TDM & Toxicology

Question 1

Serum concentration is not equivalent to the concentration of ___________

Answer 1

Receptors

[could be correlated with physiological responses in certain cases]

Question 2

Why do we monitor TDM?***

Answer 2

-to guard against overdoes or underdoses
-check for compliance

Question 3

Study of the rate of process of absorption, distribution, and biotransformation (metabolism, and excretion)

Answer 3

pharmacokinetics

Question 4

Study of biochemical physiological effects of drugs and their mechanisms of action

Answer 4

pharmacodynamics

Question 5

A discipline concerned with the study of adverse effects of agents on living systems.

Answer 5

toxicology

Question 6

What is the pharmacokinetics order of biotransformation?

Answer 6

LADME**

-liberation
-absorption
-distribution
-metabolization
-excretion

Question 7

Absorption: Rate and extent of drug absorption vary from different ________& _______

Answer 7

sites, drugs

Question 8

What is the first-pass effect?

Answer 8

***after ORAL administration, drug is absorbed by small intestine and carried via portal vein to liver where the drug is extensively metabolized.

Question 9

Mechanisms of pharmacokinetics?

Answer 9

-passive diffusion (95% of drugs)
-active diffusion (needs carrier protein, against conc. gradient)
-facilitated transport
-convective (pore) transport
-pinocytosis (fat soluble cells)

Question 10

The drug must be in true ________ solution at the site of absorption.

Answer 10

aqueous

Question 11

weak acid pKa: ______in H2O

Strong acid pKa:_____ in H2O

Answer 11

-2 ~12

< -2

Question 12

upon entering the circulatory system, most drugs will quickly equilibrate between
a ______ and _______ state

Answer 12

free, bound

Question 13

Only ______ drug is available for distribution beyond the vascular compartment.

Answer 13

free

Question 14

physiological response of drugs is dependent only the _____ form of the drug (active)

Answer 14

free

Question 15

Bound drug distribution is dependent on kinetic binding and physiological ________ parameters.

Answer 15

filtration

Question 16

major sites for biotransformation and drug metabolism?

Answer 16

major: liver
minor: kidneys, brain, lungs, skin, and GI tract

Question 17

metabolism may affect the drug in what three ways?

Answer 17

-Increase activity (prodrug)
-decrease activity (inactivation or detoxication)
-no effect on activity

Question 18

metabolites are generally more…

Answer 18

soluble

-some metabolites may still be pharmacologically active* (needs to be factored into the half-life) *****on test, trick question

Question 19

biotransformation changes the _______ of the drug

Answer 19

shape

Question 20

what happens after a prodrug is metabolized?

Answer 20

activity increases

Question 21

What are the two major metabolic pathways of drugs?

Answer 21

-phase 1- inactivation- reactions metabolize lipophilic drugs to more polar forms to facilitate renal excretion

-phase 2- Excration

Question 22

-accomplished by oxidative or deductive processes
-Cytochrome P-450 enzymes on microsomal membranes oxidize to inactive drugs
-metabolites can be metabolically active compounds

Answer 22

Phase 1- Innactivation

Question 23

what enzyme metabolises most drugs?

Answer 23

Cytochrome P-450 (polar drugs)

Question 24

-redactions involve conjugation of drugs with compounds such as glutathione, glucuronic acid, sulfate, and phosphate
-conjugates produced are water-soluble and can be excreted by the kidneys

Answer 24

Phase 2-Exreation

Question 25

lipid-soluble drugs are excreated primarily through ________.

Answer 25

bille

Question 26

The lowest drug concentration in circulation most reliable indicator of appropriateness of dosage

Answer 26

trough blood concentration

Question 27

When is trough blood concentration measured?

Answer 27

30 min before the next dose is given

Question 28

the highest drug concentration achieved within the dosing cycle when is it typically measured?

Answer 28

peak blood concentration 0.5-2 hours after the dose

Question 29

MTC =

Answer 29

minimum toxic concentration

Question 30

MEC =

Answer 30

minimum effective concentration

Question 31

How is therapeutic drug monitoring done?

Answer 31

-immunoassay*** -fluorescent polarization immunoassay -immunonephlometry -gas-liquid chromatography -HPLC

Question 32

specimen for TDM should be serum without a serum separator. why?

Answer 32

certain drugs have a tendency to be absorbed in the gel of the separator

Question 33

______________ plasma is suitable for most drug analyses. what is not usually acceptable?

Answer 33

heparinized plasma EDTA, citrate, or oxalate

Question 34

___________ is utilized for immunosuppressive drugs****

Answer 34

whole

Question 35

what are the ANTICONVULSANTS?

Answer 35

Phenobarbital / phenytoin / Valproate

Question 36

What are the cardioactive drugs?

Answer 36

Digoxin, Lidocaine, Procainamide, Quinidine, Propranol ***

Question 37

Bronchodilator drug?

Answer 37

Theophylline (works on beta receptor) also increases HR

Question 38

antibiotics?

Answer 38

Aminoglycosides, Vancomycin, Chloramphenicol

Question 39

psychotropic drugs?

Answer 39

Lithium, Tricyclic antidepressants; doxepin, imipramine, protriphylline, Neuroleptic; Haloperidol, Phenothiazine

Question 40

antineoplastic drugs?

Answer 40

Methotrexate (for tumors) , cf. leucovorin (minimizes toxic effects of chemo)

Question 41

immunosuppressant drugs?

Answer 41

Cyclosporine, Tacrolimus

Question 42

how do anticonvulsive drugs work?

Answer 42

decrease voltage-gated Na+ channels and increase GABA

Question 43

What are the drugs used to treat epilepsy and seizures?

Answer 43

Phenobarbital / phenytoin / Valproate

Question 44

what is grand mal?

Answer 44

abnormal electrical brain activity

Question 45

what drugs are used for grand mal seizers?

Answer 45

Phenobarbital and Phenytoin (dilantin)

Question 46

involves temp disturbances of the brain and small muscle twitching what drug is used?

Answer 46

petit mal Valproate

Question 47

another anticonvulsive: inactive prodrug of phenobarbital

Answer 47

primidone

Question 48

another anticonvulsive: treatment of seizures and neuralgia

Answer 48

Tegretol

Question 49

another anticonvulsive: also used to treat petit mal seizures

Answer 49

Ethosuximide

Question 50

CO =

Answer 50

HR x SV

Question 51

improves cardiac contractility by altering force of contraction through its effect on sodium potasium-ATPase pump in heart muscles that effects sodium, potassium, and calcium transport in the heart.

Answer 51

Digoxin

Question 52

-treats CHF patients -tistrubution rate is slow: peaks in 6 to 10 hours

Answer 52

Digoxin

Question 53

causes more sodium to go into cell and less calcium to go out of cell (gets stored in SR)

Answer 53

Digoxin

Question 54

Local anesthetic drug: stabilize neuronal membrane potential by inhibiting ionic fluxes

Answer 54

Lidocaine