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115 Cards in this Set
- Front
- Back
at what level of the cns/hypothalamus/brainstem do bb work
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cardiac output
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at what level of the cns/hypothalamus/brainstem do kidney blockers work
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reanl retention:
aldosterone adh sns anp |
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at what level of the cns/hypothalamus/brainstem do acei work
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circulating regulation:
ang 2 catecholamine |
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at what level of the cns/hypothalamus/brainstem do alpha blockers work
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direct innervation
a1 receptor b2 receptor |
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central sympatholytics is central mediated inhibition of ----- actiivity
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sympathetic
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what receptors are stimulated in central sympatholytics
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a2 receptors (a2a subtype)
possible inidazoline (I1, I2, I3) |
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what does the endogenous subsrate do
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clonidine displacing substance
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t/f
central sympatholytics are 1st line meds cuz they're very potent |
f
last resort agents due to side effects |
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where do the central sympatholytics work in the brain
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nucleus of solitary tract
ventral lateral medulla |
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activation of the nucleus of solitary tract and the ventral lateral medulla ---- sympathetic nerve activity
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decreases
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majority of the a2 receptors are on the pre/post synaptic side
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postsynaptic
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clonidine will activate nts and rlvm which will ------ motor nucleus of vagus which activate the lowering of CO, hr and bp
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activate
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once the nts and rlvm are acitvated by clonidine, they will then deactivate the --- sympathetic contral centers
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brainstem
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the brainstem sympathetic control centers will ------ the intermediolaterial nucleus
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deactivate
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tthe deactivation ofthe intermediolateraol nucleus will deactivate the ---- ----
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sympathetic ganglia
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a decrease in the sympathetic ganglia will decrease --- release and that will relax --- -----
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NE
blood vessels |
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what hemodynamics effects are decreased
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TPR
HR CO renin release |
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what general hemodynapmic effect is increased
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slight increase in sodium retention
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due to a decrease in NE and increase in Ach, what will be decreased in general hemodynamics
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hr
co |
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due to a block on NE release on the bl vessels what will be decreased
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tpr
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what will cause fluid retention
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slight increase in na retention
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what will cause a decrease in renin release
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effects on the alpha 2 receptors
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advantages:
decreased tpr w/ modest decrease in ------ |
co
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advantages
efficacy --- of age, race, gender |
independent
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t/f
central symp are only suitable for combo tx |
f
monotherapy |
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advantage:
sympatolytics work well in the ---- |
elderly
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t/f
central sym. lytics increase lipids |
f
no effects on lipid |
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why are we moving away from monotherapy
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cuz other agents have less SE
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general se of central sympatholytics
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drowsiness/sedation
dry mouth decreased tear production sexual dysfunction narrow therapeutic range abrupt withdrawal htn |
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why shouldn't you d/c symptolytics abruptly
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withdrawal htn
prone to stroke and mi |
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t/f
sympatholytics have a wide therapeutic range |
f
narrow therapeutic range |
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t/f
men rather take sympathlytics because it can potentiate an erection |
f
sexual dysfunction |
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what is a methyldopa metabolized to
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alpha methylnorepinephine
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what is alpha methylnorepinephine taken up by
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reuptake pump
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what is alpha methylnorepinephine converted to and by what
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converted by normal enzymes to NE
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alpha methyldopa is a potent --- agonist
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a2
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where is a methyldopa converted
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in neuron in brain
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what converts alpha methyldopa to alpha methadopamine
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dopa decarboxylase
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what's in the vesicles w/ ne
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alpha methyl NE
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what acts on the alpha 2 on the brain
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alpha methyl ne
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alpha metha dopa is converted to
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alpha methyl ne
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se of a methyldopa includes:
elevated -----, leading to fluid retention |
na
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t/f
hepatoxicity in methyldopa is irreversible |
f
reversible |
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w/ a methyldopa you can have ---- ---- rxn
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allergic skin
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fever and ---- anemia are se of a methyldopa
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hemolytic
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which sympathlytic can be used during pregnancy and w/ breast feeding mom's
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alpha methyldopa
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t/f
alpha methyldopa is 1st line tx |
f
2-3 line therapy |
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clonidine is a ---- agonist and an ----- agonist
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alpha 2a
imidazoline |
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how does clonidine has acute pressor effects
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bl vessels have both alpha 1 and 2, so clonidin will act on the alpha 2 and cause a some constriction
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overall how does clonidine cause decrease bp
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it decreases nerve activity
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what predicts potency of clonidine
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lipid solubiltiy of analogues
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decrease in sns activity, increase --- activity
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pns
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how will clonidine increase bl glucose
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inhibits insulin secretion
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w/ clonidine the diabetic pt is prone to hyper/hypo glycemia
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hyperglycemia
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clonidine decreases ---- secretion
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ADH/AVP
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clonidine causes --- retention
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na
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if clonidine often causes na retention what's it's often given w/
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diuretic
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a central effect of clonidine
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dry mouth
sedation |
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clonidine has --- activity in the spinal cord
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analgesic
so decreased dose of anesthetic required |
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se of clonidine:
---- rxn impotence -----cardia orthostatic hypotension |
withdrawal
bradycardia |
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what's dangerous about bradycardia in clonidine
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too low other areas of the heart might take over, pacemakers, which migh cause arrhythmias
ischemia! due to low bl flow |
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how is orthostatic hypotension caused
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decrease sympathetic response to a baroreflex
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off label uses of clonidine include:
--- opiate and --- withdrawal |
blunt
cocaine |
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how are withdrawal effects diminshed w/ clonidine
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due to decreased sympathetic
most s/s are due to the sympathetic response |
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t/f
clonidine can be used in adhd, migraines, dysmenorrhea |
t
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clonidine can be used for --- flushing
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menopausal
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clonidne can be used for ---- syndrome
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tourette's
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clonidine chronic ---- in dm w/ ---- ------
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diarrhea
autonomic neuropathy |
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how does clonidine prevent diarrhea
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increase Na and H2O absorption
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hot flashes due to ----
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vasodilation
clonidine has acute pressor effects |
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apraclonidine is --- agonist
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alpha2
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t/f
apraclonidine crosses bbb |
f
doesn't cross bbb |
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decrease------- mediated aqueous humor production
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a2
decreased a2 leads to an increase in aq humor |
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t/f
apraclonidine is doc for glaucoma |
f
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apraclonidine is used after --- sx
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laser
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t/f
apraclonidine is monotx only |
f
used w/ other agents when pressure not controlled |
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brimonidine ----- aq humor outlfow
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increase
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which crosses bbb:
apraclonidine or brimonidine |
brimonidine
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se of briminodine include ---tension and sedation
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hypotension
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why does briminodine cause sedation
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cuz it crosses bbb
central effects |
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apraclonidine is a ---- of the clonidine structure
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modification
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guanabenz has less --- and --- -----
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na and water retention
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t/f
guanabenz is less selective for alpha 2 than clonidine |
f
more selective |
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se of guanabenz
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sedation
dry mouth |
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which has less imdazoline activity
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guanabenz
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which is more potent guanfacin or clonidine
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clonidine
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which has occasional withdrawal symptoms guanabenz or guanfacine
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guanfacine
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which is guanafacine more selective for alpha 1 or 2
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alpha 2
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which has more sedation guanfacine or guanabenz
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guanabenz
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receptor for rilmenidine
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I1
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I1 receptors are in the --- and ---
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RVLM
NTS |
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why is rilmenidine better than clonidine
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fewer classical a2-adrenergic effects
same advantage to lowering bp, but decreased SE |
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few classical alpha 2 effects of rilmenidine
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less dry mouth
minor sedation little na and H2O retention no withdrawal syndrome no orthostatic hypotension |
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t/f
rilmenidine is a new drug approved in the us in 2007 |
f
only in europe |
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--- blocks transport into vesicles
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reserpine
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---- blocks new synthesis of vesicles
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reserpine
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reserpine blocks --- into vesicles and new ---- of vesicles
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transport
synthesis |
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reserpine depletes --- stores
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NE
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t/f
reserpine has peripheral effects only |
f
both central and peripheral |
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what does reserpine decrease
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CO
TPR HR RENIN |
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who's reserpine effective in
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in the elderly w/ diuretic
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why use a diuretic w/ reserpine
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cuz of Na H2O retention
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se of reserpine
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sedation
drowsiness fatigue dysrhythmias depression suicide |
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what did reserpine lead to the discovery of
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tricyclic antidepressants
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to prevent depression what should you do
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slow withdrawal drug
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which drug can cause dysrhythmias
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reserpine
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which drug can tx dysmenorrhea
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clonidine
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which drugs will cause sedation and dry mouth
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guanabenz
rilmenidine (less) clonidine guanfacine (less sedation only) reserpine (sedation only) |
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which drug will cause allergic skin rxn
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alpha methyldopa
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which drug will cause hemolytic anemia
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alpha methyldopa
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hepatotoxic drug
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alpha methyldopa
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which is used during pregnancy
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alpha methyldopa
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there's a + comb's test in ----% , only ---% gave true autoimmune respone
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20%
5% |
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what does comb measure
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antibodies that attack Rh factor on RBC
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which drug causes a false comb's test
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alpha methyldopa
for up to 1 yr |