pharmachologic effect
Spazmalgon is a combined analgesic with pronounced spasmolytic activity. The composition of the drug Spazmalgon includes three active components - metamizole sodium, pituopenone hydrochloride and fenpiverinia bromide.
The mechanism of action of the drug and its pharmacological effects are based on the pharmacological properties of the active components that make up its composition.
Metamizole sodium is a non-steroidal anti-inflammatory drug, a derivative of pyrazolone. Metamizole sodium has a pronounced analgesic effect, has an anti-inflammatory and antipyretic effect. The mechanism of action of metamizole sodium is associated with its ability to inhibit the activity of the enzyme cyclooxygenase, as a result of which the metabolism of arachidonic acid is disrupted and the synthesis of pro-inflammatory prostaglandins, prostacyclines and thromboxane is reduced. Metamizole sodium belongs to the group of nonselective nonsteroidal anti-inflammatory drugs and equally inhibits the activity of both isoforms of the cyclooxygenase enzyme - cyclooxygenase-1 and cyclooxygenase-2. Due to a decrease in the number of prostaglandins in the focus of inflammation, the sensitivity of chemoreceptors to the endings of afferent neurons of pain sensitivity to bradykinin and histamine decreases. In addition, a decrease in the number of prostaglandins in the inflammatory focus leads to a decrease in the production of endogenous biologically active substances taking part in the inflammatory reaction. Thus, metamizole sodium has an analgesic effect due to a decrease in the activity of the inflammatory process and a decrease in the effect of inflammatory mediators on painful ends. The antipyretic effect of the drug is associated with a decrease in the number of prostaglandins in the center of thermoregulation in the hypothalamus.
Pitophenone hydrochloride - a derivative of piperidine, has spasmolytic myotropic activity. The drug has a papaverin-like effect, causes a decrease in tone and relaxation of smooth muscles. Pitophenone hydrochloride helps to eliminate the pain syndrome caused by spasm of smooth muscles of the internal organs.
Fenpiverinia bromide is a drug of the M-cholinoblocker group, which contains quaternary nitrogen in its structure. The drug removes the spasm of the smooth muscle layer of the internal organs, reduces tone and reduces the motility of the stomach and intestines, relaxes the smooth muscles of the urinary and bile ducts.
Pharmacologically active substances that are part of the drug Spazmalgon, mutually reinforce the therapeutic effect of each other.
Pharmacokinetic properties of the drug are presented on the basis of pharmacokinetic parameters of metamizole sodium, as at the moment there is no reliable data on the pharmacokinetics of pituophenone hydrochloride and fenpiverinium bromide.
When administered orally, metamizole sodium is well absorbed in the gastrointestinal tract. In the intestinal wall, the drug is hydrolyzed to form a pharmacologically active substance, the peak concentration of the active substance in the blood plasma is observed 30-120 minutes after oral administration.
With parenteral administration, the bioavailability of the drug is about 85%.
The active substance is partially bound to plasma proteins. Metabolised in the liver with the formation of pharmacologically active metabolites. It is excreted mainly by kidneys in the form of metabolites, a small part is excreted by the liver. About 3% of the drug is excreted from the body in the form of unchanged metamizole. The amount of the drug that undergoes biotransformation individually for each patient and depends on many factors, including the genetically determined type of acetylation.
In patients suffering from cirrhosis, there is a change in the metamizole clearance.
Indications for use
The drug Spazmalgon in the form of tablets is used for symptomatic treatment of patients with pain syndrome of mild or moderate intensity, including the drug is indicated in such diseases:
Diseases of the urinary tract, which are accompanied by pain syndrome and urination disorders, including inflammatory diseases of the urinary system and urolithiasis.
Gastric and intestinal colic, diseases of the digestive tract, which are accompanied by a spasm of smooth muscles of the intestine and stomach and pain syndrome.
Dyskinesia of the biliary tract, cholelithiasis.
The drug Spazmalgon in the form of tablets is also used to relieve the pain syndrome of mild or moderate intensity in primary and secondary dysmenorrhea.
If necessary, the drug can be used for the symptomatic treatment of pain in patients suffering from musculoskeletal and neuralgia. However, in this case, the drug is recommended to be used for a short time.
The drug Spazmalgon in the form of a solution for injection is used to relieve the severe pain syndrome caused by spasms of smooth muscles, including:
Spasm of smooth muscles of the ureter and bladder, as well as renal colic, which are accompanied by a painful syndrome of mild and moderate intensity.
Diseases of the liver and bile ducts, which are accompanied by severe pain syndrome, including hepatic (biliary) colic, dyskinesia of the biliary tract, dysfunction of the sphincter of Oddi (postcholecystectomy syndrome).
Diseases of the gastrointestinal tract, which are accompanied by pains of a spastic nature, including intestinal colic and chronic colitis.
Diseases of the pelvic organs, which are accompanied by a painful syndrome of mild and moderate intensity.
Pain relief for primary and secondary dysmenorrhea.
Mode of application
Preparation Spazmalgon in the form of tablets are taken orally, the tablet is swallowed whole, not crushing and not chewing, with enough water. If necessary, the tablet can be divided. The duration of the course of treatment and the dose of the drug is determined by the attending physician individually for each patient, depending on the nature of the disease and the individual characteristics of the patient.
For the treatment of spasmodic pain, adults and adolescents over 15 years of age are usually prescribed 1-2 tablets of the drug 2-3 times a day. It is not recommended to take more than 6 tablets a day.
For the treatment of spasmodic pain, children aged 13 to 15 years are usually prescribed 1 tablet of the drug 2-3 times a day. It is not recommended to take more than 3 tablets a day.
For the treatment of spasmodic pain, children aged 9 to 12 years are usually prescribed 1/2 tablet of the drug 2-3 times a day. It is not recommended to take more than 2 tablets a day.
The drug is not recommended for more than 3 days in a row, unless the doctor has appointed otherwise.
The drug Spasmalgon in the form of a solution for injection is used only for intramuscular injection. The duration of the course of treatment and the dose of the drug is determined by the attending physician individually for each patient, depending on the nature of the disease and the individual characteristics of the patient.
Adults and adolescents over the age of 15 years are usually prescribed 2-5 ml of medication 2-3 times a day for the treatment of spasmodic pains. It is recommended to observe the interval between injections of the drug for at least 6 hours. It is not recommended to administer more than 10ml of the drug per day.
The drug is not recommended for more than 3 days in a row, unless the doctor has appointed otherwise.
In the absence of the necessary therapeutic effect, the drug is stopped. If there is a positive trend, therapy is continued with Spasmalgon in the form of tablets.