True regarding Conivaptan is -
Ans. is 'a' i.e., Vasopressin Antagonist ADH (Vasopressin) receptors VtaV1b (also called V3) o Release of vWF & Factor VIIIo Blood vessels - vasoconstrictiono Anterior pitutary -from endotheliumo Visceral smooth muscle - contractionrelease of ACTH o Liver - glycogenolysis o Platelet - aggregation o V receptors are more sensitive to ADH than V, receptors.VAPTANSo A new class of medication, the "vaptan drugs", act by inhibiting the action of vasopressin on it receptors (VIA, V1B and V2) ?Vasopressin receptor antagonists.VIA receptor antagonisto As already explained, V1 A receptors are involved in vasoconstriction ? V1 A antagonist can be used when total peripheral resistance is increased, e.g. in CHF and hypertension.Example - RelcovaptanVI B receptor antagonisto VI B receptors are expressed in brain and pituitary gland ? VI B antagonist can be used as psychiatric drugs.Example - NelivaptanV2 receptor antagonistso V2 receptors are mainly responsible for increase water permeability in kidney ? V2 antagonists can be used when there is excessive ADH induced fluid retention as in SI ADH.Examples - Lixivaptan.satavaptan, mozavaptan, Tolvaptano Tolvaptan is currently the only oral V2 antagonist approved by the U.S. FDA.Non-selective (mixed V1A/V2)o Can be used in CHF (hypervolemic hyponatremia)Examples -Conivaptan
Vasopressin Antagonist
V2 selective action
Given orally
Used in the treatment of hypernatremia
Diuretic