Intro To Hypertensives-Kruse Flashcards

1
Q

What part of the nephron does acetazolamide target?

A

PCT

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2
Q

What is the prototype carbonic anydrase inhibitor and what is its MOA?

A

Acetazolamide

Inhibits membrane-bound and cytoplasmic forms of carbonic anhydrase

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3
Q

Describe what happens to the following (increase or decrease) with the administration of acetazolamide:

___ H+ formation inside PCT cell
___ Na/H antiport
___ Na and HCO3 in lumen
___ diuresis

Urine pH is ___ and body pH is ___

A
Decrease
Decrease
Increase
Increase
Increase
Decrease
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4
Q

___ is rarely used as an antihypertensive due to low efficacy as single agents and development of metabolic acidosis. Instead, they are used for glaucoma, acute mountain sickness, and metabolic alkalosis

A

Carbonic anhydrase inhibitors

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5
Q

What are adverse effects of carbonic anhydrase inhibitors?

A

Acidosis, hypoK, renal stones, parasthesias (high doses), sulfonamide hypersensitivity

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6
Q

What are the prototype loop diuretics and what is their MOA?

A

Furosemide and ethacrynic acid

Inhibit luminal Na/K/2 Cl cotransporter

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7
Q

Describe what happens to the following (increase or decrease) when furosemide or ethacrynic acid are administered:

___ intracellular Na, K, Cl in TAL
___ back diffusion of K and positive potential
___ reabsorption of Ca and Mg
___ diuresis

A

Decrease
Decrease
Decrease
Increase

Ion transport virtually nonexistent
Among the most efficacious diuretics available

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8
Q

What are some clinical indications for loop diuretics?

What are some adverse effects of loop diuretics?

A

Used for edema, heart failure, HTN, acute renal failure, anion overdose, and hypercalcemic states

Adverse effects include hypoK, alkalosis, hypocalcemia, hypomagnesemia, hyperuricemia, ototoxicity, sulfonamide hypersensitivity

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9
Q

What is the prototype thiazide diuretic and its MOA?

A

Hydrochlorothiazide

Causes inhibition of the Na/Cl cotransporter (NCC) and blocks NaCl reabsorption in the DCT

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10
Q

Describe what happens to the following (increase or decrease) when given a thiazide diuretic:

___ luminal Na and Cl in DCT
___ diuresis
___ reabsorption of Ca in both DCT and PCT

A

Increase
Increase
Increase

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11
Q

What are some adverse effects of thiazide diuretics?

Thiazide diuretics should be used with caution in patients with ___

A

Adverse effects include hypoK, alkalosis, hypercalcemia, hyperuricemia, HYPERGLYCEMIA, HYPERLIPIDEMIA, sulfonamide hypersensitivity

DM

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12
Q

___ is the most important site of K secretion by the kidney and is the site at which all diuretic-induced changes in K balance occur-more Na delivered to this portion leads to more K secretion

A

Collecting tubule

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13
Q

What are the K sparing diuretics that are mineralocorticoid receptor antagonists and what are some of their uses?

A

Spironolactone and eplerenone

Uses include hyperaldosteronism, adjunct to K-wasting diuretics, antiandrogenic uses (female hirsutism), heart failure (REDUCES MORTALITY)

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14
Q

What are some K sparing diuretics that are ENaC inhibitors and what are some of their uses?

A

Amiloride and triamterene

Uses include adjunct to K-wasting diuretics and Lithium-induced nephrogenic diabetes insipidus (amiloride)

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15
Q

Describe the effects of carbonic anhydrase inhibitors on the following urinary electrolytes:

  • NaCl
  • NaHCO3
  • K
  • Body pH
A

NaCl-Increase (+)
NaHCO3-Increase (+++)
K-increase (+)
Body pH-decrease

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16
Q

Describe the effects of loop agents on the following urinary electrolytes:

  • NaCl
  • NaHCO3
  • K
  • Body pH
A

NaCl-increase (++++)
NaHCO3-no change
K-Increase (+)
Body pH-increase

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17
Q

Describe the effects of thiazides on the following urinary electrolytes:

  • NaCl
  • NaHCO3
  • K
  • Body pH
A

NaCl-increase (++)
NaHCO3-increase (+)
K-increase (+)
Body pH-increase

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18
Q

Describe the effects of loop agents plus thiazides on the following urinary electrolytes:

  • NaCl
  • NaHCO3
  • K
  • Body pH
A

NaCl-increase (+++++)
NaHCO3-increase (+)
K-increase (++)
Body pH-increase

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19
Q

Describe the effects of K-sparing agents on the following urinary electrolytes:

  • NaCl
  • NaHCO3
  • K
  • Body pH
A

NaCl-increase (+)
NaHCO3-slight increase (+)
K-decrease (-)
Body pH-decrease

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20
Q

What are the prototypical ACE inhibitor drugs and what are their MOA?

A

Captopril and enalapril

Inhibit the conversion of Ang I to the more active Ang II; also prevent degradation of bradykinin and other vasodilator peptides

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21
Q

What are some adverse effects associated with ACE inhibitors?

A

Hypotension
COUGH
ANGIOEDEMA
HYPERKALEMIA-avoid K-sparing diuretics
ACUTE RENAL FAILURE-particularly in pts with renal a. stenosis
Fetopathic potential (teratogen)-CONTRAINDICATED IN PREGNANCY

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22
Q

What are some drug interactions associated with ACE inhibitors?

A
Antacids
Capsaicin
NSAIDs
K sparing diuretics
Digoxin
Lithium
Allopurinol
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23
Q

What are some risk factors for ACE inhibitor-induced ARF?

A
  • MAP insufficient for adequate renal perfusion–> poor CO, low systemic vascular resistance
  • Volume depletion (diuretic use)
  • Renal vascular disease –> b/l renal a. stenosis, stenosis of dominant or single kidney, afferent arteriolar narrowing (HTN, cyclosporin A), diffuse atherosclerosis in smaller renal vessels
  • Vasoconstrictor agents –> NSAIDs, cyclosporine

-All cause renal hypoperfusion

24
Q

What type of signal transduction pathway is associated with AT1 receptors?

A

Gq –> PLC –> IP3 + DAG –> smooth m. Contraction

Major subtype in adults

25
Q

___ receptors cause production of NO and bradykinin, smooth m. dilation

A

AT2

26
Q

What are the prototype ARB drugs And what are their MOA?

A

Losartan and valsartan

Selectively block AT1 receptors

27
Q

Describe what happens to the following (increase or decrease) when given an ARB:
___ contraction of vascular smooth m.
___ aldosterone secretion
___ pressor responses
___ cardiac cellular hypertrophy and hyperplasia

A

All decrease

No effect on bradykinin metabolism

28
Q

What are some adverse effects of ARBs and when is it contraindicated?

A

Similar to ACEI’s but less cough and edema; contraindicated in pregnancy

29
Q

___ is a direct renin inhibitor that that blocks the conversion of angiotensinogen to ANG I. It does not increase bradykinin

A

Aliskiren

Similar to ACEIs and ARBs and contraindicated in pregnancy

30
Q

What are the prototypes (or the 2 that kruse wants us to know) for the non-DHP CCB’s? What are their effects?

A

Verapamil > Diltiazem

Promote cardiac effects, but also act at vascular tissues

31
Q

What are the prototypes of DHP CCB’s and their effects?

A

Amlodipine and Nifedipine

Predominantly arteriolar vasodilation effects

32
Q

What are some adverse effects and toxicity related to CCBs?

A
  • GENERALLY VERY WELL TOLERATED
  • Excessive vasodilation-dizziness, hypotension, headache, flushing, nausea; diminished by long-acting formulations and long half-life agents
  • CONSTIPATION (Esp. VERAPAMIL), PERIPHERAL EDEMA, coughing, wheezing, pulmonary edema
  • Use of verapamil/diltiazem with a B-blocker is CONTRAINDICATED b/c of potential for AV block
33
Q

These CCBs should not be used in pts with ventricular dysfunction, SA or AV nodal conduction defects and systolic BP

A

Verapamil/Diltiazem

34
Q

What are clinical uses of CCBs?

A

HTN –> most useful when combo with another agent to counteract the reflex CV responses

Hypertensive emergencies –> parenteral formulations

Angina–> reduction of O2 demand makes particularly useful

35
Q

These drugs increase K permeability, stabilizie the smooth muscle membrane at resting potential, reducing the probability of contraction

A

K channel openers

Includes Diazoxide and Minoxidil

36
Q

This K channel opener vasodilates arterioles but has diminishing use in HTN emergencies due to adverse effects such as excessive hypotension that can cause stroke and MI as well as hyperglycemia

A

Diazoxide

37
Q

This K channel opener vasodilates arterioles and clinical uses include severe HTN and baldness (topical). Adverse affects include headache, sweating, hypertrichosis, and reflex tachycardia and edema (must be used with B blocker and diuretic to avoid this)

A

Minoxidil

38
Q

___ is a D1 receptor agonist. Activation of these receptors by this drug increases blood flow to the kidneys by dilating the afferent arteriole. It is used for HTN emergencies and post-operative HTN

A

Fenoldopam

Adverse effects –> tachycardia, headache, and flushing

Should be avoided in pts with glaucoma due to increases in intraocular pressure

39
Q

THis drug release NO from endothelium and dilates arterioles but not veins. It is first line PO therapy for HTN in pregnancy, with methyldopa.

A

Hydralazine

40
Q

What are some adverse effects of hydralazine?

A
  • can induce fluid and sodium retention
  • headache, nausea, anorexia, flushing, palpitations
  • reflex tachycardia can provoke angina in pts with ischemic heart disease
  • lupus-like syndrome
41
Q

Nitroprusside and organic nitrates are used to tx HTN emergencies, heart failure, and angina (nitrates). What is the prototype?

A

Nitroglycerin

42
Q

___ dilates both arterial and venous vessels - decreases TPR and venous return. They decrease both preload and afterload. Effects are mainly relaxation of large veins –> decrease venous return –> decrease preload –> decrease O2 demand (major effect), smaller decrease in afterload

A

Nitroprusside

43
Q

What are some adverse effects of nitroprusside? Nitrates?

A

Nitroprusside: excessive hypotension, cyanide poisoning

Nitrates: orthostatic hypotension, syncope, throbbing headache

44
Q

Propanolol is this type of B-adrenoreceptor antagonist:

A

Non-selective, Non-ISA (intrinsic sympathomimetic activity)

45
Q

Metoprolol and Atenolol are this type of B-adrenoreceptor antagonist:

A

B1-selective, Non-ISA

46
Q

B blockers are no longer 1st line tx for HTN, except when concomitant with a compelling indication such as:

A

Heart failure
Recent MI
Reduced left ventricular function

47
Q

What is a relative contraindication of usage of beta blockers for HTN?

A

Asthma

48
Q

___ is a selective a1 blocker, nonselective B1 and B2 blocker, and partial agonist at B2. It is used for IV for severe HTN, and an acceptable option for HTN during pregnancy

A

Labetalol

49
Q

___ is a nonselective B blocker + a1 blocker. It has antioxidant properties

A

Carvedilol

50
Q

These drugs are non-selective vasodilating B blockers

A

Carvedilol and Labetalol

51
Q

This B1 selective drug has a very rapid onset and short DOA. It is used as IV fusion for peri-operative tachycardia and HTN, HTN emergencies, and arrhythmias. It is also used in electroconvulsive therapy

A

Esmolol

52
Q

These types of drugs are 3rd or 4th line tx for essential HTN; added to other agents from different classes in refractory cases; also used in men with concurrent HTN and BPH

A

a1 selective receptor blockers

53
Q

__ is an a2 adrenergic receptor agonist. When given IV will increase BP followed by decreased BP. When PO, will decrease BP. It is used clinically for essential HTN (Rarely used). Side effects include sudden withdrawal causing HTN crisis

A

Clonidine

54
Q

___ is a false NT concept and when released acts as a centrally acting a2 agonist and decreases central sympathetic outflow and decreases BP. It is now only used treat HTN in pregnancy because of its safety

A

Methyldopa

55
Q

These diuretics target specific membrane transport proteins:

A

Loop diuretics –> Na/K/2Cl co-transporter
Thiazide diuretics –> Na/Cl co-transporter
K sparing diuretics –> Na channels