Term
|
Definition
| insensitivity to drug caused by repeated chronic administration |
|
|
Term
| What is innate tolerance? |
|
Definition
| Genetically determined (polymorphisms) |
|
|
Term
| What are the two types of learned tolerance? |
|
Definition
Behavioral- patient learns to cope with condition( ex alcoholics)
conditioned- environmental clues related to drug use can cause reflexes |
|
|
Term
| What are the three types of acquired tolerance? |
|
Definition
Pharmacokinetic- "dispositional" deals with absorption and metabolism
pharmacodynamic- changes to receptors and mediators
Cross tolerance- tolerance to a drug similar not given due to similar structure to the one that was given |
|
|
Term
| What are the steps of G-protein coupled receptor(GPCR) desensitization? |
|
Definition
1)Phosphorylation
2)internalization
3)downregulation(degradation) |
|
|
Term
| Describe the phosphorylation step of GPCR desensitization. |
|
Definition
GPCR's are phosphorylated by kinases which causes it to uncouple
happens within seconds |
|
|
Term
| Describe the internalization step of GPCR desensitization. |
|
Definition
phosphorylated GPCR's form clusters with clathrin-coated pits which then causes it to internalize by endocytosis
after this happens it is called an early endosome
happens within minutes |
|
|
Term
| Describe the downregulation(degradation) step of GPCR desensitization. |
|
Definition
| chronic treatment can cause the GPCR to go from early endosome to late endosome and the lysosome for destruction |
|
|
Term
| What is the alternate pathway to downregulation if chronic treatment does not occur? |
|
Definition
| dephosphorylation and return of the GPCR to surface |
|
|
Term
| What is heterologous desensitization? |
|
Definition
cross tolerance
slow to develop |
|
|
Term
| What kinds of drugs are associated with tolerance and receptor desensitization? |
|
Definition
|
|
Term
|
Definition
psychological dependence
either to create euphoria or stop diseuphoria |
|
|
Term
| What is the reward and reinforcement pathway? |
|
Definition
| mesolimbic dopaminergic reward pathway |
|
|
Term
|
Definition
physiological dependence
physical symptoms
associated with withdrawal syndrome |
|
|
Term
| What are the 6 approaches to drug discovery? |
|
Definition
1)identify new drug target
2)rational drug design
3)Chemical modification of a known molecule
4)screen for biological activity
5)biotechnology and recombinant DNA
6)drug combinations |
|
|
Term
| What are the 2 methods for further development of leads? |
|
Definition
compound based approach
target based approach |
|
|
Term
| What is the compound based approach to further development? |
|
Definition
| looking at a compound to see what it can affect |
|
|
Term
| What is the target based approach to further development? |
|
Definition
| identifying a target and trying to develop a compound to affect that target |
|
|
Term
| Differentiate the three compound based methods for further development. Naturally occurring, synthetic, and metabolites. |
|
Definition
naturally occurring- isolate from natural product
synthetic- structure analyzing
metabolites- from other currently existing drugs |
|
|
Term
| Differentiate the methods of target based approach for further development. Systemic and screening |
|
Definition
| systemic is trying to understand the mechanism of action synthesizing compounds to work with it while screening is just testing a bunch of chemicals to see how they affect it |
|
|
Term
| What is combinatorial chemistry? |
|
Definition
| using a small number of precursors to make a lot of derivatives |
|
|
Term
| What is High-throughput screening? |
|
Definition
| using robotics to rapidly screen chemicals for their biological activity |
|
|
Term
| What are the ideal properties of drugs? |
|
Definition
efficacy
selectivity
efficient delivery
good ADME
no side effects
good physiochemical parameters |
|
|
Term
| How long to get a drug to market? |
|
Definition
|
|
Term
| Out of the 100 drugs that enter phase 1 trials how many make it to the market in phase 4? |
|
Definition
|
|
Term
| What are preclinical studies used to characterize? |
|
Definition
| chemical(synthesis, isomers, etc) and biochemical(toxicity) properties |
|
|
Term
| What is an investigational new drug (IND) application? |
|
Definition
| the application to the FDA to start clinical trials |
|
|
Term
| Describe phase 1 clinical trials |
|
Definition
safety
20-100 people (usually healthy)
takes up to one year |
|
|
Term
| Describe phase 2 clinical trials |
|
Definition
efficacy
hundreds of people with condition
single blind
up to 2 years |
|
|
Term
| Describe phase 3 clinical trials |
|
Definition
thousands of individuals with condition
double blind
up to 4 years |
|
|
Term
|
Definition
| postmarketing surveillance |
|
|
Term
| What is a new drug application(NDA)? |
|
Definition
| a reports thousands of pages that is submitted to FDA in order to be approved to market the drug. |
|
|
Term
| Which drugs can get to the market faster priority or accelerated? |
|
Definition
accelerated aka fast-track drugs(life threatening diseases)
priority are just special need if shortage of other agents to treat the disease |
|
|
Term
|
Definition
drugs only helping 200,000 people or less.
GOV gives incentives to make them |
|
|
Term
| What must companies submit to get a generic equivalent on the market? |
|
Definition
| ANDA abbreviated new drug application |
|
|
Term
| Whats the risk when doctors prescribe meds for off label use? |
|
Definition
|
|
Term
| Whats the issue with dietary substances concerning the FDA? |
|
Definition
| FDA doesnt have to evaluate efficacy only safety and health claims |
|
|
Term
| What does CDER do for the FDA? |
|
Definition
| oversees development, postmarket, and quality throughout life cycle |
|
|
Term
| Should you give morphine more or less frequently to newborns? |
|
Definition
| less because morphine is hydrophilic and newborns have higher body water percent than adults thus the drugs stays in the body longer |
|
|
Term
| Should you give fentanyl more or less frequently to newborns? |
|
Definition
| more since it is hydrophobic and distributes less in the newborn and is eliminated quicker |
|
|
Term
| A week after birth to 2 years old what is a childs pH in the stomach? |
|
Definition
7
this means acid liable drugs (penicillin) have way higher bioavailability in kids |
|
|
Term
| Do children have increased or decreased gastric emptying time? |
|
Definition
decreased so drug effect takes longer
slow till 6-8 months |
|
|
Term
| Is GFR reduced or increased in children? |
|
Definition
| reduced so drugs extensively eliminated through kidneys remain in body longer |
|
|
Term
| Is liver function increased or decreased in children? |
|
Definition
| decreased and it fluctuates non linearly with age |
|
|
Term
| Should parents give fever reducing medications after a child receives a vaccine? |
|
Definition
| no it can reduce effectiveness of the vaccine by 50% |
|
|
