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Pharm final > Androgens > Flashcards

Androgens Flashcards

1
Q

What are the Major categories of natural sex steroids:

A
  1. Estradiol (Estrogens)
  2. Progesterone
  3. Androgens
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2
Q

tx for 17a-hydroxylase def.

A

Estrogens, anti-HTN

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3
Q

tx. for 21-hydroxylase def

A

fluids + salt repletion and administer cortisol to lower ACTH.

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4
Q

tx. for 11B-hydroxylase def

A

estrogens and anti-HTN

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5
Q

What type of drugs are antiestrogens

A 
Receptor antagonists
- selective estrogen receptor antagonists
- Full antagonists (Fulvestrant)
aromatase inhibitors
GnRH agonists
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6
Q

Estrogens

PK

A

“EEEEDMC”

  1. Ethinyl estradiol
  2. Conjugated estrogen
  3. Mestranol
  4. Diethylstilbestrol
  5. Estradiol
  6. Estrone
  7. Estriol

•Available for oral, intramuscular, transdermal and topical administration.

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7
Q

Estrogens

PD

A

•Metabolism of estrogens relies on cytochrome P-450 system; they have enterohepatic circulation. Combination with P-450 inducers can lead to failure of contraceptive effectiveness.

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8
Q

•Diethylstilbestrol (DES) AE

A

–a nonsteroidal estrogen agonist used in pregnancy results in female child to infertility, vaginal cancer.

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9
Q

Absolute contraindications of estrogen use

A
  1. History of thromboembolism
  2. Breast & endometrial cancer
  3. Pregnancy
  4. Liver disease
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10
Q

Selective Estrogen Receptors Modulators –SERMs

A

•Mixed mechanism of actions: They exhibit agonistic action in some tissue and antagonists in other tissues.
•Tamoxifen: E-receptor antagonist effect on breast tissue but agonistic effect on liver, bone and partial agonist endometrium.
•Used in treatment of breast cancer & prophylaxis for high risk patients.
•Adverse effects:
–Hot flushes (Antagonist) and thrombosis (Agonistic)
–Risk of endometrial cancers

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11
Q

SERMs

A

•Toremifene (SERM): approved for treatment of breast cancer and prevention of breast cancer in high-risk women
•Raloxifene: E-receptor antagonist at breast and but agonist at bone. No estrogenic effect on endometrium
•No increased risk of endometrial cancer
•Uses:
–Prophylaxis against breast cancers (in high risk patients)
–Prevention of postmenopausal osteoporosis

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12
Q

Estrogen receptor antagonist in all tissues
•Fulvestrant: I.M.
AE

A
  • Used in the treatment breast cancer in tamoxifen resistant patients.
  • A.E: Hot flushes, injection site reactions & headache
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13
Q

Aromatase inhibitors
Administration
AE

A

•Inhibits conversion of androgens to estrogen
Letrozole
Anastrozole
Exemestane –an irreversible aromatase inhibitor
•Used in treatment of breast cancer (estrogen dependent) as 2nd line drugs following tamoxifen resistant.
•Oral administration
•A.E: hot flushes, decreased bone mineral density.

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14
Q

What is clomiphene

MOA

A

A fertility drug
Acts as estrogen antagonist in hypothalamus and anterior pituitary

•Used in treatment of anovulatory infertility

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15
Q

Clomiphene

Side effects

A

–Ovarian hyper-stimulation leading to enlargement of ovary.
–Multiple pregnancy 10%
–Hot flushes, nausea, vomiting, breast tenderness and weight gain.

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16
Q

Progestins

admin:

A 
"N3P D2M"
•Progesterone
•Medroxyprogesterone
•Norgestrel
•Norethindrone
•Norgestimate
•Desogestrel
•Drospirenone

ADMINISTRATION: Oral or I.M. injection

17
Q

ANTINPROGESTIN
admin
MOA
AE

A

MIFEPRISTONE - therapeutic abortificient
oral
•Competitive inhibitor of progesterone & glucocorticoid receptors.
•Controversial “morning after” drug used as an abortifacient.
•It is given concomitantly with PG-E or PG-F to increase myometrial contraction.
•Adverse effects: Excessive bleeding, gastrointestinal effects as nausea, vomiting, anorexia and abdominal pain.
44

18
Q

PROGESTERONE –Preps

A

Medroxyprogesterone, Norgestrel, Norethindrone, Norgestimate, Desogestrel –newer preps lacking of androgenic and antiestrogenic effects.

Drospirenone –a spironolactone derivative used as O.C. antagonize aldosterone effects useful in acne in females.

19
Q

Progestins AE

A

Long term use may result in

  1. Weight gain
  2. Glucose intolerance
  3. Androgenic –hirsutism & acne
  4. Anti-estrogenic (blocks lipid changes)
  5. Depression,
  6. Edema, acne
  7. increase HDL, decrease LDL & hypertension
20
Q

Synthetic androgens –17alkyl derivatives with increased anabolic effects:

A 
"Oxan, Stan, Nan, Dan, are hairy MOFs"
•Oxandrolone
•Methyltestosterone
•Stanozolol
•Fluoxymesterone
•Nandrolone
•Oxymetholone
•Danazol
21
Q

Antiandrogens

A

Receptor antagonist - Flutamide
5a-reductase inhibitor - Finasteride
Synthesis inhibitors - Ketoconazole
GnRH Agonists

22
Q

Androgens clinical uses

A
  • Substitution therapy in hypogonadism;
  • Increases bone density (prevent osteoporosis), could be used in increasing muscle mass (+ve nitrogen balance)
  • Some cases of aplastic anemia.
  • Administration: Transdermal, buccal, subcutaneous implant and I.M.
23
Q

Androgens AE

A

•Adverse effects:
–Over-masculinization
–In women could lead to hirsutism, suppression of menses, acne, and clitoral enlargement.
–hepatic adenomas & prostatic hypertrophy
–Cholestatic jaundice (elevated serum transaminations)
–Aggression & dependency
–Premature closure of epiphysis
–Illicit use in athletics
•Over-dosage of androgen can result in feminization (gynecomastia, testicular shrinkage, infertility, azoospermia) as a result of feedback inhibition (HPG axis) & conversion of exogenous testosterone into estrogen.

24
Q

Danazol MOA

AE

A
  • Danazol is an inhibitor of P450 in gonadal steroid synthesis.
  • It an androgen derivative, a partial agonist of progestin, and glucocorticoid receptors.
  • Used in endometriosis and fibrocystic disease of breast.

•AE: hepatitis –abnormal liver function tests and drug interaction due to P-450 inhibition.
55
It is a modified testosterone shows some signs of musculinising effects – acne, hirsutism, menstrual disturbances.

25
Q

•Androgen Receptor Antagonists:

A
  • Flutamide
  • Bicalutamide
  • Nilutamide
  • Cyproterone
  • Spironolactone
  • Ketoconazole
26
Q

Androgen receptor blockers –used for androgen-receptor-positive cancers.

A

Flutamide –a substituted anilide.
Bicalutamide
Nilutamide

•Primarily used in conjunction with GnRH analogs e.g., leuprolide (to ↓initial tumor flare-ups of prostate carcinoma).

27
Q

Other drugs with antiandrogen action

A
  • Spiranolactone: blocks aldosterone and competes androgen receptors. It is used in hirsutism.
  • Cyproterone: it has progesteronal effect suppresses LH & FSH. Used in hirsutism and to ↓excessive sexual drive in men
28
Q

Ketoconazole
admin
use
AE

A

oral administration
•Adrenal and gonadal steroid synthesis inhibitor
•Use: in prostate cancer but not 1st line drug.
•AE: May have drug interactions with other steroids due to P-450↓

29
Q 
5-α reductase inhibitor
Drug
Admin
USE
AE
A
  • Finasteride (PROPECIA):
  • Oral administration
  • Inhibit conversion of testosterone to dihydrotestosterone.
  • Use: BPH and promotes hair growth.
  • AE: gynecomastia, teratogenicity and impotence

Pharm final (19 decks)

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