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Review Nucleotide prodrugs for HCV therapy
Review Nucleotide prodrugs for HCV therapy

... boceprevir. Each of these compounds has completed Phase III clinical investigation and both have been shown to be efficacious in treating HCV infection when given in combination with SOC. However, each of these first generation protease inhibitors suffers from the lack of genotype coverage, undesire ...
Reyataz - Products - Bristol
Reyataz - Products - Bristol

... • Hyperbilirubinemia: Most patients experience asymptomatic increases in indirect bilirubin, which is reversible upon discontinuation. Do not dose reduce. If a concomitant transaminase increase occurs, evaluate for alternative etiologies. (5.3) • Phenylketonuria: REYATAZ (atazanavir) oral powder c ...
DATA SHEET Tramal Capsules Solution for Injection
DATA SHEET Tramal Capsules Solution for Injection

... months. Beyond six months no clinical studies investigating the safety and efficacy of tramadol are available. When tramadol treatment of pain is required long-term, careful and regular monitoring should be carried out to establish whether, and to what extent, ongoing treatment is necessary. Carcino ...
PRODUCT MONOGRAPH
PRODUCT MONOGRAPH

... Bleeding Sites ...
QA248_4Pyridostigmine_neostigmine_FINAL
QA248_4Pyridostigmine_neostigmine_FINAL

... Pyridostigmine is a reversible inhibitor of the enzyme cholinesterase with actions similar to those of neostigmine, but is slower in onset and has a longer duration of action.(1;2) Both pyridostigmine and neostigmine are licensed for the treatment of myasthenia gravis: pyridostigmine is given orally ...
HYZAAR® HYZAAR® DS
HYZAAR® HYZAAR® DS

... of reversing hypotension and/or substituting for impaired renal function; however, limited experience with those procedures has not been associated with significant clinical benefit. Neither losartan nor the active metabolite can be removed by hemodialysis. Thiazides cross the placental barrier and ...
prevpac - Takeda
prevpac - Takeda

... the peak time from approximately two to 2.5 hours. Food also increases the clarithromycin peak plasma concentration by about 24%, but does not affect the extent of clarithromycin bioavailability. Food does not affect the onset of formation of the antimicrobially active metabolite, 14-OH clarithromyc ...
Sotalol versus Amiodarone in Treatment of Atrial Fibrillation
Sotalol versus Amiodarone in Treatment of Atrial Fibrillation

... and only 2 publications directly compared sotalol to amiodarone.6 The studies were grouped according to the treatment employed, i.e. sotalol versus amiodarone, as well as the goal of therapy: AF conversion, or maintenance of sinus rhythm. For each group, a meta-analysis was performed to obtain the c ...
Ex vivo effects of low-dose rivaroxaban on specific coagulation
Ex vivo effects of low-dose rivaroxaban on specific coagulation

... lupus anticoagulant (LA) in patients given vitamin K antagonist therapy is difficult due to the coagulation defect induced by the anticoagulants, which leads to prolongation of all phospholipiddependent clotting times. The influence of rivaroxaban on thrombophilia screening assays including determin ...
Comparison of Anti-Xa and Dilute Russell Viper Venom Time
Comparison of Anti-Xa and Dilute Russell Viper Venom Time

... method for determining rivaroxaban levels (Figure 2, C). COMMENT Although routine laboratory monitoring is not required when patients are administered rivaroxaban, there are several clinical situations where determination of the level of anticoagulation is of value. There have been recent reports ev ...
Product Monograph
Product Monograph

... RAS, such as ARBs or aliskiren-containing drugs, is generally not recommended in other patients, since such treatment has been associated with an increased incidence of severe hypotension, renal failure, and hyperkalemia (see DRUG INTERACTIONS). Cardiovascular Aortic Stenosis There is concern, on th ...
Noxafil - Merck.com
Noxafil - Merck.com

... Noxafil delayed-release tablets and oral suspension are not to be used interchangeably due to the differences in the dosing of each formulation [see Dosage and Administration (2.3, 2.4, 2.5)]. Noxafil injection  Administer via a central venous line, including a central venous catheter or peripheral ...
Ketorolac Tromethamine Injection, USP
Ketorolac Tromethamine Injection, USP

... The mean apparent volume (Vβ) of ketorolac tromethamine following complete distribution was approximately 13 liters. This parameter was determined from single-dose data. The ketorolac tromethamine racemate has been shown to be highly protein bound (99%). Nevertheless, plasma concentrations as high a ...
Levitra
Levitra

... Vardenafil and its major circulating metabolite (M1) are highly bound to plasma proteins (about 95% for parent drug or M1). This protein binding is reversible and independent of total drug concentrations. Based upon measurements of vardenafil in semen of healthy subjects 90 minutes after dosing, not ...
Cialis arginine+zinc
Cialis arginine+zinc

... Levitra Professional also known as Staxyn in the US market. It has been produced in orally disintegrating tablets, so it acts faster and has all merits of vardenafil at the same tome. ...
Copyright Information of the Article Published Online TITLE Oral
Copyright Information of the Article Published Online TITLE Oral

... in these subjects, functional closure induced by PGHS inhibitors is less frequently followed by the structural closure of the ductus[5,46]. IV paracetamol may transiently increase liver enzymes concentration in patients[47]. Alan et al[48] reported 3 patients with transient increased transaminases, ...
Version 7
Version 7

... (Cmax increased 5.3-fold and AUC 4-fold). Enhanced effects and increased toxicity of buspirone may be possible when buspirone is administered with diltiazem. Subsequent dose adjustments of either drug should be based on clinical response. Verapamil: Concomitant administration of buspirone (10 mg as ...
Product Monograph
Product Monograph

... rhabdomyolysis have been reported in patients treated with ZOCOR®. Rare cases of rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with ZOCOR® and with other HMG-CoA reductase inhibitors. Myopathy, defined as muscle pain or muscle weakness in conjunction with incr ...
Acetaminophen
Acetaminophen

... the corresponding aniline derivatives, although paminophenol itself is too toxic for therapeutic purposes. Acetaminophen is weakly acidic (pKa = 9.51) and synthesized by the acetylation of p-aminophenol ...
Simvastatin
Simvastatin

... formation from mevalonate. HMG-CoA reductase activity was increased and the specific binding of LDL to the cells was increased, suggesting increased expression of the LDL receptor.1 In the rat the drug blocked cholesterol synthesis after a single oral dose with ID50 values of less than 0.2 mg.kg-1. ...
ALLEGRA-D - hebust.edu.cn
ALLEGRA-D - hebust.edu.cn

... The pharmacokinetics of fexofenadine hydrochloride and pseudoephedrine hydrochloride when administered separately have been well characterized. Fexofenadine pharmacokinetics were linear for oral doses of fexofenadine hydrochloride up to 120 mg twice daily. The mean elimination half-life of fexofenad ...
Increased risk of atherothrombotic events associated with
Increased risk of atherothrombotic events associated with

... lopidogrel is an antiplatelet drug widely used in the management of coronary artery disease. 1 It decreases the incidence of coronary artery stent thrombosis2,3 and has been approved for the management of nonST-segment elevation myocardial infarction.4 Recent reports have indicated a lack of platele ...
Amstan Tablets.FH11
Amstan Tablets.FH11

... Following oral administration of vals artan alone, peak plas ma concentrations of valsartan are reached in 2 to 4 hours. Mean absolute bioavailability is 23% . Food decreases exposure (as measured by AUC) to valsartan by about 40% and peak plasma concentration (Cmax) by about 50%. However, this redu ...
Ketorolac Tromethamine
Ketorolac Tromethamine

... approximately 13 liters. This parameter was determined from single-dose data. The ketorolac tromethamine racemate has been shown to be highly protein bound (99%). Nevertheless, plasma concentrations as high as 10 mcg/mL will only occupy approximately 5% of the albumin binding sites. Thus, the unboun ...
Prescribing information
Prescribing information

... LAMISIL Oral Granules are contraindicated for patients with chronic or active liver disease. Before prescribing LAMISIL Oral Granules, perform liver function tests because hepatotoxicity may occur in patients with and without preexisting liver disease. Cases of liver failure, some leading to liver t ...
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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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