Safiston, tablets 20 pcs

Pharmacotherapeutic group:

An analgesic combined (NSAID+analgesic non-narcotic agent+psychostimulant).

ATC code:

N02BE51

Pharmacological properties

Pharmacodynamics

Safiston is a combined drug, the effect of which is determined by the components that make up it. The combination of the three components of the drug leads to mutual enhancement of their pharmacological action. Paracetamol and propiphenazone have analgesic and antipyretic effects.

Paracetamol is a non-narcotic analgesic. It blocks cyclooxygenase (COX) only in the central nervous system (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 lack of anti-inflammatory effect.

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

Propiphenazone is a pyrazolone derivative. Its mechanism of action is by inhibiting COX, involved in the formation of prostaglandins from arachidonic acid.

Caffeine increases reflex excitability of the spinal cord, stimulates respiratory and vasomotor centers, dilates blood vessels of skeletal muscles, brain, heart and kidneys, reduces platelet aggregation, reduces sleepiness, fatigue.

In this combination low-dose caffeine has almost no stimulating effect on the central nervous system, but helps to regulate the tone of the brain vessels, reduces sleepiness, increases the analgesic effect of other drug components.

Pharmacokinetics

Paracetamol

Absorption – high, binding to plasma proteins – 15%, time to reach maximum plasma concentration (Tcmax) – 20-30 minutes. It penetrates through the blood-brain barrier (BBB). Less than 1% of dose taken by a nursing mother passes into breast milk.

Therapeutic effective concentration of paracetamol in plasma is achieved when administered at a dose of 10-15 mg/kg.

Metabolized in the liver: 80% reacts in conjugation with glucuronic and sulfuric acids to form inactive metabolites, 17% reacts in hydroxylation to form inactive metabolites, which conjugate with glutathione to form inactive metabolites.

If there is a lack of glutadione these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The elimination half-life is 2-3 hours. In elderly patients, paracetamol clearance is decreased and the elimination half-life is increased. Excreted by the kidneys unchanged in 3%.

Propifenazone

Maximum concentration of propifenazone in plasma is reached after 30 minutes. It is metabolized in the liver. Half-life period is 1-1.5 hours. Combination with paracetamol increases its elimination time by 40%, which plays a significant role as it allows reducing the number of drug intakes during a day. It is eliminated by kidneys.

Caffeine

Time of maximum concentration – 1 hour; elimination half-life – 3.5 hours; 65-80% of caffeine is eliminated by kidneys mainly as 1-methyloxatin, 1-methylureic acid and acetylated derivatives of uracil, a small amount is transformed into theophylline and theobromine.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

When using the drug for a long time (more than 5 days) it is necessary to monitor the peripheral blood picture and the functional state of the liver.

During the treatment it is necessary to refrain from drinking alcohol-containing beverages (increased risk of gastrointestinal bleeding).

The excessive use of caffeine-containing products (coffee, tea) during the treatment may cause overdose symptoms. Taking the drug may make it difficult to establish a diagnosis in acute abdominal pain syndrome.

Impact on the ability to drive vehicles and operate machinery requiring high concentration

Contraindications

Side effects

Overdose

Pregnancy use

Similarities