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Pharmacology II > Antihypertensive agents & angina pectoris > Flashcards

Antihypertensive agents & angina pectoris Flashcards

1
Q

Systolic blood pressure of 140 or greater or diastolic blood pressure of 90 or greater.

Risk factors:
•Smoking
•Metabolic syndrome
•Manifestations of end organ damage at the time of diagnosis
•Family history

A

HYPERTENSION

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2
Q

Classification of Hypertension:

A

<120/80 - Normal
120-139/80-89 - Prehypertension
>= 140/90 - Hypertension
140-159/90-99 - Stage 1
>=160/100 - Stage 2

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3
Q

Hypertension Etiology

A

Essential/primary Hypertension
Secondary Hypertension

Contributing Factors:
- Genetic factors
- Physiological stress
- Environmental & dietary factors

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4
Q

Anatomic sites of blood pressure control

A
  1. Resistance - Arterioles
  2. Capacitance - Venules
  3. Pump output - Heart
  4. Volume - Kidneys
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5
Q

BASIC PHARMACOLOGY OF ANTIHYPERTENSIVE AGENTS:

A

•DRUGS THAT ALTERS SODIUM & WATER BALANCE: DIURETICS
•DRUGS THAT ALTER SYMPATHETIC NERVOUS SYSTEM FUNCTION: SYMPATHOPLEGIC AGENTS
•DIRECT VASODILATORS:
•AGENTS THAT BLOCK PRODUCTION OR ACTION OF ANGIOTENSIN

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6
Q
  • lowers BP by depleting the body of sodium stores and reducing blood volume or other mechanisms.
  • Increase urine excretion
  • Reduce the circulating fluid volume to treat edema and hypertension.

Agents used:
Thiazide
Loop diuretics
Potassium-sparing diuretics
Osmotic diuretics

A

DIURETICS

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7
Q
  • For mild to moderate hypertension and normal renal and cardiac function.

•Hydrochlorothiazide
•Chlorthalidone

Uses:
-Hypertension
-Edema
-Prophylaxis of calculu formation

Side effects:
-Hypokalemia
-Muscle weakness
-Postural hypotension Hyperglycemia
-Increase uric acid level

A

Thiazides (Diuretics)

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8
Q

-Acts directly on the loop of Henle in the kidney to inhibit sodium and chloride reabsorption which in turn inhibits water reabsorption back into the bloodstream leading to increased urine formation.
• Furosemide
• Bumetanide

Uses:
-Edema
-Pulmonary edema
-Ascites
-Hypertension combined with antihypertensives especially in patients with kidney disease.

Side Effects:
-Fluid & electrolyte imbalance -Hypotension
-Hyperglycemia & increase uric
acid level

A

Loop Diuretics

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9
Q

-Prevent potassium depletion and enhance the natriuretic effects of other diuretics,
-Counteracts the increase of glucose and uric acid levels
•Spironolactone
•Triamterene

Uses:
-Used in combination with thiazide diuretics
-To increase the diuretic and hypotensive effects and reduce the dangers of hyperkalemia.

Side Effects:
Hyperkalemia
Fatigue, lethargy
Hypotension
Gynecomastia

A

Potassium-Sparing Diuretics

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10
Q
  • Used to reduce intracranial pressure (ICP) or intraocular pressure (IOP). - Used in emergency cases that involves cranial or spinal trauma & used to reduce the risk ofnnervous system damage from swelling.
    • Mannitol

Side Effects:
- fluid & electrolyte imbalance
- CNS symptoms
- Gl symptoms
- Tachycardia
- Allergic reactions
- Pulmonary edema

A

Osmotic Diuretics

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11
Q
  • Used for the treatment of hypertension during pregnancy.
    -Lowers BP by reducing peripheral vascular resistance with a variable reduction in heart rate and cardiac output.

Pharmacokinetics:
half-life: 2 hours
bioavailability: 25%
initial dose: 1g/day

Toxicity:
Sedation
Mental lassitude & impaired mental
concentration.
Nightmares
Mental depression
Vertigo
EPS

A

Methyldopa (CENTRALLY ACTING SYMPATHOPLEGIC DRUGS)

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12
Q
  • used in the treatment of hypertension.
  • Lowers BP in the supine position and rarely causes postural hypotension.

Pharmacokinetics:
half-life: 8-12 hours
bioavailability: 95%
initial dose: 0.2mg/day

Toxicity:
- Dry mouth
- Sedation
- Nervousness
- Tachycardia
- H/A
- Sweating

A

Clonidine (CENTRALLY ACTING SYMPATHOPLEGIC DRUGSl

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13
Q
  • Inhibits the release of norepinephrine from the sympathetic nerve endings.
  • It replaces norepinephrine and causes a gradual depletion of norepinephrine stores in the nerve endings.
    -It interferes with amine release.
  • Half-life: 5 days

Toxicity:
Symptomatic postural hypotention Delayed or retrograde ejaculation
Diarrhea

A

Guanethidine (ADRENERGIC NEURON-BLOCKING AGENTS)

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14
Q

-Blocks the ability of aminergic transmitter vesicle to take up & store biogenic amines by interfering with the vesicular membrane associated transporter (VMAT).

-Half-Life: 24-48 hours
-Bioavailability: 50%
-Initial dose: 0.25mg/day

Toxicity:
- Sedation
- Lassitude
- Nightmares
- Severe mental depression

A

Reserpine (ADRENERGIC NEURON-BLOCKING AGENTS)

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15
Q
  • Decreases BP primarily as a result of a decrease in cardiac output.
  • Inhibits the stimulation of renin production by caatecholamines.
  • Most effective in patients with high plasma renin activity.

Half-life: 3-5 hours
Bioavailability: 25%
Initial dose: 80mg/day

A

Propranolol (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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16
Q
  • Less bronchial constriction than propranolol at doses that produce equal inhibition of B-adrenoceptor responses.
  • Metabolized by CYP2D6 with high first-pass metabolism.

Half-life: 4-6 hours

A

METOPROLOL (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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17
Q
  • Less effective than metoprolol in preventing complications of hypertensions

Half-life: 6 hours

Patients with reduced renal functions should receive lower doses.

A

ATENOLOL (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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18
Q

-Non selective B-receptor antagonist. -Not metabolized & excreted in the urine.

A

Nadolol & Carteolol (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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19
Q
  • B1-selective blockers
  • Primary metabolized in the liver.
A

Betaxolol & Bisoprolol (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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20
Q
  • These drugs are partial agonist
    -Lowers BP but they are rarely used in HPN.
A

Pindolol, Acebutolol, & Penbutolol (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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21
Q
  • Labetalol is useful in the treatment of hypertension of pheochromocytoma & hypertensive emergencies. Formulated as a racemic mixture of 4 isomers.
  • Carvedilol also administered as a racemic mixture. With a half-life of 7-10 hours.
  • Nebivolol is a B1-selective blocker & vasodilating property that is not mediated by alpha blockade, with a half-life of 10-12 hours.
A

Labetalol, Carvedilol, & Nebivolol (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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22
Q
  • A BI-selective blocker, rapidly metabolized via hydrolysis by RBC esterases.
  • Short half-life: 9-10 minutes
  • Administered through IV infusion
A

Esmolol (BETA-ADRENOCEPTOR-BLOCKING AGENTS)

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23
Q
  • Produces their antihypertensive effects by selectively blocking alpha I receptors in arterioles & venules.
  • Reduces arterial pressure by dilating both resistance & capacitance vessels.
  • More effective when used in combination with B-blockers & a diuretic.

Uses:
- Prostatic hyperplasia
- Bladder obstruction symptoms
- Hypertension
- BPH

Toxicity:
Dizziness
Palpitations
H/A
Lassitude

A

Prazosin, Terazosin & Doxazosin (ALPHA I BLOCKERS)

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24
Q
  • Nonselective agents
  • Used in diagnosis & treatment of PHEOCHROMOCYTOMA & in other clinical situations.
  • used in the treatment of clonidine withdrawal syndrome in combination with B-blockers.
A

Phentolamine & Phenoxybenzamine (ALPHA ADRENOCEPTOR-BLOCKING AGENTS)

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25
Q

Oral vasodilators for long-term therapy of HPN.

A

HYDRALAZINE & MINOXIDIL (VASODILATORS)

26
Q

Parenteral vasodilators for hypertensive emergencies

A

NITROPRUSSIDE & FENOLDOPAM (VASODILATORS)

27
Q

-used in ischemic heart disease & hypertensive emergencies

A

CALCIUM CHANNEL BLOCKERS & NITRATES (VASODILATORS)

28
Q
  • Useful in combination therapy in the treatment of severe HPN..
  • Hydralazine in combination with nitrates is effective in heart failure.
  • Dilates arterioles but not veins.
  • Well-absorbed & well metabolized in the liver.

Availability: 25%
Half-life: 1.5 to 3 hours
Dose: 40 to 200mg/day

Toxicity:
H/A
Anorexia
Palpitations
Sweating
Flushing
Peripheral neuropathy
Drug fever

A

HYDRALAZINE (VASODILATORS)

29
Q
  • The effect results from the opening of potassium channels in smooth muscle membranes by minoxidil sulfate (active metabolite).
  • Increase potassium permeability stabilizes the membrane at its resting potential and makes contraction less likely.
  • Dilates arterioles but not veins

Half-life: 4 hours
Bioavailability:90%
Initial dose: 5-10mg/day
- Used in combination with B-blocker & a loop diuretic.

Toxicity:
Tachycardia
Palpitations
Angina
Edema
H/A
Sweating
Hypertrichosis

A

MINOXIDIL (VASODILATORS)

30
Q
  • Hypertensive emergencies & for severe heart failure.
  • Dilates both the arterioles and venous vessel
  • The action of sodium nitroprusside results from the activation of granylyl cyclase, either via the release of nitric oxide or by direct stimulation of the enzyme.
  • Rapidly metabolized by uptake into RBC with release of nitric oxide & cyanide.
  • Lowers BP rapidly & its effect disappear 1-to 10 minutes after discontinuation.

Toxicity:
excessive BP lowering
accumulation of cyanide
metabolic acidosis
arrythmias
death

A

SODIUM NITROPRUSSIDE (VASODILATORS)

31
Q
  • Long-acting potassium channel opener that causes hyperpolarization in smooth muscle and pancreatic B-cells.
  • Dilates the arterioles
  • Used in the treatment of hypoglycaemia in hyperinsulinism.

Half-life: approx. 24 hours

  • Partially metabolized

Toxicity:
Excessive hypotension
Angina
Ischemia
Cardiac failure

A

DIAZOXIDE (VASODILATORS)

32
Q
  • A peripheral arteriolar dilator for hypertensive emergencies & postoperative HPN.
  • Acts primarily as an agonist of dopamine DI receptors, resulting in dilation of peripheral arteries & natriuresis.
    -;Rapidly metabolized by conjugation

Half-life: 10 minutes

Toxicity:
Reflex tachycardia
H/A
Flushing
Increase intraocular pressure

A

FENOLDOPAM (VASODILATORS)

33
Q

Uses:
-Angina
-Anti-arrythmic effects
-Reduces peripheral resistance and BP

Moa:
Inhibits calcium influx into arterial smooth muscle cells.
Ex Verapamil, Diltiazem, Dihydropyridine family

NIFEDIPINE & other dihydropyridine - are more selective as vasodilators & less cardiac depressant effects than Verapamil & Diltiazem,

A

CALCIUM CHANNEL BLOKERS

34
Q

Lisinopril, Enalapril, Captopril
- Inhibition of ACE lowers BP by decreasing vasoconstriction.
- First or second line agents in the treatment of HPN are excellent alone, but can also be used in combination with diuretics & calcium channel blocker.

Side effects:
Rash/photosensitivity
Severe hypotension
Chronic dry cough or nasal congestion
hyperkalemia

A

ACE INHIBITORS

35
Q
  • Inhibit the converting enzymes peptidyl dipeptidase, that hydrolyzes angiotensin I to angiotensin II & inactivates bradykinin, a potent vasodilator that works at least in part by stimulating release of nitric oxide & prostacyclin.
  • Enalapril - prodrug
  • Good choice for patients with other serious conditions:
    •Heart failure
    •Following myocardial infarction •When high coronary disease risk exists
    •Diabetes
    •Renal disease and cardiovascular disease
  • Useful in treating patients withbchronic kidney disease because they diminish proteinuria & stabilize renal function.

Drug of Choice:
For hypertensive patients with nephropathy- they slow the progression of renal disease

A

ACE INHIBITORS

36
Q
  • The first marketed blockers of angiotensin II type I receptor.
  • They have no effect on bradykinin metabolism therefore more selective blockers of angiotensin effects than ACE inhibitors.
  • Commonly used in patients who have had adverse reactions to ACE inhibitors.
A

Losartan & Valsartan (ANGIOTENSIN RECEPTOR-BLOCKING AGENTS(ARB))

37
Q

The primary symptom of ischemic heart disease is _______ which is the most common form of angina.

A

Ischemic Heart Disease….ANGINA PECTORIS

38
Q

Chest pain resulting from decreased blood supply to the heart.

Caused by transient episodes of myocardial ischemia which are due to imbalance in the myocardial oxygen supply.

A

Angina Pectoris

39
Q

If there’s an inadequate blood flow in the presence of CAD.

Diagnosis is usually made on the basis of history and stress testing.

A

Classic/Effort Angina

40
Q

• Caused by spasm in the coronary arteries (at rest).
• Usually occurs in younger patient
• Diagnosis is made on the basis of history

A

Vasospastic/Variant/Prinzmetal Angina

41
Q

• Episodes of angina occurs at rest.
• Caused by episodes of increased epicardial coronary artery resistence or small platelet clots occurring in the vicinity of an atherosclerotic plague.
• Can happen without physical exertion.

A

Unstable Angina

42
Q

• Occurs when heart is working harder than usual.
• When a patient has brief episodes of pain, squeezing pressure or tightness in the chest. Occurs with activity or emotional stress.

A

Stable Angina

43
Q

These drugs are used for the treatment and prophylactic management of angina.
•Nitrates
•Beta-blockers
•Calcium Channel blockers

A

CORONARY VASODILATORS (TREATMENT)

44
Q

Inhibition of ACE lowers blood pressure by

A

Decreasing vasoconstriction

45
Q

Nitrates are used in hypertensive emergencies.
Vasodilators works best in combination with other antihypertensive drugs that oppose the compensatory cardiovascular response.
All vasodilators are useful in hypertension, relaxes smooth muscle arterioles, thereby decreasing systemic vascular resistance

A

True

46
Q

Diltiazem is classified as

A

Calcium channel blocker

47
Q

Produces competitive antagonism of catecholamine by a blockade of alpha 1 receptors

A

Phentolamine

48
Q

Sympatholegic agent lowers blood pressure by

A

Reducing peripheral vascular resistance, inhibiting cardiac function and increase venous pooling

49
Q

Contributing factors to the development of hypertension:
1.Genetic factors
2.Increase salt, decrease K or Ca intake
3. Psychological stress
4. Exposure to chronic stress

A

True

50
Q

This drug is sensitive to light and must be prepared fresh when administered. This deug lowers blood pressure rapidly and its effect disappear 1 to 10 minutes after discontinuation.

A

Sodium nitroprusside

51
Q

Most common side effects of antihypertensive agents:
l. Postural hypotension
II. Muscle weakness
III. Bradycardia
IV. K deficiency

A

“True or F”

52
Q

A cardioselective beta blocker used for the treatment of hypertension

A

Metoprolol
Atenolol
Esmolol

53
Q

An adverse effect of ace inhibitor

A

Dry cough

54
Q

In case of acute angina, which of the following route of administration is appropriate?

A

Sublingual

55
Q

The following are used to treat methemoglobinemia as a toxic effect of nitrites:

A

Hydroxocobalamin
Methylene blue

56
Q

A pFOX inhibitor which partially inhibit the fatty acid oxidation pathway in myocardium:

A

Trimetazidine

57
Q

used as an inhalant?

A

Amyl nitrite

58
Q

First line of choice in the treatment of chronic effort angina

A

Beta blockers

59
Q

Drugs best for intermittent claudication

A

Pentoxifylline

60
Q

Coronary vessels letters are used for the

A

Treatment of angina

61
Q

Nitroglycerin is classified as

A

Anti-angina

Pharmacology II (8 decks)

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