Drugs, Metabolism, and Their Metabolites

Question 1

metabolite of morphine

Answer 1

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

Question 2

morphine 6 glucoronide

Answer 2

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

Question 3

metabolite of meperidine

Answer 3

normeperidine

Question 4

normeperidine

Answer 4

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

Question 5

primarily metabolism of morphine

Answer 5

conjugation with glucoronic acid

Question 6

metabolism of meperidine

Answer 6

90% demethylization to normeperidine

10% hydrolysis to meperidinic acid

Question 7

metabolism of fentanyl

Answer 7

N dealkylation and hydroxylation

Question 8

metabolism of sufentanil

Answer 8

N dealkylation to inactive metabolites, and O demethlyation

Question 9

metabolite of sufentanil

Answer 9

O demethylation to desmethyl sufentanil

Question 10

metabolism of alfentanil

Answer 10

piperidine N dealkylation, amide N-dealkylation

Question 11

metabolites of alfentanil

Answer 11

piperidine N dealkylation to noralfentanil (active)

amide N-dealkylation to N-phenylpropionamide

Question 12

metabolism of remifentanil

Answer 12

metabolized by non specific plasma esterase’s

Question 13

metabolism of tramadol

Answer 13

metabolized by CYP450

Question 14

metabolite of tramodol

Answer 14

O-desmethyltramadol, which has modest analgesic effects

Question 15

metabolism of heroin

Answer 15

hydrolyzed in the CNS

Question 16

metabolites of heroin

Answer 16

monoacetylmorphine (active)

morphine (active)

Question 17

metabolism of butorphanol

Answer 17

metabolism via liver and excreted primarily in bile

Question 18

metabolite of butorphanol

Answer 18

hydroxybutorphanol (inactive)

Question 19

metabolism of naloxone

Answer 19

conjugation with glucoronic acid

Question 20

metabolite of naloxone

Answer 20

naloxone 3 glucoronide

Question 21

metabolism of nalmefene

Answer 21

hepatic conjugation

Question 22

metabolism of aspirin

Answer 22

plasma esterases, erythrocytes, and liver

Question 23

metabolite of acetaminophen

Answer 23

N acetyl p benzoquinoneimine

Question 24

metabolism of Ach

Answer 24

hydrolysis via acetylcholinesterase

Question 25

plasma cholinesterase facts

Answer 25

also called butyrylcholinesterase, or pseudocholinesterase, synthesized in the liver

Question 26

metabolism of succinylcholine

Answer 26

hydrolysis by butyrylcholinesterase to succinylmonocholine and choline.

Question 27

metabolite of succinylcholine

Answer 27

succinylmonocholine is weak NMB, metabolized to succinic acid and choline

Question 28

What does butyrylcholinesterase metabolize?

Answer 28

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

Question 29

metabolism of cisatracurium

Answer 29

hoffman elimination. no ester hydrolysis.

Question 30

metabolism of mivacurium

Answer 30

butyrylcholinesterase

Question 31

metabolites of mivacurium

Answer 31

monoester, dicarboxylic acid

Question 32

metabolism of vecuronium

Answer 32

principally by the liver

Question 33

metabolite of vecuronium

Answer 33

3-OH metabolite, has 80% neuromuscular potency

Question 34

clearance of pancuronium

Answer 34

small amount deacetylated by the liver | accumulation of 3-OH metabolite responsible for block prolongation

Question 35

clearance of rocuronium

Answer 35

primarily metabolized in liver, 30% excreted in urine

Question 36

metabolism of thiopental

Answer 36

oxidized in liver

Question 37

metabolism of midazolam

Answer 37

oxidized by CYP450

Question 38

metabolites of midazolam

Answer 38

apparently theres two active metabolites

Question 39

metabolism of diazepam

Answer 39

metabolized by hepatic microsomal enzymes using oxidative pathway of N methylation

Question 40

metabolites of diazepam

Answer 40

desmethyldiazepam (nordiazepam) and oxazepam

Question 41

metabolism of lorazepam

Answer 41

conjugated with glucoronic acid in the liver (glucoronidation)

Question 42

metabolism of oxazepam

Answer 42

conjugated by glucoronic acid to inactive metabolism

Question 43

metabolite of flurazepam

Answer 43

salkylflurazepam (active)

Question 44

metabolism of propofol

Answer 44

via CYP450, plasma esterase metabolism

Question 45

metabolite of propofol

Answer 45

4 hydroxypropofol

Question 46

metabolism of etomidate

Answer 46

hydrolysis (phase 1)

Question 47

metabolism of ketamine

Answer 47

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

Question 48

metabolite of ketamine

Answer 48

norketamine (active)

Question 49

metabolism of dexmedetomidine

Answer 49

hepatic

Question 50

metabolism of lidocaine

Answer 50

hepatic