IC9 & 10

Question 1

What does Tamoxifen act as?

Answer 1

Acts as a selective estrogen receptor modulator (SERM)

Question 2

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

Answer 2

Trans; to display anti-estrogenic activity

Question 3

What is tamoxifen used mainly for?

Answer 3

breast cancer

Question 4

What is pembrolizumab used mainly for?

Answer 4

cervical cancer

Question 5

Bicalutamide - why cannot use as monotherapy for prostate cancer?

Answer 5

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

Question 6

Bicalutamide & Leuprorelin - indication?

Answer 6

Prostate cancer

Question 7

Prostate growth depends on androgens (T/F)

Answer 7

True

Question 8

How is pembrolizumab metabolised?

Answer 8

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

Question 9

Dosage form for pembrolizumab

Answer 9

IV

Question 10

Does pembrolizumab bind to plasma protein?

Answer 10

No

Question 11

Does tamoxifen bind to plasma protein?

Answer 11

Yes, Plasma protein binding > 98%

Question 12

Action of pembrolizumab

Answer 12

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

Question 13

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

Answer 13

1. Corticosteroids
2. Immunosuppressants

Question 14

Contraindication for pembrolizumab

Answer 14

1. Pregnant women
2. Hypersensitivity

Question 15

DDI for tamoxifen

Answer 15

CYP3A4 inhibitor & CYP2D6 inhibitors (incr conc of tamoxifen)

Question 16

Dosage form for leuprorelin

Answer 16

IV/IM/SC

Question 17

Action of leuprorelin

Answer 17

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

Question 18

How is leuprorelin metabolised?

Answer 18

Degraded proteolytically into inactive peptides

Question 19

Monitoring for leuprorelin

Answer 19

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

Question 20

C/I for leuprorelin

Answer 20

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

Question 21

Dosage form for bicalutamide

Answer 21

Oral tablets

Question 22

Dosage form for tamoxifen

Answer 22

Oral

Question 23

Action of bicalutamide

Answer 23

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

Question 24

Bicalutamide: S or R isomer is active?

Answer 24

R isomer

Question 25

DDI for Bicalutamide

Answer 25

CYP3A4 inhibitor (incr Bicalutamide conc)

Question 26

Should Bicalutamide be used as monotherapy for prostate cancer?

Answer 26

No, it is usually used with GnRH analogue

Question 27

Structure of leuprorelin

Answer 27

Polypeptide

Question 28

Extent of protein binding: Metformin

Answer 28

Minimal

Question 29

Elimination of metformin

Answer 29

Renal elimination

Question 30

MOA for glipizide (SU)

Answer 30

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

Question 31

Metabolism of glipizide

Answer 31

Metabolised by liver (hydroxylation)

Question 32

Which population should not use glipizide?

Answer 32

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

Question 33

Dosage form for sitagliptin (DPP-4i)

Answer 33

Oral

Question 34

MOA for sitagliptin

Answer 34

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

Question 35

Caution use for sitagliptin

Answer 35

1. Caution use in renal impairment 2. Caution use in Hx of pancreatitis

Question 36

Class of liraglutide

Answer 36

GLP-1 agonist

Question 37

MOA for liraglutide

Answer 37

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

Question 38

Metabolism for liraglutide

Answer 38

Similar to proteins, no specific organ

Question 39

Metabolism for empagliflozin

Answer 39

Metabolised in liver (glucuronidation)

Question 40

Dosage form for liraglutide

Answer 40

SC

Question 41

MOA for empagliflozin

Answer 41

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

Question 42

Extent of protein binding for empagliflozin

Answer 42

Extensively protein bound

Question 43

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

Answer 43

True