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Featured Article
Featured Article

... A drug-eluting stent has three elements, all of which have an important effect on vascular injury and restenosis: the metallic stent, a drug-carrier vehicle or coating, and a pharmacologic agent that interferes with local neointimal proliferation(6;7). Current drug-eluting stent systems utilize comm ...
TAMIFLU Product Monograph
TAMIFLU Product Monograph

... with first dosing. These events did not lead to patient discontinuation of study drug in the vast majority of instances. At the recommended dose of 75 mg twice daily, the most frequently reported adverse events that led to patient withdrawal were nausea and vomiting. In adult/adolescent phase III tr ...
TAMIFLU Product Monograph
TAMIFLU Product Monograph

... with first dosing. These events did not lead to patient discontinuation of study drug in the vast majority of instances. At the recommended dose of 75 mg twice daily, the most frequently reported adverse events that led to patient withdrawal were nausea and vomiting. In adult/adolescent phase III tr ...
Zofran
Zofran

... of the liver [see Clinical Pharmacology (12.3)]. Because ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes (CYP3A4, CYP2D6, CYP1A2), inducers or inhibitors of these enzymes may change the clearance and, hence, the half-life of ondansetron. In patients treated with pote ...
Protease inhibitor plasma concentrations in HIV antiretroviral therapy
Protease inhibitor plasma concentrations in HIV antiretroviral therapy

... An in vitro 90% effective concentration of 2100 ng/ml against HIV-1 type IIIB (wild-type virus) in MT4 cells, after adjustment for protein binding, had been estimated. The study demonstrated that only patients with minimum concentrations above this concentration had long-term effects on plasma HIV R ...
Advances in and applications of proteasome inhibitors
Advances in and applications of proteasome inhibitors

... which only differ from the salinosporamides in the C2 alkyl side chain, have comparable potency in vitro with IC50 values in the low nanomolar range. It remains, however, to be shown if the cinnabaramides have the same anticancer properties as salinosporamide A. Further proteasome inhibitors of the ...
The practice of digoxin therapeutic drug monitoring - BN6Team-10
The practice of digoxin therapeutic drug monitoring - BN6Team-10

... how high the concentration is, and the half-life of digoxin in that patient. In a patient with normal renal function (half-life approximately 30 h) and a concentration of 3.0 nmol/l, the digoxin should be withheld for 1–2 days before restarting at the appropriately altered dose, as this will allow t ...
Piracetam Nootropil - The Filipino Doctor
Piracetam Nootropil - The Filipino Doctor

... treatment with piracetam should be continued for as long as the original cerebral disease persists. In patients with an acute episode, spontaneous evolution may occur over time and an attempt should be made every 6 months to decrease or discontinue the medicinal treatment. This should be done by red ...
Anti platelet Agents
Anti platelet Agents

... the cyclo-oxygenase activity is lost permanently, whereas the hydroperoxidase activity is not affected. An inducible form of PGH-synthase has been identified and termed PGH-synthase 2 or COX-2.13 Aspirin inhibits the cyclo-oxygenase activity of PGH-synthase 2, but at higher concentrations than those ...
Comparison of High Loading Dose Versus Usual Dose of Rectal
Comparison of High Loading Dose Versus Usual Dose of Rectal

... High Dose Versus Usual Dose of Rectal Acetaminophen tistically significant difference between the mean body temperatures of these two groups at one and three hour intervals after treatment. Although, mean temperature reductions three hours after treatment were higher in patients administered a high ...
ATACAND HCT® 16-12.5 candesartan cilexetil−hydrochlorothiazide TABLETS ATACAND HCT® 32-12.5
ATACAND HCT® 16-12.5 candesartan cilexetil−hydrochlorothiazide TABLETS ATACAND HCT® 32-12.5

... inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because candesartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Candesartan does not bind to or block other hormone recepto ...
Combined use of nonsteroidal anti-inflammatory drugs with diuretics
Combined use of nonsteroidal anti-inflammatory drugs with diuretics

... and end-stage kidney disease and death.1 Nonsteroidal antiinflammatory drugs (NSAIDs) are estimated to account for up to 7% of all cases of AKI and up to 36% of drug-induced cases.2,3 NSAID exposure has been reported to increase the risk of AKI between 1.3- and 4.1-fold and the number needed to harm ...
Prescribing information - Novartis Pharmaceuticals Corporation
Prescribing information - Novartis Pharmaceuticals Corporation

... of the liver [see Clinical Pharmacology (12.3)]. Because ondansetron is metabolized by hepatic cytochrome P450 drug-metabolizing enzymes (CYP3A4, CYP2D6, CYP1A2), inducers or inhibitors of these enzymes may change the clearance and, hence, the half-life of ondansetron. In patients treated with poten ...
ANNEX I TO PSUR CORE SAFETY PROFILE (EU SPC Sections 4.2
ANNEX I TO PSUR CORE SAFETY PROFILE (EU SPC Sections 4.2

... interactions will be less pronounced for the rectal than for the oral route because the gastro-intestinal tract is by-passed whereas after IM administration the effects of CYP3A4 modulation should not substantially differ from those seen with IV midazolam. It is therefore recommended to carefully mo ...
Allopurinol Orion 300 mg tablet ENG SmPC
Allopurinol Orion 300 mg tablet ENG SmPC

... the dose of these drugs is reduced to one-quarter of the previously prescribed dose (see section 4.5). Acute gouty attacks: Allopurinol treatment should not be started until an acute attack of gout has completely subsided, as further attacks may be precipitated. In the early stages of treatment with ...
Pain-management-1-23-13
Pain-management-1-23-13

... active opioid metabolites (e.g., morphine) from prodrugs (eg, codeine) is dependent on CYP2D6 activity. Naltrexone response: In patients treated with naltrexone for alcohol dependence, those with the GG genotype have a 15% lower average relapse rate compared to the typical on-treatment relapse rate. ...
1. NAME OF THE MEDICINAL PRODUCT Ciprinol 250 mg film
1. NAME OF THE MEDICINAL PRODUCT Ciprinol 250 mg film

... Dose adjustment is not necessary in patients in mild or moderate hepatic failure but may be considered necessary in severe hepatic failure. Impaired renal and hepatic function Dose adjustment as under impaired renal function. Patients should be carefully monitored. In specific cases it may be approp ...
NL-2854 Final SmPC - updated for national phase in NL - CBG-MEB
NL-2854 Final SmPC - updated for national phase in NL - CBG-MEB

... account the individual patient's cholesterol level and future cardiovascular risk as well as the potential risk for adverse reactions (see below). A dose adjustment to the next dose level can be made after 4 weeks, if necessary (see section 5.1). In light of the increased reporting rate of adverse r ...
ULTRACET C IV
ULTRACET C IV

... Following oral administration, tramadol is extensively metabolized by a number of pathways, including CYP2D6 and CYP3A4, as well as by conjugation of parent and metabolites. Approximately 30% of the dose is excreted in the urine as unchanged drug, whereas 60% of the dose is excreted as metabolites. ...
Tybost - Gilead Sciences, Inc.
Tybost - Gilead Sciences, Inc.

... Prior to initiating therapy with TYBOST, assess estimated creatinine clearance [see Dosage and Administration (2.2)]. Dosage recommendations are not available for drugs that require dosage adjustments in TYBOST-treated patients with renal impairment [see Adverse Reactions (6.1), Drug Interactions (7 ...
elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide

... group, the mutations that emerged were M184V/I(N = 49) and K65R/N (N = 1) in reverse transcriptase and T66T/AA/I/V (N = 2), E92Q (N = 4), Q148Q/R (N = 1) and N155H (N = 2) in integrase. Of the 8 patients with resistance development in the STRIBILD group, the mutations that emerged were M184V/I (N = ...
Cytochrome P450 Inhibition
Cytochrome P450 Inhibition

... Drug-drug interactions can occur when two drugs are coadministered and compete for the same enzyme. ...
ISOPTIN Ò SR 240mg
ISOPTIN Ò SR 240mg

... arrest in 2%. It must be appreciated that this group of patients had a serious disease with a high mortality rate. Most adverse effects responded well to dose reduction and only rarely did verapamil have to be discontinued. Use in Patients with Impaired Hepatic Function Since verapamil is highly met ...
Product Monograph
Product Monograph

... Dependence Liability: Pilocarpine HCl does not have the potential for addiction; consequently, there have been no reports of addiction with the use of pilocarpine HCl. There are no known withdrawal effects associated with pilocarpine either in animals or in humans. The pharmacologic effects, other t ...
Drug interactions involving warfarin
Drug interactions involving warfarin

... Pharmacy and Pharmaceutical Sciences, University of Alberta, in the fall of 2009.5 Since then, the practice tool has been updated as described above. ...
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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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