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Endocrine > ADME > Flashcards

ADME Flashcards

1
Q

Tamoxifen absorption

A
  • Rapid and complete oral absorption
  • Peak in 5 hours
  • Css reached in 3-4 weeks, or up to 16 weeks
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2
Q

Tamoxifen distribution

A
  • Highly plasma protein bound
  • High Vd (50-60 L/kg)
  • Good distribution to the breast, uterus, liver, kidneys, lungs, pancreas, ovaries (up to 10x higher in breast than blood)
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3
Q

Tamoxifen metabolism

A
  • CYP2D6 (hydroxylation) & CYP3A4 (N-demethylation)
  • Phase 2 (sulfation, glucuronidation)
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4
Q

Tamoxifen elimination

A
  • Similar CL as CrCL
  • T1/2 of 5-7 days
  • Feces
  • Negligible urine
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5
Q

Pembrolizumab absorption

A
  • IV 200 mg as a slow infusion, every 3 weeks
  • May reach Css in 19 weeks
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6
Q

Pembrolizumab distribution

A
  • Small Vd of 7 L
  • Not bound to albumin in any specific manner
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7
Q

Pembrolizumab metabolism

A
  • Non-specific protein catabolism
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8
Q

Pembrolizumab elimination

A
  • Unknown on the routes
  • T1/2 of 27 days
  • Factors affecting CL = albumin/bilirubin levels, type of cancer, gender
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9
Q

Leuprorelin absorption

A
  • SC/IM administration as a single depot dose
  • Cmax reached in 1-3 hours
  • Css reached in 4 weeks
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10
Q

Leuprorelin distribution

A
  • ~45% bound to albumin
  • Unclear Vd
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11
Q

Leuprorelin metabolism

A
  • Proteolytic degradation pathways
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12
Q

Leuprorelin elimination

A
  • T1/2 of 3 hours
  • Non-significant by the urine or feces
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13
Q

Bicalutamide absorption

A
  • PO once daily
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14
Q

Bicalutamide distribution

A
  • Highly albumin bound
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15
Q

Bicalutamide metabolism

A
  • S: glucuronidation
  • R: hydroxylation by 3A4, glucuronidation
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16
Q

Bicalutamide elimination

A
  • T1/2 of 6 days
  • Excreted in bile & urine
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17
Q

Metformin absorption

A
  • Taken orally
  • Duration of action: 8-12 hours
  • Onset within days, max effect up to 2 weeks
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18
Q

Metformin distribution

A
  • Not bound to plasma protein
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19
Q

Metformin metabolism

A
  • Nil liver metabolism
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20
Q

Metformin elimination

A
  • T1/2 of 3 hours
  • Mostly excreted unchanged in the urine
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21
Q

Glipizide absorption

A
  • Well absorbed
  • Absorption is delayed with food
  • Onset of action: 0.5 hours
  • Duration of action: 12-24 hours
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22
Q

Glipizide distribution

A
  • Highly bound to albumin
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23
Q

Glipizide metabolism

A
  • Hydroxylation in the liver
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24
Q

Glipizide elimination

A
  • T1/2 of 4 hours
  • < 10% excreted unchanged in the urine & feces
  • Action prolonged in renal impairments
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25
Q

Sitagliptin absorption

A
  • Relatively good oral bioavailability
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26
Q

Sitagliptin metabolism

A
  • Low liver metabolism
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27
Q

Sitagliptin elimination

A
  • T1/2 of 10-12 hours
  • 80% excreted unchanged in the urine
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28
Q

Liraglutide absorption

A
  • Daily SC dosing, steady state daily maintenance dose of 3 mg
  • 55% bioavailability
29
Q

Liraglutide distribution

A
  • C16 FA chain binds to albumin
30
Q

Liraglutide metabolism

A
  • Non-specific catabolism
31
Q

Liraglutide elimination

A
  • T1/2 of 13 hours
  • Negligible in urine & feces
32
Q

Empagliflozin absorption

A
  • 60-80% bioavailability
33
Q

Empagliflozin distribution

A
  • Highly bound to albumin
34
Q

Empagliflozin metabolism

A
  • Glucuronidation
35
Q

Empagliflozin elimination

A
  • T1/2 of 12 hours
  • 40% in feces, 50% in urine
36
Q

Carbimazole absorption

A
  • Once daily dosing
  • Inhibitory effect achieved within 12 hours
  • Effect may be delayed to 4-6 months
37
Q

Carbimazole distribution

A
  • Methimazole concentrates well in the thyroid gland
  • No plasma protein binding
  • Produces the inhibition of thyroid hormone production in 12 hours, but full effect takes up to 3-6 weeks
  • Max effect take 4-6 months
38
Q

Carbimazole metabolism

A
  • CYP450 & FMO
39
Q

Carbimazole elimination

A
  • T1/2 of 4-6 hours but clinical effect lasts a day
  • Metabolites excreted 90% in urine
40
Q

Levothyroxine absorption

A
  • Erratic absorption
  • Taken 30-60 mins before food
  • Absorption affected by polyvalent cations, increased gastric pH, fibres, GI motility
  • Onset of action 3-5 days, 6-8 hours (IV)
  • Symptomatic relief in 2-3 weeks
41
Q

Levothyroxine distribution

A
  • Highly plasma protein bound
42
Q

Levothyroxine metabolism

A
  • Deiodination by liver, kidneys and peripheral tissues
  • Glucuronidation & sulfation by liver
43
Q

Levothyroxine elimination

A
  • T1/2 of 7 days
  • Excreted in urine, feces, and metabolites in bile
44
Q

Rapid acting insulin

A
  • Onset 15-30 mins
  • Peak: 1-2 hours
45
Q

Short acting insulin

A
  • Onset 30-60 mins
  • Peak 2-4 hours
46
Q

Intermediate acting insulin

A
  • Onset 1-2 hours
  • Peak 6-12 hours
  • Duration of action: 10-16 hours
47
Q

Detemir

A
  • Onset 1-2 hours
  • Hill
  • Duration of action: 12 hours or up to 20-24 hours
48
Q

Glargine U-100

A
  • Onset 1-2 hours
  • No peak
    Duration of action: 24 hours
49
Q

Tamsulosin absorption

A
  • Once daily 0.4 mcg
  • Onset within days to weeks
50
Q

Tamsulosin distribution

A
  • Highly bound to plasma proteins
  • Small Vd of 0.2 L/kg
51
Q

Tamsulosin metabolism

A
  • CYP2D6 & 3A4
52
Q

Tamsulosin elimination

A
  • T1/2 of 10-15 hours
  • Metabolites excreted in urine
53
Q

Finasteride absorption

A
  • Orally 5 mg once daily
  • Relatively low F of 0.65
  • Delayed onset, up to 6-12 months to observe clinical improvement
  • Nil dose adjustment
54
Q

Finasteride distribution

A
  • Highly bound to plasma proteins
55
Q

Finasteride metabolism

A
  • CYP3A4
56
Q

Finasteride elimination

A
  • T1/2 of 6 hours
  • 50% excreted unchanged in feces
  • Metabolites in urine & feces
57
Q

Sildenafil absorption

A
  • Low F of 0.4
  • Onset 30-60 mins
  • Duration of action 12 hours
58
Q

Sildenafil distribution

A
  • Highly plasma protein bound
59
Q

Sildenafil metabolism

A
  • Major: CYP3A4
  • Minor: CYP2C9
60
Q

Sildenafil elimination

A
  • T1/2 of 4 hours
  • Metabolites in feces
61
Q

Ethinyl estradiol absorption

A
  • Onset 30-60 mins
  • Relatively low F of 0.4
62
Q

Ethinyl estradiol distribution

A
  • Highly bound to plasma proteins
63
Q

Ethinyl estradiol metabolism

A
  • Phase 1: Hydroxylation by CYP3A4
  • Phase 2: Glucuronidation & sulfation
  • Ethinyl estradiol sulfate undergoes enterohepatic recirculation
64
Q

Ethinyl estradiol elimination

A
  • T1/2 of 13-27 hours
  • Urine & feces
65
Q

Norethindrone absorption

A
  • Relatively low F of 0.6
66
Q

Norethindrone distribution

A
  • Highly bound to plasma proteins
67
Q

Norethindrone metabolism

A
  • Phase 1: Reduction
  • Phase 2: Glucuronidation, sulfation
  • May be metabolised into EE
68
Q

Norethindrone elimination

A
  • T1/2 of 8 hours
  • Urine & feces

Endocrine (4 decks)

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