Names and pronunciation
(ral-teg′ra-vir) Isentress, Isentress HD
Source page 1123
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Individual generic drug information
Extracted information for raltegravir only.
(ral-teg′ra-vir) Isentress, Isentress HD
Source page 1123
Func. class.: Antiretroviral
Source page 1123
Chem. class.: HIV integrase strand transfer inhibitor (ISTIs)
Source page 1123
ACTION: Inhibits catalytic activity of HIV integrase, which is an HIV-encoded enzyme needed for replication
Source page 1123
USES: HIV in combination with other antiretrovirals R
Source page 1123
Extracted information for raltegravir only.
CONTRAINDICATIONS: Breast- feeding, hypersensitivity Precautions: Pregnancy, children, geri- atric patients, hepatic disease, immune reconstitution syndrome, hepatitis, anti- microbial resistance, lactase deficiency
Source page 1123
SIDE EFFECTS CNS: Fatigue, fever, dizziness, headache, asthenia, suicidal ideation, insomnia CV: MI GI: Nausea, vomiting, diarrhea, abdomi- nal pain, asthenia, gastritis, hepatitis GU: Acute renal failure HEMA: Anemia, neutropenia INTEG: Rash, urticaria, pruritus, pain or phlebitis at IV site, unusual sweating, alopecia, Stevens-Johnson syndrome, toxic epidermal necrolysis META: Hyperamylasemia, hyperglycemia, lipodystrophy MS: Myopathy, rhabdomyolysis SYST: Immune reconstitution syndrome
Source page 1124
INTERACTIONS Increase: raltegravir effect—proton pump inhibitors, H2 blockers; UGT1A1 inhibitors (atazanavir) Increase: rhabdomyolysis, myopathy, elevated CPK—fibric acid derivatives, HMG-CoA reductase inhibitors Decrease: raltegravir levels—rifAMPin, efavirenz, tenofovir, tipranavir/ritonavir Drug/Lab Test Increase: AST, ALT, GGT, total bilirubin, alk phos, amylase/lipase, CK, serum glu- cose, total/HDL/LDL cholesterol Decrease: HB, platelets, ANC
Source page 1124
Extracted information for raltegravir only.
DOSAGE AND ROUTES Do not interchange chewable tablets, film-coated 400-mg and high-dose 600- mg tablets HIV with other antiretroviral agents • Adult: PO (400-mg film-coated tablet) 400 mg bid. During coadministration with rifampin, recommended dosage is 800 mg bid • Adolescent/child ≥25 kg: PO (400- mg film-coated tablet) 400 mg bid • Adolescent/child (weight-based dos- age): PO (chewable tablets) ≥40 kg, 300 mg bid; 28-39 kg, 200 mg bid; 20-27 kg, 150 mg bid; 14-19 kg, 100 mg bid; 11-13 kg, 75 mg bid • Child: PO (powder for suspension) 14-19 kg, 100 mg (5 mL) bid; 11-13 kg, 80 mg (4 mL) bid; ≥4 wk of age and 8-10 kg, 60 mg (3 mL) bid; ≥4 wk and 6-7 kg, 40 mg (2 mL) bid; ≥4 wk and 4-5 kg, 30 mg (1.5 mL) bid; ≥4 wk and 3 kg, 25 mg (1 mL) bid High-dose regimen • Adult: PO (600-mg film-coated tablet) 1200 mg (2 × 600 mg)/day. Coadminis- tration with rifAMPin is not recommended • Adolescent/child ≥40 mg: PO (600 mg film-coated tablet) 1200 mg (2 × 600 mg)/day. Coadministration with rifampin is not recommended
Source pages 1123, 1124
Available forms: Tabs 400, 600 mg; chew tabs 25, 100 mg; granules for oral suspension 100 mg/packet
Source page 1124
Administer: PO route • Tablets and chew tablets are not inter- changeable • Chew tabs should be chewed or swal- lowed whole • Do not break, crush, chew regular tabs • May give without regard to meals, with 8 oz of water • Store at room temperature Oral suspension: Open foil, use 5 mL of water in provided measuring cup, close cup, swirl, do not turn upside down, use oral syringe to administer, use within 30 min, discard any remain- ing suspension
Source page 1124
Extracted information for raltegravir only.
Assess: • HIV infection: CD4, T-cell count, plasma HIV RNA, viral load; resistance testing be- fore therapy, at treatment failure • Rhabdomyolysis: assess for muscle pain, darkening of urine, increased CPK; product should be discontinued • Skin eruptions: rash, urticaria, itching • Suicidal thoughts/behaviors: moni- tor for depression; more common in those with mental illness • Immune reconstitution syndrome, usually during initial phase of treatment; may give antiinfective before starting; op- portunistic infections or autoimmune dis- orders may occur • Stevens-Johnson syndrome: skin eruptions: rash, urticaria, itching • Monitor total/HDL/LDL cholesterol, blood glucose, LFTs, serum bilirubin (to- tal and direct), baseline and periodically (all may be elevated); pregnancy test, CBC with differential, hepatitis serology, plasma hepatitis C, RNA, urinalysis, base- line and periodically • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, pregnant women taking this product should enroll in the Antiretroviral Pregnancy Registry, 1-800-258-4263; do not breastfeed
Source pages 1124, 1125
Evaluate: • Therapeutic response: improvement in CD4 counts, T-cell counts, viral load • Decreased progression of AIDs, HIV
Source page 1125
CLINICAL CONSIDERATIONS
Source page 1124
Patient and caregiver information: • To take as prescribed; if dose missed, to take as soon as remembered up to 1 hr before next dose; not to double dose; not to share with others • That sexual partners need to be told that patient has HIV; that product does not cure infection, just controls symptoms; that it does not prevent infecting others • To report sore throat, fever, fatigue (may indicate immune reconstitution syn- drome) • That product must be taken in equal intervals 2×/day to maintain blood levels for duration of therapy • To notify prescriber immediately of sui- cidal thoughts/behaviors • Pregnancy: to notify prescriber if pregnancy is planned or suspected; not to breastfeed • To continue with follow-up exams, blood work • To report rash, muscle pain immediately HIGH ALERT
Source page 1125
Extracted information for raltegravir only.
PHARMACOKINETICS Max absorption 3 hr if taken on an empty stomach; half-life 9 hr; metabolized in the liver by uridine diphosphate glucuro- nosyltransferase (UGTA1A enzyme system); excreted in feces 51%, urine 32%
Source page 1124
Filter the extracted dose blocks for this individual drug.
film-coated 400-mg and high-dose 600- mg tablets HIV with other antiretroviral agents
• Adolescent/child ≥25 kg: PO (400- mg film-coated tablet) 400 mg bid
Candidate age grouping · source pages 1123, 1124
film-coated 400-mg and high-dose 600- mg tablets HIV with other antiretroviral agents
• Adolescent/child (weight-based dos- age): PO (chewable tablets) ≥40 kg, 300 mg bid; 28-39 kg, 200 mg bid; 20-27 kg, 150 mg bid; 14-19 kg, 100 mg bid; 11-13 kg, 75 mg bid
Candidate age grouping · source pages 1123, 1124
film-coated 400-mg and high-dose 600- mg tablets HIV with other antiretroviral agents
• Child: PO (powder for suspension) 14-19 kg, 100 mg (5 mL) bid; 11-13 kg, 80 mg (4 mL) bid; ≥4 wk of age and 8-10 kg, 60 mg (3 mL) bid; ≥4 wk and 6-7 kg, 40 mg (2 mL) bid; ≥4 wk and 4-5 kg, 30 mg (1.5 mL) bid; ≥4 wk and 3 kg, 25 mg (1 mL) bid High-dose regimen
Candidate age grouping · source pages 1123, 1124
film-coated 400-mg and high-dose 600- mg tablets HIV with other antiretroviral agents
• Adolescent/child ≥40 mg: PO (600 mg film-coated tablet) 1200 mg (2 × 600 mg)/day. Coadministration with rifampin is not recommended
Candidate age grouping · source pages 1123, 1124