Term
sympathetic nervous system |
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Definition
-Important regulator of activities of organs -Especially in responses to stress -Regulator of heart and peripheral vasculature |
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Definition
Drugs that mimic stimulation of sympathetic nervous system |
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Definition
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Definition
drug acts directly on the receptor |
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Term
example of direct activation |
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Definition
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Term
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Definition
Drug actions depend on release of endogenous catecholamines |
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Term
mechanisms of indirect activation |
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Definition
1. displacement 2. reuptake inhibition 3. blockade of metabolism |
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Term
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Definition
Drug causes displacement (dumping) of stored catecholamines |
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Definition
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Term
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Definition
Drugs can inhibit reuptake of catecholamines already released |
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Term
examples of re-uptake inhibition |
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Definition
cocaine and tricyclic antidepressants |
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Term
Blockade of metabolism occurs via |
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Definition
Catechol-O-methyltransferase (COMT) Monoamine oxidase (MAO) |
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Term
blockade or inhibition enzymes |
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Definition
Increases stores of catecholamines Indirectly potentiates sympathomimetic actions Example: MAO Inhibitors (Parnate, Nardil, Marplan) |
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Term
examples of MAO inhibitors |
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Definition
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Term
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Definition
Drugs can be classified by the receptors they activate |
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Term
example of spectrum of action |
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Definition
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Definition
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Definition
derived from amino acid-tyrosine |
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Term
availability of catecholamines |
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Definition
Endogenously (released from adrenal glands during stress) and As a drug |
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Term
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Definition
Not given orally- Rapidly metabolized by COMT and MAO |
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Term
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Definition
Given parentally- Short duration of action Does not significantly enter CNS through IV route |
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Term
examples of Phenylisopropylamines |
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Definition
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Term
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Definition
Are NOT catecholamines NOT metabolized by COMT and MAO Given orally Enter CNS readily Effects last longer than catecholamines |
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Term
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Definition
Sympathomimetic found in foods Not a phenylisopropylamine Is rapidly metabolized by MAO MAO Inhibitor drugs can cause tyramine toxicity |
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Term
Mechanism of Action of Sympathomimetics |
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Definition
Act via principal receptors
α – receptors ß – receptors DA – receptors |
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Definition
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Definition
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Term
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Definition
Response to drugs differs in various tissues |
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Term
Beta adrenoreceptors subtypes |
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Definition
- ß1 and ß2 (ß3 novel) - defined by affinity for EPI and NE |
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Definition
EPI = NE (equal affinity) |
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Definition
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Definition
Distinct from α and ß receptors Mainly important in brain and splanchnic and renal vasculature Highly relevant to behavior and Parkinson’s Disease |
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Term
dopamine receptors main subtypes |
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Definition
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Term
dopamine receptors subtypes within subtypes |
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Definition
D1 like- D1 , D5 D2 like- D2 , D3 , D4 AE and efficacy of antipsychotic drugs vary between subtypes |
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Definition
Drug may prefer to bind to one subgroup over another at low concentrations Not absolute (“specificity” is nearly absolute) Numeric subclass is important for drugs with selectivity |
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Definition
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Definition
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Term
prostate drugs α1 blocker |
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Definition
Hytrin (terazosin)
Lowers BP and relaxes neck of bladder |
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Term
prostate drugs α1A blocker |
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Definition
Flomax (tamsulosin) developed α1A selective, found mostly in prostate & neck bladder Results in bladder relaxation without so much BP lowering more selective |
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Term
Effects of catecholamines |
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Definition
are mediated by cell surface receptors |
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Term
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Definition
are coupled by G (guanine) proteins to produce their effects |
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Term
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Definition
is changing intracellular calcium concentration |
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Term
Stimulation of α1 receptors leads to |
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Definition
-activation of Gq-coupling protein
-This leads to release of IP3 and DAG
-IP3 stimulates release of sequestered stores of Ca++
-Increase in intracellular Ca++ causes contraction/constriction |
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Definition
Phenylephrine Effects: increase IP3, DAG |
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Definition
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Definition
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Definition
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Term
Stimulation of β receptors |
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Definition
-activate Gs coupling protein
-Results in activation of adenylyl cyclase
-Catalyzes conversion of ATP to cAMP
-Leads to Ca++ influx and release of sequestered Ca++
-Cardiac tissue=heart contractility
-SA node=increased HR
-Smooth muscle=muscle relaxation |
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Term
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Definition
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Term
beta 1 receptor antagonist |
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Definition
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Term
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Definition
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Term
beta 2 receptor antagonist |
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Definition
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Term
beta 1 and 2 receptor agonist |
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Definition
isoproterenol -increase CAMP |
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Term
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Definition
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Term
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Definition
Stimulates adenylyl cyclase = ↑ cAMP in smooth muscle = relaxation of smooth muscle (vasodilator) |
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Definition
Inhibit adenylyl cyclase = ↓ cAMP, open K channels and ↓ Ca influx |
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Term
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Definition
Fenoldopam (used for severe HTN) Effect: increase cAMP |
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Definition
Bromocriptine - many uses, Infertility, Parkinson‘s, prevent lactation Effect: decrease cAMP |
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Definition
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Definition
Clozapine- Effect: decrease cAMP |
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Definition
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Definition
tissue becomes less responsive with repeated exposure by agonist a.k.a-tolerance, refractoriness and tachyphylaxis |
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Term
Homologous desensitization |
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Definition
– loss of responsiveness exclusively only to directly exposed receptors |
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Term
Heterologous desensitization |
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Definition
loss of responsiveness to exposed and some non-exposed receptors |
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Term
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Definition
most vascular smooth muscle- constriction |
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Term
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Definition
pupillary dilator muscle- contraction= dilation of pupil |
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Definition
pilomotor smooth muscle- erects hair |
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Definition
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Definition
heart- increases force of contraction |
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Definition
postsynaptic CNS adrenoceptors- multiple effects |
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Definition
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Definition
adrenergic nerve terminals- inhibition of transmitter release |
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Definition
cholinergic nerve terminals- inhibition of transmitter release |
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Definition
some vascular smooth muscle- contraction |
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Definition
fat cells- inhibition of lipolysis |
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Definition
pancreatic B cells- inhibits insulin release |
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Definition
heart- increase force and rate of contraction |
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Definition
kidney (juxtaglomerular cells)- increase renin release |
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Definition
respiratory muscle- promote smooth muscle relaxation |
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Definition
uterine muscle- promote smooth muscle relaxation |
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Term
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Definition
vascular smooth muscle- promote smooth muscle relaxation |
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Definition
skeletal muscle- promotes potassium uptake= tremor |
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Definition
pancreatic B cells- increase insulin release |
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Term
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Definition
liver- activates glycogenolysis= increase glucose |
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Definition
fat cells- stimulates lipolysis |
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Definition
renal blood vessels- dilates renal blood vessels |
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Term
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Definition
splanchnic blood vessels- dilates renal blood vessels |
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Term
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Definition
nerve endings- modulates transmitter release |
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Term
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Definition
control peripheral vascular resistance |
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Term
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Definition
increase arterial resistance |
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Term
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Definition
promote smooth muscle relaxation |
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Term
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Definition
promote vasodilation of kidneys playing a role in natriuresis |
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Term
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Definition
effect depending on anatomical site |
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Term
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Definition
Largely determined by β1 receptors |
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Term
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Definition
-Activation results in Ca++ influx -SA node & purkinje fibers increase – positive chronotropic effect -AV node – conduction velocity ↑ & refractory period ↓ -Intrinsic contractility is increased – positive inotropic effect and relaxation is accelerated -Ejection time is decreased |
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Definition
-Produces peripheral vasoconstriction and resistance
-↑ SBP and DBP |
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Term
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Definition
Increases cardiac output (↑ HR and contractility) |
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Term
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Definition
Vasodilatation and ↓ peripheral vascular resistance |
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Definition
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Definition
increases outflow of aqueous humor from the eye – reduces IOP |
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Term
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Definition
decrease production of aqueous humor |
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Term
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Definition
decrease in accommodation- ciliary muscle |
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Term
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Definition
relaxation- bronchodilation |
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Term
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Definition
vasoconstriction- Blood vessels of upper respiratory tract mucosa (sinuses) |
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Term
a receptors mostly (b also) |
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Definition
GI smooth muscle relaxation |
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Term
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Definition
decrease salt and water flux into the lumen of the intestine |
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Term
a and b receptors contained? |
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Definition
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Term
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Definition
mediate contraction – promotes urinary incontinence |
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Term
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Definition
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Term
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Definition
Ejaculation- (ductus deferens, seminal vesicles & prostate) |
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Term
Many symphathomimetic drugs causes what? |
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Definition
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Term
apocrine sweat glands is stimulated by? |
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Definition
adrenoceptor stimulants that causes sweaty palms |
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Term
b3 in fat cells causes what? (metabolic) |
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Definition
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Term
increase in glycogenolysis in liver cause an increase in? |
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Definition
glucose (sympathomimetic drugs) |
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Term
insulin secretion is stimulated by this receptor? |
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Definition
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Term
insulin secretion is inhibited by this receptor? |
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Definition
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Term
renin secretion is stimulated by this receptors? |
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Definition
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Term
renin secretion is inhibited by this receptors? |
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Definition
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Term
beta blockers can lower what? |
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Definition
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Term
leukocytosis or an increase in WBC can be caused by what? |
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Definition
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Term
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Definition
Actions vary dramatically Depending on ability to cross BBB Usually cross in high rates of infusion Nervousness, tachycardia, tremor Elevation of mood, insomnia, anorexia |
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Term
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Definition
Epinephrine
Norepinephrine
Isoproterenol
Fenoldopam |
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Term
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Definition
Dopamine
Dopamine agonist
Dobutamine |
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Term
Epinephrine (adrenaline) is a potent agonist at all? |
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Definition
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Term
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Definition
increases BP and vasoconstriction |
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Term
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Definition
increase HR and increase contractility= cardiac stimulation |
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Term
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Definition
blood vessel dilation in skeletal muscle= bronchodilation |
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Term
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Definition
levarterenol and noradrenaline |
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Term
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Definition
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Term
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Definition
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Term
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Definition
a1 is greater than b1 and little effect on b2 |
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Term
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Definition
increase PVR and both SBP and DBP |
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Term
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Definition
increase BP = vasoconstriction |
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Term
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Definition
increase HR and increase contractility= cardiac stimulation |
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Term
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Definition
isoproterenol or isoprenaline |
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Term
Isoproterenol (isoprenaline) |
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Definition
Potent β- agonist (little α- effect) |
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Term
Isoproterenol (isoprenaline) |
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Definition
Positive chronotropic & inotropic actions= ↑ cardiac output |
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Term
Isoproterenol (isoprenaline) |
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Definition
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Term
Isoproterenol (isoprenaline) |
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Definition
↓ in diastolic & mean arterial pressure |
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Term
Isoproterenol (isoprenaline) b1 agonist |
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Definition
increase HR and increase contractility= cardiac stimulation |
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Term
Isoproterenol (isoprenaline) b2 agonist |
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Definition
blood vessel dilation in skeletal muscle= bronchodilation |
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Term
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Definition
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Term
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Definition
Activates presynaptic D2=↓ EPI release |
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Term
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Definition
Activates D1 and β2 = vasodilation (↓ PVR) |
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Term
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Definition
Activates β1 in the heart = some ↑ in HR |
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Term
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Definition
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Term
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Definition
High doses = activates α; mimics EPI |
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Term
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Definition
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Term
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Definition
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Term
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Definition
IV treatment of severe HTN |
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Term
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Definition
Bromocriptine-dopamine 2 agonist |
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Term
Bromocriptine-dopamine 2 agonist |
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Definition
Tx of Parkinson’s disease |
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Term
Bromocriptine-dopamine 2 agonist |
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
Phenylephrine (Neo-synephrine) is an? |
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Definition
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Term
Phenylephrine (Neo-synephrine) is used for? |
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Definition
decongestant and to increase BP |
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Term
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Definition
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Term
midodrine is used for treating? |
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Definition
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Term
Ephedrine (ma-huang) is a stimulant that releases? |
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Definition
catecholamines (never studied) |
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Term
Oxymetazoline (Afrin, Visine) is a? |
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Definition
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Term
Oxymetazoline (Afrin, Visine) is a vasoconstrictor used for? |
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Definition
decongestant and decrease eye redness |
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Term
Oxymetazoline (Afrin, Visine) is a type of drug? |
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Definition
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Term
Amphetamine is misused as a? |
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Definition
CNS stimulant (anorexiant and alertness) |
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Term
Amphetamine is a stimulant that releases? |
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Definition
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Term
Methamphetamine is similar to what? |
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Definition
amphetamine but more CNS effect |
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Term
Methylphenidate (Ritalin) is stimulant used for? |
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Definition
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Term
pemoline is a stimulant used for? |
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Definition
ADHD but no longer available due to hepatic failure |
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Term
modafinil or provigil is a stimulant used for? |
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Definition
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Term
a2 agonists are used for? |
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Definition
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Term
give examples of a2 agonists? |
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Definition
clonidine, methyldopa, guanfacine, guanabenz |
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Term
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Definition
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Term
an example of a beta 1 selective agonist is? |
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Definition
-dobutamine - Less vasodilation (less β2) = increase CO w/less tachycardia |
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Term
beta 2 selective agents are? |
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Definition
-Albuterol -used for asthma
-Terbutaline -used for uterine relaxation (premature labor) |
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Term
an example of a special sympathomimetics is? |
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Definition
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Term
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Definition
nerve permeability to Na=↓nerve impulse conduction Topical anesthetic (oral and nasal membranes) |
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Term
cocaine stimulates the release of? |
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Definition
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Term
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Definition
reuptake - stimulant/sympathomimetic |
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Term
cocaine stimulates the release of ? |
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Definition
DA and inhibits reuptake that causes significant euphoria = addiction |
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Term
an example of a special sympathomimetic drug? |
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Definition
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Term
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Definition
Natural occurring in body Also found in some fermented foods Not a drug, but interacts with drugs |
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Term
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Definition
Rapidly degraded by MAO in gut and liver When MAO is not available to degrade tyramine = high amounts of tyramine = release of catecholamines MAO inhibitors (Nardil, Marplan, Parnate) Results in sympathomimetic effects Increase in BP |
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Term
examples of MAO inhibitors are ? |
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Definition
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Term
Foods that contain tyramine? |
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Definition
Beer Broad beans/fava beans Cheese Chicken liver Chocolate |
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Term
Foods that contain tyramine ? |
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Definition
sausage Salami Pepperoni Pickled herring Snails Red wine |
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Term
medications that are needed to enhance blood flow and pressure? |
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Definition
Norepinepherine Phenylephrine Methoxamine Ephedrine Midodrine |
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Term
shock is a reduction in ? |
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Definition
perfusion of vital tissues |
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Term
3 major mechanisms responsible for shock |
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Definition
Hypovolemia Cardiac insufficiency Altered vascular resistance |
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Term
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Definition
One of the mainstays of treatment of shock |
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Term
volume replacement is an ? |
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Definition
Efficacy of sympathomimetic drugs are used but efficacy unclear |
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Term
medications for treating cardiogenic shock? |
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Definition
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Term
cardiogenic shock is usually due to ? |
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Definition
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Term
cardiogenic shock have poor ? |
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Definition
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Term
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Definition
positive inotropic agents with little peripheral vasoconstriction |
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Term
Conditions in which reduction of local or regional blood is needed |
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Definition
Achieving hemostasis in surgery Reducing diffusion of anesthetics away from site of administration Reducing mucous membrane congestions α receptor activation usually desired |
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Term
EPI (cardiovascular applications) |
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Definition
topical nasal packs for epistaxis In gingival string for gingivectomy Combined with local anesthetics prolongs effects and reduces toxicity |
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Term
cocaine (cardiovascular applications) |
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Definition
Used for nasopharyngeal surgery Has combination hemostatic and local anesthetic effect |
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Term
phenylphrine (cardiovascular applications) |
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Definition
Used for nasal decongestant Prolonged use can cause rebound congestions due to ischemic changes |
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Term
isoproterenol (cardiovascular application) is used for? |
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Definition
Emergency management of complete heart block and cardiac arrest |
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Term
EPI (cardiovascular application) is used for ? |
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Definition
Emergency management of complete heart block and cardiac arrest |
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Term
dobutamine (cardiovascular application) is used for ? |
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Definition
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Term
type of b2 selective agents ? |
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Definition
metaproterenol, terbutaline, and albuterol |
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Term
metaproterenol is used for ? |
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Definition
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Term
terbutaline is used for ? |
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Definition
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Term
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Definition
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Term
anaphylaxis affect both ? |
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Definition
respiratory and CV system |
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Term
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Definition
Bronchospasm
Mucous membrane congestion
Angioedema
Severe hypotension |
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Term
what is the treatment of anaphylaxis ? |
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Definition
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Term
phenylephrine is what type of medication? |
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Definition
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Term
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Definition
mydriatic agent to facilitate examination of the retina |
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Term
apraclonidine and brimonidine (a2 agonist) is what type of medication ? and what are they used for ? |
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Definition
ophthalmic medication and are used to lower IOP (glaucoma) |
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Term
ritodrine and terbutaline are medications of the ? |
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Definition
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Term
ritodrine and terbutaline are b2 agonists that are used to what? |
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Definition
relaxes the uterus and suppress premature labor |
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Term
amphetamines are medication used for the ? |
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Definition
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Term
amphetamines are used for the following effects? |
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Definition
mood elevating (euphoria) causing abuse Increases alertness (modafinil for narcolepsy) Improved attention (ADHD) Appetite suppressant |
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Term
toxicity effects of sympathomimetic drugs on CV system? |
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Definition
increase BP, increased cardiac work which precipitates cardiac ischemia and failure |
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Term
toxicity effects of sympathomimetic drugs on CNS ? |
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Definition
restlessness, tremor, insomnia, anxiety and induced paranoid state |
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Term
cocaine toxicity of sympathomimetic drugs ? |
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Definition
convulsions, cerebral hemorrhage, arrhythmias, MI |
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Term
alpha receptor antagonists can be ? |
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Definition
reversible or irreversible |
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Term
alpha receptor antagonist (reversible) |
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Definition
Dissociate from receptors & can be surmounted by high agonist concentrations Duration of action depends on t1/2 and rate of dissociation from receptor |
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Term
examples of apha receptor antagonist (reversible)? |
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Definition
prazosin and phentolamine |
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Term
alpha receptor antagonists (irreversible) |
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Definition
Do not dissociate & can’t be surmounted Effects of drug may persist after drug has cleared plasma |
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Term
an example of alpha receptor antagonist ? |
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Definition
Phenoxybenzamine- restoration of tissue responsiveness is dependent on synthesis of new receptors which takes several days |
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Term
cardiovascular effects of alpha receptor antagonists can ? |
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Definition
Cause lowering of peripheral vascular resistance and blood pressure |
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Term
often causes of alpha receptor antagonist are ? |
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Definition
Postural hypotension Reflex tachycardia More selective to alpha-1 the less tachycardia |
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Term
other effects of alpha receptor antagonists are ? |
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Definition
Miosis (constriction of pupil) Nasal stuffiness Decrease resistance in urine flow |
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Term
an example of a specific alpha blocking agents is ? |
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Definition
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Term
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Definition
-Antagonist at alpha 1 & 2
-Causes reduction in peripheral resistance
-Has limited absorption after oral administration
-Half life is 5-7 hrs
-Adverse effect: HA, nasal congestion, severe tachycardia, arrhythmias & myocardial ischemia |
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Term
phentolamine is used for treating ? |
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Definition
pheochromocytoma and erectile dysfunction |
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Term
an example of specific alpha blocking agents is ? |
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Definition
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Term
Phenoxybenzamine is used for treating ? |
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Definition
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Term
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Definition
Irreversible blockade Long duration of action:14-48 h or longer Somewhat selective for alpha-1 Also blocks H1, acetylcholine and serotonin Adverse effects: postural hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation Other effects: fatigue, sedation & nausea |
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Term
an example of a specific alpha blocking agent is? |
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Definition
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Term
prazosin is used for treating ? |
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Definition
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Term
prazosin (minipress) is ? |
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Definition
Highly selective for alpha-1 Significantly less tachycardia because less blocking of α-2 Relaxation of both arterial & venous vascular smooth muscle and smooth muscle of prostate Metabolized by the liver Half life: 3 hrs |
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Term
an example of a specific alpha blocking agents is ? |
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Definition
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Term
terazosin (hytrin) is used for treating ? |
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Definition
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Term
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Definition
Alpha-1 selective Metabolized in the liver Half life: 9-12 hrs |
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Term
an example of a specific alpha blocking agent is ? |
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Definition
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Term
doxazosin is used for treating ? |
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Definition
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Term
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Definition
Half life: 22 hrs longer than prazosin and terazosin |
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Term
an example of a specific alpha blocking agent is ? |
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Definition
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Term
Tamsulosin (Flomax) used for treating ? |
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Definition
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Term
|
Definition
Selective to alpha-1A subtype Greater potency in inhibiting contraction in prostate smooth muscle than vascular smooth muscle compared to other alpha blockers Half life: 9-15 hrs |
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Term
examples of other alpha antagonists are |
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Definition
alfuzosin (uroxatrol), indoramin, urapidil (european drug), labetalol, yohimbine |
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Term
alfuzosin (uroxatrol) is used for treating ? |
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Definition
BPH
Selective alpha-1 antagonist
Half life: 5 hrs |
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|
Term
indoramin is used for treating ? |
|
Definition
HTN
selective alpha 1 antagonist |
|
|
Term
urapidil is used for treating ? |
|
Definition
|
|
Term
labetalol is used for treating ? |
|
Definition
HTN both a1 and beta blocker |
|
|
Term
examples of neuroleptic drugs ? |
|
Definition
chlorpromazine and haloperidol |
|
|
Term
chlorpromazine and haloperidol are ? |
|
Definition
potent DA receptro antagonists
also alpha antagonists
contributes to AE of hypotension |
|
|
Term
|
Definition
|
|
Term
|
Definition
abruptly reverse the antihypertensive effects of alpha 2 agonist (clonidine) Serious drug interaction |
|
|
Term
|
Definition
alpha 2 selective antagonist |
|
|
Term
|
Definition
Tumor usually found on the adrenal medulla Typically releases EPI & NE in excess Sx: HTN, HA, palpitations & ↑ sweating Unavoidable release of catecholamines can occur during surgery |
|
|
Term
pheochromocytoma can be pretreated by this medication to control HTN before surgery ? |
|
Definition
|
|
Term
can use this medication for hypertensive emergency ? |
|
Definition
|
|
Term
this medication can be use for treating mild to moderate hypertension ? |
|
Definition
member of prazosin family |
|
|
Term
|
Definition
Interesting side effect of α-1 selective blockers Occurs within 1-3 hours of 1st dose or increased dose Transient dizziness or faintness Palpitations Orthostatic hypotension Helps to have patient take 1st or 1st increase dose at bedtime |
|
|
Term
drugs that are used for peripheral vascular disease ? |
|
Definition
phentolamine, prazosin, or phenoxybenzamine
May be used in Raynaud’s phenomenon or other conditions involving excessive reversible vasospasms |
|
|
Term
phentolamine is used to ? |
|
Definition
reverse intense local vasoconstriction caused by inadvertent infiltration of catecholamines into subcutaneous tissue that was intended to be IV |
|
|
Term
preferred drug for urinary obstruction (BPH) ? |
|
Definition
tamsulosin- Relieving symptoms involves reversal of smooth muscle contraction of neck of bladder and enlarged prostate
prazosin, doxazosin, & terazosin considered if HTN as well |
|
|
Term
drugs that are used to treat erectile dysfunction ? |
|
Definition
phentolamine with nonspecific smooth muscle relaxant papaverine
phentolamine with nonspecific smooth muscle relaxant papaverine Helps with ED when directly injected into penis Longterm use can cause fibrotic changes Other AE: priapism, orthostatic hypotension |
|
|
Term
|
Definition
little clinical usefulness
Research looking into Raynaud’s phenomenon-inhibit smooth muscle contraction Type 2 DM (alpha 2 inhibits insulin secretion) Psychiatric depression |
|
|
Term
common features of beta blockers ? |
|
Definition
Occupy & block catecholamines effects at β receptors End in –olol or –alol |
|
|
Term
differences of beta blockers ? |
|
Definition
Cardioselectivity Partial agonist activity/ISA Lipid solubility |
|
|
Term
receptors that are all over the body but predominate in certain tissues and organs ? |
|
Definition
|
|
Term
receptors that are in teh heart and kidney ? |
|
Definition
|
|
Term
the stimulation of b1 receptors causes ? |
|
Definition
↑HR, ↑contractility, ↑renin release= increase BP |
|
|
Term
receptors that are located in the lungs, liver, pancreas, and arteriolar smooth muscle ? |
|
Definition
|
|
Term
the stimulation of b2 receptors causes ? |
|
Definition
bronchodilation and vasodilation Pancreas = ↑ insulin secretion Liver = ↑ glycogenolysis |
|
|
Term
|
Definition
Blocks increase HR, contractility and renin Without blocking broncho and vasodilation of β2 receptors in lungs, glucose and arteriolar smooth muscle |
|
|
Term
Cardioselective beta blockers are preferred in ? |
|
Definition
asthma, COPD, DM and PVD
At higher doses cardioselectivity is less |
|
|
Term
examples of cardioselective beta blockers ? |
|
Definition
Acebutolol Atenolol Betaxolol Bisoprolol |
|
|
Term
examples of cardioselective beta blockers ? |
|
Definition
Celiprolol Esmolol Metoprolol Nebivolol |
|
|
Term
examples of non-selective beta blockers ? |
|
Definition
Carteolol Carvedilol Labetolol Nadolol |
|
|
Term
examples of non-selective beta blockers ? |
|
Definition
penbutol Pindolol Propranolol Sotalol Timolol |
|
|
Term
partial β-agonist activity |
|
Definition
Block effects of excessive sympathetic activity Moderately activate receptors when sympathetic tone low Therefore at rest, HR, CO and peripheral blood flow not reduced Ideally for borderline HF, sinus bradycardia aka: Intrinsic Sympathomimetic Activity (ISA) |
|
|
Term
examples of beta blockers with ISA ? |
|
Definition
Acebutolol Carteolol Celiprolol |
|
|
Term
examples of beta blockers with ISA ? |
|
Definition
Labetalol Penbutolol Pindolol |
|
|
Term
more lipophilic the more ? |
|
Definition
CNS penetration
Increase in side effects Depression Sedation |
|
|
Term
beta blockers and high lipid solubility ? |
|
Definition
Carvedilol Penbutolol Propranolol |
|
|
Term
beta blockers and moderate lipid solubility ? |
|
Definition
Labetolol Metoprolol Pindolol Timolol |
|
|
Term
beta blockers and low lipid solubility ? |
|
Definition
Acebutolol Atenolol Betaxolol Bisoprolol Carteolol Celiprolol Esmolol Nadolol Sotalol |
|
|
Term
labetolol and carvedilol are ? |
|
Definition
Non selective BB Alpha 1 blocker |
|
|
Term
nebivolol (bystlic) are ? |
|
Definition
Newest BB (approved 12/07) Cardioselective BB Nitric oxide mediated vasodilation |
|
|
Term
blocking b1 can make the heart have a ? |
|
Definition
negative chronotropic and inotropic effects |
|
|
Term
blocking b1 can make the kidney ? |
|
Definition
|
|
Term
|
Definition
Decrease in SA and AV node conduction |
|
|
Term
blocking b2 (non cardioselective BB) leads to ? |
|
Definition
increased airway constriction and bronchospasms
Use in caution w/ asthma or COPD Pts with COPD tolerate the drugs better Select cardioselective BB in these pts |
|
|
Term
Can increase or decrease glucose (B2) |
|
Definition
decrease insulin decrease glycogenolysis use with caution in diabetics |
|
|
Term
|
Definition
Chronic use can reduce HDL ISA BB’s have less altered lipid effects |
|
|
Term
|
Definition
propranolol, metoprolol, atenolol, nadolol, timolol, levobunolol, betaxolol, and esmolol |
|
|
Term
|
Definition
1st BB approved for clinical use Half life: 3.5-6hrs Selectivity: none Partial agonist activity: no Highly lipid soluble |
|
|
Term
|
Definition
Cardioselective Preferred in respiratory diseases and PVD |
|
|
Term
|
Definition
Longest durations of action Half life: 14-24 hrs |
|
|
Term
timolol, levobunolol, and betaxolol |
|
Definition
Non selective Excellent ocular hypotensive effects with opthalmic use Used in glaucoma |
|
|
Term
|
Definition
Ultra short acting Half life: 10 min Given as continuous IV infusion Selectivity: Beta 1 Useful in tx supraventricular arrhythmias |
|
|
Term
the use of BB can effectively treatment this disease ? |
|
Definition
hypertension
Proven to be effective & well tolerated Less effective in elderly & African-Americans |
|
|
Term
|
Definition
Ischemic Heart Disease Reduce frequency of anginal episodes & improve exercise tolerance Reduces oxygen demand Relative contraindications: bradycardia, hypotension, left ventricular failure, shock, heart block, active airway disease |
|
|
Term
|
Definition
Cardiac Arrhythmias
Effective in tx supraventricular & ventricular arrhythmias Slows ventricular response rates in AFib & AFlutter |
|
|
Term
|
Definition
Heart Failure
Can worsen acute CHF Chronic use can prolong life MOA uncertain
Proven efficacy metoprolol, bisoprolol or carvedilol |
|
|
Term
|
Definition
Chronic Glaucoma (open angle glaucoma)
Leading cause of Blindness As eyes age increase in IOP can occur by Over production of aqueous fluid and build up Drainage system clogging Increase in pressure causes damage to optic nerve and retina |
|
|
Term
|
Definition
Pressure is due to overproduction or blocked drainage of fluid despite open space between iris and cornea |
|
|
Term
|
Definition
Pressure is due to outflow of fluid being blocked due to structural abnormality |
|
|
Term
Narrow Angle or closed angle is usually ? |
|
Definition
acute & causes pain (unlike open) Usually treated urgently with surgery or drugs |
|
|
Term
Pre-op drugs limited to ? (narrow angle or closed angle) |
|
Definition
Cholinomimetics Acetazolamide Osmotic agents Onset of action of others too slow |
|
|
Term
5 General Drug Classes used for glaucoma ? |
|
Definition
Cholinomimetics α agonists BB Prostaglandin analogs Diuretics |
|
|
Term
|
Definition
Parasympathomimetic Directly stimulates cholinergic receptors Produces contraction of iris sphincter muscle pupillary constriction (miosis) constriction of the ciliary muscle resulting in increased accommodation reduction in intraocular pressure associated with an increase in the outflow and a decrease in the inflow of aqueous humor |
|
|
Term
examples of cholinomimetic drugs ? |
|
Definition
Pilocarpine Carbachol Physostigmine Echothiophate Demecarium |
|
|
Term
unselective alpha agonists ? |
|
Definition
Epinephrine and dipivefrin Mechanism: increase outflow |
|
|
Term
alpha 2 selective alpha agonists ? |
|
Definition
Apraclonidine and brimonidine Mechanism: decrease aqueous secretion |
|
|
Term
examples of beta blockers? |
|
Definition
Timolol, betaxolol, carteolol, levobunolol, metipranolol Mechanism: decrease aqueous secretion from the epithelium Timolol drops can be systemically absorbed Heart rate and airway effects Can interact with other oral drugs like verapamil |
|
|
Term
Carbonic anhydrase inhibitors (diurectics) |
|
Definition
Carbonic anhydrase enzyme is responsible for productions of forming hydrogen and bicarb ions from carbon dioxide and water Inhibiting this enzyme causes decrease HCO3- resulting in diuretic effect Also causes decrease aqueous secretion |
|
|
Term
examples of carbonic anhydrase inhibitors (diuretics) ? |
|
Definition
Dorzolamide, brinzolamide, acetazolamide, dichlorphenamide, methazolamide |
|
|
Term
|
Definition
Selective agonists for FP prostaglandin receptor Results in increase outflow of aqueous humor |
|
|
Term
examples of Prostaglandin F2α ? |
|
Definition
Latanoprost, bimatoprost, travoprost, unoprostone |
|
|
Term
|
Definition
Hyperthyroidism
Inhibition of thyroxine (T4) conversion to triiodothyronine (T3) Tx: thyroid storm w/ propranolol Controls supraventricular tachycardias that often precipitate heart failure |
|
|
Term
|
Definition
Neurologic Disease Migraines: propranolol reduces frequency & intensity “Stage fright”: propranolol Alcohol withdrawal in some pts |
|
|
Term
|
Definition
Esophageal varicies BB reduce portal vein pressure in cirrhosis pts Propranolol and nadolol can also prevent bleeding and decrease mortality |
|
|
Term
BB and Clinical Toxicology |
|
Definition
Rash, fever, sedation, sleep disturbances, depression More lipid soluble = more CNS side effects Nadolol and atenolol are most water soluble |
|
|
Term
BB and Clinical Toxicology |
|
Definition
Major Side Effects Worsening or respiratory diseases Life saving CVD benefits likely outweigh risk Worsening of PVD Worsening or heart failure Hypotension Bradycardia |
|
|
Term
BB and Clinical Toxicology |
|
Definition
Can produce a syndrome of sympathetic over activity agitation, headache, sweating, and nausea Can provoke rapid upswings in blood pressure |
|
|
Term
BB and Clinical Toxicology |
|
Definition
May mask symptoms of hypoglycemia in diabetics Except sweating Important counseling point |
|
|
Term
|
Definition
Performance anxiety Mitral valve prolapse Post-MI HTN Open angle glaucoma Cardiac dysrythmias Thyroid storm |
|
|
Term
|
Definition
Angina Migraine prophylaxis CHF Aggressive behavior Pheochromocytoma GI hemorrhage Essential tremors Drug overdose??? |
|
|
Term
Cocaine Overdose Management |
|
Definition
Avoid beta-blockers to treat HTN |
|
|
Term
|
Definition
Thoracolumbar “fight or flight” |
|
|
Term
|
Definition
Collection of neurons in the walls of the gastrointestinal system |
|
|
Term
|
Definition
“rest and digest” Craniosacral |
|
|
Term
Afferent (sensory) fibers |
|
Definition
Run from periphery to integrating centers Enteric plexus in gut |
|
|
Term
Cholinergic fibers release |
|
Definition
|
|
Term
Noradrenergic (adrenergic) fibers releases |
|
Definition
Norepinephrine (noradrenaline) |
|
|
Term
is an important vasodilator transmitter in renal blood vessels |
|
Definition
|
|
Term
cells that release Epi & NE? |
|
Definition
|
|
Term
Most autonomic nerves also releases ? |
|
Definition
|
|
Term
In most sympathetic postganglionic neurons, this is the primary transmitter ? |
|
Definition
|
|
Term
examples of transmitters ? |
|
Definition
ATP CGRP CCK Dopamine Enkephalin Galanin GABA GRP |
|
|
Term
examples of transmitters ? |
|
Definition
Neuropeptide Y Nitric oxide NE Serotonin (5-HT) Substance P Vasoactive intestinal peptide |
|
|
Term
cholinergic receptors are affected by ? |
|
Definition
|
|
Term
subtypes of cholinergic receptors are |
|
Definition
muscarinic receptors nicotinic receptors |
|
|
Term
CNS, sympathetic postganglionic neurons, some presynaptic sites |
|
Definition
|
|
Term
Myocardium, smooth muscle, some presynaptic sites, CNS |
|
Definition
|
|
Term
Exocrine glands, vessels (smooth muscle & endothelium), CNS neurons |
|
Definition
|
|
Term
CNS, possibly vagal nerve endings |
|
Definition
|
|
Term
Vascular endothelium, esp. cerebral vessels, CNS |
|
Definition
|
|
Term
cholinoceptors are from ? |
|
Definition
|
|
Term
Postganglionic neurons, some presynaptic cholinergic terminals |
|
Definition
|
|
Term
Skeletal muscle neuromuscular end plates |
|
Definition
|
|
Term
adrenergic receptors are affected by ? |
|
Definition
|
|
Term
examples of catecholamine are ? |
|
Definition
Norepinephrine (NE) Epinephrine (EPI) Dopamine (DA) |
|
|
Term
subtypes of adrenergic receptors are |
|
Definition
α-adrenoceptors β-adrenoceptors Dopaminergic |
|
|
Term
types of adrenoceptors are ? |
|
Definition
|
|
Term
Postsynaptic effector cells, esp. smooth muscle |
|
Definition
|
|
Term
Presynaptic adrenergic nerve terminals, platelets, lipocytes, smooth muscle |
|
Definition
|
|
Term
Post-synaptic effector cells, esp. heart, lipocytes, brain |
|
Definition
|
|
Term
Post-synaptic effector cells, esp. smooth muscle and cardiac muscle |
|
Definition
|
|
Term
Post-synaptic effector cells, esp. lipocytes and heart |
|
Definition
|
|
Term
autonomic receptors (dopamine receptors) |
|
Definition
|
|
Term
Brain, effector tissue, esp. smooth muscle of the renal vascular bed |
|
Definition
|
|
Term
Brain, effector tissues, esp. smooth muscle, presynaptic nerve terminals |
|
Definition
|
|
Term
|
Definition
|
|
Term
Brain, cardiovascular system |
|
Definition
|
|
Term
Iris radial muscle – alpha 1 (SA) |
|
Definition
|
|
Term
Ciliary muscle – beta – (SA) |
|
Definition
|
|
Term
Iris circular muscle – M3 – (PA) |
|
Definition
|
|
Term
Ciliary muscle – M3 - (PA) |
|
Definition
|
|
Term
SA node – Beta1/Beta2 – (SA) |
|
Definition
|
|
Term
Ectopic pacemakers – Beta1/Beta2 – (SA) |
|
Definition
|
|
Term
Contractility – Beta 1/Beta2 – (SA) |
|
Definition
|
|
Term
|
Definition
|
|
Term
Contractility – M2 – (PA) |
|
Definition
|
|
Term
Skin, splanchnic vessels – alpha (SA) |
|
Definition
|
|
Term
Skeletal muscle vessels – Beta2 – (SA) |
|
Definition
|
|
Term
Skeletal muscle vessels – alpha (SA) |
|
Definition
|
|
Term
Skeletal muscle vessels – M3 – (SA) |
|
Definition
|
|
Term
|
Definition
|
|
Term
Bronchiolar Smooth Muscle- Beta2 (SA) |
|
Definition
|
|
Term
Bronchiolar Smooth Muscle-M3- (PA) |
|
Definition
|
|
Term
Gastrointestinal Tract-Smooth muscle of wall – alpha 2/Beta 2 – (SA) |
|
Definition
|
|
Term
Gastrointestinal Tract- Smooth muscles of sphincters – alpha 1 – (SA) |
|
Definition
|
|
Term
Gastrointestinal Tract- Smooth muscle of wall – M3 – (SA) |
|
Definition
|
|
Term
Gastrointestinal Tract- Smooth muscles of sphincters – M3 – (SA) |
|
Definition
|
|
Term
Gastrointestinal Tract- Secretion – M3 – (SA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Bladder wall – Beta 2 – (SA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Sphincter – alpha 1 – (SA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Uterus, pregnant – Beta 2 (SA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Uterus, pregnant – alpha – (SA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Penis, seminal vesicle – alpha – (SA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Bladder wall – M3 – (PA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Sphincter – M3 – (PA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Uterus, pregnant – M3 (PA) |
|
Definition
|
|
Term
Genitourinary Smooth Muscle- Penis, seminal vesicle – M3- (PA) |
|
Definition
|
|
Term
Pilomotor smooth muscle – alpha -(SA) |
|
Definition
|
|
Term
Sweat glands – thermoregulatory – M (SA) |
|
Definition
|
|
Term
Sweat glands – apocrine (stress) – alpha (SA) |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
central integration occurs in ? |
|
Definition
Occurs in midbrain and medulla ANS fully integrated |
|
|
Term
Cooperative interactions in ANS Occur in ? |
|
Definition
brain stem, medulla, spinal cord Baroreceptor in glossopharyngeal nerve Sensory fibers in the urinary bladder wall |
|
|
Term
Example: slow infusion of NE |
|
Definition
Powerful vasoconstriction: ↑ peripheral vascular resistance → ↑ MAP |
|
|
Term
Example: slow infusion of NE (cardiac) |
|
Definition
Negative feedback baroreceptor responds to ↑ MAP |
|
|
Term
NET effect of ↑ peripheral vascular resistance, ↑ MAP, and a ? |
|
Definition
|
|
Term
autoreceptors respond to ? |
|
Definition
|
|
Term
autoreceptors modulate release of ? |
|
Definition
NT by the nerve Usually inhibitory |
|
|
Term
Heteroreceptors May be activated by ? |
|
Definition
NTs released by other nerve terminals that synapse with the nerve ending |
|
|
Term
example of heteroreceptor action |
|
Definition
Vagal fibers in myocardium synapse on sympathetic adrenergic nerve terminals and inhibit NE release. |
|
|
Term
Modulation by history of activity (postsynaptic regulation) |
|
Definition
Up-regulation or down-regulation of receptor |
|
|
Term
example of Modulation by history of activity (postsynaptic regulation) |
|
Definition
Denervation supersensitivity Reserpine |
|
|
Term
Potential Pharmacologic Targets |
|
Definition
Synthesis Storage Release Termination of action Function of receptor |
|
|
Term
Action potential propagation |
|
Definition
-Examples: local anesthetics, tetrodotoxin (toxin of puffer fish), saxitoxin (toxin of gonyaulax – red tide organism)
-Site: nerve axons
-Action: blocks sodium channel, blocks conduction |
|
|
Term
|
Definition
-Example: hemicholinium
-Site: membrane of cholinergic nerve terminals
-Action: blocks uptake of choline and slows synthesis |
|
|
Term
|
Definition
-Example: alpha-methyltyrosine (metyrosine)
-Site: cytoplasm of adrenergic nerve terminals and adrenal medulla
-Action: blocks synthesis |
|
|
Term
|
Definition
-Example: vesamicol
-Site: cholinergic terminal vesicles
-Action: prevents storage, depletes ACh |
|
|
Term
|
Definition
-Example: reserpine
-Site: adrenergic terminal vesicles
-Action: prevents storage, depletes NE and dopamine |
|
|
Term
|
Definition
-Example: NE, DA, ACh, angiotensin II, various prostaglandins
-Site: nerve terminal membrane receptor
-Action: modulates release |
|
|
Term
|
Definition
-Example: omega-conotoxin GVIA (toxin of marine snails)
-Site: nerve terminal calcium channel
-Action: reduces transmitter release |
|
|
Term
|
Definition
-Example: Botulinum toxin
-Site: cholinergic vesicles
-Action: prevents release |
|
|
Term
|
Definition
-Example: alpha latrotoxin (black widow spider venom)
-Site: cholinergic and adrenergic vesicles
-Action: causes explosive transmitter release |
|
|
Term
|
Definition
-Example: tyramine, amphetamine
-Site: adrenergic nerve terminals
-Action: promote transmitter release |
|
|
Term
Transmitter uptake after release |
|
Definition
-Example: cocaine, tricyclic antidepressants
-Site: adrenergic nerve terminals
-Action: inhibit uptake, increase transmitter effect on postsynaptic receptors |
|
|
Term
Receptor activation or blockade |
|
Definition
-Example: norepinephrine
-Site: receptors at adrenergic junctions
-Action: binds alpha receptors, causes contraction |
|
|
Term
Receptor activation or blockade |
|
Definition
-Example: phentolamine
-Site: receptors at adrenergic junctions
-Action: binds alpha receptors, prevents activation |
|
|
Term
Receptor activation or blockade |
|
Definition
-Example: isoproterenol
-Site: receptors at adrenergic junctions
-Action: binds beta receptors |
|
|
Term
Receptor activation or blockade |
|
Definition
-Example: propranolol
-Site: receptors at adrenergic junctions
-Action: binds beta receptors, prevents activation |
|
|
Term
Receptor activation or blockade |
|
Definition
-Example: nicotine
-Site: receptors at nicotinic cholinergic junctions (autonomic ganglion, neuromuscular end plates)
-Action: binds nicotinic receptors, opens ion channel in postsynaptic membrane |
|
|
Term
Receptor activation or blockade |
|
Definition
-Example: bethanechol
-Site: receptors, parasympathetic effector cells (smooth muscle, glands)
-Action: binds and activates muscarinic receptors |
|
|
Term
Receptor activation or blockade |
|
Definition
-Example: atropine
-Site: receptors, parasympathetic effector cells
-Action: binds muscarinic receptors, prevents activation |
|
|
Term
Enzymatic inactivation of transmitter |
|
Definition
-Example: neostigmine
-Site: cholinergic synapses (acetylcholinesterase)
-Action: inhibits enzyme which prolongs and intensifies transmitter action |
|
|
Term
Enzymatic inactivation of transmitter |
|
Definition
-Example: tranylcypromine
-Site: adrenergic nerve terminals (monoamine oxidase)
-Action: inhibits enzyme which increases stored transmitter pool |
|
|
Term
types of cholinomimetics drugs ? |
|
Definition
ACh agonists, achE inhibitors, muscarinic, and nicotinic |
|
|
Term
drugs that mimic ACH action? |
|
Definition
ach agonists and ACHE inhibitors |
|
|
Term
|
Definition
|
|
Term
tissues that are effected by muscarinic |
|
Definition
smooth muscle, heart, & exocrine glands |
|
|
Term
tissue that are effected by nicotinic |
|
Definition
Skeletal muscle & autonomic ganglia |
|
|
Term
muscarinic receptors (cholinoceptors) |
|
Definition
|
|
Term
nicotinic (cholinoceptors) |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
seven transmembrane segments, Gq/11 protein linked |
|
|
Term
M1 Postreceptor Mechanism: |
|
Definition
|
|
Term
|
Definition
heart, nerves, smooth muscle |
|
|
Term
M2 (cardiac M2) Structural features: |
|
Definition
seven transmembrane segments, Gi/0 protein linked |
|
|
Term
M2 (cardiac M2) Postreceptor Mechanism: |
|
Definition
inhibition of cAMP production, activation of K+ channels |
|
|
Term
|
Definition
|
|
Term
|
Definition
Glands, smooth muscle, endothelium |
|
|
Term
|
Definition
seven transmembrane segments, Gq/11 protein linked |
|
|
Term
M4 Postreceptor Mechanism: |
|
Definition
|
|
Term
|
Definition
Structural Features: seven transmembrane segments, Gi/0 protein linked |
|
|
Term
M4 Postreceptor Mechanism: |
|
Definition
inhibition of cAMP production |
|
|
Term
|
Definition
|
|
Term
|
Definition
seven transmembrane segments, Gq/11 protein linked |
|
|
Term
M5 Postreceptor Mechanism: |
|
Definition
|
|
Term
NM (muscle type, end plate receptor) Location: |
|
Definition
Skeletal muscle neuromuscular junction) |
|
|
Term
NM (muscle type, end plate receptor) Structural Features: |
|
Definition
|
|
Term
NM (muscle type, end plate receptor) Postreceptor Mechanism: |
|
Definition
Na+, K+ depolarizing ion channel |
|
|
Term
NN (neuronal type, ganglion receptor) Location: |
|
Definition
postganglionic cell body, dendrites |
|
|
Term
NN (neuronal type, ganglion receptor) Structural Features: |
|
Definition
|
|
Term
NN (neuronal type, ganglion receptor) Postreceptor Mechanism: |
|
Definition
Na+, K+ depolarizing ion channel |
|
|
Term
Direct acting cholinomimetic agents Bind M receptors and/or N receptors |
|
Definition
|
|
Term
|
Definition
“reversible” “irreversible” |
|
|
Term
are Poorly absorbed and distributed into CNS |
|
Definition
|
|
Term
Choline Ester Characteristics |
|
Definition
-Hydrophilic Poorly absorbed and distributed into CNS
-Hydrolyzed in GI tract -Differing susceptibility to hydrolysis ACh is rapidly hydrolyzed A large IV bolus lasts 5-20 seconds
-Methacholine → Carbachol, bethanechol |
|
|
Term
|
Definition
-Well absorbed from most sites of administration
-Nicotine can be absorbed through the skin
-Mainly excreted by the kidneys
-Acidifying the urine increases clearance |
|
|
Term
Direct agonist: action on Cholinoceptor |
|
Definition
muscarinic, and nicotinic |
|
|
Term
Muscarinic (ACh released from PNS) |
|
Definition
Directly alters effector organ function Binds muscarinic receptors on neurons which inhibits release of neurotransmitters |
|
|
Term
|
Definition
|
|
Term
Eye Receptor: muscarinic Sphincter muscle of iris |
|
Definition
|
|
Term
Eye Receptor: muscarinic Ciliary muscle |
|
Definition
contraction -accommodation |
|
|
Term
Cardiovascular Receptors: muscarinic SA Node |
|
Definition
|
|
Term
Cardiovascular Receptors: muscarinic atria |
|
Definition
Decrease in contractile strength & refractory period |
|
|
Term
Cardiovascular Receptors: muscarinic AV node |
|
Definition
Decrease in conduction velocity Increase in refractory period |
|
|
Term
Cardiovascular Receptors: muscarinic ventricles |
|
Definition
Small decrease in contractile strength |
|
|
Term
Cardiovascular Receptors: muscarinic net effect: |
|
Definition
reduction in peripheral vascular resistance and change in heart rate |
|
|
Term
Blood Vessels muscarinic Arteries |
|
Definition
Dilation (via EDRF) High dose direct effector response - constriction |
|
|
Term
Blood Vessels muscarinic veins |
|
Definition
Dilation (via EDRF) High dose direct effector response - constriction |
|
|
Term
Respiratory System (Lungs) Receptor: Muscarinic bronchial muscle |
|
Definition
constriction (bronchoconstriction) |
|
|
Term
Respiratory System (Lungs) Receptor: Muscarinic bronchial glands |
|
Definition
|
|
Term
Gastrointestinal Tract Receptor: muscarinic Motility |
|
Definition
|
|
Term
Gastrointestinal Tract Receptor: muscarinic sphincters |
|
Definition
|
|
Term
Gastrointestinal Tract Receptor: muscarinic secretion |
|
Definition
|
|
Term
Genitourinary tract (urinary bladder) Receptors: muscarinic Detrusor |
|
Definition
|
|
Term
Genitourinary tract (urinary bladder) Receptors: muscarinic trigone and sphincter |
|
Definition
|
|
Term
Secretory Glands Receptors: muscarinic Sweat |
|
Definition
|
|
Term
Secretory Glands Receptors: muscarinic salivary |
|
Definition
|
|
Term
Secretory Glands Receptors: muscarinic lacrimal |
|
Definition
|
|
Term
Secretory Glands Receptors: muscarinic nasopharyngeal |
|
Definition
|
|
Term
|
Definition
|
|
Term
brain is richer in what receptors? |
|
Definition
|
|
Term
spinal cord is richer in what receptors ? |
|
Definition
|
|
Term
nicotinic receptors in high levels causes ? |
|
Definition
tremor, emesis, and stimulation of the respiratory system |
|
|
Term
nicotinic receptors in higher levels causes ? |
|
Definition
convulsions which can lead to fatal coma |
|
|
Term
|
Definition
Nicotine has greater affinity for neuronal nicotinic receptors hypertension nausea vomiting diarrhea Voiding of urine |
|
|
Term
Neuromuscular junction Receptor: |
|
Definition
nicotinic on the neuromuscular end plate |
|
|
Term
nicotinic on the neuromuscular end plate result in ? |
|
Definition
immediate depolarization of the end-plates |
|
|
Term
|
Definition
ACHE
note:Butyrylcholinesterase – also inhibited |
|
|
Term
examples of cholinesterase inhibitors ? |
|
Definition
edrophonium carbamates neostigmine organophosphates echothiophate |
|
|
Term
types of direct-acting cholinomimetics ? |
|
Definition
MOA and cholinesterase inhibitors |
|
|
Term
|
Definition
-Relatively insoluble due to permanent charge
-Poor absorption from conjunctiva, skin, and lungs
-Larger oral doses required
-Negligible distribution to CNS
-Physostigmine is well absorbed though Duration determined by stability of inhibitor-enzyme complex |
|
|
Term
|
Definition
-Well absorbed from skin, lung, gut, and conjunctiva
-Effective insecticides but dangerous to humans
-Distributed to all parts of the body Exception is echothiophate
-CNS toxicity |
|
|
Term
(Alcohols) Edrophonium Uses for ? |
|
Definition
Myasthenia gravis Ileus
2-10 minutes |
|
|
Term
(Carbamates and related agents) Neostigmine Uses for ? |
|
Definition
Myasthenia gravis Ileus
1/2 hour to 2 hours |
|
|
Term
(Carbamates and related agents) pyridostigmine uses for ? |
|
Definition
myasthenia gravis
3 to 6 hours |
|
|
Term
(Carbamates and related agents) Physostigmine Uses for ? |
|
Definition
glaucoma
1/2 hour to 2 hours |
|
|
Term
(Carbamates and related agents) ambenonium uses for ? |
|
Definition
myasthenia gravis
4 to 8 hours |
|
|
Term
(Organophosphates) Echothiophate Uses for ? |
|
Definition
|
|
Term
(Organophosphates) malathion and parathion are ? |
|
Definition
Highly lipid soluble Thiophosphate prodrugs Insecticides |
|
|
Term
Indirect Pharmacodynamics- AGING! |
|
Definition
-Involves the breaking down of one oxygen-phosphorus bond of the inhibitor
-Further strengthens the phosphorus enzyme bond
-“Cholinesterase regenerators” can break the phosphorus enzyme bond if given before aging
-More difficult to break if aging has occurred |
|
|
Term
Indirect – Organ System Effects - most prominent effects are seen in ? |
|
Definition
CV system GI system Eye Skeletal muscle neuromuscular junction |
|
|
Term
CNS in Low concentrations (Indirect – Organ System Effects) |
|
Definition
diffuse activation on electroencephalogram and subjective alerting response |
|
|
Term
CNS in higher concentration (indirect-organ system effects) |
|
Definition
generalized convulsions that can lead to coma and respiratory arrest |
|
|
Term
EYE- sphincter muscle of iris (indirect organ system effect |
|
Definition
|
|
Term
EYE- ciliary muscle (indirect organ system effect |
|
Definition
contraction for near vision |
|
|
Term
RESPIRATORY- bronchial muscle (indirect organ system effect |
|
Definition
constriction (bronchoconstriction) |
|
|
Term
RESPIRATORY -bronchial glands (indirect organ system effect |
|
Definition
|
|
Term
Gastrointestinal tract -Motility (Indirect – Organ System Effect) |
|
Definition
|
|
Term
Gastrointestinal tract- sphincters (Indirect – Organ System Effects) |
|
Definition
|
|
Term
Gastrointestinal tract-secretion (Indirect – Organ System Effects) |
|
Definition
|
|
Term
Urinary Tract-Detrusor (Indirect – Organ System Effects) |
|
Definition
|
|
Term
Urinary Tract- trigone and sphincter (Indirect – Organ System Effects) |
|
Definition
|
|
Term
Cardiovascular System (Indirect – Organ System Effects) |
|
Definition
Increases activity in both sympathetic and parasympathetic ganglia
Fall in cardiac output due to bradycardia
Decrease in atrial contractility
Reduction in ventricular contractility |
|
|
Term
Vascular smooth muscle – minimal effect (Indirect – Organ System Effects) |
|
Definition
Vascular resistance may be increased |
|
|
Term
Neuromuscular junction- Low (therapeutic) concentrations (Indirect – Organ System Effects) |
|
Definition
Moderately prolong and intensify actions of ACh Increases strength of muscle contraction |
|
|
Term
Neuromuscular junction- Higher concentrations (Indirect – Organ System Effects) |
|
Definition
Accumulation of ACh Fibrillation of muscle fibers Fasciculations of entire motor unit |
|
|
Term
Eye diseases (Cholinomimetics – Clinical Use) |
|
Definition
Glaucoma Accommodative esotropia |
|
|
Term
GI/GU (Cholinomimetics – Clinical Use) |
|
Definition
Post operative atony, neurogenic bladder |
|
|
Term
Neuromuscular junction (Cholinomimetics – Clinical Use) |
|
Definition
|
|
Term
heart (Cholinomimetics – Clinical Use) |
|
Definition
certain atrial arrhythmias |
|
|
Term
Bethanechol- Cholinomimetics – Clinical Use for ? |
|
Definition
Post-op and Neurogenic Ileus and Urinary Retention |
|
|
Term
Carbachol- Cholinomimetics – Clinical Use for ? |
|
Definition
|
|
Term
Pilocarpine- Cholinomimetics – Clinical Use for ? |
|
Definition
Glaucoma, Sjogren’s Syndrome |
|
|
Term
Nicotine- Cholinomimetics – Clinical Use for ? |
|
Definition
|
|
Term
|
Definition
increased intraocular pressure |
|
|
Term
Muscarinic stimulants and AChE inhibitors reduces ? |
|
Definition
intraocular pressure
Contraction of ciliary body Facilitate outflow of aqueous humor Decrease rate of secretion of aqueous humor |
|
|
Term
Glaucoma Treatment (direct agonist) medications ? |
|
Definition
pilocarpine, methacholine, carbachol |
|
|
Term
Glaucoma Treatment (cholinesterase inhibitors) |
|
Definition
physostigmine, echothiophate |
|
|
Term
|
Definition
Topical Beta Blockers and Prostaglandin derivatives |
|
|
Term
Acute angle-closure glaucoma is a medical emergency and treated initially with ? |
|
Definition
direct muscarinic agonist and a cholinesterase inhibitor (pilocarpine plus physostigmine)
Once intraocular pressure is controlled and danger of vision loss is diminished – surgery (iridectomy) |
|
|
Term
Postoperative ileus w/o obstruction and Increase tone of LES (pts w/ reflux esophagitis/GERD/reflux) can be treated with ? |
|
Definition
Bethanechol 10-25 mg PO TID or QID Neostigmine 15 mg PO |
|
|
Term
Sjogren’s syndrome is treated with ? |
|
Definition
pilocarpine to increase salivary secretions |
|
|
Term
Urinary retention – postoperative or postpartum and Neurogenic bladder (secondary to spinal cord injury or disease) can be treated with ? |
|
Definition
Bethanechol 5mg subcutaneously, may be repeated in 30 min if necessary
Neostigmine 0.5 to 1 mg subcutaneously
Neostigmine 15 mg PO |
|
|
Term
Myasthenia gravis is disease ? |
|
Definition
affecting skeletal muscle neuromuscular junction (autoimmune process) |
|
|
Term
Neuromuscular Junction is ? |
|
Definition
Extremely sensitive to actions of drugs that interfere with neuromuscular junction – aminoglycoside antibiotics |
|
|
Term
are valuable in treating myasthenia gravis ? |
|
Definition
cholinesterase inhibitors |
|
|
Term
is used in diagnosing myasthenia gravis ? |
|
Definition
|
|
Term
long term treatment myasthenia gravis ? |
|
Definition
pyridostigmine with neostigmine or ambenonium as alternatives
Doses titrated based on changes in muscle strength
Require frequent dosing |
|
|
Term
treatment for Supraventricular tachyarrhythmias ? |
|
Definition
adenosine and calcium channel blockers
Edrophonium was once used |
|
|
Term
is amodest efficacy and significant hepatic toxicity in treatment of Alzheimer’s ? (CNS) |
|
Definition
|
|
Term
is a modest clinical benefit in treatment of Alzheimer’s ? (CNS) |
|
Definition
|
|
Term
is a direct acting nicotinic agonist used in smoking cessation ? (CNS) |
|
Definition
varenicline
Toxicity includes nausea, headache, and sleep disturbance |
|
|
Term
Direct acting Muscarinic (toxicity)- pilocarpine |
|
Definition
nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, and bronchial constriction |
|
|
Term
|
Definition
nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation and bronchial constriction
symptoms within 15-30 minutes of ingestion
Treatment: Atropine 1-2 mg parenterally |
|
|
Term
Direct acting Nicotinic (toxicity) |
|
Definition
Fatal dose of nicotine 40 mg or 1 drop of pure liquid (same amount of nicotine in 2 regular cigarettes)
CNS stimulation: convulsions, coma, respiratory arrest Skeletal muscle end plate depolarization leading to respiratory paralysis Hypertension and cardiac arrhythmias |
|
|
Term
Direct acting Nicotinic (toxicity) |
|
Definition
Acute toxicity treatment: directed towards symptoms
Muscarinic – atropine
Central stimulation – anticonvulsants (diazepam)
Neuromuscular – does not respond to drugs so mechanical respiration required
Nicotine is metabolized and excreted rapidly – pt may survive and recover completely if hypoxia and brain damage hasn’t occurred in the first 4 hrs |
|
|
Term
Cholinesterase Inhibitors (toxicity) |
|
Definition
Usually from pesticides in agriculture or home use
Signs of muscarinic excess: diarrhea, urination, miosis, bronchoconstriction, excitation (of skeletal muscle and CNS), lacrimation, and salivation and sweating → “DUMBELS” |
|
|
Term
treatment of cholinesterase inhibitors toxicity ? |
|
Definition
Maintenance of vital signs
Decontamination
Atropine parenterally as needed to control signs of muscarinic excess |
|
|
Term
examples of Direct acting Cholinomimetics ? |
|
Definition
ACh (Miochol-E) Bethanechol (Urecholine) Carbachol (Miostat) Cevimeline (Evoxac) Pilocarpine (Isopto Carpine) Varenicline (Chantix) |
|
|
Term
examples of Cholinesterase Inhibitors ? |
|
Definition
Ambenonium (Mytelase) Donepezil (Aricept) Echothiophate (Phospholine) Edrophonium (Tensilon) Galantamine (Reminyl) |
|
|
Term
|
Definition
Neostigmine (Prostigmin) Physostigmine Pyridostigmine (Mestinon, Regonol) Rivastigmine (Exelon) Tacrine (Cognex) |
|
|
Term
Cholinoceptor blocking agents block the effect of ? |
|
Definition
parasympathetic activation |
|
|
Term
examples of Antinicotinic drugs (Cholinoceptor blocking agents)? |
|
Definition
Ganglion Blockers Neuromuscular Blockers |
|
|
Term
example of Antimuscarinic (anticholinergic) / Cholinoceptor blocking agents |
|
Definition
atropine is the prototype |
|
|
Term
examples of Muscarinic antagonists (Antimuscarinic Agents) ? |
|
Definition
|
|
Term
|
Definition
Naturally occurring tertiary amine alkaloid esters Atropa belladonna and Datura stramonium
Absorbed well from the gut and conjunctival membrane |
|
|
Term
|
Definition
Hyoscyamus niger Absorbed across the skin |
|
|
Term
antimuscarinic agents -structure - tertiary amines ? |
|
Definition
Useful in eye and CNS conditions Similar structures Antihistamines, antipsychotics, antidepressants |
|
|
Term
antimuscarinic agents -structure - quaternary amines |
|
Definition
More peripheral effects Less CNS penetration |
|
|
Term
atropine (Pharmacokinetics) |
|
Definition
Distribution: CNS within 30 min to 1 hour Metabolism: plasma half life of 2 hours Excretion: 60% excreted unchanged Effects on the iris and ciliary muscle persist for more than 72 hours |
|
|
Term
|
Definition
Atropine causes reversible blockade Binds to muscarinic receptor and prevents release of IP3 and inhibits adenylyl cyclase Effect varies by tissue Tissues most affected: salivary, bronchial, and sweat glands |
|
|
Term
|
Definition
Highly selective for muscarinic receptors
Lower potency at nicotinic receptors
Does not distinguish between M1 - M3
Other antimuscarinics are moderately selective for one of the receptor subgroups |
|
|
Term
order of effects of increased dose of atropine |
|
Definition
Decreased salivary and bronchial secretions
Decreased sweating
Pupil dilation and tachycardia
Inhibition of voiding
Decreased GI motility
Decreased gastric secretions |
|
|
Term
CNS (atropine)- organ system effects |
|
Definition
Minimal stimulant effects
Longer lasting sedative effect on the brain
One of the 1st drugs used for tremor of Parkinson’s |
|
|
Term
CNS-scopolamine -organ system effects (atropine) |
|
Definition
Prevents motion sickness of vestibular disturbances
Drowsiness and amnesia
Toxic doses – excitement, agitation, hallucinations, and coma |
|
|
Term
Eye - Topical atropine -organ system effects (atropine) |
|
Definition
blocks activation in pupillary constrictor muscle
Leads to unopposed sympathetic dilator activity and mydriasis
Weakens contraction of the ciliary muscle (cycloplegia)
Loss of ability to focus for near vision
Reduces lacrimal secretion |
|
|
Term
Cardiovascular SA node (organ system effects) (atropine) |
|
Definition
very sensitive to blockade
Moderate to high doses of atropine cause tachycardia
Lower doses initially cause bradycardia |
|
|
Term
cardiovascular- AV node- organ system effects (atropine) |
|
Definition
blockade can reduce PR interval |
|
|
Term
cardiovascular- ventricles- organ system effects (atropine) |
|
Definition
intraventricular conduction block in toxic concentrations |
|
|
Term
cardiovascular- blood vessels- organ system effects (atropine) |
|
Definition
vasodilation can be blocked |
|
|
Term
Respiratory System- organ system effects (atropine) |
|
Definition
Atropine can cause some bronchodilation and reduce secretion
Limited effectiveness in treating chronic obstructive pulmonary disease (COPD)
May be valuable in some asthma patients
Often used before administration of inhalant anesthetics to reduce the accumulation of secretions and the possibility of laryngospasm |
|
|
Term
Gastrointestinal tract (organ system effects) (atropine) |
|
Definition
Blocks motility (from stomach to colon) and some secretory functions
Blocks parasympathetic vagal nerve input But GI function also controlled by local hormones and noncholinergic neurons
Blocks salivary gland leading to dry mouth
Reduction in gastric secretions
Little effect on pancreatic and intestinal secretions |
|
|
Term
Genitourinary tract (organ system effects) (atropine) |
|
Definition
Relaxes smooth muscle of ureters and bladder wall which slows voiding
Useful in treatment of spasm due to mild inflammation, surgery, and certain neurologic conditions
Urinary retention in males with prostatic hyperplasia
No significant effect on the uterus |
|
|
Term
Sweat Glands- organ system effects -atropine |
|
Definition
Atropine suppresses thermoregulatory sweating
Adults only affected when large doses used
Infants and children are more affected – “atropine fever” |
|
|
Term
CNS Disorders (Therapeutic Applications) Parkinson’s disease |
|
Definition
Adjunctive therapy in some patients |
|
|
Term
CNS Disorders-Therapeutic Applications-Motion sickness |
|
Definition
Vestibular disorders
Scopolamine for seasickness
Scopolamine patch can last 48-72 hrs but can cause sedation and dry mouth |
|
|
Term
Ophthalmologic Disorders- Therapeutic Applications- Antimuscarinics useful in eye examinations |
|
Definition
Help examine the retina Use shorter acting drugs in adults and older children Younger children may require atropine but the possibility of antimuscarinic poisoning is increased
Antimuscarinics should never be used for dilation unless cycloplegia or prolonged action is required
Prevent synechia formation in uveitis & iritis Longer lasting agents are useful |
|
|
Term
Ophthalmologic Disorders (atropine) |
|
Definition
Atropine effects last 7-10 days
Cyclopentolate effects last 1 day
Tropicamide effects last 6 hours |
|
|
Term
Atropine or scopolamine used preoperatively to decrease |
|
Definition
airway secretions and decrease laryngospasms |
|
|
Term
Scopolamine produced a postoperative ? |
|
Definition
amnesia of the events
However they increased urinary retention & intestinal hypomotility |
|
|
Term
is useful in asthma & COPD ? |
|
Definition
|
|
Term
is useful to reduced incidence of COPD exacerbations ? |
|
Definition
tiotropium
Longer bronchodilator action than ipratropium |
|
|
Term
Cardiovascular Disorders- info! |
|
Definition
Can overcome the depression of SA or AV node function that is due to reflex vagal discharge in an MI
Useful in blocking the parasympathetic actions in some people with idiopathic dilated cardiomyopathy Due to antibody formation |
|
|
Term
Gastrointestinal Disorders (Therapeutic Applications) |
|
Definition
Used to treat traveler’s diarrhea and other mild self limited hypermotility conditions Often combined with an opioid antidiarrheal drug The antimuscarinic drug is mainly present to discourage abuse of the opioid agent |
|
|
Term
Is Used to relieve bladder spasms after urologic surgery and Used to reduce involuntary voiding ? |
|
Definition
|
|
Term
Darifenacin & solifenacin |
|
Definition
Greater selectivity for M3 Once daily dosing Reduced incidence of xerostomia & constipation |
|
|
Term
Is Used in adults with urinary incontinence and Reduced incidence of dry mouth ? |
|
Definition
|
|
Term
IS Used to reduce urinary incontinence in institutionalized elderly patients and Causes significant CNS toxicity ? |
|
Definition
Imipramine
Tricyclic antidepressant with antimuscarinic actions |
|
|
Term
Cholinergic Poisoning (antimuscarinic therapy) |
|
Definition
Both nicotinic & muscarinic effects of cholinesterase inhibitors can be life threatening
To reverse muscarinic effects a tertiary amine must be used – atropine preferably
Use atropine for effects of organophosphate inhibitors, parathion, & chemical warfare nerve gas
Atropine sulfate 1-2 mg IV every 5-15 min until signs of reversal |
|
|
Term
Cholinergic Poisoning (Cholinesterase regenerator compound) |
|
Definition
Pralidoxime (PAM) & diacetylmonoxime (DAM) used for organophosphorus poisoning
Can hydrolyze the phosphorylated enzyme if the complex has not aged
Pralidoxime 1-2 g IV infusion over 15-30 min
Diacetylmonoxime crosses the BBB |
|
|
Term
Cholinergic Poisoning (Mushroom poisoning) |
|
Definition
Rapid onset within 15-30 min – nausea, vomiting, diarrhea, urinary urgency, vasodilation, reflex tachycardia (sometimes bradycardia), sweating, salivation, bronchoconstriction Parenteral Atropine 1-2 mg
Delayed onset within 6-12 hrs – nausea, vomiting, hepatic injury, renal injury
Atropine has no value |
|
|
Term
|
Definition
Directed at one organ almost always induces undesirable effects in other organs
Atropine poisoning – dry mouth, mydriasis, tachycardia, hot & flushed skin, agitation, & delirium
“Dry as a bone, blind as a bat, red as a beet, and mad as a hatter”
Children and infants are very sensitive to the hyperthermic effects of atropine – death in doses as low as 2 mg |
|
|
Term
Contraindications of Antimuscarinic drugs |
|
Definition
contraindicated in pts with glaucoma
Elderly male pts use caution & avoid if pt has prostatic hyperplasia
Slows gastric emptying – increase gastric ulcer symptoms |
|
|
Term
Ganglionic Blockade: Non-depolarizing |
|
Definition
Blockade can be overcome by increasing the concentration of an agonist |
|
|
Term
Ganglionic Blockade: depolarizing |
|
Definition
Can be produced by nicotine and even ACh |
|
|
Term
CNS Mecamylamine (Ganglion BlockingOrgan System Effect) |
|
Definition
crosses BBB
Can cause sedation, tremor, choreiform movements, mental aberrations |
|
|
Term
Eye Ciliary muscle (Ganglion BlockingOrgan System Effect) |
|
Definition
cycloplegia with the loss of accommodation |
|
|
Term
eye- pupil (Ganglion BlockingOrgan System Effect) |
|
Definition
hard to predict
Sympathetic innervation – pupillary dilation
Parasympathetic innervation – pupillary constriction
Ganglionic blockade often causes moderate dilation Ganglionic blockade often causes moderate dilation |
|
|
Term
CV Blood vessels (Ganglion BlockingOrgan System Effect) |
|
Definition
Decrease in arteriolar and venomotor tone leading to a fall in blood pressure
Hypotension in the upright position (orthostatic hypotension) |
|
|
Term
CV- cardiac (Ganglion BlockingOrgan System Effect) |
|
Definition
Diminished contractility
Moderate tachycardia |
|
|
Term
GI tract (Ganglion BlockingOrgan System Effect) |
|
Definition
Reduced secretions
Motility inhibited
Constipation |
|
|
Term
GU (Ganglion BlockingOrgan System Effect) |
|
Definition
Urinary hesitancy
Urinary retention
Impaired erection
Impaired ejaculation |
|
|
Term
Thermoregulatory sweating reduced (Ganglion BlockingOrgan System Effect) |
|
Definition
Hyperthermia usually not a concern due to cutaneous vasodilation |
|
|
Term
examples of Antimuscarinic Anticholinergic Drugs ? |
|
Definition
Atropine
Belladonna alkaloids
Dicyclomine (Bentyl) |
|
|
Term
examples of Antimuscarinic Anticholinergic Drugs ? |
|
Definition
Flavoxate (Urispas)
Glycopyrrolate (Robinul)
I-Hyoscyamine
Ipratropium (Atrovent) |
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Term
examples of Antimuscarinic Anticholinergic Drugs ? |
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Definition
Methscopolamine (Pamine)
Oxybutynin (Ditropan)
Scopolamine
Solifenacin (Vesicare) |
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Term
examples of Antimuscarinic Anticholinergic Drugs ? |
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Definition
Tiotropium (Spiriva)
Tolterodine (Detrol)
Trospium (Spasmex) |
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