Term
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Definition
CI of tyrosine hydroxylase; depletes catecholamines everywhere (sedation/depression, crystalluria, GI)
use: pheochromocytoma |
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Term
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Definition
convert to a-methyl NE. false NT. acts in CNS only.
decrease sympathetic nerve activity. |
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Term
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Definition
| prevents NE release from terminal. obsolete. |
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Term
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Definition
blocks vesicular pump (VMAT) in monoamine neurons, decreases stored NE. affects peripheral resistance and CNS.
use: HTN
contra: depression (can cause severe) |
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Term
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Definition
| inhibits Uptake I in presynaptic neurons (enhancing sympathetic). local anesthetic. |
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Term
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Definition
| NE indirect sympathomimetic |
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Term
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Definition
| alpha and b1 receptors agonist. |
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Term
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Definition
alpha and beta receptors agonist.
use: acute anaphylaxis or cardiac arrest. w/ local anesthetics. |
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Term
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Definition
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Term
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Definition
alpha 1 receptors agonist.
use: nasal decongestants, w/ local anesthetic, maint of BP, treat of PAT, eye drops, mydriatic. |
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Term
| ephedrine, pseudoephedrine |
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Definition
alpha and beta receptors agonist. CNS activity.
se: nasal decongestants, w/ local anesthetic, maint of BP, treat of PAT, eye drops, mydriatic. also CNS effects.
indirect sympathomimetic of NE. |
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Term
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Definition
alpha 2 receptor agonist. acts in CNS, decreases sympathetic activity to heart and BVs.
prob: sedation, dry mouth
also: glaucoma, analogs decrease secretion of intraocular fluid |
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Term
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Definition
beta 2 receptor agonist. bronchodilates. relaxes uterus for premature labor.
use: rescue therapy for asthma. |
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Term
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Definition
| long acting beta 2 receptor agonist. bronchodilator, NOT suitable for rescue therapy. |
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Term
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Definition
dopamine (D1) receptor agonist. dilates BV in kidney.
use: SHOCK (maybe CHF) |
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Term
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Definition
vasocontrict (innervated)
pupillary dilation
ejaculation
inhibition of micturation
GI inhibition |
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Term
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Definition
vasoconstriction (uninnervated)
prejunctional inhibition of NE release |
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Term
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Definition
cardiac stimulation (innervated)
secretion of renin |
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Term
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Definition
cardiac stimulation (uninnervated, minor)
bronchodilation
uterine relaxation
vasodilation (uninnervated)
glycogenolysis (liver) |
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Term
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Definition
decreased BP
increased HR (reflex)
nasal congestion
decreased ejaculation
sedation/depression |
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Term
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Definition
competitive alpha blocker
epi reversal |
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Term
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Definition
irreversible alpha blocker
use: pheochromocytoma
problem: excessive cardiac stimulation, more than just baro reflex |
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Term
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Definition
alpha 1 selective antagonist.
decrease TPR and reduce sympathetically-mediated SM stimulation.
use: hypertension, CHF, BPH
problem: first dose phenom = hypotension/syncope |
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Term
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Definition
angina
cardiac arrythmia
hypertension
post MI
CHF? |
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Term
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Definition
beta blocker. competitive antagonist at beta adrenergic receptors. MSA
uses: HTN, angina, arrythmia, MI
problem: first pass effect
comp: cardiac depression, bronchoconstriction, hypoglycemia (masked), CNS sedation. t1/2=3-4 hours |
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Term
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Definition
2nd gen beta blocker. selective antagonist at b1 receptors. cardioselectivity.
use: HTN, angina, cardiac arrythmia, post MI, CHF. MSA
problem: t1/2=3-4 hours |
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Term
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Definition
beta blocker.
cardioselectivity.
renal clearance (as opposed to hepatic)
t1/2=6-9 hours |
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Term
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Definition
beta blocker.
Intrinsic Sympathomimetic Activity. partial agonist at all beta adrenergic receptors.
advantages: less cardiac depression, less bronchoconstriction, reduces peripheral resistance
compared to propanolol, doesn't reduce resting HR. both prevent exercised induced increase. |
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Term
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Definition
ultra short acting.
t1/2=5-10 minutes, enzymatic clearance.
infused to reduce cathecholamine induced cardiac stimulation in surgery. |
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Term
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Definition
| first beta blocker shown to reduce mortality in CHF (excessive catecholamine stimulation of heart accelerates failure long term) |
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Term
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Definition
| destroys presynaptic proteins involved in ACh release |
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Term
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Definition
activates muscarinic ACh receptors on target tissues (parasymp and sweat glands).
G protein mediated.
symptoms: bradycardia, nausea cramps vomit, bronchconstriction, SALIVATION, SWEATING, hypotension b/c of uninnervated muscarinic receptors in BV.
No CNS activity. |
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Term
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Definition
stimulates muscarinic receptors.
use: treatment of open angle glaucoma, relief of dry mouth due to hypofunction of glands |
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Term
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Definition
synthetic ACh analog
GI stimulation or treatment of urinary retention.
highly charged, rapid clearance.
totally insensitive to AChE because of structure |
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Term
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Definition
synthetic ACh analog
provocative test for hyperreactive airways.
highly charged, rapid clearance. |
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Term
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Definition
muscarinic receptor antagonist.
glands: decreased secretions
eye: mydriasis, cycloplegia
CV: increased HR (no change in BP)
Resp: block vagal bronchoconstriction
bladder: decreased tone and constricted sphincter
GI: decreased motility and tone
CNS: block muscarinic receptors |
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Term
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Definition
more lipid soluble.
anti-muscarinic, more CNS effects.
use: motion sickness (transdermal)
prob: dry mouth, blurred vision, sedation |
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Term
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Definition
anti-muscarinic. charged so poor absorption, little systemic effect.
use: treatment of asthma and COPD
prob: few, toxic doses cause hypotension (ganglionic blockade) and muscle weakness (neuromuscular blockade) |
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Term
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Definition
anti-muscarinic w/ no selectivity in prodrug form.
use: overactive bladder
problems: lower incidence than other anti-muscarinic (but dry mouth, constipation) |
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Term
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Definition
nicotinic receptor agonist, ion channels with Na and K permeability.
all autonomic ganglia, NMJ, sensory nerve endings, CNS
CNS: stimulation, vomiting, ADH
CV: mostly stimulates SNS
GI, glands: PSNS stimuation, then BLOCK
NMJ: depolarizing blockade |
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Term
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Definition
nicotinic partial agonist, acts in CNS.
produces low release of dopamine at reward centers (reducing withdrawal)
blocks binding of nicotine (and positive reinforcement)
t1/2=24 hours, excreted unchanged in urine.
adverse: NAUSEA, headache, abnormal dreams
FDA warning: mood changes? |
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Term
| hexamethonium, mecamylamine |
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Definition
ganglionic nicotinic receptor antagonist.
paralysis of entire autonomic nervous system.
uses (limited): HTN, dissecting AA, autonomic hyperreflexia |
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Term
| predominant tone and effect of blockage |
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Definition
aterioles, SNS, hypotension
sweat glands, SNS, decreased perspiration
heart rate, PSNS, tachycardia
eye, PSNS, mydriasis, cycloplegia
gut, PSNS, decreased tone/motility
bladder, PSNS, urinary retention
salivary glands, PSNS, dry mouth |
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Term
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Definition
competitive inhibitor of acetylcholinesterase
use: test for MG, some alzheimer's benefit |
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Term
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Definition
cholinesterase substrate inhibitor
slower rxn (hydrolysis than ACh)
use: paralytic ileus or bladder, glaucoma, alzheimer's, MG |
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Term
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Definition
cholinesterase substrate inhbitor
slower rxn (hydrolysis) than ACh
charged, low bioavailability, high GI effect
use: paralytic ileus or bladder, glaucoma, alzheimer's, MG |
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Term
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Definition
organophosphate
irreversible cholinesterase substrate inhibitor
use: glaucoma. |
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Term
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Definition
| organophosphate irreversible cholinesterase inhibitor |
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Term
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Definition
| insecticide, organophosphate cholinesterase inhibitor |
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Term
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Definition
| reacts with irreversibly bound phosphate, reactivating AChE |
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