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78 Cards in this Set
- Front
- Back
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Example of ganglionic blocker
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Hexamethonium
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e.g. of neurotransmitter synthesis
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metyosine; carbidopa
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inhibition of neurotransmitter release
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bretylium (anti-arrhythmic); guanethidine (anti-hypertensive)
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facilitation of neurotransmitter release e.g.
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amphetamine, ephedrine, tyramine (these meds displace NE rather than directly stimulate)
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interference with vesicular transmitter storage
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reserpine (antihypertensive)
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e.g. of blockade of neurotransmitter reuptake
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cocaine; desipramine (tricyclic)
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e.g. of inhibition of neurotransmitter metabolism
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pargyline; selegiline (MAOI)
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e.g. agonists interacting with postsynaptic adrenergic receptors
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Epi, NE, Isoproterenol
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e.g. antagonists interacting with postsynaptic adrenergic receptors
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labatelol, prazosin, propranolol
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nonselective adrenoreceptor agonists (activate both alpha and beta)
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NE, Epi, Dobutamine
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nonselective alpha-agonists (3 e.g.)
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oxymetazoline, xylometazoline, tetrahydrozoline
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alpha 1 selective agonists (3 e.g.)
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phenylephrine, metaraminol, methoxamine
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alpha 2 selective agonists (3 e.g.)
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clonidine, guanabenz, alpha-methyldopa
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non-selective beta agonist (1 e.g.)
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isoproterenol
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beta 1 selective agonist (1 e.g.)
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xamoterol
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beta 2 selective agonists (2 e.g.)
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terbutaline, albuterol
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relative receptor affinity
phenylephrine, methoxamine |
a1 > a2 >>>>> B
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relative receptor affinity
clonidine, methylnorepinephrine |
a2 > a1 >>>>> B
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relative receptor affinity
norepinephrine |
a1 = a2; B1 >> B2
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relative receptor affinity
epinephrine |
a1 = a2; B1 = B2
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relative receptor affinities
dobutamine |
B1 > B2 >>>>> a
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relative receptor affinities
isoproterenol |
B1 = B2 >>>>> a
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relative receptor affinities
terbutaline, metaproterenol, albuterol, ritodrine |
B2 >> B1 >>>> a
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relative receptor affinities
dopamine |
D1 = D2 >> B >> a
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relative receptor affinities
fenoldopam |
D1 >> D2
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alpha1 effect on most vascular smooth muscle (innervated)
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contraction
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alpha1 effect on pupillary dilator muscle
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contraction (dilates)
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alpha 1 effect on smooth muscle
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erects hair
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alpa 1 effect on prostate
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contraction
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alpha 1 effect on heart
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increases force of contraction
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alpha 2 effect on postsynaptic CNS adrenoreceptors
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probably multiple
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alpha 2 effect on platelets
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aggregation
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alpha 2 effect on adrenergic and cholinergic nerve terminals
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inhibition of transmitter release
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alpha 2 effect on some smooth vascular muscle
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contraction
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alpha 2 effect on fat cells
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inhibition of lypolysis
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beta 1 effect on heart
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increase rate and force of contraction
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beta 2 effect on respiratory, uterine, and vascular smooth muscle
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promotes smooth muscle relaxation
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beta 2 effect on skeletal muscle
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promotes potassium uptake
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beta 3 effect on fat cells
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activates lypolysis
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D1 effect on smooth muscle
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dilates renal blood vessels
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D2 effect on nerve endings
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modulates transmitter release
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a1 agonist effects on eye
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sympathetic stimulation -- radial muscles contract => midriasis
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M3 agonist effects on eye
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parasympathetic stimulation -- sphincter muscle contracts, "pushing" pupil back into constriction
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alpha 2 agonist effects on eye
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decrease production of aqueous humor, leading to decrease in intraocular pressure
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beta 2 effects on respiratory system
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bronchodilation
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alpha 1 effects on respiratory system
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reduction of mucosal secretions
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GI effects of alpha and beta stimulation
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relax smooth muscle, decreasing peristalsis
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GI effects of alpha 2 stimulation
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reduce digestive secretions
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GU: bladder effects of alpha 1 stimulation
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bladder base and urethral sphincter contraction => continence
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GU: bladder effect of Beta 2
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mediate relaxation
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GU: prostate effect of alpha 1
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constriction
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GU: erectile tissue effect of alpha 1
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facilitate ejaculation
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GU: uterus effect of Beta 2
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relaxation, inhibiting labor
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Glandular effects: apocrine effects of adrenoreceptor agonists
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sweating
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Glandular effects: eccrine effects of adrenoreceptor stimulation
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(these have muscarinic receptors innervated by sympathetic cholinergic postganglionic nerves)
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Glandular effects: insulin effects of Beta receptors
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secretion stimulated
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Glandular effects: insulin effects of alpha 2 receptors
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inhibit insulin secretion
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glandular effects: renin secretion effects of B1 versus alpha 2
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B1: secretion stimulated
a2: secretion inhibited |
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metabolic effects: lipolysis (B3 versus alpha 2)
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B3: enhances lipolysis
a2: inhibited by a2 receptors on fat cells |
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metabolic effects: glycogenolysis effects of B receptors on liver
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B receptors activate it
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metabolic effects of high doses of sympathomimetics
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depletion of extracellular potassium and
metabolic acidosis |
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Direct-acting sympathomimetics: catecholamines
Epinephrine |
alpha1 vasoconstriction
B1 intropic, chronotropic, dromotropic B2 vasodilation, drop in diastolic |
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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 |
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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 |
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Direct-acting sympathomimetics: catecholamines
Dopamine |
D1 and presynaptic D2: LOW DOSES --vasodilatory effects on renal vasculature
a1: HIGH DOSES -- stimulates a1 => vasoconstriction |
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Direct-acting sympathomimetics: catecholamines
Fenoldopam |
D1: decreases vascular tone, especially renal; fast-acting
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Direct-acting sympathomimetics: catecholamines
Ibopamine |
similar to dopamine
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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 |
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Direct-acting sympathomimetics: non-catecholamines
phenylephrine |
a1 selective: mydriatic, decongestant and pressor
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Direct-acting sympathomimetics: non-catecholamines
methoxamine |
a1: prolonged peripheral vasoconstriction and bradycardia mediated by vagal reflex
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Direct-acting sympathomimetics: non-catecholamines
midodrine |
a1 selective: treats postural hypotension; may cause supine hypertension
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Direct-acting sympathomimetics: non-catecholamines
oxymetazoline and xylometazoline |
alpha agonists: topical nasal and ocular decong.
large doses may cause clonidine-like a2 stimulation => hypotension |
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Direct-acting sympathomimetics: non-catecholamines
clonidine, methyldopa, guanabenz |
a2 stimulation: reduces outflow of sympathetic signals from vasomotor center in medulla => decrease BP
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Direct-acting sympathomimetics: non-catecholamines
Apraclonidine |
a2 stimulation in ciliary body of eye, reducing aqueous humor production
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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 |
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Direct-acting sympathomimetics: non-catecholamines
albuterol, terbutaline, pirbuterol, bitolterol, metaproterenol |
B2 specific: treat asthma and other lung disorders
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Direct-acting sympathomimetics: non-catecholamines
salmeterol and formoterol |
B2 selective: longer duration of action (12H) due to higher lipid solubility
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Direct-acting sympathomimetics: non-catecholamines
ritodrine |
B2 selective: used IV to relax uterus and delay labor
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