Instructions Gripgo tablets blister No. 100
Composition
active ingredients: paracetamol, caffeine anhydrous, phenylephrine hydrochloride, chlorpheniramine maleate;
1 tablet contains paracetamol 500 mg, caffeine anhydrous 30 mg, phenylephrine hydrochloride 10 mg, chlorpheniramine maleate 2 mg;
excipients: microcrystalline cellulose, croscarmellose sodium, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: white biconvex capsule-shaped tablets.
Pharmacotherapeutic group
Analgesics and antipyretics. Paracetamol, combinations without psycholeptics. ATX code N02B E51.
Pharmacological properties
Pharmacodynamics
Gripgo® is a combination drug, the effect of which is due to the components that make up its composition.
Paracetamol is an analgesic-antipyretic that has antipyretic and analgesic properties, which is associated with the effect of paracetamol on the hypothalamic thermoregulation center and its ability to inhibit prostaglandin synthesis.
Caffeine is an alkaloid from the methylxanthine group, which directly stimulates the respiratory and vascular centers of the brain, improves the physical and emotional state of patients, thereby reducing the manifestations of asthenia in infectious diseases. Increases the analgesic effect of paracetamol.
Phenylephrine hydrochloride is a sympathomimetic agent that reduces swelling of the nasal mucosa and paranasal sinuses, the severity of exudative manifestations, which helps improve nasal breathing. It stimulates mainly alpha-adrenoreceptors, which causes narrowing of peripheral vessels and a decrease in their permeability, and reduces the formation of mucous secretions.
Chlorpheniramine maleate is an antihistamine that has antiallergic effects. It competitively blocks histamine H1 receptors and prevents the development of histamine effects, eliminating runny nose, itchy nose, tearing and stinging in the eyes.
Pharmacokinetics
Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract, the maximum concentration in the blood plasma is reached after 30-60 minutes. The half-life from the blood plasma is 1-4 hours. It is evenly distributed in all body fluids. Protein binding is variable. The duration of the analgesic effect of the drug is 4-6 hours, the antipyretic effect is 6-8 hours. It is excreted mainly by the kidneys in the form of conjugated metabolites, less than 5% is excreted unchanged.
Caffeine and its water-soluble salts are rapidly absorbed in the intestines (including the colon). The half-life from blood plasma is about 5-10 hours. The main part is demethylated and oxidized. About 10% is excreted by the kidneys in unchanged form.
Phenylephrine hydrochloride has low bioavailability due to uneven absorption and the influence of monoamine oxidase in the gastrointestinal tract and liver during the "first pass". It is excreted by the kidneys in the form of metabolites. Acidification of urine accelerates excretion from the body.
Chlorpheniramine maleate is slowly absorbed from the gastrointestinal tract, the maximum concentration in the blood plasma is reached after 2.5-6 hours, 70% of it is bound to blood plasma proteins. Bioavailability is from 25% to 50% of the dose taken. Chlorpheniramine undergoes metabolism during the "first pass" in the liver, is largely metabolized in the liver with the formation of metabolites desmethyl- and didesmethylchlorpheniramine. Chlorpheniramine is distributed throughout the body, passes through the blood-brain barrier. Metabolites and the drug are excreted mainly in the urine unchanged within 4-6 hours. Excretion depends on the pH of the urine and the degree of excretion. Children have a faster and more extensive absorption, excretion and half-life.
Indication
Treatment of symptoms of influenza and other acute respiratory viral diseases: fever, headache, nasal congestion, rhinitis, sinusitis, sore throat, muscle pain, cough.
Contraindication
Hypersensitivity to any component of the drug, other xanthine derivatives (theophylline, theobromine), opioids, antihistamines, sympathomimetic amines. Severe cardiovascular diseases, including unstable angina, decompensated heart failure, conduction disorders, congenital prolonged QT interval or long-term use of drugs that prolong the QT interval, arrhythmias, bradycardia, severe atherosclerosis, including coronary vessels, tendency to vasospasm, severe ischemic heart disease; severe arterial hypertension, acute period of myocardial infarction, organic diseases of the cardiovascular system. Severe liver and kidney dysfunction. Prostate adenoma with difficulty urinating, acute urinary retention in prostatic hypertrophy, bladder neck obstruction. Gastric and duodenal ulcers in the acute stage, stenosing gastric and duodenal ulcers, pyloroduodenal obstruction; acute pancreatitis, epilepsy. Blood diseases (including severe anemia, leukopenia), hematopoietic disorders. Endocrine diseases (hyperthyroidism, diabetes mellitus, pheochromocytoma, thyrotoxicosis). Lung diseases, including bronchial asthma; risk of respiratory failure. Angle-closure glaucoma. Glucose-6-phosphate dehydrogenase deficiency. Alcoholism. Increased excitability, sleep disorders, epilepsy, alcoholism. Congenital hyperbilirubinemia. Elderly age. Simultaneous use with tricyclic antidepressants, ß-blockers; with MAO inhibitors and within 2 weeks after their discontinuation.
Interaction with other medicinal products and other types of interactions
For paracetamol.
The rate of absorption of paracetamol may be increased by metoclopramide and domperidone and decreased by cholestyramine. The anticoagulant effect of warfarin and other coumarins may be enhanced by long-term regular daily use of paracetamol, with an increased risk of bleeding. Intermittent use has no significant effect.
Barbiturates reduce the antipyretic effect of paracetamol.
Anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of liver microsomal enzymes, may enhance the toxic effect of paracetamol on the liver due to an increase in the degree of conversion of the drug to hepatotoxic metabolites. With the simultaneous use of paracetamol with hepatotoxic agents, the toxic effect of drugs on the liver increases.
Simultaneous use of high doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome. Paracetamol reduces the effectiveness of diuretics.
Do not use simultaneously with alcohol.
For caffeine.
Caffeine, when used simultaneously, enhances the effect of analgesics-antipyretics (improves bioavailability), xanthine derivatives, α- and β-adrenomimetics, psychostimulants, thyroid-stimulating agents, and ergotamine (improves the absorption of ergotamine from the digestive tract).
Cimetidine, hormonal contraceptives, and isoniazid enhance the effects of caffeine.
Caffeine increases the likelihood of liver damage from hepatotoxic drugs.
Caffeine reduces the effect of opioid analgesics, anxiolytics, hypnotics and sedatives, is an antagonist of anesthetics and other drugs that depress the central nervous system, a competitive antagonist of adenosine and ATP drugs; reduces the concentration of lithium in the blood.
Ototoxic and photosensitizing drugs may increase side effects when used simultaneously.
Caffeine reduces the hypotensive effect of guanethidine, which in turn increases the alpha-adrenostimulating activity of phenylephrine. Caffeine enhances the effect of indirect anticoagulants (coumarin derivatives). Metoclopramide increases, and cholestyramine reduces the rate of absorption of caffeine. Antidepressants, antiparkinsonian and antipsychotic drugs, phenothiazine derivatives increase the risk of urinary retention, dry mouth, constipation. Glucocorticosteroids increase the risk of glaucoma.
For phenylephrine hydrochloride.
Phenylephrine hydrochloride should not be used with alpha-blockers, other antihypertensive agents, phenothiazine derivatives (e.g. promethazine), bronchodilator sympathomimetic agents, guanethidine, digitalis, rauwolfia alkaloids, indomethacin, methyldopa, glucocorticosteroids; drugs that affect appetite, amphetamine-like psychostimulants, labor stimulants, anesthetics, ergot alkaloids, other drugs that stimulate the central nervous system, theophylline.
The use of phenylephrine hydrochloride with indomethacin and bromocriptine may cause severe arterial hypertension. The simultaneous use of phenylephrine hydrochloride with sympathomimetic amines, digoxin and cardiac glycosides increases the risk of arrhythmias and myocardial infarction.
Atropine sulfate blocks the reflex bradycardia caused by phenylephrine and increases the vasopressor response to phenylephrine. Concomitant use of phenylephrine with β-blockers may lead to arterial hypertension and excessive bradycardia with possible heart block. It should be used with caution with thyroid hormones, drugs that affect cardiac conduction (cardiac glycosides, antiarrhythmic drugs). When used simultaneously with drugs that cause potassium excretion, for example, with some diuretics such as furosemide, hypokalemia and decreased arterial sensitivity to vasopressor drugs such as phenylephrine may be increased.
Should not be used together with other vasoconstrictors (by any route of administration).
Concomitant administration of phenylephrine and other sympathomimetics may result in excessive central nervous system stimulation, with nervousness, irritability, and insomnia. Convulsions may also occur. In addition, concomitant administration of other sympathomimetics with phenylephrine may potentiate the vasoconstrictor or cardiovascular effects of either drug.
For chlorpheniramine maleate.
Chlorpheniramine maleate enhances the anticholinergic effect of atropine, antispasmodics, central nervous system depressants (tranquilizers, barbiturates), and antiparkinsonian drugs.
Do not use simultaneously with alcohol. Chlorpheniramine maleate, when used simultaneously with alcohol, potentiates the effects of each other.
Simultaneous use with hypnotics, barbiturates, sedatives, neuroleptics, tranquilizers, anesthetics, narcotic analgesics, and alcohol enhances the effect of chlorpheniramine maleate.
Maprotiline (a tetracyclic antidepressant) and other anticholinergic drugs: the anticholinergic effect of these drugs or antihistamines such as chlorpheniramine may be enhanced.
Application features
Do not exceed recommended doses.
Do not use simultaneously with preparations containing paracetamol and other cold remedies; with sedatives, hypnotics.
If the symptoms of the disease do not disappear or the headache becomes constant, you should consult a doctor.
The risk of overdose increases in alcoholic liver disease. During treatment, alcohol should be avoided, as it enhances the sedative effect of chlorpheniramine maleate and the hepatotoxicity of paracetamol. It should be noted that patients with alcoholic non-cirrhotic liver disease are at increased risk of hepatotoxic effects of paracetamol. Patients who take daily analgesics for mild arthritis should consult a doctor before using the drug.
In patients with severe infections such as sepsis, which are accompanied by a decrease in glutathione levels, the risk of metabolic acidosis may be increased when taking paracetamol. Symptoms of metabolic acidosis include deep, rapid or difficult breathing, nausea, vomiting, loss of appetite. You should consult a doctor immediately if these symptoms occur.
When using the drug, you should avoid excessive consumption of coffee, strong tea, other tonic drinks and medications containing caffeine. This can cause sleep problems, tremors, tension, irritability, and palpitations. Do not drink alcohol.
3 Use with caution in compensated heart failure, patients at risk of seizures, patients with chronic obstructive airway diseases, persistent or chronic cough resulting from smoking or emphysema, when the cough is accompanied by excessive sputum secretion. Use with caution in persons prone to increased blood pressure.
The drug may affect the results of laboratory tests for blood glucose and uric acid. The use of the drug may cause a positive analytical result in doping control. With prolonged use, it is necessary to monitor peripheral blood and liver function. Before using the drug, it is necessary to consult a doctor if the patient uses warfarin or similar drugs that have an anticoagulant effect, and in patients with impaired kidney and liver function.
Phenylephrine may cause increased heart rate, dizziness, or palpitations; patients should be warned accordingly.
In case of accidental overdose, the patient should immediately consult a doctor, even if his/her well-being has not worsened.
Keep the drug out of the sight and reach of children.
Use during pregnancy or breastfeeding
Gripgo® is contraindicated during pregnancy. Breastfeeding should be discontinued during treatment with the drug.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment, you should avoid driving vehicles, working with mechanisms and other dangerous activities.
Method of administration and doses
Adults and children over 12 years of age should be prescribed 1 tablet 3-4 times a day. The maximum daily dose is 4 tablets. The maximum duration of use without consulting a doctor is 3 days, further use is on the recommendation of a doctor.
Children
The drug is contraindicated in children under 12 years of age.
Overdose
Liver damage is possible in adults who have taken 10 g or more of paracetamol, and in children who have taken more than 150 mg/kg of body weight. In patients with risk factors (long-term treatment with carbamazepine, phenobarbitone, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; regular use of excessive amounts of ethanol; glutathione cachexia (digestive disorders, cystic fibrosis, HIV infection, starvation, cachexia) the use of 5 g or more of paracetamol can lead to liver damage.
Symptoms of overdose in the first 24 hours: pallor, nausea, vomiting, anorexia and abdominal pain. Liver damage may become apparent 12-48 hours after overdose. Glucose metabolism disorders and metabolic acidosis may occur. In severe poisoning, liver failure may progress to encephalopathy, hemorrhage, hypoglycemia, coma and death. Acute renal failure with acute tubular necrosis may present with severe lumbar pain, hematuria, proteinuria and may develop even in the absence of severe liver damage. Cardiac arrhythmia and pancreatitis have also been reported.
With prolonged use of the drug in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia may develop from the hematopoietic system. When taking high doses, dizziness, psychomotor agitation and disorientation may occur from the CNS; nephrotoxicity (renal colic, interstitial nephritis, capillary necrosis) may occur from the urinary system.
Symptoms of overdose due to the action of phenylephrine and chlorpheniramine maleate: headache, hyperhidrosis, drowsiness, insomnia, behavioral changes, restlessness, irritability, tremor, convulsions, hyperreflexia, dizziness, nausea, vomiting, tachycardia, arrhythmias, extrasystole.
In case of overdose with chlorpheniramine maleate, the state may vary from depressed to excited (restlessness and convulsions). Atropine-like symptoms may be observed, including mydriasis, photophobia, dryness of the skin and mucous membranes, fever, intestinal atony; depression of the central nervous system is accompanied by respiratory disorders and disorders of the cardiovascular system.
In case of caffeine overdose, the following symptoms are observed: dehydration, hyperthermia, tinnitus, epigastric pain, increased frequency of diuresis, extrasystole, tachycardia, rapid breathing, arrhythmia, effects on the central nervous system (dizziness, insomnia, excitement, irritability, psychomotor agitation, state of affect, anxiety, tremor, vomiting, seizures, convulsions, agitation, restlessness, delirium, increased tactile or pain sensitivity).
Treatment of overdose. In case of overdose, urgent medical attention is required. The patient should be taken to hospital immediately, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting or may not reflect the severity of the overdose or the risk of organ damage. Treatment with activated charcoal should be considered if an overdose of paracetamol has been taken within 1 hour. The concentration of paracetamol in the blood plasma should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Treatment with N-acetylcysteine can be used within 24 hours of ingestion of paracetamol, but the maximum protective effect occurs when it is used within 8 hours of ingestion. The effectiveness of the antidote decreases sharply after this time. If necessary, the patient should be given N-acetylcysteine intravenously according to the established dose list. In the absence of vomiting, oral methionine can be used as a suitable alternative in remote areas outside the hospital.
Adverse reactions
On the part of the immune system: hypersensitivity reactions, including anaphylaxis, skin itching, flushing, rash on the skin and mucous membranes (usually generalized rash, erythematous, urticaria), anaphylactic shock, angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis.
From the side of the central nervous system: psychomotor agitation and disorientation, anxiety, behavioral changes, feelings of fear, anxiety, irritability, sleep disturbances, insomnia, drowsiness, dizziness, confusion, hallucinations, depressive states, tremor, tingling and heaviness in the limbs, tinnitus, headache, dizziness, coma, convulsions, increased excitability, epileptic seizures, dyskinesia.
Respiratory system: bronchospasm in patients sensitive to aspirin and other NSAIDs, nasal congestion, sore throat, hoarseness.
On the part of the organs of vision: impaired vision and accommodation, mydriasis, increased intraocular pressure, dry eyes.
On the part of the hepatobiliary system: impaired liver function, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (when using high doses), hepatotoxicity.
On the part of the endocrine system: hypoglycemia, up to hypoglycemic coma. With prolonged use in high doses, damage to the insular apparatus of the pancreas (hyperglycemia, glucosuria) and impaired glycogen synthesis up to the onset of diabetes mellitus are possible.
Metabolic disorders: zinc and copper metabolism disorders.
From the blood and lymphatic system: anemia, including hemolytic anemia, bruising or bleeding; sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), thrombocytosis, hyperproteinemia, erythropenia, neutrophilic leukocytosis.
With prolonged use in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, and thrombocytopenia are possible.
On the part of the kidneys and urinary system: when using high doses - nephrotoxicity (including papillary necrosis), urination disorders, urinary retention and difficulty urinating, dysuria, interstitial nephritis, increased creatinine clearance, increased sodium and calcium excretion, aseptic pyuria, renal colic.
With prolonged use in high doses, damage to the glomerular apparatus of the kidneys, crystalluria, and the formation of urate, cystine, and/or oxalate stones in the kidneys and urinary tract are possible.
From the cardiovascular system: arterial hypertension, tachycardia or reflex bradycardia, arrhythmia, shortness of breath, heart pain, myocardial dystrophy (dose-dependent effect with prolonged use), palpitations.
Others: general weakness, increased sweating, possible false increase in uric acid in the blood, determined by the Bittner method; slight increase in 5-hydroxyindoleacetic acid, vanillylmandelic acid and catecholamines in the urine.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging.
Keep out of reach of children.
Packaging
4 tablets in a blister; 1 blister in a cardboard box No. 4 (4x1).
4 tablets in a blister; 50 blisters in a cardboard box No. 200 (4x50).
10 tablets in a blister; 1 blister in a cardboard box No. 10 (10x1).
10 tablets in a blister; 1 blister in a cardboard box No. 10. 10 cardboard boxes in a cardboard box No. 100 (10x1x10).
10 tablets in a blister; 10 blisters in a cardboard box No. 100 (10x10).
Vacation category
Without a prescription - No. 4 (4x1), No. 10 (10x1) in blisters.
By prescription - No. 200 (4x50), No. 100 (10x10), No. 100 (10x1x10) in blisters.
Producer
KUSUM HEALTHCARE PVT LTD/KUSUM HEALTHCARE PVT LTD.
Location of the manufacturer and its business address
SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India/SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India.
