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Pharmacology > 06 The vascular system: vasodilators > Flashcards

06 The vascular system: vasodilators Flashcards

1
Q

6.01 ACE INHIBITORS

Captopril, enalapril, lisinopril - actions

A

lowers blood pressure by decreasing vasoconstrictor tone and reducing cardiac load

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2
Q

6.01 ACE INHIBITORS

Captopril, enalapril, lisinopril - MOA

A

inhibits angiotensin-converting enzyme (ACE), which reduces synthesis of vasoconstrictor angiotensin II
this decreases aldosterone secretion, which increases salt and water excretion, indirectly decreasing plasma volume and cardiac load

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3
Q

6.01 ACE INHIBITORS

Captopril, enalapril, lisinopril - abs/distrib/elim

A

all are given orally
half-lives: captopril ~2h, lisinopril 12h
enalapril is a prodrug converted to an active moiety by liver enzymes

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4
Q

6.01 ACE INHIBITORS

Captopril, enalapril, lisinopril - clinical use

A

hypertension
heart failure
ventricular dysfunction following MI
diabetic nephropathy
chronic renal insufficiency to prevent progression

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5
Q

6.01 ACE INHIBITORS

Captopril, enalapril, lisinopril - adverse effects

A

hypotension
dry cough
angioedema
renal failure can occur

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6
Q

6.01 ACE INHIBITORS

Captopril, enalapril, lisinopril - special points

A

hyperkalaemia can occur if given with potassium-sparing diuretics
the dry cough and angioedema are due to the drugs producing bradykinin by stimulating the kallikrein-kinin system

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7
Q

6.02 ANGIOTENSIN ANTAGONISTS

Losartan, valsartan, candesartan, irbesartan - actions

A

lowers blood pressure by decreasing vasoconstrictor tone

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8
Q

6.02 ANGIOTENSIN ANTAGONISTS

Losartan, valsartan, candesartan, irbesartan - MOA

A

blocks the action of angiotensin II on the angiotensin II (AT1 subtype) receptor

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9
Q

6.02 ANGIOTENSIN ANTAGONISTS

Losartan, valsartan, candesartan, irbesartan - abs/distrib/elim

A

given orally
half-life 1-2h
half-life of metabolite 3-4h

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10
Q

6.02 ANGIOTENSIN ANTAGONISTS

Losartan, valsartan, candesartan, irbesartan - clinical use

A

hypertension
congestive heart failure
nephropathy

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11
Q

6.02 ANGIOTENSIN ANTAGONISTS

Losartan, valsartan, candesartan, irbesartan - adverse effects

A

hypotension, dizziness
hyperkalaemia can occur

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12
Q

6.02 ANGIOTENSIN ANTAGONISTS

Losartan, valsartan, candesartan, irbesartan - special points

A

does not cause the dry cough or angioedema seen with the ACE inhibitors

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13
Q

6.03 CALCIUM CHANNEL BLOCKERS

Amlodipine, nifedipine, verapamil, diltiazem - actions

A

vascular dilatation lowers blood pressure
amlodipine and nifedipine dilate arterial resistance vessels
(verapamil acts mainly on the heart, slowing the rate)

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14
Q

6.03 CALCIUM CHANNEL BLOCKERS

Amlodipine, nifedipine, verapamil, diltiazem - MOA

A

block voltage-gated calcium channels in vascular smooth muscle, which inhibits calcium influx and thus contraction

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15
Q

6.03 CALCIUM CHANNEL BLOCKERS

Amlodipine, nifedipine, verapamil, diltiazem - abs/distrib/elim

A

given orally
half-lives: amlodipine 35h, nifedipine 2h, verapamil (undergoes first-pass metabolism) ~4h

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16
Q

6.03 CALCIUM CHANNEL BLOCKERS

Amlodipine, nifedipine, verapamil, diltiazem - clinical use

A

hypertension
chronic stable angina pectoris
Prinzmetal’s angina

17
Q

6.03 CALCIUM CHANNEL BLOCKERS

Amlodipine, nifedipine, verapamil, diltiazem - adverse effects

A

amlodipine and nifedipine: reflex tachycardia, hypotension and headache due to vasodilatation
ankle oedema
constipation

18
Q

6.03 CALCIUM CHANNEL BLOCKERS

Amlodipine, nifedipine, verapamil, diltiazem - special points

A

grapefruit juice increases the effects

19
Q

6.04 POTASSIUM CHANNEL ACTIVATOR

Minoxidil - actions

A

marked long-lasting vascular dilatation
lowers blood pressure

20
Q

6.04 POTASSIUM CHANNEL ACTIVATOR

Minoxidil - MOA

A

opens potassium channels
hyperpolarises smooth muscle cells

21
Q

6.04 POTASSIUM CHANNEL ACTIVATOR

Minoxidil - abs/distrib/elim

A

given orally
half-life ~4h

22
Q

6.04 POTASSIUM CHANNEL ACTIVATOR

Minoxidil - clinical use

A

very severe hypertension

23
Q

6.04 POTASSIUM CHANNEL ACTIVATOR

Minoxidil - adverse effects

A

salt and water retention, and tachycardia and angina (therefore given with a loop diuretic and a β blocker)
hirsutism

24
Q

6.04 POTASSIUM CHANNEL ACTIVATOR

Minoxidil - special points

A

also used topically to treat baldness

25
Q

6.05 VASODILATOR AND SMOOTH MUSCLE RELAXANT

Hydralazine - actions

A

relaxes arterial smooth muscle, thus lowering blood pressure

26
Q

6.05 VASODILATOR AND SMOOTH MUSCLE RELAXANT

Hydralazine - MOA

A

interferes with the release of Ca2+ from the sarcoplasmic reticulum in vascular smooth muscle cells

27
Q

6.05 VASODILATOR AND SMOOTH MUSCLE RELAXANT

Hydralazine - abs/distrib/elim

A

given orally
half-life ~1–3h

28
Q

6.05 VASODILATOR AND SMOOTH MUSCLE RELAXANT

Hydralazine - clinical use

A

very severe hypertension - particularly in pregnancy
cardiac failure, in combination with a nitrate

29
Q

6.05 VASODILATOR AND SMOOTH MUSCLE RELAXANT

Hydralazine - adverse effects

A

palpitations, tachycardia, hypotension
flushing
GIT disturbances
dizziness
allergic reactions (which can be severe with long-term use)
treatment for more than 6 months can provoke a systemic lupus erythematosus-like syndrome

30
Q

6.06 ENDOTHELIN ANTAGONIST

Bosentan - actions

A

decreases both pulmonary and systemic vascular resistance, resulting in increased cardiac output without increasing the heart rate

31
Q

6.06 ENDOTHELIN ANTAGONIST

Bosentan - MOA

A

dual endothelin receptor antagonist - i.e. affinity for both endothelin A and B (ETA and ETB) receptors

32
Q

6.06 ENDOTHELIN ANTAGONIST

Bosentan - abs/distrib/elim

A

given orally
half-life ~5h
bosentan is eliminated by biliary excretion following metabolism in the liver by the cytochrome P450 iso­enzymes, CYP2C9 and CYP3A4

33
Q

6.06 ENDOTHELIN ANTAGONIST

Bosentan - clinical use

A

idiopathic pulmonary hypertension

34
Q

6.06 ENDOTHELIN ANTAGONIST

Bosentan - adverse effects

A

anaemia
diarrhoea
flushing
gastro-oesophageal reflux disease
headache
nasal congestion
palpitations
skin reactions
syncope

Pharmacology (34 decks)

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