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Medicinal 3 > Diuretics > Flashcards

Diuretics Flashcards

1
Q

What are diuretics?

A

A chemical agent that increases the rate of urine

or
any agent that will inhibit the tubular absorption of sodium

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2
Q

What is the primary MOA of diuretics

A

Direct Inhibition of sodium transport at one or more of the four major anatomical sites of the nephron where sodium reabsorption occurs

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3
Q

What are the major applications of diuretics agents

A
  1. treatment of hypertension
  2. mobilization of edematous fluid (HF, CKD, Hepatic diseases)
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4
Q

How many nephrons does the kidney contain

A

1 million nephron

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5
Q

What is each nephron made of

A

glomerulus and the renal tubule

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6
Q

What is a glomerulus

A

a ball of capillary loops surrounded by bowmans capsule- blood flow in provides filtrates without molecules larger than 4nm in diameter

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7
Q

T/F:
Diuretics that wonk on the earlier nephron have greatest effect since they are able to block more sodium and chloride reabsorption

A

True

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8
Q

Where do the carbonic anhydrase inhibitors work

A

Proximal tubules

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9
Q

Where do loop diuretics work

A

In the loop of henle

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10
Q

Where do thiazides work

A

Between the thick ascending loop and the distal convuluted tubule

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11
Q

Where do potassium sparring diuretics work

A

distal convuluted tubule

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12
Q

Does the collecting tubule have good diuretic activity

A

No, least efficacious diuretic

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13
Q

What is the primary indication of acetazolamide

A

glaucoma
mountain sickness (cns effects)

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14
Q

does acetazolamide trigger metabolic acidosis or metabolic alkalosis

A

metabolic acidosis AND
respiratory alkalosis

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15
Q

Is acetazolamide used as a diuretic nowadays

A

No

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16
Q

What is the recent approval of acetazolamide

A

epilepsy

one of epilepsy triggers is the increase pressure in the cns due to increase fluid production
that is how acetazolamide is used in epilepsy

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17
Q

What does acetazolamide prevent the production of what

A

aquous humor

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18
Q

the body recycles what into carbonic acid

A

CO2 + H2O <-> H2CO3 (CARBONIC ACID)

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19
Q

CO2 hydration occurs in …?

A

Kidney
co2 +h2o -> h2co3

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20
Q

CO2 dehydration occurs in

A

Lungs
H2CO3 -> CO2 + H2O

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21
Q

the function of carbon anhydrase can differ depending on

A
  1. location of enzyme
  2. PH
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22
Q

What are the SE of acetazolamide

A

respiratory alkalosis
metabolic acidosis
renal stones

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23
Q

We advice patients who take diuretics to drink more water, why?

A
  1. some drugs are insoluble at urine pH -> precipitation -> stones
  2. some basic drugs can increase pH of urine -> ppt.
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24
Q

What are loop diuretics called

A

High ceiling diuretics

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25
Q

Loop diuretics causes ____ loss? and decrase of what in the blood?

A

Na+ loss (diuretic effect)
and decrease K+ in the blood -> hypokalemia

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26
Q

Do all diuretics cause hypokalemia

A

All except, potassium sparring diuretics

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27
Q

What is the MOA of loop diuretics

A

inhibits the na+/k+/2cl- carrier system primarily in the loop of henle

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28
Q

Mention 3 loop diuretics

A
  1. Bumetanide
  2. Furosemide
  3. Etharcynic acid
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29
Q

Is bumetanide soluble in urine

A

YES
completely excreted in urine

30
Q

What are the uses of bumetanide?

A
  1. edema
  2. HF
  3. hypercalcemia
  4. hyperkalemia
31
Q

What are the SE of bumetanide, furosemide

A
  1. Ototoxicity
    REVERSIBLE
  2. hyperuricimia
  3. hypokalemia
32
Q

does furosemide have a longer action duration than bumetaminide?

A

Yes due to the Cl- addition next to the sulfomyl group

33
Q

Does the chemical structure of ethacrynic acid differ than other loop diuretics?

A

Yes
but it acts on the same pump (that is why its classified in the loop diuretics section of diuretics)

34
Q

Which is more dangerous, furosemide or ethacrynic acid?

A

Ethacrynic acid is more dangerous and casuses more ototoxicity

and causes GI hemmorage

35
Q

Does ethacrynic acid have a shorter or longer activity than other loop diuretics

A

longer , because it has 2 clorines

36
Q

Is ethacrynic acid soluble in urine

37
Q

Does ethacrynic acid contain sulfur?

A

No, perfect for pts who need diuretics and have a sulfur allergy

38
Q

What are thiazides called

A

low ceiling diuretics

39
Q

Where do thiazide and thiazide look diuretics work

A

dital convoluted tubule on NA+/CL- pump

40
Q

Is there a limited Na+ absorption in the distal convoluted tubule

A

Yes
only 5-8% of the filtered load of sodium is reabsorbed

41
Q

in thiazide/ thiazide like diuretics which placement of sulfomyl group is preequisite for diuretic activity

A

Sulfomyl at G7 is ESSENTIAL

42
Q

in thiazide/ thiazide like diuretics , the sulfomyl at group 1 is essential

A

Yes, but if we replace it with any other isostere -> less activity

43
Q

In thiazide like diuretics, can we substitute g 4,5,8?

A

NO they should remain free

IF substituted -> diminished activity

44
Q

In thiazide like diuretics, can we substitute g 6

A

Yes but only with Cl-, Br-, Cf3-, NO2-

45
Q

In thiazide like diuretics, the double bond between G3-G4

A

It is better to remove the double bond for better diuretic activity
removal of = -> inc in potency 3-10 times

46
Q

In thiazide like diuretics, the NH2 in group 2, can i substitute it

A

only with small alkyl group CH3 (but the activity will be reduced)

47
Q

In thiazide like diuretics, the C in G3 can i add R to it

A

Yes
the more i add lipophilic group the duration increases

48
Q

Are thiazide diuretics well absorbed

49
Q

When is the onset of action of thiazide diuretics

A

1-2 hours
tmax 3-6 hr

50
Q

Are thiazide diuretics protein bound

51
Q

What are the SE of thiazide diuretics

A
  1. hypersensitivity reaction (sulfomyl)
  2. hypokalemia
  3. hypercalcemia
  4. hyperuricemia
52
Q

Mention 3 thiazide diuretics

A
  1. chlorothiazide
  2. hydrochlorothiazide
  3. Indapamide
53
Q

What is the MOA of chlorthiazide

A

thiazide diuretic (low ceiling)
Na+/C;- pump at distal tubule

54
Q

Theraputic uses of chlorthiazide

55
Q

Side effects of chlorthiazide

A

Hypokalcemia
hyperuricemia
hypercalcemia
hypergylcemia
hyperlipidemia

56
Q

Is there a double bond in hydrochlorothiazide

57
Q

Which is more potent
chlorthiazide or hydrochlorothiazide

A

Hydrochlorothiazide

58
Q

Is indapamide a thiazide diuretic

A

No, but since it works in the same place, it was classified under it

59
Q

Does indapamide have a short or long duration of action

A

Longer than other thiazides

60
Q

Potassium sparring diuretics work on …?

A

Aldosterone

61
Q

Mention potassium sparring diuretics

A
  1. spiranolactone
  2. eplerenone
  3. Triamterene
  4. amiloride
62
Q

Spiranolactine are …… antagonists

A

Aldosterone antagonist

63
Q

What is spiranolactone a derivative of

A

Steroid derivative

64
Q

What are the SE of spiranolactone

A

Gastric upset -> ulcers
gynecomastia
Irregular menstruation

65
Q

What is contraindicated with spiranolactone and other potassium sparring diuretics

A

any drugs that could cause hyperkalemia like ACEi and ARBs

66
Q

What is the mechanism of action of eplerenone

A

K-sparring diuretic
aldosterone antagonist

67
Q

Does eplerenone have endocrine activity

A

No, less endocrine activity

68
Q

The epoxide in eplerenone is it stable or not

69
Q

What is the MOA of amiloride

A

K-sparring diuretic
Na+/K+ pump at COLLECTING TUBULE

70
Q

What is the MOA of triamterene

A

K-sparring diuretic
Na+/K+ pump at COLLECTING tubule

71
Q

What are the side effects of triamterene

A

Leg cramps (electrolyte imbalances)

Medicinal 3 (6 decks)

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