Mr. Ibrahem/Raltegravir
Clinical data
Trade namesIsentress
AHFS/Drugs.comMonograph
MedlinePlusa608004
License data
Routes of
administration
oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability60%(FDA)
Protein binding83%
MetabolismHepatic (UGT1A1)
Elimination half-life9 hours
Excretionfeces and urine
Identifiers
  • N-(4-Fluorobenzyl)-5-hydroxy-1-methyl-2-(2-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}-2-propanyl)-6-oxo-1,6-dihydro-4-pyrimidinecarboxamide
Chemical and physical data
FormulaC20H21FN6O5
Molar mass444.423 g·mol−1
3D model (JSmol)
  • Cc1nnc(o1)C(=O)NC(C)(C)C\3=N\C(C(=O)NCc2ccc(F)cc2)=C(\O)C(=O)N/3C
  • InChI=1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30) checkY
  • Key:CZFFBEXEKNGXKS-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Raltegravir (RAL), sold under the brand name Isentress, is an antiretroviral medication used, together with other medication, to treat HIV/AIDS.[2] It may also be used, as part of post exposure prophylaxis, to prevent HIV infection following potential exposure.[3] It is taken by mouth.[2]

Common side effects include trouble sleeping, feeling tired, nausea, high blood sugar, and headaches.[3] Severe side effects may include allergic reactions including Stevens–Johnson syndrome, muscle breakdown, and liver problems.[3] It is unclear if use during pregnancy or breastfeeding is safe.[3] Raltegravir is an HIV integrase strand transfer inhibitor which blocks the functioning of HIV integrase which is needed for viral replication.[3]

Raltegravir was approved for medical use in the United States in 2007.[3] It is on the World Health Organization's List of Essential Medicines.[4] In the United Kingdom it costs the NHS about 472 pounds per month.[2] Lamivudine/raltegravir, a combination with lamivudine, is also available.[3]

References

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  1. ^ Cite error: The named reference who was invoked but never defined (see the help page).
  2. ^ a b c British national formulary : BNF 69 (69 ed.). British Medical Association. 2015. p. 429. ISBN 9780857111562.
  3. ^ a b c d e f g "Raltegravir Potassium". The American Society of Health-System Pharmacists. Archived from the original on 11 December 2017. Retrieved 8 December 2017.
  4. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.