Drugs List

Therapeutic Indications

Uses

Treatment of HIV infected adults

Adults infected with human immunodeficiency virus-1 (HIV-1) without present or past evidence of viral resistance to the integrase inhibitor class, emtricitabine or tenofovir.

Contraindications

Children under 18 years
Breastfeeding
Renal impairment - creatinine clearance below 30 ml/minute
Severe hepatic impairment

Precautions and Warnings

Hepatic impairment
Hepatitis B
Hepatitis C
Pregnancy

Discontinuation of treatment may exacerbate hepatitis in HBV co-infection
Monitor HBV levels during and after treatment in patients with co-infection
Treatment does not prevent risk of transmission of HIV
Advise ability to drive/operate machinery may be affected by side effects
Treatment should be initiated by doctor experienced in HIV management
Autoimmune disorders can occur many months after initiation of treatment
Blood lipid and glucose levels may increase requiring treatment
Monitor closely patient with pre-existing hepatic impairment
On discontinuation, may cause recurrence of hepatitis B
Advise patient to seek medical advice if joint aches or pain occur
Advise patient to seek medical advice if movement becomes difficult
Inflammatory symptoms should be evaluated and treated appropriately
May cause weight gain
May develop immune reactivation syndrome
Neonate exposed in utero: Risk of mitochondrial dysfunction
Prolonged use may lead to nephrotoxicity
Discontinue if hepatic function deteriorates in pts with hepatic impairment
Advise patient not to take St John's wort concurrently
Advise to avoid antacids/mineral supplements 2 hours before or after dose
Take another dose if vomiting occurs within one hour

Patients co-infected with hepatitis B or C are at an increased risk of severe, potentially fatal hepatic adverse events. When discontinuing treatment with bictegravir with emtricitabine and tenofovir alafenamide in patients co-infected with hepatitis B and HIV, monitor closely for several months after treatment.

Blood lipid and glucose levels may increase during antiretroviral therapy. This may be linked to disease control and lifestyle. Refer to established HIV treatment guidelines for monitoring and manage lipid and glucose level disorders as appropriate.

When combination antiretroviral therapy is initiated in HIV-infected patients with severe immune deficiency, an inflammatory reaction to asymptomatic or residual opportunist 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. Any inflammatory symptoms should be evaluated and treated appropriately.

Treatment regimens containing nucleoside or nucleotide analogues have been reported to cause mitochondrial dysfunction in HIV-negative infants exposed in utero and/or post-natally. Adverse reactions such as haematological (anaemia, neutropenia), metabolic (hyperlactataemia, hyperlipasemia) and neurological (hypertonia, convulsions, abnormal behaviour) have been reported. Consider in children exposed to nucleoside or nucleotide analogues in utero (including HIV-negative infants) and who present with neurological symptoms or severe clinical findings of unknown cause.

Bictegravir with emtricitabine and tenofovir alafenamide should be avoided but may be used in adults with end stage renal disease on chronic haemodialysis if the potential benefits outweigh the potential risks. In a study of emtricitabine and tenofovir alafenamide in combination with elvitegravir and cobicistat as a fixed-dose combination tablet in HIV-1 infected adults with end stage renal disease on chronic haemodialysis, efficacy was maintained through 96 weeks but emtricitabine exposure was significantly higher than in patients with normal renal function. No additional adverse reactions were identified, the implications of increased emtricitabine exposure remain uncertain.

Pregnancy and Lactation

Pregnancy

Use bictegravir with emtricitabine and tenofovir alafenamide with caution during pregnancy.

The manufacturer advises bictegravir with emtricitabine and tenofovir alafenamide may be used only if the benefit justifies the potential risk to the foetus. Animal studies have shown no increased risk of teratogenic or developmental effects. The potential risk in humans is unknown.

Lactation

Bictegravir with emtricitabine and tenofovir alafenamide is contraindicated during breastfeeding.

Use of bictegravir with emtricitabine and tenofovir alafenamide is contraindicated by the manufacturer. Animal data reports bictegravir with emtricitabine and tenofovir alafenamide in the breast milk, emtricitabine has found to be present in human breast milk. Effects on exposed infants are unknown.

Side Effects

Abdominal pain
Anaemia
Angioedema
Anxiety
Arthralgia
Autoimmune disorders
Autoimmune hepatitis
Behavioural disturbances
Convulsions
Depression
Diarrhoea
Dizziness
Dream abnormalities
Dyspepsia
Fatigue
Flatulence
Graves' disease
Headache
Hyperbilirubinaemia
Hypertonia
Metabolic disorders
Nausea
Neutropenia
Osteonecrosis
Pruritus
Rash
Sleep disorders
Stevens-Johnson syndrome
Suicidal tendencies
Urticaria
Vomiting

Presentation

Oral formulations of bictegravir with emtricitabine and tenofovir alafenamide.

Drugs List

Therapeutic Indications

Uses

Treatment of HIV infected adults

Adults infected with human immunodeficiency virus-1 (HIV-1) without present or past evidence of viral resistance to the integrase inhibitor class, emtricitabine or tenofovir.

Dosage

Adults

Additional Dosage Information

Contraindications

Children under 18 years
Breastfeeding
Renal impairment - creatinine clearance below 30 ml/minute
Severe hepatic impairment

Precautions and Warnings

Hepatic impairment
Hepatitis B
Hepatitis C
Pregnancy

Discontinuation of treatment may exacerbate hepatitis in HBV co-infection
Monitor HBV levels during and after treatment in patients with co-infection
Treatment does not prevent risk of transmission of HIV
Advise ability to drive/operate machinery may be affected by side effects
Treatment should be initiated by doctor experienced in HIV management
Autoimmune disorders can occur many months after initiation of treatment
Blood lipid and glucose levels may increase requiring treatment
Monitor closely patient with pre-existing hepatic impairment
On discontinuation, may cause recurrence of hepatitis B
Advise patient to seek medical advice if joint aches or pain occur
Advise patient to seek medical advice if movement becomes difficult
Inflammatory symptoms should be evaluated and treated appropriately
May cause weight gain
May develop immune reactivation syndrome
Neonate exposed in utero: Risk of mitochondrial dysfunction
Prolonged use may lead to nephrotoxicity
Discontinue if hepatic function deteriorates in pts with hepatic impairment
Advise patient not to take St John's wort concurrently
Advise to avoid antacids/mineral supplements 2 hours before or after dose
Take another dose if vomiting occurs within one hour

Patients co-infected with hepatitis B or C are at an increased risk of severe, potentially fatal hepatic adverse events. When discontinuing treatment with bictegravir with emtricitabine and tenofovir alafenamide in patients co-infected with hepatitis B and HIV, monitor closely for several months after treatment.

Blood lipid and glucose levels may increase during antiretroviral therapy. This may be linked to disease control and lifestyle. Refer to established HIV treatment guidelines for monitoring and manage lipid and glucose level disorders as appropriate.

When combination antiretroviral therapy is initiated in HIV-infected patients with severe immune deficiency, an inflammatory reaction to asymptomatic or residual opportunist 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. Any inflammatory symptoms should be evaluated and treated appropriately.

Treatment regimens containing nucleoside or nucleotide analogues have been reported to cause mitochondrial dysfunction in HIV-negative infants exposed in utero and/or post-natally. Adverse reactions such as haematological (anaemia, neutropenia), metabolic (hyperlactataemia, hyperlipasemia) and neurological (hypertonia, convulsions, abnormal behaviour) have been reported. Consider in children exposed to nucleoside or nucleotide analogues in utero (including HIV-negative infants) and who present with neurological symptoms or severe clinical findings of unknown cause.

Bictegravir with emtricitabine and tenofovir alafenamide should be avoided but may be used in adults with end stage renal disease on chronic haemodialysis if the potential benefits outweigh the potential risks. In a study of emtricitabine and tenofovir alafenamide in combination with elvitegravir and cobicistat as a fixed-dose combination tablet in HIV-1 infected adults with end stage renal disease on chronic haemodialysis, efficacy was maintained through 96 weeks but emtricitabine exposure was significantly higher than in patients with normal renal function. No additional adverse reactions were identified, the implications of increased emtricitabine exposure remain uncertain.

Pregnancy and Lactation

Pregnancy

Use bictegravir with emtricitabine and tenofovir alafenamide with caution during pregnancy.

The manufacturer advises bictegravir with emtricitabine and tenofovir alafenamide may be used only if the benefit justifies the potential risk to the foetus. Animal studies have shown no increased risk of teratogenic or developmental effects. The potential risk in humans is unknown.

Lactation

Bictegravir with emtricitabine and tenofovir alafenamide is contraindicated during breastfeeding.

Use of bictegravir with emtricitabine and tenofovir alafenamide is contraindicated by the manufacturer. Animal data reports bictegravir with emtricitabine and tenofovir alafenamide in the breast milk, emtricitabine has found to be present in human breast milk. Effects on exposed infants are unknown.

Side Effects

Abdominal pain
Anaemia
Angioedema
Anxiety
Arthralgia
Autoimmune disorders
Autoimmune hepatitis
Behavioural disturbances
Convulsions
Depression
Diarrhoea
Dizziness
Dream abnormalities
Dyspepsia
Fatigue
Flatulence
Graves' disease
Headache
Hyperbilirubinaemia
Hypertonia
Metabolic disorders
Nausea
Neutropenia
Osteonecrosis
Pruritus
Rash
Sleep disorders
Stevens-Johnson syndrome
Suicidal tendencies
Urticaria
Vomiting

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: November 2021

Reference Sources

Summary of Product Characteristics: Biktarvy 50mg/200mg/25mg film-coated tablets. Gilead Sciences Ltd. Revised September 2021.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 03 November 2021