Lecture 16 Pharmacokinetics - Cal State LA
... d. Use of medicinal chemistry to improve hydrophobic/hydrophilic balance. •Change functional groups: Alcohol (ROH) versus ether (ROR’) or ester (RO2R’) •Change the number or size of alkyl groups •Change rings Example: Cl N N ...
... d. Use of medicinal chemistry to improve hydrophobic/hydrophilic balance. •Change functional groups: Alcohol (ROH) versus ether (ROR’) or ester (RO2R’) •Change the number or size of alkyl groups •Change rings Example: Cl N N ...
File
... Rifamycins: rifampin, rifabutin, and rifapentine • Rifampin, rifabutin, and rifapentine are all considered rifamycins, a group of structurally similar macrocyclic antibiotics, which are first-line oral agents for tuberculosis. • Rifampin has broader antimicrobial activity than isoniazid and can b ...
... Rifamycins: rifampin, rifabutin, and rifapentine • Rifampin, rifabutin, and rifapentine are all considered rifamycins, a group of structurally similar macrocyclic antibiotics, which are first-line oral agents for tuberculosis. • Rifampin has broader antimicrobial activity than isoniazid and can b ...
Pharmacokinetics of the Antimycobacterial Agents
... See why this is happening, adapt, and overcome. ...
... See why this is happening, adapt, and overcome. ...
Anitmicrobial Agents General Considerations 4 Pharmacology Prof
... • Cytochrome P-450 system (CYP3A4, CYP2D6, CYP2C9, CYP1A2, CYP2E1) – Phase II • Conjugation of the parent compound with larger molecules, increasing the polarity • Generally inactivate the parent compound • Glucuronidation, sulfation, acetylation Elimination – Total body clearance (Half life) • Rena ...
... • Cytochrome P-450 system (CYP3A4, CYP2D6, CYP2C9, CYP1A2, CYP2E1) – Phase II • Conjugation of the parent compound with larger molecules, increasing the polarity • Generally inactivate the parent compound • Glucuronidation, sulfation, acetylation Elimination – Total body clearance (Half life) • Rena ...
Antimicrobial Agents (General considerations 4)
... • Cytochrome P-450 system (CYP3A4, CYP2D6, CYP2C9, CYP1A2, CYP2E1) – Phase II • Conjugation of the parent compound with larger molecules, increasing the polarity • Generally inactivate the parent compound • Glucuronidation, sulfation, acetylation Elimination – Total body clearance (Half life) • Rena ...
... • Cytochrome P-450 system (CYP3A4, CYP2D6, CYP2C9, CYP1A2, CYP2E1) – Phase II • Conjugation of the parent compound with larger molecules, increasing the polarity • Generally inactivate the parent compound • Glucuronidation, sulfation, acetylation Elimination – Total body clearance (Half life) • Rena ...
full text pdf
... bond acceptors, had a molecular weight less than 500 grams per mole, and had an octanol-water partition coefficient (log P) of less than five. These rules are used as a guideline to focus the screening process and new drugs tend to be small organic molecules with high affinity for their target as we ...
... bond acceptors, had a molecular weight less than 500 grams per mole, and had an octanol-water partition coefficient (log P) of less than five. These rules are used as a guideline to focus the screening process and new drugs tend to be small organic molecules with high affinity for their target as we ...
Rational use of anti-tuberculosis drugs in the EU: better EDITORIAL
... The fifth and final article is entitled ‘‘TB drug development and the potential to address the M/XDR-TB epidemic: relevance and implications for the rational use of drugs in the EU/EEA and beyond’’ by D. Manissero and co-workers. This will review the epidemiology of drug-resistant TB in the EU using ...
... The fifth and final article is entitled ‘‘TB drug development and the potential to address the M/XDR-TB epidemic: relevance and implications for the rational use of drugs in the EU/EEA and beyond’’ by D. Manissero and co-workers. This will review the epidemiology of drug-resistant TB in the EU using ...
ANTIBIOTICS
... inactivate some e.g. ampicillin but not others cloxacillin or meropenem To overcome this mechanism of resistance , B-Lactamase inhibitors are added to the antibiotic e.g. clavulanic acid added to ampicillin = augmentin ...
... inactivate some e.g. ampicillin but not others cloxacillin or meropenem To overcome this mechanism of resistance , B-Lactamase inhibitors are added to the antibiotic e.g. clavulanic acid added to ampicillin = augmentin ...
Protease inhibitors in chronic hepatitis C
... cells; has broad substrate specificity, and inhibiting or inducing the activity of this protein can lead to significant alterations in drug exposure ...
... cells; has broad substrate specificity, and inhibiting or inducing the activity of this protein can lead to significant alterations in drug exposure ...
Helminth Biochemistry
... “If we picture an organism as infected by a certain species of bacterium, it will … be easy to effect a cure if substances have been discovered which have a specific affinity for these bacteria and act … on these alone … while they possess no affinity for the normal constituents of the body … such s ...
... “If we picture an organism as infected by a certain species of bacterium, it will … be easy to effect a cure if substances have been discovered which have a specific affinity for these bacteria and act … on these alone … while they possess no affinity for the normal constituents of the body … such s ...
antiretroviral therapy in children
... half lives would allow quite a bit of flexibility around timing of doses. It’s clearly much more important for adherence to fit these drugs in to our patients’ lives. If they want to sleep in late at the weekend, giving doses a couple of hours later than normal should not be a problem. Gareth Tudor ...
... half lives would allow quite a bit of flexibility around timing of doses. It’s clearly much more important for adherence to fit these drugs in to our patients’ lives. If they want to sleep in late at the weekend, giving doses a couple of hours later than normal should not be a problem. Gareth Tudor ...
Naming Compounds - Mayfield City Schools
... Chemical formulas tell a great deal of information about a compound—the types of elements forming the compound, the numbers of atoms of each element in one molecule, and even some indication, perhaps, of the arrangement of the atoms when they form the molecule. In addition to having a unique chemica ...
... Chemical formulas tell a great deal of information about a compound—the types of elements forming the compound, the numbers of atoms of each element in one molecule, and even some indication, perhaps, of the arrangement of the atoms when they form the molecule. In addition to having a unique chemica ...
Result 1. IMPACT OF DIFFERENT PATTERNS OF
... Objectives: The aim of the study was to evaluate the impact of different patterns of nonadherence on treatment outcomes in patients with longterm ...
... Objectives: The aim of the study was to evaluate the impact of different patterns of nonadherence on treatment outcomes in patients with longterm ...
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
... The dose of nevirapine must be increased to account for increased metabolism due to phenytoin 3. An interaction exists between phenytoin and cotrimoxazole. They should not be administered together 4. Nevirapine may decrease phenytoin levels and therefore the dose of phenytoin may need to be increase ...
... The dose of nevirapine must be increased to account for increased metabolism due to phenytoin 3. An interaction exists between phenytoin and cotrimoxazole. They should not be administered together 4. Nevirapine may decrease phenytoin levels and therefore the dose of phenytoin may need to be increase ...
Chemistry In Everyday Life
... because their binding sites have different shape, structure and aminoacid composition. Drugs that bind to the receptor site and inhibit its natural function are called antagonists. Drugs that mimic the natural messenger by switching on the receptors are called agonists. These are useful when there i ...
... because their binding sites have different shape, structure and aminoacid composition. Drugs that bind to the receptor site and inhibit its natural function are called antagonists. Drugs that mimic the natural messenger by switching on the receptors are called agonists. These are useful when there i ...
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
... The dose of nevirapine must be increased to account for increased metabolism due to phenytoin 3. An interaction exists between phenytoin and cotrimoxazole. They should not be administered together 4. Nevirapine may decrease phenytoin levels and therefore the dose of phenytoin may need to be increase ...
... The dose of nevirapine must be increased to account for increased metabolism due to phenytoin 3. An interaction exists between phenytoin and cotrimoxazole. They should not be administered together 4. Nevirapine may decrease phenytoin levels and therefore the dose of phenytoin may need to be increase ...
`drug`.
... EC50 - The agonist concentration that causes 50% of the maximum response. pEC50 = - log10(EC50) Antagonists: Situation more complex. Antagonists displace the agonist dose-response curve rightwards – most accurate measure of potency (pA2) requires measurement of agonist binding at multiple concentrat ...
... EC50 - The agonist concentration that causes 50% of the maximum response. pEC50 = - log10(EC50) Antagonists: Situation more complex. Antagonists displace the agonist dose-response curve rightwards – most accurate measure of potency (pA2) requires measurement of agonist binding at multiple concentrat ...
Favorable review of Cytopia by Mayo`s IRB and FDA for their JAK2
... Typical symptoms include an enlarged spleen, progressive anaemia and poor overall survival. The study will also allow preliminary assessment of the compound’s activity in these patients including its effect on spleen size, haematological symptoms and quality-oflife as well as markers of aberrant JAK ...
... Typical symptoms include an enlarged spleen, progressive anaemia and poor overall survival. The study will also allow preliminary assessment of the compound’s activity in these patients including its effect on spleen size, haematological symptoms and quality-oflife as well as markers of aberrant JAK ...
anti tb drugs - PharmaStreet
... • Because of need for i.m. injections and lower margin of safety • Used only as an alternative to or in addition to other first line anti-TB drugs • Use is restricted to maximum of 2 months. • It is thus also labelled as a ‘supplemental’ first line drug. ...
... • Because of need for i.m. injections and lower margin of safety • Used only as an alternative to or in addition to other first line anti-TB drugs • Use is restricted to maximum of 2 months. • It is thus also labelled as a ‘supplemental’ first line drug. ...
Parasites 101 – Myth Busting
... population to survive drug treatments that are generally effective against the same worm species and stage of infection – Caused by changes in levels of “resistance” genes carried by worms in a population – Result of drug treatment that produces genetic selection of resistant worms in a population o ...
... population to survive drug treatments that are generally effective against the same worm species and stage of infection – Caused by changes in levels of “resistance” genes carried by worms in a population – Result of drug treatment that produces genetic selection of resistant worms in a population o ...
Head Shop Compound abuse amongst attendees of The Drug
... The DTCB laboratory analysed 209 samples of urine for Methylone, Mephedrone and BZP by LC/MS. Of these 209 samples, 46 were from suspected users of headshop compounds, 163 were random samples. Of the random samples 7.4 % were positive for Mephedrone and 1.2% positive for Methylone. Of the total 209 ...
... The DTCB laboratory analysed 209 samples of urine for Methylone, Mephedrone and BZP by LC/MS. Of these 209 samples, 46 were from suspected users of headshop compounds, 163 were random samples. Of the random samples 7.4 % were positive for Mephedrone and 1.2% positive for Methylone. Of the total 209 ...
Antiviral for respiratory viral infection
... Replication of viral components using host-cell machinery. Assembly of viral components into complete viral particles. Release of viral particles to infect new host cells. Anti-viral targeting Before cell entry This stage of viral replication can be inhibited in two ways: 1. Anti-receptor anti ...
... Replication of viral components using host-cell machinery. Assembly of viral components into complete viral particles. Release of viral particles to infect new host cells. Anti-viral targeting Before cell entry This stage of viral replication can be inhibited in two ways: 1. Anti-receptor anti ...
When Patients Cannot Take Pills: Antiretroviral Drug - IAS-USA
... of life.2 With advanced age from declining mortality, however, comes a new subset of health care issues for patients. Current treatment involves not only the use of complex antiretroviral regimens for life but may also require periodic hospital stays or outpatient visits to manage comorbidites or co ...
... of life.2 With advanced age from declining mortality, however, comes a new subset of health care issues for patients. Current treatment involves not only the use of complex antiretroviral regimens for life but may also require periodic hospital stays or outpatient visits to manage comorbidites or co ...
... factor and thus the inhibition Phospholipase A2 by pharmacological agents should have led to an antiinflammatory effect. Plants serve as sources of compounds that act a potential therapeutic agent for treatment of various diseases. In present study, an attempt was made to inhibit Phorpholipase A2 by ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
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).