Aspinat plus

General characteristics. Structure:

Active agent: acetylsalicylic acid of 500 mg; caffeine of 50 mg.

Pharmacological properties:

The combined drug which effect is defined by the components which are its part. The combination of components of drug provides the best portability of symptoms of an indisposition and fever at "catarrhal" and other infectious and inflammatory diseases, decrease in a pain syndrome of various origin. Acetylsalicylic acid has the antiinflammatory, analgeziruyushchy and febrifugal effect connected with suppression of cyclooxygenase 1 and 2, prostaglandins regulating synthesis. As a result prostaglandins providing formation of hypostasis and hyperalgesia are not formed. Decrease in content of prostaglandins (E1 is preferential) in the center of thermal control leads to decrease in body temperature owing to vasodilatation of skin and increase of sweating. The analgesic effect is caused by both the central, and peripheral action. Reduces aggregation, a platelet stickness and a thrombogenesis due to suppression of synthesis of A2 thromboxane in thrombocytes. The Antiagregantny effect remains within 7 days after a single dose (it is more expressed at men, than at women). Caffeine increases reflex irritability of a spinal cord, excites the respiratory and vasomotor centers, expands blood vessels of skeletal muscles, a brain, heart, kidneys, reduces aggregation of thrombocytes, reduces drowsiness and feeling of fatigue, increases intellectual and physical effeciency.

Pharmacokinetics. Acetylsalicylic acid during absorption is exposed to system elimination in a wall of intestines and in a liver (is deacetylated). The absorbed part quickly is hydrolyzed by cholinesterases of plasma and albuminesterase therefore T1/2 - no more than 15-20 min. In an organism circulates (for 75-90% in connection with albumine) and it is distributed in fabrics in the form of anion of salicylic acid. Cmax of salicylic acid is reached approximately in 2 h. Easily gets into many fabrics and liquids of an organism, including into cerebrospinal fluid, peritoneal and synovial liquids. Penetration into a cavity of a joint accelerates in the presence of a hyperemia and hypostasis and is slowed down in a proliferative phase of an inflammation. In small amounts salicylates are found in nervous tissue, traces - in bile, sweat, excrements. When developing acidosis the most part of salicylate turns into not ionized acid which is well getting into fabrics including into a brain. Quickly passes through a placenta, in small amounts it is removed with breast milk. It is metabolized preferential in a liver with formation of 4 metabolites found in many fabrics and urine. It is removed preferential by active secretion in tubules of kidneys in the form of actually salicylic acid (60%) and its metabolites. Removal of not changed salicylate depends from рН urine (at alkalinization of urine the ionizirovaniye of salicylates increases, their reabsorption worsens and considerably removal increases). Speed of removal depends on a dose: at reception of small doses of T1/2 - 2-3 h, with increase in a dose can increase up to 15-30 h.

Absorption of caffeine happens generally due to simple diffusion. Cmax - is reached approximately in 50-75 min. after intake. It is quickly distributed in all bodies and body tissues; easily gets through a blood-brain barrier and a placenta. Communication with blood proteins (albumine) - 25-36%. It is metabolized preferential in a liver. At adults about 80% of a dose of caffeine are metabolized in paraxanthine, about 10% - in theobromine and about 4% - in theophylline. These connections demetilirutsya afterwards in monomethylxanthines, and then in metilirovanny derivatives of uric acid. T1/2 adults have 3.9-5.3 h (sometimes - to 10 h). Removal of caffeine and its metabolites is carried out by kidneys.

Indications to use:

— moderately or poorly expressed pain syndrome of various origin (a headache, a dentagra, migraine, neuralgia, an arthralgia, a lumbago, a radicular syndrome, muscular pain, pains at periods);
— the increased body temperature at catarrhal and other infectious and inflammatory diseases (at adults and children 15 years are more senior).

Route of administration and doses:

Inside. For reduction of irritant action by a GIT drug should be accepted after food, washing down with water, milk, alkaline mineral water.
For treatment of a pain syndrome and the increased body temperature to adults and children 15 years on 1-2 tablets are more senior; maximum single dose 2 tablets; maximum daily dose of 6 tablets.
For treatment of a pain syndrome, except for states at the acute respiratory diseases caused by viral infections (risk of development of a syndrome to Reja) to children aged from 6 up to 12 years 1/2 tablets, from 12 to 15 years 1/2-1 tablet.
Single dose if necessary 3-4 times in days with an interval accept not less than 4 h. Treatment duration (without consultation with the doctor) should not exceed 7 days at appointment as anesthetic and 3 days - as an antipyretic.

Features of use:

Before surgical intervention for reduction of bleeding during operation and in the postoperative period it is necessary to cancel administration of drug in 5-7 days and to inform the doctor.
It is necessary to consider that at predisposed patients acetylsalicylic acid (even in small doses) reduces removal of uric acid from an organism and can become the reason of development of a bad attack of gout.
During treatment it is necessary to refuse alcohol intake (increase in risk of gastrointestinal bleeding).
The excessive use of kofeinsoderzhashchy products (coffee, tea) against the background of treatment can cause overdose symptoms caffeine.

Side effects:

- From digestive tract: nausea, loss of appetite, gastralgia, diarrhea.
- From system of a hemopoiesis: thrombocytopenia, anemia, leukopenia. Allergic reactions: skin rash, Quincke's disease, bronchospasm.
- From the central nervous system: sleeplessness.
- From cardiovascular system: tachycardia, increase in arterial pressure.
- Other: abnormal liver function and/or kidneys; a syndrome to Reja (encephalopathy and acute fatty dystrophy of a liver with bystry development of a liver failure).
- At prolonged use can arise: dizziness, a headache, vomiting, GIT erosive cankers, hypocoagulation, bleedings (including in a GIT), vision disorders, decrease in auditory acuity, a sonitus, a bronchospasm, intersticial nephrite, a prerenalny azotemia with a giperkreatininemiya and a hypercalcemia, a papillary necrosis, an acute renal failure, a nephrotic syndrome, aseptic meningitis, strengthening of symptoms of chronic heart failure, hypostases, increase in activity of "hepatic" transaminases.
At emergence of similar symptoms it is recommended to stop administration of drug and to see immediately the attending physician.

Interaction with other medicines:

Acetylsalicylic acid increases toxicity of a methotrexate, reducing its renal clearance, effects of narcotic analgetics, other NPVP, peroral hypoglycemic drugs, heparin, indirect anticoagulants, trombolitik and antiagregant; reduces effect of uricosuric medicines (бензбромарон, Sulfinpyrazonum), antihypertensives, diuretics (Spironolactonum, furosemide); increases concentration of digoxin, barbiturates, lithium salts in plasma. Glucocorticosteroids, ethanol and etanolsoderzhashchy medicines strengthen negative impact on a mucous membrane of a GIT and increase risk of development of gastrointestinal bleedings. The antacids containing magnesium and/or aluminum slow down and worsen absorption of acetylsalicylic acid. Miyelotoksichny medicines strengthen manifestations of a gematotoksichnost of drug.

Caffeine reduces effect of narcotic analgetics and somnolent medicines, reduces absorption of the drugs Sa2 + in a GIT, increases removal of the drugs Li + with urine, accelerates absorption and strengthens effect of cardiac glycosides, increases their toxicity. Combined use of caffeine with beta adrenoblockers can lead to mutual suppression of therapeutic effects. Meksiletin - reduces removal of caffeine to 50%; nicotine - increases caffeine removal speed.

Contraindications:

— hypersensitivity to acetylsalicylic acid, other non-steroidal anti-inflammatory drugs (NPVP), xanthines and other components of drug;
— digestive tract erosive cankers (in an aggravation phase);
— gastrointestinal bleeding;
— hemophilia, hemorrhagic diathesis, prothrombinopenia;
— the bronchial asthma induced by reception of salicylates and other NPVP;
— a full or not full combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid;
— organic diseases of cardiovascular system (including an acute myocardial infarction, atherosclerosis, the stratified aortic aneurysm);
— arterial hypertension, portal hypertensia;
— glaucoma;
— renal failure;
— alarming frustration, hyperexcitability, sleep disorder;
— lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption;
— a concomitant use with a methotrexate in a dose more than 15 mg a week;
— to children up to 6 years at a pain syndrome (for this dosage form);
— to children and teenagers aged up to 15 years (at use as febrifugal) with the acute respiratory diseases caused by viral infections in connection with risk of development of a syndrome to Reja (encephalopathy and acute fatty dystrophy of a liver with acute development of a liver failure), - pregnancy (I and III trimester);
— lactation period.

With care. With care appoint at gout, a hyperuricemia since acetylsalicylic acid in small doses can provoke a gout attack at the patients predisposed to development of gout (with reduced removal of uric acid from an organism). It is necessary to be careful in the presence in the anamnesis of cankers of the digestive tract (DT), gastrointestinal bleedings, a renal and liver failure. It is also necessary to be careful at deficit of vitamin K and glyukozo-6-fosfatdegidrogenazy.

The concomitant use of acetylsalicylic acid with a methotrexate in doses can lead less than 15 mg a week to increase in frequency of emergence of side effects from bodies of a hemopoiesis.

Use of acetylsalicylic acid can cause a bronchospasm in patients with bronchial asthma, hay fever, polipozy a mucous membrane of a nose, chronic respiratory diseases, allergic reactions to other medicines.

It is necessary to consider that at simultaneous use with acetylsalicylic acid effect of heparin and indirect anticoagulants amplifies.

It is necessary to be careful to persons with epilepsy also having tendency to convulsive attacks in view of the fact that caffeine reduces protective action of antiepileptic medicines.

Use at pregnancy and feeding by a breast
Possesses teratogenic action: at use in the I trimester of pregnancy leads to emergence at a fruit of splitting of the upper sky, in the III trimester - causes braking of patrimonial activity (suppression of synthesis of prostaglandins), premature closing of an arterial channel in a fruit, a hyperplasia of pulmonary vessels and hypertensia in a small circle of blood circulation. Administration of drug in the II trimester is possible if the potential advantage for mother exceeds risk for a fruit.
Salicylates and their metabolites in small amounts get into breast milk, for the period of treatment it is necessary to stop breastfeeding.

Use at abnormal liver functions
With an otorozhnost at a liver failure.

Use at renal failures
It is contraindicated at a renal failure.

Use for children
It is contraindicated to children up to 6 years at a pain syndrome (for this dosage form); to children and teenagers aged up to 15 years (at use as febrifugal) with the acute respiratory diseases caused by viral infections in connection with risk of development of a syndrome to Reja (encephalopathy and acute fatty dystrophy of a liver with acute development of a liver failure).

Overdose:

The overdose symptoms caused by acetylsalicylic acid can arise after a single dose of a high dose or at prolonged use. If the single dose is less than 150 mg/kg, acute poisoning 150-300 mg/kg - moderate and at use in doses consider a lung, more than 300 mg/kg - heavy.

Symptoms: At slight poisoning - a salitsilizm syndrome (nausea, vomiting, a sonitus, a vision disorder, dizziness, a severe headache, a febricula, fever - a bad predictive sign at adults).

At considerable overdose - confusion of consciousness, drowsiness, spasms and a coma, a tremor, not cardiogenic fluid lungs, an asthma, suffocation, disturbances of water and electrolytic balance, a renal failure, a collapse and shock.

The greatest risk of development of chronic intoxication is noted at elderly people at reception within several days more than 100 mg/kg / At children and patients of advanced age initial signs of a salitsilizm are not always noticeable therefore it is reasonable to determine periodically the content of salicylates in blood: concentration higher than 70 mg of % testifies to a moderate or serious poisoning; higher than 100 mg % extremely heavy, predictively adverse. At poisoning of average and heavy degree hospitalization is necessary.

Treatment: Provocation of vomiting, purpose of absorbent carbon and laxatives, urine alkalization (it is shown at concentration of salicylates higher than 40 mg of %, it is provided in/in infusion of Natrii hydrocarbonas - 88 мэкв in 1 l of 5% of solution of a dextrose, with a speed of 10-15 ml/kg/h), recovery of volume of the circulating blood and induction of a diuresis (it is reached by administration of solution of Natrii hydrocarbonas in the same dose and cultivation, repeat 2-3 times); it must be kept in mind that intensive infusion of liquid elderly can lead to a fluid lungs. Use of acetazoleamide for urine alkalization is not recommended (can cause acidosis and strengthen toxic effect of salicylates). The hemodialysis is shown at concentration of salicylates more than 100-130 mg of %, and patients with chronic poisoning have 40 mg of % and below in the presence of indications (refractory acidosis, the progressing aggravation of symptoms, severe damage of the central nervous system, a fluid lungs and a renal failure). At a fluid lungs artificial ventilation of the lungs by the mix enriched with oxygen in the mode of positive pressure at the end of an exhalation is shown; apply a hyperventilation and an osmotic diuresis to treatment of wet brain.

Caffeine in doses more than 300 mg / (including against the background of abuse of coffee - more than 4 cups of natural coffee on 150 ml) can cause a condition of alarm, a tremor, a headache, confusion of consciousness, premature ventricular contraction.

Treatment: Provocation of vomiting, reception of absorbent carbon.

Storage conditions:

In original packaging at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

Tablets of 500 mg +50 mg: 10 pieces.