scholarly journals Overview of Newer Glucocorticosteroid Preparations for Inflammatory Bowel Disease

1990 ◽  
Vol 4 (7) ◽  
pp. 407-414 ◽  
Author(s):  
R Brattsand
Keyword(s):  
Inflammatory Bowel Disease ◽  
Bowel Disease ◽  
Topical Therapy ◽  
Hepatic Metabolism ◽  
Systemic Circulation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Inflammatory Bowel ◽  
Bowel Mucosa ◽  
Pass Metabolism

Because the glucocorticosteroid receptor seems to be uniform in the human body, there is currently no support for a possibility of separating the therapeutic and adverse glucocorticosteroid actions at the receptor level. However, based on a new generation of glucocorticosteroids characterized by a high first pass metabolism in the liver, it seems possible today co reach a more selective topical therapy of inflammatory bowel disease. The properties of three new glucocorticosteroids are presented: the highly potent budesonide, fluticasone propionate and tixocortol pivalate - the latter with only low topical potency. Their properties can be exemplified by budesonide, which is currently the best documented compound. The topical potency of budesonide is 200 and 15 times higher than chose of hydrocortisone and prednisolone, respectively. This means that there is a high potential for anti-inflammatory and immunosuppressive actions on rectal and bowel mucosa. The compound is metabolically stable in the bowel compartment, which allows full retention of glucocorticosteroid activity in the target organ. However, when absorbed and distributed to the liver, there is a 90% first pass hepatic metabolism co metabolites of very low potency. This suggests that after topical application to rectal or bowel mucosa, glucocorticosteroid activity in the systemic circulation is low. This is in contrast to prednisolone, which has a hepatic first pass metabolism of just 20%.

scholarly journals A comprehensive review on buccal patches

2020 ◽  
Vol 13 (1) ◽  
pp. 130-135
Author(s):  
Seema ◽  
Kapil kumar ◽  
Deepak Teotia
Keyword(s):  
Drug Delivery ◽  
Oral Cavity ◽  
Systemic Circulation ◽  
Drug Formulation ◽  
Delivery Method ◽  
Modern Approach ◽  
Comprehensive Review ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Buccal Patches are the type of drug formulation that has normally a different course of administration through the buccal mucosa for drug delivery. The product is placed between upper gingiva (gums) and cheek to treat local and systemic conditions. Buccal patch have good accessibility to the membranes that line the oral cavity. These patches tend to help drug enter directly into the systemic circulation escaping hepatic first pass metabolism. This type of drug delivery method is considered useful for elevating the bioavailability of drugs. This review is a thorough study to apprehend the procedures involved in assessment of buccal patches and the modern approach towards this type of drug delivery. This article intends to analyze the overall profile of Buccal Patches and scope of future advances.

scholarly journals Development and evaluation of buccal patches of theophylline

2021 ◽  
Vol 16 (3) ◽  
pp. 235-240
Author(s):  
Kapil Kumar ◽  
Gurleen Kaur ◽  
Seema ◽  
Deepak Teotia ◽  
Ikram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Buccal Mucosa ◽  
Systemic Circulation ◽  
Pharmacological Response ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Buccal patches are the types of formulations in which the drug is administered through buccal mucosa. these patches are or placed in between the gums and the for the pharmacological response. The main advantage of these patches is there is no first pass metabolism takes place and easily absorb in systemic circulation through themucosa .the main objective of this drug delivery system is to elevate or increase the bioavailability of the drug. the review informs about the steps involve in the preparation of buccal patch and to promote the awareness towards this type of drug delivery system. This article intends to analyze the overall profile of Buccal Patches and scope of future advances.

scholarly journals Predicting Intestinal and Hepatic First-Pass Metabolism of Orally Administered Testosterone Undecanoate

2020 ◽  
Vol 10 (20) ◽  
pp. 7283 ◽  
Author(s):  
Atheer Zgair ◽  
Yousaf Dawood ◽  
Suhaib M. Ibrahem ◽  
Hyun-moon Back ◽  
Leonid Kagan ◽  
...  
Keyword(s):  
Liver Microsomes ◽  
Hepatic Metabolism ◽  
Hydrolysis Time ◽  
Testosterone Undecanoate ◽  
Main Site ◽  
Cell Homogenate ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

The bioavailability of orally administered drugs could be impacted by intestinal and hepatic first-pass metabolism. Testosterone undecanoate (TU), an orally administered ester prodrug of testosterone, is significantly subjected to first-pass metabolism. However, the individual contribution of intestinal and hepatic first-pass metabolism is not well determined. Therefore, the aim of the current study was to predict the metabolic contribution of each site. The hydrolysis–time profiles of TU incubation in human liver microsomes and Caco-2 cell homogenate were used to predict hepatic and intestinal first-pass metabolism, respectively. The in vitro half-life (t1/2 inv) for the hydrolysis of TU in microsomal mixtures was 28.31 ± 3.51 min. By applying the “well-stirred” model, the fraction of TU that could escape hepatic first-pass metabolism (FH) was predicted as 0.915 ± 0.009. The incubation of TU in Caco-2 cell homogenate yielded t1/2 inv of 109.28 ± 21.42 min, which was applied in a “Q gut” model to estimate the fraction of TU that would escape intestinal first-pass metabolism (FG) as 0.114 ± 0.02. Accordingly, only 11% of the absorbed fraction of TU could escape intestinal metabolism, while 91% can pass through hepatic metabolism. Hence, compared to the liver, the intestinal wall is the main site where TU is significantly metabolised during first-pass effect.

scholarly journals PHARMACOLOGY OF NOVAL CANNABINOIDS

2019 ◽  
pp. 1-5
Author(s):  
SUMITHA S. K. ◽  
VEENA S. PATTAMMADY ◽  
R. SAMBATHKUMAR
Keyword(s):  
Cannabis Sativa ◽  
Synthetic Cannabinoids ◽  
Systemic Circulation ◽  
Scientific Investigation ◽  
Direct Relation ◽  
Preclinical Research ◽  
First Pass Metabolism ◽  
First Pass ◽  
Psychoactive Effects ◽  
Pass Metabolism

Cannabis is a plant rich in various compounds that have a variety of impacts on the physiology of humans and the effects of these metabolites have a significant role in managing a variety of clinical diseases. A substantial increase in the use of SC (synthetic cannabinoids) had seen in the last few years especially infrequent cannabis users. The SCs will generate psychoactive effects that were similar to cannabis. However, the composition and pharmacological characteristics of these drugs make them possibly hazardous. Like all drugs, cannabis’ pharmacokinetics depends on the route of administration. Several studies showed that the bioavailability is less in oral administration when compared to inhalation. The main reason for this decrease in oral bioavailability is that cannabinoids undergo the first-pass metabolism before entering into the systemic circulation whereas in inhalation, it enters the circulation directly through the lungs. Cannabis sativa is a psychoactive plant that contains more than 500 components of which 104 cannabinoids had been identified. Of these, 2 components such as Δ9-THC (Δ9-tetrahydrocannabinol) and CBD (cannabidol) were under the scientific investigation. Δ9-THC is the primary cannabinoid which was responsible for the consequences of psychotrophy. The potency of cannabis is assessed based on the THC concentration of a sample that is the main psychoactive cannabinoid in cannabis. The adverse effects are in direct relation to the concentration of THC in the product after regular cannabis use. It can be assumed that several cannabinoids will find their way into the pharmacies from preclinical research within a century.

scholarly journals Budesonide Enemas for Topical Therapy of Ulcerative Colitis

1990 ◽  
Vol 4 (7) ◽  
pp. 415-416 ◽  
Author(s):  
P Rutgeerts
Keyword(s):  
Ulcerative Colitis ◽  
Topical Therapy ◽  
High Ratio ◽  
Systemic Activity ◽  
First Pass Metabolism ◽  
First Pass ◽  
Hypothalamic Pituitary Axis ◽  
Pass Metabolism

Budesonide is a nonhalogenated glucocorticosteroid that is very suitable for topical therapy in left-sided colitis because it has a high ratio of topical to systemic activity. Although it is absorbed, it is very rapidly metabolized by the liver (first pass metabolism). It does not suppress the hypothalamic-pituitary axis. Budesonide has been shown to be more effective than placebo and predinsolone enemas for the treatment of left-sided ulcerative colitis.

scholarly journals Right and Left-sided Valve Disease: A Case of Subclinical Intrapulmonary Shunt in an Adult with Malignant Carcinoid

2021 ◽  
Vol 1 (1) ◽  
Author(s):  
Ross M Hansen ◽  
Gregory D Chapman
Keyword(s):  
Systemic Circulation ◽  
Valve Disease ◽  
Intrapulmonary Shunt ◽  
Transesophageal Echocardiogram ◽  
Malignant Carcinoid ◽  
Vasoactive Hormones ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Right ◽  
Pass Metabolism

Carcinoid tumors are highly differentiated neuroendocrine tumors (NET) that most commonly originate from the gastrointestinal tract. Liver metastases bypass first-pass metabolism and liberate vasoactive hormones into systemic circulation, causing flushing and diarrhea. Prolonged levels of circulating serotonin may adversely affect the heart by creating fibrotic endocardial deposits on native valves. The remaining serotonin is metabolized in the pulmonary circuit that leads to pathognomonic valvular disease isolated to the right side of the heart. We present a case of an adult male with known carcinoid syndrome who presented with involvement of right, as well as left-sided valves. He was found to have an intrapulmonary shunt on transesophageal echocardiogram (TEE) with bubble study. Intrapulmonary shunt should be considered, in conjunction with right-to-left shunt, lung involvement, and high levels of serotonin, for carcinoid patients with right and left-sided valve disease.

scholarly journals Dose-Dependent Pharmacokinetics of Tofacitinib in Rats: Influence of Hepatic and Intestinal First-Pass Metabolism

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 318 ◽  
Author(s):  
Ji Sang Lee ◽  
So Hee Kim
Keyword(s):  
Oral Administration ◽  
Intravenous Administration ◽  
Hepatic Metabolism ◽  
Time Curve ◽  
First Pass Effect ◽  
First Pass Metabolism ◽  
First Pass ◽  
Dose Dependent ◽  
Intraduodenal Administration ◽  
Pass Metabolism

This study investigated the pharmacokinetics of tofacitinib in rats and the effects of first-pass metabolism on tofacitinib pharmacokinetics. Intravenous administration of 5, 10, 20, and 50 mg/kg tofacitinib showed that the dose-normalized area under the plasma concentration-time curve from time zero to infinity (AUC) was significantly higher at 50 mg/kg than at lower doses, a difference possibly due to saturation of the hepatic metabolism of tofacitinib. Oral administration of 10, 20, 50, and 100 mg/kg tofacitinib showed that the dose-normalized AUC was significantly higher at 100 mg/kg than at lower doses, a difference possibly due to saturation of the intestinal metabolism of tofacitinib. Following oral administration of 10 mg/kg tofacitinib, the unabsorbed fraction from the rat intestine was 3.16% and the bioavailability (F) was 29.1%. The AUC was significantly lower (49.3%) after intraduodenal, compared to intraportal, administration, but did not differ between intragastric and intraduodenal administration, suggesting that approximately 46.1% of orally administered tofacitinib was metabolized through an intestinal first-pass effect. The AUC was also significantly lower (42%) after intraportal, compared to intravenous, administration, suggesting that the hepatic first-pass effect on tofacitinib after entering the portal vein was approximately 21.3% of the oral dose. Taken together, these findings suggest that the low F of tofacitinib is due primarily to intestinal first-pass metabolism.

scholarly journals ABC of topical therapy in inflammatory bowel disease

JGH Open ◽  
2020 ◽  
Vol 4 (4) ◽  
pp. 556-557
Author(s):  
Thomas M Goodsall ◽  
Samuel P Costello ◽  
Robert V Bryant
Keyword(s):  
Inflammatory Bowel Disease ◽  
Bowel Disease ◽  
Topical Therapy ◽  
Inflammatory Bowel
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