Basic Principles

Question 1

the route of administration can effect drugs’ bioavailability? t/f

Answer 1

True

Bioavailability: tells us what % drug gets into systemic circulation

• Systemic circulation = blood supply to body
• Ex: IV = 100% bioavailable
• Ex: Orally may vary

Question 2

First pass effect will not be avoided by giving a drug rectally? t/f

Answer 2

False

The last 6 inches of the rectum bypass the liver and therefore make it to systemic circulation

First pass effect:
- when you take anything by mouth it gets absorbed and the first place it goes = mesenteric veins of GI tract then to portal system which delivers to the liver

• the liver sees the drug before the systemic circulation, and may filter it out before it does what we want
• natural mech derived so that when we eat toxin = gets rid of it so we do not die
• anything from the esophagus down goes through this system EXCEPT the last 6 in of the rectum

Question 3

Loading dose is when an amount of drug is given IV over a short duration

Answer 3

False

Loading dose: when we give a dose of meds that is larger than our maintenance dose in order to reach a steady state faster

-ex: first dose may be bigger than the rest of the doses in order to get their plasma levels higher or what not
Ex: if you give med IV over short period of time FOLLOWED by IV drip of the same med = loading dose

Question 4

bioidentical is when 2 drugs have the same pharmacologic effect

Answer 4

False

Bioidentical= means the drug is molecularly exactly the same as a hormone already in the body
ex: we give people human estrogen

same Pharmacologic effect: means they are therapeutically identical but not necessarily bioidentical

Question 5

Therapeutic knowledge:

• indications
• pharmodynamics
• contraindications
• drug interactions
• pharmocokinetics
• dosage regimen
• economic considerations

Answer 5

• indications: what are the reasons it is ok to use this drug (FDA)
• pharmodynamics: what the drug does to the body
• contraindications: is this drug going to do more harm than good (ex: severe allergy to the drug)
• drug interactions: can be fatal
• pharmocokinetics: what the body is doing to the drug (absorbed, distributed, how does it get rid of it, what metabolizes it)
• dosage regimen: parameters set, EBM approach
• economic considerations $$

Question 6

What makes up diagnosis and management

Answer 6

When you have therapeutic knowledge and performed assessment = you can have diagnosis and management

Question 7

What is a drug

Answer 7

medicine or other substance which has a psychological effect when ingested or otherwise introduced into the body (doesnt have to have a receptor = mineral oil)

Question 8

What is a receptor

Answer 8

broadly defined as any compound within the body that drug binds to = effect

• most often drugs bind to endogenous substances
• usually protein tissue type (everywhere in body)

Question 9

Iigand

Answer 9

something (usually drug or naturally in the body) that binds to a receptor to serve a biological purpose
- can counteract a process or enhance

• when ligand binds to receptor= effect

Question 10

side effect

Answer 10

when drug binds to receptors we did not intend on it binding to = causing other effects to occur

Question 11

drugs do not create effects, only modify ongoing ones (t/f)

Answer 11

true

• drugs do not put new functions into cell only effect their expression

Question 12

agonists

Answer 12

facilitate receptor response

• bind to a receptor and turn it on (mimic the neurotransmitter normally binding there)
• some have higher affinity than neurotransmiter
• can turn off a process

Question 13

antagonist

Answer 13

inhibit receptor response

• blocks neurotransmitter and agonist from binding (which prevents them from turning something on or turning something off)
• can be permanent ( body will just make a new receptor)
• just binds to the receptor-> doesn’t activate anything

Question 14

permanent binding of a drug is done with what bonds

Answer 14

covalent

Question 15

partial agonist

Answer 15

bind to receptor, can activate/turn on receptor a partial amount, but off most of the time

• get some effect but not as much as full agonist
• common pain meds

Question 16

pharmacology def

Answer 16

study of meds and how they interact with body

Question 17

toxicology vs pharmacology

Answer 17

the only difference is the dose

ex: botulism used in small doses for botox

Question 18

pharmacology vs therapeutics

Answer 18

therapeutics applies pharmacology clinically to treat disease

Question 19

pharmacist vs pharmacologist

Answer 19

pharmacist: dispense appropriate meds
- collab with prescribes = resource
- help with insurance questions
- can help manage diseases through therapeutics after given the diagnosis

pharmacologist:

• in lab, testing
• create the drug`

Question 20

Drug size

Answer 20

• vary
• avg= 100-1000 mw
• too big= difficult time moving between membranes
  ex: insulin, interferon

Question 21

sloppy drugs

Answer 21

those that bind to more than one receptor

• we want clean drugs = unique and have one specific receptor = decrease in side effects

Question 22

what are the three drug bonds

Answer 22

covalent = irreversible
electrostatic
hydrophobic

Question 23

drug shape

Answer 23

usually complimentary to shape of receptor (glove and hand)

ex why shape important: antidepressant

• causes serotonin to not be able to leave as fast
• antidepressant fits into serotonin receptor and gets stuck (bc of big trailing group) aka preventing things from passing

Question 24

shape matters

Answer 24

enantiomers and isomers= drug can be completely different or inert

aka why cheaper drugs made in unregulated places= sketchy

Question 25

what determines the duration of how long a drug works

Answer 25

how much of the drug you have the affinity of the drug to the receptor half life = rate of removal how sloppy is the drug= is it binding to right spot inert binding sites

Question 26

Pharmacokinetic principles | ADME

Answer 26

A= absorption D= distribution M= metabolism E= excertion

Question 27

A in ADME

Answer 27

A= absorption - orally (PO/SL), - rectally (supp, enema), - nasal, - parenteral (IM, IV, SC, IO, or transdermal vis path/ topical ) can be injected into bone too

Question 28

parenteral

Answer 28

administered or occurring elsewhere in the body than the mouth and alimentary canal.

Question 29

D in ADME

Answer 29

distribution - gets distributed into diff tissues at diff rates - realize that drug goes everywhere not just to target area

Question 30

M in ADME

Answer 30

m= metabolism - go to the liver to get metabolized then to kidneys for excretion - if super water soluble will just go to kidneys - we make things more hydrophilic sometimes so liver will stick polar groups on it... IDK why tho

Question 31

E in ADME

Answer 31

E= excreted - via hair, skin, breath, nails, urine

Question 32

where is the site of transformation of drugs usually

Answer 32

liver

Question 33

how do they study where the drugs go in the body

Answer 33

1. animal models 2. radiolabeled drugs 3. AI to test/predict

Question 34

What are the different receptor types

Answer 34

1. intracellular receptors 2. ion channel or pore 3. g protein mediated receptor 4. transmembrane receptor 5. ligand gated channels