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99 Cards in this Set

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Nicotinic receptor antagonists (5)
1)nicotine
2)TMA
3)DMPP
4)hexamethonium
5)mecamylamine
Nicotine, TMA, DMPP mechanism of nicotinic receptor antagonism? (3)
1)initially stimulation
2)then ganglionic blockade resulting from desensitization or hyperpolarization
3)also produced by excess amounts of ACh
Major differences b/w hexamethonium and mecamylamine (2)
hexamethonium is NON-competitive and NOT active in CNS

Mecamylamine- COMPETITIVE and has CNS activity
Sites of action nicotinic receptor antagonists (2)
1)nicotinic receptors (competitive and non-competive reversible antagonists)
2)ALL autonomic ganglia
Therapeutic uses of nicotinic antagonists (1)
treat hypertension
Adverse Reactions of nicotinic antagonists(6)
1)visual disturbances
2)xerostomia
3)urinary retention
4)impotence
5)CNS stimulation (convulsions)
6)marked postural hypotension
Marked postural hypotension?
Fainting when going from lying down to standing up due to decreased cardiac output
Why are nicotinic receptor antagonists obselete?
newer drugs are more selective with fewer side effects
3 ways to prevent neuronal release of ACh and 1 drug that does each
1)blockade of ACh release (botulinum toxin)
2)blockade of ACh synthesis leading to depletion (hemicholinium)
3)blockade of ACh transport into synaptic vesicles (vesamicol)
Prevention of neuronal release of ACh all effect....and lead to...
ANS and SMS (somatic)

resulting in death by apnea
Botulinum toxin mechanism (2)
1)blockade of ACh release
2)vesicles w/ ACh can't attach to nerve ending to perform exocytosis
How does botulinum toxin work cosmetically?
blocks somatic nerves responsible for wrinkling
Hemicholinium mechanism? (2)
1)blockade of ACh synthesis leading to depletion
2)block uptake of choline into nerve
Vesamicol mechanism
blockade of ACh transport into synaptic vesicles
Hemicholinium and Vesamicol share what common mechanism?
result in no ACh in vesicles but vesicles still fuse w/ nerve
4 direct acting adrenergic agonists?
PINE
1)phenylephrine
2)isoproterenol
3)norepinephrine
4)epinephrine
Which direct acting agonist is NOT a catecholamine?
phenylephrine
NE acts @ what adrenergic receptor?
alpha and beta
E acts @ what adrenergic receptor?
alpha and beta
Isoproterenol acts @ what adrenergic receptor?
BETA
Phenylephrine acts @ what adrenergic receptor?
ALPHA
How is NE degraded?
neuronal(reuptake), COMT, MAO
How is E degraded?
neuronal(reuptake), COMT, MAO
How is isoproterenol degraded?
COMT only
How is phenylephrine degraded?
neuronal(reuptake), MAO
Isoproterenol has the longest action of all direct acting agonists, why?
NO REUPTAKE
Order of potency of direct acting agoinst at ALPHA receptors?
E, NE > Phenylephrine >> Isoproterenol
Order of potency of direct acting agoinst at BETA receptors?
Isoproterenol > E,NE >> Phenylephrine
4 categories of therapeutic uses of adrenomimetic direct acting agonists?
1)based on vasoconstriction
2)based on cardiac actions
3)based on bronchodialtion
4)based on vasodilation
Based on vasoconstriction uses of adrenomimetic direct acting agonists for E,NE,P (3)
1)use w/ locals
2)treat hemmorrhage from minor cuts
3)hypotensive states
Based on vasoconstriction uses of adrenomimetic direct acting agonists for just P (2)
1)nasal decongestant
2)paroxysmal atrial tachycardia
How does phenylephrine work for nasal decongestant?
b/c congestion occurs when excessive bloodflow
Vasoconstriction uses of adrenomimetic direct acting agonists act at what receptors?
ALPHA
Caridac actions of adrenomimetic direct acting agonist and what agonists cause that action? (2)
1)treat heart block (E, I)
2)treat cardiac arrest (E)
Cardiac actions of adrenomimetic direct acting agonists act where?
Beta receptors
How do adrenomimetic direct acting agonists treat heart block?
stimulate B receptors causing and INCR of AV node conduction
Bronchodilation actions of adrenomimetic direct acting agonist and what agonists cause that action?
treat bronchial asthma (E, I)
Bronchodilation actions of adrenomimetic direct acting agonists act where?
Beta receptors
Cause of allergic asthma (4 steps)
1)Incr in IgE when exposed to antigen
2)IgE affixes to mast cell
3)Degranulation of mast cell causes release of histamine and leukotrienes via exocytosis
4)These both cause bronchoconstriction
Relief of symptoms of bronchial asthma by Beta agonists due to... (2)
1)relaxation of airway smooth muscle
2)inhibition of histamine/LK release by activating B2 receptors on the mast cell membrane
Vasodilation action of adrenomimetic direct acting agonists and what agonists cause that action? (2)
1)treat peripheral vascular disorder (I)
2)treat spasms (I)
Vasodilation actions of adrenomimetic direct acting agonists act where?
Beta adrenergic effects
OTHER direct acting adrenomimetic agonists (4)
1)Methoxamine
2)Clonidine
3)Dobutamine
4)Terbutaline
Methoxamine
a)active at what receptor
b)metabolism
a)ALPHA1
b)NOT by MAO, COMT, or reuptake
Therapeutic uses of Methoxamine (2)
1)hypotensive states
2)tachycardia (decr AV node conduction)
_____ is also selective for ALPHA1
Phenylephrine
Clonidine
a)active @ what receptor
b)Therapeutic uses
a)ALPHA2 in CNS
b)hypertension via decr SNS activity
Clonidine mechanism of decr hypertension (4)
1)decr SNS activity
2)this = decr NE
3)this = decr ALPHA1 stime
4)this results in vasodilation
Apraclonidine
a)active @ what receptor
b)fxn
a)ALPHA 2
b)treat open angle glaucome via decr secretion of aq. humor
Terbutaline
a)active @ what receptor
b)metabolism
c)unique feature
a)B2
b)NOT by MAO, COMT, reuptake
c)NOT catecholamine
Therapeutic uses of Terbutaline (2)
1)bronchial asthma
2)NO INCR in HR b/c no axn @ B1 receptors
OTHER selective B2 receptor agonists (6) (not sure if i need ALL of these)
1)metaproterenol
2)albuterol
3)salmeterol
4)bitolterol
5)fenoterol
6)formoterol
Adverse Effects of ALPHA receptor agonists (3) and how are these effects caused???
1)reduction of peripheral blood flow (ischemia)
2)rebound nasal congestion due to receptor desensitization
3)photophobia via mydriasis

OVERUSE of the drugs
Ischemia results in...
lack of O2 which leads to cell death
Contraindications of ALPHA RECEPTOR AGONISTS (3)
1)diabetes (via decr in insulin)
2)narrow angle glaucoma
3)hypertension (via vasoconstriction)
Adverse effects of BETA receptor agonists (6)
1)hypotension
2)cardiac arrhythmias
3)myocardial necrosis
4)anginal pain (b/c heart using more O2 than is being delivered due to ischemia)
5)tremor (via incr in ACh)
6)tachycardia
Containdications of BETA receptor agonists (3)
1)hyperthyroidism
2)diabetes (b/c incr in glycogenolysis)
3)myocardial ischemia
Mixed acting adrenomimetic (2)
Ephedrine
Amphetamine
Indirect acting adrenomimetic
Tyramine
Basic mechanism of indirect/mixed acting adrenomimetics
release NE from adrenergic neurons
Tyramine
a)metabolism
b)mechanism
c)where found
a)by MAO/reuptake, NOT COMT
b)gets in nerve and releases NE from extravesicular pool
c)in certain foods (beer, cheese)
Ephedrine
a)metabolism
b)mechanism
c)use (2)
a)reuptake but NOT MAO, COMT
b)stimulate alpha/beta receptors AND release extravesicular NE
c)bronchodilator and nasal decongestant
Amphetamine
a)mechanism (2)
1)CNS stimulation
2)get in nerve via passive diffustion and release extravesicular NE, dopamine, serotonin
Block adrenergic neuronal membrane uptake mechanism
a)drugs (3)
a)TRICYCLIC ANTIDEPRESSANTS
b)imipramine
c)amitriptylline
How do Tricyclic Antidepressants work (3)
1)potentiate released NE/E
2)do this by blocking reuptake
3)BUT this blocks effects of INdirect acting drugs and those requiring reuptake for their activity
2 categories of drugs that Block Catecholamine metabolism
1)COMT inhibitors
2)MAO inhibitors
MAO inhibitors fxns (2)
1)antidepressants
2)antihypertensive
Antihypertensive mechanism of MAO inhibitors (2)
1)ganglionic blockade (via blocking nicotinic receptors in autonomic ganglia)
2)formation of false transmitter (tyramine to octopamine)
Tyramine to Octopamine rxn and mechanism it uses for antihypertension
1)tyramine to octopamine via dopamine-B-hydroxylase
2)blocks NE formation in vesicle by tying up the above enzyme
SMALL amounts of tyramine and MAOI's =
hypotensive
LARGE amount of tyramine and NE/adrenomimetics =
hypertensive
SIF cell contains...(2)
1)NE or
2)dopamine
Adrenolytic drug categories (2)
1)adrenergic receptor antagonists
2)prevention of neuronal release of NE
Adrenergic receptor antagonists categories (2)
1)alpha receptor antagonists
2)beta receptor antagonists
Alpha receptor antagonists drugs (4)
1)phentolamine
2)phenoxybenzamine
3)prazosin
4)tamsulosin
Phentolamine mechanism
competitive reversible antagonist of ALL alpha receptor types
Phenoxybenzamine
a)mechanism
b)how to reverse effects
1)irreversible (alkylating) antagonist of ALL alpha receptor types
2)reverse effects via increasing synthesis of alpha receptors
Prazosin
a)mechanism (2)
b)MAINLY used for....and why?
1)competitive reversible antagonist
2)selective for ALPHA1 receptors only

1)HYPERTENSION, b/c selective for alpha1
Therapeutic uses of alpha receptor antagonists (5)
1)treat peripheral vascular spasms
2)hemorrhagic shock treatment via incr SNS so whole blood can be admined
3)hypertension
4)pheochromocytoma
5)treat resistance to urinary outflow in benign prostatic hyperplasia via relaxing trigone and blocking prostatic muscle contraction
Pheochromocytoma
a)what is it
b)consequences
b)treatments (2)
a)tumor that resemble adrenal medulla (have catecholamine in them)
b)incr in NE/E so HTN and incr in cardiac output
c)phenoxybenzamine at first but best is to just remove tumors
Adverse effects of alpha blockers and which is the LIMITING side effect of these drugs (6)
1)severe/postural hypotension****
2)tachycardia via reflex of blocking alpha receptors
3)nasal congestion
4)impotence
5)GI disturbance via PSNS dominance b/c SNS is not stimulating it
6)makes PE ineffective
Tamsulosin mechanism
selective for ALPHA1 receptor antagonism only
Beta receptor antagonists
a)suffix
b)2 of em
a)-olol
b)Propranolol, Metoprolol
Propranolol mechanism
competitive, reversible antagonist for ALL beta receptors
Metoprolol mechanism
competitive, reversible antagonist selective for BETA1 receptor only (heart)
Therapeutic uses of Beta blockers (7)
1)cardiac arrhythmias
2)tachycardia
3)myocardial ischemia/angina
4)hypertension
5)pheochromocytoma (when used simultaneously w/ alpha blocker)
6)open angle glaucoma (via decr in aq. humor production)
7)block ectopic foci from developing
3 ways that Beta blockers treat hypertension
1)recduces sympathetic nerve activity by acting in CNS
2)block renin release from juxtaglomerular apparatus of kidney
3)decr cardiac contractility/output
Ectopic Foci?
spots that develop on heart that have their own beat
How does renin cause incr in BP?
it causes formation of Angiotensin II that incr BP by acting on its receptors or causing release of NE
Adverse effects of Beta blockers (4)
1)heart failure
2)hypotension
3)mental depression
4)nausea and vomiting via PSNS dominance of GI
Contraindications of Beta Blockers and why for first and condition w/ 2nd (2)
1)diabetes b/c block SNS reflex that warns of hypoglycemia AND doesn't allow for SNS incr of glycogenolysis
2)bronchial asthma (use metoprolol b/c its B1 selective)
Drugs that prevent the neuronal release of NE are....
indirect adrenolytics
Prevention of neuronal release of NE categories (4)
1)blockade of release mechanism
2)blockade of NE synthesis leading to NE depletion
3)blockade of NE storage leading to NE depletion
4)formation of "new NT"
Blockade of release mechanism drug
Guanethidine
Guanethidine
a)mechanism (3)
b)prolonged treatment leads to...
b)drug categories (3)
a1)taken into adrenergic neurons by reuptake
a2)block release mechanism by preventing vesicle from attaching to nerve cell memb.
a3)competes w/ NE for reuptake mechanism
b)depletion of NE
c)prevention of neuronal release of NE (blockade of release mechanism), indirect adrenolytic
Therapeutic uses of Guanethidine (2)
1)HTN
2)glaucoma (via decr aq. humor production)
Adverse effects of Guanethidine (5)
1)postural hypotension
2)impotence
3)diarrhea (due to PSNS dominance in GI)
4)nasal congestion
5)heart failure
Contraindication of Guanethidrine and why
Pheochromocytoma b/c of supersensitivity to circulating catecholamines
Blockade of NE synthesis leading to NE depletion drug
alpha-methyl-tyrosine