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Conivaptan inhibits its own metabolism in the body, displaying non-linear pharmacokinetics. About 99% of conivaptan found is bound to human plasma proteins over the range of 10 ng/mL to 1000 ng/mL. The mean half-life of the drug is 5 hours and mean clearance is 15.2 L/hr. [2]
Tolvaptan, sold under the brand name Samsca among others, is an aquaretic drug that functions as a selective, competitive vasopressin receptor 2 (V 2) antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH).
The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors (V 1A, V 1B and V 2).These receptors have a variety of functions, with the V 1A and V 2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V 1A and V 1B receptors are expressed in the central nervous system.
Synthetic aquaretics are vasopressin receptor antagonists and include conivaptan, tolvaptan, demeclocycline, and mozavaptan (OPC-31260), as well as lithium. Conivaptan hydrochloride and tolvaptan have been approved by the FDA for treating syndrome of inappropriate antidiuretic hormone. [4] [5] Mozavaptan is approved in Japan. [citation needed]
Vasopressin receptor antagonists include the new class of "vaptan drugs" such as conivaptan, tolvaptan, mozavaptan ... Commons Attribution-ShareAlike 4.0 ...
Fischer is going to an opioid addiction treatment clinic. In Fort Collins, a doctor will meet with him for a half hour and write him a prescription for a month’s supply of buprenorphine, a medication that blunts his cravings for heroin and other short-acting opioids. Fischer has spent a dozen or so years dealing with his addiction.
The vasopressin receptor 2 blocker tolvaptan may also be used. [2] The presence of cerebral edema , or other moderate to severe symptoms, may necessitate intravenous hypertonic saline administration with close monitoring of the serum sodium levels to avoid overcorrection.
By Friday night, three days after leaving rehab, Patrick’s willpower showed signs of strain. He came home late, hours after his meeting ended. The next morning, while Anne was out jogging, Patrick left the house, telling his father that he’d be back later. He hadn’t returned by that evening.