Spasmolytics
Spasmolytics
Currently, to relieve pain in biliary dyskinesia, smooth muscle relaxants and antispasmodics are used, including several groups of drugs:
1. Anticholinergics.
2. Nitrates.
3. Calcium channel blockers.
4. Myotropic antispasmodics.
The group of anticholinergics includes the widely used M-anticholinergic drugs (belladonna drugs, platifillin, metacin, hyoscine butyl bromide). These drugs, with the exception of hyoscine butyl bromide, which is prescribed to 0.01 g 3 times a day, have currently been limited in use for the treatment of functional disorders of HIV. Additionally, M1-cholinergic receptor blocker, pirenzepine (0.05 g, 2–3 times a day), M-holinoblocker Dicycloverin (0.02 g i/m) can be prescribed.
Dicycloverinum (Dicycloverinum), Trigan. The substance is included in the composition of drugs with the following trade names: Trigan; Trigan-D (in combination with paracetamol); Dolospatabs (in combination with paracetamol).
Pharmacodynamics. Dicycloverin has anticholinergic activity, eliminates spasm of the smooth muscles of the gastrointestinal tract and reduces the pain caused by it. The effect of dicycloverin is mediated by the following mechanisms: a direct effect on smooth muscles, as indicated by the ability of dicycloverine to block histamine and bradykinin induced spasms (atropine does not change the response to these two agonists); specific anticholinergic effect on M-cholinergic receptors.
Pharmacokinetics. Dicycloverin is well absorbed, faster and easier after i/m administration (after 10 - 20 minutes), rather than after oral administration (after 1 - 1.5 hours). The half-life is 1.8 hours. Excreted in 9 - 10 hours mainly with urine (approximately 80%) and in small quantities with feces.
Indications. Colic (renal, hepatic, intestinal) algomenorrhea.
Administration routs: Dicycloverin is administered intramuscularly, orally. The dose is set individually.
Restrictions. Disruption of liver and kidney function (reduction of kidney excretion may increase the risk of adverse reactions), autonomic neuropathy, tachycardia, including with hyperthyroidism (possibly increased), heart disease (including ischemic heart disease, congestive heart failure, tachyarrhythmia), hypertension ( possible exacerbation), prostatic hypertrophy, hiatal hernia, ulcerative colitis, age under 18.
Adverse reactions.
Digestive system: dry mouth, loss of taste, nausea, constipation, anorexia, dyspepsia, vomiting, loss of appetite.
Nervous system and sense organs: dizziness, blurred vision, drowsiness, weakness, nervousness, disorientation, confusion, psychosis, short-term memory loss, dysarthria, hallucinations, ataxia, euphoria, coma, anxiety reduction, insomnia, weakness, mannerism, agitation, inadequate emotional reactions, increased intraocular pressure, accommodation paralysis.
Other: tachycardia, reduction of sweating, urinary retention, allergic reactions.
Dosage forms: Trigan (dicycloverine hydrochloride). Available in the form of a 1% solution for intramuscular administration. Ampoules of 2 ml (20 mg per amp.). 20 mg tablets. The maximum daily dose is 80 mg.
Nitroglycerin is used for rapid relief of pain, nitrosorbitol - for systematic treatment. The mechanism of action of nitrates includes the formation of free radicals of nitric oxide in smooth muscles that activates guanylate cyclase and increases the cGMP content, which leads to their relaxation. However, due to the pronounced cardiovascular effects and development, they are not very acceptable in long-term therapy for dyskinesia.
Slow calcium channel blockers:
A. Nonselective - nifedipine, verapamil, diltiazem, and others cause relaxation of smooth muscles, while having numerous cardiovascular effects. To achieve gastrointestinal effects, high doses are required, which virtually prohibits their use. However, in the literature there are examples of successful treatment with nifedipine. Patients noted the relief of subjective symptoms of CO dysfunction, which developed after cholecystectomy.
B. Selective-pinaverium bromide. These drugs mainly act at the level of the colon. Only 5–10% of drugs act at the level of the biliary tract and have indirect effects associated with a decrease in intraluminal pressure, which facilitates the passage of bile.
Pinaverium bromide. Ditsetel
Pharmacodynamics. It blocks calcium channels selectively in the smooth muscle cells of the gastrointestinal tract (mainly the biliary tract and intestines). The myotropic effect of pinaverium bromide is combined with m-anticholinergic properties. It reduces spasms of smooth muscles of the abdominal organs, accelerates the evacuation function of the stomach, reduces the secretion of hydrochloric acid. The drug in the majority (up to 85%) of patients suppresses pain and dyspeptic syndromes, normalizes biliary and intestinal motility.
Pharmacokinetics. After oral administration, less than 10% of the drug is absorbed in the gastrointestinal tract. The maximum plasma concentration is noted after 1 hour. It bunds to plasma proteins by 97%. Metabolized mainly in the liver. Excreted by the intestines, a small part - with the urine.
Methods of application. Tablets are taken with food entirely, without chewing. Tablets of 0.05 g are prescribed to be taken as1 tablet X 3 times / day. , if necessary, 2 tabl. x 3 times / day.
Contraindications. Hypersensitivity, intestinal atony, paralytic intestinal obstruction, severe ulcerative colitis, toxic megacolon.
Restrictions. Breastfeeding, pregnancy, child age.
Adverse reactions. Dyspeptic phenomena, constipation, nausea, allergic reactions, abdominal pain, diarrhea, vomiting, dysphagia, damage to the esophageal mucosa, rash, urticaria, itching, erythema, hypersensitivity.
Dosage form. Tablets of 0.05 and 0.1 g.
Non-selective myotropic antispasmodics (papaverine, drotaverine, baralgin) patients with dyskinesia of the bile excreting tracts are advised to use them to relieve a painful attack.
Currently, for planned course treatment for gallbladder dysfunction (hyperkinetic form) and Oddi's sphincter the use of selective myotropic antispasmodic (mebeverine hydrochloride) has been indicated.
Mebeverine. Duspatalin. NiaspamSpareks
Pharmacodynamics. Meberverin blocks fast sodium channels and slow channels of Ca2 + ions of the cell wall of the myocyte, inhibits the depolarization of the cell membrane and prevents the contraction of muscle fibers. Relaxes smooth muscles, mainly of the gastrointestinal tract, eliminates spasm, while not having a significant effect on the normal intestinal motility. Does not have an anticholinergic action
Pharmacokinetics. When ingested, mebeverin is not detected in plasma, as it undergoes first-pass hydrolysis in the liver with the formation of mebeverine alcohol and 3,4-dimethoxybenzoic acid (veratric acid). The drug is excreted mainly in the urine as metabolites - the metabolites of mebeverine alcohol and 3,4-dimethoxybenzoic acid are detected in bile in small quantities. Mebeverin is eliminated completely within one day after taking a single dose. It does not get accumulated in the body.
Indications. Adults: spasms of the gastrointestinal tract organs (including those caused by organic disease), biliary colic, intestinal colic; irritable bowel syndrome. Children over 12 years: functional disorders of the gastrointestinal tract, which are accompanied by abdominal pain.
Mode of application. It is taken orally, 20 minutes before a meal, without chewing and drinking water, patients older than 12 years old are prescribed 200 mg 2 times a day for 15–20 minutes before meals.
Due to the possible dizziness during the treatment with mebeverin, it is necessary to be especially careful in controlling the mechanisms and machines and driving vehicles.
Dosage form. Retard Capsules 200 mg.
Side effects. Constipation or diarrhea, dizziness (in some cases), allergic reactions (angioedema, urticaria, exanthema and facial swelling).
Trimebutin (Trimebutinum). Trimedat.
Pharmacodynamics. It regulates the motility of the gastrointestinal tract, having an effect on the intestinal enkephalinergic system. In hyperkinetic conditions of the smooth muscles of the intestine has an antispasmodic effect; in the hypokinetic states of the smooth muscles of the intestine - a stimulating effect. Trimebutin has an effect throughout the gastrointestinal tract, enhances intestinal motility and gastric emptying, reduces the pressure of the esophageal sphincter. It acts on peripheral delta, mu and kappa receptors, including those receptors that are located directly on the smooth muscle of the gastrointestinal tract. It promotes the response of the smooth muscles of the colon to food stimuli. It does not affect the central nervous system. It estores the normal physiological activity of the muscles of the intestines in various diseases of the gastrointestinal tract, which are associated with impaired motility. Trimebutin is used for abdominal pain syndrome as it provides an analgesic effect, normalizing visceral sensitivity.
Pharmacokinetics. Trimebutin is rapidly absorbed in the gastrointestinal tract. Bioavailability is 4 - 6%. The maximum concentration is reached within 1 to 2 hours after ingestion. The volume of distribution is 88 liters. It binds to plasma proteins by about 5%. It is biotransformed in the liver, excreted by the kidneys, mainly in the form of metabolites, 70% is excreted during the day. The half-life is about 12 hours. To a small extent penetrates the placental barrier.
Indications. Postoperative paralytic intestinal obstruction; irritable bowel syndrome; symptomatic treatment of pain associated with functional disorders of the biliary tract and the gastrointestinal tract; preparation for endoscopic and radiological studies of the gastrointestinal tract.
Mode of application. Trimebutin is taken orally, injected intravenously, intramuscularly, rectally. Orally - 100 - 200 mg 3 times a day; intravenously, intramuscularly - a single dose is 50 mg; rectal - daily dose is 100 - 200 mg. The frequency and duration of use depends on the clinical case. For intestinal dyskinesia, a drug is prescribed 0.2 g 3 times daily before meals, the duration of treatment is up to 3 months. For biliary dyskinesia, 0.1–0.2 g is prescribed 3 times daily before meals, the duration of treatment is 2–4 weeks.
Contraindications. Hypersensitivity, lactation, pregnancy, child age (depending on the dosage form).
