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45 Cards in this Set
- Front
- Back
Affinity |
Measures how strong a drug binds to receptor Just because strong may not guarantee a good mix |
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Efficacy |
Measure of Maximum biological effect that a drug can produce as a result of receptor binding High affinity no efficacy antagonist |
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Potency |
Amount of drug refers to amount of drug required to achieve a defined biological effect. The smaller the dose the more potent the drug |
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P450 |
Phase 1 Transformations catalyzed by chromosome ______ |
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Methanol |
When______ is in your liver it turns to formaldehyde and other awful toxin |
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Gram positive |
Thick carbohydrate cell wall |
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Gram-negative |
Thin cell wall additional outer membrane |
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Pharmodynamic |
The study of how living interact with their target binding site and produce a pharmacological effect the target mechanism |
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Pharmacokinetic |
Distribute metabolism the whole journey drug absorption drug distribution drug metabolism drug excretion |
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Prodrug |
A molecule that is inactive in itself but which is converted to the active drug in the body normally buy an enzymatic reaction Used to avoid problems related to pharmacokinetics of the active drug and for targeting |
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Bacteriostatic |
Bacteriostatic drugs inhibit the growth and multiplication of bacteria but do not directly kill them |
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Structure-activity relationships |
SAR Studies carried out to determine those atoms or functional groups which are important to drug activity |
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Pharmacophore |
The atoms and functional groups required for a specific pharmacological activity and their relative positions in space |
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Beta lactams |
Enzymes that bacteria uses to defend themselves from penicillin it deactivated by opening a beta-lactam ring |
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Hydrophobic sidechain |
High act vs. Gram-positive and has a poor act vs. Gram-negative |
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Transpeptidase |
Important bacterial enzyme that catalyzes the final crosslinking of the bacterial cell wall. Targeted by penicillin and cephalosporin. Irreversible hibited by catalyzed horsporans |
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Cephalosporins |
Disguise structure from penicillin |
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Second generation cephalosporin - cephamycins |
One has greater residents to beta-lactamase enzyme. Two not active against pseudomonas aeruginosa |
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... |
Inhibits - Blocks transglycosdiation vancomycin |
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Chloroquine |
Shows some activity against Gram-negative it was found accidentally |
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Pharmacophore of quinone and fluoroquinolones |
Pyridine ring and carboxylic acid are a must for activity |
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Protein kinase inhibitors |
Serine threonine tyrosine are the main three. Cofactor ATP. Focus on binding site to block ATP |
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Has no off switch |
Aspartate and glutamate |
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Active vs. Inactive |
GTP vs. GDP |
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Epidermal growth factor |
EGF Receptor is a tyrosine kinase inhibitor receptor |
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Ic50 |
Inhibitory concentration you want it to be a small as possible nanometers is better than micrometers |
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Isotere |
Replacing a group with same valency structure and stericy |
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Bioisotere |
May not have same valency but the body treats it the same |
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In vitro |
Pharmacodynamic |
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In viro |
Pharmacokinetic |
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Ber-abl |
Diffusion of chromosome 9 + 22 |
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Conformational blocker |
Methane group keeps group from freely rotating helps to maintain structure |
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Type 2 protein kinase inhibitor lilac |
Prevent from becoming the active form |
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Hydrogen |
In the ways of size fluorine compares to What atom |
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Ras protein |
Active _____ normally Auto catalyzes hydrolysis of GTP back to GDP. Key event attaching to hydrophobic chain |
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Metabolic blocker |
To help prevent oxidation of fluorine can replace a hydrogen |
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Ki |
Inhibition equilibrium If _____ is small then it favors the left side |
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Rigidity |
Things that don't bend but they can eventually break Zinc is a metal low enzyme co-factor |
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Antagonist |
Block natural messenger strong more binding interaction |
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Agonist |
Drug designed to mimic the natural messenger |
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Reverse antagonist |
When binds does not induce transduction signal or change shape |
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ADME |
Absorption distribution metabolism excretion |
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A levoli |
Airsoft with single cell wall surrounded by Blood capillaries around fast effective Exchange |
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:- |
Vh |
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Polar, fatty |
Orally taken drugs must be _______ to dissolve in the GI tract and blood supply but also extremely ______ to pass through the cell membranes |