TDM & Toxicology Flashcards

1
Q

Serum concentration is not equivalent to the concentration of ___________

A

Receptors

[could be correlated with physiological responses in certain cases]

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2
Q

Why do we monitor TDM?***

A

-to guard against overdoes or underdoses
-check for compliance

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3
Q

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

A

pharmacokinetics

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4
Q

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

A

pharmacodynamics

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5
Q

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

A

toxicology

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6
Q

What is the pharmacokinetics order of biotransformation?

A

LADME**

-liberation
-absorption
-distribution
-metabolization
-excretion

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7
Q

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

A

sites, drugs

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8
Q

What is the first-pass effect?

A

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

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9
Q

Mechanisms of pharmacokinetics?

A

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

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10
Q

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

A

aqueous

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11
Q

weak acid pKa: ______in H2O

Strong acid pKa:_____ in H2O

A

-2 ~12

< -2

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12
Q

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

A

free, bound

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13
Q

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

A

free

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14
Q

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

A

free

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15
Q

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

A

filtration

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16
Q

major sites for biotransformation and drug metabolism?

A

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

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17
Q

metabolism may affect the drug in what three ways?

A

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

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18
Q

metabolites are generally more…

A

soluble

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

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19
Q

biotransformation changes the _______ of the drug

A

shape

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20
Q

what happens after a prodrug is metabolized?

A

activity increases

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21
Q

What are the two major metabolic pathways of drugs?

A

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

-phase 2- Excration

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22
Q

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

A

Phase 1- Innactivation

23
Q

what enzyme metabolises most drugs?

A

Cytochrome P-450 (polar drugs)

24
Q

-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

A

Phase 2-Exreation

25
Q

lipid-soluble drugs are excreated primarily through ________.

A

bille

26
Q

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

A

trough blood concentration

27
Q

When is trough blood concentration measured?

A

30 min before the next dose is given

28
Q

the highest drug concentration achieved within the dosing cycle

when is it typically measured?

A

peak blood concentration

0.5-2 hours after the dose

29
Q

MTC =

A

minimum toxic concentration

30
Q

MEC =

A

minimum effective concentration

31
Q

How is therapeutic drug monitoring done?

A

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

32
Q

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

A

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

33
Q

______________ plasma is suitable for most drug analyses.

what is not usually acceptable?

A

heparinized plasma

EDTA, citrate, or oxalate

34
Q

___________ is utilized for immunosuppressive drugs**

A

whole

35
Q

what are the ANTICONVULSANTS?

A

Phenobarbital / phenytoin / Valproate

36
Q

What are the cardioactive drugs?

A

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

37
Q

Bronchodilator drug?

A

Theophylline (works on beta receptor) also increases HR

38
Q

antibiotics?

A

Aminoglycosides, Vancomycin, Chloramphenicol

39
Q

psychotropic drugs?

A

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

40
Q

antineoplastic drugs?

A

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

41
Q

immunosuppressant drugs?

A

Cyclosporine, Tacrolimus

42
Q

how do anticonvulsive drugs work?

A

decrease voltage-gated Na+ channels and increase GABA

43
Q

What are the drugs used to treat epilepsy and seizures?

A

Phenobarbital / phenytoin / Valproate

44
Q

what is grand mal?

A

abnormal electrical brain activity

45
Q

what drugs are used for grand mal seizers?

A

Phenobarbital and Phenytoin (dilantin)

46
Q

involves temp disturbances of the brain and small muscle twitching

what drug is used?

A

petit mal

Valproate

47
Q

another anticonvulsive:

inactive prodrug of phenobarbital

A

primidone

48
Q

another anticonvulsive:

treatment of seizures and neuralgia

A

Tegretol

49
Q

another anticonvulsive:

also used to treat petit mal seizures

A

Ethosuximide

50
Q

CO =

A

HR x SV

51
Q

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.

A

Digoxin

52
Q

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

A

Digoxin

53
Q

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

A

Digoxin

54
Q

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

A

Lidocaine