Citramon Ultra, 20 pcs., film-coated tablets
Acetylsalicylic acid: after oral administration it is absorbed quite completely. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated).
The absorbed part is quickly hydrolyzed by plasma cholinesterases and albuminesterase. In the body, acetylsalicylic acid circulates in association with proteins up to 90%. Salicylates easily penetrate into tissues and body fluids, including joint cavities, synovial and peritoneal fluids. TCmax - 2 hours for dosage forms with buffering properties.
Biotransforms in the liver to form 4 metabolites. Removal of acetylsalicylic acid is carried out mainly by active secretion in the renal tubules in the form of salicylic acid itself (60%) and its metabolites. When urine becomes alkalized, the reabsorption of ionized salicylates worsens, and their excretion increases significantly. The rate of elimination depends on the dose: when taking small doses, T1/2 is 2-3 hours, with increasing doses it can increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults. Salicylates cross the placenta and are excreted in small quantities in breast milk.
Paracetamol: quickly absorbed from the gastrointestinal tract. TCmax - 0.5-2 hours; Cmax - 5-20 mcg/ml. Communication with plasma proteins is up to 15%. Penetrates the blood-tencephalic barrier (BBB).
Metabolized in the liver by conjugation with glucuronides and sulfates, and is also partially oxidized 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 metabolic pathway are the isoenzyme CYP2E1, CYP1A2 and, to a lesser extent, CYP3A4. With glutathione deficiency, these metabolites can cause damage and necrosis of hepatocytes.
In adults, glucuronidation predominates, in newborns and small children - sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.
Additional metabolic pathways for paracetamol are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates. Excreted by the kidneys mainly in the form of conjugation products, less than 5% is excreted unchanged. T1/2 -1-4 hours. In elderly patients, drug clearance decreases and T1/2 increases.
Less than 1% of the dose of paracetamol taken by a nursing mother passes into breast milk.
Caffeine: well absorbed in the intestines. Absorption occurs primarily due to lipophilicity rather than water solubility. Tmax - 50-75 minutes after oral administration, Cmax - 1.58-1.76
mg/l. It is quickly 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, in newborns - 0.78-0.92 l/kg. Communication with blood proteins (albumin) - 25-36%.
More than 90% is metabolized in the liver, in children of the first years of life up to 10-15%. In adults, about 80% of a caffeine dose is metabolized to paraxanthine, about 10% to theobromine, and about 4% to theophylline. These compounds are subsequently demethylated into monomethylxanthines and then into methylated uric acids.
T1/2 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 primarily by the kidneys in the form of metabolites. Excretion of 1-2% of caffeine in adults and up to 85% in newborns occurs unchanged.
Citramon Ultra
Acetylsalicylic acid: after oral administration it is absorbed quite completely. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is quickly hydrolyzed by plasma cholinesterases and albuminesterase. In the body, acetylsalicylic acid circulates in association with proteins up to 90%. Salicylates easily penetrate into tissues and body fluids, including joint cavities, synovial and peritoneal fluids.
TCmax - 2 hours for dosage forms with buffering properties.
Biotransforms in the liver to form 4 metabolites.
Removal of acetylsalicylic acid is carried out mainly by active secretion in the renal tubules in the form of salicylic acid itself (60%) and its metabolites. When urine becomes alkalized, the reabsorption of ionized salicylates worsens, and their excretion increases significantly.
The rate of elimination depends on the dose: when taking small doses, T1/2 is 2-3 hours, with increasing doses it can increase to 15-30 hours.
In newborns, the elimination of salicylates is much slower than in adults.
Salicylates cross the placenta and are excreted in small quantities in breast milk.
Paracetamol: quickly absorbed from the gastrointestinal tract. TCmax - 0.5-2 hours; Cmax - 5-20 mcg/ml. Communication with plasma proteins is up to 15%. Penetrates the blood-tencephalic barrier (BBB).
Metabolized in the liver by conjugation with glucuronides and sulfates, and is also partially oxidized 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 metabolic pathway are the isoenzyme CYP2E1, CYP1A2 and, to a lesser extent, CYP3A4. With glutathione deficiency, these metabolites can cause damage and necrosis of hepatocytes. In adults, glucuronidation predominates; in newborns, sulfation predominates. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.
Additional metabolic pathways for paracetamol are hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.
Excreted by the kidneys mainly in the form of conjugation products, less than 5% is excreted unchanged. T1/2 - 1-4 hours.
In elderly patients, drug clearance decreases and T1/2 increases.
Less than 1% of the dose of paracetamol taken by a nursing mother passes into breast milk.
Caffeine: well absorbed in the intestines. Absorption occurs primarily due to lipophilicity rather than water solubility. Tmax - 50-75 minutes after oral administration, Cmax - 1.58-1.76 mg/l. It is quickly 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, in newborns - 0.78-0.92 l/kg. Communication with blood proteins (albumin) - 25-36%.
More than 90% is metabolized in the liver, in children of the first years of life up to 10-15%. In adults, about 80% of a caffeine dose is metabolized to paraxanthine, about 10% to theobromine, and about 4% to theophylline. These compounds are subsequently demethylated into monomethylxanthines and then into methylated uric acids.
T1/2 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 primarily by the kidneys in the form of metabolites. Excretion of 1-2% of caffeine in adults and up to 85% in newborns occurs unchanged.
Citramon ultra
Tablets, film-coated, light brown, biconvex, oblong, with rounded ends, scored. On a cross section, two layers are visible, the inner layer is white or almost white.
1 tab. | |
acetylsalicylic acid | 0.24 g |
paracetamol | 0.18 g |
caffeine | 0.0273 g |
Excipients: hypromellose, potato starch, aerosil, citric acid monohydrate, crospovidone, lactose monohydrate, polyethylene glycol 6000, microcrystalline cellulose, stearic acid.
Composition of the humeral membrane: Opadry II (series 85), polyvinyl alcohol, macrogol, talc, titanium dioxide, black iron oxide, yellow iron oxide, red iron oxide.
5 pieces. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 5 pieces. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 5 pieces. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 5 pieces. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 5 pieces. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 5 pieces. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 6 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 6 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 6 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 6 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 6 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 6 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 10 pieces. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 15 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 15 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 15 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 15 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 15 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 15 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 20 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs.
CITRAMON ULTRA (tablets)
He advised me to buy a painkiller that contains caffeine, which will help dilate blood vessels and raise blood pressure.
After this, the degree of pain should subside and then the painkillers will work. I didn’t want to buy an expensive foreign medicine that would cost a lot of money, while the domestic equivalent would be much cheaper. At the first pharmacy where I turned for help, the pharmacist advised me to buy the painkiller “Citramon Ultra”, which is sold in the form of tablets, 10 pieces in a blister and is produced by a Russian company.
As I realized later, when I began to periodically take this drug, any pharmacy has it in stock, since this drug is in demand by customers due to its effectiveness and affordable price. The cost of the drug, compared to other similar drugs, is really acceptable and varies in the range from 50 to 60 rubles, depending on the pharmacy and its prices for drugs.
Of course, there are similar drugs that are cheaper, for example, Askofen, but it stopped helping me a long time ago, apparently it has become addictive. With the same drug, things were different; its effect began within 15 minutes, the eyes gradually began to open, and literally after half an hour the headache subsided.
If it did not go away, then at least its degree decreased. At such moments, I waited 2 hours and drank this remedy again, and then the state became almost healthy, and I could again perceive the world around me. But, as stated in the instructions, you cannot take more than 6 tablets per day, because an overdose may occur, which is accompanied by very unpleasant symptoms, which is described in detail in the same instructions.
Indications for use are headaches, toothaches, and migraines, which made me very happy, since such attacks also occur. You can also take this remedy as an antipyretic for fever, but I have not tried its effect in this aspect. Contraindications include acute diseases of the stomach and intestines, but children's age is not indicated, apparently the drug is not so harmful, and it can be given to children if necessary.
A huge list of side effects that may occur after use is listed in the instructions; they are associated with almost all organs. I couldn’t notice anything like that in this state and was only glad that the headache went away, and I simply didn’t notice the other unpleasant symptoms, so I can’t say anything definitive about this.
Otherwise, the drug has proven itself to be an effective and high-quality remedy that helps cope not only with severe headaches, but also with migraines.
Citramon Ultra PPO tablets No. 20
Compound
Active ingredients: acetylsalicylic acid 0.24 g, paracetamol 0.18 g, caffeine 0.0273 g.
Excipients: hypromellose, potato starch, aerosil, citric acid monohydrate, crospovidone, lactose monohydrate, polyethylene glycol 6000, microcrystalline cellulose, stearic acid.
Film shell composition: Opadry II (series 85), polyvinyl alcohol, macrogol, talc, titanium dioxide, black iron oxide, yellow iron oxide, red iron oxide.
Indications for use
- Pain syndrome of mild and moderate severity (of various origins): headache; migraine; toothache; neuralgia; myalgia; arthralgia; algodismenorrhea.
- Feverish syndrome: with acute respiratory infections; with the flu.
Contraindications
- Hypersensitivity to the components of the drug;
- erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase); gastrointestinal bleeding;
- “aspirin” asthma;
- hemophilia;
- hemorrhagic diathesis;
- hypoprothrombinemia;
- portal hypertension;
- vitamin deficiency K;
- renal failure;
- I and III trimesters of pregnancy; lactation period (breastfeeding);
- deficiency of glucose-6-phosphate dehydrogenase;
- severe arterial hypertension;
- severe course of ischemic heart disease;
- glaucoma;
- increased excitability;
- sleep disorders;
- surgical interventions accompanied by bleeding;
- childhood (up to 15 years - the risk of developing Reye's syndrome in children with hyperthermia due to viral diseases).
With caution: gout, liver disease.
Directions for use and doses
Taken orally (during or after meals) every 4 hours. On average, take 3-4 times a day. The maximum frequency of administration is 8 times/day. The course of treatment is no more than 7-10 days.
If kidney or liver function is impaired, the interval between doses is at least 6 hours.
The drug should not be taken for more than 5 days when prescribed as an analgesic and more than 3 days when prescribed as an antipyretic. Other doses and regimens of use are determined by the doctor.
Storage conditions
Store at a temperature not exceeding 25 °C. Keep out of the reach of children.
Best before date
2 years. Do not use after the expiration date stated on the packaging.
special instructions
Children should not be prescribed medications containing acetylsalicylic acid, since 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 liver enlargement.
With prolonged use of the drug, monitoring of peripheral blood and the functional state of the liver is necessary.
Since acetylsalicylic acid slows down blood clotting, the patient, if he is undergoing surgery, must notify the doctor in advance about taking the drug.
In patients with hypersensitivity or asthmatic reactions to salicylates or their derivatives, acetylsalicylic acid can only be prescribed with special precautions (in an emergency setting).
Acetylsalicylic acid in low doses reduces the excretion of uric acid. In patients with a corresponding predisposition, this can in some cases provoke an attack of gout.
During treatment, you should stop drinking ethanol (increased risk of gastrointestinal bleeding).
Description
Combined analgesic drug (NSAID + analgesic non-narcotic drug + psychostimulant drug).
Use in children
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 Reye's syndrome. Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, and liver enlargement.
Pharmacodynamics
Combined drug.
Acetylsalicylic acid has an antipyretic and anti-inflammatory effect, relieves pain, especially caused by the inflammatory process, and also moderately inhibits platelet aggregation and thrombus formation, improves microcirculation at the site of inflammation.
Caffeine increases the reflex excitability of the spinal cord, stimulates the respiratory and vasomotor centers, dilates the blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation; reduces drowsiness, fatigue, increases mental and physical performance. In this combination, caffeine in a small dose has virtually no stimulating effect on the central nervous system, but helps normalize cerebral vascular tone and accelerate blood flow.
Paracetamol has an analgesic, antipyretic and extremely weak anti-inflammatory effect, which is associated with its effect on the thermoregulation center in the hypothalamus and a weak ability to inhibit the synthesis of prostaglandins in peripheral tissues.
Side effects
From the digestive system: gastralgia, nausea, vomiting, hepatotoxicity, erosive and ulcerative lesions of the gastrointestinal tract.
From the urinary system: nephrotoxicity,
Allergic reactions: skin manifestations, Stevens-Johnson syndrome, Lyell's syndrome, bronchospasm.
From the cardiovascular system: tachycardia, increased blood pressure,
With long-term use: dizziness, headache, visual impairment, tinnitus, decreased platelet aggregation, hypocoagulation, hemorrhagic syndrome (including nosebleeds, bleeding gums, purpura), kidney damage with papillary necrosis; deafness; Reye's syndrome in children (hyperpyrexia, metabolic acidosis, nervous system and mental disorders, vomiting, liver dysfunction).
Use during pregnancy and breastfeeding
Contraindicated for use in the first and third trimesters of pregnancy and during lactation (breastfeeding).
Acetylsalicylic acid has a teratogenic effect; when used in the first trimester of pregnancy, it leads to a malformation - cleft palate; in the third trimester - to inhibition of labor (inhibition of prostaglandin synthesis), to closure of the ductus arteriosus 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 the baby due to impaired platelet function.
Interaction
Strengthens the effect of heparin, indirect anticoagulants, reserpine, steroid hormones and hypoglycemic drugs.
Co-administration with other NSAIDs and methotrexate increases the risk of side effects.
Reduces the effectiveness of spironolactone, furosemide, antihypertensive drugs, as well as anti-gout drugs that promote the excretion of uric acid.
Barbiturates, rifampicin, salicylamide, antiepileptic drugs and other stimulants of microsomal oxidation contribute to the formation of toxic paracetamol metabolites that affect liver function.
Metoclopramide accelerates the absorption of paracetamol.
Under the influence of paracetamol, T1/2 of chloramphenicol increases 5 times. When taken repeatedly, paracetamol may enhance the effect of anticoagulants (dicoumarin derivatives).
The simultaneous use of paracetamol and ethanol increases the risk of developing hepatotoxic effects.
Caffeine accelerates the absorption of ergotamine.
Overdose
Symptoms:
mild intoxication
- pallor of the skin, nausea, vomiting, gastralgia, dizziness, ringing in the ears;
severe intoxication
- lethargy, drowsiness, collapse, convulsions, bronchospasm, difficulty breathing, anuria, bleeding, anorexia, impaired glucose metabolism, metabolic acidosis.
Symptoms of liver dysfunction may appear 12-48 hours after an overdose.
In case of 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 (shortness of breath, suffocation, cyanosis, increased sweating). As intoxication increases, progressive respiratory depression and uncoupling of oxidative phosphorylation 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 alkalinization of urine.
Administration of SH-group donors and precursors for the synthesis of glutathione - methionine within 8-9 hours after an overdose and acetylcysteine - within 8 hours. The need for additional therapeutic measures (further administration of methionine, intravenous administration of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.