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Endocrine and Reproductive


Pharmacology
Shan Nanji

Endocrine Pharmacology
nPropylthiouracil,

Methimazole

MOA:
n Blocks __________________
n Blocks __________________
n S/E:
n

n
n

Skin Rash

__________________
Hepatotoxicity associated with __________________

n Clinical
n

Use:

Hyperthyroidism

Shan Nanji - NanjiMD@gmail.com

Endocrine Pharmacology
nLevothyroxine, Triiodothyronine

MOA:
n Thyroxine

Replacement

n S/E:

Tachycardia
n Heat Intolerance
n Tremors
n Arrhythmias
n

n Clinical Use:
n HypOthyroidism
n Myxedema
Shan Nanji - NanjiMD@gmail.com

Endocrine Pharmacology
nDemeclocycline

(+etracycline)

MOA:
n

__________________

nS/E:
n

__________________

n Photosensitivity
n Tooth

nClinical
n

and Bone Abnormalities

Use:

__________________

Shan Nanji - NanjiMD@gmail.com

Endocrine Pharmacology
n GH
n Clinical

Use:

GH Deficiency
n Turner Syndrome
n

n Somatostatin
n Clinical
n

n
n

(Octreotide)

Use:

Esophageal Varices

__________________
__________________

Gastrinoma
n Glucagonoma
n

Shan Nanji - NanjiMD@gmail.com

Endocrine Pharmacology
nOxytocin
n Clinical

Use:

n Stimulates

Labor
n Uterine Contractions
n Lactation
n

__________________

nADH

(desmopressin)

n Clinical
n

Use:
__________________

Shan Nanji - NanjiMD@gmail.com

Endocrine Pharmacology
n Leuprolide

MOA:
n

GnRH Analog
n

Agonist Properties if ________ Administration

n Clinical
n

Pulsatile Dose
n

Use:
__________________

Continuous Dose
n Prostate Cancer (Coadministered with Flutamide)
n Uterine Fibroids
n Precocious Puberty

Shan Nanji - NanjiMD@gmail.com

Endocrine Pharmacology
n Testosterone,

MOA:
n

Methyltestosterone

Androgen Receptor Agonist


n Inhibits LH -> Produce Less Testosterone

n S/E:

Masculinization (Females)
n Gonadal Atrophy
n Increase LDL
n Decrease HDL
n Early Epiphyseal Plate Closure
n

n Clinical

Use:

Hypogonadism
n Promote Anabolism in Burn Patients
n

Shan Nanji - NanjiMD@gmail.com

Endocrine: Antiandrogens
nFinasteride
n MOA: __________________-> Slow Conversion Testosterone to

DHT
n Clinical

Use: BPH and Male Pattern Baldness

nFlutamide
n MOA: __________________
n Clinical

Use: Prostate Carcinoma

Shan Nanji - NanjiMD@gmail.com

10

Endocrine: Antiandrogens
nKetoconazole
n MOA: Inhibits 17,20-Desmolase (Steroid Synthesis)
n Clinical

Use: __________________

nSpironolactone
n MOA: Inhibits Steroid Synthesis
n Clinical

Use:

nKetoconazole
n

__________________
and Spironolactone

Used in Polycystic Ovarian Syndrome


n Prevention of Hirsuitism

Shan Nanji - NanjiMD@gmail.com

11

Endocrine Pharmacology
nEstrogens: Ethinyl

Estradiol, DES, Mestranol

MOA:
n Bind

Estrogen Receptors

n Clinical

Use:

n Hypogonadism
n Ovarian

n
n

Failure

__________________
__________________

Shan Nanji - NanjiMD@gmail.com

12

Endocrine Pharmacology
nEstrogens: Ethinyl

Estradiol, DES, Mestranol

n S/E:
n Increase

Risk Endometrial Cancer


n Postmenopausal Bleeding
n

__________________

n Contraindicated

in:
n ER-Positive Breast Cancer
n

__________________

Shan Nanji - NanjiMD@gmail.com

13

Endocrine: SERMs
(Selective Estrogen Receptor Modulator)
nClomiphene
n MOA: Partial Estrogen Receptor Agonist
n S/E:
n

__________________

n Ovarian

__________________

n Clinical

Enlargement

Use:

__________________

n PCOS

Shan Nanji - NanjiMD@gmail.com

14

Endocrine: SERMs
(Selective Estrogen Receptor Modulator)
nTamoxifen, Raloxifen
n MOA:

Antagonist at Breast
n Agonist at Bones
n

n Clinical

Use:
n Prevention of Recurrent ER-Positive Breast Cancer
n

__________________

n RELAXifen

Carcinoma
Shan Nanji - NanjiMD@gmail.com

Dont Worry about Risks of Endometrial

15

Endocrine: Pharmacology
nAnastrozole/Exemestane
n MOA: Aromatase Inhibitor
n Clinical

Use:
n Postmenopausal Patient with Breast Cancer

Shan Nanji - NanjiMD@gmail.com

16

Endocrine: Pharmacology
nProgestins

MOA:
n

Bind Progesterone Receptors


n Increase __________________

n Clinical

n
n

Use:

__________________
__________________

n Abnormal

Shan Nanji - NanjiMD@gmail.com

Uterine Bleeding

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Endocrine: Pharmacology
nMifepristone

(aka RU-486)

MOA:
n Competitive

Inhibitor of Progestins
n At Progesterone Receptors

n S/E:
n

__________________

n GI

(Nausea, Vomiting, Anorexia)


n Abdominal Pain
n Clinical Use:
n Abortifacent
n Coadministered with __________________
Shan Nanji - NanjiMD@gmail.com

18

Endocrine: Pharmacology
nTerbutaline

MOA:
n 2-Agonist

__________________

n Clinical

Use:

n Reduce

Shan Nanji - NanjiMD@gmail.com

__________________

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Endocrine: Pharmacology
nTamsulosin

MOA:
n

__________________
n Inhibits

Smooth Muscle Contraction

n Clinical

Use:
n BPH
n Selective

1A,D Receptor

n Found
n TAMEsulosin
Shan Nanji - NanjiMD@gmail.com

in Prostate
-> Least Side Effects TAME

20

Endocrine: Pharmacology
nSildenaFIL,
MOA:
nInhibit

VardenaFIL

__________________

n Increase

in cGMP -> Vasodilation

n Clinical

Use:
n Erectile Dysfunction

n __________________
n

-> Help FILL the Corpus Cavernosum with Blood!

Shan Nanji - NanjiMD@gmail.com

21

Endocrine: Pharmacology
nSildenaFIL,
n S/E:

VardenaFIL

n Dyspepsia
n Headache
n Flushing
n Impaired

__________________Color Vision

n Severe

HypOtension
n In Patients Taking Nitrates Concurrently

n PDE5

n ->

Inhibitors

Help FILL the Corpus Cavernosum with Blood!

Shan Nanji - NanjiMD@gmail.com

22

Endocrine: Pharmacology
nDanazol
MOA:
Partial Agonist at Androgen Receptors
n (Synthetic Androgen)
n Clinical Use:
n

__________________
n __________________
n S/E:
n

Weight Gain
n Edema
n Hirsutism and Acne
n Decrease HDL
n Hepatotoxicity
n

Shan Nanji - NanjiMD@gmail.com

Gastrointestinal Hormones
Shan Nanji

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Endocrine: Pharmacology
nGastrin

(G-Cells)

ACTION:
n Increase Gastric H+ Secretion
n Increase Gastric Mucosa Growth
n Increase Gastric Motility
REGULATION:
n Increase by Stomach Distention/Alkilinity
n Decrease by pH < 1.5
ORIGIN:
n G-Cells in Stomach Antrum
Shan Nanji - NanjiMD@gmail.com

25

Endocrine: Pharmacology
n(CCK)Cholecystokinin

(I-Cells)

ACTION:
n Increase Pancreatic Secretion
n Increase Gallbladder Contraction
n Increase Sphincter of Oddi Relaxation
n Decrease Gastric Emptying
REGULATION:
n Increase by Fatty Acids
n Increase by Amino Acids
ORIGIN:
n I-Cells in Doudenum and Jejunum
Shan Nanji - NanjiMD@gmail.com

26

Endocrine: Pharmacology
nSecretin
ACTION:
n Increase Pancreatic HCO3 Secretion
n Increase Bile Secretion
n Decrease Gastric Acid Secretion
REGULATION:
n Increase by Acids
n Increase by Fatty Acids in Duodenum
ORIGIN:
n

S-Cells in Doudenum

Shan Nanji - NanjiMD@gmail.com

27

Endocrine: Pharmacology
nSomatostatin
ACTION:
n Decrease Gastric Acid and Pepsinogen Secretion
n Decrease Pancreatic and Small Intestine Fluid Secretion
n Decrease Gallbladder Contraction
n Decrease Insulin and Glucagon
REGULATION:
n Increase by Acids
n Decrease by Vagal Stimulation
ORIGIN:
n D-Cells in Pancreatic Islets and GI Mucosa
Shan Nanji - NanjiMD@gmail.com

28

Endocrine: Pharmacology
nGlucose-dependent

Insulinotropic Peptide (GIP)

ACTION:
n Exocrine:
n Decrease Gastric H+ Secretion
n Endocrine:
n Increase Insulin Release
REGULATION:
n Increase by Fatty Acids
n Increase by Amino Acids
n Increase by Oral Glucose
ORIGIN:
n K-Cells in Doudenum and Jejunum
Shan Nanji - NanjiMD@gmail.com

29

Endocrine: Pharmacology
nVasoactive

Intestinal Peptide (VIP)

ACTION:
n Increase Intestinal Water and Electrolyte Secretion
n Increase Relaxation of Intestinal Smooth Muscle and Sphincters
REGULATION:
n Increase by Distension
n Increase by Vagal Stimulation
n Decrease by Adrenergic Input
ORIGIN:
n Parasympathetic Ganglia in Sphincters, Gallbladder, and Small Intestine
Shan Nanji - NanjiMD@gmail.com

30

Endocrine: Pharmacology
nMotilin
ACTION:
n Produces Migrating Motor Complexes (MMC)
REGULATION:
n Increase During Fasting State
ORIGIN:
n Small Intestine

Shan Nanji - NanjiMD@gmail.com

31

Endocrine: Pharmacology
nIntrinsic

Factor

ACTION:
n Binds Vitamin B12
REGULATION:
ORIGIN:
n Parietal Cells in Stomach

Shan Nanji - NanjiMD@gmail.com

32

Endocrine: Pharmacology
nPepsin
ACTION:
n Decrease Stomach pH
REGULATION:
n Increase by Histamine, Ach, and Gastrin
n Decrease by Somatostatin, GIP, Prostaglandins, and Secretin
ORIGIN:
n Parietal Cells in Stomach

Shan Nanji - NanjiMD@gmail.com

33

Endocrine: Pharmacology
nGastric Acid
ACTION:
n Protein Digestion
REGULATION:
n Increase by Vagal Stimulation
n Increase by Acid
ORIGIN:
n Chief Cells in Stomach

Shan Nanji - NanjiMD@gmail.com

34

Endocrine: Pharmacology
nHCO3
ACTION:
n Neutralizes Acid
REGULATION:
n Increase by Pancreatic and Biliary Secretion with Secretin
ORIGIN:
n Mucosal Cells in Stomach, Doudenum, Salivary Glands, and Pancreas
n Brunners Glands in Doudenum

Shan Nanji - NanjiMD@gmail.com