Safiston tablets, No. 20

Relief of pain syndrome of weak and medium intensity of various origins:

• headache;

• migraine;

• toothache;

• arthralgia;

• myalgia;

• algodismenorrhea;

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

Prescribe 1-2 tablets for adults, for children 12-18 years old - 1 tablet 1-3 times a day, preferably 1-2 hours after eating, drinking plenty 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 a pain reliever and no more than 3 days as an antipyretic agent without the appointment and supervision of a 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.

Tablets from white to white with a beige shade, round, with slight marbling, flat-cylindrical shape, beveled on both sides and scored on one side.

caffeine 50 mg

paracetamol 250 mg

propiphenazone 150 mg

Excipients: microcrystalline cellulose 100 mg, croscarmellose sodium 8 mg, sodium carboxymethyl starch 44.8 mg, povidone 18 mg, colloidal silicon dioxide 3.2 mg, magnesium stearate 16 mg.

• Hypersensitivity to the components of the drug;

• severe renal and / or hepatic impairment;

• 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 polyposis of the nose and paranasal sinuses and NSAID intolerance (including a history);

• conditions accompanied by respiratory depression;

• intracranial hypertension;

• acute myocardial infarction;

• coronary heart disease;

• arrhythmias;

• arterial hypertension;

• peptic ulcer of the stomach and duodenum;

• glaucoma;

• insomnia;

• pregnancy;

• lactation period;

• children under 12 years of age.

With care: benign hyperbilirubinemia (including Gilbert's syndrome, Dubin-Johnson, Rotor), old age, alcoholism, epilepsy and a tendency to seizures.

pharmachologic effect

Safiston is a combined drug, 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 propiphenazone have analgesic and antipyretic effects. Paracetamol is a non-narcotic analgesic. It blocks cyclooxygenase (COX) only in the central nervous system, 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 an anti-inflammatory effect. The lack of influence on the synthesis of prostaglandins (PG) in peripheral tissues causes the absence of a negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa.

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

Caffeine increases the reflex excitability of the spinal cord, stimulates the respiratory and vasomotor centers, dilates the blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation; reduces drowsiness, fatigue. In this combination, a small dose of caffeine practically does not have a stimulating effect on the central nervous system, however, it helps to regulate the tone of the cerebral vessels, reduces drowsiness, and enhances the analgesic effect of other components of the drug.

Pharmacokinetics

Paracetamol

Absorption - high, plasma protein binding - 15%, TCmax - 20-30 min. Penetrates the blood-brain barrier (BBB). Less than 1% of the dose taken by a nursing mother passes 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.

It is metabolized in the liver: 80% enters into a conjugation reaction with glucuronic and sulfuric acids to form inactive metabolites: 17% undergoes hydroxylation to form inactive metabolites, which converge with glutathione and form inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. T1 / 2 - 2-3 hours. In elderly patients, paracetamol clearance decreases and the half-life increases. It is excreted by the kidneys unchanged 3%.

Propyphenazone

The maximum plasma concentration of propiphenazone is reached after 30 minutes. It is metabolized in the liver. T1 / 2 is 1-1.5 hours. The combination with paracetamol increases the time of its elimination by 40%, which plays a significant role, because it allows you to reduce the number of doses of the drug during the day. It is excreted by the kidneys.

Caffeine

Time to reach Cmax - 1 hour; T1 / 2 - 3.5 h; 65-80% of caffeine is excreted by the kidneys, mainly in the form of 1-methylxatin, 1-methyl uric acid and acetylated uracil derivatives, a small amount is converted to theophylline and theobromine.

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 hematopoietic system: thrombocytopenia, agranulocytosis, hemolytic anemia.

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

Contraindications for use

• hypersensitivity to drug components;

• severe renal and / or hepatic impairment;

• 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 polyposis of the nose and paranasal sinuses and NSAID intolerance (including a history);

• conditions accompanied by respiratory depression;

• intracranial hypertension;

• acute myocardial infarction;

• coronary heart disease;

• arrhythmias;

• arterial hypertension;

• peptic ulcer of the stomach and duodenum;

• glaucoma;

• insomnia;

• pregnancy;

• lactation period;

• children under 12 years of age.

With care: benign hyperbilirubinemia (including Gilbert's syndrome, Dubin-Johnson, Rotor), old age, alcoholism, epilepsy and a tendency to seizures.

Application during pregnancy and lactation

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

Application for violations of liver function

Contraindicated in severe hepatic impairment.

Application for impaired renal function

Contraindicated in severe renal failure.

Application in children

Contraindicated in children under 12 years of age.

Use in elderly patients

With caution in old age.

special instructions

With prolonged use of the drug (more than 5 days), it is necessary to control the picture of peripheral blood and the functional state of the liver.

During treatment, you should stop drinking alcoholic beverages (increased risk of gastrointestinal bleeding).

Excessive consumption of caffeine-containing products (coffee, tea) during treatment can cause overdose symptoms.

Taking the drug can make it difficult to establish a diagnosis in acute abdominal pain syndrome.

Impact on the ability to drive vehicles and work with equipment that requires increased concentration

During the period of taking the drug, care should be taken when driving vehicles and engaging in other activities that require increased concentration of attention and speed of psychomotor reactions.

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 effects, 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 diet, symptomatic therapy, the introduction of SH-group donors and precursors of the synthesis of glutathioia-mstionia 8-9 hours after the overdose and N-acetylcysteine ??after 12 hours.

High doses of caffeine cause the following symptoms: headache, tremors, irritability, gastralgia, agitation, motor restlessness, confusion, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, nausea, vomiting, ringing in the ears, convulsions (in case of acute overdose - tonko-clonic).

Treatment: gastric lavage, intake of activated charcoal, laxatives, maintenance of ventilation for oxygenation. for convulsions, intravenous diazepam, phenobarbital, maintenance of water-electrolyte balance.

Drug interactions

The effectiveness of the drug may decrease with simultaneous use with cholestyramine, anticholinergics, antidepressants, alkaline substances.

With the simultaneous use of Safiston with barbiturates, anticonvulsants, ethanol, the hepatotoxic effect is significantly increased.

Metoclopramide accelerates the absorption of paracetamol.

Under the influence of paracetamol, the half-life of chlorafenicol is increased by 5 times.

The simultaneous use of paracetamol in high doses increases the effect of anticoagulants.

Myelotoxic agents increase the manifestations of paracetamol hematotoxicity.

Caffeine accelerates the absorption of ergotamine; reduces the 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 glcosides, increases their toxicity.

The simultaneous use of caffeine with beta-blockers can lead to mutual suppression of therapeutic effects, with beta-adrenergic agonists to additional stimulation of the central nervous system and other toxic effects.

Caffeine can decrease the clearance of theophylline, and possibly other xanthines, increasing the potential for additive pharmacodynamic and other toxic effects.

Monoamine ocendase inhibitors, 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 elimination.

Caffeine is an adenosine antagonist.

Propyphenazone can enhance the effect of oral lipid-lowering drugs, sulfa drugs., Anticoagulants, the ulcerogenic effect of glucocorticosteroids, reduces the effectiveness of potassium-sparing diuretics.