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Product Name
:
POFEN (susp)
Chemical Name
:
Ibuprofen
Therapeutic Category
:
Anti-inflammatory drugs
Pharmacologic Category
:
Nonsteroidal Anti-inflammatory Drug (NSAID), Oral - Nonsteroidal Anti-inflammatory Drug (NSAID), Parenteral
Pharmaceutical Form
:
Oral suspension
Composition
:
Ibuprofen 100mg/5ml
Dosing
 
Dosing: Adult
Inflammatory disease: Oral: 400-800 mg/dose 3-4 times/day (maximum: 3.2 g/day)
Analgesia/pain/fever/dysmenorrhea: Oral: 200-400 mg/dose every 4-6 hours (maximum daily dose: 1.2 g, unless directed by physician; under physician supervision daily doses ≤2.4 g may be used)
Analgesic: I.V. : 400-800 mg every 6 hours as needed (maximum: 3.2 g/day). Note: Patients should be well hydrated prior to administration.
Antipyretic: I.V.: Initial: 400 mg, then every 4-6 hours or 100-200 mg every 4 hours as needed (maximum: 3.2 g/day). Note: Patients should be well hydrated prior to administration.
OTC labeling (analgesic, antipyretic): Oral: 200 mg every 4-6 hours as needed (maximum: 1200 mg/24 hours); treatment for >10 days is not recommended unless directed by healthcare provider.
Migraine: 2 capsules at onset of symptoms (maximum: 400 mg/24 hours unless directed by healthcare provider)

Dosing: Pediatric

Antipyretic: Oral: 6 months to 12 years: Temperature <102.5°F (39°C): 5 mg/kg/dose; temperature >102.5°F: 10 mg/kg/dose given every 6-8 hours; maximum daily dose: 40 mg/kg/day
Juvenile idiopathic arthritis (JIA): Oral: 30-50 mg/kg/24 hours divided every 8 hours; start at lower end of dosing range and titrate upward (maximum: 2.4 g/day)
Analgesic: Oral: 4-10 mg/kg/dose every 6-8 hours
Cystic fibrosis (unlabeled use): Oral: Chronic (>4 years) twice daily dosing adjusted to maintain serum concentration of 50-100 mcg/mL has been associated with slowing of disease progression in younger patients with mild lung disease
Patent ductus arteriosus: I.V. (ibuprofen lysine): Infants between 500-1500 g and ≤32 weeks GA: Initial dose: Ibuprofen 10 mg/kg, followed by two doses of 5 mg/kg at 24 and 48 hours. Dose should be based on birth weight.
OTC labeling (analgesic, antipyretic): Oral: Note: Treatment for >10 days is not recommended unless directed by healthcare provider.
Children 6 months to 11 years: See table; use of weight to select dose is preferred; doses may be repeated every 6-8 hours (maximum: 4 doses/day)
Children ≥12 years: Refer to adult dosing.
Ibuprofen Dosing
Weight
(lb)
Age
Dosage
(mg)
12-17
6-11 mo
50
18-23
12-23 mo
75
24-35
2-3 y
100
36-47
4-5 y
150
48-59
6-8 y
200
60-71
9-10 y
250
72-95
11 y
300

Dosing: Geriatric
Refer to adult dosing.

Dosing: Renal Impairment

If anuria or oliguria evident, hold dose until renal function returns to normal.

Dosing: Hepatic Impairment

Avoid use in severe hepatic impairment.
Use
 
Oral: Inflammatory diseases and rheumatoid disorders including juvenile idiopathic arthritis (JIA), mild-to-moderate pain, fever, dysmenorrhea, osteoarthritis
Ibuprofen injection: Management of mild-to-moderate pain; management moderate-to-severe pain when used concurrently with an opioid analgesic; reduction of fever
Ibuprofen lysine injection : To induce closure of a clinically-significant patent ductus arteriosus (PDA) in premature infants weighing between 500-1500 g and who are ≤32 weeks gestational age (GA) when usual treatments are ineffective
Use - Unlabeled/Investigational
Cystic fibrosis, gout, ankylosing spondylitis, acute migraine headache
Adverse Reactions
 
Oral:
1% to 10%:
Cardiovascular: Edema (1% to 3%)
Central nervous system: Dizziness (3% to 9%), headache (1% to 3%), nervousness (1% to 3%)
Dermatologic: Rash (3% to 9%), itching (1% to 3%)
Endocrine & metabolic: Fluid retention (1% to 3%)
Gastrointestinal: Epigastric pain (3% to 9%), heartburn (3% to 9%), nausea (3% to 9%), abdominal pain/cramps/distress (1% to 3%), appetite decreased (1% to 3%), constipation (1% to 3%), diarrhea (1% to 3%), dyspepsia (1% to 3%), flatulence (1% to 3%), vomiting (1% to 3%)
Otic: Tinnitus (3% to 9%)
<1% (Limited to important or life-threatening): Acute renal failure, agranulocytosis, anaphylaxis, aplastic anemia, azotemia, blurred vision, bone marrow suppression, confusion, creatinine clearance decreased, duodenal ulcer, edema, eosinophilia, epistaxis, erythema multiforme, gastric ulcer, GI bleed, GI hemorrhage, GI ulceration, hallucinations, hearing decreased, hematuria, hematocrit decreased, hemoglobin decreased, hemolytic anemia, hepatitis, hypertension, inhibition of platelet aggregation, jaundice, liver function tests abnormal, leukopenia, melena, neutropenia, pancreatitis, photosensitivity, Stevens-Johnson syndrome, thrombocytopenia, toxic amblyopia, toxic epidermal necrolysis, urticaria, vesiculobullous eruptions, vision changes
Injection: Ibuprofen: Abdominal pain, anemia, BUN increased, cough, dizziness, dyspepsia, edema, flatulence, headache, hemorrhage, hypokalemia, hypernatremia, hypertension, nausea, neutropenia, pruritus, urinary retention, vomiting

Injection: Ibuprofen lysine :

>10%:
Cardiovascular: Intraventricular hemorrhage (29%; grade 3/4: 15%)
Dermatologic: Skin irritation (16%)
Endocrine & metabolic: Hypocalcemia (12%), hypoglycemia (12%)
Gastrointestinal: GI disorders, non NEC (22%)
Hematologic: Anemia (32%)
Respiratory: Apnea (28%), respiratory infection (19%)
Miscellaneous: Sepsis (43%)
1% to 10%:
Cardiovascular: Edema (4%)
Endocrine & metabolic: Adrenal insufficiency (7%), hypernatremia (7%)
Genitourinary: Urinary tract infection (9%)
Renal: Urea increased (7%), renal impairment (6%), creatinine increased (3%), urine output decreased (3%; small decrease reported on days 2-6 with compensatory increase in output on day 9), renal failure (1%)
Respiratory: Respiratory failure (10%), atelectasis (4%)
Frequency not defined: Abdominal distension, cholestasis, feeding problems, gastritis, GI reflux, heart failure, hyperglycemia, hypotension, ileus, infection, inguinal hernia, injection site reaction, jaundice, neutropenia, seizure, tachycardia, thrombocytopenia
Postmarketing and/or case reports: GI perforation, necrotizing enterocolitis
Contraindications
 
Hypersensitivity to ibuprofen; history of asthma, urticaria, or allergic-type reaction to aspirin or other NSAIDs; aspirin triad (eg, bronchial asthma, aspirin intolerance, rhinitis); perioperative pain in the setting of coronary artery bypass graft (CABG) surgery
Ibuprofen lysine : Preterm infants with untreated proven or suspected infection; congenital heart disease where patency of the PDA is necessary for pulmonary or systemic blood flow; bleeding (especially with active intracranial hemorrhage or GI bleed); thrombocytopenia; coagulation defects; proven or suspected necrotizing enterocolitis (NEC); significant renal dysfunction
Warnings / Precautions Drug
 
Boxed warnings:
• Cardiovascular events: See “Concerns related to adverse effects” below.
• Coronary artery bypass graft surgery: See “Disease-related concerns” below.
• Gastrointestinal events: See “Concerns related to adverse effects” below.
Concerns related to adverse effects:
• Anaphylactoid reactions: Even in patients without prior exposure anaphylactoid reactions may occur; patients with "aspirin triad" (bronchial asthma, aspirin intolerance, rhinitis) may be at increased risk. Do not use in patients who experience bronchospasm, asthma, rhinitis, or urticaria with NSAID or aspirin therapy.
• Cardiovascular events: [U.S. Boxed Warning]: NSAIDs are associated with an increased risk of adverse cardiovascular thrombotic events, including fatal MI and stroke. Risk may be increased with duration of use or pre-existing cardiovascular risk factors or disease. Carefully evaluate individual cardiovascular risk profiles prior to prescribing. Use caution with fluid retention. Avoid use in heart failure. Concurrent administration of ibuprofen, and potentially other nonselective NSAIDs, may interfere with aspirin’s cardioprotective effect. Use the lowest effective dose for the shortest duration of time, consistent with individual patient goals, to reduce risk of cardiovascular events; alternate therapies should be considered for patients at high risk.
• CNS effects: May cause drowsiness, dizziness, blurred vision, and other neurologic effects which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Discontinue use with blurred or diminished vision and perform ophthalmologic exam. Periodically evaluate vision in all patients receiving long-term therapy.
• Gastrointestinal events: [U.S. Boxed Warning]: NSAIDs may increase risk of gastrointestinal irritation, inflammation, ulceration, bleeding, and perforation. These events can be fatal and may occur at any time during therapy and without warning. Use caution with a history of GI disease (bleeding or ulcers), concurrent therapy with aspirin, anticoagulants and/or corticosteroids, smoking, use of ethanol, the elderly or debilitated patients. Use the lowest effective dose for the shortest duration of time, consistent with individual patient goals, to reduce risk of GI adverse events; alternate therapies should be considered for patients at high risk. When used concomitantly with ≤325 mg of aspirin, a substantial increase in the risk of gastrointestinal complications (eg, ulcer) occurs; concomitant gastroprotective therapy (eg, proton pump inhibitors) is recommended (Bhatt, 2008).
• Hematologic effects: Platelet adhesion and aggregation may be decreased; may prolong bleeding time; patients with coagulation disorders or who are receiving anticoagulants should be monitored closely. Anemia may occur; patients on long-term NSAID therapy should be monitored for anemia. Rarely, NSAID use has been associated with potentially severe blood dyscrasias (eg, agranulocytosis, thrombocytopenia, aplastic anemia).
• Hyperkalemia: NSAID use may increase the risk of hyperkalemia, particularly in the elderly, diabetics, renal disease, and with concomitant use of other agents capable of inducing hyperkalemia (eg, ACE-inhibitors). Monitor potassium closely.
• Ophthalmic events: Blurred/diminished vision, scotomata, and changes in color vision have been reported. Discontinue therapy and refer for ophthalmologic evaluation if symptoms occur.
• Skin reactions: NSAIDs may cause serious skin adverse events including exfoliative dermatitis, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN); discontinue use at first sign of skin rash or hypersensitivity.
Disease-related concerns:
• Aseptic meningitis: May increase the risk of aseptic meningitis, especially in patients with systemic lupus erythematosus (SLE) and mixed connective tissue disorders.
• Asthma: Do not administer to patients with aspirin-sensitive asthma; severe bronchospasm may occur. Use caution in patients with other forms of asthma.
• Coronary artery bypass graft surgery: [U.S. Boxed Warning]: Use is contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery. Risk of MI and stroke may be increased with use following CABG surgery.
• Hepatic impairment: Use with caution in patients with decreased hepatic function. Closely monitor patients with any abnormal LFT. Severe hepatic reactions (eg, fulminant hepatitis, liver failure) have occurred with NSAID use, rarely; discontinue if signs or symptoms of liver disease develop, or if systemic manifestations occur.
• Hypertension: Use with caution; may cause new-onset hypertension or worsening of existing hypertension. Response to ACE inhibitors, thiazides, or loop diuretics may be impaired with concurrent use of NSAIDs.
• Renal impairment: NSAID use may compromise existing renal function; dose-dependent decreases in prostaglandin synthesis may result from NSAID use, reducing renal blood flow which may cause renal decompensation. Patients with impaired renal function, dehydration, heart failure, liver dysfunction, those taking diuretics, and ACE inhibitors, and the elderly are at greater risk of renal toxicity. Rehydrate patient before starting therapy; monitor renal function closely. Not recommended for use in patients with advanced renal disease. Long-term NSAID use may result in renal papillary necrosis.
Special populations:
• Elderly: The elderly are at increased risk for adverse effects (especially serious gastrointestinal events, CNS effects, renal toxicity) from NSAIDs even at low doses.
Other warnings/precautions:
• Self medication (OTC use): Prior to self-medication, patients should contact healthcare provider if they have had recurring stomach pain or upset, ulcers, bleeding problems, high blood pressure, heart or kidney disease, other serious medical problems, are currently taking a diuretic, aspirin, anticoagulant, or are ≥60 years of age. If patients are using for migraines, they should also contact healthcare provider if they have not had a migraine diagnosis by healthcare provider, a headache that is different from usual migraine, worst headache of life, fever and neck stiffness, headache from head injury or coughing, first headache at ≥50 years of age, daily headache, or migraine requiring bed rest. Recommended dosages should not be exceeded, due to an increased risk of GI bleeding. Stop use and consult a healthcare provider if symptoms get worse, newly appear, fever lasts for >3 days or pain lasts >3 days (children) and >10 days (adults). Do not give for >10 days unless instructed by healthcare provider. Consuming ≥3 alcoholic beverages/day or taking longer than recommended may increase the risk of GI bleeding.
• Surgical/dental procedures: Withhold for at least 4-6 half-lives prior to surgical or dental procedures.
Metabolism/Transport Effects
Substrate (minor) of CYP2C9, 2C19; Inhibits CYP2C9 (strong)
Interactions
 
ACE Inhibitors: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the combination may result in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of ACE Inhibitors. Risk C: Monitor therapy
Aminoglycosides: Nonsteroidal Anti-Inflammatory Agents may decrease the excretion of Aminoglycosides. Data only in premature infants. Risk C: Monitor therapy
Angiotensin II Receptor Blockers: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the combination may result in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Angiotensin II Receptor Blockers. The combination of these two agents may also significantly decrease glomerular filtration and renal function. Risk C: Monitor therapy
Anticoagulants: Antiplatelet Agents may enhance the anticoagulant effect of Anticoagulants. Risk C: Monitor therapy
Anticoagulants: Nonsteroidal Anti-Inflammatory Agents may enhance the anticoagulant effect of Anticoagulants. Risk C: Monitor therapy
Antidepressants (Tricyclic, Tertiary Amine): May enhance the antiplatelet effect of NSAID (Nonselective). Risk C: Monitor therapy
Antiplatelet Agents: May enhance the anticoagulant effect of other Antiplatelet Agents. Risk C: Monitor therapy
Antiplatelet Agents: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Antiplatelet Agents. An increased risk of bleeding may occur. Nonsteroidal Anti-Inflammatory Agents may diminish the cardioprotective effect of Antiplatelet Agents. This interaction is likely specific to aspirin, and not to other antiplatelet agents. Risk C: Monitor therapy
Beta-Blockers: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Beta-Blockers. Exceptions: Levobunolol; Metipranolol. Risk C: Monitor therapy
Bile Acid Sequestrants: May decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Risk D: Consider therapy modification
Bisphosphonate Derivatives: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Bisphosphonate Derivatives. Both an increased risk of gastrointestinal ulceration and an increased risk of nephrotoxicity are of concern. Risk C: Monitor therapy
Collagenase (Systemic): Antiplatelet Agents may enhance the adverse/toxic effect of Collagenase (Systemic). Specifically, the risk of injection site bruising and/or bleeding may be increased. Risk C: Monitor therapy
Corticosteroids (Systemic): May enhance the adverse/toxic effect of NSAID (Nonselective). Risk C: Monitor therapy
CycloSPORINE: Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of CycloSPORINE. Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of CycloSPORINE. Risk D: Consider therapy modification
CycloSPORINE (Systemic): Nonsteroidal Anti-Inflammatory Agents may enhance the nephrotoxic effect of CycloSPORINE (Systemic). Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of CycloSPORINE (Systemic). Risk D: Consider therapy modification
Dasatinib: May enhance the anticoagulant effect of Antiplatelet Agents. Risk C: Monitor therapy
Deferasirox: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Risk C: Monitor therapy
Desmopressin: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
Digoxin: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Digoxin. Risk C: Monitor therapy
Drotrecogin Alfa: Antiplatelet Agents may enhance the adverse/toxic effect of Drotrecogin Alfa. Bleeding may occur. Management: When possible, avoid use of drotrecogin within 7 days of use of any IIb/IIIa antagonists, higher dose aspirin (more than 650 mg/day), or use of other antiplatelet agents. Risk D: Consider therapy modification
Eplerenone: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Eplerenone. Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Eplerenone. Risk C: Monitor therapy
Floctafenine: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Glucosamine: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
Haloperidol: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Haloperidol. Specifically including drowsiness and confusion. Risk C: Monitor therapy
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Antiplatelet Agents. Bleeding may occur. Risk D: Consider therapy modification
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Bleeding may occur. Management: Concomitant treatment with these agents should generally be avoided. If used concomitantly, increased diligence in monitoring for adverse effects (eg, bleeding, bruising, altered mental status due to CNS bleeds) must be employed. Risk D: Consider therapy modification
HydrALAZINE: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of HydrALAZINE. Risk C: Monitor therapy
Ibritumomab: Antiplatelet Agents may enhance the adverse/toxic effect of Ibritumomab. Both agents may contribute to impaired platelet function and an increased risk of bleeding. Risk C: Monitor therapy
Ketorolac: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Ketorolac (Nasal): May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Ketorolac (Systemic): May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Risk X: Avoid combination
Lithium: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Lithium. Risk D: Consider therapy modification
Methotrexate: Nonsteroidal Anti-Inflammatory Agents may decrease the excretion of Methotrexate. Risk D: Consider therapy modification
Nonsteroidal Anti-Inflammatory Agents: May enhance the adverse/toxic effect of Antiplatelet Agents. An increased risk of bleeding may occur. Nonsteroidal Anti-Inflammatory Agents may diminish the cardioprotective effect of Antiplatelet Agents. This interaction is likely specific to aspirin, and not to other antiplatelet agents. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May enhance the adverse/toxic effect of other Nonsteroidal Anti-Inflammatory Agents. Risk C: Monitor therapy
Omega-3-Acid Ethyl Esters: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
PEMEtrexed: NSAID (Nonselective) may increase the serum concentration of PEMEtrexed. Management: Patients with mild-to-moderate renal insufficiency (CrCl 45-79 mL/minute) may use ibuprofen with caution, but should avoid other NSAIDs for 2-5 days prior to, the day of, and 2 days after pemetrexed. Risk D: Consider therapy modification
Pentosan Polysulfate Sodium: May enhance the adverse/toxic effect of Antiplatelet Agents. Specifically, the risk of bleeding may be increased by concurrent use of these agents. Risk C: Monitor therapy
Pentoxifylline: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Risk C: Monitor therapy
Potassium-Sparing Diuretics: Nonsteroidal Anti-Inflammatory Agents may diminish the antihypertensive effect of Potassium-Sparing Diuretics. Nonsteroidal Anti-Inflammatory Agents may enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Risk C: Monitor therapy
PRALAtrexate: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of PRALAtrexate. More specifically, NSAIDS may decrease the renal excretion of pralatrexate. Management: Closely monitor for increased pralatrexate serum levels and/or toxicity if used concomitantly with an NSAID. Monitor for decreased pralatrexate serum levels with NSAID discontinuation. Risk C: Monitor therapy
Probenecid: May increase the serum concentration of Nonsteroidal Anti-Inflammatory Agents. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
Quinolone Antibiotics: Nonsteroidal Anti-Inflammatory Agents may enhance the neuroexcitatory and/or seizure-potentiating effect of Quinolone Antibiotics. Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Quinolone Antibiotics. Risk C: Monitor therapy
Rivaroxaban: Antiplatelet Agents may enhance the anticoagulant effect of Rivaroxaban. Management: Avoid concurrent use of clopidogrel with rivaroxaban unless the anticipated benefits outweigh the risks of bleeding. Avoid concurrent use of rivaroxaban with other antiplatelet agents whenever possible. Risk D: Consider therapy modification
Salicylates: NSAID (Nonselective) may enhance the adverse/toxic effect of Salicylates. An increased risk of bleeding may be associated with use of this combination. NSAID (Nonselective) may diminish the cardioprotective effect of Salicylates. Salicylates may decrease the serum concentration of NSAID (Nonselective). Exceptions: Choline Magnesium Trisalicylate. Risk D: Consider therapy modification
Salicylates: Antiplatelet Agents may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: May enhance the antiplatelet effect of NSAID (Nonselective). NSAID (Nonselective) may diminish the therapeutic effect of Selective Serotonin Reuptake Inhibitors. Management: Consider using alternative analgesics, when appropriate, and/or addition of an gastroprotective agent. Monitor patients closely for signs/symptoms of bleeding, and for evidence of diminished SSRI effectiveness with concurrent use. Risk D: Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the antiplatelet effect of NSAID (Nonselective). Risk C: Monitor therapy
Sodium Phosphates: May enhance the nephrotoxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the risk of acute phosphate nephropathy may be enhanced. Management: Consider avoiding this combination by temporarily suspending treatment with NSAIDs, or seeking alternatives to oral sodium phosphate bowel preparation. If the combination cannot be avoided, maintain adequate hydration and monitor renal function closely. Risk D: Consider therapy modification
Thiazide Diuretics: Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Thiazide Diuretics. Risk C: Monitor therapy
Thrombolytic Agents: Antiplatelet Agents may enhance the anticoagulant effect of Thrombolytic Agents. Risk C: Monitor therapy
Thrombolytic Agents: Nonsteroidal Anti-Inflammatory Agents may enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur. Risk C: Monitor therapy
Tositumomab and Iodine I 131 Tositumomab: Antiplatelet Agents may enhance the adverse/toxic effect of Tositumomab and Iodine I 131 Tositumomab. Specifically, the risk of bleeding-related adverse events may be increased. Risk C: Monitor therapy
Treprostinil: May enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Bleeding may occur. Risk C: Monitor therapy
Vancomycin: Nonsteroidal Anti-Inflammatory Agents may increase the serum concentration of Vancomycin. Risk C: Monitor therapy
Vitamin E: May enhance the antiplatelet effect of Antiplatelet Agents. Risk C: Monitor therapy
Vitamin K Antagonists (eg, warfarin): NSAID (Nonselective) may enhance the anticoagulant effect of Vitamin K Antagonists. Risk D: Consider therapy modification
Voriconazole: May increase the serum concentration of Ibuprofen. Specifically, concentrations of the S-(+)-ibuprofen enantiomer may be increased. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may enhance gastric mucosal irritation).
Food: Ibuprofen peak serum levels may be decreased if taken with food.
Herb/Nutraceutical: Avoid alfalfa, anise, bilberry, bladderwrack, bromelain, cat's claw, celery, chamomile, coleus, cordyceps, dong quai, evening primrose, fenugreek, feverfew, garlic, ginger, ginkgo biloba, ginseng (American, Panax, Siberian), grapeseed, green tea, guggul, horse chestnut seed, horseradish, licorice, prickly ash, red clover, reishi, SAMe (S-adenosylmethionine), sweet clover, turmeric, white willow (all have additional antiplatelet activity).
Pregnancy
 
C/D ≥30 weeks gestation
Pregnancy Implications
Adverse events were not observed in the initial animal reproduction studies; therefore, the manufacturer classifies ibuprofen as pregnancy category C (category D: ≥30 weeks gestation). NSAID exposure during the first trimester is not strongly associated with congenital malformations; however, cardiovascular anomalies and cleft palate have been observed following NSAID exposure in some studies. The use of a NSAID close to conception may be associated with an increased risk of miscarriage. Nonteratogenic effects have been observed following NSAID administration during the third trimester including: Myocardial degenerative changes, prenatal constriction of the ductus arteriosus, fetal tricuspid regurgitation, failure of the ductus arteriosus to close postnatally; renal dysfunction or failure, oligohydramnios; gastrointestinal bleeding or perforation, increased risk of necrotizing enterocolitis; intracranial bleeding (including intraventricular hemorrhage), platelet dysfunction with resultant bleeding; pulmonary hypertension. Because they may cause premature closure of the ductus arteriosus, use of NSAIDs late in pregnancy should be avoided (use after 31 or 32 weeks gestation is not recommended by some clinicians). Product labeling for Caldolor™ specifically notes that use at ≥30 weeks gestation should be avoided and therefore classifies ibuprofen as pregnancy category D at this time. The chronic use of NSAIDs in women of reproductive age may be associated with infertility that is reversible upon discontinuation of the medication. A registry is available for pregnant women exposed to autoimmune medications including ibuprofen. For additional information contact the Organization of Teratology Information Specialists, OTIS Autoimmune Diseases Study, at 877-311-8972.
Lactation
 
Enters breast milk/not recommended (AAP rates “compatible”; AAP 2001 update pending)
Breast-Feeding Considerations
Based on limited data, only very small amounts of ibuprofen are excreted into breast milk. Adverse events have not been reported in nursing infants. Because there is a potential for adverse events to occur in nursing infants, the manufacturer does not recommend the use of ibuprofen while breast-feeding. Use with caution in nursing women with hypertensive disorders of pregnancy or pre-existing renal disease.
Monitoring Parameters
 
CBC, chemistry profile, occult blood loss and periodic liver function tests; monitor response (pain, range of motion, grip strength, mobility, ADL function), inflammation; observe for weight gain, edema; monitor renal function (urine output, serum BUN and creatinine); observe for bleeding, bruising; evaluate gastrointestinal effects (abdominal pain, bleeding, dyspepsia); mental confusion, disorientation; with long-term therapy, periodic ophthalmic exams; signs of infection (ibuprofen lysine)
Reference Range
Plasma concentrations >200 mcg/mL may be associated with severe toxicity
PDA: Minimum effective concentration: 10-12 mg/L
Mechanism of Action
 
Reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties
Other proposed mechanisms not fully elucidated (and possibly contributing to the anti-inflammatory effect to varying degrees), include inhibiting chemotaxis, altering lymphocyte activity, inhibiting neutrophil aggregation/activation, and decreasing proinflammatory cytokine levels.
Pharmacodynamics / Kinetics
 
Onset of action: Oral: Analgesic: 30-60 minutes; Anti-inflammatory: ≤7 days
Duration: Oral: 4-6 hours
Absorption: Oral: Rapid (85%)
Distribution: Vd: 6.35 L; premature infants with ductal closure (highly variable between studies):
Day 3: 145-349 mL/kg
Day 5: 72-222 mL/kg
Protein binding: 90% to 99%
Metabolism: Hepatic via oxidation
Half-life elimination:
Premature infants (highly variable between studies):
Day 3: 35-51 hours
Day 5: 20-33 hours
Children 3 months to 10 years: 1.6 ± 0.7 hours
Adults: 2-4 hours; End-stage renal disease: Unchanged
Time to peak: Oral: ~1-2 hours
Excretion: Urine (primarily as metabolites; 1% as unchanged drug); some feces
 
   
 
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