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

Opiate loperamide is part of several drugs against diarrhea, the most famous among them was the eponymous "Loperamide". The substance refers to antidiarrhoeic drugs, developed in the early 70-ies of the last century. Then the practice of the application revealed dangerous side effects. Now the instruction on the application of "Loperamide" and its hollow analogs takes them into account among other contraindications.

The content of the article

The danger of opiates for the central nervous system of man has been known to science for a long time, it became one of the reasons for their prohibition around the world (the second is the addictive effect that forces drug addicts to increase their dose right up to a lethal outcome). But their ability to block the work of nerve endings remains valuable for medicine. This property is widely used for arresting pain syndrome in cancer, surgical interventions, trauma.

Operating principle

"Loperamide" was developed as a drug that retained a typical inhibitory effect on all intestinal peristalsis, but lacked narcotic and analgesic effects. It increases the tone of the musculature of the anal sphincter and reduces the rate of fluid release from the bloodstream into the intestinal cavity (necessary for the appearance of diarrhea natural mechanism), stopping diarrhea.

The lion's share of the "Loperamide" that has entered the body destroys and removes the liver together with the bile, and the remainder filters out the kidneys. "Loperamide" does not penetrate the blood-brain barrier (its own defense mechanism). Consequently, it does not have a braking or hallucinogenic effect on the cortex of the brain.

Indications

In addition to Loperamide, the substance loperamide is the basis:

  • "Imodium"
  • "Lopeziuma";
  • "Superiloma";
  • "Suprilola";
  • "Diaries";
  • "Enterobene".

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

Indications for Loperamide include 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 tablets "Loperamide" for chronic disorders of stools should not exceed two days. The requirement is associated with the probability of not only a marked inhibition of intestinal peristalsis in representatives of all age groups, but also immobilization of the muscles of the lower back and small pelvis in children.

Restrictions on the appointment

As for the question of whether Luperamide is given to children, then for a long time children's products based on the same substance were popular and were included in vital lists 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 children's body. They consisted in the appearance of paralytic scoliosis. This complication occurs after a polio disease and is characterized by the failure of a part of the spine supporting the muscles. 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 a complex operation on a twisted segment if the posture can not be restored in other ways. But as a complication from 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. (In many countries - less than eight years old or even until the transition to a teenage age category).

In Russia, the drug "lasted" in the list of vital drugs (their production or purchase is controlled by the state) for only five years. At the moment in the Russian Federation he is excluded from this list. Restrictions on its reception concern:

  • — 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 doctors' opinions, the ban on its appointment to children under the age of 12 is also not groundless;
  • — чья работа связана с повышенным вниманием, физическими нагрузками и быстрой реакцией (водители, спасатели, промышленные альпинисты, полицейские); part of the adult population - whose work is associated with increased attention, physical exertion and quick response (drivers, rescuers, industrial climbers, policemen);
  • — поскольку печень «переваривает» основную часть принятого лоперамида. patients with hepatic insufficiency - as the liver "digests" the bulk of the accepted loperamide.

Contraindications

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

  • . Pregnancy . The question is whether Loperamide is possible in pregnancy, theoretically remains open, since the effect of the drug on the fetus is poorly understood, the percentage of its penetration through the chorionic villi (the protective barrier of the placenta) is unknown. In favor of his reception says the inability of "Loperamide" to overcome the chorionic analogue of the chorionic blood-brain barrier. And against - the high potential danger of the drug for the musculature and central nervous system of the fetus (taking into account its proven harm for already-born children). Additional risk factors are the undeformed intrinsic protective mechanisms of the fetal body (blood-brain barrier) and the permeability of the placental barrier that can change under the influence of a number of factors. Despite the lack of research on this topic, "Loperamide" and its complete analogs are prohibited for use during pregnancy and breastfeeding.
  • . Nausea and vomiting . "Loperamide" is not a means to stop them, and can themselves provoke them. This happens if the need for evacuation of the contents of the digestive tract remains, and one of its ways is blocked by the action of the drug. Plus, taking any means other than antiemetic, in this case is useless (they will be evacuated from the stomach with vomiting before they have time to act).
  • . Pancreatitis . Acute pancreatitis is deadly, and chronic pancreatitis is accompanied by nausea, intestinal indigestion, swelling and diarrhea. Stool disorder in pancreatitis is associated with a deficiency of pancreatic juice - the main digestive environment of the intestine, which leads to the formation of substandard (semi-digested) stool. Their timely removal, 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 the peristalsis of the duodenum, spreading to other digestive organs, which aggravates the problem of outflow of digestive fluid.
  • . Gastritis . And also an ulcer of the stomach or intestines. Reception "Loperamide" with them is undesirable, although it is not excluded. With gastritis and ulceration, the drug will further irritate the walls of the stomach, resulting in possible pain in the stomach, the occurrence of vomiting. Both pathologies require an emphasis on the intake of soluble forms of drugs with loperamide - drops, syrup or "effervescent" tablets. But its aqueous solutions have more pronounced side effects, especially with regard to paralysis of the muscles of the back.
  • . Reception of alcohol . Alcoholic beverages are incompatible with "Loperamide", since they have an oppositely directed effect on the central nervous system and peristalsis of the intestine. Ethyl alcohol is synthesized in the intestine in order to speed up its contractions, blood flow in its walls and absorb the digested food components into the blood. The same dose of alcohol has a similar effect. And "Loperamide", on the contrary, inhibits the activity of the intestinal walls and their muscles.
The drug is contraindicated for use in obstruction and atony of the intestine, individual intolerance of the components of the drug, colitis (inflammation of the rectum) of any etiology. With the appointment of antibiotics, the use of "Loperamide" is excluded, even if their course provoked diarrhea. Otherwise, the probability or severity of side effects increases.

Side effect

Reviews about capsules "Loperamid" are mostly positive. Provided that the reception was strictly according to the indications, short (not more than two days) courses and in therapeutic doses. Side effects in this case are poorly expressed and pass themselves soon after the drug is discontinued. Among the negative reactions appear:

  • — и зуд как признаки аллергии; urticaria - and itching as signs of an allergy;
  • — при сочетании препарата с полусинтетическими антибиотиками последнего поколения; anaphylactic shock - when the drug is combined with semi-synthetic antibiotics of the latest generation;
  • — а также метеоризм, тошнота, рвота; pain in the abdomen - 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 distracted attention, dizziness, increased fatigue, which are 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 cardiac contractions, until it stops.

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

The most formidable complications from the digestive tract when taking "Loperamide" are: acute constipation, intestinal paralysis followed by the development of paralytic ileus (obstruction). Their likelihood increases, if the reception of "Loperamide" is carried out simultaneously with the course of other opiates, for example, painkillers. And his overdose, in addition to cardiac arrest, can result in a stop of breathing.

Instructions for use with loperamide

The dosage of "Loperamide" at the first intake is twice as high as all the subsequent doses. Take it should be inside, before meals or after meals, "washing down" them every episode of emptying 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 the "starting" drops, the dosage is 60 drops, and all the subsequent ones - 30 drops in each.
  • . Children older than five years . They are given a starting dose in the amount of 2 mg (or 30 drops), and all subsequent - 1 mg (15 drops) after each stool with liquid masses, but not more than 8 mg per day (that is, half as much as adults).
  • . Children under five . Prescribe drugs on the basis of loperamide at this age is only the right pediatrician, 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 the body weight of the baby.

The course "Loperamide" should be discontinued immediately, as soon as the stool is normalized. Or with side effects. If, after stopping diarrhea, new urges for defecation are not observed during the day (for children and adolescents - half a day or longer), you should consult a doctor. Return to the reception of "Loperamide" and preparations based on it in the future is not recommended.

A green arrow is drawn on the woman's belly

Options for safe replacement

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

  • . Probiotics . Packaged cultures of lacto- and / or bifidobacteria. They help from disorders of stool and gases provoked by intestinal dysbiosis. Probiotics are recommended for admission 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 preparations in capsules that dissolve only in the intestine. The use of probiotics 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 useful part of the intestinal microflora (most often high-carbohydrate). Patients who adhere to a normal, not dietary diet, there is no need for their separate admission. And in the presence of restrictions on carbohydrates, for example, diabetes mellitus, their use makes sense only in combination with probiotics.
  • . Antibiotics . Semisynthetic and fully synthetic. The use of drugs of this group is relevant for intestinal infections, poisoning and enterobiosis.
  • . Enterosorbents . Absorbers are foreign to the digestive tract or irritating components. The most famous representatives of this series are: black (wood burning product) and white (diosmectite, silicon) activated carbon. And also a "liquid" version of white coal (available under the trade name "Smecta") and povidone. Absorbents can cope with diarrhea caused by light food poisoning (stale food, but not poisonous fungi or rotten meat), common fungal and bacterial invasions. Most of the viruses and intestinal parasites do not act, they only alleviate the symptoms by absorbing the products of their vital activity.

A good antidiarrhoeal effect is provided by water decoctions of blueberry and bird cherry (a moderately poisonous plant), as well as pomegranate peels. In terms of side effects, they are safer (if there is no allergy) and are effective against prolonged diarrhea, which can last even a week if rotavirus infection occurs. At the same time, indications for the use of "Loperamide" contain a two-day restriction on the timing of its admission, which is important to observe because of the probability of severe intestinal atony. This makes it difficult to treat medicines with loperamide of many intestinal disorders.

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