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 you need to know about loperamide
Keep loperamide and all other medicines out of the reach of children, never share your medicine with other people, and use it only as directed.
Before using loperamide, be sure to consult your doctor.
Sources
Loperamide / Drugs.com
Loperamide/National register of medicinal products (ukr.)
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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.
How to take loperamide?
You should take loperamide according to the instructions or individual doctor's prescription.
You should not take a dose of the drug more than recommended in the instructions. Overdose can cause serious heart problems and other negative effects.
Pay attention to the difference in dosages for adults and children. Doses for children of different ages are different, so read the instructions carefully.
Loperamide in tablet and capsule form should be taken with a full glass of water.
Diarrhea causes fluid loss that needs to be replaced, so if you have this condition, you should drink plenty of water to avoid dehydration.
The rules for using loperamide depend on the form of the drug, for example, a chewable tablet must be chewed before swallowing. Loperamide in the form of an oral suspension (liquid) should be shaken before administration and the dose indicated in the instructions should be taken. It must be measured only using a special device for measuring the dose of medicine, which is included with the package, and not with a kitchen spoon.
The drug must be stored at room temperature, avoiding moisture and sunlight. Loperamide in liquid and suspension form should not be frozen.
Be careful!
Stop using the drug and call your doctor if, after 2 days of using loperamide, your diarrhea does not go away or you experience bloating.
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.
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.
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 .
What should you not do while taking loperamide?
Loperamide should not be taken with tonic water; the interaction between the two may cause heart problems.
Stay hydrated and drink plenty of fluids. If you are dehydrated, do not engage in intense exercise or be outside in hot weather.
Study the effect of the drug on you before driving a car or operating complex machinery. The speed of your reactions may be impaired. If the medicine causes drowsiness and slower reactions, do not drive or operate complex machinery after using it.
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.
Consequences of an overdose of loperamide
Get emergency medical help if you think you have taken too much loperamide.
Symptoms of overdose are as follows:
- cardiopalmus;
- irregular heartbeat;
- fainting.
Be careful!
If you have these symptoms, call your doctor or seek emergency medical help immediately. If you become unconscious, the person near you should immediately seek emergency medical attention.
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.
#3 Disadvantages of loperamide
People 18 to 60 years of age who are not taking any medications or have other medical conditions are likely to experience the following side effects:
- Constipation (as a consequence of taking more loperamide).
- Dizziness or drowsiness, which may affect your ability to drive or operate machines.
- Bloating, loss of appetite, abdominal pain and skin rash.
The drug may not be suitable for you in the following cases:
- with intestinal obstruction, abdominal pain without diarrhea, blood or mucus with diarrhea;
- with rare hereditary forms of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome, since the capsules may contain lactose;
- during pregnancy and breastfeeding, except on the advice of a doctor.
Be careful!
In general, older adults and children, people with liver or kidney disease, heart disease, diabetes and seizures, and people taking other medications that interact with ibuprofen are at greater risk of developing a wide range of side effects.
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 .
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.
