Rilpivirine parenteral
- Drugs List
- Therapeutic Indications
- Dosage
- Administration
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Parenteral formulations of rilpivirine.
Drugs List
Therapeutic Indications
Uses
HIV infection-combined with other antiretrovirals
Treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA less than 50copies/ml) and on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with, agents of the NNRTI and INI class.
Dosage
Patients should be carefully selected who agree to the required injection schedule and should be counselled regarding the importance of adherence to scheduled dosing visits to help maintain viral suppression and reduce the risk of viral rebound and potential development of resistance associated with missed doses.
Following discontinuation of rilpivirine in combination with cabotegravir injection, it is important to follow an alternative, fully suppressive antiretroviral regimen no later than one month after the last 'every one month' injection of rilpivirine or two months after the last 'every two months' injection.
Adults
Oral lead in
25mg tablet, once daily for one month (at least 28 days).
Every one month dosing
Initial dose
900mg administered on the final day of oral lead in.
Maintenance dose
600mg once a month, patients may be given injections up to 7 days before or after the date of the monthly injection schedule.
Every two month dosing
Initial dose
900mg administered on the final day of oral lead in. A second 900mg is administered one month later, patients may be given the second injection up to 7 days before or after the date of the monthly injection schedule.
Maintenance dose
900mg every two months beginning at month 5, patients may be given injections up to 7 days before or after the date of every two months injection schedule.
Dosing recommendations when switching from monthly to every two months injections
900mg administered one month after the last 600mg injection, then 900mg every two months thereafter.
Dosing recommendations when switching from every two months to monthly injections
600mg administered two months after the last 900mg injection, then 600mg monthly thereafter.
Additional Dosage Information
Missed doses
Missed every one month injection
If a scheduled injection is missed by more than 7 days, oral treatment (25mg once daily) may be used to replace up to two consecutive monthly injection visits. The first dose of oral treatment should be taken one month (up to 7 days before or after) from the last injection doses. Once oral treatment is complete, injection dosing can re-initiate.
If the time since last receiving an injection of rilpivirine is less than or equal to two months ago, then continue with monthly 600mg injections as soon as possible.
If the time since last receiving an injection of rilpivirine is over two months ago then re-initiate with a 900mg dose, then continue to follow monthly 600mg schedule.
Missed every two months injection
If a scheduled injection is missed by more than 7 days, oral treatment (25mg once daily) may be used to replace one 'every two months' injection visit. The first dose of oral treatment should be taken one month (up to 7 days before or after) from the last injection doses. Once oral treatment is complete, injection dosing can re-initiate.
If the time since last receiving injection 2 (month 3) of rilpivirine is less than or equal to two months ago, then continue with 900mg injection as soon as possible and continue with every two month injection schedule.
If the time since last receiving injection 2 (month 3) of rilpivirine is over two months ago then re-initiate with a 900mg dose, followed by a second 900mg initiation injection one month later. Then follow the every two months injection schedule.
If the time since last receiving injection 3 or later (month 5 onwards) of rilpivirine is less than or equal to three months ago, then continue with 900mg injection as soon as possible and continue with every two month injection schedule.
If the time since last receiving injection 3 or later (month 5 onwards) of rilpivirine is over three months ago then re-initiate with a 900mg dose, followed by a second 900mg initiation injection one month later. Then follow the every two months injection schedule.
Administration
For intramuscular use only via the ventrogluteal or the dorsogluteal sites.
Rilpivirine and cabotegravir injections should be administered at separate gluteal injection sites during the same visit.
Contraindications
Children under 18 years
Breastfeeding
Hepatitis B
Severe hepatic impairment
Precautions and Warnings
Obese patients with a BMI equal or greater than 30kg/m2
Hepatitis C
HIV infection with A6 or A1 subtype
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
Autoimmune disorders can occur many months after initiation of treatment
Monitor hepatic function in patients with hepatitis C co-infection
Inflammatory symptoms should be evaluated and treated appropriately
May develop immune reactivation syndrome
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
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 jirovecii pneumonia. These reactions are usually observed within the first few weeks or months after treatment initiation.
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.
Residual concentrations of rilpivirine may remain in the systemic circulation for prolonged periods and should be considered upon discontinuation.
Pregnancy and Lactation
Pregnancy
Use rilpivirine with caution during pregnancy.
The manufacturer does not recommend using rilpivirine during pregnancy unless the expected benefit justifies the potential risk. At the time of writing there is limited published information regarding the parenteral use of rilpivirine during pregnancy, potential risks are unknown. However, data for oral use of rilpivirine during pregnancy indicates no malformative or foetal toxicity. Animal studies do not indicate reproductive toxicity. Rilpivirine may remain in systemic circulation for up to 4 years after discontinuation in some patients.
Lactation
Rilpivirine is contraindicated during breastfeeding.
Use of rilpivirine when breastfeeding is contraindicated by the manufacturer. Animal data reports levels of rilpivirine in the breast milk however presence in human milk and effects on exposed infants are unknown. Rilpivirine may be present in human breast milk for up to 4 years after discontinuation in some patients.
Side Effects
Abdominal discomfort
Abdominal pain
Alterations in pancreatic enzymes
Anxiety
Asthenia
Decrease in haemoglobin
Decreased appetite
Depressed mood
Depression
Diarrhoea
Dizziness
Dream abnormalities
Dry mouth
Elevated serum LDL cholesterol
Elevated serum lipase
Fatigue
Flatulence
Graves' disease
Headache
Hepatotoxicity
Immune Reactivation/Reconstitution Syndrome
Increase in plasma triglyceride concentration
Increase in serum transaminases
Increase in total cholesterol
Injection site reactions
Insomnia
Malaise
Myalgia
Nausea
Pyrexia
Rash
Reduced platelet count
Serum bilirubin increased
Sleep disturbances
Somnolence
Vasovagal syncope
Vomiting
Weight gain
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: December 2021
Reference Sources
Summary of Product Characteristics: Rekambys 900mg prolonged-release suspension for injection. Janssen-Cilag Ltd. Revised January 2021.
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