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NRS 270: Pharmacology > Adrenergic Pharmacology > Flashcards

Adrenergic Pharmacology Flashcards

1
Q

Alpha 1 receptors: general

A

mostly smooth muscle of the vasculature, bladder base, urethral sphincter and prostate

activation: leads to arterial and venous vasoconstriction → increased BP

in normal pts if BP is increased baroreflex will kick in and counteract ⇒ need to be careful with pts with impaired autonomic functions as giving an alpha 1 agonist will lead to uncompensated vasoconstriction = HIGH BP

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2
Q

Alpha 2 Receptors: general

A
  1. Peripheral vasculature: when activated → vasoconstriction (similar effeccts as alpha 1)
  2. CNS (on presynaptic neurons): pure central alpha 2 agonist introduced → sympatholytic response (less sympathetic neurotransmitters) and inhibition of sympathetic tone which lowers BP i.e. clonidine
    a. pts with autonomic failure that are given a central alpha 2 agonist can cause increase BP
    * decrease secretion from beta islet cells of pancreas
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3
Q

Chronotropy

A

heart rate

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4
Q

inotropy

A

contractility

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5
Q

dromotropy

A

conduction between AV node

positive dromotropy = increased cardiac output

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6
Q

Beta receptor: general

A
  • Beta-1 in heart:
    • ​activation = increased HR, contractility, conductivity
  • beta -2: bronchioles and peripheral vasculature
    • activation = bronchodilation
  • Beta-3: bladder and adipose tissue, urethral smooth muscle (sphincter)
    • activation =relaxation of sphincter
      • allows bladder to fully empty
      • used for overactive bladder
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7
Q

Epinephrine

A
  • agonist at both alpha and beta receptors
  • very potent vasoconstrictor and cardiac stimulant
    • positive inotropy (contractility) and chronotropy (HR)
    • vascular bed vasoconstriction = increased BP
  • Toxicities:
    • STROKE
    • restlessness
    • throbbing HA
    • tremor
    • palpitations
    • cardiac arrhythmias
    • cerebral hemorrhage
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8
Q

Norepinephrine

A
  • acts most on Alpha 1, 2, and 1; less on beta 2
  • increases peripheral resistance and BP (both diastolic and systolic)
  • Contraindications:
    • severe volume depletion
    • vascular thrombosis
    • use of MAO inhibitor
    • extravasation → necrosis
  • SE:
    • HA, anxiety
    • tachycardia
    • severe HTN →stroke
    • asthma exacerbation
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9
Q

Differences in effects of Epi and Norepi

A
  • Cardiac: Epi >NE
    • HR: Epi>NE
    • Cardiac Output: Epi >>> NE
  • Peripheral Circulation:
    • Total peripheral resistance NE>Epi
    • Cerebral blood flow and muscle blood flow Epi >>> NE
    • Splanchnic blood flow Epi >>> NE
  • Metabolic effects: Epi > NE
    • oxygen consumption
    • blood glucose
    • blood lactic acid
    • eosinpenic response
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10
Q

Dopamine: general

A
  • Functions: precursor of norepi and epi
    • CNS -reward system ⇒addiction
    • regulating Na excretion and renal function
    • regulation of movements
      • deficiency in basal ganglia in Parkinson’s disease
  • When stimulating the peripheral dopamine receptors = vasodilation
  • Contraindications:
    • pheochromocytoma: tumor in adreal glands and associated with high BP
    • tachyarrhythmias
    • occlusive vascular disease
  • SE:
    • tachycardia/angina/HTN
    • HA/N/V/anxiety
    • Extravasation →tissue necrosis
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11
Q

Dopamine effects at low, intermediate, and high dose

A
  • 0.5-2 mcg/kg/min = only dopaminergic response
  • 2-10mcg/kg/min = both dopaminergic and beta 1 response
    • increase HR, increase contractility, increase urine output
  • >10mcg/kg/min = mostly affect alpha 1 as well as Beta 1 and dopaminergic
    • increased BP
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12
Q

Phenylephrine

A
  • selective alpha 1 agonist
  • can increase BP affecting HR
  • less side effects on the heart as it avoids beta 1 stimulation
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13
Q

Midodrine

A
  • selective alpha 1 agonist
  • prodrug
  • indication: orthostatic hypotension
  • Blackbox warning: may induce supine BP elevation
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14
Q

clonidine

A
  • central acting alpha 2 agonist
  • suppressses outflow of sympathetic activity → lowers BP
  • well PO absorption (~100% bioavailability)
  • Indications:
    • HTN
    • relieve withdrawal (w/d) sxs of narcotics, alcohol, and tobacco addiction →decreases cravings
  • SE: dry mouth
    • sedation
    • sexual dysfunction
  • Caution:
    • w/d rxn following abrupt d/c of long-term therapy
      • need to taper off drug
      • can use phentolamine for this w/d
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15
Q

Non-selective Alpha receptor antagonists

A

phenoxybenzamine

phentoalmine

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16
Q

Alpha 1 selective blockers

A
  • “osin”
  • prazosin
  • terazosin
  • doxazosin
  • alufzosin
  • tamsulosin
  • indoramin
  • urapidil
  • bunazosin
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17
Q

alpha 2 selective blocker

A

yohimbine

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18
Q

non-selective (first generation) beta blocker

A
  • nadolol
  • penbutolol
  • pindolol
  • propranolol
  • timolol
  • sotalol
  • levobunolol
  • metipranolol
19
Q

Beta 1 selective blockers (second generation)

A
    • acebutolol
  • atenolol
  • bisporolol-long half life
  • esmolol-shortest half life
  • metoprolol– lipid solublility is moderate
20
Q

non-selective beta blockers (third generation)

A
  • carteolol
  • carvedilol
  • bucindolol
  • labetalol
  • alpha 1 and beta 1 selective:
    • carvedilol and labetalol
    • carvedilol = ca2+ ebntry blockage and antioxidant activity
    • also have systemic effects → peripheral vasodilation
21
Q

Beta 1 selective blockers(3rd generation)

A
  • betaxolol
  • celiprolol
  • nebivolol
22
Q

highly lipid soluble beta blockers

A
  • Non-selective:
    • penbutolol
    • pindolol
  • beta 1-selective:
    • metoprolol
23
Q

Sympathetic postanglionic nerves that use acetycholine or dopamine instead of adrenergic neurotransmitters

A

sweat glands: acetycholine

renal vascular smooth muscle: dopamine

24
Q

pheochromocytoma

A
  • rare, benign tumor on the adrenal gland that increases the release of Epi and NE
  • can be treated with alpha 1 antagonists →phenoxybenzamene and phentolamine
25
Q

tocolytic

A
  • suppress premature labor
  • beta 2 sympathomimetics are tocolytics
    *
26
Q

isoproterenol

A
  • beta 1 and beta 2 non selective agonist
  • relaxaes almost all smooth muscles especially bronchial and GI
27
Q

oxymetazoline

A
  • alpha 1 and alpha 2 nonselective agonist
  • peripheral acting
  • topical nasal spray decongestant
28
Q

long acting beta 2 agonists

A
  • formoterol
    • long duration → bronchial dilation may persist for 12 hours
    • tx: asthma and COPD
  • Arformoterol:
    • twice as potent as formoterol
29
Q

Reserpine

A
  • indications: HTN and psychosis
  • blocks the action of VMAT (vesicular monoamine transporter)
  • prevents dopamine from entering the vesicles
  • depletes the storage of NE which leads to lowered blood pressure
30
Q

Tyramine, amphetamines and ephedrine

A
  • high affinity for NET (NE transporter: which brings NE back into the cell)
  • NE gets displaced and remains in the synaptic cleft for action
    • higher sympathetic tone = increase HR, BP, bronchodilation
31
Q

Dopamine Receptors

A

mostly in brain and the smooth muscle of the renal vascular bed

32
Q

MAO and COMT

A

enzymes that break down the catecholamines (epi, norepi, and dopamine)

33
Q

Stimulation of beta receptors and effects on NE

A
  • increased release of norepi
34
Q

stimulation of alpha 2 receptors and effect on NE

A

slows down the release of NE

35
Q

mydriasis

A
  • eye dilation due to contraction of radial muscle of iris
  • sympathetic response
36
Q

miosis

A
  • constriction of iris due to contraction of sphincter muscle of the iris
  • parasympathetic response
37
Q

ciliary muscle

A
  • controls the lens of the eye
  • when relaxed = far vision = sympathetic
  • when contracted = near vision = parasympathetic
38
Q

Antimuscarinic Agents Toxicity and Cautions

A
  • Toxicity:
    • dry mouth
    • mydriasis
    • tachycardia
    • hot flushed skin
    • agitation
    • delirium
  • Cautions:
    • glaucoma
    • BPH (benign prostatic hyperplasia)
      • urinary retention
    • PUD (peptic ulcer disease)
      • slow emptying of the stomach can worsen
39
Q

Dicyclomine

A
  • muscarinic antagonist
  • treatment for IBS
40
Q

Beta receptors

A
  • Beta 1: increased HR, contractility, and conductivity
    • increased renin secretion
  • Beta 2: bronchodilation and peripheral vasodilation
    • relaxation of uterus
  • Beta 3: bladder and adipose tissue
    • relaxation of sphincter, allows bladder to fully empty
    • used for overactive bladder
41
Q

Phentolamine Indications and SE

A

Alpha blocker

  • pheochromocytoma and HTN crisis follow abrupt withdrawal of clonidine
  • SE:
    • hypotension
    • tachycardia (reflex)
    • arrythmias
    • MI
42
Q

indications and side effects of alpha 1 blockers

A

Indications: HTN, BPH

SE: orthostatic hypotension, syncope, HA, dizziness, impaired ejaculation

43
Q

Beta Blocker Effects and SE

A
  • Effects:
    • Lower the BP
    • increase airway resistance
    • reduce intraocular pressure
  • SE:
    • bradycardia
    • mild sedation
    • cold hands
    • vivid dreams
    • worsen preexisting asthma (nonselective)
    • decreased mycocardial contractility and excitability (not good in CHF!!)
44
Q

Indirect Acting Adrenergic Agonists

A

Releasing agents: amphetamine, tyramine
Uptake inhibitor: cocaine
MOA inhibitors: selegiline
COMT inhibitors: entacapone

NRS 270: Pharmacology (14 decks)

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