Description
Pharmacological action
Pharmacotherapeutic group:
Combined analgesic (NSAIDs + non-narcotic analgesics + psychostimulant).
ATX code:
N02BE51
Pharmacological properties of
Pharmacodynamics
Safiston 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 propiphenazone 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 anti-inflammatory effect.
The absence of an effect on the synthesis of prostaglandins (PG) in peripheral tissues leads to the absence of a negative effect on the water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa.
Propiphenazone 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 the skeletal muscles, brain, heart, kidneys, reduces platelet aggregation, reduces drowsiness, and a feeling of tiredness.
In this combination, a small dose of caffeine practically does not have a stimulating effect on the central nervous system, but it helps to regulate the tone of the brain vessels, reduces drowsiness, and enhances the analgesic effect of other components of the drug.
Pharmacokinetics
Paracetamol
Absorption – high, binding to plasma proteins – 15%, time to reach maximum plasma concentration (TCmax) – 20-30 min. Penetrates through the blood-brain barrier (BBB). Less than 1% of the dose taken by the nursing mother passes into breast milk.
Therapeutic effective plasma concentration of paracetamol is achieved when administered at a dose of 10-15 mg / kg.
Metabolized in the liver: 80% undergoes a conjugation reaction with glucuronic and sulfuric acids to form inactive metabolites 17% undergoes hydroxylation to form inactive metabolites that conjugate with glutathione and form inactive metabolites.
With a lack of glutadione, these metabolites can block the hepatocyte enzyme systems and cause their necrosis. The elimination half-life is 2-3 hours. In elderly patients, paracetamol clearance decreases and the elimination half-life increases. It is excreted by the kidneys unchanged 3%.
Propiphenazone
The maximum concentration of propiphenazone in plasma is reached after 30 minutes. Metabolized in the liver. The half-life is 1-1.5 hours. The combination with paracetamol increases its elimination time by 40%, which plays a significant role, as allows you to reduce the number of doses of the drug during the day. It is excreted by the kidneys.
Caffeine
Time to reach maximum concentration – 1 h half-life – 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.
Indications
Used to relieve mild to moderate intensity pain of various origins: headache, migraine, toothache, arthralgia, myalgia, algodismenorrhea, as well as an antipyretic for febrile illnesses against the background of infectious and inflammatory diseases (ARVI, in flu, etc.).
Contraindications
Hypersensitivity to the components of the drug,
severe renal and / or liver failure,
deficiency of the glucose-6-phosphate dehydrogenase enzyme,
inhibition of bone marrow hematopoiesis, leukemia, acute leukemia, lemopenia, complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to non-steroidal anti-inflammatory drugs (including history), conditions accompanied by respiratory depression,
intracranial hypertension,
acute myocardial infarction,
coronary heart disease, arrhythmia, arrhythmia, arrhythmia, arrhythmia intestines,
glaucoma,
insomnia,
pregnancy,
lactation in women,
children under 12 years old.
Caution
benign hyperbilirubinemia (including Gilbert, Dubin-Johnson, Rotor syndrome), advanced age, alcoholism, epilepsy and a tendency to seizures.
Use during pregnancy and lactation
The use of the drug during pregnancy and during breastfeeding is contraindicated.
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 caffeinated products (coffee, tea) during treatment may cause overdose symptoms. Taking the drug may make it difficult to diagnose acute abdominal pain.
Effect on the ability to drive vehicles and work with equipment that requires an 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.
Composition of
For 1 tablet:
active substance:
caffeine – 50.0 mg,
paracetamol – 250.0 mg,
propiphenazone – 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
Dosage and administration
Assign 1 to 2 tablets to adults, children 12 to 18 years of age -1 tablet 1 to 3 times a day, preferably 1 to 2 hours after eating, drinking plenty of fluids.
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 without the appointment and supervision of a doctor.
An increase in the daily dose or duration of treatment is possible only under medical supervision. 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, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome).
Drug Interactions
The effectiveness of the drug may decrease with the simultaneous use of cholistiramine, anticholinergics, antidepressants, 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 chlorofenicol increases by 5 times. The simultaneous use of paracetamol in high doses increases the effect of anticoagulants. Myelotoxic drugs increase the hematotoxicity of paracetamol.
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 glycosides, 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 may decrease clearance of theophylline, and possibly other xanthines, increasing the potential for additive pharmacodynamic and other toxic effects. Monoamine oxidase 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 excretion of caffeine. Caffeine is an antagonist of adenosine.
Propiphenazole can enhance the effect of oral hypolipidemic drugs, sulfa drugs, anticoagulants, the ulcerogenic effect of glucocorticosteroids, and reduces the effectiveness of potassium-sparing diuretics.
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 effects, in severe cases – liver failure, increased activity, hepatonec Liver transaminases, an increase in prothrombin time, encephalopathy and coma.
Treatment: gastric lavage, administration of activated carbon, symptomatic therapy, administration of SH-group donors and precursors of glutathione-methionine synthesis 8 9 hours after overdose and N-acetylcysteine 12 hours later.
High doses of caffeine cause the following symptoms: headache, tremor, irritability, gastralgia, agitation, motor anxiety, confusion, tachycardia, arrhythmia, hyperthermia, rapid urination, headache, nausea, vomiting, tinnitus, cramps (in case of acute overdose tonic-clonic).
Treatment: gastric lavage, intake of activated charcoal, laxatives, maintenance of lung ventilation and oxygenation, with convulsions, intravenous diazepam, phenobarbital, maintenance of water-electrolyte balance.
Storage conditions
In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
The Expiration of
is 3 years.
Terms of delivery from pharmacies
Over-the-counter
Form of Treatment
tablets