Raltegravir (Oral)

As an antiretroviral agent, raltegravir slows the reproduction of HIV and delays or reduces the chance of the onset of AIDS.

Overview

Raltegravir is an antiretroviral drug that, along with other medications, is used to treat human immunodeficiency virus (HIV) infection. Unfortunately, raltegravir does not cure HIV infections or AIDS or prevent transmission to others, but it does slow the reproduction of HIV and the destruction of the immune system. This may either delay or reduce the chances of HIV infection developing into the acquired immunodeficiency syndrome (AIDS) or cancer. Using raltegravir, along with positive changes in daily activities and safer sex practices, can elongate the life of people with HIV.

Conditions treated

  • Human immunodeficiency virus (HIV) infection
  • Acquired immunodeficiency syndrome (AIDS)

Type of Medicine

  • Antiretroviral agent

Side effects

There are many side effects that are possible for some patients to experience while taking raltegravir. Many side effects can be managed with either over-the-counter medications or help from a physician. Other less common side effects can be severe and should be treated as an emergency situation. The lists of side effects included here are not necessarily complete and not all side effects are experienced by patients. Should any condition become extremely painful or persistently bothersome, notify a physician immediately.

Severe side effects from the administration of raltegravir are included in the list below. If any of these symptoms occur, stop taking raltegravir and consult a physician immediately.

  • Kidney problems (change in amount or color of urine)
  • Persistent nausea and vomiting
  • Loss of appetite
  • Severe stomach and abdominal pain
  • Skin reactions (such as rash, blisters, mouth sores, peeling, etc.)
  • Eyelids, face, lips, hands, lower legs, and/or feet begin to swell

Less common or rare side effects that should also be noted are listed below. A physician should be contacted immediately if any of these side effects occur.

  • Stinging or burning skin
  • Fever or chills
  • Yellowed eyes and skin
  • General or unusual tiredness or weakness
  • Pain in the upper right stomach
  • A feeling of chest tightness
  • Increased thirst
  • Pain in the genitals or groin
  • Harsh back pain below the ribs
  • Pain in the lower back and/or side
  • Fast heartbeat
  • Painful blisters and/or cold sores on the genitals, nose, eyes or lips
  • Skin redness
  • Light-colored stools
  • Hoarseness
  • Trouble breathing and/or swallowing

Common, minor side effects may include a headache, nausea, diarrhea, heartburn, stomachache and trouble sleeping. The occurrence of these common and minor side effects do not necessarily need specific medical attention immediately, as they can occur as a patient's body is adjusting to the medication. If these side effects worsen or persist, contact a physician for help in managing these issues.

During the time the patient is taking raltegravir treatments for HIV, the immune system may gain strength and begin to fight other infections that were hidden in the body or become overactive. This may cause other symptoms in the patient, and a physician should be notified of any changing, new or worsening symptoms during treatment with raltegravir. These symptoms can include weight loss, tiredness, weakness, headaches, joint pain, limb numbness, vision changes, heat intolerance, nervousness, irritability, bulging eyes, overactive thyroid, or nerve problems. Symptoms may also shed light on a potential hidden autoimmune disorder such as Graves' disease, polymyositis, or Guillain-Barre syndrome. The condition that occurs when the immune system begins to recover after treatment with raltegravir is called immune reconstitution inflammatory syndrome (IRIS) and is a possible side effect of the administration of raltegravir.

If any of these side effects are experienced during the administration of raltegravir, the patient should contact a physician, as the pain might be managed through other medications or prescriptions. Other side effects not included in this list may be experienced by some patients and a physician should be contacted if the patient has any questions.

Dosage

The manufacturer of raltegravir recommends generic dosages as basic guidelines, but these recommendations may differ from the prescribed dosage by a physician. The dosage and frequency prescribed by a physician should be followed by generic guidelines from the manufacturer, and only the prescribed dosage from the physician should be taken.

In addition, any directions included on the label of the drug should be read and followed along with recommendations from the physician. Each patient has different needs and a physician can prescribe different dosages for each, which makes following the instructions given to a patient increasingly important. The physician is able to take the patient's specific medical conditions and needs into account when choosing a dosage. Any expired medication should be disposed of as recommended. If the physician recommends that a medication is discontinued, the patient should stop taking the medication, regardless if any is left.

Raltegravir is commonly used in combination with other antiretroviral agents for the treatment of HIV infection, and is the preferred regimen for HIV post-exposure prophylaxis. The treatment should begin as soon as possible after exposure to HIV infection. It should be reiterated that raltegravir is not a cure for HIV, but can significantly reduce the reproduction of the infection, and taking the drug soon after exposure has occurred is the best course of action.

The oral dosage can be dispensed as an oral suspension, a chewable tablet, or a film-coated tablet and may be taken with or without food. The chewable tablets can be swallowed whole or chewed, but the film-coated tablets must only be swallowed whole. The oral suspension should be kept in the container it is dispensed in, and the foil packet of powder should only be opened right before use. If a patient is using the oral suspension, pour the contents of the single-use packet into 5 millilitres of water and mix thoroughly. A dosing syringe comes with the packet and will measure the correct dose that has been prescribed. The dose in the syringe should be administered up to 30 minutes after mixing the suspension and any additional suspension left over should be disposed of as instructed by the pharmacist or physician. The oral suspension, chewable tablets and film-coated tablets may not be substituted for each other in any circumstance. If the patient has any questions regarding these types of oral medications, alert a physician.

For adults, a manufacturer recommended oral dosage is taken in film-coated tablets at 400 milligrams twice daily. If the exposure to HIV was not via sexual intercourse, but through health services, there is a duration for the administration of raltegravir that should be observed, and is usually 28 days.

For children, the dosage strength is based on body weight and there are three options for types of an oral dosage. The maximum dosage for children is 100 milligrams twice daily in oral suspension or 300 milligrams twice daily in chewable tablets. As with adults, if exposure of HIV is through other means and is caught right away, the administration duration of raltegravir is typically observed for 28 days.

Missing dosages should be avoided to maximize the efficacy of raltegravir. As the missed dosage is recognized, the missed dosage should be taken. If the patient recognizes the missed dosage when it is almost time to take the next dosage, the patient should continue to take the next dosage as scheduled. In this case, the missed dosage should be skipped. The patient should avoid taking double dosages, or two dosages at the same time. If any questions arise about a missed dosage or the timeliness of dosages, a physician should be consulted.

Side effects from overdosing on raltegravir include, but are not limited to, passing out or trouble breathing. If a patient recognizes that an overdose may have occurred or if a patient experiences any signs or symptoms as those above associated with an overdose, they need immediate medical attention. Immediate medical care can be achieved by dialling 911 or the Poison Control Center (1-800-222-1222).

Interactions

The desired effects of medications can be altered if some medications are taken in combination. Medication interactions can make any medications being taken ineffective, or potentially cause dangerous reactions. Due to potentially harmful drug interactions, each patient should keep a list of the medications that are currently being taken to give a physician at any given time. The medication list should include the name listed on the label of the medication, the type of medication or what it is used to treat, the frequency the medication is being taken and the dosage rate.

The list should not only include prescribed medications but any non-prescribed medications, like over-the-counter medications or vitamins. Even over-the-counter medications or vitamins counteract the desired results of the medications being prescribed. A physician can use this information to choose which medication to prescribe, change the treatment plan or dosage, and use known drug interactions to take precautions.

There are several known drug interactions with raltegravir. Using raltegravir in combination with the following medications is not generally recommended, but ultimately should be decided by the patient's physician. They can decide to change the patient's treatment medications or dosages to fit the best plan of treatment depending on the patient's medical condition.

  • Magnesium Carbonate
  • Aluminum Phosphate
  • Magnesium Trisilicate
  • Dihydroxyaluminum Aminoacetate
  • Aluminum Carbonate, Basic
  • Dihydroxyaluminum Sodium Carbonate
  • Fosamprenavir
  • Magaldrate
  • Aluminum Hydroxide
  • Orlistat
  • Magnesium Hydroxide
  • Amprenavir
  • Magnesium Oxide

The following medications have noted medical interaction with raltegravir and may increase the risk of side effects. Again, the decision to prescribe both raltegravir with any of these medications is a decision best made by a physician.

  • Etravirine
  • Omeprazole
  • Rifampin

Warnings

If the patient is aware of any allergies to any medications or any allergies with raltegravir or similar medications, they should inform their physician prior to using raltegravir or any other medication. The patient should also advise their physician of the medications they are taking as well as their medical history and current health problems.

If the patient is aware that they have any of the following conditions, it is crucial to consult a physician prior to taking raltegravir. Raltegravir may interfere with the current treatments of these existing conditions, or these conditions may be worsened with the administration of raltegravir. The list below considers significant medical conditions that are known to be affected or affect the use of raltegravir, but it is not all-inclusive. A physician should be alerted to any existing medical conditions the patient is known to have, regardless if it is on the list below.

  • Liver problems
  • History of rhabdomyolysis or myopathy (muscle disorders that can also cause kidney problems)
  • Increased levels of creatine kinase in the blood (an enzyme found largely in the heart, brain, and skeletal muscle)
  • Phenylketonuria, also known as PKU (the artificial sweetener in the chewable tablet of raltegravir contains aspartame, a source of phenylalanine)
  • Kidney dialysis treatment
  • Pregnancy or planning to become pregnant
  • Breastfeeding or planning to breastfeed
  • Use of hormone-based birth control

Also, a physician should be notified of the current treatment the patient uses to treat their HIV infection, as this medicine suite may need to be altered if raltegravir is to be prescribed.

All demographics have not had clinical studies completed to conclude the safety, efficacy, or potential negative risks of administering raltegravir. Due to a lack of adequate and controlled studies in some demographics, raltegravir should only be used if directed by a physician.

Other than animal studies, there have been no formal clinical studies to draw conclusions on the effects to pregnant women or the fetuses. It has also not been established if raltegravir is excreted in human breast milk. Any questions about the administration of raltegravir to pregnant or breastfeeding women should be directed to a knowledgeable physician. A physician can determine any potential benefits from administering the raltegravir and take precautions with any potential negative risks.

There are no formal clinical studies or reports to evaluate the effects, safety or efficacy in the case of administering raltegravir to children younger than four weeks of age.

Finally, clinical studies have also not been completed to show any geriatric-specific problems that would limit the usefulness of the drug in the elderly. For geriatric patients with age-related kidney, liver or heart problems, consult a physician, as dosages may need to be adjusted to compensate.

As noted, this medication will not prevent the transmission of HIV; HIV can be transmitted through sexual intercourse or exposure to HIV positive blood. Precautions such as barrier methods like latex condoms should be used in the practice of safe sex, regardless if the other person already has HIV. Syringes and needles used on a person with HIV should be disposed of responsibly to prevent giving HIV to others.

Storage

Medications need proper storage conditions to achieve the desired effects of the medication. A pharmacist or physician can direct the best way to store medication. All medications should be kept out of reach of children and pets. Others who have not been prescribed this medication should not take it. The accompanying information can also be used for more information on medication storage. Expired medication should not be taken, but disposed of as the efficacy of this medication is compromised. Take-back programs are the safest way to dispose of any medication but if no program exists, consult a physician for advice on disposal.

Raltegravir should be kept in a tight and closed container and preferably the container in which it was dispensed. The storage area should be at room temperature and away from excess heat and moisture. Avoid storing raltegravir in the bathroom to reduce exposure to moisture, and keep the desiccant in the medication if possible. If the seal has been broken or is missing, do not use raltegravir, as this may indicate the medication has been tampered with. If an oral suspension is chosen, keep the medication in the container it came in and do not open the foil packet of powder prior to use.

Summary

Raltegravir, in combination with other antiretroviral agents, can be a successful treatment for patients with HIV infection to reduce the reproduction of HIV in the body and slow the onset of AIDS. HIV and AIDS have a long, severe list of symptoms, and raltegravir does not eliminate these symptoms. In fact, raltegravir has a list of its own severe and bothersome side effects that could include skin conditions, severe abdominal pain, or kidney problems.

A physician should be notified if certain medical conditions like liver or kidney problems, PKU or muscle disorders or pregnancy exists prior to the administration of raltegravir, as it can worsen or interact with these conditions. Dosages, while ultimately determined by a physician, are usually taken twice daily and in children, based largely on body weight. Approximately 16 drug interactions exist with raltegravir, so the patient should always provide the physician with a current list of any and all medications being taken, including over-the-counter treatments and vitamins.

While raltegravir does not cure HIV infections, AIDS or prevent transmission to others, when taken correctly, raltegravir does slow the reproduction of HIV and the destruction of the immune system. This may either delay or reduce the chances of HIV infection developing into AIDS or cancer. Using raltegravir, along with positive changes in daily activities and safer sex practices, can give patients with HIV longer and healthier lives.

 

Resources
Last Reviewed:
January 31, 2018
Last Updated:
April 05, 2018