Solpadeine Fast (Tablets) Instructions for Use

ATC Code

N02BE51 (Paracetamol in combination with other drugs, excluding psycholeptics)

Active Substances

Caffeine (Ph.Eur.)

Paracetamol (Rec.INN)

Clinical-Pharmacological Group

Analgesic-antipyretic

Pharmacotherapeutic Group

Analgesic and antipyretic agent

Pharmacological Action

Solpadeine Fast has an analgesic and antipyretic effect.

Paracetamol

It blocks COX in the CNS, affecting the centers of pain and thermoregulation (in inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX), which explains the almost complete absence of an anti-inflammatory effect.

The lack of effect on the synthesis of prostaglandins in peripheral tissues determines the absence of a negative effect on water-salt metabolism (retention of sodium and water) and the gastrointestinal mucosa.

This property of paracetamol makes the drug particularly suitable for patients with a history of gastrointestinal diseases (for example, patients with a history of gastrointestinal bleeding or elderly patients), or patients receiving concomitant drug therapy in which inhibition of peripheral prostaglandins may be undesirable.

Caffeine

The analgesic adjuvant effect of caffeine is due to the following mechanisms: blockade of the peripheral pronociceptive action of adenosine, activation of central noradrenergic pathways, which represent an endogenous pain suppression system, and stimulation of the CNS with subsequent modulation of the effective component of pain.

Caffeine enhances the effect of paracetamol and reduces the time to onset of the analgesic effect.

Clinical data have shown that the Paracetamol/Caffeine combination provides more effective pain relief compared to standard paracetamol (p < 0.05).

Caffeine also stimulates the psychomotor centers of the brain, has an analeptic effect, enhances the effect of analgesics, eliminates drowsiness and fatigue, and increases physical and mental performance.

Sodium bicarbonate does not have an analgesic effect.

Pharmacokinetics

Absorption and Distribution

Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. Distribution in body fluids is relatively uniform. At therapeutic concentrations, the binding of paracetamol to plasma proteins is minimal. No saturation of paracetamol elimination processes with subsequent risks of increased T_1/2 and toxicity was noted. No interaction of active substances was noted.

Caffeine is completely and rapidly absorbed from the gastrointestinal tract. C_max is reached within 5-120 min depending on the dose, patient condition and concomitant drugs. No signs of presystemic metabolism were recorded. Caffeine is actively distributed throughout the body. The binding of caffeine to plasma proteins averages about 35%.

The drug contains sodium bicarbonate, which promotes the absorption of the drug.

According to clinical studies, the absorption of paracetamol and caffeine is faster during the first 60 min (decrease in T_max and increase in AUC_{0-10 h}) compared to the drug Solpadeine Express, film-coated tablets.

Metabolism

Paracetamol is metabolized in the liver and excreted by the kidneys in the form of glucuronide and sulfate metabolites, less than 5% is excreted unchanged.

Caffeine is almost completely (≈99%) metabolized in the liver by oxidation and demethylation to various xanthine derivatives, which are excreted by the kidneys. The hepatic isoenzyme CYP1A2 is involved in the enzymatic metabolism of caffeine.

Elimination

The average T_1/2 of paracetamol when taking a therapeutic dose is about 2-3 hours.

In adult patients, the elimination of caffeine occurs almost entirely through hepatic metabolism.

Only a small amount (1-2%) of the ingested dose of caffeine is excreted unchanged by the kidneys in humans.

Individual variability in elimination rate is observed in adults. The average T_1/2 of caffeine from blood when taking a therapeutic dose is about 4.9 hours, with a range of 1.9-12.2 hours.

Indications

For adults and children over 12 years of age as

• An analgesic (for pain of mild to moderate intensity) for:
  • Toothache, including tooth extraction and after dental procedures;
  • Headache and migraine;
  • Sore throat;
  • Muscle and joint pain, including back pain;
  • Pain caused by osteoarthritis;
  • Ear pain (otalgia);
  • Neuralgia;
  • Painful menstruation (dysmenorrhea).

• For symptomatic treatment to reduce elevated body temperature in:
  • Acute respiratory and acute respiratory viral diseases, including influenza;
  • After vaccination.

ICD codes

Dosage Regimen

Tablets

For oral administration.

Do not exceed the indicated dose.

The lowest dose necessary to achieve the effect should be used for the shortest possible period of time.

The minimum interval between doses of Solpadeine Fast should be at least 4 hours.

Adults (including the elderly) and children over 12 years: 1-2 tablets up to 4 times/day, as needed. The interval between doses should be at least 4 hours.

Maximum single dose – 2 tablets, maximum daily dose – 8 tablets.

The drug is not recommended to be used for more than 5 days as an analgesic and for more than 3 days as an antipyretic without a doctor’s prescription and supervision.

If the recommended dose of the drug is exceeded, the patient should immediately seek medical help, even if feeling well. Paracetamol overdose can cause liver failure.

Special patient groups

Patients with impaired renal function. Before using Solpadeine Fast, patients with impaired renal function should consult a doctor. Restrictions associated with the use of drugs containing a combination of caffeine and paracetamol in patients with impaired renal function are mainly related to the paracetamol content in the drug.

Patients with impaired liver function. Before using Solpadeine Fast, patients with impaired liver function should consult a doctor. Restrictions associated with the use of drugs containing a combination of caffeine and paracetamol in patients with impaired liver function are mainly related to the paracetamol content in the drug.

Adverse Reactions

In recommended doses, the drug is usually well tolerated.

The following adverse reactions were identified spontaneously during post-registration use of the drug.
Adverse reactions are classified by system organ class and according to frequency of occurrence. The frequency of adverse reactions is defined as follows: very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1000 and <1/100), rare (≥1/10,000 and <1/1000), very rare (≥1/100,000 and <1/10,000), frequency not known (frequency cannot be estimated from the available data).

Paracetamol

Blood and lymphatic system disorders very rare – thrombocytopenia, leukopenia, methemoglobinemia, agranulocytosis, hemolytic anemia.

Immune system disorders very rare – anaphylaxis, hypersensitivity skin reactions, including skin rash, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Respiratory, thoracic and mediastinal disorders very rare – bronchospasm in patients with hypersensitivity to acetylsalicylic acid and intolerance to other NSAIDs.

Hepatobiliary disorders very rare – liver function disorders.

With long-term use of the drug in high doses, the likelihood of hepatotoxic effects, nephrotoxic effects and pancytopenia increases.

In case of long-term use of the drug, blood count monitoring is necessary.

Caffeine

Nervous system disorders very rare – dizziness, headache.

Cardiac disorders very rare – palpitations.

Psychiatric disorders very rare – insomnia, restlessness, anxiety, irritability, nervousness.

Gastrointestinal disorders very rare – gastrointestinal disorders.

When using Solpadeine Fast, it is not recommended to consume caffeine-containing products, as this increases the risk of adverse reactions such as insomnia, irritability, anxiety, headache, gastrointestinal disorders, tachycardia, cardiac arrhythmia.

If any of the listed adverse reactions occur, the patient should stop taking the drug and immediately consult a doctor.

Contraindications

• Hypersensitivity to paracetamol, caffeine and any other component of the drug;
• Severe renal impairment;
• Severe hepatic impairment;
• Arterial hypertension;
• Glaucoma;
• Sleep disorders;
• Epilepsy;
• Pregnancy;
• Breastfeeding period;
• Children under 12 years of age;
• Sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption, because the drug contains sorbitol;
• Simultaneous use with other drugs containing Paracetamol, lithium, as well as with caffeine-containing drinks.

With caution

• Benign hyperbilirubinemias (including Gilbert’s syndrome);
• Viral hepatitis;
• Alcoholic liver disease;
• Chronic alcoholism;
• Glucose-6-phosphate dehydrogenase deficiency;
• Mild to moderate hepatic impairment;
• Mild to moderate renal impairment;
• Presence of severe infections, because taking the drug may increase the risk of metabolic acidosis;
• Use in patients with glutathione deficiency (in particular, in extremely malnourished patients suffering from anorexia, or patients with low body mass index).

If any of the listed diseases/conditions/risk factors are present, it is necessary to consult a doctor before taking the drug.

Use in Pregnancy and Lactation

Pregnancy

The use of the drug during pregnancy is contraindicated.

Paracetamol. The lowest dose necessary to achieve the effect should be taken for the shortest possible period of time.

Caffeine. The use of caffeine may increase the risk of spontaneous abortion, so its use is not recommended during pregnancy.

Breastfeeding period

The use of the drug during breastfeeding is contraindicated.

Paracetamol is excreted in breast milk, but in clinically insignificant amounts when used in recommended doses.

Caffeine passes into breast milk and may have a stimulating effect on the breastfed infant, however, significant toxicity has not been noted.

Use in Hepatic Impairment

Contraindicated in severe hepatic impairment.

Use with caution in mild to moderate hepatic impairment.

Use with caution in viral hepatitis, alcoholic liver disease.

To avoid toxic liver damage, patients taking Solpadeine Express should refrain from drinking alcohol. The drug is not recommended for chronic alcoholism.

Use in Renal Impairment

Contraindicated in severe renal impairment.

Use with caution in mild to moderate renal impairment.

Pediatric Use

Contraindicated in children under 12 years of age.

Geriatric Use

The drug is approved for use in elderly patients in accordance with the indications and dosage regimen.

Special Precautions

If there is no improvement when taking the drug, or the headache becomes constant, it is necessary to consult a doctor.

Solpadeine Fast should not be used with other paracetamol-containing drugs, since the combined use of drugs can cause paracetamol overdose.

Overdose of paracetamol may lead to liver failure, which may require liver transplantation or lead to death.

Solpadeine Fast should not be taken with caffeine-containing food products (tea, coffee, etc.), as this may lead to restlessness, anxiety, irritability, insomnia, headache, gastrointestinal disorders, tachycardia, cardiac arrhythmia.

Patients with glutathione deficiency due to eating disorders, cystic fibrosis, HIV infection, starvation, exhaustion are susceptible to overdose, so precautions must be taken and it is recommended to consult a doctor before taking the drug.

Cases of liver failure/liver dysfunction have been reported with a small overdose of paracetamol (5 g or more) in patients with low glutathione levels, in particular, in extremely malnourished patients suffering from anorexia, chronic alcoholism or patients with low body mass index.

The use of Solpadeine Fast by patients with low glutathione levels, for example, in sepsis, may increase the risk of developing metabolic acidosis, accompanied by symptoms of rapid, difficult breathing (feeling of shortness of breath, dyspnea), nausea, vomiting, loss of appetite.

If these symptoms occur simultaneously, you should immediately consult a doctor.

To avoid toxic liver damage, Paracetamol should not be combined with the intake of alcoholic beverages, and should not be taken by persons prone to chronic alcohol consumption.

Concomitant liver diseases increase the risk of further liver damage when taking Solpadeine Fast.

When taking the drug in patients with non-alcoholic cirrhosis of the liver, there is a high risk of overdose.

Patients suffering from atopic bronchial asthma or hay fever have an increased risk of developing allergic reactions.

When conducting tests to determine uric acid and blood glucose levels, the doctor should be informed about taking the drug.

The drug may change the results of doping control tests in athletes.

Patients on a salt-free or low-salt diet should take into account the sodium content in the tablet (427 mg) when calculating daily salt intake.

The drug contains sorbitol. Patients with fructose intolerance should not use this drug.

Effect on ability to drive vehicles and machinery

The effect of the drug on the ability to drive a car and machinery is unlikely.

Overdose

Symptoms (caused by paracetamol)

Paracetamol overdose can cause liver failure, which may require liver transplantation or lead to death. In addition, acute pancreatitis is observed, accompanied by liver dysfunction and hepatotoxicity.

Hepatotoxic effect in adults occurs when taking paracetamol in an amount of 10 g or more.

In the presence of factors affecting the hepatotoxicity of paracetamol (see sections “Drug Interactions”, “Special Precautions”), liver damage can occur after taking paracetamol in an amount of 5 g or more.

The first signs of overdose usually appear after 24-48 hours and reach maximum development on days 4-6.

Within the first 24 hours after overdose, the following symptoms may appear: nausea, vomiting, stomach pain, pale skin, anorexia.

After 1-2 days, signs of liver damage (pain in the liver area, increased activity of liver enzymes) are determined, and disturbances in carbohydrate metabolism and metabolic acidosis may develop.

In severe cases of overdose, as a result of liver failure, encephalopathy (impaired brain function), bleeding, hypoglycemia, cerebral edema, up to death, the need for liver transplantation, death may develop.

Acute renal failure with acute tubular necrosis may also develop, characterized by pain in the lumbar region, hematuria (presence of blood or red blood cells in the urine), proteinuria (increased protein in the urine), while severe liver damage may be absent.

Cases of cardiac arrhythmia and pancreatitis have been reported.

Treatment

In case of suspected overdose with Solpadeine Fast, even in the absence of pronounced initial symptoms, it is necessary to discontinue the use of the drug and immediately consult a doctor for medical assistance. Within the first hour after overdose, but no later than 4 hours, gastric lavage and administration of enterosorbents (activated charcoal, polyphepan) are recommended. The plasma concentration of paracetamol should be determined, but not earlier than 4 hours after overdose (earlier results are unreliable).

Administration of acetylcysteine within 24 hours after overdose. The maximum protective effect is provided within the first 8 hours after overdose; the effectiveness of the antidote decreases sharply over time. If necessary, acetylcysteine is administered intravenously. In the absence of vomiting before the patient is admitted to the hospital, methionine can be used.

The need for additional therapeutic measures (administration of methionine, intravenous administration of acetylcysteine) is determined depending on the plasma concentration of paracetamol, as well as the time elapsed after its intake.

Treatment of patients with severe liver impairment 24 hours after paracetamol intake should be carried out in conjunction with specialists from a toxicology center or a specialized liver disease department.

Symptoms (caused by caffeine)

Epigastric pain, vomiting, frequent urination, tachycardia, arrhythmia, CNS stimulation (insomnia, restlessness, agitation, anxiety, increased neuro-reflex excitability, tremor, and convulsions). It should be taken into account that the appearance of clinically significant symptoms of caffeine overdose when taking the drug is always associated with severe liver damage due to paracetamol overdose.

Treatment

There is no specific antidote. Treatment includes supportive measures, such as plenty of fluids and maintenance of vital signs. Administration of activated charcoal is recommended within 1 to 4 hours after overdose. To reduce the impact of caffeine on CNS functions, intravenous administration of sedatives and β-adrenergic receptor antagonists is recommended to reduce the cardiotoxic effect.

Sodium Bicarbonate

Symptoms high doses of sodium bicarbonate can cause gastrointestinal reactions, including nausea and vomiting. In addition, high doses of sodium bicarbonate can cause hypernatremia.

Treatment if hypernatremia is suspected, electrolyte levels should be monitored and appropriate treatment should be administered.

Drug Interactions

If the patient is already taking other medications, a doctor should be consulted before starting to take Solpadeine Fast.

With regular long-term use, the drug enhances the effect of indirect anticoagulants (warfarin and other coumarins), which increases the risk of bleeding. Occasional intake of a single dose of the drug does not have a significant effect on the action of indirect anticoagulants.

It enhances the effect of MAO inhibitors.

Barbiturates, carbamazepine, phenytoin, primidone and other anticonvulsants, ethanol, rifampicin, phenylbutazone, butadione, St. John’s wort preparations and other inducers of microsomal oxidation increase the production of hydroxylated active metabolites, creating the possibility of severe liver damage even with small overdoses of paracetamol (5 g and more).

Inhibitors of liver microsomal enzymes (cimetidine) reduce the risk of hepatotoxic action.

Under the action of paracetamol, the elimination time of chloramphenicol increases 5 times, thereby increasing the risk of chloramphenicol poisoning.

Metoclopramide and domperidone increase, while cholestyramine reduces the absorption rate of paracetamol.

The drug may reduce the effectiveness of uricosuric drugs.

Concomitant intake of paracetamol and alcoholic beverages increases the risk of liver damage and acute pancreatitis.

Caffeine accelerates the absorption of ergotamine. The drug should not be taken simultaneously with caffeine-containing products.

Caffeine may enhance the excretion of lithium from the body, therefore concurrent use of the drug with lithium-containing preparations is not recommended.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 4 years. Do not use after the expiration date.

Dispensing Status

The drug is available without a prescription.

ORIGINAL DRUG(according to information from JSC “Heleon Rus”)

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.