High Quality Western Medicine Loperamide Hydrochloride Capsules 2mg GMP.

• Application: Internal Medicine
• Usage Mode: For oral administration
• Suitable for: Elderly, Children, Adult
• State: Solid
• Shape: Capsules
• Type: Organic Chemicals
• Model NO.: NO.
• Pharmaceutical Technology: Chemical Synthesis
• Drug Reg./Approval No.: Available
• Drug Ad Approval No.: Available
• Term of Validity: 60 Months
• Transport Package: Box/Carton
• Specification: 2mg
• Trademark: OEM
• Origin: China
• HS Code: 3004909099
• Production Capacity: 100000 Boxes/Day

Product Description

Product information:

Product name	Loperamide hydrochloride capsules
Term of validity	60 months
Storage	Seal and store in a dry place

Indication:
Antidiarrheal drugs are used to control the symptoms of acute and chronic diarrhea.
It can reduce the amount and frequency of defecation and increase the consistency and hardness of stool.

Taboo:
It is forbidden to be used for those who are known to be allergic to this product.
This product should not be used as the main treatment for the following diseases:
·The main symptoms were acute bacillary dysentery with high fever and purulent stool
·Acute ulcerative colitis
·Bacterial enterocolitis caused by invasive pathogens such as Salmonella, shigella or Campylobacter
·Pseudomembranous enteritis caused by broad-spectrum antibiotics
In general, this product should not be used when intestinal obstruction, megacolon and toxic megacolon may occur due to inhibition of intestinal peristalsis. In case of constipation, abdominal distension and intestinal obstruction, it should be stopped immediately.
When used for diarrhea, it is only symptomatic treatment. After the etiology has been determined, specific treatment should be given.

Matters needing attention:
Diarrhea patients, especially children, often suffer from water and electrolyte loss. Replenishing water and electrolytes is the most important treatment.
For acute diarrhea, if taking this product for 48 hours, the clinical symptoms do not improve. This product should be discontinued and recommended by your doctor.
AIDS patients with diarrhea, such as the early symptoms of abdominal distension. Treatment with this product should be discontinued. It has been reported that a few AIDS patients used loperamide hydrochloride in the treatment of infectious colitis caused by virus and bacteria.
Although there is no pharmacokinetic data of this drug in patients with liver dysfunction, liver dysfunction may lead to drug overdose due to its high first pass metabolic characteristics. Therefore, we should pay attention to the symptoms of central nervous system toxicity.
Since most of the product can be metabolized, the metabolites and prototype drugs can be excreted through feces, so there is no need for dose adjustment in patients with nephropathy.
When treating diarrhea, it may appear fatigue, dizziness or drowsiness. Therefore, attention should be paid when driving and operating the machine.
Please keep it out of reach of children.

Drug interactions:
The combination of loperamide (single dose of 4mg) and itraconazole {CYP3A4 and P-glycoprotein inhibitor) can increase the plasma concentration of loperamide by 3-4 times. In the same experiment, gemfibrozil, a cyp2c8 inhibitor, increased the plasma concentration of loperamide by about 2 times. In combination with itraconazole and gemfibrozil, the plasma peak value of loperamide was increased by 4 times and the total plasma exposure was increased by 13 times. By means of consciousness activity tests, such as subjective sleepiness and digit symbol substitution test, it is considered that these increases do not lead to central nervous system response.
The combination of loperamide (single dose of 16 mg) and ketoconazole (CYP3A4 and P-glycoprotein inhibitor) increased the plasma concentration of loperamide by 5 times. The results showed that these increases did not lead to an increase in pharmacokinetics.
The combination of loperamide and oral resulted in a 3-fold increase in plasma concentration  which may be caused by slow gastrointestinal peristalsis.
The effect of loperamide may be increased by the combination of drugs similar to that of loperamide, and may be reduced by combination with drugs that increase gastrointestinal peristalsis.

Pharmacokinetics:
Absorption: most of loperamine was absorbed by intestinal wall, but the bioavailability of loperamine was only 0.3% due to the obvious first pass effect. The absorption rate and degree of loperamine hydrochloride (hard umbilicus sac, soft capsule, coated tablet, chewing tablet, mouth disintegration tablet, oral liquid) with or without coating are bioequivalent.
Distribution: the distribution of the study showed that the distribution of the rats had high affinity with the intestinal wall, and was easy to bind to the receptor in the longitudinal muscle layer. The binding rate of loperamine to plasma protein (mainly albumin) was 95%. The pre clinical data showed that loperamine was a P-glycoprotein substrate.
Metabolism: loperamine is almost all ingested by the liver, and is metabolized, combined and excreted by bile. The main metabolic pathway of loperamine is through the oxidation of N-demethylation, and is regulated by CYP3A4 and cyp2c8. Due to the very strong first pass effect, the plasma concentration of drug prototypes is very low.
Excretion: the elimination half-life of loperamine in human body is 11 (9-14) hours. The drug prototype and metabolites are excreted mainly through feces.
Pediatric population: pharmacokinetic studies were not conducted in pediatric population, and it is expected that children and adults have similar pharmacokinetic characteristics and similar drug interaction characteristics.