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RUSVM Pharmacology > Diuretics > Flashcards

Diuretics Flashcards

1
Q

Classes of Diuretics

A

Cardiovascular Diuretics

Physiological Diuretics

Osmotic Diuretics

Loop (High Ceiling) Diuretics

Thiazide Diuretics

Potassium Sparing Diuretics

Carbonic Anhydrase Inhibitors

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2
Q

Physiologic Diuretics

A

Not diuretic by definition, but have diuretic effect

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3
Q

Major effects of Alpha 1 adrenoceptors

A

Vasoconstriction

Increased peripheral resistance

Increased blood pressure

Mydrasis

Increased closure of internal sphincter of the bladder

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4
Q

Therapeutic uses of osmotic diuretics

A

Treatment of cerebral edema

Treatment of glaucoma

Treatment of acute renal failure

Mobilization of edema fluid

Used in patients with drug overdose

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5
Q

Examples of Carbonic Anhydrase Inhibitors

A

Acetazolamide

Methazolamide

Dorzolamide and Brinzolamide (Topical Ophthalmic)

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6
Q

Adverse effects of Thiazide diuretics

A

Electrolyte imbalances

Hyperglycemia

Hypersensitivity reactions

Hyperlipidema

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7
Q

Most effective diuretics are

A

Loop diuretics

________________________________

Inhibit the most reabsorption of Na acting on ALoH

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8
Q

Diuretic efficacy of Spironolactone depends on

A

Levels of endogenous aldosterone

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9
Q

Pharmacokinetics of Triamterine and Amiloride

A

Admistered orally

Amiloride is excreted by the kidneys

Triamterene is convered to an active metabolite in the liver whihc is actively secreted in the urine

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10
Q

What osmotic diuretic is not metabolized and is elimiated rapidly by the kidney

A

Mannitol

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11
Q

Pharmacokinetics of Thiazide Diuretics

A

Administered orally

Absorption is slow and incomplete

Bind extensively to plasma proteins

Excreted maily by the kidneys and are actively secreted in urine by the organic acid secretory machanism

Decreased renal blood flow decreases their effectiveness

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12
Q

Glycerin and isosorbide are administered

A

Orally

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13
Q

Pharmacokinetics of Spironolactone

A

Administered orally

Readily absorbed and is highly bound to plasma protein

Extensively metabolized by the liver and is converted to an active metabolite

Onset of action is slow (2-3 days) and duration of action is long

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14
Q

Diuretic

A

Medication that increases urine flow or urine volume

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15
Q

T/F: Diuretics are drugs that increase urination

A

False

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16
Q

Potency of diuretics depends on

A

Where it acts in the nephron

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17
Q

Examples of physiologic diuretics

A

Water

Sodium Chloride

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18
Q

Therapeutic uses of Thiazide Diuretics

A

Treatment of edema of CHF, liver cirrhosis, nephrotic syndrome and acute glomerular nephritis

Treatment of hypertension alone or combined with other antihypertensive drugs

Treatment of nephrogenic diabetes insipidus and useful in central diabetes insipidus

Treatment of calcium nephrolithiasis and may be useful for the treatment of osteoporosis

Treatment of udder edema in cows

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19
Q

Duretics ranked from most effect to least effective

A

Loop Diuretics > Thiazide Diuretics > Osmotic Diuretics > Potassium Sparing Diuretics

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20
Q

Adverse effects of carbonic anhydrase inhibitors

A

Mild systemic acidosis

Hypokalemia

Hyperglycemia

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21
Q

Mechanism of Action of Osmotic Diuretics

A
  1. Interfere with transport mechanisms in the thick ascending limb increasing the urinary excretion of Na, K, Ca, Mg, Cl, HCO3 and phosphate
  2. Osmotic effect in the tubule and reduce medullary tonicity
  3. Increase renal blood flow and renal medullary blood flow by several mechanisms
22
Q

Mechanism of action of Loop or Ceiling Diuretics

A
  1. Inhibit Na-K-Cl Symporter in the loop of henle
  2. Inhibits the paracellular reabsorption of Na, Ca, Mg
  3. Increased Na delivery to late distal tubule and collecting duct increases depolarization of the luminal membrane creating a lumen -negative transmembrane potentail difference - facilitates K excretion
  4. Stimulate Renin-Angiotension- Aldosterone
  5. Increases total renal blood flow
  6. Increase systemic venous capacitance
23
Q

Therapeutic uses of Triamterine and Amiloride

A

Treatment of hypokalemia and hypomagnesemia

Occassionally used in edematous disorders and hypertension - very weak diuretics

24
Q

Mannitol and urea are administered

A

IV

25
Q

Mechanism of action of Spironolactone

A
  1. Competitively blocks aldosterone binding to aldosterone receptor in the late distal tubule and collecting duct
  2. Excretion of NaCl and diuresis as well as retention of K and H
26
Q

Major effects of Alpha 2 adrenoceptors

A

Inhibition of norepinephrine release

Inhibition of insulin release

27
Q

Mechanism of Action of Thiazide Diuretics

A
  1. Inhibit the Na-Cl symporter in distal convoluted tubule - inhibition of tubular reabsorption of Na, Cl and diuresis
  2. Inhibit K and Mg reabsorption but increase reabsorption of Ca
  3. Cause hypokalemia and systemic alkalosis similarly to loop diuretics
28
Q

Examples of Loop or Ceiling Diuretics

A
29
Q

Therapeutic uses of Spironolactone

A

Diuretic

Treatment of primary and secondary hyperaldosteronism

30
Q

Adverse effects of loop or ceiling diuretics

A

Ototoxicity

Hypokalemia

Hypomagnesemia

Acute hypovolemia

Hypotension

Cardiact arrhythmias

Hyperglycemia

Hyperuricemia

Systemic alkalosis

Hypersensitivity reactions

31
Q

Pharmacokinetics of carbonic anhydrase inhibitors

A

Acetazolamide is administered orally

Onset of action is about 30 minutes and duration of action is 4-6 hours in small animals

Acetazolamide is eliminated maily by the kidneys and is actively secreted in urine by the organic acid secretory mechanism

Dorzolamide and Brinzolamide are administerd topically on the eye

32
Q

Adverse effects of Spironolactone

A

Hyperkalemia

Systemic acidosis

Adverse effects on reproduction because it acts on progesterone and androgen receptors

33
Q

Important Adrenoceptors

A

Alpha 1

Alpha 2

Beta 1

Beta 2

34
Q

Adverse effects of Triamterine and Amiloride

A

Hyperkalemia

Systemic acidosis

35
Q

Examples of Thiazide Diuretics

A

Hydrochlorothiazide

Chlorothiazide

36
Q

Therapeutic use of cardiovascular diuretics

A

Treatment of edema associated with congestive heart failure

37
Q

Mechanisms by which Loop or Ceiling Diuretics contribute to hypokalemia and systemic alkalosis

A
  1. K excretion through K channel in the luminal membrane of the principal cell and H secretion in type A intercalated cell into the lumen
  2. Stimulating the renin-angiotension-aldosterone
38
Q

Examples of Potassium Sparing Diuretics

A

Spironolactone

Triamterene

Amiloride

39
Q

General mechanism of action of all diuretics

A

Inhibit the reabsorption of Na

40
Q

Examples of osmotic diuretics

A

Mannitol

Urea

Glycerin

Iso

41
Q

Examples of cardiovascular diuretics

A

Digitalis

Phosphodiesterase inhibitors

42
Q

Pharmacokinetics of Furosemide

A

Administered orally and IV

Onset of action is rapid and duration is short

Partially metabolized by conjunction and partially excreted unchanged in urine and actively secreted in urine by the organic acid secretory mechanism

43
Q

Cardiovascular Diuretics

A

Not a diuretic by definition, but have diuretic effect

Any drug that cause increased contractility/ cardiac output of the heart to have a diuretic effect due to increased renal blood flow

44
Q

Osmotic diuretics act on what portion of the nephron

A

Act both on the loop of henle (primary site) and proximal tubule (secondary site)

45
Q

Mechanism of action of Triamterine and Amiloride

A
  1. Block epithelial Na channels in the luminal membrane of the principal cells in the late distal tubule and collecting duct
  2. Excretion of Na and diuresis as well as retention of K and H
46
Q

Therapeutic uses of carbonic anhydrase inhibitors

A

Treatment of open-angle glaucoma

Acetazolamide has been used in udder edmea

47
Q

Therapeutic uses of loop or ceiling diuretics

A

Treatment of pulmonary edema and pulmonary congestion

Treatment of generalized edema associated with CHF, chronic renal failure and liver cirrhosis

Combined with isotonic saline to treat hypercalcemia and prevent volume depletion

May be used in patients with acute renal failure

Treatment of increased intracranial pressure and udder edema

Etc.

48
Q

Major effects of Beta 2 adrenoceptors

A

Vasodilation

Slightly decreased peripheral resistance

Bronchodilation

Increased muscle and liver glycogenolysis

Increased release of glucagon

Relaxed uterine smooth muscle

49
Q

Mechanism of action of carbonic anhydrase inhibitors

A
  1. Reversible inhibition of carbonic anhydrase (CA) which inhibits the exchange of hydrogen for sodium in the proximal tubule which is the primary site
  2. Secondary site is the collecting duct
  3. Carbonic anhydrase inhibitors lower intraocular pressure by inhibition of carbonic anhydrase in the eye decreasing formation of aqueous humor
50
Q

Major effects of Beta 1 adrenoceptors

A

Tachycardia

Increased lipolysis

Increased myocardial contractility

RUSVM Pharmacology (19 decks)

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