Loperamide hydrochloride – description of the drug, instructions for use, reviews

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Manufacturers: Vasudha Pharma Chem Limited, Quimica Sintetica

Active ingredients

• Loperamide

Disease class

• Functional diarrhea
• Bacterial intestinal infection, unspecified

Clinical and pharmacological group

• Not indicated. See instructions

Pharmacological action

• Antidiarrheal

Pharmacological group

• Antidiarrheals

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.

Release form and composition

Dosage form - capsules: cylindrical with hemispherical ends, hard, gelatinous, white or white with a yellowish tint; contents – white or white granules with a yellowish tint (in a cardboard box there are 1–2 strip packs of 10 capsules each and instructions for use of Loperamide hydrochloride).

Composition of 1 capsule:

• active substance: loperamide hydrochloride – 2 mg;
• auxiliary components: magnesium stearate, corn starch, lactose monohydrate;
• capsule shell composition: gelatin, sodium lauryl sulfate, glycerin, propyl parahydroxybenzoate E 216, methyl parahydroxybenzoate E 218, titanium dioxide E 171, purified water.

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.

Story

Loperamide hydrochloride was first synthesized by Paul Janssen of Janssen Pharmaceutica in Beers, Belgium, following the previous discoveries of diphenoxylate hydrochloride (1956) and fentanyl citrate (1960).[3]

The first clinical description of loperamide was published in 1973 in the Journal of Medicinal Chemistry, one of the authors was the drug's creator.[4]

Clinical placebo-controlled trials of loperamide were launched in December 1972 and continued until February 1974. The results of the study were published in 1977 in the journal Gut, a publication of the British Society of Gastroenterology.[5]

The drug was patented in the United States in 1973.[6][7]

In 1973, Janssen began marketing loperamide under the brand name Imodium.

In December 1976, Imodium received approval from the US Food and Drug Administration (FDA).[8]

In the 1980s, Imodium became the best-selling prescription anti-diarrhea drug in the United States.[9]

In March 1988, McNeil Pharmaceuticals began marketing loperamide as an over-the-counter drug under the trade name Imodium AD.[10]

Imodium packaging in the form of lozenges

The 1980s also saw the introduction of loperamide in the form of drops (Imodium drops) and syrup. The drug was originally intended for children, but Johnson & Johnson withdrew the drug from the market in 1990 after 18 cases of paralytic scoliosis (6 cases were fatal) were reported to the World Health Organization in Pakistan.[11] In subsequent years (1990–1991), products containing loperamide were contraindicated for use by children in a number of countries (children 2 to 5 years of age).[12][13]

In the late 1980s, before the US patent expired on January 30, 1990,[9] McNeil began developing Imodium Advanced, containing loperamide and simethicone, for the treatment of diarrhea and bloating. The company patented this formula in March 1997.[14] In June 1997, the drug received FDA approval under the name Imodium Multi-Symptom Relief in chewable tablet form.[15]

In November 1993, loperamide was released in the form of loperamide lozenges, developed using Zydis technology.[16][17] Imodium® Instant Melts are currently the only loperamide-containing loperamide loperamide available in lozenge form.[18][19]

In Russia, “Imodium” was included in the list of VED in 2010[20], and in 2015, instant loperamide (“Imodium” lyophilized tablets) was excluded from the list of VED[21].

In 2013, loperamide 2 mg tablets was added to the WHO Model List of Essential Medicines.[2]

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 .

Loperamide and Imodium: the difference between the drugs

These two drugs are used to treat diarrhea and contain the same active ingredient, namely loperamide hydrochloride. But why are they called differently and why is the cost of Imodium so much higher than Loperamide?

Everything is explained by the fact that Imodium is the original drug, and Loperamide is generic. That is, Imodium was first invented: scientists derived its formula, conducted preclinical and clinical studies and received a patent for this medicine. And then, when the patent expired, it became possible for other companies to produce it, only under a different name and with a slightly different composition from the original. The difference lies in the list and dosages of excipients.

It is worth noting that only original drugs must undergo preclinical and clinical studies; this is not required from generics, since the effectiveness of the formula used in them has already been proven. However, all of the above does not mean that generics are less effective and safe than the originals. For example, Loperamide has been tested for pharmaceutical equivalence (the rate and extent of absorption of the drug) and is considered no less effective than Imodium.

Now you know that Imodium and Loperamide are the same medicine, differing only in name, price and composition of excipients. The cost of Imodium is higher, since it is a patented original drug and has undergone a number of studies. The next time you buy Loperamide or Imodium at the pharmacy, you will already understand the difference between them.

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.

Content

• 1. History
• 2 Pharmacological action
• 3 Pharmacokinetics
• 4 Application
• 5 Contraindications 5.1 Restrictions on use
• 5.2 Use during pregnancy and breastfeeding

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.