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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

Efficacy

Measure of Maximum biological effect that a drug can produce as a result of receptor binding



High affinity no efficacy antagonist

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

P450

Phase 1 Transformations catalyzed by chromosome ______

Methanol

When______ is in your liver it turns to formaldehyde and other awful toxin

Gram positive

Thick carbohydrate cell wall

Gram-negative

Thin cell wall additional outer membrane

Pharmodynamic

The study of how living interact with their target binding site and produce a pharmacological effect the target mechanism

Pharmacokinetic

Distribute metabolism the whole journey


drug absorption drug distribution drug metabolism drug excretion

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

Bacteriostatic

Bacteriostatic drugs inhibit the growth and multiplication of bacteria but do not directly kill them

Structure-activity relationships

SAR


Studies carried out to determine those atoms or functional groups which are important to drug activity

Pharmacophore

The atoms and functional groups required for a specific pharmacological activity and their relative positions in space

Beta lactams

Enzymes that bacteria uses to defend themselves from penicillin it deactivated by opening a beta-lactam ring

Hydrophobic sidechain

High act vs. Gram-positive and has a poor act vs. Gram-negative

Transpeptidase

Important bacterial enzyme that catalyzes the final crosslinking of the bacterial cell wall. Targeted by penicillin and cephalosporin. Irreversible hibited by catalyzed horsporans

Cephalosporins

Disguise structure from penicillin

Second generation cephalosporin - cephamycins

One has greater residents to beta-lactamase enzyme. Two not active against pseudomonas aeruginosa

...

Inhibits - Blocks transglycosdiation vancomycin

Chloroquine

Shows some activity against Gram-negative it was found accidentally

Pharmacophore of quinone and fluoroquinolones

Pyridine ring and carboxylic acid are a must for activity

Protein kinase inhibitors

Serine threonine tyrosine are the main three. Cofactor ATP. Focus on binding site to block ATP

Has no off switch

Aspartate and glutamate

Active vs. Inactive

GTP vs. GDP

Epidermal growth factor

EGF


Receptor is a tyrosine kinase inhibitor receptor

Ic50

Inhibitory concentration you want it to be a small as possible nanometers is better than micrometers

Isotere

Replacing a group with same valency structure and stericy

Bioisotere

May not have same valency but the body treats it the same

In vitro

Pharmacodynamic

In viro

Pharmacokinetic

Ber-abl

Diffusion of chromosome 9 + 22

Conformational blocker

Methane group keeps group from freely rotating helps to maintain structure

Type 2 protein kinase inhibitor lilac

Prevent from becoming the active form

Hydrogen

In the ways of size fluorine compares to What atom

Ras protein

Active _____ normally Auto catalyzes hydrolysis of GTP back to GDP. Key event attaching to hydrophobic chain

Metabolic blocker

To help prevent oxidation of fluorine can replace a hydrogen

Ki

Inhibition equilibrium




If _____ is small then it favors the left side

Rigidity

Things that don't bend but they can eventually break



Zinc is a metal low enzyme co-factor

Antagonist

Block natural messenger strong more binding interaction

Agonist

Drug designed to mimic the natural messenger

Reverse antagonist

When binds does not induce transduction signal or change shape

ADME

Absorption distribution metabolism excretion

A levoli

Airsoft with single cell wall surrounded by Blood capillaries around fast effective Exchange

:-

Vh

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