Names and pronunciation
(fos-tem′sa-vir) Rukobia
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Drug reference
(fos-tem′sa-vir) Rukobia
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Func. class.: Antiretroviral
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Chem. class.: gp120 attachment inhibitor
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ACTION: Binds to the HIV-1 protein glycoprotein 120 subunit, inhibits the interaction between the virus and cellular CD4 receptors, prevents attachment
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USES: Treatment of HIV-1 infection with other antiretrovirals in multidrug- resistant HIV-1 infection
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CONTRAINDICATIONS: Breastfeeding, hypersensitivity, use of strong CYP3A inducers (enzalutamide, car- bamazepine, phenytoin, rifampin, St. John’s wort) Precautions: Pregnancy, infants, liver disease, myelo- suppression, infections
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SIDE EFFECTS CNS: Fatigue, headache, dizziness, drowsi- ness, insomnia, abnormal dreams, periph- eral neuropathy CV: QT prolongation GI: Nausea, vomiting, abdominal pain, diarrhea, dyspepsia, increased LFTs META: Hyperbilirubinemia, hypercholester- olemia, hyperglycemia, hypertriglyceridemia HEMA: Anemia, neutropenia INTEG: Rash, pruritus
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INTERACTIONS Many drug interactions, refer to manu- facturer’s information
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DOSAGE AND ROUTES HIV-1 infection Adult PO: 600 mg bid with other antiretrovirals
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Available forms: Ext rel tablets 600 mg F
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Administer: PO route • Give without regard to food; swallow whole; do not chew, crush, split
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Assess: • HIV: CBC with differential, blood chem- istry, blood glucose, plasma HIV RNA, abso- lute CD4+/CD8+ cell counts, serum ICD+24 antigen levels, cholesterol, serum bilirubin (total and direct), serum lipid profile, urinalysis baseline and periodically • Hepatotoxicity: Monitor LFTs, signs of hepatotoxicity in HBV and/or HCV coinfec- tion; continue with or start anti-HBV therapy in those coinfected with HBV • Monitor for QT prolongation in those with a history of prolonged QT interval, preexist- ing cardiac disease, or those taking drugs known to cause torsades de pointes • Hepatitis B virus coinfection: Use with caution; elevations in LFTs are more com- mon in patients with HBV coinfection, which may be related to HBV reactivation. Monitor hepatitis B serology, plasma hepatitis C RNA • Peripheral neuropathy: May occur and last for several months, where nerves are close to the skin • Bowel pattern before, during treatment; if severe abdominal pain or constipation occurs, notify prescriber; monitor hydration • Hypersensitivity: Skin eruptions, rash, urticaria, itching; assess allergies before treatment, reaction to each medication; may occur quickly or later after continued use • Immune reconstitution syndrome: With combination therapy, patients may develop immune reconstitution syndrome with inflammatory response to an opportu- nistic infection during initial HIV treatment or activation of autoimmune disorders (Graves disease, polymyositis, Guillain- Barre syndrome, autoimmune hepatitis) • Pregnancy/breastfeeding: identify if pregnancy is planned or suspected, or if breastfeeding; if pregnant, register with the Antiretroviral Pregnancy Registry, 800-258-4263, obtain a pregnancy test
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Evaluate: • Therapeutic response: Increased CD4 cell counts; decreased viral load; slowing progression of HIV-1 infection
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That hypersensitive reactions may oc- cur; rash, pruritus; to stop product, con- tact prescriber • That product is not a cure for HIV-1 infec- tion but controls symptoms; HIV-1 can still be transmitted to others; that product is to be used in combination only with other an- tiretrovirals • To notify prescriber if pregnancy is suspected; not to breastfeed
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PHARMACOKINETICS Onset unknown, peak 2 hr, duration unknown, protein binding 88.4%, half- life 11 hr
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