Pharmacology: Katzung Drugs used in Hypertension Flashcards

1
Q

What diuretics are used to treat hypertension?

A

Hydrochlorothiazide
Chlorothalidone
Furosemide

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2
Q

What is the MOA and clinical applications for hyrochlorothiazide and chlorothalidone?

A

They block the Na/Cl transporter in the distal convoluted tubule and are used for

(1) hypertension
(2) mild edema

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3
Q

What is the MOA and clinical application for Furosemide?

A

Furosemide blocks the Na/K/2Cl transporter in the TALH. It is used for

(1) HTN
(2) Heart failure
(3) edema
(4) hypercalcemia

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4
Q

What adverse effects are associated with Hydrochlorothiazide and chlorothalidone?

A

(1) Hypokalemia
(2) metabolic alkalosis
(3) Hyperglycemia
(4) Hyperlipidemia
(5) Hyperuricemia
(6) Hypercalcemia

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5
Q

What are the adverse effects associated with Furosemide?

A

(1) Hypokalemia
(2) Hypovolemia
(3) OTOTOXICITY

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6
Q

Why are diuretics used to treat hypertension?

A

Because diuretics will decrease blood volume and this will decrease the systemic blood pressure.

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7
Q

What are sympathoplegics?

A

Sympathoplegics are durgs that interfere with sympathetic control of cardiovascular function

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8
Q

Why are sypathoplegics used to treat hypertension?

A

Because they can decrease venous tone, HR, contractile force, cardiac output, and total peripheral resistance. Altogether this will decrease the blood pressure.

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9
Q

What centrally acting sympathoplegics are used to treat hypertension?

A

Clonidine

Methyldopa

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10
Q

What is the MOA of clonidine?

A

clonidine is an alpha 2 agonist that decreases sympathetic outflow

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11
Q

What are the adverse effects associated with clonidine?

A

(1) sedation
(2) Danger of rebound hypertension if drug is stopped.
(3) dry mouth

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12
Q

What is the MOA for methyldopa?

A

Methyldopa is a prodrug that is converted to methylnorepinephrine in the CNS with results like clonidine.

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13
Q

What are the adverse effects associated with methyldopa?

A

(1) sedation

2) hemolytic antibodies (positive coombs test

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14
Q

What are the ganglion blocking drugs that can be used to treat hypertension?

A

(1) Hexamthonium (obsolete)
(2) Trimethaphan
(3) Mecamylamine

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15
Q

What is trimethaphan used for?

A

Trimethaphan is used as a short acting ganglion blocker in hypertensive emergencies. Creates controlled hypotension.

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16
Q

What is mecamylamine and what is it used for?

A

Mecamylamine is an oral ganglion blocker with a duration of several hours which is under investigation for use in smoking cessation.

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17
Q

What is the major compensatory response to ganglion blockers?

A

salt retention.

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18
Q

What toxicities are associated with ganglion blockers?

A

(1) blurred vision
(2) constipation
(3) urinary hesitancy
(4) sexual dysfunction (sympathetic blockade)
(5) orthostatic hypotension (sympathetic blockade

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19
Q

Which post ganglionic neuron blockers are used to treat hypertension?

A

(1) reserpine

(2) Guanethidine

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20
Q

What are the clinical applications and MOA of reserpine?

A

reserpine blocks the loading of vesicles with catecholamines. It is used to treat

(1) hypertension
(2) Huntington’s disease

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21
Q

What are the adverse effects associated with reserpine?

A

(1) sedation

2) severe psychiatric depression (at high doses

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22
Q

What are the adverse effects and MOA of Guanethidine?

A

Guanethidine blocks re-uptake of norepinephrine. However, it causes severe orthostatic hypertension and is therefore no longer used.

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23
Q

Why are post ganglionic blockers used to treat hypertension?

A

Because they deplete stores of catcholamines thus inhibiting sympathetic activity. This decreases cardiac output and TPR.

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24
Q

What is the compensatory response to post ganglion blockers?

A

salt and water retention

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25
Q

Which alpha blockers are used to treat hypertension?

A

Prazosin
Doxazosin
Terozosin

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26
Q

What is the mechanism of action for alpha blockers?

A

The alpha blockers

(1) reduce TPR
(2) reduce prostatic smooth muscle tone

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27
Q

What is prazosin used for?

A

(1) mild hypertension

(2) benign prostatic hyperplasia.

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28
Q

What adverse effects are associated with prazosin?

A

First dose orthostatic hypertension.

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29
Q

What differentiates doxazosin and terazosin from prazosin?

A

doxazosin and terazosin have a longer duration of action.

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30
Q

Which beta blockers are used to treat hypertension?

A

(1) Propranolol
(2) Atenolol
(3) Metoprolol
(4) labetalol
(5) Carvedilol

31
Q

What is the mechanism of action for propranolol?

A

Propranolol is a non selective beta blocker that reduces cardiac output and possibly renin release also.

32
Q

What are the adverse effects associated with the beta blockers?

A

(1) bronchospasm in asthmatics
(2) excessive cardiac depression
(3) sexual dysfunction
(4) sedation
(5) sleep disturbances

33
Q

What differentiates Atenolol and metoprolol from propranolol?

A

Atenolol and metoprolol are beta 1 selective and have fewer adverse effects.

34
Q

What differentiates Labetalol and carvedilol from propranolol?

A

Labetalol and carvedilol are alpha and beta blockers and can be given orally and parenterally.

35
Q

What calcium channel blockers are used to treat hypertension?

A

Verpamil
Diltiazem
Nifedipine
dyhydropyridines

36
Q

Why are calcium channel blockers used to treat hypertension?

A

they relax vascular smooth muscle and reduce cardiac output. They can also be given orally.

37
Q

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

A

They inhibit L-type calcium channels thus reducing contractility in smooth/cardiac muscle.

38
Q

What are the clinical applications for Verpamil and Diltiazem?

A

verpamil and diltiazem and used for

(1) hypertension
(2) angina
(3) arrythmias.

39
Q

What are the adverse effects associated with calcium channel blockers?

A

(1) Excessive cardiac depression

(2) Constipation

40
Q

What differentiates nifedipine and the dihydropyridines from verpamil and diltiazem?

A

Nifedipine and the dihydropyridines are more vasodilatory and less cardiosupressant.

41
Q

What are the older oral vasodilators?

A

Hydralazine

Minoxidil

42
Q

What is the MOA of hydralazine?

A

it causes the release of NO by endothelial cells causing arteriolar dilation

43
Q

What are the clinical applications of Hydralazine?

A

(1) Hypertension

(2) heart failure

44
Q

What are the adverse effects associated with hydralazine?

A

(1) Tachycardia
(2) salt/water retention
(3) lupus like syndrome

45
Q

What is the MOA for Minoxidil?

A

Minoxidil is a prodrug sulfate metabolite that opens K+ channels and causes arteriolar smooth muscle hyperpolarization and vasodilation

46
Q

What are the clinical applications for minoxidlil?

A

(1) severe hypertension

(2) male pattern baldness

47
Q

What adverse effects are associated with minoxidil?

A

(1) marked tachycardia
(2) salt and water retention
(3) hirsutism.

48
Q

Which parenteral vasodilators are used to treat hypertension?

A

(1) Nitroprusside
(2) Diazoxide
(3) Fenoldopam

49
Q

What is the MOA of Nitroprusside?

A

It releases NO from the drug molecule

50
Q

What are the clinical applications for Nitroprusside?

A

(1) Hypertensive emergencies

(2) cardiac decompensation

51
Q

What are the adverse effects associated with Nitroprusside?

A

(1) excessive hypotension

(2) Prolonged infusion may cause thiocyanate or cyanide toxicity.

52
Q

What is the MOA for Diazoxide?

A

Diazoxide opens K+ channels in smooth muscle and secretory cells.

53
Q

What are the clinical applications for Diazoxide?

A

(1) hypertensive emergencies

(2) Hypoglycemia due to insulin secreting tumors.

54
Q

What are the adverse effects associated with Diazoxide?

A

(1) hyperglycemia
(2) Edema
(3) Excessive hypotension.

55
Q

What is the mechanism of action for fenoldopam?

A

Fenoldopam is a D1 agonist that causes arteriolar dilation

56
Q

What are the clinical uses for fenoldopam?

A

Hypertensive emergencies.

57
Q

What adverse effects are associated with Fenoldopam?

A

Excessive hypotension

58
Q

Which drug functions as a Renin antagonist?

A

Aliskiren

59
Q

What is the MOA of Aliskiren?

A

It is a renin inhibitor that reduces angiotensin I synthesis.

60
Q

What is the clinical application for aliskiren?

A

It is used for hypertension

61
Q

What adverse effects are associated with aliskiren?

A

(1) Angioedema
(2) Renal impairment
(3) headache
(4) diarrhea

62
Q

To what class of drugs do Captopril, benzapril, enalapril, and lisinopril belong to?

A

They are all ACE inhibitors

63
Q

What is the MOA of ACE inhibitors?

A

ACE inhibitors prevent the conversion of angiotensin I to angiotensin II by angiotensin converting enzyme.

64
Q

What are the clinical applications for ACE inhibitors?

A

(1) hypertension
(2) diabetic renal failure
(3) heart failure

65
Q

What are the adverse effects associated with ACE inhibitors?

A

Hyperkalemia, teratogen, cough

Cough
Angioedema
contraindicated in Pregnancy
metalic Taste
hypOtension
Potassium elevation
Rash
Increased renin
Lower angiogensin II and aldosterone
66
Q

What differentiates Captopril from the other ACE inhibitors?

A

Captopril has a shorter half life.

67
Q

To what class of drugs do Losartan, Candesartan, and irbesartan belong to?

A

They are angiotensin II receptor blockers (ARBs)

68
Q

What is the MOA of ARBs?

A

They block angiotensin receptors thus preventing angiotensin mediated vasoconstriction and fluid retention.

69
Q

What are the clinical uses for ARBs?

A

They are used for hypertension.

70
Q

What are the adverse effects associated with ARBs?

A

(1) hyperkalemia

(2) teratogen

71
Q

What are the five components to the stepped care of hypertension?

A

Used in more severe hypertension

(1) lifestyle changes
(2) diuretics
(3) sympathoplegics (beta blockers)
(4) ACE inhibitors
(5) Vasodilators (calcium channel blockers)

72
Q

What drugs are more likely to be effective in treating hypertension in older patients?

A

Older patients respond better to diuretics and beta blockers than to ACE inhibitors

73
Q

What drugs are more likely to be effective in the treatment of african americans with hypertension?

A

African americans are more likely to respond to diuretics and calcium channel blockers than to ACE inhibitors