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17 Cards in this Set

  • Front
  • Back
Pharmacokinetics
What the body does to the drug
Pharmacodynamics
What the drug does to the body
molecular complementarity
D and R are 3D so they must fit together

lock and key-shape, size, sterochemistry
recognition site
place where drug binds in preference to other sites
Acetycholine
Acetycholineesterase
-->possible inhibitor
Acetycholinesterase attracts acetycholine at anionic and esteratic site-->hydrolysis at esteratic site to form choline

inhibitor is EDROPHONIUM
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
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)
Nitrosoureas
-->reacts with ?
-->forms
-->example
reacts with water to form products that react with DNA and Proteins (DNA repair enzymes)

ex: Carmustine (BCNU)
Types of Reversible attractive forces
Ionic
Ion-Dipole
Dipole-Dipole
Hydroven
Van Der Waals
Hydrophobic
Ionic Bonds
-->bond strength and proportions
attraction between oppositely charged ions

5Kcal/mol

q1q2/r

example groups-- AA, carboxyl, phosphate
Dipoles
-->Bond strength
-->proportions
based on electronegativity of atoms and polarizability

1-5Kcal/mol

1/(r1*r2)
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
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
Hydrophobic Interactions
Driving force bringing the drug- and receptor-nonpolar groups together is increased entropy resulting from lower ordering

-->complex Vand Der Waals forces at work
D-R attracton and binding
Combination of several weak reversible bonds formed simultaneously is required to produce sufficiently strong D-R complex to differentiate specific from non-specific binding
specific vs non-specific binding
Major difference between non-specific binding and specific binding: strength of binding greater in specific binding
(and it produces a pharmacological effect)
complementarity: cholinergics
acetylcholine (binds withmuscarinic and nicotinic receptors)

replace methyl groups loose activity

No more thatn 5 atoms between N and H terminal