Intro I and II, Drug Development Flashcards
Define chemical name
specific compound’s structure; long
Define generic name
derived from chemical name; shorter-ish
Describe schedule I substance and examples
substances with no currently accepted medical use and high potential for abuse
Ex. heroin, LSD, marijuana, MDMA
Describe schedule II substances and examples
substances with a high potential for abuse w/ use potentially leading to severe psychological of physical dependence; accepted medical use
Ex. methylphenidate, methamphetamine, oxycodone, morphine, methadone, hydromorphone, fentanyl, cocaine
Describe schedule III substances and examples
moderate to low abuse potential compared to schedule II
Ex. anabolic steroids, testosterone, codeine, ketamine
Describe schedule IV substances and examples
Schedule IV: lower abuse potential and risk of dependence compared to schedule III
Ex. diazepam, lorazepam, phenobarb, propoxyphene, tramadol
Describe schedule V substances and examples
lowest abuse potential
Ex. low dose opioids in cough meds, lamotil, pregabalin
Define pharmacokinetics (PK). What is it composed of?
what the body does to the drug
absorption, distribution, metabolism, excretion (ADME)
Define pharmacodynamics (PD). What is it composed of?
what the drug does to the body
MOA, dose response, effects, SE
Describe absorption, passive diffusion
H2O and water soluble substance and small lipids move w/ concentration gradient
Describe absorption, active transport
minerals, some sugars, and most amino acids move against a concentration gradient w/ an input of energy
What factors affect distribution
-tissue permeatbility
-BF
-binding plasma proteins
-binding to subcellular components
What organ is a major site of drug elimination?
kidney
Define clearance rates for excretion
ability of all organs and tissues to eliminate drug or ability of single organ/tissue to eliminate drug
Define half-life of excretion
amount of time required for 50% of drug remaining in body to be eliminated
Phase I drug metabolism; what happens and what is involved
oxidation (CYP 450) and reduction
polar (water soluble) metabolite often still active
Phase II drug metabolism; what happens
conjugation of reactive groups inserted in phase I
large polar metabolite by adding endogenous hydrophilic groups to form water-soluble inactive compounds
Components of phase II drug metabolism
Glucuronidation, sulphate, glycine, acetylation, methylation
Define bioavailability
amount of substance that enters the bloodstream and is available for the body to use
Define bioequivalence
two different versions of a drug that work the same way
What are major organs of drug metabolism and excretions?
liver and kidneys
What factors affect the variations to drug response?
-disease
-genetics
-age
-diet
-gender
-drug interactions
-environmental
-obesity
-exercise
-cigs/alcohol
Define dose response
provides info about dosage range over which drug is effective
Define potency
quantity of drug necessary to produce of given effect
Define efficacy
maximum response that can be achieved with a drug
Define median effective dose
E50
dose 50% of population responds to drug in specific manner
Define median toxic
T50
dose 50% of group exhibits AR’s
Define median lethal dose
L50
dose causes death in 50% of the group; not used in human trials
Define agonist/full agonist
affinity or efficacy
Define partial agonist
do not evoke max response and does not fully activate receptor
Define antagonist
affinity only (but may have efficacy by inhibiting inhibitory neuron)
Define additive effects
2 chemical effects = sum of 2 chemicals taken separately
Define synergistic effects
2 chemical effects > sum of separate effect at same doses
Define tolerance, dependence, addiction
T: decreased rxn to drug after repeated use
D: person dependent on drug to fx
A: inability to control drug use
Describe the 3 main stages of the progress of drug development
-preclinical testing (animal trials provide info about PK and PD, dosage and toxicity)
-human clinical trials
-post marketing surveillance
What are the 4 phases of drug development
I: is it safe? PK?
II: does it work?
III: does it work double-blind?
IV: post marketing surveillance
Define investigational new drug (IND), new drug app (NDA), FDA
Investigational new drug: a drug that is not approved by FDA
New drug application: app to get approval from FDA
Food and drug admin: approves drugs
List the various routes of admin (6)
oral, sublingual/buccal rectal, inhalation, injection, topical
Oral vs parenteral route of admin
parenteral skips 1st pass
first pass: drug metabolized BEFORE reaching circulation (goes through digestive system)
