A fast and effective remedy for acute diarrhea

Loperamide is a medical substance that can provide fast and reliable relief from acute diarrhea symptoms. Such an antidiarrheal agent should always be included in any medicine cabinet or travel pharmacy. Find out here what exactly Loperamide is, how it works and what you need to know about its use.

What is Loperamide?

Loperamide is a drug from the group of peristaltic inhibitors and, as a so-called mock opioid, belongs to the drug class of opioids. It is used as an antidiarrheal agent in the treatment of the symptoms of diarrheal diseases of various causes. Loperamide was first synthesized in 1969 and marketed under the trade name Imodium® in 1973. In 2013 it was included in the WHO list of essential medicines.

At present, Loperamide is the best-selling non-prescription gastrointestinal drug on the German drug market. There are a large number of different generics containing the active ingredient Loperamide, mostly in the form of the salt Loperamide Hydrochloride. Usually, these generic drugs are available in the form of tablets, fused tablets, capsules or soft capsules. One example is Loperamid akut Aristo®, which is taken orally as a two-milligram tablet and is suitable for short-term, rapid and acute treatment of diarrhea symptoms.

For which areas of application is Loperamide recommended?

As an antidiarrheal agent, Loperamide is suitable for the symptomatic treatment of diarrheal diseases of various causes. The German Society for General and Family Medicine recommends Loperamide as a medication on demand for acute diarrhea. Typical causative diseases for the symptom diarrhea are:

• Acute, unspecific diarrhea
• travel diarrhea
• diarrhea due to motility disorder
• diarrhea due to irritable bowel syndrome

In no case does Loperamide replace a causal therapy of the disease, but serves only for acute symptomatic treatment. The scope of application is specifically limited to diarrhea complaints and not generally to gastrointestinal complaints of various kinds.

How does Loperamide work?

Unlike many other opioids, Loperamide acts primarily directly in the intestine. Thus, neither a psychotropic effect nor side effects in the nervous system such as an analgesic effect, respiratory depression or miosis occur. The active substance docks to the opioid receptors of the intestine and therefore reduces the activity of the circular smooth and longitudinal muscles in the wall of the small intestine. The intestinal movement (motility) decreases, which in turn slows down the intestinal passage of stool.

The intestinal contents thus remain in contact with the intestinal mucosa for a longer time, allowing the body to absorb more fluid, electrolytes and nutrients from it. Another effect of Loperamide is to increase the tone of the anal closing muscle. This leads to improved stool continence.

What side effects are to be expected when using Loperamide?

The active ingredient Loperamide is generally considered to be well tolerated. However, the following side effects may occur:

• In about one in ten users: constipation, nausea, bloating, dizziness, or headaches
• In about one in 100 users: gastrointestinal pain, dry mouth, vomiting, indigestion, skin rash

If these or other side effects occur after taking loperamide, a doctor or pharmacist must be consulted immediately.

How to take Loperamide?

Generic drugs with Loperamide as the active ingredient are usually taken orally, whether in the form of tablets, fused tablets, capsules or soft capsules. Taking Loperamid akut Aristo® is only recommended from the age of twelve years. Exceeding the treatment period of two days is only possible under medical prescription and observation of the course of treatment. The tablets, each containing two milligrams of the active substance, are taken orally, one by one, without being chewed, with liquid. If, despite taking the medication, the symptom of diarrhea persists after two days, a doctor must be consulted.

At the beginning of the treatment with Loperamid akut Aristo®, an initial dose of four milligrams, i.e. two tablets, is recommended for adults. Adolescents aged twelve years and older should start taking one tablet as the first dose. This is followed by a further dose of two milligrams after each excessively liquid bowel movement. For adults, the maximum daily dose is six tablets, and for adolescents aged twelve and older, four tablets. The treatment can and should be discontinued as soon as the bowel movement returns to normal.

What should be observed before the self-medication with Loperamide

In cases of diarrhea accompanied by fever, or if blood, mucus or pus appears in the stool, medical help must be consulted and self-medication with Loperamide is strictly advised against. This is sometimes a bacterial infection which can be worsened by the administration of Loperamide.

People who suffer from pre-existing conditions, especially chronic diarrhea or liver disease, should only consider treatment with Loperamide by the doctor’s order. This also applies to pregnant women and nursing mothers.

Excessive consumption of quinine-containing soft drinks such as tonic water is not recommended while taking Loperamide, as this combination can lead to respiratory arrest. Patients using other medications, especially Ritonavir, Itraconazole, Ketoconazole, Quinidine, Verapamil, Gemfibrozil and Desmopressin, should discuss the medication with Loperamide in detail with their doctor in advance. In interaction with these medications negative effects on the central nervous system and respiratory depression  may occur.

What to do with Loperamide in case of overdose?

If side effects occur or if the maximum recommended daily dose of six tablets in adults or four tablets in adolescents between the ages of 12 and 18 years is exceeded, a doctor should be consulted immediately. Relative overdose may result in liver dysfunction. Such relative overdose may occur if the patient is taking other drugs besides Loperamide which are broken down in the liver by the same enzyme systems.

A single overdose may already result in coordination disorders, drowsiness, muscle stiffness, respiratory weakness, increased heart rate, irregular heart rate or constipation up to intestinal obstruction. Therefore, it is essential to consult a doctor in this case as well.

How can the cause of the diarrhea disease be eliminated?

In addition to an appropriate adjustment of the diet, the most sensible treatment measure for diarrhea symptoms is to ensure adequate replacement of fluids and electrolytes. These are quickly excreted with the stool in acute and severe diarrhea. In addition to fighting the symptoms with Loperamid akut Aristo®, the glucose-electrolyte mixture Saltadol® is therefore recommended as a supporting treatment for diarrhea. As an oral rehydration solution, it ensures rapid compensation of water and electrolyte losses. Both Loperamid akut Aristo® and Saltadol® should have a permanent place in every travel and home pharmacy.