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The importance of residence and recognition time of drug
The importance of residence and recognition time of drug

... slowest offrates – all with scaffold E had highest biological potency ...
Pharmacology Jeopardy Part 1
Pharmacology Jeopardy Part 1

... Ara-C – These agents are either antimetabolites, or interfere with purine or pyrimadine synthesis ...
Revised: April 2014 AN. 01865/2013 SUMMARY OF PRODUCT
Revised: April 2014 AN. 01865/2013 SUMMARY OF PRODUCT

... fluoroquinolones. They modulate the topological state of DNA through cleaving and resealing reactions. Initially, both strands of the DNA double helix are cleaved. Then, a distant segment of DNA is passed through this break before the strands are resealed. Target inhibition is caused by non-covalent ...
HIVTRI workshop: Treatment information for doctors and
HIVTRI workshop: Treatment information for doctors and

... May not have choice to wait ...
Epirubicin-Induced Oxidative DNA Damage and Evidence for Its
Epirubicin-Induced Oxidative DNA Damage and Evidence for Its

... Different anthracycline derivatives have been used successfully in the treatment of a wide spectrum of neoplasias for over two decades (1). Intracellular production of free radicals along with intercalation with DNA and subsequent inhibition of topoisomerase II is generally accepted as the major mec ...
Baytril 10% Oral Solution - Veterinary Medicines Directorate
Baytril 10% Oral Solution - Veterinary Medicines Directorate

... passed through this break before the strands are resealed. Target inhibition is caused by non-covalent binding of fluroquinolone molecules to an intermediate state in this sequence of reactions, in which DNA is cleaved, but both strands are retained covalently attached to the enzymes. Replication fo ...
Current trends in the development of antiviral drugs
Current trends in the development of antiviral drugs

... For hundreds of years, people were trying to find safe ways of the treatment of viral infections. But this was found to be very difficult due to the ability of viruses to use the host-cell in order to replicate, so the drugs may cause harm also to host cells.[4] Nevertheless, today some methods are ...
First Major European Viral Hepatitis Study Reports Serious Gaps in
First Major European Viral Hepatitis Study Reports Serious Gaps in

... The Hep-CORE Report was conducted under the direction of Prof. Jeffrey V. Lazarus of ISGlobal, University of Barcelona. According to Lazarus, “2016 has been a turning point for viral hepatitis thanks to the adoption of the first-ever WHO Global health sector strategy on viral hepatitis. The European ...
Basics of HIV Resistance and Testing
Basics of HIV Resistance and Testing

... High cost compared with other tests routinely used in HIV care Cannot be reliably performed when HIV RNA ...
Powerpoint
Powerpoint

... • We know even less about what side effects they might have - receptors are unknown • Drug discovery seems to be approached in a very consistent and conventional way • The cost of bringing a drug to market is huge ~$800M – drug reuse is a big business • The cost of failure is even higher e.g. Vioxx ...
Antiinfective drugs Chemotherapy: is the treatment of a disease by
Antiinfective drugs Chemotherapy: is the treatment of a disease by

... Mechanism of action: They inhibit protein synthesis by irreversible binding to 30S which lead to misread the genetic code and production of false protein. Activity: They are effective against aerobic organim, since anaerobes lack the oxygen-requiring transport system which is necessory to transport ...
3. antibacterial2
3. antibacterial2

... active mainly against Gram-positive bacteria. It acts by inhibiting bacterial protein synthesis . • As the sodium salt, the drug is well absorbed from the gut and is distributed widely in the tissues. Some is excreted in the bile and some metabolized. • Unwanted effects such as gastrointestinal dist ...
Untitled
Untitled

... Revised II semester syllabus paper-II (2014-2015) Unit:I Drug Design and Drug Discovery (15 periods) Introduction to drug discovery. Folklore drugs, stages involved in drug discovery- disease, drug targets, bioassay. Chiral drugs: Role of chirality on biological activity: examples of Distomers – a) ...
targeting estrogen receptor sites in human breast cancer
targeting estrogen receptor sites in human breast cancer

... Kdtolrofen thiosemicarbazone (IV) was prepared by reacting I (0.254g, 0.001mole) and thiosemicarbazide (0.091g, 0.001mole) both dissolfed in methanol (10 ml) with one drop of concentrated hydrochloric acid and bringing the reaction mixare to a reflux on the water batfi for two hours. A white colored ...
C
C

... vascular disease.[5] In addition, ALLHAT participants randomised to lisinopril experienced a higher risk of stroke, combined cardiovascular disease and angioedema than those assigned to the calcium channel antagonist amlodipine, but conversely experienced less heart failure.[5,6] In general, ACE inh ...
2016 International Symposium on Chemical Biology of the
2016 International Symposium on Chemical Biology of the

... (rapalogues), which act as allosteric inhibitors. More recently, ATP-competitive inhibitors that directly target the active site of the mTOR kinase domain were developed. Both types of drugs may easily lose their potency by single point mutations in the respective binding domains. Based on the recen ...
PREMEDICATION DRUGS
PREMEDICATION DRUGS

...  Enhance the hypnotic effects of G.A agents  Reduce P.O.N.V  Prodcuce amnesia  Prevent aspiration  Attenuate vagal reflexes  Attenuate sympathoadrenal response ...
Drug Interactions
Drug Interactions

... Ciprofloxin increases clozapine levels threefold Estrogen containing oral contraceptives or replacement hormones moderately inhibit 1A2 leading to toxicities with use of caffeine, clozapine and haldol. ...
anti-depressants
anti-depressants

... Monoamine Oxidase Inhibitors: MAO is a mitochondrial enzyme found in nerve and other tissues, such as the liver and gut. The MAO inhibitors may reversibly or irreversibly inactivate the enzyme, permitting neurotransmitter molecules to escape degradation and, therefore, to both accumulate within the ...
Bio05 Enzymes
Bio05 Enzymes

... • The 2nd part of an enzymes name tells us the type of reaction it facilitates. • The 3rd part of an enzymes name is “-ase”. This indicates that the molecule is an enzyme. ...
Current Concepts in Antiretroviral Therapy Failure - IAS-USA
Current Concepts in Antiretroviral Therapy Failure - IAS-USA

... had lower baseline viral load, and who had an absence of an AIDS diagnosis, and among men who reported having sex with men as a risk factor. It is important to note, however, that in many US clinics there are increasing numbers of patients who have acquired HIV through injection drug use or who are ...
Enzymes, Coenzymes, And Energy
Enzymes, Coenzymes, And Energy

... • A new, temporary molecule called the enzymesubstrate complex is formed. • Enzymes are specific to certain substrate molecules because their shape can only combine with specific parts of certain molecules. ...
Interferons
Interferons

... • It inhibits the replication of a variety of RNA and DNA viruses and is serves as an immunomodulator to enhance type 1 cytokine production. This increases the end of treatment response and reduces ...
Fluoroquinolones and Uroseptics
Fluoroquinolones and Uroseptics

... Generally, bacteria has circular DNA. During replication, this circular DNA needs few enzymes for it to be replicated. They are o Helicase  Use in unwinding the double helix DNA to form the repilcation fork  It also stabilizes the unwinded DNA strands so that it wont stick back together o DNA Gyra ...
treatment of gastrointestinal ulcers
treatment of gastrointestinal ulcers

... the risk of GI ulceration in animals predisposed to ulcer formation.  Cytoprotective agents include antacids and sucralfate. Antacids are weak bases that neutralize gastric acid within the stomach lumen; they may also promote gastric prostaglandin production. ...
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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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