Lekadol plus C

Lekadol plus enters the category of drugs with analgesic and antipyretic effects.

Indications Lekadola plus C

It is used to eliminate signs of flu or cold - headaches, sore throats, fever and pain that appear in the joints with muscles.

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Release form

The release of the drug produced in granules for the manufacture of oral liquid; 5 g of substance inside the bag. The pack contains 10 or 20 such bags.

Pharmacodynamics

Lekadol plus c is a complex remedy that contains vitamin C with paracetamol.

Paracetamol is an effective antipyretic and analgesic agent. It inhibits PG binding within the central nervous system, helps relieve pain and reduce fever. If we compare it with NSAIDs, it does not have a negative impact on the gastrointestinal tract, which allows it to be used in gastric diseases and ulcers in the gastrointestinal tract, available in history.

The drug should be prescribed to people who can not use aspirin. Anti-inflammatory activity of paracetamol is quite weak and does not have clinical significance.

Ascorbic acid is a necessary element required for the stable operation of a variety of body systems. It is a cofactor of a large number of enzyme processes, prevents the destruction of cells under the action of oxidation processes (antioxidant properties), increases the degree of intestinal absorption of iron, is a participant in the formation of collagen (connective tissue necessary for cartilage, bones and epidermis), and at the same time maintains vascular integrity endothelium.

The increase in the need for receiving ascorbic acid in the case of inflammation, fever or during pregnancy is caused by the main antioxidant effect of the substance - a decrease in the number of free radicals. In preclinical tests, it turned out that this vitamin demonstrates immunomodulating activity with respect to nonspecific and humoral immunity during inflammation.

Pharmacokinetics

Paracetamol is almost completely absorbed at high speed inside the gastrointestinal tract, reaching Cmax values inside the plasma after 0.5-1 hour from the moment of administration. The level of bioavailability of the substance is 88 ± 15%. Half-life is 2 ± 0.4 hours.

Intraplasmic drug values of paracetamol are 10-20 μg / ml; the size of the toxic concentration of a substance is more than 300 μg / ml. Intlasma synthesis with protein is 10-30%.

Paracetamol is able to penetrate the BBB and the placenta, as well as excreted with mother's milk. The main part of the element undergoes metabolic processes in which glucuronic acid with conjugates (60%), as well as sulfate (30%) and cysteine (3%) are formed.

Over 85% of the component is excreted with the urine in the form of metabolic products over a 24-hour period, and only 1% is excreted unchanged. A small amount of the element is excreted in the bile.

After ingestion of ascorbic acid, it is absorbed at high speed from the upper region of the small intestine. Indicators Cmax substances inside the blood serum are observed after 2-3 hours from the time of use. The stable serum drug level is 10 mg / l.

The component penetrates the placenta and is excreted in the mother’s milk. The exchange processes lead to the formation of oxalic and dehydroascorbic acids, and in addition, partially - 2-sulfate-ascorbic acid.

The half-life of an element is approximately 10 hours. The elimination of all metabolic products of the vitamin occurs through the kidneys.

Both components do not affect the degree of absorption of each other.

Dosing and administration

You need to take the drug orally, on the first bag of granules 4-6 times a day. Per day is allowed to receive a maximum of 6 bags. The interval between use should be at least 4 hours.

The duration of therapy is chosen individually, taking into account the course of the disease and the personal tolerance of the drug (but it should not last more than 5 days).

It is necessary to pour the granules from the bag into a glass or cup, then pour them hot (but it should not be boiling) with water or tea (0.2 l) and stir until the substance is completely dissolved. Drink the liquid should be warm, so the medicine should be prepared immediately before taking it.

Eating can reduce the severity of absorption of Lekadol.

Persons with impaired kidney or liver function, as well as people with Gilbert's disease, should use small portions of the medication (or over large periods of time).

Because hemodialysis reduces the blood parameters of paracetamol, after dialysis procedures, the patient is required to additionally introduce a portion of this substance.

Use Lekadola plus C during pregnancy

It is forbidden to use Lekadol Plus C in the 1st trimester. On the 2nd and 3rd trimesters, use is allowed only with the permission of the doctor. Pregnant women should use the medication for a minimum period of time in personalized portions, in situations where the likely benefits are more expected than the risk of negative symptoms in the fetus.

Paracetamol is able to stand out with mother's milk, which is why it is necessary to refuse breastfeeding at the time of drug intake.

Contraindications

The main contraindications:

• severe intolerance associated with paracetamol, C-vitamin or other elements of the drug;
• lack of liver function in the severe stage (> 9 points in accordance with the Child-Pugh classification);
• lack of work of the kidneys in severe form;
• people with a deficiency of the G6PD enzyme, in whom the use of C-vitamin in high portions can lead to the development of hemolysis (sometimes hemolysis can also occur with the introduction of paracetamol);
• jaundice;
• phenylketonuria (because as part of the drug has aspartame, which is the source of the component phenylalanine);
• giperoxalatrium;
• the presence of oxalate stones inside the kidneys;
• urolithiasis, in cases where the daily portion of C-vitamin is more than 1 g. 

Side effects Lekadola plus C

Among the side effects are:

• blood disorders: occasionally anemia of a hemolytic nature occurs. Leuko-, pancyto- or thrombocytopenia, as well as agranulocytosis, appears singly. Hemolysis may occur in people with a deficiency of the G6PD component, as well as the progression of the development of scurvy with the introduction of high portions of C-vitamin;
• immune lesions: rarely there are signs of allergies (rash, asthma attack, itching, urticaria, or erythema), in which you need to cancel the medication and perform procedures aimed at eliminating anaphylactic manifestations. Dyspnea, nausea, angioedema, hyperhidrosis, a decrease in blood pressure and bronchial spasm in individuals with a predisposition (associated with analgesics, asthma);
• disorders of the hepatobiliary system: jaundice rarely develops or the activity of hepatic transaminases increases. Liver intoxication is rarely observed (due to the use of too large portions or prolonged use of drugs);
• problems with urinary activity: the introduction of very large portions of C-vitamin may cause hyperoxalaturia or the formation of kidney stones. The toxic form of nephropathy, which has an analgesic nature (due to the use of large dosages of drugs), is singled out individually. In the case of the use of portions exceeding 0.6 g of C-vitamin, a moderate increase in diuresis is possible;
• metabolic disorders: a violation of VEB or suppression of cobalamin activity may develop;
• NS abnormalities: insomnia or headaches may occur;
• lesions affecting the vascular system: there may be a surge of blood to the skin on the face;
• digestive disorders: vomiting, diarrhea, heartburn and nausea, as well as epigastric pain.

Overdose

Drug poisoning often occurs in children, the elderly, people with hepatic diseases, and in addition with poor nutrition, alcoholism, having a chronic nature, and the combined use of drugs that induce hepatic enzymes.

Toxic activity of paracetamol can develop with a single overdose, and in the case of repeated doses (6-10 g per day in a 1-2-day period).

Paracetamol intoxication leads to the formation of a large number of toxic metabolic product N-acetyl-para-benzoquinone imine, synthesized with sulfhydryl subgroups of liver cells, which leads to their damage. The occurrence of encephalopathy with metabolic acidosis can provoke a comatose condition and death.

When taking large portions of drugs, during the first 12-24 hours a feeling of drowsiness, vomiting, hyperhidrosis and nausea may appear. After a 12-48-hour period from the moment of poisoning, the activity of hepatic transaminases (ALT together with ACT), bilirubin and lactate dehydrogenase increases; in addition, the PTV rate rises.

After 2 days from the moment of intoxication, pain may occur in the abdominal area, which is the first sign of liver damage.

Manifestations such as jaundice, loss of appetite and bleeding inside the gastrointestinal tract can occur after a 3-day period. Hepatic necrosis, the severity of which depends on the size of the dosage of the drug, is a severe toxic reaction caused by paracetamol poisoning.

Clinical signs of hepatotoxicity acquire maximum severity after 4-6 days. Even if the severe stage of hepatotoxicity does not develop, paracetamol poisoning can provoke acute renal failure, accompanied by acute tubular necrosis.

Paracetamol intoxication causes pancreatitis and myocardial disorders.

Large portions of ascorbic acid lead to the formation of kidney stones, diarrhea and inflammation of the gastric mucosa.

In people with a deficiency of the G6PD component, large dosages of C-vitamin lead to the development of hemolysis.

The victim must be hospitalized immediately. With the recent use of drugs should induce vomiting, perform gastric lavage (during the first 6 hours), and also give the patient activated charcoal. Symptomatic interventions are carried out.

Methionine with N-acetylcysteine is used as an antidote for paracetamol poisoning. Acetylcysteine is introduced in / in the method. First (the interval of the first 8 hours) it is necessary to inject intravenously at 0.15 g / kg of the substance (20% liquid in a 0.2 liter of a 5% glucose solution). The duration of the infusion is 15 minutes.

Intravenous procedures should be continued — 50 mg / kg of acetylcysteine should be administered at 4-hour intervals (0.5 l of 5% glucose), and later at 0.1 g / kg, with a 16-hour interval. After 12 hours thereafter, it is allowed to start acetylcysteine orally. Prolonged use of acetylcysteine allows for 48-hour protection.

A significant amount of paracetamol under the guise of sulfate with glucuronide is excreted from the blood plasma through hemodialysis.

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Interactions with other drugs

The combination of the drug with microsome hepatic enzyme inducer drugs (phenytoin with rifampicin and phenobarbital with carbamazepine among them) increases the likelihood of hepatic damage due to the increase in the number of metabolic products of paracetamol formed inside the liver.

The likelihood of hepatotoxicity increases with the combination of paracetamol and isoniazid. With such a violation is required to limit the use of drugs.

The simultaneous use of Lekadola Plus C and anticoagulants can enhance their properties. For persons using the medication (more than 2 g of paracetamol daily) with anticoagulants (warfarin with other coumarins), over a long period of time (more than 7 days), it is necessary to monitor the values of PTV.

Paracetamol can prolong the half-life of chloramphenicol, as a result of which the toxicity of the latter is enhanced.

The combination of medication with zidovudine causes the appearance of granulocytopenia, because of which they can be taken together only with the permission of the treating doctor.

The combined administration of drugs with Kolestiramin weakens the absorption of paracetamol (the patient must use the drug 1 hour before or after 3 hours after using Kolestiramine).

Domperidone with metoclopramide increase the absorption of paracetamol.

Absorption of paracetamol inside the gastrointestinal tract is slowed down in the case of a combination of a drug with anticholinergic substances (for example, propanthelin) or activated carbon.

Probenecid reduces the rate of hepatic metabolism of paracetamol, which reduces its clearance. Combining the drug with probenecid requires a lower dosage.

The combination of the drug and ciprofloxacin causes a delay in the activity of exposure to paracetamol.

Introduction together with a granisetron or tropisetron completely blocks the analgesic effect of Lekadol.

Prolonged combination of the drug with aspirin or other antipyretic drugs and analgesics is prohibited, because it increases the likelihood of nephropathy and renal necrosis of a medullary nature.

The combination of the drug with nephrotoxic agents increases the likelihood of acute tubular necrosis.

Salicylamide prolongs the half-life of paracetamol.

In individuals with alcoholism and people taking ethyl alcohol in large quantities, when combined with the drug increases the likelihood of hepatic lesions and bleeding inside the stomach.

Use with substances containing Fe, leads to the fact that under the influence of ascorbic acid increases the absorption of iron and increases its toxicity relative to tissues.

The introduction of large portions of C-vitamin reduces the absorption of warfarin inside the gastrointestinal tract, and also reduces the glomerular reabsorption of alkaline drugs of a specific nature (tricyclics or amphetamine).

The combined use of high dosages of ascorbic acid with estrogens (ethinyl estradiol) can cause an increase in the plasma values of the latter.

C-vitamin is able to reduce plasma indicators of propranolol, because it affects its absorption and intrahepatic metabolic processes of the 1st passage.

Combination with NSAIDs leads to a potentiation of its main effect and adverse symptoms.

Storage conditions

Lekadol plus C is required to be kept in a place closed from the penetration of small children. Temperature values - within the mark of 25 ° C.

Shelf life

Lekadol plus C can be used for a 3-year period from the moment of release of the pharmaceutical substance.

Application for children

It is forbidden to use the medicine in pediatrics (younger than 12 years of age).

Analogs

Analogues of the drug are drugs Caffetine, Paracetamol, Panadol with Cefecone D, and besides this Efferalgan, Antigrippin and Theraflu.

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