Men and Women Health

Question 1

What is the mode of action of tamsulosin?

Answer 1

Inhibits alpha 1 adrenergic receptors

Inhibit vasoconstriction by endogenous catecholamines

Decreases muscle tone and reduce bladder obstruction

Relax smooth muscle and improve urodynamic

Question 2

Why is tamsulosin preferred to the other alpha adrenergic antagonist?

Answer 2

Increased selectivity towards alpha 1A receptors
Effects maintained during long term therapy
Delays the need for surgery and improve urinary flow rate

Question 3

How is tamsulosin absorbed?

Answer 3

Orally

Question 4

How is tamsulosin distributed?

Answer 4

High plasma protein binding

Question 5

How is tamsulosin metabolized?

Answer 5

Through the liver by CYPs

Question 6

What are significant DDI to consider for those on tamsulosin?

Answer 6

CYP450 inducers and inhibitors
Grapefruit juice

Question 7

How is tamsulosin excreted?

Answer 7

Urine

Question 8

What are some of the adverse effects of tamsulosin?

Answer 8

Abnormal ejaculation

Back pain

Question 9

What is the mode of action of finasteride?

Answer 9

Inhibition of 5 alpha reductase inhibits the conversion of testosterone to DHT

Decrease in prostate size occurs allowing better urine flow, help with acute retention of urine and decrease the need for surgery

Question 10

What are the adverse effects of finasteride?

Answer 10

Loss of libido and sexual potency
Gynecomastia

Question 11

Who are contraindicated towards the use of finasteride?

Answer 11

Women, children
Those that are pregnant

Question 12

What is the mode of action of sildenafil?

Answer 12

Inhibit PDE5 in penis

Increases cGMP level in response to nitric oxide released by sexual stimulation

Smooth muscle relaxation occurs and blood flows to cavernosa

Erection occurss

Question 13

What is a clinical benefit of sildenafil?

Answer 13

Selective to cavernosa of penis but poorly to PDE5 in myocardium

Question 14

How is sildenafil absorbed?

Answer 14

Orally

Question 15

Does sildenafil require dose adjustment for renal and liver failure?

Answer 15

No

Question 16

How is the distribution like for sildenafil?

Answer 16

Widely distributed

Question 17

How is sildenafil metabolized? What enzymes are involved?

Answer 17

Liver
Major pathway: CYP3A4
Minor pathway: CYP2C9

Question 18

How is sildenafil excreted?

Answer 18

Feces

Question 19

What are some potential adverse effects of sildenafil?

Answer 19

Headache
Flushing
Dyspepsia
Dizziness
Back pain
Blurred vision
Priapism

Question 20

What is a significant DDI to avoid with sildenafil and why?

Answer 20

GTN
Can potentiate vasodilation effect on GTN by increasing cGMP causing potential hypotension

Question 21

What is the mode of action of ethinyl estradiol?

Answer 21

Act as estrogen receptor agonist by inhibiting FSH from anterior pituitary

Suppressing the development of ovarian follicle

Making it difficult for endometrial to implant mature ovum

Question 22

What are the indications for the use of ethinyl estradiol?

Answer 22

Menopause
Gynecological disorder
Hormone sensitive cancer

Question 23

How is ethinyl estradiol absorbed?

Answer 23

Oral

Question 24

How is ethinyl estradiol distributed?

Answer 24

High plasma protein binding

Question 25

How is ethinyl estradiol metabolized and discuss the metabolic pathway

Answer 25

Enterohepatic circulation also occurs Metabolized in the liver via Phase 1 hydroxylation Phase 2 conjugation, glucuronidation and sulphation Forms ethinylestradiol glucuronide and sulfate

Question 26

How is ethinyl estradiol eliminated?

Answer 26

Faeces and urine

Question 27

List some of the mild adverse effects of ethinyl estradiol

Answer 27

Breast tenderness Headache Fluid retention Nausea Dizziness Weight gain

Question 28

List some of the major adverse effects of ethinyl estradiol.

Answer 28

VTE Breast cancer Myocardial infarction Liver damage

Question 29

What are some contraindications to know of ethinyl estradiol? (HINT: Avoid in patients with...)

Answer 29

Known history or susceptibility to VTE Advanced DM with vascular disease Hypertension > 160/100 Breast feeding (<21 days post partum) Breast cancer

Question 30

What is the mode of action of norethindrone?

Answer 30

Synthetic progesterone inhibits LH release Prevents ovulation by making endometrial unstable for implantation of ovum

Question 31

What are some indications of norethindrone?

Answer 31

Endometriosis Abnormal periods / bleeding

Question 32

How is norethindrone absorbed?

Answer 32

Orally

Question 33

How is norethindrone dsitributed?

Answer 33

High plasma protein binding

Question 34

How is norethindrone metabolized?

Answer 34

Via the liver through Phase I reduction and Phase II glucuronidation and sulfation

Question 35

How is norethindrone excreted?

Answer 35

Urine and feces

Question 36

What are some adverse effects of norethindrone?

Answer 36

Headache, dizziness, bloating, weight gain, unpredictable spotting and bleeding, amenorrhea

Question 37

What is one special advice to counsel patients who intent to start on norethindrone?

Answer 37

Not desirable for women planning a pregnancy after cessation as effect can last up to 1.5 years