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. 1 A
Pharmacokinetics requ ires an understanding of half-life, volume of distribution, and clearance rates. Drug eliminati on, th
•2
a drug exits the body, is an important pharmacokineti c considerat ion.
·3
• 4 Which of the following drugs demonstrat es a constant rate of elimination at therapeutic levels?
·5
·6 A. Bethanechol
·7
B. Misoprostol
·8
•9 C. Phenytoin
• 10 0 . Propranolol
· 11
E. Rifampin
• 12
• 13
• 14
• 15
. 16
. 17
• 18
• 19
• 20
. 21
. 22
. 23
• 24
• 25
• 26
. 27
8
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1
•2
The correct a nswer is C. 6 7 °/o chose this .
Zero-order elim inat ion of a drug implies t hat that its rate of eliminat ion is const ant regardless of its plasma concentrat i
•3
amount of drug is elim inat ed per unit time. As a result, the plasma concent rat ion of the drug decreases linearly wit h tim
•4 a few drugs, includ ing et hanol and high-dose aspiri n, which fo llow zero-order elim ination. A caveat, however, is that et
. 5 zero-order eliminat ion under cert ain concent rat ions. Of note, ot her drug examples with zero-order elim ination include t
warfarin and heparin.
.6
Warfarin Phenytoin Aspirin Ethanol Heparin Blood plasma Anticoagulant
• 7
A is not correct . 7°/o chose this.
•8
Bethanechol is a drug that undergoes first-order elim ination, meaning t hat t he rate of its elim inat ion is proportional to
•9
so t hat a constant f raction of drug is elim inated per unit t ime. As a result , t he plasma concent rat ion of bethanechol dec
• 10 with t ime . The majori ty of drugs follow f irst-order elim ination at t herapeut ic levels .
Blood plasma Biological half-life Bethanechol
· 11
• 12 B is not correct. 7% chose t his .
• 13 Misoprostol is a drug t hat undergoes f irst-order elimination, meaning t hat the rate of its elimination is proportional to t
• 14 so t hat a constant f raction of drug is elim inated per unit t ime. As a result , t he plasma concent rat ion of misoprostol dec
with t ime . The majori ty of drugs follow f irst-order elim ination at t herapeut ic levels .
• 15 Biological half-life Misoprostol Blood plasma
. 16
D is not correct. 10% c hose this .
. 17
Proprano lol is a 13- blocker t hat undergoes first -order elim inat ion, meaning that t he rat e of its elim ination is proportiona
• 18 concentration so t hat a constant f raction of drug is eliminated per unit t ime . As a result , t he plasma concentration of pr
• 19 exponent ially with t ime . The majority of drugs follow f irst-order elim ination at t herapeut ic levels .
Biological half-life Propranolol Blood plasma
• 20
. 21 E is not correct. 9°/o chose this .
. 22 Ri famp in is a drug t hat undergoes first -order elim inat ion, meaning that t he rat e of its elimination is proportional t o t he
• 23
t hat a constant f raction of drug is elim inated per unit t ime. As a result , t he plasma concent rat ion of ri fampi n decreases
t ime . The majori ty of drugs follow f irst-order elim ination at t herapeut ic levels .
• 24 Biological half-life Blood plasma Rifampicin
• 25
• 26
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. 27
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•2
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·3
• 4
Zero-order drug elimination fo llows a linear pattern, whereas first-order elimination is proportional t o drug concentrat
include Phenytoin, Ethanol, and Aspirin (mnemonic: PEA), although this may vary under certain conditions.
·5 Blolog•c~l hAif· hfe Mnenon~c
·6
·7
14l if.ii·11•J f or
FlltST A IO FA c·s
y ear : 2017 •
•9
• 10
· 11
Elimination of drugs
• 12
• 13 Zero-order Rate of elimination is constant regardless of CP Capacity-limited elimination .
• 14 elimination (ie, constant amount of drug eliminaled per PJt: \ . (A pea is round, shaped Iike t
• 15 unit time). cp l linearly with time. l~xamples zero-order.)
. 16 of drugs- Phenytoin, Ethanol, and Aspirin (<ll
. 17 high or toxic concentrations).
• 18
First-order elimination Rate of elimination is directly proportional Flow-dependent elimination .
• 19
to the drug concentration (ie, conslan t
• 20
fraction of drug eliminated per unil time).
. 21
CP l exponentially with time. Applies to mosl
. 22
. 23
drugs .
• 24 Zero-order elimination First-order elimination
• 25 [ 'Tllna , rate ~ ooe e
• 26 4 U/h
~ 2U/h
. 27
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1
•2
·3 Elimination of drugs
• 4 Zero-order Rate of elimination is constant regardless of CP Capacity-limited elimination.
·5 elimination (ie, constant amount of drug eliminated per PE \ . (A pea is round, shaped like t
·6 unit time). CP l linearly with time. Examples t.cro-order.)
·7 of drugs-Phen) loin, 1-.thanol, and \ spirin (at
high or toxic concentrations).
•9
• 10
First-order elimination Rate of elimination is directly proportional Flo" -dependent elimination.
· 11
to the drug concentration (ie, constant
• 12 fraction of drug eliminated per unit time).
• 13 cp l exponentially with time. pplies to most
• 14 drugs.
• 15
Zero-order elimination First-order elimination
. 16
C1m1nat.on rate s ope te , ope)
. 17
• 18
nme of 1112 is constant
• 19
nme of 1112 J. as as concentration ,j.
• 20 concentration J,
. 21
. 22
. 23
• 24 Secondt112• I 0.5U/h
• 25 ~
• 26 nmelhl nme!hl
. 27
8
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Mark -<J
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N@xt Labl
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Calcula t o r
. 1 A
Pharmacokinetics requ ires an understanding of half-life, volume of distribution, and clearance rates. Drug eliminati on, th
•2
a drug exits the body, is an important pharmacokineti c considerat ion.
·3
• 4 Which of the following drugs demonstrat es a constant rate of elimination at therapeutic levels?
·5
·6 A. Bethanechol
·7
B. Misoprostol
·8
•9 C. Phenytoin
• 10 0 . Propranolol
· 11
E. Rifampin
• 12
• 13
• 14
• 15
. 16
. 17
• 18
• 19
• 20
. 21
. 22
. 23
• 24
• 25
• 26
. 27
8
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, Item: 1 of 66 ~ ,• Mark <::J [:::> ""I ~· ~'j
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1
•2
The correct a nswer is C. 6 7 °/o chose this .
Zero-order elim inat ion of a drug implies t hat that its rate of eliminat ion is const ant regardless of its plasma concentrat i
•3
amount of drug is elim inat ed per unit time. As a result, the plasma concent rat ion of the drug decreases linearly wit h tim
•4 a few drugs, includ ing et hanol and high-dose aspiri n, which fo llow zero-order elim ination. A caveat, however, is that et
. 5 zero-order eliminat ion under cert ain concent rat ions. Of note, ot her drug examples with zero-order elim ination include t
warfarin and heparin.
.6
Warfarin Phenytoin Aspirin Ethanol Heparin Blood plasma Anticoagulant
• 7
A is not correct . 7°/o chose this.
•8
Bethanechol is a drug that undergoes first-order elim ination, meaning t hat t he rate of its elim inat ion is proportional to
•9
so t hat a constant f raction of drug is elim inated per unit t ime. As a result , t he plasma concent rat ion of bethanechol dec
• 10 with t ime . The majori ty of drugs follow f irst-order elim ination at t herapeut ic levels .
Blood plasma Biological half-life Bethanechol
· 11
• 12 B is not correct. 7% chose t his .
• 13 Misoprostol is a drug t hat undergoes f irst-order elimination, meaning t hat the rate of its elimination is proportional to t
• 14 so t hat a constant f raction of drug is elim inated per unit t ime. As a result , t he plasma concent rat ion of misoprostol dec
with t ime . The majori ty of drugs follow f irst-order elim ination at t herapeut ic levels .
• 15 Biological half-life Misoprostol Blood plasma
. 16
D is not correct. 10% c hose this .
. 17
Proprano lol is a 13- blocker t hat undergoes first -order elim inat ion, meaning that t he rat e of its elim ination is proportiona
• 18 concentration so t hat a constant f raction of drug is eliminated per unit t ime . As a result , t he plasma concentration of pr
• 19 exponent ially with t ime . The majority of drugs follow f irst-order elim ination at t herapeut ic levels .
Biological half-life Propranolol Blood plasma
• 20
. 21 E is not correct. 9°/o chose this .
. 22 Ri famp in is a drug t hat undergoes first -order elim inat ion, meaning that t he rat e of its elimination is proportional t o t he
• 23
t hat a constant f raction of drug is elim inated per unit t ime. As a result , t he plasma concent rat ion of ri fampi n decreases
t ime . The majori ty of drugs follow f irst-order elim ination at t herapeut ic levels .
• 24 Biological half-life Blood plasma Rifampicin
• 25
• 26
Bottom Line :
. 27
8
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1
•2
Botto m Line :
·3
• 4
Zero-order drug elimination fo llows a linear pattern, whereas first-order elimination is proportional t o drug concentrat
include Phenytoin, Ethanol, and Aspirin (mnemonic: PEA), although this may vary under certain conditions.
·5 Blolog•c~l hAif· hfe Mnenon~c
·6
·7
14l if.ii·11•J f or
FlltST A IO FA c·s
y ear : 2017 •
•9
• 10
· 11
Elimination of drugs
• 12
• 13 Zero-order Rate of elimination is constant regardless of CP Capacity-limited elimination .
• 14 elimination (ie, constant amount of drug eliminaled per PJt: \ . (A pea is round, shaped Iike t
• 15 unit time). cp l linearly with time. l~xamples zero-order.)
. 16 of drugs- Phenytoin, Ethanol, and Aspirin (<ll
. 17 high or toxic concentrations).
• 18
First-order elimination Rate of elimination is directly proportional Flow-dependent elimination .
• 19
to the drug concentration (ie, conslan t
• 20
fraction of drug eliminated per unil time).
. 21
CP l exponentially with time. Applies to mosl
. 22
. 23
drugs .
• 24 Zero-order elimination First-order elimination
• 25 [ 'Tllna , rate ~ ooe e
• 26 4 U/h
~ 2U/h
. 27
8
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A
1
•2
·3 Elimination of drugs
• 4 Zero-order Rate of elimination is constant regardless of CP Capacity-limited elimination.
·5 elimination (ie, constant amount of drug eliminated per PE \ . (A pea is round, shaped like t
·6 unit time). CP l linearly with time. Examples t.cro-order.)
·7 of drugs-Phen) loin, 1-.thanol, and \ spirin (at
high or toxic concentrations).
•9
• 10
First-order elimination Rate of elimination is directly proportional Flo" -dependent elimination.
· 11
to the drug concentration (ie, constant
• 12 fraction of drug eliminated per unit time).
• 13 cp l exponentially with time. pplies to most
• 14 drugs.
• 15
Zero-order elimination First-order elimination
. 16
C1m1nat.on rate s ope te , ope)
. 17
• 18
nme of 1112 is constant
• 19
nme of 1112 J. as as concentration ,j.
• 20 concentration J,
. 21
. 22
. 23
• 24 Secondt112• I 0.5U/h
• 25 ~
• 26 nmelhl nme!hl
. 27
8
Lode.
