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Description of the active substance Dicyclomine / Dicyclomine.
Formula: C19H35NO2, the chemical name: 1-cyclohexylcyclohexanecarboxylic acid, beta- (diethylamino) ethyl ether (as hydrochloride).
Pharmacological group: vegetotrophic agents / cholinolytic agents / m-cholinolytics; organotropic agents / antispasmodic myotropic.
Pharmacological action: myotropic, anticholinergic, spasmolytic.
Dicyclomine is a quaternary amine. Dicyclomine has anticholinergic activity, eliminates spasm of smooth muscles of the gastrointestinal tract and reduces the pain syndrome caused by it. In animal studies (in vitro studies using isolated guinea-pig small intestine), it has been established that the effect of Dicyclomine is mediated by the following mechanisms: direct action on smooth muscles, as indicated by the ability of dicycols to block histamine and bradykinin-induced spasms (atropine does not alter the response to these two agonists); a specific anticholinergic effect on the acetylcholine receptor sites, which is similar to the action of atropine (antimuscarinic activity). In in vivo studies in dogs and cats, Dicyclomine was approximately equally effective against intestinal spasms, which are caused by barium chloride and acetylcholine. The absence of a significant effect of Dicyclomine on the secretion of salivary glands (in studies in rabbits, dicyclosterin showed 1/300 of atropine activity), and also on the pupil (in studies on mice, the activity of mydriatic effects was about 1/500 of atropine activity).
Data on the possible mutagenicity and carcinogenicity of Dicyclomine hydrochloride in humans are absent. There were no long-term animal studies to assess the possible carcinogenicity of Dicyclomine.
Dicyclomine did not have a dangerous effect on reproduction, conception and labor in studies in rats when administered at doses up to 100 mg / kg per day.
Dicyclomine is well absorbed, and faster and easier after intramuscular injection (10 to 20 minutes) than after oral administration (after 1 to 1.5 hours). The elimination half-life is 1.8 hours. It is excreted from the body after 9 to 10 hours mainly with urine (approximately 80%) and in small amounts – with feces.
Colic (renal, hepatic, intestinal), algodismenorea.
Method of application of Dicyclomine and dose
Dicyclomine is administered intramuscularly, taken internally. The dose is set individually.
Before using Dicyclomine, it should be clarified whether the patient has tachycardia, because Dicyclomine can increase the heart rate.
Caution is prescribed Dicyclomine at high ambient temperature (due to decreased sweating, the risk of hyperthermia and heat stroke increases). It is necessary to know that diarrhea can be an early symptom of incomplete intestinal obstruction, especially in patients with colostomy or ileostomy. In these cases, dicyclosterin hydrochloride therapy is not indicated and, possibly, will be dangerous.
There are reports that in patients with hypersensitivity anticholinergic drugs can cause psychosis.
Action on the central nervous system manifests itself in the development of symptoms such as disorientation, confusion, short-term memory loss, dysarthria, hallucinations, ataxia, euphoria, coma, decreased anxiety, insomnia, weakness, mannerisms, agitation, inadequate emotional reactions. After discontinuation of dicyclosterine, these symptoms usually decrease within 12 to 24 hours.
When treating Dicyclomine, potentially dangerous activities that require increased attention, rapid mental and motor reactions (including the management of vehicles, mechanisms) should be avoided.
Contraindications for use
Hypersensitivity, obstructive diseases of the gastrointestinal, urinary and hepatic tracts, reflux-esophagitis, peptic ulcer and duodenal ulcer, severe ulcerative colitis (there may be a decrease in intestinal peristalsis, up to the development of paralytic intestinal obstruction, the appearance or exacerbation of toxic megacolon), myasthenia gravis , glaucoma, unstable cardiovascular system with acute bleeding, hypovolemic shock, children’s age (up to 6 months), pregnancy, ne The rate of breastfeeding.
Restrictions on the use
Impaired liver and kidney function (decreased kidney excretion may increase the risk of adverse reactions), autonomic neuropathy, tachycardia, including in hyperthyroidism (possibly amplification), heart disease (including coronary heart disease, congestive heart failure, tachyarrhythmia), hypertension (possibly exacerbation), hypertrophy of the prostate gland, hernia of the esophageal opening of the diaphragm, ulcerative colitis, age under 18 years.
Application in pregnancy and lactation
During pregnancy, the use of dicyclovir is contraindicated. Strictly controlled and adequate studies in humans are not conducted. In reproductive studies in rabbits and rats that received Dicyclomine hydrochloride in doses up to 33 times higher than the maximum recommended doses for humans (3 mg / kg or 160 mg / day), undesirable effects on the fetus or effects on fertility have not been revealed. Dicycloceridine is contraindicated in breastfeeding. It has been reported that Dicyclomine hydrochloride is excreted in breast milk; in children who are breastfed, development of a respiratory distress syndrome is possible. It is necessary to stop breastfeeding for the duration of Dicyclomine therapy.
Side effects of Dicyclomine
Digestive system: dry mouth, loss of taste, nausea, constipation, anorexia, dyspepsia, vomiting, decreased appetite.
Nervous system and sensory organs: dizziness, blurred vision, drowsiness, weakness, nervousness, disorientation, confusion, psychosis, short-term memory loss, dysarthria, hallucinations, ataxia, euphoria, coma, decreased anxiety, insomnia, weakness, mannerisms, agitation, inadequate emotional reactions, increased intraocular pressure, paralysis of accommodation.
Other: tachycardia, decreased sweating, urinary retention, allergic reactions.
Interaction of Dicyclomine with other substances
The effects of Dicyclomine, including side effects, may enhance drugs that have anticholinergic activity: class I antiarrhythmics (eg, quinidine), amantadine, antihistamines, benzodiazepines, antipsychotics (eg phenothiazines), monoamine oxidase inhibitors, nitrites and nitrates, narcotic drugs analgesics, tricyclic antidepressants, sympathomimetics.
Anticholinergic drugs (including Dicyclomine) counteract the effect of antiglaucoma drugs.
In the presence of increased intraocular pressure, anticholinergic drugs (including Dicyclomine) can be dangerous when used in conjunction with corticosteroids.
Anticholinergic drugs (including Dicyclomine) can affect the absorption in the digestive tract digoxin and increase the concentration of digoxin in the blood plasma.
Anticholinergic drugs (including Dicyclomine) can counteract the effects of drugs that alter the motor activity of the gastrointestinal tract (metoclopramide).
Antacids can act on the absorption of anticholinergic drugs (including dicyclosterin), so avoid sharing them.
Oppression with anticholinergic drugs (including Dicyclomine) secretion of hydrochloric acid counteracts the action of drugs that are used to test gastric secretion or therapy with achlorhydria.
With an overdose of Dicyclomine, nausea, vomiting, dry mouth, difficulty swallowing, headache, dizziness, dilated pupils, prolonged blurred vision, tachycardia, increased respiration, fever, heat, dry skin, excitation of the central nervous system; perhaps curare-like action (i.e. neuromuscular blockade, which leads to muscle weakness and, possibly, paralysis).
Treatment: induction of vomiting, gastric lavage, the use of activated charcoal; for arresting excitation used drugs with sedative effect (benzodiazepines, short-acting barbiturates); as an antidote, in the presence of indications, appropriate cholinergic drugs may be used.
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