Raltegravir

Drug Forms:
• Raltegravir tablets (below)
• Raltegravir Oral tablet

Español:
• Tableta oral de raltegravir
• Raltegravir, Tableta oral

Raltegravir tablets

What is raltegravir?

RALTEGRAVIR is an antiretroviral drug. It is used with other medicines to treat some strains of HIV. This medicine is not a cure for HIV. It will not stop the spread of HIV to others.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• liver disease
• an unusual or allergic reaction to raltegravir, other medicines, lactose, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. You can take it with or without food. Do not cut, crush, or chew this medicine. Take your medicine at regular intervals. Do not take your medicine more often than directed. For your anti-HIV therapy to work as well as possible, take each dose exactly as prescribed. Do not skip doses or stop your medicine even if you feel better. Skipping doses may make the HIV virus resistant to this medicine and other medicines. Do not stop taking except on your doctor's advice.

A patient information sheet for the product will be given with each prescription and refill. Read this sheet carefully each time. The sheet may change frequently.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with raltegravir?

• medicines for cholesterol like atorvastatin
• rifampin

Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking raltegravir?

Visit your doctor or health care professional for regular check ups. Discuss any new symptoms with your doctor. You will need to have important blood work done while on this medicine.

HIV is spread to others through sexual or blood contact. Talk to your doctor about how to stop the spread of HIV.

What side effects might I notice from taking raltegravir?

Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• breathing difficulties
• dark urine
• fever or chills, sore throat
• increased hunger or thirst
• muscle pain or weakness
• trouble passing urine or change in the amount of urine
• unusual bleeding or bruising
• unusually weak or tired
• weight gain around waist, back, or thinning of face, arms, legs

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• diarrhea
• dizziness
• headache
• nausea, vomiting
• stomach pain

Where can I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Raltegravir

Systematic (IUPAC) name
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
Identifiers
CAS number	871038-72-1
ATC code	J05AX08
PubChem	11598201
Chemical data
Formula	C20H21FN6O5
Mol. mass	444.42 g/mol
Pharmacokinetic data
Bioavailability	?
Protein binding	83%
Metabolism	Hepatic (UGT1A1)
Half life	9 hours
Excretion	feces and urine
Therapeutic considerations
Licence data	EU EMEA:link, US FDA:link
Pregnancy cat.	C(US)
Legal status	POM(UK) ℞-only(US)
Routes	oral

Raltegravir (MK-0518, brand name Isentress) 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) in October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval.^[1][2]

Contents 1 Mechanism 2 Dosage 3 Indications 4 Efficacy 5 Research 6 References 7 External links

Mechanism

Raltegravir targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV. The drug is metabolized away via glucuronidation.^[3]

Dosage

This section does not cite any references or sources. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (November 2009)

Isentress tablets

Raltegravir is taken orally twice daily.^[2] Doses of 200, 400, and 600 mg have been studied.

At the 2007 Conference on Retroviruses and Opportunistic Infections, researchers presented Phase III data showing that 77% of patients taking the 400 mg dose of raltegravir plus other antiretroviral drugs reached HIV viral loads below 400 copies, nearly twice as many compared with a control group.

Indications

This section does not cite any references or sources. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (November 2009)

Raltegravir is approved only for use in individuals whose infection has proven resistant to other HAART drugs^[2]. As with any HAART medication, raltegravir is unlikely to show durability if used as monotherapy.

Efficacy

In a study of the drug as part of combination therapy, raltegravir exhibited potent and durable antiretroviral activity similar to that of efavirenz at 24 and 48 weeks but achieved HIV-1 RNA levels below detection at a more rapid rate. After 24 and 48 weeks of treatment, raltegravir did not result in increased serum levels of total cholesterol, low-density lipoprotein cholesterol, or triglycerides.^[4][5]

Research

Raltegravir significantly alters HIV viral dynamics and decay and further research in this area is ongoing. In clinical trials patients taking raltegravir achieved viral loads less than 50 copies per millitre sooner than those taking similarly potent Non-nucleoside Reverse Transcriptase Inhibitors or Protease Inhibitors. This statistically significant difference in viral load reduction has caused some HIV researchers to begin questioning long held paradigms about HIV viral dynamics and decay.^[6] Research into raltegravir's ability to affect latent viral reservoirs and possibly aid in the eradication of HIV is currently ongoing.^[7]

Research results were published in the New England Journal of Medicine on July 24, 2008. The authors concluded that "raltegravir plus optimized background therapy provided better viral suppression than optimized background therapy alone for at least 48 weeks." ^[8]

References

This article's citation style may be unclear. The references used may be made clearer with a different or consistent style of citation, footnoting, or external linking. (April 2008)

• Savarino A (December 2006). "A historical sketch of the discovery and development of HIV-1 integrase inhibitors". Expert Opin Investig Drugs 15 (12): 1507–22. doi:10.1517/13543784.15.12.1507. PMID 17107277. 

1. ^ "[www.fda.gov/ForConsumers/ByAudience/ForPatientAdvocates/HIVandAIDSActivities/ucm124040.htm FDA approval of Isentress (raltegravir)]". U.S. Food and Drug Administration (FDA). June 25, 2009. www.fda.gov/ForConsumers/ByAudience/ForPatientAdvocates/HIVandAIDSActivities/ucm124040.htm. Retrieved 2009-11-15. 
2. ^ ^{a b c} "[www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022145_Isentress.cfm Isentress Drug Approval Package]". U.S. Food and Drug Administration (FDA). February 22, 2008. www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022145_Isentress.cfm. Retrieved 2009-11-15. 
3. ^ HIV Antiretroviral Agents in Development
4. ^ Markowitz M, Nguyen BY, Gotuzzo E, et al. (2007). "Rapid and durable antiretroviral effect of the HIV-1 Integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled study". J. Acquir. Immune Defic. Syndr. 46 (2): 125–33. doi:10.1097/QAI.0b013e318157131c. PMID 17721395. http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?doi=10.1097/QAI.0b013e318157131c. 
5. ^ Stephenson J (2007). "Researchers buoyed by novel HIV drugs: will expand drug arsenal against resistant virus". JAMA 297 (14): 1535–6. doi:10.1001/jama.297.14.1535. PMID 17426263. http://jama.ama-assn.org/cgi/pmidlookup?view=long&pmid=17426263. 
6. ^ Faster Viral Decay With Raltegravir
7. ^ ClinicalTrials.gov NCT00554398 Impact of MK-0518 (Raltegravir) Intensification on HIV-1 Viral Latency in Patients With Previous Complete Viral Suppression
8. ^ Steigbigel RT, Cooper DA, Kumar PN, et al. (July 2008). "Raltegravir with optimized background therapy for resistant HIV-1 infection". N. Engl. J. Med. 359 (4): 339–54. doi:10.1056/NEJMoa0708975. PMID 18650512. http://content.nejm.org/cgi/content/abstract/359/4/339. 

External links

• Manufacturer's website
• MK-0518 at Aidsmedscom
• Integrase Inhibitor Raltegravir (MK-0518) Doubles HIV Suppression in Treatment-Experienced Patients (Aidsmap 28 February 2007)
• RMK-0518 Abstract from CROI 2007
• Interim Results From Phase II Study Of MK-0518
• World patent covering the potassium salt
• Raltegravir Pharmacokinetics

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