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Presented by Group 4
Drugs That Act on the
Kidney
_Anum Sajid…
Introduction
 Drugs that act on the kidney have important
applications in renal, cardiovascular, and
endocrine disorders. These disorders mainly
involve sodium and water homeostasis.

CARBONIC
ANHYDRASE
INHIBITORS
Carbonic
Anhydrase
• Carbonic anhydrase enzymes are found in the:
• Proximal convoluted tubules (PCTs) of
the kidneys: involved in HCO3
– reabsorption
• Eyes: involved in aqueous humor production
• Glial cells in the brain: involved in CSF
production
 In PCT carbonic anhydrase catalyze:
Dehydration of H2CO3 to CO2 at the
luminal membrane.
Rehydration of CO2 to H2CO3 in the
cytoplasm.
Carbonic
Anhydrase
Inhibitor
 It is Sulphonamide derivative.
 Duration of action: 8-12hrs
 Well absorbed orally.
 Include:
Acetazolamide
Methazolamide
 Dorzolamide
Pharmacokinetics
Acetazolamide
• Readily absorbed
• Half-life: 2.5‒9 hours
• Not metabolized
Methazolamide
• Relatively
slower absorption
• Half-life: 14 hours
• Metabolizes slowly
within the GI tract
Mechanism of
Action
 Non-competitively and reversible inhibit
Carbonic Anhydrase in Proximal tube;
 Block resorption of bicarbonate ions; preventing
Na/H exchange.
• Inhibition of carbonic anhydrase:
• Keeps HCO3
– in the renal tubules.
• Prevents secretion of HCO3
– into the
aqueous humor in the eyes.
• Prevents secretion of HCO3
– into the CSF in
the brain.

Physiologic
effects
of CAIs
 Use of CAI’s results in:
• ↑ HCO3
– excretion leading to metabolic
acidosis.
• ↑ Na+ excretion → water follows Na+ →
diuresis.
• ↓ Intraocular pressure (IOP) due to ↓
aqueous humor production
• ↓ Intracranial pressure (ICP) due to ↓ CSF
production
Therapeutic
Uses
 Glaucoma—Dec. formation of
aqueous humor thereby lowering
the intraocular pressure.
 Prophylaxis and treatment of acute
Mountain sickness.
 To Alkalinize urine for UTIs.
 Periodic Paralysis
 Edema
Adverse
Reactions
 Acidosis
 Hypokalemia
 Drowsiness, paresthesia
 Abdominal discomfort,
 Hypersensitivity reactions.
 Bone marrow depression.
 Interfere with elimination of NH3 in urine.
 CONTRAINDICATED in Liver disease.
The End

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Drugs That Act on the Kidney.pptx

  • 1. Presented by Group 4 Drugs That Act on the Kidney _Anum Sajid…
  • 2. Introduction  Drugs that act on the kidney have important applications in renal, cardiovascular, and endocrine disorders. These disorders mainly involve sodium and water homeostasis.
  • 3.
  • 4.
  • 6. Carbonic Anhydrase • Carbonic anhydrase enzymes are found in the: • Proximal convoluted tubules (PCTs) of the kidneys: involved in HCO3 – reabsorption • Eyes: involved in aqueous humor production • Glial cells in the brain: involved in CSF production
  • 7.  In PCT carbonic anhydrase catalyze: Dehydration of H2CO3 to CO2 at the luminal membrane. Rehydration of CO2 to H2CO3 in the cytoplasm.
  • 8. Carbonic Anhydrase Inhibitor  It is Sulphonamide derivative.  Duration of action: 8-12hrs  Well absorbed orally.  Include: Acetazolamide Methazolamide  Dorzolamide
  • 9. Pharmacokinetics Acetazolamide • Readily absorbed • Half-life: 2.5‒9 hours • Not metabolized Methazolamide • Relatively slower absorption • Half-life: 14 hours • Metabolizes slowly within the GI tract
  • 10. Mechanism of Action  Non-competitively and reversible inhibit Carbonic Anhydrase in Proximal tube;  Block resorption of bicarbonate ions; preventing Na/H exchange.
  • 11. • Inhibition of carbonic anhydrase: • Keeps HCO3 – in the renal tubules. • Prevents secretion of HCO3 – into the aqueous humor in the eyes. • Prevents secretion of HCO3 – into the CSF in the brain.
  • 12.
  • 13. Physiologic effects of CAIs  Use of CAI’s results in: • ↑ HCO3 – excretion leading to metabolic acidosis. • ↑ Na+ excretion → water follows Na+ → diuresis. • ↓ Intraocular pressure (IOP) due to ↓ aqueous humor production • ↓ Intracranial pressure (ICP) due to ↓ CSF production
  • 14. Therapeutic Uses  Glaucoma—Dec. formation of aqueous humor thereby lowering the intraocular pressure.  Prophylaxis and treatment of acute Mountain sickness.  To Alkalinize urine for UTIs.  Periodic Paralysis  Edema
  • 15. Adverse Reactions  Acidosis  Hypokalemia  Drowsiness, paresthesia  Abdominal discomfort,  Hypersensitivity reactions.  Bone marrow depression.  Interfere with elimination of NH3 in urine.  CONTRAINDICATED in Liver disease.