Pentalgin NEO (paracetamol, naproxen, caffeine)

Instructions for Pentalgin NEO) (paracetamol, naproxen, caffeine)

Description
The pills are oval, biconvex, covered with a film coating from light violet to violet. The cross-section of the kernel is white or almost white.

Active substances Pentalgin NEO
Caffeine + Naproxen + Paracetamol
Release Form
Tablets

Composition
Active ingredients: paracetamol - 325.0 mg, sodium naproxen - 220.0 mg, anhydrous caffeine - 50.0 mg.

Auxiliary substances Pentalgin NEO:
microcrystalline cellulose (microcrystalline cellulose 101) - 175.50 mg, povidone (medium-molecular polyvinylpyrrolidone, povidone K-30) - 36.00 mg, crocarmellose (sodium crocarmellose) - 34.00 mg, potato starch - 30.00 mg, talc - 18.00 mg, magnesium stearate - 7.00 mg, silicon dioxide - 4 colloidal 50 mg.

Envelope: Opadrai 13A200004 PURPLE - 30,000 mg [Hypromellose-2910 (hydroxypropylmethylcellulose-2910) - 14,604 mg, talc - 5,061 mg, povidone - 4,644 mg, titanium dioxide - 2,925 mg, polysorbate-80 - 1,320 mg, red carmine dye (carmine 50%) - 1.167 mg, indigocarmine aluminum lacquer (blue 2) - 0.279 mg].

Pharmacological effect Pentalgin NEO

This combination drug has a powerful pharmacological effect combining several active ingredients.

Naproxen, one of the active components of the drug, is an NSAID that provides analgesic, antipyretic and anti-inflammatory effects. The mechanism of its action is suppression of the activity of the enzymes COX-1 and COX-2, which regulate the process of prostaglandin synthesis. Moreover, the use of naproxen in the form of a sodium salt ensures its rapid absorption and the immediate beginning of an analgesic action.

Paracetamol, another active substance in the composition of the preparation, has both an antipyretic and an analgesic effect. Its action is explained by the blockage of the enzymes cyclooxygenase in the central nervous system, which leads to a decrease in body temperature and the suppression of pain reactions.

Caffeine, the third component of the combination, helps to mitigate sleepiness and fatigue, improves both physical and mental performance. It also dilates the vessels of skeletal muscles, heart, and kidneys and reduces platelet clotting. In the presented combination, caffeine, with a small dosage, does not have a stimulating effect on the central nervous system, but rather increases the tone of cerebral vessels and promotes active blood flow. Caffeine also increases the permeability of histohemic barriers and increases the bioavailability of non-narcotic analgesics, as well as reduces the activity of COX enzymes, through its antagonistic effect on adenosine receptors A(2A) and A(2B). Such an interaction increases the analgesic pain relief effect of analgesics.

Pharmacokinetics Pentalgin NEO

Naproxen is fully and rapidly absorbed from the gastrointestinal tract, providing a high bioavailability rate of 95%. Peak blood levels are reached within 1 to 2 hours after administration. Protein binding of plasma is more than 99%. Half-life with an average lifetime (T1/2) of 12 to 15 hours. Metabolism is carried out in the liver to form dimethylnaproxen, with the participation of the isoenzyme CYP2C9. Excretion is carried out mainly through the kidneys (98%), with 10% of the drug being excreted unchanged and 0.5-2.5% - with bile. Plasma equilibrium concentration is established after 4 to 5 doses of the drug (2 to 3 days).

Acetaminophen is well absorbed from the gastrointestinal tract and peaks at a concentration of 5 to 20 mcg/mL, 0.5 to 2 hours after ingestion. Plasma protein binding is 15%. The drug is capable of penetrating through the blood-brain barrier. Metabolism occurs in the liver, and elimination occurs primarily via the kidneys in the form of glucuronides and sulfate conjugates. Less than 5% of acetaminophen is excreted unchanged. Half-life can range from 1 to 4 hours.

Caffeine is absorbed fully and rapidly from the gastrointestinal tract, peaking at 50 to 75 minutes after ingestion. Its concentration in the blood is 1.58-1.76 mg/l. Caffeine is readily distributed to all organs and tissues in the body without interfering with penetration through the blood-brain barrier and placenta. Blood protein binding is 25 to 36%. More than 90% of caffeine is metabolized in the liver. Half-life in adults is usually 3.9 to 5.3 hours, sometimes up to 10 hours. Excretion is via the kidneys (1 to 2% unchanged).

Indications for Pentalgin NEO

• this combination drug include treatment of various types of pain:
• musculoskeletal pain (including osteoarthritis, radicular syndrome, arthritis, myalgia),
• neuralgia,
• toothache,
• headache,
• migraine,
• algodysmenorrhea,
• and pain after injury or surgery accompanied by inflammation.