Safiston - instructions for use, dose, side effects, contraindications

Active vegetation: caffeine 50.0 mg, paracetamol 250.0 mg, propiphenazone 150.0 mg. Excipients: cellulose microcrystalline - 100.0 mg, croscarmellose sodium - 8.0 mg, sodium carboxymethyl starch - 44.8 mg, povidone (polyvinylpyrrolidone) - 18.0 mg, silicon dioxide colloid - 3.2 mg, magnesium stearate - 16.0 mg .

Description:

Round tablets from white to white with a beige shade of color, with an insignificant marble, a flat-cylindrical shape, with a facet on both sides and a risk on one side.

Pharmacotherapeutic group:Analgesic combined (NSAIDs + analgesic non-narcotic remedy + psychostimulant)

ATX: & nbsp

N.02.B.E Anilides

Pharmacodynamics:

Safiston is a combination drug, the effect of which is determined by the components that make up its composition. The combination of the three components of the drug leads to a mutual enhancement of their pharmacological action.

Paracetamol and propifenazone have an analgesic and antipyretic effect. Paracetamol non-narcotic analgesic. It blocks cyclooxygenase (COX) only in the central nervous system (CNS), affecting the centers of pain and thermoregulation (in inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX), which explains the almost complete absence of anti-inflammatory effect. The absence of influence on the synthesis of prostaglandins (PG) in peripheral tissues determines the absence of a negative influence on the water-salt metabolism (sodium and water retention) and the mucosa of the gastrointestinal tract.

Propyphenazone is a derivative of pyrazolone. The mechanism of action is carried out by inhibiting COX involved in the formation of prostaglandins from arachidonic acid.

Caffeine increases the excitability of spinal cord reflex, excites the respiratory and vasomotor centers, dilates blood vessels in skeletal muscle, brain, heart, kidneys, reducing platelet aggregation; reduces drowsiness, fatigue. In this combination caffeine in a small dose practically does not have a stimulating effect on the central nervous system, but it contributes to the regulation of the tone of the vessels of the brain, reduces drowsiness, intensifies the analgesic effect of other components of the drug.

Pharmacokinetics:

Paracetamol

Absorption is high, the connection with plasma proteins is 15%, the time to reach the maximum concentration in the blood plasma (TCata) - 20-30 min. Penetrates through blood-brain barrier (BBB). Less than 1% of the accepted dose of breastfeeding mothers penetrates into breast milk. The therapeutic effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg.

Metabolised in the liver: 80% reacts with glucuronic acid and sulfuric acid to form inactive metabolites; 17% is hydroxylated to form inactive metabolites, which are conjugated to glutathione and form inactive metabolites. With a lack of glutadione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The half-life is 2-3 hours. In elderly patients paracetamol clearance decreases and the half-life increases.It is excreted by the kidneys in an unchanged form of 3%.

Propyphenazone

The maximum concentration of propiphenazone in plasma is reached after 30 minutes. Metabolised in the liver. The half-life period is 1-1.5 hours. The combination with paracetamol increases the time of its elimination by 40%, which plays a significant role, since it allows reducing the number of medications during the day. It is excreted by the kidneys. Caffeine

The time to reach the maximum concentration -1h; the half-life is 3.5 hours; 65- 80% caffeine is excreted by the kidneys mainly in the form of 1-methylxatine, 1-methyl uric acid and acetylated derivatives of uracil, a small amount turns into theophylline and theobromine.

Indications:

Apply for the relief of pain syndrome of mild and moderate intensity of different genesis: headache, migraine, toothache, arthralgia, myalgia, algodismenorea, and also as an antipyretic agent in feverish conditions against the background of infectious and inflammatory diseases (ARVI, including influenza, etc.).

Contraindications:

Hypersensitivity to the components of the drug, severe renal and / or liver failure, deficiency of the enzyme glucose-6-phosphate dehydrogenase, oppression of bone marrow hematopoiesis (leukopenia, anemia, incl.hemorrhagic), acute hematoporphyria, complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to the anti-inflammatory drugs (including in the anamnesis), conditions accompanied by respiratory depression, intracranial hypertension, acute myocardial infarction, coronary heart disease, arrhythmias, arterial hypertension, peptic ulcer of stomach and duodenum, glaucoma, insomnia, pregnancy, lactation in women, children under 12 years.

Carefully:

benign hyperbilirubinemia (including Gilbert syndrome, Dubin-Johnson syndrome, Rotor), elderly age, alcoholism, epilepsy and propensity to convulsive seizures.

Pregnancy and lactation:

The use of the drug during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

Assign adults for 1 - 2 tablets, children 12-18 years - 1 tablet 1-3 times a day, preferably 1-2 hours after eating, squeezed large amounts of liquid. The maximum single dose of 2 tablets. The daily dose should not exceed 6 tablets.

The drug should not be taken for more than 5 days as an anesthetic and not more than 3 days as an antipyretic agent without prescribing and monitoring the doctor. An increase in the daily dose or duration of treatment is possible only under the supervision of a physician.

Do not exceed the recommended dose.

Side effects:

From the central nervous system: dizziness, insomnia.

From the gastrointestinal tract: nausea, vomiting, heaviness and discomfort in the stomach;

From the hematopoietic system: thrombocytopenia, agranulocytosis, hemolytic anemia;

Allergic reactions: skin rash, itching, urticaria, Quincke's edema, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome).

Overdose:

Symptoms: (caused by paracetamol, appear after taking 10-15 g) pallor of the skin, decreased appetite, nausea, vomiting, pain in the epigastric region, hepatotoxic and nephrotoxic effect, in severe cases - liver failure, hepatonecrosis, increased activity of "liver" transaminases, increase prothrombin time, encephalopathy and coma.

Treatment: gastric lavage, the appointment of activated charcoal, symptomatic therapy, the introduction of donators SH-groups and precursors of glutathione-methionine synthesis 8-9 hours after an overdose and N-acetylcysteine after 12 hours. High doses of caffeine cause the following symptoms: headache, tremor, irritability, gastralgia, agitation, motor anxiety, confusion, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, nausea, vomiting, ringing in the ears, convulsions (with acute overdose - tonic-clonic). Treatment: gastric lavage, the reception of activated carbon, laxatives, maintenance of ventilation and oxygenation, with convulsions intravenously diazepam, phenobarbital, maintaining the water-electrolyte balance.

Interaction:

The effectiveness of the drug may decrease with simultaneous use with holistiramine, anticholinergics, antidepressants, alkaline substances. With the simultaneous use of Safiston with barbiturates, anticonvulsant drugs, ethanol, hepatotoxic effect is significantly increased. Metoclopramide accelerates the absorption of paracetamol.Under the influence of paracetamol, the half-life of chloraphenicol increases five-fold. Simultaneous use of paracetamol in high doses increases the effect of anticoagulants. Myelotoxic agents increase the manifestation of hematotoxicity of paracetamol.

Caffeine accelerates the absorption of ergotamine; reduces absorption of calcium preparations; reduces the effect of narcotic and hypnotics, increases the excretion of lithium preparations; accelerates absorption and enhances the action of cardiac glycosides, increases their toxicity. Simultaneous use of caffeine with beta-blockers can lead to mutual suppression of therapeutic effects, with beta-adrenomimetics to additional stimulation of the central nervous system and other toxic effects. Caffeine can reduce the clearance of theophylline, and possibly other xanthines, increasing the possibility of additive pharmacodynamic and other toxic effects. Inhibitors of monoamine oxidase, furazolidone, procarbazine, selegiline and large doses of caffeine can cause the development of dangerous cardiac arrhythmias or a marked increase in blood pressure. Nicotine increases the caffeine removal rate. Caffeine is an adenosine antagonist.

Propifenazole can increase the effect of oral lipid-lowering drugs, sulfonamide drugs, anticoagulants, ulcerogenic effect of glucocorticosteroids, reduces the effectiveness of potassium-sparing diuretics.

Special instructions:With prolonged use of the drug (more than 5 days), control of the picture of peripheral blood and the functional state of the liver is necessary. During treatment, you should stop using alcohol-containing beverages (increased risk of gastrointestinal bleeding). Excessive consumption of caffeinated products (coffee, tea) on the background of treatment can cause symptoms of an overdose. Taking the drug may make it difficult to establish a diagnosis for acute abdominal pain syndrome.

Effect on the ability to drive transp. cf. and fur:During the period of taking the drug, care should be taken when driving vehicles and engaging in other activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Pills.

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50, 60 or 100 tablets in cans of polymeric for medicines. One jar or 1, 2, 3, 4, 5, 6 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-002203

Date of registration:27.08.2013

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp27.08.2013

Illustrated instructions

Instructions

Safiston (Safiston)