Pharmadol

General characteristics. Structure:

Active ingredients: 1 tablet contains acetylsalicylic acid 300 mg, paracetamol of 100 mg, caffeine of 50 mg;

excipients: citric acid, monohydrate; potato starch; lactoses monohydrate; povidone; sodium of a kroskarmeloz; cellulose microcrystallic; calcium stearate.

Pharmacological properties:

Фармадол® is the combined drug with antiinflammatory, febrifugal and analgetichesky effects. Effect of drug is defined by its components.

The antipyretic effect of acetylsalicylic acid is implemented through the central nervous system by oppression of synthesis of PGE2 prostaglandin in a hypothalamus in response to effect of endogenous pyrogens. Its analgetichesky efficiency has as peripheral (braking of synthesis of prostaglandins in the inflammation center, the prevention of a sensitization of pain receptors to mechanical and chemical irritants), and central (action on the centers of a hypothalamus, without oppressing at the same time consciousnesses by hypnotic effect or decrease in a mental threshold of pain) an origin.

Paracetamol slows down synthesis of prostaglandins in a brain thanks to what also the antipyretic effect is carried out its analgeticheskiya. It is weaker inhibitor of peripheral system of biosynthesis of prostaglandins which play an important role in development of reaction of an inflammation.

The mechanism of effect of caffeine is caused by oppression of activity of phosphodiesterase that leads to accumulation of tsAMF. An important link in the mechanism of effect of caffeine is its interaction with purine receptors of a brain. It strengthens analgetichesky effect of acetylsalicylic acid and paracetamol and accelerates its beginning.

The pharmacokinetics is not investigated.

Indications to use:

The weak or moderately expressed pain syndrome (headache, migraine, dentagra, neuralgia, arthralgia, primary dysmenorrhea); the diseases which are followed by a hyper thermal syndrome (as an antipyretic).

Route of administration and doses:

Adult Pharmadol® to appoint inside on 1-2 tablet 2-3 times a day after food, to wash down with a large amount of liquid. The highest daily dose makes 6 tablets in 3 receptions. It is not necessary to accept drug more than 5 days as anesthetic and more than 3 days – as an antipyretic.

Features of use:

Use during pregnancy or feeding by a breast.

Drug is contraindicated during pregnancy. During treatment it is necessary to stop feeding by a breast.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

At use of high doses of drug it is necessary to refrain from control of motor transport or work with other mechanisms owing to possible side reactions from a nervous system (dizziness, a hyperexcitability, orientation disturbance).

Children. Drug is contraindicated to children because of risk of development of a syndrome Reja at a hyperthermia against the background of viral diseases (a hyper pyrexia, a metabolic acidosis, disturbance from a nervous system and mentality, vomiting, an abnormal liver function).

Side effects:

At use of drug for certain patients side reactions which are characteristic of drugs of acetylsalicylic acid, paracetamol or caffeine can be observed.

From a digestive tract: dyspepsia, nausea, vomiting, heartburn, pain in epigastric area and abdominal pain; an inflammation and erosive cankers of a digestive tract which can cause gastrointestinal hemorrhages and perforation with the corresponding laboratory indicators and clinical manifestations; a tranzitorny liver failure with increase in level of transaminases of a liver; гепатонекроз (dozozavisimy effect), ulcers on a mucous membrane of an oral cavity.

From bodies of a hemopoiesis: a leukopenia, hemolitic anemia, an agranulocytosis, a sulfatgemoglobinemiya, a methemoglobinemia (cyanosis, short wind, a heartache), at prolonged use in high doses – aplastic anemia, a pancytopenia, a neutropenia, thrombocytopenia; hemorrhages that can lead to acute and chronic posthemorrhagic anemia / an iron deficiency anemia (owing to the so-called latent microbleeding) with the corresponding laboratory manifestations and clinical symptoms, such as an adynamy, pallor of an integument, hypoperfusion.

From immune system: hypersensitivity reactions, including rhinitis, a nose congestion, a Quincke's disease, an anaphylaxis, an acute anaphylaxis; not cardiogenic fluid lungs. At patients with bronchial asthma increase in frequency of emergence of a bronchospasm is possible.

From skin and hypodermic cellulose: itch, feeling of heat; an enanthesis and mucous membranes, including erythematic rashes, a small tortoiseshell; multiformny exudative erythema; Stephens-Johnson's syndrome; toxic epidermal necrolysis.

From the central and peripheral nervous system: headache, paresthesias, tremor, nervousness, concern; dizziness and a ring in ears, a vision disorder that can demonstrate overdose; sleeplessness, hyperexcitability, orientation disturbance, uneasiness, irritability, sensation of fear.

From urinogenital system: nephrotoxicity (renal colic, intersticial nephrite, papillary necrosis).

From cardiovascular system: short-term tachycardia, increase in arterial pressure, arrhythmia, heart consciousness, hemorrhages.

From endocrine system: a hypoglycemia up to a hypoglycemic coma.

Owing to antiagregantny action on thrombocytes acetylsalicylic acid can increase risk of development of bleedings (intraoperative hemorrhages, hematomas, bleedings from bodies of urinogenital system, nasal bleedings, odontorrhagias; heavy bleedings, such as hemorrhages of a digestive tract, brain hemorrhages (especially at patients with uncontrollable arterial hypertension and/or at simultaneous use of anti-hemostatics) which in isolated cases can potentially threaten life.

Interaction with other medicines:

Paracetamol: antidepressants and other stimulators of a microsomal oxidation – these drugs increase a producing the hydroxylated active metabolites influencing function of a liver, predetermining a possibility of development of heavy intoxications at small overdoses of drug. Speed of absorption of paracetamol can increase at simultaneous use with Metoclopramidum and domperidony and decrease at use with holestiraminy. Paracetamol reduces efficiency of diuretics. Derivatives of coumarin (warfarin) at prolonged use of paracetamol increase risk of development of bleedings.

Caffeine: Cimetidinum, hormonal contraceptives, an isoniazid strengthen effect of caffeine. Caffeine reduces effect of opioid analgetik, anxiolytics, hypnotic drugs and sedatives, is an antagonist of anesthetics and other drugs, the oppressing TsNS, the competitive antagonist of drugs, the oppressing TsNS, the competitive antagonist of drugs of adenosine, ATP. At simultaneous use of caffeine with ergotamine absorption of ergotamine from a digestive tract improves, with thyritropic means – the thyroid effect increases. Caffeine reduces concentration of lithium in blood. Simultaneous use of caffeine with MAO inhibitors can cause dangerous increase in arterial pressure therefore such combination is contraindicated. Caffeine increases effect (improves bioavailability) analgetikov-antipyretics, exponentiates effects of derivatives of xanthine, a-and b-adrenomimetikov, psychogogic means.

Acetylsalicylic acid: the combination with a methotrexate in a dosage      of 5 mg a week or more is contraindicated. Simultaneous use with uricosuric means, such as бензобромарон, пробенецид, reduces effect of removal of uric acid (thanks to the competition of removal of uric acid renal tubules). At simultaneous use with digoxin concentration of the last in a blood plasma increases owing to decrease in renal excretion. APF inhibitors in a combination with high doses of acetylsalicylic acid cause decrease in filtering in balls owing to inhibition of vazodilatatorny prostaglandins and decrease in hypotensive effect. Selective serotonin reuptake inhibitors: the risk of bleedings from upper parts of a digestive tract because of a possibility of synergy effect increases. At simultaneous use with valproic acid acetylsalicylic acid forces out it from communication with blood plasma proteins, increasing toxicity.

Drug strengthens action of the means reducing fibrillation and aggregation of thrombocytes, side effect of corticosteroids, sulphonylurea, a methotrexate. The methotrexate – at the combined use with salicylates in a dose of 15 mg/week and raises hematologic toxicity of a methotrexate in a consequence of decrease in renal clearance of a methotrexate by antiinflammatory agents and its replacement more from communication with plasma proteins therefore such combination is contraindicated.

It is necessary to avoid combinations with barbiturates, anticonvulsants, salicylates, rifampicin, alcohol.

Contraindications:

Hypersensitivity to components of drug or salicylates, to other derivatives of xanthines (theophylline, theobromine); the bronchial asthma caused by use of salicylates or other non-steroidal anti-inflammatory drugs (NPVS) in the anamnesis. Inborn hyperbilirubinemia; inborn insufficiency glyukozo-6-fosfatdegidrogenazy; blood diseases, including a leukopenia, anemia, hemophilia. Conditions of a hyperexcitability, epilepsy, sleep disorders. Acute gastrointestinal ulcers, gastrointestinal bleedings. A serious cardiovascular illness, including disturbances of a rhythm, the expressed atherosclerosis, a severe form of coronary heart disease, the expressed heart failure, the expressed arterial hypertension. The expressed renal failure, the expressed liver failure. Advanced age, glaucoma, alcoholism, hemorrhagic diathesis, acute pancreatitis, heavy diabetes mellitus, hyperthyroidism, prostatauxe. During use of monoamine oxidase inhibitors (MAO) and within 2 weeks after the termination of their use. The combination with a methotrexate in a dosage of 15 mg/week or is more (see the section "Interaction with Other Medicines and Other Types of Interactions"); a combination with tricyclic antidepressants or β-blockers..........

Appropriate security measures at use

 

Before use of drug it is necessary to consult with the doctor. If symptoms do not disappear, it is necessary to see a doctor.

At surgeries (including dental) use of the drugs containing acetylsalicylic acid can increase probability of emergence/strengthening of bleeding that it is caused by oppression of aggregation of thrombocytes throughout some time after use of acetylsalicylic acid.

At patients with allergic complications, including with bronchial asthma, allergic rhinitis, a small tortoiseshell, a skin itch, a rhinedema and a pollinosis, and also at their combination to persistent infections of respiratory tracts and at patients with hypersensitivity to non-steroidal anti-inflammatory drugs (NPVS) during treatment with drug development of a bronchospasm or attack of bronchial asthma is possible.

Diseases of a liver increase risk of damage of a liver paracetamol.

Danger of overdose is higher at patients with netsirrozny alcoholic diseases of a liver. During treatment drug does not recommend to take excessive amount of the drinks containing caffeine (for example coffee, tea).

Not to use drug with other means containing paracetamol, acetylsalicylic acid. Not to exceed the specified doses. To use drug with care at gastrointestinal ulcers in the anamnesis, including at a chronic or recurrent peptic ulcer or gastrointestinal bleedings in the anamnesis; simultaneous use of anticoagulants; at disturbances of functions of kidneys and/or a liver.

In 5-7 days prior to surgical intervention it is necessary to cancel drug use (for decrease in risk of the raised bleeding).

With care to apply at the raised bleeding or at simultaneous performing antiinflammatory therapy. The acetylsalicylic acid which is a part of drug even in small doses reduces removal of uric acid from an organism that can become the reason of a bad attack of gout at sensitive patients. At a renal failure and a liver the interval between receptions has to be not less than 8 hours. During treatment by drug it is necessary to refuse alcohol intake. At prolonged use control of system of a blood coagulation and level of hemoglobin is necessary.

Can change results of analyses of a drug test at athletes.

Complicates diagnosis at an acute abdominal pain syndrome.

Overdose:

Overdose symptoms acetylsalicylic acid: it is possible because of the chronic intoxication which arose owing to long therapy (use        over 100 mg/kg a day more than 2 days can become the reason of toxic effects), and also because of acute intoxication which threatens life (overdose) and which reasons can be, for example, an accidental use 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, meets, as a rule, only after repeated receptions of high doses.

Symptoms of chronic poisoning: balance disturbance, dizziness, a ring in ears, deafness, the strengthened potovydeleniye, nausea, vomiting, a headache, confusion of consciousness. The specified symptoms can be controlled a dose decline. The ring in ears can be noted at concentration of salicylates in a blood plasma over 150-300 mkg/ml. Heavy side reactions meet at concentration of salicylates in a blood plasma       over 300 mkg/ml.

The expressed change of acid-base balance which can differ depending on age and weight of intoxication testifies to acute intoxication. Weight of a state cannot be estimated only on the basis of concentration of salicylates in a blood plasma. Absorption of acetylsalicylic acid can be slowed down in connection with a delay of gastric emptying, formation of concrements in a stomach.

Treatment: intoxication caused by overdose by acetylsalicylic acid is defined by severity, clinical symptoms and is provided with standard methods which apply at poisoning. All taken measures have to be directed to bystry removal of drug and recovery of electrolytic and acid-base balance. To apply absorbent carbon, the forced alkaline diuresis. Depending on a condition of acid-base equilibrium and electrolytic balance to carry out infusional administration of solutions of electrolytes. At a serious poisoning the hemodialysis is shown. At prolonged use of high doses are possible aplastic

anemia, thrombocytopenia, pancytopenia, agranulocytosis, neutropenia, leukopenia. At reception of high doses emergence of disturbances from the central nervous system (dizziness, psychomotor initiation, disturbance of orientation and attention, sleeplessness, a tremor, nervousness, concern) is possible, from an urinary system – nephrotoxicity (renal colic, intersticial nephrite, a papillary necrosis). In case of overdose the raised potovydeleniye, psychomotor excitement or oppression TsNS, drowsiness, consciousness disturbance, disturbance of a cordial rhythm, tachycardia, premature ventricular contraction, a tremor, a hyperreflexia, spasms can be observed.

Overdose symptoms paracetamol: damage of a liver is possible at adults who accepted 10 g and more paracetamol, and at children who accepted drug in a dose over 150 mg/kg of body weight. In the first 24 hours: pallor, nausea, vomiting, anorexia, abdominal pain, гепатонекроз, increase in activity of hepatic transaminases, increase in a prothrombin ratio. Damage of a liver can be shown in 12-48 hours after reception of overdoses of drug. There can be a disturbance of metabolism of glucose and a metabolic acidosis. At a serious poisoning the liver failure can progress in encephalopathy, a coma and to lead to a lethal outcome. The acute renal failure with an acute necrosis of tubules can develop even in the absence of severe damage of kidneys. Also cardiac arrhythmia was noted.

Treatment: at overdose quick medical care is necessary even if symptoms of overdose are absent. Purpose of methionine orally or Acetylcysteinum can intravenously give positive effect within 48 hours after overdose. It is necessary to apply also all-supporting measures.

Overdose symptoms caffeine: high doses of caffeine can become the reason of the accelerated breath, premature ventricular contraction, dizziness, the heat of passion, epigastric pain, vomiting, the raised diuresis, tachycardia or cardiac arrhythmia, stimulation of the central nervous system (sleeplessness, concern, excitement, alarm, a syndrome of the increased neuroreflex irritability, a headache, a tremor, spasms, nervousness and irritability). Clinically important symptoms of overdose are connected by caffeine also with damage of a liver paracetamol.

Treatment: the supporting measures, such as use of antagonists of β-adrenoceptors, can facilitate cardiotoxic effects. The specific antidote is absent.

Storage conditions:

Period of validity 2 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister. On 1 or 3, or 5 blisters in a pack.