Paracetamol phenylephrine pheniramine. Phenylephrine hydrochloride: what is it? Instructions, application

Included in the preparations

ATX:

N.02.B.E Anilides

N.02.B.E.51 Paracetamol in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Combined drug.

It has analgesic, antipyretic, antihistamine, vasoconstrictor, sedative, bronchodilator and antitussive effects.

Paracetamol

It has antipyretic, analgesic and anti-inflammatory effects. Inhibits cyclooxygenase, mainly in the central nervous system, affects the centers of pain and thermoregulation. It does not have a negative effect on water-salt metabolism and the mucous membranes of the gastrointestinal tract, and therefore has a slight effect on the synthesis of prostaglandins in peripheral tissues.

Phenylephrine

α 1-adrenergic agonist causes constriction of arterioles and reduces vascular permeability of the nasal mucosa, reduces swelling, facilitates breathing, reduces rhinorrhea and lacrimation. Causes pupil dilation without affecting accommodation, lowers intraocular pressure in glaucoma.

Pheniramine

The H1 receptor blocker has antihistamine, antiserotonin, anticholinergic, and sedative effects. Constricts the vessels of the nasal cavity, suppresses the symptoms of allergic rhinitis: rhinorrhea, sneezing, itching of the nose and eyes.

Pharmacokinetics:

Paracetamol

After oral administration, it is completely absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is achieved after 20-30 minutes. Plasma protein binding is 15%. Penetrates the blood-brain barrier and enters breast milk.

Metabolism in the liver by glucuronidation and sulfation (80%) with the formation of inactive metabolites, about 17% undergoes hydroxylation to active metabolites, which are subsequently deactivated after conjugation with sulfates and glutathione. With a lack of glutathione, these metabolites block liver enzyme systems, causing necrosis of hepatocytes.

The half-life is 2-3 hours. Elimination by the kidneys, about 3% unchanged.

Phenylephrine

After oral administration, up to 30% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 3 hours. The binding to plasma proteins is 70%. Penetrates the blood-brain barrier.

Metabolism in the liver.

Pheniramine

After oral administration, up to 30% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2.5 hours. The connection with plasma proteins is 70%. The therapeutic effect develops 1 hour after administration and continues for 24 hours. Penetrates the blood-brain barrier.

Metabolism in the liver.

The half-life is 2 hours. Elimination by the kidneys.

Indications:

Used to treat influenza and colds accompanied by headache, fever, and rhinitis. Used for allergic rhinitis.

X.J10-J18.J11 Flu, virus not identified

X.J20-J22.J22 Acute lower respiratory tract respiratory infection, unspecified

X.J30-J39.J39 Other upper respiratory tract diseases

Contraindications:

Bleeding in the gastrointestinal tract, phenylketonuria, glucose-6-phosphate dehydrogenase deficiency, portal hypertension, anemia, leukopenia, thrombocytopenia, individual intolerance.

Carefully:

Gilbert's syndrome, viral hepatitis, old age, alcoholism.

Pregnancy and lactation: Directions for use and dosage:

Inside 1 sachet 4 times a day.

Highest daily dose: 4 sachets.

Highest single dose: 1 sachet.

Side effects:

Central and peripheral nervous system: weakness, drowsiness, hallucinations, impaired coordination of movements.

Hematopoietic system: rarely aplastic anemia, pancytopenia.

Digestive system: dry mouth, constipation.

Dermatological reactions: exfoliative dermatitis.

Sense organs: diplopia.

Urinary system: difficulty urinating.

Allergic reactions.

Overdose:

Necrosis of liver cells due to the formation of a toxic metabolite of acetaminophen - N-acetyl-p-benzoquinoneimine.

Symptoms: nausea, vomiting, pallor of the skin, hepatonecrosis, tubular necrosis.

Treatment: use of donors SH -groups, precursors for the synthesis of glutathione - methionine and N -acetylcysteine ​​within 12 hours after an overdose.

Interaction:

Enhances the effect of indirect coagulants and the toxicity of chloramphenicol.

Taking ethanol during treatment with the drug leads to the development of acute pancreatitis.

Simultaneous use with stimulants of microsomal oxidation in the liver: barbiturates, rifampicin, ethanol, phenylbutazone, phenythionine increases the toxicity of paracetamol.

Microsomal oxidation inhibitors () reduce the risk of hepatotoxicity.

Special instructions:

Monitoring the content of glucose and uric acid in plasma, the composition of peripheral blood, and the functional state of the liver.

Instructions

Russian name

Paracetamol + Phenylephrine + Pheniramine + Ascorbic acid

Latin name of the substances Paracetamol + Phenylephrine + Pheniramine + Ascorbic acid

Paracetamolum + Phenylephrinum + Pheniraminum + Acidum ascorbinicum ( genus. Paracetamoli + Phenylephrini + Pheniramini + Acidi ascorbinici)

Pharmacological group of substances Paracetamol + Phenylephrine + Pheniramine + Ascorbic acid

Nosological classification (ICD-10)

Typical clinical and pharmacological article 1

Pharmaceutical action. Combined drug. Paracetamol is a non-narcotic analgesic, acting on the centers of pain and thermoregulation, and has an analgesic and antipyretic effect. Pheniramine is a blocker of H1-histamine receptors, reduces rhinorrhea and lacrimation, eliminates spastic phenomena. Phenylephrine is an adrenergic agonist with a moderate vasoconstrictor effect (stimulation of alpha 1 adrenergic receptors). Ascorbic acid is involved in the regulation of redox processes, carbohydrate metabolism, blood clotting, tissue regeneration, and in the synthesis of steroid hormones; increases the body's resistance to infections, reduces vascular permeability, reduces the need for vitamins B 1, B 2, A, E, folic acid, pantothenic acid. Improves the tolerability of paracetamol and prolongs its action (associated with prolongation of T1/2).

Indications. Feverish syndrome (“colds” and infectious diseases). Pain syndrome (mild and moderate severity): arthralgia, myalgia, neuralgia, migraine, toothache and headache, algomenorrhea. Sinusitis, rhinorrhea (acute rhinitis, allergic rhinitis).

Contraindications. Hypersensitivity; portal hypertension; alcoholism; renal failure; pregnancy (I and III trimesters), lactation period; deficiency of glucose-6-phosphate dehydrogenase.

Carefully. Congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), childhood (up to 15 years - for the dosage form intended for adults), childhood (up to 6 years - for the pediatric dosage form), angle-closure glaucoma, prostatic hyperplasia.

Dosing. Inside, 1 packet is dissolved in 200 ml of water, 4 times a day.

Side effect. Allergic reactions (skin rash, itching, urticaria, angioedema), nausea, epigastric pain; anemia, thrombocytopenia, agranulocytosis. Increased excitability, dizziness, increased blood pressure, difficulty falling asleep. Mydriasis, accommodation paresis, increased intraocular pressure, dry mouth; urinary retention. With long-term use in large doses - hepatotoxic effect, hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia; nephrotoxicity (renal colic, glycosuria, interstitial nephritis, papillary necrosis).

Overdose. Symptoms (due to paracetamol): pale skin, decreased appetite, nausea, vomiting; hepatonecrosis (the severity of necrosis due to intoxication directly depends on the degree of overdose). Toxic effects in adults are possible after taking more than 10-15 g of paracetamol: increased activity of “liver” transaminases, increased prothrombin time (12-48 hours after administration); a detailed clinical picture of liver damage appears after 1-6 days. Rarely, liver failure develops rapidly and can be complicated by renal failure (tubular necrosis).

Treatment: administration of SH-group donors and precursors for the synthesis of glutathione - methionine 8-9 hours after an overdose and N-acetylcysteine ​​after 12 hours.

The need for additional therapeutic measures (further administration of methionine, intravenous administration of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after its administration.

Interaction. Enhances the effects of MAO inhibitors, sedatives, ethanol.

Ethanol enhances the sedative effect of antihistamines.

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

GCS increase the risk of developing increased intraocular pressure.

Paracetamol reduces the effectiveness of uricosuric drugs and increases the effectiveness of indirect anticoagulants.

Tricyclic antidepressants enhance their sympathomimetic effect; simultaneous administration of halothane increases the risk of developing ventricular arrhythmia.

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

Special instructions. During the treatment period, it is necessary to refrain from drinking ethanol (possible development of hepatotoxic effects), driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

State register of medicines. Official publication: in 2 volumes - M.: Medical Council, 2009. - Volume 2, part 1 - 568 pp.; Part 2 - 560 s.

Interactions with other active ingredients

Trade names

Name The value of the Vyshkowski Index ®

In modern medicine, quite often there is a need to use adrenergic agonists, as well as vasoconstrictors. And in such cases, doctors often prescribe medications that contain phenylephrine hydrochloride. What it is? What properties does the substance have? How does it affect the body? In what cases is it advisable to take this medicine? The answers to these questions are of interest to many patients.

Phenylephrine hydrochloride: what is it? Release form, trade names

This remedy is often used in modern medicine. But what properties does phenylephrine hydrochloride have? What it is? To begin with, it’s worth understanding the general information.

This product is a white, sometimes yellowish, crystalline powder. This substance dissolves easily and quickly in water and alcohol.

Today, a solution for intravenous or subcutaneous administration (available in ampoules under the name “Phenylephrine”) is widely used. In addition, this substance is an active component of eye drops. In particular, it is present in such drugs as Irifrin and Neosynephrine.

Components such as pheniramine maleate and phenylephrine hydrochloride are included in many cold remedies, in particular Grippocitron. There are also nasal sprays/drops containing this component - they have vasoconstrictor properties. There are also rectal suppositories that are used for hemorrhoids (as part of complex therapy), although not so often.

Phenylephrine hydrochloride. Action and pharmacological properties

This drug belongs to the group of adrenergic agonists. It acts on postsynaptic alpha-adrenergic receptors. Under the influence of the drug, a narrowing of the arterioles and an increase in blood pressure are observed. Compared to adrenaline and norepinephrine, this drug does not increase blood pressure so quickly and sharply. At the same time, the effect lasts much longer, since the medicine is slowly metabolized.

It was also noted that the drug stimulates the central nervous system, although to a small extent. After taking the medicine, a narrowing of the pulmonary vessels is observed, which leads to an increase in pressure in the pulmonary artery. The drug stimulates blood circulation in the abdominal cavity and limbs.

Intravenous administration is considered the most effective. The effect of the medicine appears almost immediately. Metabolism of phenylephrine occurs in the liver. Metabolic products are excreted from the body along with urine.

The solution is also used externally, in the form of eye drops. This substance ensures rapid dilation of the pupil, as well as the outflow of intraocular fluid. One of the effects of the drug is vasoconstriction. Immediately after instillation, contraction of the smooth muscles of the arterioles of the conjunctiva and the pupillary dilator is observed. The effect appears 10 minutes after the procedure and lasts about 4-6 hours.

When should you use nasal drops?

When is it advisable to use nasal spray or drops that contain phenylephrine hydrochloride? The use of the drug is justified in the presence of swelling of the mucous membrane.

Drops are prescribed to patients for colds, flu, hay fever and other allergic diseases of the upper respiratory tract if the disease is accompanied by swelling of the mucous membrane. This drug allows you to quickly ease breathing and significantly improve the patient’s condition.

Solution. Indications for use

As already mentioned, this remedy belongs to the group of adrenergic drugs. Injections are carried out in the following cases:

  • acute arterial hypertension;
  • vascular insufficiency, including that which developed as a result of taking too many vasodilators;
  • shock conditions, including traumatic and toxic;
  • the drug is also administered when using local anesthetics (as a vasoconstrictor).

Eye drops. Features of application

Eye drops containing phenylephrine are also widely used in modern ophthalmology:

  • to dilate the pupil during diagnostic procedures;
  • for the prevention of iridocyclitis;
  • A 10% solution is used before eye surgery in order to dilate the pupil as much as possible;
  • to eliminate the so-called red eye syndrome;
  • in the treatment of glaucomocyclic crises.

How and in what doses should the solution be used?

Of course, the dosage and schedule of administration are selected by the attending physician. As a rule, with a moderate decrease in blood pressure, the solution is administered intramuscularly or subcutaneously. No more than 2-5 mg of the active substance is administered at a time. To achieve a greater effect, the solution can be administered intravenously - in this case, a single dose is equal to 0.2 mg of phenylephrine.

If we are talking about jet administration using a dropper, then 10 mg of the drug is diluted in 9 ml of purified water for injection. For infusion, the same amount of phenylephrine is diluted using 500 ml of 9% saline solution or 5% glucose solution.

As a rule, 1 or 2% eye drops are used for therapeutic and prophylactic purposes. A solution with a concentration of 10% is used only before surgery.

The application regimen is simple: 2-3 drops are instilled into the conjunctival sac. It is important to ensure that the tip of the bottle does not touch the mucous membrane of the eye. The effect of the procedure lasts for several hours.

Nasal spray/drops. Instructions for use

The dosage of nasal medications depends on the age of the patient. If we are talking about babies in the first year of life, then experts recommend instilling one drop into each nostril. The break between procedures should last at least six hours.

Children from 1 to 6 years old can instill 2 drops into each nasal passage. A single dosage for patients over 6 years of age is 4 drops.

In modern otolaryngology, nasal spray is also used, however, it can only be prescribed to patients over 12 years of age. Experts recommend 2-3 sprays into each nostril. The drug can be used no more often than once every four hours. Therapy in most cases lasts three days, although the right to change the treatment schedule remains with the doctor.

Contraindications to therapy

Is it possible to use medications containing phenylephrine hydrochloride in all cases? Eye drops have some contraindications:

  • violation of the integrity of the eyeball;
  • narrow-angle and closed-angle glaucoma, regardless of severity;
  • diseases of the cardiovascular and cerebrovascular system, especially when it comes to elderly patients;
  • impaired tear production;
  • congenital forms of glucose-6-phosphate dehydrogenase deficiency;
  • hyperthyroidism at any stage of development;
  • hepatic form of porphyria.

There are also age restrictions - drops are not prescribed to children under 12 years of age, as well as to adolescent patients with insufficient body weight. A 10% solution cannot be instilled in the presence of an arterial aneurysm.

In what other cases should a drug such as phenylephrine hydrochloride not be used? Nasal drops are not instilled in the following cases:

  • in the presence of sclerosis of the coronary vessels, angina pectoris and some other pathologies of the cardiovascular system;
  • during a severe hypertensive crisis;
  • for thyrotoxicosis and diabetes mellitus;

Drops should also not be used by children under six years of age.

It is also worth noting that there are restrictions on injections using phenylephrine hydrochloride solution. The instructions for use contain information that therapy may be dangerous in the following cases:

  • with high blood pressure;
  • with ventricular fibrillation;
  • in some forms of cardiomyopathy;
  • with decompensated forms of heart failure;
  • in severe forms of ischemic disease;
  • with damage to the cerebral arteries;
  • in the presence of pheochromocytoma.

There are also relative contraindications. For example, if a patient has hypoxia, hypercapnia, metabolic acidosis, hypovolemia, or thyrotoxicosis, the medicine can be used, but the patient must be constantly monitored and strictly adhere to the dose prescribed by the doctor. The list of restrictions can be supplemented with such pathologies as shock conditions after a heart attack, bradycardia, ventricular arrhythmia, and arterial hypertension. Age also matters - the drug is prescribed with caution to elderly people, as well as to patients under 18 years of age.

Are there any complications? List of adverse reactions

Is it safe to use medications that contain phenylephrine hydrochloride? Instructions for use, as well as reviews from doctors, indicate that most often the body tolerates therapy well. However, the possibility of adverse reactions cannot be ruled out. Their list includes:

  • increase or decrease in blood pressure;
  • chest pain;
  • migraine;
  • sleep problems, in particular insomnia;
  • tremor;
  • general weakness;
  • increased heart rate, increased heart rate;
  • heart rhythm disturbances, including arrhythmias, tachycardia, bradycardia;
  • frequent dizziness, unexplained anxiety, constant irritability;
  • occlusion of coronary arteries;
  • nausea ending in vomiting;
  • myocardial infarction;
  • pronounced pallor of the skin;
  • respiratory dysfunction;
  • increased sweat production;
  • increased intraocular pressure;
  • thromboembolism.

Some patients complain of pain and swelling at the injection site. Sometimes soft tissue necrosis may develop in this area.

What else could be dangerous about drugs containing phenylephrine hydrochloride? Eye drops may cause burning and irritation of the mucous membrane. Sometimes there is increased lacrimation. Some patients complain of blurred vision, which, however, goes away on its own.

There are other side effects that occur with the use of phenylephrine hydrochloride. Nasal drops/spray can sometimes cause irritation to the mucous membrane. Some patients complain of severe itching and burning in the nose, which occurs immediately after instillation. If any deterioration occurs, you should immediately consult a doctor.

What to replace the medicine with?

What should I do if, for one reason or another, a medicine containing phenylephrine hydrochloride is not suitable for the patient? Analogues of medicines, of course, exist.

For example, effective adrenergic agonists are drugs such as Mezaton and Midodrine. As for nasal drops, products such as Nazol and Otrivin will be effective. If we are talking about eye drops, the doctor may prescribe the use of “Atropine”, “Cycloptic”, “Tropicamide”.

Overdose information

What happens if too much of a drug such as phenylephrine hydrochloride enters the body? The instructions contain information that overdose is rarely recorded.

As a rule, patients in such cases complain of a feeling of heaviness in the head and limbs. Sometimes there is a sharp increase in blood pressure. Possible complications include ventricular tachycardia and extrasystole. In case of overdose, intravenous administration of beta and alpha adrenergic blockers is indicated.

Interaction with other drugs

You already know in what cases it is advisable to take phenylephrine hydrochloride, what it is and in what forms it is available. But it is worth remembering that during a medical examination it is important to tell the specialist about all the medications you are taking.

Simultaneous use of this drug with other adrenergic blockers, as well as Furosemide and other diuretics, can lead to a weakening of the vasoconstrictor effect.

The combination of this drug with cyclopropane, halothane and other anesthetics sometimes leads to the development of ventricular fibrillation.

Phenylephrine is also not recommended to be taken together with MAO inhibitors - at least three weeks should pass between courses. You should not combine this medicine with reserpine, as there is a risk of developing severe arterial hypertension.

Of course, this remedy is widely used in modern medicine - sometimes its use is simply vital. However, improper use is dangerous, so you should not self-medicate. Only the attending physician can draw up the correct treatment regimen.

Formula: C16H20N2, chemical name: N,N-dimethyl-3-phenyl-3-pyridin-2-yl-propan-1-amine.
Pharmacological group: intermediates/ histaminergic agents/ histaminolytics/ H1-antihistamines.
Pharmachologic effect: antiallergic.

Pharmacological properties

Pheniramine is a histamine H1 receptor blocker. Pheniramine reduces exudation and has an antiallergic effect. After oral administration, the effects occur within one hour and last up to a day. When taken orally, the maximum plasma concentration in the blood is achieved after 1 - 2.5 hours. The terminal half-life is 16 - 19 hours. Pheniramine is 70-83% excreted in the urine in the form of metabolites and unchanged.

Indications

Hay fever (hay fever), allergic conjunctivitis, rhinitis; skin itching of various origins; neurodermatitis; urticaria, Quincke's edema, insect bites, 1st degree thermal burns, drug dermatitis; general malaise during radiation therapy.

Method of administration of pheniramine and dose

The dosage regimen for pheniramine is individual. Pheniramine is taken orally after meals and administered intramuscularly. For oral administration, the average single dose for adults is 25 mg, the frequency of administration is 2 - 3 times a day. The maximum daily dose is 3 mg/kg. For intramuscular administration, the average single dose for adults is 45.5 mg, the frequency of administration is 1 - 2 times a day. Average single doses for children are established depending on age.
During outpatient treatment, it is necessary to take into account a possible decrease in the speed of psychomotor reactions. During therapy, observation by an ophthalmologist is necessary.

Contraindications for use

Angle-closure glaucoma, prostatic hypertrophy, hypersensitivity.

Restrictions on use

No data.

Use during pregnancy and breastfeeding

During pregnancy (especially in the 1st trimester) and during lactation, pheniramine is used only when prescribed by a doctor according to strict indications.

Side effects of pheniramine

Feeling of fatigue, decreased speed of psychomotor reactions, drowsiness, dyspeptic symptoms, dry mouth, tachycardia, allergic reactions, urinary retention, dermatitis, increased intraocular pressure in patients with closed-angle glaucoma, agitation, anxiety, confusion, hallucinations.

Interaction of pheniramine with other substances

When pheniramine is used together with monoamine oxidase inhibitors, alcohol, sleeping pills, and tranquilizers, the inhibitory effect on the central nervous system may be enhanced.

Overdose

No data.

Trade names of drugs with the active ingredient pheniramine

Combined drugs:

Paracetamol + Phenylephrine + Pheniramine + Ascorbic acid: GrippoFlu for colds and flu, GrippoFlu extra for colds and flu, Zvezdochka Flu, Influnorm, Maxicold Rhino, Stopgripan, Stopgripan forte, TeraFlu® for flu and colds;
Caffeine + Paracetamol + Phenylephrine + Pheniramine: Rinzasip, Rinicold HotMix;
Paracetamol + Phenylephrine + Pheniramine: TeraFlu®, TeraFlu® for flu and colds Extra, TeraFlu® Extra, Flucomp;
Paracetamol + Pheniramine + Ascorbic acid: Fastoric, Febricet, Fervex, Fervex for children, Flukoldin;
Naphazoline + Pheniramine: Opcon-A®;
Caffeine + Paracetamol + Phenylephrine + Pheniramine + [Ascorbic Acid]: Rinzasip with Vitamin C;
Drotaverine + Caffeine + Naproxen + Paracetamol + Pheniramine maleate.

Included in the preparations

ATX:

N.02.B.E Anilides

N.02.B.E.51 Paracetamol in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Combined drug.

It has analgesic, antipyretic, antihistamine, vasoconstrictor, sedative, bronchodilator and antitussive effects.

Paracetamol

It has antipyretic, analgesic and anti-inflammatory effects. Inhibits cyclooxygenase, mainly in the central nervous system, affects the centers of pain and thermoregulation. It does not have a negative effect on water-salt metabolism and the mucous membranes of the gastrointestinal tract, and therefore has a slight effect on the synthesis of prostaglandins in peripheral tissues.

Phenylephrine

α 1-adrenergic agonist causes constriction of arterioles and reduces vascular permeability of the nasal mucosa, reduces swelling, facilitates breathing, reduces rhinorrhea and lacrimation. Causes pupil dilation without affecting accommodation, lowers intraocular pressure in glaucoma.

Pheniramine

The H1 receptor blocker has antihistamine, antiserotonin, anticholinergic, and sedative effects. Constricts the vessels of the nasal cavity, suppresses the symptoms of allergic rhinitis: rhinorrhea, sneezing, itching of the nose and eyes.

Ascorbic acid

Regulates the processes of transport of hydrogen ions in redox reactions, being involved in the process at any stage of the Krebs cycle. Participates in the regulation of carbohydrate metabolism. Ensures the absorption of iron in the intestine, converting it from trivalent to divalent form, facilitating its inclusion in heme. Participates in the formation of tetrahydrofolic acid, the synthesis of steroid hormones, norepinephrine and adrenaline, collagen, prothrombin, glycogen. Inactivates hyauuronidase, activating tissue regeneration and normalizing capillary permeability. Neutralizes toxins and has an antioxidant effect by trapping free radicals. Takes an active part in the regulation of immune processes: enhances the formation of antibodies, phagocytic activity and interferon synthesis. Inhibits the release of histamine and enhances its degeneration, suppresses the release of inflammatory mediators and allergic reactions.

Extends the effect of paracetamol by slowing its elimination and improves its tolerability.

Pharmacokinetics:

Paracetamol

After oral administration, it is completely absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is achieved after 20-30 minutes. Plasma protein binding is 15%. Penetrates the blood-brain barrier and enters breast milk.

Metabolism in the liver by glucuronidation and sulfation (80%) with the formation of inactive metabolites, about 17% undergoes hydroxylation to active metabolites, which are subsequently deactivated after conjugation with sulfates and glutathione. With a lack of glutathione, these metabolites block liver enzyme systems, causing necrosis of hepatocytes.

The half-life is 2-3 hours. Elimination by the kidneys, about 3% unchanged.

Phenylephrine

After oral administration, up to 30% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 3 hours. The binding to plasma proteins is 70%. Penetrates the blood-brain barrier.

Metabolism in the liver.

Pheniramine

After oral administration, up to 30% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2.5 hours. The connection with plasma proteins is 70%. The therapeutic effect develops 1 hour after administration and continues for 24 hours. Penetrates the blood-brain barrier.

Metabolism in the liver.

The half-life is 2 hours. Elimination by the kidneys.

Ascorbic acid

Completely absorbed from the gastrointestinal tract after oral administration. Plasma protein binding is 25%. The normal concentration of ascorbic acid in the blood is 15-20 mcg/ml. The concentration of ascorbic acid in erythrocytes and blood plasma is lower than in platelets and leukocytes.

Ascorbic acid is oxidized to dehydroascorbic acid, metabolized to inactive ascorbate-2-sulfate and oxalic acid, then excreted in the urine. In cases where the dose is exceeded (over 200 mg), it is eliminated unchanged by the kidneys.

Indications:

Used to treat influenza and colds accompanied by headache, fever, and rhinitis. Used for allergic rhinitis.

X.J10-J18.J11 Flu, virus not identified

X.J20-J22.J22 Acute lower respiratory tract respiratory infection, unspecified

X.J30-J39.J39 Other upper respiratory tract diseases

Contraindications:Bleeding in the gastrointestinal tract, phenylketonuria, glucose-6-phosphate dehydrogenase deficiency, portal hypertension, anemia, leukopenia, thrombocytopenia, individual intolerance. Carefully:

Gilbert's syndrome, viral hepatitis, old age, alcoholism.

Pregnancy and lactation: Directions for use and dosage:

Inside 1 sachet 4 times a day.

Highest daily dose: 4 sachets.

Highest single dose: 1 sachet.

Side effects:

Central and peripheral nervous system: weakness, drowsiness, hallucinations, impaired coordination of movements.

Hematopoietic system: rarely aplastic anemia, pancytopenia.

Digestive system: dry mouth, constipation.

Dermatological reactions: exfoliative dermatitis.

Sense organs: diplopia.

Urinary system: difficulty urinating.

Allergic reactions.

Overdose:

Necrosis of liver cells due to the formation of a toxic metabolite of acetaminophen - N-acetyl-p-benzoquinoneimine.

Symptoms: nausea, vomiting, pallor of the skin, hepatonecrosis, tubular necrosis.

Treatment: use of donors SH -groups, precursors for the synthesis of glutathione - methionine and N -acetylcysteine ​​within 12 hours after an overdose.

Interaction:

Enhances the effect of indirect coagulants and the toxicity of chloramphenicol.

Taking ethanol during treatment with the drug leads to the development of acute pancreatitis.

Simultaneous use with stimulants of microsomal oxidation in the liver - barbiturates, rifampicin, ethanol, phenylbutazone, phenythionine, increases the toxicity of paracetamol.

Microsomal oxidation inhibitors () with reduce the risk of hepatotoxicity.

Special instructions:

Monitoring the content of glucose and uric acid in plasma, the composition of peripheral blood, and the functional state of the liver.

Instructions