THE ANTICOAGULANT EFFECT OF IBUPROFEN AND INTERACTIONS
ABSTRACT
Ibuprofen (IBU) is a non-steroidal anti-inflammatory drug (NSAID). A
clinician wishing to avoid opioid pain control may consider a
combination of orally administered ibuprofen (IBU) and acetaminophen for
pain control. In dentistry, it is commonly recommended to take oral IBU
400-800mg and acetaminophen 325-1000 mg to control postoperative pain
following third molar extraction(s). This combination can avoid the use
of a narcotic prescription for pain control. However, many patients are
taking anticoagulants for a variety of medical conditions and are told
not to take IBU fearing an additive effect of IBU with the
anticoagulant. This mini-review paper addresses the anticoagulant
effects of IBU when administered as a single agent and the interactions
with orally administered anticoagulant, antiplatelet, or antithrombotic
agents.
THE ANTICOAGULANT EFFECT OF IBUPROFEN
INTRODUCTION
Ibuprofen (IBU) is an over-the-counter (OTC) non-steroidal
anti-inflammatory drug (NSAID) (Fig. 1). It is sold as the racemic S
enantiomer to produce the desired pharmacologic action. IBU has an
elimination half-life of 2 hours (1,2). IBU is used to treat fever,
pain, and inflammation (3,4,5). IBU may not be as effective of an
anti-inflammatory agent when compared to other NSAIDs (6). Literature on
the safety of IBU is plentiful (1). NSAIDs when combined with
acetaminophen are highly effective for postoperative pain control (2).
Combining ibuprofen 200 mg with acetaminophen 500 mg has significantly
more analgesia effect than an opioid medication such as oxycodone 15 mg
with acetaminophen (2). Thus, it may be appropriate to use opioids only
for severe or refractory pain (2).
There may be a misconception that NSAIDs may have an unacceptable risk
of bleeding. Nonetheless, the bleeding risk profile of OTC IBU and the
prescription strength (600-800 mg) are not well defined. That is, with
the OTC use of IBU there are few controlled studies regarding the
anticoagulation effect of OTC use in the general population (1,2).
Gastrointestinal bleeding can occur with OTC IBU use. The GI-bleeding
complication hospitalization rate for OTC comparable doses of IBU is
less than 0.2%. (1) With increasing age and concomitant medication use,
the incidence of bleeding events does increase (1). Nonetheless, there
has been no consistent IBU dose-anticoagulation response relationship
elucidated. This may mean that patients are poor historians when
describing their side effects or there are genetic metabolic differences
that produce different outcomes, along with other potential reasons (7).
It is agreed that there appears to be a low incidence of bleeding events
with OTC IBU.
OTC drugs for pain control are intended for short-term use and should
not be taken for analgesia for more than 10 days. Longer use increases
possible side effects. To avoid gastric side effects, IBU should be
taken with food. Increased age, anemia, smoking, carcinoma, alcohol use,
liver disease, frailty, anticoagulants, and selective serotonin reuptake
inhibitors (SSRIs) are comorbidities that may increase the risk for
gastric side effects. (2,4,5, 8,9,10,11).
METHODOLOGY
A PubMed search was done using the terms, ibuprofen, ibuprofen AND
anticoagulant, ibuprofen AND drug interactions, and ibuprofen AND
complications. No other search engine was used. The articles retrieved
were assessed for relevance and those deemed relevant are included
herein. No human or animal subjects were used what so ever in this work.
PHARMACODYNAMICS OF IBUPROFEN
IBU
inhibits the cyclooxygenase-1
and -2 (COX-1 and
COX-2) enzymes. Inhibition
of COX-1 affects the prostaglandin-induced protection of the
gastrointestinal tract, and this action is well understood (10).
Nonetheless, various isoforms of IBU can cause varying degrees of
gastric damage (12). Selective COX-2 inhibitors are known to induce less
gastric damage (12). COX-2 leads to the production of prostaglandin E2
(PGE2) which produces redness, pain, and swelling; inhibition of COX-2
produces analgesia (5). Prostaglandins are converted
to thromboxane
A2 (TxA2) by Cox-1 enzymes (5,13). TxA2
stimulates platelet
aggregation for blood clotting. Thus, COX enzymes are inhibited, and
then ultimately TxA2 production is reduced along with platelet
aggregation and coagulation (12,14,15).
COAGULATION
Blood coagulation or thrombosis is the biologic action where liquid
blood is converted to a gel or a clot (Fig. 2). Coagulation involves
platelets and vascular protein factors (16) (Fig. 1). When vascular
subendothelial collagen is damaged and exposed to platelets, coagulation
begins. Platelets bind directly to the subendothelial collagen to form a
plug to occlude the injury. Platelets release stored granules of several
clotting factors that then bind fibrinogen. The fibrinogen crosslinks to
a glycoprotein and aggregates more platelets completing initial
hemostasis (17). Factor VII then induces fibrin formation to strengthen
the platelet plug.
The second stage of coagulation has two pathways that are artificially
named; (i) extrinsic or tissue factor and (ii) intrinsic or contact
activation pathways. Both pathways play a role in fibrin formation to
seal off bleeding or leaking blood vessels.
The extrinsic or tissue factor pathway is the more important. This
pathway is a cascade of enzymatic reactions by coagulation factors. The
main role of the extrinsic pathway is the rapid release of thrombin
(18).
The intrinsic pathway is a cascade of reactions that aid clot formation,
but its main role appears to be in inflammation and immunity (18,19). A
therapeutic blockage of the intrinsic pathway does not increase the risk
for significant bleeding but can contribute to the prevention of
thrombosis (19).
In the end, the extrinsic and intrinsic pathways both end into a final
common interactive pathway of factor X, thrombin, and fibrin.
Coagulation is a complex physiologic series of chemical and enzymatic
reactions that are activated and inhibited by a large variety of enzymes
and chemicals. In the end, without interference, a thrombus forms and
bleeding ceases (18,19,20).
IBUPROFEN AND COAGULATION
IBU has the lowest risk for gastrointestinal bleeding and platelet
inactivation of all NSAIDs (21). A single preoperative dose of 400 mg of
IBU does not have a significant intraoperative or postoperative
increased occurrence of bleeding. (22,23,24).
To reduce the risk of GI bleeding IBU should not be taken for more than
10 days (25). The lowest dose that produces the appropriate clinical
effect is the dose that should be taken (26,27).
Some studies report a low incidence of GI bleeding events with the use
of 200-600mg IBU for 10 days (1). The gastrointestinal bleeding
incidence among those using OTC-comparable doses ranged from 0 to 3.19
per 1000 patient years. The incidence of a GI bleeding-related events
increased with age and polypharmacy (1). However, there was an
inconsistent statistically significant ibuprofen
dose-dependent-anticoagulant response relationship. The relative risk of
any GI bleeding-related events ranges from 1.1 to 2.4% for users of
200-600mg IBU doses for 10 days when compared to non-users (1).
There are few published studies that have specifically investigated OTC
IBU use (1). Unfortunately, the large variety of methodologies,
exposures and outcomes preclude a direct comparison of many studies by
means of a meta-analysis (1). The various outcomes may imply that there
are human differences in IBU metabolism (1). Thus, patients with
susceptible phenotypes that effect IBU metabolism may react with varying
degrees of gastrointestinal bleeding severity (28).
IBUPROFEN INTERACTION WITH ANTICOAGULANT, ANTI-PLATELET, AND DIRECT
ANTI-THROMBOTIC AGENTS
Anticoagulants inhibit clot formation. There are many available with
various mechanisms of action. Since IBU acts to inhibit platelet
aggregation, there may be an increased clinical anticoagulation effect
when co-administered with other anti-coagulants, anti-thrombotic, or
anti-platelet agents (28).
Ibuprofen and warfarin
In one study, the effect of IBU anticoagulation interaction with
warfarin on hemostasis was tested in 20 patients taking warfarin for
venous thromboembolism (27). IBU 600 mg taken three times per day orally
was tested for 1 week (30). Bleeding time, prothrombin time, platelet
count and urinalysis for hemoglobin were observed. These tests were
performed just before, 90 minutes after the first dose of IBU and after
a one-week duration of treatment. Bleeding time was significantly
prolonged after 90 minutes following a single IBU 600mg dose, and after
1 week. Hematuria and hematoma were seen in all cases following
week-long co-administration. It was concluded that ibuprofen can cause
significant anticoagulation issues in patients being treated with
concurrent warfarin after one week (30). Thus, older patients under
anticoagulant and polypharmacy therapy may be at increased risk for
bleeding complications (30,31,32,33,34).
Warfarin (Coumadin®) acts by blocking the enzymatic
reduction of vitamin K. Vitamin K is an important cofactor in the
synthesis of clotting Factors II (prothrombin), VII, IX, and X. It can
take 3-5 days for warfarin to have a full therapeutic effect due to the
pre-treatment reservoir of Factors II, VII, IX, and X. (30,34)
IBU causes an increase of the INR in these warfarin patients by an
additive effect (35,36). IBU 600 mg taken orally three times a day for 7
days can cause an increase in the INR of patients taking warfarin
(35,36); however, there may not be a significant effect on platelet
count and prothrombin time. So, the increase in anticoagulation in most
patients may remain within normal limits. Nonetheless, microscopic
hematuria and hematoma can occur in these patients. These sequalae may
be problematic in elderly polypharmacy patients (33,34). Thus, if IBU is
to be administered for an extended time-period in these patients, the
dental clinician should consult with the patient’s physician who should
monitor the warfarin INR before and during concurrent IBU-warfarin
therapy. If the INR is prolonged beyond the intended clinical range, the
IBU treatment should be discontinued (36,37).
Much of the work on IBU-warfarin interaction was done on rats. Rats are
much more sensitive to this interaction than humans, nonetheless,
extrapolation to human clinical usage may not be appropriate (36,37).
Ibuprofen and Aspirin
The anti-platelet agent aspirin (ASA, acetyl salicylic acid) is a
non-selective COX inhibitor NSAID. A single dose of ASA inhibits
platelet function for 48 hours and inhibits platelet aggregation for the
life of the platelet (32,33). Short-term usage of IBU slightly reduces
platelet aggregation as compared to aspirin (25,26,32,35,36). The action
of ASA occurs at different loci in the coagulation cascade than IBU.
Nonetheless, IBU does interfere with the antiplatelet effect of aspirin
(ASA), and this makes the ASA less effective for cardio-protection and
stroke prevention (32,33). IBU can inhibit low-dose ASA’s ability to
reduce the antiplatelet effect (31,32). This problem can be avoided by
waiting 30-120 minutes after the ASA dose to administer the IBU or
administer the IBU dose 6-8 hours prior to the ASA dose (32,34,35).
However, due to the delayed absorption of enteric coated ASA, this time
frame may not apply. Another study suggested that IBU may be taken with
a 30 to 60-minute hiatus before or after ASA oral administration to
prevent an interaction (31,32). However, if IBU is taken only as an
occasional single dose or for a short term, then there is minimal
disruption of the ASA cardiovascular protective action (32,34).
Recent reports have minimized the therapeutic effect of ASA (38). Since
ASA and IBU are NSAIDs this may mean that the effects of these agents
are uncertain as well as their interaction. Further investigation needs
to be done to elucidate the therapeutics and interactions.
Ibuprofen and Direct Acting Antithrombotics
The direct-acting antithrombotics (DAA) (non-vitamin K antagonists) act
by inhibiting elements of the coagulation cascade factor Xa and IIa
(39,40). Dabigatran (Pradaxa®) is a direct thrombin
inhibitor and rivaroxaban (Xarelto®) and apixaban
(Eliquis®) are direct Factor Xa inhibitors (40). These
commonly prescribed anticoagulants do not require routine monitoring
(41). While this is an advantage, the patient has less contact with the
prescriber and may not be mindful of the potential for interactions of
OTC medications (41). Nonetheless, the incidence of serious interactions
with IBU is low when OTC guidelines are followed, 200mg 4-6 hours for
less than 10 days (42). Nonetheless, IBU can increase the incidence of
bleeding in patients taking apixaban (Eliquis), rivaroxaban (Xarelto),
dabigatran (Pradaxa) by an additive effect (40). Thus, co-administration
of IBU with these medications should be avoided.
Ibuprofen and Fish Oil
Many patients routinely take the omega-3 antioxidant fish oil as an OTC
medication. Fish oil has been known to have an anti-coagulant effect
(43). The additive effects of ibuprofen with fish oil have not been well
studied (43). Nonetheless, the clinician should be mindful of the
potential for an adverse effect on coagulation.
Ibuprofen and Selective Serotonin Reuptake Inhibitors
Long-term use of selective serotonin reuptake inhibitors (SSRI) has a
small anticoagulation side effect (44,45,46). There is frequent
self-administration of IBU by patients taking SSRIs (44,45,46). There is
no evidence of significant increased GI bleeding with the concomitant
use of SSRI and IBU or of the safety of this combination (44,45,46). The
SSRI bleeding risk is about the same as IBU as solo agents, but when
taken together the risk increases (47). The issue of concern is the
long-term concomitant use of these agents which may lead to significant
upper gastrointestinal bleeding (47).
Considerations
Table 1 provides a list of considerations before prescribing IBU (Table
1) (48). If IBU must be prescribed, then close monitoring of the
patient’s compliance and coagulation status should be done (48, 49,50).
CONCLUSIONS
Current information shows that IBU effects coagulation by mildly
inhibiting platelet aggregation when taken for less than 10 days. IBU
400 mg every 6 hours taken for less than 48 hours is unlikely to induce
an adverse bleeding event in patients taking anticoagulants. However,
after 10 days of daily dosing there may be an increased risk for
bleeding.
Most patients have poor compliance, and if IBU is to be administered,
the clinician should be certain that the patient understands the
implications of IBU dosing and potential drug interactions.
Investigations of these interactions are needed to provide the clinician
with appropriate prescribing protocols.
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