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78 Cards in this Set

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Example of ganglionic blocker
Hexamethonium
e.g. of neurotransmitter synthesis
metyosine; carbidopa
inhibition of neurotransmitter release
bretylium (anti-arrhythmic); guanethidine (anti-hypertensive)
facilitation of neurotransmitter release e.g.
amphetamine, ephedrine, tyramine (these meds displace NE rather than directly stimulate)
interference with vesicular transmitter storage
reserpine (antihypertensive)
e.g. of blockade of neurotransmitter reuptake
cocaine; desipramine (tricyclic)
e.g. of inhibition of neurotransmitter metabolism
pargyline; selegiline (MAOI)
e.g. agonists interacting with postsynaptic adrenergic receptors
Epi, NE, Isoproterenol
e.g. antagonists interacting with postsynaptic adrenergic receptors
labatelol, prazosin, propranolol
nonselective adrenoreceptor agonists (activate both alpha and beta)
NE, Epi, Dobutamine
nonselective alpha-agonists (3 e.g.)
oxymetazoline, xylometazoline, tetrahydrozoline
alpha 1 selective agonists (3 e.g.)
phenylephrine, metaraminol, methoxamine
alpha 2 selective agonists (3 e.g.)
clonidine, guanabenz, alpha-methyldopa
non-selective beta agonist (1 e.g.)
isoproterenol
beta 1 selective agonist (1 e.g.)
xamoterol
beta 2 selective agonists (2 e.g.)
terbutaline, albuterol
relative receptor affinity

phenylephrine, methoxamine
a1 > a2 >>>>> B
relative receptor affinity

clonidine, methylnorepinephrine
a2 > a1 >>>>> B
relative receptor affinity

norepinephrine
a1 = a2; B1 >> B2
relative receptor affinity

epinephrine
a1 = a2; B1 = B2
relative receptor affinities

dobutamine
B1 > B2 >>>>> a
relative receptor affinities

isoproterenol
B1 = B2 >>>>> a
relative receptor affinities

terbutaline, metaproterenol, albuterol, ritodrine
B2 >> B1 >>>> a
relative receptor affinities

dopamine
D1 = D2 >> B >> a
relative receptor affinities

fenoldopam
D1 >> D2
alpha1 effect on most vascular smooth muscle (innervated)
contraction
alpha1 effect on pupillary dilator muscle
contraction (dilates)
alpha 1 effect on smooth muscle
erects hair
alpa 1 effect on prostate
contraction
alpha 1 effect on heart
increases force of contraction
alpha 2 effect on postsynaptic CNS adrenoreceptors
probably multiple
alpha 2 effect on platelets
aggregation
alpha 2 effect on adrenergic and cholinergic nerve terminals
inhibition of transmitter release
alpha 2 effect on some smooth vascular muscle
contraction
alpha 2 effect on fat cells
inhibition of lypolysis
beta 1 effect on heart
increase rate and force of contraction
beta 2 effect on respiratory, uterine, and vascular smooth muscle
promotes smooth muscle relaxation
beta 2 effect on skeletal muscle
promotes potassium uptake
beta 3 effect on fat cells
activates lypolysis
D1 effect on smooth muscle
dilates renal blood vessels
D2 effect on nerve endings
modulates transmitter release
a1 agonist effects on eye
sympathetic stimulation -- radial muscles contract => midriasis
M3 agonist effects on eye
parasympathetic stimulation -- sphincter muscle contracts, "pushing" pupil back into constriction
alpha 2 agonist effects on eye
decrease production of aqueous humor, leading to decrease in intraocular pressure
beta 2 effects on respiratory system
bronchodilation
alpha 1 effects on respiratory system
reduction of mucosal secretions
GI effects of alpha and beta stimulation
relax smooth muscle, decreasing peristalsis
GI effects of alpha 2 stimulation
reduce digestive secretions
GU: bladder effects of alpha 1 stimulation
bladder base and urethral sphincter contraction => continence
GU: bladder effect of Beta 2
mediate relaxation
GU: prostate effect of alpha 1
constriction
GU: erectile tissue effect of alpha 1
facilitate ejaculation
GU: uterus effect of Beta 2
relaxation, inhibiting labor
Glandular effects: apocrine effects of adrenoreceptor agonists
sweating
Glandular effects: eccrine effects of adrenoreceptor stimulation
(these have muscarinic receptors innervated by sympathetic cholinergic postganglionic nerves)
Glandular effects: insulin effects of Beta receptors
secretion stimulated
Glandular effects: insulin effects of alpha 2 receptors
inhibit insulin secretion
glandular effects: renin secretion effects of B1 versus alpha 2
B1: secretion stimulated
a2: secretion inhibited
metabolic effects: lipolysis (B3 versus alpha 2)
B3: enhances lipolysis
a2: inhibited by a2 receptors on fat cells
metabolic effects: glycogenolysis effects of B receptors on liver
B receptors activate it
metabolic effects of high doses of sympathomimetics
depletion of extracellular potassium and
metabolic acidosis
Direct-acting sympathomimetics: catecholamines

Epinephrine
alpha1 vasoconstriction
B1 intropic, chronotropic, dromotropic
B2 vasodilation, drop in diastolic
Direct-acting sympathomimetics: catecholamines

Norepinephrine
a1: potent vasoconstrictor
B1: same as epi, but inotropic effect prodominates because vagal reflex compensates for chrono and dromotropic effects
B2: no effect, leading to net vasoconstriction, increased TPR, and rise in systolic and diastolic pressure
Direct-acting sympathomimetics: catecholamines

isoproterenol
B1: same as epi; B1 dominates => increase in pulse pressure
a1: no effect
B2: same as epi => decrease in diastolic pressure
Direct-acting sympathomimetics: catecholamines

Dopamine
D1 and presynaptic D2: LOW DOSES --vasodilatory effects on renal vasculature

a1: HIGH DOSES -- stimulates a1 => vasoconstriction
Direct-acting sympathomimetics: catecholamines

Fenoldopam
D1: decreases vascular tone, especially renal; fast-acting
Direct-acting sympathomimetics: catecholamines

Ibopamine
similar to dopamine
Direct-acting sympathomimetics: catecholamines

Dobutamine
B1: selective -- similar to epi's beta effects
a1: isomers offset each other, so racemic mixture needed for vascular equilibrium
Direct-acting sympathomimetics: non-catecholamines

phenylephrine
a1 selective: mydriatic, decongestant and pressor
Direct-acting sympathomimetics: non-catecholamines

methoxamine
a1: prolonged peripheral vasoconstriction and bradycardia mediated by vagal reflex
Direct-acting sympathomimetics: non-catecholamines

midodrine
a1 selective: treats postural hypotension; may cause supine hypertension
Direct-acting sympathomimetics: non-catecholamines

oxymetazoline and xylometazoline
alpha agonists: topical nasal and ocular decong.

large doses may cause clonidine-like a2 stimulation => hypotension
Direct-acting sympathomimetics: non-catecholamines

clonidine, methyldopa, guanabenz
a2 stimulation: reduces outflow of sympathetic signals from vasomotor center in medulla => decrease BP
Direct-acting sympathomimetics: non-catecholamines

Apraclonidine
a2 stimulation in ciliary body of eye, reducing aqueous humor production
Direct-acting sympathomimetics: non-catecholamines

prenalterol and xamoerol
B1 selective, like dobutamine

less tachy and bronchodialation than non-selective B agonists, but tolerance develops over time
Direct-acting sympathomimetics: non-catecholamines

albuterol, terbutaline, pirbuterol, bitolterol, metaproterenol
B2 specific: treat asthma and other lung disorders
Direct-acting sympathomimetics: non-catecholamines

salmeterol and formoterol
B2 selective: longer duration of action (12H) due to higher lipid solubility
Direct-acting sympathomimetics: non-catecholamines

ritodrine
B2 selective: used IV to relax uterus and delay labor