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Frcr Oncology > HORMONES > Flashcards

HORMONES Flashcards

1
Q

Tamoxifen is FDA approved for

A

Premenopausal breast cancer
DCIS

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2
Q

Class of tamoxifen

A

Serm, non steroidal anti estrogen

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3
Q

Dose of tamoxifen

A

20 mg oral once daily

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4
Q

Duration of tamoxifen

A

Dcis 5 years
Invasive ca breast 10 yrs increased OS

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5
Q

Positive effects of tamoxifen

A

Decrease in total cholesterol
Preservation of bone density in post menopausal

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6
Q

Negative effects of tamoxifen

A

Negative effects on bone marrow in pre menopausal
Hot flashes
Endometrial ca in post menopausal
Thromboembolism when used along with chemo
Vaginal dryness

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7
Q

Treatment of hot flashes

A

Antidepressants like venlafaxine, desvenlafaxine, citalopram,
Anticonvulsant like gabapentin and pregabalin

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8
Q

Moa of tamoxifen

A

Competes with estrogen in binding to ER causes ER dimerisation which is transported to nucleus
Blocking estrogen stimulation of breast cancer cells - translocation and nuclear binding of ER.

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9
Q

Metabolites of tamoxifen

A

4 hydroxy tamoxifen 7 percent
N desmethyl tamoxifen further converted to Endoxifen major

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10
Q

Metabolism of tamoxifen

A

Liver - cyp2D6 - endoxifen most abundant

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11
Q

Distribution of tamoxifen

A

Plasma
Liver, lungs, brain, pancreas, skin and bones

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12
Q

Polymorphism in cyp2D6 causes , and how to treat it

A

Recurrence due to reduced endoxifen levels
Alternate hormonal therapy or high dose of tamoxifen 40 mg per day dose

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13
Q

Is tamoxifen cell cycle specific

A

Mid G1 phase

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14
Q

Absorption, excretion of tamoxifen

A

In GI tract
Excreted in feces 75 percent

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15
Q

Drug interactions of tamoxifen

A

Inhibitors of Cyp2D6 like SSRI SNRI cimetidine quinine terfanadine inhibits tamoxifen metabolism, lowers the level of active tamoxifen metabolites

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16
Q

Can u breast feed with tamoxifen

A

No cat D

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17
Q

What is tumor flare

A

In tamoxifen first two weeks ,
Increased bone pain, urinary retention, back pain

18
Q

Does tamoxifen cause myelosuppression

A

No

19
Q

Classify aromatise inhibitors

A

Steroidal : 2nd gen - formestane
3 rd gen x exemestane

Non steroidal
1st gen aminogletheamine
2 nd gen fadrozole
3 rd gen letrozole anastrozole and vorzole

20
Q

Action of AI

A

Steroidal : compete with endogenous steroids; irreversibly inhibits by suicide capture , covalent binding

Non steroidal : reversible binding to endogenous substrate ; ionic bonds

21
Q

Class of anastrozole

A

Non steroidal AI

22
Q

Moa of anastrozole

A

Inhibits Aromatase
No inhibition of adrenal glands

23
Q

No of days after which estrogen falls in anastrozole therapy

A

Suppressed by 90% within 14 days of treatment
Completely suppressed in 6 weeks

24
Q

Absorption of anastrozole

A

85% oral within 2 hrs

25
Q

Distribution of anastrozole

A

40% plasma protein binding

26
Q

Metabolism and excretion of anastrozole

A

Liver

Excretion in feces / renal 10%

27
Q

Indications and dose of anastrozole

A

1 mg PO once daily for 5 years

In hormone positive post menopausal women and premenopausal women after ovarian ablation

28
Q

Adverse effects of anastrozole

A

Decrease in BMD - supplement with calcium 1200 to 1500 and vit D
If bmd decrease can also start on zoledronic acid

29
Q

Dose of letrozole

A

2.5 mg PO once daily for five years in post menopausal women

30
Q

Should you reduce anastrozole letrozole doses

A

Anastrozole dose need not be reduced

Letrozole reduce by 50% in cirrhoses and hepatic dysfunction- 2.5 mg PO every alternate day

31
Q

What happens even we give letrozole in pre menopausal group

A

No efficacy
Increased benign ovarian tumours and cystic ovarian disease

32
Q

Moa of exemestane

A

Steroidal ai
Irreversibly inhibits Aromatase

33
Q

Causes of resistance in exemestane

A

Cross between steroidal and non steroidal Ai

34
Q

PHARMA OF EXEMESTANE

A

Absorption : oral 85%
Distribution: 90% plasma protein
Metabolism : cyp3A4 liver
Excretion: feces , renal only 10%

35
Q

Indications of exemestane

A

25 mg PO once Daily

36
Q

Interaction of exemestane

A

Drugs that inhibit cyp3A4 decrease the metabolism of exemestane

37
Q

What are bisphosphonates

A

Pyrophosphate analogues that bind to calcium phosphate with high affinity
Affect bone resorption by osteoclasts inhibition

38
Q

Additional Moa of Za

A

Inhibits the tumor cell adhesion to ECM

39
Q

Dose of ZA

A

4mg intravenous over 15 mins every4 weeks

40
Q

Complications of ZA

A

Orn of jaw
Renal insufficiency
Check RFT

Frcr Oncology (7 decks)

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