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Rexulti (b
Rexulti (b

... Recommended starting dose: 1 mg PO qDay on Days 1 through 4 Recommended target dose: 2-4 mg PO qDay; titrate to 2 mg qDay on Days 5 through 7, and then to 4 mg/day on Day 8 based on the patient’s clinical response and tolerability ...
N Engl J Med, 2015, 373: 511-520
N Engl J Med, 2015, 373: 511-520

... REVERSE-AD: Takeaways • Demonstrated that idarucizumab safely and efficaciously reverses anticoagulation induced by dabigatran administration • Standardization of laboratory testing and monitoring will be necessary on an institution-to-institution basis • dTT vs. ECT vs. TT vs. aPTT • Consideration ...
Inhibitors of Protein Synthesis
Inhibitors of Protein Synthesis

... Highly polar molecules, do not distribute well into body compartments. Administration iv and im only Narrow therapeutic index. ...
BOSENTAN and POSSIBLE DRUG INTERACTIONS (No 1
BOSENTAN and POSSIBLE DRUG INTERACTIONS (No 1

... Background Sitaxentan is metabolised in the liver by Cytochrome P450 (CYP) isoenzymes CYP2C9 (major pathway) and CYP3A4 (minor pathway). Approximately half of an oral dose is excreted in the urine with the remainder eliminated in the faeces. Although there is potential for interaction with CYP2C9 an ...
Pharmacotherapy of Angina Pectoris
Pharmacotherapy of Angina Pectoris

... having a longer duration of action for prophylaxis b. Isosorbide dinitrate [ISDN] – converted to ISMN ...
Novel Anti-platelet Agents and Anticoagulants
Novel Anti-platelet Agents and Anticoagulants

... There are approximately 500,000 individuals taking anticoagulants in the UK as prophylaxis against or treatment of: • The  thromboembolic  complications  associated  with  atrial  fibrillation  (AF)   • Venous  thrombosis  and  pulmonary  embolism   • The  thromboembolic ...
PDF Version - Cardiological Society of India
PDF Version - Cardiological Society of India

... (ii) body weight less than 60 kg; (iii) concomitant use of strong P-glycoprotein inhibitors. Concomitant use of verapamil increases AUC of edoxaban by 53%, a decrease of edoxaban dose by 50% is thus recommended when used along with verapamil.1 For stroke prevention in AF, NOACs are found useful an ...
Advanced Medicinal Chemistry
Advanced Medicinal Chemistry

... Progress of Reaction ...
Advanced Medicinal Chemistry
Advanced Medicinal Chemistry

... Progress of Reaction ...
Delipid
Delipid

... concentration. HDL-triglyceride is usually decreased slightly. Gemfibrozil usually increases the HDL-cholesterol fraction in healthy individuals and patients with hyperlipoproteinemia, an action that may be beneficial in slowing the progression of atherosclerosis and in reducing the risk of coronary ...
Glicron CR Capsule
Glicron CR Capsule

... Care should be exercised in patients with hepatic and/or renal impairment and a small starting dose should be used with careful patient monitoring. As with our other sulfonylureas, hypoglycemia will occur if the patients’ dietary intake is reduced or if they are receiving a larger dose of gliclazide ...
What can we do now and what are the gaps in our knowledge?
What can we do now and what are the gaps in our knowledge?

... Even if we have the “best” PK/PD marker for monitoring drug activity and a validated assay, can we define a “therapeutic range”?: – Variability in anti-Xa activity depending on patients characteristics (e.g.: renal function) as well as by indication. – Different clinical situations may require diffe ...
New Approaches to Chronic Anticoagulation
New Approaches to Chronic Anticoagulation

... Rivaroxaban: Conclusions • Is a selective, reversible, active-site directed Factor Xa inhibitor that inhibits coagulation triggered by both the collagen (intrinsic) and tissue factor (extrinsic) pathways • Reduces thrombus formation in both venous and arterial thrombosis models • Has a bleeding ris ...
activated partial thromboplastin time (APTT) (aPTT) (PTT) the period
activated partial thromboplastin time (APTT) (aPTT) (PTT) the period

... activated partial thromboplastin time (APTT) (aPTT) (PTT) the period required for clot formation in recalcified blood plasma after contact activation and the addition of platelet substitutes; used to address the intrinsic and common pathways of coagulation. bleeding time the duration of bleeding aft ...
on September 22, 2014. For personal use only. All other... Downloaded from www.ccjm.org
on September 22, 2014. For personal use only. All other... Downloaded from www.ccjm.org

... gestation. Amlodipine has been shown to prolong both the gestation period and the duration of labor in rats at this dose. There are no adequate and well-controlled studies in pregnant women. Amlodipine should be used during pregnancy only if the potential benefit justifies the potential risk to the ...
Diapro MR Prescribing Information
Diapro MR Prescribing Information

... treatment should also be used when switching to treatment with Diamicron 30 mg MR  Tablets, i.e. a starting dose of 30 mg/day, followed by a stepwise increase in dose,  depending on the metabolic response.   It is recommended that the minimum daily starting dose of 30 mg is used.   Dose In Renal Imp ...
EACA - Blood CME Center
EACA - Blood CME Center

... http://www.ohri.ca/programs/clinical_epidemiology/thrombosis_group/studies/BART.asp. Accessed May 8, 2008; US Food and Drug Administration. Available at http://www.fda.gov/Cder/drug/early_comm/aprotinin.htm. Accessed May 8, 2008. ...
Drugs used for treatment of AIDS
Drugs used for treatment of AIDS

... Inducer of hepatic cytochrome P450 It is typically used as a component of combination therapy  Very effective for prevention of transmission as a single dose at time of labor and followed by oral dose to neonate with in three days ...
Regional anaesthesia in patients on newer
Regional anaesthesia in patients on newer

... from22%to 68%, occurs in 3 hrs after dosing and is maintainedfor at least 12 h. Rivaroxaban has a terminal half-life of 5.7–9.2 h, but can be as long as 11–13 h inelderly patients. One-third of the drug is eliminated by the kidneys, one-third by the faecal/biliary route, and one-third is metabolized ...
Anticoagulants
Anticoagulants

... results of this Mini‐Sentinel assessment indicate that bleeding rates associated with new use of [dabigatran] do not appear to be higher than bleeding rates associated with new use of warfarin ….” ...
Slide 1
Slide 1

... on different diseases • Pharmacodynamic : The effects of drugs on living system • Pharmacokinetic : The fate of drugs in living system • Pharmacognosy : Natural sources of drugs • Pharmacogenetic : Different responses to drugs because of genetic variations ...
Slide 1
Slide 1

... on different diseases • Pharmacodynamic : The effects of drugs on living system • Pharmacokinetic : The fate of drugs in living system • Pharmacognosy : Natural sources of drugs • Pharmacogenetic : Different responses to drugs because of genetic variations ...
Exondys 51
Exondys 51

... No studies have been done in patients with renal impairment No studies have been done in patients with hepatic impairment ...
Geriatric Drug-Drug Interactions
Geriatric Drug-Drug Interactions

... • Older BP patients may be slow to improveduration of adequate treatment trial not clear; • Optimal doses/concentrations not defined; • Some patients respond to low concentrations, e.g. of lithium. • Patients with dementia, and mild cognitive impairments, may have slower/attenuated benefit and great ...
Linköping University Post Print Effects of the oral, direct thrombin inhibitor
Linköping University Post Print Effects of the oral, direct thrombin inhibitor

... thrombosis. Millions of patients have been treated and the knowledge of pros and cons of this very efficient drug is well established, including effects on coagulation assays. One of the draw backs is the need for monitoring by measuring prothrombin time to achieve appropriate degree of anticoagulat ...
< 1 ... 54 55 56 57 58 59 60 61 62 ... 65 >

Discovery and development of direct thrombin inhibitors



Direct thrombin inhibitors (DTIs) are a class of anticoagulant drugs that can be used to prevent and treat embolisms and blood clots caused by various diseases. They inhibit thrombin, a serine protease which affects the coagulation cascade in many ways. DTIs have undergone rapid development since the 90's. With technological advances in genetic engineering the production of recombinant hirudin was made possible which opened the door to this new group of drugs. Before the use of DTIs the therapy and prophylaxis for anticoagulation had stayed the same for over 50 years with the use of heparin derivatives and warfarin which have some well known disadvantages. DTIs are still under development, but the research focus has shifted towards factor Xa inhibitors, or even dual thrombin and fXa inhibitors that have a broader mechanism of action by both inhibiting factor IIa (thrombin) and Xa. A recent review of patents and literature on thrombin inhibitors has demonstrated that the development of allosteric and multi-mechanism inhibitors might lead the way to a more safer anticoagulant.
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