Pentalgin Neo pills 50mg+220mg+325mg, 20pcs

Composition

Active ingredients: paracetamol – 325.0 mg, naproxen sodium-220.0 mg, caffeine anhydrous-50.0 mg. Auxiliary substances: microcrystalline cellulose (microcrystalline cellulose 101) – 175.50 mg, povidone (polyvinylpyrrolidone medium molecular weight, povidone K-30) – 36.00 mg, croscarmellose (croscarmellose sodium) – 34.00 mg, potato starch-30.00 mg, talc-18.00 mg, magnesium stearate-7.00 mg, colloidal silicon dioxide-4.50 mg. Shell:  Opadray 13 A 200004 VIOLET – 30,000 mg [Hypromellose-2910 (hydroxypropylmethylcellulose-2910) – 14.604 mg, talc-5.061 mg, povidone-4.644 mg, titanium dioxide-2.925 mg, polysorbate-80-1.320 mg, dye carmine red (carmine 50%) – 1.167 mg, indigo carmine aluminum varnish (blue 2) – 0.279 mg].

Pharmacological action

Pharmacotherapeutic group: combined analgesic agent (nonsteroidal anti-inflammatory agent + non-narcotic analgesic agent + psychostimulant agent). ATX Code: N02BE71 Pharmacological properties

Pharmacodynamics :

Naproxen: non-steroidal anti-inflammatory drug, has analgesic, antipyretic and anti-inflammatory effects. The mechanism of action is due to non-selective inhibition of cyclooxygenase -1 and -2 (COX-1, COX-2), which regulates prostaglandin synthesis. The use of naproxen in the form of naproxen sodium salt provides faster absorption and a rapid onset of analgesic effect.

Paracetamol: a non-narcotic analgesic, has an antipyretic and analgesic effect due to the blockade of cyclooxygenase in the central nervous system and the effect on the pain centers and thermoregulation.

Caffeine: reduces drowsiness, fatigue, increases mental and physical performance; dilates the blood vessels of skeletal muscles, heart, kidneys, reduces platelet aggregation. In this combination, caffeine in a small dose practically does not have a simulating effect on the central nervous system, increases the tone of brain vessels and accelerates blood flow. Caffeine increases the permeability of histohematic barriers and increases the bioavailability of non-narcotic analgesics, and also reduces the activity of COX, since it is an antagonist of adenosine A(2A) and A(2B) receptors, which contributes to the strengthening of the analgesic effect of analgesics.

A registered clinical trial of Pentalgin ® NEO confirmed the superiority of the effect on overall pain relief (TOTPAR indicator) over the monopreparation of naproxen and over the combined preparation of paracetamol and caffeine.

Pharmacokinetics Aproxen is rapidly and completely absorbed from the gastrointestinal tract (GIT). Bioavailability – 95% (food intake practically does not affect either the fullness or the rate of absorption). The time to reach the maximum concentration in the blood (Tmax) is 1-2 hours. Binding to plasma proteins > 99%. The half-life (T 1/2) is 12-15 hours. Metabolism occurs in the liver to dimethylnaproxene with the participation of the CYP2C9 isoenzyme. Clearance – 0.13 ml / min / kg. It is excreted 98% by the kidneys,10% is excreted unchanged, with bile – 0.5-2.5%. Steady-state plasma concentration is determined after taking 4-5 doses of the drug (2-3 days).

Paracetamol: easily absorbed in the gastrointestinal tract, the Cmax is reached in 0.5-2 hours and is 5-20 mcg / ml, the connection with plasma proteins is 15%. Penetrates the blood-brain barrier. Paracetamol is metabolized in the liver and excreted by the kidneys, mainly in the form of glucuronides and sulfate conjugates. Less than 5% of paracetamol is excreted unchanged. T1 / 2 varies from 1 to 4 hours.

Caffeine: completely and quickly absorbed in the gastrointestinal tract, the maximum concentration is reached in 50-75 minutes and is 1.58-1.76 mg/l. It is quickly distributed in all organs and tissues of the body, easily penetrates the blood-brain barrier and the placenta. The relationship with blood proteins is 25-36%. More than 90% is metabolized in the liver. T 1/2 in adults is 3.9-5.3 hours (sometimes up to 10 hours) The elimination of caffeine and its metabolites is carried out by the kidneys (1-2% is excreted unchanged in adults).

Indications

Pain syndrome of various origins:

• in diseases of the musculoskeletal system (osteoarthritis of the peripheral joints and spine, including those with radicular syndrome, arthritis, myalgia);
• neuralgia;
• toothache;
• headache, migraine;
• algodismenorrhea;
• post-traumatic (sprains and bruises) and postoperative pain syndrome accompanied by inflammation.

The drug Pentalgin ® NEO is used for symptomatic therapy (to reduce pain and inflammation) and does not affect the progression of the underlying disease.

Use during pregnancy and lactation

Use of the drug Pentalgin® NEO is contraindicated during pregnancy and lactation.

Contraindications

• Hypersensitivity to naproxen, naproxen sodium, other nonsteroidal anti-inflammatory drugs (NSAIDs), or xantina; hypersensitivity to other components of the drug;
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance of acetylsalicylic acid and other NSAIDs (including in the anamnesis);
• the period after the coronary artery bypass surgery;
• erosive-ulcerative lesions of the gastrointestinal tract (in acute phase), active gastrointestinal bleeding;
• hemophilia and other disorders of blood coagulation and hemostatic disorders;
• cerebrovascular bleeding or other bleeding;
• decompensated heart failure;
• organic cardiovascular disease (acute myocardial infarction, severe coronary disease, severe hypertension), paroxysmal tachycardia, frequent ventricular premature beats;
• severe hepatic impairment or active liver disease;
• severe renal insufficiency (creatinine clearance (CC) of less than 30 ml/min), progressive kidney diseases, confirmed hyperkalemia;
• irritability, sleep disturbance, anxiety disorders (agoraphobia, panic disorder);
• pregnancy, lactation;
• children up to age 18 years.

With caution

Ischemic heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia/hyperlipidemia, diabetes mellitus, mild to moderate hepatic insufficiency with elevated transaminases, benign hyperbilirubinemia (including Gilbert’s syndrome, alcoholic liver damage), peripheral arterial diseases, smoking, glaucoma, impaired renal function (creatinine clearance 30-60 ml/min), a history of gastrointestinal ulceration, infection Helicobacter pylori, glucose-6-phosphate dehydrogenase deficiency; epilepsy and a tendency to convulsive seizures, advanced age, systemic lupus erythematosus or mixed connective tissue diseases (Sharp’s syndrome), long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants, antiplatelet agents, oral glucocorticoids, selective serotonin reuptake inhibitors. If you have one of these diseases/If you have any serious medical conditions, be sure to consult your doctor before taking the drug.

Side effects

Undesirable effects that may develop during treatment with Pentalgin ® NEO are classified according to the following frequency of occurrence: :

very common (> 1/10), common (≥ 1/100 to >< 1/10), infrequent (≥1/1,000 to < 1/100), rare (≥1/10,000 to < 1/1,000), very rare (

Disorders of the blood and lymphatic system: infrequently: eosinophilia, granulocytopenia, leukopenia, thrombocytopenia; very rarely – methemoglobinemia, hemolytic anemia.

Nervous system disorders: common: headache, vertigo, dizziness, drowsiness; uncommon: tremor, paresthesia, headache, depression, sleep disorders, attention disorder, insomnia, malaise.

Mental disorders: often: nervousness; infrequently: insomnia; rarely: anxiety, euphoric mood, internal tension.

Visual disturbances: common: visual impairment.

Hearing disorders and labyrinth disorders: common: tinnitus, hearing loss; infrequent: hearing loss.

Cardiac disorders: often: swelling, palpitation; infrequently: congestive heart failure, tachycardia, arrhythmia; frequency unknown-increased blood pressure.

Respiratory, thoracic and mediastinal disorders: common: shortness of breath; uncommon: eosinophilic pneumonia; very rare: bronchospasm (in patients with hypersensitivity to acetylsalicylic acid and other NSAIDs).

Disorders of the gastrointestinal tract: common: constipation, abdominal pain, dyspepsia, nausea, diarrhea, stomatitis, flatulence; uncommon: gastrointestinal bleeding and/or gastric perforation, bloody vomiting, melena, vomiting; dry mouth; very rare: relapse or exacerbation of ulcerative colitis or Crohn’s disease; frequency unknown: gastritis.

Liver and biliary tract disorders: infrequently: increased activity of “liver” enzymes, jaundice; very rare: impaired liver function.

Skin and subcutaneous tissue disorders: common: pruritus, skin rash, ecchymosis, purpura; uncommon: alopecia, photodermatosis; very rare: bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.

Musculoskeletal and connective tissue disorders:infrequently: myalgia and muscle weakness.

Kidney and urinary tract disorders:infrequently: glomerulonephritis, hematuria, interstitial nephritis, nephrotic syndrome, renal failure, renal papillary necrosis.

General disorders and disorders at the injection site:often: thirst, increased sweating; infrequently: hypersensitivity reactions, menstrual irregularities, hyperthermia (chills and fever).

There are no data on the enhancement or expansion of the spectrum of adverse events of individual components when used in combination in accordance with the instructions for medical use.

If you experience side effects, you should consult a doctor.

Interaction

Other NSAIDs, including selective cyclooxygenase-2 inhibitors, corticosteroids: increased risk of developing gastrointestinal side effects of naproxen.

Propranolol and other beta-blockers: naproxen may reduce the antihypertensive effect of medications. Caffeine may inhibit the therapeutic effects of beta-blockers.

Cardiac Glycosides: caffeine accelerates the absorption and enhances the action of cardiac glycosides, increases their toxicity.

Diuretics: naproxen can reduce the diuretic effect of diuretics, inhibit the natriuretic effect of furosemide. Diuretics may increase the risk of nephrotoxicity of NSAIDs.

Lithium: naproxen reduces the excretion of lithium, which leads to an increase in the concentration of lithium in the blood plasma.

Myelotoxic drugs: increased hematoxicity of naproxen.

Cyclosporine: increased risk of developing kidney failure.

Probenecid: increases the concentration of naproxen in the blood plasma.

Methotrexate, phenithione, sulfonamide: naproxen slows down their excretion, which increases the risk of developing their toxic effects.

Antacids containing magnesium and aluminum: reduction of naproxen absorption.

Anticoagulants: naproxen can enhance the effect of anticoagulants, paracetamol with prolonged use increases the effect of indirect anticoagulants.

Antiplatelet drugs, selective serotonin reuptake inhibitors: increased risk of gastrointestinal bleeding.

Mifepristone: Concomitant use of NSAIDs for 8-12 days after mifepristone use is not recommended.

Tacrolimus: concomitant use of NSAIDs increases the risk of nephrotoxicity.

Diflunisal: an increase in the concentration of paracetamol in the blood plasma, which increases the risk of hepatotoxicity.

Inducers of microsomal liver enzymes: possible increase in the hepatotoxic effect of paracetamol.

Inhibitors of microsomal liver enzymes: reducing the risk of hepatotoxic effects of paracetamol.

Chloramphenicol: paracetamol increases the elimination time of chloramphenicol.

Metoclopramide, domperidone: increased absorption rate of paracetamol.

Colestyramine: reduced absorption rate of paracetamol.

Theophylline: caffeine reduces the excretion of theophylline.

Barbiturates, primidone, anticonvulsants: it is possible to increase the metabolism and increase the clearance of caffeine.

Cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin: it is possible to reduce the metabolism of caffeine in the liver (slowing its excretion and increasing its concentration in the blood).

Calcium supplements: caffeine reduces their absorption in the gastrointestinal tract.

Narcotic and hypnotic drugs: caffeine reduces their effectiveness.

Alcohol: increased risk of liver damage and acute pancreatitis.

How to take, course of use and dosage

Inside. Tablets should be taken with a sufficient amount of water. Single dose – 1 tablet. The frequency of admission is 1-3 times a day, with an interval of at least 4 hours. The maximum daily dose is 3 tablets. The duration of use of the drug is no more than 5 days.

Overdose

Symptoms: drowsiness, dyspeptic disorders (heartburn, nausea, vomiting, abdominal pain), headache, tinnitus, weakness, sweating, pallor of the skin, anxiety, agitation, motor restlessness, anorexia, confusion, tachycardia, arrhythmia, hyperthermia, tremor or muscle twitching; in severe cases-bloody vomiting, melena, impaired consciousness, convulsions, renal and/or liver failure. If you suspect an overdose of the drug, you should immediately seek medical help.

Treatment. The victim should be given a gastric lavage and enterosorbents (activated charcoal) should be prescribed. The need for additional therapeutic measures is determined depending on the severity of the condition and the severity of intoxication symptoms.

Description

Pentalgin Neo is a new combined analgesic for modern and active people, which has a faster analgesic effect (due to the naroxen salt compared to naproxen-containing drugs). Compared to the monopreparation of naproxen and the combination of paracetamol with caffeine, as well as the dual mechanism of pain control.

Pentalgin Neo has an anti-inflammatory effect directly in the focus of pain and activates a person’s own analgesic system in the brain. Due to the naproxen salt contained in the composition, Pentalgin Neo enters the blood faster. Due to its combined composition, Pentalgin Neo has a pronounced analgesic effect.

Functional benefits

• faster in the bloodstream due to the Active ingredient salt of naproxen compared with preparations containing naproxen;
• increased analgesic effect due to the precise combination of active substances;
• the effect on pain of different origin, including acute pain due to the optimized formula;
• the lack of habituation and good absorption from the gastrointestinal tract due to the carefully selected dosages of active ingredients;
• non-prescription status.

Special instructions

Generally do not exceed the doses specified in the instructions. To reduce the risk of adverse events, the minimum effective dose should be used in the shortest possible course.

If the pain syndrome persists or increases during therapy, you should consult a doctor.

With prolonged use of the drug, monitoring of peripheral blood and the functional state of the liver is necessary.

The drug should not be taken together with other anti-inflammatory and painkillers, except as prescribed by a doctor.

You should avoid taking the drug for 48 hours before surgery. If it is necessary to determine 17-corticosteroids, the drug should be discontinued 48 hours before the study. Similarly, naproxen may affect the determination of 5-hydroxyindoleacetic acid in the urine.

The use of naproxen, as well as other drugs that block prostaglandin synthesis, can affect fertility, so it is not recommended for women planning pregnancy.

During treatment, you should stop using alcoholic beverages (see the section “Drug interactions”).

When using the drug, you should limit the consumption of products containing caffeine, since excessive intake of caffeine can lead to nervousness, irritability, insomnia and, in some cases, palpitations.

Effects on laboratory parameters The use of paracetamol may affect the results of uric acid determination by the phosphor-wolframic acid method and glycemia by the glucose oxidase/peroxidase method.

Caffeine can distort the results of the dipyridamole test; during the study, it is necessary to refrain from taking caffeine for 8-12 hours.

Each tablet of the drug contains approximately 20 mg of sodium. When limiting salt intake, this should be taken into account.

Influence on the ability to drive vehicles and mechanisms

Naproxen and caffeine, which are part of the drug, can affect the speed of psychomotor reaction, so during the reception period, care should be taken when driving a car and performing tasks that require increased attention.

Form of production

Pentalgin Neo is available in the form of film-coated tablets in packages No. 10 and No. 20. The drug in package No. 10 is suitable for a traveler’s first-aid kit, in package No. 20-for a home first-aid kit.

Storage conditions

Store in a dry place at a temperature not exceeding 25 °C in the original packaging (blister pack). Keep out of reach of children.

Shelf

life is 2 years. Do not use after the expiration date indicated on the package.

Active ingredient

Caffeine, Naproxen, Paracetamol

Dosage form

Tablets