EXAM 4 Flashcards
Pharmacodynamics (definition, includes what, affected by what)
- study of effects of drugs on body
- includes: 1) site of action, 2) mechanism of action, 3) receptor bindings, 4) post-receptor effects, 5) chemical interactions
- affected by: 1) disease/disorder, 2) age, 3) drug-drug interactions
Receptor subtypes
1) enzymes
2) ion channels
3) membrane receptors
Chemical interactions that affect drug binding
1) electrostatic interactions (intermolecular forces)
2) hydrophobic interactions
3) covalent bonds
4) stereospecific interactions (enantiomers)
Pharmacokinetics affect the following: (4)
1) drug administration
2) therapeutic dosing
3) time intervals between drug dosing
4) toxic dosing
Factors affecting bioavailability: (8)
1) MW of drug
2) drug formulation
3) drug stability (pH sensitivity)
4) first pass metabolism (liver)
5) blood flow
6) gastric emptying (food slows process)
7) intestinal motility
8) drug interactions
Distribution of a drug (influenced by 6 things)
1) blood
2) total body water
3) extracellular fluids
4) lymphatic fluids
5) cerebrospinal fluids
6) protein binding
hydrolysis metabolizes what types of bonds?
- esters
- amides
- nitriles
- occurs in the pancreas
REDOX metabolizes with what?
- cytochrome P450 (liver)
main routes of excretion (4):
- kidneys (majority)
- feces (unabsorbed/metabolites from bile)
- lungs (anesthetics)
- sweat (not common)
Lipinski rule of 5
- describes drug potential for a new chemical entity (NCE) that is used as a tool too measure potential bioavailability
Lipinski rule of 5 based on:
- H bond donors (amines/alcohols)
- H bond acceptors (total number of N, O and F)
- MW
- calculated partition coefficient (cLogP)
violation of more than 1 rule = not orally available
lipophilic moiety
charge transfer
hydrophilic moiety
- h bonding
- van der waals
ester linkage
- dipole interaction
- van der Waals interaction
functional groups with increased toxicity (5)
- aromatic anilines
- nitroaromatics
- aliphatic halides
- polycyclic aromatic hydrocarbons
- thiophenes