Pentalgin neo composition. Pentalgin ®

Prohibited during pregnancy

Prohibited while breastfeeding

Forbidden to children

Has restrictions for the elderly

Has limitations for liver problems

Has limitations for kidney problems

Majority pathological processes arising in the body are accompanied by the appearance of a pronounced pain syndrome. With the ineffectiveness of monocomponent drugs, it becomes necessary to use stronger combined agents containing an analgesic and substances that enhance and prolong its action. Popular in our country is Pentalgin N.

General information about the drug

The choice of analgesic drug is influenced by factors such as the mechanism of pain (somatogenic, neurogenic or psychogenic), individual characteristics the patient's body, the presence concomitant diseases. Combined analgesics have a number of pronounced clinical effects: analgesic, anti-inflammatory, antipyretic, sedative, antispasmodic.

Drug group, INN, scope

According to the International Anatomical Therapeutic Classification medical preparations Last revision, Pentalgin N belongs to the group "N02 Analgesics", a subgroup - combinations of metamizole sodium with psycholeptics. Pharmacological group- non-steroidal anti-inflammatory drugs, combinations of propionic acid derivatives.

According to the international recommendations of the World Health Organization for stepwise pain therapy, Pentalgin N is used at the 2nd stage with the ineffectiveness of non-opioid monocomponent drugs - salicylates, paracetamol and other NSAIDs.

Forms, composition and prices for the drug, average in Russia

Pentalgin N is produced by the Russian company Pharmstandard in tablet form. For round tablets white color(slightly beige shade is allowed) on one side there is a dividing strip. Carton packs contain one or two blisters with 10 tablets. Since June 2012, all codeine-containing drugs are dispensed only with a prescription from a doctor.

The active ingredients that have a therapeutic effect are:

  1. () - 0.3 g.
  2. Caffeine-sodium benzoate - 50 mg.
  3. Codeine phosphate - 8 mg.
  4. Naproxen - 0.1.
  5. Phenobarbital - 10 mg.

To shape and protect the components from premature splitting when exposed to the aggressive environment of the gastrointestinal tract, Pentalgin N includes potato starch, sodium citrate, lactose monohydrate, microcellulose, magnesium stearate, povidone-iodine.

Unlike tablets with codeine, you can buy ordinary Pentalgin without a prescription. The composition of the Pentalgin preparation includes paracetamol (an analgesic), naproxen (NSAIDs), drotaverine (an antispasmodic), pheniramine ( antihistamine), caffeine (psychostimulant).

Pharmacodynamics and pharmacokinetics

As the main active substance acts metamizole sodium, commonly known as analgin. The mechanism of action is associated with blocking the activity of the cyclooxygenase enzyme, which reduces the concentration of inflammatory mediators - prostaglandins, kinins. It also has a regulatory effect on lipid peroxidation reactions, disrupts the conduction of pain impulses along nerve fibers increases heat transfer.

Naproxen is a non-steroidal anti-inflammatory drug with antipyretic, analgesic, and antiplatelet properties. Non-selectively reduces the action of COX type 1 and 2, which leads to inhibition of the synthesis of arachidonic acid and other prostaglandin precursor products. Also, naproxen reduces the aggregation properties of platelets and reduces the migration of leukocytes.

The sedative and weak hypnotic effect of Pentalgin N is due to the presence of phenobarbital (a derivative of barbituric acid) in the composition. It reduces the excitability of the central nervous system due to competitive binding to the barbituric receptors of neurons, and also increases the concentration of GABA (inhibitory neurotransmitter).

Caffeine not only enhances the analgesic and anti-inflammatory effects of naproxen and analgin, but also has a general tonic and psychostimulant effect. This is due to the blocking of central and peripheral adenosine receptors, inhibition of phosphodiesterase activity, and stabilization of transmission in dopaminergic synapses.

Codeine is an opioid receptor agonist. Enhances analgesic action of NSAIDs by stimulating the antinociceptive system. Able to influence the perception of pain by a person.

Indications and contraindications

The drug has a pronounced effect on somatic, neurogenic pain of varying intensity. Most often, Pentalgin N is prescribed in the presence of the following symptoms and diseases:

Pentalgin N is used for colds, acute respiratory diseases to relieve cough and fever.

Use the drug for people suffering from arterial hypertension, ischemic disease heart, heart failure, as well as those who have had myocardial infarction and stroke are prohibited.

Contraindications to the appointment of Pentalgin N are also:

  • individual intolerance to one of the components;
  • gastritis, stomach ulcer and/or duodenum;
  • bronchial asthma;
  • traumatic brain injury;
  • increased intracranial and intraocular pressure;
  • hepatic and kidney failure;
  • violations heart rate.

Use during pregnancy is contraindicated due to possible teratogenic effects. If it is necessary to take the drug, a nursing woman should stop breastfeeding for 48 hours after taking the tablets. Prescribing the drug to children under 14 years of age is strictly prohibited.

Instructions for use

Before prescribing Pentalgin N, you should carefully read the instructions for use. In addition to the correct calculation of the dosage, it is important to familiarize yourself with the list side effects that may occur during therapy in order to pay attention to them in a timely manner and consult a specialist.

Features of administration and dosage

The tablets are intended for oral administration. They can not be crushed, chewed and absorbed. Drink only clean water, since juices, tea, coffee can disrupt pharmacological properties drug and cause side effects.

Usually this medicine used for the relief of acute pain syndrome once. However, if there is a need for longer therapy, the benefits and risks of taking these tablets should be evaluated.

The maximum course of treatment is 5 days. You can drink no more than 4 tablets per day, while the minimum time interval between doses is 4-5 hours.

Possible side effects and overdose

With intolerance to the drug, the development of adverse reactions is possible. They are accompanied by violation general condition- Excessive drowsiness, irritability, lethargy. When taking Pentalgin, the following undesirable effects may develop:

  • headache;
  • tachycardia;
  • skin itching, rash;
  • indigestion (diarrhea, constipation, feeling of heaviness in the intestines);
  • toxic hepatitis with an increase in liver tests;
  • feeling of nausea, vomiting that does not bring relief;
  • anemia and leukopenia.

When using large doses of the drug, an overdose may occur. Its main manifestations include:

  • respiratory failure, bronchospasm;
  • pain in the epigastric region;
  • vomit;
  • violation of the heart rhythm.

If these symptoms occur, it is necessary to immediately wash the stomach, drink a sufficient amount of liquid and take sorbents.

drug interaction

AT complex therapy it is important to consider the compatibility of the tool:


Analogues

Pharmstandard company ( Russian Federation) produces several varieties of the drug:


A cheap analogue of Pentalgin N is Plivalgin, the manufacturer is Pliva Horvatska, the Croatian Republic. It has a pronounced antipyretic, antianginal and anti-inflammatory effect due to the combination of NSAIDs (propyphenazone), caffeine, phenobarbital and codeine in it. The cost of packing 10 tablets is an average of 240-250 rubles.

The combined analgesics-antipyretics with codeine, often used in our country, include Sedal-M. It is produced by the Bulgarian pharmaceutical company Sopharma. Contains in its composition two NSAIDs - analgin (150 mg) and paracetamol (300 mg). The action of these substances is enhanced by caffeine, codeine, phenobarbital. The average price in Moscow for package No. 10 is 287-290 rubles.

Pentalgin-N is a combined drug intended for the treatment inflammatory diseases accompanied by pain syndrome.

What is the composition and form of release of Pentalgin-N?

The active ingredients in Pentalgin-N are represented by the following compounds: metamizole sodium - 300 milligrams, caffeine - 50 mg, naproxen - 100 mg, phenobarbital - 10 mg, codeine phosphate, the content of which is 8 mg. Auxiliary components of the pharmaceutical product: potato starch, sodium citrate, in addition, polyvinylpyrrolidone, magnesium stearate.

The drug Pentalgin-N is available in flat white tablets with a slight creamy tint, on one side of which is the designation "PENT-N". One package contains 10 tablets. The medicine is dispensed upon presentation of a prescription.

What is the effect of Pentalgin-N?

The drug Pentalgin-N has the following pharmacological actions: analgesic (pain reliever), antipyretic and anti-inflammatory. The action of a pharmaceutical product is determined by a complex chemical composition.

Metamizole sodium is a derivative of pyrazolone, the mechanism of its action is based on the inactivation of the cyclooxygenase enzyme, which is responsible for the biosynthesis of prostaglandins from precursors.

A decrease in the amount of prostaglandins in the central nervous system leads to blocking of the processes of transmission and generation of electrical impulses in some structures of the central nervous system responsible for the formation of pain.

A characteristic feature of metamizole sodium is practically complete absence anti-inflammatory action due to destruction medicinal substance, enzymes contained in peripheral tissues.

Naproxen belongs to the group of non-steroidal anti-inflammatory drugs. The mechanism of action of this component of the drug is associated with the suppression of reactions of formation of inflammatory mediators. Clinically, this is expressed in the suppression of the main symptoms of inflammatory pathology: redness, swelling, soreness, and so on.

Caffeine is a stimulant of the activity of the nervous system, the mechanism of action is based on the expansion blood vessels brain and activation of many metabolic reactions in most structures of the nervous system.

The presence of caffeine in the preparation serves several purposes. Firstly, it can increase the bioavailability coefficient of non-narcotic analgesics, acting as their synergist (increases the effect).

Secondly, it improves the functional state of the nervous system, increases efficiency, stimulates mood, suppresses migraine headaches, helps to relieve depressive mood.

Codeine is an opioid receptor stimulant that can activate many parts of the antinociceptive system, which modifies the perception of pain. This component potentiates the analgesic effect of other components of the drug Pentalgin-N.

All components of the drug are well absorbed from the intestine. The therapeutic concentration of most of them is formed after a few hours. In the excretion processes, for the most part, it is involved excretory system.

What are the indications for use of Pentalgin-N?

Tablets Pentalgin-N instructions for use allows you to use in medicinal purposes in the presence of pain syndrome varying degrees severity (mild to moderate). Below is a list of conditions under which medication is possible:

Feverish conditions of infectious etiology;
Headache;
Migraine;
Pain in joints and muscles;
Toothache.

Before using the pharmaceutical, you should visit a specialist, since the list of conditions prohibiting the use of this medication is quite voluminous.

What are the contraindications for Pentalgin-N?

The instructions for use do not allow taking Pentalgin-N (tablets) for medicinal purposes in the following cases:

severe renal failure;
Stomach ulcer;
Liver failure;
Bronchial asthma and bronchospastic phenomena;
Arterial hypertension;
Pregnancy;
Heart rhythm disturbances;
Alcohol intoxication;
Acute myocardial infarction;
Respiratory depression of any etiology;
Glaucoma;
Increased sensitivity.

In addition, inhibition of bone marrow hematopoiesis.

What is the use of Pentalgin-N? What is the dosage of Pentalgin-N?

It is recommended to use the medicine 1 tablet 3 times a day. The maximum daily dosage is 4 tablets. As a pain reliever maximum duration treatment should be 5 days. As an antipyretic drug, you can use it for up to 3 days. If the symptoms of the disease persist in the specified period of time, you need to stop taking the drug and seek help from a specialist.

Pentalgin-N - drug overdose

The symptoms are: severe pain in the abdomen, vomiting, headache, weakness, delirium, palpitations, shortness of breath. Treatment is symptomatic and should be aimed at maintaining the vital functions of the body. During the first two hours after ingestion, gastric lavage is recommended.

What are the side effects of Pentalgin-N?

Taking Pentalgin-N medication can cause the following side effects: drowsiness, dizziness, weakness, allergic reactions, nausea, constipation, vomiting, drug-induced hepatitis, cardiac arrhythmias, allergic reactions.

special instructions

Professional athletes competing high level should refrain from using this pharmaceutical product as it may lead to false positive doping tests.

In addition, all patients whose activities are associated with an increased risk should refrain from work or exercise extreme caution, since some components of the drug may cause lethargy and drowsiness.

How to replace Pentalgin-N, what analogs to use?

Piralgin.

Conclusion

I remind you that the terms of use of the drug are strictly regulated. If the drug is ineffective, do not increase the dosage or prolong therapeutic measures. In this case, you need to seek professional help.

The combined drug has analgesic, antipyretic and anti-inflammatory effects.

Metamizole sodium is an analgesic-antipyretic, a derivative of pyrazolone. It has a pronounced analgesic effect.

Naproxen - NSAIDs, has anti-inflammatory, analgesic and antipyretic effects associated with non-selective suppression of COX activity, which regulates the synthesis of prostaglandins.

Caffeine causes vasodilation of skeletal muscles, brain, heart, kidneys. Increases mental and physical performance, helps eliminate fatigue and drowsiness. Increases the permeability of histohematic barriers and increases the bioavailability of non-opioid analgesics, thereby enhancing the therapeutic effect.

Codeine stimulates opioid receptors in various departments CNS, which leads to the activation of the antinociceptive system and a change in the emotional perception of pain.

Phenobarbital and codeine increase the analgesic effect of metamizole sodium and naproxen.

Pharmacokinetics

The components of the drug are well absorbed in the gastrointestinal tract.

Metamizole sodium

In the intestinal wall, it is hydrolyzed to form the active metabolite, 4-methyl-amino-antipyrine, which in turn is metabolized to 4-formyl-amino-antipyrine and other metabolites. The binding of the active metabolite to proteins is 50-60%. Metabolites are excreted by the kidneys and excreted in breast milk.

Naproxen

Bioavailability is 95%. Binds to blood proteins. T 1 / 2 - 12-15 hours. Excreted in the urine mainly as a metabolite (dimethylnaproxen), in small quantities - with bile.

Well absorbed in the intestines. T 1/2 - 5 hours (sometimes up to 10 hours). It is excreted mainly by the kidneys in the form of metabolites, about 10% - unchanged.

Slightly binds to plasma proteins. Undergoes biotransformation in the liver (10% by demethylation passes into morphine). Excreted by the kidneys (5-15% - unchanged).

Phenobarbital

Bioavailability is 80%. Plasma protein binding - 50%. It penetrates well through the placental barrier. Biotransformed in the liver. The main metabolite has no pharmacological activity. Excreted by the kidneys, incl. 20-25% - unchanged.

Release form

Tablets are white or white with a yellowish or creamy tint, flat-cylindrical, with the abbreviated name of the drug "PENT-N" embossed on one side.

Excipients: potato starch, low molecular weight polyvinylpyrrolidone (povidone), sodium citrate, magnesium stearate.

10 pieces. - cellular contour packings (1) - packs of cardboard.

Dosage

The drug is prescribed for 1 tab. 1-3 times / day. Maximum daily dose- 4 tab.

The drug should not be taken for more than 5 days as an anesthetic and for more than 3 days as an antipyretic without a doctor's prescription.

Overdose

Symptoms: nausea, vomiting, gastralgia, drowsiness, tachycardia, cardiac arrhythmias, delirium, weakness, respiratory depression.

Treatment: induction of vomiting, gastric lavage through a tube, the appointment of adsorbents ( activated carbon), symptomatic therapy aimed at maintaining vital functions.

Interaction

Simultaneous use of the drug with other non-opioid analgesics can lead to increased toxic effects.

Tricyclic antidepressants, oral contraceptives, allopurinol increase the toxicity of metamizole sodium, which is part of the drug.

Barbiturates, phenylbutazone and other inducers of microsomal liver enzymes weaken the action of metamizole sodium.

The simultaneous use of metamizole sodium with cyclosporine reduces the level of the latter in the blood.

Sedatives and tranquilizers enhance the analgesic effect of the drug.

Side effects

From the side digestive system: epigastric pain, nausea, vomiting, constipation; with prolonged use in high doses- impaired liver function.

On the part of the hematopoietic system: rarely - hematopoietic depression (leukopenia, granulocytopenia, agranulocytosis).

From the side of the central nervous system: dizziness, drowsiness.

From the side of cardio-vascular system: heartbeat.

From the urinary system: with prolonged use in high doses - impaired renal function.

Allergic reactions: skin rash, itching, urticaria.

Indications

  • mild and moderate pain syndrome of various origins (including pain in the joints, muscles, sciatica, algomenorrhea, neuralgia, headache, migraine, toothache);
  • febrile conditions, colds and other diseases accompanied by pain and inflammation.

Contraindications

  • severe liver failure;
  • severe renal failure;
  • peptic ulcer stomach and duodenum in the acute phase;
  • bronchial asthma;
  • bronchospasm;
  • anemia, leukopenia;
  • conditions accompanied by respiratory depression;
  • traumatic brain injury;
  • arterial hypertension severe degree;
  • acute infarction myocardium;
  • arrhythmias;
  • alcohol intoxication;
  • glaucoma;
  • deficiency of glucose-6-phosphate dehydrogenase;
  • pregnancy;
  • childhood up to 12 years;
  • hypersensitivity to the components of the drug.

The drug should be used with caution in mild to moderate arterial hypertension. medium degree severity, gastric ulcer and / or duodenal ulcer in remission, as well as in elderly patients.

Application features

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation ( breastfeeding).

If necessary, the appointment of the drug during lactation, breastfeeding should be discontinued.

Application for violations of liver function

The drug is contraindicated for use in severe liver dysfunction.

Application for violations of kidney function

The drug is contraindicated for use in severe renal dysfunction.

Use in children

Contraindication: children under 12 years of age.

Use in elderly patients

The drug should be used with caution in elderly patients.

special instructions

With prolonged (more than 5 days) taking the drug, it is necessary to monitor the picture of peripheral blood and liver function tests.

Taking the drug Pentalgin ® -N can make it difficult to establish a diagnosis in acute abdominal pain syndrome.

Patients with atopic bronchial asthma and hay fever have an increased risk of developing hypersensitivity reactions while taking the drug Pentalgin ® -N.

Against the background of the use of the drug, it is possible to change the results of doping control in athletes.

Influence on the ability to drive vehicles and control mechanisms

When taking the drug Pentalgin ® -N, you should refrain from driving vehicles and engaging in potentially dangerous species activities that require increased concentration of attention and speed of psychomotor reactions.

Pentalgin-N: instructions for use and reviews

Latin name: Pentalginum-N

ATX Code: N02BB72

Active substance: codeine + caffeine + metamizole sodium + naproxen + phenobarbital (codeine + caffeine + metamizole sodium + naproxen + phenobarbital)

Manufacturer: Pharmstandard-Tomskhimfarm, OJSC (Russia)

Description and photo update: 22.11.2018

Pentalgin-N - combination drug with analgesic, antipyretic and anti-inflammatory action.

Release form and composition

Dosage form of Pentalgin-N - tablets: flat-cylindrical, from white to white with a cream or yellowish tint, with the abbreviated name of the drug "PENT-N" printed on one of the sides (in a cellular or non-cellular contour package 10 pcs., in cardboard box 1 or 2 packs).

Composition of one tablet:

  • active substances: analgin (metamisole sodium) - 300 mg, naproxen - 100 mg, caffeine - 50 mg, phenobarbital - 10 mg, codeine (in the form of codeine or codeine phosphate) - 8 mg;
  • auxiliary components: potato starch, low molecular weight povidone (medical low molecular weight polyvinylpyrrolidone), sodium citrate, magnesium stearate.

Pharmacological properties

Pharmacodynamics

The composition of Pentalgin-N includes active substances that have analgesic, antispasmodic, antipyretic, anti-inflammatory and sedative effects.

Metamizole sodium is a derivative of pyrazolone. It has analgesic and antipyretic effects.

Naproxen, being a non-steroidal anti-inflammatory drug, has anti-inflammatory, analgesic and antipyretic properties, which are due to non-selective inhibition of the activity of the cyclooxygenase enzyme responsible for the production of prostaglandins from arachidonic acid.

Caffeine helps to expand the blood vessels of skeletal muscle tissue, heart, brain, kidneys, increase physical and mental performance, reduce fatigue and drowsiness. By increasing the permeability of blood-tissue barriers and increasing the bioavailability of non-narcotic analgesics, caffeine leads to an increase in their therapeutic effect.

Codeine has the property of stimulating opioid receptors in various parts of the central nervous system, leading to the activation of the antinociceptive system and an improvement in the perception of pain at an emotional level.

Phenobarbital and codeine increase analgesic action metamizole sodium and naproxen.

Pharmacokinetics

The active substances of the drug are well absorbed in the gastrointestinal tract.

Some pharmacokinetic characteristics of the active components of Pentalgin-N:

  • metamizole sodium: hydrolyzed in the intestinal wall, forming the active metabolite 4-methyl-amino-antipyrine, which is metabolized, in turn, to 4-formyl-amino-antipyrine and other metabolites. 50-60% of the active metabolite binds to plasma proteins. The substance can penetrate into breast milk. Metabolites are excreted in the urine;
  • naproxen: bioavailability is 95%, binds to plasma proteins. The half-life (T1 / 2) is from 12 to 15 hours. It is excreted mainly by the kidneys in the form of a metabolite (dimethylnaproxen), with bile - in small quantities;
  • caffeine: well absorbed in the intestines. T1 / 2 is 5 hours (in some cases - up to 10 hours). It is excreted mainly in the urine in the form of metabolites, unchanged - approximately 10%;
  • phenobarbital: bioavailability - about 80%, about 50% binds to plasma proteins. It has the ability to penetrate the placental barrier well. Metabolism occurs in the liver with the formation of metabolites, the main of which has no pharmacological activity. Excreted in the urine, including unchanged, - 20-25%;
  • Codeine: It binds insignificantly to plasma proteins. Metabolized in the liver. By demethylation, 10% of the substance is converted to morphine. It is excreted mainly by the kidneys, unchanged - 5-15%.

Indications for use

  • pain syndrome of various origins of mild to moderate severity (including headache, neuralgia, migraine, muscle and joint pain, sciatica, toothache, algomenorrhea);
  • colds and other diseases accompanied by fever, inflammation and pain.

Contraindications

Absolute:

  • severe renal and / or liver dysfunction;
  • anemia, leukopenia;
  • bronchial asthma, bronchospasm;
  • respiratory depression;
  • gastric and / or duodenal ulcer in the acute stage;
  • severe degree of arterial hypertension;
  • acute myocardial infarction;
  • arrhythmias;
  • traumatic brain injury;
  • glaucoma;
  • deficiency of glucose-6-phosphate dehydrogenase;
  • state of alcoholic intoxication;
  • children's age up to 12 years;
  • pregnancy, lactation;
  • increased individual sensitivity to any component that is part of Pentalgin-N.

Relative (the use of the drug requires caution):

  • arterial hypertension of mild and moderate severity;
  • peptic ulcer of the stomach and / or duodenum in remission;
  • elderly age.

Instructions for use Pentalgin-N: method and dosage

Pentalgin-N tablets are taken orally.

Side effects

  • from the side of the central nervous system: dizziness, drowsiness;
  • from the digestive system: nausea, vomiting, pain in the epigastric region, constipation; with prolonged use of high doses - violations of the functioning of the liver;
  • from the side of the cardiovascular system: palpitations;
  • from the hematopoietic system: rarely - hematopoietic disorders (granulocytopenia, leukopenia, agranulocytosis);
  • from the urinary system: with prolonged use in high doses - impaired functioning of the kidneys;
  • allergic reactions: itching, skin rash, urticaria.

Overdose

With an overdose of Pentalgin-N, the following symptoms may develop: nausea, vomiting, drowsiness, weakness, gastralgia, cardiac arrhythmias, tachycardia, delirium, respiratory depression.

Treatment in case of overdose consists of induction of vomiting, gastric lavage through a tube, the use of adsorbents (eg, activated charcoal), symptomatic therapy aimed at maintaining the functioning of vital organs.

special instructions

While taking Pentalgin-N, it may be difficult to establish a diagnosis in case of acute abdominal pain syndrome.

In patients with pollinosis and atopic bronchial asthma, the risk of developing hypersensitivity reactions increases with the use of the drug.

In the case of prolonged (more than five days) administration of Pentalgin-N, it is necessary to monitor liver function indicators and the picture of peripheral blood.

During the period of use of the drug, the results of doping control in athletes may change.

Influence on the ability to drive vehicles and complex mechanisms

Since Pentalgin-N can cause such adverse reactions, as dizziness and drowsiness, when taking pills, you should refrain from driving vehicles and performing potentially hazardous activities that require increased concentration and a quick psychomotor reaction.

Use during pregnancy and lactation

According to the instructions, Pentalgin-N is contraindicated for use by pregnant and lactating women.

If necessary, the use of the drug during the lactation period, breastfeeding should be discontinued.

Application in childhood

Children under 12 years of age are prohibited from prescribing Pentalgin-N.

For impaired renal function

The drug is contraindicated in patients with severe renal insufficiency.

For impaired liver function

With severe violations of liver function, it is not recommended to prescribe Pentalgin-N.

Use in the elderly

Elderly patients should be careful when taking the drug.

drug interaction

The use of Pentalgin-N simultaneously with some medicines can lead to the development of the following effects:

Keep away from children.

Shelf life - 3 years.

LS-002271

Active substance:

caffeine, codeine, metamizole sodium, naproxen, phenobarbital

Dosage form:

tablets

Composition:

Composition per tablet:

Active substances: metamizole sodium (analgin) - 300 mg, naproxen - 100 mg, caffeine - 50 mg, codeine or codeine phosphate in terms of codeine - 8 mg, phenobarbital - 10 mg.

Excipients: potato starch - 242 mg, low molecular weight povidone (polyvinylpyrrolidone low molecular weight medical) - 9 mg, sodium citrate - 4 mg, magnesium stearate - 7 mg.

Description:

tablets are white or white with a yellowish or creamy tint, flat-cylindrical. On one side of the tablet, the abbreviated name of the drug "PENT-N" is applied by embossing.

Pharmacotherapeutic group:

analgesic (opioid analgesic + non-steroidal anti-inflammatory drug + psychostimulant + barbiturate)

ATH:

  • Metamizole sodium in combination with psycholeptics
  • Pharmacodynamics:

    The combined drug has analgesic, anti-inflammatory and antipyretic effects.

    Naproxen and
    metamizole sodium - have analgesic and anti-inflammatory effects.

    Codeine stimulates opiate receptors in various parts of the central nervous system, which leads to the activation of the antinoceceptive system and a change in the emotional perception of pain.
    Phenobarbital and
    codeine increase the analgesic efficacy of metamizole sodium and naproxen.

    Caffeine causes vasodilation of skeletal muscles, brain, heart, kidneys; increases mental and physical performance, helps to eliminate fatigue and drowsiness; increases the permeability of histohematic barriers and increases the bioavailability of non-narcotic analgesics, thereby enhancing the therapeutic effect.

    Pharmacokinetics:

    The components of the drug are well absorbed in the gastrointestinal tract.

    Metamizole sodium: in the intestinal wall, it is hydrolyzed to form the active metabolite, 4-methyl-amino-antipyrine, which in turn is metabolized to 4-formyl-amino-antipyrine and other metabolites. The level of binding of the active metabolite to proteins is 50-60%. Excretion of metabolites passes through the kidneys. In addition, metabolites are excreted in breast milk.

    Naproxen: bioavailability is 95%. Binds to blood proteins. The half-life is 12-15 hours. It is excreted in the urine mainly as a metabolite (dimethylnaproxen), in small amounts - with bile.

    Caffeine: well absorbed in the intestine, half-life -5 hours (sometimes up to 10 hours). It is excreted mainly by the kidneys in the form of metabolites, about 10% - unchanged.

    Codeine: slightly associated with plasma proteins. Undergoes biotransformation in the liver (10% by demethylation passes into
    morphine). Excreted by the kidneys (5-15% - unchanged).

    Phenobarbital: bioavailability is 80%. In plasma, it binds to proteins by 50% and crosses the placenta well. Biotransformed in the liver. The main metabolite has no pharmacological activity. Excreted by the kidneys, including 20-25% - unchanged.

    Indications for use

    It is taken with mild and moderate pain syndrome of various origins (including pain in the joints, muscles, sciatica, menstrual pain, neuralgia, as well as headaches, migraines, toothaches). It can be used for febrile conditions, colds and other diseases accompanied by pain and inflammation.

    Contraindications

    Hypersensitivity, severe liver and / or kidney failure, peptic ulcer of the stomach and duodenum in the acute stage, bronchial asthma, bronchospasm. Conditions accompanied by respiratory depression. Deficiency of glucose-6-phosphate dehydrogenase; anemia, leukopenia; conditions accompanied by respiratory depression; traumatic brain injury, acute myocardial infarction; arrhythmias, severe arterial hypertension, alcohol intoxication, glaucoma, children's age (up to 12 years).

    Carefully:

    Peptic ulcer of the stomach and duodenum (in remission), old age, mild to moderate arterial hypertension.

    Pregnancy and lactation:

    The drug is contraindicated for use during pregnancy.

    If it is necessary to use the drug during lactation, it is necessary to resolve the issue of stopping breastfeeding.

    Dosage and administration

    The drug is usually taken 1 tablet 1-3 times a day. The maximum daily dose is 4 tablets. The drug should not be taken for more than 5 days as an anesthetic and for more than 3 days as an antipyretic without a doctor's prescription.

    Side effect

    Possible dyspeptic disorders (nausea, vomiting, constipation), skin allergic reactions (rash, itching, urticaria), epigastric pain, dizziness, drowsiness, palpitations. Rarely - oppression of hematopoiesis (leukopenia, granulocytopenia, agranulocytosis). At long-term use in high doses, liver and kidney function may be impaired.

    Overdose:

    Symptoms: nausea, vomiting, stomach pain, tachycardia, cardiac arrhythmias, weakness, drowsiness, delirium, respiratory depression.

    Treatment: induction of vomiting, gastric lavage through a tube, administration of adsorbents (activated charcoal), symptomatic therapy aimed at maintaining vital functions.

    Interaction

    Simultaneous use of the drug with other non-narcotic analgesics can lead to increased toxic effects. Tricyclic antidepressants, oral contraceptives,
    allopurinol increase the toxicity of metamizole sodium (analgin), which is part of the drug. barbiturates,
    phenylbutazone and other inducers of microsomal liver enzymes weaken the action of metamizole sodium (analgin). The simultaneous use of metamizole sodium (analgin) with cyclosporine reduces the level of the latter in the blood. Sedatives and tranquilizers enhance the analgesic effect of the drug.

    Special instructions:

    When used for more than 5 days, it is necessary to control the picture of peripheral blood and functional state liver.

    Due to the presence of codeine and phenobarbital in the preparation, it is possible to obtain positive results when using test systems, including during doping control.

    It makes it difficult to establish a diagnosis in acute abdominal pain syndrome.

    In patients suffering from atopic bronchial asthma, hay fever, there is an increased risk of developing hypersensitivity reactions.

    Influence on the ability to drive a vehicle:

    Due to the possibility of developing a sedative effect, during treatment it is not recommended to drive vehicles and engage in other potentially hazardous activities that require increased concentration of attention, speed of psychomotor and motor reactions.

    Release form:

    tablets.

    Package:

    10 tablets in a blister pack.

    1 or 2 blisters with instructions for use in a carton pack.

    Storage conditions:

    Store at a temperature not exceeding 25 °C. Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiry date stated on the packaging.

    Conditions for dispensing from pharmacies:

    Without recipe

    Registration certificate holder:

    Registration Certificate Holder: OTICEPHARM JSC

    Manufacturer

    PHARMSTANDART-LEKSREDSTVA, JSC Russia

    Representation: