Citramon-ExtraCap, 240 mg+27, 45 mg+180 mg capsules 10 pcs.

Pharmacotherapeutic group: analgesic combined agent (NSAID + non-narcotic analgesic + psychostimulant)

ATX code: [N02BA71]

Pharmacological properties

Pharmacodynamics

A combination drug.

Acetylsalicylic acid (ASA) has antipyretic and anti-inflammatory effects, relieves pain, especially caused by inflammation, and inhibits thrombosis, improves microcirculation in the inflamed area.

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; it reduces sleepiness and fatigue and increases mental and physical efficiency. In this combination, a small dose of caffeine has practically no stimulating effect on the central nervous system; it increases the tone of cerebral blood vessels and accelerates blood flow.

Paracetamol has analgesic, antipyretic and mild anti-inflammatory effects due to its effect on the thermoregulation center in the hypothalamus and a weak ability to inhibit the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics

ASK: When taken orally, absorption is complete. During absorption it undergoes presystemic elimination in the intestinal wall and systemic elimination in the liver (deacetylated). The resorbed part is quickly hydrolyzed by cholinesterases and albumin esterase, so the half-life is no more than 15-20 minutes. Circulates in the body (75-90% in connection with albumin) and is distributed in tissues as salicylic acid anion. Time of reaching maximum concentration is 2 hours. Metabolized mainly in liver with formation of 4 metabolites found in many tissues and urine. It is excreted by active secretion in the renal tubules as salicylate (60%) and its metabolites. Excretion of unchanged salicylate depends on urine pH (when urine is alkaline, ionization of salicylates increases, their reabsorption worsens, and excretion significantly increases). The elimination rate depends on the dose: when taking small doses, the elimination half-life is 2-3 hours, with increasing doses it can increase up to 15-30 hours. In infants the elimination of salicylates is much slower than in adults.

Paracetamol: adsorption is high, the maximum concentration is reached after 0.5-2 hours and is 5-20 mcg/ml, plasma protein binding is 15%. It penetrates the blood-brain barrier. Less than 1% of the dose taken by a nursing mother penetrates into breast milk. The therapeutically effective plasma concentration of paracetamol is achieved at a dose of 10-15 mg/kg. It is metabolized in the liver (90-95%): 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione to form already inactive metabolites. In glutathione deficiency, these metabolites can block hepatocyte enzyme systems and cause necrosis. The CYP2E1 isoenzyme is also involved in metabolism. The elimination half-life is 1-4 hours. It is excreted by kidneys as metabolites, mainly as conjugates. Only 3% are eliminated unchanged. In elderly patients the drug clearance is decreased and the elimination half-life is increased.

Caffeine: when taken orally absorption is good, occurs throughout the intestine. Absorption is mainly due to lipophilicity rather than water solubility. Maximum concentration is reached after 50-75 min and is 1.58-1.76 mg/l. It is rapidly distributed in all organs and tissues of the body: easily penetrates through the blood-brain barrier and the placenta. Distribution volume is 0.4-0.6 l/kg in adults and 0.78-0.92 l/kg in newborns. Blood protein (albumin) binding is 25-36%. It is metabolized in liver by more than 90 %, in children of first years of life by 10-15 %. In adults, about 80% of caffeine doses are metabolized to paraxanthine, about 10% to theobromine, and about 4% to theophylline, which are later demethylated to monomethylxanthines, and then to methylated uric acids. The half-life in adults is 3.9-5.3 hours (sometimes up to 10 hours), in infants it is 65-130 hours (by 4-7 months of life it decreases to adult values). Excretion of caffeine and its metabolites is by the kidneys (1-2% in adults is excreted unchanged, in infants – up to 85%).

Indications

Active ingredient

Composition

Active substances:

acetylsalicylic acid – 240.0 mg,

paracetamol – 180.0 mg,

caffeine – 27.45 mg;

excipients:

citric acid (citric acid monohydrate) – 5.00 mg,

p> potato starch – 20.95 mg,

talc – 10.00 mg,

Low molecular weight povidone (polyvinylpyrrolidone low molecular weight medical 12600±2700 or K-17) – 3.00 mg,

calcium stearate – 1.00 mg,

colloidal silicon dioxide (aerosil) – 2.60 mg.

Solid gelatin capsules #00.

Composition of the capsule shell (body and cap):

Titanium dioxide (E 171) – 2.6666 %, quinoline yellow (E 104) – 1.8394 %, sunset yellow dye (E 110) – 0.0088 %, gelatin – up to 100 %.

How to take, the dosage

Interaction

Contraindications

Side effects

Overdose

Similarities