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Endocrine Pharmacology
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Endocrine
� 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
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
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)
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Methimazole
� Antithyroid
� Thiourea, thyroid hormone synthesis inhibitor
� Inhibits peroxidase & iodination & coupling of tyrosine residue of thyroglobulin
� ↓ thyroxine secretion
� Hyperthyroidism – Grave’s ds
� Rash
� Agranulocytosis
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
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
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
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
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
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
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
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
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