lecture 1 Flashcards
trade name of semaglutide
ozempic
trade name of sertraline
zoloft
trade name of fluoxetine
prozac
trade name of alprolazam
xanax
drugs that have an anxiolytic effect and where they target
benzodiazepine and xanax
amygdala
what did thalidomide do and why and also what was it originally used for
birth defects in children in Germany - limb abnormalities; R-enantiomer(sedative) had different effects than S-enantiomer (Sinister); for sleep, morning sickness, leprosy, and blood cancers
what are compound centered drugs w examples
mix of natural and synthetic products w complex structures; penicillin (mold), cyclosporine, paclitaxel, morphine
paclitaxel used for what and why is it controversial
breast cancer, prostate cancer, ovarian and lung cancer; Pacific Yew tree is not common and dies after stripping bark
first antimitotic group and isolated from where and what does it do
taxanes; Western yew tree; stops microtubules from being broken down so that cells become clogged and can’t divide –> cell death by apoptosis
given as a neoadjuvant chemotherapy
paclitaxel
drugs that use natural compound as starting point
Insulin, L-DOPA, natural agonist serves as a skeleton that can be modified to create a
better agonist or antagonist.
– glucagon-like peptide-1 (GLP-1), an
incretin hormone with important effects on glycemic control and body weight regulation, led to efforts to extend its half-life and make it therapeutically effective in
people with type 2 diabetes (T2D).
ex. of GLP-1 agonist (mimics GLP)
ozempic
target-centered drugs are what? give an example
drugs against a biochemical or
molecular target associated with the disease e.g. HMG-CoA
reductase inhibitors block cholesterol synthesis (Statin drugs- Lipitor)
for atherosclerosis
high through-put screening drugs need what? give example
assay and library of
compounds needed e.g. Nonnucleoside reverse
transcriptase inhibitors - inhibit HIV Reverse Transcriptase- used as part of highly active antiretroviral
therapy (HAART) for the treatment of HIV type 1
structure based design drugs use what? give example
NMR or x-ray crystallography.
e.g. 1. HIV protease inhibitor has an unusual substrate
specificity (F-P bond rarely cleaved in humans)- ritonavir
(Box 38-3)
2. Gleevec for CML - Chronic Myelogenous Lukeimia
what are granulocytes and what do they do
white blood cells: neutrophils (phagocytes! also a white blood cell in the bloodstream), eusinophils (kill parasites and antigen-presenting cells), basophils (have receptors that can bind to IgE, IgG, complement, and histamine)
thalidomide binds what complex and what does this do
Cereblon (CRBN) E3 ligase complex; halts myeloma growth in Multiple myeloma
how do clinical drug trials work?
first, there is extensive preclinical research conducted which involves years of animal testing, ADME (absorption, distribution, metabolism, excretion), and may involve human cells, goes through FDA –> IND application –> PHASE 1: assesses drugs safety on 20-100 volunteers, pharmacokinetics and maximum dose before toxicity, major side effects, non-blinded –> PHASE 2: drug’s efficacy, randomized with a control group (placebo) and experimental group, may include several hundreds of people –> PHASE 3: provides thorough understanding of effectiveness, benefits, side effects, randomized and blind trials, large scale testing to thousands –> FDA approval –> Late Phase III/IV studies: monitor long-term effectiveness and cost effectiveness, as well as compare drug with others on the market
sildenafil failed to treat ____ and treated _____
hypertension/angina, erectile dysfunction
