Acetylcysteine
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Pharmacological properties
n-acetylcysteine has a mucolytic effect. the presence of sulfhydryl groups in the structure of acetylcysteine helps to break the disulfide bonds of acid mucopolysaccharides of sputum, which leads to the depolarization of mucoproteins and to a decrease in the viscosity of mucus. the drug remains active in the presence of purulent sputum.
Moreover, acetylcysteine has a direct antioxidant effect due to the presence of a free thiol (-SH) nucleophilic group, which easily interacts with the electrophilic groups of oxidizing radicals. In particular, current evidence that acetylcysteine protects the α-antitrypsin protein that inhibits elastase from destruction by perchloric acid, a pronounced oxidizing agent that is produced by the myeloperoxidase protein of activated phagocytes, is of interest.
Therefore, acetylcysteine can be used to treat patients with acute and chronic diseases of the respiratory system, accompanied by thick and viscous secretion.
Due to its molecular structure, acetylcysteine can easily penetrate cell membranes. Inside the cell, acetylcysteine is deacylated to L-cysteine, an amino acid that is necessary for the synthesis of glutathione.
Glutathione is a highly reactive tripeptide, which is a pronounced factor in intracellular protection not only from oxidative toxins of both exogenous and endogenous origin, but also from a number of cytotoxic substances.
Pharmacokinetics Acetylcysteine is completely absorbed by oral administration. Due to the metabolism in the intestinal walls and the effect of the first passage, the bioavailability of acetylcysteine when taken orally is very low (≈10%). Cmax in plasma reached 1-3 hours after administration and remains high for 24 hours. Acetylcysteine is distributed both unchanged (20%) and metabolites (80%), mainly distributed in the liver, kidneys, lungs and bronchial a secret.
The volume of distribution of acetylcysteine is from 0.33 to 0.47 l / kg body weight. Communication with proteins is ≈50% 4 hours after ingestion and decreases to 20% after 12 hours.
Acetylcysteine after oral administration is rapidly metabolized in the walls of the intestines and liver.
About 30% is excreted by the kidneys. T½ acetylcysteine is 6.25 hours
Indications
A mucolytic agent for the treatment of acute and chronic diseases of the bronchopulmonary system, accompanied by increased sputum formation.
Application
200 mg tablets
Adults:
400-600 mg / day in 2-3 doses, depending on the clinical conditions.
Children aged:
2–6 years - 200–400 mg / day in 1–2 doses;
6–12 years - 400–600 mg / day in 2–3 doses, depending on the clinical conditions.
12 years - doses for adults.
The doctor determines the duration of the course of treatment individually, depending on the nature of the disease (acute or chronic).
Caution for patients on a sodium-restricted diet: Each effervescent tablet contains 191 mg of sodium.
600 mg tablets
Adults and children over the age of 14 years - 1 effervescent tablet 1 time per day (equivalent to 600 mg of acetylcysteine per day).
Caution for patients on a low sodium diet: Each effervescent tablet contains 150 mg of sodium.
In acute uncomplicated diseases, the drug is used for no more than 4-5 days without medical supervision.
The period of treatment of chronic diseases is determined by the doctor. The drug is recommended to be taken after meals. Effervescent tablets are dissolved in ½ cup of water, juice or iced tea. When dissolving acetylcysteine, it is necessary to use glassware, avoid contact with metal and rubber surfaces. Do not mix this solution with other drugs.To enhance the mucolytic effect of acetylcysteine, additional fluid intake is recommended.
Contraindications
Hypersensitivity to the active substance or to any of the excipients. stomach and duodenal ulcer in the acute stage, hemoptysis, pulmonary hemorrhage.
Side effects
On the part of the immune system: hypersensitivity reactions, anaphylactoid reactions, anaphylactic shock, Quincke edema.
From the nervous system: headache.
On the part of the organ of hearing: ringing in the ears.
From the cardiovascular system: tachycardia.
Vascular disorders: hemorrhages.
From the respiratory system: bronchospasm, shortness of breath.
From the digestive system: stomatitis, abdominal pain, nausea, vomiting, diarrhea, dyspepsia.
From the skin and its appendages: urticaria, rash, angioedema, itching.
General disorders: hyperthermia, facial edema.
Research results: lowering blood pressure.
Very rarely reported cases of anemia. In rare cases, skin reactions are possible, such as Stevens-Johnson syndrome, Lyell syndrome.
There have been cases of decreased platelet aggregation, but the clinical significance of this has not been determined.
special instructions
Patients with BA require strict monitoring during treatment due to the possible development of bronchospasm. in case of bronchospasm, treatment with acetylcysteine should be stopped immediately. it is recommended to use the drug with caution in patients with a history of gastric and duodenal ulcers, especially in the case of concomitant use of other drugs that irritate the gastric mucosa.
The use of acetylcysteine, mainly at the beginning of treatment, can cause thinning of the bronchial secretion and increase its volume. If the patient is not able to cough up sputum effectively, postural drainage and broncho-aspiration are necessary. A slight sulfuric smell is not a sign of a change in the drug, but is specific to the active substance. It is necessary to take into account the sodium content in patients who follow a diet with sodium intake control.
The drug contains sorbitol. If the patient is intolerant of certain sugars, a doctors consultation is required before taking this drug.
Use during pregnancy and lactation. During pregnancy and lactation, the use of acetylcysteine is possible only if the expected benefits to the mother outweigh the potential risk to the fetus / baby.
Children. 200 mg tablets are used in children aged 2 years and over. 600 mg tablets are used in children over the age of 14.
The ability to influence the reaction rate when driving vehicles or working with other mechanisms. No data.
Interactions
The use of antitussive agents simultaneously with acetylcysteine can increase sputum congestion due to suppression of the cough reflex.
When used simultaneously with antibiotics such as tetracyclines (with the exception of doxycycline), ampicillin, amphotericin B, their interaction with the thiol group of acetylcysteine is possible, which leads to a decrease in the activity of both drugs. Therefore, the interval between the use of these drugs should be at least 2 hours.
The simultaneous use of acetylcysteine and nitroglycerin can lead to increased vasodilator and disaggregant effects of the latter.
Activated carbon reduces the effectiveness of acetylcysteine.
Dissolution in one glass of acetylcysteine with other drugs is not recommended. Acetylcysteine reduces the severity of the toxic effect of paracetamol.
Influence on laboratory research. Acetylcysteine can affect the colorimetric studies of salicylates and the determination of urates and ketone bodies.
Overdose
There are no data on cases of overdose of dosage forms of acetylcysteine intended for oral administration.
Acetylcysteine when taken at a dose of 500 mg / kg / day does not cause signs and symptoms of an overdose.
Symptoms Overdosing can occur with gastrointestinal symptoms such as nausea, vomiting, and diarrhea.
Treatment. There is no specific antidote for acetylcysteine poisoning, symptomatic therapy.
Storage conditions
Protected from light at a temperature not exceeding 25 ° C.
137 Items
2020-07-30
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