Caffeine

GRIPOUT

Euro lifecare N02B E51

COMPOSITION AND FORM OF ISSUE:

tab., No. 4, No. 10

No. UA / 9253/01/01 from 12/17/2008 to 12/17/2013

since d / p r-d d / per. approx. 5 g bag, orange flavor, No. 5

No. UA / 1483/01/01 from 10/13/2009 to 10/13/2014

since d / p r-d d / per. approx. 5 g sachet, with lemon flavor, No. 5

No. UA / 3879/01/01 from 13.10.2009 to 13.10.2014

tab. blister, number 10

No. UA / 1190/01/01 from 06.25.2009 to 06.25.2014

PHARMACOLOGICAL PROPERTIES:

Pharmacokinetics
Paracetamol blocks COX, which leads to the cessation of prostaglandin synthesis, has an antipyretic and analgesic effect.
Chlorphenamine blocks H₁histamine receptors. It has anti-allergic and decongestant effects. Helps reduce vascular permeability of the mucous membrane of the upper respiratory tract, eliminates edema and hyperemia of the nasal mucosa, reduces the severity of symptoms of allergic rhinitis, facilitates breathing.
Phenylephrine hydrochloride - stimulator mainly α₁-adrenoreceptors. It has a vasoconstrictor effect, mainly in relation to the vessels of the upper respiratory tract, reduces increased mucus formation and thus helps to eliminate nasal congestion.
Caffeine It has a stimulating effect on the central nervous system, enhances the analgesic effect of paracetamol, reduces the feeling of fatigue and drowsiness, increases physical and mental performance.
Vitamin C necessary for the synthesis of steroid hormones and procollagen. It regulates the permeability of the vascular wall, blood coagulation, stimulates the regeneration processes. Ascorbic acid promotes the activation of the immune system, replenishes the increased need for vitamin C with influenza and SARS, and strengthens the bodys defense mechanisms.
Pharmacodynamics
Paracetamol quickly and almost completely absorbed in the digestive tract, mainly in the small intestine. After a single dose of 500 mg C_max in the blood is reached after 10-60 minutes. Paracetamol is rapidly and evenly distributed in most body tissues. About 25% of paracetamol in the blood binds to plasma proteins. Paracetamol is metabolized by the microsomal liver enzyme system. About 80–85% of paracetamol in the body undergoes conjugation mainly with glucuronic acid and, to a lesser extent, with sulfuric acid. T_½ is 1-3 hours. Paracetamol is excreted in the urine mainly in the form of paracetamol-glucuronide with small amounts of paracetamol sulfate, mercaptate and unchanged.
Phenylephrine unevenly absorbed in the digestive tract and easily metabolized. After oral administration, its effect appears after 15–20 minutes and persists for 2–4 hours. Bioavailability of phenylephrine is low. Phenylephrine is biotransformed in the walls of the intestine during absorption and in the liver. Less than 16% of the dose is excreted unchanged along with metabolites in the urine.
Chlorpheniramine absorbed relatively slowly GIT, C_max in blood plasma is achieved 2.5-6 hours after ingestion. Bioavailability is 25-50%. Chlorpheniramine undergoes significant metabolism during the first passage through the liver. About 70% of chlorpheniramine in the systemic circulation binds to plasma proteins. T_½ ranges from 2 to 43 hours. Chlorpheniramine is distributed throughout the body, penetrates the BBB. Chlorpheniramine is actively metabolized. Metabolites include desmethyl and didesmethylchlorpheniramine. Unchanged chlorpheniramine and metabolites are excreted mainly in the urine for 4-6 hours.Children have faster and more significant absorption, faster clearance and shorter T_½.
Caffeine well absorbed after oral administration. WITH_max in blood plasma is reached in 15–45 minutes. It has been proven that caffeine improves the absorption of the remaining components of the drug. Caffeine is rapidly distributed in the tissues of the body, it easily overcomes the placental barrier and the BBB. About 17–36% of the dose binds to plasma proteins. Caffeine metabolism is associated with isoenzyme 1A2 of cytochrome P450. In adults, the drug is rapidly metabolized in the liver to 1-methyluric acid and 7-methylxanthine. T_½ is about 3 hours. Caffeine and its metabolites are excreted by the kidneys; about 1% of the dose of caffeine is excreted unchanged.
Vitamin C quickly and almost completely (70–90% of the dose) is absorbed after oral administration. Evenly distributed in the tissues of the body, easily penetrates the placental barrier, passes into breast milk. About 25% of ascorbic acid binds to plasma proteins. Ascorbic acid is reversibly oxidized to dehydroascorbic acid. A small amount of vitamin C is metabolized to inactive components, such as ascorbic acid disulfate and oxalic acid. Metabolism products and a small amount of unchanged substance are excreted by the kidneys.

INDICATIONS:

symptomatic treatment of acute respiratory viral infections and influenza, which are accompanied by headache, myalgia, fever, lacrimation, rhinitis, nasal congestion.

APPLICATION:

Gripout
Adults and children over the age of 12 years - 1 tablet 3-4 times a day. The daily dose should not exceed 4 tablets.
The course of treatment is no more than 5 days.
Gripeout baby
Take orally after a meal with plenty of water.
Children aged 6-12 years: 10 ml 3 times a day (a measuring cap is attached). The interval between doses should be at least 4-6 hours. The duration of treatment is 3 days.
Gripout Hotmix
It is taken orally by 1 sachet up to 4 times a day with an interval of 4-6 hours. Before use, the contents of 1 sachet are dissolved in a glass of hot water. The duration of use is not more than 5 days.
Gripaut Extra Pills
Adults and children over the age of 12 years - 2 tablets up to 4 times a day, 6-12 years old - 1 tablet up to 4 times a day with an interval of 4-6 hours. The course of treatment is no more than 5 days.

CONTRAINDICATIONS:

hypersensitivity to any of the components of the drug, cardiovascular disorders (tachycardia, AH), glaucoma, pregnancy and lactation, age up to 12 years, impaired liver and / or kidney function (liver and kidney failure), congenital hyperbilirubinemia (Gilbert syndrome, Dubin - Johnson, Rotor), glucose-6-phosphate dehydrogenase deficiency, severe anemia, leukopenia, increased irritability, epilepsy, severe atherosclerosis, the elderly, coronary heart disease, angle-closure glaucoma, asthma, gastric ulcer and twelve atiperstnoy ulcer in the acute stage, hyperthyroidism, prostatic hypertrophy, diabetes, severe, the simultaneous use of MAO inhibitors. Gripaut Extra Pills and Gripeout baby contraindicated in children under 6 years of age. Gripout and Gripout Hotmix contraindicated in children under 12 years of age.

SIDE EFFECTS:

the drug is well tolerated, however, in some patients, side effects may occur.
On the part of the skin and subcutaneous tissue: pruritus, rash on the skin and mucous membranes (usually erythematous, urticaria), erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyells syndrome).
From the immune system: anaphylactic shock, angioedema.
From the central nervous system (usually develops when taken in high doses): dizziness, psychomotor agitation and disorientation, sleep disturbance, anxiety, headache, fear, irritability, insomnia, confusion, psychotic conditions, tremor.
From the side of the organ of vision: violation of accommodation, increased intraocular pressure.
From the gastrointestinal tract: nausea, vomiting, epigastric discomfort, epigastric pain, hypersalivation, loss of appetite, abdominal pain, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (dose-dependent effect).
From the endocrine system: hypoglycemia, up to the development of hypoglycemic coma.
From the blood system and lymphatic system: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, pain in the heart), hemolytic anemia (especially in patients with glucose-6-phosphate dehydrogenase deficiency). With prolonged use in high doses - aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia.
From the urinary system: (when taken in high doses) - nephrotoxicity (renal colic, interstitial nephritis, papillary necrosis), painful urination.
From the cardiovascular system: AH, tachycardia.
Others: general weakness, increased sweating.

SPECIAL INSTRUCTIONS:

the drug is not used simultaneously with MAO inhibitors and preparations containing paracetamol and phenylephrine. The drug is prescribed with caution in hypertension, persons with heart disease, cerebral arteriosclerosis, kidney and liver diseases. During treatment, alcohol should be excluded.
Gripout Hotmix contains sugar in an amount of 2895.92 mg in 1 sachet, therefore, patients with diabetes should use the drug with caution. Gripeout baby apply no more than 3 days (with prolonged use of the drug, damage to the liver, kidneys and hematopoiesis system is possible). If signs of the disease persist or their severity increases, you must always consult a doctor.
Use during pregnancy and lactation. Contraindicated.
Children. Gripaut Extra Pills and Gripeout baby used in children over the age of 6 years. Gripout and Gripout Hotmix used in children over the age of 12 years.
Influence on the ability to drive vehicles or work with other mechanisms.
During treatment, you should avoid driving, working with machinery, and other hazardous activities.

INTERACTIONS:

with the simultaneous use of barbiturates, tricyclic antidepressants, as well as with alcohol, an increase in T is possible_½ paracetamol. Prolonged use of anticonvulsants may decrease paracetamol activity. The simultaneous use of paracetamol in high doses with isoniazid increases the risk of developing hepatotoxic syndrome. Paracetamol reduces the effectiveness of diuretics. With the simultaneous use of phenylephrine hydrochloride with atropine, tachycardia can be noted.
The drug reduces the hypotensive effect of guanethidine, which, in turn, increases the α-adrenostimulatory activity of phenylephrine.
Paracetamol enhances the effect of indirect anticoagulants (coumarin derivatives). Metoclopramide increases, and colestyramine reduces the rate of absorption. Barbiturates reduce the antipyretic effect of the drug. With simultaneous use with barbiturates, diphenin, carbamazepine, rifampicin, inducers of microsomal liver enzymes, the risk of hepatotoxic action of paracetamol increases. With the simultaneous use of paracetamol with zidovudine, the toxicity of both drugs increases, granulocytopenia is often noted.
The interaction of phenylephrine with MAO inhibitors causes a hypertensive effect. Phenylephrine reduces the effectiveness of β-adrenergic blockers and antihypertensive drugs. The simultaneous use of MAO inhibitors potentiates the effects of phenylephrine.
Ascorbic acid enhances the absorption of penicillin, reduces the effect of heparin and indirect anticoagulants.With simultaneous use with salicylates, the risk of developing crystalluria increases.
Antidepressants, antiparkinsonian and antipsychotic drugs, phenothiazine derivatives increase the risk of urinary retention, dry mouth, and constipation. GCS increase the risk of developing glaucoma.
Alcohol reduces the therapeutic effect of paracetamol, and can also lead to the development of acute pancreatitis.

OVERDOSE:

usually caused by paracetamol and is manifested by pallor of the skin, anorexia, nausea, vomiting, abdominal pain, hepatonecrosis, increased activity of hepatic transaminases, an increase in prothrombin index.
Symptoms of liver damage are noted 12–48 hours after an overdose. Impaired glucose metabolism and metabolic acidosis may occur. With severe poisoning, liver failure can progress and lead to the development of toxic encephalopathy with impaired consciousness, in some cases with a fatal outcome. ARF with acute tubular necrosis can develop even in the absence of severe kidney damage. Cardiac arrhythmia was also noted. Liver damage is possible in adults with a dose of ≥10 g of paracetamol, and in children who have taken> 150 mg / kg body weight.
In case of an overdose, increased sweating, psychomotor agitation or depression of the central nervous system, drowsiness, impaired consciousness, cardiac arrhythmias, tachycardia, extrasystole, tremor, hyperreflexia, convulsions may be noted.
Treatment: gastric lavage, followed by the use of activated carbon, symptomatic therapy. The use of methionine orally or iv acetylcysteine ​​is effective within 48 hours after an overdose. Supportive therapy should also be prescribed. If necessary, α-adrenoreceptor blockers are used.

STORAGE CONDITIONS:

at a temperature not exceeding 25 ° C; Gripout - at a temperature of 15–25 ° С.