Rilpivirine (Oral)

Rilpirivine works through decreasing the level of HIV in the bloodstream. Although rilpivirine cannot be considered a cure for HIV, it may reduce the chances of a patient developing acquired immunodeficiency syndrome (AIDS) and serious HIV-related illnesses.

Overview

Rilpivirine is a drug that is used to treat human immunodeficiency virus (HIV) infection. HIV is the virus that leads to acquired immune deficiency syndrome (AIDS). Rilpivirine is typically given to those patients who have not previously received any form of HIV treatment.

The medicine cannot be considered as a cure, for either AIDS or HIV infection. It works by reducing the level of HIV in a patient's bloodstream and also helps to boost the immune system. Both actions of the drug can delay the onset of other conditions that are typically the result of HIV or AIDS such as life-threatening infections and cancer.

Patients who are prescribed rilpivirine may still continue to suffer from problems arising from AIDS and HIV disease and the medicine does not prevent the transmission of HIV to others, but taking the drug at the same time as introducing other lifestyle alterations and practising safe sex can significantly reduce the risk that the patient will spread the HIV virus to others.

Rilpivirine comes in a tablet form and is administered orally. Each dose is usually taken once a day with food.

Conditions Treated

  • HIV/AIDS

Type of Medicine

  • Non-nucleoside reverse transcriptase inhibitor (NNRTI).

Side Effects

Rilpivirine can lead to a range of minor side effects that will not typically lead to a patient needing to seek medical help. It is possible that a number of these side effects will fade as a patient's system becomes accustomed to the drug. If a patient is bothered by the side effects outlined below, or if they have any questions about side effects, they should speak to their medical professional, who will be able to offer advice and suggest preventative measures.

Patients may find that the minor side effects of this medicine can include a degree of abdominal and stomach pain, along with diarrhoea, nausea and vomiting. They may also experience abnormal or unusual dreams, reduced appetite, some periods of dizziness, tiredness or fatigue and excessive drowsiness. Headaches, skin rashes and nervousness can also occur when taking rilpivirine.

Rilpivirine can also have a number of more serious side effects. Some patients can experience severe skin reactions when taking this medicine and should seek urgent medical help if they begin to suffer from peeling or loose skin, sores, rashes, extensive or serious acne, lesions, blisters, chills or fever while on rilpivirine.

This drug has also been known to trigger a range of serious allergic reactions. These include anaphylaxis – a life-threatening condition that requires immediate medical intervention – and drug reaction with eosinophilia and systemic symptoms, which is also known as DRESS syndrome. Any patient on rilpivirine who develops a rash, hoarseness, a sensation of dizziness, breathing or swallowing difficulty or swelling of the limbs, face or mouth, should seek help, as these could be signs of an allergic reaction.

Rilpivirine patients who begin to experience depression or who have feelings of wanting to hurt themselves or others should report these thoughts or any troubling behaviour to a medical professional, particularly if these thoughts are new or worsen suddenly.

This drug may also lead to significant liver problems, which may be a particular risk for patients who have a history of hepatitis B or C infection. A patient taking rilpivirine should contact their doctor immediately if they notice symptoms such as dark urine, decreasing appetite, itching, nausea or vomiting, yellow eyes or skin, clay-coloured stools, swelling or nausea and vomiting, as these may indicate a liver-related problem.

It is also possible that taking rilpivirine might increase a patient's risk of contracting some infections or autoimmune disorders as it changes the way in which your immune system works. It is possible that these side effects may occur many months after the beginning of rilpivirine treatment, and patients who experience these symptoms should contact a doctor.

The side effects to look out for that could indicate a new infection or autoimmune disorder include swollen glands, stomach pain, weight loss, fever, night sweats and mouth sores. Pain when attempting to breathe, dry coughing, breathlessness, cold sores or sores in the genital or anal region may also be a sign of infection, as can a rapid heart rate, difficulty with balance and eye movement, anxiety or irritability and a feeling of prickliness. Rilpivirine patients may also experience some trouble with speaking and swallowing, severe pain in the lower back, some loss of bladder or bowel control, changes to their menstrual cycle, impotence or declining interest in sex, all of which may indicate infection or autoimmune problems.

In addition, rilpivirine can lead to an increase or decrease in the level of body fat. This may be an increase in fat located in the upper back and neck or in the stomach and chest area or a decrease in fat from the arms, face and legs. Patients who experience a significant change in body shape while taking rilpivirine should contact their medical practitioner.

Besides those side effects mentioned above, rilpivirine can also cause a feeling of abdominal and stomach fullness, behavioural changes, urine that is cloudy or bloody, indigestion and a general loss of pleasure and interest in life. These side effects should be referred to a doctor even if the patient feels able to cope with them.

Dosage

The recommended dose for this medicine will differ from patient to patient and will be determined by a patient's doctor.

When used to treat HIV infection, the standard dose for adults and children over twelve, weighing at least 35 kilograms is to take one 25 milligram tablet once per day. If rilpivirine is used in conjunction with the drug rifabutin, the dosage above may be increased to 50 milligrams per day but is likely to revert to 25 milligrams per day if rifabutin is stopped.

For patients with mild or moderate renal dysfunction, no dose adjustment is typically required, but patients with severe renal problems or end-stage renal disease should be monitored for side effects while taking the standard dose stated above. Patients suffering from mild to moderate liver problems will typically be prescribed the standard dose.

Patients should strictly adhere to the instructions given by their doctor on dosage. These should also be repeated on the label of the rilpivirine packaging. If the dose a patient has been prescribed differs from the standard dose listed above, patients should adhere to the prescribed dose.

Rilpivirine is generally taken in combination with other medicines. It is important for patients to take all their prescribed medications at the correct time of day as stated by their healthcare professional. This will ensure that the medications work at maximum effectiveness.

Rilpivirine is best taken at the same time as food. If a patient is also taking a stomach drug to combat heartburn or ulcers, such as cimetidine, Axid, Pepcid, Tagamet, famotidine, nizatidine, ranitidine, or Zantac, the heartburn medication should be ingested either twelve hours before or four hours after they take their rilpivirine. If a patient is using antacids containing aluminium, calcium or magnesium, these should be ingested at least two hours before or four hours after taking rilpivirine. The same timing precautions apply to patients taking didanosine, which should also be taken on an empty stomach.

Should a patient miss their dose of rilpivirine, they are advised to take the relevant dose as soon as possible, unless it is almost time for their next dose, in which case, they should skip a dose. Patients should not double their dose to make up for a missed dose.

It has not been possible to establish whether rilpivirine is safe or effective in patients under the age of twelve, so it is not recommended for use by anyone under that age.

Interactions

It is possible that some other medicines could interact with rilpivirine to cause unpleasant or dangerous effects. A number of drugs are known to have potentially serious interactions with rilpivirine. These include:

  • Carbamazepine
  • Oxcarbazepine
  • Phenobarbital
  • Phenytoin
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Esomeprazole
  • Lansoprazole
  • Omeprazole
  • Pantoprazole
  • Rabeprazole;
  • Dexamethasone;
  • St. John's wort
  • Delavirdine
  • Efavirenz
  • Etravirine
  • Nevirapine

If a patient is taking any of these medications while using rilpivirine they could be exposing themselves to the risk of serious medical issues or even death, and a patient's doctor may wish to alter their treatment programme if they use any of the medicines listed above.

In addition, patients should ensure that they inform their doctor or pharmacist about any other medications, either prescription or non-prescription, that they are using, as well as details of any vitamin or nutritional supplements, or herbal products, whether these are used before the course of rilpivirine starts or during rilpivirine treatment. In particular, it is important for patients to inform their doctor if they are using or are prescribed any of the following medications:

  • Fluconazole (Diflucan)
  • Itraconazole (Sporanox)
  • Ketoconazole (Nizoral)
  • Posaconazole (Noxafil)
  • Voriconazole (Vfend)
  • Other antifungal medications
  • Arsenic trioxide (Trisenox)
  • Cisapride
  • Carithromycin (Biaxin)
  • Dmperidone (Motilium)
  • Rythromycin (E-Mycin, Eryc, Ery-Tab, PCE, Pediazole)

Other medications that may have potentially significant interactions with rilpivirine include drugs that are used in the treatment of angina or irregular heart rhythms; medications for the treatment of malaria; a number of drugs that are typically used in the case of mental illness or Tourette's syndrome and the following medicines:

  • Methadone (Dolophine)
  • Moxifloxacin (Velox)
  • Other medications to treat HIV/AIDS
  • Pentamidine (NebuPent, Pentam)
  • Probucol (Lorelco)
  • Sparfloxacin (Zagam)
  • Telithromycin (Ketek)
  • Terfenadine (Seldane)
  • Troleandomycin (TAO)
  • Vandetanib (Zactima).

If a patient is prescribed or begins to take any of these drugs while taking rilpivirine, they should consult their doctor, who may wish to alter the doses of the other medications and where appropriate, monitor the patient for unwanted side effects.

Warnings

While taking rilpivirine, patients should ensure that they visit their doctor regularly to ensure that the drug is working effectively. This may involve a range of health checks, including blood tests, and questions about unwanted or potentially troublesome side effects.

It is important for patients to remember that this medicine does not remove the danger of transmitting HIV infection to other people, either through sexual contact or through contamination of the blood. While using rilpivirine, HIV may still be transmitted from or passed to other people via contaminated body fluids. This includes blood, semen or vaginal fluids.

Patients who are infected with HIV and taking rilpivirine are advised to continue to practice safe sex. This includes avoiding any form of sexual activity that involves or is likely to involve an exchange of body fluids with another person. If a patient using rilpivirine has sex with another partner, they should in all circumstances use a condom, and should only use condoms that are made from latex or polyurethane. Condoms should be used on every occasion when there is likely to be contact with blood, vaginal fluids or semen.

Patients on rilpivirine should also continue to avoid dangerous practices such as sharing needles or similar equipment or using dirty needles.

When taking HIV medications such as rilpivirine, a patient's immune system may begin to grow stronger and this can sometimes lead to their bodies beginning to fight infections that were previously hidden. These infections can include potentially serious types such as pneumonia, tuberculosis or herpes. It is also possible that patients on rilpivirine can develop a range of autoimmune disorders including Graves disease, polymyositis or Guillain-Barre syndrome as their immune system strengthens. It is important for all patients on rilpivirine to speak to their doctor as soon as they notice any significant changes in their health.

Rilpivirine can have a range of interactions with other drugs and can affect the results of some standard medical tests. It is therefore important for patients to inform their doctor if they are taking any other medication, whether this is prescription or non-prescription, and to tell other medical health care professionals that they are using rilpivirine before undergoing medical tests or treatments of any kind. If a patient is due to undergo dental surgery or any kind of surgical intervention while taking rilpivirine, it is important that they notify the medical health care professional who is supervising that treatment.

Patients taking rilpivirine should inform their doctor if they are pregnant, if they become pregnant, or if they are planning to become pregnant. Patients should not breastfeed if they are infected with HIV or are taking rilpivirine, and should inform their doctor if they are breastfeeding before being prescribed the drug.

Finally, patients who know or who suspect that they may be allergic to rilpivirine or any of the ingredients of rilpivirine should not take the drug and should notify their doctor of the relevant allergies. A pharmacist will also be able to provide a list of rilpivirine ingredients if a patient is concerned about potential allergic reactions.

Storage

Rilpivirine should be stored in the container in which it was prescribed and should be kept tightly closed at room temperature and away from conditions of excessive heat, light or moisture.

Patients should ensure that their rilpivirine is kept out of the sight and reach of young children as many containers used for this drug are not child-proof and can be easily opened by children. In order to ensure the safety of young children, rilpivirine should always be kept in a safe place, and if the drug container incorporates a safety cap, this should always be put back on when a patient has taken a dose of the drug.

Rilpivirine that is no longer required should be disposed of carefully to ensure that it cannot be ingested by pets, children or other people. It is not appropriate to dispose of unwanted medicine by flushing it down the toilet. Patients should speak to their local pharmacist or recycling organisation to find out the best way to dispose of the drug.

Summary

Rilpivirine is one of a class of drugs known as non-nucleoside reverse transcriptase inhibitors (NNRTIs). It effectively blocks the HIV virus and prevents it from growing and infecting other cells. It is typically prescribed for patients who have not previously taken HIV drugs.

Rilpivirine is an important component of many HIV treatment plans and is used with a number of other medications in order to help control a patient's HIV infection. By contributing to a reduction in the level of HIV in the bloodstream, it gives a patient's immune system a chance to work more effectively. As a result, rilpivirine can contribute towards a lower risk of developing serious HIV complications including new infections and cancer, and can make a significant contribution towards improving a patient's quality of life.

While it has a major role to play in HIV treatment, rilpivirine should not be considered a cure for HIV. Patients who have been prescribed rilpivirine should continue to take all necessary steps to ensure that they keep the risk of transmitting HIV to a minimum, including using effective barrier methods when taking part in sexual activity and not sharing personal items including toothbrushes, razors or needles.

Rilpivirine can also have a range of unpleasant and potentially life-threatening side effects and patients who are suffering from liver or renal conditions, who are pregnant or are planning to become pregnant, or who have an allergy to the drug or its ingredients should seek clarification and advice from their doctor before taking this medicine.

 

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Last Reviewed:
January 30, 2018
Last Updated:
January 27, 2018