Drug Interactions
No evidence of enzyme induction.
Specific Drugs
| Drug |
Interaction |
Comments |
| ACE inhibitors |
Reduced BP response to ACE inhibitor
Possible deterioration of renal function in individuals with renal impairment |
Monitor BP |
| Alcohol |
Increased risk of GI bleeding |
|
| Angiotensin II receptor antagonists |
Reduced BP response to angiotensin II receptor antagonist
Possible deterioration of renal function in individuals with renal impairment |
Monitor BP |
| Antacids (aluminum- and magnesium-containing) |
No effect on ibuprofen absorption |
|
| Aspirin |
Antagonism of the irreversible platelet-aggregation inhibitory effect of aspirin; may limit the cardioprotective effects of aspirin
Increased risk of GI ulceration and other complications
No consistent evidence that low-dose aspirin mitigates the increased risk of serious cardiovascular events associated with NSAIAs |
Manufacturer states that concomitant use not recommended
Regular ibuprofen use not recommended in patients taking aspirin for cardiovascular prophylaxis
For occasional use with immediate-release low-dose aspirin: Administer single dose of ibuprofen 400 mg for self-medication at least 8 hours before or at least 30 minutes after aspirin
Enteric-coated low-dose aspirin: No recommendations regarding timing of administration with single dose of ibuprofen |
| Diuretics (furosemide, thiazides) |
Reduced natriuretic effects |
Monitor for diuretic efficacy and renal failure |
| H2 antagonists (cimetidine, ranitidine) |
Serum ibuprofen concentrations not appreciably altered |
|
| Lithium |
Increased plasma lithium concentrations |
Monitor for lithium toxicity; monitor lithium concentrations; lithium dosage reduction may be required |
| Methotrexate |
Pharmacokinetics of methotrexate may be altered |
Caution advised |
| Warfarin |
Reports of bleeding |
Caution advised |
Pharmacokinetics
Absorption
Bioavailability
Well absorbed following oral administration; peak plasma concentration usually attained within 1–2 hours.
Onset
Pain relief and/or antipyretic activity achieved within 1 hour.
Food
Food reduces peak plasma concentration by about 30–50% and delays time to reach peak plasma concentration by about 30–60 minutes but does not affect extent of absorption.
Distribution
Plasma Protein Binding
>99%.
Elimination
Metabolism
Extensively metabolized.
Elimination Route
Excreted mainly in urine as metabolites.
Half-life
1.8–2 hours.
Half-life 10-fold longer in neonates than in adults.
Stability
Storage
Oral
Capsules and Tablets
20–25°C.
Suspension
20–25°C.
Actions
- Inhibits cyclooxygenase-1 (COX-1) and COX-2.
- Pharmacologic actions similar to those of other prototypical NSAIAs; exhibits anti-inflammatory, analgesic, and antipyretic activity.
- Permits closure of the ductus arteriosus in premature neonates by inhibiting prostaglandin synthesis.
Advice to Patients
Pending revision, the material in this section should be considered in light of more recently available information in the MEDWATCH notification at the beginning of this monograph.
- Importance of reading the medication guide for NSAIAs that is provided each time the drug is dispensed.
- When used for self-medication, importance of reading the product labeling.
- When used for self-medication, importance of using the lowest effective dosage and of not exceeding the recommended dosage or duration of therapy.
- When used for self medication, importance of reviewing the warning information provided by the manufacturer.
- Risk of serious cardiovascular events with long-term use.
- Risk of GI bleeding and ulceration.
- Risk of serious skin reactions. Risk of anaphylactoid and other sensitivity reactions.
- Risk of hepatotoxicity.
- Importance of notifying clinician if signs and symptoms of a cardiovascular event (chest pain, dyspnea, weakness, slurred speech) occur.
- Importance of notifying clinician if signs and symptoms of GI ulceration or bleeding, unexplained weight gain, or edema develops.
- Importance of discontinuing ibuprofen and contacting clinician if rash or other signs of hypersensitivity (blisters, fever, pruritus) develop. Importance of seeking immediate medical attention if an anaphylactic reaction occurs.
- Importance of discontinuing therapy and contacting clinician immediately if signs and symptoms of hepatotoxicity (nausea, fatigue, lethargy, pruritus, jaundice, upper right quadrant tenderness, flu-like symptoms) occur.
- Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Importance of avoiding ibuprofen in late pregnancy (third trimester).
- Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.
- Importance of informing patients of other important precautionary information. (See Cautions.)