Composition
Active ingredients:
paracetamol-0.500 g,
caffeine-0.065 g
. excipients:
potato starch,
microcrystalline cellulose,
croscarmellose sodium,
hyprolose (oxypropyl cellulose),
colloidal silicon dioxide,
magnesium stearate,
copovidone,
talc,
titanium dioxide,
silicone emulsion (50% solution)
Pharmacological action
Migrenium is a combined drug, the action of which is determined by the components that make up its composition.
Caffeine has a psychostimulating (stimulates the psychomotor centers of the brain), analeptic effect, enhances the effect of analgesics, eliminates drowsiness and fatigue, increases physical and mental performance. Affects the cardiovascular system: increases the frequency and strength of heart contractions( HR), increases blood pressure (BP) in hypotension (does not change the normal). Expands the bronchi, biliary tract, blood vessels of skeletal muscles, heart, kidneys, narrows the vessels of the abdominal cavity. Reduces platelet aggregation. It stimulates the secretion of gastric glands, increases basal metabolism, and has a moderate diuretic effect.
Paracetamol – antipyretic and analgesic effect (due to inhibition of cyclooxygenase (COX) and inhibition of prostaglandin synthesis (Pg) affects the center of thermoregulation in the hypothalamus and the conduct of pain impulses in the central nervous system (CNS). The drug blocks cyclooxygenase I and II mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains the almost complete absence of its anti-inflammatory effect.
The drug does not have a negative effect on water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract (GIT) due to the lack of influence on the synthesis of prostaglandins in peripheral tissues. The possibility of methemoglobin formation is unlikely.
Pharmacokinetics
Caffeine and its water-soluble salts are well absorbed in the intestines (including the colon). The half – life of the drug (T 1/2) is about 5 hours, in some individuals-up to 10 hours. The main part is demethylated and oxidized. About 10% is excreted unchanged by the kidneys.
Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. The plasma concentration reaches a peak after 30-60 minutes. T 1/2 of plasma-1-4 hours is metabolized in the liver. It is excreted in the urine, mainly in the form of esters with glucuronic and sulfuric acids; less than 5% is excreted unchanged
Indications
Pain syndrome (mild to moderate severity): headache, migraine, ossalgia, myalgia, neuralgia, arthralgia, algodismenorrhea, toothache; febrile syndrome, “cold” diseases, acute respiratory viral infections (including flu)
Contraindications
Hypersensitivity, severe hepatic and / or renal insufficiency, epilepsy, glucose-6-phosphate dehydrogenase deficiency, senile age, children (up to 12 years)
Side effects
Allergic reactions (skin rash, angioedema, urticaria), dyspeptic disorders (including nausea, epigastric pain).
In rare cases-hemolytic anemia, thrombocytopenia, methemoglobinemia.
With prolonged use in large doses – hepatotoxicity, pancytopenia, nephrotoxicity (renal colic, pyuria, interstitial nephritis, papillary necrosis)
Interaction
Increases the effect of monoamine oxidase (MAO) inhibitors. Reduces the effectiveness of uricosuric drugs.
Caffeine accelerates the absorption of ergotamine.
Under the influence of paracetamol, the elimination time of chloramphenicol increases by 5 times. With prolonged use, paracetamol may increase the effect of anticoagulants (dicoumarin derivatives).
Concomitant use of paracetamol and ethanol increases the risk of hepatotoxic effects and acute pancreatitis.
Barbiturates, phenytoin, ethanol, rifampicin, phenylbutazone, tricyclic antidepressants, etc. stimulators of microsomal oxidation increase the production of hydroxylated active metabolites, causing the possibility of severe intoxication with small overdoses.
Microsomal oxidation inhibitors (cimetidine) reduce the risk of hepatotoxic effects. Metoclopramide and domperidone increase, and colestyramine reduces absorption.
How to take, course of use and dosage
Inside, adults and children after 12 years – 2 tablets 4 times a day with an interval of at least 4 hours. The maximum daily dose is 8 tablets.
Duration of application-no more than 3 days (as an antipyretic) and no more than 5 days (as an analgesic).
Overdose
Symptoms: pallor of the skin, decreased appetite, nausea, vomiting, sometimes with blood; hepatonecrosis (the severity of necrosis due to intoxication directly depends on the degree of overdose), gastralgia, agitation, anxiety, agitation, motor restlessness, confusion, delirium, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, increased tactile or pain sensitivity, tremor or muscle twitching; tinnitus, epileptic seizures (with acute overdose – tonic-clonic), increased activity of “hepatic” transaminases, increased prothrombin time; a detailed clinical picture of liver damage is manifested in 1-6 days.
Treatment: use of SH-group donors and glutathione – methionine synthesis precursors 8-9 hours after overdose and N-acetylcysteine – after 12 hours. To prevent late hepatotoxic effects, gastric lavage is performed.
Special instructions
Excessive consumption of caffeinated products (coffee, tea) during treatment may cause symptoms of overdose.
With prolonged (more than 1 week) treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver.
Without consulting a doctor, take no more than 3 days for the treatment of febrile syndrome and no more than 5 days for pain syndrome.
It can change the results of athletes ‘ doping control tests. It makes it difficult to establish a diagnosis in acute “acute abdomen”. Patients with atopic bronchial asthma and hay fever have an increased risk of developing allergic reactions. During treatment, you should stop using ethanol (increased risk of hepatotoxicity)
Storage conditions
Store in a dry place protected from light at a temperature not exceeding 25 °C. Keep out of reach of children.
Shelf
life is 3 years.
Active ingredient
Caffeine, Paracetamol
Dosage form
Tablets
Description
For pregnant women as prescribed by a doctor, For children over 12 years of age, For adults, For nursing mothers as prescribed by a doctor
Indications
Sciatica, Lumbago, Cold, Myositis, Flu, Neuritis, Osteochondrosis, Sciatica, Migraine
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