Solpadein Fast, 65 mg+500 mg 24 pcs

Pharmacological group:
Analgesic and antipyretic
ATX code: N02BE51.

Pharmacodynamics:
The drug Solpadein Fast has analgesic and antipyretic effect. The drug contains a combination of two active ingredients: paracetamol and caffeine.

Paracetamol
Paracetamol blocks cyclooxygenase (COX) in the central nervous system, affecting the centers of pain and thermoregulation (in inflamed tissues cell peroxidase neutralizes the effect of paracetamol on COX), which explains the almost complete absence of anti-inflammatory effect. The lack of effect on the synthesis of prostaglandins in peripheral tissues determines its lack of negative effect on water-salt metabolism (sodium and water retention) and gastrointestinal mucosa. This property of paracetamol makes the drug especially suitable for patients with a history of gastrointestinal diseases (e.g., patients with a history of gastrointestinal bleeding or elderly patients) or patients taking concomitant medication, in which inhibition of peripheral prostaglandins may be undesirable.

Caffeine
The analgesic adjuvant action of caffeine is due to the following mechanisms: blockade of peripheral pronociceptive action of adenosine, activation of central noradrenergic pathways, which is an endogenous system of pain suppression, and CNS stimulation with subsequent modulation of the effective pain component. Caffeine enhances the effect of paracetamol and shortens the time to the onset of analgesic effect. Clinical data have shown that the paracetamol-caffeine combination provides more effective pain relief than just paracetamol (p < 0.05). Also caffeine stimulates psychomotor centers of the brain, has an analeptic effect, enhances the effect of analgesics, eliminates drowsiness and fatigue, increases physical and mental performance.

Sodium bicarbonate has no analgesic effect.

Pharmacokinetics:
Absorption and distribution:

Paracetamol is quickly 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. There is no saturation of the excretion of paracetamol with the subsequent risk of increased elimination half-life and toxicity. No interaction of active substances was noted.

Caffeine is completely and quickly absorbed from the gastrointestinal tract. Maximal concentrations are reached in 5-120 minutes depending on the dose, patient’s condition and concomitant drugs. No evidence of presystemic metabolism has been recorded. Caffeine is actively distributed throughout the body. Average binding of caffeine to plasma proteins is about 35 %.

The drug contains sodium bicarbonate, which promotes absorption of the drug. According to clinical studies, absorption of paracetamol and caffeine is faster during the first 60 minutes (decrease in Tmax and increase in AUC0-10 h) compared to the drug Solpadein Fast, film-coated tablets.

Metabolism:

Paracetamol is metabolized in the liver and excreted by the kidneys as glucuronide and sulfate metabolites – less than 5% is excreted as unchanged paracetamol.

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 cytochrome P450 isoenzyme CYP1A2 is involved in the enzymatic metabolism of caffeine.

Excretion:
In adult patients, caffeine is almost completely excreted by hepatic metabolism. Only a small amount (1-2%) of the taken dose of caffeine in humans is excreted unchanged by the kidneys. In adults, there is individual variability in excretion rate. The average blood elimination half-life of caffeine at a therapeutic dose is about 4.9 hours, with a range of 1.9-12.2 hours.

Indications

The drug Solpadein Fast is used in adults and children over 12 years as:

– Anesthetic (with pain syndrome of mild and moderate intensity) for:
– toothache, including tooth extraction and after dental interventions;
– headache and migraine;
– sore throat;
– Pain in the muscles and joints, including back pain;
– pain caused by osteoarthritis;
– ear pain (othalgia);
– neuralgia;
– painful menstruation (dysmenorrhea).

– As symptomatic treatment to reduce fever in:
– Acute respiratory and acute respiratory viral diseases, including flu;
– After vaccinations.

Active ingredient

Caffeine, Paracetamol

Composition

Active ingredient:

One tablet contains: paracetamol 500 mg; caffeine 65 mg

Excipients: Sodium bicarbonate, citric acid (anhydrous), sodium carbonate (anhydrous), sorbitol, sodium saccharinate, povidone (K-25), dimethicone, sodium lauryl sulfate.

How to take, the dosage

For oral administration. Do not exceed the indicated dose! Use the smallest dose necessary to achieve the effect for the shortest time possible! The minimum interval between doses of the preparation Solpadein Fast should be not less than 4 hours.

Adults (including elderly) and children over 12 years:
1-2 tablets dissolved in half a glass of water every 4-6 hours, as needed, but no more than 4 times a day. The maximum daily dose is 8 tablets. The maximum duration of continuous use without medical advice: 5 days as analgesic and 3 days as antipyretic.

If you exceed the recommended dosage of the drug seek immediate medical attention, even if you feel well. Paracetamol overdose may cause hepatic failure.

Patients with impaired renal function:
Before using the drug Solpadein Fast patients with impaired renal function should first consult a physician. Limitations associated with the use of drugs containing a combination of caffeine and paracetamol in patients with impaired renal function, mainly related to the content of paracetamol in the drug.

Patients with impaired liver function:
Before using the drug Solpadein Fast patients with impaired liver function should consult with the doctor. Limitations associated with the use of drugs containing a combination of caffeine and paracetamol in patients with hepatic impairment are mainly related to the content of paracetamol in the drug.

Interaction

If the patient is already taking other drugs, before starting to take the drug Solpadein Fast it is necessary to consult a physician.

When taking regularly for a long time the drug increases the effect of indirect anticoagulants (warfarin and other coumarins), which increases the risk of bleeding. Episodic use of a single dose of the drug has no significant effect on the effect of indirect anticoagulants. It increases the effect of MAO inhibitors.

Inhibitors of paracetamol: barbiturates, carbamazepine, phenytoin, primidone and other anticonvulsants, ethanol, rifampicin, phenylbutazone, butadion, preparations of St. John’s wort and other inducers of microsomal oxidation increase production of hydroxylated active metabolites, causing possible severe liver damage in small overdoses (5 g or more). Inhibitors of microsomal liver enzymes (cimetidine) decrease the risk of hepatotoxic action.

Excretion time of chloramphenicol increases by 5 times under paracetamol action; thereby the risk of levomycetin (chloramphenicol) poisoning increases.

Metoclopramide and domperidone increase, and colestyramine decreases the rate of absorption of paracetamol. The drug may reduce the effectiveness of uricosuric drugs.

Simultaneous administration 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 increase excretion of lithium from the body, so it is not recommended to use the drug simultaneously with lithium-containing drugs.

Special Instructions

If while taking the drug there is no improvement in the condition, or the headache becomes permanent, you should consult a doctor.

The drug Solpadein Fast should not be used with other paracetamol-containing drugs, because the combined use of drugs can cause an overdose of paracetamol.

Paracetamol overdose may cause liver failure that may lead to liver transplantation or death.

The drug Solpadein Fast should not be taken with caffeinated food products (tea, coffee, etc.).etc.) because it may lead to anxiety, restlessness, irritability, insomnia, headache, gastrointestinal disorders, tachycardia, cardiac arrhythmia.

Patients with glutathione deficiency due to eating disorders, cystic fibrosis, HIV infection, starvation, exhaustion, are prone to overdose, so it is necessary to take precautions and is recommended to consult a doctor before taking the drug. Cases of hepatic failure/liver function abnormalities have been recorded in small overdoses of paracetamol (5 g or more) in patients with low glutathione levels, particularly in extremely emaciated patients with anorexia, chronic alcoholism or patients with a low body mass index.

The use of the drug Solpadein Fast in patients with low levels of glutathione, for example, in sepsis, may increase the risk of metabolic acidosis accompanied by symptoms of rapid, difficult breathing (shortness of breath, shortness of breath), nausea, vomiting, loss of appetite. In the simultaneous manifestation of these symptoms should immediately consult a physician.

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

Associated liver diseases increase the risk of further liver damage when taking the drug Solpadein Fast. There is a high risk of overdose when taking the drug in patients with non-alcoholic cirrhosis of the liver. Patients with atopic bronchial asthma, pollinosis have a high risk of allergic reactions.

During uric acid and blood glucose tests the doctor should be informed about the drug intake.

The drug may alter the results of doping control tests in athletes. The sodium content of the tablet (427 mg) should be taken into account while calculating the daily salt intake for patients on a salt-free or low-salt diet.

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

Impact of the drug on the ability to drive vehicles and mechanisms.

Contraindications

– Hypersensitivity to paracetamol, caffeine or any other drug component;
– Severe hepatic and renal disorders;
– Arterial hypertension;
– Glaucoma, sleep disorders;
– Children under 12 years old;
– Pregnancy and breastfeeding;
– Epilepsy;
– Sugars/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption.

– Simultaneous use with other drugs containing paracetamol, lithium and caffeine-containing drinks.

With caution:
– Benign hyperbilirubinemia (incl.ч. Gilbert syndrome)
– Viral hepatitis;
– Alcoholic liver disease;
– Chronic alcoholism;
– Deficiency of glucose-6-phosphate dehydrogenase;
– Mild and moderate degree of liver and kidney function disorders;
– Presence of severe infections.к.
– Usage in patients with glutathione deficiency (in particular in extremely emaciated patients suffering from anorexia or patients with low body mass index).

If any of the above mentioned diseases/conditions/risk factors are present before taking the drug it is necessary to consult with the doctor.

Side effects

The drug is usually well tolerated in the recommended doses. The following adverse reactions were detected spontaneously during post-registration use of the drug.

Adverse reactions are classified by body systems and according to the frequency of development. The frequency of adverse reactions is defined as follows: very common (> 1/10), common (> 1/100 and < 1/10), infrequent (> 1/1000 and < 1/100), rare (>1/10 000 and < 1/1000), very rare (< 10 000), frequency unknown (frequency cannot be estimated based on available data).

Paracetamol:

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

Immune system disorders: very rarely: anaphylaxis, skin hypersensitivity reactions, including skin rash, angioedema (Quincke’s edema), Stevens-Johnson syndrome, toxic epidermal necrolysis.

Respiratory, chest and mediastinal disorders: very rare: bronchospasm in patients with hypersensitivity to acetylsalicylic acid and intolerance to other non-steroidal anti-inflammatory drugs.

Liver and biliary tract disorders: very rarely: liver function disorders.

During long-term use in high doses the possibility of hepatotoxic effect, nephrotoxic effect and pancytopenia increases. If the drug is used for a long time the blood picture should be controlled.

Caffeine:

Disorders of the central nervous system: very rarely: dizziness, headache.

Disorders of the heart: very rarely: palpitation.

Mental disorders: very rare: insomnia, anxiety, irritability, nervousness.

Gastrointestinal disorders: very rare: gastrointestinal disorders.

When using the drug Solpadein Fast it is not recommended to take caffeine-containing products, because it increases the risk of adverse reactions such as insomnia, irritability, anxiety, headache, disorders of the gastrointestinal tract, tachycardia, cardiac arrhythmia.

If any of these adverse reactions occurs, stop taking the drug and consult a physician immediately.

Overdose

Symptoms (due to paracetamol):

Paracetamol overdose can cause liver failure, which may lead to the need for liver transplantation or death. In addition, acute pancreatitis accompanied by hepatic dysfunction and hepatotoxicity has been observed.

Hepatotoxic effects in adults occur when 10 g or more of paracetamol is taken. In the presence of factors affecting the liver toxicity of paracetamol (see sections “Interaction with other medicinal products”, “Particular indications”), liver damage may occur after taking paracetamol in an amount of 5 g or more.

The first signs of overdose are usually seen after 24^48 h and reach maximum development on 4-6 days. During the first 24 hours after overdose the following symptoms may appear: nausea, vomiting, stomach pain, pale skin, anorexia. In 1-2 days the signs of liver damage are determined (painfulness in the liver area, increased activity of “liver enzymes”).

In severe cases of overdose due to liver failure encephalopathy (brain function failure), bleeding, hypoglycemia, brain edema may develop until death, liver transplantation may be required, death. Acute renal failure with acute tubular necrosis is also possible, characterized by pain in the lumbar region, hematuria (blood or red blood cells in the urine), proteinuria (high protein content in the urine), while severe liver damage may not be present. There have been noted cases of cardiac arrhythmias, pancreatitis.

Treatment:

In case of suspected overdose of the drug Solpadein Fast, even in the absence of pronounced initial symptoms, it is necessary to stop using the drug and immediately contact a doctor for medical attention. Within the first hour after overdose, but no later than 4 hours, it is recommended to wash the stomach and take enterosorbents (activated charcoal, polyphepan). 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 during the first 8 hours after overdose, with time the effectiveness of the antidote decreases sharply. If necessary, acetylcysteine is administered intravenously. If there is no vomiting before the patient is admitted to the hospital, methionine may be used.

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

Treatment of patients with severe liver dysfunction 24 hours after paracetamol administration should be done in conjunction with specialists from a toxicology center or a specialized liver disease unit.

Symptoms (due to caffeine):

Epigastric pain, vomiting, frequent urination, tachycardia, arrhythmia, CNS stimulation (insomnia, restlessness, agitation, anxiety, increased neuroreflex excitability, tremors and seizures). 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 against overdose of paracetamol.

Treatment:

There is no specific antidote. Treatment includes supportive measures such as copious drinking and maintenance of vital signs. Within 1 h to 4 h after an overdose, administration of activated charcoal is recommended. To reduce the effects of caffeine on CNS function it is recommended to administer intravenous sedatives and beta adrenoreceptor antagonists to reduce the cardiotoxic effect.

High doses of sodium hydrogen carbonate may cause symptoms of the gastrointestinal tract, including nausea and vomiting. In addition, high doses of sodium bicarbonate may cause hypernatremia.

If hypernatremia is suspected, the patient should have electrolyte levels monitored and appropriate treatment provided.

Pregnancy use

Pregnancy:

The use of the drug during pregnancy is not recommended.

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

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

Breast-feeding period:

Use of the drug during breast-feeding is not recommended.

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

Caffeine
Caffeine penetrates the breast milk and may have a stimulating effect on the breastfed infant, but no significant toxicity has been noted.

Similarities

Migraineum