1.5, 1.6 Adrenergic Pharmacology Flashcards

1
Q

SNS stimulation mediated by release of __________ which activates adrenoceptors

A

norepinephrine

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2
Q

sympathomimetic drugs mimic the actions of?

A

epinephrine or norepinephrine

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3
Q
  • promote release of endogenous catecholamines
  • displace stored catecholamines (amphetamine and tyramine)
  • inhibit reuptake of catecholamines (cocaine)
A

indirect acting agents

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4
Q
  • in peripheral vasculature: contract smooth muscle, increase blood pressure
  • PLC activation, IP3 - calcium mobilization, DAG -PKC activation
A

alpha 1 adrenoceptors

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5
Q

presynaptic autoregulation of neurotransmitter release, inhibit adenylyl cyclase activity
-decrease intracellular cAMP levels

A

alpha 2 adrenoceptors

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6
Q
  • approximately equal affinity for epi and NE
  • found in vasculature, lung, eye, and most other end organs
  • increase cAMP levels
A

beta 1 adrenoceptors

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7
Q
  • high affinity for epi than NE
  • found in vasculature, lung, eye, and most other end organs
  • increase cAMP levels
A

beta 2 adrenoceptors

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8
Q
  • important in the brain
  • found in splanchnic and renal vasculature
  • D1 stimulates, D2 inhibits adenylyl cyclase
A

dopamine receptors

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9
Q

-_______ may limit therapeutic response to sympathomimetics

A

desensitization

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10
Q

Sympathomimetic drugs: in blood vessels alpha receptors __________ arterial resistance, and beta2 receptors __________ vascular smooth muscle

A

increase

relax

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11
Q

skin and splanchnic vessels have primarily _____ receptors

A

alpha

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12
Q

skeletal muscle vessels have predominantly _______ receptors

A

beta 2

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13
Q

sympathomimetics:
- in the heart _______ receptor activity predominates
- activation results in increased calcium influx in cardiac cells, AV conduction velocity increased, refractory period decreased

A

beta-1

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14
Q

______ agonists in the eye contract the radial pupillary dilator muscle –> mydriasis (dilation), can slighlty increased drainage of aqueous humor

A

alpha

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15
Q

_______ agonists in the eye increase aqeuous humor secretion by the ciliary epithelium, antagonists are important in the treatment of glaucoma

A

beta agonists

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16
Q

in the respiratory tract, ________ relax bronchial smooth muscle

A

beta 2 receptors

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17
Q

in the respiratory tract, ______ receptors in blood vessels of upper respiratory mucosa produce decongestion upon contraction

A

alpha 1

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18
Q

in the GI tract, _______ receptors on smooth muscle cells mediate relaxation
-alpha 2 activation ________ PNS drive on enteric nervous system

A

beta

decreases

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19
Q

in the GI tract, alpha-1 receptors _______ the bladder base, promoting urinary retention

A

contract

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20
Q

in the GU tract, beta 2 receptors of bladder wall _____ smooth muscle, promoting urinary retention

A

relax

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21
Q

increase lipolysis
enhance glycogenolysis
increase glucose release
increase insulin secretion

A

beta receptor activation

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22
Q

______ receptor activation decreases insulin resistance

A

alpha-2

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23
Q
  • very potent vasoconstrictor (alpha-1) and cardiac stimulant (beta-1)
  • positive inotropic and chronotropic actions on heart (beta-1)
  • also activates beta-2 receptors
  • mixed effects on TPR, increases venous capacitance
A

epinephrine

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24
Q
  • effects similar to epi on alpha-2 receptors in the heart
  • similar potency at beta-1 receptors
  • relatively little effect on beta-2 receptors
  • increases peripheral resistance
  • increases both diastolic and systolic blood pressure
  • compensatory vagal reflexes overcome positive direct chronotropy, at high doses may directly increase HR
A

norepinephrine

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25
potent nonselective beta receptor agonist --> positive chronotropic and inotropic actions --> increases cardiac output -decreases both diastolic and mean arterial pressures
isoproterenol
26
activates D1 receptors in renal vasculature, increases renal blood flow
dopamine
27
relatively beta-1 selective synthetic catecholamine | -also activates alpha-1 receptors
dobutamine
28
- prototypic alpha-1 agonist - not inactivated by COMT --> longer duration of action than other catecholamines - mydriatic and decongestant, can raise BP
phenylephrine
29
alpha 1 selective sympathomimetic
methoxamine
30
first orally active sympathomimetic drug
ephedrine
31
widely available OTC decongestant, indirect effects on releasing endogenous NE
pseudoephedrine
32
direct alpha-1 agonist, used as topical decongestants
oxymetazoline, xylometazoline
33
- clonidine, methyldopa, guanfacine, guanabenz - antihypertensives - diminish SNS outflow
alpha-2 selective agonists
34
- dobutamine - prenalterol - increase CO with less reflex tachycardia, lack of beta-2 stimulated venous dilation
beta-1 selective agonists
35
- albuterol, salmeterol, terbutaline, ritodrine | - asthma, uterine relaxation in premature labor
beta-2 agonists
36
- indirect sympathomimetic - marked stimulant effects on mood and alertness - depressant effect on appetite - common drug of abuse
amphetamine
37
-similar to amphetamine but has higher ratio of central to peripheral actions
methamphetamine
38
amphetamine variant used in ADHD
methylphenidate
39
- local anesthetic | - sympathomimetic due to blockade of uptake 1
cocaine
40
- release stored catecholamines, found in high concetrations in fermented foods - MAO inhibitor potentiate effects - can produce hypertensive crisis
tyramine
41
- related to extension of pharmacologic effects in the CV and central nervous systems - hypertension, tachycardia, restlessness, tremor, insomnia, anxiety, paranoia
toxicity of sympathomimetic drugs
42
_______ receptor antagonists lower peripheral vascular resistance and reduce blood pressure
alpha
43
- can reverse pressor effects of epinephrine | - may cause postural hypotension and reflex tachycardia
alpha receptor antagonists
44
- prototypic alpha antagonist - nonselective between alpha1 and alpha2 - competitive blockade of receptors - reduces TPR, MAP - produces reflex tachycardia (SNS reflex) - tolazoline is similar
phentolamine
45
- irreversible - binds covalently to alpha receptors - somewhat selective for alpha1 receptors - treatment of pheochromocytoma (Adrenal tumor) - postural hypotension and tachycardia can limit use
phenoxybenzamine
46
- selective for alpha1 receptors | - 1,000 fold less potent at alpha2
prazosin, terazosin
47
- alpha1 antagonist with longer half life | - used in treatment of hypertension and BPH
doxazosin
48
- competitive alpha1 antagonists, structurally different | - BPH
tamsulosin, alfuzosin
49
apha2 selective antagonist, no clinical role, has been used in ED
yohimbine
50
- irreversibly blocks VMAT, unprotected neurotransmitters are metabolized by MAO - effects long lasting, neurotransmitters never excite post synaptic cell
reserpine
51
- tumor of adrenal medullar - release mix of epi and norepi | - symptoms and signs of catecholamine excess - HTN, headaches, palpitations, sweating
pheochromocytoma
52
rapid hydrolysis beta antagonist, half life of 10 minutes
esmolol
53
- lower BP in patients with HTN | - negative inotropic and chronotropic effects, slowed AV conduction, increased PR interval
beta blockers
54
beta blocking agents _______ intraocular pressure in the eye, and decrease aqueous humor production
reduce
55
- partial agonist activity of beta blockers | - prevents precipitation of asthma, bradycardia, alteration of plasma lipid profile
intrinsic sympathomimetic activity
56
prototypical beta blocking drug, nonselective
propanolol
57
beta 1 selective drugs
metoprolol, atenolol
58
very long duration of action beta blockers
nadolol and timolol
59
significant intrinsic sympathomimetic effect
pindolol, acebutolol, carteolol
60
reversible alpha1 antagonist, also nonselective beta adrenoceptor antagonist, hypotension with less tachycardia than alpha blockers
labetalol
61
ultra short acting beta1 selective antagonist, structure contains an ester linkage
esmolol
62
- used in ischemic heart disease - reduce frequency of anginal episodes - improve exercise tolerance, decrease cardiac work, reduce myocardial oxygen demand - long term use prolongs survival after MI
beta blockers
63
- effective in supraventricular and ventricular arrhythmias - post MI survival may be due to suppression of arrhythmias - increase AV node refractory period - slows ventricular response rate in a. fib
beta blockers
64
- topical administration reduces intraocular pressure | - reduced production of aqueous humor by the ciliary epithelium
beta blocker treatment of glaucoma
65
- worsening of preexisting asthma and other airway obstruction - depression of myocardial contractility and excitability - supersensitivity with abrupt discontinuation after chronic use, gradual tapering can prevent hypertensive crisis - can exacerabte hypoglycemic episodes in diabetics
toxicity of beta receptor antagonists