Faspic

Ibuprofen arginine.

Pharmacology: Pharmacodynamics: Ibuprofen is a synthetic analgesic and anti-inflammatory agent with a marked antipyretic effect.
Chemically, it represents the progenitor of phenylpropionic derivatives w/ anti-inflammatory activity. Its analgesic activity is not narcotic. Ibuprofen is a powerful prostaglandin synthesis inhibitor and exerts its activity by inhibiting its synthesis peripherally.
Pharmacokinetics: Ibuprofen arginine, due to the presence of a basic amino acid eg, arginine, allows ibuprofen solubilization and assures an excellent and prompt absorption of the active ingredient after oral administration.
Studies on man show that ibuprofen arginine, a new ibuprofen preparation enables a prompter drug absorption with respect to other traditional pharmaceutical forms (the peak concentration appears earlier) and with a serum bioavailability higher in the 1st hour following drug administration.
The peak plasma concentration is reached approximately within 15-30 min and plasma levels are attained within 5-10 min after oral administration. This feature is particularly advantageous in clinical conditions (eg, intense pain) where a prompt analgesic effect is required.
Ibuprofen arginine administration did not result in the accumulation of either the drug or its metabolites since excretion is practically complete after 24 hrs.
Toxicology: Preclinical Safety Data: Toxicological tests performed in various animal species by different routes of administration demonstrated that ibuprofen is well-tolerated and did not show teratogenic effects. It must however be pointed out that administration of NSAIDs to pregnant rats may induce a restriction of Botallo's duct.

Relief of mild to moderate pain with inflammation.
Pain Treatment: Headache, dental pain including pain after tooth extraction, dysmenorrhea, neuralgia, joint and muscular pains, episiotomy and post-partum pain, postoperative pain, pain due to small lesions or pain brought about by trauma.
Inflammatory Rheumatoid Forms: Rheumatoid arthritis, ankylosing spondylitis, Still's disease.
Degenerative Rheumatic Forms: Osteoarthritis (cervical, dorsal and lumbar arthrosis, gonarthritis, coxarthritis, polyarthritis, etc).
Extra-articular Rheumatic Forms: Tendonitis, fibrositis, bursitis, myalgia, lumbago, scapulohumeral periarthritis, ischialgia, radiculoneuritis.

Faspic is restricted to adult patients only.
Adults: 2-4 tab daily. Maximum Daily Dose: 1800 mg.
For rheumatic pain, it is suggested to administer the 1st daily dose in the morning before meals in order to improve the joint's rigidity while the following doses are to be administered during or after meals.
Patients should discuss with their doctors the risks and benefits of using NSAIDS and the importance of using the lowest effective dose for the shortest duration possible if treatment for NSAID is required. Do not take this drug continuously for more than 10 days unless prescribed by the physician.
Elderly: Dosage must be carefully established by the physician, taking into consideration the possible reduction of the aforementioned dosages.

In case of overdosage, gastrolavage and hematic electrolytes adjustment are indicated. No specific antidote for ibuprofen is available.

Absolute Contraindications: History of Stroke: Cerebrovascular accident (CVA); Heart Attack: Myocardial infarction (MI), Coronary artery by pass Graft: CABG uncontrolled hypertension, congestive heart failure (CHF) NYHA II-IV.
Hypersensitivity to the active ingredient, to other NSAIDs or to any of the components of Faspic.
Patients with history of hypersensitivity to Acetylsalicylic acid or any other Nonsteriodal anti-inflammatory drugs; with previous or active peptic ulceration; with cardiac, liver and renal disease. Dose adjustment like using the lowest effective dose and monitoring of renal and liver functions should be instituted.
Patients who experienced asthma, urticaria, angioneurotic edema or other allergic reactions after using compounds with similar action (eg, acetylsalicylic acid or other NSAIDs).
Gastrointestinal bleeding, intestinal inflammatory disease, severe hepatic failure, severe renal failure.
In case of systemic lupus erythematosus and collagen diseases, consult the attending physician before using Faspic.
Patients with hemorrhagic diathesis or other coagulation alterations.
Pregnancy (see use in pregnancy and lactation under Precaution).

Special caution is recommended in patients with pre-existing GI disturbances, previous gastric or duodenal ulcer, ulcerative colitis, Crohn's disease and alcoholism. Due to the possible onset of digestion problems, especially GI bleeding, an accurate monitoring of these patients is required during administration of ibuprofen or other nonsteroidal anti-inflammatory drugs (NSAIDs).
Caution is likewise required in patients with previous episodes of bronchospasm especially following the use of other drugs.
Faspic must be administered with extreme caution in patients with a history of heart failure, hypertension and preexisting edema of any nature and in patients with hepatic or renal impairment.
As a precautionary measure all patients under long-term treatment with ibuprofen must be subjected to a regular monitoring of the renal, hepatic and hematologic function by providing regular blood profile.
Ibuprofen, like other NSAIDs, can prolong the bleeding time and therefore must be used with due caution in patients with blood coagulation disorders.
Since visual or ocular alterations, though rare, were reported during treatment with ibuprofen, it is recommended to discontinue the treatment in case of any onset of visual disturbances and ophthalmologic examination must be performed.
Like any other prostaglandin synthesis and cyclooxygenase inhibitors is not recommended in women with pregnancy plans. Administration of the drug must be suspended in women with fertility problems or are currently undergoing fertility investigations.
Effects on the Ability to Drive or Operate Machinery: Driving and use of machinery must be avoided in patients who, during ibuprofen treatment, experience symptoms eg, dizziness, vertigo, visual alterations or other CNS disturbances.
Use in pregnancy & lactation: The use of Faspic during pregnancy, lactation and children is not recommended.

Gastrointestinal Tract: Irritation, anorexia, nausea, vomiting, dyspepsia, gastric pyrosis, abdominal disturbance, Gastrointestinal bleeding and ulcer activation may be experienced with the use of Ibuprofen. Gastrointestinal effects are frequently reported.
Central Nervous System: Headache, confusion, tinnitus and somnolence have a minor incidence with respect to GI effects.
Cases of psychotic and depression were reported.
Isolated case on the use of ibuprofen was followed by the onset of severe headache, nausea, vomiting, fever, rigidity of the neck muscles and sensorium obnubilation (initial signs of meningitis).
Sense Organs: Reversible effects on the eyes eg, toxic amblyopia, blurred vision and color blindness were observed.
Skin and Hypersensitivity Reactions: Various types of rash including urticaria, exanthema and purpura, associated or not with itching, as well as Stevens-Johnson syndrome were reported.
Generalized hypersensitivity reactions are only seldom reported. The symptoms may include fever associated with rash, abdominal pain, headache, nausea and vomiting, signs of hepatic dysfunction together with meningism and anaphylactic phenomena. Systemic lupus erythematosus or other collagen disease represent risk factors for serious forms of generalized hypersensitivity. Seldom does ibuprofen include bronchospasm in predisposed patients.
Hematology: Daily dose exceeding 1 g of ibuprofen may prolong the bleeding time. Alterations of various nature and intensity affecting the blood profile eg, thrombocytopenia, granulocytopenia, agranulocytosis, hemolytic and aplastic anemia were reported. These blood dyscrasias occur particularly after prolonged administration of high doses.
Hepatic Effects: Cases of liver alterations (high serum transaminases) and jaundice were reported. Hepatoxicity can occur in cases of generalized hypersensitivity reactions.
Renal Effects: Cases of sodium and liquid retention or edema are known. Cases of dysuria and acute interstitial nephritis were also reported. Kidney failure of various degree of severity could occur, particularly after prolonged administration of high doses.
Acute kidney failure may occur in case of generalized hypersensitivity reactions. Renal damage (papilla necrosis) were also reported.
Other Effects: Occasionally, stomatitis, menstrual irregularities, increase in serum urate levels were reported. The onset of adverse events during treatment implies the immediate suspension of therapy and the attending physician must be notified and consulted immediately.

Generally, NSAIDs must be used with caution when they are concomitantly administered with other drugs that may increase the risk of GI ulcer and bleeding or renal impairment.
Notable interaction involving NSAIDs include enhancement of the effects of the oral anticoagulants (especially azapropazone and phenylbutazone) and increased plasma concentrations of lithium, methotrexate and cardiac glycosides.
The risk of nephrotoxicity may be increased if given with ACE inhibitors, ciclosporin, tacrolimus or diuretics. Effects on renal function may lead to reduce excretion of some drugs. There may be also an increase risk of hyperkalemia with ACE inhibitors and K-sparing diuretics.
The antihypertensive effects of some antihypertensives include ACE inhibitors, β-blockers and diuretics may be reduced.
Convulsions may occur due to an interaction with quinolones.
NSAIDs may enhance the effects of phenytoin and sulfonylurea antidiabetics.
The effects of NSAIDs might be enhanced by use with moclobemide.
The concomitant use of >1 NSAID (including aspirin) should be avoided because of the increased risk of adverse effects.
The risk of gastrointestinal bleeding and ulceration associated with NSAIDs is increased when used with corticosteroids, the antiplatelets, clopidogrel and ticlopidine, or possibly alcohol, biphosphonates or oxpentifylline (pentoxifylline).
There may be an increased risk of hematotoxicity during concomitant use of zidovudine and NSAIDs; blood counts 1-2 weeks after starting use together are recommended.
Ritonavir may increase the plasma concentrations of NSAIDs.
The manufacturer of mifepristone advises that NSAIDs or aspirin should be avoided for 8-12 days after mifepristone use because of the theoretical risk that this prostaglandin synthetase inhibitors may alter the efficacy of mifepristone.
There have been occasional reports of increased adverse events when NSAIDs were given with misoprostol although such combinations have sometimes been employed to decrease the Gastrointestinal toxicity of NSAIDs.

Store at temperatures not exceeding 25°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AE01 - ibuprofen ; Belongs to the class of propionic acid derivatives of non-steroidal antiinflammatory and antirheumatic products.

Rx