Cabotegravir is available in two forms: oral tablets and injectable formulations.

Oral Form: The oral form is typically used in the initial phase of HIV treatment to help ensure that the body tolerates the medication. The usual starting dose for adults is 30 mg once daily for the first 4 weeks. This is followed by the transition to the injectable form for long-term maintenance.

Injectable Form: Cabotegravir injectable is used for HIV maintenance treatment. The injectable form is administered by a healthcare provider, and is given intramuscularly. The dosing is started with a loading dose of 600 mg, administered every 4 weeks for the first 2 months. Then the patient will receive the maintenance dose of 400 mg administered every 8 weeks or every 2 months.

Cabotegravir is administered intramuscularly for PrEP (pre-exposure prophylaxis) as 600 mg every 4 weeks for the first month, then 400 mg every 8 weeks.

Injections should only be received from a healthcare provider, and dosing should follow the recommended schedule to achieve the best efficacy.

Cabotegravir works by specifically inhibiting the integrase enzyme, which is critical for the integration of HIV’s genetic material into the DNA of the host’s cells. HIV relies on integrase to insert its viral genome into the host’s DNA, which is essential for the virus to replicate and propagate.

Cabotegravir stops the replication of the virus, thus reducing viral load and enabling the immune system to recover, by blocking this step. This is crucial in fighting HIV because it does not only reduce the viral load but also prevents HIV from turning into AIDS.

As with all medicines, cabotegravir also has side effects that affect some patients but not everyone. The common cabotegravir side effects include:

Injection site reactions: This includes pain, swelling, redness, or tenderness at the injection site. This is more common with the injectable form of cabotegravir.

Headache: Some people experience mild to moderate headaches while using cabotegravir, especially when starting treatment.

Fever and chills: Some patients may experience mild flu-like symptoms such as fever, chills, or body aches, particularly after the initial injections.

Nausea: Nausea and some kind of gastrointestinal upset often is experienced but subsides over time.

Fatigue: Fatigue or a tired feeling is very common early in treatment.

Allergic reactions: Patients should be aware of an allergic reaction, as this also occurs with all medications. Any symptoms of an allergic reaction should be reported promptly to a healthcare provider.

Hepatic impairment: Patients who have liver pathology or who are coinfected with hepatitis B and C should be monitored very closely, since cabotegravir increases the likelihood of hepatotoxicity.

Pregnancy and lactation: Cabotegravir has been classified under Category B for pregnancy. In general, it is believed to be safe for use during the time of pregnancy. In any case, it can be used only if it is justified with the risks involved. Furthermore, use of cabotegravir is not advisable in cases of breastfeeding women. Its use should either be halted or avoided due to a possibility of excretion through breast milk.

Interactions with other drugs: Other drugs, especially other antiretrovirals and drugs that influence liver enzyme levels, may interact with cabotegravir. The patient should report other medications taken to the prescriber to avoid these potential interactions.

CYP3A4 Inducers: Drugs like rifampin, carbamazepine, or phenytoin can reduce cabotegravir levels by inducing CYP3A4, potentially decreasing its effectiveness.

CYP3A4 Inhibitors: Strong inhibitors, such as ketoconazole or ritonavir, may increase cabotegravir levels, raising the risk of side effects like liver toxicity or gastrointestinal issues.

Antacids: High doses of antacids or H2 antagonists can reduce cabotegravir absorption, potentially lowering its effectiveness. It’s recommended to separate the administration.

Other Antiretrovirals: When used with other antiretroviral drugs, drug interactions must be closely monitored, especially with integrase inhibitors, to optimize efficacy and minimize adverse effects.

For HIV Treatment (in combination with other antiretroviral agents):

Oral dose: 30 mg daily during the first 4 weeks as part of the initiation phase.

Injectable dose: 600 mg intramuscular injection every 4 weeks for the first 2 months, followed by 400 mg every 8 weeks for maintenance.

For PrEP (Pre-exposure Prophylaxis):

Injectable dose: 600 mg every 4 weeks for the first month, followed by 400 mg every 8 weeks.

Cabotegravir is a prescription drug that should only be prescribed by a health care provider with experience in the treatment of HIV. It requires evaluation before initiation of treatment, including a history of exposure to HIV and potential contraindications, particularly regarding liver health and other ongoing medications.

Patients need to be followed up regularly by their healthcare provider to monitor viral load, liver function, and any side effects that may occur.

1. What is Cabotegravir?

   • Cabotegravir is an antiretroviral medication used for the treatment and prevention of HIV infection.

2. How does Cabotegravir work?

   • Cabotegravir works by inhibiting the integrase enzyme, preventing the integration of viral DNA into the host cell’s DNA, thereby blocking HIV replication.

3. Is Cabotegravir used for HIV treatment or prevention?

   • Cabotegravir can be used for both HIV treatment (as part of a combination regimen) and pre-exposure prophylaxis (PrEP) to prevent HIV infection.

4. What is the recommended dosing schedule for Cabotegravir?

   • For HIV prevention, Cabotegravir is administered as an injection once every one or two months, depending on the regimen. For treatment, it is usually taken orally daily in combination with other antiretrovirals.

5. What are the common side effects of Cabotegravir?

   • Common side effects may include injection site reactions, fatigue, headache, and gastrointestinal symptoms like nausea.

6. Can Cabotegravir be used during pregnancy?

   • Cabotegravir is not recommended during pregnancy for HIV prevention due to potential risks; however, it may be used in treatment if the benefits outweigh the risks.

7. What should I do if I miss a dose of Cabotegravir?

   • For oral doses, take it as soon as you remember. If it’s close to the next scheduled dose, skip the missed dose. For injections, consult your healthcare provider about rescheduling.

8. Are there any contraindications for taking Cabotegravir?

   • Cabotegravir should not be used in individuals with a known hypersensitivity to cabotegravir or any of its components.

9. How is Cabotegravir administered?

   • For prevention, it is administered as an intramuscular injection. For treatment, it can be taken as a daily oral tablet.

10. What are the major drug interactions with Cabotegravir?

    • Cabotegravir may interact with other medications that affect liver enzymes, particularly in the cytochrome P450 system, which can alter its effectiveness.

11. How effective is Cabotegravir as PrEP?

    • Clinical trials have shown that Cabotegravir is highly effective as PrEP, reducing the risk of HIV transmission by more than 90% when taken as directed.

12. Can Cabotegravir be used in children?

    • Cabotegravir is currently approved for use in adults and is being studied in adolescents and children; consult a healthcare provider for specific guidance.

13. What are the implications of Cabotegravir for those with kidney problems?

    • Patients with significant kidney impairment should consult their healthcare provider, as kidney function can affect the medication’s effects and dosing.

14. Does Cabotegravir have an impact on bone health?

    • There are concerns about potential effects on bone density; patients should discuss any bone health concerns with their healthcare provider.

15. Is Cabotegravir safe to take long-term?

    • Long-term safety data is still being assessed, but ongoing studies and monitoring are in place to evaluate long-term use. Always consult with a healthcare provider.

16. What is the difference between Cabotegravir and other HIV medications?

    • Cabotegravir is an integrase inhibitor, while other classes of HIV medications, such as protease inhibitors and NNRTIs (non-nucleoside reverse transcriptase inhibitors), work through different mechanisms.

17. Can Cabotegravir cause weight gain?

    • Some patients may experience changes in weight, but individual responses vary. Consult your healthcare provider if you have concerns about weight changes while taking Cabotegravir.

18. How is Cabotegravir monitored during treatment?

    • Regular follow-up appointments with a healthcare provider are necessary to monitor viral load, kidney function, and potential side effects.

19. Is there a risk of developing resistance to Cabotegravir?

    • Like other antiretroviral medications, there is a risk of developing resistance if not taken as prescribed. Regular adherence to dosing is critical for maintaining its efficacy.

20. Where can I find more information about Cabotegravir?

    • Patients can find more information from healthcare providers, reputable medical websites, or through patient support organizations focused on HIV education and resources.