Names and pronunciation
(nell-fin′a-ver) Viracept
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Drug reference
(nell-fin′a-ver) Viracept
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Func. class.: Antiretroviral
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Chem. class.: Protease inhibitor
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Do not confuse: Viracept/Viramune
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ACTION: Inhibits human immunode- ficiency virus (HIV-1) protease, which prevents maturation of the infectious virus Uses: HIV-1 in combination with other antiretrovirals
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CONTRAINDICATIONS: Hyper- sensitivity to protease inhibitors Precautions: Pregnancy, breastfeeding, renal/hepatic disease, hemophilia, PKU, pancreatitis, diabetes, infection, immune reconstitution syndrome
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SIDE EFFECTS CNS: Headache, asthenia, poor concen- tration, seizures, suicidal ideation CV: Bleeding, QTc prolongation, torsades de pointes ENDO: Hyperglycemia, hyperlipidemia GI: Diarrhea, anorexia, dyspepsia, nau- sea, flatulence, hepatitis, pancreatitis GU: Sexual dysfunction HEMA: Anemia, leukopenia, thrombocy- topenia, HB abnormalities INTEG: Rash, dermatitis, anaphylaxis MISC: Hypoglycemia, redistribution/ accumulation of body fat, immune recon- stitution syndrome MS: Pain, arthralgia, myalgia, myopathy
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INTERACTIONS Increase: serious dysrhythmias—ami- odarone, ergots, lovastatin, midazolam, pimozide, quiNIDine, simvastatin, triazolam, salmeterol Increase: effect of—atorvastatin, azithro- mycin, rifabutin, indinavir, saquinavir, cycloSPORINE, tacrolimus, sirolimus, sildenafil, alfentanil, alosetron, buprenor- phine, busPIRone, bortezomib, calcium channel blockers, cilostazol, disopyra- mide, dofetilide, DOCEtaxel, donepezil, ethosuximide, fentaNYL, galantamine, gefitinib, levomethadyl, systemic lido- caine, PACLitaxel, sibutramine, SUFent- anil, vinca alkaloids, ziprasidone, zonisamide, traZODone, tricyclic antide- pressants, sildenafil Increase: nelfinavir levels—ketoconazole, indinavir, ritonavir; delavirdine, other HIV protease inhibitors Decrease: nelfinavir levels—rifamycins, nevirapine, PHENobarbital, phenytoin, carBAMazepine Decrease: effect of—didanosine, metha- done, oral contraceptives, phenytoin Drug/Herb • Decrease: antiretroviral effect—St. John’s wort; do not use concurrently Drug/Lab Test Increase: AST, ALT, alk phos, total biliru- bin, CPK, LDH, lipids, uric acid Decrease: WBC, platelets
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DOSAGE AND ROUTES HIV infection • Adult/child >13 yr: PO 750 mg tid or 1250 mg bid, max 2500 mg/day in com- bination • Child 2-12 yr: PO 25-35 mg/kg tid or 45-55 mg/kg bid, max 2500 mg/day bid or 2250 mg/day tid in combina- tion
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Available forms: Tabs 250, 625 mg
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Administer: PO route Do not mix with juice or acidic fluids • Tabs may be crushed and dispersed in water or mixed with food; consume im- mediately, rinse and have patient con- sume all liquid
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Assess: • HIV: serum lipid profile, plasma HIV RNA, blood glucose, viral load, CD4 cell counts at baseline and throughout treatment • Resistance testing at initiation, or with failure of treatment • Signs of infection, anemia • Hepatic studies: ALT, AST • Bowel pattern before, during treat- ment; if severe abdominal pain with bleeding occurs, product should be dis- continued; monitor hydration • Immune reconstitution syndrome: occurs with combination therapy, including MAC, CMV, PCP, TB, requiring treatment • Anaphylaxis, hypersensitivity reac- tion: wheezing, flushing; swelling of lips, tongue, throat, skin eruptions, rash, urti- caria, itching • Pregnancy/breastfeeding: enroll preg- nant patients in Antiretroviral Pregnancy Registry; use only if potential benefit is greater than risk; do not breastfeed Evaluate • Therapeutic response: decreased viral load, improved CD4+ cell count, re- duced opportunistic infections
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To avoid taking with other medications unless directed by prescriber • Diarrhea is most common side effect; may use loperamide to control • That product does not cure but does manage symptoms; that product does not prevent transmission of HIV to others • Sexual dysfunction: If using with sildenafil report change in vision, pain with erection, decreased B/P, do not use ≥25 mg/48 hr • If dose is missed, to take as soon as remembered up to 1 hr before next dose; N not to double dose; to take with food • To report symptoms of hyperglycemia, bleeding, abdominal pain; yellowing of skin, eyes • Phenylketonuria: that powder con- tains phenylalanine • To advise all providers of this product; to advise prescriber of all OTC products, prescription products, or herbal prod- ucts taken • Pregnancy: to use a nonhormonal form of birth control while taking this product if using contraceptives
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PHARMACOKINETICS Half-life 3½-5 hr, excreted in feces (87%), peak 2-4 hr, 98% protein bind- ing; metabolized by CYP3A4 enzyme sys- tem; potent inhibitor of CYP3A4
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• Adult/child >13 yr: PO 750 mg tid or 1250 mg bid, max 2500 mg/day in com- bination
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• Child 2-12 yr: PO 25-35 mg/kg tid or 45-55 mg/kg bid, max 2500 mg/day bid or 2250 mg/day tid in combina- tion
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