Pharmacodynamics and pharmacokinetics
Loperamide Hydrochloride is an antidiarrheal drug that is effective in inhibiting intestinal motility. The effect of the drug is manifested due to the binding of its active ingredient to opioid receptors located in the intestinal walls, resulting in suppression of the release of prostaglandin E2α and acetylcholine . As a result of this effect, the movement of intestinal contents and its peristalsis , and the absorption time of electrolytes and water . In addition to this, the drug has an antisecretory effect, reduces the urge to defecate , increases the tone of the anal sphincter and helps to contain feces.
T1/2 of a drug is on average 11 (from 9 to 14) hours. The connection with plasma proteins (mainly with albumin ) is at the level of 95%. Elimination is carried out due to oxidative N-demethylation, which is the main pathway of metabolic transformations of the drug. It is excreted from the human body mainly with feces.
What is loperamide used for?
The drug is aimed at getting rid of an attack of diarrhea. It works as follows: the active substance, entering the intestines, begins its effect on its muscles and ability to contract. As a result, taking Loperamide stops bowel activity while simultaneously increasing the tone of the anal sphincter, so that loose stool cannot be released uncontrollably from the rectum. An inactive state of the intestines, close to paralysis, allows food to have time to be absorbed into the bloodstream and slowly move towards the exit.
Indications for use
The use of Loperamide Hydrochloride is indicated for the symptomatic treatment of chronic and acute diarrhea.
The drug can be used for prevention against traveler's diarrhea . In this case, therapy should continue for at least 48 hours. blood is detected in the stool should the drug intake be interrupted until the exact cause of this phenomenon is determined.
Contraindications
Prescribing the drug is not allowed for:
- pathologies associated with sugar intolerance ;
- personal hypersensitivity to loperamide hydrochloride or other components of the tablets;
- pseudomembranous colitis or acute ulcerative colitis that developed due to previous antibiotic therapy ;
- acute dysentery (with manifestations of fever and the presence of blood in the stool);
- bacterial enterocolitis , due to exposure to bacteria of the genera Campylobacter , Shigella and Salmonella ;
- liver pathologies;
- children under 6 years old.
Side effects
The immune system:
- anaphylactoid reactions;
- anaphylactic shock.
Nervous system:
- insomnia / drowsiness ;
- headache;
- convulsions;
- increased fatigue;
- tremor;
- dizziness;
- depression / loss of consciousness .
Digestive system:
- colic / stomach cramps
- nausea , vomiting ;
- ileus;
- constipation;
- forced formation of toxic megacolon ;
- dyspepsia;
- dry mouth;
- flatulence;
- intestinal obstruction (paralytic).
Urinary system:
- urinary retention.
Skin:
- erythema multiforme;
- skin rashes;
- hives;
- Stevens-Johnson syndrome;
- angioedema;
- epidermal toxic necrolysis.
Instructions for use of Loperamide Hydrochloride (Method and dosage)
According to the instructions for Loperamide Hydrochloride, the drug is intended for oral administration by patients over 6 years of age.
For acute diarrhea, an initial dose of 4 mg is indicated for adult patients and 2 mg for children. Subsequently, despite the patient’s age, it is recommended to take 2 mg of the drug after each loose bowel movement .
For chronic diarrhea, 4 mg is prescribed daily for adult patients and 2 mg for children. In the future, you should individually select a maintenance dose of the drug, for which loperamide hydrochloride is dosed in such a way that the number of acts of solid bowel movements per day is 1-2 times. In this case, the individual dosage regimen varies in the range of 2-12 mg per 24 hours.
For any manifestation of diarrhea (chronic/acute), the maximum daily dosage for adults is considered to be 16 mg. For children, this dose is calculated based on their weight, in the ratio of 6 mg per 20 kg of body weight.
If there is no clinical effectiveness in treating acute diarrhea within 48 hours, the drug should be discontinued.
For the treatment of elderly patients and patients with kidney pathologies, no dosage adjustment is required.
In case of liver pathologies, the drug should be prescribed with caution, due to a possible slowdown in first-pass metabolic transformations.
The drug is not prescribed for the initial treatment of severe diarrhea , which occurs with a decrease in the level of electrolytes and fluid in the body. In childhood, this loss should be compensated for by oral and/or parenteral replacement therapy.
Loperamide instructions: from what
The prescription of the drug is not always associated with the onset of diarrhea, although it is the main indication. If stool disorder occurs due to a reaction to taking medications, you should take Loperamide, which will stop the rapid movement of food through the intestines, and along with it, the medication taken.
This will allow the active substances not to be evacuated through the anus, but to remain in the intestine in order to have time to be absorbed into the blood and provide the expected therapeutic assistance. Diarrhea is often caused by taking antibiotics. If the patient takes antibacterial drugs, and they, along with frequent loose stools, immediately leave the body, no treatment will work. Therefore, diarrhea caused by taking medications is the first indication for prescribing Loperamide.
In addition, the drug is indicated for use in case of metabolic disorders. In this case, the patient, no matter how much he eats, does not gain weight, does not receive enough nutrients, as a result of which the body is rapidly depleted. Loperamide allows food to stay in the intestines, and vitamins and minerals to be absorbed through its walls.
If the patient has had surgery to remove the end of the intestine through an opening in the abdominal cavity, Loperamide may be prescribed to reduce the frequency of bowel movements and also allow food to remain in the lumen, which is especially important for those patients whose intestinal length has been significantly reduced as a result of the operation .
Overdose
If the dosage regimen is violated and excessive doses of the drug are taken, the following may be observed: stupor , drowsiness , loss of coordination, miosis , respiratory depression , hypertonicity of the skeletal muscles, urinary retention , as well as symptoms of intestinal obstruction . the blood-brain barrier not fully functioning .
The antidote for the drug is Naloxone . Due to the fact that loperamide hydrochloride acts 1-3 hours longer than Naloxone , it may be necessary to re-apply the antidote. To detect possible CNS depression, the patient must be under medical supervision for at least 48 hours. In parallel with the use of an antidote , symptomatic treatment can be carried out, including cleaning the gastrointestinal tract and taking sorbents .
Adverse reactions
The following negative effects may occur:
- allergy;
- bloating;
- weakness;
- gagging;
- difficult emptying;
- feeling of dry mouth;
- dizziness;
- discomfort and pain in the abdominal area.
In rare cases, there may be urinary retention.
Interaction
Combined use with anticholinergic drugs ( atropine ) causes a mutual increase in effectiveness, and therefore it is better to avoid such a combination of drugs.
You should not treat with loperamide hydrochloride when the patient is using drugs that suppress the central nervous system (especially children).
Parallel use of drugs that are inhibitors of P-glycoproteins ( Ritonavir , Quinidine ) and dosages of loperamide hydrochloride close to the maximum increases the plasma level of the latter by 2-3 times. The significance of this interaction for clinical therapy in the dose range of loperamide hydrochloride 2-16 mg has not been established.
special instructions
It is worth remembering that the use of loperamide hydrochloride for the treatment of diarrhea is symptomatic. In the case when the cause of diarrhea is accurately diagnosed, it is better to carry out targeted therapy using medications indicated specifically for this painful condition.
Purely against the background of diarrhea , especially in children, an imbalance of electrolytes and dehydration . When observing these phenomena, first of all, measures should be taken to replenish electrolytes and fluids in the body.
When taking loperamide hydrochloride to treat diarrhea in patients with immunodeficiency , if the first symptoms of abdominal bloating , therapy should be stopped immediately. Also, in patients with AIDS , isolated cases of the formation of toxic megacolon with parallel infectious colitis both bacterial and viral etiology .
Despite the absence of deviations in the pharmacokinetic parameters of loperamide hydrochloride in the treatment of patients with liver pathologies , this group of patients should prescribe the drug with caution, due to the slowdown in first-pass metabolic transformations. For timely detection of possible symptoms of toxic damage to the central nervous system, such patients should be under constant observation.
Due to the presence of lactose , its use is prohibited for patients with sugar intolerance .
In case of formation of bloating , constipation , partial intestinal obstruction , as well as megacolon , diverticulosis , enterocolitis associated with exposure to Salmonella bacteria , therapy should be stopped immediately.
How to take Loperamide for diarrhea
First of all, it is important to understand the etiology of diarrhea. If diarrhea occurs due to excitement, or during a trip that provokes tourist syndrome, Loperamide will come in handy. The tablet must be taken immediately after defecation. That is, if there is a feeling that a bowel movement is about to occur, the feces should be allowed to come out, and then immediately take the drug. Loperamide will stop the bowels and strengthen the anal sphincter. If you do not allow a portion of feces to escape, intoxication may occur.
In case of poisoning, taking Loperamide is not justified, since the drug is not a sorbent and does not help stop the absorption of toxic substances into the blood. Instead, it will simply cause the intestines to freeze, and given the fact that there is low-quality food inside it, which caused diarrhea, the patient’s condition will only worsen, since the toxic substances will remain inside the gastrointestinal tract.
Analogs
Level 4 ATC code matches:
Loperamide
Imodium Plus
Imodium
Lopedium
- Loflatil;
- Diaremix;
- Uzara;
- Imodium Plus.
During pregnancy and lactation
data on the embryotoxic and teratogenic effects of loperamide hydrochloride . Despite this, during pregnancy , especially in the first trimester, prescribing the drug is permissible only if the positive effect for the mother significantly exceeds the possible risk for the fetus/child.
A certain amount of the drug is found in the milk of a nursing mother, and therefore breastfeeding .
Can I take Loperamide during pregnancy?
Diarrhea that occurs during pregnancy should not become a reason to decide on self-medication. First of all, it is necessary to examine a pregnant woman for the presence of an intestinal infection. Then it is important to evaluate her diet in order to draw conclusions about the need to adjust the menu. If diarrhea is not the result of serious gastrointestinal disorders, Loperamide may be approved for use provided that the pregnancy is not in the first trimester.
Reviews
When looking through reviews of loperamide hydrochloride, you should remember that this drug is mainly intended for the symptomatic treatment of diarrhea for a short period of time. In the case of bacterial , exudative , invasive , etc. origin, the drug will be at least ineffective, and in some cases may lead to masking of the symptoms of the pathological process and, as a result, to the progression of the disease.
How much does Loperamide Akrikhin cost?
There are many manufacturers producing Loperamide under different names. The addition “Akrikhin” indicates that the drug belongs to a specific company. The manufacturer Akrikhin KhFK JSC is not a representative of companies selling drugs at high prices, therefore, if the pharmacy does not have just Loperamide, and the pharmacist offers an analogue with the postscript “Akrikhin”, do not be alarmed. The price for a package of 20 tablets will cost about 59 rubles, and a box with a dozen tablets will cost only 30 rubles.
