Comprehensive Overview of Antidiuretics

 

 Antidiuretics

  • Content
    • List of Antidiuretic Drugs
    • Mechanism of Action
    • Adverse Effects
    • Therapeutic Uses of Vasopressin Analogues and Antagonists (including Desmopressin)

Introduction to Antidiuretics

  • Definition: Drugs that reduce urine output by increasing water reabsorption in the kidneys.
  • Key Hormone: Vasopressin (Antidiuretic Hormone, ADH)
    • Regulates water balance in the body.

List of Antidiuretic Drugs

  • Vasopressin Analogues:
    • Desmopressin (DDAVP)
    • Terlipressin
  • Vasopressin Antagonists:
    • Tolvaptan
    • Conivaptan

Mechanism of Action of Vasopressin Analogues

  • Vasopressin Receptors:
    • V1 Receptors: Found in vascular smooth muscle – cause vasoconstriction.
    • V2 Receptors: Found in renal collecting ducts – increase water reabsorption.
  • Desmopressin (DDAVP):
    • Selective for V2 receptors.
    • Promotes insertion of aquaporin-2 channels in collecting ducts.
    • Results in water reabsorption and concentrated urine.

Adverse Effects of Vasopressin Analogues

  • Common Side Effects:
    • Headache
    • Nausea
    • Flushing
  • Serious Side Effects:
    • Hyponatremia (water intoxication)
    • Seizures
    • Allergic reactions

Therapeutic Uses of Desmopressin

  • Clinical Indications:
    • Central Diabetes Insipidus
    • Nocturnal Enuresis (bedwetting)
    • Bleeding Disorders (e.g., von Willebrand Disease, mild Hemophilia A)

Vasopressin Antagonists: Mechanism of Action

  • Tolvaptan & Conivaptan:
    • Vasopressin Receptor Antagonists (V1 and V2 receptors).
    • Inhibit V2 receptor activity in the kidneys.
    • Promote excretion of free water (aquaresis) without affecting electrolyte balance.

Adverse Effects of Vasopressin Antagonists

  • Common Side Effects:
    • Dry mouth
    • Thirst
    • Polyuria
  • Serious Side Effects:
    • Hypernatremia
    • Liver toxicity (with Tolvaptan in long-term use)

Therapeutic Uses of Vasopressin Antagonists

  • Clinical Indications:
    • Syndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH)
    • Hyponatremia associated with heart failure or cirrhosis

Summary

  • Vasopressin Analogues:
    • Enhance water reabsorption through V2 receptors.
    • Used for Diabetes Insipidus, nocturnal enuresis, and certain bleeding disorders.
  • Desmopressin:
    • A key vasopressin analogue with selective V2 receptor action.
  • Vasopressin Antagonists:
    • Promote water excretion by inhibiting V2 receptors.
    • Treat SIADH and hyponatremia.

 Presentation for Antidiuretics

  

                                      END OF THE CHAPTER


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