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Drugs for the functional GIT disorders


Functional gastrointestinal disorders represent a group of symptoms and ill states in which there is the increased or reduced intestinal motility. This means that the smooth intestinal musculature has a too strong, too weak or complete uncontrolled reaction to stimuli, causing disorders in the flow of the intestinal contents through the digestive tract-either there is constipation or constant diarrhea. Abdominal pain and cramps are specific for these disorders. Cramps can be hardly tolerable. They are mostly only symptoms of some other ill states. Those are the syndrome of the irritable colon, spastic colitis, diverticulosis and ileus.

The treatment of GIT disorders includes:
  • parasympatolitics (spasmolitics) - atropine, mebeverin, N-butyl scopolamine – they reduce the spasticity of the smooth muscle of GIT and cramps
  • Propulsives (metaclopramid and cysaprid) - they increase the mobility of GIT.
Mebeverin is a synthetic equivalent of papeverin from Papaver somniferum. It does not have any effect on the CNS. As spasmolitics, synthetic derivates of papaverin are used today, and that is mebeverin. In contrast to papaverin, mebeverin is a spasmolitic with selective effect on the smooth musculature of GIT, especially the colon. It has a direct effect on the smooth muscles. It belongs to the group of neurothropic-musculothropic spasmolitics. It is used in the treatment of: syndrome of the irritable colon, symptoms followed by organic stomach and intestinal diseases such as colon diverticulosis, etc.

Side effects are rare. Rash and urticaria are the most usual. In some cases, it can come to dizziness, headache, pain in the chest, palpitation, tachycardia, sleep disorder, pain in the abdomen, sickness and vomiting.

Butilscoppolamin - it is a semi-synthetic derivate of scopolamine, natural alkaloid veleherbs and similar herbs from the family Solanaceae. It belongs to the group of antiholoenergics or antimuscarine drugs. It relaxes the smooth muscles of the digestive tract, gall and urinary ducts and female sexual organs, and it calms cramps and pain. It is used in the treatment of spasm and pain due to stomach and intestinal hypermotility, gall and urinary tract, spastic constipation and dysmenorrheal. It can come to the so called antiholienergic effects, i.e. the reduction of secretion of sweat and spit and acceleration of heart rhythm.

It rarely causes passing antiholienergetic reactions.

Cysaprid is a gastrointestinal procinetic drug-propulsive. It increases the release of acetylholin in the digestive tract. That is how it accelerates and normalizes peristaltics of digestive organs and prevents the delay and reflux of the content of the digestive organs. It inhibits dopamine receptors. It is mostly metabolized by means of the liver enzymes. It is used in the treatment of heavy inflammation of the esophagus, heavy forms of gastroparesis.
It can come to passing abdominal cramps, flatulence or diarrhea. Rarely, there are dizziness and headaches. It can come to reactions of hypersensitivity, abnormality of the liver function, gynecomastia and galactorrhea, frequent urination, retention of urine and cystitis. Convulsions and extrapyramidal signs are possible.

Metoclopramide is at the same time an antiemetic and propulsive. It expresses a parasympatomitetic activity, and it is also a dopamine antagonist in the CND with the direct effect on hemoreceptor zone. It possesses antagonistic effect on serotonine receptors. The result of the combination of these effects is reflected in the increase of the threshold for vomiting and speeding up of defecation. It stimulates the motility of the upper gastrointestinal system , accelerating the gastric and duodenal peristaltics. It leads to lifting of the tonus of the gastroesophageal sphincter at rest. It is applied in the states of distrurbed motility of the gastrointestinal tract, gastroesophageal reflux and dyspepsia, for the prevention of sickness and vomiting. It has the effect on the CNS, causing unrest, sleepiness, tiredness.

The major side effects are neurological and mental, and those are sleepiness, tiredness, irritability, sedation and depression. Extrapyramidal are more usual in women and children. These reactions are manifested in the form of trismus, torticolis, facial spasm, dysphagia, urinary retention and reactions similar to tetanus. Insomnia, upset, headache, depression, delirium, mania and dysphoria can occur rarely , as well as neuroleptic malignant syndrome. Due to the increased secretion of prolactin, in some patients, gynecomastia, galactorrhea and breast enlargement are possible. There are also abdominal problems, arrhythmias, hypotension and hypertensive crises, urticaria, maculopapular rash and anaphylaxia.
Atropine is one of the oldest drugs. It is received from herbs Atropa belladonna, Hyosciamus niger, Scopolia carniolica and Datura stramonium. It has the effect on the autonomous nervous system, i.e. parasympaticus causing its blockage. Because of that, parasympaticus remains blocked and because of that atropine is called spasmolitic. Parasympaticus innervates the digestive tract and its blockage is started being dominated by the influence of sympaticus which causes the relaxation of the smooth muscles and contraction of the sphincter. The drug of such an effect will alleviate cramps and stop too large motility of the intestines. It won’t work only on the digestive systmen but on the whole body. It is used in the form of injections in the spasm of pylorus, hypertonus of the small intestine, hypermotility of the colon, biliary spasm, ureteral colics and larynx spasm, as well as the prevention and reduction of secretion activity of the respiratory tract.
Intravenous application of atropine with the purpose of anesthetic premediaction includes the expected risk of side effects. Heart arrhythmias are expected in almost 1/3 of patients. Due to the reduced salivation, it comes to dry mouth and throat. In higher dosage, it comes to hoarseness, thirst, skin redness and tachycardia. In some cases, it can come to the side effects on the gastrointestinal system: changes of taste, sickness, vomiting, dysphagia, constipation, the feeling of flatulence, paralytic ileus; on the genitourinary system, on the eyes (midriasis, photophobia, cycloplegia, increased eye pressure; on the cardiovascular system (palpitations, bradycardia); on the CNS (headache, redness of the face, unrest, dizziness, confusion, insomnia, high body temperature. In rare cases, it can come to anaphylaxia, urticaria, suppression of lactation and nose congestion.

Registered drugs:

  • mebeverin – Rudakol (Belupo Croatia),
  • dimetikon – Gasvan (Srbolek Serbia),
  • simeticone – Espumisan L (Berlin-Chemie AG Germany),
  • atropine – Atropin sulfat (Verofarm Russia),
  • butylscopolamine – Buscopan (Zdravlje Serbia)
  • pitofenon, metamizole-sodium, fenpiverinium–bromide – Baralgetas (Jugoremedia Serbia),
  • metoclopramide – Klometol (Galenics Serbia), Reglan (Alkaloid Macedonia),
  • cisaprid – Cisap (Health Serbia), Bymaral (Alkaloid Macedonia)

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