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CVS > L11: Vasodilator Pharmacology > Flashcards

L11: Vasodilator Pharmacology Flashcards

1
Q

How do we get vasoconstriction occurring in smooth muscle

A

1) voltage gated smooth channels open during depolarisation
2) calcium influx occurs
3) sarcoplasmic reticulum releases stored calcium
4) calcium binds to move the troponin c from the actin binding site
5) myosin head can join the actin binding site = contraction

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2
Q

What other channels apart form the voltage gated calcium channels cause the intracellular calcium to increase and give contraction

A

Alpha adrenoceptors

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3
Q

What happens when noradrenaline binds to alpha adrenoceptors

A

1) gQ proteins stimulates IP3

2) IP3 causes the release of stored calcium from the sarcoplasmic reticulum

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4
Q

What are the 2 main groups that vasodilators are classed as

A

Direct

Indirect

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5
Q

What does indirect vasodilators effect

A

Block the vasoconstrictors i.e circulating substances

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6
Q

Give examples of indirect vasodilators

A

Beta blockers
RAAS inhibitor
Endothelins blockers

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7
Q

What are the main action of direct vasodilators

A

Drugs that interfere with intracellular calcium

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8
Q

What are 3 main targets of intracellular calcium

A

Voltage gated calcium channels
CGMP (which affects voltage gated calcium channel)
CGMP (which affect actin-myosin contraction)

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9
Q

When can we use vasodilator

A

Hypertension

Angina

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10
Q

What is angina

A

The chest pain when there is inadequate coronary blood flow

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11
Q

What are the causes of angina

A

Obstruction of the coronary artery

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12
Q

What other drugs can be used in angina that are not vasodilator so

A

Beta blockers : reduce cardiac work

Ivabrodine : reduce pacemaker current

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13
Q

What are the vasodilator drugs used in angina

A

Glyceryl trinitrate

Isosorbide mono/di nitrate

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14
Q

How do organic nitrates make their action

A

1) GTN breaks down to give NO
2) NO gives increased CGMP
3) CGMP gives vasodilation by acting on the voltage gated calcium channels

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15
Q

Which vessels does GTN act on

A

Systemic vessels i.e mostly venous

Coronary vessels

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16
Q

What are the side effects of GTN

A

Excess vasodilation can lead to hypotension
Headache due to vasodilation in the head
Reduces mobility to GIT which results in constipation

17
Q

How is GTN administered

A

Sublingual: spray under the tongue

Transdermal

18
Q

What other drugs can be used in angina

A

Calcium channel blockers

19
Q

Name examples of calcium channel blockers

A

Amlodipine
Verapamil
Diltiazem

20
Q

Which vessels do calcium channel blockers act on

A

Systemic vessels

Coronary vessels

21
Q

What is the side effect of calcium channel blocker

A

Flushing

Reduced GIT activity: constipation

22
Q

What are the other clinical uses of vasodilator

A

Peripheral vascular disease e.g raynouds disease
Impotence
Hair loss
Stroke

23
Q

What is Raynouds disease

A

When the skin vessel vasoconstriction in cold weather

24
Q

What is impotence

A

Erection

25
Q

To establish erection what must happen to the blood

A

Increase in blood flow to the corpora cavernosa

26
Q

Which part of the intracellular pathway is targeted for erectrion

A

CGMP

27
Q

Which enzyme breaks down CGMP

A

Phosphodiesterase (PDE)

28
Q

If we inhibit PDE what will happen to CGMP levels

A

Increase

29
Q

If we increase CGMP what will happen

A

Vasodilation as voltage gated calcium channel will be inhibited and actin-myosin contraction will be inhibited

30
Q

Name a PDEA inhibitor we use to treat impotence

A

Viagra (sidenafil)

31
Q

What are the side effects of viagra

A

Drug interaction with GTN

32
Q

What is the treatment used for hair loss

A

Minoxidil

33
Q

Name a minoxidil

A

Regaine

34
Q

How does minoxidil cause local vasodilation

A

Open potassium channels to give hyperpolarisation

35
Q

What are the 2 causes of stroke

A

Haemorrhage

Blockage of blood vessels

CVS (19 decks)

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