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17 Cards in this Set
- Front
- Back
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Pharmacokinetics
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What the body does to the drug
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Pharmacodynamics
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What the drug does to the body
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molecular complementarity
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D and R are 3D so they must fit together
lock and key-shape, size, sterochemistry |
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recognition site
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place where drug binds in preference to other sites
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Acetycholine
Acetycholineesterase -->possible inhibitor |
Acetycholinesterase attracts acetycholine at anionic and esteratic site-->hydrolysis at esteratic site to form choline
inhibitor is EDROPHONIUM |
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IRREVERSIBLE BINDING
types bond strength result of bond |
covalent bond forms(alkylation, acylation, phosphorylation, or carbamoylation)
Bond Strength0 50-150Kcal/mol longlasting effect or cell death |
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Phenoxybenzamine
receptor site drug action |
long lasting blockade of alfa-adrenergic receptors
selective for alkylation of amino, sulfahydryl, or corboxyl groups antihypertensive drugs carcinogenic (high doses- and non-selective DNA alkylation) |
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Nitrosoureas
-->reacts with ? -->forms -->example |
reacts with water to form products that react with DNA and Proteins (DNA repair enzymes)
ex: Carmustine (BCNU) |
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Types of Reversible attractive forces
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Ionic
Ion-Dipole Dipole-Dipole Hydroven Van Der Waals Hydrophobic |
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Ionic Bonds
-->bond strength and proportions |
attraction between oppositely charged ions
5Kcal/mol q1q2/r example groups-- AA, carboxyl, phosphate |
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Dipoles
-->Bond strength -->proportions |
based on electronegativity of atoms and polarizability
1-5Kcal/mol 1/(r1*r2) |
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Hydrogen bons
-->bond strengths (atom dependent) -->drug examples |
-->special type of dipole-dipole bond
-->hydrogen partial positive linked to partial negative on O, N, F, S atoms 1-3Kcal/mol O-H..N > O-H..O > N-H..N ≈ N-H..O |
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Vander Waals Interactions
-->bond strength -->proportions |
non polar groups that aren't dipoles
-->Electrostatic attractive forces between induced dipole resulting from transient polarization of electron clouds of normal bonds in molecules most important groups are aliphatic or aromatic -->0.5-1Kcal/mol -->(1/r to the fourth)-(1/r to the sixth) --->mc must be really close for bond to occur |
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Hydrophobic Interactions
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Driving force bringing the drug- and receptor-nonpolar groups together is increased entropy resulting from lower ordering
-->complex Vand Der Waals forces at work |
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D-R attracton and binding
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Combination of several weak reversible bonds formed simultaneously is required to produce sufficiently strong D-R complex to differentiate specific from non-specific binding
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specific vs non-specific binding
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Major difference between non-specific binding and specific binding: strength of binding greater in specific binding
(and it produces a pharmacological effect) |
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complementarity: cholinergics
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acetylcholine (binds withmuscarinic and nicotinic receptors)
replace methyl groups loose activity No more thatn 5 atoms between N and H terminal |
