Alka-Prim

General characteristics. Structure:

Active agents: acetylsalicylic acid of 330 mg; glycine of 100 mg

Excipients: citric acid, Natrii hydrocarbonas.

Pharmacological properties:

Acetylsalicylic acid concerns to the NPVP group. Is ether of salicylic acid with analgeziruyushchy, antiinflammatory and febrifugal properties.
The mechanism of effect of acetylsalicylic acid is based on oppression of synthesis of prostaglandins — E2 (PGE2) prostaglandin, A2 (PGA2) prostaglandin and A2 thromboxane due to braking of TsOG of arachidonic acid (braking of activity of TsOG-1 and/or TsOG-2). These connections induce inflammatory process by influence on leukotrienes, increase permeability of walls of vessels and sensitivity of pain receptors to action of neurotransmitters (serotonin, bradikinin, acetylcholine), increase hypostasis. In the subcrustal centers PGE2 is a strong pyrogenic factor, and oppression of its synthesis leads to decrease in body temperature. NPVP have also analgeziruyushchy effect at the mild nociceptive and neurogenic pain caused by inflammatory process (or other reasons) where pernicious impulses increase activity of TsOG, increasing synthesis of peroxides and prostaglandins. Many data demonstrate that also central mechanism of analgeziruyushchy action of NPVP is possible.
Acetylsalicylic acid suppresses also aggregation of thrombocytes. Irrevocable braking of TsOG is especially expressed in thrombocytes as they cannot synthesize this enzyme again. The aminoacetic acid reduces irritant action of acetylsalicylic acid by a mucous membrane of a stomach, and also dispeptic frustration.

Indications to use:

Pain syndrome of weak and average intensity (for example headache, muscle and joints pain); a feverish state at cold, viral infections and other states.

Route of administration and doses:

Drug is accepted during food. Before reception the tablet should be dissolved in ¾ a glass of water.
Such dosage is usually recommended: adult — 1–2 tablets 2–4 times a day. The daily dose should not exceed 3 g of drug. Children aged from 16 years — 2–3 tablets a day.
Symptomatic treatment without consultation of the doctor it is possible to spend no more than 3 days. It is necessary to apply a minimal effective dose.

Features of use:

It is not necessary to appoint drug: to the patients accepting peroral gipoglikemiziruyushchy drugs from group of sulphonylurea, considering risk of strengthening of gipoglikemiziruyushchy action; the patient accepting antigouty medicines; to patients with pathology of vessels of a kidney, a hypovolemia, sepsis.
At patients with a juvenile pseudorheumatism and/or a system lupus erythematosus, and also with an abnormal liver function and kidneys drug should be used with care. As toxicity of salicylates increases, at these patients it is necessary to control function of a liver and kidneys.
Use of medicine in a minimal effective dose during the shortest span necessary for achievement of effect and reduction of manifestation of symptoms, promotes decrease in risk of emergence of side reactions.
Reception of acetylsalicylic acid should be cancelled in 5–7 days prior to the planned surgical intervention, considering risk of increase in a bleeding time both during operation, and after it.
It is necessary to be careful at use of drug with a methotrexate in doses of less than 15 mg/week, considering strengthening of toxic action of a methotrexate on marrow. Simultaneous use with a methotrexate in the doses exceeding 15 mg/week, contraindicated.
It is necessary to use with care drug at: uterine bleedings, plentiful menstrual bleedings, use of intrauterine contraceptives, AG, and also heart failure.
During treatment by acetylsalicylic acid it is not necessary to take alcohol, considering the increased risk of injury of a mucous membrane of a GIT.
At patients of advanced age drug should be used in the minimum doses and through big intervals of time, considering the increased risk of development of side effects in this group of patients.
There are proofs that the medicines suppressing TsOG can cause disturbance of fertility in women by impact on an ovulation. This effect has passing character and disappears after the end of treatment.
Patients with tendency to arterial hypotension need to control the ABP level and, in case of need, to carry out drug dose adjustment: acetylsalicylic acid is appointed in the minimum doses and on condition of regular control of the ABP. At decrease in the ABP below usual level reception of medicine is stopped, the ibuprofen can reduce the inhibiting effect of acetylsalicylic acid concerning aggregation of thrombocytes. In case of use of drug before reception of an ibuprofen as anesthetic the patient has to consult with the doctor.
Acetylsalicylic acid can cause development of a bronchospasm or attack OH, or other hypersensitivity reactions. Risk factors include OH in the anamnesis, hay fever, polyposes of a mucous membrane of a nose or a chronic respiratory disease, allergic reactions (skin reactions, an itch, urticaria) on other substances in the anamnesis. Because of the inhibiting effect of acetylsalicylic acid concerning aggregation of thrombocytes which remains for several days after reception use of the drugs containing acetylsalicylic acid can increase risk of strengthening of bleeding at surgical interventions (including insignificant surgical interventions, for example an odontectomy). It is not necessary to use without consultation with the doctor the drugs containing acetylsalicylic acid at children and teenagers with an acute respiratory viral infection which is followed or is not followed by fervescence. At some viral diseases, especially at flu A, B and chicken pox, there is a risk of development of a syndrome of Ray which is very rare, but life-threatening disease that demands urgent medical intervention. The risk can be raised if acetylsalicylic acid is applied as the accompanying medicine, however relationship of cause and effect in this case is not proved. If the specified states are followed by constant vomiting, it can be manifestation of a syndrome of Ray.
Period of pregnancy and feeding by a breast
Pregnancy. Suppression of synthesis of prostaglandins can adversely affect the course of pregnancy and affect fetation. Data of epidemiological researches indicate the increased risk of an abortion and emergence of the inborn heart diseases, the alimentary system connected using inhibitors of synthesis of prostaglandins during the early period of pregnancy.
Absolute increase in risk of development of defects of cardiovascular system in these researches made from <1 to nearly 1,5%. Possibly, the risk of emergence of above-mentioned shortcomings increases with increase in a dose of drug, and also increase in the period of treatment.
At newborns whose mothers accepted acetylsalicylic acid before childbirth, bleedings, such as were noted: subconjunctival hemorrhage, hamaturia, petechia, cephalohematoma.
In other researches frequent cases of intracraneal hemorrhages at premature children whose mothers accepted acetylsalicylic acid one week prior to childbirth were noted.
At animals the lethal dose for a fruit was higher, than the doses applied in clinical practice. At animals to whom entered inhibitors of synthesis of prostaglandins in the period of an organogenesis, increase in frequency of inborn defects, including defects of cardiovascular system was noted.
Acetylsalicylic acid easily gets through a placental barrier. Within the first 6 months of pregnancy drug can be used only in urgent cases. In need of use of acetylsalicylic acid for women who became pregnant or in the I-II trimester of pregnancy it is necessary to accept the smallest effective dose during the shortest period.
In the last trimester of pregnancy all drugs from group of inhibitors of synthesis of prostaglandins can exert a negative impact on a fruit:

• on the blood circulatory system (pulmonary hypertensia with premature closing of an aortal channel);
• on kidneys (development of the renal failure in a fruit connected with an oligoamnios is possible).
All drugs from group of inhibitors of synthesis of prostaglandins which are applied in the III trimester of pregnancy can:

• to prolong a bleeding time both at mother, and at newborns and to have anti-aggregation effect even at reception of very low doses;
• to suppress sokratitelny ability of a uterus — such influence was connected with the increased deviation of frequency and a delay of childbirth at animals.
In this regard acetylsalicylic acid is contraindicated in the last trimester of pregnancy.
Feeding period breast. Use of drug during feeding by a breast contraindicated.
Children. Drug is used at children aged from 16 years.
Influence on ability to manage vehicles and to work with mechanisms. Does not influence.

Side effects:

Pain in epigastric area and a stomach, an itch, decrease in concentration of attention, a headache, tension, irritability, OPN, a GIT inflammation, erosive cankers of a GIT, bleeding, including perioperatsionny hemorrhages, hematomas, bleedings from bodies of urinogenital system, nasal bleedings, odontorrhagias; heavy bleedings, such as GIT hemorrhages, cerebral hemorrhages (especially at patients from uncontrollable AG and/or at simultaneous use of anti-hemostatics) which can potentially threaten life. The cover, hypoperfusion can lead hemorrhages to an acute and chronic posthemorrhagic/iron deficiency anemia (owing to the so-called latent microbleeding) with the corresponding laboratory indicators and clinical symptoms, such as an adynamy, pallor skin. At patients with severe forms of insufficiency glyukozo-6-fosfatdegidrogenazy hemolysis or hemolitic anemia were noted.
Hypersensitivity reactions with the corresponding laboratory and clinical manifestations from a respiratory path, a GIT and cardiovascular system, heart and respiratory failure.

Interaction with other medicines:

Use of a methotrexate in doses of 15 mg/week and raises hematologic toxicity of a methotrexate above (decrease in renal clearance of a methotrexate by antiinflammatory agents and replacement by methotrexate salicylates from communication with proteins of a blood plasma).
Combinations which should be applied with care
APF inhibitors: acetylsalicylic acid can reduce anti-hypertensive effect of APF inhibitors.
Acetazoleamide: acetylsalicylic acid can increase considerably concentration and by that toxicity of acetazoleamide.
Antiepileptic drugs: acetylsalicylic acid increases toxicity of valproic acid and, in turn, strengthens anti-aggregation effect of acetylsalicylic acid.
Diuretics: acetylsalicylic acid can reduce efficiency of these drugs and increase ototoxicity of furosemide.
Methotrexate: acetylsalicylic acid strengthens toxic action of a methotrexate on marrow. Simultaneous use of acetylsalicylic acid with a methotrexate in doses of 15 mg/week or above is contraindicated.
NPVP: simultaneous use of acetylsalicylic acid and NPVP is not recommended as the risk of development of side effects from a GIT increases.
System use of GKS: except for the hydrocortisone applied as replacement therapy at Addison's disease, their reception in combination with acetylsalicylic acid increases risk of development of stomach ulcer and a duodenum, gastrointestinal bleeding, and also reduces concentration of salicylates in a blood plasma during treatment, and after completion of use increases risk of overdose by salicylates.
Gipoglikemiziruyushchy drugs: acetylsalicylic acid strengthens effect of gipoglikemiziruyushchy drugs. Medicine should not be applied along with sulphonylurea derivatives.
The drugs increasing removal of uric acid (пробенецид, Sulfinpyrazonum): salicylates reduce effect of drugs, increase removal of uric acid. Medicine should not be applied along with antigouty drugs.
Digoxin: acetylsalicylic acid can strengthen effect of digoxin.
Thrombolytic drugs: acetylsalicylic acid can strengthen thrombolytic effect of such medicines as Streptokinasa and an alteplaza.
Ibuprofen: simultaneous use interferes with irreversible oppression of thrombocytes acetylsalicylic acid. Treatment by an ibuprofen of patients with risk of development of cardiovascular diseases can limit cardiotyre-tread effect of acetylsalicylic acid.
Anticoagulants: at simultaneous use the risk of development of bleeding increases.
Uricosuric means: simultaneous use of a benzobromaron, probenetsid reduces effect of removal of uric acid (thanks to the competition of removal of uric acid renal tubules).
Antidiabetic drugs: at simultaneous use of high doses of acetylsalicylic acid with antidiabetic drugs from group of derivatives of sulphonylurea or insulin the effect of the last due to gipoglikemiziruyushchy effect of acetylsalicylic acid and replacement of the sulphonylurea connected with proteins of a blood plasma amplifies.
GKS: simultaneous use increases risk of development of gastrointestinal bleeding. Reduce the level of salicylates in blood and increase risk of overdose after the end of treatment.
Selective serotonin reuptake inhibitors: increase risk of bleeding from upper parts of a GIT because of a possibility of synergy effect.
At simultaneous use with valproic acid acetylsalicylic acid forces out it from communication with proteins of a blood plasma, increasing toxicity of the last.
Ethanol: increases the frequency and intensity of the bleedings from a GIT caused by acetylsalicylic acid. During treatment it is not necessary to take alcohol.
Omeprazol and ascorbic acid do not influence absorption of acetylsalicylic acid.
The aminoacetic acid reduces toxicity of anticonvulsant, antipsychotic means (neuroleptics), anxiolytics, antidepressants. At the combined use with hypnotic drugs, tranquilizers and antipsychotic means the effect of braking of TsNS amplifies.

Contraindications:

Drug should not be used at the following states:

• hypersensitivity to active ingredient or any excipient; hypersensitivity to acetylsalicylic acid is noted in 0,3% of population, including at 20% of patients OH or a chronic small tortoiseshell. Hypersensitivity symptoms: a small tortoiseshell and even shock, can arise during 3 h after reception of acetylsalicylic acid;
• hypersensitivity to other NPVP; symptoms — a small tortoiseshell, a bronchospasm, rhinitis, shock, a Quincke's disease;
• hemorrhagic diathesis, arterial hypotension;
• OH, chronic diseases of respiratory system, hay fever or rhinedema;
• an exacerbation of stomach ulcer and/or a duodenum, and also inflammatory processes or bleedings from a GIT (development of gastrointestinal bleeding or a recurrence of stomach ulcer and/or a duodenum is possible);
• heavy liver or renal failure;
• heavy heart failure;
• disturbance of coagulability of blood (for example hemophilia, thrombocytopenia), and also the patients accepting anticoagulants (for example coumarin derivatives, heparin);
• inborn deficit glyukozo-6-fosfatdegidrogenazy;
• simultaneous use with a methotrexate in doses of 15 mg/week or above, in view of a negative impact on function of marrow;
• age up to 16 years, especially at acute viral infections, considering risk of development of a syndrome of Ray;
• III trimester of pregnancy and period of feeding by a breast.

Overdose:

After overdose by acetylsalicylic acid such symptoms can appear: nausea, vomiting, hurried breathing, sonitus.
Also the hearing loss, a vision disorder, a headache, motive excitement, drowsiness and a coma, spasms, a hyperthermia were noted. At heavy intoxication there come disturbances of acid-base equilibrium and water and electrolytic balance (a metabolic acidosis and dehydration). Easy or moderately severe symptoms of toxicity develop at use of acetylsalicylic acid in a dose of 150-300 mg/kg of body weight. Heavy symptoms of poisoning arise after reception of 300-500 mg/kg of body weight. The potential lethal dose of acetylsalicylic acid makes more than 500 mg/kg of body weight. Death as a result of poisoning with acetylsalicylic acid is noted after reception by the adult of a single dose 10–30 g.
The overdose of salicylates is possible because of the chronic intoxication which arose owing to long therapy (use> of 100 mg/kg/days more than 2 days can cause toxic effect), and also because of acute intoxication which poses threat for life (overdose) and which reasons can be, for example, an accidental reception by children or unexpected overdose.
Chronic poisoning with salicylates can have the hidden character as its signs are not specific. The moderate chronic intoxication caused by salicylates, or a salitsilizm are noted, as a rule, only after repeated receptions of high doses.
Symptoms. Balance disturbance, dizziness, a ring in ears, deafness, the strengthened sweating, nausea and vomiting, a headache, confusion of consciousness. The ring in ears can be noted at concentration of salicylates in a blood plasma more than 150-300 mkg/ml. Serious side reactions arise at concentration of salicylates in a blood plasma> 300 mkg/ml.
The expressed change of acid-base balance which can differ depending on age of the patient and weight of intoxication testifies to acute intoxication. The most general indicator for children is the metabolic acidosis. Weight of a state cannot be estimated only on the basis of concentration of salicylates in a blood plasma.
Treatment. The patient needs to be hospitalized. The specific antidote is absent.
Urgent measures: it is artificial to cause vomiting or to carry out a gastric lavage (for the purpose of absorption reduction). Such actions are effective during 3–4 h after reception of acetylsalicylic acid, and in case of reception of a high dose — even to 10 h.
To enter absorbent carbon in the form of water suspension (50–100 g — the adult, 30–60 g — to children).
Decrease in body temperature (at a hyperthermia) by maintenance of low temperature of external environment and use of cold compresses.
Constant control of water and electrolytic balance and elimination of its disturbances.
For acceleration of elimination of acetylsalicylic acid kidneys and at treatment of acidosis it is necessary to enter into hydrosodium carbonate.
Patients with normal function of kidneys can carry out an alkaline diuresis before achievement of values рН between 7,5–8. At a serious poisoning it is possible to apply a hemodialysis or peritoneal dialysis. By dialysis it is possible to bring effectively acetylsalicylic acid out of an organism and quicker to recover acid-base equilibrium and water and electrolytic balance.
At increase in a prothrombin time it is necessary to enter vitamin K.
It is not necessary to use at the same time drugs which have the oppressing effect on TsNS, for example barbiturates, in connection with risk of oppression of a respiratory center.
Patients with disturbances of respiratory function should appoint oxygenation. If it is necessary, to carry out an intubation and IVL.
In case of symptoms of shock to appoint standard antishock treatment.
Symptomatic treatment.

Storage conditions:

In the dry place at a temperature not above 25 °C.

Issue conditions:

Without recipe

Packaging:

Tab. thorn. strip, No. 2, No. 10.