Description

Simple

A medication used to treat HIV infections.

Clinical

An antiretroviral agent used for the treatment of HIV infections in conjunction with other antiretrovirals.

Overview

Raltegravir is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval.

Pharmacology

Indication

For the treatment of HIV-1 infection in conjunction with other antiretrovirals.

Pharmacodynamic

Information currently not available.

Mechanism of action

Raltegravir inhibits HIV integrase to prevent the viral genome being incorporated into the human genome. Raltegravir is primarily metabolized by glucuronidation.

Absorption

Absorbed from the gastrointestinal tract.

Protein binding

83%

Volume of distribution

Approximately 83% bound to human plasma protein and is minimally distributed into red blood cells (blood-to-plasma partitioning ratio of 0.6).

Clearance

The major mechanism of clearance of raltegravir in humans is glucuronidation mediated by UGT1A1, the renal clearance of unchanged drug is a minor pathway of elimination of raltegravir (9% of total dose).

Half life

9 hours

Route of elimination

Feces and urine

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Hypersensitivity:
    • false
  • Regions: US

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Acetylcysteine zinc
Acetylcysteine zinc can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acipimox
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Raltegravir is combined with Acipimox.
Adenine
The metabolism of Raltegravir can be decreased when combined with Adenine.
Adenovirus type 7 vaccine live
The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Raltegravir.
Alendronic acid
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Alendronic acid is combined with Raltegravir.
Almasilate
The serum concentration of Raltegravir can be decreased when it is combined with Almasilate.
Aloglutamol
The serum concentration of Raltegravir can be decreased when it is combined with Aloglutamol.
Aluminium
The serum concentration of Raltegravir can be decreased when it is combined with Aluminium.
Aluminium acetoacetate
The serum concentration of Raltegravir can be decreased when it is combined with Aluminium acetoacetate.
Aluminium clofibrate
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Raltegravir is combined with Aluminium clofibrate.
Aluminium glycinate
The serum concentration of Raltegravir can be decreased when it is combined with Aluminium glycinate.
Aluminium phosphate
The serum concentration of Raltegravir can be decreased when it is combined with Aluminium phosphate.
Aluminum cation
The serum concentration of Raltegravir can be decreased when it is combined with Aluminum cation.
Aluminum chloride
Aluminum chloride can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide
The serum concentration of Raltegravir can be decreased when it is combined with Aluminum hydroxide.
Aluminum sulfate
Aluminum sulfate can cause a decrease in the absorption of Raltegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Amiodarone
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Amiodarone is combined with Raltegravir.
Amitriptyline
The metabolism of Raltegravir can be decreased when combined with Amitriptyline.
Amphotericin B
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Amphotericin B is combined with Raltegravir.
Amprenavir
The serum concentration of Raltegravir can be decreased when it is combined with Amprenavir.
13 References
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  2. 2 . Barau C, Furlan V, Yazdanpanah Y, Fagard C, Molina JM, Taburet AM, Barrail-Tran A: Characterization of binding of raltegravir to plasma proteins. Antimicrob Agents Chemother. 2013 Oct;57(10):5147-50. doi: 10.1128/AAC.00625-13. Epub 2013 Jul 15.PubMed: 23856784
  3. 3 . Arora R, de Beauchene IC, Polanski J, Laine E, Tchertanov L: Raltegravir flexibility and its impact on recognition by the HIV-1 IN targets. J Mol Recognit. 2013 Sep;26(9):383-401. doi: 10.1002/jmr.2277.PubMed: 23836466
  4. 4 . Eron JJ, Cooper DA, Steigbigel RT, Clotet B, Gatell JM, Kumar PN, Rockstroh JK, Schechter M, Markowitz M, Yeni P, Loutfy MR, Lazzarin A, Lennox JL, Strohmaier KM, Wan H, Barnard RJ, Nguyen BY, Teppler H: Efficacy and safety of raltegravir for treatment of HIV for 5 years in the BENCHMRK studies: final results of two randomised, placebo-controlled trials. Lancet Infect Dis. 2013 Jul;13(7):587-96. doi: 10.1016/S1473-3099(13)70093-8. Epub 2013 May 7.PubMed: 23664333
  5. 5 . Winston A, Mallon PW, Boffito M: The clinical pharmacology of antiretrovirals in development. Expert Opin Drug Metab Toxicol. 2006 Jun;2(3):447-58.PubMed: 16863445
  6. 6 . O'Neal R: MK-0518 and GS-9137: two promising integrase inhibitors in the pipeline. BETA. 2006 Summer;18(4):13-6.PubMed: 17019786
  7. 7 . James JS: Integrase inhibitor MK-0518: Merck opens expanded-access program. AIDS Treat News. 2006 Jul-Sep;(419):5.PubMed: 17096488
  8. 8 . Markowitz M, Morales-Ramirez JO, Nguyen BY, Kovacs CM, Steigbigel RT, Cooper DA, Liporace R, Schwartz R, Isaacs R, Gilde LR, Wenning L, Zhao J, Teppler H: Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr. 2006 Dec 15;43(5):509-15.PubMed: 17133211
  9. 9 . Colquitt AR, Pham PA: Expanded access drug profile: raltegravir (RAL, MK-0518). Hopkins HIV Rep. 2007 Jan;19(1):11-2.PubMed: 17569171
  10. 10 . Authors unspecified: Raltegravir demonstrates potency. AIDS Patient Care STDS. 2007 Apr;21(4):288.PubMed: 17506141
  11. 11 . Authors unspecified: Anti-HIV agents. Raltegravir--other issues. TreatmentUpdate. 2007 Feb;19(2):9-10.PubMed: 17447317
  12. 12 . Authors unspecified: Anti-HIV agents. Integrase inhibitor raltegravir makes its mark. TreatmentUpdate. 2007 Feb;19(2):8-9.PubMed: 17447316
  13. 13 . Cahn P, Sued O: Raltegravir: a new antiretroviral class for salvage therapy. Lancet. 2007 Apr 14;369(9569):1235-6.PubMed: 17434380