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Pharmacology I > Kinetics > Flashcards

Kinetics Flashcards

1
Q

what are the main causes of the main alterations in ADME

A
  • age
  • genetic factors
  • end organ damage
  • drug interactions
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2
Q

what are the types of variability in ADME

A
  • pharmacokinetics
  • pharmacodynamic
  • idiosyncratic
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3
Q

describe idiosyncratic variability

A
  • occur in a small minority of patients
  • sometimes with low or normal doses
  • poorly understood
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4
Q

what is a pharmacodynamic interaction

A

interaction between 2 or more drugs that leads to:
-accentuation/synergism
- attenuation/antagonisn

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5
Q

what is an example of accentuation/synergism

A

calcium channel blocker and a beta blocker

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6
Q

what is an example of attenuation/antagonism

A

narcan and opiods

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7
Q

do pharmacodynamic interactions have to do with ADME

A

no

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8
Q

do pharmacokinetic interactions have anything to do with ADME

A

yes

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9
Q

what drugs do we need to check for interactions with/what drugs have many other drug interactions

A
  • warfarin
  • digoxin
  • TCAs
  • phenytoin
  • carbamazepine
  • lithium
  • methotrexate/cyclosporine/tacrolimus
  • HIV medications - protease inhibitors
  • rifampin
  • paxlovid
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10
Q

what is the result of the interaction of tetracycline and antacids

A

antacid impairs absorption of ABX resulting in decrease ABX efficacyw

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11
Q

what is the result of the interaction between erythromycin/clarithromycin/ metronidazole/ciprofloxacin/trimethaprim- sulfamethoxazole and warfarin

A

ABX inhibits the metabolism of warfarin resulting in increased serum concentration of warfarin and increasing the risk of bleeding

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12
Q

what is the result of the interaction between NSAID and warfarin

A

additive effect on decreased platelet aggregation resulting in additive risk for bleeding, especially GI bleeding

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13
Q

what is the result of the interaction between ASA and warfarin

A

additive effect on decreased platelet aggregation ->additive risk for bleeding, especially GI bleeding

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14
Q

what is the result of the interaction between tramadol and antidepressants

A

increased risk of serotonin syndrome

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15
Q

what is the result of the interaction between protease inhibitors and BZD

A

protease inhibitors are CYP 450 3A4 inhibitors -> decreased metabolism of benzodiazepine -> increased benzodiazepine concentrations -> increased risk of benzodiazepine side effects which are increased sedation depth and duration

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16
Q

what are the things to consider with pregnant patients

A
  • increased cardiac output increases distribution of drugs
  • increased renal blood flow increases elimination of drugs and decreases the duration and effects of drugs
  • decreased albumin which decreases binding of drugs -> more free drug to act -> drugs have more pronounced effects
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17
Q

what are the considerations for patients with uncontrolled DM

A
  • gastric stasis -> decreases rate of absorption of drugs
  • nephrotic syndrome -> glomerulus gets damaged -> protein gets in kidneys -> proteinuria -> damages kidneys and generalized edema in body -> decreases rate of absorption of drugs -> decreased albumin -> more pronounced drug effect
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18
Q

what medications will worsen myasthenia gravis

A
  • aminoglycosides
  • fluoroquinolones
  • tetracyclines
  • macrolides
  • magnesium
  • beta blockers
  • procainamide
  • neuromuscular blockers
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19
Q

what is a side effect and give example

A

unrelated to clinical drug effect, predictable, dose related
- ex: an ABX causing GI upset

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20
Q

what is a toxic reaction and give example

A
  • an exaggeration of the clinical effect, predictable, dose related, happens when you take too much of. adrug
  • EX: taking beta blocker twice -> drop in BP and dizzy
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21
Q

describe an allergic reaction

A

immune mediated responses, happen quickly and are very dangerous

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22
Q

what is the positive to dental drugs

A
  • primarily single dose or short term tx
  • large margin of safety
  • extensive hx of use
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23
Q

what is pharmacokinetics

A

what the body does to the drug

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24
Q

what is pharmacodynamics

A

what the drug does to the body

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25
Q

how do we use kinetics

A
  • important in drug development and clinical testing, needed to determine optimal dose
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26
Q

how are kinetics important in the clinical setting

A
  • toxicology
  • therapeutic monitoring
  • drug interactions
  • dose adjustments
  • effect of illness, organ dysfunction
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27
Q

time course of drug concentration in kinetics depends on ______

A

ADME

28
Q

kinetics focuses on:

A

concentrations of drug in plasma

29
Q

what can you use to calculate precise doses to achieve a precise concentration

A

kinetics

30
Q

what is the goal of plasma concentration

A

get plasma concentration within a therapeutic window in order to elicit appropriate response without causing toxicity

31
Q

what does clearance determine

A

the maintenance dose-rate

32
Q

what does the volume distribution determine

A

the loading dose

33
Q

what does the half life determine

A

the time to steady state and dosing interval

34
Q

CL, VD, and half life are derived from a:

A

time/concentration curve

35
Q

what is the definition of clearance

A

volume of plasma cleared of drug per unit of time

36
Q

the clearance is the index of:

A

how well a drug is removed irreversibly from the circulation

37
Q

the clearance determines the dose/rate required to:

A

maintain a CP

38
Q

how do you calculate clearance of a drug - what is the formula

A
  • creatinine clearance
  • males: 140 - age / SCR
  • women: 140 - age/ SCR ) x 0.85
39
Q

describe zero order kinetics

A
  • rate of absorption/elimination doesnt depend on the drug concentration
  • rate limited process- fixed number of enzymes, carrier, or active transport proteins; saturation occurs
  • half life decreases over time
40
Q

what are the only drugs that undergo zero order kinetics

A
  • phenytoin
  • warfarin
  • heparin
  • ethanol
  • aspirin (high dose)
  • theophylline
41
Q

what is the relationship on zero order kinetics

A

linear

42
Q

half life _____ with decreasing concentration in zero order kinetics

A

decreases

43
Q

describe first order kinetics

A
  • the decline in plasma concentration is not constant with time, but varies with concentration
  • the half life stays the same
  • concentration decreases by 50% per each half life
  • majority of drugs follow first order elimination
44
Q

what is the relationship of first order kinetics

A

logarithmis

45
Q

length of half life in first order kinetics is _____

A

constant

46
Q

what does the rate constant measure and what is its variable

A
  • KE
  • KE = 0.693 / half life
47
Q

what is the formula for clearance

A

CL = KE x VD

48
Q

to maintain steady state plasma concentration administration rate must equal:

A

rate of elimination

49
Q

how will the CP eventually reach steady state

A

when repeated doses of a drug are given in short enough intervals and elimination is first order

50
Q

during IV infusion, drug levels:

A

increases exponentially in a way equivalent to the drugs half life

51
Q

how many half lives is steady state achieved after

A

5

52
Q

what does volume of distriution tell you

A

volume into which a drug appears to be distributed with a concentration equal to that of plasma
- tells you where the drug distributes

53
Q

what is an equation for VD

A

F x dose /CP0

54
Q

what is the bioavailability for IV drugs

A

1 (100%)

55
Q

what does a large VD indicate

A

tells us it gets everywhere in the body and are more lipophilicd

56
Q

drugs will small VD:

A

are more polar and water soluble

57
Q

what does half life provide an index of

A
  • time course of drug elimination
  • time course of drug accumulation
  • choice of drug interval
58
Q

how many half lives does it take for drugs to be eliminated from the body

A

5

59
Q

what is the definition of steady state kinetics

A
  • point at which the amount absorbed equals amount eliminated per unit time
60
Q

what is the formula for concentration of steady state kinetics

A
  • CSS = KA / (VD x KE)
61
Q

what is the formula for CSS in calculating oral doses

A
  • CSS = (1.44 x DM x F x half life) / (T x VD)
62
Q

what is the formula for calculating an initial load dose

A

D = (VD x CSS) / F

63
Q

what is the formula for repeat loading dose

A

D = (VD)(CSS - Cmeasured) / F

64
Q

what is the formula for loading dose

A

D = Vd x CSS

65
Q
A

Pharmacology I (12 decks)

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