Names and pronunciation
(kon-ih-vap′tan) Vaprisol
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Drug reference
(kon-ih-vap′tan) Vaprisol
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Func. class.: Vasopressin receptor antagonist
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ACTION: Dual arginine vasopressin (AVP) antagonist with affinity for V1A, V2 receptors; level of AVP in circulating blood is critical for regulation of water, electro- lyte balance and is usually elevated in euvolemic/hypervolemic hyponatremia
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USES: Euvolemia hyponatremia in hospitalized patients; not indicated for HF, hypervolemic hyponatremia
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Unlabeled uses: Increased intracranial pressure
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CONTRAINDICATIONS: Hyper- sensitivity, hypovolemia Precautions: Pregnancy, breastfeeding, orthostatic disease, renal disease, heart failure, rapid correction of serum sodium
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SIDE EFFECTS CNS: Headache, confusion, insomnia CV: Hypo/hypertension, orthostatic hypotension GI: Nausea, vomiting, constipation, dry mouth GU: Hematuria, infertility (women), polyuria INTEG: Erythema, injection site reaction META: Dehydration, hypokalemia, hypo- magnesemia, hyponatremia MISC: Oral candidiasis
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INTERACTIONS Increase: effect of—CYP3A4 substrates (alfuzosin, ARIPiprazole, bexarotene, bortez omib, bosentan, bupivacaine, buprenor- phine, carBAMazepine, cevimeline, cilo- stazol, cinacalcet, clopidogrel, colchicine, cyclobenzaprine, dapsone, darifenacin, disopyramide, DOCEtaxel, donepezil, DOXO- rubicin, dutasteride, eletriptan, eplerenone, ergots, erlotinib, eszopiclone, ethinyl estra- diol, ethosuximide, etoposide, fentaNYL, galantamine, gefitinib, ifosfamide, irinote- can, lidocaine, loperamide, loratadine, mefloquine, methadone, modafinil, PACLi- taxel, paricalcitrol, pimozide, praziquantel, quiNIDine, quiNINE, ramelteon, repaglinide, rifabutin, sibutramine, sildenafil, sirolimus, SUFentanil, SUNItinib, tacrolimus, tamoxi- fen, teniposide, testosterone, tiaGABine, tini- dazole, trimetrexate, vardenafil, vinca alka- loids, ziprasidone, zolpidem, zonisamide); do not use concurrently
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DOSAGE AND ROUTES • Adult: IV INFUSION loading dose 20 mg given over 30 min then CONT IN- FUSION of 20 mg over 24 hr; after day 1, give 20 mg/24 hours for an additional 1-3 days; can be titrated up to 40 mg/day if serum sodium is not rising at desired rate; max time 4 days Hepatic/renal dose • Adult: IV Child-Pugh A-C or CCr 30-60 mL/min: give IV loading dose over 10 min then CONTINUOUS IV INFUSION 10 mg over 24 hr × 2-4 days
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Available forms: Injection (premixed) 0.2 mg/mL in 100 mL D5W
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Administer: Intermittent IV Infusion • Premixed, do not need dilution (0.2 mg/mL) Continuous IV INFUSION route • Give over 24 hrs or 40 mg/24 hr
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Assess: • Renal, hepatic function • Sodium levels/volume status: mon- itor serum sodium levels q2-3hr until stable; overly rapid correction of sodium concentration (>12 mEq/L per 24 hr) may result in osmotic demyelination syndrome • Neurologic status: confusion, headache • Injection site reactions: redness, in- flammation, pain; if these occur, product needs to be discontinued • CV status: atrial fibrillation, hypo/hy- pertension, orthostatic hypotension; mon- itor B/P, pulse baseline and periodically • Monitor other electrolytes (magnesium and potassium) • Pregnancy/breastfeeding: no well- controlled studies; use in pregnancy only if benefits outweigh fetal risk, may cause fetal harm; discontinue breastfeeding or discontinue product; excretion is unknown
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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: • To report neurologic changes: head- ache, insomnia, confusion • About administration procedure and expected results C • To report injection site pain, redness, swelling CONTRACEPTIVES, HORMONAL Monophasic, Oral
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PHARMACOKINETICS Protein binding 99%, metabolized by CYP3A4, half-life 5 hr
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• Adult: IV INFUSION loading dose 20 mg given over 30 min then CONT IN- FUSION of 20 mg over 24 hr; after day 1, give 20 mg/24 hours for an additional 1-3 days; can be titrated up to 40 mg/day if serum sodium is not rising at desired rate; max time 4 days Hepatic/renal dose
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• Adult: IV Child-Pugh A-C or CCr 30-60 mL/min: give IV loading dose over 10 min then CONTINUOUS IV INFUSION 10 mg over 24 hr × 2-4 days
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