Loperamide (acute) – Dosage and side effects

Loperamide (active ingredient: loperamide hydrochloride) is an acute diarrhea remedy. It is used for symptomatic treatment for adults and adolescents from the age of 12 if no causal therapy is available.

What symptoms can I use loperamide for?

Diarrhea can have very different causes. Regardless of the cause, adequate replacement of fluids and electrolytes is very important to prevent dehydration.

IMPORTANT: Loperamide is only used for short-term symptomatic treatment and does not combat the root cause of the diarrhea.

Especially in diarrhea with an infectious cause - which is the most common cause - the intake of loperamide can lead to an extension of the course of the disease, since the germs causing the disease cannot be excreted.

If the diarrhea is accompanied by fever, vomiting, joint pain or blood in the stool, a doctor must be consulted as soon as possible!

When should I not take loperamide?

• If you have a known allergy to loperamide hydrochloride or other components of the drug
• In conditions in which a slowdown in bowel activity must be avoided, e.g. distended body, constipation and bowel obstruction
• With accompanying fever and / or bloody stool
• For diarrhea that occurs during or after taking antibiotics
• For chronic diarrhea (these diseases may only be treated with loperamide hydrochloride according to a doctor's prescription)
• In an acute episode of ulcerative colitis

Side effects in liver diseases

If there is liver disease, loperamide should only be taken as prescribed by a doctor, because in such cases the breakdown of loperamide may be delayed and the risk of side effects may be increased.

Caution with children

Children under 2 years of age are not allowed treatment with loperamide. Children between 2 and 12 years of age can only be treated with loperamide if prescribed by a doctor

Caution with pregnancy and lactation

Even if no clear indications of a fetus-damaging effect have been shown so far, loperamide should not be taken during pregnancy due to the insufficient evidence available. Small amounts of loperamide can pass into breast milk during breastfeeding - therefore, loperamide should not be used here either.

Side effects from lactose intolerance

Most loperamide supplements contain lactose. Lactose intolerance sufferers should consult their doctor about this when taking loperamide. For example, an additional intake of lactase tablets is possible to avoid another digestive disorder caused by lactose intolerance.

What drug interactions can occur?

Medicines with effects similar to loperamide can increase the effects of intestinal movement inhibition, while others can speed up the gastrointestinal passage. If you take the following medication regularly or occasionally, you should definitely consult a doctor:

• Ritonavir (to treat HIV infection)
• Itraconazole. ketoconazole (to treat a fungal infection)
• Quinidine (to treat irregular heartbeat)
• Gemfibrozil (to treat high blood lipid levels)
• Desmopressin (to treat increased urination)

Where do I get loperamide from and how is it taken?

Loperamide is an over-the-counter medication that is available in pharmacies or online. It is often known under the trade names “Imodium®” or “Lopedium®” and is available in different forms: Hard capsules, film-coated tablets, orodispersible tablets, effervescent tablets or solutions. The prices vary depending on the manufacturer and form of consumption, e.g. for a pack of 10 tablets between about 1.50 - 5.00 euros. Despite the price differences, the different products generally show comparable effectiveness. However, it should be noted that some products contain additional active ingredients (e.g. simeticon to relieve flatulence).

Recommended dosage for loperamide hydrochloride

**The duration of use of 2 days must not be exceeded, as it can lead to severe constipation! **

What side effects can occur?

The following side effects have been observed in clinical studies:

Frequently (in up to 1/10 of those treated)

• Constipation
• Nausea
• Bloating
• Dizziness
• Headache

Occasionally (in up to 1/100 of the treated)

• Pain and discomfort in the gastrointestinal area
• Dry mouth
• Abdominal pain, vomiting
• Indigestion
• Rashes

Rare (in up to 1/1000 of those treated)

• Bloating

In general, loperamide is very well tolerated and serious side effects are very rare. In the unlikely event of serious or persistent side effects, a doctor must be consulted!

Loperamide in irritable bowel syndrome

In the current, common guideline of the German Society for Digestive and Metabolic Diseases (DGVS) and the German Society for Neurogastroenterology and Motility (DGNM), loperamide is highly recommended for the treatment of diarrhea in adult patients with RDS-D irritable bowel syndrome. This conclusion is based on three clinical studies, all of which demonstrate the efficacy of loperamide in this group of patients in terms of stool consistency, urgency, and general abdominal discomfort. However, there have been isolated reports of nocturnal abdominal discomfort while taking loperamide.

In addition to loperamide, some preparations also contain the defoaming substance simethicon, which is used to relieve bloating and associated complaints (feeling of fullness, feeling of tension in the upper abdomen) in the event of excessive gas accumulation in the gastrointestinal tract. To date, there are no studies on the effectiveness of simethicon in irritable bowel patients. Despite this insufficient level of evidence, at least one treatment attempt with a preparation containing simethicone is recommended, since this active ingredient has shown positive effects in other diseases with similar symptoms.

On the other hand, there is a strong consensus that therapy for flatulence in irritable bowel syndrome with pancreatic enzymes is not useful.

CONCLUSION: According to the current guideline, for treatment of diarrhea and flatulence in irritable bowel patients (RDS-D) loperamide preparations (possibly with added simethicone) are highly recommended!

The dosage should be as needed, e.g. 1 × 2 mg with every liquid bowel movement (up to approx. 5 - 8 × daily). The dose can be increased if diarrhea persists. Continuous therapy or prophylactic use the evening before in the case of diarrhea early in the morning can also make sense.

Loperamide for traveler’s diarrhea

Travel diarrhea is usually caused by infection. In addition to fluid replacement, antibiotic therapy is essential. Loperamide can be used for the symptomatic treatment of diarrhea. But loperamide should never be administered as the sole medication without an antibiotic, as this can slow down the elimination of toxin-producing pathogens and promote their multiplication in the intestine.

Abuse of loperamide as an addictive substance

Loperamide works by binding to specific opioid receptors in the intestinal tract, which leads to a reduction in intestinal activity. In contrast to other opioids, which also have a strong effect on opioid receptors in the central nervous system (brain and spinal cord), the effectiveness of loperamide when taken orally and at therapeutic doses is mainly limited to the intestinal tract. This is because, unlike the other opioids, loperamide cannot cross the blood-brain barrier and therefore does not reach the central nervous system when taken properly.

Reports of abuse of loperamide have been increasing in recent years. People try to achieve an intoxicating effect using various tricks (including a strong overdose) here. Above all, the low cost and easy availability seem to be factors that make loperamide attractive as a substance for drug addicts.

Keep in mind: The improper use of loperamide is not only illegal, but also potentially life-threatening!

With severe overdoses, there can be numerous side effects, including serious constipation, respiratory depression and in the worst case even fatal cardiac arrhythmia!