II. Class
- Anti-retroviral agent
- Integrase Strand Transfer Inhibitor
III. Mechanism
- Integrase Strand Transfer Inhibitor prevents viral DNA from integrating into host DNA
- Blocks the integrase enzyme
IV. Indications
- Anti-retroviral naive patients
- Anti-retroviral experienced patients
V. Preparations
- Bictegravir (Biktarvy)
- Dolutegravir (Tivacay)
- Raltegravir (Isentress)
- Dose: One 400 mg tablet orally twice daily
VI. Efficacy
- Drug resistance is common
VII. Adverse Effects: Raltegravir
- Diarrhea
- Nausea
- Headache
- Serum Creatinine phosphokinase (CPK) increases
- Myopathy
- Rhabdomyolysis
- Insomnia
VIII. Drug Interactions
- Typically fewer Drug Interactions than other Anti-Retroviral Agents
- Phenytoin
- Rifampin
- St John's Wort
- Avoid taking at the same time as calcium, Magnesium, aluminum and iron containing agents
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| isentress (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| ISENTRESS 400 MG TABLET | $22.34 each | |
| ral (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| RALOXIFENE HCL 60 MG TABLET | Generic | $1.24 each |
Ontology: Integrase Inhibitors (C0376601)
| Definition (MSH) | Compounds which inhibit or antagonize biosynthesis or actions of integrase. |
| Concepts | Pharmacologic Substance (T121) , Biologically Active Substance (T123) |
| MSH | D019429 |
| SnomedCT | 427965001, 428617003 |
| English | Inhibitors, Integrase, INTEGRASE INHIB, INHIB INTEGRASE, Integrase strand transfer inhibitor (substance), Integrase inhibitor, Integrase strand transfer inhibitor (product), Integrase strand transfer inhibitor, Integrase Inhibitors, integrase inhibitors, integrase inhibitor |
| French | Inhibiteurs de l'intégrase |
| Swedish | Integrashämmare |
| Czech | integrasa - inhibitory |
| Finnish | Integraasinestäjät |
| Russian | INTEGRAZY INGIBITORY, ИНТЕГРАЗЫ ИНГИБИТОРЫ |
| Spanish | inhibidor de la integrasa, inhibidor de la transferencia de cadenas por la integrasa (sustancia), inhibidor de la transferencia de cadenas por la integrasa, inhibidor de la transferencia de cadenas por la integrasa (producto), Inhibidores de Integrasa |
| Polish | Inhibitory integrazy |
| Japanese | インテグラーゼ阻害剤, インテグラーゼインヒビター |
| German | Integrase-Inhibitoren |
| Italian | Inibitori dell'integrasi |
| Portuguese | Inibidores de Integrase |
Ontology: raltegravir (C1871526)
| Definition (NCI) | A small molecule with activity against human immunodeficiency virus (HIV). Raltegravir is an integrase inhibitor that blocks the integration of the viral genome into the host DNA, a critical step in the pathogenesis of HIV. |
| Concepts | Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114) |
| MSH | C507898 |
| SnomedCT | 429707008, 429368003 |
| LNC | LP102418-3, MTHU036457 |
| English | Raltegravir (substance), Raltegravir, Raltegravir (product), N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide, raltegravir, RALTEGRAVIR |
| Spanish | raltegravir (producto), raltegravir, raltegravir (sustancia) |
Ontology: dolutegravir (C3253985)
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | C562325 |
| LNC | LP157327-0, MTHU045713 |
| English | dolutegravir, (4R,9aS)-5-hydroxy-2-methyl-6,10-dioxo-3,4,6,9,9a,10-hexahydro-2H-1-oxa-4a,8a-diaza-anthracene-7-carboxylic acid- 2,4 difluorobenzylamide, 2H-Pyrido(1',2':4,5)pyrazino(2,1-b)(1,3)oxazine-9- carboxamide, N-((2,4-difluorophenyl)methyl)-3,4,6,8,12,12a- hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, (4R,12aS)-, Dolutegravir, antiretrovirals dolutegravir, dolutegravir (medication), DOLUTEGRAVIR |
