Citramon Ultra - instructions for use, dose, side effects, contraindications

Excipients: hydroxypropylmethylcellulose (hypromellose), potato starch, silicon dioxide colloid (aerosil), citric acid monohydrate, crospovidone, lactose monohydrate, polyethylene glycol 6000 (macrogol 6000), microcrystalline cellulose, stearic acid;

auxiliary substances for the film sheath: Opadrai II (series 85), polyvinyl alcohol, macrogol, talc, titanium dioxide, iron oxide black, iron oxide yellow, iron oxide red.

Description:

The tablets covered with a film membrane of light brown color, biconvex, oblong with rounded ends, with a risk.On the cross-section, two layers are visible, the inner layer is white or almost white.

Pharmacotherapeutic group:Analgesic agent (non-steroidal anti-inflammatory drug + analgesic non-narcotic agent + psychostimulating agent)

ATX: & nbsp

N.02.B.A.51 Acetylsalicylic acid in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Combined a drug, including acetylsalicylic acid, caffeine and paracetamol.

Acetylsalicylic acid has antipyretic and anti-inflammatory effect, relieves pain, especially caused by the inflammatory process, and also inhibits platelet aggregation and thrombosis, improves microcirculation in the focus of inflammation. Paracetamol possesses analgesic, antipyretic and extremely weak anti-inflammatory effect, which is associated with its influence on the center of thermoregulation in the hypothalamus and weakly expressed ability fast hydrolyzed to inhibit the synthesis of prostaglandins in peripheral tissues.

Caffeine increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, dilates blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation; reduces drowsiness, fatigue, increases mental and physical operability. In this combination caffeine in a small dose practically not renders stimulating effect on the central nervous system (CNS), but it contributes to the normalization of the vascular tone of the brain and the acceleration of blood flow.

Pharmacokinetics:

Acetylsalicylic acid: after intake is sufficiently absorbed. During absorption, the presystem elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is sufficient fast hydrolysed cholinesterases of plasma 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 in the joint cavity, synovial and peritoneal fluids. TS_max - 2h for medicinal forms with buffer properties. Biotransformiruetsya in the liver with education 4 metabolites.

Excretion acetylsalicylic acids carried out mainly by active secretion in the renal tubules in the form of salicylic acid proper (60%) and its metabolites. When alkalization urine worsens reabsorption ionized salicylates, excretion their significantly increases. The rate of excretion depends on the dose: at taking small doses of T1 / 2 is 2-3 hours, with increasing doses - can increase up to 15-30 hours. Have newborns elimination of salicylates is carried out much slower than in adults. Salicylates penetrate the placenta, in small quantities are excreted in breast milk.

Paracetamol: quickly absorbed from the gastrointestinal tract. ТСmax - 0.5-2 hours; Cmax is 5-20 μg / ml. The connection with plasma proteins is up to 15%. Penetrates through the blood-brain barrier (BBB). Metabolized in the liver by conjugation with glucuronides and sulfates, and also partially oxidation microsomal enzymes liver. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated to glutathione, and then to cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this pathway of metabolism are isoenzyme CYP2E1, CYP1A2 and to a lesser extent CYP3A4. With a deficiency of glutathione, these metabolites can cause damage and necrosis of hepatocytes. Have of adults prevails glucuronidation, in newborns sylvitation. Conjugated metabolites paracetamol (glucuronides, sulfates and conjugates with glutathione) possess low pharmacological (including toxic) activity.

Additional ways of metabolizing paracetamol are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates. It is excreted by the kidneys mainly in the form of conjugation products, less than 5% is excreted unchanged. T1 / 2 1-4 h. In elderly patients the clearance of the drug decreases and T1 / 2 increases. Less than 1% of the dose of paracetamol taken by the lactating mother penetrates into breast milk.

Caffeine: well absorbed in intestines. Absorption occurs mainly due to lipophilicity, and not water solubility. TS_max - 50-75 minutes after ingestion, Cmax - 1.58-1.76 mg / l. Rapidly distributed in all organs and tissues of the body, easily penetrates the GEB and the placenta. The volume of distribution in adults is 0.4-0.6 l / kg, in newborns it is 0.78-0.92 l / kg. Communication with blood proteins (albumins) is 25-36%.

Metabolism in the liver is more than 90%, in children of the first years of life up to - 10-15%.In adults, about 80% of the dose of caffeine is metabolized to paraxanthin, about 10% to theobromine and about 4% to theophylline. These compounds subsequently demethylated at 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.

It is excreted mainly by kidneys in the form of metabolites. Excretion of 1-2% of caffeine in adults and up to 85% in newborns is carried out unchanged.

Indications:

Pain syndrome of mild to moderate severity (of different origins):

- Headache of different origin;

- Migraine;

- Toothache;

- Myalgia;

- Arthralgia;

- Neuralgia;

- Algodismenorea;

- Feverish condition in ARVI (including influenza).

Contraindications:

Hypersensitivity to the components of the drug; complete or incomplete combination of bronchial asthma, polyposition of nose and intolerance of acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (NSAIDs); erosive and ulcerative lesions of the gastrointestinal tract, gastric ulcer and duodenal ulcer (in the phase of exacerbation), gastrointestinal bleeding; hypocoagulation, hemophilia,hemorrhagic diathesis, hypoprothrombinemia; surgical interventions accompanied by bleeding; portal hypertension; severe course of ischemic heart disease, severe arterial hypertension; avitaminosis K; kidney failure; pregnancy (I and III trimesters), lactation period; deficiency of glucose-6-phosphate dehydrogenase, lactase, lactose intolerance, glucose-galactose malabsorption; glaucoma; anxiety disorders (agoraphobia, panic disorders), increased excitability, sleep disturbances; Children under 15 years of age (the risk of developing Reye's syndrome in children with hyperthermia in the presence of viral diseases).

Carefully:

Gout, liver disease, renal and hepatic insufficiency, benign hyperbilirubinemia (including Gilbert's syndrome), alcoholic liver damage, alcoholism, pregnancy, lactation period, elderly age.

Pregnancy and lactation:Acetylsalicylic acid has a teratogenic effect; when applied in the first trimester leads to a developmental defect - splitting of the upper palate; at III trimester - to inhibition of labor (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 small circle of blood circulation. Isolated with breast milk, which increases the risk of bleeding in the child due to impaired platelet function.

Dosing and Administration:

Adults and children over 15 years of age take orally (during or after meals) 1 -2 tablets 3-4 times per day with intervals between doses of 4-8 hours. The maximum daily dose is 8 tablets. 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 appointment and supervision by a doctor). An increase in 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, hepagotoxicity, erosive-ulcerative lesions of the gastrointestinal tract.

From the cardiovascular system: tachycardia, increased blood pressure. Allergic reactions: skin rash, itching, angioedema, skin hyperemia, Stevens-Johnson syndrome, Dyel, bronchospasm.

From the side of the central nervous system: dizziness, headache.

From the side of the urinary system: nephrotoxicity, kidney damage with papillary necrosis.

From the coagulation system: anemia, methemoglobinemia, decreased platelet aggregation, thrombocytopenia, hypocoagulation, haemorrhagic syndrome (epistaxis, bleeding gums, purpura, etc.).

From the sense organs: visual disturbances, noise in the ears, deafness.

Reye's syndrome in children (hyperpyrexia, metabolic acidosis, disorders of the nervous system and psyche, vomiting, liver dysfunction).

Paracetamol. There may be nausea, pain in the epigastrium (abdominal region, located immediately below the point of convergence of the ribs and sternum); allergic reactions in the form of skin rash, itching, hives, swelling of Quincke. Rarely, anemia (a decrease in hemoglobin in the blood), thrombocytopenia (a decrease in the number of platelets in the blood), methemoglobinemia (elevated blood levels of methemoglobin, a hemoglobin derivative that is incapable of transferring oxygen). With prolonged use in high doses, it is possible to hepatotoxic (damaging the liver) action.

With prolonged use, especially in high doses, paracetamol can have nephrotoxic (kidney-damaging) effect.

Acetylsalicylic acid. Dyspeptic phenomena (nausea, pain in the stomach). With prolonged use may occur gastritis, peptic ulcer of the stomach and duodenum, gastric bleeding is possible. Sometimes there are allergic reactions: bronchial spasm, Quincke's edema, skin reactions.

Caffeine. Sometimes, when caffeine is used, insomnia, palpitation, trembling of the limbs, ringing in the ears, dyspnoea and vomiting occur. In addition, with the abuse of the drug may develop drug dependence.

Overdose:

Symptoms:

slight intoxication - pallor of the skin, nausea, vomiting, gastralgia, dizziness, ringing in the ears;

severe intoxication - retardation, drowsiness, collapse, convulsions, bronchospasm, shortness of breath, anuria, bleeding, anorexia, glucose metabolism disorder, metabolic acidosis.

Symptoms of liver dysfunction 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 liver damage); arrhythmia, pancreatitis.

Initially, central hyperventilation of the lungs leads to respiratory alkalosis (dyspnea, choking, cyanosis, increased sweating). As the intoxication intensifies, progressive respiratory depression and dissociation of oxidative phosphorylation cause respiratory acidosis.

Treatment: constant control of acid-base and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Increased reserve alkalinity increases the excretion of acetylsalicylic acid due to alkalinization of urine.

Introduction donators SH-groups and precursors of the synthesis of glutathione-methionine for 8-9 hours after overdose and acetylcysteine-for 8 hours. The need for additional therapeutic measures (further introduction of methionine, iv injection of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time that has elapsed since it was received.

Interaction:

Strengthens the action of heparin, indirect anticoagulants, reserpine, steroid hormones and hypoglycemic drugs.Simultaneous administration with other NSAIDs, methotrexate increases the risk of side effects. Long-term combined use of paracetamol and other NSAIDs increases the risk of developing an "analgesic" nephropaand renal papillary necrosis, the onset of the terminal stage of renal failure.

Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer. Reduces the effectiveness of spironolactone, furosemide, antihypertensive drugs, as well as uricosuric agents that promote the excretion of uric acid. Inductors of microsomal liver enzymes (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs (AFROM) increase the production of hydroxylated active metabolites, which causes the possibility of severe intoxication even with a slight overdose. Long-term use of barbiturates reduces the effectiveness of paracetamol. Inductors of microsomal liver enzymes (including cimetidine) Reduce the risk of hepatotoxic effects of paracetamol.

Metoclopramide accelerates the absorption of paracetamol. Under the influence of paracetamol T1/2 Chloramphenicol increased by 5 times. At repeated reception paracetamol can enhance the effect of anticoagulants (coumarin derivatives) by reducing the synthesis of procoagulant factors in the liver. Simultaneous reception of paracetamol and ethanol increases the risk of developing acute cancreatitis.

Diflunisal increases the plasma concentration of paracetamol by 50%, which leads to the risk of hepatotoxicity.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Caffeine accelerates the absorption of ergotamine.

Special instructions:

Children under 15 years of age should not be prescribed medications containing acetylsalicylic acid, since in the case of a viral infection they can increase the risk of developing Reye's syndrome. Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver. With continued use of the drug, control of peripheral blood and the functional state of the liver is necessary.Patients with hypersensitivity or with asthmatic reactions to salicylates or their derivatives of acetylsalicylic acid can be prescribed only with special precautions (in emergency medical services). Since acetylsalicylic acid slows blood clotting, the patient, if he is to undergo surgery, must warn the doctor in advance about taking the drug. Acetylsalicylic acid in low doses reduces the excretion of uric acid. In patients with an appropriate predisposition, this can in some cases provoke an attack. During treatment, ethanol should be discarded (increased risk of gastrointestinal bleeding).

Effect on the ability to drive transp. cf. and fur:Impact on the ability to drive and other vehicles During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets.

Packaging:

By 5, 6, 10, 12, 15, 20 tablets into the contour cell pack of film polyvinylchloride and aluminum foil printed lacquered.

According to 1, 2, 3, 4, 5, 6 contour cellular Packages together with the application is placed in a pack of cardboard.

Storage conditions:

In a dry, dark place at a temperature of not more than 25 ° C.

Shelf life:

Shelf life 2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-004843/10

Date of registration:27.05.2010

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp21.11.2013

Illustrated instructions

Instructions

Citramon Ultra (Citramon-Ultra)