Summery Info-DD Flashcards
Phase One Reactions
Oxidations
Hydrolysis
Reductions
Phase Two Reactions
Conjugations
Phase One Enzymes
CYP450
esterase-amidase
reductase
Phase Two Enzymes
Transferase
Gen Polymorph Phase 1 and 2
significant
Phase One Induce- Inhibit
Significant
Phase Two Induce-Inhibit
Possible- Less
FDA Regulates
Drugs to be sold to the public
Evaluate new drug safety
Prescription vs non
State regulates
who can prescribe drugs
Local regulates
drug use in their area
Schedule 1
no medical use
high abuse potential
high phys/psy dependance
Schedule 2
medical use
high abuse potential
high phy/psy dependence
Schedule 3`
Medical use
Moderate abuse potential
moderate/high dependence
Schedule 4
medical use
Low abuse
Low dependence
Schedule 5
medical use
limited abuse
lowest dependence
Phase One CT
is it safe?
Pharmacodynamics- metabolism, toxicity, response
~100 Healthy human
Phase Two CT
Does it work in patients?- compare placebo/existing treatment with new
Also safety and dose
200-300 Subjects
Phase Three CT
Does it work Double Blind-
a. Compare established therapies
b. Adverse rxn studies
c. FDA grants approval
1000-6000 people
Phase Four CT
Post market surveillance
a. Mortality/morbidity
b. Physicians must report adverse reactions
Animal Studies
Follows in vitro tests (synthesis and bio products)
Efficacy
Safety
Mechanism
Most rapid (sec to min) onse
Inhalational (volatile gas-aerosol), intravenous
Intermediate (5-15 min) onset
Sublingual, intramuscular, subcutaneous, buccal
Slower (15-30 min) onset
Oral - immediate release formulations
Slowest Onset (hours)
Transdermal, Oral - enteric-coated and sustained release formulations, IM and SC (depot forms)
Vd 3-5 compartment
Highly bound to plasma proteins
Vd 12-15 compartment
Highly water soluble. enters the cell poorly
Vd 42 L compartment
drugs that freely enter cells
Over 50 Vd
often highly lipid soluble
Sequesters at spesific site ex: CNS, Fate, Protein
pH>pKa
A- and B predominate
pH<pKa
HA and BH+ predominate
Inducer/Inhibitor definition
Inducer: Increase CL (7-10 days)
Inhibitor: Inhibit CL, inc drug levelsto possibly toxic
Cimetidine
Inhibitor
Phenytoin
Inducer
Erthromycin/clarithromycin
inhibitor
Azol Antifungal
Inhibitor
Carbamazepine
Inducer
Phase One saturablity
minimal