What is loperamide? Uses and side effects of Loperamide

Diarrhea is one of the common problems of the digestive system, which is usually associated with increased emptying and loss of fluids from the intestines. This complication can be caused by various factors, including viral and bacterial infections, consumption of contaminated food, or many other causes. If diarrhea is not managed properly, it can lead to dehydration (too much fluid loss) and other serious problems. Loperamide drug is one of the drugs that relieves acute, chronic and travel diarrhea in patients with its mechanism of action. In addition to its use in diarrhea, loperamide may have side effects and risks associated with its use, which we will discuss in detail in this article.

Pharmaceutical forms of loperamide

Loperamide is available in liquid dosage forms of 1 mg/5 ml and 1 mg/7.5 ml, suspension 1 mg/7.5 ml, tablet 2 mg, capsule 2 mg, chewable tablet 2 mg.

Loperamide uses

This medicine is used to treat sudden diarrhea (including traveler’s diarrhea) that works by slowing down bowel movements. This will reduce the number of bowel movements and make the stool less watery. Loperamide is also used to reduce the amount of secretion in patients who have undergone ileostomy and to treat persistent diarrhea in people with inflammatory bowel disease. Note that this medicine only treats the symptoms and will not affect the cause of the disease. The most important uses of this drug are acute diarrhea, chronic diarrhea, and traveler’s diarrhea.

Pharmacological effects and mechanism of action of Loperamide drug

Loperamide slows down intestinal motility through opioid receptors and has a direct effect on circular and longitudinal muscles. It also reduces stool volume and increases viscosity. The maximum plasma time of this drug is 5 hours (capsule); It is 2.5 hours (liquid), which is distributed with weak penetration through the blood-brain barrier. This drug has significant first-pass metabolism, which leads to very low levels of the drug in plasma. Finally, through feces (30-40%), urine (1%) will be excreted.

Dosage of Loperamide

Before taking loperamide, check the drug information on the drug package. Take this medication orally after each loose stool or as directed by your doctor. In children, the dose is determined based on age and weight. Also, adults should not take more than 8 mg per 24 hours in case of self-medication or 16 mg per 24 hours in case of doctor’s prescription. If you are using a chewable tablet, take this medicine on an empty stomach. Also, chewable tablets should be chewed completely before swallowing.

Time to take loperamide tablets

The time of use is different in different dosage forms of loperamide, if you are using tablets that dissolve quickly, dry your hands before opening the blister pack to remove the tablet carefully and do not squeeze the tablet from inside the blister pack. Place the tablet on the tongue, let it dissolve completely, then swallow it with saliva. Diarrhea will cause dehydration in your body, so drink plenty of fluids and minerals (electrolytes) to replace the lost substances. Tell your doctor immediately if you develop symptoms of dehydration (such as extreme thirst, decreased urination, muscle cramps, weakness, fainting).

Dosage of loperamide in adults

1. To treat acute diarrhea, take 4 mg at first and then 2 mg after each diarrhea. Note that the total dosage should not exceed 16 mg per day (8 mg per day for self-medication) per day. If there is no improvement after 48 hours, stop taking the medicine and consult a doctor.
2. For chronic diarrhea, use 4 mg after the first diarrhea and then 2 mg after each stool. Note that the total intake should not exceed 8 mg per day.
3. Traveller’s diarrhea, take 4 mg after the first loose stool, then 2 mg after each bowel movement. The total intake should not exceed 8 mg per day.

Dosage of loperamide in children

1. For the treatment of acute diarrhea on the first day of treatment, in children 2 to 6 years (13 to 20 kg) 1 mg orally every 8 hours, for children 6 to 8 years (20 to 30 kg) 2 mg every 12 hours Orally, children 8 to 12 years old (over 30 kg) 2 mg orally every 8 hours.
2. Also, for acute diarrhea for the second and subsequent doses, 1 mg/kg after each loose stool, which should not exceed the recommended dose for the first 24 hours.
3. Chronic diarrhea in children, 0.24-0.8 mg/kg orally in 12-hour doses.
4. Traveller’s diarrhea in children 6 to 8 years, take 2 mg after the first loose stool, then 1 mg after each bowel movement. Note that the dosage should not exceed 4 mg per day.
5. Traveller’s diarrhea in children 8 to 12 years, 2 mg after the first loose stool, then 1 mg after each bowel movement. The total intake should not exceed 6 mg per day.
6. Traveller’s diarrhea in children over 12 years, 4 mg after the first loose stool, then 2 mg after each stool. Make sure that the total amount of consumption should not exceed 8 mg per day.

Precautions

1. Loperamide may cause drowsiness or dizziness that impairs physical abilities to operate heavy machinery or work that requires mental alertness.
2. Allergic reactions including anaphylaxis, rash, urticaria, and rare cases of Johnson-Steven syndrome or toxic epidermal necrolysis have been reported in some patients.
3. If there is no improvement in patients with acute diarrhea within 48 hours or worse symptoms, swelling or abdominal distension develop, stop taking the drug and consult a doctor.
4. Discontinue use immediately if constipation, abdominal pain or distension, blood in the stool, or ileus occur. Do not use when inhibition of peristalsis must be avoided (due to possible ileus, megacolon, or toxic megacolon).
5. Discontinue treatment if symptoms of abdominal distension occur in patients with AIDS. Cases of toxic megacolon with infectious colitis, caused by viral or bacterial pathogens, have been reported.
6. Use with caution in patients with liver failure due to reduced first-pass metabolism. Monitor for signs of CNS toxicity.
7. Use of higher than recommended doses or misuse of loperamide can lead to serious cardiac side effects including QT prolongation, torsade de pointes, or other ventricular arrhythmias, syncope, and cardiac arrest. In cases of abuse, people often use other drugs together with loperamide in an attempt to increase its absorption and penetration in the blood-brain barrier, inhibit the metabolism of loperamide and increase its euphoric effects.
8. from combining loperamide with drugs or herbal products known to prolong the QT interval, including class 1A (eg, quinidine, procainamide) or class III (eg, amiodarone, sotalol) antiarrhythmics, antipsychotics (eg, chlorpromazine, haloperidol), antibiotics (eg, (eg, moxifloxacin) or any other drug that prolongs the QT interval (eg, pentamidine, methadone).
9. Avoid prescribing therapy to patients with risk factors for QT prolongation, including patients with congenital long QT syndrome, a history of cardiac arrhythmia or other heart disease, elderly patients, and individuals with electrolyte abnormalities.
10. Patients with a history of abnormal heartbeat or liver disease should consult their doctor before using the drug. Overdosing can cause serious heart problems or death.

Loperamide contraindications

1. Hypersensitivity, bloody diarrhea, high fever, infectious diarrhea, pseudomembranous colitis
2. Less than 2 years
3. Patients in whom constipation should be avoided.
4. Abdominal pain without diarrhea
5. Avoid use as primary treatment for acute bloody diarrhea (bloody stools and high fever, acute ulcerative colitis, bacterial enterocolitis caused by Salmonella, Shigella, and Campylobacter), pseudomembranous colitis associated with antibiotic use.

Loperamide side effects

Dizziness, drowsiness, pain, fatigue or constipation are some of the side effects of Loperamide. If any of these effects persist or worsen, tell your doctor right away. Most people who use this drug do not experience serious side effects. If you have any very serious side effects, including constipation, severe nausea or vomiting, stomach and abdominal pain, skin rashes, itching and swelling (especially in the face, tongue and throat), severe dizziness, breathing problems, etc., stop taking the medicine. And see a doctor.

1. dizziness
2. tiredness
3. stomach ache
4. constipation
5. nausea
6. dry mouth
7. angioedema
8. Blistering eruptions
9. Flatulence
10. urticaria

Loperamide drug interactions

1. Category X interactions (avoid): lasmiditan
2. Reduction of loperamide effects by drugs: lomacaftor and ivacaftor, P-gp/ABCB1 inducers
3. Increased effects of drugs by loperamide: desmopressin, eloxadoline, haloperidol, drugs that prolong the QT interval (highest risk), quinidine, ramosterone
4. Increasing the effects of loperamide by drugs: ardafetinib, lasmiditan, lomacaftor and ivacaftor, quinidine, ranolazine.

Taking Loperamide during pregnancy and breastfeeding

Loperamide is in group B in terms of risk during pregnancy. This means that animal studies have shown that this drug is not dangerous to the fetus, but there have not been enough human studies in pregnant women. However, loperamide is generally considered safe to take during pregnancy. This drug is widely used to treat diarrhea in pregnant women. If you are pregnant or breastfeeding, consult your doctor regarding the risks of use to the baby or fetus.

Loperamide storage conditions

Loperamide should be stored at room temperature and away from light and moisture. Also, all chemical and herbal medicines should be kept out of the reach of children and animals.

The last word about Loperamide

As we said in this article from Positive Green Pharmacy magazine, loperamide is an important option in the treatment of diarrhea and can help improve the symptoms of diarrhea and reduce its frequent and uncontrolled discharges. This medicine is of great importance and people with sufficient information and under the supervision of a doctor can use this medicine to improve their health and reduce discomfort caused by diarrhea. In this article, we examined diarrhea as a common problem in the digestive system and examined the role of loperamide in the treatment of this condition.

Site source: Medscape