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Understanding and Managing Drug Interactions in HIV Disease
Understanding and Managing Drug Interactions in HIV Disease

... benefit. This is especially problematic, given that cross-class resistance among PIs is common. In general, patients failing therapy with one PI often do not experience sustained benefit from switching to another PI; (NB: an exception to this is with nelfinavir, where the presence of an isolated D30 ...
Genvoya - Gilead
Genvoya - Gilead

... ----------------------------INDICATIONS AND USAGE---------------------------GENVOYA is a four-drug combination of elvitegravir, an HIV-1 integrase strand transfer inhibitor (INSTI), cobicistat, a CYP3A inhibitor, and emtricitabine and tenofovir alafenamide (TAF), both HIV1 nucleoside analog reverse ...
Antibacterial Agents which Act Against Cell Metabolism
Antibacterial Agents which Act Against Cell Metabolism

...  Therefore, two enzymes in the one biosynthetic route are inhibited.  This is a very effective method of inhibiting a biosynthetic route and has the advantage that the doses of both drugs can be kept down to safe levels. To get the same level of inhibition using a single drug, the dose level of th ...
Inhibiting the breakdown of endogenous opioids and
Inhibiting the breakdown of endogenous opioids and

... opioid system, which has a key role in discriminating between innocuous and noxious sensations2,3. However, chronic pain can occur after several pathophysiological processes, as well as without any identifiable cause (such as in fibromyalgia)4. One example is neuropathic pain — a frequent complicati ...
The Structure, Function, and Inhibition of Influenza Virus
The Structure, Function, and Inhibition of Influenza Virus

... NSW 2582, Australia. Viral Membrane Proteins: Structure, Function, and Drug Design, edited by Wolfgang Fischer. Kluwer Academic / Plenum Publishers, New York, 2005. ...
Natural Flavonoids Isolated From the Leaves of Enhydra
Natural Flavonoids Isolated From the Leaves of Enhydra

... has been reported to have antidiarrheal activity (Uddin et al., 2005). Recently, the free-radical scavenging potential of crude extract and different fractions have been reported (Sannigrahi et al., 2010a). Ethyl's acetate fraction of the plant exhibits anticancer activity against EAC cell in mice ( ...
Antidiabetic drugs
Antidiabetic drugs

... evidence of autoimmunity). This form is more common among individuals of African and Asian origin. Patients periodically develop ketoacidosis. ...
Allosteric Binding Sites on Muscarinic Acetylcholine Receptors
Allosteric Binding Sites on Muscarinic Acetylcholine Receptors

... the affinity of the endogenous ligand for the orthosteric site (such allosteric agents are also referred to as allosteric enhancers or inhibitors, respectively) and/or for exogenously applied orthosteric ligands. During the past decade, considerable efforts have been focused on developing novel ther ...
Pharmacologyonline 3: 201-216 (2006) Kumarappan et al. CT
Pharmacologyonline 3: 201-216 (2006) Kumarappan et al. CT

... market. Despite the successes that have been achieved over the years with natural products as a platform for drug discovery has waxed and waned in popularity with various pharmaceutical companies. Natural products today are most likely going to continue to exist and grow to become even more valuable ...
Type 2 Diabetes
Type 2 Diabetes

...  TZDs alone or in combination are associated with a higher risk of fractures compared to other agents (high strength of evidence). In 2007, the FDA issued an alert and changed labeling to state that TZDs cause or exacerbate CHF in some patients. In 2010, the FDA placed additional prescribing restri ...
Interactive Properties of Tizanidine (Zanaflex)
Interactive Properties of Tizanidine (Zanaflex)

... healthy subjects, pretreatment with fluvoxamine (100 mg/day for 4 days) resulted in a dramatic 33-fold increase in tizanidine area under the plasma concentration–time curve (AUC).1 The marked increases in tizanidine plasma concentrations were accompanied by pharmacodynamic changes, such as marked re ...
Functional analyses and molecular modeling of two c-Kit mutations
Functional analyses and molecular modeling of two c-Kit mutations

... work (Pricl et al., 2005). Accordingly, only a brief outline of the method is reported. All simulations were carried out using the Sander modulus of AMBER 7.0 (Case et al., 2000) and the Cornell et al. (1995) force field. The 1.60-Å-resolution coordinates of the kinase domain of KIT in complex with ...
Macrolids
Macrolids

... The prototype drug, erythromycin, which consists of two sugar moieties attached to a 14-atom lactone ring, was obtained in 1952 from Streptomyces erythreus. Clarithromycin and azithromycin are semisynthetic derivatives of erythromycin. ...
APTAMERS ROLE IN BASIC DRUG RESEARCH AND DEVELOPMENT - AN... Review Article  STALIN.C*, DINESHKUMAR.P.
APTAMERS ROLE IN BASIC DRUG RESEARCH AND DEVELOPMENT - AN... Review Article STALIN.C*, DINESHKUMAR.P.

... Since the introduction of the technology for isolation of nucleic acid Aptamers in 1990, there has been a steady annual increase in the number of publications related to Aptamers. During the last 10 years Aptamers binding to for example cells, proteins, peptides, low molecular weight molecules (like ...
Genvoya - Gilead
Genvoya - Gilead

... • Warnings and Precautions, Fat Redistribution [removed] ...
efavirenz - WHO archives - World Health Organization
efavirenz - WHO archives - World Health Organization

... In Argentina a program similar to that of Brazil provides even greater coverage. A special fund has been established to pay for antiretroviral drugs for those not covered by social security (such as street vendors, small business people, the unemployed, low-income pregnant women) 5. Through the UNAI ...
Insert Slide Title Here - Academy for Infection Management
Insert Slide Title Here - Academy for Infection Management

... Nucleic acid synthesis inhibitors • Antibiotics that inhibit bacterial nucleic acid synthesis include: – precursor synthesis inhibitors: sulphonamides, trimethoprim – DNA replication inhibitors: quinolones – RNA polymerase inhibitors: rifampicin ...
KIRGANELIA RETICULATA CARRAGEENAN
KIRGANELIA RETICULATA CARRAGEENAN

... attributed in part to kinins, prostaglandins, neutrophils, and lipoxygenase products of arachidonic acid metabolism. The probable mechanism of anti-inflammatory action of extract may be due to its influence on the second phase of inflammation, the cyclooxygenase pathway rather than the lipoxygenase ...
Pancreatic Lipase Inhibition IC 50 Chemicals.
Pancreatic Lipase Inhibition IC 50 Chemicals.

... the small intestine, which may be achieved by inhibiting pancreatic lipase. The pharmaceutical orlistat is a commonly prescribed pancreatic lipase inhibitor shown to be effective in treating obesity and hyperlipidemia. However, many gastrointestinal side effects have been associated with orlistat (m ...
Draft Guidance for Industry Drug Interaction Studies
Draft Guidance for Industry Drug Interaction Studies

... the liver or gut mucosa, or by excretion, usually by the kidneys and liver. In addition, protein therapeutics may be eliminated through a specific interaction with cell surface receptors, followed by internalization and lysosomal degradation within the target cell. Hepatic elimination occurs primari ...
Click Chemistry in Carbohydrate
Click Chemistry in Carbohydrate

... Many of the carbohydrate-based drugs currently in clinical use are indeed mimics of endogenous carbohydrates and act as inhibitors of carbohydrate-protein binding events or modulators of glycan metabolism (Table 1.1).2-4,7,9 Carbohydrates linked to many natural products are often a prerequisite for ...
zidovudine and lamivudine - WHO archives
zidovudine and lamivudine - WHO archives

... on the WHO Model List of Essential Medicines Both drugs are members of the therapeutic class of HIV nucleoside analogue reverse transcriptase inhibitors Summary of Proposal Since the first clinical evidence of AIDS was reported over twenty years ago, an estimated 25 million people have died as a res ...
Inhaled phosphodiesterase type 5 inhibitors restore chloride transport in cystic fibrosis mice
Inhaled phosphodiesterase type 5 inhibitors restore chloride transport in cystic fibrosis mice

... molecular and biological mechanisms underlying cystic fibrosis (CF) lung disease has resulted in exciting new targets for treatment. Fundamental research focusing on correcting F508del mutant protein can be considered as disease-modifying approaches and would be beneficial for most CF patients. Inde ...


... of ex vivo LTB4 production by leukocytes. ABT-761 (R(+)-N- (3- (5-( 4-fluorophenylmethyl )-2thi-enyl)-1-methyl-2-propynyl)-N-hydroxy-urea) is a novel, se-cond generation 5-LO inhibitor. In previous studies, a single dose of 200 mg ABT-761 has been shown to inhibit LTB4 release from human neutrophils ...
INTERACTION BETWEEN GRAPEFRUIT JUICE AND DRUGS*
INTERACTION BETWEEN GRAPEFRUIT JUICE AND DRUGS*

... Orange juice is not associated with the inhibitory actions described above. Because the expression of a molecular species of CYP3A is reduced by grapefruit juice, it is evident that this inhibition is not a simple competitive action on the metabolism of the substrate. Grapefruit juice reduced the po ...
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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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