Prokinetics - what is it? Prokinetics of the new generation: list
Prokinetics - what is it? In the space of the CIS countries there is no common opinion about what medicines are included in this group, therefore each gastroenterologist determines what to include in this list and what is not. Prokinetics - what is it? This we will try to find out.
Definition and brief description of
Prokinetics - what is it? This is a group of drugs that stimulate the motility of the digestive tube and prevent the appearance of anti-peristaltic waves.
Diseases of the gastrointestinal tract are often accompanied by the casting of chyme from the lower parts of the intestinal tube into the overlying ones, by breaking the passage of the food lump or by its stagnation in the segment of the intestine. All these manifestations are associated with a violation of the progression of chyme along the digestive tube, which means that symptoms can be removed by affecting the contractions of smooth muscles in its walls. Prokinetics are needed for this. Their therapeutic effect is associated with the blocking of the mechanism of ion transport( dopamine, 5-HT4 receptors, combined) or an effect on the metabolism of acetylcholine. Achievement of the clinical effect occurs due to the increase in the amount of acetylcholine in the synaptic cleft or the increase in the production of cholinesterase, which increases the decomposition of the ACS, the decrease in the output of the ACH by nerve endings.
Physiologically, the effects of taking medications are manifested in an increase in the tone of the cardiac esophageal sphincter, evacuation of the stomach contents, coordination between the antrum and duodenum, productive intestinal peristalsis.
The first group of drugs
Prokinetics are drugs that block D2-dopamine receptors, thereby stimulating the activity of muscle fibers of the gastrointestinal tract and providing an antiemetic effect. These medicines include: "Metoclopramide"( the first generation, representatives - "Tserukal" and "Reglan"), "Bromopride", "Domperidon"( second generation), "Dimetpramid", Itopride.
Medications prokinetics are used in the therapy of gastroesophageal reflux disease( GERD), YaZHPP, functional dyspepsia, narrowing of the esophagus after trauma and as a result of the development of adhesions, paresis of postoperative intervention in the abdominal cavity, violation of bile outflow, increased gas production.
Prokinetics are also drugs that can be used for nausea and vomiting caused by poisoning or eating disorders, diseases of viral or bacterial etiology, pregnancy in the first trimester, acute coronary insufficiency, head trauma, anesthesia, radiation and chemotherapy. Ineffective in vomiting of vestibular origin, as they do not affect the middle ear and medulla oblongata.
Neuroleptics that help with vomiting
"Sulpiride" and "Levosulpiride", which are neuroleptics with a similar mechanism of action, they also have a positive antiemetic effect, so they can be used in gastroenterological practice.
"Metoclopramide"( prokinetics): instructions for use
"Metoclopramide" is a direct stimulant of smooth muscles and has all the necessary properties for achieving clinically significant results, but due to permeability through hematohistological barriers it should be used with caution. Possible side effects, such as spasm of the facial muscles, a symptom of the "goose paw", rhythmic protrusion of the tongue, bulbar disorders, spasm of the ectraocular muscles, spasmodic torticollis, excessive tone of the extensor muscles, Parkinson's syndrome, drowsiness, weakness, ringing in the ears, headaches,anxiety, absent-mindedness.
When is it undesirable to take prokinetics? The application instruction says that it is undesirable to use in cases of hypersensitivity to the drug components, adrenal cortex tumor, intestinal obstruction, intestinal perforation and bleeding caused by it, prolactin-dependent tumor, epilepsy and extrapyramidal disorders, before the 16th week of childbearing, during lactation, to children5 years. With caution should be appointed with reduced clearance of creatinine, increased arterial pressure, bronchial asthma, age of 14 years.
The medicine is swallowed half an hour before a meal, on a tablet at 9:00, 12:00, 15:00 and 18:00.Duration of treatment - from four to six weeks, sometimes can be extended to six months.
If the form of release is liquid, then injected intramuscularly or intravenously. For adults and children over 14 years - 10 mg. Maximum at one time - 20 mg, daily dose - 60 mg. The contents of the ampoule can be diluted in isotonic solution or in 5% glucose solution.
"Domperidon": instruction on the use of
"Domperidone" is a more selective blocker of dopamine receptors, besides it does not penetrate the BBB, therefore, the side effects described above do not develop when it is taken. But, increasing the secretion of prolactin, it provokes gynecomastia, galactorrhea and the absence of menstruation. In addition, patients noted skin rash, dry mouth, diarrhea and headaches.
It is not recommended for use in people with allergic reactions to the components of the drug, bleeding from the digestive tract, intestinal obstruction, prolactinoma, during breastfeeding, up to 5 years of age or weighing up to 20 kilograms. Take with caution during pregnancy, kidney and / or liver failure.
Drink twenty minutes before each meal of 10 mg, if necessary, you can drink and before going to bed. The maximum daily dose is 80 mg. If there are antacids in the treatment that reduce the secretion of gastric juice, then they should be drunk separately from domperidone, sharing eating.
"Itopride": instruction for the use of
"Itopride" combines the properties of a dopamine receptor antagonist and acetylcholinesterase blocker. It affects the hypothalamic-pituitary-adrenal system, increasing somatostatin concentrations and decreasing adrenocorticotropic hormone. Negative action is expressed in leukopenia, thrombocytopenia, hypersensitivity reaction, hyperprolactinemia, nausea, tremor, jaundice. During the reception, it is necessary to monitor the condition of peripheral blood and make sure there are no side effects.
It is not recommended to take people with immediate or delayed hypersensitivity, gastrointestinal hemorrhage in the history, obturation of the intestinal lumen with a foreign body or compression from the outside, up to sixteen years of age, during pregnancy, breast-feeding.
The drug should be taken orally 50 mg three times a day.
Antagonists of "Acetylcholine"
This group includes:
- "Acekledin"( M-cholinomimetic);
- Physiostigmine, Galantamine, Tegaserod, Prukalopride( reversible cholinesterase inhibitors)
These drugs are only partially attributed to the prokinetic group because of their side effects: the effect on the exchange of potassium ions, and as a consequence, the prolongation of the QT interval, whichleads to violations of the heart rhythm. A number of medicines were withdrawn from the pharmacological market precisely for this reason.
"Acekledin": instruction on the use of
Prokinetics - what is it, how and in what cases do they apply? In any case, a doctor's consultation is mandatory and an attentive introduction to the instructions for use.
"Aceclydine" is used to eliminate loss of tone of the gastrointestinal tract and bladder after operations, reduces intraocular pressure, so it can be used in ophthalmologists. The form of release - a solution for injections, is injected subcutaneously on 1-2 ml of 0.2% solution. The maximum amount per reception is 0.004 g, with a day not more than 0.012 g. Side effects are pentavism, sweating, diarrhea.
Contraindications to use are ischemic heart disease, increased HDL, bronchial asthma, hyperkinesis and other parkinsonisms, pregnancy, bleeding from the abdominal organs.
"Physiostigmine" is used mainly in ophthalmic practice, but can sometimes be used in gastroenterology for intestinal paresis. The drug is injected under the skin for 0.5-1 ml of 0.1% solution. The maximum amount of the drug per day should not exceed 0,001.
Side effects are increased salivation, bronchospasm, spasm of the muscles of the intestine, changes in the heart rate, convulsions.
Contraindications: angina pectoris, epilepsy, bronchial asthma, mechanical intestinal obstruction, peritonitis, sepsis, pregnancy.
"Galantamine": instructions for use
"Galantamine" in special cases is used as an antagonist for muscle relaxants in the postoperative period with a decrease in the tone of the muscles of the intestine and bladder. Contraindications to use are hypersensitivity, epilepsy, bronchial asthma, blood pressure above 139/99 mm Hg, COPD, mechanical obstruction of the intestinal tube, decreased kidney function, age to 9 years. Limited to the purpose of pregnancy in those cases where the potential harm exceeds the benefit. During lactation can be transmitted to the child through milk.
Side effects: decreased heart rate, TTP, AV blockade, extrasystole, nausea, vomiting, diarrhea, indigestion, muscle spasms, urinary incontinence, hematuria, tremor.
Can be administered subcutaneously, intramuscularly, intravenously, percutaneously, orally. The dose is selected individually, based on an anamnesis of the disease, and must be corrected by the attending physician. On average, the daily intake for adults is 10 to 40 mg divided into two or four doses.
Prokinetics of the new generation
On the basis of itopride today, such drugs as "Ganaton", "Itomed", "Pramer" are produced. One of the newest and most effective are prokinetics of a new generation, like "Coordination" and "Prepulcide."Although they can cause serious side effects in the work of the heart.
The most popular among gastroenterologists remains "Motilium"( the active substance is domperidone), which combines the qualities of metoclopramide, but does not have its negative consequences.
What are the most effective aprokinetics? The list of drugs for today includes:
- "Itopride"( active ingredient) - "Ganaton", "Itomed", "Primer"( commercial names).
- "Metoclopramide" - "Reglan", "Cerucal".
- "Cisapride" - "Coordinate", "Prepulsed."
- Domperidon - Motilium, Motilak, Motinorm, Passazs.
Now we know what prokinetics are. The list of them, as you can see, is very large. But remember, before applying any medication you need to consult a doctor! Be healthy!