What are the contraindications and cautions for using Cabotegravir (Apretude) for Pre-Exposure Prophylaxis (PrEP)?

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Last updated: November 13, 2025View editorial policy

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Contraindications and Cautions for Cabotegravir (Apretude) PrEP

Absolute Contraindications

Cabotegravir is absolutely contraindicated in three specific situations that must be ruled out before initiating therapy. 1

  • Positive HIV-1 status: Never initiate cabotegravir PrEP in anyone with confirmed HIV infection, as monotherapy will lead to rapid resistance development 1
  • Previous hypersensitivity reaction to cabotegravir: Any prior allergic or hypersensitivity reaction to the drug precludes its use 1
  • Concurrent use of potent enzyme inducers: Specifically carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, and rifapentine, which significantly reduce cabotegravir levels below protective thresholds 1

Critical Pre-Initiation Requirements

Before the first injection, comprehensive HIV testing including BOTH a fourth- or fifth-generation antigen/antibody test AND an HIV RNA test with lower limit of quantification ≤50 copies/mL is mandatory. 2, 3 This dual testing approach is essential because:

  • Standard antibody tests alone can miss acute HIV infection 4
  • Cabotegravir can delay HIV seroconversion and mask early infection, creating a phenomenon called LEVI (long-acting early viral inhibition) 2
  • Starting cabotegravir in someone with undetected HIV leads to integrase inhibitor resistance 3

If clinical suspicion exists for acute HIV infection (fever, rash, lymphadenopathy, flu-like illness), do not initiate cabotegravir until HIV RNA results confirm negative status. 2

Important Cautions and Special Populations

Drug Interactions Requiring Dose Adjustment

  • Rifabutin coadministration requires dose adjustment of rifabutin when used with cabotegravir 2
  • All potent UGT1A1 inducers should be avoided as they reduce cabotegravir concentrations 2

Anatomical Considerations

  • Use with caution in individuals with gluteal implants or fillers, as the intramuscular injection site may be compromised 2

Injection Site Reactions

  • Injection site reactions occur in up to 81% of recipients but typically diminish over time 3, 5
  • These are not contraindications but require patient counseling for adherence 6

Renal Considerations

  • Baseline serum creatinine and estimated creatinine clearance are required before initiation 2
  • Unlike tenofovir-based PrEP, cabotegravir actually causes less decrease in creatinine clearance, making it potentially advantageous in those with borderline renal function 6

Mandatory Baseline Testing Before First Injection

Beyond HIV testing, the following must be completed 2:

  • Hepatitis B surface antigen (to identify those needing HBV treatment, not a contraindication to cabotegravir)
  • Hepatitis C antibody
  • Serum creatinine/estimated creatinine clearance
  • Pregnancy test for individuals of childbearing potential
  • STI screening (gonorrhea, chlamydia, syphilis)

Ongoing Monitoring Requirements

HIV testing must be repeated before EVERY subsequent injection using point-of-care rapid antibody test plus laboratory antigen/antibody test (RNA testing not routinely needed for follow-up unless breakthrough suspected). 2, 3

Common Pitfalls to Avoid

  • Failing to perform HIV RNA testing at initiation: Antigen/antibody tests alone miss 10-15% of acute infections 2, 4
  • Not having oral PrEP backup available: Patients need a 1-month supply of tenofovir-based oral PrEP for bridging if injections are delayed ≥7 days 3
  • Missing drug interaction screening: Specifically asking about anticonvulsants, rifamycins, and herbal supplements that induce metabolism 1
  • Inadequate counseling about injection site reactions: Setting expectations prevents discontinuation 5

Related Questions

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Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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