07 Endocrine & Reproductive

+Endocrine and Reproductive Pharmacology Shan Nanji

+Endocrine Pharmacology

nPropylthiouracil, Methimazole

MOA: nBlocks __________________ nBlocks __________________

nS/E: n Skin Rash

n __________________ n Hepatotoxicity associated with __________________

nClinical Use: n Hyperthyroidism

Shan Nanji - [email protected]

2


nLevothyroxine, Triiodothyronine MOA:

n Thyroxine Replacement nS/E:

n Tachycardia n Heat Intolerance n Tremors n Arrhythmias

nClinical Use: n HypOthyroidism n Myxedema


3


nDemeclocycline (+etracycline)

MOA: n __________________

nS/E: n __________________ n Photosensitivity n Tooth and Bone Abnormalities

nClinical Use: n __________________


4



5

nGH n Clinical Use:

n GH Deficiency n Turner Syndrome

nSomatostatin (Octreotide) n Clinical Use:

n Esophageal Varices n __________________ n __________________ n Gastrinoma n Glucagonoma



6

nOxytocin nClinical Use:

n Stimulates Labor n Uterine Contractions n Lactation

n __________________

nADH (desmopressin) nClinical Use:

n __________________



7

nLeuprolide MOA:

n GnRH Analog

n Agonist Properties if ________ Administration n Clinical Use:

n Pulsatile Dose

n __________________ n Continuous Dose

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



8

nTestosterone, Methyltestosterone MOA:

n Androgen Receptor Agonist n Inhibits LH -> Produce Less Testosterone

n S/E: n Masculinization (Females) n Gonadal Atrophy n Increase LDL n Decrease HDL n Early Epiphyseal Plate Closure

n Clinical Use: n Hypogonadism n Promote Anabolism in Burn Patients

+Endocrine: Antiandrogens


9

nFinasteride nMOA: __________________-> Slow Conversion Testosterone to

DHT n Clinical Use: BPH and Male Pattern Baldness

nFlutamide nMOA: __________________ n Clinical Use: Prostate Carcinoma

+Endocrine: Antiandrogens


10

nKetoconazole nMOA: Inhibits 17,20-Desmolase (Steroid Synthesis) n Clinical Use: __________________

nSpironolactone nMOA: Inhibits Steroid Synthesis

n Clinical Use: __________________

nKetoconazole and Spironolactone n Used in Polycystic Ovarian Syndrome

n Prevention of Hirsuitism



11

nEstrogens: Ethinyl Estradiol, DES, Mestranol MOA:

n Bind Estrogen Receptors

nClinical Use: n Hypogonadism n Ovarian Failure

n __________________ n __________________



12

nEstrogens: Ethinyl Estradiol, DES, Mestranol nS/E:

n Increase Risk Endometrial Cancer n Postmenopausal Bleeding

n __________________ n Contraindicated in:

n ER-Positive Breast Cancer

n __________________

+Endocrine: SERMs (Selective Estrogen Receptor Modulator)


13

nClomiphene nMOA: Partial Estrogen Receptor Agonist nS/E:

n __________________ n Ovarian Enlargement n __________________

n Clinical Use: n __________________ n PCOS

+Endocrine: SERMs (Selective Estrogen Receptor Modulator)


14

nTamoxifen, Raloxifen nMOA: n Antagonist at Breast n Agonist at Bones

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

n RELAXifen Dont Worry about Risks of Endometrial Carcinoma

+Endocrine: Pharmacology


15

nAnastrozole/Exemestane nMOA: Aromatase Inhibitor n Clinical Use:

n Postmenopausal Patient with Breast Cancer



16

nProgestins MOA: n Bind Progesterone Receptors

n Increase __________________

n Clinical Use: n __________________ n __________________ n Abnormal Uterine Bleeding



17

nMifepristone (aka RU-486) MOA: n Competitive Inhibitor of Progestins

n At Progesterone Receptors nS/E:

n __________________ n GI (Nausea, Vomiting, Anorexia) n Abdominal Pain

n Clinical Use: n Abortifacent n Coadministered with __________________



18

nTerbutaline MOA: n2-Agonist

n __________________ n Clinical Use:

n Reduce __________________



19

nTamsulosin MOA:

n __________________ n Inhibits Smooth Muscle Contraction

n Clinical Use: n BPH n Selective 1A,D Receptor

n Found in Prostate

n TAMEsulosin -> Least Side Effects TAME



20

nSildenaFIL, VardenaFIL MOA:

nInhibit __________________ n Increase in cGMP -> Vasodilation

n Clinical Use: n Erectile Dysfunction

n__________________ n -> Help FILL the Corpus Cavernosum with Blood!



21

nSildenaFIL, VardenaFIL nS/E:

n Dyspepsia n Headache n Flushing

n Impaired __________________Color Vision n Severe HypOtension

n In Patients Taking Nitrates Concurrently

n PDE5 Inhibitors n-> Help FILL the Corpus Cavernosum with Blood!



22

nDanazol MOA: n 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

+Gastrointestinal Hormones Shan Nanji



24

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



25

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



26

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



27

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



28

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



29

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



30

nMotilin ACTION: n Produces Migrating Motor Complexes (MMC)

REGULATION: n Increase During Fasting State

ORIGIN: n Small Intestine



31

nIntrinsic Factor ACTION: n Binds Vitamin B12

REGULATION:

ORIGIN: n Parietal Cells in Stomach



32

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



33

nGastric Acid ACTION: n Protein Digestion

REGULATION: n Increase by Vagal Stimulation n Increase by Acid

ORIGIN: n Chief Cells in Stomach



34

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

07 Endocrine & Reproductive

Documents

Transcript of 07 Endocrine & Reproductive