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Antidepressant Agents
Antidepressant Agents

Diuretic - e
Diuretic - e

... Structure of carbonic anhydrase inhibitors ...
kinetics of iv bolus: urine data
kinetics of iv bolus: urine data

Attachment: Product Information Brivaracetam
Attachment: Product Information Brivaracetam

... 27,863 AED-treated patients was 0.43%, compared to 0.24% among 16,029 placebo-treated patients, representing an increase of approximately one case of suicidal thinking or behaviour for every 530 patients treated. There were four suicides in drug-treated patients in the trials and none in placebo-tre ...
Drug-induced peptic ulcer disease
Drug-induced peptic ulcer disease

... prostaglandins. As prostaglandins play a major role in the maintenance of ...
Pharmacokinetics of drug infusions
Pharmacokinetics of drug infusions

... On stopping an infusion, three possible processes contribute to a decline in plasma concentration: distribution to the second and third compartments, and excretion. The relative contributions of these to the initial decline in plasma concentration vary according to the duration of the infusion. The ...
The possible risks of proton pump inhibitors
The possible risks of proton pump inhibitors

... Given that both of these conditions present with diarrhoea, which is a side effect of PPIs, it may be that this association is the result of detection bias, as individuals using PPIs are more likely to be investigated to rule out microscopic colitis or SIBO. The hypergastrinaemia documented in long ...
OAB Conversation Starters
OAB Conversation Starters

... tolerability, the dose may be increased to 8 mg once daily. (2) The daily dose of Toviaz should not exceed 4 mg in the following populations: • Patients with severe renal impairment (CLCR <30 mL/min) (2) • Patients taking potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, and clarithromyc ...
NSAIDs Guidelines
NSAIDs Guidelines

... COX and LOX selectivity, and NSAID adverse effects Inhibition of COX-1, the enzyme predominantly associated with homeostatic functions, is reported to be the cause of most NSAID-induced side effects such as gastric ulcers and blood dyscrasias. In an attempt to avoid this, NSAIDs with a greater prope ...
Part IB Summary of Product Characteristics
Part IB Summary of Product Characteristics

... Rabeprazole is approximately 97% bound to human plasma proteins. Metabolism and excretion: Rabeprazole sodium, as is the case with other members of the proton pump inhibitor (PPI) class of compounds, is metabolised through the cytochrome P450 (CYP450) hepatic drug metabolising system. In vitro studi ...
Antifungal Drugs
Antifungal Drugs

... White field ointment : 12% Benzoic acid & 6% Salicylic acid . Castellani paint. ...
Epilim Chrono 500mg
Epilim Chrono 500mg

... Children under 20kg An alternative formulation of Epilim should be used in this group of patients, due to the tablet size and need for dose titration. Epilim Liquid (sugar-free) or Epilim Syrup are alternatives. Elderly Although the pharmacokinetics of Epilim are modified in the elderly, they have l ...


... Due to their non-selectivity, they are also found to be toxic. Though the drug staurosporine is known for ...
Chemotherapy regimen: Dose adjusted EPOCH
Chemotherapy regimen: Dose adjusted EPOCH

... CHOP One study evaluated the clinical impact of co-administration of combination antiretroviral therapy (cART) with CHOP (cyclophosphamide 750 mg/m2, doxorubicin 50 mg/m2, vincristine 1.4 mg/m2 [max 2 mg], prednisone 100 mg/m2) in the context of treatment for non-Hodgkin’s lymphoma. In comparison wi ...
How to Conduct a Low Energy (Carbon-14) Radiolabel Human AME study
How to Conduct a Low Energy (Carbon-14) Radiolabel Human AME study

... Determine the exposure of the parent compound and its major metabolites – quantify metabolites relative to parent and the total(测定受试物及代谢产物的暴 露量) ...
7. antihyperlipidemics
7. antihyperlipidemics

... produce liver toxicity in patient with liver disease or a history of alcohol abuse. Minor increases in creatine kinase activity in plasma. Myopathy may occur when used in combination with fibrates. Concomitant use of reductase inhibitors with amiodarone or verapamil also causes an increased risk of ...
Prescribing Information
Prescribing Information

... interfere with the controlled release properties of DURLAZA. Renin-angiotensin system (RAS) inhibitors: In patients who are elderly, volume-depleted (including those on diuretic therapy), or who have compromised renal function, coadministration of NSAIDs, including DURLAZA, with RAS inhibitors may r ...
Slide 1
Slide 1

... known to be the mechanism of action of aspirin and other non-steroidal antiinflammatory drugs (NSAIDs) such as ibuprofen. However, their action in blocking COX-1 is known to be responsible for also causing the unwanted gastrointestinal side effects associated with these drugs. Paracetamol has no sig ...
753_Module3_KidneyFunction
753_Module3_KidneyFunction

... Formation and Composition of Urine (3 primary factors) 1. Cellular regulation of osmolarity (figure 29-2,29-3 G & G) a. Transport of small ions Review general sites and mechanisms for ion transport. b. Transport of organic acids and bases Active, competitive, bidirectional transporters with signific ...
Heart Failure
Heart Failure

... Sodium nitrite: It oxidizes some iron of haemoglobin to ferric state and converts it to methaemoglobin. Cyanide preferntially binds to methaemoglobin to form cyanmethaemoglobin. Administration of sodium thiosulphate converts cyanmethaemoglobin to thiocyanate, sulfite and haemoglobin. Thiocyanate is ...
Inhibition of Purified Factor Xa Amidolytic Activity May Not Be
Inhibition of Purified Factor Xa Amidolytic Activity May Not Be

... actor Xa (fXa) has long been viewed as a target for anticoagulation therapy because it is at the intersection of the intrinsic and extrinsic coagulation pathways, and its selective inhibition is presumed to have a major anticoagulatory effect. The prothrombinase complex, of which fXa is the enzymati ...
Clinical uses
Clinical uses

... Fibrin clot ...
No Slide Title
No Slide Title

... Traditional NSAIDs at full therapeutic doses inhibit both enzymes • Most have greater effect on COX-1 than COX-2 The new drugs are highly selective for COX-2 • >300-fold more effective against COX-2 • This difference allows • Major reduction in COX-2 production of proinflammatory PGs • Sparing of CO ...
NEW ZEALAND DATA SHEET IBUPROFEN
NEW ZEALAND DATA SHEET IBUPROFEN

... Ibuprofen is a non-steroidal anti-inflammatory agent. Its mode of action, like that of other non-steroidal anti-inflammatory agents, is not completely understood, but may be related to prostaglandin synthetase inhibition. Ibuprofen has shown antiinflammatory, analgesic and antipyretic activity in bo ...
Setor 11. Farmacologia Clínica, Farmacocinética
Setor 11. Farmacologia Clínica, Farmacocinética

... Introduction: According to World Health Organization the infertility reaches 15% of active sex life population and 50 % of these cases are caused by male factor as primary factor or in association with female ones. About one-third of reproductive age people smoke cigarettes and it can also be involv ...
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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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