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IC > Adrenergic Pharmacology II > Flashcards

Adrenergic Pharmacology II Flashcards

1
Q

Adrenoreceptor Antagonist Drugs

A

Effects vary according to drug’s receptor selectivity

Block either alpha or beta receptors

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2
Q

Phentolamine

A

Reversible alpha receptor antagonist

Competitive antagonist
Nonselective between alpha 1 and 2
Reduces TPR, MAP
Produces reflex tachy (SNS reflex)

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3
Q

Phenoxybenzamine

A

Irreversible alpha receptor antagonist
Longer duration of action than phentolamine because irreversible
Tx for pheochromocytoma
Predictable side effects of postural hypotension, reflex tachycardia
Somewhat selective for alpha1 receptors but less so than prazosin

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4
Q

Alpha receptor antagonist pharmacologic effects

A

Alpha1- peripheral vasculature

  • Reduce peripheral resistance, and reduce MAP because largely determined by alpha actions of SNS tone
  • Reduce blood pressure
  • Alpha antagonist can reverse pressor effects (epinephrine)
  • May cause postural hypotension and reflex tachycardia
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5
Q

Prazosin and terazosin

A

Alpha receptor antagonist

Selective alpha1 receptors

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6
Q

-Zosin

A

all alpha1 selective antagonist

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7
Q

Doxazosin

A

Alpha 1 antagonist with longer 1/2 life

Htn and bph tx

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8
Q

Tamsulosin, Alfuzosin

A

Competitive alpha1 ant

Good efficacy in BPH and helps with urinary retention

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9
Q

Yohimbine

A

Alpha2 selective antagonist
Alpha2 receptors are inhibitor, autoregulatory, and inhibit norepinephrine release
-Can get runaway catecholamine effects
-Can produce htn with this

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10
Q

Reserpine

A

Indirect sympatholytic agent

  • Inhibits VMAT (vesicular monoamine transporter) so that catecholamines are not stored in vesicles, and are sensitive to metabolism by MAO or COMT by adjacent cell
  • Overtime catecholamines will be depleted, so even if system is activated, no chemical will be released
  • Not therapeutically useful, just experimental to remove SNS
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11
Q

Alpha receptor antagonist- clinical use

A

Pheochromocytoma, htn emergencies (vasodilators preffered, nitrates), chronic htn (effective, but lots of side effects and heart failure) , urinary obstruction in BPH

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12
Q

Pheochromocytoma

A
  • tumor of adrenal medulla which releases mix of epinephrine and norepinphrine
  • symptoms and signs of catecholamine excess (htn, headaches, palpitations, sweating)
  • rarely tx with metyrosine but mostly use alpha antagonists to block activation of peripheral receptors
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13
Q

Beta receptor antagonist

A
  • Blocks effects of catecholamines at beta receptors
  • Selectivity for beta1 or beta2 have imp clinical implications
  • But there is some crossover even with beta1 specific drugs
  • Good oral bioavailability, peak effect within 1-3 hrs (major exception is esmolol)
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14
Q

Esmolol

A

is a beta antagonist
Unlike others, because it has an ester has a half life of 10 minutes because of rapid hydrolysis
Constant infusion in inpatient setting

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15
Q

Propanolol

A

Nonselective
Extensive first pass (hepatic) metabolism
-Accommodate for in parenteral vs oral
-Individual differences in metabolism

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16
Q

Beta blocker effects on CV

A
  • Lower Bp in pts with htn
  • Produce effects on heart, vasc, renin-angio system
  • Conventional doses usually doesn’t cause hypotension in normal subjects
  • Cardiac- neg inotropic and chronotropic effects
  • Slowed atroventricular conduction, increased PR interval
17
Q

Beta blocker effects on Resp tract

A

Bronchial smooth muscle- beta2 blockade increases airway resistance (adverse)

  • beta1 antagonists can also increase airway resistance in asthmatics
  • Nonselective beta blockers should be avoided in pts who are asthmatic
18
Q

Beta blocker effects on eye

A
  • Secretion of aqueous humor is controlled by beta receptors at ciliary epithelium
  • Block beta receptors- reduce secretion of aqueous humor (open angle glaucoma)
  • Topical eye drops
19
Q

Beta blocker effects on metabolism and endocrine

A
  • beta3 mediated effects on liver and adipose tissue- energy usage in fight or flight situation
  • move towards energy storage with meds
  • Symptoms- plasma VLDL, dec HDL, shifts in blood-glucose regulation
  • Should be used with caution in insulin-dep diabetics
20
Q

Intrinsic sympathomimetic activity

A

In some beta blocking drugs- partial agonist activity

  • By limiting extent of antagonism, can avoid AE: precipitation of asthma, bradycardia, alteration of plasma lipid prolife
  • Pindolol
21
Q

Propranolol

A

prototypical beta-blocking drug (nonselective)

22
Q

Beta1 selective drugs

A

Metoprolol, atenolol- more cardioselective, less effects on lung and liver

23
Q

Nadolol and timolol

A

beta blockers with long DOA

timolol used as eye drops in open angle glaucoma

24
Q

Pindolol, acebutolol, carteolol

A

partial agonists

Intrinsic sympathomimetic effects

25
Q

Labetalol

A
  • beta blocker AND alpha1 antagonist
  • nonselective beta blocker
  • Anti htnsive drug, but less compensatory tachycardia because of beta blocking ability
26
Q

Butoxamine

A
  • Beta2 antagonist
  • Bronchoconstriction, precipitate asthma
  • Tox= toxin, no clinical application
27
Q

Beta blockers, clinical uses

A

Htn (in combo with diuretics, vasodilators), ischemic herat disease (reduce anginal episodes, improve exercise tolerance, dec cardiac work, reduce myocardial oxygen demand, good evidence that long term use prolongs survival after MI), cardiac arrythmias (slow propogation of electrical signals through electrical pathways within myocardium, increase refractory period at AV node, reduce ventricular ectopic beats), glaucoma (open angle- topical drops to inh sec of aqueous humor), hyperthyroidism (limiting excessive catecholamine activity)

28
Q

Toxicity of beta receptor antagonist

A
  • well tolerated
  • minor: rash, fever, sedation, depression with chronic use
  • major: exacerbation of asthma, shifts in metabolic profile
29
Q

Nonselective alpha antagonist list

A

phentolamine, phenoxybenzamine, tolazoline

30
Q

alpha1 selective antagonist list

A

prazosin, terzosin, doxazosin, tamsulosin, alfuzosin, silodosin, labetalol

31
Q

alpha2 selective antagonist list

A

yohimbine

32
Q

adrenergic neuron blocking drugs list

A

reserpine, guanadrel

33
Q

nonselective beta antagonist list

A

propranolol, nadolol, timolol, [pindolol, cartelolol, penbutolol,-partial agonists], levopunalol, metipranolol, labetalol

34
Q

beta1 selective antagonist list

A

metoprolol, esmolol, atenolol, acebutolol, betaxolol, bisoprolol, nebivolol

35
Q

beta2 selective antagonist list

A

butoxamine

IC (31 decks)

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