Drug-Receptor Interactions
... Receptors fluid, flexible surfaces or pockets ◦ Can change 3-D structure as ligand docks ◦ Most receptors are sites for natural ligands ◦ Small portion or surface of a macromolecule Includes: Enzymes, components of cell membranes, intracellular protein or nucleic acid, antibodies, DNA, RNA ...
... Receptors fluid, flexible surfaces or pockets ◦ Can change 3-D structure as ligand docks ◦ Most receptors are sites for natural ligands ◦ Small portion or surface of a macromolecule Includes: Enzymes, components of cell membranes, intracellular protein or nucleic acid, antibodies, DNA, RNA ...
Enzyme
... Although activation of enzymes may be exploited therapeutically, most effects are produced by enzyme inhibition. Inhibition caused by drugs may be either reversible or irreversible. A reversible situation occurs when an equilibrium can be established between the enzyme and the inhibitory drug. A com ...
... Although activation of enzymes may be exploited therapeutically, most effects are produced by enzyme inhibition. Inhibition caused by drugs may be either reversible or irreversible. A reversible situation occurs when an equilibrium can be established between the enzyme and the inhibitory drug. A com ...
Pharmacology Definitions
... and thus no response is ever achieved by its binding. There are several forms of antagonism, the main ones being reversible and irreversible competitive antagonism, and non-competitive antagonism. Competitive binding Competitive binding describes the event whereby there are two different molecules w ...
... and thus no response is ever achieved by its binding. There are several forms of antagonism, the main ones being reversible and irreversible competitive antagonism, and non-competitive antagonism. Competitive binding Competitive binding describes the event whereby there are two different molecules w ...
Pediatric Pharmacology
... Basics: medications given to children have to be dose and interval adjusted; there are a few medications that can still cause adverse events even in the presence of appropriate dosing Tetracyclines: contraindicated in kids under 8 due to teeth discoloration Fluoroquinolones: can cause tendon problem ...
... Basics: medications given to children have to be dose and interval adjusted; there are a few medications that can still cause adverse events even in the presence of appropriate dosing Tetracyclines: contraindicated in kids under 8 due to teeth discoloration Fluoroquinolones: can cause tendon problem ...
Introduction to Pharmacology NAPNES Guidelines
... through the oral or gastric mucosa, the small intestine, or rectum ...
... through the oral or gastric mucosa, the small intestine, or rectum ...
KINETICS OF ELIMINATION
... At low doses, follow first order kinetics As the plasma conc. increases Elimination processes get saturated ...
... At low doses, follow first order kinetics As the plasma conc. increases Elimination processes get saturated ...
Chirality in Pharmaceutical Synthesis
... • This is true for all “lock and key” interactions. • Dopa is a neurotransmitter which exhibits optical isomerism – only the L form is active in the brain. • The structure of L-Dopa follows. ...
... • This is true for all “lock and key” interactions. • Dopa is a neurotransmitter which exhibits optical isomerism – only the L form is active in the brain. • The structure of L-Dopa follows. ...
Representation and Manipulation of 3D Molecular Structures
... • Data mining for conformational properties and intermolecular interactions (CSD & PDB) • Data mining for information about intermolecular interactions (CSD & PDB) • Further understanding of the nature of protein structure and its relationship to amino acid sequence (PDB) • Homology modeling (compar ...
... • Data mining for conformational properties and intermolecular interactions (CSD & PDB) • Data mining for information about intermolecular interactions (CSD & PDB) • Further understanding of the nature of protein structure and its relationship to amino acid sequence (PDB) • Homology modeling (compar ...
Designer Drug Update - Commonwealth Prevention Alliance
... known as bath salts. Bath salts have been connected to a range of violent incidents and a spike in emergency room visits since they became popular several years ago. Last fall, the Drug Enforcement Administration banned three chemicals used in bath salts, and 38 states have enacted their own bans, b ...
... known as bath salts. Bath salts have been connected to a range of violent incidents and a spike in emergency room visits since they became popular several years ago. Last fall, the Drug Enforcement Administration banned three chemicals used in bath salts, and 38 states have enacted their own bans, b ...
Prescription_Drugs_Information_Fact_Sheet
... prescribed to treat pain and include chemicals like morphine, codeine, oxycodone, and hydrocodone. Amphetamines are also sold as stimulant prescription drugs, primarily to treat deficit hyperactivity disorder and narcolepsy. There are also over-the-counter drugs that are abused or misused. For examp ...
... prescribed to treat pain and include chemicals like morphine, codeine, oxycodone, and hydrocodone. Amphetamines are also sold as stimulant prescription drugs, primarily to treat deficit hyperactivity disorder and narcolepsy. There are also over-the-counter drugs that are abused or misused. For examp ...
Advantages - pharmacist
... The mechanism of iontophoresis Mechanism is based on the physical phenomenon that “like charges repel and opposite charges attract”. The drugs are forced Across the skin by simple electronic repulsion of similar charges. Thus, anionic drugs Can cross the skin by using a negatively charged electrode ...
... The mechanism of iontophoresis Mechanism is based on the physical phenomenon that “like charges repel and opposite charges attract”. The drugs are forced Across the skin by simple electronic repulsion of similar charges. Thus, anionic drugs Can cross the skin by using a negatively charged electrode ...
ABC`s of Drug Testing
... Summary and conclusions • All drug tests have strengths and limitations • All specimen types have strengths and limitations, and are at risk of tampering • Individual characteristics of a drug user will impact drug testing results • Work with the laboratory to get the best ...
... Summary and conclusions • All drug tests have strengths and limitations • All specimen types have strengths and limitations, and are at risk of tampering • Individual characteristics of a drug user will impact drug testing results • Work with the laboratory to get the best ...
STUDY OF HALOGEN SUBSTITUENT ON DOCKING AND 3D
... receptor (PDB code 1 OHV) and interaction studies were carried out with active residues of GABAAT i.e. Lysine 329A and Arginine 192A. Pyridoxal phosphate (PLP) based grip docking was performed and the results were compared with vigabatrin. All 21 molecules showed better binding energies than vigabat ...
... receptor (PDB code 1 OHV) and interaction studies were carried out with active residues of GABAAT i.e. Lysine 329A and Arginine 192A. Pyridoxal phosphate (PLP) based grip docking was performed and the results were compared with vigabatrin. All 21 molecules showed better binding energies than vigabat ...
Tuberculosis
... used in combination because resistance occurs to one drug alone very rapidly. They are used in combination with each other initially as well as other drugs. Bacilli must become resistant to two drugs in order to remain viable. Statistically, the chances are verv small of the bacilli becoming resista ...
... used in combination because resistance occurs to one drug alone very rapidly. They are used in combination with each other initially as well as other drugs. Bacilli must become resistant to two drugs in order to remain viable. Statistically, the chances are verv small of the bacilli becoming resista ...
Pharmacology MCQs
... of Autonomic nervous system drugs, Autocoids 1. The apparent volume of distribution of a drug a. is usually larger for a basic drug than an acidic drug. b. is obtained by dividing the dose administered by its free concentration in the plasma. c. is inversely related to its elimination half-life d. m ...
... of Autonomic nervous system drugs, Autocoids 1. The apparent volume of distribution of a drug a. is usually larger for a basic drug than an acidic drug. b. is obtained by dividing the dose administered by its free concentration in the plasma. c. is inversely related to its elimination half-life d. m ...
Done By: Walaa Wahdan Advanced Technology Lecture #8 Last
... necessary each sample contains the composition, because it’s a physical mixture of crystal). If we pass the solid solution in DSC, it will give one peak because we have single solid phase. The ratio of 2 components in the crystal depends on: ratio of drug and carrier, affinity of both and most stabl ...
... necessary each sample contains the composition, because it’s a physical mixture of crystal). If we pass the solid solution in DSC, it will give one peak because we have single solid phase. The ratio of 2 components in the crystal depends on: ratio of drug and carrier, affinity of both and most stabl ...
Bio-Instruments Signal Processing : A Prospective GRID
... • Data and results exchange between different work groups. ...
... • Data and results exchange between different work groups. ...
Describe in YOUR OWN WORDS, WITHOUT using equations or
... this is true. We must set acceptable levels for the risks of type I and II error. a. Define type I error and type II error. b. Suppose you expect a mortality rate in the group treated with the new drug stent of 5 %, while the expected restenosis rate in the group treated with the current stent is 7 ...
... this is true. We must set acceptable levels for the risks of type I and II error. a. Define type I error and type II error. b. Suppose you expect a mortality rate in the group treated with the new drug stent of 5 %, while the expected restenosis rate in the group treated with the current stent is 7 ...
Paediatrics - Durban University of Technology
... “children, especially infants, have a much higher body surface area to weight ratio, and this translates into relatively more water loss from skin compared with adults.” “children, especially infants, have higher respiratory rates, and this equates to higher insensible losses from the respirator ...
... “children, especially infants, have a much higher body surface area to weight ratio, and this translates into relatively more water loss from skin compared with adults.” “children, especially infants, have higher respiratory rates, and this equates to higher insensible losses from the respirator ...
novel paradigms for drug discovery shotgun
... Multitargeting: multiple low Kd can work synergistically; screening for targets and antitargets simultaneously. Knowledge based: potential from known structures, will have a big matrix relating drugs, targets, PK, ADME, solubility, bioavailability, toxicity, etc.; rich dataset for combining our biop ...
... Multitargeting: multiple low Kd can work synergistically; screening for targets and antitargets simultaneously. Knowledge based: potential from known structures, will have a big matrix relating drugs, targets, PK, ADME, solubility, bioavailability, toxicity, etc.; rich dataset for combining our biop ...
Drug design
Drug design, sometimes referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target. The drug is most commonly an organic small molecule that activates or inhibits the function of a biomolecule such as a protein, which in turn results in a therapeutic benefit to the patient. In the most basic sense, drug design involves the design of molecules that are complementary in shape and charge to the biomolecular target with which they interact and therefore will bind to it. Drug design frequently but not necessarily relies on computer modeling techniques. This type of modeling is often referred to as computer-aided drug design. Finally, drug design that relies on the knowledge of the three-dimensional structure of the biomolecular target is known as structure-based drug design. In addition to small molecules, biopharmaceuticals and especially therapeutic antibodies are an increasingly important class of drugs and computational methods for improving the affinity, selectivity, and stability of these protein-based therapeutics have also been developed.The phrase ""drug design"" is to some extent a misnomer. A more accurate term is ligand design (i.e., design of a molecule that will bind tightly to its target). Although design techniques for prediction of binding affinity are reasonably successful, there are many other properties, such as bioavailability, metabolic half-life, side effects, etc., that first must be optimized before a ligand can become a safe and efficacious drug. These other characteristics are often difficult to predict with rational design techniques. Nevertheless, due to high attrition rates, especially during clinical phases of drug development, more attention is being focused early in the drug design process on selecting candidate drugs whose physicochemical properties are predicted to result in fewer complications during development and hence more likely to lead to an approved, marketed drug. Furthermore, in vitro experiments complemented with computation methods are increasingly used in early drug discovery to select compounds with more favorable ADME (absorption, distribution, metabolism, and excretion) and toxicological profiles.