Pyralgin
Medical supervision is required while taking the drug.
When using the drug for more than 5 days, it is necessary to monitor the peripheral blood picture and the functional state of the liver.
Taking the drug may make it difficult to establish a diagnosis for acute pain in the abdominal area.
During the period of productive cough, it is able to suppress the cough reflex, which can lead to the accumulation of sputum in the lumen of the bronchi and, as a result, to a deterioration in the patient’s condition. The patient must be informed that with prolonged use of the drug without appropriate medical supervision, addiction and drug dependence may develop.
During treatment with Piralgin, it is necessary to refrain from drinking alcohol due to worsening tolerability of the drug.
Piralgin should not be taken by patients who have previously experienced hypersensitivity to medications containing metamizole sodium.
The drug should be avoided in patients with gastric and duodenal ulcers in the acute phase, as well as in patients with severe renal and liver failure.
Metamizole sodium contained in the drug Piralgin may turn the urine red, but this has no clinical significance.
The drug Piralgin should be taken with caution in elderly patients in whom signs of intoxication occur more often.
Long-term use of the drug Piralgin can lead to the development of codeine addiction.
Phenobarbital can be addictive. The formation of dependence can occur with long-term uncontrolled use of the drug. If a patient develops an addiction, the intervention of a specialist narcologist is required.
Participation of the CYP2D6 isoenzyme in metabolism
Codeine is metabolized by the CYP2D6 isoenzyme to the active metabolite, morphine. If the patient has insufficient activity of this isoenzyme, or this enzyme is absent in the body, it is not possible to achieve a sufficient analgesic effect during treatment. An estimated 7% of the Caucasian population has insufficient CYP2D6 activity. With high metabolic activity of codeine, there is an increased risk of developing adverse effects of opioid toxicity, even when taking the drug in recommended doses. In patients in this group, codeine is rapidly metabolized to morphine, which reaches higher plasma concentrations than in the rest of the population.
Common symptoms of opioid toxicity include: confusion, drowsiness, shallow breathing, constricted pupils, nausea, vomiting, constipation and lack of appetite. In severe cases, circulatory and respiratory collapse may develop, which poses a threat to the patient's life.
The expected frequency of high isoenzyme activity for different isoenzymes in different populations is shown below:
| Population | Frequency % |
| Africans/Ethiopians | 29% |
| African Americans | 3,4-6,5% |
| Mongoloid race | 1,2-2% |
| Caucasian | 3,6-6,5% |
| Greeks | 6,0% |
| Hungarians | 1,9% |
| Northern Europeans | 1-2% |
I.B. Muravyova, JSC "Research and Production, pharmacist"
PIRALGIN is the drug of choice for moderate pain. As defined by the International Association for the Study of Pain (IASP), pain is an unpleasant sensory and emotional sensation associated with actual or potential tissue damage, or described in terms of such damage. On the one hand, the ability to feel pain helped a person survive in the process of evolution, since, being a mechanism of adaptation to existence in the surrounding aggressive environment, it gave a signal about existing damage, the need to stop contact with the aggressive factor and mobilize the body’s strength for recovery . However, pain can be not only a signal of danger. Under conditions of strong and prolonged irritation, it itself can acquire the features of an irritating factor, causing severe stress and depletion of the reserves of the nervous, endocrine and cardiovascular systems of the body, causing painful shock. Pain is the most common symptom, for which almost half of all patients seek medical help. Each specific manifestation of a pain reaction requires the prescription of a drug from a specific pharmacological group. The most pronounced analgesic effect among drugs that reduce the concentration of endogenous algogens is possessed by drugs from the pharmacological group “Non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs”. The mechanism of anti-inflammatory, analgesic and antipyretic action of non-steroidal anti-inflammatory drugs is associated with inhibition of the activity of a special enzyme - cyclooxygenase (COX), which occurs both in peripheral tissues and in the structures of the central nervous system. Non-narcotic analgesics and most NSAIDs block the activity of both isoforms of cyclooxygenase. The effectiveness and toxicity of “standard” drugs from the group “Non-narcotic analgesics, including NSAIDs and other anti-inflammatory drugs” is usually associated with their low selectivity, i.e. ability to suppress the activity of both to the same extent • NSAIDs that significantly suppress the activity of COX-1 (acetylsalicylic acid, indomethacin, piroxicam) more often cause damage to the digestive tract than
• NSAIDs that exhibit equivalent inhibitory activity against both isoforms of COX (diclofenac sodium, ibuprofen, pyralgin, etc.), and even more so
• NSAIDs-selective COX-2 inhibitors, which are considered the least toxic, however, can increase the risk of heart attacks (Celecoxib, Rofecoxib, etc.).
When prescribing drugs in this group, one should take into account the safety of use for the patient, the cause and intensity of pain, as well as the severity of the concomitant inflammatory process. The chosen remedy should eliminate pain as much as possible and not cause serious side effects. The traditional tactics recommended by WHO (1986) for the treatment of chronic and acute pain are to prescribe non-opioid analgesics from the pharmacological group “NSAIDs, including non-narcotic analgesics”. For moderate to severe pain that is not relieved by non-opioid analgesics, your doctor will prescribe an opioid analgesic on a special prescription form. The drug Piralgin tablets, produced by the Belarusian enterprise RUE Belmedpreparaty, is a drug prescribed for moderate pain syndrome and is sold in pharmacies without a doctor’s prescription. One tablet of the drug Piralgin contains 300 mg of analgin (metamizole sodium), 100 mg of naproxen, 50 mg of caffeine, 10 mg of phenobarbital, 8 mg of codeine. The drug has analgesic, antipyretic, anti-inflammatory, antispasmodic, and sedative effects. Piralgin is a combination drug that combines the properties of active ingredients. Metamizole sodium and naproxen are drugs from the group of non-narcotic analgesics that have a pronounced anti-inflammatory, antipyretic effect, and analgesic activity, which is enhanced by codeine (blocks opiate receptors, stimulates the antinociceptive system and changes the emotional perception of pain). Iieeeeeeeea .5 2008 tel./fax editorial office: (495) 6727029\92, 3684703
Iaa.ieiaey Naproxen also has a pronounced anti-inflammatory effect. Phenobarbital has a sedative effect. Caffeine causes dilation of blood vessels in skeletal muscles, brain, heart, kidneys; increases mental and physical performance, helps eliminate fatigue and drowsiness; increases blood pressure during hypotension; increases the permeability of histohematic barriers and increases the bioavailability of non-narcotic analgesics, thereby enhancing the therapeutic effect. The components of the drug are well absorbed in the gastrointestinal tract. Metamizole sodium: in the intestinal wall it is hydrolyzed to form an active metabolite, 4-methyl-amino-antipyrine, which in turn is metabolized to 4-formyl-amino-antipyrine and other metabolites. The level of binding of the active metabolite to proteins is 50–60%. Excretion of metabolites passes through the kidneys. In addition, metabolites are excreted in breast milk. Naproxen: bioavailability is 95%. Binds to blood proteins. The half-life is 12–15 hours. It is excreted in the urine mainly in the form of a metabolite (dimethylnaproxen), in small quantities in bile. Caffeine: well absorbed in the intestine, half-life is 5 hours (sometimes up to 10 hours). It is excreted primarily by the kidneys in the form of metabolites, about 10% unchanged. Codeine: slightly bound to plasma proteins. It undergoes biotransformation in the liver (10% is converted into morphine by demethylation). Excreted by the kidneys (5–15% unchanged). Phenobarbital: bioavailability is 80%. In plasma, it is 50% protein bound and penetrates well through the placenta. Biotran is formed in the liver. The main metabolite has no pharmacological activity. It is excreted by the kidneys, including 20–25% unchanged. Piralgin is indicated for moderately severe pain syndromes of various origins. Particularly effective
Iieeeeeeeea .5 2008 tel./fax editorial office: (495) 6727029\92, 3684703
effective for pain in joints, muscles, radiculitis, menstrual pain, neuralgia, as well as for headaches, migraines, toothaches. Piralgin can be used for fevers, colds and other diseases accompanied by pain and inflammation. The drug is usually prescribed 1 tablet 1-3 times a day. The maximum daily dose is 4 tablets. The drug should not be taken for more than 5 days as an anesthetic without a doctor's prescription. When using the drug, dyspeptic disorders, allergic skin reactions, epigastric pain, dizziness, drowsiness, and palpitations are possible. Rarely, suppression of hematopoiesis. The main contraindications include hypersensitivity to the components of the drug, severe dysfunction of the liver or kidneys, peptic ulcer of the stomach and duodenum in the acute stage, bronchospasm, blood diseases, increased intracranial pressure, cranial trauma, acute myocardial infarction, alcohol intoxication, glaucoma, pregnancy and breastfeeding, as well as children under 12 years of age. Thus, the 5-component composition of the drug, significantly expanding the range of indications for use, the unique composition of components that mutually enhance each other’s effects, a longer anti-inflammatory effect, a proven therapeutic effect in combination with its affordability for patients - there, with limited financial resources, there are advantages of Piralgin compared to other drugs of the pharmacological group “Non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs”.
Literature 1. Guidelines “Procedure and timing of prescribing narcotic analgesics,” Ministry of Health of the Russian Federation, No. 2001/129 dated July 19, 2001.
2. Kukushkin M.L. Etiopathogenetic principles of treatment of chronic pain, journal “Attending Physician”, No. 4, April 2008.
3. Ananyev L.P. “Combined analgesics in the treatment of pain syndromes”, journal “Consilium medicum”, volume 07/№08/2005.
