Coldact with vit. From the tablet, No. 10
Expiration Date: 05/2027
Russian Pharmacy name:
Колдакт с вит. С таблетки, №10
For oral administration. A single dose is taken 2-3 times / day, depending on age. The interval between doses is at least 4 hours.
In patients with impaired liver or kidney function and in elderly patients, the interval between doses should be at least 8 hours.
Film-coated tablets of a reddish-brown color, biconvex, oblong, with rounded ends, smooth on both sides; cross-section: the core is almost white and the shell is reddish-brown.
1 tab.
paracetamol 650 mg
phenylephrine hydrochloride 10 mg
ascorbic acid 30 mg
chlorphenamine (chlorpheniramine) maleate 4 mg
Excipients: colloidal silicon dioxide - 15 mg, pregelatinized starch - 50 mg, microcrystalline cellulose - 95.65 mg, sodium carboxymethyl starch - 30 mg, povidone K30 - 30 mg, talc - 5 mg, magnesium stearate - 9 mg.
Erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase), severe renal and / or hepatic failure;
alcoholism;
angle-closure glaucoma;
phenylketonuria;
hyperplasia of the prostate;
children under 3 years old;
children under 15 years of age (for dosage forms intended for adults);
pregnancy, lactation (breastfeeding);
hypersensitivity to the components of the combination.
Carefully
Renal and / or hepatic failure, deficiency of glucose-6-phosphate dehydrogenase, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), viral hepatitis, alcoholic hepatitis, old age.
pharmachologic effect
Combined drug.
Paracetamol is an antipyretic analgesic. It has analgesic, antipyretic and weak anti-inflammatory effects. The mechanism of action is associated with inhibition of the synthesis of prostaglandins, a predominant effect on the center of thermoregulation in the hypothalamus.
Ascorbic acid is involved in the regulation of redox processes, carbohydrate metabolism, blood clotting, tissue regeneration, in 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 tolerance of paracetamol and lengthens its action (associated with lengthening T1 / 2).
Chlorphenamine - a blocker of histamine H1 receptors, has an antihistamine, weak anticholinergic, sedative effect. Reduces the severity of allergic reactions mediated by the action of histamine, reduces capillary permeability, narrows blood vessels, eliminates swelling and hyperemia of the mucous membrane of the nasal cavity, nasopharynx and paranasal sinuses; reduces local exudative manifestations, suppresses the symptoms of allergic rhinitis: sneezing, rhinorrhea, itchy eyes, nose.
Phenylephrine is a sympathomimetic, has a pronounced alpha-adrenergic activity, narrows the vessels of the nasal mucosa, eliminates swelling and hyperemia of the nasal mucosa.
Pharmacokinetics
Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax in plasma is achieved within 10-60 minutes after ingestion. Distributed into most body tissues. Penetrates through the placental barrier, excreted in breast milk. At therapeutic concentrations, binding to plasma proteins is negligible, but increases with increasing concentration. Undergoes primary metabolism in the liver. It is excreted mainly in the urine in the form of glucuronides and sulfates. T1 / 2 is from 1 to 3 hours.
Ascorbic acid is rapidly and completely absorbed from the gastrointestinal tract. Plasma protein binding - 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.
Chlorphenamine after oral administration is relatively slowly absorbed from the gastrointestinal tract. Cmax is achieved in 2.5-6 hours. Bioavailability is low - 25-50%. Undergoes a 'first pass' effect through the liver. Plasma protein binding is about 70%. It is widely distributed in organs and tissues of the body, penetrates into the central nervous system. It is extensively metabolized in the liver to form desmethyl- and didesmethylchlorphenamine. It is excreted mainly in the urine unchanged and in the form of metabolites. Excretion depends on urine pH and urine flow rate. In feces, only trace amounts of chlorphenamine are determined. T1 / 2 varies from 2 hours to 43 hours.
Phenylephrine. Absorption after oral administration varies markedly, it undergoes intensive first-pass metabolism. As a result, its systemic bioavailability is only 40%, and Cmax in plasma is reached within 1-2 hours after ingestion. Vd is 200-500 liters, and the average T1 / 2 from plasma is 2-3 hours. After absorption, it undergoes intensive biotransformation in the intestinal wall. After oral administration, 24% of phenylephrine is deaminated, since most of the ingested drug is metabolized by sulfation even before it reaches the liver.
Side effect
From the side of the nervous system: in isolated cases - headache, 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 side of the hematopoietic system: in isolated cases - anemia, hemolytic anemia (especially for patients with deficiency of glucose-6-phosphate dehydrogenase); extremely rare - thrombocytopenia.
Allergic reactions: skin rash, itching, urticaria, Quincke's edema, anaphylactoid reactions (including anaphylactic shock), exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).
Others: in isolated cases - hypervitaminosis C, metabolic disorders, a feeling of heat, paresis of accommodation, urinary retention.
Application during pregnancy and lactation
Use during pregnancy and lactation (breastfeeding) is contraindicated.
Application for violations of liver function
The drug is contraindicated for use in case of impaired liver function.
Application in children
Use in children under 3 years of age is contraindicated. In children under the age of 15, use in the form of dosage forms intended for adults is contraindicated.
special instructions
If you are taking metoclopramide, domperidone, or cholestyramine, you should also consult your doctor.
With prolonged use in doses significantly higher than recommended, the likelihood of impaired liver and kidney function increases, monitoring of the peripheral blood picture is necessary.
Paracetamol and ascorbic acid can distort laboratory tests (quantitative determination of glucose and uric acid in blood plasma, bilirubin, activity of 'hepatic' transaminases, LDH).
In order to avoid toxic damage to the liver, paracetamol should not be combined with the intake of alcoholic beverages, as well as taken by persons prone to chronic alcohol consumption. The risk of developing liver damage increases in patients with alcoholic hepatosis.
The administration of ascorbic acid to patients with rapidly proliferating and intensely metastatic tumors can aggravate the course of the process.
In patients with an increased iron content in the body, ascorbic acid should be used in minimal doses.
Drug interactions
Ethanol enhances the sedative effect of antihistamines.
Antidepressants, antiparkinsonian, antipsychotic drugs (phenothiazine derivatives) increase the risk of side effects (urinary retention, dry mouth, constipation).
GCS 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.
Inhibitors of microsomal oxidation (cimetidine) reduce the risk of hepatotoxic effects.
Paracetamol reduces the effectiveness of uricosuric drugs.
With the simultaneous use of oral contraceptives, the concentration of ascorbic acid in the blood plasma decreases. It is possible to increase the concentration of ethinyl estradiol in the blood plasma with its simultaneous use as part of oral contraceptives.
When used simultaneously with iron preparations, ascorbic acid, due to its regenerating properties, converts trivalent iron into bivalent, which helps to improve its absorption.
With simultaneous use with warfarin, it is possible to reduce the effects of warfarin.
With the simultaneous use of ascorbic acid increases the excretion of iron in patients receiving deferoxamine.
With simultaneous use with tetracycline, the excretion of ascorbic acid in the urine increases.
Phenylephrine
Reduces the hypotensive effect of diuretics and antihypertensive drugs (including methyldopa, mecamylamine, guanadrel, guanethidine).
Phenothiazines, alpha-blockers (phentolamine), furosemide and other diuretics reduce the hypertensive effect.
MAO inhibitors (including furazolidone, procarbazine, selegiline), oxytocin, ergot alkaloids, tricyclic antidepressants, methylphenidate, adrenostimulants increase the pressor effect and arrhythmogenicity of phenylephrine.
Beta-blockers reduce the cardiac stimulating activity, arterial hypertension is possible against the background of reserpine (due to the depletion of catecholamines in the adrenergic endings, the sensitivity to adrenergic agonists increases).
Inhalation anesthetics (including chloroform, enflurane, halothane, isoflurane, methoxyflurane) increase the risk of severe atrial and ventricular arrhythmias, since they sharply increase the sensitivity of the myocardium to sympathomimetics.
Ergometrine, ergotamine, methylergometrine, oxytocin, doxapram increase the severity of the vasoconstrictor effect.
Reduces the antianginal effect of nitrates, which in turn can reduce the pressor effect of sympathomimetics and the risk of arterial hypotension (simultaneous use is allowed depending on the achievement of the desired therapeutic effect).
Thyroid hormones increase (mutually) the effect and the associated risk of coronary insufficiency (especially in coronary atherosclerosis).
The simultaneous use of phenylephrine and other sympathomimetic amines can lead to an increase in blood pressure and other side effects from the cardiovascular system.
Concomitant use of cardiac glycosides (eg, digoxin) and phenylephrine may increase the risk of arrhythmias and myocardial infarction.