8/13/24, 11:17 AM
Med Chem Exam 3 Diuretics
Jeremiah
Terms in this set (27)
-HTN
-Edema
-Glaucoma
-Reducing CSF
Uses of Diuretics
-↑ excretion of water + sodium
-↑ urine outflow
-If a drug ↑ excretion of sodium and potassium, its a Saluretic
B: Glomerulus
C: Proximal Tubule. 65%
The Nephron D+E: Loop of Henle. 25%
F: Distal Tubule 8%
G: Collecting Duct. 2%
-Osmotic Diuretics
-Sulfonamide Diuretics
-Loop Diuretics
Types of Diuretics
-Potassium Sparing Diuretics:
^(Endocrine Antagonists)
^(Pteridine + Pyrazinoyl-Guanidine Derivatives)
-Water moves according to the osmotic gradient
-Osmotic diuretics ↑ osmolality of the urine and as such draw water out of the filtrate
(Na flows out)
Osmotic Diuretics
-Drugs are VERY POLAR
-Given IV to ↓ blood volume
USE: severe edema
Osmotic Diuretics: Urea (Carmal) Given IV
Med Chem Exam 3 Diuretics
VERY POLAR
1/7
, 8/13/24, 11:17 AM
USE: severe edema
Osmotic Diuretics: Mannitol (Osmitrol) Given IV
VERY POLAR
-Considered ACIDIC drugs
-Can cause allergic reactions because they initiate the formation of antibodies
Sulfonamide Diuretics -Liver does not like to metabolize sulfonamides...
METABOLIZED BY KIDNEY
-All are lipophilic: High plasma protein binding
(May lead to DDI with other drugs that have high PPB)
a: Carbonic Anhydrase Inhibitors
-no protons exchanged w/ Na in proximal tubules
-Need to be used at high dose to see an effect to inhibit 100% of the enzyme
b: Thiazides
-IV dosing= formulate as Na salt
-SOA: Distal tubules
-Cause Hypokalemia
c: Quinazolinone Derivatives (Thiazide similar)
-replace sulfonamido in thiazide ring w/ an amide
(non-classical bio-isosteric replacement)
Types of Sulfonamide Diuretics
d: Phthalimidine Derivatives
-COMPETES W/ Na + K AT CHANNELS
(in urine comoetes w/ Na)
-Much longer acting (sometimes once every 3 day dosing)
-Monosubstituted unfused ring
-Everything that applies to thiazides also applies to this group
-Often given w/ HCTZ to minimize effects on K+ levels
-LARGE + CHARGE
e: Indoline Derivatives
-Indole nucleus
-Single substituted aromatic ring w/ very lipophilic tail
--Everything that applies to thiazides also applies to this group
USE: Glaucoma
Sulfonamide: Carbonic Anhydrase Inhibitors:
Methazolamide (Neptazane)
USE: Glaucoma
Sulfonamide: Carbonic Anhydrase Inhibitors:
Acetazolamide (Diamox)
2/7
Med Chem Exam 3 Diuretics
Jeremiah
Terms in this set (27)
-HTN
-Edema
-Glaucoma
-Reducing CSF
Uses of Diuretics
-↑ excretion of water + sodium
-↑ urine outflow
-If a drug ↑ excretion of sodium and potassium, its a Saluretic
B: Glomerulus
C: Proximal Tubule. 65%
The Nephron D+E: Loop of Henle. 25%
F: Distal Tubule 8%
G: Collecting Duct. 2%
-Osmotic Diuretics
-Sulfonamide Diuretics
-Loop Diuretics
Types of Diuretics
-Potassium Sparing Diuretics:
^(Endocrine Antagonists)
^(Pteridine + Pyrazinoyl-Guanidine Derivatives)
-Water moves according to the osmotic gradient
-Osmotic diuretics ↑ osmolality of the urine and as such draw water out of the filtrate
(Na flows out)
Osmotic Diuretics
-Drugs are VERY POLAR
-Given IV to ↓ blood volume
USE: severe edema
Osmotic Diuretics: Urea (Carmal) Given IV
Med Chem Exam 3 Diuretics
VERY POLAR
1/7
, 8/13/24, 11:17 AM
USE: severe edema
Osmotic Diuretics: Mannitol (Osmitrol) Given IV
VERY POLAR
-Considered ACIDIC drugs
-Can cause allergic reactions because they initiate the formation of antibodies
Sulfonamide Diuretics -Liver does not like to metabolize sulfonamides...
METABOLIZED BY KIDNEY
-All are lipophilic: High plasma protein binding
(May lead to DDI with other drugs that have high PPB)
a: Carbonic Anhydrase Inhibitors
-no protons exchanged w/ Na in proximal tubules
-Need to be used at high dose to see an effect to inhibit 100% of the enzyme
b: Thiazides
-IV dosing= formulate as Na salt
-SOA: Distal tubules
-Cause Hypokalemia
c: Quinazolinone Derivatives (Thiazide similar)
-replace sulfonamido in thiazide ring w/ an amide
(non-classical bio-isosteric replacement)
Types of Sulfonamide Diuretics
d: Phthalimidine Derivatives
-COMPETES W/ Na + K AT CHANNELS
(in urine comoetes w/ Na)
-Much longer acting (sometimes once every 3 day dosing)
-Monosubstituted unfused ring
-Everything that applies to thiazides also applies to this group
-Often given w/ HCTZ to minimize effects on K+ levels
-LARGE + CHARGE
e: Indoline Derivatives
-Indole nucleus
-Single substituted aromatic ring w/ very lipophilic tail
--Everything that applies to thiazides also applies to this group
USE: Glaucoma
Sulfonamide: Carbonic Anhydrase Inhibitors:
Methazolamide (Neptazane)
USE: Glaucoma
Sulfonamide: Carbonic Anhydrase Inhibitors:
Acetazolamide (Diamox)
2/7
