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Year 2 Pharma > SNS Antagonists > Flashcards

SNS Antagonists Flashcards

1
Q

What do alpha 1 receptors generally do?

A

Vasoconstriction, relaxation of GIT

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2
Q

What do alpha 2 receptors generally do?

A

Inhibit transmitter release, contraction of vascular smooth muscle, CNS actions

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3
Q

What do beta 1 receptors generally do?

A

Increase cardiac rate and force, relaxation of GIT, renin release from kidney

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4
Q

What do beta 2 receptors generally do?

A

Bronchodilation, vasodilation, relaxation of visceral smooth muscle, hepatic glycogenolysis

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5
Q

What do beta 3 receptors generally do?

A

Lipolysis

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6
Q

Give an example of a totally non-selective adrenoceptor antagonist?

A

Carvedilol

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7
Q

Give an example of an alpha adrenoceptor antagonist?

A

Phentolamine

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8
Q

Give an example of an alpha 1 adrenoceptor antagonist

A

Prazosin

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9
Q

Give an example of a beta adrenoceptor antagonist?

A

Propanolol

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10
Q

Give an example of a beta 1 adrenoceptor antagonist?

A

Atenolol

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11
Q

What is hypertension defined as?

A

Blood pressure consistently above 140/90mmHg when sitting or lying down as an average 30 year old male

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12
Q

What is the single most important risk factor for stroke, myocardial infarction and chronic kidney disease

A

Hypertension

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13
Q

What are the main contributors to hypertension?

A

Blood volume
Cardiac output
Vascular tone

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14
Q

Where are the tissue targets for antihypertensive drugs

A 
The heart
Sympathetic nerves that release NA
Kidney - blood vol and vasoconstriction
Arterioles - determine TPR
CNS - determines BP set point and regulates some systems involved in blood pressure control and autonomic NS
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15
Q

What do beta blockers target

A

Beta 1 receptors on:
Heart, Sympathetic nerves, Kidney, CNS control of BP
Beta 2 receptors on:
Sympathetic nerves and CNS

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16
Q

What do beta blockers do in the heart?

A

Decrease HR and force of contraction leading to a decrease in CO. The heart does not have to work as hard - reduced BP

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17
Q

How do beta blockers work in the heart

A

Beta receptors positively coupled with adenylate cyclase, leading to ATP -> cAMP -> PKA. Block the beta receptor so decrease PKA

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18
Q

What do beta blockers do in the kidney?

A

Block sympathetic nerve receptors so decrease renin production, leading to a decrease in angiotensin II release. Loss the vasoconstriction effect and aldosterone production increases

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19
Q

What will a blockade of the facilitatory effects of presynaptic nerve terminals beta adrenoceptors do?

A

decrease NA secretion

Noradrenaline causes vasoconstriction

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20
Q

What are examples of beta blockers?

A 
Propanolol
Carvedilol
Atenolol
Nebicolol
Sotalol
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21
Q

What does propanolol have affinity to?

A

Equal affinity for beta 1 and beta 2 receptors

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22
Q

What does carvedilol have affinity to?

A

It is a mixed beta and alpha receptor

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23
Q

What are the cardioselective beta blockers?

A

Beta 1 selective agents eg atenolol and pindelol

Never totally selective to one receptor, there is always some affinity to the others too

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24
Q

What other effect does the beta blocker nebivolol have?

A

Also potentiates NO

selective to b1

25
Q

What other effect does the beta blocker Sotalol have?

A

Aso inhibits K+ channels

It is also non selective so has affinity to beta 1 and 2

26
Q

Side effects of beta blockers?

A

Bronchoconstriction - dont give to asthmatics and COPD
Cardiac failure - needs some sympathetic drive to the heart
Hypoglycemia - mask the symptoms of hypoglycemia/inhibit glycogen breakdown
Fatigue - decrease cardiac output and muscle perfusion
Cold extremities - loss of b receptor mediated vasodilation in cutaneous vessels
Bad dreams

27
Q

What is the advantage of atenolol over propanolol?

A

Atenolol is more b1 specific so it won’t affect the liver and lungs as much as they are b2 driven - asthmatics and diabetics

28
Q

What are beta 2 liberated responses in lungs and liver

A

Lungs - dilate airways

Liver - liberate glucose

29
Q

What advantage does carvediol have over atenolol and propranolol?

A

It targets a1 too making a more powerful hypotensive effect due to vasodilator properties so decrease TPR (more side effects too)

30
Q

What protein receptor is linked to a1 receptors? what else are a1 receptors linked to?

A

Gq linked and PLC and calcium influx

31
Q

What is the effect of a2 receptors and why?

A

linked to AC which decreases PKA and cAMP due to it being linked to the inhibitory G protein Gi

32
Q

When is a non selective alpha blocker used?

A

To treat phaechromocytoma induced hypertension (tumour in adrenal medulla that pumps out adrenaline)

33
Q

What is an example of a non selective alpha blocker?

A

phentolamine

34
Q

When is an alpha 1 specific blocker used?

A

Inhibit the vasoconstrictor activity of NE - which has modest blood pressure lowering effects and is only used as adjunctive treatment

35
Q

What is an example of an alpha 1 specific blocker?

A

Prazosin

36
Q

What are side effects of phentolamine

A

GI - increase in function leading to diarrhoea

37
Q

Why do alpha 2 receptors reduce the effectiveness of phentolamine?

A

Alpha 2 receptors blocked, reduce negative feedback, so more NA released in synapse which makes competitive reaction between NA and phentolamine and its ability to block

38
Q

Why do baroreceptors reduce the effectiveness of phentolamine?

A

If interfere with vasculature - dilate blood vessels and baroreceptor responses fall, lose vagus nerve activity therefore increases sympathetic activity, so SV increases

39
Q

Give an example of a false transmitter

A

Methyldopa

40
Q

What does methyldopa replace

A

DOPA in the noradrenaline pathway leading to the formation of alpha methyl noradrenaline

41
Q

What is the difference between alpha methyl noradrenaline and noradrenaline?

A

Less active with beta/alpha 1 receptors and more selective to alpha 2 - more neg feedback effect. Also not well metabolised by MAO - so more likely to accumulate and displace NA in the vesicle

42
Q

Why is alpha methyl noradrenaline not being metabolised by MAO relevant and useful?

A

It accumulates in larger quantites than NA therefore can displace NA from vesicles

43
Q

Method of action of methyldopa

A
  • Less active than NA on a1-receptors – less effective in causing vasoconstriction.
  • More active on presynaptic a2-receptors – more negative feedback on NE release.
  • Some minor effects on CNS – stimulates vasopressor centre.
44
Q

Methyldopa side effects

A

Salivary glands - dry mouth

Blood vessels - causes so much hypotension (even tho thats what you want) that it can be limiting

45
Q

What is the main cause of arrhythmias?

A

Myocardial ischemia (damage to heart tissue itself)

46
Q

What can exacerbate the problem of a arrhythmia?

A

Increased sympathetic activity so you want to normlaly slow the heart down

47
Q

Why are beta blockers usually used to treat arrhythmias?

A

b1 drives heart rate and contraction

48
Q

What drug generally used for arrhythmias?

A

Propranolol

49
Q

What are the characteristics of a stable angina?

A

Pain on exertion. Increased demand on the heart. There is still enough blood flow at rest to match tissue demand

50
Q

What is a stable angina due to?

A

Fixed narrowing of the coronary vessels eg atheroma

51
Q

What are the characteristics of an unstable angina?

A

Pain with less and less exertion, culminating with pain at rest

52
Q

What is an unstable angina due to?

A

Platelet-fibrin thrombus associated with a ruptured atheromatous plaque, but without complete occlusion of the vessel. There is risk of infarction

53
Q

What are the characteristics of a variable angina

A

Occurs at rest

54
Q

What is a variable angina?

A

Coronary artery spasm - associated with atheromatous disease

55
Q

How can beta blockers be used to treat an angina?

A

At low doses the b1 selective agents eg metoprolol reduce HR and myocardial contractile activity without affecting bronchial smooth muscle. This reduces oxygen demand whilst maintaining the same degree of effort

56
Q

What is a glaucoma characterized by?

A

Increased intraocular pressure

57
Q

What is a glaucoma caused by?

A

Poor drainage of the aqueous humour

58
Q

What happens if a glaucoma is left untreated?

A

It permanently damages the optic nerve leading to blindness

59
Q

How do beta blockers treat glaucoma?

A

b1 receptors are coupled with carbonic anhydrase. If block b1 then stop the carbonic anhydrase making bicarbonate ions that contribute to the ciliary body making aqueous humour

Year 2 Pharma (34 decks)

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