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Step One > Pharm repro > Flashcards

Pharm repro Flashcards

1
Q

What is the mechanism of leuprolide? Clinical use? Toxicity?

A

GnRH analog with agonist properties when used in pulsatile fashion; antagonist when used in continuous fashion (decr. FSH/LH)

Infertitility (pulsatile)
Prostate cancer (following adrogen receptor blockade)
Uterine fibroids
Precocious puberty

Antiandrogen, N/V

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2
Q

What type of drugs are ethinyl estradiol, DES (2), and mestranol? Mechanism? Clinical use? Toxicity? Of 2? CIs?

A

Bind estrogen receptors

Hypogonadism or ovarian failure
Menstrual abnormalities
HRT in menopause
Androgen dependent prostate cancer

Incr. risk of endometrial cancer
bleeding in post meno women
1=clear cell adenoCA of vagina
Incr. risk of thrombi

CI=ER+ breast cancer, history of DVTs

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3
Q

What type of drug is clomiphene? Mechanism? Clinical use? Toxicity?

A

SERM

Antagonist at ER in hypothalamus
PRevents normal feedback inhibition leadin to incr. rlease of LH and FSH from pit, which stimulates ovulation

Infertility due to anovulation (PCOS)

Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

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4
Q

What type of drug is tamoxifen? Mechanism? clinical use? toxicity?

A

SERM

Antagonist at breast,
agonist at bone and uterus

Treat and prevent recurrence of ER/PR + breast cancer

Incr. risk of TE events and endometrial cancer

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5
Q

What type of drug is raloxifene? Mechanism? Clinical use? Toxicity?

A

SERM

Antag at breast, uterus
Agonist at bone

Osteoporosis

Incr. risk of TE events, but no incr. risk of endometrial cancer

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6
Q

What is the clinical use of HRT? What does it consist of? Toxicity?

A

Used for relief or prevention of menopausal symptoms (hot flashes, vaginal atrophy), osteoporosis (incr. estrogen, decr. osteoclast activity)

Progesterone is used to prevent endometrial cancer.

Possible CV risk.

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7
Q

What is the mechanism and clinical use of anastrozole and exemestane?

A

Aromatase inhibitors

Post meno women with ER+ breast cancer

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8
Q

What is the mechanism and clinical use of anastrozole and exemestane?

A

Aromatase inhibitors

Post meno women with ER+ breast cancer

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9
Q

What is the mechanism of progestins? Clinical use?

A

Bind progesterone receptors
Decr. growth and incr. vascularization of endometrium

OCPs and to treat endometrial cancer, abnormal uterine bleeding.

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10
Q

What is the mechanism of mifepristone (RU-486)? Clinical use? What is it administered with? Toxicity?

A

Competetive inh. of progestins at progesterone receptors.

Termination of pregnancy
Administered with misoprostol (PGE1)

Heavy bleeding, GI effects, abdom pain

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11
Q

What is the mechanism of oral contraceptives? CIs?

A

Estrogen and progestins inhibit LH/FSH and prevent estrogen surge.
No estrogen surge=no LH surge=no ovulation.
Progestins cause thickening of cervical mucus, thereby limiting access of sperm to uterus.
They also inhibit endometrial prolif making it less suitable for implantation.

Smokers > 35 (incr CV risk)
History of TE and stroke
History of estrogen dependent tumor

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12
Q

What is the mechanism of terbutaline and ritodrine? Clinical use?

A

Beta agonists that relax the uterus

Decr. contraction frequency in women during labor

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13
Q

What is the mechanism of danazol? Clinical use? Toxicity?

A

Synth androgen that acts as a partial agonist at androgen receptors

Endometriosis, hereditary andioedema

Weight gain, edema, acne, hirsutism, masculinization, decr. HDL levels, hepatotoxicity

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14
Q

What is the mechanism of testosterone and methyltestosterone? Clinical use? Toxicity?

A

Agonists at androgen receptors

Hypogonadism
Promotes development of secondary sex characteristsics
Stimulation of anabolism to promote recovery after burn or injury

Masculin. in females
Decr. intra testicular testosterone in males by inhibiting release of LH (gonadal atrophy)
Premature closure of epiphyseal plates
Incr. LDL, decr. HDL

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15
Q

What is the mechanism of finasteride? Uses?

A

5 alpha reductase inhibit.

BPH and male pattern baldness

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16
Q

What is the mechanism of flutamide? Uses?

A

a nonsteroidal competitive inhibitor at androgen receptors.

Prostate CA

17
Q

What is the mechanism of ketoconazole? Uses? Sx?

A

Inhibits steroid synth (17,20 desmolase)

PCOS (reduce androgenic symptoms)

gynecomastia and amenorrhea

18
Q

What is the mechanism of spironolactone? Uses? Sx?

A

Inhibits steroid binding, 17 alpha hydroxylase, and 17,20 desmolase

PCOS (reduce androgenic symptoms)

gynecomastia and amenorrhea

19
Q

What is the mechanism of tamsulosin? Clinical use?

A

alpha 1 antag used to treat BPH by inhibiting smooth muscle contraction.
Selective for alpha 1A,D receptors (on prostate) vs. alpha 1B receptors (vascular)

20
Q

What is the mechanism of tamsulosin? Clinical use?

A

alpha 1 antag used to treat BPH by inhibiting smooth muscle contraction.
Selective for alpha 1A,D receptors (on prostate) vs. alpha 1B receptors (vascular)

21
Q

What is the mechanism of sildenafil, vardenafil, and tadalafil? Clinical use? Toxicity?

A

Inhibit PDE-5 leading to incr. cGMP, smooth muscle relaxation in corpus cavernosum leadin to incr. blood flow, penile erection

Erective dysfunction

Headache, flushing, dyspepsia, cyanopsia
Risk of life threatening hypotension if taking nitrates.

22
Q

What is the mechanism of minoxidil? Clinical use?

A

Director arteriolar vasodilator

Androgenetic alopecia
Severe refractory hypertension.

23
Q

What drugs are P450 inducers?

A 
Chronic alcohol use
St. Johns wort
phenytoin
phenobarbital
nevirapine
rifampin
griseofulvin
carbamazepine

Chronic alcholics STeal Phen-Phen and NEVer RIfuse Greasy Carbs

24
Q

What are some P450 substrates?

A

Anti-epileptics
Theophylline
Warfarin
OCPs

Always Think When Outdoors

25
Q

What are some P450 inhibitors

A 
Acute Alcohol Abuse
Ritonavir
Amiodarone
Cimetidine
Ketoconazole
Sulfonamides
Isoniazid (INh)
Grapefruit juice
Quinidine
Macrolides (except azithro)

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