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P. aeruginosa
P. aeruginosa

... Many infectious diseases once considered incurable and lethal are now may be treatment with them. The remarkably powerful and specific activity of antimicrobial drugs is due to their selectivity for targets that are either unique to microorganisms or much more important in them than in humans. Among ...
Antihypertensive Drugs 1
Antihypertensive Drugs 1

... aldosterone levels with treatment. In comparison to the ACE Inhibitors, the bradykinin levels are not elevated, this may prevent the cough associated with ACE but removes the vasodilatatory benefit provided by bradykinin. ACE inibitors also block both AT1 and AT2, however ARBs only block AT1, it has ...
The Organic Chemistry of Drug Design and Drug Action
The Organic Chemistry of Drug Design and Drug Action

... drug nebivolol, the (+)-isomer is a -blocker; the (-)-isomer causes vasodilation by a different mechanism. Therefore, it is sold as a racemate to take advantage of both vasodilating pathways. ...
Interaction of quinidine, disopyramide and
Interaction of quinidine, disopyramide and

... which is why some toxic effects of drug administration occur much faster [24, 25]. The drugs binding to melanin include sympathomimetic amines [26], antibiotics [27, 28], b-blockers [23, 29, 30], antimalarials [31–34], local anaesthetics [35, 36], and drugs acting on the central nervous system [31, ...
log P
log P

... QSAR study of other structural types of general anesthetics – each case a parabolic curve. Although constants are different, optimum hydrophobicity (log p0) – close to 2.3. Suggesting that all general anesthetics – act in a similar fashion (also, depend on hydrophobicity of structure) log p value of ...
Hutchison MediPharma R&D briefing Friday, 17 October 2014 9:30am to 1pm
Hutchison MediPharma R&D briefing Friday, 17 October 2014 9:30am to 1pm

... • Inadequate inhibition of primary target typically limits efficacy (e.g. Crizotinib) • Lack of potency means many compounds have high dose and poor PK (e.g. Lapatanib) • Precise mechanism of action still unclear in some patients (e.g. Sorafenib) ...
Aspirin - Learnblock
Aspirin - Learnblock

... • 1763 Edward Stone described efficacy of salicylate-containing plant extracts for the treatment of malarian fever and rheumatic complaints. • 1860 - salicylic acid was chemically synthesized by Kolbe • 1898 - acetylsalicylic acid used medicinally (aspirin - a from acetyl and spirin, an older name g ...
The rise and fall of the COX-2 inhibitors
The rise and fall of the COX-2 inhibitors

... arthritis. Gastro-intestinal toxicity represents some of the mostserious adverse drug reactions of this class of drugs. In an attempt to minimize these side-effects, selective cyclo-oxygenase-2 (COX-2) inhibitors were developed. In light of increasing concerns regarding their safety, two COX-2 inhib ...
bioassay screenings- importance in drug research
bioassay screenings- importance in drug research

... side chains (it requires the protein sample to be enriched in 15N). ...
Medicaid Approved Formulary Drug List
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... misuse or abuse potential, or have lower-cost alternatives. Brand-name drugs with generic equivalents available require prior authorization to encourage utilization of appropriate generic alternatives as first-line therapies. Prior to prescribing any brand-name medications, physicians are encouraged ...
vitekta - Gilead
vitekta - Gilead

... Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety assessment of VITEKTA is ...
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... Activator Protein-1 (AP-1) response element (5) was used for the functional study of EGF-stimulated signal transduction events in this pathway of interest. • Kinase inhibitors as well as RNAi were used for validation of the pathway, and to analyze possible combinatorial effects when used in tandem. • ...
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753_Module3_KidneyFunction

... Account for 7% of oxygen consumption in the body Filter 120 ml/min of plasma into nephron (measured by determining creatinine) Only 1% actually ends up in urine ** Something important must be going on ! Three primary roles for kidneys 1. Excrete metabolic end products and toxins 2. Control concentra ...
e-c - United Nations Interpreters
e-c - United Nations Interpreters

... 2. A substance, such as a metallic ion or coenzyme, that must be associated with an enzyme in order for the enzyme to function. 3. A situation or activity that may increase a person's susceptibility to AIDS. Examples of cofactors are: other infections, drug and alcohol use, poor nutrition, genetic f ...
Molecular determinants of drug–receptor binding kinetics
Molecular determinants of drug–receptor binding kinetics

... to be influenced more by short-range drug–receptor interactions such as hydrogen bonds, salt bridges and van der Waals (especially hydrophobic) contacts [22,23]. Binding of a charged acetylcholinesterase inhibitor, for instance, was 50-fold faster, and unbinding 10-fold slower, than that of a near ...
Antimicrobial Agents
Antimicrobial Agents

... • Dose of drug has to be sufficient to produce effect inhibit or kill the microorganism: • However concentration of the drug must remain below those that are toxic to human cells – • If can be achieved – microorganism susceptible to the ATB • If effective concentration is higher than toxicmicroorgan ...
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development of polymeric drug delivery systems for biotech products
development of polymeric drug delivery systems for biotech products

... Since the early 80’s the forward steps in genetics and proteomics, have led a particular interest to biotech products, such as DNA and proteins. Although difficult, their large-scale production enabled the therapeutic use of this compounds. Proteins and DNA sequences can be very interesting therapeu ...
Beware: Clinically Significant Drug Interactions in the Treatment of HIV
Beware: Clinically Significant Drug Interactions in the Treatment of HIV

... • Several medications in each ARV class are affected by ...
What`s in the Pipeline: New HIV Drugs
What`s in the Pipeline: New HIV Drugs

... TAG recently co-organized an international workshop, in conjunction with the National Institutes of Health (NIH) Office of AIDS Research (OAR), to develop scientific consensus on future directions in STI research, including the implications for when to start ART. There was a surprising consensus tha ...
Phage display for target-based antibacterial drug discovery
Phage display for target-based antibacterial drug discovery

... N-terminus. Short peptides (<10 amino acids) can also be The typical protocol for affinity selection, summarized displayed at the N-terminus of the major coat protein pVIII in Figure 1, begins with immobilization of the target on (Ref. 53). These simple phage-display systems are very usethe surface ...
Biochemistry 304 2014 Student Edition Enzymes and Enzyme
Biochemistry 304 2014 Student Edition Enzymes and Enzyme

... enzyme kinetics. •Know the Michaelis-Menten equation and how to plot it. •Understand the concepts of Km and Vmax. •Understand the Lineweaver-Burke Plot, be able to plot it and extract kinetic constants. Be aware that there are other types of kinetic plots •Understand enzyme reaction reversibility an ...
Statins induced myopathy
Statins induced myopathy

... lovastatin(mevacor- pro drug), simvastatin(zocorpro drug), pravastatin(pravachol) Second generation(10-20 mg/day) fluvastatin(lescol) Third generation atorvastatin(lipitor), cerivastatin(Baycol), rosuvastatin(crestor) ...
Bifunctional drugs for the treatment of asthma and chronic obstructive pulmonary disease
Bifunctional drugs for the treatment of asthma and chronic obstructive pulmonary disease

... It is now clear that the treatment of asthma and COPD can also benefit from the use of fixed-dose combinations of two or more drugs [8]. Today, the treatment of asthma and COPD globally is dominated by the use of inhaled fixed-dose combinations of a long-acting b2-agonist (LABA) and an inhaled corti ...
Inhibition of Amyloid Fibril Formation by Polyphenols: Structural
Inhibition of Amyloid Fibril Formation by Polyphenols: Structural

... polyphenols were suggested primarily by Yamada and coworkers (51). In this paper, they proposed that the compact and symmetric structure of curcumin and rosmarinic acid might be suitable for specific binding of free b-amyloid and inhibition of its polymerization into the fibrillar form (specific IC5 ...
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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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