Citrapak (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmstandard-UfaVITA OJSC (Russia)

ATC Code

N02BA71 (Acetylsalicylic acid in combination with psycholeptics)

Dosage Form

Citrapak

Tablets: 20 pcs.

Dosage Form, Packaging, and Composition

Tablets are round, flat-cylindrical, with a bevel and a score, from light brown to brown in color with inclusions of white and brown, with a slight characteristic cocoa odor.

Excipients: cocoa powder – 9 mg, citric acid – 4 mg, potato starch – 64 mg, povidone (low molecular weight polyvinylpyrrolidone, povidone K17) – 11 mg, talc – 6 mg.

10 pcs. – contour cell packs (2) – cardboard packs.

Clinical-Pharmacological Group

Combination analgesic-antipyretic

Pharmacotherapeutic Group

Analgesics; other analgesics and antipyretics; salicylic acid and its derivatives

Pharmacological Action

Combined medicinal product.

Acetylsalicylic acid has antipyretic and anti-inflammatory effects, relieves pain, especially that caused by the inflammatory process, and also moderately inhibits platelet aggregation and thrombus formation, improving microcirculation in the focus of inflammation.

Paracetamol is an analgesic-antipyretic. It has analgesic, antipyretic and weak anti-inflammatory effects. The mechanism of action is associated with inhibition of prostaglandin synthesis, with a predominant effect on the thermoregulation center in the hypothalamus.

Ascorbic acid is involved in the regulation of redox processes, carbohydrate metabolism, blood clotting, tissue regeneration, and the synthesis of steroid hormones; increases the body’s resistance to infections, reduces vascular permeability, reduces the need for vitamins B₁, B₂, A, E, folic acid, pantothenic acid. Improves the tolerability of paracetamol and prolongs its action (associated with the prolongation of T_1/2).

Caffeine stimulates the psychomotor centers of the brain, has an analeptic effect, enhances the effect of analgesics, eliminates drowsiness and fatigue, and increases physical and mental performance.

Pharmacokinetics

After oral administration of the drug, Acetylsalicylic acid is rapidly and almost completely absorbed from the gastrointestinal tract. It is partially metabolized during absorption. Bioavailability is about 70%, but this value is characterized by significant individual variability due to presystemic hydrolysis in the mucous membranes of the gastrointestinal tract and in the liver with the formation of salicylic acid under the action of enzymes. The bioavailability of salicylic acid is 80-100%. C_max of acetylsalicylic acid in blood plasma is reached 10-20 minutes after oral administration, and of salicylic acid – after 0.3-2 hours. Acetylsalicylic acid and salicylic acid are highly bound to plasma proteins and are rapidly distributed throughout the body. The degree of binding of salicylic acid to plasma proteins depends on the concentration and is non-linear. At low concentrations (<100 µg/ml), up to 90% of salicylic acid is bound to plasma proteins, at high concentrations (>400 µg/ml) – up to 75%. Salicylic acid crosses the placental barrier and is found in breast milk. Salicylic acid is metabolized under the influence of enzymes, mainly in the liver, to form metabolites (phenyl salicylate, salicyl glucuronide and salicyluric acid) found in many tissues and body fluids. In women, the metabolic process is slower (lower activity of enzymes in the blood serum). Acetylsalicylic acid and its metabolites are excreted primarily by the kidneys. T_1/2 of acetylsalicylic acid from blood plasma is 15-20 minutes, and of salicylic acid – 2-3 hours when taking acetylsalicylic acid in low doses and increases significantly when taking acetylsalicylic acid in high doses due to saturation of enzyme systems. In patients with normal renal function, 80-100% of a single dose of acetylsalicylic acid is excreted by the kidneys within 24-72 hours.

Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. C_max in plasma is reached 10-60 minutes after oral administration. It is distributed in most body tissues. It crosses the placental barrier and is excreted in breast milk. In therapeutic concentrations, binding to plasma proteins is insignificant but increases with increasing concentration. It undergoes primary metabolism in the liver. It is excreted mainly in the urine as glucuronides and sulfates. T_1/2 ranges from 1 to 3 hours.

Ascorbic acid is rapidly and completely absorbed from the gastrointestinal tract. Binding to plasma proteins is 25%. It is excreted in the form of metabolites in the urine. Ascorbic acid taken in excessive amounts is rapidly excreted unchanged in the urine.

Caffeine is rapidly absorbed from the gastrointestinal tract and distributed throughout the body. Caffeine is almost completely metabolized in the liver by oxidation and demethylation into metabolites that are excreted in the urine. T_1/2 is 4-9 hours.

Indications

Moderate and mild pain syndrome (including headache, toothache, neuralgia, algodismenorrhea), to reduce elevated body temperature in infectious-inflammatory and cold diseases.

ICD codes

Dosage Regimen

Take the tablets orally with a sufficient amount of liquid.

For adults and adolescents over 15 years of age, take one tablet as a single dose.

Repeat the dose 2-3 times per day as needed for pain or fever relief.

Maintain an interval of at least 4 hours between consecutive doses.

Do not exceed a maximum daily dose of 3 tablets.

For patients with impaired renal function or impaired liver function, extend the dosing interval to at least 8 hours.

Use the drug for no more than 5 days as an analgesic for pain relief.

Use the drug for no more than 3 days as an antipyretic for fever reduction.

If symptoms persist beyond these durations, discontinue use and consult a physician.

Do not use the medication for prolonged periods without medical supervision.

Follow any alternative dosage or regimen specifically prescribed by a doctor.

Adverse Reactions

Rarely skin allergic reactions (rash, itching, urticaria), palpitations, dizziness, nausea, stomach pain.

With long-term use in high doses, impaired liver and kidney function is possible.

Contraindications

Peptic ulcer of the stomach and duodenum, gastrointestinal bleeding, severe impairment of liver or kidney function. Genetic absence of glucose-6-phosphate dehydrogenase. Blood diseases with a tendency to hemorrhage and bleeding. Glaucoma, bronchial asthma. Pregnancy and breastfeeding period. Children under 15 years of age. Hypersensitivity to the components of the combination.

With caution

Elderly patients, impaired liver and kidney function. Combination of the drug with barbiturates, anticonvulsants, and rifampicin should be avoided.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Pediatric Use

Contraindicated for use in children under 15 years of age.

Special Precautions

Consultation with a doctor is necessary if patients have bronchial asthma, emphysema or chronic bronchitis; if symptoms do not go away within 5 days or are accompanied by severe fever lasting for 3 days, rash or persistent headache.

To avoid toxic liver damage, the combination product should not be combined with the consumption of alcoholic beverages.

The use of other medications should be agreed with a doctor.

Do not use the drug simultaneously with the consumption of alcoholic beverages.

Signs of acute poisoning are nausea, vomiting, stomach pain, sweating, pale skin, tachycardia. If poisoning is suspected, seek medical help immediately. Gastric lavage with activated charcoal should be performed on the victim.

Effect on the ability to drive vehicles and mechanisms

The combined medicinal product may cause drowsiness, therefore, during treatment, it is not recommended to drive vehicles or engage in other activities that require concentration and high speed of psychomotor reactions.

Drug Interactions

Paracetamol reduces the effectiveness of uricosuric drugs.

When the drug is prescribed simultaneously with barbiturates, phenytoin, carbamazepine, rifampicin and other inducers of liver microsomal enzymes, the risk of hepatotoxic effects of paracetamol increases.

It enhances the effect of agents that reduce blood clotting and platelet aggregation, as well as the side effects of glucocorticosteroids, sulfonylurea derivatives, methotrexate, non-narcotic analgesics and NSAIDs.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.