Adenergic receptors Flashcards

1
Q

α1(Target action)

A
  • Vascular, genitourinary smooth muscle contraction
  • Intestinal smooth muscle relaxation
  • Liver: glycogenolysis, gluconeogenesis
  • Salivary secretion
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2
Q

α2(target action)

A
  • Panreas: decrease insulin secretion
  • Nerve terminals: Decrease NE release
  • CNS: decrease sympathetic tone
  • Platelet aggregation
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3
Q

β1(Target action)

A
  • Heart: Increase force(+ionotropic), Increase rate(+ chronotropic) Increase AV conduction velocity
  • Kidney: increase renin release
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4
Q

β2(Target action)

A
  • Smooth muscle relaxation
  • Skeletal muscle glycogenolysis
  • Liver: glycogenolysis, Gluconeogenesis
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5
Q

D1(Target action)

A

Dilates renal vasculature

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6
Q

Direct acting sympathomimetic drugs

A
Clonidine
Albuterol
Norepinephrine
Phenylephrine
Isoproterenol
Epinephrine
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7
Q

Indirect acting sympathomimetic drugs

A
Mao inhibitors 
Tyramine
Ephedrine
Amphetamine
Cocaine
Tricyclic antidepressants
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8
Q

Epinephrine(selectivity)

A

α, β nonselective

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9
Q

Norepinephrine(selectivity)

A

α, β1 > β2

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10
Q

Isoproterenol(selectivity)

A

β

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11
Q

Phenylephrine(selectivity)

A

α1

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12
Q

Albuterol(selectivity)

A

β2

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13
Q

Clonidine(selectivity)

A

α2(centrally active)

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14
Q

Therapeutic uses of adrenergic agonists and target

A
  • Nasal decongestants(α1)
  • Slow absorption of local anesthetics(α1)
  • Antihypertensive(α2)
  • Treatment of shock(β1, dopamine)
  • Cardiopulmonary resuscitation( α1 epi)
  • Asthma(β2, airway smooth muscle)
  • Anaphylactic reactions(mast cells β2; α1 resistance vessels)
  • Mydriasis (radial muscle α1)
  • Wide angle glaucoma(α1 for vasoconstriction: α2 for reduced secretion)
  • Delay premature labor( uterine β2)
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15
Q

Toxicity & side effects of adrenergic agonist

A
  • Hypertensive reactions– cerebral hemorrhage( α1)
  • Cardiac ventricular arrhythmias
  • Myocardial ischemia
  • Vasoconstriction, ischemia
  • CNS Stimulation-Rebound nasal congestion
  • withdrawal syndrome from α2 agonists
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16
Q

Therapeutic uses of adrenergic antagonists( α-antagonist)

A
  • Hypertension
  • Management of pheochromocytoma
  • Raynaud’s disease
  • Congestive heart failure
  • Benign prostatic hyperplasia
17
Q

Therapeutic uses of adrenergic antagonists(β-antagonist)

A
  • Hypertension
  • Angina
  • Cardiac arrhythmias
  • Reducing mortality after myocardial infarction
  • Hyperthyroidism
  • anxiety states
  • open-angle glaucoma
  • migraine(prophylaxis)
18
Q

Toxicity of adrenergic α-antagonist

A
  • Postural hypotension
  • reflex tachycardia
  • myocardial ischemia
  • Salt and water retention
  • Peripheral edema
  • GI stimulation
  • inhibition of ejaculation
19
Q

Toxicity of adrenergic β-antagonist

A
  • Bronchoconstriction
  • Bradycardia
  • Precipitation of CHF
  • exacerbation of angina and increased risk of death after abrupt withdrawal
  • fatigue
  • cold extremeties
20
Q

β receptor order of selectivity for phenylephrine, isoproterenol, and epinephrine

A

Isoproterenol > Epi&raquo_space; Phenylephrine

21
Q

α receptor order of selectivity for phenylephrine, isoproterenol, and epinephrine

A

Epi > phenylephrine&raquo_space; Isoproterenol

22
Q

How many subtypes of α1 and α2 receptors are there?

A

At least 3 subtypes of each

23
Q

How is Epi made(step by step chemicals)

A

Tyrosine–> L-DOPA –> Dopamine –> Norepi –> Epi