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Pharmacology N926 > Drugs, Metabolism, and Their Metabolites > Flashcards

Drugs, Metabolism, and Their Metabolites Flashcards

1
Q

metabolite of morphine

A

morphine 3 glucoronide (75%, inactive), morphine 6 glucoronide (25%, active)

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2
Q

morphine 6 glucoronide

A

longer DOA than morphine, 65x higher analgesic potency than morphine

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3
Q

metabolite of meperidine

A

normeperidine

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4
Q

normeperidine

A

half as active as meperidine, elimination half life 15 hours, but can be >30 hours in renal patients. may be involved in meperidine delirium, don’t do PCA, hydrolysis to meperidinic acid occurs

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5
Q

primarily metabolism of morphine

A

conjugation with glucoronic acid

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6
Q

metabolism of meperidine

A

90% demethylization to normeperidine

10% hydrolysis to meperidinic acid

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7
Q

metabolism of fentanyl

A

N dealkylation and hydroxylation

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8
Q

metabolism of sufentanil

A

N dealkylation to inactive metabolites, and O demethlyation

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9
Q

metabolite of sufentanil

A

O demethylation to desmethyl sufentanil

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10
Q

metabolism of alfentanil

A

piperidine N dealkylation, amide N-dealkylation

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11
Q

metabolites of alfentanil

A

piperidine N dealkylation to noralfentanil (active)

amide N-dealkylation to N-phenylpropionamide

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12
Q

metabolism of remifentanil

A

metabolized by non specific plasma esterase’s

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13
Q

metabolism of tramadol

A

metabolized by CYP450

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14
Q

metabolite of tramodol

A

O-desmethyltramadol, which has modest analgesic effects

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15
Q

metabolism of heroin

A

hydrolyzed in the CNS

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16
Q

metabolites of heroin

A

monoacetylmorphine (active)

morphine (active)

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17
Q

metabolism of butorphanol

A

metabolism via liver and excreted primarily in bile

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18
Q

metabolite of butorphanol

A

hydroxybutorphanol (inactive)

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19
Q

metabolism of naloxone

A

conjugation with glucoronic acid

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20
Q

metabolite of naloxone

A

naloxone 3 glucoronide

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21
Q

metabolism of nalmefene

A

hepatic conjugation

22
Q

metabolism of aspirin

A

plasma esterases, erythrocytes, and liver

23
Q

metabolite of acetaminophen

A

N acetyl p benzoquinoneimine

24
Q

metabolism of Ach

A

hydrolysis via acetylcholinesterase

25
Q

plasma cholinesterase facts

A

also called butyrylcholinesterase, or pseudocholinesterase, synthesized in the liver

26
Q

metabolism of succinylcholine

A

hydrolysis by butyrylcholinesterase to succinylmonocholine and choline.

27
Q

metabolite of succinylcholine

A

succinylmonocholine is weak NMB, metabolized to succinic acid and choline

28
Q

What does butyrylcholinesterase metabolize?

A

succinylcholine, mivacurium, procaine, chloroprocaine, tetracaine, cocaine, heroin

29
Q

metabolism of cisatracurium

A

hoffman elimination. no ester hydrolysis.

30
Q

metabolism of mivacurium

A

butyrylcholinesterase

31
Q

metabolites of mivacurium

A

monoester, dicarboxylic acid

32
Q

metabolism of vecuronium

A

principally by the liver

33
Q

metabolite of vecuronium

A

3-OH metabolite, has 80% neuromuscular potency

34
Q

clearance of pancuronium

A

small amount deacetylated by the liver

accumulation of 3-OH metabolite responsible for block prolongation

35
Q

clearance of rocuronium

A

primarily metabolized in liver, 30% excreted in urine

36
Q

metabolism of thiopental

A

oxidized in liver

37
Q

metabolism of midazolam

A

oxidized by CYP450

38
Q

metabolites of midazolam

A

apparently theres two active metabolites

39
Q

metabolism of diazepam

A

metabolized by hepatic microsomal enzymes using oxidative pathway of N methylation

40
Q

metabolites of diazepam

A

desmethyldiazepam (nordiazepam) and oxazepam

41
Q

metabolism of lorazepam

A

conjugated with glucoronic acid in the liver (glucoronidation)

42
Q

metabolism of oxazepam

A

conjugated by glucoronic acid to inactive metabolism

43
Q

metabolite of flurazepam

A

salkylflurazepam (active)

44
Q

metabolism of propofol

A

via CYP450, plasma esterase metabolism

45
Q

metabolite of propofol

A

4 hydroxypropofol

46
Q

metabolism of etomidate

A

hydrolysis (phase 1)

47
Q

metabolism of ketamine

A

demethylation by CYP450 micro enzymes (phase 1). metabolism depends on hepatic blood flow

48
Q

metabolite of ketamine

A

norketamine (active)

49
Q

metabolism of dexmedetomidine

A

hepatic

50
Q

metabolism of lidocaine

A

hepatic

Pharmacology N926 (16 decks)

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