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Year 1 - HLB Core Drugs > Alpha adrenoreceptor blocker/antagonists > Flashcards

Alpha adrenoreceptor blocker/antagonists Flashcards

1
Q

How many alpha receptors are there?

A
  • 2
  • alpha 1
  • alpha 2
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2
Q

Do adrenergic receptors act on the sympathetic or parasympathetic system?

A
  • sympathetic
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3
Q

Which catecholamines act on the adrenergic receptors?

A
  • adrenaline
  • noradrenaline
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4
Q

What are the main functions of the adrenergic alpha 1 receptors?

A
  • smooth muscle vasoconstriction
  • sweating
  • bladder sphincter closure
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5
Q

What are the main functions of the adrenergic alpha 2 receptors?

A
  • inhibit release of noradrenaline
  • inhibit release of ACh
  • inhibit release of Insulin
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6
Q

Adrenergic receptors are all GPCR, specifically which GPCR are present on alpha 1 and 2 receptors?

A
  • alpha 1 = Gaq
  • alpha 2 = Gai
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7
Q

What is the basic intracellular pathway once Gaq has been activated?

A
  • GCPR, specifically Gaq
  • phospholipase C cleaves PiP2
  • forms IP3 and DAG
  • IP3 stimulates ⬆️ Ca2+ release
  • Ca2+ and DAG activate protein kinase C
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8
Q

What is the basic intracellular pathway once Gai has been activated?

A
  • inhibits adenylyl cyclase released by Gas
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9
Q

When treating hypertension, we need to remember how to calculate BP, which is cardiac output (CO) x systemic vascular resistance (SVR). Therefore what are the main effects on CO and/or SVR that alpha inhibitors have?

A
  • inhibit vasoconstriction of blood vessels
  • ⬇️ systemic vascular resistance
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10
Q

What is a common drug prescribed as an alpha 1 inhibitor that we need to know about?

A
  • doxazosin
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11
Q

What is the mechanism of action of the alpha 1 inhibitor doxazosin?

A
  • binds to alpha 1 receptors
  • inhibits Gaq
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12
Q

Is doxazosin a competitive or non-competitive inhibitor?

A
  • competitive
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13
Q

Is doxazosin a selective or non-selective alpha inhibitor?

A
  • selective alpha 1 inhibitor
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14
Q

Doxazosin is a selective competitive alpha inhibitors. What is the main effect of this drug?

A
  • vasodilation of smooth muscle
  • ⬇️ systemic vascular resistance and BP
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15
Q

What are the 2 most common side effects of the alpha 1 antagonist doxazosin?

A
  • postural hypotension
  • tachycardia (reflex tachycardia)
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16
Q

Doxazosin can cause postural hypotension in older patients, why is this?

A
  • Doxazosin vasodilates blood vessels
  • upon standing blood vessels do not contract quickly
  • fall in blood pressure occurs and patients faint
17
Q

Doxazosin can cause postural hypotension in older patients, which in turn causes tachycardia reflex, commonly known as palpitations. What is tachycardia reflex?

A
  • ⬇️ in BP causes ⬆️ in adrenalin
  • ⬆️ in HR follows to compensate and maintain CO

Year 1 - HLB Core Drugs (21 decks)

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