Coldrex^® Caps (Capsules) Instructions for Use

Marketing Authorization Holder

Stada Arzneimittel, AG (Germany)

ATC Code

N02BE51 (Paracetamol in combination with other drugs, excluding psycholeptics)

Dosage Form

Coldrex® Caps

Capsules: 10 or 20 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size No. 1, opaque, cap – yellow, body – white; capsule contents – powder from white to white with a yellowish tint.

Excipients: glyceryl tristearate, gelatin, lactose monohydrate – 2.5 mg.

Capsule body composition gelatin, water, titanium dioxide (E171).
Capsule cap composition gelatin, quinoline yellow dye (E104), water, sunset yellow FCF dye (E110) – 0.0026 mg, titanium dioxide (E171).

10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.

Clinical-Pharmacological Group

Drug for symptomatic therapy of acute respiratory diseases

Pharmacotherapeutic Group

Analgesics; other analgesics and antipyretics; anilides

Pharmacological Action

Combined drug.

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 prolongation of T_1/2).

Chlorphenamine is a histamine H₁-receptor blocker, has antihistamine, weak anticholinergic, and sedative effects. Reduces the severity of allergic reactions mediated by the action of histamine, reduces capillary permeability, constricts blood vessels, eliminates swelling and hyperemia of the nasal mucosa, nasopharynx, and paranasal sinuses; reduces local exudative manifestations, suppresses symptoms of allergic rhinitis: sneezing, rhinorrhea, itching of the eyes, nose.

Caffeine has an antispasmodic (relaxing) effect, dilates the bronchi, tones the cerebral vessels, stimulates the heart, and has a general tonic effect.

Pharmacokinetics

Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. C_max in plasma is reached within 10-60 minutes after oral administration. It is distributed to 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 urine as metabolites. Ascorbic acid, taken in excessive amounts, is rapidly excreted unchanged in the urine.

Chlorphenamine after oral administration is relatively slowly absorbed from the gastrointestinal tract. C_max is reached in 2.5-6 hours. Bioavailability is low – 25-50%. It undergoes a first-pass effect through the liver. Binding to plasma proteins is about 70%. It is widely distributed in the organs and tissues of the body and penetrates the central nervous system. It is intensively metabolized in the liver to form desmethyl- and didesmethylchlorphenamine. It is excreted mainly in the urine unchanged and as metabolites. Excretion depends on urine pH and urine flow rate. Only trace amounts of chlorphenamine are found in feces. T_1/2 varies from 2 hours to 43 hours.

Caffeine is completely and rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It is almost completely metabolized in the liver by oxidation and demethylation into metabolites, which are excreted by the kidneys. The average T_1/2 when taking a therapeutic dose is about 4-9 hours.

Indications

Febrile syndrome in infectious and inflammatory diseases; pain syndrome of moderate or mild intensity (headache, migraine, toothache, neuralgia, myalgia, arthralgia, algodysmenorrhea).

ICD codes

Dosage Regimen

Take orally with water.

Adults and children over 15 years: take 1-2 capsules as a single dose.

Repeat dosing 2-3 times per day as needed for symptom relief.

Maintain a minimum 4-hour interval between consecutive doses.

Do not exceed 8 capsules within a 24-hour period.

For patients with hepatic impairment, renal impairment, or elderly patients, extend the dosing interval to at least 8 hours.

Limit the total duration of use to 3-5 days for fever and 5 days for pain without medical supervision.

Discontinue use if symptoms persist or worsen.

Avoid concomitant use of other products containing paracetamol.

Adverse Reactions

From the nervous system in isolated cases – headache, feeling of fatigue, drowsiness.

From the digestive system: in isolated cases – nausea, pain in the epigastric region, dry mouth.

From the endocrine system in isolated cases – hypoglycemia (up to the development of coma).

From the hematopoietic system in isolated cases – anemia, hemolytic anemia (especially for patients with glucose-6-phosphate dehydrogenase deficiency); extremely rarely – thrombocytopenia.

Allergic reactions skin rash, itching, urticaria, angioedema, anaphylactoid reactions (including anaphylactic shock), multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Other in isolated cases – hypervitaminosis C, metabolic disorder, feeling of heat, accommodation paresis, urinary retention.

Contraindications

Hypersensitivity to the components of the combination; gastrointestinal bleeding; portal hypertension; alcoholism; severe hepatic and/or renal failure; pregnancy (I and III trimesters), breastfeeding period; children under 15 years of age; angle-closure glaucoma; prostatic hyperplasia with residual urine formation; severe arrhythmias; uncontrolled arterial hypertension.

With caution

Renal and/or hepatic insufficiency, glucose-6-phosphate dehydrogenase deficiency, congenital hyperbilirubinemias (Gilbert’s, Dubin-Johnson and Rotor syndromes), viral hepatitis, alcoholic hepatitis, old age.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindication: severe hepatic failure, portal hypertension.

With caution: hepatic insufficiency, congenital hyperbilirubinemias (Gilbert’s, Dubin-Johnson and Rotor syndromes), viral hepatitis, alcoholic hepatitis.

Use in Renal Impairment

Contraindication: severe renal failure.

With caution: renal failure.

Pediatric Use

Contraindicated for use in children under 15 years of age.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

When taking metoclopramide, domperidone, or cholestyramine, it is also necessary to consult a doctor.

With long-term use in doses significantly exceeding the recommended ones, the likelihood of impaired liver and kidney function increases; monitoring of the peripheral blood picture is necessary.

Paracetamol and Ascorbic acid may distort laboratory test results (quantitative determination of glucose and uric acid in blood plasma, bilirubin, activity of liver transaminases, LDH).

To avoid toxic liver damage, Paracetamol should not be combined with the intake of alcoholic beverages, and should not be taken by persons prone to chronic alcohol consumption. The risk of liver damage increases in patients with alcoholic hepatosis.

Prescribing ascorbic acid to patients with rapidly proliferating and intensively metastasizing tumors may exacerbate the course of the process.

Ascorbic acid should be used in minimal doses in patients with increased iron content in the body.

Drug Interactions

Ethanol enhances the sedative effect of antihistamine drugs.

Antidepressants, antiparkinsonian, antipsychotic drugs (phenothiazine derivatives) increase the risk of side effects (urinary retention, dry mouth, constipation).

Corticosteroids increase the risk of developing glaucoma.

Microsomal oxidation inducers (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, increasing the risk of severe intoxication with small overdoses.

Microsomal oxidation inhibitors (cimetidine) reduce the risk of hepatotoxic effects.

Paracetamol reduces the effectiveness of uricosuric drugs .

With simultaneous use of oral contraceptives, the concentration of ascorbic acid in the blood plasma decreases. An increase in the concentration of ethinyl estradiol in the blood plasma is possible with its simultaneous use as part of oral contraceptives.

When used simultaneously with iron preparations, Ascorbic acid, due to its reducing properties, converts ferric iron to ferrous iron, which contributes to improved absorption.

When used simultaneously with warfarin, a decrease in the effects of warfarin is possible.

With simultaneous use, Ascorbic acid increases the excretion of iron in patients receiving deferoxamine .

When used simultaneously with tetracycline, the excretion of ascorbic acid in the urine increases.

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.