Immodium heals stomach pain

Loperamide

This is how loperamide works

Loperamide acts on the so-called opioid receptors in the intestine - docking points for certain hormones (endorphins), which slow down the intestinal passage. The subdued movements of the large intestine lead to an increased absorption of water from the digestive pulp, which thickens it - diarrhea is stopped. Many other opioids such as fentanyl and opiates such as morphine, which are used as strong pain relievers, have a side effect that slows down the intestinal passage.

Loperamide can potentially also act as an opioid in the central nervous system, i.e. it can have an analgesic and soporific effect. However, these effects do not occur in patients with a healthy blood-brain barrier, since penetrated loperamide is immediately transported out again via certain transport proteins.

Loperamide uptake and excretion

After ingestion, the active ingredient loperamide mainly binds directly to the intestinal wall. It is absorbed into the blood and quickly broken down by the liver, so that less than one percent of the amount of active ingredient ingested reaches the large bloodstream. About eleven hours after ingestion, half of the active ingredient is excreted in the stool. The breakdown products that accumulate in the liver also leave the body with the stool.

When is loperamide used?

Loperamide is used for the symptomatic treatment of acute diarrhea in adolescents from the age of twelve and adults.

Special low-dose preparations are available for the treatment of children from two years of age.

A treatment duration of more than two days requires medical supervision.

This is how loperamide is used

Loperamide is usually taken in the form of tablets, capsules, orodispersible tablets, or soft capsules. The preparations usually contain the active ingredient in the form of the salt loperamide hydrochloride.

At the beginning of treatment, four milligrams of loperamide (usually two tablets or capsules) are taken, followed by a further dose (two milligrams) after each unformed stool. The maximum daily dose of six tablets or capsules must not be exceeded.

For adolescents between the ages of twelve and 18, one tablet or capsule is taken at the beginning, then another one after each unformed stool. The maximum daily dose is four tablets or capsules.

Loperamide must not be used for diarrhea associated with fever, blood or pus in the stool. These symptoms indicate a bacterial cause, which can be made worse by the administration of the diarrhea medicine.

Due to the loss of fluids and salts (electrolytes) in severe diarrhea, it can make sense to replace the lost substances in the body during and after the diarrhea with so-called oral rehydration solutions. Furthermore, the intestinal flora can be specifically strengthened and rebuilt with preparations made from dry yeast and / or bacterial cultures.

What are the side effects of loperamide?

Loperamide side effects such as headache, dizziness, constipation, nausea and flatulence occur in one in ten to one hundred people treated.

Furthermore, one in a hundred to a thousand people who are treated experience side effects such as drowsiness, abdominal pain, dry mouth, vomiting, indigestion and rashes.

What should be considered when taking loperamide?

Some drugs are broken down in the liver by the same enzyme systems as loperamide. If taken at the same time, the breakdown of the diarrhea drug can be inhibited, which leads to increased loperamide blood levels. In addition, substances that block the corresponding transport protein at the blood-brain barrier can lead to an increased concentration of loperamide in the central nervous system. These drugs include, for example, quinidine (anti-arrhythmia drug), ritonavir (anti-HIV drug), itraconazole, ketoconazole (anti-fungal drug) and gemfibrozil (blood lipid lowering drug).

Although studies have not shown any harmful effects on the unborn child or infant, as a precautionary measure, the use of loperamide should be avoided during pregnancy and breastfeeding.

The diarrhea medicine should only be used with caution and under medical supervision in patients with liver dysfunction or disease.

No dose adjustment is necessary in the elderly or in patients with renal impairment.

How to get drugs with loperamide

Preparations with loperamide in small packs with up to twelve tablets or capsules containing two milligrams of active ingredient do not require a prescription, as this represents the maximum dose for two days. If the patient is still suffering from diarrhea after that, it is essential to see a doctor. These packs are often printed with “acute loperamide” to make it clear that they are intended for self-treatment of acute diarrhea.

Larger packs are also available with a prescription for long-term treatment.

How long has loperamide been known?

Loperamide was discovered in 1969 by scientists at the pharmaceutical company Janssen Pharmaceutica in Belgium. After the publication of the new active ingredient in 1972, the market launch followed a year later. There are now many generics with the active ingredient Loperamide.

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