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Pharmacology > Adrenergic Agonists and Antagonists > Flashcards

Adrenergic Agonists and Antagonists Flashcards

1
Q

Effects of stimulating Alpha 1 receptors?

A
  • vasoconstriction
  • increased peripheral resistance
  • increased BP
  • mydriasis (pupil dilation)
  • increased closure of bladder sphincter
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2
Q

Effects of stimulating Alpha 2 receptors?

A
  • inhibits NE release
  • inhibits ACh release
  • inhibits insulin release
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3
Q

Effects of stimulating beta 1 receptors?

A
  • tachycardia (increased HR)
  • increased lipolysis
  • increased heart contractility
  • increased release of renin
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4
Q

Effects of stimulating beta 2 receptors?

A
  • vasodilation
  • decreased peripheral resistance
  • bronchodilation
  • increased glycogenolysis
  • increased release of glucagon
  • uterine dilation
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5
Q

Selegiline?

A
  • MOA inhibitor

- prevents degradation of NE

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6
Q

Cocaine?

A
  • NET inhibitor

- prevents uptake of NE, prolongs stimulation

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7
Q

Tyramine and Amphetamine?

A
  • similar structure to NE
  • they are uptaken into presynaptic cell and deplete NE out of vesicle
  • increase NE stimulation
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8
Q

Entacapone?

A
  • COMT inhibitor

- prevents degradation of NE

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9
Q

Why do catecholamines have a short duration of action?

A
  • OH groups on C3 and C4 make them reactive and easily degraded by COMT and MOA
  • cannot be taken orally because MOA and COMT have a lot of enzymes in GI tract
  • more polar so cannot cross BBB
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10
Q

Mechanism of alpha 1 receptors?

A
  1. Gq protein coupled
  2. phospholipase C generates IP3 and DAG
  3. increases Calcium inside the cell
  4. smooth muscle contraction, vasoconstriction
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11
Q

Norepinephrine?

A
  • alpha agonist
  • stimulates all receptors, but mainly alpha 1 at low doses

Effects:

  • vasoconstriction
  • increases peripheral resistance
  • increases BP
  • reflex bradycardia due to high BP

Clinical use:

  • shock (IV slow drip)
  • rapid onset, short duration
  • monitor closely for high BP

ADR:

  • increased BP (hypertension)
  • reflex bradycardia
  • nasal dryness
  • blurred vision (pupils dilated)
  • tissue necrosis (IV infiltration, use alpha antagonist)
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12
Q

Phenylephrine?

A

-selective alpha 1 agonist

Effects:

  • increased BP
  • vasoconstriction

Clinical use:

  • nasal decongestant
  • drops for mydriasis (pupil dilation)
  • relieve redness for eyes

ADR:

  • increased BP, cardiac failure, arrhythmia
  • reflex bradycardia
  • infiltration necrosis
  • rebound nasal congestion (don’t use long term)
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13
Q

Naphazoline and Oxymetazoline?

A
  • non selective alpha agonist

- relief of redness of eyes from swimming, cold, or allergy

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14
Q

Clonidine?

A

-selective alpha 2 agonist

Effects:

  • stimulates alpha 2 in CNS to decreases sympathetic outflow to periphery
  • reduce NE
  • blood vessel dilation
  • reduced BP

Clinical use:

  • hypertension
  • withdrawal from opiates, tobacco, benzodiazepines

ADR:

  • lethargy, sedation
  • constipation
  • dry mouth
  • rebound hypertension, taper slowly
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15
Q

Mechanism of beta 1 receptor activation?

A
  1. Gq protein coupled
  2. adenylyl cyclase activated to increase cAMP
  3. increased calcium
  4. increases HR and contractility
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16
Q

Mechanism of beta 2 receptor activation?

A
  1. increase cAMP
  2. inactivate myosin LC kinase
  3. dissociation of actin and myosin
  4. smooth muscle relaxation
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17
Q

Isoproterenol?

A

-nonselective beta agonist

Effects:

  • stimulates heart
  • relaxes smooth muscle

Clinical use:

  • longer half life than Epi (metabolized by COMT, not MAO)
  • treat heart block, bradycardia, ventricular arrhythmia
  • do not use to treat asthma (stimulates heart as well as dilating blood vessels)

ADR:

  • tachycardia
  • headache
  • flushing
  • ischemia
  • arrhythmia in CHD patients
18
Q

Dobutamine?

A

-selective beta 1 agonist

Effects:
-increase HR and contractility of heart

Clinical use:
-parenterally for acute CHS as inotropic drug

ADR:

  • ventricular arrhythmia
  • tolerance after prolonged use
19
Q

Albuterol and Terbutaline?

A

-selective beta 2 agonist, use lower dose

Effects:

  • relaxes smooth muscle
  • bronchodilation
  • uterine dilation
  • vasodilation

Clinical use:

  • parenterally, short acting (3-6 hours)
  • relieve acute bronchospasm in asthma via inhaler
  • inhibits uterine contractions in premature labor (terbutaline)
  • Salmeterol and Formoterol are long acting, combined with steroid for asthma

ADR:

  • tremor
  • tachycardia
  • higher does cause beta 1 stimulation
20
Q

Epinephrine?

A

-stimulates all adrenergic receptors (higher affinity for beta 2 at lower dose)

Clinical use:

  • rapid onset and brief duration
  • asthma
  • anaphylaxis shock (epipen)
  • angioedema
  • cardiac arrest, bradycardia, heart block in ER

ADR:

  • ventricular arrhythmias
  • headache
  • restlessness
21
Q

Effect of NE on HR, BP, and peripheral resistance?

A
  • stimulates alpha 1, vasoconstriction
  • increases PR significantly
  • SBP and DBP increases, increasing MAP
  • MAP activates baroreceptors to reduce HR
22
Q

Effect of Epi on HR, BP, and peripheral resistance?

A
  • Epi stimulates all receptors
  • net effect of is blood vessel dilation
  • reduces PR slightly, due to vasoconstriction of alpha 1
  • DBP decreases
  • HR and contractility increases
  • CO and SBP increases
  • MAP has no change due to decreases in DBP and increases is SBP
23
Q

Effect of Isoproterenol on HR, BP, and peripheral resistance?

A
  • stimulates beta receptors nonselectively
  • blood vessel dilation
  • decreases PR significantly
  • DBP decreases significantly
  • SBP increases slightly
  • MAP decreases
  • less stimulation of baroreceptors
  • HR increases significantly
24
Q

Trimethaphan?

A
  • blocks autonomic ganglion
  • when given before phenylephrine, baroreceptor stimulation is not complete
  • phenylephrine will increase BP due to vasoconstriction
  • HR won’t change due to baroreflex block by trimethaphan
25
Q

Dopamine?

A

Effects:

  • low dose causes vasodilation in kidney and GI to generate more urine and maintain kidney function
  • medium dose- Beta 1 increased HR
  • high dose- alpha 1 vasoconstriction

Clinical use:

  • circulatory shock
  • acute heart failure
  • Epi and NE would vasoconstriction the kidneys, shutting them down

ADR:

  • tachycardia
  • angina pain
  • arrhythmias
  • headache
26
Q

Fenoldopam?

A
  • selective peripheral Dopamine 1 antagonist (D1)

- raid vasodilator for treating severe hypertension

27
Q

Ephedrine and Pseudoephedrine?

A
  • stimulates alpha and beta receptors in CNS
  • mixed acting

Clinical use:

  • use as nasal decongestant
  • increase BP
28
Q

Phentolamine?

A
  • reversible (competitive) nonselective alpha antagonist or blocker
  • short acting

Clinical use:

  • diagnose and treat pheochromocytoma (tumor in adrenal gland that increases BP)
  • used to treat hypertension

ADR:

  • reflex tachycardia
  • postural hypotension
  • sexual dysfunction
  • Epi reversal
29
Q

Phenoxybenzamine?

A
  • irreversible (noncompetitive) nonselective alpha blocker or antagonist
  • long acting

Clinical use:
-management of pheochromocytoma (adrenal tumor)

ADR:

  • reflex tachycardia
  • postural hypotension
  • sexual dysfunction
  • Epi reversal
30
Q

Prazosin?

A

-selective alpha 1 blocker

Effects:

  • blocks alpha 1 and prevents NE from stimulating vasoconstriction
  • blood vessel is more dilated

Clinical use:

  • treat benign prostate hyperplasia
  • reduces urinary hesitancy
  • allows relaxation and ease of passing urine

ADR:

  • postural hypotension (feel dizzy when stand up), give at bed time
  • head ache, dizziness, nasal congestion, blurred vision
  • reflex tachycardia
  • sexual dysfunction
  • Epi reversal- if alpha blocker is given before, Epi becomes a beta stimulator only, reduces PR and MAP
31
Q

Adverse effects of beta blockers?

A
  • Asthma and COPD
  • diabetic difficulties (hypoglycemia)
  • abrupt withdrawal due to receptor up regulation
32
Q

Propanolol?

A
  • nonselective beta blocker
  • membrane stabilizing ability
  • most lipid soluble beta blocker

Clinical use:

  • used to treat arrhythmia
  • do not give to patients with asthma or COPD
  • may influence diabetics insulin dose
33
Q

Timolol and Nadolol?

A
  • more potent nonselective beta blocker than propranolol
  • no membrane stabilizing ability

Clinical use:

  • Nadolol long duration of action, use for hypertension, angina, migraine
  • Timolol treats open angle glaucoma (topical), hypertension, migraine
34
Q

Pindolol?

A
  • non selective beta blocker
  • intrinsic sympathetic activity

Clinical use:
-use as antihypertensive in people with diminished cardiac reserve (beta 1 stimulation is low, need to stimulate heart to respond for more CO)

35
Q

Metoprolol and Atenolol?

A
  • selective beta 1 blockers
  • Metoprolol has membrane stabilizing effects

Clinical use:

  • hypertension
  • angina
  • acute MI
  • heart failure
  • tachycardia
36
Q

Esmolol?

A
  • selective beta 1 blocker
  • very short half life, given via IV

Clinical use:

  • hypertensive crisis
  • acute SVT
37
Q

Nebivolol?

A
  • selective beta 1 blocker
  • can stimulate NO release causing vasodilation

Clinical use:
-use for hypertension

38
Q

Acebutolol?

A
  • selective beta 1 blocker
  • half life is 3 hours
  • active metabolite is Diacetolol (half life 8-12 hours)
  • has membrane stabilizing effect
  • has intrinsic sympathetic effect

Clinical use:
-ventricular arrhythmias

39
Q

Labetalol and Carvedilol?

A

-alpha 1 and nonselective beta blockers

Effects:

  • decreases PR and CO
  • balanced approach to inhibiting sympathetic system

Clinical use:

  • Labetalol (IV) used for hypertension, hypertensive emergencies, and pheochromocytoma (blocks alpha 1 reducing CO)
  • Carvedilol is used for heart failure, it reduces lipid oxidation, reduces vascular wall thickening

ADR:

  • combo of alpha and beta blocks
  • hepatic injury
40
Q

Reserpine?

A
  • adrenergic neuronal blocker
  • depletes serotonin and dopamine in CNS
  • inhibits Dopamine from being transported into vesicles

Clinical use:

  • hypertension
  • outdated use for antipsychosis

ADR:

  • hypotension
  • reflex tachycardia
  • increased GI
  • CNS depression
41
Q

Guanethidine?

A
  • adrenergic neuronal blocker
  • reduces fusion of vesicle to nerve terminal, reduces NE release

Clinical use:
-hypertension

ADR:

  • hypotension
  • reflex tachycardia
  • increased GI
  • CNS depression

Pharmacology (9 decks)

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