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PHRM3041 > Diuretics > Flashcards

Diuretics Flashcards

1
Q

Is xanthine diuretics well used?

A

No, because low efficacy

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2
Q

Mercurial diuretics MOA

R-C-C-Hg

A

React with sulfhydryl groups in cells of ascending limb of henle, inhibiting Cl- transport
Very strong diuretic

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3
Q

Is mercurial diuretics still used?

A

No, because of Hg toxicity

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4
Q

Osmotic diuretics MOA

A

Osmotically impair proximal tubule fluid re-absorption, giving lower Na+ concentration in ascending limb of loop of henle and distal tubule
Decrease osmotic reabsorption in the loop of henle
IV ONLY

modest effect

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5
Q

Whatare Carbonic anhydrase inhibitors derived from?

A

From sulphonamide antibacterials

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6
Q

What is an example of carbonic anhydrase inhibitor?

A

acetazolamide

orally active, high effective

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7
Q

How come the CAI does not have sulphur cross sensitivities?

A

because of no arylamine

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8
Q

SAR of CAI

A

ACYL group larger than acetyl (CH3CO-) increases SE

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9
Q

MOA of CAI

A

At the proximal tubule, it decrease more than 80% of HCO3- reabsorption
small diuretic effect

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10
Q

Thiazides/ benzothiadiazides SAR

A

Weak acidic
H atoms at N2 is most acidic due to neighbouring sulfone (s=o) group (e- withdrawing effect)

Less acidic in sulfonamide Group at C7

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11
Q

What is the purpose of acidic protons?

A

formation of water soluble sodium salt for IV dosing

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12
Q

K+ sparing diuretic

aldosterone antagonist

A

structurally related to aldosterone (lactone group on C17) –> spiro nomenclature

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13
Q

What does non-aldosterone antagonist molecules have?

A

pteridines (two benzene rings with 4 N - triamterene)
or pyrazine (benezene ring with 2N - amiloride)
e.g. triamterene

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14
Q

Most modification in SAR of triamterene (non-aa)

A

decreases activity

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15
Q

Maintain activity of triamterene by

A

replace amine group with a lower alkylamine

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16
Q

Decrease acitivity by 50% by..

A

adding p-CH3 group to phenyl ring

17
Q

Making triamterene INACTIVE by…

A

adding p-OH group on phenyl ring

18
Q

MOA of triamterene

A

interefere with cationic exchange by blocking Na+ channels
actively transport into lumen of proximal tubule
act only in collecting duct
induce a modest increase in Na+ excretion with Cl-
little change in K+ excretion

19
Q

Examples of of High ceiling loop diuretics

A

ethacrynic acid, frusemide, bumetanide

20
Q

What does the ethacrynic acid mimic?

A

mimic mercurial diuretic

21
Q

Increase activity of ethacrynic acid by

A

adding electron withdrawing group (Cl-) ORTHO to unsaturated ketone

Most action in ORTHO and META

22
Q

Efficacy in relation to structure

A

Site of action predicts efficacy

multiple sites of action with one effect

23
Q

What is the therapeutic strategy for diuretic?

A

combination of diuretics - multi-modal site of action

24
Q

What is essential in thiazides

A

Electron withdrawing group at position 6

25
Q

Removing halogen on C6 on thiazide will

A

make the compound inactive

26
Q

Swapping C6 group to electron donating will

A

decrease potency

27
Q

Replacing one halogen to more electronegative halogen will have

A

no change in potency

but longer DOA

28
Q

Saturation of the thiadiazine ring to give 3,4-DIHYDROderivative will

A

increase activity by 10 fold

hydrochlorothiazide

29
Q

Substituting R3 with a lipophilic group (alkyl) in thiazides will

A

increase potency and DOA

30
Q

Making R2 and R3 with CH3 and halogenated alkyl group in thiazides will

A

increase potency by 10-20x

31
Q

Replacing benzene ring with pyridine (benzene ring with N) in thiaizide will

A

decrease activity

32
Q

Replacing or removing sulfonamide group at 7C will

A

give little or no activity

33
Q

Alkyl substitution on 2N wiill

A

decrease POLARITY,

increase DOA

34
Q

How is bumetanide different to other loop diuretics like ethacrynic acid and frusemide?

A

Bumetanide does not have Cl-

PHRM3041 (9 decks)

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