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Drug Action I > Block 2 - Diuretic Med Chem > Flashcards

Block 2 - Diuretic Med Chem Flashcards

(48 cards)

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1
Q

Label the corresponding diuretic and how it effects the the nephron pathology

A
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2
Q

What is the MOA of osmotic diuretics?

A

Allows water to be retained in the tubules preventing it from being reabsorbed into systemic circulation

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3
Q

What is the predominant osmotic diuretic? When is it used?

A

Mannitol (Osmitrol) is used is the hospital for trauma (head) patients usually with CNS fluid retention

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4
Q

Example of osmotic diuretics?

A

Mannitol
Sorbital
Glycerin
Isosorbide

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5
Q

MOA of carbonic anhydrase inhibitors?

A

Causes diuresis by inhibiting H+ formation -> less Na+ and H2O reabsorption

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6
Q

What are the disadvantages of using carbonic anhydrase?

A

Being the oldest diuretic class, 99% of the drug must be inhibited to be effective
Therefore, not considered first-line

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7
Q

How much of sodium is filtered by carbonic anhydrase?

A

2-5%

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8
Q

Example of carbonic anhydrase?

A

Acetazolamide (Diamox)

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9
Q

What is Acetazolamide’s indication?

A

Diamox is used to treat glaucoma by reducing the amount of aqueous humor that causes the pressure

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10
Q

How does Diamox’s structure contribute to its bioavailability and excretion?

A

Sulfonamide has a negative charge, however, lipophilic structure gives it >90% PO F and excreted unchanged

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11
Q

What is the outcome of chronic Acetazolamide use?

A

Prolonged use causes urine to become alkaline -> acidosis in blood and use is very limited

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12
Q

What functional group became the basis of popular diuretic structures?

A

Sulfonamide

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13
Q

How does thiazide structures differ from carbonic anyhydrase?

A

Contain disulfonamide analogues

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14
Q

What increases thiazide activity?

A

Chloro and amino substitutions causes acetylation of amino groups causing ring closure

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15
Q

What is the MOA of benzothiadiazines?

A

Inhibits Na+/Cl- transporter in the DCT -> Inhibits Na+ reabsorption (saluretic)

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16
Q

What is the main diurectics indicated for HTN?

A

Thiazides

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17
Q

Describe the thiazides SAR?

A
  1. Benzothiadiazide-1,1-dioxide is essential
  2. Sulfonamide @C7 is essential for activity
  3. EWG @C6 greatly enhances activity (EDG reduces)
  4. 3,4-dihydro derivative enhance activity 10-fold
  5. Lipophilic group @C3 increases DOA
  6. Alkyl substitution @N2
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18
Q

Chlorothiazide? F? t1/2? DOA? Metabolism?

A
  1. Diuril is least potent and simplest thiazide
  2. Low F
  3. 1-2hrs
  4. 6-12hrs
  5. Unchanged urinary excretion
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19
Q

Hydrochlorothiazide? F? t1/2? DOA? Metabolism?

A
  1. HydroDiuril has medium potency
  2. High F
  3. 6-15hrs
  4. 6-12 hrs
  5. Unchanged urinary excretion

Most popular diuretic for HTN

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20
Q

Trichloromethiazide? DOA? Metabolism?

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A

Diurese is one of the most potent thiazide
DOA: 24 hrs
Metabolism: Unchanged urinary excretion

21
Q

Methyclothiazide? DOA? Metabolism?

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A

Enduron, Aquatensen is one of the most potent thiazide
DOA: 24 hrs
Metabolism: Unchanged urinary excretion

22
Q

Polythiazide? DOA? Metabolism?

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A

Renese is one of the most potent thiazide
DOA: 24-48 hrs
Metabolism: Unchanged urinary excretion

23
Q

Hydroflumethiazide? F? t1/2? DOA? Metabolism?

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A

Saluron has a low potency
t1/2: 17 hrs
DOA: 18-24 hr
Metabolism: unchanged urinary excretion

24
Q

What is the most dangerous ADR of diuretics?

25
Bendroflumethizide? F? T1/2? DOA? Metabolism?
Naturein is a potent thiazide F: 90% due to lipophilicity t1/2: 8-9 hrs DOA: 6-12 hrs Metabolism: unchanged urinary excretion
26
ADRS of thiazide? How do you prevent them?
1. Hypokalemia, thiazides are usually administered with K+ supplements 2. Hypochloremia, hypoatremia, hypercalcemia, hyperuricemia, supplements and gout meds are given
27
Long term use leads to what kind of ADRs?
glucose intolerance and/or increased blood lipids
28
Characteristics of loop diuretics?
1. High-ceiling (more potent=more diuresis) 2. Sulfonamide derivatives
29
Describe loops site of action? Onset? DOA?
1. thick ascending limb of the loop of Henle 2. Quick onset 3. Short DOA
30
Loop diuretic MOA?
1. Diuresis effect by inhibiting Na+/K+/2Cl- 2. Prevents ion from being reabsorbed in ascending portion that doesn't allow water to be reabsorbed -> more diuresis
31
ADRs of loops?
Hypokalemia and hypocalcemia
32
Furosemide? Onset? DOA? Excretion?
Lasix is more acidic than thiazide (carboxylate), 8-10 fold more potent than thiazides Onset: 30 min DOA: 6-8 hr Metabolism: Primarily excreted unchanged
33
What is Lasix primarily used for?
Furosemide: CHF, renal/hepatic edema, other edemas not primarily for HTN
34
How does bumetanide differ from lasix structurally? How does this benefit?
1. 4-Cl has been replaced by 4-phenoxy 2. 6 amino has been moved to 5-amino Bumedex's structural changes leads to 50x more potency than lasix
35
What is the indications for torsemide? Onset? DOA?
Demadex is indicated for CHF and some HTN 1. Sulfonamide is changed to sulfonylurea Onset: 1-2 hrs DOA: 6 hrs
36
How does ethacrynic acid differ from other loop diuretics?
1. Edecrin is a phenoxyacetic acid derivative 2. Sulfhydryl enzymes allows solute reabsorption, however Edecrin (olefin) covalently binds to enzymes disengaging it
37
What is the MOAs of Edecrin?
1. Sulfhydryl inhibitor 2. Olefin reduction -> diuresis
38
What is potassium sparing diuretics? MOA?
Aldosterone antagonist that inhibits it from promoting K+ excretion and Na+/Cl- reabsorption
39
What are the dangers of diuretics other than K+-sparing?
K+ wasting leading to hypokalemia which can be fatal
40
What is spironolactone's indication? Binding? ADR?
Aldactone Edema from cirrhosis given concurrently with K+ wasters Produrg that binds to aldosterone receptors once activated
41
ADRs of Aldactone?
Hyperkalemia Decreased libido and impotence
42
How is ALDACTONE metabolized?
Prodrug (Aldactone) -> Canrenone
42
What is eplerenone? Indication? t1/2? Metabolism?
HTN and CHF t1/2: 5-6 hrs Its lipophilicity requires more metabolism therefore, it undergoes extensive metabolized to inactive metabolites
42
What are other K+ sparing diuretics? ADRs?
1. Epithelial sodium channel inhibitors 2. Non-aldosterone based drugs
43
Triamterine? Class? t1/2? Metabolism?
Dyrenium, Dyazide Class: triame, Blocks Na/K channel t1/2: 2h Metabolism: 4-hydroxytriamterine (inactive)
43
Amiloride? Class? t1/2? Metabolism? Structure?
Midamor Class: diamine guanidine, block Na/K channel t1/2: 6-10 h Metabolism: excreted unchanged
44
What are the general MOAs of K+ sparing diuretics? ADRs?
Blocks Na+ reabsorption Hyponatremia and hypocalcemia
45
What is the epithelial sodium channel MOA?
No K+ is allowed to be excreted

Drug Action I (32 decks)

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