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

Excipients: cocoa beans (cocoa) - 0.019 g; citric acid - 0.005 g; potato starch - 0.067 g; talc - 0.005 g; calcium stearate - 0.003 g; sucrose (sugar) 0.001 g

Description:

tablets of light brown color with inclusions plane-cylindrical with a smell of cocoa.

Pharmacotherapeutic group:analgesic agent combined (non-steroidal anti-inflammatory drug + analgesic non-narcotic remedy + psycho-stimulant).

ATX: & nbsp

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

Pharmacodynamics:

Acetylsalicylic acid (ASA) has antipyretic and anti-inflammatory effect, relieves pain, especially caused by the inflammatory process, and also moderately inhibits platelet aggregation and thrombosis, improves microcirculation in the inflammatory focus.

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

Paracetamol has an analgesic, antipyretic and extremely weak anti-inflammatory effect, which is associated with its influence on the center of thermoregulation in the hypothalamus and a weak ability to inhibit the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics:

Acetylsalicylic acid

At intake the absorption is complete. During absorption, it undergoes presystemic elimination in the intestinal wall and systemic in the liver (deacetylated). The resorbed part is rapidly hydrolyzed by cholinesterases and albumin esterase, therefore the elimination half-life is no more than 15-20 minutes.

In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid. Time to reach a maximum concentration of 2 hours. Metabolized mainly in the liver with the formation of 4 metabolites, found in many tissues and urine.
It is excreted mainly by active secretion in the renal tubules in the form of salicylate (60%) and its metabolites. Removal of unchanged salicylate depends on the pH of the urine (with alkalinization of urine ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly). The rate of excretion depends on the dose: when taking small doses, the half-life period is 2-3 hours, with an increase in the dose may increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults.

Paracetamol

Absorption is high, the time to reach the maximum concentration is reached after 0.5-2 h; the maximum concentration is 5-20 μg / ml. Connection with plasma proteins - 15%. Penetrates through the blood-brain barrier. Less than 1% of the dose of paracetamol taken by the lactating mother penetrates into breast milk. The therapeutically effective concentration of paracetamol in the plasma is achieved when it is administered at a dose of 10-15 mg / kg.

Metabolised in the liver (90-95%): 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites, which are conjugated to glutathione with the formation of already inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. In the metabolism of the drug is also involved isoenzyme CYP2E1. T1 / 2 1-4 h. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, the clearance of the drug decreases and the half-life increases.

Caffeine

When ingested absorption is good, occurs throughout the intestine. Absorption occurs mainly due to lipophilicity, and not water solubility. The time to reach the maximum concentration is 50-75 minutes after ingestion, the maximum concentration is 1.58-1.76 mg / l. Quickly distributed in all organs and tissues of the body; easily penetrates the blood-brain barrier 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 (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 are subsequently demethylated into monomethylxanthines, and then to methylated uric acids. The half-life in adults is 3.9-5.3 hours (sometimes up to 10 hours), in newborns (up to 4-7 months of life) - 65-130 hours. The excretion of caffeine and its metabolites is carried out by the kidneys (unchanged in adults 1-2 %, in newborns - up to 85%).

Indications:

"Citramon P" is used for:

- painful syndrome of mild and moderate severity (of different genesis): headache, migraine, toothache, neuralgia, myalgia, arthralgia, algodismenorea.

- febrile syndrome: in acute respiratory infections, including influenza.

Contraindications:

hypersensitivity;

- erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);

- gastrointestinal bleeding;

- bronchial asthma, urticaria or acute rhinitis, triggered by the use of ASA or other non-steroidal anti-inflammatory drugs;

- hemophilia;

- hemorrhagic diathesis;

- hypoprothrombinemia;

- portal hypertension;

- avitaminosis K;

- kidney failure;

- 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;

- Children's age (under 15 years - the risk of developing Reye's syndrome in children with hyperthermia

background of viral diseases).

Carefully:Carefully prescribe the drug for gout, liver disease.

Pregnancy and lactation:

"Citramon P" is contraindicated in pregnancy (I and III trimesters) and during lactation;

Dosing and Administration:

"Citramon P" is taken orally (during or after a meal). Adults and children over 15 years 1-2 tablets 2-3 times a day. The interval between doses should be at least 4 hours. The average daily dose is 3-4 tablets, the maximum daily dose is 8 tablets. The course of treatment is not more than 7-10 days.

The drug should not be taken more than 5 days as an analgesic drug and more than 3 days - antipyretic (without appointment and supervision of a doctor). Other dosages and schedules are prescribed by the doctor.

Side effects:

Allergic reactions (including Stevens-Johnson syndrome, Lyell), bronchospasm.

From the side of the digestive tract: gastralgia, nausea, vomiting, hepatotoxicity, erosive and ulcerative lesions of the gastrointestinal tract.

On the part of the hematopoiesis system: with long-term use - reduced platelet aggregation, hypocoagulation, hemorrhagic syndrome (epistaxis, bleeding gums, purpura, etc.).

From the cardiovascular system: increased blood pressure, tachycardia.

From the central nervous system: with prolonged use - dizziness, headache, visual disturbances, tinnitus, deafness.

From the urinary system: nephrotoxicity, with long-term use, renal damage with papillary necrosis.

Possible development in children of Reye's syndrome (hyperpyrexia, metabolic acidosis,nervous system and psyche, vomiting, impaired liver function).

Overdose:

Symptoms: with light intoxication - nausea, vomiting, gastralgia, dizziness, ringing in the ears; severe intoxication - retardation, drowsiness, collapse, convulsions, bronchospasm, shortness of breath, anuria, bleeding, encephalopathy, coma.Initially, central hyperventilation of the lungs leads to respiratory alkalosis (dyspnea, choking, cyanosis, sweating). With increasing intoxication, progressive paralysis of respiration and dissociation of oxidative phosphorylation cause respiratory acidosis. After a day - two are determined signs of liver damage (liver failure).

Treatment: gastric lavage, the appointment of adsorbents (Activated carbon); constant monitoring of acid-base state and electrolyte balance; depending onstanding metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Increased reserve alkalinity increases the excretion of ASA due to alkalinization of urine.

Interaction:

Simultaneous use of the drug "Citramon P" strengthens act:

- heparin,

- oral anticoagulants,

- reserpine,

- steroid hormones,

- hypoglycemic agents.

At repeated reception of a preparation "Citramon P" paracetamol can enhance the effect of anticoagulants (coumarin derivatives).

Simultaneous use of the drug "Citramon P" with methotrexate and non-steroidal anti-inflammatory drugs increases the risk of side effects.

Simultaneous use of the drug "Citramon P" reduces the efficiency:

- spironolactone,

- furosemide,

- antihypertensive drugs,

- antidotal agents that promote the excretion of uric acid.

Simultaneous use of the drug Citramon P with

- barbiturates,

- rifampicin,

- salicylamide,

- antiepileptic drugs,

- other stimulants of microsomal oxidation promotes the formation of toxic metabolites of paracetamol, affecting liver function.

Simultaneous reception of paracetamol and ethanol enhances risk of hepatotoxic effects.

When a joint application of the drug "Citramon P" with metoclopramide, the latter accelerates absorption of paracetamol.

Under the influence of paracetamol, the half-life of chloramphenicol increases 5 times.

Caffeine accelerates absorption of ergotamine.

Special instructions:

With continued use of the drug, control of peripheral blood and the functional state of the liver is necessary.

Since ASA slows blood clotting, the patient, if he is to undergo surgery,must warn the doctor in advance about taking the drug.

ASA in low doses reduces the excretion of uric acid. In patients with a corresponding predisposition, this can in some cases provoke a gout attack.

During treatment should be abandoned the use of ethanol (increased risk of gastrointestinal bleeding).

ASA has a teratogenic effect; when applied in the first trimester leads to a developmental defect - splitting of the upper palate; in the third trimester - to inhibition of labor (inhibition of the synthesis of prostaglandins), 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.

In 1 tablet contains 68 mg of carbohydrates (starch and sugar), which corresponds to 0.0057 grain unit (XE). The maximum daily dose (8 tablets) corresponds to 0.0456 XE. This should be taken into account by patients with diabetes mellitus.

Effect on the ability to drive transp. cf. and fur:not described

Form release / dosage:

Pills.

Packaging:

For 10 tablets in a planar cell package.

For 6 or 10 tablets in a contour non-jawed package.

For 1, 2, 3, 5 or 10 contour packs, together with instructions for use in cardboard packs.

Contoured packages, together with an equal number of instructions for use, are placed in a group package.

Storage conditions:

In a dry place, at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

4 years.

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

Terms of leave from pharmacies:Without recipe

Registration number:P N003262 / 01

Date of registration:09.02.2009

The owner of the registration certificate:MEDISORB, CJSC MEDISORB, CJSC Russia

Manufacturer: & nbsp

MEDISORB, CJSC Russia

Information update date: & nbsp30.03.2011

Illustrated instructions

Instructions

Citramon P (Citramon P)