Search results for: Loperamide.

Authors: Iman A. Elkiweri, Ph.D, Martha C. Tissot van Patot, Ph.D., Yan Ling Zhang, Ph.D., Uwe Christians, Ph.D., Thomas K. Henthorn, M.D.,

Abstract:

Verapamil has been shown to inhibit fentanyl uptake in vitro and is a potent P-glycoprotein inhibitor. Tissue partitioning of loperamide, a commercially available opioid, is closely controlled by the P-gp efflux transporter. The following studies were designed to evaluate the effect of opioids on verapamil partitioning in the lung and brain, in vivo. Opioid (fentanyl or loperamide) was administered by intravenous infusion to Sprague Dawley rats alone or in combination with verapamil and plasma, with lung and brain tissues were collected at 1, 5, 6, 8, 10 and 60 minutes. Drug dispositions were modeled by recirculatory pharmacokinetic models. Fentanyl slightly increased the verapamil lung (PL) partition coefficient yet decreased the brain (PB) partition coefficient. Furthermore, loperamide significantly increased PLand PB. Fentanyl reduced the verapamil volume of distribution (V1) and verapamil elimination clearance (ClE). Fentanyl decreased verapamil brain partitioning, yet increased verapamil lung partitioning. Also, loperamide increased lung and brain partitioning in vivo. These results suggest that verapamil and fentanyl may be substrates of an unidentified inward transporter in brain tissue and confirm that verapamil and loperamide are substrates of the efflux transporter P-gp.

Keywords: Efflux transporter, elimination clearance, partition coefficient, verapamil

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Authors: Fatima U. Maigari, Musa Halilu, M. Maryam Umar, Rabiu Zainab

Abstract:

Plants as therapeutic agents are used as drug in many parts of the world. Medicinal plants are mostly used in developing countries due to culture acceptability, belief or due to lack of easy access to primary health care services. Jatropha curcas is a plant from the Euphorbiaceae family which is widely used in Northern Nigeria as an anti-diarrheal agent. This study was conducted to determine the anti-diarrheal effect of the leaf extract on castor oil induced diarrhea in albino rats. The leaves of J. curcas were collected from Balanga Local government in Gombe State, north-eastern Nigeria; due to its bioavailability. The leaves were air-dried at room temperature and ground to powder. Phytochemical screening was done and different concentrations of the extract was prepared and administered to the different categories of experimental animals. From the results, aqueous leaf extract of Jatropha curcas at doses of 200mg/Kg and 400mg/Kg was found to reduce the mean stool score as compared to control rats, however, maximum reduction was achieved with the standard drug of Loperamide (5mg/Kg). Treatment of diarrhea with 200mg/Kg of the extract did not produce any significant decrease in stool fluid content but was found to be significant in those rats that were treated with 400mg/Kg of the extract at 2hours (0.05±0.02) and 4hours (0.01±0.01). A significant reduction of diarrhea in the experimental animals signifies it to possess some anti-diarrheal activity.

Keywords: Anti-diarrhea, Diarrhea, Jatropha curcas, Loperamide.

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Authors: Simon Bambang Widjanarko, Novita Wijayanti, Aji Sutrisno

Abstract:

There is long history of konjac tubers being used as a cure for certain diseases in China and Japan. Konjac flour is prepared from konjac tubers and it contains high concentration of glucomannan. Konjac Glucomannan (KGM) is dietary fiber and the role of which has been demonstrated in weight reduction, lowering blood cholesterol and sugar level, promoting intestinal activity etc. Konjac glucomanan has a property of swelling by absorbing water, more than a hundred times its own weight. Therefore it helps increasing weight of feces, water content of feces, and promotes satiety feeling. Mode of actions of dietary fibre as laxatives agents includes holding water inside the bowel lumen, inhibition of water absorption in the colon and stimulating colonic motility. Number of fecal pellets did not effected in rats were fed on 300 and 600 mg/kg of konjac flour, as well as constipated control and Dulcolax treatment. Water content, weight of fecal pellets and gastrointestinal transit ratio were higher in rats treated with 600 mg/kg than 300 mg/kg of konjac flour. Rats were administered with Dulcolax showed the highest gastrointestinal transit ratio, followed by 600 mg/kg konjac flour. The lowest feed consumption was noted in 600 mg/kg konjac flour diet group.

Keywords: Laxative, konjac flour, Amorphophallus muelleri Blume, glucomannan, constipation.

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