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Antimycobacterial Drugs (抗分枝杆菌药)
Antimycobacterial Drugs (抗分枝杆菌药)

... clearance is less than 30 mL/min or the patient is on hemodialysis, the dose is 15 mg/kg two or three times per week. Most tubercle bacilli are inhibited by streptomycin, 1–10 mcg/mL, in vitro. Nontuberculosis species of mycobacteria other than Mycobacterium avium complex (MAC) and Mycobacterium kan ...
Selective Serotonin Reuptake Inhibitors (SSRIs) with Dual
Selective Serotonin Reuptake Inhibitors (SSRIs) with Dual

... relieve the symptoms of repetitive behaviors. However, the elevated 5-HT level also stimulates inhibitory autoreceptors (5-HT1B/1D) which by definition, regulate the release of 5-HT in an inhibitory manner and negatively affect the mode of action of SSRIs [5,6]. It is, thus, anticipated that coadmin ...
Welcome to Week 6 Chapter 10 - Lead Discovery 10.1 In Vitro
Welcome to Week 6 Chapter 10 - Lead Discovery 10.1 In Vitro

... put through a battery of tests ‐ the filtering process that we discussed in sections 10.3, 10.4, and  10.5 ‐ to make sure that only the most promising compounds are advanced as leads.  Once a lead, a  molecule will require more and more resources from the pharmaceutical company.  One aspect of lead  ...
GIST clinical trials - The Life Raft Group
GIST clinical trials - The Life Raft Group

... Where is the trial site? Am I eligible to go there? How often to I have to go there? For how long? At what costs? ...
PRC2 crystal clear Epigenetic mechanisms control the combination
PRC2 crystal clear Epigenetic mechanisms control the combination

... into solving the EZH2 structure. What makes this enterprise particularly challenging is that EZH2 is active only when it is part of a larger, multi-protein complex called polycomb repressive complex 2 (PRC2). Other components of the PRC2 complex include EED, SUZ12 and RBBP4. In particular, EED and a ...
Beta-lactams_E
Beta-lactams_E

... be given 20 to 40 mg/kg/d up to a maximum of 1 g/d. Except for cefuroxime axetil, these drugs are not predictably active against penicillin-resistant pneumococci and should be used cautiously, if at all, to treat suspected or proved pneumococcal infections. Cefaclor is more susceptible to β-lactamas ...
Indirect cholinergic agonists
Indirect cholinergic agonists

... -Drugs differ in their CNS effects, scopolamine permeates the blood-brain barrier -At therapeutic doses atropine has negligible effects upon the CNS, scopolamine even at low doses has prominent CNS effects. ...
PHARMACOTHERAPY OF HYPERTENSION
PHARMACOTHERAPY OF HYPERTENSION

... ACE inhibitors increase plasma levels of digoxin and lithium (dosage adjustment is necessary) Increase hypersensitivity reactions to allopurinol. Contraindications: Bilateral renal artery stenosis and pregnancy ...
Structure-based drug design meets the ribosome
Structure-based drug design meets the ribosome

... rapidly, in both, hospital and community settings [1]. Yearly, approximately 90,000 hospital patients in the United States die as a result of a bacterial infection. This death rate increased almost an order of magnitude since 1992, when it was 13,300 [1]. In over 70% of these bacterial infections, t ...
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... Norepinephrine reuptake inhibitors (NRIs), also known as noradrenaline reuptake inhibitors (NARIs), are compounds that elevate the extracellular level of the neurotransmitter norepinephrine in the central nervous system by inhibiting its reuptake from the synaptic cleft into the presynaptic neuronal ...
Infection, Genetics and Evolution
Infection, Genetics and Evolution

... HIV-1 drug resistance resulting from antiretroviral therapy far exceeds that from pre-exposure prophylaxis ...
VIRTUAL SCREENING AND LEAD OPTIMIZATION TO IDENTIFY
VIRTUAL SCREENING AND LEAD OPTIMIZATION TO IDENTIFY

... structures for structure-based drug design methods, and to model the docking of compounds and their target proteins. The need for ongoing development of new drugs needs to emphasis in light of the current global situation of health and disease. Traditionally, the process of drug development has rev ...
maximizing the effectiveness of highly active
maximizing the effectiveness of highly active

... Although many highly active antiretroviral therapy (HAART) regimens using 3 drugs have demonstrated potent and durable antiretroviral effects, cohort studies have shown that treatment failure occurs in about 30% to 50% of patients. This failure rate prompts a closer look into the causes of treatment ...
Department of Pharmacology
Department of Pharmacology

...  dr hab. Przemysław Mikołajczak, prof. UM  is available most Tuesday’s between 11.30-12.30  an appointment should be made by e-mail ([email protected]) Schedule coordinator and students affairs:  dr hab. Marzena Dworacka, prof. UM  is available most Thursday’s between 12.00-13.30  an appoint ...
BALANCING ANTI-AMYLOID AND ANTI-CHOLINESTERASE CAPACITY IN A SINGLE CHEMICAL INSILICO Research Article
BALANCING ANTI-AMYLOID AND ANTI-CHOLINESTERASE CAPACITY IN A SINGLE CHEMICAL INSILICO Research Article

... Alzheimer’s disease (AD), the most common form of dementia, is a complex neurodegenerative disorder [1, 2]. The fact that complexity and multiple etiologies of AD make single-target strategy difficult to shed desirable therapeutic effect makes the choice of Multi-TargetDirected Ligand (MTDL) to be a ...
Rib_Inh_15
Rib_Inh_15

... In vivo, a series of enzymatic steps converts dihydrostreptose and streptidine 6-phosphate into streptomycin. European Journal of Biochemistry. 1980, 105:139-144. ...
Angiotensin-Converting Enzyme Inhibitors
Angiotensin-Converting Enzyme Inhibitors

... ACE Inhibitors Post MI Subgroup analysis of SAVE (Uniformity of Captopril in SAVE Study) and TRACE (Trandolapril Cardiac Evaluation Study- ACE post MI) document beneficial effect of long term use of ACE inhibitors post MI  Beneficial effects in preventing LVH and Heart failure persist even when an ...
Suggestion from clinicians
Suggestion from clinicians

... are insufficient data over a broad dose range. It is therefore impossible with this analysis to be certain that there are no blood pressure lowering differences between one or more of the drugs. It would require headto-head trials of different ACE inhibitors at equivalent BP lowering doses to assess ...
Treatment of Cough
Treatment of Cough

... Treatment of Cough 1. Antitussive a. Opioid i. Codeine (methylmorphine) b. Non – opioid i. Dextromethorphan 2. Expectorant a. Guaifenesin 3. Mucolytics a. N – actylcysteine b. Bromhexine c. Ambroxol (active metabolite of Bromhexine) ...
Click here for the PowerPoint presentation
Click here for the PowerPoint presentation

... After attending the lecture and discussion, the attendee should be able to: Compare and contrast newly approved drugs with older agents regarding their pharmacology, pharmacokinetics, efficacy, safety, dosage and cost. Apply the “formulary approach” to evaluating new drugs. Analyze potential util ...
Thrombin = anticoagulant
Thrombin = anticoagulant

... • Which class of drugs will be better ? – This question will remain unanswered until the appropriate head-to-head clinical trials are performed. – At the moment, both classes appear promising. ...
File - Developing Anaesthesia
File - Developing Anaesthesia

... Factor Xa acts as an amplifier, generating more than 1000 molecules of thrombin for each molecule of Factor Xa. Rivaroxaban is an orally active highly selective direct Factor Xa inhibitor. By this action Prothrombin is prevented from converting to thrombin, (see appendix 1 below). This action is in ...
BIOASSAY SCREENINGS- IMPORTANCE IN DRUG RESEARCH
BIOASSAY SCREENINGS- IMPORTANCE IN DRUG RESEARCH

... side chains (it requires the protein sample to be enriched in 15N). ...
Inhibition of Purified Factor Xa Amidolytic Activity May Not Be
Inhibition of Purified Factor Xa Amidolytic Activity May Not Be

... position. As shown in Figure 1, all of the chosen compounds were capable of inhibition of fXa at low nanomolar concentrations and, when assayed in the same concentration range, did not cross-react with the related serine protease thrombin. Representative inhibitors from the 3 classes (C2092-28, C194 ...
Department of Pharmacology
Department of Pharmacology

... o The whole course of the seminars is considered successfully completed and the student earns a credit if the following condition is met:  A student gains a minimum grade of 3.0 calculated as a mean value from all the Component Tests they wrote (each student must take the Component Test at the end ...
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Discovery and development of integrase inhibitors

The first human immunodeficiency virus (HIV) case was reported in the United States in the early 1980s. Many drugs have been discovered to treat the disease but mutations in the virus and resistance to the drugs make development difficult. Integrase is a viral enzyme that integrates retroviral DNA into the host cell genome. Integrase inhibitors are a new class of drugs used in the treatment of HIV. The first integrase inhibitor, raltegravir, was approved in 2007 and other drugs were in clinical trials in 2011.
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