Tolvaptan is a Medicine belongs to V2-receptor antagonist group whose information about Brand can be referenced from   Book : Martindale    Page : 270   Edition : 12  

  ►   Brandname : Samsca
  ►  Strength : Tablet with 15 mg.  Tablet with 30 mg. 

Reference of this Medicine for its Strength can be taken from   Book : Basic & Clinical pharmacology    Page : 270   Edition : 12  
A Route of administration in pharmacology and toxicology is the path by which a drug, fluid, poison, or other substance is taken into the body. Routes of administration are generally classified by the location at which the substance is applied. Common examples include oral and intravenous administration.

  ►  Route of administration : Oral
Reference :-   Book : Goodman    Page : 714   Edition : 12  

Dosing of Medicine differ in Adult & Pediatrics ↓

Adult Dose

S.No Ailment   Route   Dose Min   Dose Max   Unit   Dosage Form   Frequency   Additional Info
1 Euvolaemic and hypervolaemic hyponatraemia including that in heart failure, syndrome of inappropriate antidiuretic hormone secreation and cirrhosis. Oral 15 mg Tablet Given as single daily dose, which may be increased after at least 24 hours to 30 mg. the dose should be adjust up to a maximum of 60 mg once daily to achieve the desired serum sodium concentration.

Ref :-  Book : Martindale    Page : 2641   Edition : 37  



Pediatric Dose

S.No Ailment   Age Min   Age Max   Weight ( Kg ) Route   Dose Min   Dose Max   Unit   Dosage Form   Frequency  Additional Info  
1

Ref :- Book :    Page :    Edition :   
►  Side Effect : Hyperglycemia, Pyrexia, Cerebrovascular accident, Deep venous thrombosis, Intravascular coagulation and thrombosis, Intra cardiac thrombus, Ventricular fibrillation, Urethral hemorrhage, Vaginal hemorrhage, Pulmonary embolism, Respiratory failure, Diabetic ketoacidosis, Ischemic colitis, Increase in prothrombin time, Rhabdomyolysis, GI effects
Ref :-   Book : Goodman    Page : 717   Edition : 12.  

►  Drug Interaction : Drug interaction of Tolvaptan is with , Barbiturates , , ,  Clarithromycin , Ketoconazole , Indinavir, Itraconazole , Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Diltiazem , Erythromycin , Fluconazole , Verapamil , Rifampicin , Rifabutin , Rifapentine , Carbamazapine , Phenytoin , Cyclosporine , Phenytoin
Ref :-   Book : Martindale    Page : 2641   Edition : 37.  


  ►    Mechanism of Drug Drug Interaction :  As a substrate of the cytochrome P450 isoenzymes CYP3A4, concentrations of tolvaptan can be increased by CYP3A4 inhibitors.The use of tolvaptan with potent CYP3A4 inhibitors such as clarithromycin, ketoconazole, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin is contraindicated. Use of tolvaptan with moderate CYP3A4 inhibitors such as aprepitant, diltiazem, erythromycin, fluconazoleand verapamil should also be avoided on theoretical grounds that an increase in tolvaptan concentrations would also be expected. Rifampicin is a CYP3A4 inducer and significantly reduces tolvaptan concentrations. It is expected that other CYP3A4 inducers such as rifabutin, rifapentine, barbiturates, carbamazepine, phenytoin, St. john’s wort would have the same effect. Cyclosporin or grapefruit juice may increase tolvaptan concentrations. Hyperkalaemia has been reported in patients taking tolvaptan at same time as angiotensin II receptor antagonists, ACE inhibitors, or potassium sparing diuretics. Monitoring of potassium serum concentratios is recommended when any of these drugs are given with tolvaptan
Ref :-   Book : Martindale    Page : 2641   Edition : 37.  


►  Contraindication : Tolvaptan is contraindicated in hypovolaemic hyponatraemia, in patients who required a rapid increase in serum sodium concentratios, and in those who can not sense or who respond inappropriately to thirst., Rapid correction of sodium serum concentration with tolvaptan could increase the risk of osmotic demyelination syndrome. Tolvaptan is ineffective and therefore inappropriate to use in anuric patients., Tolvaptan should be used with caution in patients with cirrhosis because of an increased risk of gastrointestinal bleeding.
Ref :-   Book : Martindale    Page : 2641   Edition : 37.  
  ►  Mechanism of Action :   Selective vasopressin V2 -receptor antagonist.
Ref :-   Book : Martindale    Page : 2641   Edition : 37.  

Pathway of DIETARY Product


​   ► Act.Comp / Nutrient / Food / Herb as follows :- NA


DIETARY Substance Interactions


​   ► This Medicine interact with :- NA



ContraIndication DIETARY Substance


​   ► This Medicine contraindicate with :- NA

►   Route of Elimination :   Renal
Ref :-   Book : Goodman    Page : 714   Edition : 12.  

►    Plasma Half-life :   Min value :-   6 hours,    Max value :-   8 hours.  
Ref :-   Book : Goodman    Page : 714   Edition : 12.  

►    Peak Plasma Concentration :   Min value :-   2 hours,    Max value :-   4 hours.  
Ref :-   Book : Martindale    Page : 2641   Edition : 37.