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Gentamicin
... by a large number of gram-negative organisms. It usually is used in combination with a second agent, because an aminoglycoside alone may not be effective for infections outside the urinary tract. • Gentamicin is of the first choice when these infections occurs 1) urinary tract infections, bacteremia ...
... by a large number of gram-negative organisms. It usually is used in combination with a second agent, because an aminoglycoside alone may not be effective for infections outside the urinary tract. • Gentamicin is of the first choice when these infections occurs 1) urinary tract infections, bacteremia ...
Pathway-Dependent Inhibition of Paclitaxel Hydroxylation by Kinase
... thought to be associated with different expressions and activities of CYP2C8, CYP3A4, and P-gp, and numerous studies have been conducted to examine the role of polymorphisms in CYP enzymes and their relationship with intersubject variability in efficacy and neurotoxicity. Recent reports suggest that ...
... thought to be associated with different expressions and activities of CYP2C8, CYP3A4, and P-gp, and numerous studies have been conducted to examine the role of polymorphisms in CYP enzymes and their relationship with intersubject variability in efficacy and neurotoxicity. Recent reports suggest that ...
Investigating Differences in Solubility between Crystalline
... •Poor solubility, poor absorption of drugs into the body, poor bioavailability. • Solubility is pH dependent, so is determined at physiologically relevant pH. • Increasingly more drugs with poor solubility being made. • Solubility determined early in the drug discovery process, to assess risks invol ...
... •Poor solubility, poor absorption of drugs into the body, poor bioavailability. • Solubility is pH dependent, so is determined at physiologically relevant pH. • Increasingly more drugs with poor solubility being made. • Solubility determined early in the drug discovery process, to assess risks invol ...
triumeq - GSK Source
... [INSTI]), abacavir, and lamivudine (both nucleoside analogue reverse transcriptase inhibitors) is indicated for the treatment of HIV-1 infection. (1) Limitations of Use: • TRIUMEQ alone is not recommended for use in patients with current or past history of resistance to any components of TRIUMEQ. (1 ...
... [INSTI]), abacavir, and lamivudine (both nucleoside analogue reverse transcriptase inhibitors) is indicated for the treatment of HIV-1 infection. (1) Limitations of Use: • TRIUMEQ alone is not recommended for use in patients with current or past history of resistance to any components of TRIUMEQ. (1 ...
PHARM4515-16 (NSAIDs)
... Mechanism of Action Inhibitors of cyclooxygenase reduce the amount of Prostaglandins and thereby reduce the inflammation process primary insult: Unionized at stomach pH that allows passage into gastric mucosal cells. The inside higher pH ionize them which can not pass through lipid barriers and is ...
... Mechanism of Action Inhibitors of cyclooxygenase reduce the amount of Prostaglandins and thereby reduce the inflammation process primary insult: Unionized at stomach pH that allows passage into gastric mucosal cells. The inside higher pH ionize them which can not pass through lipid barriers and is ...
elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
... displayed antiviral activity in vitro against HIV-1 clades A, C, D, E, F, and G (IC50 values ranged from 0.007 to 0.075 M) and showed strain specific activity against HIV2 (IC50 values ranged from 0.007 to 1.5 M). Tenofovir alafenamide: The antiviral activity of tenofovir alafenamide against labor ...
... displayed antiviral activity in vitro against HIV-1 clades A, C, D, E, F, and G (IC50 values ranged from 0.007 to 0.075 M) and showed strain specific activity against HIV2 (IC50 values ranged from 0.007 to 1.5 M). Tenofovir alafenamide: The antiviral activity of tenofovir alafenamide against labor ...
Cephalosporins
... Many cephalosporins are administered parenterally because they aren’t absorbed from the GI tract. Some cephalosporins are absorbed from the GI tract and can be administered orally, but food usually decreases the absorption rate of these oral cephalosporins, though not the amount absorbed. Two cephal ...
... Many cephalosporins are administered parenterally because they aren’t absorbed from the GI tract. Some cephalosporins are absorbed from the GI tract and can be administered orally, but food usually decreases the absorption rate of these oral cephalosporins, though not the amount absorbed. Two cephal ...
Mycobacterium tuberculosis from Tshwane Metropolitan OLUWASEGUN OLAYINKA ATANDA
... Tuberculosis (TB) is a chronic airborne infectious disease caused by Mycobacterium tuberculosis and primarily affects the lungs. In 2012 the World Health Organisation (WHO) estimated 2 billion people, 8.3 new cases and 1.3 million deaths (WHO, 2013). South Africa has a particularly high burden of TB ...
... Tuberculosis (TB) is a chronic airborne infectious disease caused by Mycobacterium tuberculosis and primarily affects the lungs. In 2012 the World Health Organisation (WHO) estimated 2 billion people, 8.3 new cases and 1.3 million deaths (WHO, 2013). South Africa has a particularly high burden of TB ...
An Update on Artemisinin- A Multifaceted Drug
... humans, even against highly drug resistant strains of Plasmodium sp. Artemisinins act more rapidly than other types of antimalarials, both in killing the parasites and in inhibiting their major metabolic processes, such as glycolysis, nucleic acid and protein synthesis. The naturally rare endoperoxi ...
... humans, even against highly drug resistant strains of Plasmodium sp. Artemisinins act more rapidly than other types of antimalarials, both in killing the parasites and in inhibiting their major metabolic processes, such as glycolysis, nucleic acid and protein synthesis. The naturally rare endoperoxi ...
HIV/AIDS Guidelines
... Considerations for Antiretroviral Use in Special Patient Populations ........................................I-1 Acute HIV Infection .....................................................................................................................I-1 Table 10. Identifying, Diagnosing, and Managin ...
... Considerations for Antiretroviral Use in Special Patient Populations ........................................I-1 Acute HIV Infection .....................................................................................................................I-1 Table 10. Identifying, Diagnosing, and Managin ...
Click Chemistry in Carbohydrate
... products possessing anti-microbial and anti-cancer properties, such as the aminoglycosides, saponins and anthracyclines. 10 Despite the plethora of disease states that involve carbohydrate-recognition phenomena, comparatively few carbohydratebased drugs are in clinical use. The failure of many carbo ...
... products possessing anti-microbial and anti-cancer properties, such as the aminoglycosides, saponins and anthracyclines. 10 Despite the plethora of disease states that involve carbohydrate-recognition phenomena, comparatively few carbohydratebased drugs are in clinical use. The failure of many carbo ...
Application of NMR and Molecular Docking in Structure
... evaluating ADME-toxicology [25–27], and identifying and validating therapeutic targets [28, 29]. Nevertheless, there are still intrinsic costs to maintaining an NMR instrument, screening a compound library, and producing significant quantities of a protein. One way to significantly reduce experiment ...
... evaluating ADME-toxicology [25–27], and identifying and validating therapeutic targets [28, 29]. Nevertheless, there are still intrinsic costs to maintaining an NMR instrument, screening a compound library, and producing significant quantities of a protein. One way to significantly reduce experiment ...
Drugs: Safety and Effectiveness
... safety and effectiveness. That postapproval (postmarket) phase lasts as long as the drug is on the market. Beginning with the Food and Drugs Act of 1906, Congress has incrementally refined and expanded FDA’s responsibilities regarding drug approval and regulation. The progression to drug approval be ...
... safety and effectiveness. That postapproval (postmarket) phase lasts as long as the drug is on the market. Beginning with the Food and Drugs Act of 1906, Congress has incrementally refined and expanded FDA’s responsibilities regarding drug approval and regulation. The progression to drug approval be ...
The impact of penicillin on therapeutic outcomes
... andhadinvivoactivityinmice.Ithadonly0.1%oftheactivityofpenicillinGagainstsensitivestaphylococci,although itsactivityagainstGramͲnegativebacteriaequaledthatofpenicillinG. AlthoughneitherpenicillinNnorcephalosporinCwasevercommercialized,theyledtoimportantkn ...
... andhadinvivoactivityinmice.Ithadonly0.1%oftheactivityofpenicillinGagainstsensitivestaphylococci,although itsactivityagainstGramͲnegativebacteriaequaledthatofpenicillinG. AlthoughneitherpenicillinNnorcephalosporinCwasevercommercialized,theyledtoimportantkn ...
Mechanism-based Inhibition: Deriving KI and kinact
... Germany) based on the method described by GENTEST with slight modifications as described in summary below. All incubations were performed in either 50 mM (CYP 1A2) or 200 mM (CYP 3A4) potassium phosphate buffer at pH 7.4 containing 8.1 µM NADP+, 0.41 mM MgCl2, 0.4 mM glucose-6phosphate and 0.2 IU/ml ...
... Germany) based on the method described by GENTEST with slight modifications as described in summary below. All incubations were performed in either 50 mM (CYP 1A2) or 200 mM (CYP 3A4) potassium phosphate buffer at pH 7.4 containing 8.1 µM NADP+, 0.41 mM MgCl2, 0.4 mM glucose-6phosphate and 0.2 IU/ml ...
Emtricitabine / rilpivirine / tenofovir disoproxil fumarate
... Emtricitabine: a synthetic nucleoside analogue of cytidine, is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate. Emtricitabine 5'-triphosphate inhibits the activity of the HIV-1 RT by competing with the natural substrate deoxycytidine 5'-triphosphate by being incorporated int ...
... Emtricitabine: a synthetic nucleoside analogue of cytidine, is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate. Emtricitabine 5'-triphosphate inhibits the activity of the HIV-1 RT by competing with the natural substrate deoxycytidine 5'-triphosphate by being incorporated int ...
abstracts
... to treat a variety of diseases ranging from cancer, autoimmune diseases to metabolic diseases. Albeit their huge potentials, one of the major hurdles has yet to overcome is drug delivery problem. Unlike small drug molecules, these drugs cannot be given orally because they are destroyed extensively b ...
... to treat a variety of diseases ranging from cancer, autoimmune diseases to metabolic diseases. Albeit their huge potentials, one of the major hurdles has yet to overcome is drug delivery problem. Unlike small drug molecules, these drugs cannot be given orally because they are destroyed extensively b ...
PDF - AIDS Research and Therapy
... combination formulations and does not require laboratory monitoring for toxicity. In 2006, WHO recommended reduced doses of stavudine following the findings of a systematic review that lower doses caused less toxicity without reducing efficacy [1,5]. Most, if not all, of stavudine’s adverse drug rea ...
... combination formulations and does not require laboratory monitoring for toxicity. In 2006, WHO recommended reduced doses of stavudine following the findings of a systematic review that lower doses caused less toxicity without reducing efficacy [1,5]. Most, if not all, of stavudine’s adverse drug rea ...
Modifying effects of boswellia carteri on clarithromycine action: In
... inhibition of Boswellia carteri ranged from 6mmfor Pseudomonas aeruginosa to 14mm for Klebsiella pneumonia the p value was insignificant p ˃0.05 but the combined mixture showed significant differences from either clarithromycine or boswellia carteri p ˂0.05. The MIC ranged from 8-32mg/ml,8-64mg/ml a ...
... inhibition of Boswellia carteri ranged from 6mmfor Pseudomonas aeruginosa to 14mm for Klebsiella pneumonia the p value was insignificant p ˃0.05 but the combined mixture showed significant differences from either clarithromycine or boswellia carteri p ˂0.05. The MIC ranged from 8-32mg/ml,8-64mg/ml a ...
FDA Enforcement of Criminal Liability for Clinical
... effective. The process usually begins with Phase I clinical studies, 25. See 21 U.S.C. § 355(a) (“No person shall introduce or deliver for introduction into interstate commerce any new drug, unless an approval of an application . . . is effective with respect to such drug.”). Medical devices and bio ...
... effective. The process usually begins with Phase I clinical studies, 25. See 21 U.S.C. § 355(a) (“No person shall introduce or deliver for introduction into interstate commerce any new drug, unless an approval of an application . . . is effective with respect to such drug.”). Medical devices and bio ...
Morphine - ISpatula
... *Methadone is orally active, has similar activity to morphine, but is less euphorigenic and has a longer duration of action. Although it is as potentially addictive as morphine, the withdrawal symptoms are different and much less severe than with other drugs such as heroin, so that methadone and Bup ...
... *Methadone is orally active, has similar activity to morphine, but is less euphorigenic and has a longer duration of action. Although it is as potentially addictive as morphine, the withdrawal symptoms are different and much less severe than with other drugs such as heroin, so that methadone and Bup ...
View/Open
... sequencing, the coding sequence of Plasmodium berghei multidrug resistance gene 1 (PbMDR-1) was analyzed, which is orthologous to the gene associated with quinoline resistance in Plasmodium falciparum. The results did not show any nucleotide polymorphism within the coding region. Further broader seq ...
... sequencing, the coding sequence of Plasmodium berghei multidrug resistance gene 1 (PbMDR-1) was analyzed, which is orthologous to the gene associated with quinoline resistance in Plasmodium falciparum. The results did not show any nucleotide polymorphism within the coding region. Further broader seq ...
as PDF
... compounds cause damage to DNA by different mechanisms such as alkylation or other interactions that can lead to mutation of the genetic codes. In general, chemists employ the terms "genotoxic" and "mutagenic" synonymously; however, there is a subtle distinction. Genotoxicity pertains to all types of ...
... compounds cause damage to DNA by different mechanisms such as alkylation or other interactions that can lead to mutation of the genetic codes. In general, chemists employ the terms "genotoxic" and "mutagenic" synonymously; however, there is a subtle distinction. Genotoxicity pertains to all types of ...
Antidepressant specificity of serotonin transporter suggested by three LeuT–SSRI structures Zheng Zhou
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
![](https://en.wikipedia.org/wiki/Special:FilePath/RTenzyme-hand.jpg?width=300)
Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development.Discovery and development of NNRTIs began in the late 1980s and in the end of 2009 four NNRTI had been approved by regulatory authorities and several others were undergoing clinical development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy (HAART).