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3152 > IC9 & 10 > Flashcards

IC9 & 10 Flashcards

1
Q

What does Tamoxifen act as?

A

Acts as a selective estrogen receptor modulator (SERM)

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2
Q

Is Cis/ trans isomer of Tamoxifen used for breast cancer?

A

Trans; to display anti-estrogenic activity

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3
Q

What is tamoxifen used mainly for?

A

breast cancer

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4
Q

What is pembrolizumab used mainly for?

A

cervical cancer

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5
Q

Bicalutamide - why cannot use as monotherapy for prostate cancer?

A

Blocks A -> incr LH secretion -> (+) higher serum testosterone levels

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6
Q

Bicalutamide & Leuprorelin - indication?

A

Prostate cancer

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7
Q

Prostate growth depends on androgens (T/F)

A

True

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8
Q

How is pembrolizumab metabolised?

A

General protein degradation (recall: Mabs are big in size)

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9
Q

Dosage form for pembrolizumab

A

IV

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10
Q

Does pembrolizumab bind to plasma protein?

A

No

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11
Q

Does tamoxifen bind to plasma protein?

A

Yes, Plasma protein binding > 98%

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12
Q

Action of pembrolizumab

A

PD1-blocker
(basically prevent PD-L1 on tumour cells from binding to PD-1 that would inactivate T cell action

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13
Q

What should be stopped when initiating pembrolizumab? (added back aft initiation)

A
  1. Corticosteroids
  2. Immunosuppressants
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14
Q

Contraindication for pembrolizumab

A
  1. Pregnant women
  2. Hypersensitivity
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15
Q

DDI for tamoxifen

A

CYP3A4 inhibitor & CYP2D6 inhibitors (incr conc of tamoxifen)

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16
Q

Dosage form for leuprorelin

A

IV/IM/SC

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17
Q

Action of leuprorelin

A

GnRH analogue -> inhibits FSH and LH release -> decr androgen synthesis -> decr testosterone production -> apoptosis of prostate cancer cells

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18
Q

How is leuprorelin metabolised?

A

Degraded proteolytically into inactive peptides

19
Q

Monitoring for leuprorelin

A

Measure PSA, LH and FSH in 1st few weeks, and testosterone aft 4 weeks of therapy

20
Q

C/I for leuprorelin

A
  1. Hypersensitivity to leuprorelin/ other GnRH agonists, 2. pre-existing heart disease
  2. risks for osteoporosis
21
Q

Dosage form for bicalutamide

A

Oral tablets

22
Q

Dosage form for tamoxifen

A

Oral

23
Q

Action of bicalutamide

A

Inhibits androgen receptor -> inhibits AR-dependent transcription -> impairs cell proliferation & triggers apoptosis in cancer cells

24
Q

Bicalutamide: S or R isomer is active?

A

R isomer

25
Q

DDI for Bicalutamide

A

CYP3A4 inhibitor (incr Bicalutamide conc)

26
Q

Should Bicalutamide be used as monotherapy for prostate cancer?

A

No, it is usually used with GnRH analogue

27
Q

Structure of leuprorelin

A

Polypeptide

28
Q

Extent of protein binding: Metformin

A

Minimal

29
Q

Elimination of metformin

A

Renal elimination

30
Q

MOA for glipizide (SU)

A

Binds to SU receptor of ATP-sensitive potassium channels -> inhibits K+ efflux, triggers Ca-dependent exocytosis of insulin from pancreatic beta cells

31
Q

Metabolism of glipizide

A

Metabolised by liver (hydroxylation)

32
Q

Which population should not use glipizide?

A

Should not be used in ppl w/o functional beta cells

33
Q

Dosage form for sitagliptin (DPP-4i)

A

Oral

34
Q

MOA for sitagliptin

A

Inhibits DPP-4 -> inhibits the breakdown of GLP-1 -> incr glucose- stimulated insulin release

35
Q

Caution use for sitagliptin

A
  1. Caution use in renal impairment
  2. Caution use in Hx of pancreatitis
36
Q

Class of liraglutide

A

GLP-1 agonist

37
Q

MOA for liraglutide

A

Binds to GLP-1 -> activates adenyl cyclase -> incr cAMP -> activates PKA -> incr insulin secretion & decr glucagon release

38
Q

Metabolism for liraglutide

A

Similar to proteins, no specific organ

39
Q

Metabolism for empagliflozin

A

Metabolised in liver (glucuronidation)

40
Q

Dosage form for liraglutide

A

SC

41
Q

MOA for empagliflozin

A

Inhibits SGLT2 in proximal renal tubule, decr reabsorption of filtered glucose -> decr blood glucose

42
Q

Extent of protein binding for empagliflozin

A

Extensively protein bound

43
Q

Use of empagliflozin could predispose one to UTI (T/F)

A

True

3152 (18 decks)

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