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145

Current guidelines for bridging are based on the results of case series,

observational studies, and nonrandomized trials involving patients with various

indications for anticoagulation, including valve replacement. The decision to use

bridging depends on the risk of bleeding associated with continued anticoagulation

for the surgery or procedure to be performed and on the risk of thromboembolism

associated with underanticoagulation in the patient in question. Recently, a large

registry called The Outcomes Registry for Better Informed Treatment of Atrial

Fibrillation (ORBIT-AF) included patients with atrial fibrillation that underwent

temporary interruption of oral anticoagulation therapy and showed that bridging was

associated with higher risk of bleeding and adverse events.

146 Shortly after, the

interim results of the BRIDGE trial (Bridging Anticoagulation in Patients who

Require Temporary Interruption of Warfarin Therapy for an Elective Invasive

Procedure or Surgery) that randomized patients with atrial fibrillation to receive

bridging therapy with LMWH or placebo showed similar findings to the ORBIT-AF

registry. The study showed no difference in the rate of arterial thromboembolism

between the bridging and nonbridging group; however, the bridging group showed

significantly higher rates of major bleeding. The mean CHADS2 score was 2.3 and

patients with mechanical heart valve or stroke, systemic embolism, and transient

ischemic attack within the previous 12 weeks were excluded from the trial. Major

surgical procedures associated with high rates of arterial thromboembolism and

bleeding were also underrepresented. Therefore, the results from the BRIDGE trial

should not be applied to patients that were underrepresented.

147

Individualized risk assessment and bridge therapy planning are necessary for each

patient who may require temporary discontinuation of warfarin. Current

recommendations for risk stratification are outlined in Table 11-25. High-risk and

moderate-risk patients typically receive bridge therapy if warfarin needs to be

withheld, whereas in low-risk patients, warfarin is simply withheld before the

invasive procedure, without the need for bridging. The bleeding risk of a performed

procedure or surgery must also be weighed. Efforts should be made to continue oral

anticoagulation in a patient with high thromboembolic risk undergoing a procedure

with low-bleeding risk, such as a dental extraction or cataract surgery. Table 11-26

includes examples of high- versus low-bleeding risk surgeries.

Clinical outcomes in patients bridged with LMWH or UFH are similar and overall

costs are lower for LMWH because of the avoidance of hospital admission for IV

UFH administration; therefore, the use of LMWH is recommended whenever

possible.

145 UFH may be preferred in patients with significant renal impairment

(CrCl < 30 mL/minute), and if LMWHs are used, reduced doses are suggested.

21

Monitoring anti-Xa levels for accumulation may be prudent if patients require a

prolonged course of therapy (over 7 days). A guideline for bridge therapy based on

the risk of thromboembolism and on renal function is presented in Table 11-27.

Table 11-25

Risk Stratification for Determining the Need for Bridge Therapy

Indication for VKA Therapy

Risk Stratum Mechanical Heart Valve Atrial Fibrillation Venous Thromboembolism

High Any mitral valve prosthesis

Older (caged-ball or tilting

disk) aortic valve

prosthesis

Recent (within 6 months)

stroke or transient

ischemic attack

CHADS2

score of 5 or 6

Recent (within 3 months)

stroke or transient

ischemic attack

Rheumatic valvular heart

disease

Recent (within 3 months)

VTE

Severe thrombophilia (e.g.,

deficiency of protein C,

protein S or antithrombin,

antiphospholipid antibodies,

or multiple abnormalities)

Moderate Bileaflet aortic valve

prosthesis and one of the

following: atrial fibrillation,

prior stroke or transient

ischemic attack,

hypertension, diabetes,

congestive heart failure,

age >75 years

CHADS2

score of 3 or 4 VTE within the past 3 to 12

months (consider VTE

prophylaxis rather than full

intensity bridge therapy)

Nonsevere thrombophilic

conditions (e.g.,

heterozygous factor V

Leiden mutation,

heterozygous factor II

mutation)

Recurrent VTE

Active cancer (treated within

6 months or palliative)

Low Bileaflet aortic valve

prosthesis without atrial

fibrillation and no other

risk factors for stroke

CHADS2

score of 0 to 2

(no prior stroke or

transient ischemic attack)

Single VTE occurred greater

than 12 months ago and no

other risk factors

VTE, venous thromboembolism.

Source: Douketis JD et al. Perioperative management of antithrombotic therapy: 9th ed: American College of

Chest Physicians Evidence-Based Clinical Practice Guidelines. Chest. 2012; 141(2)(Suppl):e326S–e350S.

p. 202

p. 203

Table 11-26

Bleed Risk of Selected Procedures

Low Risk

(2-Day Major Bleed Risk of 0%–2%)

High Risk

(2-Day Major Bleed Risk of 2%–4%)

Abdominal hernia repair Abdominal aortic aneurysm repair

Cataract surgery Any surgery lasting > 45 minutes

Cholecystectomy Major cancer surgery

Colonoscopy Major cardiac surgery (heart valve replacement &

CABG)

Cutaneous biopsies Major orthopedic surgery (joint replacement)

Cystoscopy Major vascular surgery

Dilation and curettage Transurethral prostate resection

Dental extractions Neurosurgical procedures

GI endoscopy ± biopsy Polypectomy, variceal treatment

Skin cancer excision Renal biopsy

Adapted from Spyropoulos AC. Perioperative bridging therapy for the at-risk patient on chronic anticoagulation.

Dis Mon. 2005;51:183–193.

Because L.P. has a mechanical mitral valve replacement, her risk of

thromboembolism associated with underanticoagulation is considered high.

Therefore, she should receive bridge therapy with an injectable anticoagulant while

warfarin is held. Her renal function is normal, and her healthcare insurance covers

injectable drugs. Therefore, her plan will include early discontinuation of warfarin 5

days before the procedure and substitution with enoxaparin 1 mg/kg every 12 hours

when the INR falls below the lower limit of the therapeutic range. The last dose of

enoxaparin should be given 24 hours before the procedure to minimize the risk of

bleeding at the time of the procedure. After the procedure, warfarin should be

restarted at her usual dose, and enoxaparin should be continued until the INR is

greater than 2.5, the lower limit of L.P.’s therapeutic range. For indications other than

mechanical valves, enoxaparin 1.5 mg/kg every 24 hours may be used as an

alternative to avoid twice-daily injections.

DRUG INTERACTIONS

Interactions with Prescription Drugs

CASE 11-13

QUESTION 1: P.T., a 48-year-old woman, received a mechanical mitral valve prosthesis 5 years ago and has

been anticoagulated with warfarin 6 mg/day with good control. She asks to see you today in your

anticoagulation clinic, after returning from an urgent appointment with her primary care physician for treatment

of a skin infection that tested positive for community-acquired methicillin-resistant Staphylococcus aureus

(MRSA), and was given a prescription for trimethoprim–sulfamethoxazole (TMP-SMX) twice a day for 10

days today. She is allergic to penicillin and has gastric intolerance to tetracycline. How will the combination of

warfarin and TMP-SMX affect P.T.’s anticoagulation control? Should her warfarin dosage be adjusted or

another drug substituted for TMP-SMX?

Table 11-27

Bridge Therapy Guidelines of Invasive Procedures

Action

Day Warfarin LMWH Laboratories

−6 Last warfarin dose N/A INR; skip dose if

supratherapeutic

−5 No warfarin N/A

−4 No warfarin Start LMWH

−3 No warfarin LMWH

−2 to −1 No warfarin LMWH; last dose 24–36

hours prior to procedure

0—day of procedure Resume warfarin at usual

dose if hemostasis is

achieved

a

No LMWH Ensure INR is appropriate

for surgery

b

CBC

1 Resume warfarin if not

started day prior

LMWH; resume following

minor surgery

No LMWH following

major surgery

2–3 Warfarin LMWH; resume following

major surgery if bleeding

controlled

4 Warfarin LMWH

5–7 Warfarin LMWH INR; discontinue when

therapeutic

Consider CBC, CrCl, antiXa level with continued

need for LMWH

aConsider giving 1.5 times usual warfarin dose for first 2 days when warfarin reinitiated.

b

INR < 1.5 required for most surgical procedures.

INR, international normalized ratio; LMWH, low-molecular-weight heparin; CBC, complete blood count; CrCl,

creatinine clearance.

Drug interactions with warfarin occur by a number of different mechanisms and

can have a significant impact on the anticoagulant effect of warfarin.

148,149 Elevations

or reductions in INR have been observed when interacting drugs are added to or

discontinued from the medication regimens of patients taking warfarin or when used

intermittently. Clinically significant hemorrhagic or thromboembolic complications

can result. Careful selection of both prescription and nonprescription medications,

appropriate INR monitoring, and detailed patient education regarding drug

interactions are important interventions for pharmacists caring for patients taking

warfarin. A selection of the hundreds of drugs that have been reported to interact

with warfarin, including mechanisms of interaction and effect on INR, is provided in

Table 11-28. Further information regarding the management of drug interactions can

be found in Chapter 3, Drug Interactions.

p. 203

p. 204

Table 11-28

Warfarin Drug Interactions

Target Effect Response Examples (Not Inclusive)

Clotting

factors

Increased

synthesis

Decreased

INR

Vitamin K

Decreased

synthesis

Increased

INR

Broadspectrum

antibiotics

Increased

catabolism

Increased

INR

Thyroid

hormones

Decreased

catabolism

Decreased

INR

Methimazole Propylthiouracil

Warfarin Inhibition Increased Acetaminophen Allopurinol Amiodarone Azole

metabolism INR antifungals

Cimetidine Fluoroquinolones Macrolides Metronidazole

Propafenone SSRIs Statins Sulfa

antibiotics

Induction Decreased

INR

Barbiturates Carbamazepine Doxycycline Griseofulvin

Nafcillin Phenytoin Primidone Rifampin

Hemostasis Additive

antithrombotic

effects

Increased

bleeding

risk

Aspirin NSAIDs Salicylates GPIIb/IIIa

inhibitors

Additive

anticoagulant

response

Increased

bleeding

risk

Heparin LMWH Direct thrombin

inhibitors

Thrombolytics

Decreased

INR

Cholestyramine Colestipol Sucralfate

Absorption Reduced Decreased

INR

Ascorbic acid Azathioprine Corticosteroids Cyclosporine

Unknown Increased

INR

Androgens Fenofibrate Cyclophosphamide Gemfibrozil

GP, glycoprotein; INR, international normalized ratio; LMWH, low-molecular-weight heparin; NSAIDs,

nonsteroidal anti-inflammatory drugs.

Although warfarin is highly bound to protein (primarily to albumin), and can be

displaced from protein-binding sites by a number of weakly acidic drugs, these

interactions typically do not result in clinically significant elevations in PT/INR.

150

Warfarin displaced from protein-binding sites is readily available for elimination by

hepatic metabolism, resulting in increased clearance without a significant change in

the free drug concentration.

Other types of interactions with warfarin are much more significant.

Pharmacodynamic interactions are those that alter the physiology of hemostasis,

particularly interactions that influence the synthesis or degradation of clotting factors

or that increase the risk of bleeding through inhibition of platelet aggregation.

Pharmacokinetic interactions influence the absorption and metabolism of warfarin,

and many clinically significant interactions with warfarin occur when warfarin

metabolism is induced or inhibited. Interactions involving agents known to influence

the hepatic microsomal enzyme systems responsible for the metabolism of the more

potent S(−)-warfarin (CYP2C9) are more significant than those that influence the

enzymes that metabolize R(+)-warfarin (CYP1A2, CYP3A4).

Sulfamethoxazole can increase the effect of warfarin significantly by

stereoselectively inhibiting the metabolism of the more potent S(−)-enantiomer of

warfarin. Potentiation of warfarin activity after inhibition of metabolism usually

takes several days, and the effect may be slow to resolve once the offending agent is

discontinued. In addition, fever associated with the infection for which TMP-SMX

has been prescribed may enhance the catabolism of vitamin K-dependent clotting

factors, resulting in an accentuated hypoprothrombinemic response. This effect will

dissipate as the fever abates with antibiotic therapy.

For P.T., the ideal choice would be to discontinue TMP-SMX and use a

noninteracting alternative. The decision of which agent to use must consider both the

treatment(s) of choice for the clinical indication along with patient factors such as

reported allergies or intolerances. In P.T.’s case, she has a penicillin allergy and

intolerance to tetracyclines, both of which would prevent their use. If a noninteracting

alternative is not clinically appropriate, the concomitant use of an interacting agent is

not absolutely contraindicated in patients taking warfarin. Use of TMP-SMX in P.T.

would be acceptable if she is monitored frequently and carefully, with adjustment of

warfarin dosages as necessary to maintain her INR within the therapeutic INR range

of 2.5 to 3.5 and with attention to potential hemorrhagic complications. No initial

change in the dosage of warfarin should be made because it may take several days for

the interaction to become apparent. The INR should be repeated within 3 days, with

warfarin dosing adjustments and subsequent monitoring guided by initial INR results.

p. 204

p. 205

CASE 11-14

QUESTION 1: G.H. is a 54-year-old man on long-term anticoagulation for multiple, bilateral DVTs, most

recently 1 year ago, for which he takes warfarin 7.5 mg daily. He had a knee replacement surgery 6 months

ago and had a complication of infected hardware, for which he needs to start IV rifampin in a skilled nursing

facility for several weeks. His orthopedic physician is asking about whether G.H. can be switched to an

alternate anticoagulant, because he knows that there is a drug interaction with warfarin and rifampin. What

options are available to him?

Although the DOACs are less prone to drug interactions than warfarin, all of them

are P-glycoprotein substrates and can have their concentrations reduced by rifampin,

which is a strong P-gp inducer.

151 At this time, dabigatran, rivaroxaban, apixaban,

and edoxaban are all contraindicated with rifampin per package labeling and are not

suitable options for G.H.

The interaction with warfarin and rifampin can be significant, with a potentially

large dose increase (sometimes up to 3 times the original dose) of warfarin necessary

to maintain G.H. in the therapeutic range. If G.H. is in a facility where his INRs can

be measured frequently, such as every few days, it may be appropriate to maintain

him on warfarin while continuing the rifampin, until the degree of the interaction can

be detected, and a new stable dose can be determined. Alternatively, if G.H. is

receiving the antibiotics at home, it may be appropriate for him to acquire a home

INR meter and perform warfarin self-testing of his INRs. It has been shown that

individuals performing patient self-testing (almost all testing weekly) had better time

in therapeutic range (TTR) than those who underwent in-clinic testing every 4 weeks

using high-quality anticoagulation management.

152 A substudy of this trial also

showed that individuals on chronic anticoagulation who perform self-testing more

often (i.e., weekly or twice weekly) had a modestly higher TTR compared to monthly

testing.

153 The costs of the self-testing meter and supplies are often covered by the

patient’s insurance; however, sometimes the poor reimbursement for managing

anticoagulation services this way can limit providers’ willingness to offer patientself testing. If reimbursement is not a concern (such as in a closed insurance system),

then patient self-testing can be a way to empower patients to take more control of

their warfarin management and reduce the burden of INR monitoring.

LMWH, UFH, and fondaparinux are also reasonable options for G.H. to use,

especially if his INRs cannot be stabilized while receiving the rifampin. However,

again, there could be barriers to self-injection and insurance limitations that may

make it difficult to continue these agents for a prolonged length of time.

CASE 11-14, QUESTION 2: Can G.H. return to using his ibuprofen for pain control?

This question illustrates one of the most difficult therapeutic dilemmas for a patient

taking warfarin. All NSAIDs have the potential to cause gastric irritation by

inhibiting cytoprotective prostaglandins, thereby providing a focus for GI bleeding.

In addition, most NSAIDs inhibit platelet aggregation, which compromises effective

clotting and can lead to bleeding complications.

154

These effects can increase the risk of hemorrhagic complications significantly in

patients taking warfarin who are prescribed concurrent NSAID therapy. In a

retrospective cohort study of patients age 65 years or older, the risk of

hospitalization for bleeding peptic ulcer disease was approximately 3 times higher

for patients taking concurrent warfarin and an NSAID versus patients taking either

drug alone, and almost 13 times higher than in patients taking neither warfarin nor an

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