V2-Receptor Antagonist (Vasopressin Antagonist)
Pregnancy: Avoid — teratogenic in animal studies
Tolvaptan
Brand names: Samsca
Adult dose
Dose: 15 mg OD, may increase to 30 mg OD then 60 mg OD at intervals ≥24h as required
Route: Oral
Frequency: Once daily
Max: 60 mg OD
For hyponatraemia (Na+ <125 mmol/L or symptomatic). Initiate in hospital. Correct Na+ at ≤12 mmol/L/24h to avoid osmotic demyelination.
Paediatric dose
Route: N/A
Frequency: N/A
Max: Not licensed in children
No established paediatric dosing
Dose adjustments
Renal
Caution in renal impairment; not effective if anuria
Hepatic
Contraindicated in patients unable to perceive/respond to thirst. Caution in hepatic impairment — hepatotoxicity reported.
Clinical pearls
- SALT-1/SALT-2: effective for SIADH and hypervolaemic hyponatraemia in CHF/cirrhosis
- Must initiate in hospital — risk of overcorrection of Na+
- Ensure fluid access — patients must be able to drink freely
- FDA added hepatotoxicity warning — avoid prolonged use in cirrhosis
Contraindications
- Hypovolaemic hyponatraemia
- Anuria
- Inability to perceive or respond to thirst
- Hypernatraemia
- Concomitant strong CYP3A4 inhibitors
Side effects
- Thirst (very common)
- Dry mouth
- Polyuria/pollakiuria
- Hypernatraemia (overcorrection)
- Hepatotoxicity (rare but serious)
- Dizziness
Interactions
- Strong CYP3A4 inhibitors (ketoconazole) — contraindicated
- P-gp inhibitors — increased tolvaptan levels
- Digoxin — increased digoxin levels
- Hypertonic saline — risk of rapid Na+ rise
Monitoring
- Serum sodium (frequently in first 24–48h)
- Fluid balance
- LFTs (hepatotoxicity monitoring)
- Signs of volume depletion
Reference: BNFc; SALT Trials (Schrier et al, NEJM 2006); BNF; FDA Drug Safety Communication 2013. Verify against your local formulary and the latest BNF before prescribing.
Related
Curated clinical cross-links plus same-class fallbacks.
Pathways
- Acute Heart Failure · ESC 2021 Heart Failure Guidelines; NICE NG106
- NSTEMI / Unstable Angina · ESC 2020 NSTEMI Guidelines; NICE NG185
- New-Onset Atrial Fibrillation · ESC 2020 AF Guidelines; NICE NG196
- Hypertensive Emergency · ESC/ESH 2018 Hypertension Guidelines; NICE NG136
- Bradycardia Management · Resuscitation Council UK ABCDE; ESC 2021 Pacing Guidelines
- Ventricular Tachycardia / Fibrillation · Resuscitation Council UK ACLS; ESC 2022 Ventricular Arrhythmia Guidelines