Reviewing the reality: why we need to change * Peter J. Lin Introduction
... The limitations associated with warfarin therapy have resulted in the global problem of under-treatment with anticoagulants for the prevention of strokes in AF. In Italy, for example, only about one in five hospitalized patients with AF will receive oral anticoagulation and only 25% of chronic AF pat ...
... The limitations associated with warfarin therapy have resulted in the global problem of under-treatment with anticoagulants for the prevention of strokes in AF. In Italy, for example, only about one in five hospitalized patients with AF will receive oral anticoagulation and only 25% of chronic AF pat ...
Versatile Oligo(N-Substituted) Glycines: The
... of treating HIV infection [1]. Several peptoids, similar in sequence to Tat49±57, have been synthesized with the intention of preventing the HIV-Tat/Tar interaction, and thus preventing HIV replication [24, 25, 30, 31]. However, only recently has this class of peptoids been applied to membrane trans ...
... of treating HIV infection [1]. Several peptoids, similar in sequence to Tat49±57, have been synthesized with the intention of preventing the HIV-Tat/Tar interaction, and thus preventing HIV replication [24, 25, 30, 31]. However, only recently has this class of peptoids been applied to membrane trans ...
Newer Therapies for Chronic Obstructive Pulmonary Disease
... and T lymphocytes. These cells release a battery of proteins called as chemokines and cytokines which get involved in the various complex inflammatory and destructive pathways leading to chronic bronchitis and emphysema. Moreover, the steroids which arrest asthmatic inflammation quite effectively ar ...
... and T lymphocytes. These cells release a battery of proteins called as chemokines and cytokines which get involved in the various complex inflammatory and destructive pathways leading to chronic bronchitis and emphysema. Moreover, the steroids which arrest asthmatic inflammation quite effectively ar ...
Anti-platelet agents
... • Is not a very effective antithrombotic drug • Dipyridamole also has a vasodilatory effect and should be used with caution in patients with severe coronary artery disease; chest pain may be aggravated in patients with underlying coronary artery disease who ...
... • Is not a very effective antithrombotic drug • Dipyridamole also has a vasodilatory effect and should be used with caution in patients with severe coronary artery disease; chest pain may be aggravated in patients with underlying coronary artery disease who ...
Open PDF File - Array BioPharma
... Literature compounds with a greater than 10-fold preference for AAG demonstrated a greater than three-fold decrease in the free fraction with increasing AAG levels: ritonavir, imatinib, nelfinavir, docetaxel, chlorpromazine, imipramine, erythromycin, and propranolol. Test compounds that had a modera ...
... Literature compounds with a greater than 10-fold preference for AAG demonstrated a greater than three-fold decrease in the free fraction with increasing AAG levels: ritonavir, imatinib, nelfinavir, docetaxel, chlorpromazine, imipramine, erythromycin, and propranolol. Test compounds that had a modera ...
An inadequate absorption, distribution, metabolism, excretion
... to have yogavahi property that is, it enhances the activity of drugs co-administered with it. This study examined the effect of Kajjali on single dose oral pharmacokinetics of Rifampicin in healthy Wistar rats. Two groups (n=6) were employed; of which one received single dose of Rifampicin alone and ...
... to have yogavahi property that is, it enhances the activity of drugs co-administered with it. This study examined the effect of Kajjali on single dose oral pharmacokinetics of Rifampicin in healthy Wistar rats. Two groups (n=6) were employed; of which one received single dose of Rifampicin alone and ...
Hit discovery and hit-to-lead approaches
... be screened in biochemical assays. Several factors are easier to control in fragment-based lead discovery because the number of samples is significantly smaller than that used for HTS. Compounds can be prefiltered for solubility, purity and reactive functional group considerations, and structural as ...
... be screened in biochemical assays. Several factors are easier to control in fragment-based lead discovery because the number of samples is significantly smaller than that used for HTS. Compounds can be prefiltered for solubility, purity and reactive functional group considerations, and structural as ...
Oral anticoagulation in atrial fibrillation – Balancing the risk of stroke
... Events in AF, ASA—acetylsalicylic acid, CAD—coronary artery disease, CrCl—creatinine clearance, CYP—cytochrome P450, DM—diabetes mellitus, GI—gastrointestinal, HF—heart failure, HTN—hypertension, INR—international normalized ratio, LVEF—left ventricular ejection fraction, MI—myocardial infarction, N ...
... Events in AF, ASA—acetylsalicylic acid, CAD—coronary artery disease, CrCl—creatinine clearance, CYP—cytochrome P450, DM—diabetes mellitus, GI—gastrointestinal, HF—heart failure, HTN—hypertension, INR—international normalized ratio, LVEF—left ventricular ejection fraction, MI—myocardial infarction, N ...
New Drugs in the Management of Type 2 Diabetes
... Contraindications GFR < 45 (or 60 for dapagliflozin) ...
... Contraindications GFR < 45 (or 60 for dapagliflozin) ...
Updated Guidelines on Outpatient Anticoagulation
... may require lower initiation dosages.1 For persons who are healthy enough to be treated as outpatients, the ACCP guidelines provide an alternative warfarin initiation dosage of 10 mg daily for the first two days of therapy, rather than the anticipated maintenance dosage.1 After baseline INR is deter ...
... may require lower initiation dosages.1 For persons who are healthy enough to be treated as outpatients, the ACCP guidelines provide an alternative warfarin initiation dosage of 10 mg daily for the first two days of therapy, rather than the anticipated maintenance dosage.1 After baseline INR is deter ...
Angiotensin-II receptor antagonists: what is Volume 20
... is indicated but an ACE inhibitor cannot be used because of an intolerable ACE inhibitor-induced cough – The major benefit of A2RAs over ACE inhibitors is their lower rate of cough. However, cough may not be as common with ACE inhibitors as many health professionals perceive. The percentage of peop ...
... is indicated but an ACE inhibitor cannot be used because of an intolerable ACE inhibitor-induced cough – The major benefit of A2RAs over ACE inhibitors is their lower rate of cough. However, cough may not be as common with ACE inhibitors as many health professionals perceive. The percentage of peop ...
The Role of Ligand Efficiency Measures in Drug Discovery
... intermolecular interaction to the ligand alone. Secondly, it assumes the binding energies per atom are additive. Thus for a given ligand efficiency (the gradient) there is a linear relationship between the free energy of binding and the number of heavy atoms, where it is assumed a ligand with zero a ...
... intermolecular interaction to the ligand alone. Secondly, it assumes the binding energies per atom are additive. Thus for a given ligand efficiency (the gradient) there is a linear relationship between the free energy of binding and the number of heavy atoms, where it is assumed a ligand with zero a ...
European Heart Rhythm Association Practical patients with non-valvular atrial fibrillation
... See further Tables and text for discussion on dose considerations. Hatching, as (being) studied in Phase 3 clinical trial; not yet approved by EMA. ...
... See further Tables and text for discussion on dose considerations. Hatching, as (being) studied in Phase 3 clinical trial; not yet approved by EMA. ...
Fatty acid amide hydrolase - The Scripps Research Institute
... Moreover, the most efficacious FAAH inhibitors are carbamates, which appear to inactivate the enzyme by an irreversible mechanism in vivo [33]. Thus, the development of potent and selective reversible inhibitors of FAAH remains a major challenge for future research efforts. Fortunately, advances i ...
... Moreover, the most efficacious FAAH inhibitors are carbamates, which appear to inactivate the enzyme by an irreversible mechanism in vivo [33]. Thus, the development of potent and selective reversible inhibitors of FAAH remains a major challenge for future research efforts. Fortunately, advances i ...
European Heart Rhythm Association Practical Guide on the use of
... the different AF anticoagulation trials, there are still many under-explored aspects of NOAC that are relevant already today when these drugs are used by cardiologists, neurologists, geriatricians, and general practitioners. Each of the new NOACs entering the market will be accompanied by tools for ...
... the different AF anticoagulation trials, there are still many under-explored aspects of NOAC that are relevant already today when these drugs are used by cardiologists, neurologists, geriatricians, and general practitioners. Each of the new NOACs entering the market will be accompanied by tools for ...
INSILICO DRUG DESIGN AND MOLECULAR DOCKING STUDIES OF SOME NOVEL
... bacterial infection in human beings. The Objective of the study is too carried out the docking studies of benzothiazole derivatives containing oxadiazole groups or amino groups with known anti-cancer and anti-inflammatory targets like estrogen receptor, cox1 and cox2 by using Argus lab and Auto dock ...
... bacterial infection in human beings. The Objective of the study is too carried out the docking studies of benzothiazole derivatives containing oxadiazole groups or amino groups with known anti-cancer and anti-inflammatory targets like estrogen receptor, cox1 and cox2 by using Argus lab and Auto dock ...
Update for Nurse Anesthetists - American Association of Nurse
... fluid retention, increased insulin sensitivity, and antiinflammatory properties.2 Another advantage of ACE inhibitors is the minimal development of tolerance to their antihypertensive effect.18 Unlike other classes of antihypertensive drugs, ACE inhibitors do not cause orthostatic hypotension, rebou ...
... fluid retention, increased insulin sensitivity, and antiinflammatory properties.2 Another advantage of ACE inhibitors is the minimal development of tolerance to their antihypertensive effect.18 Unlike other classes of antihypertensive drugs, ACE inhibitors do not cause orthostatic hypotension, rebou ...
Part 1 - American Association of Nurse Anesthetists
... fluid retention, increased insulin sensitivity, and antiinflammatory properties.2 Another advantage of ACE inhibitors is the minimal development of tolerance to their antihypertensive effect.18 Unlike other classes of antihypertensive drugs, ACE inhibitors do not cause orthostatic hypotension, rebou ...
... fluid retention, increased insulin sensitivity, and antiinflammatory properties.2 Another advantage of ACE inhibitors is the minimal development of tolerance to their antihypertensive effect.18 Unlike other classes of antihypertensive drugs, ACE inhibitors do not cause orthostatic hypotension, rebou ...
Expert position paper on the use of proton pump inhibitors in
... Proton pump inhibitors have been shown to reduce warfarin metabolism and clearance leading to increased prothrombin time prolongation induced by warfarin.31,32 In studies of rats, a neutral or basic gastric pH was associated with faster warfarin absorption from the stomach into the plasma pool compa ...
... Proton pump inhibitors have been shown to reduce warfarin metabolism and clearance leading to increased prothrombin time prolongation induced by warfarin.31,32 In studies of rats, a neutral or basic gastric pH was associated with faster warfarin absorption from the stomach into the plasma pool compa ...
Antihypertensive Drugs 1
... the vasodilatatory benefit provided by bradykinin. ACE inibitors also block both AT1 and AT2, however ARBs only block AT1, it has been postulated that AT2 stimulation is renal protective. Angiotensin I may also be converted by enzymes other than ACE therefore ARBs may block more completely. Aldoster ...
... the vasodilatatory benefit provided by bradykinin. ACE inibitors also block both AT1 and AT2, however ARBs only block AT1, it has been postulated that AT2 stimulation is renal protective. Angiotensin I may also be converted by enzymes other than ACE therefore ARBs may block more completely. Aldoster ...
Interactive Association of Drugs Binding to Human
... drugs is the concerted rearrangement of Arg218 and Arg222, the principal effect of which is to substitute Arg222 instead of Arg218 as a binding partner for the carbonyl group of PLZ [53]. Additionally, Huang et al. think the presence of fatty acid is necessary for drugs’ co-binding in IIA subdomain ...
... drugs is the concerted rearrangement of Arg218 and Arg222, the principal effect of which is to substitute Arg222 instead of Arg218 as a binding partner for the carbonyl group of PLZ [53]. Additionally, Huang et al. think the presence of fatty acid is necessary for drugs’ co-binding in IIA subdomain ...
hMg-CoA-reductase inhibitors and neuropathy: reports to the
... as amiodarone, enalapril, hydralazine and the HMG-CoAreductase inhibitors.1 The overall prevalence of peripheral neuropathy is approximately 2400 per 100,000 population (2.4%), but in patients older than 55 years the prevalence rises to about 8000 per 100,000.12 Possible risk factors for developing ...
... as amiodarone, enalapril, hydralazine and the HMG-CoAreductase inhibitors.1 The overall prevalence of peripheral neuropathy is approximately 2400 per 100,000 population (2.4%), but in patients older than 55 years the prevalence rises to about 8000 per 100,000.12 Possible risk factors for developing ...
The rise and fall of the COX-2 inhibitors
... tomoxiprol, meclofenamate, sulindac and diclofenac have a less than five-fold selectivity to COX-2. 9,10 Nimesulide, celecoxib, meloxicam and etodolac have a five to fifty fold selectivity towards COX-2, whilst still producing full inhibition of COX-1. Rofecoxib has a greater than 50fold selectivity ...
... tomoxiprol, meclofenamate, sulindac and diclofenac have a less than five-fold selectivity to COX-2. 9,10 Nimesulide, celecoxib, meloxicam and etodolac have a five to fifty fold selectivity towards COX-2, whilst still producing full inhibition of COX-1. Rofecoxib has a greater than 50fold selectivity ...
Molecular Basis of Multidrug Transport by ATP
... the ester moieties are rapidly cleaved by intracellular esterases and the resulting carboxylates are not substrates for P-glycoprotein and LmrA (Homolya et al., 1993; Bolhuis et al., 1996a), and (iii) the kinetics of ATP-dependent transport of Hoechst 33342 by P-glycoprotein in insideout membrane ve ...
... the ester moieties are rapidly cleaved by intracellular esterases and the resulting carboxylates are not substrates for P-glycoprotein and LmrA (Homolya et al., 1993; Bolhuis et al., 1996a), and (iii) the kinetics of ATP-dependent transport of Hoechst 33342 by P-glycoprotein in insideout membrane ve ...
Word version of Full Report
... 23 Rivaroxaban SPAF Public Summary Document March 2013. Accessed on 15 April 2016. Available at: ...
... 23 Rivaroxaban SPAF Public Summary Document March 2013. Accessed on 15 April 2016. Available at: ...