Prokinetics - what is it? In the space of the CIS countries there is no consensus about which drugs are included in this group, therefore, each gastroenterologist himself determines what to add to this list and what not. Prokinetics - what is it? This is what we will try to find out.
Definition and brief description
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.
Gastrointestinal diseases are often accompanied by the throwing of the chyme from the lower sections of the intestinal tube into the overlying ones, a violation of the passage of the food lump or its stagnation in the intestine. All these manifestations are associated with a violation of the movement of the chyme along the digestive tube, so you can remove the symptoms by affecting the smooth muscle contractions in its walls. For this, prokinetics are needed. Their therapeutic effect is associated with blocking the mechanism of ion transfer (dopamine, 5-HT4 receptors combined) or affecting the metabolism of acetylcholine. Achieving the clinical effect is due to an increase in the amount of acetylcholine in the synaptic cleft or to an increase in cholinesterase production, which enhances the decomposition of ACC, a decrease in the production of ACC by nerve endings.
Physiologically, the effects of taking the drugs are manifested in an increase in the tone of the cardiac esophageal sphincter, evacuation of the contents of the stomach, coordination between the antrum and the duodenum, and productive intestinal motility.
First group of drugs
Prokinetics are drugs that block D2-dopamine receptors, thus stimulating the activity of muscle fibers of the gastrointestinal tract and providing an antiemetic effect. These drugs include: "Metoclopramide" (first generation, representatives - "Tserukal" and "Raglan"), "Bromoprid", "Domperidone" (second generation), "Dimetramid", "Itoprid".
Prokinetics are used in the treatment of gastroesophageal reflux disease (GERD), YaRPD, functional dyspepsia, narrowing of the esophagus after injuries and as a result of adhesions, paresis of postoperative intervention in the abdominal cavity, impaired bile outflow, increased gas formation.
Also, prokinetics are drugs that can be used for nausea and vomiting caused by poisoning or violation of the rules of eating, diseases of viral or bacterial etiology, pregnancy in the first trimester, acute coronary insufficiency, head injuries, anesthetics, radiation and chemotherapy. Ineffective for vomiting of vestibular origin, as they do not affect the middle ear and medulla oblongata.
Antipsychotics for vomiting
"Sulpiride" and "Levosulpiride", which are antipsychotics with a similar mechanism of action, they also have a positive antiemetic effect, therefore, can be used in gastroenterological practice.
"Metoclopramide" (prokinetics): instructions for use
"Metoclopramide" is a direct stimulator of smooth muscles and has all the necessary properties to achieve clinically significant results, but because of its permeability through hematohistological barriers, it should be used with caution. Side effects are possible, such as spasm of the facial muscles, goose paws symptom, rhythmic protrusion of the tongue, bulbar disorders, spasm of the extraocular muscles, spasmodic torticollis, excessive tone of extensor muscles, Parkinson's syndrome, drowsiness, weakness, tinnitus, headaches, anxiety, distraction.
In what cases is it undesirable to take prokinetics? The instructions for use say that it is undesirable to use in cases of hypersensitivity to the components of the drug, tumors of the adrenal cortex, intestinal obstruction, perforation of the intestine and the bleeding caused by it, prolactin-dependent tumors, epilepsy and extrapyramidal disorders, up to 16 weeks of gestation, while breastfeeding, children up to 5 years. With caution should be prescribed with reduced creatinine clearance, high blood pressure, bronchial asthma, under the age of 14 years.
The medicine is swallowed half an hour before meals, on a tablet at 9:00, 12:00, 15:00 and 18:00. The duration of treatment is from four to six weeks, sometimes it can be extended to six months.
If the release form is liquid, then it is administered intramuscularly or intravenously. For adults and children over 14 years old - 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.
"Domperidone": instructions for use
Domperidone is a more selective dopamine receptor blocker; moreover, it does not penetrate the BBB; therefore, when it is taken, the side effects described above do not develop. 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 by people with allergic reactions to the components of the drug, bleeding from the digestive tract, intestinal obstruction, prolactinoma, during lactation, up to 5 years old or weighing up to 20 kilograms. Use with caution during pregnancy, renal and / or liver failure.
Drink twenty mg before each meal of 10 mg, if necessary, you can drink before you go to bed. The maximum dose per day is 80 mg. If antacids that reduce the secretion of gastric juice are present in the treatment, then they should be drunk separately from domperidone, sharing food intake.
"Itoprid": instructions for use
Itoprid combines the properties of a dopamine receptor antagonist and an acetylcholinesterase blocker. It affects the hypothalamic-pituitary-adrenal system, increasing the concentration of somatostatin and reducing the adrenocorticotropic hormone. The negative effect is expressed in leukopenia, thrombocytopenia, hypersensitivity reactions, hyperprolactinemia, nausea, tremors, jaundice. During administration, it is necessary to monitor the condition of peripheral blood and make sure that there are no side effects.
It is not recommended to take people with an immediate or delayed hypersensitivity, a history of gastrointestinal bleeding, obstruction of the intestinal lumen by a foreign body or compression from the outside, under the age of sixteen years, during pregnancy, breastfeeding.
The drug is taken orally before meals, 50 mg three times a day.
Acetylcholine Antagonists
This group includes:
- "Aceclidine" (M-cholinomimetic);
- Physiostigmine, Galantamine, Tegaserod, Prucaloprid (reversible cholinesterase inhibitors)
These drugs are only partially attributed to the troupe of prokinetics due to their side effects: effects on the exchange of potassium ions, and as a result, lengthening of the QT interval, which leads to heart rhythm disturbances. A number of drugs were withdrawn from the pharmacological market precisely for this reason.
"Aceclidine": instructions for use
Prokinetics - what is it, how and in what cases to use them? In any case, it is mandatory to consult a doctor and carefully read the instructions for use.
"Aceclidine" is used to eliminate loss of tone of the digestive tract and bladder after surgery, reduces intraocular pressure, and therefore can be used in ophthalmologists. The release form is an injection, it is administered subcutaneously in 1-2 ml of a 0.2% solution. The maximum amount at one time is 0.004 g, with no more than 0.012 g per day. Side effects - ptyalism, sweating, diarrhea.
Contraindications for use are coronary heart disease, high HDL, bronchial asthma, hyperkinesis and other parkinsonism, pregnancy, bleeding from the abdominal organs.
Physiostigmine is used mainly in ophthalmic practice, but sometimes it can also be used in gastroenterology for intestinal paresis. The medicine is injected under the skin with 0.5 - 1 ml of a 0.1% solution. The maximum amount of the drug per day should not exceed 0.001 g.
Side effects are increased salivation, bronchospasm, intestinal muscle spasm, changes in heart rate, and cramps.
Contraindications: angina pectoris, epilepsy, bronchial asthma, mechanical obstruction of the intestines, 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 muscle tone of the intestines and bladder. Contraindications to use are hypersensitivity, epilepsy, bronchial asthma, blood pressure above 139/99 mm Hg, COPD, mechanical blockage of the intestinal tube, decreased kidney function, age up to 9 years. It is limited to the appointment during pregnancy in cases where the potential harm exceeds the benefit. During lactation, it can be transmitted to the baby through milk.
Side effects: decreased heart rate, TTP, AV blockade, extrasystole, nausea, vomiting, diarrhea, dyspepsia, muscle cramps, urinary incontinence, hematuria, tremor.
It can be administered subcutaneously, intramuscularly, intravenously, percutaneously, orally. The dose is selected individually, based on the medical history, and should be corrected by the attending physician. On average, the daily dose for adults is from 10 to 40 mg, divided into two to four doses.
Prokinetics of the new generation
On the basis of itopride today produce such drugs as "Ganaton", "Itomed", "Pramer". One of the newest and most effective are such new generation prokinetics as Coordinax and Prepulside. Although they can cause serious side effects in the work of the heart.
The most popular among gastroenterologists is Motilium (the active ingredient is domperidone), which combines the qualities of metoclopramide, but does not have its negative consequences.
What are the most effective prokinetics? The list of drugs today includes:
- "Itopride" (active substance) - "Ganaton", "Itomed", "Primer" (commercial names).
- "Metoclopramide" - "Raglan", "Tserukal".
- "Tsizaprid" - "Coordinax", "Prepulside".
- “Domperidon” - “Motilium”, “Motilak”, “Motinorm”, “Passenger”.
Now we know what prokinetics are. The list of them, as you see, is very long. But remember, before using any drug you need to consult a doctor! Be healthy!