Pentased

Pentased is a medication with antipyretic and analgesic effects. Its therapeutic effect is provided by the activity of the active ingredients.

Paracetamol is a non-narcotic analgesic with antipyretic and analgesic activity. [1]

The propyphenazone component also has an intense analgesic and antipyretic effect. [2]

Codeine also has analgesic properties.

Phenobarbital demonstrates a hypnotic, sedative, and also a weak muscle relaxant effect.

Caffeine has analeptic activity.

Indications Pentased

It is used for moderate and mild pains of various origins: dental, muscle, headache, menstrual or joint pain , as well as neuralgia . May be prescribed in case of a febrile condition associated with flu or colds.

Release form

The drug is produced in tablets - 10 pieces inside a blister pack. The box contains 1 such package.

Pharmacodynamics

The effect of paracetamol is provided by the suppression of the binding of PG and other inflammatory and pain mediators (mainly within the central nervous system). Also, the substance weakens the excitability of the thermoregulatory center of the hypothalamus.

The effects of propiphenazone are also associated with blocking the binding of PGs (mainly within the central nervous system). When administered in large portions, the component demonstrates anti-inflammatory, and at the same time moderate antispasmodic activity.

Codeine promotes the excitation of opiate endings within different parts of the central nervous system, as well as peripheral tissues, as a result of which the activity of the antinociceptive system is stimulated and the emotional sensation of pain is reduced. Together with this, the element has a central antitussive effect, inhibiting the excitatory activity of the cough center.

Phenobarbital suppresses the activity of the central nervous system and reduces the emotional response to pain stimuli.

Caffeine stimulates psychomotor cerebral centers, potentiates the effect of analgesics, relieves fatigue along with drowsiness, and also increases intellectual and physical performance.

Pharmacokinetics

Paracetamol is absorbed at high speed inside the digestive system and synthesized with intraplasmic protein. The half-life is 1-4 hours. Intrahepatic metabolic processes contribute to the formation of paracetamol sulfate and glucuronide. Excretion is realized through the kidneys, mainly in the form of conjugation elements; up to 5% of the component is excreted unchanged.

Caffeine is well absorbed inside the intestines. Metabolic processes are carried out inside the liver. Excretion is carried out in the urine (10% unchanged).

Phenobarbital is fully absorbed, but at a low rate. Metabolic processes are carried out inside the liver; the component induces intrahepatic microsomal enzymes. The half-life is 3-4 days. Excretion is carried out through the kidneys in the form of non-active metabolic elements (25-50% of the substance is excreted unchanged). Phenobarbital crosses the placenta without complications.

The lipophilicity of codeine allows it to overcome the BBB at a high speed and accumulate inside adipose tissues, as well as, less voluminously, inside tissues with a high perfusion rate (kidneys with lungs, spleen and liver). Codeine hydrolysis is carried out with the participation of tissue esterases (the methyl category is cleaved off) with further intrahepatic conjugation with glucuronic acid. The metabolic elements of codeine have their own analgesic effects. Excretion of codeine occurs to a greater extent in the urine; significantly smaller volumes of metabolic components synthesized with glucuronic acid are excreted in the bile. In persons with insufficient renal function, the accumulation of active metabolic elements is possible, due to which the therapeutic effect of drugs is prolonged.

Propyphenazone at high speed, is fully absorbed when taken orally. Metabolic processes take place mainly inside the liver; in this case, N-desmethylpropyphenazone is formed. Excretion of propyphenazone occurs in the urine - mainly in the form of a conjugate of glucuronic acid. The substance crosses the placenta and is excreted in breast milk. In case of insufficiency of renal / liver function, metabolic processes and excretion of propyphenazone may be suppressed.

Dosing and administration

An adult needs to take 1-2 tablets 1-3 times a day with plain water. Recommended to be consumed after meals.

Teenagers from 12 years old are required to use a 0.5-1-well tablet 1-2 times per day.

Children can use a maximum of 3 tablets per day, and adults - 6 tablets (for 3-4 uses).

The duration of the treatment cycle is determined by the tolerability and effectiveness of the treatment. It often lasts a maximum of 5 days (for pain) or 3 days (for febrile conditions).

• Application for children

The medicine is not prescribed to persons under the age of 12.

Use Pentased during pregnancy

Pentaced is not used for lactation or pregnancy.

Contraindications

Among the contraindications:

• severe intolerance associated with the elements of the drug, and in addition to pyrazolone or related ligaments (includes aminophenazone and phenazone with metamizole and propyphenazone), phenylbutazone, aspirin and opioid pain relievers;
• failure of liver / kidney function in a severe stage;
• lack of G6FD component;
• leuko- or granulocytopenia, as well as anemia and agranulocytosis;
• respiratory pathologies in which obstruction and dyspnea are noted (this includes conditions against which respiratory depression is observed, and asthma);
• an increase in ICP indicators;
• glaucoma;
• a strong decrease in blood pressure or an increase in it;
• myocardial infarction in the active phase;
• intoxication with alcohol or alcoholism;
• pancreatitis;
• increased excitability and sleep disorders;
• active porphyria;
• congenital hyperbilirubinemia;
• drug or drug addiction (also its presence in the anamnesis);
• diabetes;
• epilepsy;
• blood pathology;
• myasthenia gravis;
• hypertrophy of the prostate;
• organic lesions of the CVS (cardiac conduction disorders, decompensated heart failure, severe atherosclerosis, a tendency to develop vascular spasms and ischemic heart disease);
• thyrotoxicosis;
• depressive disorders, in which there is a tendency to suicidal behavior, or depression;
• elderly age;
• the time interval after the operation in the area of the bile ducts;
• head injury;
• introduction together with MAOI, as well as use within 14 days from the moment of termination of their intake;
• appointment to persons using β-blockers or tricyclics.

Side effects Pentased

With the development of negative signs, you need to stop taking the medication and immediately consult a doctor. The use of therapeutic portions usually does not lead to complications. Side symptoms are often associated with the presence of paracetamol in the composition of drugs.

When administered in standard dosages, but together with substances that contain caffeine, it is possible to potentiate the negative signs associated with caffeine. Among them are severe excitability, headaches, disorders in the gastrointestinal tract, dizziness, anxiety, increased heart rate, anxiety, insomnia and irritability. Other manifestations:

• digestive disorders: pain and a feeling of heaviness in the epigastric zone, nausea, constipation and vomiting. Long-term use of the drug in large portions can provoke a hepatotoxic effect. Hepatonecrosis also develops (depending on the size of the portion), xerostomia, dyspepsia, acute pancreatitis in persons with a history of cholecystectomy, ulcers on the oral mucosa and heartburn;
• problems with the work of the hepatobiliary system: jaundice, disorders of hepatic function, including failure of hepatic activity (hepatotoxicity is often associated with paracetamol poisoning), and an increase in the activity of intrahepatic enzymes;
• lesions associated with NS: excitement, which has a paradoxical nature, as well as tremors, dizziness, anxiety and drowsiness, and in addition to this euphoria, confusion, anxiety and fear. There is also a weakening of concentration of attention and the speed of development of motor-psychic reflexes, headaches, sleep disorders, irritability, dysphoria, and at the same time disorientation and psychomotor agitation. Paresthesias, hallucinations, severe fatigue, ataxia, insomnia, depression, nystagmus, cognitive disorders and impaired motor coordination, as well as hyperkinesis (in pediatrics) appear. Sedation and the development of dependence may occur (with prolonged intake of large portions);
• disorders of the cardiovascular system: tachycardia, arrhythmia, palpitations, heart pain, bradycardia and changes in blood pressure indicators (for example, a strong decrease in them);
• disorders affecting the blood structure and lymph: leuko- or granulocytopenia, anemia (hemolytic and pernicious), leukocytosis, agranulocytosis or lymphocytosis, bleeding or bruising, as well as sulf- and methemoglobinemia (dyspnoea, cyanosis and pain in the heart). Prolonged administration of large doses leads to the appearance of neutro-, thrombocyto- or pancytopenia, agranulocytosis or aplastic anemia;
• problems with urinary function: impaired renal function, urinary retention, necrotizing papillitis, renal colic and tubulointerstitial nephritis. Long-term use of large dosages can lead to nephrotoxic effects;
• immune disorders: MEE (this also includes SJS), anaphylaxis, Quincke's edema, symptoms of intolerance, including epidermal itching and rashes on the mucous membranes and skin (often hives or erythematous or generalized rashes), and TEN;
• lesions of the epidermis and subcutaneous layer: purpura, photosensitivity, dermatitis of exfoliative or allergic origin and hemorrhage;
• respiratory symptoms: bronchial spasm in persons with NSAID intolerance;
• others: miosis, impotence, hypoglycemia (can reach hypoglycemic coma), folate deficiency and hyperhidrosis. Prolonged administration increases the likelihood of an osteogenesis disorder. In the case of a sharp cessation of drug intake, a withdrawal syndrome may occur, in connection with which there is an increase in temperature, as well as nervousness, difficulty breathing, the appearance of nightmares and an increase in the size of the lymph nodes.

Overdose

In the case of poisoning with Pentaced, different symptoms may develop, specific to each of its active elements. Usually intoxication is associated with paracetamol.

In people with risk factors (fasting, prolonged use of phenytoin, St. John's wort, carbamazepine, primidone, as well as phenobarbital with rifampicin or other substances that induce liver enzymes, cachexia, alcohol abuse, glutathione structure deficiency, AIDS and cystic fibrosis) when administered 5+ g of paracetamol hepatic impairment may develop.

Overdose causes gastralgia, vomiting, hyperhidrosis, nausea, abdominal pain, blanching of the epidermis, anorexia and hepatonecrosis, and in addition, arrhythmia, suppression of the respiratory center, tachycardia, decreased blood pressure, disorientation and an increase in PTI values or the activity of intrahepatic transaminases.

It should be borne in mind that taking more than 6000 mg of paracetamol can provoke severe hepatic damage, which manifests itself after 12-48 hours from the moment the disorder develops.

The appearance of metabolic acidosis or disorders of glucose metabolism is possible. Severe intoxication can aggravate liver failure, causing the appearance of encephalopathy of a toxic nature, accompanied by a disorder of consciousness. This sometimes leads to death.

ARF, in which there is an active phase of tubular necrosis, can occur in individuals without severe renal impairment. The occurrence of cardiac arrhythmias is also observed. The liver is affected with the introduction of 10+ g of the drug (adult) or 0.15 g / kg (child).

Large portions of caffeine can cause vomiting, pain in the epigastric zone, increased urine output, extrasystole, increased breathing, cardiac arrhythmia or tachycardia. They also affect the function of the central nervous system (irritability, loss of consciousness, affect, convulsions, anxiety, insomnia, tremor and nervous excitement).

Poisoning with propyphenazone leads to damage to the central nervous system (coma and convulsions).

Phenobarbital intoxication causes nystagmus, headaches, nausea, weakness and ataxia, tachycardia, respiratory depression (it can reach a complete stop), a decrease in blood pressure (up to a state of collapse) and suppression of the CVS function (heart rhythm disorders). Large portions lead to a slowdown in the pulse rate, suppression of the action of the central nervous system (up to a coma), a decrease in body temperature and a weakening of urine output.

Severe intoxication causes the progression of liver failure with the development of hemorrhages, coma, encephalopathy and hypoglycemia, with possible subsequent death. With acute renal failure with an active phase of tubular necrosis, hematuria, sharp pain in the lumbar region and proteinuria are noted. This disorder can also occur in people without severe hepatic lesions. There is evidence of the development of pancreatitis and cardiac arrhythmias.

As a result of codeine poisoning, acute suppression of the respiratory center develops, in which there is a slowdown in breathing, cyanosis and drowsiness; occasionally pulmonary edema may occur. In addition, the appearance of apnea, seizures and dyspnea, a decrease in blood pressure and urinary retention are possible.

In case of intoxication with paracetamol, immediate medical attention is required, so the victim must be quickly taken to the hospital. Of the signs, only vomiting with nausea can be observed, or they may not reflect the intensity of poisoning or the severity of damage to internal organs. An option with the intake of activated charcoal may be considered (in the case when less than 60 minutes have passed since the paracetamol overdose). Plasma values of paracetamol should be measured after 4+ hours from the moment of application (earlier values will be unreliable).

The antidotes of paracetamol are the substances methionine with acetylcysteine. Therapy with the use of N-acetylcysteine is allowed to be carried out within 24 hours from the moment of paracetamol administration, but its maximum protective effect develops if taken within a period of up to 8 hours. Later this period, the effect of the antidote is sharply weakened. If necessary, N-acetylcysteine is administered intravenously, in accordance with the selected dosage. In the absence of vomiting, oral methionine is allowed (as an alternative if it is impossible to get to the hospital). In addition, general supporting actions are performed.

Therapy in case of codeine poisoning: symptomatic actions, including procedures that support the activity of the respiratory center: monitoring the basic values of the state of the body (breathing with a pulse, blood pressure and temperature). If respiratory depression occurs or coma develops, naloxone should be used. It is necessary to monitor the condition of the victim for at least 4 hours after admission or 8 hours when carrying out supportive measures.

Interactions with other drugs

Administration together with medications that suppress the action of the central nervous system (hypnotics or sedatives, alcoholic beverages, muscle relaxants and tranquilizers) can mutually potentiate side symptoms (suppression of the respiratory center and central nervous system function, as well as a decrease in blood pressure values).

Use in combination with substances that induce microsome oxidation processes (carbamazepine with salicylamide, barbiturates, nicotine and phenytoin with rifampicin), tricyclics and alcoholic beverages significantly increases the likelihood of hepatotoxic activity.

Combination with drugs that contain paracetamol can lead to poisoning with this element. The combination of paracetamol and hepatotoxic substances (phenytoin, isoniazid, carbamazepine with rifampicin and alcoholic beverages) increases their toxic effects on the liver.

Paracetamol weakens the drug effect of diuretics. When using domperidone, an increase in the rate of absorption of paracetamol may occur.

Administration together with oral anticoagulants (warfarin or acenocoumarol) or NSAIDs can cause the development of side signs from the gastrointestinal tract.

The anticoagulant activity of warfarin and other coumarins is potentiated by prolonged daily use of paracetamol. It also increases the likelihood of bleeding. With periodic use of drugs, significant effects do not develop.

The use of caffeine along with various substances leads to the following disorders:

• procarbazine, MAOIs, selegiline and furazolidone contribute to the appearance of dangerous cardiac arrhythmias or a strong increase in blood pressure;
• pyrimidine, barbiturates and anticonvulsants (hydantaine derivatives, especially phenytoin) lead to potentiation of the metabolic processes of caffeine and an increase in its clearance;
• ciprofloxacin, ketoconazole, enoxacin with disulfiram, as well as pipemidic acid and norfloxacin cause a slowdown in the excretion of caffeine and an increase in its blood values;
• fluvoxamine increases the plasma level of caffeine;
• mexiletine reduces the excretion of caffeine by 50%;
• nicotine increases the rate of caffeine excretion;
• methoxalen reduces the volumes of excreted caffeine, which can lead to potentiation of its effect and the appearance of toxic activity;
• administration with clozapine increases the blood values of this element;
• the combination with β-blockers causes mutual suppression of the drug effect;
• the combination with calcium substances reduces the absorption rate of both agents.

Drugs and drinks that contain caffeine, when combined with Pentaced, can cause excessive stimulation of the central nervous system.

Caffeine potentiates the effect (increasing bioavailability) of antipyretic analgesic drugs, and also enhances the activity of psychostimulants, xanthine derivatives, MAOIs (procarbazine with furazolidone and selegiline) and α- with β-adrenomimetics.

Caffeine weakens the effects of hypnotics, anxiolytics and sedatives; it is an antagonist of anesthetics and other drugs that suppress the action of the central nervous system, and in addition, a competitive antagonist of ATP and adenosine.

The combination of caffeine and ergotamine enhances the absorption of the latter from the gastrointestinal tract; the introduction together with thyroid-stimulating elements increases thyroid activity. Caffeine lowers lithium blood counts. The effect of caffeine is potentiated when combined with isoniazid or hormonal contraception.

Codeine is able to inhibit the effect of domperidone with metoclopramide in relation to gastrointestinal motility. In addition, it potentiates the activity of substances that suppress the function of the central nervous system (among them hypnotics, tricyclics, alcoholic beverages, sedatives, anesthetics and phenothiazine-type tranquilizers), but this interaction has no clinical effect when using the recommended portions.

Phenobarbital causes the induction of intrahepatic enzymes, due to which it can increase the rate of metabolic processes of some drugs, whose metabolism is realized with the help of these enzymes (this includes antimicrobial, hormonal, antiarrhythmic, antiviral and antihypertensive drugs, and in addition anticonvulsants, SG, cytostatics, antimycotics, immunosuppressants, antidiabetic drugs for oral administration and indirect anticoagulants). Phenobarbital also potentiates the activity of local anesthetics, alcoholic beverages, substances that suppress the action of the central nervous system (antipsychotics, anesthetics and tranquilizers), and analgesics.

The combination of phenobarbital and other substances with a sedative effect causes the potentiation of sedative-hypnotic activity, against the background of which respiratory depression can develop. Medicines that have the properties of acids (ammonia and C-vitamin) potentiate the effect of barbiturates. An effect on blood counts of phenytoin, clonazepam and carbamazepine can be expected. MAOIs prolong the therapeutic effect of phenobarbital. Rifampicin is capable of weakening the properties of phenobarbital. Use with gold products increases the likelihood of kidney damage.

Prolonged administration along with NSAIDs can provoke the development of bleeding and gastric ulcers.

The combination of phenobarbital and zidovudine leads to the mutual potentiation of their toxic activity. Phenobarbital is also able to increase the metabolic rate of oral contraception, which is why it loses its therapeutic effect.

Prolonged use of anticonvulsants can weaken the activity of paracetamol.

Re-introduction of paracetamol potentiates the properties of anticoagulants (dicoumarin derivatives).

The use of phenobarbital together with antiarrhythmic drugs causes the potentiation of the antihypertensive effect (sotalol) and an increase in the rate of metabolic processes (mexiletine).

Propyphenazone potentiates the properties of oral hypoglycemic substances, anticoagulants and sulfonamides, as well as the ulcerogenic effect of corticosteroids.

The weakening of the effectiveness of Pentaced is noted when administered simultaneously with anticholinergics, alkaline elements, cholestyramine and antidepressants.

Paracetamol increases the rate of excretion of chloramphenicol; absorption of paracetamol is accelerated by the use of metoclopramide.

Caffeine increases the rate of absorption of ergotamine.

Storage conditions

Pentased is required to be stored in a place closed from the penetration of children. Temperature level - no more than 25 ° С.

Shelf life

Pentaced can be applied within a 2-year term from the date of marketing of the therapeutic substance.

Analogs

Analogues of the drug are Analgin, Piralgin, Tempalgin and Tetralgin with Analdim, Reopirin and Andipal, and in addition Pyatirchatka, Andifen is, Kofalgin and Benalgin. Also on the list are Tempanginol, Benamil, Tempaldol and Pentalgin with Tempimet, as well as Revalgin, Tempanal and Sedalgin plus with Sedal.

Reviews

Pentased is receiving good reviews for its therapeutic efficacy. The medicine helps with various pains, as well as colds. Of the minuses, the unpleasant taste of the tablet and its too large size are noted, which creates some inconvenience in the use of drugs.