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ANS Adrenergic Flashcards

1
Q

acebutolol

A

Beta 1 selective receptor antagonists. Class II antiarrhythmic fast Na+ blocker.

TX. prohylaxis post-MI and supraventricular tachyarrhythmias. angina, HT,

less effect vasospasm, bronchospasm, uterus, metabolism.Safer in asthma, diabetes, peripheral vascular disease. ISA: intrinsic sympatomimetic activity as partial agonist with less bradycardia (-b1) and slight vaso/broncho dilation (-b2) and no change in lipids (-b2) adv. some sedation

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2
Q

Albuterol

A

Beta 2 agonist Tx asthma

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3
Q

Alpha 1 receptor activation effects

A

Gq (phospholipase C, Ip3, DAG, Ca+2) eye mydriasis: radial dilator contraction (no cycloplegia!) arterioles contraction veins contraction bladder trigone and sphincter contraction male sex organs vas deferens ejaculation liver glycogenolysis kidney DECREASED renin release

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3
Q

Alpha 1 effects on HR and BP

A

arterioles contraction veins contraction Increase TPR and BP potential bradycardia reflex CO may decrease, offset by increase venous return NO-change in pulse pressure (systolic-diastolic) *phenylephrine and methoxamine

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3
Q

Alpha 2 effects on HR and BP

A

prejunctional nerve terminals *DECREASE NE* platelets aggregation decreased CNS SANS prejunctional outflow used in mild to moderate HTN clonidine, methyldopa

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5
Q

Alpha 2 receptor activation effects

A

Gi (decrease adenylyl cyclase, cAMP) **prejunctional nerve terminals DECREASE NE release** platelets aggregation pancrease DECREASE insulin

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6
Q

amphetamines

A

indirect acting adrenergic receptor agonists releaser displace NE from mobile pool (neurojunction) psychostimulant do to central release of DA, NE, 5HT Tx. methyl phenidate in narcolepsy and ADHD

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6
Q

Alpha receptor antagonist

A

decrease TPR, mean BP potential reflex tachycardia, salt/water retention tx. HT, pheochromocytoma, BPH phentolamine, phenoxybenzamine prazosin, doxazosin, terazosin, tamsulosin yohimbine, mirtazapine

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7
Q

atenolol

A

Beta 1 selective receptor antagonists

TX. angina, HTN, post-MI

adv. Blood lipids increases LDL and TGs, sexual dysfunction, cardiovascular depression. Caution (but safer) in asthma, vasospastic disorders, diabetics (decreases insulin secretion), pregnancy

No sedation

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8
Q

Baroreceptor reflex

A

Increased BP elicits baroreceptor discharge to cardiovascular center. Nn blockers to block reflex at ganglionic synapse Nm2 block reflex bradycardia HR (vagal tone) B1 block reflex tachycardia HR, contractile force and vasoconstriction.

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9
Q

Beta agonist effects on HR and BP

A

beta 1: SA node positive chronotropy AV node positive dromotropy atrial/ventricular muscle positive inotropy His-purkinje positive dromotrophy beta 2: blood vessel vasodilate (non-innervated) beta 2 decrease BP (decrease TPR) beta 1 increase HR (increase SV, CO, pulse pressure= systolic-diastolic) isoproterenol, dobutamine salmeterol, albuterol, terbutaline, ritodrine

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10
Q

Beta receptor antagonists

A

Beta 1 blockade: decreased HR, SV, CO, renin, aqueous humour production beta 2 blockade: may precipitate bronchospasm, vasospasm block glycogenolysism gluconeogenesis increase LDL and TGs Chronic use leads to receptor upregulation; therefor important to taper use to avoid rebound of endogenous amines. acebutolol, atenolol, metoprolol, pindolol, propranolol, timolol labetalol, carvedilol, sotalol

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11
Q

Beta1 receptor activation effects

A

Gs (increase adenylyl cyclase, cAMP) SA node positive chronotropy AV node positive dromotropy atrial/ventricular muscle positive inotropy His-purkinje positive dromotrophy kidney increased renin

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12
Q

Beta2 receptor activation effects

A

Gs (increase adenylyl cyclase, cAMP) mostly non-innervated blood vessels vasodilate uterus relaxation brochioles dilation skeletal glycogenolysis (tremor) liver glycogenolysis pancrease increase insulin (metabolize fat and gluconeogenesis)

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13
Q

carvedilol

A

combined alpha 1 and beta blocker

tx. CHF

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14
Q

Catechol-O-methyltransferase (COMT)

A

degrades NE at synapse

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16
Q

Clonidine

A

alpha 2 agonists

  • decreases CNS SANS prejunctional outflow of NE
    • decrese TPR and HR

TX. mild to moderate HTN and opiate withdrawl

ADV. CNS depression, edema.

DI: TCAs decrease antiHTN effets

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17
Q

Cocaine

A

indirect acting adrenergic receptor agonists reuptake inhibitor NE (neurojunction)

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17
Q

Closed Angle Glaucoma

A

Acute or Chronic increased introccular pressure due to blockage of cannal of schlemm Tx. SURGERY. cholinomimetics, carbonic anhydrase inhibitors, mannitol. C/I alpha 1 agonist (myadriasis further closing the angle cannal)

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18
Q

dobutamine

A

B1>B2 agonist

TX. CHF

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19
Q

Dopamine

A

sympathomimetic. vasodilate renal, mesenteric, coronary vascular beds

Synthesized from Tyr hydroxylase metabolite: homovanillic acid

  • Dopamine will stimulate D1(Gs) at low dose,
  • beta 1 at medium dose alpha 1 at high dose

TX. CHF

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20
Q

doxazosin

A

Alpha 1 selective receptor antagonist

  • decrease arteriolar, venous, sphincter resistance

TX. HTN, BPH (decrease urinary frequency and nocturia) [good effect on lipid profil]

ADV reflex tachycardia, first dose effect, orthostatic hypotension, urinary incontenence.

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21
Q

Ephedrine

A

indirect acting adrenergic receptor agonists releaser displace NE from mobile pool (neurojunction) tx. cold medication

22
Q

Epinephrine

A

Synthesized from Tyr from Dopa/NE by adrenal medula. metabolite: vanillylmandelic acid (VMA) mixed acting agonist low dose beta > alpha effects: b1: increased HR, SV, CO, pulsepressure. b2: decreased TPR, BP medium dose opposing alpha 1 effect of increased TRP, BP high dose effect similar to NE alpha > beta with potential reflex bradycardia. *alpha1 blocker to reverse HT in OD to eliminate vasatone and unmask beta 2 effects* Tx. cardiac arrest, adjunct to local anesthetic, hypotension, anaphylaxis, asthma

23
Q

esmolol

A

Class II antiarrhythmic fast Na+ blocker.

IV.

TX. acute supraventricular tachyarrhythmias

24
Q

Fenoldopam

A

D1 agonist Tx severe hypertension at high dose D1, beta1, alpha1 agonist as dose increases

25
Q

Glucagon receptors of the heart

A

Gs coupled glucagon receptors positive inotropic and chronotropic effects on the heart *beta blockers in glucagon OD*

26
Q

Guanethidine

A

act directly on the granule of NE in perjunctional nerve, decreasing NE release

28
Q

isoproterenol

A

B1=B2 agonist

TX. bronchospasm, heart block, bradyarrythmias

Adv. flushing, angina, arrhythmias

28
Q

labetalol

A

combined alpha 1 and beta blocker tx. CHF

29
Q

methoxamine

A

alpha 1 agonist paroxysmal atrial tachycardia through vagal reflex

30
Q

methyldopa

A

alpha 2 agonists

  • decreases CNS SANS prejunctional outflow of NE
    • decrese TPR and HR

TX. mild to moderate HTN (safe in pregnancy)

ADV. CNS depression, edema, positive coombs test.

DI: TCAs decrease antiHTN effets

31
Q

metoprolol

A

Beta 1 selective receptor antagonists

TX. angina, HTN, post-MI

adv. some sedative and blood lipids increases LDL and TGs, sexual dysfunction, cardiovascular depression. Caution (but safer) in asthma, vasospastic disorders, diabetics (decreases insulin secretion)

33
Q

Monoamine Oxidase (MAO)

A

inactivates NE in the prejunctional nerve terminal MAO-a: liver and anywhere metabolizes NE, 5HT, tyramine MAO-b: brain metabolizes DA

33
Q

mirtazapine

A

Alpha 2 selective receptor antagonist tx. antidepressant

35
Q

non-selective Adrenergic effects on receptors at varying doses

A

non selective adrenergics responses at low dose beta > alpha at high dose alpha > beta Dopamine will stimulate D1 at low dose, beta 1 at medium dose alpha 1 at high dose

36
Q

Norepinephrine

A

Synthesized from Tyr from Dopa within nerve ending vessicles. stored as granules metabolite: vanillylmandelic acid (VMA)

mixed acting agonist (alpha 1/2, beta1)

increase TRP, BP, HR, SV, CO, increase pulse pressure=systolic-diastolic

potential reflex bradycardia no effect Beta2

Tx. cardiac arrest, adjunct to local anesthetic, hypotension

37
Q

Open angle glaucoma

A

chronic painless increased intraocular pressure due to decreased reabsorption of aqueous humour tx. beta blocker - timolol (decrease NE at ciliary epithelial tereby decreasing fluid formation) M3 agonist -pilocarpine (contract ciliary muscle to increase drainage) AchE Inhibitor - echothiophate

38
Q

phenoxybenzamine

A

Alpha receptor noncompetitive antagonist (Vmax decreased, Km unchanged)

39
Q

phentolamine

A

Alpha receptor competitive antagonist (Vmax same, Km increased)

40
Q

phenylephrine

A

alpha 1 agonist nasal decongestant and opthalmic myadriasis (without cycloplegia)

41
Q

pindolol

A

non selective beta receptor antagonists

ISA: intrinsic sympatomimetic activity as partial agonist with less bradycardia (-b1) and slight vaso/broncho dilation (-b2) and no change in lipids (-b2)

tx. angina, HTN, post-MI
adv. some sedation

43
Q

Prazosin

A

Alpha 1 selective receptor antagonist

  • decrease arteriolar, venous, sphincter resistance

TX. HTN, BPH (decrease urinary frequency and nocturia) [good effect on lipid profil]

ADV reflex tachycardia, first dose effect, orthostatic hypotension, urinary incontenence.

43
Q

propranolol

A

non selective beta receptor antagonists. and Class II antiarrhythmic fast Na+ blocker.

TX. prohylaxis post-MI, supraventricular tachyarrhythmias, HTN

tx. angina, HT, post-MI, class II antiarrhythmic, migraine, thyrotoxicosis, performance anxiety, essential tremor
adv. ++sedative and blood lipids (-b2), increases LDL and TGs, sexual dysfunction, cardiovascular depression. Caution in asthma, vasospastic disorders, diabetics (decreases insulin secretion)

45
Q

Reserpine

A

reduce NE levels in the prejunctional terminal by inhibiting granule reuptake

46
Q

Ritodrine

A

Beta 2 agonist Tx premature labour (relax uterus)

47
Q

Salmeterol

A

Beta 2 agonist Tx asthma

48
Q

sotalol

A

combined K+ channel and beta blocker

49
Q

Sympathetic autonomic Muscarinic Ach

A

Sweat glands, piloerector muscles

50
Q

tamsulosin

A

Alpha 1 selective receptor antagonist

51
Q

terazosin

A

Alpha 1 selective receptor antagonist

  • decrease arteriolar, venous, sphincter resistance

TX. HTN, BPH (decrease urinary frequency and nocturia) [good effect on lipid profil]

ADV reflex tachycardia, first dose effect, orthostatic hypotension, urinary incontenence.

52
Q

Terbutaline

A

Beta 2 agonist Tx asthma

53
Q

timolol

A

non selective beta receptor antagonists adv. +sedative and blood lipids (-b2) tx. angina, HT, post-MI, open angle glaucoma

54
Q

Tricyclic antidepressants

A

indirect acting adrenergic receptor agonists reuptake inhibitor NE (in part) (neurojunction)

55
Q

Tyramine

A

indirect acting adrenergic receptor agonists (red wine, cheese) releaser displace NE from mobile pool (neurojunction) oral bioavail limited by MAO in GI (MAO inhibitors can lead to hypertensive crisis)

56
Q

yohimbine

A

Alpha 2 selective receptor antagonist tx. postural hypotension and impotence

Pharmacology (18 decks)

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