Coldrelief (Tablets) Instructions for Use

Marketing Authorization Holder

Advanced Pharma, LLC (Russia)

ATC Code

N02BE71 (Paracetamol in combination with psycholeptics)

Dosage Form

Coldrelief

Tablets 30 mg+500 mg+10 mg+2 mg: 10 pcs.

Dosage Form, Packaging, and Composition

Tablets from orange to light orange with orange speckles from orange to dark orange and from white to almost white, capsule-shaped, biconvex, with a score on one side.

Excipients: sodium carboxymethylcellulose – 25 mg, povidone K30 – 30 mg, corn starch – 27.1 mg, microcrystalline cellulose (type 102) – 100 mg, sunset yellow FCF dye – 0.9 mg, talc – 7 mg, magnesium stearate – 3 mg, colloidal anhydrous silicon dioxide – 5 mg.

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – jars (1) – cardboard packs.

Clinical-Pharmacological Group

Drug for symptomatic therapy of acute respiratory diseases

Pharmacotherapeutic Group

Analgesics; other analgesics and antipyretics; anilides

Pharmacological Action

A combined drug that has antipyretic, analgesic, alpha-adrenergic stimulating, vasoconstrictive, and antihistamine effects, and relieves cold symptoms.

Paracetamol is a non-narcotic analgesic; it blocks COX, mainly in the CNS, affecting the centers of pain and thermoregulation; it has analgesic and antipyretic effects.

Phenylephrine is an alpha-adrenergic agonist with a moderate vasoconstrictive effect.

Chlorphenamine is an H₁-histamine receptor blocker. It constricts the vessels of the nose, eliminates swelling and hyperemia of the nasal mucosa, nasopharynx, and paranasal sinuses; reduces exudative manifestations, suppresses symptoms of allergic rhinitis.

Caffeine stimulates the psychomotor centers of the brain, enhances the effect of analgesics, eliminates drowsiness and fatigue, increases physical and mental performance, shortens reaction time, temporarily reduces fatigue and drowsiness.

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 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 is from 1 to 3 hours.

Phenylephrine is absorbed from the gastrointestinal tract. It is metabolized during the “first pass” through the intestinal wall and in the liver, so when taken orally, Phenylephrine Hydrochloride is characterized by limited bioavailability. Cmax in plasma is reached in the interval from 45 minutes to 2 hours. It is excreted by the kidneys almost completely in the form of sulfate compounds. T_1/2 is 2-3 hours.

Chlorphenamine after oral administration is relatively slowly absorbed from the gastrointestinal tract. Cmax is reached in 2.5-6 hours. Bioavailability is low – 25-50%. It undergoes the “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 CNS. 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 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

Symptomatic treatment of acute respiratory diseases, acute respiratory viral infections (including influenza), accompanied by fever, pain syndrome, rhinorrhea.

ICD codes

Dosage Regimen

Take the tablets orally with water.

Adhere strictly to a single dose of one tablet.

Maintain an interval of 4-6 hours between doses.

Do not exceed four doses (four tablets) in 24 hours.

Limit the total duration of treatment to a maximum of 5 days.

Do not use for pain relief for more than 5 days or for fever for more than 3 days unless directed by a physician.

Consult a doctor if symptoms persist or worsen after this period.

Avoid concomitant use of other products containing paracetamol.

Do not exceed the maximum daily dose of 2000 mg of paracetamol from all sources.

Patients with hepatic impairment, chronic alcoholism, or low glutathione reserves require a reduced total daily dose or increased dosing interval; consult a physician.

Do not crush or chew the tablets.

Adverse Reactions

Allergic reactions skin rash, itching, urticaria, angioedema.

From the nervous system headache, dizziness, insomnia, drowsiness, increased excitability.

From the cardiovascular system increased blood pressure, tachycardia.

From the digestive system dry mouth, nausea, vomiting, epigastric pain, hepatotoxic effect.

From the organ of vision mydriasis, accommodation paresis, increased intraocular pressure.

From the hematopoietic system anemia, thrombocytopenia, agranulocytosis, hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia.

From the urinary system renal colic, glucosuria, interstitial nephritis, papillary necrosis, difficulty urinating.

From the respiratory system dryness of the nasal mucosa, bronchoconstriction.

Contraindications

Severe atherosclerosis of the coronary arteries; arterial hypertension; portal hypertension; diabetes mellitus; erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; severe renal failure; severe hepatic failure; pheochromocytoma; hyperthyroidism; angle-closure glaucoma; alcoholism; simultaneous use of tricyclic antidepressants, MAO inhibitors, beta-blockers; pregnancy; lactation period; children under 15 years of age; hypersensitivity to the components of the combination; simultaneous use of other drugs containing components of this combination.

With caution

Thyroid diseases, diabetes mellitus, bronchial asthma, COPD, emphysema, chronic bronchitis, glucose-6-phosphate dehydrogenase deficiency, blood diseases (including hemolytic anemia), congenital hyperbilirubinemias (Gilbert’s syndrome, Dubin-Johnson syndrome, Rotor syndrome), acute hepatitis, viral hepatitis, alcoholic hepatitis, hepatic and/or renal failure, progressive malignant diseases, prostatic hyperplasia, pyloroduodenal obstruction, stenosing gastric and/or duodenal ulcer, epilepsy, dehydration, hypovolemia, anorexia, bulimia, cachexia (insufficient glutathione reserve in the liver), simultaneous use of inducers of liver microsomal enzymes.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

With caution in hepatic insufficiency.

Use in Renal Impairment

With caution in renal insufficiency.

Pediatric Use

Contraindicated for use in children under 15 years of age.

Special Precautions

During treatment, peripheral blood counts and liver functional state should be monitored.

During treatment, hypnotic and anxiolytic drugs (tranquilizers) should not be taken.

Do not take together with other drugs containing Paracetamol.

If the symptoms of the disease do not disappear within 5 days, you should consult a doctor.

During treatment, it is necessary to refrain from consuming ethanol (hepatotoxic effects may develop).

Effect on ability to drive vehicles and mechanisms

During treatment, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

It enhances the effects of MAO inhibitors, sedatives, ethanol.

Ethanol enhances the sedative effect of antihistamine drugs.

Antidepressants, antiparkinsonian and antipsychotic drugs, phenothiazine derivatives increase the risk of urinary retention, dry mouth, constipation.

Corticosteroids increase the risk of glaucoma.

Paracetamol reduces the effectiveness of uricosuric drugs.

Chlorphenamine concurrently with MAO inhibitors, furazolidone may lead to hypertensive crisis, agitation, hyperpyrexia.

Tricyclic antidepressants enhance the adrenomimetic effect of phenylephrine.

Concomitant use of halothane increases the risk of ventricular arrhythmia.

It reduces the hypotensive effect of guanethidine, which in turn enhances the alpha-adrenergic stimulating activity of phenylephrine.

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.