Faspik

General characteristics. Structure:

Active ingredient: 400 mg of an ibuprofen (in the form of salt of L-arginine).

Excipients: L-arginine, Natrii hydrocarbonas, кросповидон, magnesium stearate, gipromelloza, sucrose, titanium dioxide, macrogoal 4000.

Pharmacological properties:

Pharmacodynamics. The ibuprofen - active agent of drug Faspik - is derivative propionic acid and has analgetic, febrifugal and antiinflammatory effect due to not selective blockade of cyclooxygenase 1 and 2 and exerts the inhibiting impact on synthesis of prostaglandins.

Analgetic action is most expressed at pains of inflammatory character. Analgetic activity of drug does not belong to narcotic type.

As all NPVP, Faspik shows antiagregantny activity.

The analgesic effect at Faspik's use (an ibuprofen in the form of salt of L-arginine) develops in 10-45 minutes after reception.

Pharmacokinetics. Absorption: it is well absorbed from a stomach. At Faspik's use the maximum concentration (Stakh) of an ibuprofen in plasma about 25 μг/мл and 40 μг/мл are reached within 20-30 minutes after administration of drug on an empty stomach in a dose of 200 mg and 400 mg respectively.

Distribution: the ibuprofen approximately for 99% contacts proteins of plasma. It is slowly distributed in synovial fluid and brought out of it more slowly, than out of plasma.

Biotransformation: the ibuprofen is exposed to metabolism in a liver mainly by a hydroxylation and a carboxylation of isobutyl group. Metabolites pharmacological are inactive.

Removal: has two-phase kinetics of elimination. The elimination half-life (T1/2) makes 1-2 hours of plasma. To 90% of a dose it can be revealed in urine in the form of metabolites and their conjugates. Less than 1% are excreted in not changed view with urine and, to a lesser extent, with bile.

Indications to use:

• Feverish syndrome of various genesis.
• Pain syndrome of various etiology (including pharyngalgia, headache, migraine, dentagra, neuralgia, postoperative pains, posttraumatic pains, primary альгодисменорея).
• Inflammatory and degenerative diseases of joints and a backbone (including the pseudorheumatism ankylosing a spondylitis).

Route of administration and doses:

The initial dose for adults and children is more senior than 12 years inside makes 400 mg, if necessary - to 400 mg there are each 4-6 hours; the maximum daily dose - 1200 mg. The tablet is washed down with a glass of water (200 ml).

It is impossible to use drug more than 7 days or in higher doses without consultation with the doctor.

For decrease in risk of development of dispeptic effects it is recommended to accept drug during food.

At patients with a renal failure, a liver or heart the dose has to be reduced.

Features of use:

Use at pregnancy and a lactation. Contraindicated.

At emergence of symptoms of bleeding from digestive tract Faspik has to be cancelled (see the section of the Contraindication).

Faspik can mask objective and subjective symptoms of an infection therefore therapy by an ibuprofen at patients with an infection has to be appointed with care.

Emergence of a bronchospasm is possible at the patients having bronchial asthma or allergic reactions in the anamnesis or in the present.

Side effects can be reduced at use of a minimal effective dose at the shortest duration of treatment. At prolonged use of analgetics the risk of development of an analgetic nephropathy is possible.

Faspik's use can negatively influence female fertility and is not recommended to the women planning pregnancy.

Drug contains 16,7 mg of sucrose in 1 tablet, and it has to be taken into account in the presence at patients of the corresponding hereditary intolerance of fructose, a glyukozo-galaktozny malyabsorbtsionny syndrome or deficit of sucrose-isomaltase.

Patients who note vision disorders at therapy by Faspik have to stop treatment and undergo ophthalmologic inspection.

NPVP can increase the level of "hepatic" enzymes.

During treatment control of a picture of peripheral blood and a functional condition of a liver and kidneys is necessary.

At emergence of symptoms of a gastropathy the careful control including carrying out an ezofagogastroduodenoskopiya, blood test with definition of hemoglobin, a hematocrit, the analysis a calla on the occult blood is shown.

For the prevention of development of the NPVP-gastropathy it is recommended to combine with prostaglandin E drugs (мизопростол).

In need of definition of 17 ketosteroids drug should be cancelled in 48 hours prior to a research.

Patients have to abstain from all types of activity requiring special attention, bystry mental and motor reaction.

During treatment ethanol reception is not recommended.

Side effects:

• Digestive Tract (DT): NPVP-gastropathy (abdominal pains, nausea, vomiting, heartburn, loss of appetite, diarrhea, meteorism, lock; seldom - ulcerations mucous a GIT which in some cases are complicated by perforation and bleedings); irritation or dryness of a mucous oral cavity, mouth pain, ulceration mucous gums, aphthous stomatitis, pancreatitis.
• Gepato-biliarnaya system: hepatitis.
• Tsykhatelny system: asthma, bronchospasm.
• Sense bodys: hearing disorder: decrease in hearing, ring or sonitus.
• Central and peripheral nervous system: a headache, dizziness, sleeplessness, uneasiness, nervousness and irritability, psychomotor excitement, drowsiness, depressions, confusion of consciousness, a hallucination, it is rare - aseptic meningitis (more often at patients with autoimmune diseases).
• Cardiovascular system: Heart failure, tachycardia, increase in arterial pressure.
• Urinary system: Acute renal failure, allergic nephrite, nephrotic syndrome (hypostases), polyuria, cystitis.
• Allergic reactions: Skin rash (usually erythematic or urtikarny), skin itch, Quincke's edema, anaphylactoid reactions, acute anaphylaxis, bronchospasm or диспноэ, fever, mnogoformny exudative erythema (including Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), eosinophilia, allergic rhinitis.
• Bodies of a hemopoiesis: Anemia (including hemolitic, aplastic), thrombocytopenia and Werlhof's disease, agranulocytosis, leukopenia.
• Organs of sight: Toxic damage of an optic nerve, not clear sight or doubling, scotoma, dryness and irritation of eyes, chemosis and century (allergic genesis).

The risk of development of ulcerations mucous a GIT, bleedings (gastrointestinal, gingival, uterine, hemorrhoidal), vision disorders (disturbance of color sight, scotoma, damage of an optic nerve) increases at prolonged use of drug in high doses.

Laboratory indicators:

• a bleeding time (can increase)
• concentration of glucose in serum (can decrease)
• clearance of creatinine (can decrease)
• a hematocrit or hemoglobin (can decrease)
• serumal concentration of creatinine (can increase)
• activity of "hepatic" transaminases (can raise)

Interaction with other medicines:

• Efficiency of furosemide and tiazidovy diuretics can be reduced because of the delay of sodium connected with inhibition of synthesis of prostaglandins in kidneys.
• Strengthens effect of indirect anticoagulants, antiagregant, fibrinolitik (increase in risk of emergence of hemorrhagic complications)
• At co-administration with acetylsalicylic acid the ibuprofen reduces its antiagregantny action (possibly increase in frequency of development of acute coronary insufficiency in the patients receiving small doses of acetylsalicylic acid as antiagregantny means).
• Reduces hypotensive activity of vazodilatator (including blockers of slow calcium channels and APF inhibitors).
• In literature isolated cases of increase in plasma concentration of digoxin, Phenytoinum and lithium at a concomitant use of an ibuprofen were described. The means blocking canalicular secretion reduce removal and increase plasma concentration of an ibuprofen.
• Faspik (it is similar to other NPVP) has to be applied with care in a combination with acetylsalicylic acid or other NPVP (it increases risk of development of adverse influences of drug on digestive tract).
• Faspik can increase concentration of a methotrexate in plasma.
• The combined treatment by a zidovudine and Faspik can increase risk of a hemarthrosis and a hematoma at the HIV-positive patients having hemophilia.
• The combined Faspik's use and a takrolimusa can increase risk of development of nephrotoxic action because of reduction of synthesis of prostaglandins in kidneys.
• The ibuprofen strengthens hypoglycemic action of oral hypoglycemic means and insulin; there can be a need of dose adjustment.
• Ulcerogenic action with bleedings at a combination to colchicine, estrogen, ethanol, glucocorticosteroids is described.
• Antacids and Colestyraminum reduce absorption of an ibuprofen.
• Caffeine strengthens analgeziruyushchy effect.
• At appointment with anticoagulating and trombotichesky means (alteplazy, Streptokinasa, an urokinase) the risk of development of bleedings at the same time increases.
• Tsefamandol, цефаперазон, цефотетан, valproic acid, пликамицин increase the frequency of development of a prothrombinopenia.
• Myelotoxic strengthen manifestations of a gematotoksichnost of drug.
• Cyclosporine and drugs of gold strengthen influence of an ibuprofen on synthesis of prostaglandin in kidneys that is shown by increase in nephrotoxicity. The ibuprofen increases plasma concentration of cyclosporine and probability of development of its hepatotoxic effects.
• Inductors of a microsomal oxidation (Phenytoinum, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase products of hydroxylated active metabolites, increasing risk of development of heavy hepatotoxic reactions.
• Inhibitors of a microsomal oxidation reduce risk of a hepatotoxic action.

Contraindications:

• Hypersensitivity to any of the ingredients which are a part of drug. Hypersensitivity to acetylsalicylic acid or other NPVP in the anamnesis.
• Erosive and ulcer diseases of bodies of digestive tract (including a peptic ulcer of a stomach and duodenum in aggravation stages, a disease Krone, nonspecific ulcer colitis).
• "Aspirinovy" asthma.
• Hemophilia and other disturbances of coagulability of blood (including hypocoagulation), hemorrhagic diathesis.
• Bleedings of any etiology.
• Pregnancy.
• Lactation period.
• Children's age up to 12 years.
• Diseases of an optic nerve.

Care is required in the following cases:

• advanced age;
• heart failure;
• arterial hypertension;
• cirrhosis with portal hypertensia;
• liver and/or renal failure, nephrotic syndrome, hyperbilirubinemia;
• a peptic ulcer of a stomach and duodenum (in the anamnesis), gastritis, enteritis, colitis;
• diseases of blood of not clear etiology (leukopenia and anemia);

Overdose:

Symptoms: abdominal pains, nausea, vomiting, block, drowsiness, depression, headache, sonitus, metabolic acidosis, coma, acute renal failure, lowering of arterial pressure, bradycardia, tachycardia, fibrillation of auricles, apnoea.

Treatment: a gastric lavage (only within an hour after reception), absorbent carbon, alkaline drink, an artificial diuresis, symptomatic therapy (correction of an acid-base state, arterial pressure).

Storage conditions:

Period of validity - 3 years. Not to use after the period of validity specified on packaging. To store at a temperature not above 25 °C. To store in the places unavailable to children.

Issue conditions:

Without recipe

Packaging:

On 6 tablets in the blister (polyethylene-aluminum-polyamide). On 1, 2, 4 or 5 blisters together with the instruction on a medical use place in a cardboard pack.