Antidiuretic
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this is a almost complete presentation on pharmacological as well as therapeutic aspect of anti-diuretic drugs..
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Antidiuretic
- 2. Presentation Anti Diuretic Agents Presented by: Md. Masum Billal Pharm-d 3rd year
- 3. Content Of Presentation • Introduction. • Synthesis , Release and Function of ADH. • Classification of Anti-diuretic agents. • Pharmacodynamics , Pharmacokinetics ,Indication , Contraindication , Adverse effect , Side effect and Drug interaction of anti-diuretic agonist. • Pharmacodynamics and Pharmacokinetics of anti-diuretic antagonist. • Key point • Conclusion .
- 4. Introduction Anti-diuretics agents: anti-diuretics or anti-aquatic are drugs that reduce urine volume particularly in diabetes insipidus by inhibiting water excretion without affecting salt excretion.
- 5. Synthesis Release and Function of ADH Decreased blood volume Low blood pressure Informed Mid brain Informed hypothalamus for stimulating SON and PVN ADH with neurophysin Release of ADH Concentration ADH leads to Vasoconstriction Stimulate V2 receptor and reabsorption of water
- 6. Classification of anti-diuretics agents Antidiuretics Antidiuretics hormone and its analogues • Vasopressin • Desmopressin • Lypressin • Terlipressin Natriuretic • Thiazide • Amiloride Miscellaneous • Carbamazepine • Chlorpropamide • Indomethacin
- 7. Bind with V2 receptor on nephron ↓ Stimulate Gs subunits of GPCR receptor ↓ Activate adenylyl cyclase activity ↓ Increased Camp level ↓ Increased protein kinase-A activity ↓ Stimulate aquaporin-2 vesicle ↓ Set the aquaporin-2 into luminal site ↓ Permit to water reabsorption ↓ Maintain blood osmolality Bind with V1 receptor on smooth muscle ↓ Stimulate Gq subunits of GPCR receptor ↓ Activate phospholipase-C activity which breakdowns PIP2 into two products IP3 ↓ Release endoplasmic ca++ ↓ Ca-calmodulin complex form ↓ Activate cam protein kinase ↓ Induce action potential ↓ Leads to vasoconstriction DAG ↓ Increased protein kinase-C activity ↓ Activate phosphate dependent ion channel ↓ Influx of ca++ ↓ Induce action potential ↓ Leads to vasoconstriction Pharmacodynamics of vasopressin Mechanism of action Vasopressin
- 8. . Pharmacokinetics of vasopressin Absorption Metabolism: Elimination: Half life: 10-20 min (parenteral) Excretion: urine (5-10%) Metabolized in liver and kidney Rapidly removed from plasma Bioavailability: destroyed by trypsin in GI tract. Must be administered parenterally or intranasally
- 9. Vasopressin • Diabetes insipidus • Abdominal distension • Abdominal roentgenography • Gastrointestinal haemorrhage • Vasodilatory shock • Prolonged exposure lead to Vascular hypertrophy • Abdominal cramp • Diarrhoea • Tremor • vertigo • hypersensitivity indication contraindication Adverse effect Side effect • Allergic reaction • Angina • Vertigo • Nausea 1. Amitriptyline, amoxapin, carbamazine increases effect of vasopressin by pharmacodynamics synergism. 2. Ethanol , heparin decreases the effect of vasopressin by pharmacodynamics antagonism. Drug interaction
- 10. Bind with V2 receptor on nephron ↓ Stimulate Gs subunits of GPCR receptor ↓ Activate adenylyl cyclase activity ↓ Increased Camp level ↓ Increased protein kinase-A activity ↓ Stimulate aquaporin-2 vesicle ↓ Set the aquaporin-2 into luminal site ↓ Permit to water reabsorption ↓ Maintain blood osmolality Pharmacodynamics of Desmopressin Mechanism of action Desmopressin
- 11. Pharmacokinetics of Desmopressin Absorption Elimination: unknown Bioavailability: 3.3-4.1% (stimate); 3.5% (nasal) Urine : 52% Metabolism:
- 12. Desmopressin • Diabetes insipidus • Bedwetting in children and nocturia in adults. • Renal concentration test • Haemophilia , von willebrands disease • Dry Mouth • Transient Headache • Flushing • Mometasone intranasal indication contraindication Adverse effect Side effect • Belching • Abdominal cramps • pallor • Nausea 1. chlorpropamide, benzphetamine, carbamazine, dobutamine, dopamine increases effect of vasopressin by pharmacodynamics synergism. Drug interaction
- 13. Bind with V1 receptor on smooth muscle ↓ Stimulate Gq subunits of GPCR receptor ↓ Activate phospholipase-C activity which breakdowns PIP2 into two products IP3 ↓ Release endoplasmic ca++ ↓ Ca-calmodulin complex form ↓ Activate cam protein kinase ↓ Induce action potential ↓ Leads to vasoconstriction DAG ↓ Increased protein kinase-C activity ↓ Activate phosphate dependent ion channel ↓ Influx of ca++ ↓ Induce action potential ↓ Leads to vasoconstriction Pharmacodynamics of lypressin Mechanism of action lypressin • It is 8-lysin vasopressin. • It is used in place of 8-arginine vasopressin (AVP) mostly for V1 receptor mediated actions.
- 14. Bind with V1 receptor on smooth muscle ↓ Stimulate Gq subunits of GPCR receptor ↓ Activate phospholipase-C activity which breakdowns PIP2 into two products IP3 ↓ Release endoplasmic ca++ ↓ Ca-calmodulin complex form ↓ Activate cam protein kinase ↓ Induce action potential ↓ Leads to vasoconstriction DAG ↓ Increased protein kinase-C activity ↓ Activate phosphate dependent ion channel ↓ Influx of ca++ ↓ Induce action potential ↓ Leads to vasoconstriction Pharmacodynamics of Terlipressin Mechanism of action Terlipressin • It is synthetic prodrug of vasopressin • It is used for bleeding oesophageal varices • It appears to produce less severe adverse effects than lypressin.
- 15. Pharmacodynamics of Thiazide Mechanism of action Thiazide • It is paradoxically exert an antidiuretic effect in DI and by this treatment K+ supplement are needed. • It reduces urine volume in both pituitary origin as well as renal DI • But the mechanism of action is not well understood. The possible explanation is: Induce sustained electrolyte depletion ↓ That glomerular filtrate is more completely reabsorbed iso- osmotically in PT ↓ Smaller volume of dilute urine in CD ↓ Leads to management of DI Reduce G.F.R rate ↓ Reduce less water excretion ↓ Minimize the condition of DI
- 16. Pharmacodynamics of Amiloride Mechanism of action Amiloride • It is the drug of choice for lithium induced nephrogenic DI. Blocks the entry of lithium along with blocking entry of Na+ ↓ Reduced the damage of luminal cell of nephron ↓ Minimize the condition of nephrogenic DI
- 17. Pharmacodynamics of Indomethacin Mechanism of action Indomethacin • It is used combined with a thiazide or amiloride in nephrogenic DI Reduce renal PG synthesis ↓ Reduce polyuria in renal DI
- 18. Pharmacodynamics of Chlorpropamide Mechanism of action Chlorpropamide • It is a long acting sulfonyl urea oral hypoglycaemic agents • It found to reduce urine volume in DI of pituitary origin but not in renal DI.
- 19. Pharmacodynamics of Carbamazepine Mechanism of action Carbamazepine • It is an antiepileptic agents • It reduces urine volume in DI of pituitary origin but mechanism of action is not clear. • Higher doses are needed , adverse effect are marked . • It is of little value in treatment of DI
- 20. Vasopressin antagonists Vasopressin antagonist are mainly: 1. Tolvaptan 2. Mozavaptan 3. Conivaptan 1. Tolvaptan • It is orally active nonpeptide selective V2 receptor antagonist that is used to recently to treat hyponatremia due to CHF Cirrhosis of liver Syndrome of inappropriate ADH secretion tolvaptan ↓ Increases free water clearance by kidney ↓ Lead to low plasma Na+ levels Mechanism of action • It is selective V2 antagonist 2. Mozavaptan • It is V1 and V2 antagonist 3. Conivaptan