Safiston pills 50mg+250mg+150mg, 20pcs

Composition

For 1 tablet:  active substance:  

• caffeine – 50.0 mg,
• paracetamol-250.0 mg,
• propifenazone-150.0 mg.

excipients: microcrystalline cellulose-100.0 mg, croscarmellose sodium-8.0 mg, sodium carboxymethyl starch -44.8 mg, povidone (polyvinylpyrrolidone) – 18.0 mg, colloidal silicon dioxide-3.2 mg, magnesium stearate-16.0 mg

Pharmacological action

Pharmacotherapy group: Combined analgesic (NSAID+non-narcotic analgesic+psychostimulant). ATX code: N02BE51 Pharmacological PROPERTIESPharmacodynamics AFISTON is a combination drug whose action is determined by the components that make up its composition. The combination of the three components of the drug leads to a mutual strengthening of their pharmacological action. Paracetamol and propifenazone have analgesic and antipyretic effects. Paracetamol is a 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 an anti-inflammatory effect. The lack of influence on the synthesis of prostaglandins (PG) in peripheral tissues means that it has no negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa. Propifenazone is a pyrazolone derivative. The mechanism of action is achieved by inhibiting COX, which is involved in the formation of prostaglandins from arachidonic acid. Caffeine increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, expands the blood vessels of skeletal muscles, brain, heart, kidneys, reduces 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 helps regulate the tone of brain vessels, reduces drowsiness, and increases the analgesic effect of other components of the drug. Pharmacokineticsparacetamolabsorption-high, binding to plasma proteins-15%, time to reach the maximum concentration in blood plasma (TMAX) – 20-30 minutes. 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 prescribed at a dose of 10-15 mg / kg. It is metabolized in the liver: 80% reacts by conjugation with glucuronic and sulfuric acids to form inactive metabolites; 17% undergoes hydroxylation to form inactive metabolites that conjugate with glutathione and form inactive metabolites. When glutathione is deficient, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The elimination half-life is 2-3 hours. In elderly patients, the clearance of paracetamol decreases and the elimination half-life increases. 3% is excreted unchanged by the kidneys. Propifenazone The maximum plasma concentration of propifenazone is reached after 30 minutes. It is metabolized in the liver. The half-life is 1-1.5 hours. Combination with paracetamol increases the time of its elimination by 40%, which plays a significant role, because it reduces the number of drug doses during the day. It is excreted by the kidneys. Caffeine The time to reach the maximum concentration is 1 hour; the half-life is 3.5 hours; 65-80% of caffeine is excreted by the kidneys mainly in the form of 1-methylxatin,1-methylmoic acid and acetylated uracil derivatives, a small amount is converted to theophylline and theobromine.

Indications

It is used for relief of mild and moderate intensity pain syndrome of various genesis: headache, migraine, toothache, arthralgia, myalgia, algodismenorrhea, as well as as an antipyretic agent for febrile conditions against the background of infectious and inflammatory diseases (ARVI, including influenza, etc. ).

Use during pregnancy and lactation

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

Contraindications

• Hypersensitivity to the drug,
• severe renal and/or hepatic insufficiency,
• deficiency of the enzyme glucose-6-phosphate dehydrogenase,
• inhibition of bone marrow hematopoiesis (leukopenia, anemia, including hemolytic),
• sharp hematoporphyrin,
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to non-steroidal anti-inflammatory drugs (including in history), condition accompanied by respiratory depression,
• intracranial hypertension,
• acute myocardial infarction,
• ischemic heart disease, arrhythmias,
• arterial hypertension,
• gastric ulcer and duodenal ulcer,
• glaucoma,
• insomnia,
• pregnancy,
• lactation in women,
• children up to age 12 years.

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

Side effects

From the central nervous system: dizziness, insomnia. From the gastrointestinal tract: nausea, vomiting, heaviness and unpleasant sensations in the stomach; From the hematopoietic system: thrombocytopenia, agranulocytosis, hemolytic anemia; Allergic reactions: skin rash, pruritus, urticaria, angioedema, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Interaction

The effectiveness of the drug may decrease when used simultaneously with cholistyramine, cholinolytics, antidepressants, and alkaline substances. With the simultaneous use of Safiston with barbiturates, anticonvulsants, ethanol, the hepatotoxic effect significantly increases. Metoclopramide accelerates the absorption of paracetamol. Under the influence of paracetamol, the half-life of chlorafenicol increases by 5 times. Concomitant 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 hypnotic drugs, increases the excretion of lithium preparations; accelerates the absorption and enhances the effect of cardiac glycosides, increases their toxicity. Concomitant 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 may reduce the clearance of theophylline, and possibly other xanthines, increasing the possibility of additive pharmacodynamic and other toxic effects. Monoamine oxidase inhibitors, furazolidone, procarbazine, selegiline, and high doses of caffeine can cause dangerous cardiac arrhythmias or a pronounced increase in blood pressure. Nicotine increases the rate of caffeine elimination. Caffeine is an adenosine antagonist. Propifenazole can enhance the effect of oral lipid-lowering agents, sulfonamide preparations, anticoagulants, ulcerogenic effect of glucocorticosteroids, reduces the effectiveness of potassium-sparing diuretics.

How to take, course of use and dosage

Assign adults 1-2 tablets, children 12-18 years-1 tablet 1-3 times a day, preferably 1-2 hours after meals, washed down with 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 an analgesic and no more than 3 days as an antipyretic without a doctor’s prescription and supervision. An increase in the daily dose or duration of treatment is possible only under the supervision of a doctor. Do not exceed the recommended dose.

Overdose

Symptoms: (due to paracetamol, appear after taking 10-15 g) pallor of the skin, decreased appetite, nausea, vomiting, epigastric pain, hepatotoxic and nephrotoxic effects, in severe cases-liver failure, hepatonecrosis, increased activity of “liver” transaminases, increased prothrombin time, encephalopathy and coma. Treatment: gastric lavage, use of activated charcoal, symptomatic therapy, use of SH-group donors and glutathione – methionine synthesis precursors 8-9 hours after overdose and N-acetylcysteine after 12 hours. High doses of caffeine cause the following symptoms: headache, tremor, irritability, gastralgia, restlessness, motor restlessness, confusion, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, nausea, vomiting, ringing in the ears, convulsions (in acute overdose-tonic-clonic). Treatment: gastric lavage, taking activated charcoal, laxatives, maintaining lung ventilation and oxygenation, intravenous diazepam, phenobarbital for convulsions, maintaining water and electrolyte balance.

Special instructions

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

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

Excessive consumption of caffeinated products (coffee, tea) during treatment can cause symptoms of overdose. Taking the drug may make it difficult to establish a diagnosis of acute abdominal pain syndrome.

Influence on the ability to drive vehicles and work with equipment that requires 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 increased concentration of attention and speed of psychomotor reactions.

Storage conditions

In a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years.

Active ingredient

Caffeine, Paracetamol, Propifenazone

Dosage form

Tablets