cabotegravir

Action and Spectrum

Actions and Spectrum:

Actions:

It works by blocking the action of an enzyme called integrase, that is essential for the replication of the HIV virus.

Spectrum:

The spectrum of activity of cabotegravir refers to the range of HIV strains that the drug is effective against a pathogen. cabotegravir is a highly potent integrase inhibitor, and it is effective against a wide range of HIV-1 strains, including those resistant to other classes of antiretroviral drugs.

Drug Interaction

Adverse Reaction

Frequency Defined

>10%:

Injection site reaction (38-82%)

Headache (4-12%)

Creatine phosphokinase increased (2-15%)

1-10%:

Pyrexia (≤4%)

Fatigue (3-4%)

Nausea (3-4%)

Sleep disorders (1-3%)

Abdominal pain (1-2%)

Vomiting (≤2%)

Flatulence (≤1%)

Back pain (≤1%)

Diarrhea (4%)

Myalgia (≤2%)

Rash (≤2%)

<1%:

Abnormal dreams

Anxiety

Headache

Nausea

Black Box Warning

Black Box Warning:

It is essential to test for HIV-1 infection before starting cabotegravir for PrEP, and to confirm that the individual is negative for HIV-1 before initiating treatment. It ensures that the individual is not already infected with the virus, as cabotegravir is not a treatment for established HIV-1 infection.

It is also essential to monitor drug-resistant HIV-1 variants during treatment with cabotegravir, as these variants may emerge in individuals with undiagnosed HIV-1 infection. If an individual becomes infected with HIV-1 while receiving cabotegravir for PrEP, they must transition to a complete HIV-1 treatment regimen to effectively manage their infection.

Contraindication / Caution

Contraindication/Caution:

Contraindications:

• Allergy or hypersensitivity: cabotegravir is contraindicated in individuals with known hypersensitivity to the drug or its components.
• Liver disease: cabotegravir has been associated with liver toxicity in some patients and should exercise caution in individuals with liver disease
• Other medications: cabotegravir may interact with other medications, and it is essential to inform your healthcare provider of all medications you are taking, including prescription and over-the-counter drugs, before starting treatment.
• Risk of HIV transmission: cabotegravir should not be used as a substitute for other established methods of preventing the transmission of HIV, such as safe sex practices and needle exchange programs.

Cautions:

• Pregnancy and breastfeeding: The safety of cabotegravir in pregnant women and women who are breastfeeding has not been established and should exercise caution in these populations.

Pregnancy / Lactation

Pregnancy consideration:

No data is available regarding the use in pregnant women.

Breastfeeding warnings:

No data is available regarding the secretion of the drug in breast milk.

Pregnancy category:

Category A: well-controlled and satisfactory studies do not show risk to the fetus in the first/later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology:
cabotegravir is an antiviral medication used to treat human immunodeficiency virus (HIV) and for pre-exposure prophylaxis (PrEP) to prevent HIV infection. It is a member of a class of drugs known as integrase strand transfer inhibitors (INSTIs). It works by blocking the activity of the HIV integrase enzyme, which is critical for the replication of the virus.

Pharmacodynamics:

The pharmacodynamic effects of cabotegravir are focused on its ability to suppress the replication of HIV. By inhibiting the activity of the HIV integrase enzyme, cabotegravir reduces the number of new virus particles produced and decreases the overall viral load in individuals with HIV. This results in improved health and a reduced risk of disease progression.

Pharmacokinetics:

Absorption

Peak plasma is achieved in 3 hours

The peak plasma concentration is 8 mcg /ml

The area under the curve is 145 mcg⋅h/mL

Distribution

The bound protein is more than 99.8%

Metabolism

cabotegravir is metabolized by UGT1A1 and UGT1A9 receptors

Elimination

The half-life of the drug is 41 hours for oral administration

5.6-11.5 weeks for intramuscular administration

The drug is excreted 27% in feces and 59% in urine

Adminstartion

Administration:

Intramuscular (IM) injection: cabotegravir is administered as a once-monthly IM injection, typically in the buttock muscle. The recommended dose is 600 mg every 4 weeks. This formulation is intended for use in individuals with established HIV-1 infection.

Oral tablet: cabotegravir is also available in an oral tablet formulation. The recommended dose is 30 mg, taken once daily. This formulation is intended for use as pre-exposure prophylaxis (PrEP) to prevent HIV infection in individuals who are at high risk of exposure.

Patient Information Leaflet

Patient information leaflet

Generic Name: cabotegravir

Pronounced: KA-boe-TEG-ra-vir

Why do we use cabotegravir?

• Treatment of HIV-1 infection: cabotegravir is used with other antiretroviral drugs to manage HIV-1 infection. The medication works by inhibiting the reverse transcriptase enzyme, which is essential for virus replication. By blocking this enzyme, cabotegravir helps to slow the progression of HIV-1 and improve overall health outcomes in individuals with HIV-1 infection.
• Pre-exposure prophylaxis (PrEP): cabotegravir is also used a prophylactic treatment to prevent HIV infection in individuals at high risk of exposure. The medication works by providing a barrier against the virus before exposure, reducing the likelihood of transmission and infection.