Pentalgin^® (Tablets) Instructions for Use

Marketing Authorization Holder

Otisipharm, JSC (Russia)

Manufactured By

Pharmstandard-Lexredstva OJSC (Russia)

ATC Code

N02BE71 (Paracetamol in combination with psycholeptics)

Dosage Form

Pentalgin®

Film-coated tablets: 2, 4, 6, 8, 10, 12, 20 or 24 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets from light green to green in color, biconvex, capsule-shaped with bevelled edges, with a score on one side and an embossing “PENTALGIN” on the other; on the cross-section, the tablet is light green in color with white inclusions.

Excipients: microcrystalline cellulose – 128 mg, potato starch – 55.38 mg, croscarmellose sodium – 32 mg, hypromellose (hydroxypropylcellulose) – 32.52 mg, citric acid monohydrate – 3 mg, butylated hydroxytoluene (E321) – 0.3 mg, magnesium stearate – 7.2 mg, talc – 16.12 mg, quinoline yellow dye (E104) – 0.4608 mg, indigo carmine (E132) – 0.0192 mg.

Shell composition: hypromellose (hydroxypropyl methylcellulose) – 12.17 mg, povidone (polyvinylpyrrolidone medium molecular weight medical, povidone K25) – 3.87 mg, polysorbate 80 (tween 80) – 1.1 mg, titanium dioxide – 3.43 mg, talc – 4.218 mg, quinoline yellow dye (E104) – 0.2 mg, indigo carmine (E132) – 0.0127 mg,
Or Opadry 13A210001 Green coating (OPADRY 13A210001 GREEN) – 25.0007 mg [hypromellose – 12.17 mg, povidone – 3.87 mg, polysorbate 80 – 1.1 mg, titanium dioxide – 3.43 mg, talc – 4.218 mg, quinoline yellow – 0.2 mg, FD&C blue #2/ indigo carmine – 0.0127 mg].

2 pcs. – contour cell blisters (1) – cardboard packs.
2 pcs. – contour cell blisters (2) – cardboard packs.
4 pcs. – contour cell blisters (1) – cardboard packs.
4 pcs. – contour cell blisters (2) – cardboard packs.
6 pcs. – contour cell blisters (1) – cardboard packs.
6 pcs. – contour cell blisters (2) – cardboard packs.
10 pcs. – contour cell blisters (1) – cardboard packs.
10 pcs. – contour cell blisters (2) – cardboard packs.
12 pcs. – contour cell blisters (1) – cardboard packs.
12 pcs. – contour cell blisters (2) – cardboard packs.

Clinical-Pharmacological Group

Spasm analgesic

Pharmacotherapeutic Group

Analgesic agent (NSAID + non-narcotic analgesic agent + psychostimulant agent + spasmolytic agent + H1-histamine receptor blocker)

Pharmacological Action

A combined drug that has analgesic, anti-inflammatory, spasmolytic, and antipyretic effects.

Paracetamol is an analgesic-antipyretic; it has an antipyretic and analgesic effect due to the blockade of COX in the CNS and its effect on the pain and thermoregulation centers.

Naproxen is an NSAID; it has an anti-inflammatory, analgesic, and antipyretic effect associated with non-selective suppression of COX activity, which regulates the synthesis of prostaglandins.

Caffeine is a psychostimulant; it causes dilation of blood vessels in skeletal muscles, the heart, and kidneys; increases mental and physical performance, helps eliminate fatigue and drowsiness; increases the permeability of histohematic barriers and increases the bioavailability of non-narcotic analgesics, thereby contributing to an enhancement of the therapeutic effect. It has a tonic effect on the blood vessels of the brain.

Drotaverine has a myotropic spasmolytic effect due to the inhibition of PDE 4; it acts on the smooth muscles of the gastrointestinal tract, biliary tract, genitourinary system, and blood vessels.

Pheniramine is a histamine H₁-receptor blocker. It has a spasmolytic and mild sedative effect, reduces exudation phenomena, and also enhances the analgesic effect of paracetamol and naproxen.

Pharmacokinetics

Data on the pharmacokinetics of the drug Pentalgin^® are not provided.

Indications

• Pain syndrome of various origins, including joint pain, muscle pain, radiculitis, algodysmenorrhea, neuralgia, toothache, headache (including that caused by spasm of cerebral blood vessels);
• Pain syndrome associated with spasm of smooth muscles, including in chronic cholecystitis, cholelithiasis, postcholecystectomy syndrome, renal colic;
• Post-traumatic and postoperative pain syndrome, including that accompanied by inflammation;
• Cold illnesses accompanied by febrile syndrome (as symptomatic therapy).

ICD codes

Dosage Regimen

Administer the drug orally.

Take one tablet up to three times per day as needed for pain or fever.

Do not exceed a maximum daily dose of four tablets.

Limit the duration of use to no more than three days for the treatment of febrile conditions.

Limit the duration of use to no more than five days for the management of pain.

Consult a physician for any treatment extending beyond these specified durations.

Swallow the tablet whole with a sufficient amount of water.

Avoid taking the medication on an empty stomach to minimize potential gastrointestinal irritation.

Adhere strictly to the indicated doses; do not increase the dose or frequency of administration.

Discontinue use and seek medical advice if symptoms persist or worsen.

Exercise particular caution regarding the total daily intake of paracetamol from all combined sources to prevent overdose and hepatotoxicity.

Adverse Reactions

Allergic reactions: skin rash, itching, urticaria, angioedema.

From the hematopoietic system: thrombocytopenia, leukopenia, agranulocytosis, anemia, methemoglobinemia.

From the CNS: excitation, anxiety, hyperreflexia, tremor, headache, sleep disorders, dizziness, decreased concentration.

From the cardiovascular system: palpitations, arrhythmias, increased blood pressure.

From the digestive system: erosive and ulcerative lesions of the gastrointestinal tract, nausea, vomiting, epigastric discomfort, abdominal pain, constipation, impaired liver function.

From the urinary system: impaired renal function.

From the sensory organs: hearing loss, tinnitus, increased intraocular pressure in patients with angle-closure glaucoma.

Other: dermatitis, tachypnea (rapid breathing).

If any of the side effects mentioned in the instructions worsen, or the patient notices any other side effects not listed in the instructions, they should inform their doctor.

Contraindications

• Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;
• Gastrointestinal bleeding;
• Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in history);
• Severe hepatic insufficiency;
• Severe renal failure;
• Bone marrow depression;
• Condition after coronary artery bypass surgery;
• Severe organic diseases of the cardiovascular system (including acute myocardial infarction);
• Paroxysmal tachycardia;
• Frequent ventricular extrasystole;
• Severe arterial hypertension;
• Hyperkalemia;
• Pregnancy;
• Lactation period (breastfeeding);
• Children and adolescents under 18 years of age;
• Hypersensitivity to the components of the drug.

With caution, the drug should be used in patients with cerebrovascular diseases, diabetes mellitus, peripheral arterial diseases, a history of ulcerative lesions of the gastrointestinal tract, with mild or moderate renal and hepatic insufficiency, viral hepatitis, alcoholic liver damage, benign hyperbilirubinemia (Gilbert’s, Dubin-Johnson and Rotor syndromes), epilepsy, with a tendency to convulsive seizures, glucose-6-phosphate dehydrogenase deficiency, and in elderly patients.

If any of the listed diseases or conditions are present, the patient should consult a doctor before using the drug.

Use in Pregnancy and Lactation

The drug is contraindicated for use during pregnancy.

If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Use in Hepatic Impairment

Contraindicated in severe hepatic insufficiency.

Use in Renal Impairment

Contraindicated in severe renal failure.

Pediatric Use

Contraindication: children and adolescents under 18 years of age.

Geriatric Use

The drug should be used with caution in elderly patients.

Special Precautions

Simultaneous use of the drug Pentalgin^® with other products containing Paracetamol and/or NSAIDs, as well as with remedies for relieving symptoms of colds, flu, and nasal congestion, should be avoided.

When using the drug Pentalgin^® for more than 5-7 days, peripheral blood counts and the functional state of the liver should be monitored.

Paracetamol distorts the results of laboratory tests for glucose and uric acid levels in blood plasma.

If it is necessary to determine 17-ketosteroids, Pentalgin^® should be discontinued 48 hours before the study. It should be taken into account that Naproxen increases bleeding time.

The effect of caffeine on the CNS depends on the type of nervous system and can manifest as either excitation or inhibition of higher nervous activity.

During the treatment period, alcohol-containing beverages should not be consumed.

Effect on ability to drive vehicles and operate machinery

During the treatment period, the patient should exercise caution when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: pallor of the skin, anorexia (lack of appetite), abdominal pain, nausea, vomiting, gastrointestinal bleeding, agitation, motor restlessness, confusion, tachycardia, arrhythmia, hyperthermia (increased body temperature), frequent urination, headache, tremor or muscle twitching; epileptic seizures, increased activity of liver transaminases, hepatonecrosis, increased prothrombin time. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose, liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis; arrhythmia, pancreatitis develop. If an overdose is suspected, immediate medical attention should be sought.

Treatment: gastric lavage followed by administration of activated charcoal. The specific antidote for paracetamol poisoning is acetylcysteine. Administration of acetylcysteine is relevant within 8 hours after paracetamol intake. In case of gastrointestinal bleeding, administration of antacids and gastric lavage with ice-cold 0.9% sodium chloride solution is necessary; maintain lung ventilation and oxygenation; for epileptic seizures – intravenous administration of diazepam; maintain fluid and electrolyte balance.

Drug Interactions

When Pentalgin^® is taken simultaneously with barbiturates, tricyclic antidepressants, rifampicin, ethanol, the risk of hepatotoxic effects increases (these combinations should be avoided).

Paracetamol enhances the effect of indirect anticoagulants and reduces the effectiveness of uricosuric drugs.

Long-term use of barbiturates reduces the effectiveness of paracetamol.

When paracetamol is used simultaneously with ethanol, the risk of acute pancreatitis increases.

Microsomal oxidation inhibitors (including cimetidine) reduce the risk of hepatotoxic effects of paracetamol.

When used simultaneously with diflunisal, the plasma concentration of paracetamol increases by 50%, which increases the risk of hepatotoxicity.

Naproxen can cause a decrease in the diuretic effect of furosemide, enhance the effect of indirect anticoagulants, increases the toxicity of sulfonamides and methotrexate, reduces the excretion of lithium and increases its concentration in blood plasma.

When caffeine and barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin) are used together, an increase in metabolism and an increase in caffeine clearance are possible; when caffeine is taken simultaneously with cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin – a decrease in the metabolism of caffeine in the liver (slowing its excretion and increasing its concentration in the blood).

Simultaneous consumption of caffeine-containing drinks and other CNS stimulants may lead to excessive CNS stimulation.

When used simultaneously, drotaverine may weaken the antiparkinsonian effect of levodopa.

When pheniramine is used simultaneously with tranquilizers, hypnotics, MAO inhibitors, ethanol, an enhancement of the inhibitory effect on the CNS is possible.

Storage Conditions

Store at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is available without a prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.