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Pharm final > GONADAL HORMONES > Flashcards

GONADAL HORMONES Flashcards

1
Q

17 α-hydroxylase deficiency

A

leads to ↓sex hormones and cortisol and ↑ in mineralocorticoids.

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2
Q

Patients presents with ↑BP,↓K+
 XY: ↓DHT may show cryptorchidism and indistinct genitalia.
Rx: androgens, glucocorticoids and Anti-hypertensives
XX outwardly Phenotypic female with normal internal sex organs but lack 20 sexual characteristics. Rx: Estrogens, anti-HTN

A

17 α-hydroxylase deficiency

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3
Q

21-hydroxylase deficiency

A

↑ sex hormones and ↓ cortisol and in mineralocorticoids.

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4
Q

Presents with ↓BP; ↑K+;↑renin activity and volume depletion.
Over masculinization – pseudohermaphroditism in females.
 Rx: fluids + salt repletion & administer cortisol to ↓ACTH

A

21-hydroxylase deficiency

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5
Q

11β-hydroxylase deficiency

A

leads to ↑ sex hormones and ↓ cortisol and in mineralocorticoid (aldosterone) but ↑11-deoxycorticosterone.

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6
Q

Patients present with ↑BP due to ↑mineralocorticoid 11-deoxycorticosterone
Over masculinization. Rx: estrogens, anti-HTN

A

11β-hydroxylase deficiency

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7
Q

WHICH ESTROGEN IS THE MOST POTENT

A

Estradiol is more potent than Estrone and Estriol

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8
Q

Important physiological effects of estrogens on:

- Pro-coagulation state

A

–Increases factor II, VII, IX, X and XII in higher doses

–Decreases antithrombin III, protein C and S

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9
Q

Important physiological effects of estrogens on:

- Lipid profile

A

•Favorable Lipid profile
–Increase HDL
–Decrease LDL

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10
Q

Important physiological effects of estrogens on:
HORMONE LEVELS
AND CHOLESTEROL

A

•Effect on hormone levels
–Increases the transport protein level of various hormones (cortisol, thyroxine, sex steroids)
–free hormone level is unaffected
•Increase cholesterol in bile –formation of gall stone

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11
Q

Estrogens NAMES

A
  1. Ethinyl estradiol
  2. Conjugated estrogen
  3. Mestranol
  4. Diethylstilbestrol
  5. Estradiol
  6. Estrone
  7. Estriol
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12
Q

a prodrug is converted into Ethinyl estradiol, present in some contraceptives. ↑bio-availability, ↑half-life and ↓FSH & LH via feed-back

A

MESTRANOL

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13
Q

ESTORGENS METANOLIZED BY?

A

P450

Combination with P-450 inducers can lead to failure of contraceptive effectiveness.

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14
Q

what kind of estrogens are used in females with hypogondadism?

A

I.M. Long acting estrogen preparations

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15
Q

Estrogens AE

A
  • Increased incidence of thromboembolism.
  • Increased incidence of breast cancers
  • Endometrial hyperplasia & cancers (unless progestin is added).
  • Migraine, Cholestasis, and mood changes.
  • Nausea, breast tenderness and bloating
  • Diethylstilbestrol (DES) –a nonsteroidal estrogen agonist use in pregnancy results in female child to infertility, vaginal cancer
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16
Q

SERMs

A

Tamoxifen
Toremifene
Raloxifene
- Mixed mechanism of actions: They exhibit agonistic action in some tissue and antagonists in other tissues.

17
Q

•Fulvestrant:
PK
USE
AE

A

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

18
Q

Aromatase inhibitors
Drug names?
PK
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.

19
Q

Clomiphene?
PK
AE

A

Fertility drug - used in anovulatory infertility

  • Acts as estrogen antagonist in hypothalamus and anterior pituitary
  • prevents feedback inhibition of GnRH release by hypothalamus

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

20
Q

Progestins

A
  • Progesterone
  • Medroxyprogesterone
  • Norgestrel
  • Norethindrone
  • Norgestimate
  • Desogestrel
  • Drospirenone
21
Q

Antiprogestin

A

Mifepristone

- therapeutic abortificient

22
Q

PROGESTERONE - Preps:

Medroxyprogesterone, Norgestrel, Norethindrone, Norgestimate, Desogestrel

A

–newer preps lacking of androgenic and antiestrogenic effects.

23
Q

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

A

Drospirenone

24
Q

Progestins –Adverse effects

Long term use may result in:

A
  1. Weight gain
  2. Glucose intolerance
  3. Androgenic –hirsutism & acne
  4. Anti-estrogenic (blocks lipid changes)
  5. Depression,
  6. Edema, acne
  7. increased HDL, decreased LDL & hypertension
25
Q 
Antiprogestins
- RU 486 or Mifepristone
PD
PK
AE
A

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.

26
Q

ANDROGENS

A 
•Testosterone –natural
Synthetic androgens –17alkyl derivatives with increased anabolic effects:
•Oxandrolone
•Methyltestosterone
•Stanozolol
•Fluoxymesterone
•Nandrolone
•Oxymetholone
•Danazol
27
Q

Antiandrogens

MOA and drug name?

A 
Receptor Antagonist:
- Flutamide
5-α-Reductase Inhibitor:
- Finasteride
Synthesis Inhibitors:
- Ketoconazole
•Bicalutamide
•Nilutamide
•Cyproterone
•Spironolactone
GnRH Agonists
28
Q

GnRH inhibitors?

A

Degarelix
Abarelix
(remember same as Ganirelix and cetrorelix)

29
Q

Androgen overdose can result in?

A

feminization (gynecomastia, testicular shrinkage, infertility, azoospermia) as a result of feedback inhibition (HPG axis) & conversion of exogenous testosterone into estrogen.

30
Q

Danazol
MOA
USE
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.
It is a modified testosterone shows some signs of musculinising effects – acne, hirsutism, menstrual disturbances.

31
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).

32
Q

Spiranolactone: MOA

USE?

A

blocks aldosterone and competes androgen receptors. It is used in hirsutism.

33
Q

Cyproterone:
MOA
USE

A

it has progesteronal effect suppresses LH & FSH. Used in hirsutism and to ↓excessive sexual drive in men

34
Q

Ketoconazole
PK
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↓

35
Q

5-α reductase inhibitor

  • name drug
  • PK
  • MOA
  • 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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