Ascorbic acid, Paracetamol, Pheniramine

Pharmacological properties

Pharmacological effects due to the components that make up the drug fairex:

- pheniramine maleate - blocker H₁-receptors, provides a desensitizing effect, manifested by a decrease in the severity of the inflammatory reaction of the mucous membranes of the upper respiratory tract (nasal breathing improves, rhinorrhea, sneezing and lacrimation decrease);

- paracetamol has an antipyretic and analgesic effect, facilitating the severity of pain and fever (headache, myalgia);

- ascorbic acid compensates for the bodys need for vitamin C.

Paracetamol after oral administration is rapidly and almost completely absorbed in the digestive tract. C_max paracetamol in blood plasma is reached 30-60 minutes after administration. Paracetamol is rapidly distributed in all tissues. Concentrations in blood, saliva and plasma are similar. Plasma protein binding is weak. Paracetamol is metabolized in the liver to form compounds with glucuronic acid and sulfates. The secondary metabolic pathway, which is catalyzed by cytochrome P 450, leads to the formation of an intermediate reagent (N-acetylbenzoquinoneimine), which under normal conditions of use is rapidly neutralized with reduced glutathione and excreted in the urine after conjugation with cysteine ​​and mercapturic acid. However, with severe poisoning, the amount of this toxic metabolite increases.

It is excreted in the urine, mainly in the form of metabolites. 90% of the dose taken is excreted by the kidneys within 24 hours, mainly in the form of conjugates with glucuronic acid (60–80%), sulfate conjugates (20–30%).

In unchanged form, about 5% of the dose taken is excreted. T_½ is about 2 hours

Pheniramine maleate is well absorbed in the digestive tract. It is allocated mainly by kidneys. T_½ - 60–90 minutes

Ascorbic acid is well absorbed in the digestive tract. It is excreted mainly with urine.

Indications

Fervex for adults: symptomatic treatment of colds, rhinitis, rhinopharyngitis, flu-like conditions manifested by rhinorrhea, lacrimation, sneezing, fever and / or headache.

Fervex for children: symptomatic treatment of colds, rhinopharyngitis in children (aged 6 years) and conditions manifested by rhinorrhea, lacrimation, sneezing, fever and / or headache.

Application

Fervex for adults. Inside adults and children over the age of 15 years, the drug is prescribed 1 sachet 2-3 times a day. Dissolve the contents of the sachet in a sufficient amount of cold or warm water. solution to take immediately after preparation. for patients with symptoms of a cold, it is better to take a warm solution of the drug in the evening. the interval between doses should be at least 4 hours. The maximum duration of treatment is 5 days.

For patients with impaired renal function (creatinine clearance of 10 ml / min), the interval between doses should be at least 8 hours.

If the symptoms of the disease do not disappear or worsen, a doctors consultation is necessary.

Fairx for children. For oral use. The contents of the sachets are dissolved in a sufficient amount of cold or warm water.

This release form is intended for use only in children (from the age of 6 years):

6-10 years - 1 sachet 2 times a day;

10-12 years - 1 sachet 3 times a day;

12-15 years old - 1 sachet 4 times a day.

The interval between doses should be at least 4 hours. The maximum duration of treatment is 3 days.

For patients with impaired renal function (creatinine clearance of 10 ml / min), the interval between doses should be at least 8 hours.

If the symptoms of the disease do not disappear or worsen, a doctors consultation is necessary.

Contraindications

Fervex for adults.hypersensitivity to drug components or antihistamines, severe liver and / or kidney dysfunctions, congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism, blood diseases, severe anemia, leukopenia, severe ag, unstable angina, severe cardiac conduction disturbances, acute myocardial infarction, severe atherosclerosis, decompensated heart failure, hyperthyroidism, acute urinary retention with prostatic hypertrophy, urinary neck obstruction Vågå bubble pyloroduodenal obstruction, gastric ulcer and duodenal ulcer in the acute stage, angle-closure glaucoma, thrombosis, thrombophlebitis, severe diabetes, epilepsy, elderly; fructose intolerance, glucose / galactose malabsorption syndrome, or sucrose-isomaltose deficiency due to sucrose content.

Do not use with MAO inhibitors and within 2 weeks after stopping MAO inhibitors. Fervex for adults is contraindicated in patients who take tricyclic antidepressants or β-adrenergic blockers for urolithiasis - provided that ascorbic acid enters the body at a dose of 1 g / day.

Fairx for children. Hypersensitivity to drug components or antihistamines, severe liver and / or kidney dysfunctions, phenylketonuria, congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism, blood diseases, severe anemia, leukopenia, severe hypertension, unstable angina, severe cardiac impairment acute myocardial infarction, severe atherosclerosis, decompensated heart failure, hyperthyroidism, acute urinary retention with prostatic hypertrophy, obstructive urinary bladder neck function, pyloroduodenal obstruction, gastric and duodenal ulcer in the acute stage, angle-closure glaucoma, thrombosis, thrombophlebitis, severe diabetes mellitus, epilepsy. Do not use with MAO inhibitors and within 2 weeks after stopping MAO inhibitors. Contraindicated in patients taking tricyclic antidepressants or β-adrenergic blockers. Urolithiasis - provided that ascorbic acid enters the body at a dose of 1 g / day.

Childrens age up to 6 years; fructose intolerance, glucose-galactose malabsorption syndrome or sucrose-isomaltose deficiency due to sucrose content.

Side effects

From the hematopoietic and lymphatic systems: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, pain in the heart), hemolytic anemia, thrombosis, hyperprothrombinemia, erythrocytopenia, thrombocytopenia, agranulocytosis, neutrophilia leukocytosis.

On the part of the immune system: anaphylaxis, anaphylactic shock, skin hypersensitivity reactions, including pruritus, rashes on the skin and mucous membranes (usually erythematic, urticaria), angioedema, erythema multiforme (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyells syndrome).

From the respiratory system: bronchospasm in patients sensitive to acetylsalicylic acid and other NSAIDs.

From the digestive tract: dry mouth, nausea, heartburn, vomiting, constipation, epigastric pain, diarrhea, impaired liver function, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (dose-dependent effect).

From the endocrine system: hypoglycemia up to hypoglycemic coma.

From the nervous system: rarely - headache, dizziness, sleep disturbance, insomnia, drowsiness, confusion, hallucinations, nervousness, trembling; in some cases - coma, convulsions, dyskinesia, changes in behavior, increased irritability; imbalance and memory, distraction, especially in elderly patients.

From the cardiovascular system: in isolated cases - tachycardia, myocardial dystrophy (dose-dependent effect with prolonged use), orthostatic hypotension.

From the side of metabolism: metabolic imbalance of zinc, copper.

From the urinary system: urinary retention and difficulty urinating, aseptic pyuria, renal colic.

On the part of the skin: eczema.

From the side of the organ of vision: dry eyes, mydriasis, impaired accommodation.

With prolonged use in high doses: damage to the glomerular apparatus of the kidneys, crystalluria, the formation of urate, cystine and / or oxalate calculi in the kidneys and urinary tract; damage to the insular apparatus of the pancreas (hyperglycemia, glucosuria) and impaired glycogen synthesis before the development of diabetes mellitus.

special instructions

In the case of high body temperature or prolonged fever that persists for 5 days against the background of the use of the drug, or if signs of superinfection appear, you should consult a doctor to determine the feasibility of further use of the drug.

Use with caution in patients with diabetes.

Alcohol enhances the sedative effect of pheniramine maleate, hepatotoxicity of paracetamol.

Ascorbic acid can change the results of laboratory tests (glucose, blood bilirubin, transaminase activity).

The risk of predominantly mental dependence appears when exceeding the recommended doses and with prolonged treatment.

To prevent overdose, all preparations containing paracetamol should be checked and excluded.

For adults with a body weight of 50 kg, the total dose of paracetamol should not exceed 4 g / day.

The maximum recommended doses of Fervex for children:

· Children with a body weight of 37 kg: the total dose of paracetamol should not exceed 80 mg / kg of body weight per day;

· Children weighing 38-50 kg: the total dose of paracetamol should not exceed 3 g / day;

· Children weighing 50 kg: the total dose of paracetamol should not exceed 4 g / day.

Precautionary measures. The use of alcoholic beverages or the use of sedatives (especially barbiturates) increase the sedative effect of pheniramine maleate, therefore, the use of these substances should be avoided during treatment.

Each sachet of Fervex for adults and Fervex for adults with raspberry flavor contains 11.5 g of sucrose, which should be considered for patients with diabetes mellitus and patients on a diet with a low sugar content.

Each Fervex sachet for children contains 2.4 g of sucrose, which should be considered for patients with diabetes mellitus and patients on a diet with a low sugar content.

Use during pregnancy and lactation. Since the effect of the drug on the course of pregnancy or breastfeeding is not well understood, it should not be prescribed during these periods.

Children. Fervex for adults is not used in children under the age of 15 years.

Fervex for children is used in children aged 6 to 15 years.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. The drug can cause drowsiness, so during its administration should refrain from driving vehicles or working with other mechanisms.

Interactions

Unwanted combinations. due to the presence of pheniramine, ethanol enhances the sedative effect of H1 receptor blockers, so you should refrain from driving vehicles or working with other mechanisms. during treatment, the use of alcoholic beverages and the use of medicines containing ethyl alcohol should be avoided.

Combinations to pay attention to. Due to the presence of pheniramine, other sedatives can cause CNS depression, these are drugs such as morphine derivatives (analgesics, cough suppressants, and replacement therapy), antipsychotics, barbiturates, benzodiazepines, anxiolytics, nonbenzodiazepines (e.g. meprobamate), hypnotics, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), sedative blockers N₁receptors, central antihypertensive agents, baclofen and thalidomide.

Due to the presence of feniramine, drugs that have an atropine-like effect, such as imipramine antidepressants, most atropine H blockers₁receptors, anticholinergics, antiparkinsonian drugs, atropine antispasmodics, disopramide, phenothiazine antipsychotics and clozapine can add undesirable atropine effects, such as urinary retention, constipation and dry mouth.

When taken with oral anticoagulants, there is a risk of their increased effect and an increased risk of bleeding when taking paracetamol in maximum doses (4 g / day) for at least 4 days. Check the INR regularly. If necessary, the dose of anticoagulant can be adjusted when taking paracetamol and after stopping treatment with paracetamol.

Reception of paracetamol can influence blood glucose results by glucose oxidase peroxidase method with abnormally high concentrations.

Reception of paracetamol can affect the results of determination of urea in the blood by the method of phosphoric tungsten acid.

The absorption rate of paracetamol may increase due to the simultaneous use with metoclopramide and domperidone and may decrease due to the use with colestyramine. Barbiturates reduce the severity of the antipyretic effect of paracetamol.

Anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of microsomal liver enzymes, can enhance the toxic effects of paracetamol on the liver due to an increase in the degree of conversion of the drug to hepatotoxic metabolites. With the simultaneous use of paracetamol with isoniazid, the risk of developing hepatotoxic syndrome increases. Paracetamol reduces the effectiveness of diuretics.

Do not use simultaneously with alcohol.

Ascorbic acid increases the absorption of iron in the intestine, the level of ethinyl estradiol, penicillin, tetracycline; reduces the level of antipsychotic drugs, phenothiazine derivatives in the blood. GCS reduces the reserves of ascorbic acid. The simultaneous administration of ascorbic acid and deferoxamine increases the tissue toxicity of iron, especially in the heart muscle, which can lead to decompensation of the circulatory system. It can be used only 2 hours after injection of deferoxamine. High doses of ascorbic acid reduce the effectiveness of tricyclic antidepressants. The absorption of ascorbic acid is reduced with the simultaneous use of oral contraceptives, the use of fruit or vegetable juices, alkaline drinking.

Overdose

Associated with pheniramine. an overdose of feniramine can cause seizures (especially in children), impaired consciousness, coma.

Associated with paracetamol. There is a risk of intoxication in the elderly and especially in young children (cases of therapeutic overdose and accidental poisoning are noted quite often).

An overdose of paracetamol can be fatal.

Symptoms Nausea, vomiting, anorexia, pallor, excessive sweating, abdominal pain, usually appear during the first 24 hours.

An overdose of more than 10 g of paracetamol in 1 dose in adults and 150 mg / kg of body weight in 1 dose in children causes hepatic cytolysis, which can lead to complete and irreversible necrosis, hepatocellular insufficiency, metabolic acidosis, encephalopathy, which, in turn, can determine coma and death.

At the same time, elevated levels of hepatic transaminases, LDH and bilirubin are noted against the background of an elevated level of prothrombin, which can occur 12–48 hours after application.

Urgent Activities:

- immediate hospitalization;

- determination of the initial level of paracetamol in blood plasma;

- immediate elimination of the applied drug by gastric lavage;

- the usual treatment of overdose includes the use of an antidote N-acetylcysteine ​​iv or orally. The antidote should be used as early as possible, preferably within 10 hours after an overdose;

- methionine as a symptomatic therapy.

Storage conditions

At temperatures up to 25 ° C.