6254187.ppt

PTP 546
Endocrine Pharmacology
Module 11
Jayne Hansche Lobert, MS, RN, ACNS-BC, NP
1
Lobert

Adrenalcorticoids
• Naturally Occurring Adrenal Corticoids
– Negative feedback loop
• Hypothalamus CRH Pituitary  ACTH  adrenal
cortex cortisol
– Glucocorticoids
• Cortisol, Corticosterone
– Glucose, protein and lipid metabolism
– Anti-Inflammatory effects
– Immunosuppressive effect
– Mineralcorticoids
• Aldosterone
– Fluid and electrolyte control
2
Lobert

Adrenalcorticoids
• Pharmacologic Glucocorticoids
– Ex:Dexamethasone (Decadron)
– Ex:Hydrocortisone (Cortef)
– Ex:Methylpredisolone (Medrol)
– Ex:Prednisone (Deltasone)
– Ex:Triamcinolone (Azmacort)
• Routes of Administration
– IV, inhaled, oral, intraarticular, topical, nasal,
ophthalmic, otic, etc.
3
Lobert

Adrenalcorticoids
• Glucocorticoids
– Action: inhibit the production of proinflammatory
substances suppression of inflammation;
inhibit immune cell synthesis  suppression of
the immune response
– Therapeutic Use
• Replacement associated with adrenal insufficiency
• Reduce inflammation in many conditions
• Suppression of the immune response
4
Lobert

Adrenalcorticoids
Inflammatory Disorders
• Allergic Reactions,
Anaphylaxis
• Psoriasis, Dermatitis
• Osteoarthritis, Gouty
Arthritis, Rheumatoid
Arthritis
• Bursitis, Synovitis
• Leukemia's, Lymphomas
• Closed Head Injury, Spinal
Cord Injury, Brain Tumors
• Organ Transplantations
• Crohn’s, Ulcerative Colitis
• Bronchial Asthma, COPD
• Pneumonias
• Scarcidosis
• Multiple Sclerosis,
Myasthenia Gravis
• Systemic Lupus
Erythematosus (SLE)
5
Lobert

Adrenalcorticoids
• Glucocorticoids
– Side Effects:
• Dyspepsia, gi upset, gi bleed, peptic ulcers
• Increased risk for infection
• Mood changes, labile emotions
• Sodium retention, hypertension
• Bone loss, osteoporosis, fracture risk
• Muscle atrophy, delayed wound healing
• Hyperglycemia
• Increased appetite, weight gain
• Changes in appearance: “Moon face”, truncal obesity, acne, “buffalo
hump”, thin limbs, increased body hair
– Side Effects:
• Reflect an excess of adrenal hormone; Cushing’s Syndrome/Disease;
Adrenal Hypersecretion
6
Lobert

Adrenalcorticoids
• Precautions
– Avoid abrupt withdrawal
• Taper off prior to discontinuation of med
• Rapid Adrenal Insufficiency Addison’s
Syndrome/Disease/ Adrenal Crisis
– Life Threatening Effects: lethargy, confusion & coma
– Recognize value of glucocorticoids
– Recognize significant side effects of
glucocorticoids
7
Lobert

Adrenalcorticoids
• Mineralcorticoids
– Ex: Fludrocortisone (Florinef)
– Action: causes sodium reabsorption & water
retention, potassium loss in distal renal tubules
– Therapeutic Effect: replacement of
mineralcorticoids with conditions of adrenal
insufficiency such as Addison’s Disease; Post
Adrenalectomy
– Side Effects: hypertension, sodium retention,
water retention, edema, weight gain, hypokalemia
8
Lobert

Sex Hormones
• Naturally Occurring Male Sex Hormones
– Androgens
• Testosterone
– Effect of Androgens
• Development of male sexual characteristics
– Increased body hair, increased skeletal muscle mass, voice
change, maturation of external genitalia
• Stimulation of spermatogenesis
– Facilitate growth and maturation of developing sperm
Lobert 9

Sex Hormones
• Pharmacologic Androgens
– Examples:
• Fluxymesterone (Android)
• Methylestesterone (Durabolin)
• Oxandrolone (Oxandrin)
• Testosterone Gel (Androderm)
• Testosterone Transdermal (Androgel)
Lobert 10

Sex Hormones
– Action: mimic androgenic effects development of
male sexual characteristics and mimics anabolic
effects  development of muscles, increase in the
lean muscle mass
– Therapeutic Use:
• Replacement therapy
• Catabolic states
• Delayed puberty
• Breast Cancer
Lobert 11

Sex Hormones
– Side Effects:
• Women: hair growth, voice deepening, irregular
menstruation, acne
• Male: bladder irritation, breast swelling, prolonged
erections, increased risk of prostate cancer
• Children: accelerated sexual maturation, impairment of
bone growth
• General: hypertension, elevation in lipid profile, liver
damage, liver cancer
Lobert 12

Sex Hormones
• Naturally Occurring Female Hormones
– Estrogen
• Estradiol
– Progestins
• Progesterone
– Effects:
• Development of female sexual characteristics
• Development of female reproductive system
• Facilitation and maintenance of pregnancy
Lobert 13

Sex Hormones
• Pharmacologic Female Hormones
– Examples:
• Conjugated estrogens (Premarin)
• Estradiol(Estraderm, Depo-Estradiol)
• Medroxyprogesterone (Provera)
• Levonorgestrel (Norplant)
Lobert 14

Sex Hormones
– Action: mimics naturally occurring hormones
– Therapeutic Use:
• Replacement therapy
• Hypogonadism
• Failure of ovarian development
• Menstrual irregularities
• Endometriosis
• Carcinoma
Lobert 15

Sex Hormones
– Side Effects:
• Myocardial Infarctions, thromboembolism, stroke
• Abnormal clotting thrombophlebitis, pulmonary
embolism
• Increase risk for ovarian, endometrial and breast
cancers
• Transient nausea
• Sodium and water retention
Lobert 16

Sex Hormones
• Selective Estrogen Receptor Modulators
– Ex: Tamoxifen (Nolvadex)
– Ex: Raloxifene (Evista)
– Action: blocks estrogen receptors
– Therapeutic Effect: used for treatment of
hormone specific cancers
– Side Effects: hot flashes, joint pain, nausea and
vomiting
Lobert 17

Sex Hormones
• AntiProgestins
– Ex: Mifepristone (RU486)
– Action: stimulate uterine contractions embryo
expulsion
– Therapeutic Effect: pregnancy termination
– Side Effects: excessive contractions, incomplete
abortion, excessive bleeding
Lobert 18

Sex Hormones
• Hormonal Contraceptives
– Ex: Estradiol & Norethidrone (Loestrin)
– Ex: Estradiol & Etonogestrel (Nuva Ring)
– Ex: Levonorgestrel (Norplant)
– Ex: Medroxyprogesterone (Depo-Provera)
Lobert 19

Sex Hormones
• Hormonal Contraceptives
– Action: inhibit ovulation, impairs uterine
endometrial implantation
– Therapeutic Effect: prevention of pregnancy
– Side Effects: cardiovascular effects such as
thromboembolism, stroke, MI, liver cancer with
prolonged use, nausea, headache, weight gain
Lobert 20

Thyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• Naturally Occurring Thyroid Hormone
– T4 (Thyroxine) and T3 (Triiodothyronine)
• Maintain body temperature
• Increase basal metabolic rate
• Facilitates normal growth and development
• Increase heart rate and myocardial contractility
• Enhance glucose absorption
• Enhance lipolysis
Lobert 21

• Drugs to Treat Hyperthyroidism
– Antithyroid Agents
• Ex: Methimazole (Tapazole)
• Ex: Propylthiouracil (PTU)
– Iodide
• Ex: SSKI
– Radioactive Iodine
• Ex: RA 131
Lobert 22

– Antithyroid Agents
• Ex: Methimazole (Tapazole)
• Ex: Propylthiouracil (PTU)
– Action: inhibits conversion of T4T3; blocks
thyroid peroxidase enzyme
– Therapeutic Effect: reduction of thyroid hormone
synthesis
– Side Effects: agranulocytosis, itching, rash
Lobert 23

– Iodide
• Action: inhibits all steps in thyroid hormone synthesis;
dramatically reduces thyroid hormone in limited
situations
• Side Effects: stains teeth
– Radioactive Iodine: RA 131
• Action: destroys thyroid tissue
• Side Effects: hypothyroidism
Lobert 24

• Drugs to Treat Hypothyroidism
– Thyroid Hormone
• Ex: Levothyroxine (Levothroid, Synthroid)
• Ex: Liothyronine (Cytomel)
– Action: Supplement/replace T3 and/or T4
reduction of TSH; mimics function of the thyroid
gland
– Therapeutic Effect: treatment of thyroid deficiency
related to hypothyroidism, thryroidectomy, etc.
Lobert 25

Side Effects of too little thyroid
hormone replacement
• Lethargy
• Weight gain
• Constipation
• Bradycardia
• Weakness
• Facial edema
• Concentration difficulties
• Fatigue
• Coarse skin
Side Effects of excess thyroid
hormone replacement
• Fatigue
• Weight loss
• Diarrhea
• Tachycardia
• Muscle wasting
• Increased appetite
• Insomnia
• Menstrual irregularities
• Exopthalmos
Lobert 26

• Regulation of Bone Mineral Homeostasis
– Parathyroid Hormone (PTH)
• Increases blood calcium levels & increases phosphate excretion;
stimulates Vitamin D  increased calcium absorption from
intestines
• High levels of PTH bone breakdown
• Normal levels of PTH bone synthesis
– Vitamin D
• Helps increase calcium, phosphate enhances bone formation
– Calcitonin
• Physiologic antagonist of PTH; lowers blood calcium by stimulating
bone formation; incorporates phosphate into bone
Lobert 27

• Phamacoloigics for Bone Mineral Homeostasis
– Calcium Supplements
– Vitamin D
– Biphosphonates
– Calcitonin
– Estrogen
Lobert 28

• Calcium Supplements
– Ex: Calcium Carbonate (Os-Cal); Calcium Citrate
(Citracal)
– Action: mimics calcium effects in body
– Therapeutic Effect: supports bone formation
assoc. with dietary insufficiency,
hypoparathyroidism; rickets
– Side Effects: constipation, fatigue
– Post Menopausal Intake: 1200-1500 mg/day
Lobert 29

• Vitamin D Supplements
– Ex: Vitamin D (OsCal & D)
– Action: mimics Vit D effects in body; necessary for
calcium absorption in the intestines
– Therapeutic Effect: enhances bone mineralization
– Side Effects: headache, thirst, metallic taste
Lobert 30

• Biphosphonates
– Ex: Alendronate (Fosamax)
– Action: directly reduces bone resorption
– Therapeutic Effect: prevent bone loss assoc with
steroid use; treatment of osteoporosis to reduce
risk of vertebral fractures; treatment of Pagets
disease
– Side Effects: gi upset and esophagitis (remain
upright for 30 minutes following administration to
prevent)
Lobert 31

• Calcitonin
– Ex: Calcitonin (Calcimar)
– Action: mimics endogenous calcitonin
decreased blood calcium levels ensuring calcium
availability for bone mineralization
– Therapeutic Effect: use in conditions that are
characterized by increased bone resorption
– Side Effects: redness & swelling following
injections, gi upset
Lobert 32

Treatment of Diabetes Mellitus
• Type I Diabetes
– Etiology: young age, viral trigger for autoimmune
response
– Pathophysiology: destruction of pancreatic beta
cells total lack of insulin production
– Clinical Signs & Symptoms: rapid onset of the
clinical manifestations of polyuria, polydipsia,
polyphagia
Lobert 33

• Type II Diabetes
– Etiology: aging individuals; genetic predisposition;
obesity, lack of exercise, poor dietary intake
– Pathophysiology: reduced tissue sensitivity to
insulin (insulin resistance); reduction in insulin
production; irregular release of insulin
– Clinical Signs & Symptoms: slow and gradual onset
of the clinical manifestations of delayed wound
healing, fatigue; blurred vision
Lobert 34

• Complications of Diabetes
– Microvascular
• Retinopathies blindness
• Nephropathies renal failure
• Neuropathies
– Sensory
– Autonomic
– Macrovascular
• Hypertension, myocardial infarction, cerebral vascular
accidents, peripheral arterial disease, amputations
Lobert 35

• Prevention of Complications
– Diabetes Control and Complications Trial (DCCT) &
United Kingdom Prospective Diabetes Study
(UKPDS)
• Prolonged elevations in blood glucose structural and
functional changes in vascular cells
– Tight Glycemic Control Prevents Complications
• Maintain blood glucose 70-100mg/dl
• Side Effect: risk for hypoglycemia
Lobert 36

• Management of Diabetes Mellitus
– Diet
– Exercise
– Medications
• Oral hypoglycemic agents
• Insulin
– Blood Glucose Monitoring
Lobert 37

• Insulin
– Types (Onset/Peak/Duration)
• Immediate Acting (<0.5 hr/1.5 hr/3-6hr)
– Lispro (Humalog); Aspart (Novolog)
• Rapid Acting (.5 hr/2-4hr/5-7 hr)
– Regular (Humulin R, Novolin R)
• Intermediate Acting (1-3 hr/6-12hr/18-24 hr)
– Isophane (Humulin N, Novolin N)
– Insulin Zinc (Humulin L, Novolin L)
• Long Acting ( 2hr/ no peak/24 hrs)
– Glargine (Lantus)
Lobert 38

• Insulin
– Routes: IV, subcutaneous injections, insulin pump
subcutaneous
– Action: mimics endogenous insulin; facilitates
glucose transport into cells
– Therapeutic Effect: reduction of blood glucose
– Side Effects: Hypoglycemia
Lobert 39

• Antidiabetic Agents
– Sulfonylureas
• Ex: Glipizide (Glucotrol)
– Biguanides
• Ex: Metformin (Glucophage)
– Alpha-Glucosidase Inhibitors
• Ex: Acarbose (Precose)
– Thiazolinediones
• Ex: Rosiglitazone (Avandia)
– Meglitinides
• Ex: Repaglinide (Prandin)
– Glucagon Like Peptide/ Incretin Mimic
• Ex: Exenatide (Byetta)
– Dipeptidyl Peptidase-4 Inhibitor (DDP-4)
Lobert 40

• Oral Antidiabetic Agents
– Sulfonylureas
– Ex: Glipizide (Glucotrol); Glyburide (DiaBeta)
– Action: increase insulin secretion from pancreatic
beta cells
– Therapeutic Effect: reduces blood glucose;
reduces hepatic glucose production
– Side Effects: weight gain, hypoglycemia, gi upset
Lobert 41

– Biguanides
• Ex: Metformin (Glucophage)
– Action: decreases hepatic glucose production;
increases muscle tissue sensitivity to insulin
– Side Effects: diarrhea, gi disturbances; rarely lactic
acidosis occurs, to avoid  hold IV contrast media
for 48 hrs
Lobert 42

– Alpha-Glucosidase Inhibitors
• Ex: Acarbose (Precose)
– Action: inhibits breakdown of glucose and delays
absorption of glucose in the intestine
– Side Effects: gi disturbances, bloating, gas,
diarrhea
Lobert 43

– Thiazolinediones
• Ex: Rosiglitazone (Avandia)
– Action: increases glucose uptake in muscles,
decreases glucose production
– Therapeutic Effect: reduces blood glucose
– Side Effects: weight gain, edema
Lobert 44

– Meglitinides
• Ex: Repaglinide (Prandin)
– Action: stimulates rapid release of insulin from the
pancreas
– Side Effects: weight gain, hypoglycemia
Lobert 45

– Dipeptidyl Peptidase-4 Inhibitor (DDP-4)
• Ex: Sitagliptin (Januvia)
– Action: enhances incretin system, stimulates
release of insulin from the pancreas, decreases
hepatic glucose production
– Side Effects: upper respiratory tract infections,
sore throat, diarrhea
Lobert 46

• Miscellaneous Injectable Antidiabetic Agents
– Glucagon Like Peptide/Incretin Mimic
• Ex: Exenatide (Byetta)
– Amylin Analog
• Ex: Pramlintide (Symlin)
– Action: decrease gastric emptying, decrease
glucagon production, increased satiety
– Side Effects: hypoglycemia, nausea, vomiting
Lobert 47

• Hypoglycemic Side Effect
– Signs & Symptoms
• Confusion, irritability, diaphoresis, tremors, hunger,
weakness, visual disturbances coma, seizures, death
– Treatment
• Oral Glucose
– 10-15 g of CHO= 6 oz. Orange juice, 8 oz. milk
– Glucose tablets, glucose paste
• IV Glucose
– 50% Dextrose Injection
• Intramuscular Glucagon
Lobert 48

• Hypoglycemia
– Causes/Contributing Factors
• Imbalance of exercise, meds and meals
• Hypoglycemic unawareness
– Prevention
• Education
• Awareness
• Preparedness
Lobert 49

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