Loperamide and its complete analogues: efficacy and risks in the treatment of diarrhea

Opiate loperamide is part of several drugs for diarrhea, the most famous among which was the eponymous "Loperamide." The substance belongs to the antidiarrheal drugs, developed in the early 70s of the last century. Then the practice of application revealed dangerous side effects to health. Now the instructions for use of "Loperamide" and its hollow analogues takes them into account, among other contraindications.

The content of the article

The danger of opiates for the central nervous system of man has long been known to science, it has become one of the reasons for their prohibition throughout the world (the second is the addictive effect, forcing drug addicts to increase the dose or even to death). But their ability to block the work of nerve endings remains valuable for medicine. This property is widely used to relieve pain in cancer, surgery, trauma.

Operating principle

Loperamide was developed as a drug that retains the inhibitory effect on intestinal peristalsis typical for all opiates, but lacking narcotic and analgesic effects. It increases the muscle tone of the anal sphincter and reduces the rate of fluid release from the bloodstream into the intestinal cavity (a natural mechanism for diarrhea to occur), stopping diarrhea.

The lion's share of the ingested "Loperamide" destroys and removes the liver along with the bile, and the rest is filtered kidneys. Loperamide does not penetrate the blood-brain barrier (its own defense mechanism). Therefore, it does not inhibit or hallucinogenic effects on the cerebral cortex.

Indications

In addition to "Loperamide", the substance loperamide forms the basis of:

  • "Imodium"
  • "Lopedium";
  • Superilom;
  • Suprilola;
  • "Diar";
  • "Enterobene".

Thus, the tool is released in the form of tablets for ingestion (in the shell) or resorption (lyophilized), syrup and aqueous solution for oral administration.

The indications for Loperamide relate to diarrhea of ​​any origin, including:

  • food poisoning;
  • rotavirus infection;
  • intestinal dysbiosis;
  • enteroviruses and intestinal infections (bacterial, fungal).
The drug is suitable for the treatment of acute diarrhea, and the use of loperamide tablets for chronic disorders of the stool should not exceed two days. The requirement is connected with the probability of not only a marked inhibition of intestinal motility in representatives of all age groups, but also of immobilization of the muscles of the lower back, pelvic in children.

Limitations to the appointment

As for the question of whether Loperamide is given to children, for a long time, children's preparations based on the same substance were popular and were included in the lists of essential in some countries of Western Europe and the former USSR. But in the 90s of the last century, WHO (World Health Organization) discovered and confirmed the side effects of loperamide on the children's organism. They consisted in the appearance of paralytic scoliosis. This complication occurs after polio and is characterized by the failure of part of the muscles supporting the spine. There is a deep curvature of the back, most often - in the lumbar region.

Paralytic scoliosis, as a complication of poliomyelitis, is compatible with life, although it may require complex surgery on a curved segment if the posture cannot be restored by other means. But as a complication of taking loperamide, he provoked several deaths. This led to a ban on the use of drugs, which include the substance in children under five years of age. (In many countries - under eight years of age or even until the transition to adolescence).

In Russia, the drug “lasted” on the list of vital drugs (their production or procurement is controlled by the state) for only five years. At the moment in the Russian Federation it is excluded from this list. Restrictions to its reception relate to:

  • — но судя по отзывам врачей, запрет на его назначение детям младше 12 лет тоже не лишен оснований; children under five years old - but judging by the opinions of doctors, the ban on his appointment to children under 12 is also not without reason;
  • — чья работа связана с повышенным вниманием, физическими нагрузками и быстрой реакцией (водители, спасатели, промышленные альпинисты, полицейские); parts of the adult population - whose work is associated with increased attention, physical exertion and quick response (drivers, rescuers, industrial climbers, police officers);
  • — поскольку печень «переваривает» основную часть принятого лоперамида. patients with liver failure - because the liver "digests" the main part of the loperamide taken.

Contraindications

"Loperamide" is not a means of preventing intestinal disorders, and its overdose can result in arrhythmia and cardiac arrest. Contraindications to its use affect a wide range of conditions and drugs taken with it. Among them are the following cases.

  • . Pregnancy The question of whether Loperamide is possible during pregnancy is theoretically open, since the effect of the drug on the fetus is poorly understood, the percentage of its penetration through the villi of the chorion (the protective barrier of the placenta) is unknown. The inability of Loperamide to overcome the hematoencephalic barrier similar to chorionic villi speaks in favor of its reception. And against - high potential danger of the drug to the muscles and central nervous system of the fetus (taking into account its proven harm to children already born). Additional risk factors are the failure of the fetal body's own defense mechanisms (blood-brain barrier) and the permeability of the placental barrier to change under the influence of a number of factors. Despite the lack of research on this topic, "Loperamide" and its full analogues are prohibited to use during pregnancy and during breastfeeding.
  • . Nausea and vomiting . "Loperamide" is not a means to stop them, and can provoke them themselves. This happens if the need to evacuate the contents of the digestive tract is preserved, and one of its ways is blocked by the action of the drug. Plus, taking any means other than anti-emetic is useless in this case (they will be evacuated from the stomach with vomiting before they have time to act).
  • . Pancreatitis . Acute pancreatitis is deadly, and chronic is accompanied by nausea, intestinal indigestion, bloating and diarrhea. Stool disorder in pancreatitis is associated with a deficiency of pancreatic juice - the main intestinal digestive environment, which leads to the formation of poor-quality (semi-digested) feces. Their timely elimination, from a biological point of view, is better than trying to “keep” them in the rectum. In addition, with pancreatitis of any origin, there are difficulties with the outflow of pancreatic juice from the pancreas into the intestinal cavity. The action of "Loperamide" is not limited to blocking duodenal motility, spreading to other organs of the digestive system, which aggravates the problem of the outflow of the digestive fluid.
  • . Gastritis . As well as a stomach or intestinal ulcer. Reception "Loperamide" with them is undesirable, although not excluded. In gastritis and ulcers, the drug will further irritate the stomach walls, with the result that stomach pains and the appearance of emetic urges are possible. Both pathologies require an emphasis on taking soluble forms of drugs with loperamide - drops, syrup, or "effervescent" tablets. But its aqueous solutions have more pronounced side effects, especially in relation to paralysis of the back muscles.
  • . Reception of alcohol . Alcoholic beverages are incompatible with "Loperamide" because they have an oppositely directed action on the central nervous system and intestinal motility. Ethyl alcohol is synthesized in the intestine itself in order to accelerate its contractions, blood flow in its walls and absorption of digested food components into the blood. The same effect has the accepted dose of alcohol. And "Loperamide", by contrast, inhibits the activity of the intestinal walls and their muscles.
The tool is contraindicated for use in obstruction and intestinal atony, individual intolerance to the components of the drug, colitis (inflammation of the rectum) of any etiology. When prescribing antibiotics, the use of "Loperamide" is excluded, even if their course provoked diarrhea. Otherwise, the likelihood or severity of side effects increases.

Side effect

Reviews of capsules "Loperamid" are mostly positive. Provided that the reception was strictly according to the indications, short (no more than two days) courses and in therapeutic doses. Side effects in this case are mild and disappear shortly after discontinuation of the drug. Among the negative reactions are:

  • — и зуд как признаки аллергии; urticaria - and itching as signs of allergies;
  • — при сочетании препарата с полусинтетическими антибиотиками последнего поколения; anaphylactic shock - when the drug is combined with the latest generation of semi-synthetic antibiotics;
  • — а также метеоризм, тошнота, рвота; abdominal pain - as well as flatulence, nausea, vomiting;
  • — с рассеянным вниманием, головокружениями, повышенной утомляемостью, которые наступают благодаря тормозящему действию лоперамида и других опиатов на головной мозг; drowsiness - with diffuse attention, dizziness, fatigue, which occur due to the inhibitory effect of loperamide and other opiates on the brain;
  • — снижение частоты сокращений сердца, вплоть до его остановки. arrhythmia - reducing the frequency of contractions of the heart, until it stops.

Usually, arrhythmia is observed when coadministered "Loperamide" with macrolides (a type of antibiotics with a special structure and conditionally lower toxicity on the patient's body), antiviral and antifungal agents.

The most terrible complications of the digestive tract when taking Loperamide are: acute constipation, intestinal paralysis with the subsequent development of paralytic ileus (obstruction). Their likelihood increases when taking Loperamide is carried out simultaneously with a course of other opiates, for example, painkillers. And his overdose, in addition to cardiac arrest, may result in respiratory arrest.

Instructions for use of drugs with loperamide

The dosage of "Loperamide" at the first dose is prescribed twice as high as all subsequent ones. It should be taken inside, before meals or after meals, “washing it down” with them every episode of emptying with liquid masses.

  • . Adults . A single dose of loperamide for them in the first dose is 4 mg, all subsequent - 2 mg. The total daily dosage should not exceed 16 mg. When taking the drug in drops, the “starting” dosage is 60 drops, and all subsequent doses, 30 drops each.
  • . Children over five years old . They are prescribed a starting dose in a volume of 2 mg (or 30 drops), and all subsequent doses - 1 mg (15 drops) after each stool in liquid masses, but not more than 8 mg per day (that is, twice less than in adults).
  • . Children under five . Only a pediatrician has the right to prescribe drugs on the basis of loperamide at this age, and treatment should be under his supervision. With his approval, it is allowed to give the child syrup with loperamide no more than three times a day, based on the calculation of 1 ml of syrup for every 10 kg of body weight of the baby.

The course "Loperamide" must be stopped as soon as the chair normalizes. Or with the appearance of side effects. If, after stopping diarrhea, new urges to defecate are not observed during the day (in children and adolescents - half a day or longer), you should consult a doctor. It is not recommended to return to the reception of "Loperamide" and drugs based on it in the future.

Green arrow drawn on female belly

Safe Replacement Options

Analogues of drugs with loperamide are endless rows of drugs against diarrhea with different composition and action.

  • . Probiotics . Packed cultures of lacto-and / or bifidobacteria. They help from stool disorders and gas provoked by intestinal dysbiosis. Probiotics are recommended for use with a deficiency of lactase (an enzyme that breaks down breast and other milk), after a course of antibiotics and chemotherapy. When choosing them, it is better to focus on drugs in capsules that dissolve only in the intestine. The use of probiotic solutions is unreasonable, since the lion's share of bacteria in their composition will not survive in the hydrochloric acid of the stomach.
  • . Prebiotics . Nutrient medium for the beneficial part of the intestinal microflora (most often high carbohydrate). Patients who adhere to a normal, but not dietary diet, do not need their separate reception. And in the presence of restrictions on carbohydrates, for example, in diabetes mellitus, their use makes sense only in combination with probiotics.
  • . Antibiotics . Semi-synthetic and fully synthetic. The use of drugs in this group is important for intestinal infections, poisoning and enterobiasis.
  • . Enterosorbents . Foreigners for the digestive tract or irritants. The most famous representatives of this series are: black (wood burning product) and white (diosmectite, silicon) activated carbon. As well as the "liquid" version of white coal (manufactured under the trade name "Smekta") and povidone. Absorbents can cope with diarrhea caused by light food poisoning (stale food, but not poisonous mushrooms or rotten meat), common fungal and bacterial invasions. They do not act on the majority of viruses and intestinal parasites, they only alleviate the symptoms due to the absorption of their metabolic products.

A good antidiarrheal effect is provided by water decoctions of blueberry and bird cherry fruits (moderately poisonous plant), as well as pomegranate peel. In terms of side effects, they are safer (if not allergic) and are effective against prolonged diarrhea, which can last for a week with rotavirus infection. At the same time, the indications for the use of "Loperamide" contain a two-day restriction on the timing of its reception, which is important to observe because of the likelihood of severe bowel atony. This makes it difficult for many intestinal disorders to be treated with loperamide.

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