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Lopra Actions |
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Synthetic antidiarrheal.
Pharmacology: Pharmacodynamics: Lopra binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing propulsive peristalsis and increasing intestinal transit time.
Lopra increases the tone of the anal sphincter, thereby reducing incontinence and urgency.
Due to its high affinity to the gut wall and its high first-pass metabolism, Lopra hardly reaches the systemic circulation.
Pharmacokinetics: Lopra is easily absorbed from the gut, but it is almost completely extracted by the liver, where it is metabolized, conjugated and excreted via the bile.
The half-life of Lopra in man is about 11 hrs with a range of 9-14 hrs. Studies on distribution in rats show a high affinity for the gut wall with a preference for binding to receptors of the longitudinal muscle layer. Elimination mainly occurs by oxidative N-demethylation, which is the main metabolic pathway of Lopra. Excretion of the unchanged Lopra and the metabolites mainly occurs through the feces.
Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.
Take Lopra with a full glass of water. Drink extra water while you are taking this medication to keep from getting dehydrated.
Lopra is usually taken at the first sign of diarrhea, and again if diarrhea comes back. The first dose of Lopra is usually twice as much as the following doses. Do not take this medication more than 3 times in 24 hours without your doctor's advice.
The Lopra chewable tablet must be chewed before swallowing.
Shake the oral suspension (liquid) well just before you measure a dose. Measure the liquid with a special dose measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose measuring device, ask your pharmacist for one.
Immodium A-D Liquid and New Immodium A-D Liquid contain two different strengths of Lopra. If you switch from using one brand to using the other, follow the dosing instructions carefully. Immodium A-D Liquid also contains a small amount of alcohol, but New Immodium A-D Liquid does not.
It may take up to 48 hours before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve after 10 days of treatment.
Store at room temperature away from moisture and heat. Do not freeze liquid Lopra.
Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.
Take Lopra with a full glass of water. Drink extra water while you are taking this medication to keep from getting dehydrated.
Lopra is usually taken at the first sign of diarrhea, and again if diarrhea comes back. The first dose of Lopra is usually twice as much as the following doses. Do not take this medication more than 3 times in 24 hours without your doctor's advice.
The Lopra chewable tablet must be chewed before swallowing.
Shake the oral suspension (liquid) well just before you measure a dose. Measure the liquid with a special dose measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose measuring device, ask your pharmacist for one.
Immodium A-D Liquid and New Immodium A-D Liquid contain two different strengths of Lopra. If you switch from using one brand to using the other, follow the dosing instructions carefully. Immodium A-D Liquid also contains a small amount of alcohol, but New Immodium A-D Liquid does not.
It may take up to 48 hours before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve after 10 days of treatment.
Store at room temperature away from moisture and heat. Do not freeze liquid Lopra.
In vitro and animal studies show that Lopra® (Lopra hydrochloride) acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Lopra binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing peristalsis, and increasing intestinal transit time. Lopra increases the tone of the anal sphincter, thereby reducing incontinence and urgency.
In man, Lopra® (Lopra hcl) prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Clinical studies have indicated that the apparent elimination half-life of Lopra in man is 10.8 hours with a range of 9.1 - 14.4 hours. Plasma levels of unchanged drug remain below 2 nanograms per mL after the intake of a 2mg capsule of Lopra® (Lopra hcl). Plasma levels are highest approximately five hours after administration of the capsule and 2.5 hours after the liquid. The peak plasma levels of Lopra were similar for both formulations. Elimination of Lopra mainly occurs by oxidative N-demethylation. Cytochrome P450 (CYP450) isozymes, CYP2C8 and CYP3A4, are thought to play an important role in Lopra N-demethylation process since quercetin (CYP2C8 inhibitor) and ketoconazole (CYP3A4 inhibitor) significantly inhibited the N- demethylation process in vitro by 40% and 90%, respectively. In addition, CYP2B6 and CYP2D6 appear to play a minor role in Lopra N-demethylation. Excretion of the unchanged Lopra and its metabolites mainly occurs through the feces. In those patients in whom biochemical and hematological parameters were monitored during clinical trials, no trends toward abnormality during Lopra® (Lopra hcl) therapy were noted. Similarly, urinalyses, EKG and clinical ophthalmological examinations did not show trends toward abnormality.
Users | % | ||
---|---|---|---|
After food | 4 | 66.7% | |
Before food | 1 | 16.7% | |
Empty stomach | 1 | 16.7% |
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Information checked by Dr. Sachin Kumar, MD Pharmacology
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