Formulary
Raltegravir: Indications, Dosing, Side Effects and Interactions
Raltegravir is an inhibitor of HIV integrase.
MedNext Academy | 5 min read
Raltegravir: Indications, Dosing, Side Effects and Interactions
Raltegravir is an inhibitor of HIV integrase.
Drug action
Raltegravir is an inhibitor of HIV integrase.
Indications and dose
**HIV-1 infection (initiated by a specialist)**
- **Adult** (By Mouth Using Tablets): 400 mg twice daily, alternatively 1200 mg once daily, once daily dosing for use in patients who are treatment naive or virologically suppressed on an initial regimen of 400 mg twice daily-use 600 mg tablets only.
**HIV-1 infection (initiated by a specialist) for raltegravir**
- **Child (body-weight 25 kg and above)** (By mouth using tablets): 400 mg twice daily.
- **Child (body-weight 40 kg and above)** (By mouth using tablets): 1200 mg once daily, once daily dosing for use in patients who are treatment naive or virologically suppressed on an initial regimen of 400 mg twice daily-use 600 mg tablets only.
- **Child (body-weight 11-13 kg)** (By mouth using chewable tablets): 75 mg twice daily.
- **Child (body-weight 14-19 kg)** (By mouth using chewable tablets): 100 mg twice daily.
- **Child (body-weight 20-27 kg)** (By mouth using chewable tablets): 150 mg twice daily.
- **Child (body-weight 28-39 kg)** (By mouth using chewable tablets): 200 mg twice daily.
- **Child (body-weight 40 kg and above)** (By mouth using chewable tablets): 300 mg twice daily.
- **Neonate up to 7 days (body-weight 2 kg)** (By mouth using oral suspension): 4 mg once daily.
- **Neonate up to 7 days (body-weight 3 kg)** (By mouth using oral suspension): 5 mg once daily.
- **Neonate up to 7 days (body-weight 4 kg)** (By mouth using oral suspension): 7 mg once daily.
- **Neonate 7 days to 28 days (body-weight 2 kg)** (By mouth using oral suspension): 8 mg twice daily.
- **Neonate 7 days to 28 days (body-weight 3 kg)** (By mouth using oral suspension): 10 mg twice daily.
- **Neonate 7 days to 28 days (body-weight 4 kg)** (By mouth using oral suspension): 15 mg twice daily.
- **Child (body-weight 3 kg)** (By mouth using oral suspension): 25 mg twice daily.
- **Child (body-weight 4-5 kg)** (By mouth using oral suspension): 30 mg twice daily.
- **Child (body-weight 6-7 kg)** (By mouth using oral suspension): 40 mg twice daily.
- **Child (body-weight 8-10 kg)** (By mouth using oral suspension): 60 mg twice daily.
- **Child (body-weight 11-13 kg)** (By mouth using oral suspension): 80 mg twice daily.
- **Child (body-weight 14-19 kg)** (By mouth using oral suspension): 100 mg twice daily.
Cautions
Psychiatric illness (may exacerbate underlying illness including depression); risk factors for myopathy; risk factors for rhabdomyolysis
Contraindications
Pre-term neonates-no information available
Side effects
Common or very common Akathisia; appetite abnormal; asthenia; behaviour abnormal; depression; diarrhoea; dizziness; fever; gastrointestinal discomfort; gastrointestinal disorders; headaches; nausea; skin reactions; sleep disorders; vertigo; vomiting Uncommon Alopecia; anaemia; anxiety; arrhythmias; arthralgia; arthritis; body fat disorder; burping; cachexia; chest discomfort; chills; cognitive disorder; concentration impaired; confusion; constipation; diabetes mellitus; drowsiness; dry mouth; dyslipidaemia; dysphonia; erectile dysfunction; feeling jittery; glossitis; gynaecomastia; haemorrhage; hepatic disorders; hot flush; hyperglycaemia; hypersensitivity; hypertension; immune reconstitution inflammatory syndrome; increased risk of infection; lipodystrophy; lymph node abscess; lymphatic abnormalities; malaise; memory loss; menopausal symptoms; mood altered; myalgia; myopathy; nasal congestion; nephritis; nephrolithiasis; nerve disorders; neutropenia; nocturia; odynophagia; oedema; osteopenia; pain; palpitations; pancreatitis acute; polydipsia; psychiatric disorder; renal cyst; renal impairment; sensation abnormal; severe cutaneous adverse reactions (SCARs); skin papilloma; submandibular mass; suicidal behaviours; sweat changes; taste altered; tendinitis; thrombocytopenia; tinnitus; tremor; visual impairment; weight increased Frequency not known Osteonecrosis Side-effects, further information Rash occurs commonly. Discontinue if severe rash or rash accompanied by fever, malaise, arthralgia, myalgia, blistering, mouth ulceration, conjunctivitis, angioedema, hepatitis, or eosinophilia.
Interactions
**Severe interactions:**
- In some studies, co-administration of raltegravir 400 mg tablets twice daily with darunavir resulted in a modest but clinically insignificant decrease in darunavir plasma concentrations.
- Inhibitors of UGT1A1 Co-administration of atazanavir with raltegravir 1,200 mg once daily significantly increased plasma levels of raltegravir; therefore, co-administration of raltegravir 1,200 mg...
- Agents that increase gastric pH Population pharmacokinetic analysis from ONCEMRK (Protocol 292) showed that co-administration of raltegravir 1,200 mg once daily with PPIs or H 2 blockers did not...
- Nucleoside/tide reverse transcriptase inhibitors tenofovir disoproxil fumarate (raltegravir 400 mg twice daily) raltegravir AUC 49 % raltegravir C 12hr 3 % raltegravir C max 64 % (mechanism of...
- H 2 BLOCKERS AND PROTON PUMP INHIBITORS omeprazole (raltegravir 400 mg twice daily) raltegravir AUC 37 % raltegravir C 12hr 24 % raltegravir C max 51 % (increased solubility) No dose...
**Other interactions (35):**
- In vitro , raltegravir is a weak inhibitor of organic anion transporter (OAT) 1 (IC 50 of 109 M) and OAT3 (IC 50 of 18.8 M).
- Caution is recommended when co-administering raltegravir 1,200 mg once daily with sensitive OAT1 and/or OAT3 substrates.
- In vitro studies indicate that raltegravir is not a substrate of cytochrome P450 (CYP) enzymes, does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 or CYP3A, does not inhibit UDP...
- Based on in vitro and in vivo studies, raltegravir is eliminated mainly by metabolism via a UGT1A1-mediated glucuronidation pathway.
- Considerable inter- and intra-individual variability was observed in the pharmacokinetics of raltegravir.
- Effect of raltegravir on the pharmacokinetics of other medicinal products In drug interaction studies performed using raltegravir 400 mg twice daily, raltegravir did not have a clinically meaningful...
Pregnancy
Manufacturer advises avoid-toxicity in animal studies.
Hepatic impairment
Manufacturer advises caution in severe impairment (no information available), and in patients with chronic hepatitis B or C (consider interrupting or discontinuing treatment if impairment worsens; increased risk of hepatic side-effects).
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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