• Rating:
  • Manufacturer:
  • Model:
    1873
  • Available:
    In stock
  • Availability date:
    2020-07-30
  • Dosage form:
    solution
  • In stock:
    749 Items

$28.50
In stock
Guaranteed refund or reship if you haven't received your order
Secure and encrypted payment processing
We ship to over 40 countries including the USA, UK, Europe, Australia and Japan

Composition:


active ingredient: floroglucinol dihydrate, trimethylfloroglucinol;


4 ml of the solution for injection contains floroglucinol dihydrate 40 mg, which corresponds to floroglucinol 31.12 mg, trimethylfloroglucinol 0.04 mg;


excipients: sodium chloride, hydrochloric acid, water for injection.


Dosage form. Solution for injection.


Basic physical and chemical properties: transparent colorless or slightly yellowish solution without visible mechanical inclusions.


Pharmacotherapeutic group. Other remedies for the treatment of functional disorders of the gastrointestinal tract. ATX code A03A X12.


Pharmacological properties.


Pharmacodynamics.


The drug relieves spasms of smooth muscle fibers and soothes pain.


The chemical compound floroglucinol, together with its methylated form trimethylfloroglucinol, is a phenol derivative with non-specific antispasmodic properties.


The mechanism of action of floroglucinol and its derivatives is based on direct blocking of potential-dependent calcium channels of smooth muscles. Floroglucinol inhibits the action of catechol-O-methyltransferase (COMT), inducing smooth muscle relaxation (reducing the intensity of spasms). Compounds that block t-type calcium channels can eliminate visceral hypersensitivity in animal models.


An equally important mechanism of action of floroglucinol is its inhibitory effect on cyclooxygenase-1 and cyclooxygenase-2. in this way, the effect of floroglucinol on the arachidonic acid Cascade and prostaglandin biosynthesis is realized. And this leads to changes in the implementation of inflammatory reactions and the work of various parts of the body's immune system.


Inhibition of NO-mediated mechanisms facilitates the transmission of arousal due to stretching of the gastrointestinal tract and, as a result, the promotion of intra-intestinal contents along the tract; significantly reduces the tone of smooth muscle cells in in vitro experiments and in vivo trials, including on healthy volunteers.


The protective effect of floroglucinol on cells is carried out under conditions of oxidative stress mediated by catalase activation.


Thus, due to the complex combined mechanism of action, the antispasmodic effect of floroglucinol is realized at the body level: smooth muscle spasms are inhibited with preserved peristaltic activity.


The study of the effect of floroglucinol on the gallbladder and bile ducts showed that this compound partially blocked the contraction of the isolated gallbladder, stimulation of bile outflow and potentiation of the effects of catecholamines.


No less effective was the use of floroglucinol in urology. In particular, a randomized trial was conducted on the efficacy of tamsulosin, nifedipine, and floroglucinol in expulsive therapy of the distal ureters. In these clinical trials, the effectiveness of floroglucinol was confirmed by such indicators as the length of hospital stay, the time of stone removal, the analgesic effect, the need for further hospitalization and endoscopic treatment, as well as the number of working days lost, the level of quality of life and the presence of side effects.


Administration of floroglucinol significantly reduces renal dysfunction and histological damage caused by ischemia and reperfusion injury.


Floroglucinol has an antispasmodic effect on the uterus. In particular, clinical studies have confirmed the ability of the drug, the active ingredients of which are floroglucinol and trimethylfloroglucinol, to effectively improve the opening of the cervix during childbirth and were well tolerated by both the mother and the newborn.


Unlike many other phenols, its pharmacological activity does not decrease under conditions of intravenous administration.


Pharmacokinetics.


The drug is metabolized in the liver by glucuronidation.


In the urine and feces, floroglucinol is excreted unchanged from the body, as well as in the form of sulfo -, glucuronic - and hydroxypohides, such as dimethoxy-1,3-hydroxy-5-benzene and trimethoxybenzene. The elimination Half-Life is about 1 hour and 40 minutes.


Clinical characteristics.


Indications.


* Symptomatic treatment of acute pain associated with functional disorders of the digestive tract and biliary tract;


* treatment of acute spastic and pain syndrome in diseases of the urinary tract (renal colic);


* symptomatic treatment of acute pain syndrome in gynecology.


Contraindications.


Hypersensitivity to the active substance or to any excipient of the drug.


Interactions with other drugs and other types of interactions.


It is necessary to avoid combining Florospasmil with strong painkillers, such as morphine or its derivatives, due to their spasmogenic effect.


Application features.


Use during pregnancy or lactation.


Animal studies have not revealed any teratogenic effects of floroglucinol.


In clinical practice, the use of floroglucinol is quite common; so far, no obvious risk of fetal malformations has been identified.


The drug should be prescribed during pregnancy only as prescribed by a doctor.


In the absence of data, it is recommended to avoid using the drug during breast-feeding.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


Florospasmil does not affect the reaction rate and does not change the ability to drive vehicles or other mechanisms.


Dosage and administration.


Method of application: intravenously, intramuscularly.


Intravenously or intramuscularly, the contents of 1 ampoule are administered – 4 ml of a solution of floroglucinol dihydrate 40 mg and trimethylfloroglucinol 0.04 mg. If necessary, the dose is repeated, but the maximum daily dose should not exceed 12 ml of the solution (contents of 3 ampoules), which corresponds to floroglucinol dihydrate 120 mg and trimethylfloroglucinol 0.12 mg.


Children. Children have no experience of using it.


Overdose.


No overdose cases have been reported. Adverse reactions may occur or increase.


Adverse reactions.


Skin-mucous and allergic manifestations: rash, rarely-urticaria, very rarely – angioedema, anaphylactic shock; hypotension.

Tags: Florospasmil