Citramon Ultra pills 10 pcs
Condition: New product
984 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Acetylsalicylic acid + Caffeine + Paracetamol
Release form
Pills
Composition
Acetylsalicylic acid - 0.2400 g, paracetamol -0.1800 g, caffeine- 0.0273 g in terms of caffeine monohydrate 0.0300 g; Excipients: hydroxypropylmethylcellulose (hypromellose), potato starch, colloidal silicon dioxide (aerosil), citric acid acid monohydrate, crospovidone, lactose monohydrate, polyethylene glycol 6000 (macrogol 6000), microcrystalline cellulose, stearic acid; Film auxiliary substances: Opadry II (series 85), polyvinyl alcohol, macrogol, talc, titanium dioxide, ferric oxide, iron o Ksid yellow, iron oxide red.
Pharmacological effect
Pharmacotherapeutic group: analgesic agent (nonsteroidal anti-inflammatory drug + analgesses non-narcotic counterparts + psycho-stimulant) Pharmacodynamics: A combination drug that includes acetylsalicylic acid, caffeine and paracetamol. Acetylsalicylic acid has antipyretic and anti-inflammatory agents, anti-inflammatory, anti-inflammatory, caffeine and paracetamol. platelet count and thrombosis, improves microcirculation in the inflammatory focus. Paras Etamol has analgesic, antipyretic and extremely weak anti-inflammatory effect, which is associated with its effect on the thermoregulation center in the hypothalamus and the weakly expressed ability to inhibit the synthesis of prostaglandins in peripheral tissues. Caffeine increases the reflex excitability of the spinal cord, stimulates the respiratory and vasomotor centers, expands the blood circulation of the spinal cord, expands the respiratory and vasomotor centers, expands the blood and the vasculature, extension, the subscipients, and the subunits of the spinal cord, stimulates the respiratory and vasomotor centers, expanding blood circulation, spontaneous excitability of the spinal cord, respiratory and vasomotor centers, and in the circuit, it can be used to extend the respiratory and vasomotor centers, extents, the respiratory and vasculomotor centers, the proliferative reflex excitability of the spinal cord; brain, heart, kidney, decreases platelet aggregation; reduces sleepiness, fatigue, increases mental and physical performance. In this combination, a small dose of caffeine has little or no stimulating effect on the central nervous system (CNS), but it helps normalize the vascular tone of the brain and accelerate blood flow. Pharmacokinetics: Acetylsalicylic acid: after ingestion, it is completely absorbed. During absorption, it is subjected to presystemic elimination in the intestinal wall and in the liver (it is deacetylated).The absorbed part is rapidly hydrolyzed by plasma cholinesterase and albumin esterase. In the body, acetylsalicylic acid circulates in connection with proteins up to 90%. Salicylates easily penetrate into tissues and body fluids, including joints, synovial and peritoneal fluids. TCmax - 2 hours for dosage forms with buffering properties. Biotransformed in the liver to form 4 metabolites. Removal of ascorbic acid is carried out mainly by the active secretion in the tubules of the kidneys in the form of salicylic acid itself (60%) and its metabolites. With alkalization of urine, the reabsorption of ionized salicylates worsens, their excretion increases significantly. The rate of elimination depends on the dose: when taking small doses, T 1/2 is 2-3 hours, with an increase in dose, it can increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults. Salicylates penetrate the placenta, in small quantities are excreted in breast milk. Paracetamol: quickly absorbed from the gastrointestinal tract. TCmax - 0.5-2 h; Cmax - 5-20 mcg / ml. Communication with plasma proteins is up to 15%. Penetrates through the hematoencephalic barrier (BBB). Metabolized in the liver by conjugation with glucuronides and sulfates, and also partially subjected to oxidation by microsomal liver enzymes. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated with glutathione, and then with cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this pathway are the isoenzyme CYP2E1, CYP1A2 and to a lesser extent CYP3A4. With a deficiency of glutathione, these metabolites can cause damage and necrosis of the hepatocytes. In adults, glucuronidation prevails, in newborns and young children - sulfation. Conjugated paracetamol metabolites (glucuronides, sulphates and conjugates with glutathione) have low pharmacological (including toxic) activity. Additional pathways of paracetamol metabolism are hydroxylation to 3-hydroxy paracetamol and to oxidation to 3-methoxy paracetamol, which has already been applied with a similar blood glucose mass of up to 3-hydroxy paracetamol and up to 3-methoxy paracetamol, which has already been applied with the same ready-to-breakdown blood glucose matrix, which has already been exposed to the same blood glucose mass, up to 3-hydroxy paracetamol, and methoxylation to 3-methoxy paracetamol, which subsequently put to the normal blood glucose matrix, which has been applied to the lactic glucose monolithic monosylase, which has already been exposed to the blood glucose mass. Excreted by the kidneys mainly in the form of conjugation products, less than 5% is excreted unchanged. T 1/2 - 1-4 hours. In elderly patients, the clearance of the drug decreases and T 1/2 increases. Less than 1% of the paracetamol dose taken by the nursing mother gets into breast milk. Caffeine: is well absorbed in the intestine.Absorption occurs mainly due to lipophilicity, but not water solubility. TCmax - 50-75 minutes after ingestion, Cmax - 1.58-1.76 mg / l. It is rapidly distributed in all organs and tissues of the body, easily penetrates the BBB and the placenta. The volume of distribution in adults is 0.4-0.6 l / kg, and in newborns it is 0.78-0.92 l / kg. Communication with blood proteins (albumin) - 25-36%. More than 90% of children undergo metabolism in the liver, up to 10-15% in children of the first years of life. In adults, about 80% of the dose of caffeine is metabolized to paraxanthin, about 10% to theobromine, and about 4% to theophylline. These compounds are subsequently demethylated to monomethylxanthines, and then to methylated uric acids. T 1/2 in adults — 3.9–5.3 hours (sometimes up to 10 hours), in newborns (up to 4–7 months of life) - up to 130 hours. predominantly by the kidneys in the form of metabolites. The excretion of 1-2% caffeine in adults and up to 85% in newborns is carried out unchanged.
Indications
Pain syndrome of mild and moderate severity (of various genesis): Headache of different origin; Migraine; Toothache; Myalgia; Arthralgia; Neuralgia; Algomenorrhea; Fever with ARVI (including flu).
Contraindications
Hypersensitivity to the drug; complete or incomplete combination of asthma, nasal polyposis and intolerance to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (NSAIDs); erosive and ulcerative lesions of the gastrointestinal tract, peptic ulcer and 12 duodenal ulcers (in the acute phase), gastrointestinal bleeding; hypocoagulation, hemophilia, hemorrhagic diathesis, hypoprothrombinemia; surgical intervention involving bleeding; portal hypertension; severe ischemic heart disease, severe hypertension; avitaminosis K; renal failure; pregnancy (I and III trimesters), lactation; deficiency of glucose-6-phosphate dehydrogenase, lactase, lactose intolerance, glucose-galactose malabsorption; glaucoma; anxiety disorders (agoraphobia, panic disorders), irritability, sleep disturbances; children up to 15 years old (risk of Reye’s syndrome in children with hyperthermia on the background of viral diseases). With caution: Gout, liver disease, renal and hepatic failure, benign hyperbilirubinemia (including Gilbert's syndrome), alcoholic liver damage, alcoholism , pregnancy, lactation, old age.
Use during pregnancy and lactation
Acetylsalicylic acid has a teratogenic effect; when applied in the first trimester leads to malformations - splitting of the upper palate; in the third trimester - to the inhibition of labor activity (inhibition of prostaglandin synthesis), to the closure of the arterial duct in the fetus, which causes hyperplasia of the pulmonary vessels and hypertension in the vessels of the pulmonary circulation. It is excreted in breast milk, which increases the risk of bleeding in a child due to dysfunction of platelets.
Dosage and administration
Adults and children over 15 years old should be taken orally (during or after a meal) with 1-2 pills 3-4 times a day with an interval between doses of 4-8 hours. The maximum daily dose is 8 pills. The duration of the drug intake is not more than 5 days as an analgesic drug and not more than 3 days - as an antipyretic (without prescription and doctor's observation). Increasing the daily dose of the drug or the duration of treatment is possible only after consulting a doctor.
Side effects
From the gastrointestinal tract: gastralgia, nausea, vomiting, hepatotoxicity, erosive and ulcerative lesions of the gastrointestinal tract. From the cardiovascular system: tachycardia, increased blood pressure. Allergic reactions: skin rash, pruritus, angioedema, hyperemia of the skin , Stevens-Johnson syndrome, Layel, bronchospasm. From the central nervous system: dizziness, headache. From the urinary system: nephrotoxicity, kidney damage with papillary necrosis. From the side of coagulation blood system: anemia, methemoglobinemia, decreased platelet aggregation, thrombocytopenia, hypocoagulation, hemorrhagic syndrome (nosebleeds, bleeding gums, purpura, etc.). From the sense organs: visual disturbances, tinnitus, deafness. Reye syndrome in children hyperpyrexia, metabolic acidosis, disorders of the nervous system and psyche, vomiting, abnormal liver function). Paracetamol. Nausea, epigastric pain (abdominal area, located directly under the point of convergence of the costal arches and sternum) are possible; allergic reactions such as skin rash, itching, urticaria, angioedema.Rarely - anemia (decrease in hemoglobin in the blood), thrombocytopenia (decrease in the number of platelets in the blood), methemoglobinemia (elevated blood levels of methemoglobin - a derivative of hemoglobin that is not capable of carrying oxygen). With long-term use in high doses, hepatotoxic (damaging the liver) action is possible. With prolonged use, especially in large doses, paracetamol may have a nephrotoxic (damaging kidney) effect. Acetylsalicylic acid. Dyspeptic symptoms (nausea, stomach pain). With prolonged use may occur gastritis, gastric ulcer and duodenal ulcer, possible gastric bleeding. Sometimes allergic reactions occur: bronchospasm, angioedema, skin reactions. Caffeine. Sometimes when using caffeine, insomnia, palpitations, trembling of the limbs, ringing in the ears, shortness of breath and vomiting occur. In addition, drug abuse may develop drug dependence.
Overdose
Symptoms: mild intoxication - pallor of the skin, nausea, vomiting, gastralgia, dizziness, tinnitus, severe intoxication - lethargy, drowsiness, collapse, seizures, bronchospasm, difficulty breathing, anuria, bleeding, anorexia, anemia Symptoms of abnormal liver function may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe damage to the liver); arrhythmia, pancreatitis. Initially, central hyperventilation of the lungs leads to respiratory alkalosis (shortness of breath, asphyxiation, cyanosis, increased sweating). As intoxication increases, progressive respiratory depression and oxidative phosphorylation dissociation cause respiratory acidosis. Treatment: constant monitoring of acid-base and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Increasing reserve alkalinity enhances the excretion of acetylsalicylic acid due to alkalization of urine. The introduction of SH-group donators and precursors of the synthesis of glutathione - methionine within 8-9 hours after overdose and acetylcysteine - within 8 hoursThe need for additional therapeutic measures (the further introduction of methionine, in / in the introduction of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after taking it.
Interaction with other drugs
Enhances the action of heparin, indirect anticoagulants, reserpine, steroid hormones and hypoglycemic drugs. The simultaneous appointment with other NSAIDs, methotrexate increases the risk of side effects. Prolonged use of paracetamol and other NSAIDs increases the risk of developing analgesic nephropathy and renal papillary necrosis, the onset of end-stage renal failure. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer. funds, as well as uricosuric agents that promote the excretion of uric acid. Inductors of liver microsomal enzymes (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol, and hepatotoxic drugs (HP) increase the production of hydroxylated active metabolites, which makes it possible for severe intoxication to develop even with a small overdose. Prolonged use of barbiturates reduces the effectiveness of paracetamol. Inductors of liver microsomal enzymes (including cimetidine) reduce the risk of hepatotoxic action of paracetamol. Metoclopramide accelerates the absorption of paracetamol. Under the influence of paracetamol T1 / 2chloramphenicol increases 5 times. With repeated use of paracetamol can enhance the effect of anticoagulants (coumarin derivatives) by reducing the synthesis of procoagulant factors in the liver. Simultaneous intake of paracetamol and ethanol increases the risk of developing acute pancreatitis. Diflunisal increases the plasma concentration of paracetamol by 50%, which causes the risk of hepatotoxicity. Myelotoxic drugs increase the hematotoxicity of the drug. Caffeine accelerates the absorption of ergotamine.
special instructions
Children under 15 years old can not prescribe drugs containing acetylsalicylic acid, because in the case of a viral infection, they can increase the risk of Reye's syndrome. Symptoms of Reye’s syndrome are prolonged vomiting, acute encephalopathy, and enlarged liver. With prolonged use of the drug requires monitoring of peripheral blood and the functional state of the liver. Patients with hypersensitivity or asthma reactions to salicylates or their derivatives of acetylsalicylic acid can be prescribed only with the observance of special precautions (in terms of emergency services). Since acetylsalicylic acid slows down blood coagulation, the patient, if he is to undergo surgery, must notify the doctor in advance about taking the drug. Acetylsalicylic acid in low doses reduces uric acid excretion. In patients with a corresponding predisposition, this can in some cases provoke an attack of gout. During treatment, you should abandon the use of ethanol (increased risk of gastrointestinal bleeding). Impact on the ability to drive a car and other vehicles psychomotor reactions.