Men and Women Health Flashcards
What is the mode of action of tamsulosin?
Inhibits alpha 1 adrenergic receptors
Inhibit vasoconstriction by endogenous catecholamines
Decreases muscle tone and reduce bladder obstruction
Relax smooth muscle and improve urodynamic
Why is tamsulosin preferred to the other alpha adrenergic antagonist?
Increased selectivity towards alpha 1A receptors
Effects maintained during long term therapy
Delays the need for surgery and improve urinary flow rate
How is tamsulosin absorbed?
Orally
How is tamsulosin distributed?
High plasma protein binding
How is tamsulosin metabolized?
Through the liver by CYPs
What are significant DDI to consider for those on tamsulosin?
CYP450 inducers and inhibitors
Grapefruit juice
How is tamsulosin excreted?
Urine
What are some of the adverse effects of tamsulosin?
Abnormal ejaculation
Back pain
What is the mode of action of finasteride?
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
What are the adverse effects of finasteride?
Loss of libido and sexual potency
Gynecomastia
Who are contraindicated towards the use of finasteride?
Women, children
Those that are pregnant
What is the mode of action of sildenafil?
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
What is a clinical benefit of sildenafil?
Selective to cavernosa of penis but poorly to PDE5 in myocardium
How is sildenafil absorbed?
Orally
Does sildenafil require dose adjustment for renal and liver failure?
No
How is the distribution like for sildenafil?
Widely distributed
How is sildenafil metabolized? What enzymes are involved?
Liver
Major pathway: CYP3A4
Minor pathway: CYP2C9
How is sildenafil excreted?
Feces
What are some potential adverse effects of sildenafil?
Headache
Flushing
Dyspepsia
Dizziness
Back pain
Blurred vision
Priapism
What is a significant DDI to avoid with sildenafil and why?
GTN
Can potentiate vasodilation effect on GTN by increasing cGMP causing potential hypotension
What is the mode of action of ethinyl estradiol?
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
What are the indications for the use of ethinyl estradiol?
Menopause
Gynecological disorder
Hormone sensitive cancer
How is ethinyl estradiol absorbed?
Oral
How is ethinyl estradiol distributed?
High plasma protein binding
How is ethinyl estradiol metabolized and discuss the metabolic pathway
Enterohepatic circulation also occurs
Metabolized in the liver via Phase 1 hydroxylation
Phase 2 conjugation, glucuronidation and sulphation
Forms ethinylestradiol glucuronide and sulfate
How is ethinyl estradiol eliminated?
Faeces and urine
List some of the mild adverse effects of ethinyl estradiol
Breast tenderness
Headache
Fluid retention
Nausea
Dizziness
Weight gain
List some of the major adverse effects of ethinyl estradiol.
VTE
Breast cancer
Myocardial infarction
Liver damage
What are some contraindications to know of ethinyl estradiol? (HINT: Avoid in patients with…)
Known history or susceptibility to VTE
Advanced DM with vascular disease
Hypertension > 160/100
Breast feeding (<21 days post partum)
Breast cancer
What is the mode of action of norethindrone?
Synthetic progesterone inhibits LH release
Prevents ovulation by making endometrial unstable for implantation of ovum
What are some indications of norethindrone?
Endometriosis
Abnormal periods / bleeding
How is norethindrone absorbed?
Orally
How is norethindrone dsitributed?
High plasma protein binding
How is norethindrone metabolized?
Via the liver through Phase I reduction and Phase II glucuronidation and sulfation
How is norethindrone excreted?
Urine and feces
What are some adverse effects of norethindrone?
Headache, dizziness, bloating, weight gain, unpredictable spotting and bleeding, amenorrhea
What is one special advice to counsel patients who intent to start on norethindrone?
Not desirable for women planning a pregnancy after cessation as effect can last up to 1.5 years
