Ibuprofen; Uses, Dosage, Side Effects, Interactions

Mechanism of Action of Ibuprofen

The exact mechanism of action of ibuprofen is unknown. Ibuprofen is a non-selective inhibitor of cyclooxygenase, an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. Its pharmacological effects are believed to be due to inhibition cyclooxygenase-2 (COX-2) which decrease the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling. Antipyretic effects may be due to action on the hypothalamus, resulting in increased peripheral blood flow, vasodilation, and subsequent heat dissipation. Inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration. Ibuprofen is administered as a racemic mixture. The R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo. The S-enantiomer is believed to be the more pharmacologically active enantiomer.

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We previously showed the non-steroidal anti-inflammatory drug (NSAID) ibuprofen suppresses inflammation and amyloid in the APPsw (Tg2576) Tg2576 transgenic mouse. The mechanism for these effects and the impact on behavior are unknown. We now show ibuprofen’s effects were not mediated by alterations in amyloid precursor protein (APP) expression or oxidative damage (carbonyls). Six months of ibuprofen treatment in Tg+ females caused a decrease in open field behavior (p < 0.05), restoring values similar to Tg- mice. Reduced caspase activation per plaque provided further evidence for a neuroprotective action of ibuprofen. The impact of a shorter 3-month duration ibuprofen trial, beginning at a later age (from 14 to 17 months), was also investigated. Repeated measures ANOVA of Abeta levels (soluble and insoluble) demonstrated a significant ibuprofen treatment effect (p < 0.05). Post-hoc analysis showed that ibuprofen-dependent reductions of both soluble Abeta and Abeta42 were most marked in the entorhinal cortex (p < 0.05). Although interleukin-1beta and insoluble Abeta were more effectively reduced with longer treatment, the magnitude of the effect on soluble Abeta was not dependent on treatment duration.

Indications of Ibuprofen

IbuprofenTablet is used for the treatment, control, prevention, & improvement of the following diseases, conditions, and symptoms

• For symptomatic treatment of rheumatoid arthritis, juvenile rheumatoid arthritis, and osteoarthritis. May be used to treat mild to moderate pain and for the management of dysmenorrhea. May be used to reduce fever. Has been used with some success for treating ankylosing spondylitis, gout, and psoriatic arthritis. May reduce pain, fever, and inflammation of pericarditis. May be used IV with opiates to relieve moderate to severe pain. Ibuprofen lysine may be used IV to treat patent ductus arteriosus (PDA) in premature neonates.
• Treatment of a hemodynamically significant patent ductus arteriosus in preterm newborn infants less than 34 weeks of gestational age
• Prevention of patent ductus arteriosus in premature neonates of less than 34 weeks of gestational age
• Polyarthralgia
• Muscles stiffness in nerve diseases
• Morning stiffness
• Multiple joint pain
• Steroid induce arthritis
• Osteoarthritis
• Rheumatoid arthritis
• Ankylosing spondylitis
• Gouty arthritis
• Pain due to especially musculoskeletal system
• Muscles stiffness in spinal
• Muscles stiffness in muscle diseases
• Muscles stiffness in the joint diseases
• Lumbago
• Low back pain
• Pain caused by nonaticular rheumatism
• Periarthritis of scapulohumeral
• Ischiadynia
• Treatment of patent ductus arteriosus
• Temporarily reduces fever

Temporarily relieves minor aches and pains due to

Therapeutic Indications of Ibuprofen

• Analgesics, Non-Narcotic; Anti-Inflammatory Agents, Non-Steroidal; Cyclooxygenase Inhibitors
• Ibuprofen is used for relief of the pain and inflammation of acute gouty arthritis and acute calcium pyrophosphate deposition disease (pseudogout; chondrocalcinosis articularis; synovitis, crystal-induced). Only immediate-release dosage forms are recommended for relief of acute attacks because of their more rapid onset of action relative to delayed-release or extended-release dosage forms.
• Ibuprofen is indicated for the relief of mild to moderate pain, especially when anti-inflammatory actions may also be desired, e.g., following dental, obstetric, or orthopedic surgery, and for the relief of musculoskeletal pain due to soft tissue athletic injuries (strains or sprains). Only immediate-release dosage forms are recommended for relief of acute pain because of their more rapid onset of action relative to delayed-release or extended-release dosage forms.
• Ibuprofen is used in the treatment of psoriatic arthritis.
• Ibuprofen is indicated for relief of acute or chronic juvenile arthritis.
• Ibuprofen is indicated for the relief of acute or chronic ankylosing spondylitis.
• Ibuprofen is indicated for relief of acute or chronic osteoarthritis.
• Ibuprofen is indicated for the treatment of acute or chronic rheumatoid arthritis.
• A non-steroidal anti-inflammatory agent that possesses analgesic & antipyretic activity indicated for relief of symptoms of rheumatoid arthritis & osteoarthritis.
• For the relief of primary dysmenorrhea, ibuprofen therapy should be started with the earliest onset of pain .
• For the management of juvenile rheumatoid arthritis in the symptomatic treatment of acute and chronic rheumatoid arthritis and osteoarthritis .

Contra-Indications of Ibuprofen

Dysmenorrhea

• 200 to 400 mg orally every 4 to 6 hours as needed.

Osteoarthritis

• Initial dose: 400 to 800 mg orally every 6 to 8 hours.
• Maintenance dose: May be increased to a maximum daily dose of 3200 mg based on patient response and tolerance.

Rheumatoid Arthritis

• Initial dose: 400 to 800 mg orally every 6 to 8 hours.
• Maintenance dose: May be increased to a maximum daily dose of 3200 mg based on patient response and tolerance.

Headache

• 600 mg orally 90 minutes prior to the initial ECT session

Pain

• 200 to 400 mg orally every 4 to 6 hours as needed. Doses greater than 400 mg have not been proven to provide greater efficacy.
• IV: (Patients should be well hydrated before IV ibuprofen administration):
• Pain: 400 to 800 mg intravenously over 30 minutes every 6 hours as needed.

Fever

• 200 to 400 mg orally every 4 to 6 hours as needed.
• IV: (Patients should be well hydrated before IV ibuprofen administration):
• Fever: Initial: 400 mg intravenously over 30 minutes
• Maintenance: 400 mg every 4 to 6 hours or 100 to 200 mg every 4 hours as needed.

Pediatric Dose for Fever

Greater than 6 months to 12 years

• 5 mg/kg/dose for temperature less than 102.5 degrees F (39.2 degrees C) orally every 6 to 8 hours as needed.
• 10 mg/kg/dose for temperature greater than or equal to 102.5 degrees F (39.2 degrees C) orally every 6 to 8 hours as needed.
• The recommended maximum daily dose is 40 mg/kg.
• OTC pediatric labeling (analgesic, antipyretic): 6 months to 11 years: 7.5 mg/kg/dose every 6 to 8 hours; Maximum daily dose: 30 mg/kg

Pediatric Dose for Pain

• Infants and Children: 4 to 10 mg/kg orally every 6 to 8 hours as needed.
• The recommended maximum daily dose is 40 mg/kg.
• OTC pediatric labeling (analgesic, antipyretic): 6 months to 11 years: 7.5 mg/kg/dose every 6 to 8 hours; Maximum daily dose: 30 mg/kg

Pediatric Dose for Rheumatoid Arthritis

6 months to 12 years

• Usual: 30 to 40 mg/kg/day in 3 to 4 divided doses; start at lower end of dosing range and titrate; patients with milder disease may be treated with 20 mg/kg/day; doses greater than 40 mg/kg/day may increase risk of serious adverse effects; doses greater than 50 mg/kg/day have not been studied and are not recommended.
• Maximum dose: 2.4 g/day

Side Effects of Ibuprofen

The most common

• GI disorders (e.g. dyspepsia, abdominal pain, nausea, vomiting, diarrhoea, flatulence, constipation,, ulcerative stomatitis, ),indigestion,
• Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
• Drowsiness and lightheadedness
• Nausea and vomiting
• joint pain
• Nausea and vomiting
• Severe stomach ache
• Severe diarrhea
• Vaginal thrush
• Skin rash
• Headache
• Chest pain
• Diarrhea or loose stools
• Difficulty with breathing
• Dizziness
• Heartburn
• Muscle pain

More common

• Abdominal or stomach pain,
• Chills or fever
• Headache,
• Joint or back pain
• Muscle aching or cramping
• Muscle pains or stiffness
• Chest pressure or squeezing pain in chest
• Excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• Constipation
• Diarrhoea
• Loss of muscle coordination
• Sleepiness or unusual drowsiness
• Clumsiness or unsteadiness
• Drowsiness

Rare

• Anxiety
• change in vision
• seizures
• abnormal or fast heart rate
• tremors
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• discomfort in arms, shoulders, neck or upper back

Drug Interactions of Ibuprofen

Ibuprofen may interact with following drugs, supplyments & may change the efficacy of drugs

• aminoglycoside antibiotics (e.g., amikacin, gentamicin, tobramycin)
• angiotensin converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
• angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
• beta-adrenergic blockers (e.g., metoprolol, atenolol)
• calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
• celecoxib
• cilostazol
• clopidogrel
• corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
• cyclosporine
• diuretics (water pills; e.g., furosemide, hydrochlorothiazide,)
• 5-ASA medications (e.g. sulfasalazine)
• glucosamine
• haloperidol
• heparin
• methotrexate
• multivitamins
• other non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, ketorolac, naproxen)
• Omega-3 fatty acids
• pentoxifylline
• quinolone antibiotics (e.g., ciprofloxacin, ofloxacin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine,fluoxetine,paroxetine, sertraline)
• serotonin/norepinephrine reuptake inhibitors (SNRIs;  duloxetine, )
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
• warfarin