lecture 1

Question 1

trade name of semaglutide

Answer 1

ozempic

Question 2

trade name of sertraline

Answer 2

zoloft

Question 3

trade name of fluoxetine

Answer 3

prozac

Question 4

trade name of alprolazam

Answer 4

xanax

Question 5

drugs that have an anxiolytic effect and where they target

Answer 5

benzodiazepine and xanax
amygdala

Question 6

what did thalidomide do and why and also what was it originally used for

Answer 6

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

Question 7

what are compound centered drugs w examples

Answer 7

mix of natural and synthetic products w complex structures; penicillin (mold), cyclosporine, paclitaxel, morphine

Question 8

paclitaxel used for what and why is it controversial

Answer 8

breast cancer, prostate cancer, ovarian and lung cancer; Pacific Yew tree is not common and dies after stripping bark

Question 9

first antimitotic group and isolated from where and what does it do

Answer 9

taxanes; Western yew tree; stops microtubules from being broken down so that cells become clogged and can’t divide –> cell death by apoptosis

Question 10

given as a neoadjuvant chemotherapy

Answer 10

paclitaxel

Question 11

drugs that use natural compound as starting point

Answer 11

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).

Question 12

ex. of GLP-1 agonist (mimics GLP)

Answer 12

ozempic

Question 13

target-centered drugs are what? give an example

Answer 13

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

Question 14

high through-put screening drugs need what? give example

Answer 14

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

Question 15

structure based design drugs use what? give example

Answer 15

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

Question 16

what are granulocytes and what do they do

Answer 16

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)

Question 17

thalidomide binds what complex and what does this do

Answer 17

Cereblon (CRBN) E3 ligase complex; halts myeloma growth in Multiple myeloma

Question 18

how do clinical drug trials work?

Answer 18

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

Question 19

sildenafil failed to treat ____ and treated _____

Answer 19

hypertension/angina, erectile dysfunction