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Last Updated on January 15, 2019

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Loperamide

The active ingredient Loperamide is a so-called opioid and is one of the most commonly used agents for diarrhea. He is generally well tolerated, can lead to constipation, in rare cases, however. Here you can read everything about the use of Loperamide, dosage and side effects.

How Loperamide works

Loperamide acts in the so-called opioid receptors in the gut -Andockstellen for certain hormones (endorphins), which slow down the intestinal transit. Due to the damped motion of the colon there is an increased uptake of water from the digesta, thereby this is thickened – is stopped. Many other opioids such as fentanyl and opiates such as morphine, which are used as strong painkillers, cause as a side effect to a slowing of intestinal transit.

Loperamide may potentially also act in the central nervous system as an opioid, that produce an analgesic and soporific effect. However, these effects occur in patients with a healthy blood-brain barrier is not on, because penetrated Loperamide is also promoted immediately on certain transport proteins.

absorption and excretion of Loperamide

After taking the drug Loperamide binds mainly directly to the intestinal wall. It is absorbed into the blood and rapidly degraded by the liver so that less than one percent of the occupied amount of drug enters the systemic circulation. About eleven hours after taking half of the drug is excreted in the stool. The degradation products produced in the liver, leaving the body with the chair.

When is Loperamide used?

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

Special low dosed preparations are used to treat children from two years.

A treatment duration of more than two days requires a doctor’s supervision.

How Loperamide is applied

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

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At the beginning of treatment four milligrams Loperamide (usually two tablets or capsules) taken, later each another dose (two milligrams) after each unformed stool. The daily maximum dose of six tablets or capsules must not be exceeded.

In adolescents from twelve to 18 years a tablet or capsule is at the beginning taken, then also after each unformed stool another. The maximum daily dose is four tablets or capsules.

Loperamide must not be used in case of diarrhea, with blood or pus in the stool accompanied. These symptoms suggest a bacterial cause towards which can be aggravated by the handover of the diarrheal agent.

Due to the loss of fluid and salts (electrolytes) in severe diarrhea, it may be advisable after the diarrhea to replace the lost substances while and the body, with the so-called oral rehydration solutions. Furthermore, can be specifically strengthened the intestinal flora with preparations of dried yeast and / or bacteria cultures and rebuilt.

What are the side effects of Loperamide?

In a step down from ten to one hundred patients treated Loperamide side effects such as nausea and bloating.

In addition, it comes with a hundred to a thousand of those treated for side effects like drowsiness, abdominal pain, dry mouth, vomiting, indigestion and skin rashes.

What should be considered when taking Loperamide?

Some drugs are broken down by the liver in the same enzyme systems such as Loperamide. Concomitant administration can therefore be inhibited the degradation of the diarrheal agent, which leads to increased blood levels of Loperamide. In addition, substances that block the corresponding transport protein in the blood-brain barrier, lead to increased Loperamide concentration in the central nervous system. These drugs include, for example quinidine (medicines for irregular heart beat), ritonavir (HIV medication), itraconazole, ketoconazole (antifungal) and gemfibrozil (lipid lowering agents).

Although in studies showed no harmful effects on the unborn child and the infant, should be avoided as a precaution during pregnancy and lactation on taking Loperamide.

In patients with liver dysfunction or disease, the diarrheal agents should be used only under medical supervision and with caution.

No dosage adjustment in elderly patients or patients with renal impairment is not necessary.

How to obtain medicines with Loperamide

preparations with Loperamide are prescription free in small packages of up to twelve tablets or capsules to two milligrams of active ingredient, as that is the maximum dose for two days. If the patient then are still suffering from diarrhea, a doctor must necessarily be consulted. Often these packages are printed with “Loperamide acute” to make it clear that they are intended for self-therapy of acute diarrhea.

prescription for the long-term treatment are also larger packages available.

Since when Loperamide is known?

Loperamide in 1969 discovered by scientists at Janssen Pharmaceutica in Belgium pharmaceutical company. After the publication of the new drug in the year 1972, a year later, followed by the launch. Meanwhile there are many generic products with the active ingredient Loperamide .