Universal reference book for medicines
Name of the drug: SAFISTON (SAFISTON)

Active substance: caffeine, paracetamol, propyphenazone

Type: Analgesic-antipyretics of combined composition

Manufacturer: ATOLL (Russia) manufactured by OZONE (Russia)

Composition, form of production and packaging
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Tablets from white to white with a beige shade of color, round, with a slight marble, flat-cylindrical shape, with a facet on both sides and risk from one side.
1 tab.

caffeine 50 mg

paracetamol 250 mg

propiphenazone 150 mg

[PRING] cellulose microcrystalline 100 mg, croscarmellose sodium 8 mg, sodium carboxymethyl starch 44.8 mg, povidone 18 mg, silicon dioxide colloid 3.2 mg, magnesium stearate 16 mg.

10 pieces.
- Cellular outline packaging (aluminum / PVC) (1) - cardboard packs.
10 pieces.
- Cellular outline packaging (aluminum / PVC) (2) - cardboard packs.
10 pieces.
- Cellular outline packaging (aluminum / PVC) (3) - cardboard packs.
10 pieces.
- Cellular outline packaging (aluminum / PVC) (4) - cardboard packs.
10 pieces.
- Cellular outline packaging (aluminum / PVC) (5) - cardboard packs.
10 pieces.
- Cellular outline packaging (aluminum / PVC) (6) - cardboard packs.
10 pieces.
- Cellular outline packaging (aluminum / PVC) (10) - cardboard packs.
10 pieces.
- polymer cans (1) - packs of cardboard.
20 pcs.
- polymer cans (1) - packs of cardboard.
30 pcs.
- polymer cans (1) - packs of cardboard.
40 pcs.
- polymer cans (1) - packs of cardboard.
50 pcs.
- polymer cans (1) - packs of cardboard.
60 pcs.
- polymer cans (1) - packs of cardboard.
100 pieces.
- polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Safiston is a combined preparation, the action 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 is a non-narcotic analgesic. It blocks cyclooxygenase (COX) only in the central nervous system, affecting the centers of pain and thermoregulation (in inflammatory 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 gastrointestinal mucosa.
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 reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, dilates the blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation;
reduces drowsiness, fatigue. In this combination, caffeine in a small dose has virtually no stimulating effect on the central nervous system, but it helps regulate the tone of the brain vessels, reduces drowsiness, and increases the analgesic effect of other components of the drug.
PHARMACOKINETICS

Paracetamol

Absorption is high, the connection with plasma proteins is 15%, TC max is 20-30 min.
Penetrates through the 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.
Metabolized in the liver: 80% conjugates with glucuronic and sulfuric acids with the formation of inactive metabolites: 17% is hydroxylated to form inactive metabolites that are konjugated with glutathione and form inactive metabolites.
With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. T 1/2 - 2-3 hours. In elderly patients paracetamol clearance decreases and 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. T 1/2 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 a day. It is excreted by the kidneys.
Caffeine

Time to reach C max - 1 h;
T 1/2 - 3.5 hours; 65-80% of caffeine is excreted by the kidney 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

Management of pain syndrome of mild and moderate intensity of various genesis:

- headache;

- Migraine;

- toothache;

- arthralgia;

- myalgia;

- algodismenorea;

As an antipyretic agent in feverish conditions against the background of infectious and inflammatory diseases (ARVI, including influenza, etc.).

DOSING MODE

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 is 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 EFFECT

From the side of the central nervous system: dizziness, insomnia.

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

From the hemopoietic system: thrombocytopenia, agranulocytosis, hemolytic anemia.

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

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, including hemolytic);

- acute hematoporphyria;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to NSAIDs (including in history);

- conditions accompanied by respiratory depression;

- intracranial hypertension;

acute myocardial infarction;

- cardiac ischemia;

- arrhythmia;

- arterial hypertension;

- Stomach ulcer and duodenal ulcer;

- glaucoma;

- Insomnia;

- Pregnancy;

- lactation period;

- Children under 12 years old.

With caution: benign hyperbilirubinemia (including Gilbert's 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.

APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated in severe renal failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in severe hepatic insufficiency.

APPLICATION FOR CHILDREN

Contraindicated for children under 12 years.

APPLICATION IN ELDERLY PATIENTS

With caution in old age.

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.

Influence on the ability to drive vehicles and work with techniques that require increased concentration of attention

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.

OVERDOSE

Symptoms: (due to paracetamol, appear after taking 10-15 g) pallor of the skin, decreased appetite, nausea, vomiting, pain in the epigastric region, hepatotoxic and nephrotoxic action, in severe cases - liver failure, hepatonecrosis.
increased activity of "hepatic" transaminases, increased prothrombin time, encephalopathy and coma.
Treatment: gastric lavage, the appointment of an activated fistula, symptomatic therapy, the introduction of donors of SH-groups and the precursors of the synthesis of glutathione -mstionium in 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 - tons-clonic).

Treatment: gastric lavage, reception of activated carbon, laxatives, maintenance of ventilation of lungs and oxygens.
with convulsions intravenously diazepam, phenobarbital, maintenance of water-electrolyte balance.
DRUG INTERACTION

The effectiveness of the drug may decrease with simultaneous use with colestyramine, 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 glkkozidov, increases their toxicity.
Simultaneous use of caffeine with beta-adrenoblocker can lead to mutual suppression of therapeutic effects, with beta-adrenomimetics to additional stimulation of the CNS 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 rate of caffeine withdrawal.

Caffeine is an antagonist of adenosine.

Propiphenazone can increase the effect of oral hypolipidemic drugs, sulfonamide drugs., Anticoagulants, ulcerogenic effect of glucocorticosteroids, reduces the effectiveness of potassium-sparing diuretics.

TERMS OF RELEASE FROM PHARMACY

Without recipe.

TERMS AND CONDITIONS OF STORAGE

In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children. Shelf life - 3 years.
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