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Endocrine

Endocrine Pharmacology

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Endocrine Pharmacology

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Page 1: Endocrine Pharmacology

Endocrine

Page 2: Endocrine Pharmacology

� Acarbose

� Alendronate

� Calcitonin

� Danazol

� Desmopressin

� Ergocalciferol

� Ethinyl estradiol & drospirenone

� Ethinyl estradiol & norethindrone

� Finasteride

� Fludrocortisone

� Glyburide

� Hydrocortisone

� Insulin

� Levothyroxine

� Medroxyprogesterone

� Metformin

� Methimazole

� Mifepristone

� Octreotide

� Oxytocin

� Pioglitazone

� Prednisone

� Raloxifene

� Repaglinide

� Somatropin

� Testosterone

Page 3: Endocrine Pharmacology

Acarbose

� Antidiabetic

� α-glucosidase inhibitor

� Inhibits intestinal enzyme that

converts oligosaccharides &

disaccharides to glucose

� ↓ digestion of starch & sucrose

� ↓ postprandial blood glucose &

HbA1c

� Type II DM

� Intestinal bloating

� Flatulence

� ↑ oral bioavailability of

metformin

� ↓ iron absorption

Page 4: Endocrine Pharmacology

Alendronate� Bone resorption inhibitor

� Bisphosphonate

� Prevents attachment of osteoclast precursor cells to bone

� ↓ metabolic activity of osteoclasts & ability to resorbbone

� Prevent/Tx� Osteoporosis

� Corticosteroid-induced osteoporosis

� Paget’s ds of bone

� hypercalcemia

� Absorption ↓ by Ca supplements, antacids, foods, beverages (except water)

Page 5: Endocrine Pharmacology

Calcitonin

� Ca hormone

� Thyroid gland hormone

� Binds calcitonin receptor on

osteoclasts

� ↑ cAMP & inhibits osteoclast

activity

� ↓ bone resorption, bone pain, &

serum [Ca]

� Postmenopausal osteoporosis

� Paget’s ds of bone

� hypercalcemia

Page 6: Endocrine Pharmacology

Danazol� Ovarian inhibitor

� Synthetic androgen, antiestrogen

� Feedback inhibits pituitary FSH & LH secretion ↓ ovarian estrogen secretion & stim. endometrial & breast tissue.

� Endometriosis

� Fibrocystic breast ds

� Hereditary angioedema

� ↑ C1 esterase inhibitor & C4 complement component

� CI in pregnancy – androgenic effects on female fetus

� Emotional lability

� Deepening voice

� Acne

� Hirsutism

� Amenorrhea

� ↓ breast size

Page 7: Endocrine Pharmacology

Desmopressin� Posterior pituitary hormone

� Vasopressin, ADH analogue

� Mimics natural vasopression

� Increases water reabsorption in kidneys

� Vasoconstriction

� DI

� Nocturnal enuresis

� Control bleeding in hemophilia & wWF’s ds

� Intranasal, oral, or IV

Page 8: Endocrine Pharmacology

Ergocalciferol� Vit. D

� Fat-soluble

� Activated in liver & kidneys to form calcitriol� ↑ Ca & phosphorus absorption

from gut

� Vit. D deficiency� Rickets, osteomalacia

� Chronic renal failure

� Familial hypophosphatemia

� Hypocalcemia d/t hypoparathyroidism

� Postoperative & idiopathic tetany

� Hypercalcemia

� Hypercalciuria

� Cholestyramine inhibits vit. D absorption

� Induce vit. D metabolism� Phenytoin

� Barbiturates

Page 9: Endocrine Pharmacology

Ethinyl estradiol & drospirenone

� OCP

� Estrogen & progesterone

� Feedback inhibit GnRH

� Estrogen

� ↓ FSH secretion & maturation

of dominant follicle

� Progesterone

� Inhibits midcycle LH surge &

ovulation

� Contraception

� Regulate menstrual cycle

� Acne in women

� Drospirenone

� Antiandrogenic

� Blocks aldosterone

� ↓ salt & water retention

� ↓ BP

� Thromboembolism

� ↑ risk w/ smoking

� Edema

� Efficacy ↓ w/

� ABX

� Carbamazepine

� phenytoin

Page 10: Endocrine Pharmacology

Ethinyl estradiol & norethindrone

� OCP

� Estrogen & progesterone

� Feedback inhibit GnRH

� Estrogen

� ↓ FSH secretion & maturation

of dominant follicle

� Progesterone

� Inhibits midcycle LH surge &

ovulation

� Contraception

� Regulate menstrual cycle

� Acne in women

� Norethidrone

� Slightly androgenic

� Thromboembolism

� Edema

� Depression

� Gallbladder ds

Page 11: Endocrine Pharmacology

Finasteride

� Androgen synthesis inhibitor

� 5-α-reductase inhibitor

� Inhibits conversion testosterone

���� dihydrotestosterone & ↓

androgenic stimulation of

prostate & skin

� ↓ prostate size & promotes hair

growth

� BPH

� Male pattern baldness

� CI pregnancy

� Risk to male fetus

� Do NOT handle tablets

� Impotence

Page 12: Endocrine Pharmacology

Fludrocortisone� Corticosteroid

� Mineralocorticoid

� Activates aldosterone receptors in renal distal tubule

� ↑ Na reabsorption

� ↑ K & H excretion

� Adrenal insufficiency

� Addison’s ds

� Congenital adrenogenital syn

� Tx idiopathic orthostatic hypotension w/ ↑ Na intake

� Hypokalemia

� ↑ by thiazide & loop diuretics

Page 13: Endocrine Pharmacology

Glyburide

� Antidiabetic

� Sulfonylurea hypoglycemia

� Closes ATP-sensitive K

channels preventing K efflux &

depolarizing pancreas B cells

� Influx Ca & relaxing insulin

� ↑ amount of insulin secreted

during each pulse

� Type II DM

� Photosensitivity

� Hypoglycemia

Page 14: Endocrine Pharmacology

Hydrocortisone

� Short-acting corticosteroid, low-

potency topical corticosteroid

� Glucocorticoid

� Replaces endogenous cortisol in

deficiency states

� Suppresses inflammation &

immune response – topical

� Adrenocortical insufficiency

� Topical

� Insect bites

� Contact dermatitis

Page 15: Endocrine Pharmacology

Insulin

� Antidiabetic

� Pancreatic hormone

� Replaces endogenous

insulin

� DM

� Rapid acting – lispro

� Intermediate acting – lente

� Long acting – ultralente

� Hypoglycemia

� β-blockers mask signs of

hypoglycemia & prolong

recovery

Page 16: Endocrine Pharmacology

Levothyroxine

� Thyroid hormone

� Tetraiodothyronine

� Binds nuclear receptors & ↑ gene transcription

� ↑ metabolic rate, protein synthesis, gluconeogenesis, cell growth & differentiation, & CNS development

� Converted to T3 in tissues

� Hypothyroidism

� Insomnia

� Irritability

� Tachycardia

� Wt loss

� Bile acid sequestrants ↓absorption

Page 17: Endocrine Pharmacology

Medroxyprogesterone� Progestin, contraceptive

� Progesterone analogue

� ↓ endometrial hyperplasia in women receiving estrogen

� Prevents conception by thickening cervical mucus

� Estrogen-progestin HRT

� Injectable contraceptive

� Progestin-only injectable contraceptive

� IM depot injection lasts 3mo

� Amenorrhea

� Breakthrough bleeding

� Dysmenorrhea

Page 18: Endocrine Pharmacology

Metformin� Antidiabetic

� Biguanide, antihyperglycemic

� ↑ # & affinity of insulin receptors in peripheral tissues

� ↓ hepatic glucose output

� ↓glucose absorption from gut

� ↑ glucose uptake & utilization in skeletal m. & adipose tissue

� Type II DM

� Used in combo w/ sulfonylureas

� N, V, D

� Abdominal bloating

Page 19: Endocrine Pharmacology

Methimazole

� Antithyroid

� Thiourea, thyroid hormone synthesis inhibitor

� Inhibits peroxidase & iodination & coupling of tyrosine residue of thyroglobulin

� ↓ thyroxine secretion

� Hyperthyroidism – Grave’s ds

� Rash

� Agranulocytosis

Page 20: Endocrine Pharmacology

Mifepristone

� Abortificient

� Progesterone antagonist

� Partial agonist or antagonist

progesterone receptors

� Medical termination of

pregnancy through 49d gestation

� Single dose + prostaglandin for

48hr stim. uterine contractions

� Abdominal pain

� Diarrhea

� N, V

� Uterine bleeding

� Cramping

Page 21: Endocrine Pharmacology

Octreotide� GH inhibitor, antidiarrheal

� Somatostatin analogue w/ greater effects on GH than insulin secretion

� Suppresses secretion of GH, insulin-like growth factors, 5-HT & GI peptides – gastrin, motilin, secretin, & VIP

� Acromegaly

� Severe diarrhea & flushing d/t carcinoid tumors & VIP tumors

� Bleeding GE varices

� Complications of pancreatic surgery

� Arrhythmias

� Hyperglycemia

� Hypoglycemia

� Constipation

� Diarrhea

� Flatulence

� N

Page 22: Endocrine Pharmacology

Oxytocin� Oxytocic

� Posterior pituitary hormone

� Stim. Uterine smooth m. & induce labor

� Stim. mammary gland smooth m. & lactation

� Induce labor @ term

� Facilitate uterine contractions

� Postpartum control of uterine bleeding

� Promote milk let-down

� IV for uterine stim.

� Nasal for milk let-down

� Excessive & painful uterine contractions

Page 23: Endocrine Pharmacology

Pioglitazone� Antidiabetic

� Thiazolidinedioneantihyperglycemic

� Activates peroxisome proliferator-activated receptor-γ in adipose tissue, skeletal m., & liver

� ↑ gene transcription, insulin sensitivity, & glucose transports in muscle & adipose tissue

� Suppresses hepatic glucose output

� Type II DM

� Used w/ metformin

Page 24: Endocrine Pharmacology

Prednisone

� Anti-inflammatory

� Corticosteroid

� Suppresses inflammation

& immune response

� Inflammatory, allergic,

autoimmune, & neoplastic ds

� Prevent organ transplant

rejection

� Asthma

� Depression or euphoria

� HTN

� Acne

� Impaired wound healing

� Adrenal suppression

� Muscle wasting

� Osteoporosis

� Cushingoid appearance

� Moon facies

� Buffalo hump

� ↑ susceptibility to infection

Page 25: Endocrine Pharmacology

Raloxifene� Bone resorption inhibitor

� Selective estrogen receptor modulator – SERM

� Estrogen-like effect on bone & lipid metabolism

� Estrogen antagonist in breast & uterine tissue

� ↑ bone mineral density & ↓vertebral fractures

� Osteoporosis in postmenopausal women

� Used in woman @ risk for breast cancer

� Hot flashes

� Cholestyramine inhibits absorption

Page 26: Endocrine Pharmacology

Repaglinide

� Antidiabetic

� Meglitinide hypoglycemic

� Closes ATP-sensitive K

channels & ↑ insulin secretion

� ↓ postprandial blood glucose &

[HbA1c]

� Taken before meals to control

postprandial hyerglycemia

� Used w/ metformin

� NOT sulfonylureas

� Hypoglycemia

Page 27: Endocrine Pharmacology

Somatropin� GH

� Recombinant somatotropin

� ↑ release of insulin-like growth factors in liver & cartilage

� Stim. skeletal growth, AA transport, protein synthesis, nucleic acid synthesis & cell prolif.

� Short stature in children d/t GH deficiency

� Turner syn

� Chronic renal failure

� Prader-Will syn

Page 28: Endocrine Pharmacology

Testosterone� Androgen

� Gonadal steroid

� Activated gene transcription & development of male sex organs & secondary sex characteristics

� ↑ lean body mass

� Stim. skeletal growth

� Accelerates epiphyseal closure

� ↑ sebaceous gland sebum production

� ↑ EPO secretion

� ↓ HDL levels

� Hypogonadism in androgen-deficient men

� Delayed puberty in males

� Edema

� Acne

� Gynecomastia

� Impotence

� Oligospermia

� Priapism