Rinzip tablets №10х1

NameRinzip tabl. Main active ingredient Caffeine + paracetamol + phenylephrine + chlorphenamine Release form tablets The risk of drowsiness increases with the use of alcoholic beverages, drugs containing alcohol, or sedatives. The risk of developing a predominantly mental dependence appears only at doses exceeding the recommended ones, and with long-term treatment. To avoid the risk of overdose, make sure that other medicines taken by the patient do not contain paracetamol. For adults weighing more than 50 kg, the total dose of paracetamol should not exceed 4 g per day. Caution regarding caffeine. The recommended dose of the drug contains about the same amount of caffeine as is in a cup of coffee. While taking the drug, you should limit the use of drugs, drinks and foods containing caffeine, since excessive consumption of caffeine causes nervousness, irritability, insomnia and sometimes tachycardia. Pharmacological properties Pharmacodynamics Caffeine is a methylxanthine that inhibits the activity of the phosphodiesterase enzyme and is an antagonist of the central adenosine receptors. It has a stimulating effect on the central nervous system, especially on the centers of mental activity, which leads to a decrease in fatigue and drowsiness, to an increase in mental performance. Caffeine affects the respiratory center, resulting in increased frequency and depth of breathing. It stimulates muscle activity, causing an increase in physical performance. Additionally, caffeine also has a weak bronchodilatory and diuretic effect. Paracetamol has an analgesic and antipyretic effect mainly by inhibiting the synthesis of prostaglandins in the central nervous system, as well as by affecting the centers of pain and thermoregulation. The main link in the antipyretic action of paracetamol is its effect on the cerebral endothelium, which is reduced to selective inhibition of COX-2 by restoring its oxidized forms to a catalytically inactive state. The drug does not affect the synthesis of prostaglandins in peripheral tissues, which leads to the absence of a negative effect on the water-electrolyte balance (does not cause sodium and water retention) and on the gastrointestinal mucosa. In the foci of inflammation, cellular peroxidases and other oxidizing agents neutralize the restorative effect of paracetamol on cyclooxygenase, which explains the almost complete absence of its anti-inflammatory effect. Phenylephrine is a sympathomimetic agent similar in its action to ephedrine. It is a selective ?1 receptor agonist; ?-receptors activates only in very high concentrations. The drug is active in the form of the l-isomer. It does not have a central effect and has little effect on cardiac output and the force of myocardial contraction, which, however, is accompanied by an increase in myocardial reactivity. Due to the activation of baroreceptors, bradycardia can occur, and the vasoconstrictor effect leads to an increase in blood pressure. When used in doses contained in the drug (PM) Rinzip® phenylephrine hydrochloride has a moderate vasoconstrictor effect – reduces swelling and hyperemia of the mucous membranes of the upper respiratory tract and paranasal sinuses. Pheniramine has antiallergic activity. It eliminates itching of the eyes, nose and throat, swelling and hyperemia of the mucous membranes of the nasal cavity, nasopharynx and paranasal sinuses, reduces exudative manifestations. Pheniramine is an alkylamine antihistamine used primarily in combination preparations for the treatment of colds and allergies. Like all alkylamine derivatives, it is a potent H1 receptor antagonist. The action of pheniramine is due to reversible competitive inhibition of the interaction of histamine with H1 receptors on the cell surface, which prevents the effect of histamine on target organs. Pheniramine inhibits the inflammatory component of the response to intradermal histamine injections. Along with other H1 receptor antagonists, it blocks vasodilation mediated by H1 receptors on endothelial cells; however, for the full suppression of the vasodilating effect, the simultaneous administration of H2 antagonists is required. In animals, pheniramine blocked the bronchoconstrictor function of histamine at the level of airway smooth muscle cells. It also has a protective effect in anaphylactic bronchospasm. Pheniramine effectively binds to H1 receptors in the CNS and even at therapeutic doses has a sedative effect. In comparison with other H1-antagonists, the antihistamine activity of pheniramine and other alkylamine agents is somewhat superior to that of ethanolamines and ethylenediamines, and is the same as the activity of promethazine. Pharmacokinetics The pharmacokinetics of the active substances of the drug, caffeine, paracetamol, phenylephrine hydrochloride and pheniramine, does not change with combined use. Caffeine is rapidly absorbed after ingestion and is extensively distributed throughout the body. Caffeine enters directly into the central nervous system and is excreted in saliva in significant amounts. It penetrates the hemato-placental barrier and is excreted in breast milk. Caffeine has been shown to have a dose-dependent and satiating metabolism. In adults, caffeine is metabolized almost completely in the liver due to oxidation, demethylation and acetylation and is excreted in the urine in the form of metabolites, the proportion of which varies in different animal species: 1-methylene acid, 1-methylxanthine, 7-methylxanthine, paraxanthine, AFMU, etc. P. The proportion of unchanged drug does not exceed 1%. The elimination period of the drug is 3-7 hours and can vary fivefold in healthy people. It decreases under the influence of smoking and physical activity, increases with liver diseases and does not depend on age. Paracetamol is rapidly absorbed from the gastrointestinal tract and distributed to most organs and tissues. The maximum concentration in blood plasma is established after 15 minutes and is 15 – 30 μg / ml. The volume of distribution of paracetamol is 1 l/kg. It crosses the blood-brain barrier and binds weakly to plasma proteins. Paracetamol is biotransformed in the liver with the formation of glucuronides and sulfates, while a small part (about 4%) is metabolized with the participation of isoenzymes of the cytochrome P450 system with the formation of an intermediate metabolite (N-acetylbenzoquinoneimine), which under normal conditions is quickly neutralized by reduced glutathione and excreted in the urine after binding with cysteine and mercaptopuric acid. However, with significant intoxication, the amount of this toxic metabolite increases. The half-life of paracetamol is from 1.25 to 3 hours, and the total clearance is 18 l / h. Paracetamol is excreted mainly in the urine; while 90% of the dose taken is excreted by the kidneys within 24 hours, mainly in the form of glucuronide (60-80%) and sulfate (20-30%), less than 5% is excreted unchanged. Phenylephrine hydrochloride is characterized by low oral bioavailability (38%) due to significant destruction in the gastrointestinal tract. The concentration-time curve corresponds to an open two-compartment model. The volume of distribution in the equilibrium state many times exceeds the body weight, which indicates the accumulation of the substance in certain organs. The volume of central distribution of phenylephrine in humans is approximately 40 liters. When taken orally, phenylephrine undergoes first pass metabolism in the liver to form phenolic conjugates. 86% of the substance is excreted in the urine approximately 48 hours after a dose, while 2.6% is in the form of free amines. Pheniramine after oral administration is rapidly absorbed, and the maximum serum concentrations of the substance are determined 2 hours after oral administration. The half-life of the drug (16-19 hours) is comparable to that characteristic of chlorpheniramine. The volume of distribution of pheniramine reaches 150 liters. The drug is metabolized in the liver to N-desmethylpheniramine and N-didesmethylpheniramine. Up to 80% of the oral dose is excreted in the urine (up to 40% in unchanged form). Indications for use Short-term symptomatic treatment of colds, rhinitis, nasopharyngitis and influenza-like conditions in adults and children aged 15 years and older, accompanied by clear nasal discharge and watery eyes, sneezing, headache and / or fever. Method of application and doses Adults are prescribed 1 tablet 3-4 times / day with intervals between doses of at least 4-6 hours. The maximum daily dose is 4 tablets. The course of treatment is no more than 5 days. Use during pregnancy and lactation The drug is contraindicated during pregnancy. Paracetamol and chlorpheniramine – category A (according to FDA classification): the use of these drugs does not lead to an increase in the incidence of malformations or other direct or indirect harmful effects on the fetus. Paracetamol crosses the placental barrier. Animal studies with paracetamol did not reveal any risk to pregnancy or embryonic and fetal development. Adequate and well-controlled studies with the use of chlorpheniramine in pregnant women have not been conducted, although it has been described that neonates whose mothers received antihistamines during the last two weeks of pregnancy developed retrolental fibroplasia (RLF). Pregnant women should limit their caffeine intake. The drug is not recommended during breastfeeding. Paracetamol is excreted in breast milk. Studies in humans with paracetamol have shown no risk in breastfeeding. Chlorpheniramine and other antihistamines may suppress lactation and may be excreted into breast milk. Caffeine passes into breast milk and can cause agitation and sleep disturbance as it is slowly eliminated from the body of infants. Phenylephrine is excreted in breast milk and is strictly contraindicated in nursing mothers. Precautions In case of ongoing febrile syndrome against the background of using the drug for more than 3 days and pain syndrome for more than 5 days, you should consult a doctor. You should also consult your doctor if symptoms include a sore throat that does not go away for more than 3 days, with fever, headache, rash, nausea, or vomiting. The simultaneous use of other medicinal products containing paracetamol should be avoided. When using the drug, it is not recommended to drink alcoholic beverages, since ethyl alcohol while taking paracetamol can cause liver dysfunction. You should always consult your doctor before using this drug in patients with the following conditions: hypertension cardiovascular disease diabetes hyperthyroidism increased intraocular pressure (glaucoma) pheochromocytoma enlarged prostate vascular obliterans (such as Raynaud’s phenomenon) epilepsy bronchitis bronchiectasis bronchial asthma liver and kidney disease. Caution should be exercised in patients with kidney problems and in patients with hepatic insufficiency, due to the fact that this agent contains paracetamol and chlorpheniramine, which increase the risk of paracetamol-related liver damage. Patients who have been diagnosed with liver or kidney failure should consult a doctor before taking this medicine. Chlorpheniramine may potentiate the effects of alcohol and therefore concomitant use should be avoided. Simultaneous use with drugs that cause sedation, such as tranquilizers and hypnotics, can lead to an increase in sedation, so you should consult a doctor before taking chlorpheniramine concomitantly with these drugs. LS Rinzip® should not be used with other antihistamines. The elderly are more likely to experience neurological anticholinergic effects and paradoxical arousal (eg, restlessness, nervousness). When taking chlorpheniramine late in the evening, the symptoms of gastroesophageal reflux may increase. When chlorpheniramine is used in combination with ototoxic agents, symptoms of ototoxicity may be masked. Phenylephrine may contribute to false positive doping control results in athletes. With caution: advanced age, concomitant use with antihypertensive drugs. Keep out of the reach of children. Interaction with other drugs Paracetamol Coumarins (including warfarin). The anticoagulant effect can be enhanced with long-term regular daily use of Rinzip®. A single occasional dose has no effect. It may be necessary to reduce the dose of anticoagulants if long-term treatment with Rinzip® is necessary. Prokinetics (metoclopramide). Increase the absorption of paracetamol. Cholinolytics (propantheline, antidepressants with anticholinergic properties, narcotic analgesics). Reduce the absorption of paracetamol. Chloramphenicol. The concentration of paracetamol is increased. Hepatotoxic drugs or drugs that stimulate liver enzymes (alcohol, anticonvulsants). The risk of paracetamol toxicity may be increased. Probenecid. Changes the concentration of paracetamol. Colestyramine. Reduces the absorption of paracetamol if administered within one hour before or after ingestion. Treatment of tuberculosis with rifampicin and isoniazid increases the hepatoxicity of paracetamol. Chlorpheniramine Monoamine oxidase inhibitors. Enhance the anticholinergic effects of chlorpheniramine. Sleeping pills and anxiolytics, alcohol. Increases drowsiness. Phenytoin. May increase toxicity. Potentiates the action of antiparkinsonian and antipsychotic drugs, inhibits the action of anticoagulants and interacts with progesterone, reserpine, thiazide diuretics. Oral contraceptives may reduce the effectiveness of antihistamines. Phenylephrine should be used with caution: Monoamine oxidase inhibitors (including moclobemide). risk of developing hypertension. Sympathomimetic amines. Risk of cardiovascular reactions. Beta-blockers and antihypertensives (debrizoquine, guanethidine, reserpine, methyldopa). Reduces efficiency. The risk of hypertension and other cardiovascular reactions may be increased. Tricyclic antidepressants (eg amitriptyline). May increase the risk of cardiovascular reactions. Ergotamine and methysergide. Increased risk of ergotism. Digoxin and cardiac glycosides. Increased risk of arrhythmia or myocardial ischemia. Contraindications Hypersensitivity to the components of the drug; diseases of the cardiovascular system (severe forms of coronary heart disease, myocardial infarction, unstable angina pectoris, stenosis of the aortic mouth, severe atherosclerosis, cardiac arrhythmias, decompensated heart failure, uncontrolled arterial hypertension); severe renal dysfunction and / or liver; congenital hyperbilirubinemia (Gilbert, Dubin-Johnson, Rotor syndrome); glucose-6-phosphate dehydrogenase deficiency; alcoholism, epilepsy; erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, acute pancreatitis; pheochromocytoma; hyperthyroidism; diabetes mellitus; angle-closure glaucoma; prostatic hypertrophy with urinary retention; diseases of the blood system, severe leukopenia, anemia; vasospastic diseases (Raynaud’s syndrome); bronchial asthma, chronic obstructive pulmonary disease; children under 15 years of age; pregnancy, lactation period; psychomotor agitation, sleep disturbance; do not take concomitantly with monoamine oxidase (MAO) inhibitors and within 2 weeks after discontinuation of MAO inhibitors; do not take simultaneously with other paracetamol-containing drugs, decongestants, agents for the treatment of symptoms of colds and flu; do not take simultaneously with tricyclic antidepressants, beta-blockers, sympathomimetics. Composition Each tablet contains: active ingredients: paracetamol – 325 mg, caffeine – 30 mg, phenylephrine hydrochloride – 10 mg, chlorpheniramine maleate – 2 mg; excipients: Ponceau 4R E 124, anhydrous colloidal silicon dioxide, magnesium stearate, sodium starch glycolate, talc, povidone, corn starch. OverdoseSymptoms caused by paracetamol. Liver damage is possible in adults who have taken 10 g or more of paracetamol. Taking 5 g or more of paracetamol can lead to liver damage if the patient has the risk factors listed below. Risk factors long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. pallor, nausea, vomiting, loss of appetite, and abdominal pain. Liver damage may appear 12 to 48 hours after ingestion. Possible violations of glucose metabolism and metabolic acidosis. In severe poisoning, liver failure can progress to encephalopathy, bleeding, hypoglycemia, cerebral edema, and death. Acute renal failure with acute necrosis, low back pain, hematuria, and proteinuria may develop even in the absence of severe liver damage. Perhaps the appearance of arrhythmias and pancreatitis. Immediate measures are of great importance in the treatment of paracetamol overdose. Patients should be referred urgently to the hospital. Symptoms may be limited to nausea or vomiting and may not be consistent with the severity of the overdose or the risk of organ damage. The provision of assistance should be carried out in accordance with accepted recommendations. Treatment with activated charcoal is effective if the overdose occurs within 1 hour. Plasma concentrations of paracetamol should be measured every 4 hours after ingestion. Treatment with N-acetylcysteine can be used within 24 hours after taking paracetamol, however, the maximum protective effect is achieved when taken in the first 8 hours after taking the drug, after which the effectiveness decreases sharply. If necessary, N-acetylcysteine should be administered to the patient intravenously, in accordance with the established dosing schedule. If the patient is not vomiting, oral methionine may be an alternative. Symptoms caused by potentiation of the parasympathetic action of chlorpheniramine. Additional symptoms may include paradoxical arousal, toxic psychosis, seizures, apnea, dystonic and cardiovascular reactions, which can seriously affect the ability to drive and use machines. With the simultaneous use of sedatives, tranquilizers or alcohol, drowsiness may increase. Overdose symptoms associated with caffeine include: CNS stimulation, nervousness, restlessness, insomnia, agitation, confusion, seizures. From the side of the cardiovascular system: tachycardia, cardiac arrhythmias. From the gastrointestinal tract: abdominal pain. Other: diuresis, redness of the face. Treatment of caffeine overdose is mostly symptomatic and supportive. With increased urination, it is necessary to maintain water and electrolyte balance, to relieve symptoms from the central nervous system, intravenous administration of diazepam. Phenylephrine Overdose symptoms include increased blood pressure and hypertension-associated reflex bradycardia and arrhythmias. Elevated blood pressure should be treated with an ?-receptor antagonist (phentolamine, prazosin or doxazosin intravenously). A decrease in blood pressure leads to a reflex increase in heart rate, if necessary, this condition can be alleviated by the administration of atropine. Side effects The frequency of possible side effects listed below is defined as follows: Very often (> 1/10) Often (> 1/100 to <1/10) Infrequently (> 1/1000 to <1/100) Rarely (> 1/10) 10,000 to <1/1000) Very rare (< 1/10,000) Not known (cannot be estimated from the available data) Paracetamol (frequency of reactions not determined, but usually rare). From the hematopoietic and lymphatic system: thrombocytopenia. From the immune system: anaphylaxis; skin hypersensitivity reactions, including skin rash, Quincke's edema and Stevens-Johnson syndrome. On the part of the respiratory system: bronchospasm in patients sensitive to aspirin and other NSAIDs. From the hepatobiliary system: liver dysfunction. Chlorpheniramine From the immune system: not known - allergic reactions, Quincke's edema, anaphylactic reactions. From the digestive system: not known - anorexia. From the side of the central nervous system: not known - confusion*, agitation*, irritability*, nightmares*. Very often - lethargy, drowsiness, impaired attention and coordination, dizziness, headache Often - blurred vision, mydriasis, paresis of accommodation, increased intraocular pressure. From the cardiovascular system: not known - hypotension, tachycardia and arrhythmia. From the respiratory system: not known - increased viscosity of bronchial secretions. From the digestive system: often - nausea, dry mouth, vomiting, abdominal pain, diarrhea, dyspepsia. For the skin: not known - exfoliative dermatitis, rash, urticaria, photosensitivity. From the musculoskeletal system: not known - muscle twitching, muscle weakness. From the excretory system: not known - urinary retention. General disorders: often - fatigue, a feeling of tightness in the chest. * Children and the elderly are more susceptible to neurological anticholinergic effects and paradoxical arousal (eg, agitation, anxiety, nervousness). Phenylephrine The following side effects have been observed in clinical trials with phenylephrine and are therefore the most commonly reported side effects. From the side of the cardiovascular system: increased blood pressure. From the digestive system: nausea, vomiting. From the side of the central nervous system: nervousness, irritability, anxiety and excitability, headache, dizziness, insomnia. Adverse reactions identified during post-marketing use are listed below. The frequency of these reactions is not known, but they are likely to be very rare. From the side of the cardiovascular system: tachycardia, palpitations. From the excretory system: dysuria, urinary retention (in patients with prostatic hyperplasia). From the skin: allergic reactions (eg, rash, urticaria, allergic dermatitis). Cross sensitivity to other sympathomimetics. Disorders of the organ of vision: mydriasis, acute and angle-closure glaucoma. Caffeine From the side of the central nervous system: nervousness, dizziness. When the recommended dosage regimen is combined with dietary caffeine intake, higher doses of caffeine may increase the potential for caffeine-related side effects such as insomnia, restlessness, anxiety, irritability, headaches, gastrointestinal disturbances, and palpitations. Storage conditions In a place protected from light and moisture, at a temperature not exceeding 25 ° C. Keep out of the reach of children. Buy Rinzip tablets No. 10x1 Price for Rinzip tablets No. 10x1