Product Overview
[Drug Name]
Trade Name: Imodium
English Name: Loperamide Hydrochloride Capsules
Chinese Pinyin: Yansuan Lvbenpaixuanan
[Ingredients]
The main ingredient is loperamide hydrochloride.
[Properties]
This product consists of green or gray capsules containing white powder.
[Indications]
Antidiarrheal drug used for acute and chronic diarrhea of various causes. It can reduce stool volume and frequency and increase stool consistency in patients undergoing ileostomy.
[Dosage and Administration]
This product is suitable for adults and children over 5 years of age.
Acute diarrhea: Starting dose: 2 capsules for adults. 1 capsule for children over 5 years of age. Subsequently, take 1 capsule after each unformed stool.
Chronic diarrhea: Starting dose: 2 capsules for adults. 1 capsule for children over 5 years of age. The daily dose can be adjusted to maintain 1-2 normal bowel movements daily. The typical maintenance dose is 1-6 capsules per day.
Maximum daily dose: No more than 8 capsules for adults and 3 capsules for children per 20 kg of body weight.
[Adverse Reactions]
Adverse reactions are mild and may include allergic reactions such as rash, gastrointestinal symptoms such as dry mouth, abdominal distension, loss of appetite, gastrointestinal cramps, nausea, vomiting, constipation, as well as dizziness, headache, and fatigue.
[Contraindications]
This product is contraindicated in patients with a known allergy to this product. This product should not be used as the primary treatment for the following conditions: acute bacillary dysentery with primary symptoms of high fever and bloody stools; acute ulcerative colitis; bacterial enterocolitis caused by invasive pathogens such as Salmonella, Shigella, or Campylobacter; pseudomembranous colitis caused by the use of broad-spectrum antibiotics. In general, this product should not be used in cases where intestinal obstruction, megacolon, or toxic megacolon may occur due to inhibition of intestinal motility. If constipation, abdominal distension, or intestinal obstruction occurs, this product should be discontinued immediately. This product is used for symptomatic treatment only for diarrhea. Specific treatment should be initiated after the cause is determined.
[Precautions]
For acute diarrhea, if clinical symptoms do not improve after 48 hours of taking this product, this product should be discontinued and consultation with a physician is recommended. When using this drug to treat diarrhea in patients with HIV/AIDS, if early symptoms of abdominal distension occur, treatment should be discontinued. There have been reports of toxic megacolon in individual patients with HIV/AIDS using loperamide hydrochloride for viral and bacterial infectious colitis. Although the pharmacokinetic data for this drug in patients with hepatic dysfunction are not available, due to its high first-pass metabolism, hepatic dysfunction may lead to a relative overdose, and attention should be paid to symptoms of central nervous system toxicity. Since the majority of this drug is metabolized, with metabolites and unchanged drug excreted in the feces, no dose adjustment is required in patients with renal disease. This drug may cause fatigue, dizziness, or drowsiness when used to treat diarrhea. Therefore, caution should be exercised when driving or operating machinery. Keep out of the reach of children.
[Use in Special Populations]
Precautions for Children:
Patients with diarrhea, especially children, often experience water and electrolyte depletion. Rehydration of these electrolytes is the most important treatment measure. This drug should be used in children under the guidance of a physician. Loperamide hydrochloride is contraindicated in infants and children under 2 years of age. Children under 5 years of age should not be treated with loperamide hydrochloride capsules.
Precautions During Pregnancy and Lactation:
Although this drug is not teratogenic or embryotoxic, pregnant women, especially those in the first trimester, should still consider the risks and benefits of its use. Small amounts of this drug are excreted in breast milk, so it should not be used by lactating women.
Precautions for Elderly Patients:
The use of loperamide in elderly patients is the same as for adults.
[Drug Interactions]
Coadministration of loperamide (a single 4 mg dose) with itraconazole (a CYP3A4 and P-glycoprotein inhibitor) resulted in a 3- to 4-fold increase in loperamide plasma concentrations. In similar studies, the CYP2C8 inhibitor gemfibrozil resulted in a 2-fold increase in loperamide plasma concentrations. The combination of itraconazole and gemfibrozil resulted in a 4-fold increase in peak loperamide plasma exposure and a 13-fold increase in total plasma exposure. These increases were not considered to result in central nervous system effects as assessed by cognitive activity tests, such as subjective sleepiness and the digit symbol substitution test. Coadministration of loperamide (single 16 mg dose) with ketoconazole (a CYP3A4 and P-glycoprotein inhibitor) resulted in a 5-fold increase in loperamide plasma concentrations. Pupillometry testing suggests that these increases are not associated with increased pharmacokinetics. Coadministration of loperamide with oral desmopressin resulted in a 3-fold increase in desmopressin plasma concentrations, possibly due to decreased gastrointestinal motility. Coadministration of drugs with similar pharmacological effects to loperamide may enhance its effects; coadministration with drugs that increase gastrointestinal motility may reduce its effects.
[Pharmacological Actions]
1. Pharmacology: This drug is an atropine receptor agonist. By stimulating u-opioid receptors in the intestinal wall and blocking the release of acetylcholine and prostaglandins, it antagonizes smooth muscle contraction, thereby reducing intestinal motility and secretion and prolonging intestinal retention. This drug increases anal sphincter tone, thereby inhibiting fecal incontinence and urgency. 2. Toxicology: Long-term toxicology studies of loperamide in dogs for 12 months and in rats for 18 months showed some reduction in weight gain and increased food consumption at doses of 5 mg/kg/day (30 times the maximum human dose) and 40 mg/kg/day (240 times the maximum human dose), respectively, but no other toxic effects were observed. The results indicated that the no-toxic effect level (NTEL) for dogs and rats was 1.25 mg/kg/day (8 times the maximum human dose) and 10 mg/kg/day (60 times the maximum human dose), respectively. In vitro and in vivo specific toxicology studies demonstrated that loperamide was non-genotoxic and non-carcinogenic. In reproductive toxicity studies, high-dose loperamide (40 mg/kg/day - 240 times the maximum human dose) administered to pregnant and/or lactating rats resulted in maternal toxicity, impaired fertility, and reduced fetal survival. At low doses, loperamide does not affect maternal or fetal health, nor does it affect the intrapartum and postpartum development of pups. The toxic effects observed in the preclinical toxicology studies described above were observed only at doses many times higher than the human dose and with long-term use. These effects were not observed within the clinical dosage range.
[Storage]
Sealed and stored in a dry place.
[Strength]
2 mg
[Packaging]
Aluminum-plastic blister pack; 6 tablets/box
[Expiration]
60 months
[Approval Number]
National Medicine Standard H10910085
[Manufacturer]
Company Name: Xi'an Janssen Pharmaceuticals Co., Ltd.
