Lecadol plus C

Lekadol plus C belongs to the category of drugs with analgesic and antipyretic effects.

Indications Lecadol plus C

It is used to eliminate the symptoms of flu or colds – headaches, sore throats, fever and pain in the joints and muscles.

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Release form

The medicinal product is released in granules for the production of oral liquid; 5 g of the substance inside the sachet. The pack contains 10 or 20 such sachets.

Pharmacodynamics

Lekadol Plus C is a complex product that contains vitamin C and paracetamol.

Paracetamol is an effective antipyretic and analgesic. It inhibits the binding of PG inside the central nervous system, helps to relieve pain and reduce elevated temperature. Compared to NSAIDs, it does not have a negative effect on the gastrointestinal tract, which allows it to be used for gastric diseases and ulcers in the gastrointestinal tract, which are present in the anamnesis.

The drug should be prescribed to people who cannot use aspirin. The anti-inflammatory activity of paracetamol is quite weak and has no clinical significance.

Ascorbic acid is an essential element required for the stable functioning of many body systems. It is a cofactor for a large number of enzymatic processes, prevents cell destruction under the influence 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 the integrity of the vascular endothelium.

The increased need for ascorbic acid in cases of inflammation, fever or pregnancy is caused by the main antioxidant effect of the substance – a decrease in the number of free radicals. Preclinical tests have shown that this vitamin demonstrates immunomodulatory activity in relation to non-specific and humoral immunity during inflammation.

Pharmacokinetics

Paracetamol is almost completely and rapidly absorbed in the gastrointestinal tract, reaching Cmax values in plasma after 0.5-1 hour from the moment of administration. The level of bioavailability of the substance is 88±15%. The half-life is within 2±0.4 hours.

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

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

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

After oral administration of ascorbic acid, it is absorbed at high speed from the upper part of the small intestine. The Cmax values of the substance in the blood serum are noted after 2-3 hours from the moment of consumption. The stable serum level of the drug is 10 mg/l.

The component penetrates the placenta and is excreted with mother's milk. Metabolic processes lead to the formation of oxalic and dehydroascorbic acids, and also, partially, 2-sulfate-ascorbic acid.

The half-life of the element is approximately 10 hours. 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

The drug should be taken orally, 1 packet of granules 4-6 times a day. A maximum of 6 packets can be taken per day. The interval between doses should be at least 4 hours.

The duration of therapy is selected individually, taking into account the course of the disease and personal tolerance of the medication (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 hot (but it should not be boiling) water or tea (0.2 l) over them and stir until the substance is completely dissolved. The liquid should be drunk warm, so the medicine should be prepared immediately before taking it.

Eating food may reduce the absorption of Lekadol.

People with impaired kidney or liver function, as well as people with Gilbert's disease, need to take small doses of the medication (or at long intervals).

Because hemodialysis reduces blood levels of paracetamol, the patient is required to receive an additional dose of this substance after dialysis procedures.

Use Lecadol plus C during pregnancy

It is prohibited to use Lekadol Plus C in the 1st trimester. In the 2nd and 3rd trimesters, use is allowed only with the permission of a doctor. Pregnant women should use the medicine for a minimum period of time in personally prescribed doses, in situations where the probable benefit is more expected than the risk of negative signs in the fetus.

Paracetamol can be excreted in breast milk, which is why breastfeeding should be discontinued while taking the medicine.

Contraindications

Main contraindications:

• severe intolerance associated with paracetamol, vitamin C or other components of the medication;
• severe liver failure (>9 points according to the Child-Pugh classification);
• severe renal failure;
• people with a deficiency of the enzyme G6PD, for whom the use of vitamin C in high doses can lead to the development of hemolysis (sometimes hemolysis can also occur when taking paracetamol);
• jaundice;
• phenylketonuria (because the drug contains aspartame, which is the source of the component phenylalanine);
• hyperoxalaturia;
• the presence of oxalate stones inside the kidneys;
• urolithiasis, in cases where the daily dose of vitamin C is more than 1 g.

Side effects Lecadol plus C

Side effects include:

• blood disorders: hemolytic anemia occasionally occurs. Leukopenia, pancyto- or thrombocytopenia, as well as agranulocytosis, may occasionally occur. Hemolysis may occur in people with a deficiency of the G6PD component, as well as the progression of scurvy when high doses of vitamin C are administered;
• immune disorders: occasionally, signs of allergy (rash, asthma attack, itching, urticaria or erythema) are observed, in which case it is necessary to stop taking the drug and perform procedures aimed at eliminating anaphylactic manifestations. Dyspnea, nausea, Quincke's edema, hyperhidrosis, decreased blood pressure and bronchial spasm in predisposed individuals (analgesic-associated asthma) occur sporadically;
• disorders of the hepatobiliary system: jaundice occasionally develops or the activity of liver transaminases increases. Liver intoxication is observed sporadically (due to the use of too large doses or prolonged use of drugs);
• problems with urination: when very large doses of vitamin C are administered, hyperoxaluria or kidney stones may develop. A toxic form of nephropathy of an analgesic nature (due to the use of large doses of drugs) is occasionally observed. When using doses of vitamin C exceeding 0.6 g, a moderate increase in diuresis is possible;
• metabolic disorders: EBV disorder or suppression of cobalamin activity may develop;
• disorders of the nervous system: insomnia or headaches may occur;
• lesions affecting the vascular system: flushing of the skin on the face may be observed;
• digestive dysfunction: vomiting, diarrhea, heartburn and nausea may develop, as well as pain in the epigastric region.

Overdose

Drug poisoning most often occurs in children, the elderly, people with liver disease, and also in cases of poor nutrition, chronic alcoholism, and the combined use of drugs that induce liver enzymes.

The toxic activity of paracetamol can develop both with a single overdose and in the case of using repeated doses (6-10 g per day over a 1-2-day period).

Paracetamol intoxication results in the formation of a large amount of the 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 acidosis of a metabolic nature can provoke a comatose state and death.

When taking large doses of the drug, during the first 12-24 hours a feeling of drowsiness, vomiting, hyperhidrosis and nausea may occur. After 12-48 hours from the moment of poisoning, the activity of liver transaminases (ALT together with AST), bilirubin and lactate dehydrogenase increases; in addition, the PTT index increases.

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

Symptoms such as jaundice, loss of appetite, and gastrointestinal bleeding may occur after a 3-day period. Liver necrosis, the severity of which depends on the dosage of the drug, is a severe toxic reaction caused by paracetamol poisoning.

Clinical signs of hepatotoxicity become most pronounced after 4-6 days. Even if severe hepatotoxicity does not develop, paracetamol poisoning can provoke acute renal failure, accompanied by acute tubular necrosis.

Paracetamol intoxication causes pancreatitis and myocardial disorders.

Large amounts 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 doses of vitamin C lead to the development of hemolysis.

The victim must be hospitalized immediately. In case of recent drug use, vomiting should be induced, gastric lavage should be performed (during the first 6 hours), and activated carbon should be given to the patient. Symptomatic measures are taken.

Methionine with N-acetylcysteine is used as an antidote for paracetamol poisoning. Acetylcysteine is administered intravenously. At first (within the first 8 hours), 0.15 g/kg of the substance (20% liquid in 0.2 l of 5% glucose solution) should be administered intravenously. The duration of the infusion is 15 minutes.

Intravenous procedures should be continued - 50 mg/kg acetylcysteine should be administered at 4-hour intervals (in 0.5 l of 5% glucose), and later at 0.1 g/kg, at 16-hour intervals. After 12 hours, oral acetylcysteine can be started. Continued use of acetylcysteine provides 48-hour protection.

A significant amount of paracetamol in the form 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 drugs that induce liver microsomal enzymes (including phenytoin with rifampicin and phenobarbital with carbamazepine) increases the likelihood of liver damage due to an increase in the number of paracetamol metabolic products formed inside the liver.

The risk of hepatotoxicity increases with the combination of paracetamol and isoniazid. In such cases, it is necessary to limit the use of the drug.

Simultaneous use of Lekadol Plus C and anticoagulants may enhance their properties. In individuals using the medication (over 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 PT values.

Paracetamol can prolong the half-life of chloramphenicol, thereby increasing the toxicity of the latter.

The combination of the drug with zidovudine causes granulocytopenia, which is why they can be taken together only with the permission of the attending physician.

The combined use of drugs with cholestyramine weakens the absorption of paracetamol (the patient should take the drug 1 hour before or 3 hours after taking cholestyramine).

Domperidone with metoclopramide enhances the absorption of paracetamol.

The absorption of paracetamol in the gastrointestinal tract is slowed down when the drug is combined with anticholinergic substances (for example, propantheline) or activated carbon.

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

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

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

Long-term combination of the drug with aspirin or other antipyretics and analgesics is prohibited, because this increases the likelihood of nephropathy and medullary renal necrosis.

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

Salicylamide prolongs the half-life of paracetamol.

In people with alcoholism and people who consume ethyl alcohol in large quantities, when combined with the drug, the likelihood of liver damage and bleeding inside the stomach increases.

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

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

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

Vitamin C is able to reduce plasma levels of propranolol because it affects its absorption and first-pass intrahepatic metabolic processes.

Combination with NSAIDs leads to potentiation of its main effect and side effects.

Storage conditions

Lekadol plus C should be stored in a place closed to small children. Temperature values - within the mark of 25 ° C.

Shelf life

Lekadol plus C can be used for a period of 3 years from the date of release of the pharmaceutical substance.

Application for children

The drug is prohibited for use in pediatrics (under 12 years of age).

Analogues

The analogs of the drug are the drugs Caffetin, Paracetamol, Panadol with Cefekon D, and also Efferalgan, Antigrippin and Teraflu.

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