InterChem #Colds_and_flu #Fever #HEALTH_CARE
Pharmacological properties
Pharmacodynamics. Antipyretic, analgesic, antihistamine, vasoconstrictor combined agent, the action of which is due to the properties of the components that make up its composition.
Paracetamol has antipyretic, analgesic and anti-inflammatory effects. Paracetamol predominantly inhibits the synthesis of prostaglandins in the central nervous system and, to a lesser extent, affects the peripheral nervous system, blocking the conduction of pain impulses.
It is well absorbed, penetrates the placental barrier, enters breast milk in small amounts, is metabolized in the liver, excreted by the kidneys, T½ - 1–4 hours. The duration of action is 3-4 hours.
Pheniramine is an antihistamine, a blocker of histamine H1 receptors on effector cells, reduces vascular permeability, prevents the development of tissue edema, reduces the severity of local exudative processes, eliminates lacrimation, itching in the eyes and nose.
It is well absorbed, metabolized in the liver, excreted mainly by the kidneys, T1 / 2 - 16-18 hours.
Phenylephrine is a sympathomimetic that mainly stimulates α-adrenergic receptors, has a vasoconstrictor effect, reduces swelling of the nasal mucosa and paranasal sinuses.
Guaifenesin is an expectorant. It acts by increasing the volume and decreasing the viscosity of the secretion in the trachea and bronchi, which facilitates the secretion of sputum when coughing.
Pharmacokinetics. Paracetamol is rapidly and almost completely absorbed in the gastrointestinal tract. With oral administration, Cmax in blood plasma is reached 10-60 minutes after administration. 95% of paracetamol is metabolized in the liver by sulfo- and glucuroconjugation, as well as oxidation by the cytochrome P450 system. It is excreted by the kidneys, mainly in the form of metabolites, 3% of paracetamol is excreted unchanged. T½ is 1–4 hours. Paracetamol crosses the placental barrier, a small part of it passes into breast milk.
Guaifenesin is rapidly absorbed in the gastrointestinal tract. With oral administration, Cmax in blood plasma is achieved 15 minutes after administration. Guaifenesin is metabolized in the kidneys by oxidation to β- (2-methoxyphenoxide) lactic acid, an inactive metabolite that is excreted in the urine. T½ is 1 hour.
Phenylephrine hydrochloride is absorbed unevenly in the gastrointestinal tract and undergoes presystemic metabolism with the help of MAO in the intestine and liver. Thus, orally administered phenylephrine has reduced bioavailability. Cmax in blood plasma is achieved within 1-2 hours. T½ is 2-3 hours. It is excreted in the urine almost completely in the form of a sulfate conjugate.
Ascorbic acid compensates for the increased need for vitamin C in respiratory infections, enhances the body's nonspecific resistance. It is rapidly absorbed, metabolized in the liver, excreted by the kidneys.
Indications
Symptomatic treatment of acute respiratory infections and influenza: fever, headache, nasal congestion, runny nose, pain and muscle aches.
For preparations Amicitron plus and Amicitron plus without sugar also: productive cough with difficult sputum production.
Application
The preparation is prescribed for adults and children over the age of 14. are taken orally in the form of a solution. the contents of the sachet are dissolved in a glass of hot water (not boiling water). can be taken every 3-4 hours, but not more than 3 sachets per day. the maximum period of use without consulting a doctor is 3 days, further admission - on the recommendation of a doctor
Amicitron plus and Amicitron plus without sugar: apply orally in the form of a solution. Dissolve the contents of 1 sachet in 250 ml of hot water, but not boiling water. Use the prepared solution warm. Elderly adults, children over 12 years of age: 1 sachet every 4-6 hours if necessary. The maximum daily dose is 4 sachets. The maximum period of application without consulting a doctor is 3 days. If the symptoms of the disease persist, it is necessary to see a doctor. For children under 12 years of age, preparations are contraindicated.
Amicitron Extratab: adults and children over 12 years of age: 1 tablet every 4 hours. Drink with water. The maximum daily dose - 6 tablets - should not be exceeded. The maximum period of application without consulting a doctor is 3 days. Further use is possible only under medical supervision.
Contraindications
Hypersensitivity to the components of the preparation; pyloroduodenal obstruction; acute pancreatitis; severe impairment of liver and / or kidney function; congenital hyperbilirubinemia (including Zhilber's syndrome); deficiency of glucose-6-phosphate dehydrogenase; diabetes; hyperthyroidism; hypertrophy of the prostate with urinary retention; obstruction of the bladder neck; severe forms of arrhythmias, arrhythmias, atherosclerosis, coronary heart disease, blood diseases (including leukopenia, severe anemia); thrombosis; thrombophlebitis; ba; glaucoma; epilepsy; alcoholism, states of increased excitement; concomitant treatment with MAO inhibitors and a period of 2 weeks after discontinuation of their use.
Amicitron plus and Amicitron plus without sugar also: pheochromocytoma, phenylketonuria; rare hereditary problems associated with fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency. During pregnancy and breastfeeding. Age up to 12 years.
Do not use simultaneously with tricyclic antidepressants, paracetamol-containing preparations, β-adrenergic receptor blockers, sympathomimetics.
Side effects
On the part of the skin and subcutaneous tissue: dermatitis.
From the immune system: anaphylaxis, hypersensitivity reactions, including itching, rash on the skin and mucous membranes (usually generalized, erythematous rash, urticaria), angioedema, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (toxic epidermal necrolysis syndrome) Lyell).
From the nervous system: headache, dizziness, tremor, psychomotor agitation and disorientation, anxiety, nervous irritability, fear, irritability, sleep disturbance, insomnia, drowsiness, confusion, hallucinations, depressions, paresthesias, tinnitus, in in some cases - coma, convulsions, dyskinesia, changes in behavior.
From the side of the organ of vision: visual impairment and accommodation, mydriasis, increased intraocular pressure, dry eyes.
From the respiratory system: bronchospasm in patients sensitive to acetylsalicylic acid and other NSAIDs.
From the digestive tract: nausea, vomiting, heartburn, dry mouth, discomfort and pain in the epigastric region, constipation, diarrhea, flatulence, aphthae, hypersalivation, hemorrhages.
From the hepatobiliary system: impaired liver function, increased activity of hepatic enzymes, usually without the development of jaundice, hepatonecrosis (when using high doses).
From the endocrine system: hypoglycemia, up to hypoglycemic coma.
From the urinary system: nephrotoxicity, interstitial nephritis, papillary necrosis, dysuria, urinary retention and difficulty urinating, aseptic pyuria.
From the side of the cardiovascular system: hypertension, arrhythmias (tachycardia, bradycardia, etc.), shortness of breath, pain in the heart.
From the blood and lymphatic system: anemia (including hemolytic anemia), sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, pain in the heart), thrombocytopenia, agranulocytosis, bleeding, bruising.
Others: general weakness.
Special instructions
Do not exceed the recommended doses. in case of overdose, consult a doctor immediately due to the risk of liver damage, even if the patient is feeling well.
If you have an established intolerance to some sugars, you should consult your doctor before taking this medication. Amicitron contains sucrose, so the preparation should not be taken by patients with rare hereditary diseases associated with fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency. Amicitron contains sodium, so patients who follow a sodium-controlled diet should use this preparation with caution. The medicinal product contains FCF (E110) sunset yellow dye, which may cause allergic reactions.
Do not use simultaneously with other preparations intended for the symptomatic treatment of colds and rhinitis (vasoconstrictor, paracetamol-containing). Patients with mild arthritis who take analgesics every day, and patients who use warfarin or similar preparations that cause an anticoagulant effect, should consult a doctor before using the preparation.
In patients with severe infections such as sepsis, which are accompanied by a decrease in glutathione levels, the risk of metabolic acidosis increases with paracetamol. The symptoms of metabolic acidosis are deep, rapid or labored breathing, nausea, vomiting, and loss of appetite. You should immediately consult a doctor if these symptoms appear.
In case of liver or kidney disease, consult a doctor before using the preparation. It should be borne in mind that in patients with alcoholic non-cirrhotic lesions of the liver, the risk of the hepatotoxic effect of paracetamol increases.
Prescribe with caution for Raynaud's disease, hypertension, heart disease, arrhythmias (bradycardia, etc.), for prostatic hypertrophy, pheochromocytoma, for diseases of the thyroid gland, liver and kidneys, for glaucoma, chronic lung diseases and the elderly. The preparation contains phenylephrine, which can lead to angina attacks.
The preparation may affect the results of laboratory tests on the content of glucose and uric acid in the blood.
If symptoms persist (in particular if the headache becomes persistent), you should see your doctor.
Long-term use of the preparation without consulting a doctor can be dangerous.
Amicitron Plus and Amicitron Plus Sugar Free contain aspartame (E951), a source of phenylalanine that is dangerous for people with phenylketonuria.
Use during pregnancy and lactation. Do not use.
The ability to influence the reaction rate when driving or working with other mechanisms. When using Amicitron, it is not recommended to drive a car or work with other mechanisms, since the preparation may cause dizziness, drowsiness.
Interactions
The absorption rate of paracetamol may increase with the use of metoclopramide and domperidone and decrease with the use of cholestyramine. barbiturates reduce the severity of the antipyretic effect of paracetamol. anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of microsomal liver enzymes, can increase the toxic effect of paracetamol on the liver due to an increase in its conversion to hepatotoxic metabolites. with the simultaneous use of paracetamol with hepatotoxic agents, the toxic effect of preparations on the liver increases. the simultaneous use of paracetamol in high doses with isoniazid increases the risk of developing hepatotoxic syndrome. the anticoagulant effect of warfarin and other coumarins may increase with the simultaneous long-term regular daily use of paracetamol with an increased risk of bleeding; periodic intake does not cause significant effect. paracetamol reduces the effectiveness of diuretics. do not use simultaneously with alcohol.
The interaction of phenylephrine with MAO inhibitors causes a hypertensive effect, tricyclic antidepressants (amitriptyline) - increases the risk of cardiovascular side effects, digoxin and cardiac glycosides - leads to arrhythmias and heart attack. Phenylephrine with other sympathomimetics increases the risk of adverse cardiovascular reactions, may reduce the effectiveness of β-adrenergic receptor blockers and other antihypertensive preparations (reserpine, methyldopa) with an increased risk of hypertension and adverse cardiovascular reactions.
Pheniramine enhances the anticholinergic effect of atropine, antispasmodics, tricyclic antidepressants, antiparkinsonian preparations. The simultaneous use of feniramine with hypnotics, barbiturates, sedatives, antipsychotics, tranquilizers, anesthetics, narcotic analgesics, alcohol can significantly increase the severity of its inhibitory effect.
When taken orally, ascorbic acid enhances the absorption of penicillin, iron, reduces the effectiveness of heparin and indirect anticoagulants, increases the risk of crystalluria in the treatment of salicylates and the risk of glaucoma in the treatment of corticosteroids, in high doses reduces the effectiveness of tricyclic antidepressants. Antidepressants, antiparkinsonian and antipsychotic preparations, phenothiazine derivatives increase the risk of urinary retention, dry mouth, and constipation. Ascorbic acid can be taken only 2 hours after the injection of deferoxamine, since their simultaneous intake increases the toxicity of iron, especially in the myocardium. Long-term use in high doses during treatment with disulfiram inhibits the disulfiram-alcohol reaction.
Guaifenesin enhances the effect of sedatives and muscle relaxants.
Overdose
If the patient has taken the preparation in a dose higher than the recommended one, you should immediately consult a doctor because of the risk of liver damage. liver damage is possible in adults who have taken ≥10 g of paracetamol, and in children who have used paracetamol at a dose of 150 mg / kg body weight. taking ≥5 g of paracetamol can lead to liver damage in patients with risk factors (long-term use of carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. eating behavior, HIV infection, starvation, cystic fibrosis, cachexia).
Symptoms of a paracetamol overdose in the first 24 hours: pallor, nausea, vomiting, loss of appetite and abdominal pain. Liver damage can occur 12–48 hours after an overdose. Disorders of glucose metabolism and metabolic acidosis may occur. In severe poisoning, liver failure can progress to encephalopathy, hemorrhage, hypoglycemia, coma, and death. ARF with acute tubular necrosis can present with severe lumbar pain, hematuria, proteinuria, and develop even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have also been reported.
With long-term use of paracetamol in high doses on the part of the hematopoietic organs, aplastic anemia, pancytopenia, agranulocytosis, leukopenia (including neutropenia), and thrombocytopenia may develop. When taken in high doses from the central nervous system, dizziness, psychomotor agitation, disorientation, sleep disturbance are possible; from the urinary system - nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis).
In case of an overdose, an ambulance is needed. The patient should be taken to hospital immediately, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting, or may not reflect the severity of the overdose or the risk of organ damage. Treatment with activated charcoal should be considered if an excessive dose of paracetamol has been taken within 1 hour. The plasma concentration of paracetamol should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Treatment with N-acetylcysteine can be applied within 24 hours after taking paracetamol, but the maximum protective effect occurs when it is used within 8 hours after administration. The effectiveness of the antidote decreases sharply after this time. If necessary, the patient should be injected intravenously with N-acetylcysteine according to the current recommendations. In the absence of vomiting, oral methionine can be used as an appropriate alternative in remote areas outside the hospital.
In case of an overdose of phenylephrine, hyperhidrosis, psychomotor agitation or depression of the central nervous system, headache, dizziness, drowsiness, impaired consciousness, arrhythmias, tremors, hyperreflexia, convulsions, nausea, vomiting, irritability, anxiety, hypertension occur.
With an overdose of pheniramine, atropine-like symptoms occur: mydriasis, photophobia, dry skin and mucous membranes, hyperthermia, intestinal atony. Inhibition of the central nervous system leads to disruption of the respiratory and cardiovascular systems (bradycardia, arterial hypotension, collapse).
In case of an overdose of ascorbic acid, nausea, vomiting, bloating and abdominal pain, itching, skin rashes, and increased excitability occur. Doses of 3000 mg can cause temporary osmotic diarrhea and gastrointestinal disorders, impaired metabolism of zinc, copper, myocardial dystrophy, glucosuria, crystalluria, nephrolithiasis.
Guaifenesin. Overdose in small or moderate doses can cause dizziness or vertigo, gastrointestinal disturbances (in particular, nausea, vomiting). Very high doses can cause symptoms such as agitation, confusion, and respiratory depression.
Treatment: symptomatic therapy. Within 6 hours after an overdose, gastric lavage should be performed, and within the first 8 hours, methionine or intravenous cysteamine or N-acetylcysteine should be administered orally.
Storage conditions
In its original packaging at a temperature not exceeding 25 ° c.
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