Names and pronunciation
(tole-vap′tan) Jinarc, Jynarque, Samsca
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Drug reference
(tole-vap′tan) Jinarc, Jynarque, Samsca
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Func. class.: Antihypertensive
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Chem. class.: Vasopressin receptor antagonist, V2
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ACTION: Arginine vasopressin (AVP) antagonist with affinity for V2 receptors; level of circulating AVP in circulating blood is critical for the regulation of water and the electrolyte balance, and it is usually elevated with euvolemic/ hypervolemic hyponatremia
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USES: Hypervolemic/euvolemic hypo- natremia with heart failure, cirrhosis, SIADH
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CONTRAINDICATIONS: Hyper- sensitivity, hypovolemia, anuria Precautions: Pregnancy, breastfeeding, children, dehydration, geriatric patients, hyperkalemia, autosomal dominant PKD, malnutrition, alcoholism, hepatic disease
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Black Box Warning: Osmotic demyeli- nation syndrome; requires a specialized care setting Black Box Warning: Osmotic demyeli- nation syndrome: frequent sodium vol status; overly rapid correction of sodium concentration (>12 mEq/L per 24 hr); may occur in alcoholism, severe malnutrition, advanced liver disease, syndrome of inap- propriate antidiuretic hormone; correct so- dium levels slowly, may result in dysarthria, mutism, dysphagia, coma, seizure, death • CV status: ventricular fibrillation, hy- pertension; monitor B/P, pulse • Monitor electrolytes (sodium, potassium) Black Box Warning: Specialized care setting: needed so that neurologic status and sodium can be monitored • Liver injury: fatigue, abdominal pain, dark urine, clay-colored stools, jaundice • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; do not breastfeed
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SIDE EFFECTS CNS: Fever, dizziness CV: Ventricular fibrillation, DIC, stroke, thrombosis GI: Nausea, vomiting, constipation, colitis, hepatic injury GU: Polyuria HEMA: Bleeding META: Dehydration, hyperglycemia, hyperkalemia, hypernatremia MS: Rhabdomyolysis RESP: Respiratory depression, pulmo nary embolism
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INTERACTIONS Increase: concentrations of tolvaptan— CYP3A4 inhibitors (efavirenz, fosampre- navir, quiNINE); P-gp inhibitors (cyclo- SPORINE, azithromycin, mefloquine, palperidone, propafenone, quiNIDine, testosterone) Decrease: concentration of tolvaptan— CYP3A4 inducers (carBAMazepine, dexa- methasone, etravirine, flutamide, griseo- fulvin, metyraPONE, modafinil, nafcillin, nevirapine, OXcarbazepine, phenytoin, rifAMPin, rifabutin, rifapentine, topiramate) Drug/Herb Decrease: tolvaptan effect—CYP3A4 inducer (St. John’s wort) Drug/Food • Grapefruit/grapefruit juice; do not use together
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DOSAGE AND ROUTES • Adult: PO 15 mg daily; after 24 hr, may increase to 30 mg daily; max 60 mg/day max 30 days
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Available forms: Tabs 15, 30, 45, 60, 90 mg
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Administer: • PO with/without food • Avoid fluid restriction for first 24 hr • Initiate in hospital setting • Do not use with grapefruit, grapefruit juice
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Assess: • Renal, hepatic function
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Evaluate: • Therapeutic response: correction of serum sodium levels
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • About administration procedure and expected results; that product will be used for ≤30 days • To report difficulty swallowing, speak ing, seizures, dizziness, drowsiness; em bolism may be the cause • To drink fluid in response to thirst • Not to use grapefruit juice • To notify prescriber before using other products • To report right upper abdominal pain, nausea, vomiting, anorexia, dark urine, yellowing of skin, eyes (hepatic injury) • That product will be started or re- started in the hospital when monitoring is possible • To avoid pregnancy, breastfeeding while taking this product
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PHARMACOKINETICS Peak 2-4 hr, protein binding 99%, metab- olized by CYP3A4, terminal half-life 12 hr
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• Adult: PO 15 mg daily; after 24 hr, may increase to 30 mg daily; max 60 mg/day max 30 days
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