Cabotegravir

Cabotegravir is a prescription medicine used for pre-exposure prophylaxis and treatment of HIV infection.

• Cabotegravir is available under the following different brand names: Vocabria, Apretude.

Common side effects of Cabotegravir include:

• nausea, 
• abnormal dreams, 
• anxiety, 
• headache, and
• sleep problems (insomnia)

Serious side effects of Cabotegravir include:

• hives, 
• difficulty breathing, 
• swelling of the face, lips, tongue, or throat, 
• severe dizziness,
• extreme tiredness, 
• fever, 
• feeling unwell, 
• rash, 
• muscle or joint pain, 
• blisters or sores in or around the mouth, 
• red or puffy eyes, 
• unusual mood changes (sadness, hopeless, anxiety, or restless),
• thoughts of self-harm, 
• loss of appetite, 
• nausea, 
• vomiting, 
• stomach pain (upper right side), 
• dark urine, 
• clay-colored stools, and
• yellowing of the skin or eyes

Rare side effects of Cabotegravir include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 30 mg (Vocabria)

Injection, extended-release IM suspension

• 600 mg/3 mL (Apretude)

HIV Infection Treatment

Adult dosage

• Oral lead-in dosing before Cabenuva
  • 30 mg orally every day plus rilpivirine 25 mg orally every day for at least 28 days to assess tolerability
  • Take the last oral dose on the same day injections with Cabenuva are started
• Oral replacement dose for planned missed Cabenuva injections
  • If the patient plans to miss scheduled Cabenuva (cabotegravir; rilpivirine) ER injectable suspensions by more than 7 days, take daily oral therapy to replace up to 2 consecutive monthly or 1 scheduled every-2-month injection visit(s)
  • 30 mg orally every day plus rilpivirine 25 mg orally every day as a replacement for up to 2 consecutive months
  • Take the first dose of oral therapy at approximately the same time as the planned missed injection and continue until the day injection dosing restarted

HIV Pre-exposure Prophylaxis

Adult and pediatric dosage

• IM
  • Initiation injections: 600 mg IM x 2 doses 1 month apart; may administer second initiation injection up to 7 days before or after the date scheduled to receive the injection, THEN
  • Continuation injections: 600 mg IM every 2 months
• Oral
  • Oral lead-in dosing before Apretude IM
  • 30 mg orally every day for ~1 month (at least 28 days)
  • Following oral lead-in, initiate cabotegravir IM on the last day of oral lead-in or within 3 days
  • Oral replacement dose for planned missed Apretude injections
  • If the patient plans to miss scheduled Apretude (cabotegravir) ER injectable suspension by more than 7 days, take daily oral therapy to replace up to 2 consecutive monthly injection visits
  • 30 mg orally every day as a replacement for up to 2 consecutive months
  • Take the first oral dose ~2 months after the last injection of cabotegravir IM injection
  • Restart cabotegravir IM every 2 months on the day oral dosing completes or within 3 days

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Cabotegravir has severe interactions with the following drugs:
  • apalutamide
  • carbamazepine
  • cigarette smoking
  • desogestrel
  • lamotrigine
  • nicotine gum
  • nicotine inhaled
  • nicotine intranasal
  • nicotine lozenge
  • nicotine transdermal
  • phenobarbital
  • phenytoin
  • primidone
  • rifabutin
  • rifampin
  • testosterone
• Cabotegravir has serious interactions with at least 31 other drugs.
• Cabotegravir has moderate interactions with the following drugs:
  • aluminum hydroxide
  • aluminum hydroxide/magnesium carbonate
  • aluminum hydroxide/magnesium trisilicate
  • aspirin/citric acid/sodium bicarbonate
  • calcium carbonate
  • calcium/vitamin D
  • magaldrate
  • magnesium chloride
  • magnesium citrate
  • magnesium hydroxide
  • magnesium oxide
  • ublituximab
  • zinc
• Cabotegravir has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Previous hypersensitivity to cabotegravir
• Coadministration with UGT1A1 inducers such as carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, and rifapentine, owing to possible loss of virologic response
• HIV-1 treatment: Before initiating cabotegravir PO, note that the use of Cabenuva ER injectable suspensions with rifabutin is contraindicated
• HIV-1 PrEP: Unknown or positive HIV-1 status

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Cabotegravir?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Cabotegravir?”

Cautions

• Hepatotoxicity reported in patients with or without known preexisting hepatic disease or known risk factors; monitoring of liver chemistries recommended; discontinue treatment if hepatotoxicity suspected
• Depressive disorders (including depressed mood, depression, mood altered, mood swings) reported; promptly evaluate if symptoms emerge; determine whether risks of continued therapy outweigh benefits
• Owing to use in combination with rilpivirine, consider contraindications, cautions, and drug interactions associated with rilpivirine
• Hypersensitivity
  • Serious or severe hypersensitivity reactions reported with other integrase inhibitors
  • Discontinue immediately if signs or symptoms of hypersensitivity reactions develop (including, but not limited to, severe rash, or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, mucosal involvement [oral blisters or lesions], conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing)
  • Monitor clinical status, including liver transaminases, and initiate appropriate therapy as warranted
• Drug interaction overview
  • Other antiretroviral medications for HIV-1 infection
  • Cabotegravir plus rilpivirine is a complete ART regimen
  • Coadministration with other ARTs is not recommended
  • UGT1A1 or UGT1A9 inducers
  • Contraindicated
    • Primarily metabolized by UGT1A1 with some contribution from UGT1A9
    • Strong UGT1A1 or 1A9 inducers are expected to decrease cabotegravir plasma concentrations and may result in loss of virologic response
  • Polyvalent cation-containing products
  • Modify dosage schedule
  • Coadministration with antacids containing polyvalent cations (eg, aluminum, magnesium hydroxide, calcium carbonate) may decrease cabotegravir absorption
  • Administer antacids at least 2 hr before or 4 hr after taking cabotegravir

Pregnancy and Lactation

• Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263; rate of miscarriage is not reported in the APR; the background risk for major birth defects and miscarriage for the indicated population is unknown
• Data are insufficient regarding use during pregnancy to adequately assess the drug-associated risk of birth defects and miscarriage
• While there are insufficient human data to assess the risk of neural tube defects (NTDs) with exposure to cabotegravir during pregnancy, NTDs were associated with dolutegravir, another integrase inhibitor
• Data from a birth outcome surveillance study in Botswana showed that dolutegravir, another integrase inhibitor, was associated with an increased risk of NTDs when administered at the time of conception and in early pregnancy; data from clinical trials are insufficient to address this risk with cabotegravir
• Healthcare providers should discuss benefit-risk of using drugs with individuals of childbearing potential or during pregnancy
• Clinical considerations
  • Cabotegravir was detected in systemic circulation for up to 12 months or longer after discontinuing IM injections; therefore, consider the potential for fetal exposure during pregnancy
• Lactation
  • Unknown if present in human breast milk affects human milk production or effects on breastfed infants
  • Because of the potential for HIV-1 transmission (in HIV-1–negative infants), developing viral resistance (in HIV-1–positive infants), and adverse reactions in a breastfed infant similar to those seen in adults, instruct HIV-1–infected mothers not to breastfeed if they are receiving the drug for the treatment of HIV-1 infection
  • Due to detectable cabotegravir concentrations in systemic circulation for up to 12 months or longer after discontinuing IM injections, females should breastfeed only if the expected benefit justifies the potential risk to the infant
  • For uninfected mothers receiving the drug for HIV-1 PrEP, assess the benefit-risk of the drug to the infant while breastfeeding
  • CDC recommends that females in the United States should not breastfeed their infants because of the risk of the following
  • Postnatal HIV transmission (in HIV-negative infants)
  • Developing viral resistance (in HIV-positive infants)
  • Adverse reactions in nursing infants