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IC > 1.5, 1.6 Adrenergic Pharmacology > Flashcards

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
Q

potent nonselective beta receptor agonist –> positive chronotropic and inotropic actions –> increases cardiac output
-decreases both diastolic and mean arterial pressures

A

isoproterenol

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26
Q

activates D1 receptors in renal vasculature, increases renal blood flow

A

dopamine

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27
Q

relatively beta-1 selective synthetic catecholamine

-also activates alpha-1 receptors

A

dobutamine

28
Q
  • prototypic alpha-1 agonist
  • not inactivated by COMT –> longer duration of action than other catecholamines
  • mydriatic and decongestant, can raise BP
A

phenylephrine

29
Q

alpha 1 selective sympathomimetic

A

methoxamine

30
Q

first orally active sympathomimetic drug

A

ephedrine

31
Q

widely available OTC decongestant, indirect effects on releasing endogenous NE

A

pseudoephedrine

32
Q

direct alpha-1 agonist, used as topical decongestants

A

oxymetazoline, xylometazoline

33
Q
  • clonidine, methyldopa, guanfacine, guanabenz
  • antihypertensives
  • diminish SNS outflow
A

alpha-2 selective agonists

34
Q
  • dobutamine
  • prenalterol
  • increase CO with less reflex tachycardia, lack of beta-2 stimulated venous dilation
A

beta-1 selective agonists

35
Q
  • albuterol, salmeterol, terbutaline, ritodrine

- asthma, uterine relaxation in premature labor

A

beta-2 agonists

36
Q
  • indirect sympathomimetic
  • marked stimulant effects on mood and alertness
  • depressant effect on appetite
  • common drug of abuse
A

amphetamine

37
Q

-similar to amphetamine but has higher ratio of central to peripheral actions

A

methamphetamine

38
Q

amphetamine variant used in ADHD

A

methylphenidate

39
Q
  • local anesthetic

- sympathomimetic due to blockade of uptake 1

A

cocaine

40
Q
  • release stored catecholamines, found in high concetrations in fermented foods
  • MAO inhibitor potentiate effects
  • can produce hypertensive crisis
A

tyramine

41
Q
  • related to extension of pharmacologic effects in the CV and central nervous systems
  • hypertension, tachycardia, restlessness, tremor, insomnia, anxiety, paranoia
A

toxicity of sympathomimetic drugs

42
Q

_______ receptor antagonists lower peripheral vascular resistance and reduce blood pressure

A

alpha

43
Q
  • can reverse pressor effects of epinephrine

- may cause postural hypotension and reflex tachycardia

A

alpha receptor antagonists

44
Q
  • prototypic alpha antagonist
  • nonselective between alpha1 and alpha2
  • competitive blockade of receptors
  • reduces TPR, MAP
  • produces reflex tachycardia (SNS reflex)
  • tolazoline is similar
A

phentolamine

45
Q
  • irreversible - binds covalently to alpha receptors
  • somewhat selective for alpha1 receptors
  • treatment of pheochromocytoma (Adrenal tumor)
  • postural hypotension and tachycardia can limit use
A

phenoxybenzamine

46
Q
  • selective for alpha1 receptors

- 1,000 fold less potent at alpha2

A

prazosin, terazosin

47
Q
  • alpha1 antagonist with longer half life

- used in treatment of hypertension and BPH

A

doxazosin

48
Q
  • competitive alpha1 antagonists, structurally different

- BPH

A

tamsulosin, alfuzosin

49
Q

apha2 selective antagonist, no clinical role, has been used in ED

A

yohimbine

50
Q
  • irreversibly blocks VMAT, unprotected neurotransmitters are metabolized by MAO
  • effects long lasting, neurotransmitters never excite post synaptic cell
A

reserpine

51
Q
  • tumor of adrenal medullar - release mix of epi and norepi

- symptoms and signs of catecholamine excess - HTN, headaches, palpitations, sweating

A

pheochromocytoma

52
Q

rapid hydrolysis beta antagonist, half life of 10 minutes

A

esmolol

53
Q
  • lower BP in patients with HTN

- negative inotropic and chronotropic effects, slowed AV conduction, increased PR interval

A

beta blockers

54
Q

beta blocking agents _______ intraocular pressure in the eye, and decrease aqueous humor production

A

reduce

55
Q
  • partial agonist activity of beta blockers

- prevents precipitation of asthma, bradycardia, alteration of plasma lipid profile

A

intrinsic sympathomimetic activity

56
Q

prototypical beta blocking drug, nonselective

A

propanolol

57
Q

beta 1 selective drugs

A

metoprolol, atenolol

58
Q

very long duration of action beta blockers

A

nadolol and timolol

59
Q

significant intrinsic sympathomimetic effect

A

pindolol, acebutolol, carteolol

60
Q

reversible alpha1 antagonist, also nonselective beta adrenoceptor antagonist, hypotension with less tachycardia than alpha blockers

A

labetalol

61
Q

ultra short acting beta1 selective antagonist, structure contains an ester linkage

A

esmolol

62
Q
  • 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
A

beta blockers

63
Q
  • 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
A

beta blockers

64
Q
  • topical administration reduces intraocular pressure

- reduced production of aqueous humor by the ciliary epithelium

A

beta blocker treatment of glaucoma

65
Q
  • 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
A

toxicity of beta receptor antagonists

IC (29 decks)

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