Is there any available literature regarding the drug interaction between Paxlovid and DOACs, specifically apixaban? Any recommendation on what to do with apixaban during 5-day Paxlovid treatment?

Comment by InpharmD Researcher

Product labels indicate that the ritonavir component of Paxlovid is a potent cytochrome P450 3A4 and a P-glycoprotein inhibitor that may increase the blood concentration of apixaban and subsequently the risk of bleeding with concomitant use. Available guidelines and expert opinions proposed several management strategies, mainly withholding apixaban or reducing the dose by 50% in patients receiving 5 or 10 mg BID while receiving Paxlovid. Additionally, Paxlovid is not recommended in patients receiving apixaban 2.5 mg BID. Case reports demonstrated successful use of a reduced dose of apixaban in HIV-infected patients on ritonavir without adverse outcomes. Overall, decisions on adjusting direct oral anticoagulants should be individualized to each patient during Paxlovid regimen.

Background

A 2022 American College of Cardiology (ACC) clinical bulletin board provides a list of drug-drug interactions with nirmatrelvir/ritonavir (Paxlovid) and select cardiovascular medications. Interaction effects between Paxlovid and direct oral anticoagulants (DOACs) in specific are potentially increased risk of bleeding due to increased DOACs concentration with concomitant use; thus, the management recommendation is to hold DOAC during Paxlovid therapy. This list of information is intended for reference only and does not replace clinical judgment and shared decision-making for individualized patients. [1]

The National Institutes of Health (NIH) COVID-19 treatment guidelines list direct oral DOACs as common outpatient medications that have clinically relevant drug-drug interactions with ritonavir-boosted nirmatrelvir. Additionally, the panel recommends adjusting doses of concomitant apixaban and monitoring for adverse effects. While specific dose adjustments are not provided, temporarily withholding medication (if clinically appropriate) or using an alternative agent may be considered if the doses of interacting medications cannot be adjusted. [2]

The Infectious Disease Society of America (IDSA) guidelines for the management of drug interactions with Paxlovid recommend reducing the dose of apixaban 5 mg and 10 mg by 50% until 3 days after treatment with Paxlovid. For patients taking apixaban 2.5 mg, the panel recommends avoiding the use of Paxlovid. [3]

The Scientific and Standardization Committee (SSC) of the International Society on Thrombosis and Haemostasis (ISTH) suggests that when a patient is taking a DOAC and may be eligible to receive Paxlovid, an individualized, patient-centric approach should be taken. Several management options were suggested for patients receiving potentially interacting medications, including temporarily holding the dose of DOAC, reducing the dose, and monitoring the patient closely for at least seven days from the time of Paxlovid initiation. While low molecular weight heparin may be used as alternative anticoagulation therapy, it was recommended to continue oral anticoagulants whenever possible. The panel recommended against switching DOACs to warfarin due to increased variability of INR in patients with newly diagnosed COVID-19. [4]

A 2022 review discussed the management of drug-drug interactions (DDI) between Paxlovid and anticoagulants, including DOACs. Since DOACs are substrates of cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp), significant DDIs are expected when these agents are coadministered with ritonavir, a potent CYP3A4 and P-gp inhibitor. However, no adverse outcomes were reported in HIV-infected patients treated with low-dose apixaban while on ritonavir-boosted antiretroviral therapy (Table 1 and Table 2). Despite prescribing information for apixaban recommending administering the medication at a reduced dose (2.5 mg BID) when combined with strong CYP3A4 and P-gp inhibitors (e.g., ritonavir), it was suggested to avoid concomitant use of Paxlovid with apixaban. [5]

A 2022 commentary provided an algorithmic approach to manage drug-drug interactions of oral anticoagulants with Paxlovid. The authors recommended reducing the dose of apixaban to 2.5 mg BID when Paxlovid is used. For patients already taking apixaban at a dose of 2.5 mg daily, concurrent use of Paxlovid with apixaban should be avoided. [6]

A case series described the successful use of reduced-dose apixaban in six human immunodeficiency virus (HIV) patients who were receiving ritonavir- or cobicistat-boosted antiretroviral therapy (ART) (see Table 1). The case series suggests apixaban or dabigatran may be safely used in HIV patients taking ART regimens containing ritonavir, and apixaban may be concomitantly used with cobicistat. [7]

References:

[1] Bhave N, Gluckman T, Wiggins B. American College of Cardiology: Drug-Drug Interactions With Nirmatrelvir/Ritonavir (Paxlovid) and Select Cardiovascular Medications. Accessed August 9, 2022. https://www.acc.org/-/media/Clinical/PDF-Files/Approved-PDFs/2022/06/24/19/07/COVID-Drug-Clinical-Bulletin.pdf?la=en&hash=5E52306AC0BC6E9EB19777F25ABF481B502EE491
[2] National Institutes of Health COVID-19 Treatment Guidelines Panel. Drug-Drug Interactions Between Ritonavir-Boosted Nirmatrelvir (Paxlovid) and Concomitant Medications. Updated May 13, 2022. Accessed August 9, 2022. https://www.covid19treatmentguidelines.nih.gov/therapies/antiviral-therapy/ritonavir-boosted-nirmatrelvir--paxlovid-/paxlovid-drug-drug-interactions/
[3] Management of Drug Interactions With Nirmatrelvir/Ritonavir (Paxlovid®): Resource for Clinicians: IDSA COVID-19 Treatment and Management Guideline Panel on Behalf of the Infectious Disease Society of America. Infectious Disease Society of America 2022; Version 1.1. Accessed August 9, 2022. https://www.idsociety.org/practice-guideline/covid-19-guideline-treatment-and-management/management-of-drug-interactions-with-nirmatrelvirritonavir-paxlovid/
[4] Spyropoulos AC, Connors JM, Douketis JD, Goldin M, Hunt BJ, Kotila TR, Lopes RD, Schulman S; International Society on Thrombosis and Haemostasis. Good practice statements for antithrombotic therapy in the management of COVID-19: Guidance from the SSC of the ISTH. J Thromb Haemost. 2022 Jul 7:10.1111/jth.15809. doi: 10.1111/jth.15809. Epub ahead of print. PMID: 35906715; PMCID: PMC9349985.
[5] Marzolini C, Kuritzkes DR, Marra F, Boyle A, Gibbons S, Flexner C, Pozniak A, Boffito M, Waters L, Burger D, Back DJ, Khoo S. Recommendations for the Management of Drug-Drug Interactions Between the COVID-19 Antiviral Nirmatrelvir/Ritonavir (Paxlovid) and Comedications. Clin Pharmacol Ther. 2022 May 14:10.1002/cpt.2646. doi: 10.1002/cpt.2646. Epub ahead of print. PMID: 35567754; PMCID: PMC9348462.
[6] Rizk JG, Lazo JG Jr, Gupta A, Lavie CJ, Effron MB. Proposal for a Simple Algorithmic Approach to Manage Drug-Drug Interactions of Oral Anticoagulants with Nirmatrelvir/Ritonavir in COVID-19 Outpatients. Semin Thromb Hemost. 2022 Jun 23. doi: 10.1055/s-0042-1750024. Epub ahead of print. PMID: 35738295.
[7] Nisly SA, Stevens BN. Ritonavir- or cobicistat-boosted antiretroviral therapy and direct oral anticoagulants: A case for apixaban. Int J STD AIDS. 2019 Jun;30(7):718-722. doi: 10.1177/0956462419832099. Epub 2019 Apr 11. PMID: 30975070.












Relevant Prescribing Information

​Nirmatrelvir and ritonavir (Paxlovid) [8]
PAXLOVID (nirmatrelvir co-packaged with ritonavir) is a strong inhibitor of CYP3A and may increase plasma concentrations of drugs that are primarily metabolized by CYP3A. Co-administration of PAXLOVID with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events is contraindicated.

Apixaban tablet [9]
For patients receiving apixaban tablets doses of 5 mg or 10 mg twice daily, reduce the dose by 50% when apixaban tablet is coadministered with drugs that are combined P-glycoprotein (P-gp) and strong cytochrome P450 3A4 (CYP3A4) inhibitors (e.g., ketoconazole, itraconazole, ritonavir). In patients already taking 2.5 mg twice daily, avoid coadministration of apixaban tablets with combined P-glycoprotein (P-gp) and strong CYP3A4 inhibitors.

Metabolism: Apixaban is metabolized mainly via CYP3A4 with minor contributions from CYP1A2, 2C8, 2C9, 2C19, and 2J2.

References:

[8] ​​​​Nirmatrelvir and ritonavir (Paxlovid). Prescribing information. Pfizer Laboratories Div Pfizer Inc; 2022.
[9] Apixaban. Prescribing information. Indoco Remedies Limited; 2021.

Literature Review

A search of the published medical literature revealed 2 studies investigating the researchable question:

Is there any available literature regarding the drug interaction between Paxlovid and DOACs - specifically apixaban? Any recommendation on what to do with apixaban during 5-day Paxlovid treatment?

Level of evidence

A - Multiple high-quality studies with consistent results  Read more→



Please see Tables 1-2 for your response.


 

Case Summary
  Patient 1 Patient 2 Patient 3 Patient 4 Patient 5 Patient 6

Past medical history

HIV (>20 years), T2DM, chronic HCV (treatment-naive), NSTEMI (with DES)

HIV (5 years), HTN, CKD Stage III, COPD HIV (>5 years), CAD (with DES), AF HIV (17 years), HTN, T2DM, chronic HCV (achieved SVR) HIV (30 years), history of two AAA repairs, prior VTE, PVD, HTN, HLD HIV (11 years)
ART regimen

Lopinavir/ritonavir 400/100 mg BID

Abacavir/lamivudine 600/300 mg daily

Darunavir 800 mg daily

Ritonavir 100 mg daily

Abacavir/lamivudine 600/300 mg daily

Darunavir 800 mg daily

Ritonavir 100 mg daily

Etravirine 200 mg BID

Raltegravir 400 mg BID

Darunavir 600 mg BID

Ritonavir 100 mg BID

Etravirine 200 mg BID

Raltegravir 400 mg BID

Elvitegravir/cobicistat/ emtricitabine/tenofovir AF 150/150/200/10 mg daily

Darunavir 800 mg daily

Atazanavir 300 mg daily

Ritonavir 100 mg daily

Abacavir/lamivudine 600/300 mg daily

Tenofovir DF 300 mg daily

After 5 months on apixaban, changed to:

Darunavir/cobicistat 800/150 mg daily

Abacavir/lamivudine 600/300 mg daily

Tenofovir AF 300 mg daily

After 11 months on apixaban, changed to:

Dolutegravir/abacavir/lamivudine 50/600/300 mg daily

Tenofovir AF 25 mg daily

Baseline HIV laboratory values

HIV RNA VL 1,800 copies/mL

CD4 cell count 440 cells/mm3 (27%)

HIV RNA VL < 20 copies/mL

CD4 cell count 640 cells/mm3 (55%)

HIV RNA VL < 20 copies/mL

CD4 cell count 374 cells/mm3 (27%)

HIV RNA VL < 20 copies/mL

CD4 cell count 376 cells/mm3 (17%)

HIV RNA VL < 20 copies/mL

CD4 cell count 506 cells/mm3 (28%)

HIV RNA VL 2,010 copies/mL

CD4 cell count 59 cells/mm3 (5%)

DOAC Indication

Acute VTE Acute VTE AF Acute VTE Acute VTE Acute VTE
Dose of DOAC

Apixaban 10 mg BID x 4 doses, then held.

Resumed at apixaban 2.5 mg BID

Apixaban 5 mg BID for 7 days, then 2.5 mg BID Apixaban 2.5 mg BID indefinitely Apixaban 10 mg BID x 7 days, then apixaban 2.5 mg BID

Apixaban 5 mg BID x 7 days, then Apixaban 2.5 mg BID x 3 weeks, then Dabigatran 150 mg BID

Apixaban 10 mg BID x 7 days, then apixaban 5 mg BID x 7 days, then apixaban 2.5 mg BID

Total documented duration of DOAC

3 months 6 months Indefinitely 12 months 6 months 13 months

Baseline laboratory values

Hgb 8.7 g/dL

SCr 2.33 mg/dL

Estimated CrCl 35 mL/min

Hgb 11.7 g/dL

SCr 1.56 mg/dL

Estimated CrCl 60 mL/min

Hgb 13.3 g/dL

SCr 0.88 mg/dL

Estimated CrCl 65 mL/min

Hgb 9.9 g/dL

SCr 7.47 mg/dL

HD initiated

Hgb 16.1 g/dL

SCr 1.22 mg/dL

Estimated CrCl 65 mL/min

Hgb 11.4 g/dL

SCr 0.83 mg/dL

Estimated CrCl > 100 mL/min

Additional pertinent medications increasing bleeding risk

Clopidogrel 75 mg daily

Aspirin 81 mg daily

None None  Aspirin 81 mg daily Naproxen 250 mg q8h PRN pain None
Events

Surgical site bleed while on apixaban 10 mg BID.

No events or complications with apixaban 2.5 mg BID

No events or complications No events or complications No events or complications Regimen changed mid-therapy; No events or complications on either regimen No events or complications

HIV: human immunodeficiency virus; T2DM: type 2 diabetes mellitus; HCV: hepatitis C virus; NSTEMI: non-ST elevated myocardial infarction; DES: drug-eluting stent; HTN: hypertension; CKD: chronic kidney disease; COPD: chronic obstructive pulmonary disease; CAD: coronary artery disease; AF: atrial fibrillation; SVR: sustained virologic response; AAA: abdominal aortic aneurysm; VTE: venous thromboembolism; PVD: peripheral vascular disease; HLD: hyperlipidemia; AF: alafenamide; ART: antiretroviral therapy; BID: twice daily; CrCl: creatinine clearance per Cockcroft–Gault; DOAC: direct oral anticoagulant; Hgb: hemoglobin; RNA: ribonucleic acid; SCr: serum creatinine.

 

References:

Adopted from: Nisly SA, Stevens BN. Ritonavir- or cobicistat-boosted antiretroviral therapy and direct oral anticoagulants: A case for apixaban. Int J STD AIDS. 2019 Jun;30(7):718-722. doi: 10.1177/0956462419832099

 

Use of Apixaban in Atrial Fibrillation With Ritonavir-Boosted Antiretroviral Therapy: A Case Report

Design

Case report  

Case presentation

A 73-year-old male presented to the emergency department with altered mental status and respiratory distress with an oxygen saturation of 70%. The patient was on warfarin (goal international normalized ratio [INR] 2-3) for non-valvular atrial fibrillation and ritonavir-based highly active antiretroviral therapy (HAART). Due to blood observed from the endotracheal tube upon intubation and brown secretions noted from the orogastric tube, warfarin was held due to his bleeding from multiple sites, and 5 mg of vitamin K was subsequently administered via the orogastric tube. The patient did not receive his HAART until hospital day 2, and viral load was undetectable during admission. Given the fluctuations of INR levels regardless of careful adjustments in the warfarin dosing regimen, a therapeutic heparin intravenous (IV) drip was initiated on hospital day 20 to maintain anticoagulation status prior to tracheostomy placement. On hospital day 23, IV heparin was replaced by low molecular weight heparin Q12H. 

To optimize anticoagulation therapy, on hospital day 31, the decision was made to initiate apixaban at a reduced dose of 2.5 mg BID due to the potential drug-drug interaction with ritonavir. The patient did not experience any adverse effects, including bleeding or recurrent thrombus, and was subsequently discharged on hospital day 34 due to improvement in clinical status. Apixaban was deemed to be continued indefinitely. 

Study Author Conclusions

This case report adds to the growing evidence that dose-reduced apixaban can be safely administered concurrently with ritonavir-containing HAART. The patient did not experience any adverse effects from the drug nor did they experience any events indicating failure of anticoagulation, such as a recurrent thrombotic event.

Since the patient was discharged after only 4 days of apixaban therapy, we are not able to comment directly on the long-term safety and efficacy of apixaban use in this setting. As there are currently no in-vitro, in-vivo, or randomized controlled trials analyzing the interaction between ritonavir and apixaban, additional prospective study of this topic is warranted. 

 

References:

Lomakina V, Sozio SJ, Tekle J. Use of Apixaban in Atrial Fibrillation With Ritonavir-Boosted Antiretroviral Therapy: A Case Report. J Pharm Pract. 2022 Feb 9:8971900221074938. doi: 10.1177/08971900221074938