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Y2S1-Pharmacology > Antihypertensive medication 2 > Flashcards

Antihypertensive medication 2 Flashcards

1
Q

Calcium channel blockers are the first line treatment for hypertension in?

A

Elderly

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2
Q

Where are the calcium channels found?

A

1) Heart
2) Blood vessels

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3
Q

Are calcium blockers safe in renal failure?

A

Yes (along with clonidine “sympatholytic”, and others)

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4
Q

What is the use of calcium channel blockers?

A
  • They’re useful in hypertension as they dilate peripheral arteries and decrease the TPR by relaxing the vascular smooth muscle
  • They can be used alone or combined with other drugs
  • Well tolerated in renal failure
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5
Q

What are the classes of calcium channel blockers?

A

1) Dihydropyridines (DHPs, like Nifedipine)

2) Phenylalkylamines (verapamil)

3) Benzothiazepines (diltiazem)

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6
Q

What are the different drugs under dihydropyridine?

A

1) Nifedipine

2) Amlodipine

3) Nitrendipine

4) Nisoldipine

5) Nicardipine

6) Isradipine

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7
Q

What is the mechanism of action of the dihydropyridine calcium channel blockers?

A

They work on the BV more than the heart, causing vasodilation, which will lead to reflex tachycardia as they don’t work much on the heart

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8
Q

What are the drugs under phenylalkylamines?

A

Verapamil

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9
Q

What is the mechanism of action of phenylalkylamines?

A

Blocks the calcium channel in the heart mainly and to a small extent in the blood vessels, and thus it has an important effect on tachyarrhythmias, making it an anti-arrhythmic, vasodilating, and cardio-suppressive drug.

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10
Q

What are the drugs under benzothiazepines?

A

Diltiazem (the only one used clinically)

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11
Q

What is the mechanism of action of benzothiazepines?

A

same same phenylalkylamines

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12
Q

What are the commonly used calcium channel blockers?

A

1) Nifedipine

2) Amlodipine

3) Felodipine

4)Verapamil (auses gingival hyperplasia)

5) Diltiazem

6) Clevidipine (formulated for IV only)

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13
Q

What is the site of action of dihydropyridines?

A

They act mainly on the smooth muscles of the blood vessels, resulting in coronary vasodilation, which is associated with reflex tachycardia (amlodipine reflex tachycardia is milder than nifidepine) and increased CO

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14
Q

When is dihydropyridine used?

A

Hypertension

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15
Q

What is the site of action of verapamil (phenylalkylamine)?

A

It affects all calcium channels but mainly those of the heart, causing vasodilation and slowing the AV conduction reducing the force of contraction of the heart

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16
Q

When is phenylalkylamine used?

A

1) Hypertension

2) Angina

3) In some SVTs

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17
Q

What is the site of action of diltiazem?

A

With an intermediate property, it results in vasodilation and depresses the AV conduction mildly with mild inotropic effects

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18
Q

When is diltiazem used?

A

1) Angina

2) In some Arrhythmias

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19
Q

What are the adverse effects of calcium channel blockers?

A

1) Constipation

  • Due to the relaxation of the smooth muscles of the GI
  • Most common with verapamil and diltiazem and it can be avoided by avoiding high doses

2) Heart failure

  • Verapamil and diltiazem depress the contractility of the heart which could worsen/result in heart failure
  • More likely if they are used with cardiac depressants like beta-blockers
  • We still combine b-blockers to CCB in cases of angina, IHD, & Severe hypertension but it should be done cautiously

3) Disturbance of the cardiac conduction

  • The AV-node suppression can result in AV node block, which could lead to sinus arrest, sino-atrial block, sinus bradycardia, or AV block

4) Exacerbation of ischemic chest pain

  • Dihydropyridines like nifedipine can worsen angina as it cause reflex tachycardia
  • DHP should be avoided in myocardial infarction ad it can be fatal

5) Vascular headache

  • Due to vasodilation of the cerebral blood vessels, most common with DHP
20
Q

What are the drug-drug interactions of calcium channel blockers?

A

1) Beta-blockers

  • Can be used with nifedipine and DHP
  • Should be avoided with verapamil unless the patient has a normal cardiac function other than that it could lead to cardiac failure

2) Digoxin

  • Verapamil increases digoxin plasma levels by 30-50% which could lead to AV block
  • Digoxin has a narrow therapeutic index and thus this could lead to toxicity

3) Grape-fruit

  • It inhibits hepatic microsomal enzyme increasing the bioavailability of nifedipine which could lead to toxicity, and this might cause hypotension

4) Cytochrome P450 Inhibitors

  • CCB particularly DHP, are metabolized by oxidation in the liver and they might compete with other drugs for this pathway
21
Q

What is a direct vasodilator?

A

They are a group of drugs that relax the smooth muscles lowering the peripheral resistance

  • Their use is declining
22
Q

What are the different classes and drugs of direct vasodilation?

A

1) Hydralazine (Aprizoline)

2) Minoxidil (loniten)

3) Sodium nitroprusside (nipride, nitropress)

4) Diazoxide (hyperstat)

5) Fenoldopam

23
Q

What is the mechanism of action of hydralazine?

A

It reduces blood pressure by relaxing the smooth muscles of the arteries increasing the K+ efflux and decreasing the Ca+2 influx

  • It elicits the baroreceptor reflex which means that it has to be coadministered with a diuretic to counteract the sodium and water retention, and a b-blocker to prevent the tachycardia
24
Q

What is the clinical use of hydralazine?

A
  • Safe in pregnancy (along with carvedilol, labetalol, nifedipine, and methyldopa)
  • It is used in chronic hypertension and hypertensive crises which accompanies acute glomerulonephritis/eclampsia
25
Q

What are the adverse effects of hydralazine?

A

Lupus-like syndrome

  • Test for marker to make sure it is not lupus
26
Q

What is the mechanism of action of minoxidil?

A

Similar to hydralazine increasing potassium efflux and decreasing the activity of L-type calcium channels

  • It elicits the baroreceptor reflex which necessitates the use of a b-adrenoceptor antagonist and a diuretic
27
Q

What is the clinical use of minoxidil?

A

Used in long-term therapy for refractory hypertension (high blood pressure that remains uncontrolled despite the use of multiple antihypertensive medications)

28
Q

What is the adverse effects of minoxidil?

A

Hair growth

29
Q

What is the mechanism of action of sodium nitroprusside?

A
  • It dilates both resistance and capacitance BV, it increases the HR but not CO
  • Rapid effect, used in emergencies necessitating continuous infusion
  • Usually administered with furosemide (a diuretic)
30
Q

How is sodium nitroprusside administered?

A

IV drip it should be freshly prepared and covered with foil to protect it from light damage

31
Q

What is the adverse effect of sodium nitroprusside?

A

It can be converted to cyanide and thiocyanate whose accumulation in he body has a risk for toxicity, this risk is minimized by administering sodium thiosulfate/hydroxocobalamin with it

32
Q

Which drug is used in case of hypertensive crises?

A

Hydralazine

sodium nitroprusside

Diazoxide

Fenoldopam

33
Q

What is the mechanism of action of diazoxide?

A
  • Administered intravenously to reduce BP rapidly in case of emergencies
  • Administered with furosemide a diuretic
  • Its use has been declining as it causes unpredictable action and adverse effects like inhibiting insulin release from the pancreas
34
Q

What is the mechanism of action of fenoldopam?

A
  • Peripheral arteriolar dilator, used in hypertensive emergencies and postoperative hypertension
  • It is a dopamine D1 agonist receptor dilating peripheral arteries
35
Q

What are the adverse effects of fenoldopam?

A

1) Reflex tachycardia

2) Headache

3) Increases intraocular pressure so must be avoided in patients with glaucoma

36
Q

Which drugs can be used in Heart failure?

A

1) Thiazide diuretic

2) Beta-Blockers

3) Ace-Inhibitors

4) Angiotensin-receptor-blocker

5) Aldosterone antagonist

37
Q

Which drugs can be used in post-myocardial infarction?

A

1) Beta-Blockers

2) Ace-Inhibitors

3) Aldosterone antagonist

38
Q

Which drugs can be used in patients with a high risk for congestive vascular disease?

A

1) Thiazide diuretic

2) Beta-Blockers

3) Ace-Inhibitors

4) Calcium Channel Blocker

39
Q

Which drugs can be used in diabetes?

A

1) Thiazide diuretic

2) Beta-Blockers

3) Ace-Inhibitors

4) Angiotensin-receptor-blocker

5) Calcium Channel Blocker

39
Q

Which drugs can be used in chronic kidney disease?

A

1) Ace-Inhibitors

2) Angiotensin-receptor-blocker

40
Q

Which drugs can be used to prevent recurrent stroke?

A

1) Thiazide diuretic

2) Ace-Inhibitors

41
Q

What is the first-line drugs in treating a diabetic patient with hypertension?

A

ACEI

42
Q

Which drug should be used in treating hypertension in a patient with benign prostatic hyperplasia?

A

a1 receptor antagonist (a-blockers) like terazosin

43
Q

Hypertension with recurrent migraine, which drug should be used?

A

alpha blockers like

44
Q

Which drugs should be used to treat hypertensive patients with congestive heart failure?

A

1) Diuretic

2) ACEI

3) Spironolactone

4) Receptor antagonist

Y2S1-Pharmacology (14 decks)

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