Module 10 Flashcards
Pharmacodynamic can be affected by?
-age
-disease or disorder
-drug-drug interaction
Pharmacodynamic includes:
- site of action
- MOA
- receptor binding
- post-receptor effect
- chemical interaction
Receptor subtypes include:
- enzymes
- Ion channels
- membrane receptors
type of chemical interactions that drugs use to bind to receptors?
electrostatic interactions (INTERmolecular forces)
hydrophobic interactions
covalent bonds
stereospecific interactions (enantiomers)
Drug properties
Affinity
efficacy
potency
Affinity
how well the drug binds to the receptor
efficacy
how well the drug produces its desired effect
potency
term used to compare the relative affinity of competing drugs
Categories of Drugs
Agonist
antagonists (competitive and non-competitive)
Methods of drug administration
enteral (oral), parenteral (other than intestine) that include: intramuscular, subQ, IV, Inh
What determines the time to maximal concentration at the receptor to produce peak effect?
absorption rate
Bioavailability definition:
how much of the administered drug is actually absorbed (esp. in oral meds)
Factors that affect bioavailability?
MW
drug formulation
drug stability
1st pass metabolism
blood flow
gastric emptying
intestinal motility
drug interaction (polypharm)
What influences volume distribution?
blood,
total body H20,
ECF,
lymphatic fluids,
cerebrospinal fluids,
protein-binding
What are prodrugs?
convert from inactive form to active form
Two common chemical reactions of drugs being metabolized?
hydrolysis (esters, amides, nitriles)
REDOX reactions (P450)
What are the major routes of excretion?
kidney, feces, lungs, and sweat
What % of drugs fail in clinical testing?
90%
How many years is the drug development process?
usually 13 year process
Lipinski Rule of 5 used for?
used as a tool to measure a new chemical entity’s potential bioavailability
&
describes drug potential for a new chemical entity
Lipinski rule of 5 include?
hydrogen bond donor
hydrogen bond acceptors
MW
cLogP
What does more than one rule violation mean for the Lipinski Rule of 5?
(NCE) new chemical entity is non-orally available
Low ___ drugs with a low __ can easily cross cell membranes?
MW ; cLogP
What are the structural alerts? (5) why?
functional groups that have been linked to increased toxicity due to their metabolites.
aromatic anilines
nitroaromatics
aliphatic halides
polycyclic aromatic hydrocarbons
thiophenes
