Drugs List

Therapeutic Indications

Uses

HIV infection-combined with other antiretrovirals

Contraindications

Children under 12 years
Breastfeeding
Galactosaemia
Severe hepatic impairment

Precautions and Warnings

Patients over 65 years
Glucose-galactose malabsorption syndrome
Hepatitis B
Hepatitis C
Lactose intolerance
Moderate hepatic impairment
Pregnancy
Severe renal impairment

Treatment does not prevent risk of transmission of HIV
Advise ability to drive/operate machinery may be affected by side effects
Must be used in combination with other antiretrovirals
Treatment should be initiated by doctor experienced in HIV management
Contains lactose
Indigestion remedies should not be taken at the same time
Autoimmune disorders can occur many months after initiation of treatment
Evaluate for physical signs of fat redistribution
Inflammatory symptoms should be evaluated and treated appropriately
Risk of developing opportunistic infections
Advise patient not to self medicate with antacids or acid suppressants
Advise patient not to take St John's wort concurrently
Avoid concurrent use of proton pump inhibitors

Genotypic resistance testing (when available) should be carried out prior to treatment.

Treatment with rilpivirine resulted in an early small increase of mean serum creatinine levels which remained stable over time and is not considered clinically relevant.

When combination antiretroviral therapy is initiated in HIV-infected patients with severe immune deficiency, an inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise. This can lead to the aggravation of symptoms or other serious clinical conditions such as cytomegalovirus retinitis, mycobacterial infections or Pneumocystis jiroveci pneumonia. These reactions are usually observed within the first few weeks or months after treatment initiation. Any inflammatory symptoms should be evaluated and treated appropriately.

The combination of rilpivirine and proton pump inhibitors should be avoided as co-administration is likely to result in the loss of therapeutic effect of rilpivirine.

The combination of rilpivirine and antacids should be used with caution. Antacids should only be administered either at least 2 hours before or at least 4 hours after rilpivirine.

The combination of rilpivirine and H2-receptor antagonists should be used with caution. H2-receptor antagonists should be administered at least 12 hours before or at least 4 hours after rilpivirine.

Pregnancy and Lactation

Pregnancy

Use rilpivirine with caution in pregnancy.

Rilpivirine should only be used in pregnant women if the potential benefits clearly outweigh the potential risks. Studies with rilpivirine in pregnant women have shown reduced exposure of the drug, and a subsequent increase in the risk of virological failure. Viral load should be closely monitored in these patients.

It is not known whether rilpivirine crosses the human placenta, but its molecular weight and long elimination terminal half-life suggest placental transfer may occur. No evidence of increased teratogenicity has been found in studies in rats and rabbits. A moderate amount of data indicate no malformative or feto/neonatal toxicity of rilpivirine.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Rilpivirine is contraindicated in breastfeeding.

It is not known whether rilpivirine is excreted in human milk. Rilpivirine is excreted in the milk of rats. Because of both the potential for HIV transmission and the potential for adverse reactions in breastfed infants, mothers should be instructed not to breastfeed if they are receiving rilpivirine.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Abdominal discomfort
Abdominal pain
Alterations in pancreatic enzymes
Autoimmune hepatitis
Decrease in haemoglobin
Decreased appetite
Depressed mood
Depression
Dizziness
Dream abnormalities
Dry mouth
Elevated serum LDL cholesterol
Elevated serum lipase
Fatigue
Graves' disease
Headache
Immune Reactivation/Reconstitution Syndrome
Increase in plasma triglyceride concentration
Increase in serum transaminases
Increase in total cholesterol
Insomnia
Lipodystrophy
Nausea
Rash
Reduced platelet count
Serum bilirubin increased
Sleep disturbances
Somnolence
Vomiting
White blood cell count decreased

Presentation

Oral formulation of rilpivirine

Drugs List

Therapeutic Indications

Uses

HIV infection-combined with other antiretrovirals

Dosage

Adults

Elderly

Children

Additional Dosage Information

Contraindications

Children under 12 years
Breastfeeding
Galactosaemia
Severe hepatic impairment

Precautions and Warnings

Patients over 65 years
Glucose-galactose malabsorption syndrome
Hepatitis B
Hepatitis C
Lactose intolerance
Moderate hepatic impairment
Pregnancy
Severe renal impairment

Treatment does not prevent risk of transmission of HIV
Advise ability to drive/operate machinery may be affected by side effects
Must be used in combination with other antiretrovirals
Treatment should be initiated by doctor experienced in HIV management
Contains lactose
Indigestion remedies should not be taken at the same time
Autoimmune disorders can occur many months after initiation of treatment
Evaluate for physical signs of fat redistribution
Inflammatory symptoms should be evaluated and treated appropriately
Risk of developing opportunistic infections
Advise patient not to self medicate with antacids or acid suppressants
Advise patient not to take St John's wort concurrently
Avoid concurrent use of proton pump inhibitors

Genotypic resistance testing (when available) should be carried out prior to treatment.

Treatment with rilpivirine resulted in an early small increase of mean serum creatinine levels which remained stable over time and is not considered clinically relevant.

When combination antiretroviral therapy is initiated in HIV-infected patients with severe immune deficiency, an inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise. This can lead to the aggravation of symptoms or other serious clinical conditions such as cytomegalovirus retinitis, mycobacterial infections or Pneumocystis jiroveci pneumonia. These reactions are usually observed within the first few weeks or months after treatment initiation. Any inflammatory symptoms should be evaluated and treated appropriately.

The combination of rilpivirine and proton pump inhibitors should be avoided as co-administration is likely to result in the loss of therapeutic effect of rilpivirine.

The combination of rilpivirine and antacids should be used with caution. Antacids should only be administered either at least 2 hours before or at least 4 hours after rilpivirine.

The combination of rilpivirine and H2-receptor antagonists should be used with caution. H2-receptor antagonists should be administered at least 12 hours before or at least 4 hours after rilpivirine.

Pregnancy and Lactation

Pregnancy

Use rilpivirine with caution in pregnancy.

Rilpivirine should only be used in pregnant women if the potential benefits clearly outweigh the potential risks. Studies with rilpivirine in pregnant women have shown reduced exposure of the drug, and a subsequent increase in the risk of virological failure. Viral load should be closely monitored in these patients.

It is not known whether rilpivirine crosses the human placenta, but its molecular weight and long elimination terminal half-life suggest placental transfer may occur. No evidence of increased teratogenicity has been found in studies in rats and rabbits. A moderate amount of data indicate no malformative or feto/neonatal toxicity of rilpivirine.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Rilpivirine is contraindicated in breastfeeding.

It is not known whether rilpivirine is excreted in human milk. Rilpivirine is excreted in the milk of rats. Because of both the potential for HIV transmission and the potential for adverse reactions in breastfed infants, mothers should be instructed not to breastfeed if they are receiving rilpivirine.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Abdominal discomfort
Abdominal pain
Alterations in pancreatic enzymes
Autoimmune hepatitis
Decrease in haemoglobin
Decreased appetite
Depressed mood
Depression
Dizziness
Dream abnormalities
Dry mouth
Elevated serum LDL cholesterol
Elevated serum lipase
Fatigue
Graves' disease
Headache
Immune Reactivation/Reconstitution Syndrome
Increase in plasma triglyceride concentration
Increase in serum transaminases
Increase in total cholesterol
Insomnia
Lipodystrophy
Nausea
Rash
Reduced platelet count
Serum bilirubin increased
Sleep disturbances
Somnolence
Vomiting
White blood cell count decreased

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: August 2015

Reference Sources

Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 10th edition (2015) ed. Briggs, G., Freeman, R. Wolters Kluwer Health, Philadelphia.

Joint Formulary Committee. British National Formulary(online) London: BMJ Group and Pharmaceutical Press. Accessed on 10 August 2015.

Summary of Product Characteristics: Edurant 25mg film-coated tablets. Janssen-Cilag Ltd. Revised December 2019.