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Renal Module > Renal Pharmacology: Diuretics and Aquaretics > Flashcards

Renal Pharmacology: Diuretics and Aquaretics Flashcards

1
Q

What class of drug is Acetozolamide?

A

Acetozolamide is a carbonic anhydrase inhibitor

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2
Q

What is the MOA for acetozolamide?

A

Acetozolamide inhibits carbonic anhydrase which is responsible for converting CO2 and H2O into carbonic acid and vice versa.

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3
Q

Where is acetozolamide active in the body?

A

(1) 90% in the proximal tubule

(2) 10% in the distal tubule

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4
Q

What is the physiological effect of acetozolamide?

A

(1) it increases bicarbonate excretion
(2) Thus it alkalinates the urine
(3) It also decreases Cl- reabsorption

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5
Q

What is acetozolamide used for?

A

(1) it is used as a diuretic
(2) it is used to to alkalinized the urine (cystinuria)
(3) It is used in the prophylaxis of altitude sickness.
(4) Reduces intra-occular pressure
(5) management of siezures (unkown)

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6
Q

What are the adverse effects associated with acetozolamide?

A

(1) metabolic acidosis

2) hypokalemia (increases K+ lost in the urine

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7
Q

What class of drug is mannitol?

A

Mannitol is an osmotic diuretic

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8
Q

What is the MOA for mannitol?

A

(1) mannitol creates an osmotic gradient that inhibits the reabsorption of Na+ and water in the proximal tubule. (minor)
(2) Decreases medullary tonicity (in general they interfere with fluid/electrolyte movements in the loop of henle)

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9
Q

What are the effects of mannitol?

A

(1) it expands the ECF as it draws water out of cells
(2) it increases urine flow
(3) increases blood pressure.

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10
Q

How is mannitol used?

A

(1) to treat dialysis disequilibrium syndrome

(2) to decrease intracranial and intraoccular pressure.

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11
Q

What adverse effects are associated with mannitol?

A

Volume overload. Contraindicated in cardiac failure.

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12
Q

Name the loop diuretics?

A

(1) furosemide
(2) bumetanide
(3) torsemide

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13
Q

What is the MOA of the loop diuretics?

A

(1) they inhibit the Na/K/2Cl co transporter in the TALH.
(2) stimulate the synthesis of prostaglandins
(3) They help maintain GFR (by increasing renin release, increasing renal blood flow and they inhibit the ability of the macula densa to sense NaCl.

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14
Q

What are the effects of loop diuretics?

A

(1) they mobilize most NaCl for excretion
(2) prevent kidneys from concentrating urine
(3) they increase the urinary loss of K, H, Ca, and Mg
(4) Copious diuresis (impaired ability to concentrate urine)

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15
Q

What are the uses for loop diruetics (furosemide)?

A

(1) edema (cardiac, renal, or hapatic in origin)(oral)(For pulmonary give IV)
(2) Hypercalcemia
(3) protect against renal failure (protect GFR)
(4) Wash out toxins by increasing urine flow.
(5) anti-hypertensive

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16
Q

What are the adverse effects of loop diuretics?

A

(1) They can cause fluid/electrolyte imbalances (Hypokalemia, pH)
(2) They are OTOTOXIC
(3) increased BUN
(4) hyperglycemia
(5) hyperuricemia
(6) inflammation of the SALIVARY GLANDS

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17
Q

What is unique about furosemide?

A

(1) it has a high margin of safty
(2) it dilates veins possibly decreasing cardiac load
(3) Is secreted by organic acid transporter
(4) extensively protein bound (65% excreted in the urine)

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18
Q

How is furosemide administered?

A

Oral, IV or IM

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19
Q

What is unique about bumetanide?

A

Bumetanide is used with warfarin and is more potent than furosemide

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20
Q

What is unique about torsemide?

A

torsemide is a vasodilator (lowers BP) and has a long half life

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21
Q

List the Thiazide diuretics?

A

(1) Hydrochlorothiazide
(2) Chlorthalidone
(3) Quinethazone
(4) Metolazone (class II) More potent
(5) Indapamide (class II) More potent

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22
Q

What is the MOA for the thiazide diuretics?

A

They inhibit the NaCl co-transporter in the early DCT.

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23
Q

What are the effects of Thiazide diuretics?

A

(1) They cause moderate excretion of Na, K, Mg, and Cl
(2) They increase the urine flow rate
(3) Reduce the GFR
(4) They increase acid secretion in the CD
(5) They decrease the excretion of Ca. (hypercalcemia)

24
Q

What are thiazide diuretics used for?

A

(1) To reduce edema (CHF, Cirrhosis, Nephrotic)
(2) to treat hypercalciuria
(3) To reduce BP
(4) to treat nephrogenic diabetes insipidus (by increasing water reabsorption in PCT)

25
Q

What are the adverse effects associated with thiazide diuretics?

A

(1) Depletion phenomenon: (hypokalemia, Hypomagnesemia, Hypochloremic alkalosis, dilutional hyponatremia.
(2) Retentions phenomena: (hyperuricemia, hypercalceimia,
(3) metabolic changes: (hyperglycemia, Hyperlipidemia, increased renin/aldosterone)
(4) Hypersensitivities: (fever, rash, purpura, pancreatitis, sialadenitis, withdrawl edema.

26
Q

What is unique about hydrochlorothiazide?

A

(1) It is a class I teratogen
(2) It must be used with a GFR above 50
(3) must be secreted into the lumen.

27
Q

What is unique about metolazone?

A

(1) class II: meto. and Quin.

(2) Use with GFR 30-50

28
Q

List the aldosterone antagonists?

A

(1) spirinolactone (aldactone)

2) Eplenrone (inspra

29
Q

What is the MOA of the adlosterone inhibitors?

A

They bind and block aldosterone receptors in the cytoplasm from being expressed on the cell surface. This leads to a decrease in Na+ reabsorption in the CD and the inability to concentrate the urine. They also decrease K+ secretion.

30
Q

What is unique about the use of spirinolactone and its effects?

A

Spirinolactone causes hyperkalemia and is usually used with hydrochlorothiazide. It is HIGHLY METABOLIZED. Can cause gynecomastia, hirsutism, and uterine bleeding. Spirinolactone is the drug of choice for cirrhosis.

31
Q

What is unique about eplenerone?

A

eplenerone has less affinity for the androgen receptor and therefore has less severe side effects.

32
Q

List the K+ sparing diuretics?

A

(1) triamterene (dyrenium)

2) Amiloride (Midamor

33
Q

What is the MOA for the K+ sparing diuretics?

A

They bind and inhibit the Na+ channels in the principal cells of the late DCT and CD.

34
Q

What are the effects of the K+ sparing diuretics?

A

(1) they increase the excretion of Na+

(2) They inhibit the secretion of K+ and H+

35
Q

How are the K+ sparing diuretics used?

A

They are usually combined with hydrochlorothiazide for increased effect.

36
Q

What are some adverse effects associated with K+ sparing diuretics?

A

(1) Hyperkalemia

(2) Megaloblastic anemia in liver cirrhosis patients

37
Q

What kind of drug is Nesiritide?

A

Nesiritide is a synthetic ANP (atrial-natriuretic peptide)

38
Q

What is the MOA of nesiritide?

A

Nesiritide binds the natriuretic peptide receptor and activates guanylyl cyclase –> this creates an increase in cGMP –> increased cGMP then inactivates Na+ transporters and NKA transporters in the tubules.

39
Q

What are the effects of nesiritide?

A

(1) increases Na secretion
(2) inhibits RAAS
(3) decreases BP (important in decreasing intra-atrial pressure)

40
Q

What class of drugs do arginine vasopressin, and desmopressin (DDAVP) belong to?

A

the artificial ADH class (pressins)

41
Q

What is the MOA of arginine vasopressin?

A

arginine vasopressin is a V1 and V2 agonist.

42
Q

What are the effects of arginine vasopressin?

A

(1) V1 increases constriction (mobilizes Ca)
(2) V2 increases water reabsorption

Can be used to decrease mucosal bleeding and counteract post operative ileus.

43
Q

What is the MOA of desmopressin?

A

Desmopressin is a V2 agonist.

44
Q

What is the effect of desmopressin?

A

Desmopressin increases water reabsorption

45
Q

What are the uses for desmopressin ?

A

(1) bed wetting kids
(2) central diabetes insipidus
(3) some bleeding disorders (vWF disease to release extra vWF from the wiebel-palade bodies)

46
Q

What is unique about arginine vasopressin?

A

It is synthesized in the paraventricular and supraoptic nuclei of the hypothalamus

47
Q

Where are the V1 and V2 receptors found?

A

(1) V1 is found in smooth muscle cells everywhere.

(2) V2 is found in renal CD principal cells and is found everywhere.

48
Q

To which class of drugs to convaptan and tolvaptan belong?

A

They are vaptans (V2 antagonists)

49
Q

What is the MOA of the vaptans?

A

They inhibit the V2 receptor and thus inhibit the activity of ADH.

50
Q

For what are the Vaptans used?

A

They are used as diuretics primarily in SIADH along with water restriction. Demeclocylcin is an antibiotic that also inhibits V2 ADH receptors.

51
Q

What is unique about the way vaptans are used?

A

THEY ARE ONLY USED IN THE HOSPITAL when a patient is hyponatriemic

52
Q

How are the vaptans metabolized?

A

They are CYP3 metabolized.

53
Q

How do loop diuretics increase renin release?

A

(1) they inhibit the macula densa
(2) activate the sympathetic nervous system
(3) Stimulate intrarenal baroreceptors

54
Q

What drug interactions are associated with furosemide?

A

(1) interactions with Li
(2) Indomethacin
(3) probenecid
(4) warfarin

55
Q

What are some drugs that cause SIADH?

A

(1) psychotropics
(2) Sulfonylureas
(3) Vinca alkaloids

56
Q

What are some adverse effects associated with the vaptans?

A

(1) hyperglycemia
(2) GI disturbance
(3) Clotting problems.

Renal Module (17 decks)

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