Adrenergic Drugs Flashcards

1
Q

name the inhibitors of catecholamine storage

A
  • amphetamine
  • pseudoephedrine
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2
Q

amphetamine

A

inhibitor of catecholamine storage

  • moa
    • releases NE and dopamine (DA) from nerve terminals
    • block reuptake of NE by blocking NE transporters
    • overall increase of NE levels in synaptic cleft in sympathetic NS and in CNS
  • clinical use
    • treatment of ADHD
  • side effect
    • drug abuse
    • increased DA in brain = paranoia + hallucinations
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3
Q

pseudoephedrine

A

inhibitor of catecholamine storage

  • moa
    • releases stored NE from nerve terminals
    • α and β agonist activity
  • clinical use
    • treatment of nasal and sinus congestion
  • side effect
    • CNS stimulation
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4
Q

name inhibitors of catecholamine reuptake

A
  • cocaine
  • imipramine
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5
Q

cocaine

A

inhibitor of catecholamine reuptake

  • moa
    • inhibits NE transporter
  • clinical use
    • previous use = local anesthetic
  • side effect
    • drug abuse
    • leads to depletion of dopamine which triggers cravings
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6
Q

imipramine

A

inhibitor of catecholamine reuptake

  • moa
    • blocks NE transporter
  • clinical use
    • treats mild depression
  • side effect
    • postural hypotension
    • tachycardia
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7
Q

iproniazid (discontinued now)

A

inhibitor of catecholamine metabolism

  • moa
    • blocks metabolism of NE in the nerve terminals
    • MAOIs increase NE levels which provide more NE available for release into synaptic cleft
  • clinical use
    • treats depression
  • side effect
    • must not eat food containing tyramine (fermented foods) since is causes release of NE from nerve terminals
      • can cause massive vasoconstriction leading to “hypertensive crisis” which can result in a stroke
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8
Q

name the α agonists

A
  • oxymetazoline
    • α1 and α2 agonist
  • phenylephrine
    • α1 agonist
  • clonidine
    • α2 agonist
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9
Q

describe the moa of α agonists

A
  • causes vasoconstriction that increases the total peripheral resistance and increases BP
  • no effect on heart but due to causing an increased BP will cause reflex bradycardia
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10
Q

clinical usage of oxymetazoline

A
  • nasal decongestant (relief due to nasal vasoconstriction)
  • ophthalmic hyperemia (vasoconstriction of the conjunctiva)
    • eye drops relieve redness and itchy eyes
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11
Q

clinical usage of phenyleprhine

A

α1 agonist

  • emergency treatment of shock
  • nasal decongestant (relief due to vasoconstrictor effect on nasal mucosa
  • side effect: hypertension
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12
Q

clinical usage of clonidine

A

α2 agonist

  • treatment of hypertension
  • use in treatment of symptoms associated with drug withdrawal
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13
Q

name the β blockers

A
  • propranolol
    • non-selective β blocker
  • atenolol
    • selective β1-blocker
  • pindolol
    • partial β1 agonist
      • reduces the effect of endogenous NE at β1 receptors
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14
Q

name the function of β blockers

A
  • all β blockers are competitive antagonists
  • decreases HR and CO
  • decrease SA and AV nodal activity
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15
Q

clinical usage and side effects of propranolol

A
  • clinical use
    • treatment for hypertension and angina
  • side effect
    • non-competitive, thus more severe sedation, bronchodilation and dyspnea
    • bronchoconstriction (COPD + ashtma patients)
    • metabolic disturbances (diabetes patients)
      • due to decreased glycogenolysis and glucagon secretion
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16
Q

clinical use and side effects of atenolol

A

selective β1-blocker

  • clinical use
    • treatment for hypertension and angina
    • reduces blood voluma via decreased renin production
17
Q

clinical usage and side effects of pindolol

A

partial β1 agonist

  • treatment for hypertension in patients with bradycardia or low cardiac reserve
  • side effects:
    • bronchoconstriction
    • metabolic disturbances
    • partial agonists are weak antagonists, thus weak stimulatory effects on both β1 and β2 receptors
18
Q

name α antagonists

A
  • phenoxybenzamine
    • α1 and α2 antagonist
    • irreversible and non-competitive
  • phentolamine
    • α1 and α2 antagonist
    • reversible and competitive antagonist of NE/Epi
  • tamsulosin
    • α1 antagonist
19
Q

what is the moa of α antagonists

A
  • prevent sympathetically mediated vasoconstriction and hence cause vasodilation and profound fall in BP
20
Q

name clinical use and side effects of phenoxybenzamine

A

α1 and α2 antagonist

  • given prior to removal of tumor surgically as to avoid hypertensive crisis
  • given for long-term management of pheochromocytoma where surgery not an obvious option
  • side effect:
    • postural hypotension
    • nasal congestion
    • failure of ejaculation
21
Q

describe clinical use of phentolamine

A
  • treatment of pheochromocytoma
    • preferable to phenoxybenzamine since it is reversible
22
Q

name clinical use and side effect of tamsulosin

A

α1 antagonist

  • used to treat benign prostatic hyperplasia
    • relaxes internal sphincter (trigone muscle) of bladder and relaxes smooth muscle associated with prostate gland which relieves urinary hesitancy
  • α1A subtype of the α receptor preferentially expressed in genitourinary smooth muscle
  • side effect: postural hypotension, nasal congestion, less reflex tachycardia
23
Q

name clinical use and side effect of prazosin

A
  • used to reduce blood pressure
  • side effects: marked postural hypotension (particularly after first dose)
24
Q

name the β agonists

A
  • dobutamine
    • β1 agonist
  • albuterol
    • β2 agonist
25
Q

name moa, clinical use and side effects of dobutamine

A

β1 agonist

  • moa
    • increase HR and force of contraction, thus increasing CO
  • clinical use
    • used in acute management of heart failure (NOT chronic heart failure)
  • side effect
    • not usually used for treatment of chronic heart failure since they also increase HR, which makes the heart work harder
26
Q

name the moa, clinical use and side effects of albuterol

A

β2 agonist

  • moa
    • powerful bronchodilator effect due to relaxation of bronchial smooth muscle
  • clinical use
    • used for treatment of asthma
  • side effect
    • restlessness, anxiety
    • tachycardia with high doses due to stimulation of β1