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Non commercial use only - Italian Journal of Medicine
Non commercial use only - Italian Journal of Medicine

... as clotting or chromogenic assays to measure anti-Factor Xa activity, have been studied. Anti-Factor Xa assays (without exogenous antithrombin) and specific PT assays can be used with rivaroxaban plasma calibrants to determine the drug level. The chromogenic tests found a dose-dependent relationship ...
DEVELOPMENT AND VALIDATION OF HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC
DEVELOPMENT AND VALIDATION OF HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC

... emergence of multi drug resistant bacteria, which are resistant to first-line anti-tuberculosis drugs, isoniazid and rifampin.1 Rifampicin or rifampin (in USA) (RIF) (Figure 1) is a semisynthetic derivative of a complex macrocyclic antibiotic called rifamycin2. It is used extensively in the treatmen ...
INTRAVASCULAR DOSING
INTRAVASCULAR DOSING

... Short term infusion  When will the concentration be below 7mg/L?  7mg/L=255 mg/L(1-e^-0.178*0.5)(e^-0.178*tpi)  6.36 hours +0.5 hours=6.88 hours ...
Potassium chloride
Potassium chloride

... toxicity. However, ingestion of larger amount of salt can result in hyperkalemia (potassium accumulates in plasma at high concentrations). Toxic effects may include: vomiting, diarrhea, abdominal cramps, and weakness. Cardiac toxicity may occur in patients with normal renal function, but with underl ...
Using a Tritiated Compound to Elucidate Its Preclinical Metabolic
Using a Tritiated Compound to Elucidate Its Preclinical Metabolic

... significant) metabolite. Likewise, ambiguity might arise when calculating 3H recovery from biofluids undergoing organic extraction; low organic phase 3H levels may be ascribed to highly polar metabolites, HTO, or both. For total radioactivity PK analyses, 3H exchange causes similar data interpretati ...
PRODUCT INFORMATION DIFFLAM FORTE ANTI
PRODUCT INFORMATION DIFFLAM FORTE ANTI

... Animal models show that, when administered systemically, benzydamine is effective against pain and oedema due to inflammatory conditions. It also inhibits granuloma formation. At concentrations used for topical treatment, benzydamine possesses local anaesthetic action. Benzydamine does not cause ero ...
Nonclinical pharmacokinetics and metabolism of EPZ
Nonclinical pharmacokinetics and metabolism of EPZ

... proof of concept in histone methyltransferase (HMT) inhibition [9,10]. Further expansion of our medicinal chemistry efforts generated the potent molecule EPZ-5676 ((2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl) ethyl)cyclobutyl)(isopropyl)amino)met ...
Oral Hypoglycemic Agents
Oral Hypoglycemic Agents

... They are effectively absorbed  from gastrointestinal tract. Food can reduce the absorption of  sulfonylurea. Sulfonylureas are more effective  when given 30 minutes before eating. Plasma protein binding is high 90 –  99 % .. mainly bind to albumen. ...
Use of angiotensin receptor antagonists in patients with ACE
Use of angiotensin receptor antagonists in patients with ACE

... Accepted February 2004 ...
Complications of Antiretroviral Therapy
Complications of Antiretroviral Therapy

... should be lowered because of decreased metabolism of CRIXIVAN. Patients with renal insufficiency have not been studied. • Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and cush ...
Influence of Two Commercial Fibers in the Pharmacokinetics of
Influence of Two Commercial Fibers in the Pharmacokinetics of

... In order to avoid its adverse effects, EE is used at low doses; in particular, the dose of EE, when used for oral contraception, has been reduced to 30 to 50 mg per day. When other drugs and/or foods are administered at the same time, interactions may appear and EE blood concentrations may be ineffe ...
Bergamottin and “The Grapefruit Juice Effect”
Bergamottin and “The Grapefruit Juice Effect”

... thought that bergamottin and derivatives may be poorly absorbed or extensively metabolized in the gut so that they have little chance to inactivate or inhibit the liver cytochrome P450’s . The Bergamottin compound is a mechanism-based inactivator, a subclass of irreversible inhibitors, of cytochrome ...
(i) C1 inhibitor concentrates
(i) C1 inhibitor concentrates

... 20% no prior family history – spontaneous mutations More than 150 different mutations reported Varied clinical pattern may be explained by variable effect of mutations on C1 inhibitor synthesis and secretion as well as differences in Bradykinin metabolism ...
(i) C1 inhibitor concentrates
(i) C1 inhibitor concentrates

... 20% no prior family history – spontaneous mutations More than 150 different mutations reported Varied clinical pattern may be explained by variable effect of mutations on C1 inhibitor synthesis and secretion as well as differences in Bradykinin metabolism ...
cntctfrm_6ced61d6f78882958b2832b002fc9c08_Manuscript
cntctfrm_6ced61d6f78882958b2832b002fc9c08_Manuscript

... carrageenan induced rat paw edema model, the production of prostanoids has been through the serum expression of COX-2 by a positive feedback mechanism. Therefore, it is suggested that the mechanism of action of ethanol extract of Seenthil churanam may be related to prostaglandin synthesis inhibition ...
Selective phosphodiesterase inhibitors for the treatment
Selective phosphodiesterase inhibitors for the treatment

... amounts of other PDE isoenzymes in addition to PDE4 in the target tissues [4,5]. Therefore, just as combined inhibition of PDE3 and PDE4 is more effective than inhibition of a single isoenzyme family in relaxing pre-contracted human airways smooth muscle [6,7], a more effective suppression of inflam ...
TOPICALLY APPLIED NSAIDs IN THE TREATMENT OF PAIN
TOPICALLY APPLIED NSAIDs IN THE TREATMENT OF PAIN

... assessed as “moderate”. In the diclofenac group, assessment of the results was positive in 74% of the patients. In 24% of the patients of this group, the physician’s assessment of the success of the treatment was “not satisfactory”. The majority of physicians and patients were satisfied with the tol ...
Coagulation
Coagulation

... - Hold warfarin, give vitamin K (10 mg by slow I.V. infusion), and supplement with fresh plasma transfusion or prothrombin complex concentrate (factor X complex) ...
Pharmacokinetic profile and safety of 150 mg of
Pharmacokinetic profile and safety of 150 mg of

... maraviroc dosing schedules being utilized in clinical practice, reported similar maraviroc Ctrough exposure of 43 ng/mL (IQR 35 –55) to that seen in our study in the group receiving the same antiretroviral regimen.21 Within this cohort, when higher doses of maraviroc were utilized in clinical practi ...
NOVEL FAK-SELECTIVE INHIBITORS
NOVEL FAK-SELECTIVE INHIBITORS

... FAK is a non-receptor tyrosine kinase which is overexpressed (through either gene amplification or increased levels of protein expression), or over-activated in many human cancers (including solid tumours and acute myelogenous leukaemia (AML)). Increased levels of FAK and/or phosphorylated FAK are o ...
brufen sustained release (sr)
brufen sustained release (sr)

Lecture 3 - Renin Angiotensin Pathway
Lecture 3 - Renin Angiotensin Pathway

... • The renin-angiotensin pathway is integral to controlling blood volume and pressure. Pathway overactivation causes hypertension. • It is controlled by the action of two main enzymes renin and angiotensin-converting enzyme (ACE). • Drugs have been developed as ACE inhibitors, angiotensin II receptor ...
Bergamottin and “The Grapefruit Juice Effect”
Bergamottin and “The Grapefruit Juice Effect”

... increased by approximately 400 Da following inactivation could result because of formation of a covalent adduct with one molecule of bergamottin plus three oxygen groups 2 this shows that hydroxylation occurred twice on the geranyloxy side chain alone on the bergamottin2. Complete inactivation of th ...
Inhibition of Human Aldehyde Oxidase Activity by Diet
Inhibition of Human Aldehyde Oxidase Activity by Diet

... modeling was used to glean mechanistic insight into AO inhibition. Docking studies indicated that the tested constituents bound within the AO active site and elucidated key enzyme-inhibitor interactions. Quantitative structure-activity relationship modeling identified three structural descriptors th ...
Comparison of the Circulating Metabolite Profile of PF
Comparison of the Circulating Metabolite Profile of PF

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Discovery and development of cyclooxygenase 2 inhibitors



Cyclooxygenases are enzymes that take part in a complex biosynthetic cascade that results in the conversion of polyunsaturated fatty acids to prostaglandins and thromboxane(s).Their main role is to catalyze the transformation of arachidonic acid into the intermediate prostaglandin H2, which is the procursor of a variety of prostanoids with diverse and potent biological actions.Cyclooxygenases have two main isoforms that are called COX-1 and COX-2 (as well as a COX-3). COX-1 is responsible for the synthesis of prostaglandin and thromboxane in many types of cells, including the gastro-intestinal tract and blood platelets. COX-2 plays a major role in prostaglandin biosynthesis in inflammatory cells and in the central nervous system. Prostaglandin synthesis in these sites is a key factor in the development of inflammation and hyperalgesia.COX-2 inhibitors have analgesic and anti-inflammatory activity by blocking the transformation of arachidonic acid into prostaglandin H2 selectively.
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