Pentaseced

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

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

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

Codeine also has pain-relieving properties.

Phenobarbital exhibits hypnotic, sedative, and weak muscle relaxant effects.

Caffeine has analeptic activity.

Indications Pentaseced

It is used for moderate and mild pain of various origins: toothache, muscle pain, headache, menstrual or joint pain, as well as neuralgia. It can be prescribed in case of feverish condition associated with flu or cold.

Release form

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

Pharmacodynamics

The effect of paracetamol is ensured by the suppression of the binding of PG and other inflammatory and pain mediators (mainly within the CNS). The substance also weakens the excitability of the thermoregulatory center of the hypothalamus.

The effects of propifenazone are also associated with blocking the binding of PG (mainly within the CNS). When administered in large doses, the component demonstrates anti-inflammatory and at the same time moderate spasmolytic activity.

Codeine stimulates opiate endings within different parts of the central nervous system, as well as peripheral tissues, which results in the stimulation of the antinociceptive system and a decrease in the emotional sensation of pain. At the same time, the element has a central antitussive effect, inhibiting the excitatory activity of the cough center.

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

Caffeine helps stimulate psychomotor brain centers, potentiates the effects of analgesics, eliminates the feeling of fatigue along with drowsiness, and also increases intellectual and physical performance.

Pharmacokinetics

Paracetamol is absorbed at high speed within 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 in the intestine. Metabolic processes are realized in the liver. Excretion occurs with urine (10% unchanged).

Phenobarbital is absorbed completely, but at a low rate. Metabolic processes occur inside the liver; the component induces intrahepatic microsomal enzymes. The half-life is 3-4 days. Excretion occurs through the kidneys in the form of inactive 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 high speed and accumulate inside fatty tissues, as well as, to a lesser extent, inside tissues with a high perfusion index (kidneys with lungs, spleen and liver). Codeine hydrolysis is realized with the participation of tissue esterases (the methyl category is split off) with subsequent intrahepatic conjugation with glucuronic acid. Metabolic elements of codeine have their own analgesic effect. Codeine is excreted to a greater extent with urine; significantly smaller volumes of metabolic components synthesized with glucuronic acid are excreted with bile. In individuals with renal insufficiency, accumulation of active metabolic elements is possible, due to which the therapeutic effect of the drug is prolonged.

Propiphenazone is rapidly and completely absorbed when taken orally. Metabolic processes occur mainly in the liver; N-desmethylpropiphenazone is formed. Propiphenazone is excreted in the urine, mainly in the form of a glucuronic acid conjugate. The substance crosses the placenta and is excreted in breast milk. In case of renal/liver dysfunction, metabolic processes and excretion of propiphenazone may be suppressed.

Dosing and administration

An adult should take 1-2 tablets 1-3 times a day with plain water. It is recommended to take it after meals.

Teenagers aged 12 years and over are required to take 0.5-1 tablet 1-2 times per day.

Children can take a maximum of 3 tablets per day, and adults – 6 tablets (in 3-4 doses).

The duration of the treatment cycle is determined by the tolerability and effectiveness of the treatment. Often it lasts a maximum of 5 days (in case of pain) or 3 days (in case of fever).

• Application for children

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

Use Pentaseced during pregnancy

Pentased is not used during lactation or pregnancy.

Contraindications

Among the contraindications:

• severe intolerance associated with the components of the drug, as well as with pyrazolone or related compounds (includes aminophenazone and phenazone with metamizole and propyphenazone), phenylbutazone, aspirin and opioid painkillers;
• severe liver/kidney failure;
• G6PD deficiency;
• leukopenia or granulocytopenia, as well as anemia and agranulocytosis;
• respiratory pathologies characterized by obstruction and dyspnea (this includes conditions that result in respiratory depression and asthma);
• increase in intracranial pressure;
• glaucoma;
• a strong decrease in blood pressure or its increase;
• myocardial infarction in the active phase;
• alcohol intoxication or alcoholism;
• pancreatitis;
• increased excitability and sleep disorders;
• active porphyria;
• congenital hyperbilirubinemia;
• drug or medicinal addiction (also its presence in the anamnesis);
• diabetes mellitus;
• epilepsy;
• blood pathologies;
• myasthenia;
• prostate hypertrophy;
• organic lesions of the cardiovascular system (cardiac conduction disorders, decompensated heart failure, severe atherosclerosis, tendency to develop vascular spasms and coronary heart disease);
• thyrotoxicosis;
• depressive disorders, in which there is a tendency towards suicidal behavior, or depression;
• old age;
• time interval after surgery in the area of the bile ducts;
• head injury;
• administration together with MAOIs, as well as use for 14 days from the moment of stopping their use;
• appointment to persons using β-blockers or tricyclics.

Side effects Pentaseced

If negative symptoms develop, you should stop taking the medication and immediately consult a doctor. Using therapeutic doses usually does not lead to complications. Side effects are often associated with the presence of paracetamol in the drug.

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

• digestive disorders: pain and heaviness in the epigastric region, nausea, constipation and vomiting. Long-term use of the drug in large portions can provoke a hepatotoxic effect. Hepatonecrosis (depending on the portion size), xerostomia, dyspepsia, acute pancreatitis in people with a history of cholecystectomy, ulcers on the oral mucosa and heartburn also develop;
• problems with the hepatobiliary system: jaundice, liver dysfunction, including liver failure (hepatotoxicity is often associated with paracetamol poisoning), and increased activity of intrahepatic enzymes;
• lesions associated with the nervous system: agitation of a paradoxical nature, as well as tremor, dizziness, anxiety and drowsiness, as well as euphoria, confusion, anxiety and fear. Also noted is a weakening of concentration and the rate of development of motor-mental reflexes, headaches, sleep disorders, irritability, dysphoria, as well as disorientation and agitation of a psychomotor nature. Paresthesia, hallucinations, severe fatigue, ataxia, insomnia, depression, nystagmus, cognitive disorders and motor coordination disorders, as well as hyperkinesis (in pediatrics) appear. Sedation and the development of dependence may be observed (with prolonged use of large doses);
• disorders of the cardiovascular system: tachycardia, arrhythmia, palpitations, heart pain, bradycardia and changes in blood pressure (for example, a strong decrease);
• disorders affecting the blood structure and lymph: leukopenia or granulocytopenia, anemia (hemolytic and pernicious), leukocytosis, agranulocytosis or lymphocytosis, bleeding or bruising, as well as sulf- and methemoglobinemia (dyspnea, cyanosis and pain in the heart region). Prolonged administration of large doses leads to the appearance of neutro-, thrombocyto- or pancytopenia, agranulocytosis or anemia of aplastic nature;
• urinary problems: renal dysfunction, urinary retention, necrotic papillitis, renal colic and tubulointerstitial nephritis. Long-term use of high doses may result in nephrotoxic effects;
• immune disorders: MEE (this also includes SJS), anaphylaxis, Quincke's edema, intolerance symptoms, including epidermal itching and rashes on the mucous membranes and skin (often urticaria or erythematous or generalized rashes), and TEN;
• lesions of the epidermis and subcutaneous layer: purpura, photosensitivity, dermatitis of exfoliative or allergic origin and hemorrhages;
• respiratory symptoms: bronchial spasm in individuals with NSAID intolerance;
• Others: miosis, impotence, hypoglycemia (may reach hypoglycemic coma), folate deficiency and hyperhidrosis. Long-term administration increases the likelihood of osteogenesis disorder. In case of abrupt cessation of drug intake, withdrawal syndrome may be observed, due to which an increase in temperature is observed, as well as nervousness, difficulty breathing, the appearance of nightmares and an increase in the size of the lymph nodes.

Overdose

In case of poisoning with Pentased, different symptoms may develop, specific to each of its active ingredients. 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 deficiency, AIDS and cystic fibrosis), liver damage may develop when 5+ g of paracetamol is administered.

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

It should be taken into account that taking more than 6000 mg of paracetamol can provoke severe liver damage, which manifests itself after 12-48 hours from the moment the disorder develops.

Metabolic acidosis or glucose metabolism disorders may occur. Severe intoxication may increase liver failure, causing toxic encephalopathy accompanied by impaired consciousness. Sometimes this leads to death.

ARF, in which the active phase of tubular necrosis is observed, may also occur in individuals without severe renal damage. Cardiac arrhythmia may also occur. The liver is affected when 10+ g of the drug is administered (adult) or 0.15 g/kg (child).

Large doses of caffeine can cause vomiting, pain in the epigastric region, increased diuresis, extrasystole, increased respiratory rate, 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).

Propyphenazone poisoning leads to damage to the central nervous system (comatose state and convulsions).

Phenobarbital intoxication causes nystagmus, headaches, nausea, weakness and ataxia, tachycardia, respiratory depression (may reach complete cessation), decreased blood pressure (up to collapse) and suppression of cardiovascular function (cardiac arrhythmia). Large doses lead to a slowdown in pulse rate, suppression of the central nervous system (up to a comatose state), a decrease in body temperature and a weakening of diuresis.

Severe intoxication causes progression of liver failure with development of hemorrhages, coma, encephalopathy and hypoglycemia, with possible subsequent death. In acute renal failure with active phase of tubular necrosis, hematuria, sharp pain in the lumbar region and proteinuria are observed. Such disorder can also occur in people without severe forms of liver damage. There is data on development of pancreatitis and cardiac arrhythmia.

Codeine poisoning results in acute respiratory depression, with slow breathing, cyanosis, and drowsiness; pulmonary edema may occasionally occur. In addition, apnea, seizures, and dyspnea, decreased blood pressure, and urinary retention may occur.

In case of paracetamol intoxication, immediate medical assistance is required, so the victim must be quickly taken to the hospital. The only symptoms may be vomiting with nausea, or they may not reflect the intensity of poisoning or the severity of damage to internal organs. The option of taking activated charcoal may be considered (if less than 60 minutes have passed since the paracetamol overdose). Plasma paracetamol levels should be measured after 4+ hours from the moment of use (earlier values will be unreliable).

Antidotes to paracetamol are methionine and acetylcysteine. Therapy using N-acetylcysteine is allowed to be carried out within 24 hours from the moment of administration of paracetamol, but its maximum protective effect develops in case of taking it within 8 hours. After 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, methionine can be taken orally (as an alternative if it is impossible to get to the hospital). In addition, general supportive measures are performed.

Therapy in case of codeine poisoning: symptomatic actions, including procedures to support the respiratory center: monitoring the body's basic parameters (breathing with pulse, blood pressure and temperature). If respiratory depression occurs or a comatose state develops, naloxone should be used. The victim's condition should be monitored for at least 4 hours after ingestion or 8 hours when providing 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 effects (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 microsomal 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 containing paracetamol may lead to poisoning with this element. Combination of paracetamol and hepatotoxic substances (phenytoin, isoniazid, carbamazepine with rifampicin and alcoholic beverages) increases their toxic effect on the liver.

Paracetamol weakens the medicinal effect of diuretics. When using domperidone, the rate of absorption of paracetamol may increase.

Administration together with orally administered anticoagulants (warfarin or acenocoumarol) or NSAIDs may cause the development of adverse effects from the gastrointestinal tract.

The anticoagulant activity of warfarin and other coumarins is potentiated by prolonged daily use of paracetamol. This also increases the likelihood of bleeding. No significant effects develop with periodic use of the drug.

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

• procarbazine, MAOIs, selegiline and furazolidone contribute to the development of dangerous cardiac arrhythmias or a strong increase in blood pressure;
• pyrimidine, barbiturates and anticonvulsants (hydantoin derivatives, especially phenytoin) lead to potentiation of caffeine metabolic processes 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 plasma caffeine levels;
• mexiletine reduces caffeine excretion by 50%;
• nicotine increases the rate of caffeine excretion;
• methoxsalen reduces the volume of excreted caffeine, which can lead to a potentiation of its effect and the appearance of toxic activity;
• administration with clozapine increases blood levels of this element;
• combination with β-blockers causes mutual suppression of the drug effect;
• combination with calcium substances reduces the absorption rate of both agents.

Medicines and drinks containing caffeine, when combined with Pentased, may 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- and β-adrenergic agonists.

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

The combination of caffeine and ergotamine enhances the absorption of the latter from the gastrointestinal tract; administration together with thyrotropic elements increases thyroid activity. Caffeine reduces blood lithium levels. The effect of caffeine is potentiated by combination with isoniazid or hormonal contraception.

Codeine can inhibit the effect of domperidone with metoclopramide on gastrointestinal motility. In addition, it potentiates the activity of substances that suppress the function of the central nervous system (including sleeping pills, tricyclics, alcoholic beverages, sedatives, anesthetics and tranquilizers of the phenothiazine type), but such interactions do not have a clinical effect when using the recommended doses.

Phenobarbital causes the induction of intrahepatic enzymes, due to which it can increase the rate of metabolism of some drugs, the metabolism of which is realized with the help of these enzymes (these include antimicrobial, hormonal, antiarrhythmic, antiviral and hypotensive drugs, as well as 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 (neuroleptics, anesthetics and tranquilizers), and analgesics.

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

Long-term administration together with NSAIDs may provoke the development of bleeding and gastric ulcers.

Combining phenobarbital and zidovudine leads to mutual potentiation of their toxic activity. Phenobarbital is also capable of increasing the rate of metabolism of oral contraception, which causes it to lose its therapeutic effect.

Long-term use of anticonvulsants may reduce the activity of paracetamol.

Repeated administration of paracetamol potentiates the properties of anticoagulants (dicumarin derivatives).

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

Propyphenazone potentiates the properties of orally administered hypoglycemic agents, anticoagulants and sulfonamides, as well as the ulcerogenic effect of corticosteroids.

A decrease in the effectiveness of Pentased is observed 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 should be stored in a place closed to children. Temperature level – no more than 25°С.

Shelf life

Pentased can be used within a 2-year period from the date of sale of the therapeutic substance.

Analogues

Analogues of the drug are Analgin, Piralgin, Tempalgin and Tetralgin with Analdim, Reopyrin and Andipal, as well as 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 receives good reviews regarding its therapeutic effectiveness. The medicine helps with various pains, as well as colds. The disadvantages include the unpleasant taste of the tablet and its too large size, which creates some inconvenience in using the medicine.