GELOFEN 400 

Ibuprofen

Soft Gelatin Cap.400 mg

Gelofen^®

(Ibuprofen)

Soft gelatin capsules

Description

Gelofen^® is a non-steroidal anti-inflammatory drug (NSAID) which is used to treat a variety of painful and inflammatory conditions.

Clinical pharmacology

Gelofen^® inhibits the activity of the enzyme cyclo-oxygenase, resulting in decreased formation of precursors of prostaglandins and thromboxanes from arachidonic acid.

Analgesic activity

Gelofen^® may block pain impulse generation via a peripheral action that involves reduction of the prostaglandins activity, and possibly inhibition of synthesis or action of other substances which sensitize pain receptors to mechanical or chemical stimulation.

Anti-inflammatory activity

Exact mechanisms have not been determined.

Gelofen^® may act peripherally in inflamed tissue, probably by reducing prostaglandin activity in these tissues and possibly by inhibiting the synthesis and actions of other local mediators of the inflammatory response inhibition of leukocyte migration, inhibition of the release and actions of lysosomal enzymes and actions on other cellular and immunological processes in mesenchymal and connective tissue maybe involved.

Antipyretic activity

It acts centrally on the hypotalmic heat-regulation center to produce peripheral vasodilatation resulting in increased blood flow through the skin, sweating and heatloss. The central action probably involves reduction of prosloglandin in the hypothalamus.

Antidysmenorrheal activity

By inhibiting the synthesis and activity of intrauterine prostaglandins, Gelofen® decrease uterine contractivity and pressure, increase uterine perfusion and relieve ischemic as well as spasmodic pain.

Vascular headache prophylactic and suppressant

Gelofen^® may directly prevent or relieve certain types of headache thought to be caused by prostaglandin- induced dilation or constriction of cerebral blood vessels.

Most of the NSAID_S inhibit platelet aggregation. However, their antiplatelet effect, unlike that of aspirin, is reversible.

Pharmacokinetics

Oral absorption > 90%

Presystemic metabolism 50%

Plasma half – life 1.8-2 h

Volume of distribution 0.15 L.kg^-1

Plasma protein binding 99.%

Indication

1- Arthritis , rheumatoid

2- Osteoarthritis

3- Menstrual cramps

4- Fever

5- Pain( toothache, muscular aches, backache)

6- Vascular headache (Prophylaxis and treatment)

Contraindication

Gelofen^® is contraindicated in patients who have shown hypersensivity to Ibuprofen or other NSAID_S, in nasal polyps associated with aspirin-induced bronchospasm,

Precaution

· Before Gelofen^® administration, previous hypersensivity reactions to NSAID_S must be determined because of cross hypersensivity among them.

· Gelofen^® should be used with caution in geriatrics specially who are at increased risk of serious gastrointestinal toxicity during NSAID therapy and who have renal function impairment.

· Risk-benefit should be considered when history of anemia, asthma, congestive heart disease, edema, hypertension, diabetes mellitus, sepsis, stomatitis, hemophilia or other bleeding problems, hepatic and/or renal function impairment exit.

Gelofen^® may induce or exacerbate active or history of blood dyscrasias and also bone, marrow depression.

Pregnancy

Pregnancy category B

There are no adequate and well controlled studies in pregnant women. Safety for use during pregnancy has not been established; use is not recommended.

Breast feeding

Gelofen^® is excreted in human milk in low concentrations. Caution should be exercised when it is administered to a nursing woman.

Dosage

Usual adult and adolescent dose

Antirhumatic – oral, 1200 to 3200 mg a day in three or four divided doses. After a satisfactory response has been obtained, dosage should be reduced to the lowest maintenance dose that provides continuing control of symptoms.

Note: Higher doses generally are required in rheumatoid arthritis than in osteoarthritis.

Analgesic, antipyretic: or antidysmenorrheal-

Oral, 200 to 400 mg every four to six hours as needed

Usual adult prescribing limits

Antirhematic- up to 3600 mg per day. The maximum dosage should be used only if the clinical benefit is increased sufficiently to offset the higher risk of adverse effects.

Analgesic, antipyretic: or antidysmenorrheal-

For patient self-medication (over- the-counter use):

Not to exceed 1200 mg per day.

Usual pediatric dose

Antirheumatic- infants up to 6 months of age: safety and effectiveness have not been established.

Patient consultation

· Be cautious if any kind of surgery (including dental surgery) or emergency treatment is required.

· Take medication at the same time each day to maintain the therapeutic effect.

· Don’t take more medication than prescribed by physician.

· Check with your physician if confusion, dizziness or lightheadedness, drowsiness or vision problems occurs.

· If pregnancy is suspected, notify your physician immediately.

· Be Cautious if photosensivity occurs.

· For oral medicine, you should take this drug with food and a full glass of water.

· Do not take for more than 3 days for fever, or more than 10 days for pain. If symptoms persist, worsen, or if new symptoms develop, contact a physician

· Avoid alcoholic beverages.

· May cause drowsiness, if affected do not drive or operate machinery.

Warning

· Gelofen^® is contraindicated for treatment of preoperative pain in the setting of coronary artery bypass graft (CABG) surgery.

· The medication may induce or exacerbate blood dyscrasias and bone marrow depression.

· Gelofen^® may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke which can be fetal.

· This medicine should be prescribed with extreme caution in those with a prior history of ulcer disease or gastrointestinal bleeding.

Interaction

· Prolonged concurrent use of acetaminophen with Gelofen^® may increase the risk of adverse renal effects.

· Gelofen^® can increase the plasma concentration of lithium by impairing its renal excretion.

· Concurrent use of aspirin or other NSAIDs with Gelofen^® may increase the risk of gastrointestinal toxicity, including ulceration or hemorrhage and increase the risk of bleeding at other sites because of additive inhibition of platelet aggregation.

· The medicine can increase the plasma concentration of digoxin, but no clinical signs of overdosage have been encountered.

· Various non-steroidal anti-inflammatory agents such as Gelofen^® are liable to inhibit the activity of diuretics and to potentiate the effects of potassium sparing diuretics, thus during concurrent usage monitoring of serum potassium levels is necessary.

· Concurrent use of Gelofen^® and methotrexate within 24 h of each other may increase methotrexate plasma levels, resulting in increased toxicity.

Laboratory value alteration

· Gelofen^® may decrease hematocrit, hemoglobin, Leukocyte and platelet count.

· Administration of Gelofen^® may decrease blood glucose concentrations.

· Blood urea nitrogen (BUN), serum creatinin urinary protein, urinary uric acid and urine volume may increase in patients receiving Gelofen^®.

Adverse reactions

Those adverse effect indicating need for medical attention

· Incidence rare

Perforation of peptic ulcers, gastrointestinal hemorrhage, blood dyscrasias and anaphylaxis.

Those indicating need for medical attention only if they continue or are bothersome.

Epigastric pain, nausea, diarrhea, vomiting, abdominal cramps, dyspepsia, anorexia, vertigo, headache and slight dizziness. These symptoms are often transient and disappear with continuation of medication elevation of ALT and AST, rashes or skin eruptions, drowsiness and tiredness urticaria, oedema, and liver function disorders with or without jaundice occur rarely and disturbance of sensation, vision, behavior and hearing, or convulsions, pancreatitis, constipation, parasthaesia, memory disturbance, disorientation, insomnia, irritability, depression, anxiety, nightmares, tremor, psychiatric reactions, aseptic meningitis, tinnitus, taste disturbances, acute renal insufficiency, urinary abnormalities, interstitial nephritis, nephrotic syndrome, papillary necrosis, vasculitis, pneumonitis, palpitations, chest pain, hypertension and congestive heart failure have only been reported in isolated cases.

Overdose

Since there is no specific antidote for overdose with Gelofen^®, treatment should be symptomatic and supportive. It is removable by hemodialysis..

Storage and stability condition

· Store below 30°C