Safiston 10 pcs Table

Description

Composition
Active substance:
Caffeine – 50.0 mg paracetamol – 250.0 mg, propyphenazone – 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
Description:
Circular tablets from white to white and beige color shade, with little marbling, ploskotsilindricheskoy shape, bevelled on both sides and scored on one side.
Product form:
Tablets.
10 tablets in blisters of PVC film and aluminum foil printed patent.
Or
10 tablets in banks for polyethylene terephthalate or polypropylene drugs for medicines, caps of the capped high-pressure polyethylene having a first opening control, or polypropylene caps System “push-turn” or caps of high density polyethylene with a first control opening.
One bank 1 or contour cell package together with instructions for use placed in a cardboard box (pack).
Contraindications
Increased sensitivity to the drug, severe kidney and / or liver failure, deficiency of the enzyme glucose-6-phosphate dehydrogenase, inhibition of bone marrow hematopoiesis (leukopenia,
anemia, including hemolytic), acute gematoporfiriya, full or partial combination of asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to nonsteroidal anti-inflammatory drugs (including history), states accompanied by respiratory depression, intracranial hypertension, acute myocardial infarction, coronary heart disease, arrhythmias, hypertension, peptic ulcer and duodenal ulcer,
glaucoma, insomnia, pregnancy, lactation in women, children up to 12 years.
Precautions: benign hyperbilirubinemia (including Gilbert syndrome, Dubin-Johnson syndrome, Rotor), old age, alcoholism, epilepsy and susceptibility to seizures.
Indications
Used for pain of mild to moderate intensity of different origin: headache, migraine, toothache, arthralgia, myalgia, tuberculosis, as well as an antipyretic in febrile states against the background of infectious and inflammatory diseases (acute respiratory viral infections, including influenza, etc. .P.).
Interaction with other drugs
Efficacy may be reduced, while the use holistiraminom, anticholinergic antidepressants, alkaline substances. With simultaneous application Safiston® with barbiturates, anticonvulsant, ethanol increases significantly hepatotoxic effect. Metoclopramide accelerates the absorption of paracetamol. Under the influence of the half-life of paracetamol hlorafenikola increased 5 times. The simultaneous use of high doses of paracetamol enhances the anticoagulant effect. Myelotoxicity means increase the expression gematotoksichnosti paracetamol.
Caffeine speeds up the absorption of ergotamine; reduces the absorption of calcium supplementation; reduces the effect of narcotic and hypnotic drugs, increases the excretion of drugs lithium;
It accelerates the absorption and enhances the action of cardiac glycosides and increases their toxicity. The simultaneous use of caffeine with beta-blockers may lead to mutual suppression therapeutic effects, with the beta-adrenergic agonist to an additional stimulation of the central nervous system and other toxic effects.
Caffeine can decrease the clearance of theophylline and other xanthines possible, increasing the possibility of 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 severe high blood pressure. Nicotine increases the rate of caffeine withdrawal. Caffeine is an antagonist of adenosine.
Propifenazol can enhance the effect of oral lipid lowering agents,
sulfa drugs, anticoagulants, corticosteroids ulcerogenic effect reduces the effectiveness of potassium-sparing diuretics.
Overdose
Symptoms (caused by paracetamol occur after ingestion 10-15 g) paleness of the skin, loss of appetite, nausea, vomiting, epigastric pain, nephrotoxicity and hepatotoxicity, in severe cases – hepatic failure, gepatonekroz, increased activity “liver” transaminases , increased prothrombin time, encephalopathy and coma.
Treatment: gastric lavage, appointment of activated carbon, symptomatic therapy, administration donators SH-groups and precursors of glutathione synthesis – methionine through 8-9 hours after the overdose and N-acetylcysteine ​​after 12 hours.
High doses of caffeine cause the following symptoms: headache, tremor, irritability, gastralgia, agitation, restlessness, confusion, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, nausea, vomiting, ringing in the ears, seizures (in acute overdose – tonic-clonic).
Treatment: gastric lavage, administration of activated charcoal, laxatives, maintain ventilation and oxygenation, in convulsions intravenous diazepam, phenobarbital, maintaining fluid and electrolyte balance.
pharmachologic effect
Pharmacodynamics:
Safiston® is a combined preparation, the effect of which is determined by components in its composition. The combination of the three components of the drug leads to mutual reinforcement of their pharmacological action.
Paracetamol and propyphenazone possess analgesic and antipyretic action.
Paracetamol – a non-narcotic analgesic.
Blocking the cyclooxygenase (COX) only in the central nervous system (CNS), acting on pain centers and thermoregulation (in inflamed tissues cellular peroxidase neutralize the effect of paracetamol on (COX), which explains the almost complete absence of anti-inflammatory effect. No effect on the synthesis of prostaglandins (PGs) in peripheral tissues causes lack of a negative effect on water-salt exchange (sodium and water retention) and the mucous of the gastrointestinal tract.
Propyphenazone a pyrazolone derivative. 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. This combination of caffeine in a small dose substantially no stimulating effect on the central nervous system, the brain but contributes to the regulation of vascular tone, reduces somnolence, enhances analgesic effects of other components of the preparation.
Pharmacokinetics:
Paracetamol
Absorption – high, communication with the plasma protein – 15%, time to reach maximum plasma concentration (TSmah) – 20-30 minutes. It penetrates the blood-brain barrier (BBB). Less than 1% of the dose received nursing mother enters the breast milk. The therapeutic effective concentration of paracetamol in plasma achieved when administered at a dose of 10-15 mg / kg.
It is metabolized in the liver: 80% enters the conjugation reaction with glucuronic acid and sulfuric acid with the formation of active metabolites; 17% undergoes hydroxylation with the formation of active metabolites which are conjugated with glutathione to form inactive metabolites. With a lack of glutadiona these metabolites may block the enzyme systems of hepatocytes and cause their death. The half -. 2-3 hours in elderly patients decreases clearance of paracetamol increases the half-life. Excreted by the kidneys unchanged to 3%.
propyphenazone
Propyphenazone maximum concentration in plasma is achieved after 30 minutes. It is metabolized in the liver. The half-life of 1-1.5 hours. The combination with paracetamol increases the time of its removal by 40%, which plays a significant role since reduces the number of receptions of the drug throughout the day. Excreted by the kidneys.
Caffeine
Time to maximum concentration – 1 hour; half-life – 3.5 hours; 65-80% caffeine mainly excreted by the kidneys in the form metilksatina-1, 1-metilmochevoy acids and acetylated derivatives of uracil, a small number of turns in the theophylline and theobromine.
Pregnancy and breast-feeding
Use of the drug during pregnancy and breast-feeding period is contraindicated.
Conditions of supply of pharmacies
Without recipe
side effects
Central nervous system: dizziness, insomnia.
On the part of the gastrointestinal tract: nausea, vomiting, heaviness and discomfort in the stomach;
On the part of the hemopoietic system: thrombocytopenia, agranulocytosis, hemolytic anemia;
Allergic reactions: skin rash, pruritus, urticaria, angioneurotic edema, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).
special instructions
With long-term use of the drug (over 5 days) necessary to monitor patterns of peripheral blood and functional state of the liver. During treatment should abandon the use of alcoholic beverages (increased risk of gastrointestinal bleeding). Excessive consumption of caffeine-containing products (coffee, tea) during treatment can cause symptoms of overdose. The drug may make it difficult to establish the diagnosis at acute abdominal pain syndrome.
Effects on ability to drive and operate machinery which requires high concentration of attention
During the period of administration of the drug should be careful when driving and occupation of other activities that require high concentration and psychomotor speed reactions.
Storage conditions
In the original package (blisters or bank embedded in a pack) at a temperature not higher than
25 ° C.
Keep out of the reach of children.
Dosing and Administration
Assign an adult to 1-2 tablets, children 12-18 years – 1 tablet 1-3 times a day, preferably 1-2 hours after eating, drinking plenty of fluids. The maximum single dose is 2 tablets. The daily dose should not exceed 6 tablets.
The drug should not take more than five days as an analgesic and not more than 3
days as antipyretic without prescription and a physician monitoring. Increasing daily dose or duration of treatment is possible only under medical supervision. Do not exceed the recommended dose.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist