DesGrippin effervescent pills 500mg+10mg+200mg lime flavor, 10pcs

Composition

Active ingredients:  paracetamol-500.0 mg; chlorphenamine maleate-10.0 mg;ascorbic acid-200.0 mg. Auxiliary substances:  aspartame-30.9 mg; acesulfame potassium-30.9 mg; povidone K-30-31.5 mg; colloidal silicon dioxide-20.6 mg; lactose monohydrate-4126.1 mg; Lemon-lime or Lemon-honey flavor (lemon and honey flavors in the ratio of 1: 1) either Raspberries or Cranberries – 50.0 mg

Pharmacological action

Combined drug.

Pharmacodynamics

Paracetamol has analgesic and antipyretic effects; eliminates headaches and other types of pain, reduces fever.

Chlorphenamine is a blocker of H1-histamine receptors, has an anti-allergic effect, facilitates breathing through the nose, reduces nasal congestion, sneezing, lacrimation, itching and redness of the eyes. Ascorbic Acid (Vitamin C) participates in the regulation of redox processes, carbohydrate metabolism, increases the body’s resistance.

Pharmacokinetics

Paracetamol

Absorption is high, the maximum concentration is reached in 0.5-2 hours; the maximum concentration is 5-20 mcg / ml. Binding to plasma proteins is 15%. Penetrates the blood-brain barrier. Less than 1% of the dose of paracetamol taken by a nursing mother passes into breast milk. A therapeutically effective plasma concentration of paracetamol is achieved when it is administered at a dose of 10-15 mg / kg.

It is metabolized in the liver (90-95%): 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione to form already inactive metabolites.

When glutathione is deficient, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The CYP2E1 isoenzyme is also involved in drug metabolism. The elimination half-life is 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, the clearance of the drug decreases and the half-life increases.

Chlorphenamine maleate

Chlorphenamine is relatively slowly absorbed from the gastrointestinal tract, the maximum concentration of chlorphenamine in blood plasma is reached 2.5-6 hours after taking the drug. The substance has a low bioavailability of 25-50%. About 70% of chlorphenamine in the bloodstream binds to plasma proteins. It undergoes a wide distribution in body tissues, including the central nervous system.

Chlorphenamine undergoes significant metabolism during its primary passage through the liver. The duration of action is 4-6 hours. Children have faster and more complete absorption, faster clearance, and a shorter half-life.

The elimination half-life ranges from 2 to 43 hours, even with an average duration of 4-6 hours. Part of the chlorphenamine in unchanged form with metabolites is excreted by the kidneys.

Ascorbic acid

It is absorbed in the gastrointestinal tract (mainly in the jejunum). Binding to plasma proteins is 25%. Diseases of the gastrointestinal tract (peptic ulcer of the stomach and duodenum 12, constipation or diarrhea, helminthic invasion, giardiasis), the use of fresh fruit and vegetable juices, alkaline drinking reduce the absorption of ascorbic acid in the intestines.

The normal concentration of ascorbic acid in plasma is approximately 10-20 micrograms / ml. The time of maximum concentration in blood plasma after oral use is 4 hours. It easily penetrates into white blood cells, platelets, and then into all tissues; the highest concentration is achieved in glandular organs, white blood cells, liver and lens of the eye; it penetrates through the placenta.

The concentration of ascorbic acid in white blood cells and platelets is higher than in red blood cells and in plasma. In deficient states, the concentration in white blood cells decreases later and more slowly and is considered as a better criterion for assessing the deficit than the concentration in plasma.

It is mainly metabolized in the liver to deoxyascorbic acid and then to oxaloacetic acid and ascorbate-2-sulfate. It is excreted by the kidneys, through the intestines, with sweat in unchanged form and in the form of metabolites. Smoking and drinking ethanol accelerate the breakdown of ascorbic acid (conversion to inactive metabolites), dramatically reducing the body’s reserves. It is excreted during hemodialysis.

Indications

Infectious and inflammatory diseases (ARVI, flu), accompanied by fever, chills, headache, pain in the joints and muscles, nasal congestion and pain in the throat and sinuses. The drug is intended for symptomatic treatment.

Use during pregnancy and lactation

Use during pregnancy and lactation is contraindicated.

Contraindications

• Hypersensitivity to paracetamol, ascorbic acid, chlorphenamine or any other component of the drug.

• Erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase).

• Severe renal and / or hepatic insufficiency.

• Alcoholism. Angle-closure glaucoma.

• Portal hypertension.

• Prostatic hyperplasia.

• Lactose intolerance, lactase deficiency, glucose-galactose malabsorption. Due to the content of aspartame, it is contraindicated in patients with phenylketonuria.

• Children’s age (up to 15 years).

• Pregnancy and breast-feeding period.

With caution

Renal and/or hepatic insufficiency, glucose-6-phosphate dehydrogenase deficiency, congenital hyperbilirubinemia (Gilbert’s, Dubin-Johnson’s and Rotor’s syndromes), hyperoxalaturia, progressive malignancies, viral hepatitis, alcoholic hepatitis, elderly age, simultaneous or within the previous 2 weeks taking monoamine oxidase inhibitors (MAO), tricyclic antidepressants; simultaneous use of drugs diseases that can negatively affect the liver; diabetes mellitus; in patients with bronchial asthma, chronic bronchitis.

Side effects

The drug is well tolerated in the recommended doses. Extremely rare: from the central nervous system:  headache, feeling of fatigue;from the gastrointestinal tract:  nausea, epigastric pain, diarrhea; endocrine system disorders:  hypoglycemia (up to the development of coma); from the hematopoietic organs:  anemia, hemolytic anemia (especially for patients with glucose-6-phosphate dehydrogenase deficiency), pancytopenia, leukopenia, hemolytic anemia, thrombocytopenia; from the liver and biliary tract:  impaired liver function; severe skin reactions:  acute generalized exanthematous pustulosis; allergic reactions:  skin rash, pruritus, urticaria, angioedema, anaphylactoid reactions (including anaphylactic shock), erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome). other services:  hypervitaminosis, metabolic disorders, heat sensation, dry mouth, accommodation paresis, urinary retention, drowsiness, mydriasis, hepatotoxic effect, nephrotoxicity, bronchospasm. All side effects of the drug should be reported to the doctor.

Interaction

Paracetamol

The anticoagulant effect of warfarin and other coumarins can be enhanced with prolonged regular use of paracetamol, while increasing the risk of bleeding. Periodic use of paracetamol has no significant effect.

Hepatotoxic substances can lead to the accumulation of paracetamol and overdose. The risk of hepatotoxicity of paracetamol is increased by the use of drugs that induce microsomal liver enzymes, such as barbiturates, antiepileptic drugs (for example, phenytoin, phenobarbital, carbamazepine) and drugs for the treatment of tuberculosis, such as rifampicin and isoniazid.

Metoclopramide increases the rate of absorption of paracetamol and increases its maximum concentration in blood plasma. Similarly, domperidone may increase the rate of absorption of paracetamol.

Paracetamol may increase the elimination half-life of chloramphenicol. Paracetamol can lead to a decrease in the bioavailability of lamotrigine, with a possible decrease in the effect of the latter, which can lead to a possible induction of metabolism in the liver.

The absorption of paracetamol may be reduced when co-administered with colestyramine, but the decrease in absorption is insignificant if colestyramine is used an hour later.

Regular use of paracetamol concomitantly with zidovudine may cause neutropenia and increase the risk of liver damage.

Probenecid affects the metabolism of paracetamol. The dose of paracetamol should be reduced in patients taking probenecid concomitantly.

The hepatotoxicity of paracetamol increases with prolonged excessive use of ethanol (alcohol). Myelotoxic drugs increase the manifestation of paracetamol hematoxicity. Paracetamol may affect the results of phosphor-tungsten uric acid tests.

Phenytoin reduces the effectiveness of paracetamol, therefore, patients taking phenytoin should avoid frequent use of paracetamol, especially in high doses. Indirect anticoagulants: repeated use of paracetamol for more than 4 days increases the anticoagulant effect.

The international normalized ratio (INR) should be monitored during and after the end of concomitant use of paracetamol (especially in high doses and/or for a long time) and coumarin derivatives.

Irregular use of paracetamol does not have a significant effect.Propanthelin and other drugs that slow gastric evacuation reduce the rate of absorption of paracetamol, which may delay or reduce the onset of the effect.

Long-term concomitant use of paracetamol and other NSAIDs increases the risk of developing” analgesic ” nephropathy and renal papillary necrosis, the onset of end-stage renal failure. Concomitant long-term use of high-dose paracetamol and salicylates increases the risk of developing kidney or bladder cancer.

Chlorphenamine maleate

Antihistamines such as chlorphenamine can enhance the effects of opioid analgesics, anticonvulsants, antidepressants (tricyclic and monoamine oxidase inhibitors), other antihistamines, antiemetics and antipsychotics, anxiolytics, sleeping pills, ethanol (alcohol) and other central nervous system depressants.

Since chlorphenamine has some anticholinergic activity, the effects of anticholinergic drugs (for example, certain psychotropic drugs, atropine, and urinary incontinence medications) may be enhanced by the use of this drug. This can lead to tachycardia, dryness of the oral mucosa, gastrointestinal disorders (such as colic), urinary retention, and headache.

Phenytoin metabolism may be inhibited by chlorphenamine, and phenytoin toxicity may develop.

Ascorbic acid

Ascorbic acid increases the absorption of penicillin and iron drugs, reduces the clinical effect of heparin and indirect anticoagulants, increases the risk of crystalluria in the treatment with short-acting salicylates and sulfonamides, slows down the excretion of acids by the kidneys, increases the excretion of drugs with an alkaline reaction (including alkaloids), reduces the concentration of oral contraceptives in the blood.

It should not be administered during the first month of deferoxamine treatment due to increased iron toxicity. High doses of ascorbic acid can lead to an increase in the concentration of ethinyl estradiol in blood plasma in women taking oral contraceptives. Simultaneous use of ascorbic acid and fluphenazine may lead to a decrease in the concentration of fluphenazine in blood plasma.

How to take, course of use and dosage

Inside. Adults and children over 15 years of age: 1 sachet 2-3 times a day. The contents of 1 sachet should be completely dissolved in a glass (200 ml) of warm water (50-60 °C) and the resulting solution should be drunk immediately. It is better to take the drug between meals. The maximum daily dose is 3 sachets. The interval between doses of the drug should be at least 4 hours. In patients with impaired liver or kidney function and in elderly patients, the interval between doses of the drug should be at least 8 hours. The duration of admission without consulting a doctor is not more than 5 days when prescribed as an analgesic and 3 days as an antipyretic.

Overdose

Symptoms of overdose with the drug are caused by its constituent substances, mainly the presence of paracetamol.

Paracetamol

The clinical picture of acute paracetamol overdose develops within 24 hours after taking it. Gastrointestinal disorders appear (nausea, vomiting, decreased appetite, abdominal discomfort and / or abdominal pain, pallor of the skin).

With simultaneous use of 7.5 g or more to adults or 140 mg/kg to children, cytolysis of hepatocytes occurs with complete and irreversible liver necrosis, the development of liver failure, metabolic acidosis and encephalopathy, which can lead to coma and death.

Ingestion of 5 g or more of paracetamol may cause liver damage in the presence of risk factors (long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John’s wort, or other drugs that are inducers of microsomal liver enzymes; ethanol abuse, glutathione deficiency, digestive disorders, cystic fibrosis, HIV infection, starvation, cachexia).

12-48 hours after paracetamol use, there is an increase in the activity of microsomal liver enzymes, lactate dehydrogenase, bilirubin concentration, and a decrease in prothrombin content. Clinical symptoms of liver damage appear 2 days after paracetamol overdose and reach a maximum on day 4-6.

Overdose can lead to intoxication, especially in elderly patients, children, patients with liver diseases (caused by chronic alcoholism), in patients with nutritional disorders, as well as in patients taking inducers of microsomal liver enzymes, and may develop lightning-fast hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis, sometimes with a fatal outcome.

In severe cases of overdose, as a result of liver failure, encephalopathy (impaired brain function), brain edema, bleeding, hypoglycemia, up to a fatal outcome can develop.

It is possible to develop acute renal failure with acute tubular necrosis, the characteristic signs of which are pain in the lumbar region, hematuria (an admixture of blood or red blood cells in the urine), proteinuria (increased protein content in the urine), while severe liver damage may be absent. There were cases of cardiac arrhythmias, pancreatitis.

Treatment. Immediate hospitalization. If an overdose is suspected, even in the absence of pronounced first symptoms, it is necessary to stop using paracetamol and immediately seek medical help.

It is necessary to determine the level of paracetamol in the blood plasma, but not earlier than 4 hours after overdose (earlier results are not reliable). Laboratory tests of the activity of microsomal liver enzymes should be performed at the beginning of treatment and then every 24 hours.

use of SH-group donors and glutathione synthesis precursors-methionine and acetylcysteine-is most effective in the first 8 hours.

Within 1 hour after overdose, gastric lavage and use of enterosorbents (activated charcoal, etc. ) are recommended. In most cases, the activity of microsomal liver enzymes normalizes within 1-2 weeks.

In very severe cases, a liver transplant may be required. use of acetylcysteine within 24 hours of overdose. The maximum protective effect is provided during the first 8 hours after an overdose; over time, the effectiveness of the antidote drops sharply.

If necessary, acetylcysteine is administered intravenously. If there is no vomiting before the patient is admitted to the hospital, methionine may be used. The need for additional therapeutic measures (further use of methionine, intravenous use of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after taking it.

Treatment of patients with severe hepatic impairment 24 hours after taking paracetamol should be carried out in conjunction with specialists of the toxicology center or specialized department of liver diseases.

Chlorphenamine maleate

Symptoms of chlorphenamine maleate overdose include drowsiness, respiratory arrest, seizures, anticholinergic effects, dystonic reactions, and cardiovascular collapse, including arrhythmia. In children, overdose symptoms may include impaired coordination, agitation, tremors, behavior changes, hallucinations, seizures, and anticholinergic effects.

Treatment. Includes gastric lavage in case of a massive overdose, or stimulation of vomiting. After that, it is possible to prescribe activated charcoal and laxatives to slow down absorption. In case of convulsions, sedation should be performed with intravenous diazepam or phenytoin. In severe cases, hemoperfusion may be performed.

Ascorbic acid

Symptoms of ascorbic acid overdose: nephrolithiasis, insomnia, irritability, hypoglycemia. Treatment. Treatment of ascorbic acid overdose is symptomatic, and forced diuresis may be required.

Special instructions

If you are taking metoclopramide, domperidone, or colestyramine, you should also consult your doctor. With prolonged use in doses significantly higher than recommended, the likelihood of impaired liver and kidney function increases, and monitoring of the peripheral blood picture is necessary.

Paracetamol and ascorbic acid can distort laboratory tests (quantitative determination of glucose and uric acid in blood plasma, bilirubin, activity of “hepatic” transaminases, LDH).

In order to avoid toxic liver damage, paracetamol should not be combined with the intake of alcoholic beverages, as well as taken by people who are prone to chronic alcohol consumption. The risk of developing liver damage increases in patients with alcoholic hepatosis.

Patients with glutathione deficiency are susceptible to overdose, and caution should be exercised. Cases of liver failure have been reported in patients with low glutathione levels, in particular in extremely emaciated patients with anorexia, people with chronic alcoholism, or patients with a low body mass index.

The use of paracetamol in patients with low glutathione levels, such as sepsis, may increase the risk of developing metabolic acidosis.

Paracetamol can cause serious skin reactions, such as acute generalized exanthematous pustulosis, Stephen-Johnson syndrome, toxic epidermal necrolysis.At the first appearance of a rash or other hypersensitivity reactions, the drug should be discontinued.

Prescribing ascorbic acid to patients with rapidly proliferating and intensely metastatic tumors may worsen the course of the process. In patients with high iron content in the body, ascorbic acid should be used in minimal doses.

It is possible to develop drowsiness within a few hours after taking the drug.

Influence on the ability to drive vehicles and mechanisms

When using the drug, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date.

Active ingredient

Paracetamol, Chlorphenamine, [Ascorbic Acid]

Dosage form

tablets soluble