Version January 2024
HIV-1 infection, treatment: Note: Do not use raltegravir in combination with darunavir and ritonavir in patients with HIV RNA >100,000 copies/mL and/or CD4 count <200 cells/mm3, or in combination with abacavir and lamivudine in patients with HIV RNA >100,000 copies/mL (Ref).
Treatment-naive patients: Oral: Film-coated tablet:
Isentress: 400 mg twice daily.
Note: Patients virologically suppressed on an initial regimen of raltegravir 400 mg twice daily may switch to once daily dosing with Isentress HD.
Isentress HD: 1.2 g once daily (2 × 600 mg tablet).
Note: Once daily dosing is not recommended for use during pregnancy (Ref).
Treatment-experienced patients: Oral: Film-coated tablet: Isentress: 400 mg twice daily.
HIV-1 nonoccupational postexposure prophylaxis (nPEP) (off-label use): Oral: Film-coated tablet: Isentress: 400 mg twice daily for 28 days in combination with other antiretroviral agents. Initiate therapy within 72 hours of exposure (Ref).
HIV-1 occupational postexposure prophylaxis (oPEP) (off-label use): Oral: Film-coated tablet: Isentress: 400 mg twice daily for 4 weeks with concomitant emtricitabine/tenofovir. Initiate therapy as soon as possible after occupational exposure (and within 72 hours) (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Mild, moderate, and severe impairment: No dosage adjustment necessary.
End-stage renal disease (ESRD) on intermittent hemodialysis (IHD): Dose after dialysis on dialysis days.
Film-coated tablet (Isentress 400 mg tablet), chewable tablet, oral suspension:
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: There are no dosage adjustments provided in manufacturer’s labeling (has not been studied).
Film-coated tablet (Isentress HD 600 mg tablet): Use is not recommended (has not been studied).
Refer to adult dosing.
(For additional information see "Raltegravir: Pediatric drug information")
Note: Raltegravir film-coated tablets (including Isentress HD) and chewable tablets or oral suspension are not bioequivalent and are not substitutable on a mg/mg basis.
HIV-1 infection, treatment: Note: Use in combination with other antiretroviral (ARV) agents; evaluate gene mutation and ARV resistance patterns (refer to https://www.iasusa.org and https://hivdb.stanford.edu for more information).
Oral suspension (10 mg/mL):
Infants and Children weighing <20 kg:
Weight-directed dosing: Oral: 6 mg/kg/dose twice daily; maximum dose: 100 mg/dose.
Fixed dosing: Oral:
3 to <4 kg: 25 mg twice daily.
4 to <6 kg: 30 mg twice daily.
6 to <8 kg: 40 mg twice daily.
8 to <11 kg: 60 mg twice daily.
11 to <14 kg: 80 mg twice daily.
14 to <20 kg: 100 mg twice daily.
Chewable tablets: Note: The film-coated tablets are preferred in children and adolescents weighing ≥25 kg who are able to swallow a tablet whole.
Infants, Children, and Adolescents weighing ≥3 kg:
Weight-directed dosing: Oral: 6 mg/kg/dose twice daily; maximum dose: 300 mg/dose.
Fixed dosing: Oral:
3 to <6 kg: 25 mg twice daily.
6 to <10 kg: 50 mg twice daily.
10 to <14 kg: 75 mg twice daily.
14 to <20 kg: 100 mg twice daily.
20 to <28 kg: 150 mg twice daily.
28 to <40 kg: 200 mg twice daily.
≥40 kg: 300 mg twice daily.
Film-coated tablets:
Isentress: 400 mg tablets: Children and Adolescents ≥25 kg: Oral: 400 mg twice daily.
Isentress HD: 600 mg tablets: Children and Adolescents ≥40 kg: Oral: 1,200 mg once daily. Note: Regimen appropriate for treatment-naive patients, or patients virologically suppressed on an initial regimen of raltegravir 400 mg twice daily.
HIV-1 nonoccupational postexposure prophylaxis (nPEP) (Ref): Note: Initiate therapy within 72 hours of exposure and continue for 28 days; use in combination with other antiretroviral agents.
Infants and Children <2 years: Oral: Oral suspension (10 mg/mL): 6 mg/kg/dose twice daily.
Children ≥2 years: Oral:
Chewable tablets:
11 to <14 kg: 75 mg twice daily.
14 to <20 kg: 100 mg twice daily.
20 to <28 kg: 150 mg twice daily.
28 to <40 kg: 200 mg twice daily.
≥40 kg: 300 mg twice daily.
Film-coated tablet: Isentress 400 mg tablet: Children ≥6 years weighing >25 kg who are able to swallow a tablet whole: 400 mg twice daily.
Adolescents: Oral: Film-coated tablet: Isentress 400 mg tablet: 400 mg twice daily for 28 days.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Infants, Children, and Adolescents:
Mild, moderate, or severe impairment: No dosage adjustment required.
End-stage renal disease (ESRD) on intermittent hemodialysis (IHD): Dose after dialysis on dialysis days.
Film-coated tablet (400 mg formulation at standard twice-daily dose), chewable tablet, oral suspension:
Infants, Children, and Adolescents:
Mild to moderate hepatic impairment: No dosage adjustment required.
Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Film-coated tablet (600 mg formulation [Isentress HD]): Pediatric patients ≥40 kg: Use is not recommended in any degree of hepatic impairment (has not been studied).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reaction incidence is for combination therapy in adults unless otherwise indicated.
>10%: Hepatic: Increased serum alanine aminotransferase (grade 2 to 4: ≤11%)
1% to 10%:
Endocrine & metabolic: Increase in fasting plasma glucose (grade 2: 126 to 250 mg/dL: 7% to 10%; grade 3: 251 to 500 mg/dL: 2% to 3%)
Gastrointestinal: Abdominal pain (<2%), decreased appetite (≥2%), diarrhea (≥2%), dyspepsia (<2%), flatulence (≥2%), gastritis (<2%), increased serum amylase (grade 2 to 4: ≤4%), increased serum lipase (grade 2 to 4: 1% to 7%), nausea (1% to 3%), vomiting (<2%)
Genitourinary: Genital herpes simplex (<2%)
Hematologic & oncologic: Decrease in absolute neutrophil count (grade 2 to 4: ≤4%), decreased hemoglobin (grade 2 to 4: ≤1%)
Hepatic: Hepatitis (<2%), increased serum alkaline phosphatase (grade 2 to 4: ≤2%), increased serum aspartate aminotransferase (grade 2 to 4: ≤9%), increased serum bilirubin (grade 2 to 4: ≤6%)
Hypersensitivity: Hypersensitivity reaction (<2%)
Infection: Herpes zoster infection (<2%)
Nervous system: Abnormal dreams (≥2%), asthenia, depression, dizziness (≤2%), fatigue (2%), headache (≤4%), insomnia (≤4%), nightmares (≥2%), suicidal ideation (<2%), suicidal tendencies (<2%)
Neuromuscular & skeletal: Increased creatine phosphokinase in blood specimen (grade 2 to 4: 2% to 5%)
Renal: Increased serum creatinine (grade 2 to 3: ≤1%), nephrolithiasis (<2%), renal failure syndrome (<2%)
<1%: Nervous system: Abnormal behavior (grade 3: children and adolescents), psychomotor agitation (grade 3: children and adolescents)
Frequency not defined:
Dermatologic: Skin rash
Endocrine & metabolic: Increased HDL cholesterol, increased LDL cholesterol, increased serum cholesterol, increased serum triglycerides
Hematologic & oncologic: Malignant neoplasm
Postmarketing:
Dermatologic: Stevens-Johnson syndrome, toxic epidermal necrolysis
Endocrine & metabolic: Diabetes mellitus (Fong 2017, O’Halloran 2022)
Hematologic: Thrombocytopenia
Hypersensitivity: Drug reaction with eosinophilic and systemic symptoms (Perry 2013)
Immunologic: Immune reconstitution syndrome
Nervous system: Anxiety, cerebellar ataxia, paranoid ideation
Neuromuscular & skeletal: Myopathy, rhabdomyolysis
There are no contraindications listed in the manufacturer's labeling.
Canadian labeling: Hypersensitivity to raltegravir or any other component of the formulation
Concerns related to adverse effects:
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
• Myopathy: Grade 2 to 4 creatine kinase (CK) increases have been observed and myopathy and rhabdomyolysis have been reported; use caution in patients with a history of rhabdomyolysis, myopathy, or increased serum creatine kinase or who have risk factors for CK elevations and/or skeletal muscle abnormalities, including taking other drugs known to cause myopathy or rhabdomyolysis.
• Skin and hypersensitivity reactions: Severe, life-threatening or fatal cases of Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported. Hypersensitivity reactions (rash, constitutional symptoms, organ dysfunction) have also been reported. Discontinue immediately if a severe skin reaction or hypersensitivity symptoms develop. Monitor clinical status, including liver transaminases.
Dosage form specific issues:
• Chewable tablet: Contains phenylalanine; avoid or use with caution in patient with phenylketonuria.
• Tablets and oral suspension: Raltegravir film-coated tablets and chewable tablets or oral suspension are not bioequivalent and are not substitutable on a mg/mg basis.
At birth, the enzyme responsible for the metabolism of raltegravir (UGT1A1) is low and raltegravir elimination in neonates may be prolonged. The activity of UGT1A1 increases rapidly over the first 4 to 6 weeks of life (HHS [perinatal] 2023). Raltegravir also competes with bilirubin for albumin protein-binding sites and may increase unconjugated bilirubin concentrations, which could be particularly concerning in neonates due to kernicterus risk in the presence of high raltegravir concentrations. However, in vitro data suggest that this effect is unlikely to be significant at typical serum concentrations (Clarke 2013; HHS [pediatric] 2023). Additionally, in 42 neonates who received ≤6 weeks of raltegravir therapy and were followed for 24 weeks, there were only 2 cases of nonserious bilirubin elevations for which no treatment was necessary and no drug-related clinical adverse reactions were observed.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Packet, Oral:
Isentress: 100 mg (60 ea) [contains polyethylene glycol (macrogol); banana flavor]
Tablet, Oral:
Isentress: 400 mg
Isentress HD: 600 mg
Tablet Chewable, Oral:
Isentress: 25 mg [contains aspartame, saccharin sodium; orange banana flavor]
Isentress: 100 mg [scored; contains aspartame, saccharin sodium; orange banana flavor]
No
Chewable (Isentress Oral)
25 mg (per each): $2.39
100 mg (per each): $9.55
Pack (Isentress Oral)
100 mg (per each): $9.55
Tablets (Isentress HD Oral)
600 mg (per each): $38.21
Tablets (Isentress Oral)
400 mg (per each): $38.21
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Isentress: 400 mg [contains polyethylene glycol (macrogol)]
Isentress HD: 600 mg
Tablet Chewable, Oral:
Isentress: 25 mg, 100 mg [contains aspartame, saccharin sodium]
May be administered without regard to meals.
Chewable tablets: May be chewed or swallowed whole; the 100 mg chewable tablet may be divided into equal halves.
Film-coated tablets: Must be swallowed whole.
Oral suspension: Using provided mixing cup, pour packet contents into 10 mL water, close lid and swirl in a circular motion for 45 seconds; do not shake. Do not turn the mixing cup upside down. Once mixed, measure recommended suspension dose with an oral syringe (concentration of suspension is 10 mg/mL). Administer within 30 minutes of mixing with water. Discard any remaining suspension in the trash.
Oral: May be administered without regard to meals.
Chewable tablets: May be chewed, crushed (25 mg), or swallowed whole; 100 mg chewable tablet can be split in half.
Patients unable to chew the chewable tablet: The 25 mg tablet may be crushed by placing tablet and ~5 mL of liquid (eg, water, juice, breast milk) in a small cup; the tablet should break apart within 2 minutes; crush any remaining pieces of undispersed tablet with a spoon and administer the entire mixture immediately. If any dose remains in cup, add ~5 mL of liquid, swirl, and administer immediately.
Film-coated tablets: Must be swallowed whole.
Oral suspension: Administer dose (at a concentration of 10 mg/mL) within 30 minutes of reconstitution.
HIV-1 infection, treatment: Treatment of HIV-1 infection in combination with other antiretroviral agents
HIV-1 nonoccupational postexposure prophylaxis; HIV-1 occupational postexposure prophylaxis
Substrate of UGT1A1
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Aluminum Hydroxide: May decrease the serum concentration of Raltegravir. Management: Avoid the use of oral / enteral aluminum hydroxide with raltegravir. No dose separation schedule has been established that adequately reduces the magnitude of interaction. Risk X: Avoid combination
Betibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Betibeglogene Autotemcel. Risk X: Avoid combination
Calcium Carbonate: May decrease the serum concentration of Raltegravir. Management: Use of once-daily raltegravir with calcium carbonate is not recommended; dose separation does not appear to be adequate to minimize the significance of this interaction. Use of other raltegravir products do not require any dose change. Risk D: Consider therapy modification
Elivaldogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Elivaldogene Autotemcel. Management: Avoid use of antiretroviral medications for at least one month, or for the amount of time required for elimination of the retroviral medication, prior to stem cell mobilization and until the all apheresis cycles are finished Risk X: Avoid combination
Etravirine: May decrease the serum concentration of Raltegravir. Management: Concurrent use of etravirine with once-daily raltegravir (Isentress HD) is not recommended. Concurrent use of other raltegravir products with etravirine does not require any dose change. Risk C: Monitor therapy
Fibric Acid Derivatives: Raltegravir may enhance the myopathic (rhabdomyolysis) effect of Fibric Acid Derivatives. Risk C: Monitor therapy
Fosamprenavir: May decrease the serum concentration of Raltegravir. Raltegravir may decrease the serum concentration of Fosamprenavir. Risk X: Avoid combination
HMG-CoA Reductase Inhibitors (Statins): Raltegravir may enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy
Magnesium Salts: May decrease the serum concentration of Raltegravir. Management: Avoid the use of oral / enteral magnesium salts with raltegravir. No dose separation schedule has been established that adequately reduces the magnitude of interaction. Risk X: Avoid combination
Mitapivat: May decrease the serum concentration of UGT1A1 Substrates. Risk C: Monitor therapy
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy
Polyvalent Cation Containing Products: May decrease the serum concentration of Raltegravir. Management: Administer raltegravir 2 hours before or 6 hours after administration of the polyvalent cations. Dose separation may not adequately minimize the significance of this interaction. Risk D: Consider therapy modification
Rifabutin: May decrease the serum concentration of Raltegravir. Risk C: Monitor therapy
RifAMPin: May decrease the serum concentration of Raltegravir. Management: Increase raltegravir dose to 800 mg twice daily (adult dose) when used concomitantly with rifampin. Concurrent use of rifampin with once-daily raltegravir (Isentress HD) is not recommended. Risk D: Consider therapy modification
Rifapentine: May increase the serum concentration of Raltegravir. Rifapentine may decrease the serum concentration of Raltegravir. Risk C: Monitor therapy
Tipranavir: May decrease the serum concentration of Raltegravir. Management: Concurrent use of tipranavir/ritonavir with once-daily raltegravir (Isentress HD) is not recommended. Risk C: Monitor therapy
Zidovudine: Raltegravir may enhance the myopathic (rhabdomyolysis) effect of Zidovudine. Risk C: Monitor therapy
Variable absorption depending upon meal type (low- vs high-fat meal) and dosage form. Management: Raltegravir was administered without regard to meals in clinical trials.
Contraception is not required to initiate or continue antiretroviral therapy.
The US Department of Health and Human Services (HHS) perinatal HIV guidelines consider raltegravir an alternative integrase strand transfer inhibitor for patients with HIV who are not yet pregnant but are trying to conceive.
Maximum viral suppression sustained below the limits of detection prior to conception is recommended for all persons with HIV who are planning a pregnancy. Optimization of the health of the person who will become pregnant is recommended. Selection of or changes to a specific antiretroviral regimen prior to pregnancy should be done as part of a shared decision-making process. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender-diverse people assigned female sex at birth.
Health care providers caring for couples planning a pregnancy when one or both partners are diagnosed with HIV may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).
Raltegravir has high transfer across the human placenta.
No increased risk of overall teratogenic effects has been observed following first trimester exposure according to data collected by the antiretroviral pregnancy registry. Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm birth, low birth weight, and small for gestational age infants. Actual risks may be influenced by maternal factors such as disease severity, gestational age at initiation of therapy, and specific ART regimen; therefore, close fetal monitoring is recommended. Because there is clear benefit to appropriate treatment, maternal ART should not be withheld due to concerns for adverse neonatal outcomes. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children not diagnosed with HIV but who were exposed to ART in utero or as a neonate and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential metabolic dysfunction.
The US Department of Health and Human Services (HHS) Perinatal HIV Guidelines consider raltegravir an alternative integrase strand transfer inhibitor (INSTI) for pregnant patients with HIV who are antiretroviral-naive, who have had ART therapy in the past but are restarting, or who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen). In addition, patients who become pregnant while taking raltegravir may continue if viral suppression is effective and the regimen is well tolerated. INSTIs can rapidly suppress viral load. Raltegravir may be useful as part of an alternative regimen when drug interactions or the potential for preterm delivery with protease inhibitors are a concern. In addition, use of raltegravir may be part of an alternative regimen in patients with HIV who are not on ART and present for care late in pregnancy.
The pharmacokinetics of raltegravir are variable. Dose adjustments are not required in pregnant patients; however, once daily dosing is not recommended until more data in pregnancy are available.
ART is recommended for all pregnant people with HIV to maximize their health, maintain the viral load below the limit of detection, and reduce the risk of perinatal transmission. Selection of or changes to a specific antiretroviral regimen during pregnancy should be done as part of a shared decision-making process. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitoring of patients who are pregnant is more frequent than in patients who are not pregnant. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender-diverse people assigned female sex at birth.
Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Health care providers should enroll all patients exposed to antiretroviral medications during pregnancy in the Antiretroviral Pregnancy Registry (1-800-258-4263). Enrollment should be done as early in pregnancy as possible.
Health care providers caring for pregnant patients with HIV and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).
Raltegravir is present in breast milk.
Data related to the presence of raltegravir in breast milk are available from 1 case report following maternal use of raltegravir 800 mg once daily in combination with emtricitabine and tenofovir disoproxil which started prior to pregnancy and continued postpartum. Delivery was at 41 + 3 weeks gestation and maternal blood, breast milk, and infant blood were sampled at 4 and 8 months postpartum. The average breast milk concentration of raltegravir at 4 months postpartum was 0.66 mg/L (based on the AUC over 12 hours). The milk-to-plasma ratio was 0.46 (based on the AUC over 12 hours). The infant was exclusively breastfed during this time. Infant blood samples taken 4 and 8 months postpartum 4 hours after the maternal dose were below the limit of quantification for raltegravir (<0.01 mg/L) (Feiterna-Sperling 2020).
Maintaining maximum viral suppression during pregnancy and postpartum decreases but does not eliminate the risk of HIV transmission via breast milk. In addition, multiclass-resistant virus has been detected in breastfeeding infants who acquire HIV despite maternal therapy. In the United States, where formula is usually accessible, affordable, safe, and sustainable, and the risk of infant mortality due to diarrhea and respiratory infections is low, the Health and Human Services perinatal HIV guidelines do not recommend breastfeeding for patients with HIV when safer infant feeding options are available. Persons with HIV who maintain an undetectable viral load while taking antiretroviral therapy (ART) should evaluate infant feeding options (formula, banked donor milk, or breastfeeding) as part of a shared decision-making process (if breastfeeding is being considered, see guidelines for measures to reduce the risk of HIV transmission). When the HIV status at delivery is not known, breast milk may be expressed and stored until a negative test is available. If HIV infection is diagnosed after breastfeeding has been initiated, breastfeeding should be discontinued immediately. Breastfeeding is not recommended for persons with HIV who are not taking ART and/or who do not have sustained viral suppression.
Information is available for counseling and managing patients with HIV who are considering breastfeeding (1-888-448-8765). In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender-diverse people assigned female sex at birth (HHS [perinatal] 2023).
Some products may contain phenylalanine; avoid or use with caution in patient with phenylketonuria.
Viral load, CD4 count, signs of skin rash, signs/symptoms of depression and suicidal ideation
HIV occupational postexposure prophylaxis (PEP) (Kuhar, 2013): Documented HIV test (at baseline and 6 weeks, 12 weeks and 6 months after exposure); if confirmation that a fourth generation HIV p2 antigen-HIV antibody test is being used, monitor at baseline, 6 weeks and 4 months after exposure. CBC, renal and hepatic function assessments at baseline and 2 weeks after exposure (minimum recommendations, others dictated by clinical assessment)
Incorporation of viral DNA into the host cell’s genome is required to produce a self-replicating provirus and propagation of infectious virion particles. The viral cDNA strand produced by reverse transcriptase is subsequently processed and inserted into the human genome by the enzyme HIV-1 integrase (encoded by the pol gene of HIV). Raltegravir inhibits the catalytic activity of integrase, thus preventing integration of the proviral gene into human DNA.
Note: The pharmacokinetic profile of raltegravir in pediatric patients receiving recommended doses was similar to that observed in adults.
Absorption: Film-coated tablet (400 mg formulation): AUC increased twofold with high-fat meal; Chewable tablet: AUC decreased by ~6% with high-fat meal (not clinically significant); Oral suspension: The effect of food was not studied.
Protein binding: ~83%.
Metabolism: Primarily hepatic glucuronidation mediated by UGT1A1.
Bioavailability: 600 mg film-coated tablet, chewable tablet, and oral suspension have higher bioavailability compared to 400 mg film-coated tablet; dosage forms are not interchangeable.
Half-life elimination:
Neonates (GA ≥37 weeks):
PNA ≤48 hours: Single dose: Geometric mean range: 14.4 to 15.8 hours (Clarke 2020).
PNA 15 to 18 days: Geometric mean range: 2.5 to 2.9 hours (Clarke 2020).
Children ≥2 to <6 years: Median: 3.1 hours (Nachman 2014).
Children ≥6 years and Adolescents: Median range: 2.9 to 3.8 hours (Nachman 2014).
Adults: ~9 hours.
Time to peak, plasma: Film-coated tablet (400 mg formulation): ~3 hours; film-coated tablet (600 mg formulation): ~1.5 to 2 hours.
Excretion: Feces (~51%, as unchanged drug); urine (~32%; 9% as unchanged drug).
Pediatric: At birth, the enzyme responsible for the metabolism of raltegravir (UGT1A1) is low and raltegravir elimination in neonates may be prolonged. The activity of UGT1A1 increases rapidly over the first 4 to 6 weeks of life (HHS [perinatal] 2023). Raltegravir also competes with bilirubin for albumin protein-binding sites and may increase unconjugated bilirubin concentrations (HHS [perinatal] 2023).
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