Pharmacodynamics and Pharmacokinetics

Question 1

When will you have the greatest response in a drug?

Answer 1

when all all receptors are bound (ex. paralytics)

Question 2

List the types of bonds agonist and antagonists make

Answer 2

Ion (electrovalent), Hydrogen (to electronegative atom), Van der Waals (weak fluctuating bonds). All reversible

Question 3

In competitive antagonism you will see a shift to the ___

Answer 3

right

Question 4

List the inverse agonists provided in class

Answer 4

Propanolol, metoprolol, cetirizine, loratidine, prazosin, naloxone

Question 5

The number of receptors in a drug increase or decrease based on

Answer 5

comorbidity or drug therapy

Question 6

What are drug examples of Tolerance/Tachyphylaxis?

Answer 6

Albuterol (overuse, down regulation of receptors), Ephedrine (NE, E not as responsive), Pheochromocytoma (decreased B receptors in response to NE, E)

Question 7

Most anesthesia drug receptors are located

Answer 7

lipid bilayer, membrane bound (opioids, bzd, b-blockers, NE,E, NMBD)

Question 8

Intracellular protein receptor drug examples

Answer 8

Insulin, steriods, pcor

Question 9

Circulating protein receptor drug examples

Answer 9

anticoagulants (wafarin, protein bound)

Question 10

Pharmacokinetics determines the concentration of the drug in the ___ and at the ____, but varies

Answer 10

plasma, effector site, patient to patient

Question 11

What is the 1 Compartment Model

Answer 11

model that describes the body working as a “single or uniform” compartment in how the drug is distributed

Question 12

% body mass vessel rich

Answer 12

10

Question 13

% body mass vessel poor

Answer 13

10

Question 14

% body mass muscle

Answer 14

50

Question 15

% body mass fat

Answer 15

20

Question 16

% of CO vessel poor

Answer 16

0

Question 16

% of CO vessel rich

Answer 16

75

Question 17

% of CO muscle

Answer 17

19

Question 18

% of CO fat

Answer 18

6

Question 19

what is the central compartment in the 1 compartment model

Answer 19

what dilutes the drug in the first minute following injection (venous blood in the arm, inferior vena cava, right heart, pulm vessels, lungs, left heart- aorta)

Question 20

Explain how the 2-compartment differs from the 1-compartment model

Answer 20

2-compartment takes into account the peripheral compartment (fat, muscle), Drug leaves the central compartment , goes to peripheral , and then back to central compartment

Question 21

Drugs with that are fat soluble have ____ VD

Answer 21

high

Question 22

Drugs that are taken up in first pass (through lungs) exceeding 65%

Answer 22

Lidocaine, propanolol, merperidine, fentanyl, sufentanil, alfentanil

Question 23

Acidic drugs bind primarily to ___

Answer 23

albumin

Question 24

What can cause low albumin?

Answer 24

Malnutrition, liver failure, burns, pregnancy, age

Question 25

Alkalotic drugs primarily bind to ___ proteins

Answer 25

a1-acid glycoproteins

Question 26

Only ____ drugs can cross the cell membrane

Answer 26

"free", unbound

Question 27

Only the "free" drug can determine the ___ available to receptor (potency)

Answer 27

concentration

Question 28

if Normal free fraction of drug is 2% (98% bound to Albumin) And 50% of plasma proteins are lost… how much is the free fraction of the drug

Answer 28

4%

Question 29

These drugs have high VD, have poor protein binding and are lipophilic

Answer 29

propofol, valium, thiopental, diazepam (this makes their effects longer)

Question 30

Highly protein bound to plasma protein will have ___ VD, and be ______ hydro/lipophilic

Answer 30

low, hydro (ex. wafarin)

Question 31

Examples of active metabolites

Answer 31

Diazepam, Propanolol, Morphine

Question 32

what drug has two active metabolites

Answer 32

morphine

Question 33

what is a prodrug and an example

Answer 33

drug that becomes active when ingested, codeine

Question 34

Most drugs are metbolized via ____

Answer 34

CYP450

Question 35

In plasma drugs are metabolized via _____ elimination and ____ hydrolysis

Answer 35

Hoffman, Ester

Question 36

In the GI tract and placenta drugs are metabolized via tissue ___

Answer 36

esterase

Question 37

In Phase I you increase the polarity of a drug via ___

Answer 37

oxidation, reduction, hydrolysis

Question 38

Oxidation

Answer 38

catalyzed by CYP450, lose electrons

Question 39

Reduction

Answer 39

removes O2 or adds Hydrogen

Question 40

Hydrolysis

Answer 40

uses water to break bonds

Question 41

Phase 1 makes a drug more ___

Answer 41

water soluble to be excreted

Question 42

Phase 2 reactions

Answer 42

covalently link with highly polar molecule to become more water soluble (conjugation)

Question 43

CYP450 has ___- isoforms

Answer 43

10

Question 44

CYP450 are ___ bound, contain a ___ co factor

Answer 44

membrane, heme

Question 45

the more numbers you add on the more ___ you are in CYP450

Answer 45

homologous

Question 46

CYP2 Homologous %

Answer 46

40

Question 47

CYP2A Homologous %

Answer 47

55

Question 48

CYP2A6 Homologous %

Answer 48

this is the individual enzyme

Question 49

what is the most common CYP in anesthesia drugs

Answer 49

CYP3A4

Question 50

What drugs does CYP3A4 metabolize

Answer 50

opioids, BZP, LA, immunosuppressnts, antihistamines

Question 51

Induction ____ the amount of P450

Answer 51

increases, thus less conc of the drug--> more metabolism

Question 52

Grapefruit juice is an example of ____

Answer 52

inhibition of P450

Question 53

for most anesthetic drugs ____ is constant

Answer 53

clearance

Question 54

capacity limited metabolism

Answer 54

at some point metabolism is exceeded since liver capability is not unlimited

Question 55

Rate or drug metabolism formula ??

Question 56

Renal Clearance involves

Answer 56

GFR (controls the amount of drug entering the tubule)

Question 57

Active tubular secretion is from the ______ and involves ____ transport

Answer 57

peritubular capillaries, active (ex. penicillins)

Question 58

passive tubular reabsorption is __ if the drug is lipid soluble (example)

Answer 58

lipid soluble, thiopental

Question 59

Passive Tubular reabsorption is zero if the drug is ___-

Answer 59

water soluble, excreted in the urine

Question 60

Half Time

Answer 60

time it takes to eliminate 50% the drug from the plasma

Question 61

Half Life

Answer 61

time is takes to eliminate 50% drug from the body

Question 62

You give 100 mcg of Drug An IV, E ½ time is 10 minutes, In 20 minutes what will plasma concentration be?

Answer 62

25 mcg

Question 63

Context Sensitive Half Time

Answer 63

time to a 50% decrease AFTER infusion discontinued

Question 64

context half life increases the ___ the infusion increases

Answer 64

increases

Question 65

drugs such as ___ and __ have a higher context half life than prop, -fentanils, and versed

Answer 65

fentanyl and thiopental

Question 66

When pK and pH are identical ____

Answer 66

50% drug is ionized, 50% drug non-ionized

Question 67

Barbituates are weak ____

Answer 67

acids

Question 68

LA and Opioids are weak ____

Answer 68

bases

Question 69

Acids are ____ in alkaline oh

Answer 69

ionized

Question 70

Bases are ionized in ____ ph

Answer 70

acidic

Question 71

if a drug is unionized it is ____ soluble, and active/inactive, can or cannot cross lipid barriers, excreted or not excreted in kidneys , metabolized in liver?

Answer 71

lipid, active, can cross, not excreted, metabolized in liver

Question 72

So if a weak acid (pk 7.6) is put in a basic ph (blood 7.8) is it ionized?

Answer 72

yes, 0.2

Question 73

___ numbers are unionized

Answer 73

negative

Question 74

Example in class that if a drug is ionized it cant cross barriers so it is called

Answer 74

ion trapping

Question 75

why will and nerve block not work on an ischemic foot

Answer 75

the ischemic tissue is acidic, opioid is basic , therefore highly ionized so it cant cross over and work

Question 76

examples of genetic disorders that affect pharmacodynamics

Answer 76

atypical cholinesterase activity, malignant hyperthermia

Question 77

potency

Answer 77

concentration vs response, less drug with more effect

Question 78

efficacy

Answer 78

the ability of the drug to produce a clinical effect

Question 79

ED50

Answer 79

* ED50 : dose required to produce effect in 50% of patients

Question 80

LD50

Answer 80

: Dose required to produce death in 50% of patients

Question 81

Therapeutic Index

Answer 81

ratio between (LD50/ED50 )

Question 83

Stereochemistry

Answer 83

* How drug molecules are structured In 3 dimensions

Question 84

Chiral compounds

Answer 84

molecules with asymmetrical centers, mirror images, chemically identical

Question 85

enantiomers

Answer 85

optical isomers

Question 86

In enantiomers what are the R & L rotation in light called

Answer 86

Left: Levorotatory Right: Dextrorotary

Question 87

Molecule sequence of optical isomers

Answer 87

R: Rectus, S: Sinister

Question 88

S-enantiomer of ketamine has ___ delrium but __ potent

Answer 88

less, more

Question 89

l-bupivicaine has less ___

Answer 89

cardiac toxicity

Question 90

Nimbex is the isomer or ____ and lacks __ effects

Answer 90

atracurium, histamine

Question 91

albuterol and xopenex are examples of

Answer 91

enantiomers