Exam 4 Study Guide Flashcards

1
Q

what is a lead compound

A

structure that had some activity against the chosen target, but not yet good enough to be the drug itself

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2
Q

what is meant by SAR

A

Structure-Activity-Relationships

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3
Q

pharmacophore definition

A

the structural features directly responsible for activity

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4
Q

pharmacodynamics vs pharmacokinetics

A
  • pharmacodynamics = explores what a drug does to the body
  • pharmacokinetics = explores what the body does to the drug
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5
Q

how do most pharmaceutical companies choose the disease of interest

A

big market, developed countries

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6
Q

what is the orphan drug act of 1983

A

encourage pharmaceutical companies to develop drugs to treat diseases which affect fewer than 200k people in the US

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7
Q

how has human genome mapping helped with drug development

A

people can work with a specific enzyme or receptor to discover its structure and biological function

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8
Q

in vitro definition

A

in an artificial environment

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9
Q

in vivo definition

A

in the living body

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10
Q

ex vivo definition

A

doing test on tissue taken from a living organism

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11
Q

in vitro advantages and disadvantages

A
  • advantages: speed and small amount needed
  • disadvantages: may not translate into living animal
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12
Q

in vivo advantages and disadvantages

A
  • advantages: can be translated to living organism
  • disadvantages: more expensive, can cause suffering/side effects
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13
Q

ways for companies to find lead compounds

A
  1. screening natural products
  2. screening synthetic banks
  3. using someone else’s lead
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14
Q

once the lead is discovered, why is studying the SAR important

A

to identify the pharmacophore, or exactly what is responsible for the biological activity; can enable a more precise and active molecule

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15
Q

what is the ADME of drugs

A

Absorption
Distribution
Metabolism
Excretion

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16
Q

what is Phase I of metabolism

A

small chemical changes that make the compound more hydrophilic so it can be eliminated by kidneys; detoxify or toxify

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17
Q

what is cytochrome P450

A

responsible for most Phase I metabolism reactions

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18
Q

what is Phase II of metabolism

A

links drug to more polar molecules to make it even easier to excrete; commonly detoxify

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19
Q

what is Phase III of metabolism

A

uses drug transporters to move drug across cellular barriers

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20
Q

what are some of the key issues for a company when manufacturing a new drug

A

toxicity, drug must be able to be “scaled up” in quantity to be sold at a profit, efficient synthetic route needed

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21
Q

thalidomide tragedy

A

prescribed for morning sickness, caused malformities, led to laws requiring safety tests for during pregnancy before approval

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22
Q

Type A vs Type B ADRs

A

Type A: known but undesirable, dose-related
Type B: unknown, rare, unpredictable

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23
Q

detoxification vs toxification

A

Detox: make less toxic
Toxify: make toxic

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24
Q

6 mechanisms of toxicology

A
  1. allergic responses
  2. receptor, ion channel, and enzyme-mediated toxicity
  3. biochemical pathways
  4. organ-directed toxicity
  5. mutagenesis and carcinogenesis
  6. teratogenicity
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25
Type I vs Type II hypersensitivity
Type I: IgE-mediated, anaphylactic Type II: antibody-mediated, deplete blood cells
26
example of receptor-mediated toxicity
puffer fish uses tetrodotoxin to block Na+ channels
27
example of a toxin that blocks a biochemical pathway
cyanide prevents cellular respiration
28
what two organs are common targets for toxicity
liver and kidneys
29
hepatic necrosis definition
necrosis of liver
30
hepatitis definition
inflammation of liver
31
cirrhosis definition
chronic liver damage
32
how is acetaminophen toxic
can cause mitochondria damage
33
what are three ways kidneys are affected by toxins
1. changes to GFR 2. allergic nephritis 3. chronic nephritis
34
mutagenesis definition
changes to cell DNA that are passed on when cell divides
35
carcinogen definition
agent that produces a neoplastic cell
36
proto-oncogene vs tumor suppressor gene
Proto-onco: promote cell cycle progression, cause uncontrolled dividing Tumor: inhibits cell cycle progression, stops tumors from being disposed of
37
three important steps/tests in pre-clinical testing
1. in vitro cytogenetic evaluation 2. carcinogenicity testing 3. reproductive testing
38
what is LD-50
lethal dose 50; dose of drug to kill 50% treated
39
what is the NOAEL
no observed adverse effects lethal; highest concentration with no toxic response
40
how does the NOAEL translate to the HED
1. determine NOAEL 2. convert to Human Equivalent Dose (HED) 3. apply >10 fold safety factor
41
what is the LOAEL
lowest observed adverse effects lethal
42
what is the therapeutic index
the ratio of the dose of drug that produces an unwanted effect to that producing a wanted effect
43
why is sulfonamide disaster of 1937 important
antifreeze; killed over 100 patients; led to the 1938 Federal Food, Drug, and Cosmetic Act
44
clinical trial definition
a prospective biomedical or behavioral research study of human subjects that is designed to answer specific questions about biomedical or behavioral interventions
45
what is the IRB
Institutional Review Board; intended to review and approve biomedical research involving people
46
what is meant by informed consent
people have enough cognitive ability and information to make the proper decision on whether or not they want to participate in the study
47
important points of a clinical trial
1. Phase I - first time to evaluate safety 2. Phase II - efficacy and further evaluate safety 3. Phase III - test efficacy in large groups 4. Phase IV - after market, monitor long-term side effects
48
goal of aseptic technique
to prevent contamination, healing without infection
49
4 basic sources of bacteria in a surgical situation
1. air 2. patient 3. personnel 4. instruments and tools
50
contamination definition
the process by which something is rendered unclean or non-sterile
51
sterile field definition
area where there are no living microorganisms present
52
initial procedures for aseptic technique
1. clean and disinfect operating room 2. prep incision site and draping the animals 3. aseptic prep for surgical team 4. sterilization of surgical instruments and materials
53
in what situations is sterile technique required
survival, major, and minor surgeries
54
how to avoid contamination of sterile field
do not touch anything unsterile or dirty, keep hands above waist, do not touch materials
55
criteria for a good surgical room
well-organized with space to move and minimal clutter; high air exchange rate
56
criteria for good personnel in a surgical room
communication, attention to detail, work well under pressure
57
scrub technique
1. cap, mask, shoe covers 2. cover hands and forearms with soap 3. clean nails scrub with bristle from fingertip to elbow 4. each surface 5 mins 5. fingers 10 strokes each surface, fingernails/hands 20 strokes each, arms 10 strokes each surface 6. rinse 7. repeat twice 8. dry with sterile towel
58
clean but not sterile vs sterile
clean: visibly clean sterile: no contamination
59
steps to surgically prep a patient
1. food withdrawal if needed 2. physical exam 3. clean/groom 4. hair removal 5. surgical soap 5 mins 70% ethyl alcohol 6. drapes
60
what are antiseptics
prevents growth of microorganisms
61
what are sterile drapes
place around the proposed surgical incision to keep bacteria out of incision and body cavity
62
ways to maintain sterility
follow aseptic techniques, use only sterile equipment
63
forceps function
for compressing and grasping tissue
64
needle holders function
hemostat-like device to hold needles used to suture wounds closed
65
scalpel and blades function
cutting of tissue and skin
66
scissors function
cut things usually blunt-blunt, blunt-sharp, or sharp-sharp
67
retractors function
pull overlying tissue away from surgical site
68
sutures types and sizes
thickest is 6, bigger number is smaller diameter synthetic or natural
69
gauze pad function
sponges used for soaking up blood and other fluids from surgical site
70
different ways to sterilize equipment
1. steam 2. chemical 3. dry heat
71
anesthesia definition
abolition of sensation
72
general vs local anesthesia
General: fully unconscious Local: numbed body part
73
what makes something an ideal general anesthetic
unconsciousness, amnesia, analgesia
74
analgesia definition
loss of pain perception
75
amnesia definition
inability to recall what took place
76
methods of administering anesthesia
1. inhalation 2. intravenous 3. intramuscular
77
what is the mechanism of action of an anesthetic
1. hyper polarize neurons 2. suppress nervous system communication 3. suppress norepinephrine 4. cardiovascular depressant 5. respiratory depressant
78
4 stages of anesthesia
1. Stage I - onset 2. Stage II - excitement 3. Stage III - surgical 4. Stage IV - OD/death
79
what are adjuvants
drugs that are given with the anesthetic before, during, and after anesthesia
80
what are other medications used in conjunction with anesthetics
1. preoperative medications 2. sedative-hypnotics 3. antiemetics 3. antihistamines 4. narcotics
81
what makes something an ideal anesthetic
1. rapid and pleasant induction 2. rapid changes in depth 3. adequate muscle relaxation 4. wide margin of safety 5. lack of toxic/adverse effects
82
risk factors for anesthesia
1. CNS factors 2. cardiovascular factos 3. respiratory factors 4. renal and hepatic function
83
what is the MOA for inhaled anesthetics
cross blood brain barrier, enter plasma membrane and disrupt sodium channel structure, decreases neuronal excitability
84
unique features of inhaled anesthetics
eliminated unchanged
85
what is MAC
minimum alveolar concentration how anesthetic potency is measured
86
what is malignant hyperthermia
A drastic and uncontrolled increase in skeletal muscle oxidative metabolism, which overwhelms the body's capacity to supply oxygen, remove carbon dioxide, and regulate body temperature
87
methods to monitor patient under anesthesia
1. body temp 2. CRT 3. pulse 4. breathing 5. eye position 6. machines 7. body temp
88
what is included in appropriate post-op care
1. food and water 2. watch behavior 3. recovery cage 4. BE ALERT
89
acute pain symptoms
1. guarding 2. crying 3. self-mutilation 4. restlessness 5. sweating/panting 6. tooth grinding 7. recumbency 8. ambulation 9. abnormal posture
90
chronic pain symptoms
1. limping 2. licking and rubbing 3. reluctant to rise and move 4. loss of apetite 5. behavior change 6. change in bowels/urination 7. lack of self-grooming