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Pronunciation |
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(eye
byoo PROE
fen) |

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U.S. Brand
Names |
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Advil®[OTC]; Bayer®
Select® Pain
Relief Formula [OTC]; Children's Advil® Oral Suspension
[OTC]; Children's Motrin® Oral Suspension
[OTC]; Dynafed® IB [OTC]; Genpril®[OTC];
Haltran®[OTC]; IBU®; Ibuprin®[OTC];
Ibuprohm®[OTC]; Junior Strength Motrin®[OTC];
Menadol®[OTC]; Midol® IB [OTC]; Motrin®;
Motrin® IB [OTC]; Nuprin®[OTC]; Saleto-200®[OTC];
Saleto-400®; Saleto-600®;
Saleto-800® |

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Generic
Available |
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Yes: Tablet |

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Canadian Brand
Names |
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Actiprofen®; Apo®-Ibuprofen;
Novo-Profen®; Nu-Ibuprofen |

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Synonyms |
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p-Isobutylhydratropic
Acid |

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Pharmacological Index |
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Nonsteroidal Anti-Inflammatory Agent (NSAID) |

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Use |
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Dental: Management of pain and swelling
Medical: Inflammatory diseases and rheumatoid disorders including juvenile
rheumatoid arthritis, mild to moderate pain, fever, dysmenorrhea, gout,
ankylosing spondylitis, acute migraine headache |

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Pregnancy Risk
Factor |
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B (D in 3rd trimester) |

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Contraindications |
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Hypersensitivity to ibuprofen, any component, aspirin, or other nonsteroidal
anti-inflammatory drugs (NSAIDs) |

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Warnings/Precautions |
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Do not exceed 3200 mg/day; use with caution in patients with congestive heart
failure, dehydration, hypertension, decreased renal or hepatic function, history
of GI disease (bleeding or ulcers), or those receiving anticoagulants; safety
and efficacy in children <6 months of age have not yet been established;
elderly are a high-risk population for adverse effects from nonsteroidal
anti-inflammatory agents. As much as 60% of elderly can develop peptic
ulceration and/or hemorrhage asymptomatically. |

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Adverse
Reactions |
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>10%:
Central nervous system: Dizziness, fatigue
Dermatologic: Rash, urticaria
Gastrointestinal: Abdominal cramps, heartburn, indigestion, nausea
1% to 10%:
Central nervous system: Headache, nervousness
Dermatologic: Itching
Endocrine & metabolic: Fluid retention
Gastrointestinal: Dyspepsia, vomiting, abdominal pain, peptic ulcer, GI
bleed, GI perforation
Otic: Tinnitus
<1%: Edema, congestive heart failure, arrhythmias, tachycardia,
hypertension, confusion, hallucinations, mental depression, drowsiness,
insomnia, aseptic meningitis, erythema multiforme, toxic epidermal necrolysis,
Stevens-Johnson syndrome, polydipsia, hot flashes, gastritis, GI ulceration,
cystitis, polyuria, neutropenia, anemia, agranulocytosis, inhibition of platelet
aggregation, hemolytic anemia, bone marrow suppression, leukopenia,
thrombocytopenia, hepatitis, peripheral neuropathy, vision changes, blurred
vision, conjunctivitis, dry eyes, toxic amblyopia, decreased hearing, acute
renal failure, allergic rhinitis, shortness of breath, epistaxis
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Overdosage/Toxicology |
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Symptoms include apnea, metabolic acidosis, coma, and nystagmus;
leukocytosis, renal failure
Management of a nonsteroidal anti-inflammatory drug (NSAID) intoxication is
primarily supportive and symptomatic. Fluid therapy is commonly effective in
managing the hypotension that may occur following an acute NSAID overdose,
except when this is due to an acute blood loss. Seizures tend to be very
short-lived and often do not require drug treatment; although, recurrent
seizures should be treated with I.V. diazepam. Since many of the NSAIDs undergo
enterohepatic cycling, multiple doses of charcoal may be needed to reduce the
potential for delayed toxicities. |

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Drug
Interactions |
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CYP2C8 and 2C9 enzyme substrate
Increased toxicity: May increase digoxin, methotrexate, and lithium serum
concentrations; other nonsteroidal anti-inflammatories may increase adverse
gastrointestinal effects |

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Mechanism of
Action |
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Inhibits prostaglandin synthesis by decreasing the activity of the enzyme,
cyclo-oxygenase, which results in decreased formation of prostaglandin
precursors |

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Pharmacodynamics/Kinetics |
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Onset of analgesia: 30-60 minutes
Duration: 4-6 hours
Onset of anti-inflammatory effect: Up to 7 days
Peak action: 1-2 weeks
Absorption: Oral: Rapid (85%)
Time to peak serum concentration: Within 1-2 hours
Protein binding: 90% to 99%
Metabolism: In the liver by oxidation
Half-life: 2-4 hours
End-stage renal disease: Unchanged
Elimination: In urine (1% as free drug); some biliary excretion occurs
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Usual Dosage |
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Oral:
Antipyretic: 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 rheumatoid arthritis: 30-70 mg/kg/24 hours divided every 6-8 hours
<20 kg: Maximum: 400 mg/day
20-30 kg: Maximum: 600 mg/day
30-40 kg: Maximum: 800 mg/day
>40 kg: Adult dosage
Start at lower end of dosing range and titrate upward; maximum: 2.4 g/day
Analgesic: 4-10 mg/kg/dose every 6-8 hours
Adults:
Inflammatory disease: 400-800 mg/dose 3-4 times/day; maximum dose: 3.2 g/day
Analgesia/pain/fever/dysmenorrhea: 200-400 mg/dose every 4-6 hours; maximum
daily dose: 1.2 g (unless directed by physician)
Dosing adjustment/comments in severe hepatic impairment: Avoid use
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Dietary
Considerations |
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Food: May decrease the rate but not the extent of oral absorption; drug may
cause GI upset, bleeding, ulceration, perforation; take with food or milk to
minimize GI upset |

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Monitoring
Parameters |
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CBC; 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 |

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Reference Range |
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Plasma concentrations >200 mg/mL may be
associated
with severe toxicity |

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Mental Health: Effects
on Mental Status |
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Drowsiness and dizziness are common; may cause nervousness; may rarely cause
insomnia, confusion, hallucinations, or depression |

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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause agranulocytosis; use caution with clozapine and
carbamazepine; may decrease lithium clearance resulting in an increase in serum
lithium levels and potential lithium toxicity; monitor serum lithium
levels |

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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |

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Dental Health:
Effects on Dental Treatment |
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<1% of patients experience dry mouth; NSAID formulations are known to
reversibly decrease platelet aggregation via mechanisms different than observed
with aspirin. The dentist should be aware of the potential of abnormal
coagulation. Caution should also be exercised in the use of NSAIDs in patients
already on anticoagulant therapy with drugs such as warfarin
(Coumadin®). |

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Patient
Information |
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If self-administered, use exactly as directed (do not increase dose or
frequency); adverse reactions can occur with overuse. Do not take longer than 3
days for fever, or 10 days for pain without consulting medical advisor. Take
with food or milk. While using this medication, do not use alcohol, excessive
amounts of vitamin C, or salicylate containing foods (curry powder, prunes,
raisins, tea, or licorice), other prescription or OTC medications containing
aspirin or salicylate, or other NSAIDs without consulting prescriber. Maintain
adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid
intake). May discolor urine (red/pink). You may experience nausea, vomiting,
gastric discomfort (frequent mouth care, small frequent meals, chewing gum,
sucking lozenges may help). GI bleeding, ulceration, or perforation can occur
with or without pain. Stop taking medication and report ringing in ears;
persistent cramping or pain in stomach; unresolved nausea or vomiting;
difficulty breathing or shortness of breath; unusual bruising or bleeding
(mouth, urine, stool); skin rash; unusual swelling of extremities; chest pain;
or palpitations. Pregnancy/breast-feeding precautions: Inform prescriber
if you are or intend to be pregnant. Consult prescriber if
breast-feeding. |

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Nursing
Implications |
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Do not crush tablet |

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Dosage Forms |
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Caplet: 100 mg
Drops, oral (berry flavor): 40 mg/mL (15 mL)
Suspension, oral: 100 mg/5 mL [OTC] (60 mL, 120 mL, 480 mL)
Suspension, oral, drops: 40 mg/mL [OTC]; 50 mg/1.25 mL
Tablet: 100 mg [OTC], 200 mg [OTC], 300 mg, 400 mg, 600 mg, 800 mg
Tablet, chewable: 50 mg, 100 mg |

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References |
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Berde C, Ablin A, Glazer J, et al,
"American Academy of Pediatrics Report of the Subcommittee on Disease-Related Pain in Childhood Cancer,"
Pediatrics, 1990, 86(5 Pt 2):818-25.
Brewer EJ, "Nonsteroidal Anti-inflammatory Agents," Arthritis Rheum,
1977, 20(2):513-25.
Brooks PM and Day RO,
"Nonsteroidal Anti-inflammatory Drugs - Differences and Similarities," N Engl
J Med, 1991, 324(24):1716-25.
Castillo M, Lam, YW, Dooley MA, et al,
"Disposition and Covalent Binding of Ibuprofen and its Acyl Glucuronide in the Elderly,"
Clin Pharmacol Ther, 1995, 57(6):636-44.
Clinch D, Banerjee AK, Ostick G,
"Absence of Abdominal Pain in Elderly Patients With Peptic Ulcer," Age
Ageing, 1984, 13(2):120-3.
Clive DM, Stoff JS,
"Renal Syndromes Associated With Nonsteroidal Anti-inflammatory Drugs," N
Engl J Med, 1984, 310(9):563-72.
Court H and Volans GN,
"Poisoning After Overdose With Nonsteroidal Anti-inflammatory Drugs," Adverse
Drug React Acute Poisoning Rev, 1984, 3(1):1-21.
Davies NM, "Clinical Pharmacokinetics of Ibuprofen. The First 30 Years,"
Clin Pharmacokinet, 1998, 34(2):101-54.
Dionne RA, "New Approaches to Preventing and Treating Postoperative Pain,"
J Am Dent Assoc, 1992, 123(6):26-34.
"Drugs for Pain," Med Lett Drugs Ther, 1998, 40(1033):79-84.
Gobetti JP, "Controlling Dental Pain," J Am Dent Assoc, 1992,
123(6):47-52.
Graham DY,
"Prevention of Gastroduodenal Injury Induced by Chronic Nonsteroidal Anti-inflammatory Drug Therapy,"
Gastroenterology, 1989, 96(2 Pt 2 Suppl):675-81.
Gurwitz JH, Avorn J, Ross-Degnan D, et al,
"Nonsteroidal Anti-Inflammatory Drug-Associated Azotemia in the Very Old,"
JAMA, 1990, 264(4):471-5.
Hall AH, Smolinske SC, Conrad FL, et al, "Ibuprofen Overdose: 126 Cases,"
Ann Emerg Med, 1986, 15(11):1308-13.
Hawkey CJ, Karrasch JA, Szczepanski L, et al,
"Omeprazole Compared With Misoprostrol for Ulcers Associated With Nonsteroidal Anti-inflammatory Drugs,"
N Engl J Med, 1998, 338(11):727-34.
Hoppmann RA, Peden JG, and Ober SK,
"Central Nervous System Side Effects of Nonsteroidal Anti-inflammatory Drugs. Aseptic Meningitis, Psychosis, and Cognitive Dysfunction,"
Arch Intern Med, 1991, 151(7):1309-13.
Kauffman RE and Nelson MV,
"Effect of Age on Ibuprofen Pharmacokinetics and Antipyretic Response," J
Pediatr, 1992, 121(6):969-73.
Kim J, Gazarian M, Verjee Z, et al,
"Acute Renal Insufficiency in Ibuprofen Overdose," Pediatr Emerg Care,
1995, 11(2):107-8.
Konstan MW, Byard PJ, Hoppel CL, et al,
"Effect of High-Dose Ibuprofen in Patients With Cystic Fibrosis," N Engl J
Med, 1995, 332(13):848-54.
Lesko SM and Mitchell AA,
"An Assessment of the Safety of Pediatric Ibuprofen. A Practitioner-Based Randomized Clinical Trial,"
JAMA, 1995, 273(12):929-33.
McElwee NE, Veltri JC, Bradford DC, et al,
"A Prospective, Population-Based Study of Acute Ibuprofen Overdose: Complications Are Rare and Routine Serum Levels are Not Warranted,"
Ann Emerg Med, 1990, 19(6):657-62.
Mixter CG 3d, Meeker LD, and Gavin TJ,
"Preemptive Pain Control in Patients Having Laparoscopic Hernia Repair: A Comparison of Ketorolac and Ibuprofen,"
Arch Surg, 1998, 133(4):432-7.
Olsen KM, Gurley BJ, Davis GA, et al,
"Comparison of Fluid Volumes With Whole Bowel Irrigation in a Simulated Overdose of Ibuprofen,"
Ann Pharmacother, 1995, 29(3):246-50.
Pearlman B, Boyatzis S, Daly C, et al,
"The Analgesic Efficacy of Ibuprofen in Periodontal Surgery: A Multicentre Study,"
Aust Dent J, 1997, 42(5):328-34.
Pounder R, "Silent Peptic Ulceration: Deadly Silence or Golden Silence?"
Gastroenterology, 1989, 96:(2 Pt 2 Suppl)626-31.
Smolinske SC, Hall AH, Vandenberg SA, et al,
"Toxic Effects of Nonsteroid Anti-inflammatory Drugs in Overdose. An Overview of Recent Evidence on Clinical Effects and Dose-Response Relationships,"
Drug Saf, 1990, 5(4):252-74.
Turturro MA, Paris PM, and Seaberg DC,
"Intramuscular Ketorolac Versus Oral Ibuprofen in Acute Musculoskeletal Pain,"
Ann Emerg Med, 1995, 26(2):117-20.
Vale JA and Meredith TJ,
"Acute Poisoning Due to Nonsteroidal Anti-inflammatory Drugs," Med
Toxicol, 1986, 1(1):12-31.
Verbeeck RK,
"Pharmacokinetic Drug Interactions With Nonsteroidal Anti-inflammatory Drugs,"
Clin Pharmacokinet, 1990, 19(1):44-66.
Winter L Jr, Bass E, Recant B, et al,
"Analgesic Activity of Ibuprofen (Motrin®) in
Postoperative Oral Surgical Pain," Oral Surg Oral Med Oral Pathol, 1978,
45(2):159-66.
Wolfe TR, "Ibuprofen Overdose," Am J Emerg Med, 1995, 13(3):375.
Yeomans ND, Tulassay Z, Juhasz L, et al,
"A Comparison of Omeprazole With Ranitidine for Ulcers Associated With Nonsteroidal Anti-inflammatory Drugs,"
N Engl J Med, 1998, 338(11):719-26. |

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