Med Chem Chapter 11

Three phases of drug action are

pharamaceutical, pharmacokinetics, pharmacodynamic

Disintegration of a pill or capsule in the GIT, rease of the drug, dissolution of the drug is what

pharmaceutical phase

Absorption from the GIT into the blood supply, factors affecting the drug durviaial and progress to the target is..

pharmacokinetic phase

mechanism by which the drug interactis with the target, resulting pharmacological effect is:

pharmacodynamic phase

drug design should consider both _ interactions and _.

binding, phamacokinetics

ADME stands for

absorption, distribution, metabolism, excretion

Drug absorption:

orally taken drugs must cross the _ to reach the blood supply.

most orally active drugs pass through the cells _ in the gut wall.

Drugs are required to cross ___.

Balance of _ / _ character is required.

orally active drugs usually obey ___.

polar drugs can be administered by _.

polar drugs can be targeted vs gut infections.

gut wall, lining, 2 fatty cell membrane, hydrophobic, hydrophilic, lipinski’s rule of five, injection

many drugs have _ functional group

amine

effective drugs contain amine groups with a pka range

6-8

amines help balance the dual requirement for drugs to be _ and _.

water, fat solub;e.

Lipinkski’s rule of five:

orally active drugs generally show a balance of hydriphillic and hydrophobic properties and obey at least three of the following rules:

mw < 500, no more than 5 HBD group, no more than 10 HBA groups, log P < +5

P in the lipinski’s rule of five stands for

lipophilicity

Lipinksis rule of 5 exceptions:

Small polar molecules < , that cross the gut wall through small pores between cells.

polar molecules carried across the membrane by transport proteins - , , and some drugs (example _, transported by transport proteins for dipeptides.

mw, 200, amino acids, nucleic acid bases, Lisinopril

Drug Absorption Exceptions

_ a process allowing the passage of _ into a cell without actually crossing the cell membrane.

The drug is engulfed by the cell membrane and a membrane bound vesicle is pinched off to carry the drug across the cell and then the other side.

pinocytosis

Beber’s parameters - independe of molecular weight

_ is important to drug absorption - more _ less likely orally active.

to many _ bonds is bad for absorption

the polar surface of the molecules plays a role

_ is not a factor

molecular flexibility, flexibility, rotatable, molecular weight

drug distribution

once across the gut wall the drug entered _.

cell lining of blood vessels are _ fitting.

do you need the drug to cross cell membrane?

drugs can