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Pharmacology MBBS > Growth hormone, reproductive hormone > Flashcards

Growth hormone, reproductive hormone Flashcards

1
Q

GHRH analogues

A
  1. Sermorelin
  2. Macimorelin
  3. Tesamorelin
    Used:
  4. Diagnosis of cause of dwarfism:
    After sermorelin administration, if GH 🔼 ➡️ hypothalamic dwarfism otherwise pituitary dwarfism
  5. In patients of AIDS associated lipodystrophy
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2
Q

GH analogues

Examples and mnemonic

A 
Somatrem and Somatropin
 Small Children:
Small uses
Child S/E
ren CI
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3
Q

GH analogue uses

A 
S. Small for gestation baby
M. Malabsorption in short bowel syndrome
A. AIDS related wasting
LL. 🔽 length, dwarfism 
 Eg., Turner syndrome, Prader Willi syndrome, Noonan syndrome
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4
Q

GH analogues

side effects and contraindications

A 
S/E:
C. Carpel tunnel syndrome
H. Hyperglycemia
I. 🔼 Intracranial pressure
L. Leukemia
D. DM
CI:
RE. Retinopathy (🔼 vascularity)
N. Neoplasia
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5
Q

IGF-1 analogues

A 
Mecasermin & Mecasermin rinfabate (bound to IGF BP-3)
Rx of dwarfisms due to:
1. 🔽 IGF-1
2. GH-R mutation
3. Anti GH antibodies
S/E:
1. Hypoglycemia (unlike others)
2. Lipohypertrophy
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6
Q

Somatostatin analogues

examples and effects

A
  1. Octreotide: most useful
  2. Lanreotide
  3. Paseriotide
    Effects: 🔽 TSH & GH
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7
Q

Somatostatin analogues

Uses

A 
1. Octreotide is DoC for:
• Secretory diarrhea
• Glucagonoma, VIPoma, 
somatostatinoma, GRFoma
• Acute variceal bleeding
2. Radio-labeled octreotide: diagnosis of pituitary adenoma, carcinoid tumour
3. Vasoconstrictor to 🔽 bleeding. Eg., pancreatic surgery
4. Acromegaly (DoC is cabergoline)
5. Thyrotroph adenoma
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8
Q

Somatostatin analogues

side effects

A
  1. Hypothyroidism
  2. 🔽 gall bladder contraction ➡️ cholelithiasis (like estrogen)
  3. M/C: 🤢, 🤮
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9
Q

GH receptor antagonist

A

Pegvisomant
Use: resistant hypertrophy
S/E:
Pituitary adenoma ➡️ regular visual field examinations to be done

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10
Q

Gonadorelin

A

GnRH analogue
🔼 LH / FSH
Uses:
1. Anovulation
2. Diagnosis of hypogonadotropic hypogonadism:
After giving gonadorelin, if LH/FSH 🔼, defect in hypothalamus
S/E: multiple gestation (🔽 risk than GnRH agonists)

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11
Q

Examples of GnRH agonists

A
  1. Goserelin
  2. Buserelin
  3. Nafarelin
  4. Histrelin
  5. Triptorelin
  6. Leuprolide
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12
Q

GnRH agonists with intermittent dosing

effects, uses

A 
Pulsatile release & 🔼 LH/FSH
Uses:
1. Anovulation or Oligospermia
2. Delayed puberty 
3. Sexual infantilism
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13
Q

GnRH agonists with continuous dosing

effects

A

In the beginning: 🔼 LH/FSH (initial worsening of symptoms) ➡️
Continuous stimulation downregulates receptor ➡️
🔽 LH/ FSH

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14
Q

GnRH agonists with continuous dosing

uses

A 
In 👱🏽‍♀️:
1. Estrogen receptor +ve breast cancer
2. Fibroids 
3. Endometriosis
In👨‍🦰:
1. Prostate cancer
 DoC: goserelin
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15
Q

GnRH agonists with intermittent dosing

Side effects

A 
S/E:
1. Multiple gestation
2. Ovarian cyst
3. Ovarian cancer
CI: 🤰
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16
Q

GnRH antagonists &
GnRH agonists with continuous dosing
side effects

A 
In 👨‍🦰:
1. Impotence
2. Gynecomastia
3. Osteoporosis
In 👱🏽‍♀️: due to 🔽 estrogen
1. Hot flashes
2. Vaginal atrophy
3. Osteoporosis
CI: 🤰
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17
Q

GnRH antagonists

effects and examples

A 
🔽 LH/FSH
1. Granirelix 👵🏽
2. Abarelix
3. Cetrorelix: fibroids 
4. Dagarelix: prostate cancer
5. Elagolix (recent and different): endometriosis
CI: 🤰
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18
Q

GnRH antagonists

uses

A
  1. To prevent premature ovulation with ovarian stimulation protocol
  2. Cetrorelix: endometriosis, fibroids
  3. Dagarelix: prostate cancer
  4. Elagolix: endometriosis
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19
Q

Estradiol

A

• Metabolised in liver to estrone & estriol (can be synthesized by peripheral tissues)
• Cannot be used for therapeutic purpose due to high 1st pass metabolism and poor oral absorption
📝: estrogen 🔽LDL/🔼HDL but does not 🔽 cardiovascular related ☠️

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20
Q

Synthetic estrogen

A 
1. Ethinyl estradiol: M/C
 🔼 oral bioavailability
2. Mestronol:
 Activated in liver to ethyl estradiol 
3. Stilbesterol:
 S/E: 🔼 risk of vaginal cancer in offspring ➡️ not used
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21
Q

Estrogen uses

A
  1. Combined OCP
  2. Hormone Replacement Therapy GRT:
    • 1° ovary failure. Eg., Turner’s syndrome
    • post menopausal symptoms:
    a) 🔽 vasomotor symptoms:
    Main aim of HRT (hot flushes)
    b) Vaginal dryness
  3. Post menopausal osteoporosis:
    prophylaxis and Rx
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22
Q

Estrogen

side effects

A
  1. Uterine bleeding
  2. Gall stones (like somatostatin analogues)
  3. 🤢, 🤮
  4. 🔼 coagulation factors ➡️ thrombosis and DVT
  5. Na+/H2O retention ➡️ edema
  6. Worsens bp and migraine
  7. 🔼 risk of uterine cancer but 🔽 risk of colon cancer, ovarian cancer
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23
Q

Progesterone types

A 
1. Progesterone derivatives:
 Poor inhibitors of ovulation
2. Testosterone derivatives
3. Spironolactone derivatives
Both are potent inhibitors of ovulation
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24
Q

Progesterone derivatives

uses

A
  1. HRT
  2. Premenstrual syndrome
  3. Threatened abortion
  4. Diagnosis of estrogen secretion:
    Progesterone given for 5-7 days, then stopped: if bleeding +ve then estrogen +ve
  5. Good effect on uterus:
    Endometriosis, DUB, endometrial cancer
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25
Q

Progesterone side effects

A

A. Acne, Atherogenesis (due to androgenic effect seen with estranes)
B. Breakthrough bleeding, Breast engorgement
C. Cycle irregularities
D. Depression, Decreased libido
E. Edema with spironolactone derivatives

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26
Q

Combined OCPs

composition, uses

A 
Estrogen 30-50 mcg & progesterone 0.5-1 mg
One pill for 21 days & 7 pill free days
Other uses:
1. Polycystic Ovarian syndrome 
2. Menorrhagia
3. Fibroids
4. Ovarian cyst
S/E: same as the hormones
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27
Q

Minipills or progesterone only pills

A 
Norethindrone or Norgestrel
Use: if estrogen is CI
Mechanism: 🔼 thickening of cervical mucus ➡️🔽 penetration of sperms
(Block implantation of blastocyst)
S/E:
 Similar to progesterone
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28
Q

Emergency contraception

A
  1. Levonorgestrel: most preferred tablet
    0.75 mg of 2 tablets 12 hr apart within 72 hr, OR
    1.5 mg 1 tablets within 72 hr
  2. Ulipristal:
    30 mg within 5 days of unprotected intercourse
  3. Mifepristone:
    600 mg within 72 hr
  4. Yuzpee regimen: not preferred
    Estrogen + progesterone
  5. IUCD: within 5 days
    Best method
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29
Q

Depot or implantable contraceptives

A 
1. Levonorgestrel:
 6 capsules 36 mg reach
 sc implant for 5 years
2. Depot medroxyprogesterone acetate:
 IM 150 mg for 3 months
30
Q

Selective estrogen receptor modulators

A
  1. Tamoxifen
  2. Raloxifene
  3. Ospemifene: post menopausal dyspareunia
  4. Toremifene: tamoxifen resistant ER +ve breast cancer
31
Q

Tamoxifen

Effects

A
  1. Breast: antagonist
  2. Uterus: AGONIST
    🔼 risk of uterus cancer
  3. Bone: agonist
    🔽 bone resorption
  4. Lipids: agonist
    🔽 LDL
  5. Coagulation: agonist
    🔼 thrombosis
  6. Hot flushes: 🔼
32
Q

Raloxifen

effects

A 
1. Breast: antagonist
 prophylaxis
2. Uterus: antagonist
 protective 
3. Bone: agonist
 Rx
4. Lipids: agonist
 🔽 LDL
5. Coagulation: agonist
 🔼 thrombosis
6. Hot flushes: 🔼
33
Q

Tamoxifen

uses

A
  1. DoC in ER +ve breast cancer in pre-menopausal females
    Dose: 20 mg OD * 5 years
  2. Acromegaly by 🔽 IGF-1
  3. DoC in Riedel’s thyroiditis
34
Q

Raloxifen uses

A
  1. Prophylaxis of ER +ve breast cancer in post menopausal females
    Dose: 60 mg OD x 5 years
  2. Post menopausal osteoporosis
35
Q

Selective estrogen receptor downregulator

examples and uses

A
  1. Fluvestant:
    DoC in tamoxifen resistant ER+ve breast cancer
  2. Clomiphene:
    Infertility like anovulation and oligospermia
36
Q

Fluvestant

A

Mechanism: 🅱️ ER on breast
100 times more potent than tamoxifen but safer
Use: DoC in tamoxifen resistant ER+ve breast cancer
Dose: 250 mg sc once/month

37
Q

Clomifene

A

Mechanism: partial agonist at pituitary ER ➡️ 🔼GnRH ➡️ 🔼LH ➡️
Uses: anovulation & oligospermia (infertility)
S/E:
1. Multiple gestation (🔽 risk than GnRH agonist)
2. Ovary cyst
3. Ovarian cancer

38
Q

Mifepristone

mechanism and effects

A

Aka RU-486
Mechanism:
Partial agonist/antagonists at progesterone receptor
Effects:
1. Decidual breakdown: blocks blastocyst implantation
2. Softening of cervix
3. 🔼 PG synthesis: 🔼 uterine contraction

39
Q

Mifepristone

uses

A
  1. Medical abortion
  2. Surgical abortion: for cervical ripening
  3. Induction of labor
  4. Emergency contraception:
    600 mg within 72 hr
  5. Regular contraception: 200 mg once a month
  6. Blocks glucocorticoid receptor in Cushing disease
40
Q

Mifepristone used as medical abortion

A

600 mg of mifepristone

After 48 hr, 400 mcg of oral misoprostol or 1 mg of gemeprost pessary

41
Q

Mifepristone

side effects

A
  1. Vaginal bleeding: M/C

2. 🔼 PG: diarrhea, abdominal cramps

42
Q

Ulipristal

A

Mechanism:
partial agonist of pituitary ➡️🔽GnRH ➡️🔽 blocks ovulation
Use: emergency contraception: 30 mg within 5 days
S/E: headache and abdominal pain

43
Q

Natural testosterone

oral route

A

Has good oral absorption but high 1st pass metabolism

So cannot be used by oral route

44
Q

Alkylated testosterone

A 
Do not undergo 1st pass metabolism
Can be used orally
Eg., 
1. Methyltestosterone
2. Fluoxymesterone
3. Oxandrolone
4. Danazol
5. Stanozolol
45
Q

Alkylated testosterone

side effects

A
  1. Hepatotoxic: cholestatic jaundice
  2. HCC
  3. 🔽 HDL ➡️ atherogenesis
46
Q

Natural testosterone + esters

A 
🔼 lipid solubility ➡️ injected with oil 
Depot, when IM
Eg., 
1. Ethanate, cypionate: once a week
2. Undecanoate: once in 10 weeks
47
Q

Routes of administration of natural testosterone

A
  1. Gel
  2. Transdermal patch
  3. Buccal tablets
48
Q

Testosterone uses

A
  1. Male hypogonadism
  2. Female hypogonadism to 🔼 libido
  3. Athletes: steroid abuse
    • nandrolone decanoate: max anabolic effect
    • THG - tetrahydrogestrinone
  4. Resistant anemia: aplastic, sickle cell
  5. Prophylaxis of hereditary angioedema:
    Preferred drug: alkylated testosterone
    DoC: Danazol
49
Q

Testosterone common side effects of both genders

A 
1. Alkylated testosterone:
 Hepatotoxic, HCC, 🔽 HDL
2. Acne
3. Na+/H2O retention ➡️ edema
4. Precocious puberty
5. Stunting growth: premature closure of epiphysis
50
Q

Testosterone

side effects specific to males

A
  1. Benign prostatic hyperplasia BPH
  2. Prostate cancer
  3. Gynecomastia
  4. Oligozoospermia
51
Q

Testosterone

side effects specific to females

A
  1. Voice deepening
  2. 🔽 breast size
  3. Hirsutism
52
Q

Danazol

A 
Androgenic and progestational effects
🔽 GnRH ➡️ 🔽LH ➡️ 🔽 estrogen
Uses: 
1. Endometriosis
2. Fibrocystic disease of breast
3. 🔽 C1 esterase ➡️ DoC for prophylaxis of hereditary angioedema
53
Q

Anti-androgens or impeded androgens

examples

A
  1. Androgen receptor antagonists:
    a) progesterone derivatives
    b) synthetic: apa-lutamide, bica-lutamide, dora-lutamide 🧒🏻
  2. 5-α reductase inhibitor:
    • Finasteride
    • Dutasteride
54
Q

Androgen receptor antagonists

Progesterone derivatives

A

Older drugs
Less commonly used
1. Cyproterone: hepatotoxic
2. Megestrol

55
Q

Androgen receptor antagonists

Synthetic

A
  1. Bicalutamide
  2. Flutamide: hepatotoxic
  3. Enzalutamide: E Epilepsy
  4. Apalutamide
  5. Nilutamide: interstitial pneumonitis
  6. Doralutamide
56
Q

Androgen receptor antagonists

Uses

A
  1. Prostate cancer along with GnRH agonists

2. Hirsutism

57
Q

Androgen receptor antagonists

Side effects

A
  1. Impotence, gynecomastia: common
  2. Hepatotoxic: flutamide, cyproterone
  3. Epilepsy: enzalutamide
  4. Nilutamide: interstitial pneumonitis
58
Q

5-α reductase inhibitor

A

Testosterone is converted by the enzyme to DHT

  1. Finasteride: 🅱️ 5-α reductase II
  2. Dutasteride: 🅱️ 5-α reductase I, II
59
Q

5-α reductase inhibitors
uses
side effects

A
  1. DoC in androgenic alopecia
  2. BPH by inhibiting smooth muscle proliferation ➡️ 🔽size of prostate ➡️ 🔼 urine flow
  3. Hirsutism
    S/E:
    Impotence and gynecomastia, less than androgen receptor antagonist
60
Q

Drugs used for erectile dysfunction with mnemonic

A 
Pyar: Phentolamine 
Bi: Bremelanotide
Nahi: Naltrexone 
Kar: Ketanserin 
S. Sildenafil
A. Alprostadil 
K. 
T. Trazadone 
A. AlVIPtadil
61
Q

Drugs used for erectile dysfunction

with their class

A 
Phentolamine: α 🅱️
Bremelanotide: MCP agonist
Naltrexone: opioid 🅱️
Ketanserin: 5HT2 🅱️
Sildenafil: phosphodiesterase-5 🅱️
Alprostadil: PG-E1 analogue
K. 
Trazadone: 5HT2 🅱️
 S/E: priapism 
AlVIPtadil: VIP analogue
62
Q

Melanocortin peptide

A 
1. α-MSH:
 Binds to MC1R ➡️ pigmentation
2. ACTH: 
Binds to MC2R ➡️ steroid synthesis
3. Miscellaneous:
 MC3/4/5R ➡️ central sexual arousal
63
Q

Bremelanotide

A

Non-selective MCP-R agonist
In the beginning as tanning cream, not used now due to central sexual arousal effect
Now used for HSDD in 👱🏽‍♀️
SC route 45 min before expected intercourse

64
Q

Afamelanotide

A

Approved by FDA in 2019
α-MSH analogue ➡️🔼MC1R ➡️🔼 pigmentation
Use: in erythropoietic proteins to 🔼 pain -free sunlight exposure
SC implant above anterior ASIS

65
Q

Termination of pregnancy is advised in case of conception in a patient taking a hormonal
contraceptive

A

If pregnancy occurs during use of hormonal contraceptives—it should be terminated by suction-
aspiration, because the risk of malformations, genital carcinoma in female offspring and
undescended testes in male offspring is increased.

66
Q

Progesterone can cause increased aldosterone levels.

A

Progesterone competes with mineralocorticoid receptor in the renal tubule and result in decreased
reabsorption of Na+. This result in an increased secretion of aldosterone from the adrenal cortex

67
Q

Cyproterone acetate is a better anti androgen than cyproterone.

A

Both cyproterone and cyproterone acetate inhibit the action of androgens in the target organ, but
the acetate form has an additional progestational activity. This will suppress LH (Luteinizing
hormone) and FSH (Follicle stimulating hormone) secretion and thereby decrease the production
of androgens, so theanti androgenic effect is greater.

68
Q

Stanozolol is used for increasing body mass, strength and physical performance

A

Stanozolol is an anabolic steroid which has a higher anabolic activity than androgenic activity.
Thus it increases the muscle mass and strength. Such drugs are screened as a part of dope testing

69
Q

Methylergometrine is preferred over ergometrine in obstetrics

A

Ergometrine has very weak agonistic and practically no antagonistic action on α adrenergic
receptors: vasoconstriction is not significant. Partial agonistic action on 5-HT receptors has been
demonstrated in uterus, placental and umbilical blood vessels and in certain brain areas. However
Methylergometrine is 1½ times more potent than ergometrine on the uterus, but other actions are
less marked. It has thus replaced ergometrine at many obstetric units

70
Q

Tocolytics are combined with corticosteroids

A

Tocolytics are used in suppression of premature labor to allow the fetus to mature, to allow time for
initiating glucocorticoid therapy for fetal lung maturation or to transfer the mother in labor to a
center with proper facilities.

71
Q

Tocolytics are contraindicated in some situations.

A

An attempt to delay premature labor is likely to succeed only if cervical dilatation is < 4 cm and
‘taking up’ of lower segment is minimal. Measures to delay labor should not be undertaken if membranes have ruptured, antepartum hemorrhage is occurring, in severe toxemia of pregnancy, intrauterine infection or fetal death.In such cases, immediate delivery of the fetus should be
performed

Pharmacology MBBS (19 decks)

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