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
What is the effect of adrenoreceptors on nerve terminals?
A2 inhibition of transmitter release | B2 enhance release
26
What is the effect of adrenoreceptors on platelets?
A2 aggregation
27
What is the effect of adrenoreceptors on mast cells?
B2 inhibition of histamine release
28
What is the effect of adrenoreceptors on the brain stem?
A2 inhibition of sympathetic outflow
29
Name agonists for the adrenoceptors
``` A1 phenylephrine A2 clonidine B1 dobutamine B2 salbutamol, terbutaline, salmeterol B3 mirabegron ```
30
Name antagonists for the adrenoceptors
A1 prazosin, doxazosin A2 yohimbine, idazoxan B1 atenolol, metoprolol B2 butoxamine
31
Uses of adrenaline
Cardiac arrest to restore cardiac rhythm Acute anaphylaxis Severe asthma
32
How is adrenaline administered?
Intramuscularly | Subcutaneously
33
What are the side effects of adrenaline?
Tachycardia Vasoconstriciton Hypertension Cardiac arrhythmias
34
Uses of dobutamine
Acute heart failure
35
How is dobutamine administered?
Intravenously
36
Uses of salbutamol (terbutaline and salmaterol)
Asthma | Salbutamol only:Delay premature labour
37
How is salbutamol administered?
Orally Inhaled Intravenously
38
Uses of mirabegron
Treatment of overactive bladder syndrome
39
Uses of phenylephrine
Nasal decongestion
40
Uses of clonidine
Hypertension | Migraine
41
Use of dexmedetomidine
Intravenous sedation
42
What are side effects of B adrenoceptor antagonists?
``` Bronchoconstriction Bradycardia Hypoglycaemia Fatigue Bad dreams ```