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3152 Reprod Health > Pharmacology ADME (IC15) > Flashcards

Pharmacology ADME (IC15) Flashcards

1
Q

Describe the absorption profile of Ethinyl Estradiol (EE)

A

Well absorbed orally, onset 30-60min, F~0.45

May be administered in transdermal patch, vaginal ring as well

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2
Q

Describe the distribution profile of Ethinyl Estradiol (EE)

A

Highly plasma protein bound, ~98%

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3
Q

Describe the metabolism of Ethinyl Estradiol (EE)

A

Metabolised in liver

Phase 1: hydroxylation by CYP3A4 (think DDI, FDI)

Phase 2: conjugation with glucuronide and sulfation into hormonally inert ethinylestradiol glucuronides and ethinylestradiol sulfate

*Enterohapatic recirculation of ethinylestradioll sulfate can enhance effect of EE
(liver => bile => SI => absorption by enterocyte and transport back to liver)

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4
Q

Describe the excretion profile of Ethinyl Estradiol (EE)

A

Excreted in feces and urine

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5
Q

What are some adverse effects of EE?

*Relate back to IC16, CI in IC16

A
  • Breast tenderness
  • Headache
  • Fluid retention (bloating)
  • Nausea
  • Dizziness
  • Weight gain

More severe:
- Breast cancer
- VTE
- MI/Stroke
- Liver damage

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6
Q

Describe the absorption profile of Norethindrone

A

Well absorbed orally, once a day
F~64%

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7
Q

Describe the distribution profile of Norethindrone

A

Highly plasma protein bound (e.g., albumin)

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8
Q

Describe the metabolism of Norethindrone

A

Metabolised in liver

Phase 1: Reduction

Phase 2: Glucuronidation and Sulfation

Some evidence suggest that norethindrone can be metabolised in the liver to EE - potential cardiovascular complications (VTE)

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9
Q

Describe the excretion of Norethindrone

A

Excreted in urine and feces

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10
Q

What are some adverse effects of Norethindrone?

*Relate back to IC16

A
  • Headache
  • Dizziness
  • Bloating (more due to E)
  • Weight gain
  • Episodes of unpredictable spotting and bleeding (initially)
  • Amenorrhea
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11
Q

Why is Norethindrone not recommended for women planning a pregnancy soon?

A

Ovulation suppression can persist for as long as 1.5y

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12
Q

Describe the in depth MOA of Tamsulosin (BPH)

A

Tamsulosin - reversible alpha-1 receptor antagonist

  • Inhibits vasoconstriction induced by endogenous catecholamines (noradrenaline)
  • Blocks alpha receptor on smooth muscle of prostate, prostatic urethra, bladder neck, lead to decrease muscle tone, relaxation of prostate smooth muscle and reduction in bladder obstruction, and improvement in urinary flow
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13
Q

Explain the selectivity of Tamsulosin

A

Selective for urinary a1A receptors predominantly found in prostate and LUT

Does not favour a1B receptors on blood vessels and heart

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14
Q

Describe the absorption profile of Tamsulosin

A

Well absorbed orally, 0.4mg once a day

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15
Q

Describe the distribution profile of Tamsulosin

A

Highly bound to plasma protein (90-99%)
Small Vd (0.2L/kg)

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16
Q

Describe the metabolism of Tamsulosin

A

Metabolized in liver by CYP3A4, CYP2D6
- watch out DDI, FDI

17
Q

Describe the excretion of Tamsulosin

A

Excreted in urine

18
Q

What drugs are contraindicated with Tamsulosin?

A

Other alpha-1 adrenergic antagonists
E.g.,
- Prazosin
- Epinephrine

=> Hypotension

19
Q

Apart from decreasing prostate size (use in BPH), Finasteride (5ARI) can also cause _____

A

Increase hair growth (on scalp)
- may use 1mg daily for male pattern baldness or in hirsutism in women

*Thus, use in BPH, use in androgenic alopecia
*Dose in hair problems is 20% of that in BPH (1mg vs 5mg)

20
Q

By reducing prostate size, Finasteride reduces _____

A

Finasteride reduces:
- progression of BPH
- the need for surgical procedure (TURP, prostatectomy)

21
Q

Describe the absorption profile of Finasteride (5ARI)

A

Well absorbed orally 5mg daily
No dose adjustment required in renal insufficiency, liver failure, elderly patients

22
Q

Describe the distribution profile of Finasteride (5ARI)

A

Highly plasma protein bound ~90%

23
Q

Describe the metabolism of Finasteride (5ARI)

A

Metabolized by liver (e.g., CYP3A4)

24
Q

Describe the excretion of Finasteride (5ARI)

A

50% unchanged drug excreted in feces
Metabolites excreted in urine and feces

25
Q

Where is PDE5 enzyme highly expressed?

A

Highly expressed in the corpora cavernosa of the penis and its vasculature

Poorly expressed in the myocardium

Thus, has tissue specificity

26
Q

Describe the absorption profile of Sildenafil (PDE5i)

A

Well absorbed orally 50mg daily

*Lower initial starting dose required for pt with renal failure, elderly >= 65yo, those taking alpha blockers, and those taking CYP3A4 inhibitors

27
Q

Describe the distribution profile of Sildenafil (PDE5i)

A

Widely distributed, but can concentrate highly in penis

28
Q

Describe the metabolism of Sildenafil (PDE5i)

A

CYP3A4 - major (*require lower dose with concurrent CYP3A4 inhibitor)
CYP2C9 - minor

29
Q

Describe the excretion of Sildenafil (PDE5i)

A

Metabolites excreted in feces

3152 Reprod Health (7 decks)

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