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

Science has long known about the dangers of opiates for the central nervous system of humans, it has become one of the reasons for their prohibition around the world (the second is the addiction effect, which forces drug addicts to increase the dose until death). But their ability to block the work of nerve endings remains valuable to medicine. This property is widely used for the relief of pain in cancer, surgical interventions, and injuries.

Even the choice of drugs for diarrhea must be approached with all seriousness, so before drinking Loperamide, you need to figure out if you need this particular drug, how many tablets can be taken at a time, how often, how long can you drink, after how long can you resume taking Loperamide, if symptoms of diarrhea recur.

Operating principle

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

Indications

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

• Imodium
• Lopedium;
• "Superiloma";
• "Suprilola";
• "Diars";
• Enterobene.

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

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

• food poisoning;
• rotavirus infection;
• intestinal dysbiosis;
• enteroviruses and intestinal infections (bacterial, fungal).

Destination restrictions

Regarding the question of whether Loperamide is given to children, for a long time, children's preparations based on the substance of the same name were popular and were included in the lists of vital 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 body. They consisted in the appearance of paralytic scoliosis.This complication occurs after poliomyelitis and is characterized by a 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 the curved segment if posture cannot be restored by other methods. But as a complication from taking loperamide, he provoked several deaths. This has 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” 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 it is excluded from this list. Restrictions on its admission relate to:

• children under five - but judging by the reviews of doctors, the ban on his appointment for children under 12 years old is also not without reason;
• parts of the adult population - whose work is associated with increased attention, physical activity and quick reaction (drivers, rescuers, industrial climbers, police officers);
• patients with liver failure - since the liver "digests" the main part of the taken loperamide.

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 together with it. Among them are the following cases.

• Pregnancy. The question whether Loperamide can be used during 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 (protective barrier of the placenta) is unknown. In favor of his admission is the inability of Loperamide to overcome the blood-brain barrier similar to chorionic villi. And against - the high potential danger of the drug to the muscles and central nervous system of the fetus (taking into account its proven harm to already born children). Additional risk factors are the lack of formation of the fetal body’s own protective mechanisms (blood-brain barrier) and the permeability of the placental barrier that can change under the influence of a number of factors. Despite the insufficiency of research on this topic, Loperamide and its complete analogues are prohibited for use during pregnancy and while breastfeeding.
• Nausea and vomiting. "Loperamide" is not a means to stop them, and it can provoke them. This happens if the need to evacuate the contents of the digestive tract remains, and one of its pathways is blocked by the action of the drug. Plus, taking any medication other than antiemetics is useless in this case (they will be evacuated from the stomach with vomiting before they can act).
• Pancreatitis. Acute pancreatitis is deadly, and chronic is accompanied by nausea, intestinal indigestion, bloating and diarrhea. Stool disorder with pancreatitis is associated with a deficiency of pancreatic juice - the main digestive environment of the intestine, which leads to the formation of low-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 the peristalsis of the duodenum, spreading to other digestive organs, which exacerbates the problem of outflow of digestive fluid.
• Gastritis. As well as an ulcer of the stomach or intestines. Admission "Loperamide" with them is undesirable, although not excluded.With gastritis and an ulcer, the drug will additionally irritate the walls of the stomach, as a result of which there may be pain in the stomach, the appearance of vomiting. Both pathologies require an emphasis on the administration 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 back muscles.
• Alcohol intake. Alcoholic beverages are incompatible with Loperamide because they have the opposite effect 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 the digested food components into the blood. The taken dose of alcohol has a similar effect. And “Loperamide”, on the contrary, inhibits the activity of the intestinal walls and their muscles.

Side effect

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

• hives - and itching as signs of an allergy;
• anaphylactic shock - when combining the drug with semi-synthetic antibiotics of the latest generation;
• abdominal pain - as well as flatulence, nausea, vomiting;
• drowsiness - with distracted attention, dizziness, increased fatigue, which occur due to the inhibitory effect of loperamide and other opiates on the brain;
• arrhythmia - reduction in the frequency of contractions of the heart, up to its stop.

Usually, arrhythmia is observed when Loperamide is taken together with macrolides (a type of antibiotic with a special structure and conditionally lower toxicity to the patient’s body), antiviral and antifungal agents.

Instructions for the use of drugs with loperamide

Dosage "Loperamide" at the first dose is twice as high as all subsequent ones. It should be taken orally, before meals or after meals, "washing down" with them every episode of emptying liquid masses.

• Adults. A single portion of loperamide for them in the first dose is 4 mg, all subsequent ones - 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 ones - 30 drops each.
• Children over five. They are prescribed a starting dose of 2 mg (or 30 drops), and all subsequent doses are 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. Only a pediatrician has the right to prescribe drugs based on 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 the baby's body weight.

The course "Loperamide" must be stopped immediately, as soon as the chair is normal. Or when side effects occur.If after stopping the diarrhea there is no new urge to defecate during the day (in children and adolescents - half a day or longer), you should consult a doctor. Returning to Loperamide and drugs based on it is not recommended in the future.

Safe Replacement Options

The analogues of drugs with loperamide are endless rows of drugs against diarrhea with different composition and effect.

• Probiotics. Packaged cultures of lactobacilli and / or bifidobacteria. They help against stool and gas disorders caused 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 intestinal microflora (most often high carbohydrate). In patients who adhere to a normal rather than dietary diet, there is no need for their separate intake. And if there are restrictions on carbohydrates, for example, with diabetes, their use makes sense only in combination with probiotics.
• Antibiotics. Semi-synthetic and fully synthetic. The use of drugs of this group is relevant for intestinal infections, poisoning and enterobiosis.
• Enterosorbents. Absorbers alien to the digestive tract or irritating components. The most famous representatives of this series are: black (a product of wood burning) and white (diosmectite, silicon) activated carbon. And also a “liquid” version of white coal (produced under the trade name “Smecta") And povidone. Absorbents are able to deal with diarrhea caused by light food poisoning (stale food, but not poisonous mushrooms or rotten meat), common fungal and bacterial infestations. They do not act on most viruses and intestinal parasites, they only alleviate the symptoms by absorbing the products of their vital functions.

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

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