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Drug Action > Adrenoreceptors > Flashcards

Adrenoreceptors Flashcards

1
Q

What are adrenoceptors?

A

Specific cell membrane receptors in the sympathetic nervous system

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2
Q

What do sympathetic nerves release?

A

Noradrenaline

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3
Q

What are the two groups of adrenoceptors?

A

Alpha

Beta

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4
Q

What is the most potent agonist for the adrenoceptors?

A 
Alpha 1: noradrenaline
Alpha 2: adrenaline
Beta 1: isoprenaline
Beta 2: isoprenaline
Beta 3: isoprenaline
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5
Q

What is the structure of an adrenoceptor?

A 
G-protein coupled receptor
Integral membrane protein
Single polypeptide chain
Extracellular N-terminus
Intracellular C-terminus
7 transmembrane alpha helices
Binding site buried within the plane of the membrane
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6
Q

What are alpha1 adrenoceptors couple to?

A 
G protein Gq
Activates phospholipase C-beta
PLC acts on PIP2
Two products
IP3 and DAG
Ca2+ triggered release
Activation of protein kinase C
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7
Q

What do alpha2 adrenoceptors do?

A

Inhibit adenylyl cyclase

Decrease phosphorylation of intracellular proteins

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8
Q

What is Yohimbine?

A

Treatment of sexual dysfunction

Alpha2 antagonist

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9
Q

What do beta adrenoceptors do?

A

Stimulate adenylyl cyclase

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10
Q

What do cardiac adrenoceptors do?

A 
Beta1
Increase heart rate at sino atrial node
Increase conduction velocity at AV node
Increase contractility of atria
Increase contractility and automacity of ventricles
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11
Q

What is the effect of adrenoceptors on blood vessels?

A

Alpha1 contstriction

Beta2 dilation

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12
Q

What is the effect of adrenoceptors on bronchi?

A

Beta2 dilation

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13
Q

What is the effect of adrenoceptors on the GI tract?

A

Alpha1 and 2 contract sphincters

Beta2 relaxes

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14
Q

What is the effect of adrenoceptors on the uterus?

A

Alpha1 contracts

Beta2 relaxes

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15
Q

What is the effect of adrenoreceptors on the bladder detrusor?

A

Beta 2 and 3 relax

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16
Q

What is the effect of adrenoreceptors on the bladder sphincter?

A

Alpha 2 contract

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17
Q

What is the effect of adrenoreceptors on the Vas deferens?

A

Alpha 1 contract

18
Q

What is the effect of adrenoreceptors on the iris radial muscle?

A

Alpha 1 contract

19
Q

What is the effect of adrenoreceptors on ciliary muscle?

A

Beta 2 relax

20
Q

What is the effect of adrenoreceptors on the liver?

A

Alpha1 and beta2 glycogenolysis

21
Q

What is the effect of adrenoreceptors on adipose tissue?

A

Beta3 lipolysis, thermogenesis

22
Q

What is the effect of adrenoreceptors on skeletal muscle?

A

B2 glycogenolysis, tremor

B3 thermogenesis

23
Q

What is the effect of adrenoreceptors on pancreatic islets?

A

A2 reduced insulin secretion

24
Q

What is the effect of adrenoreceptors on salivary glands?

A

A1 potassium release

B1 amylase secretion

25
Q

What is the effect of adrenoreceptors on nerve terminals?

A

A2 inhibition of transmitter release

B2 enhance release

26
Q

What is the effect of adrenoreceptors on platelets?

A

A2 aggregation

27
Q

What is the effect of adrenoreceptors on mast cells?

A

B2 inhibition of histamine release

28
Q

What is the effect of adrenoreceptors on the brain stem?

A

A2 inhibition of sympathetic outflow

29
Q

Name agonists for the adrenoceptors

A 
A1 phenylephrine
A2 clonidine
B1 dobutamine
B2 salbutamol, terbutaline, salmeterol
B3 mirabegron
30
Q

Name antagonists for the adrenoceptors

A

A1 prazosin, doxazosin
A2 yohimbine, idazoxan
B1 atenolol, metoprolol
B2 butoxamine

31
Q

Uses of adrenaline

A

Cardiac arrest to restore cardiac rhythm
Acute anaphylaxis
Severe asthma

32
Q

How is adrenaline administered?

A

Intramuscularly

Subcutaneously

33
Q

What are the side effects of adrenaline?

A

Tachycardia
Vasoconstriciton
Hypertension
Cardiac arrhythmias

34
Q

Uses of dobutamine

A

Acute heart failure

35
Q

How is dobutamine administered?

A

Intravenously

36
Q

Uses of salbutamol (terbutaline and salmaterol)

A

Asthma

Salbutamol only:Delay premature labour

37
Q

How is salbutamol administered?

A

Orally
Inhaled
Intravenously

38
Q

Uses of mirabegron

A

Treatment of overactive bladder syndrome

39
Q

Uses of phenylephrine

A

Nasal decongestion

40
Q

Uses of clonidine

A

Hypertension

Migraine

41
Q

Use of dexmedetomidine

A

Intravenous sedation

42
Q

What are side effects of B adrenoceptor antagonists?

A 
Bronchoconstriction
Bradycardia
Hypoglycaemia
Fatigue
Bad dreams

Drug Action (19 decks)

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