO inhibitors
If you eat aged cheese and red wine that have high conc of tyramine, tyramine is substrate for VMAT -> outcompetes NE for transport into vesicles -> high NE conc in cytosol and reversal of NET -> sympathetic overload - headache, nausea, high BP and pulse
58
Amphetamines
1. Displaces endogenous catecholamines from storage vesicles 2. Blocks NET 3. A weak inhibitor of MAO
59
Methylphenidate
Inhibitor of reuptake and storage of NE. Used for ADHD.
60
Ephedrine and pseudoephedrine
Inhibitors of NE reuptake and storage. Used for nasal decongestion
61
Digoxin
Blocks Na+ K+ ATPase -> higher intracellular conc of Na+ -> reduced activity of Na+ Ca2+ exchanger -> more intracellular Ca 2+ -> increased heart contractility. Used to tx heart failure

Term 2 Flash Cards (8 decks)

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