Recommendation and Reasons
... • The Committee discussed the potential listing of raltegravir for use in treatment-naive patients with virologic failure due to resistance to at least one agent from each of the three major classes of antiretroviral agents (nucleoside/nucleotide reverse transcriptase inhibitors, non-nucleoside reve ...
... • The Committee discussed the potential listing of raltegravir for use in treatment-naive patients with virologic failure due to resistance to at least one agent from each of the three major classes of antiretroviral agents (nucleoside/nucleotide reverse transcriptase inhibitors, non-nucleoside reve ...
Fragment-based Drug Discovery of the Synthetic Small Molecule
... Fragment 1, was identified as having a Kd of 790μM for HSP90 and the experimental binding mode indicated a clear pathway to optimise the molecule After three iterations of structure-guided medicinal chemistry, compound 4 was identified which is just six heavy atoms larger than fragment 1 but is over ...
... Fragment 1, was identified as having a Kd of 790μM for HSP90 and the experimental binding mode indicated a clear pathway to optimise the molecule After three iterations of structure-guided medicinal chemistry, compound 4 was identified which is just six heavy atoms larger than fragment 1 but is over ...
Lecture6- GENERAL PHARMACOLOGY
... Define the major phase I and phase II metabolic reactions. Describe the modulation of liver microsomal enzymes by inducers and inhibitors Mention two drugs that are known as enzyme inducers and ...
... Define the major phase I and phase II metabolic reactions. Describe the modulation of liver microsomal enzymes by inducers and inhibitors Mention two drugs that are known as enzyme inducers and ...
from membrane-embedded targets to amyloid fibrils
... membrane-embedded receptors A convenient starting point in structure-based drug discovery is to identify where the native ligand or an unoptimized lead compound interacts with its target and to produce a three-dimensional model of the ligand within the binding pocket. The SSNMR method of CP-MAS (cro ...
... membrane-embedded receptors A convenient starting point in structure-based drug discovery is to identify where the native ligand or an unoptimized lead compound interacts with its target and to produce a three-dimensional model of the ligand within the binding pocket. The SSNMR method of CP-MAS (cro ...
Interactions with HIV medications
... NRTIs : NRTIs are prone to pharmacodynamic interactions such as additive and synergistic toxicities, but because they are primarily eliminated by the kidneys, not the liver, they have little impact on the CYP450 system. As such, NRTIs have few known pharmacokinetic interactions with NNRTIs or PIs. A ...
... NRTIs : NRTIs are prone to pharmacodynamic interactions such as additive and synergistic toxicities, but because they are primarily eliminated by the kidneys, not the liver, they have little impact on the CYP450 system. As such, NRTIs have few known pharmacokinetic interactions with NNRTIs or PIs. A ...
Chapter 21 Antimicrobial medications
... • In 1928, Alexander Fleming discovered that the fungi Penicillium produces a chemical that kills bacteria. He called this substance penicillin. ...
... • In 1928, Alexander Fleming discovered that the fungi Penicillium produces a chemical that kills bacteria. He called this substance penicillin. ...
ARV-based Microbicides and Resistance
... active arm and 6 in placebo arm HIV infections too few to draw conclusions on efficacy ...
... active arm and 6 in placebo arm HIV infections too few to draw conclusions on efficacy ...
lec.11-426
... • It is useful in the management of psychotic reactions, and hyperactivity. • It is a drug of choice for Tourett’s syndrome. • It is metabolized by oxidative N-dealkylation. • The oxidation products………………….. ...
... • It is useful in the management of psychotic reactions, and hyperactivity. • It is a drug of choice for Tourett’s syndrome. • It is metabolized by oxidative N-dealkylation. • The oxidation products………………….. ...
Document
... – Cause of many adverse reactions poorly understood – Drugs may be toxic to kidneys, liver, or nerves – Consideration needed when prescribing drugs to pregnant women ...
... – Cause of many adverse reactions poorly understood – Drugs may be toxic to kidneys, liver, or nerves – Consideration needed when prescribing drugs to pregnant women ...
alkylating agent
... * two camptothecin derivatives approved and used in cancer chemotherapy: * topotecan, in gynecologic tumors and small cell lung cancer; - toxicity limited to myelosuppression and mucositis; ...
... * two camptothecin derivatives approved and used in cancer chemotherapy: * topotecan, in gynecologic tumors and small cell lung cancer; - toxicity limited to myelosuppression and mucositis; ...
eprint_1_30658_130
... 3- Food has little effect on absorption (except with sertraline, for which food increases its absorption). 4- Only sertraline undergoes significant first-pass metabolism. 5- All of these agents are well distributed, having volumes of distribution far in excess of body weight (15-30 L/kg). 6- The maj ...
... 3- Food has little effect on absorption (except with sertraline, for which food increases its absorption). 4- Only sertraline undergoes significant first-pass metabolism. 5- All of these agents are well distributed, having volumes of distribution far in excess of body weight (15-30 L/kg). 6- The maj ...
Antimicrobial Medications
... Five medications termed first-line drugs preferentially because of effectiveness with low toxicity First-line drugs include rifampin, streptomycin and Isoniazid inhibits synthesis of mycolic acid Ethambutol inhibits enzymes for cell wall synthesis Pyrazinamide mechanism of action unknown ...
... Five medications termed first-line drugs preferentially because of effectiveness with low toxicity First-line drugs include rifampin, streptomycin and Isoniazid inhibits synthesis of mycolic acid Ethambutol inhibits enzymes for cell wall synthesis Pyrazinamide mechanism of action unknown ...
elevated blood glucose
... arrhythmias (Long QT) and EPS (Extra pyramidal Symptoms) EPS is a movement disorder that is similar to Parkinson’s disease Second generation drugs were developed to avoid EPS A major side effects to these drugs are: risk of drug induced diabetes and weight gain. Clozapine has the risk of fatal blood ...
... arrhythmias (Long QT) and EPS (Extra pyramidal Symptoms) EPS is a movement disorder that is similar to Parkinson’s disease Second generation drugs were developed to avoid EPS A major side effects to these drugs are: risk of drug induced diabetes and weight gain. Clozapine has the risk of fatal blood ...
Nucleoside Analogue Reverse Transcriptase Inhibitor - IAS-USA
... the codon 69-insertion complex, and the codon 151-complex can each confer cross-class resistance. There are 2 principal mechanisms of nRTI resistance, and these mechanisms can interact to further alter susceptibility patterns (Clavel and Hance, N Engl J Med, 2004). In brief, nRTI resistance can occu ...
... the codon 69-insertion complex, and the codon 151-complex can each confer cross-class resistance. There are 2 principal mechanisms of nRTI resistance, and these mechanisms can interact to further alter susceptibility patterns (Clavel and Hance, N Engl J Med, 2004). In brief, nRTI resistance can occu ...
Lec 8
... • Carboxylic acid for example is a highly polar group which can be ionized and hinder absorption of any drug containing it. • To overcome this problem we must mask it as an ester prodrug or to replace it with a bioisostere which has similar physiochemical properties and has advantage over carboxylic ...
... • Carboxylic acid for example is a highly polar group which can be ionized and hinder absorption of any drug containing it. • To overcome this problem we must mask it as an ester prodrug or to replace it with a bioisostere which has similar physiochemical properties and has advantage over carboxylic ...
diuretics
... peripheral vascular resistance and lower arterial blood pressure by causing the relaxation of both arterial and venous smooth muscle. These drugs cause only minimal changes in cardiac output, renal blood flow, and glomerular filtration rate. Postural hypotension may occur in some individuals. Prazos ...
... peripheral vascular resistance and lower arterial blood pressure by causing the relaxation of both arterial and venous smooth muscle. These drugs cause only minimal changes in cardiac output, renal blood flow, and glomerular filtration rate. Postural hypotension may occur in some individuals. Prazos ...
Enteropeptidase: A Gene Associated with a Starvation
... catalyzes the conversion of inactive trypsinogen into active trypsin via the cleavage of the acidic propeptide from trypsinogen [6]. In turn, the activation of trypsin initiates a cascade of proteolytic reactions leading to the activation of many pancreatic zymogens, such as chymotrypsinogen, proela ...
... catalyzes the conversion of inactive trypsinogen into active trypsin via the cleavage of the acidic propeptide from trypsinogen [6]. In turn, the activation of trypsin initiates a cascade of proteolytic reactions leading to the activation of many pancreatic zymogens, such as chymotrypsinogen, proela ...
499 Med Chem Chap 9 problems
... a. It a useful systemic antibacterial agent. b. Its planar shape is important to intercalation. c. The primary amine groups are protonated and interact with phosphate groups of the DNA backbone. d. When inserted into DNA, the tricyclic system can form van der Waals interactions with base pairs above ...
... a. It a useful systemic antibacterial agent. b. Its planar shape is important to intercalation. c. The primary amine groups are protonated and interact with phosphate groups of the DNA backbone. d. When inserted into DNA, the tricyclic system can form van der Waals interactions with base pairs above ...
Anti depressant drugs
... Mechanism of action • Ssri bind with serotonin transporter protein and inhibit the transport of serotonin from extra to intracellular site. ...
... Mechanism of action • Ssri bind with serotonin transporter protein and inhibit the transport of serotonin from extra to intracellular site. ...
NONSTEROIDAL ANTIINFLAMATORY DRUGS(NSAIDS)
... • Cox 1:This activity is constitutively present in nearly all cell types at constant level . • Cox 2: This activity is normally absent from cells except those of kidneys & brain but it is inducible by bacterial lyposaccharides IL2 &TNF in activated leucocytes &other inflammatory cells. • Cox 1 is a ...
... • Cox 1:This activity is constitutively present in nearly all cell types at constant level . • Cox 2: This activity is normally absent from cells except those of kidneys & brain but it is inducible by bacterial lyposaccharides IL2 &TNF in activated leucocytes &other inflammatory cells. • Cox 1 is a ...
Sulfanomides
... • Sulfonamides (sulfa drugs) are a family of antibiotics that inhibit de novo synthesis of folate. • Trimethoprim a second type of folate antagonist—prevents microorganisms from converting dihydrofolic acid to tetrahydrofolic acid, with minimal effect on the ability of human cells to make this conve ...
... • Sulfonamides (sulfa drugs) are a family of antibiotics that inhibit de novo synthesis of folate. • Trimethoprim a second type of folate antagonist—prevents microorganisms from converting dihydrofolic acid to tetrahydrofolic acid, with minimal effect on the ability of human cells to make this conve ...
Chemical Genetics: Where Genetics and Pharmacology
... reason for this? Gefitinib resistance is associated with downregulation of cellular tyrosine phosphatase activity and increased expression of EGFR/ HER2 substrates, two mechanisms that amplify the EGFR-dependent substrate phosphorylation that remains after drug treatment (Sergina et al., 2007). This ...
... reason for this? Gefitinib resistance is associated with downregulation of cellular tyrosine phosphatase activity and increased expression of EGFR/ HER2 substrates, two mechanisms that amplify the EGFR-dependent substrate phosphorylation that remains after drug treatment (Sergina et al., 2007). This ...
antiretroviral therapy in children
... Bottom line, with the NRTIs currently in use including the older ones, and with the newer, RTV-boosted PIs and NNRTIs, there are no data to support they have to be given exactly on an every 12 or 24 hour basis. All of the most recent clinical trials (ACTG 5095, Gilead 934, KLEAN, etc, etc) have been ...
... Bottom line, with the NRTIs currently in use including the older ones, and with the newer, RTV-boosted PIs and NNRTIs, there are no data to support they have to be given exactly on an every 12 or 24 hour basis. All of the most recent clinical trials (ACTG 5095, Gilead 934, KLEAN, etc, etc) have been ...
