Selective Cox-2 Inhibitor
... Celecoxib (the first Coxib developed) and rofecoxib have been licensed by the FDA for the management of inflammatory chronic pain of osteoarthritis, rheumatoid arthritis, and acute pain of primary dysmenorrhea. A number of trials of high quality have been performed in adults for the treatment of mod ...
... Celecoxib (the first Coxib developed) and rofecoxib have been licensed by the FDA for the management of inflammatory chronic pain of osteoarthritis, rheumatoid arthritis, and acute pain of primary dysmenorrhea. A number of trials of high quality have been performed in adults for the treatment of mod ...
IOSR Journal of Dental and Medical Sciences (IOSR-JDMS)
... obstacles to the achievement of optimal glycemic control in type 2 diabetes mellitus (T2DM).Current treatment for type 2 diabetes does not achieve good glycemic change.Existing treatments have dose limiting safety or tolerability issues such as hypoglycaemia (sulphonylureas), oedema (glitazones), we ...
... obstacles to the achievement of optimal glycemic control in type 2 diabetes mellitus (T2DM).Current treatment for type 2 diabetes does not achieve good glycemic change.Existing treatments have dose limiting safety or tolerability issues such as hypoglycaemia (sulphonylureas), oedema (glitazones), we ...
Guidance for Industry
... advances in nuclear magnetic resonance (NMR) spectroscopy, mass spectroscopy (MS), and synthetic methods have enabled investigators to create compounds with altered pharmacological profiles compared with naturally occurring peptides. These modified peptides may have increased receptor binding affini ...
... advances in nuclear magnetic resonance (NMR) spectroscopy, mass spectroscopy (MS), and synthetic methods have enabled investigators to create compounds with altered pharmacological profiles compared with naturally occurring peptides. These modified peptides may have increased receptor binding affini ...
Interactive Properties of Tizanidine (Zanaflex)
... healthy subjects, pretreatment with fluvoxamine (100 mg/day for 4 days) resulted in a dramatic 33-fold increase in tizanidine area under the plasma concentration–time curve (AUC).1 The marked increases in tizanidine plasma concentrations were accompanied by pharmacodynamic changes, such as marked re ...
... healthy subjects, pretreatment with fluvoxamine (100 mg/day for 4 days) resulted in a dramatic 33-fold increase in tizanidine area under the plasma concentration–time curve (AUC).1 The marked increases in tizanidine plasma concentrations were accompanied by pharmacodynamic changes, such as marked re ...
Algorithms for Diagnosis of Disorders in Hemostasis
... treated with O.A.T. drug diagnosis of deficiency is difficult. If possible, discontinue therapy briefly (heparin can be substituted) and re - test. ...
... treated with O.A.T. drug diagnosis of deficiency is difficult. If possible, discontinue therapy briefly (heparin can be substituted) and re - test. ...
Allosteric Binding Sites on Muscarinic Acetylcholine Receptors
... Maintenance of the physiological pattern of receptor activity Potential for the development of ligands with increased receptor subtype selectivity ...
... Maintenance of the physiological pattern of receptor activity Potential for the development of ligands with increased receptor subtype selectivity ...
Effects of Enoyl-Acyl Protein Carrier Reductase Mutations on
... and action site of INH is inhA gene product, namely enoyl-acyl carrier protein reductase (InhA), is catalyzing the synthesis of the fatty acids [13-19]. Different mechanisms of INH activation have been reviewed by Scior et al. [20]. More studies have also demonstrated that the mutations within katG ...
... and action site of INH is inhA gene product, namely enoyl-acyl carrier protein reductase (InhA), is catalyzing the synthesis of the fatty acids [13-19]. Different mechanisms of INH activation have been reviewed by Scior et al. [20]. More studies have also demonstrated that the mutations within katG ...
Provisional PDF - Thrombosis Journal
... between treatment groups across renal function categories (pinteraction = 0.72). Major bleeding in rivaroxaban recipients occurred in 0.8%, 1.4%, 0.9%, and 0%, respectively (ptrend = 0.50). Respective rates in enoxaparin/VKA recipients were 1.0%, 3.0%, 3.9%, and 9.1% (ptrend < 0.001). Rivaroxaban–en ...
... between treatment groups across renal function categories (pinteraction = 0.72). Major bleeding in rivaroxaban recipients occurred in 0.8%, 1.4%, 0.9%, and 0%, respectively (ptrend = 0.50). Respective rates in enoxaparin/VKA recipients were 1.0%, 3.0%, 3.9%, and 9.1% (ptrend < 0.001). Rivaroxaban–en ...
Structure- Activity Relationships (SAR)
... cardiovascular diseases, and mental diseases need new agents and approaches for treating and preventing these illnesses. • Most drugs act at a specific site such as an enzyme or receptor. Compounds with similar structures often tend to have similar pharmacological activity. However, they usually exh ...
... cardiovascular diseases, and mental diseases need new agents and approaches for treating and preventing these illnesses. • Most drugs act at a specific site such as an enzyme or receptor. Compounds with similar structures often tend to have similar pharmacological activity. However, they usually exh ...
Fragment-Based Discovery of the Pyrazol-4
... the series already possessed three hydrogen bond donors, a weakly basic morpholine group (pKa ≈ 7) was chosen in order minimize the increase in effective hydrogen bond donors. This initial strategy, as exemplified by 8 and 9, was successful in increasing cellular potency (Table 1). The increase in c ...
... the series already possessed three hydrogen bond donors, a weakly basic morpholine group (pKa ≈ 7) was chosen in order minimize the increase in effective hydrogen bond donors. This initial strategy, as exemplified by 8 and 9, was successful in increasing cellular potency (Table 1). The increase in c ...
Theranostics Polysaccharide Nanosystems for Future Progress in
... case of β-(1-3)-glucan. Its recognition and the subsequent receptor binding process via β-(1-3)-glucan binding proteins is the first step in mediating the activating effects.[20] The activation of signal transduction pathways enhance the antimicrobial activity of mononuclear cells and neutrophils wh ...
... case of β-(1-3)-glucan. Its recognition and the subsequent receptor binding process via β-(1-3)-glucan binding proteins is the first step in mediating the activating effects.[20] The activation of signal transduction pathways enhance the antimicrobial activity of mononuclear cells and neutrophils wh ...
Document
... omeprazole and not to all PPIs. Not all PPIs have the same inhibitory effect on the enzyme (CYP 2C19) that is crucial for conversion of Plavix into its active form. Pantoprazole (Protonix) may be an alternative PPI for consideration. It is a weak inhibitor of CYP2C19 and has less effect on the phar ...
... omeprazole and not to all PPIs. Not all PPIs have the same inhibitory effect on the enzyme (CYP 2C19) that is crucial for conversion of Plavix into its active form. Pantoprazole (Protonix) may be an alternative PPI for consideration. It is a weak inhibitor of CYP2C19 and has less effect on the phar ...
An Introduction to Medicinal Chemistry
... This text is aimed at undergraduates who have a basic grounding in chemistry and are interested in a future career in the pharmaceutical industry. It attempts to convey something of the fascination of working in a field which overlaps the disciplines of chemistry, biochemistry, cell biology, and pha ...
... This text is aimed at undergraduates who have a basic grounding in chemistry and are interested in a future career in the pharmaceutical industry. It attempts to convey something of the fascination of working in a field which overlaps the disciplines of chemistry, biochemistry, cell biology, and pha ...
Interactions between Grapefruit Juice and Calcium Channel
... juice can elevate the bioavailability of drugs and alter pharmacokinetic parameters of the drug. A calcium channel antagonist with lower bioavailability is likely to be more affected by grapefruit juice. The area under the concentration-time curve and peak serum concentrations of azelnidipine, efoni ...
... juice can elevate the bioavailability of drugs and alter pharmacokinetic parameters of the drug. A calcium channel antagonist with lower bioavailability is likely to be more affected by grapefruit juice. The area under the concentration-time curve and peak serum concentrations of azelnidipine, efoni ...
High performance liquid chromatography, TLC
... degradation and separation of the degradates with their identification with IR and Mass spectra were done. The International Conference of Harmonization (ICH) guideline entitiled” stability testing of new drug substances and products” requires the stress testing to be carried out to elucidate the in ...
... degradation and separation of the degradates with their identification with IR and Mass spectra were done. The International Conference of Harmonization (ICH) guideline entitiled” stability testing of new drug substances and products” requires the stress testing to be carried out to elucidate the in ...
Allosteric Modulation: a Novel Approach to Drug Discovery
... Mark P Epping-Jordan is Chief Scientific Officer and co-founder of Addex Pharmaceuticals. Prior to co-founding Addex, he was a scientist in the GlaxoSmithKline Experimental Pathology Group in Lausanne, Switzerland, where he worked with the GSK Psychiatry Center for Excellence in Drug Discovery on no ...
... Mark P Epping-Jordan is Chief Scientific Officer and co-founder of Addex Pharmaceuticals. Prior to co-founding Addex, he was a scientist in the GlaxoSmithKline Experimental Pathology Group in Lausanne, Switzerland, where he worked with the GSK Psychiatry Center for Excellence in Drug Discovery on no ...
Full Prescribing Information
... Methylergonovine maleate acts directly on the smooth muscle of the uterus and increases the tone, rate, and amplitude of rhythmic contractions. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss. The onset of action after i ...
... Methylergonovine maleate acts directly on the smooth muscle of the uterus and increases the tone, rate, and amplitude of rhythmic contractions. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss. The onset of action after i ...
Low Molecular Weight Heparins : Basic and Applied Considerations
... Currently, several newer agents are being investigated as possible substitutes for heparin. These new agents include antithrombin, anti-Xa, anti-TF, heparinoids, oral formulations of heparin, glycosaminoglycans mixtures, activated protein C and biotechnology derived SERPINS such as the recombinant A ...
... Currently, several newer agents are being investigated as possible substitutes for heparin. These new agents include antithrombin, anti-Xa, anti-TF, heparinoids, oral formulations of heparin, glycosaminoglycans mixtures, activated protein C and biotechnology derived SERPINS such as the recombinant A ...
Running head: PERSONAL DRUGS PERSONAL DRUGS Personal
... Pneumonia is a lower respiratory tract infection that involves aspiration of secretions or inhalation of microorganisms released from other infected individuals, which then activates the immune response causing vascular edema and alveolar filling, impairing gas exchange (Brashers, 2010). Different m ...
... Pneumonia is a lower respiratory tract infection that involves aspiration of secretions or inhalation of microorganisms released from other infected individuals, which then activates the immune response causing vascular edema and alveolar filling, impairing gas exchange (Brashers, 2010). Different m ...
Bioisosterism: A Rational Approach in Drug Design
... physicochemical properties. In this review an attempt has been made to quantitate, in specific instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and to correlate these values to the observed biological activity. Thus, an additional objective of this review ...
... physicochemical properties. In this review an attempt has been made to quantitate, in specific instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and to correlate these values to the observed biological activity. Thus, an additional objective of this review ...
Stroke Prevention in Atrial Fibrillation
... the three following conditions, the recommended dose is 2.5 mg twice a day: age ≥ 80 years, weight ≤ 60 kg, serum creatinine ≥ 1.5 mg/dL. The major clinical trial leading to approval of apixaban was the ARISTOTLE trial [19]. The trial randomized approximately 18,000 to apixiban or warfarin and was d ...
... the three following conditions, the recommended dose is 2.5 mg twice a day: age ≥ 80 years, weight ≤ 60 kg, serum creatinine ≥ 1.5 mg/dL. The major clinical trial leading to approval of apixaban was the ARISTOTLE trial [19]. The trial randomized approximately 18,000 to apixiban or warfarin and was d ...
PDF - Journal of Nanobiotechnology
... improve the oral bioavailability of BCS II drugs [28]. Previous in vitro and in vivo evaluations of the reference, Lipanthyl® capsules, which are a product of micronized FNB and nanosuspensions of FNB suggested the FNB is rapidly released from Lipanthyl® capsules, SDPs and nanosuspensions, and that ...
... improve the oral bioavailability of BCS II drugs [28]. Previous in vitro and in vivo evaluations of the reference, Lipanthyl® capsules, which are a product of micronized FNB and nanosuspensions of FNB suggested the FNB is rapidly released from Lipanthyl® capsules, SDPs and nanosuspensions, and that ...
6- Diuretics
... 1- -SO2NH2 group hypersensitivity 2- Ototoxicity So care must be noticed when used with aminoglycosides. 3-NSAIDs may blunt the natriuresis produced by loop diuretics in patients with preexisting impaired renal function who are on diuretic therapy NSAIDs may increase the risk of renal ...
... 1- -SO2NH2 group hypersensitivity 2- Ototoxicity So care must be noticed when used with aminoglycosides. 3-NSAIDs may blunt the natriuresis produced by loop diuretics in patients with preexisting impaired renal function who are on diuretic therapy NSAIDs may increase the risk of renal ...
Structure-Based Identification of Binding Sites, Native Ligands and
... attempts have been made to solve their structure by molecular modeling.6 –11 However, to date, bovine rhodopsin (bRho) is the only GPCR to be solved to a high resolution by X-ray crystallography.12 Electron diffraction and electron microscopy (EM) studies have succeeded in determining the structure ...
... attempts have been made to solve their structure by molecular modeling.6 –11 However, to date, bovine rhodopsin (bRho) is the only GPCR to be solved to a high resolution by X-ray crystallography.12 Electron diffraction and electron microscopy (EM) studies have succeeded in determining the structure ...
(12)Indian Patent Application ______________________________________________________________
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...