Essentials To Pharmacology

Front 1

Pharmacodynamics

Back 1

what the drug does to the body.

Hint 1

pharmaco-D-ynamics

Front 2

Drug properties

Back 2

3-D in shape, solubilities (water,oil/fat), elect charges(acid/base)
***these encourage or inhib drug from going thru body and also it's effect

Hint 2

what's it look like and move thru?

Front 3

Drug effects: actions

Back 3

act thru receptors; rely on lock-key fit; Must reach receptor at concentration to trigger effect; specific enough to limit other effects (SE), grouped into 2 processes

Front 4

Therapeutic vs adverse effect:

Back 4

Therapeutic: what trying to achieve
Adverse: (SE) what trying to avoid 1.toxic (OD,interactions) vs Idiosyncratic/allergic effects (surprise)

Front 5

Risk:Benefit Ratio

Back 5

balance btwn probability of Tx & Adv Effects

Front 6

Drug Receptors

Back 6

1.macromolecular components of an organ that drug binds
2.result in change of physiologic function
3.Most are proteins on surface of cell
4.for endogenous molecules

Front 7

Agonist

Back 7

Mimics signaling of endogenous compound

Hint 7

drug receptor interaction

Front 8

Antagonist

Back 8

Blocks normal signalling

Front 9

Partial agonist

Back 9

Yields an attenduated signaling (lock/key); close to fitting, but only partially; can start compound reaction
Ie. block hr getting too high, but won't go too low that you pass out

Front 10

What constitutes if there is a hypo- or hyper-reactivity with an interaction?

Back 10

1. concentration of the drug at the receptor
2. concentration of receptor
3. function of receptors (genetically- will mafunct if not enough receptors)
4. components of resonse distal to receptor
5. Genetic variants (can now test for enzyme before giving- a drug that could kill the person if they didn't have the enzyme)

Hint 10

think receptors

Front 11

Pharmacokinetics

Back 11

what the body does to the drug
Absorption
Distribution
Metabolism
Excretion

Front 12

Therapeutic range

Back 12

range of drug tissue concentration w/in where pahrm response is produced and adverse effects are prevented

Front 13

Bioavailability

Back 13

faction of administered dose that reaches circulation

Hint 13

f=.5 or 50%

Front 14

First pass effect

Back 14

absorbed through the GI tract and then gets processed by the liver; the dose that will never reach its systemic circulation due to breakdown
f=100% iv route: doesn't go through gi tract then liver.

Front 15

PgP
-definition and what inhibited by

Back 15

P-glyco-protein-
pumps the drug back into GI lumen, opposing their absorption
Inhibited By: durgs
Inhibition by: grapefruit juice component

Front 16

True or False:

Protein binding changes are RARELY a cause of significant interactions

Back 16

True

Front 17

Transporter Protein: Effects

Back 17

1. @ intestine will alter drug absorption
2. @kidneys or lier will alter drug metabolism
3. @ BBB will decrease CNS toxicity
4. @ tumor cells will decrease drug efficacy

Hint 17

where are they at and what happens there?

Front 18

Volume of Distribution (Vd)
definition and what it's associated with...

Back 18

A proportianlity constant relating the amt of drug in the body to the serum concentration;
Apparent volume
Assoc with:
1.increasing lipophilicity (moves into fat)
2.decreasing hydrophilicity (moves into water

Front 19

Drug Metabolism primarily at what organ?

Back 19

Liver

Front 20

Drug excretion primarily through:

Back 20

kidney

Hint 20

what organ?

Front 21

What happens to the drug when metabolized?

Back 21

changes/altered to make it more water soluble (polar or electrically charged) for easier elimination from the body

Front 22

Phase I-Metabolism

Back 22

Change in structure; by the liver
1. Oxidation:
Hydroxylation- Phenytoin, APAP
Dealkylation- diazepam
Deamination- Amphetamine
Sulfaxidaton- Chlorpromazine
2. Reduction- Sulfasalazine, Chloramphenicol
3. Hydrolysis- ASA

Hint 22

3 changes- O R H

Front 23

Phase II Metabolism

Back 23

conjugation by liver; adds mol to drug

1. Glucuronidation- apap,chloramphenicol
2. Methylation- Norepi
3. Acetylation- Procainamide, Isoniazid

Front 24

True or False:
You can have phase II without undergoing phase I of metabolism.

Back 24

True

Front 25

Cytocyhrome P450 enzyme

Back 25

aid in oxiding reactions

Front 26

Name cytochrome p450 enzyme abbrev:
1. cytochrome Superfamily
2. cytochrome family
3. cytochrome Subfamily
4. cytochrome Isoenzyme

Back 26

1. CYP
2. CYP 2
3. CYP 2C
4. CYP 2C19

Front 27

Where are the CYP?

Back 27

1. the cell-endoplasmic reticulum
2. Tissue- skin, kidneys, lungs, brain, liver, intestine

Hint 27

name 2
C---
T-----

Front 28

Drug Elimination

Back 28

fremoving drug from the body

Front 29

GFR

Back 29

describes function of the kidney; estimated by creatinine clearance (CLcr)

Front 30

CLcr

Back 30

m=(ml/min)=(140-age)x wt(kg)/ 72 x Scr
f= est CLcr male x 0.85

** use IBW if obese