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PR3152 Pharmacology and Biopharmaceutics > Men and Women Health > Flashcards

Men and Women Health Flashcards

1
Q

What is the mode of action of tamsulosin?

A

Inhibits alpha 1 adrenergic receptors

Inhibit vasoconstriction by endogenous catecholamines

Decreases muscle tone and reduce bladder obstruction

Relax smooth muscle and improve urodynamic

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2
Q

Why is tamsulosin preferred to the other alpha adrenergic antagonist?

A

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

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3
Q

How is tamsulosin absorbed?

A

Orally

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4
Q

How is tamsulosin distributed?

A

High plasma protein binding

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5
Q

How is tamsulosin metabolized?

A

Through the liver by CYPs

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6
Q

What are significant DDI to consider for those on tamsulosin?

A

CYP450 inducers and inhibitors
Grapefruit juice

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7
Q

How is tamsulosin excreted?

A

Urine

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8
Q

What are some of the adverse effects of tamsulosin?

A

Abnormal ejaculation

Back pain

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9
Q

What is the mode of action of finasteride?

A

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

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10
Q

What are the adverse effects of finasteride?

A

Loss of libido and sexual potency
Gynecomastia

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11
Q

Who are contraindicated towards the use of finasteride?

A

Women, children
Those that are pregnant

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12
Q

What is the mode of action of sildenafil?

A

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

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13
Q

What is a clinical benefit of sildenafil?

A

Selective to cavernosa of penis but poorly to PDE5 in myocardium

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14
Q

How is sildenafil absorbed?

A

Orally

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15
Q

Does sildenafil require dose adjustment for renal and liver failure?

A

No

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16
Q

How is the distribution like for sildenafil?

A

Widely distributed

17
Q

How is sildenafil metabolized? What enzymes are involved?

A

Liver
Major pathway: CYP3A4
Minor pathway: CYP2C9

18
Q

How is sildenafil excreted?

A

Feces

19
Q

What are some potential adverse effects of sildenafil?

A

Headache
Flushing
Dyspepsia
Dizziness
Back pain
Blurred vision
Priapism

20
Q

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

A

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

21
Q

What is the mode of action of ethinyl estradiol?

A

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

22
Q

What are the indications for the use of ethinyl estradiol?

A

Menopause
Gynecological disorder
Hormone sensitive cancer

23
Q

How is ethinyl estradiol absorbed?

A

Oral

24
Q

How is ethinyl estradiol distributed?

A

High plasma protein binding

25
Q

How is ethinyl estradiol metabolized and discuss the metabolic pathway

A

Enterohepatic circulation also occurs

Metabolized in the liver via Phase 1 hydroxylation
Phase 2 conjugation, glucuronidation and sulphation

Forms ethinylestradiol glucuronide and sulfate

26
Q

How is ethinyl estradiol eliminated?

A

Faeces and urine

27
Q

List some of the mild adverse effects of ethinyl estradiol

A

Breast tenderness
Headache
Fluid retention
Nausea
Dizziness
Weight gain

28
Q

List some of the major adverse effects of ethinyl estradiol.

A

VTE
Breast cancer
Myocardial infarction
Liver damage

29
Q

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

A

Known history or susceptibility to VTE

Advanced DM with vascular disease

Hypertension > 160/100

Breast feeding (<21 days post partum)

Breast cancer

30
Q

What is the mode of action of norethindrone?

A

Synthetic progesterone inhibits LH release

Prevents ovulation by making endometrial unstable for implantation of ovum

31
Q

What are some indications of norethindrone?

A

Endometriosis

Abnormal periods / bleeding

32
Q

How is norethindrone absorbed?

A

Orally

33
Q

How is norethindrone dsitributed?

A

High plasma protein binding

34
Q

How is norethindrone metabolized?

A

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

35
Q

How is norethindrone excreted?

A

Urine and feces

36
Q

What are some adverse effects of norethindrone?

A

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

37
Q

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

A

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

PR3152 Pharmacology and Biopharmaceutics (6 decks)

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