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Lobert 1
PTP 546Endocrine Pharmacology
Module 11
Jayne Hansche Lobert, MS, RN, ACNS-BC, NP
Lobert 2
Endocrine PharmacologyAdrenalcorticoids
• 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
Lobert 3
Endocrine PharmacologyAdrenalcorticoids
• 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.
Lobert 4
Endocrine PharmacologyAdrenalcorticoids
• 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
Lobert 5
Endocrine PharmacologyAdrenalcorticoids
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)
Lobert 6
Endocrine PharmacologyAdrenalcorticoids
• 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
Lobert 7
Endocrine PharmacologyAdrenalcorticoids
• 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
Lobert 8
Endocrine PharmacologyAdrenalcorticoids
• 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
Lobert 9
Endocrine PharmacologySex 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 10
Endocrine PharmacologySex Hormones
• Pharmacologic Androgens– Examples:• Fluxymesterone (Android)• Methylestesterone (Durabolin)• Oxandrolone (Oxandrin)• Testosterone Gel (Androderm)• Testosterone Transdermal (Androgel)
Lobert 11
Endocrine PharmacologySex Hormones
• Pharmacologic Androgens– 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 12
Endocrine PharmacologySex Hormones
• Pharmacologic Androgens– 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 13
Endocrine PharmacologySex 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 14
Endocrine PharmacologySex Hormones
• Pharmacologic Female Hormones– Examples:• Conjugated estrogens (Premarin)• Estradiol(Estraderm, Depo-Estradiol)• Medroxyprogesterone (Provera)• Levonorgestrel (Norplant)
Lobert 15
Endocrine PharmacologySex Hormones
• Pharmacologic Female Hormones– Action: mimics naturally occurring hormones
– Therapeutic Use:• Replacement therapy• Hypogonadism• Failure of ovarian development• Menstrual irregularities• Endometriosis• Carcinoma
Lobert 16
Endocrine PharmacologySex Hormones
• Pharmacologic Female 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 17
Endocrine PharmacologySex 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 18
Endocrine PharmacologySex Hormones
• AntiProgestins– Ex: Mifepristone (RU486)– Action: stimulate uterine contractions embryo
expulsion– Therapeutic Effect: pregnancy termination– Side Effects: excessive contractions, incomplete
abortion, excessive bleeding
Lobert 19
Endocrine PharmacologySex Hormones
• Hormonal Contraceptives– Ex: Estradiol & Norethidrone (Loestrin)– Ex: Estradiol & Etonogestrel (Nuva Ring)– Ex: Levonorgestrel (Norplant)– Ex: Medroxyprogesterone (Depo-Provera)
Lobert 20
Endocrine PharmacologySex 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 21
Endocrine PharmacologyThyroid & 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 22
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• Drugs to Treat Hyperthyroidism– Antithyroid Agents• Ex: Methimazole (Tapazole)• Ex: Propylthiouracil (PTU)
– Iodide• Ex: SSKI
– Radioactive Iodine • Ex: RA 131
Lobert 23
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• Drugs to Treat Hyperthyroidism– Antithyroid Agents• Ex: Methimazole (Tapazole)• Ex: Propylthiouracil (PTU)
– Action: inhibits conversion of T4T3; blocks thyroid peroxidase enzyme
– Therapeutic Effect: reduction of thyroid hormone synthesis
– Side Effects: agranulocytosis, itching, rash
Lobert 24
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• Drugs to Treat Hyperthyroidism– 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 25
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• 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 26
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
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 27
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• 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 28
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• Phamacoloigics for Bone Mineral Homeostasis– Calcium Supplements– Vitamin D– Biphosphonates– Calcitonin– Estrogen
Lobert 29
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• 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 30
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• 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 31
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• 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 32
Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization
• 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 33
Endocrine PharmacologyTreatment 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 34
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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 35
Endocrine PharmacologyTreatment of Diabetes Mellitus
• Complications of Diabetes– Microvascular• Retinopathies blindness• Nephropathies renal failure• Neuropathies
– Sensory– Autonomic
– Macrovascular• Hypertension, myocardial infarction, cerebral vascular
accidents, peripheral arterial disease, amputations
Lobert 36
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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 37
Endocrine PharmacologyTreatment of Diabetes Mellitus
• Management of Diabetes Mellitus– Diet– Exercise– Medications• Oral hypoglycemic agents• Insulin
– Blood Glucose Monitoring
Lobert 38
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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 39
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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 40
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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 41
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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 42
Endocrine PharmacologyTreatment of Diabetes Mellitus
• Oral Antidiabetic Agents– Biguanides• Ex: Metformin (Glucophage)
– Action: decreases hepatic glucose production; increases muscle tissue sensitivity to insulin
– Therapeutic Effect: reduction of blood glucose– Side Effects: diarrhea, gi disturbances; rarely lactic
acidosis occurs, to avoid hold IV contrast media for 48 hrs
Lobert 43
Endocrine PharmacologyTreatment of Diabetes Mellitus
• Oral Antidiabetic Agents– Alpha-Glucosidase Inhibitors• Ex: Acarbose (Precose)
– Action: inhibits breakdown of glucose and delays absorption of glucose in the intestine
– Therapeutic Effect: reduction of blood glucose– Side Effects: gi disturbances, bloating, gas,
diarrhea
Lobert 44
Endocrine PharmacologyTreatment of Diabetes Mellitus
• Oral Antidiabetic Agents– Thiazolinediones• Ex: Rosiglitazone (Avandia)
– Action: increases glucose uptake in muscles, decreases glucose production
– Therapeutic Effect: reduces blood glucose– Side Effects: weight gain, edema
Lobert 45
Endocrine PharmacologyTreatment of Diabetes Mellitus
• Oral Antidiabetic Agents– Meglitinides• Ex: Repaglinide (Prandin)
– Action: stimulates rapid release of insulin from the pancreas
– Therapeutic Effect: reduces blood glucose– Side Effects: weight gain, hypoglycemia
Lobert 46
• Oral Antidiabetic Agents– Dipeptidyl Peptidase-4 Inhibitor (DDP-4)• Ex: Sitagliptin (Januvia)
– Action: enhances incretin system, stimulates release of insulin from the pancreas, decreases hepatic glucose production
– Therapeutic Effect: reduces blood glucose– Side Effects: upper respiratory tract infections,
sore throat, diarrhea
Lobert 47
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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
– Therapeutic Effect: reduces blood glucose– Side Effects: hypoglycemia, nausea, vomiting
Lobert 48
Endocrine PharmacologyTreatment of Diabetes Mellitus
• 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 49
Endocrine PharmacologyTreatment of Diabetes Mellitus
• Hypoglycemia– Causes/Contributing Factors• Imbalance of exercise, meds and meals• Hypoglycemic unawareness
– Prevention• Education• Awareness• Preparedness