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.

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