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HORMONES

Resmia A. Maulana
What is a hormone?

– A hormone is a chemical that is made by specialist cells,


usually within an endocrine gland, and it is released into
the bloodstream to send a message to another part of the
body. It is often referred to as a ‘chemical messenger’.
Hormones are found in all multicellular organisms and their
role is to provide an internal communication system
between cells located in distant parts of the body.
Hormones

– Anterior pituitary hormones-GH, corticotropin, TSH, FSH,


LH, prolactin
– Posterior pituitary hormones-ADH (vasopressin) and
oxytocin
– Adrenal cortex hormones—cortisol and aldosterone
– Thyroid hormones—T3 (triiodothyronine) and T4
(thyroxine)
Hormones

– Parathyroid hormone—PTH
– Ovarian hormones—estrogens and progesterone
– Testicular hormone—testosterone
– Placental hormones-chorionic gonadotropin, estrogen,
progesterone, human placental lactogen
Non-Endocrine Hormones

– Cholecystokinin
– Erythropoietin
– WBCs which produce cytokines
– Prostaglandins and leukotrienes
– Sometimes neoplasms
Hormone
Pharmacokinetics

– Three mechanisms
– Inactivated by liver and kidney enzymes
– Sometimes conjugated by the liver and excreted in bile or
urine
– Inactivated at receptor sites by enzymes
Hormonal Dysfunction

– Hypofunction-Type 1 diabetes, Addison’s

– Hyperfunction—Cushing’s, Grave’s, Gigantism


Hypothalamic and
Pituitary Hormones

– Hypothalamus releases inhibitory and releasing hormones


– Corticotropin releasing hormone—released during sleep.
Increased by vasopressin and decreased by somatostatin
– Growth-hormone releasing hormone—affected by
dopamine, norepinephrine, epinephrine, GABA,
acetylcholine and serotonin. Is blocked by somatostatin
Hypothalamic and
Pituitary Hormones

– Somatostatin decreases the release of growth hormone,


CCK, vasoactive intestinal peptide, TRH, others
– TRH causes release of TSH
– GRH (gonadotropin releasing hormone) causes release of
FSH and LH
– Prolactin-releasing factor active during lactation
– Prolactin inhibitory factor active at times other than
lactation
Anterior Pituitary
Hormones

– Two act directly on target organs—growth hormone and


prolactin
– Five act indirectly by stimulating target organs to produce
hormones:
– Corticotropin –ACTH
– TSH
– FSH
Anterior Pituitary
Hormones

– Luteinizing hormone—gonadotropin, maturation and


rupture of ovarian follicle; produces corpus luteum; in
men, affects Leydig’s cells and testosterone
– Melanocyte stimulating hormone
Posterior Pituitary
Hormones

– Antidiuretic hormone—vasopressin, affects renal tubules


to regulate water balance
– Oxytocin—uterine contractions and movement of milk
from breast glands to nipples
Hypothalamic Hormones

 Equivalent to GnRH
 Zoladex (goserelin)
 Vantas (histrelin)
 Lupron (leuprolide)
 Synarel (nafarelin)
 Initially stimulate LH and FSH with chronic administration,
inhibits stimulation
 Results in equivalent to castration in males and
menopause in women
 Cannot be given orally
Hypothalamic Hormones

– Octreotide- Sandostatin; pharmacologically similar to


somatostatin
– Use for acromegaly—reduces GH and insulin like growth
factor
– Useful in vasoactive intestinal peptide tumors
– AIDS
Anterior Pituitary
Hormones

– Cortrosyn (cosyntropin)—synthetic ACTH is used to test


for adrenal insufficiency; IV or IM
– Humatrope (growth hormone)-for growth failure,
Turner’s, renal failure growth retardation. Monitor
ephiphyses.
– Chorex (HCG)-luteinizing hormone. In men to evaluate
ability of Leydig’s (testosterone); Tx hypogonadism in
pituitary problems and in cryptorchidism
Anterior Pituitary
Hormones

– Ovidrel (HCG alpha) used w/ menotropins to induce


ovulation
– Pergonal (menotropins)-contains FSH and LH; obtained
from urine of menopausal women
– Somavert (pegvisomant)—GH receptor antagonist.
– Follistim (follitropin beta)—drug preparation of FSH used
sequentially with HCG
Posterior Pituitary
Hormones

– DDAVP (desmopressin) and Pitressin (vasopressin)—ADH;


used in neurogenic DI, hemostasis in Von Willebrand’s
– Pitocin (oxytocin)-induction of labor, control postpartum
bleeding
Abuse of Growth Hormone

– Does not increase muscle mass or strength greater than


seen with exercise alone
– Not indicated for anti-aging formula
– Adverse effects include—acromegaly, diabetes,
hypertension, increased risk of cardiovascular disease,
tumor growth and cancer
Corticosteroids

– Glucocorticoids or steroids
– Adrenal cortical secretion
– Corticotropin releasing
hormone>>corticotropin>>>>cortisol
– With stress, increase in norepi, epi and cortisol; negative
feedback system overruled
– Prototype is hydrocortisone
– Mineralocortocoid activity is intermediae in
hydrocortisone, prednisolone and low in newer agents
Effects of Glucocorticoids

 Increased glucose production


 Decreased cellular use of glucose 2ndary to decreased
effect of insulin
 Increased breakdown of protein into amino acids
 Decreased rate of protein formation
 Increased breakdown of adipose tissue
 Decreaed inflammatory response by decreasing
production of inflammatory chemicals, decreases
numbers of antibodies, #s of lymphocytes
Effects of Glucocorticoids

– Modifies vascular smooth muscle tone increasing pressor


effects of catecholamines
– Stimulates renal glucocorticoid and mineralocorticoid
receptors
– Can cause muscle atrophy
– Decrease bone formation, growth and increase bone
breakdown
– Opens airways
– Stabilize mast cells
– Decrease viscosity of gastric mucous
Mineralocorticoids

– Class of steroids affecting fluid and electrolyte balance


– Conserve sodium and eliminate potassium
– Controlled by kidney function/Renin-angiotensin system
– Inadequate secretion causes hyperkalemia, hyponatremia
and ECF deficit
– Excessive secretion causes hypokalemia, hypernatremia
and ECF excess
Adrenal Sex Hormones

– Male = androgens
– Female = estrogens and progesterone
– Are secreted by both sexes
– Secondary sexual characteristics in men
– Affect libido and hair growth in women; excessive amounts
can cause masculizing effects in women
Disorders of the Adrenal
Cortex

– Addison’s Disease
– Secondary adrenocortical insufficiency
– Cushing’s disease
– Hyperaldosteronism
Actions of Exogenous
Corticosteroids

 Inhibits arachidonic acid metabolism thus affecting


prostaglandins and leukotrienes
 Stabilizes biologic membranes also affecting
prostaglandins and leukotrienes
 Inhibits production of interleukin 1, TNF and other
cytokines
 Impairs phagocytosis—cells can’t move to injured site
 Impairs functioning of lymphocytes
 Inhibit growth of tissues thus delay wound healing
Indications for use of
steroids

– Allergic or hypersensitivity disorders


– Collagen disorders-lupus, scleroderma and periarteritis
– Dermatologic
– Endocrine disorders
– Inflammatory bowel disorders
– Neoplastic disease—suppress lymphocytes
– Neurologic disorders-cerebral edema, myasthenia gravis
Indications

– Asthma and COPD


– Arthritis—if three or fewer joint, can give joint injections;
no more than three per year
– Chemotherapy induced emesis—strong anti-emetic effect,
mechanism unknown. Usually give dose with serotonin
antagonist and Reglan.
Contraindications

– Systemic fungal infections


– Hypersensitivity
– Those at risk for infections
– Diabetes mellitus (be cautious)
– Peptic ulcer disease
– Heart failure
– Renal insufficiency (can accumulate and cause s/s of
hypercorticism)
Steroid Preparations

– Beconase-beclamethasone nasally
– Nasonex (mometasone)
– Celestone-(betamethasone) orally
– Decadron (dexamethasone) po or IM
– Hydrocortisone—IV, IM, rectally
– Solu-Medrol (methylprednisolone)—po, IM, IV
– Kenalog(triamcinolone)—IM or topical
– Florinef (fludrocortisone)*****mineralocorticoid
Contraindication

– Daily administration of 15-20mg of hydrocortisone or its


equivalent for 2 weeks suppresses the HPA axis
– MUST taper down
Thyroid and Antithyroid
Drugs

– Thyroid produces three hormones: thyroxine,


triidothyronine and calcitonin
– T3 more potent but with a shorter duration of action
– Production of thyroid hormones is dependent on iodine
and tyrosine (needed to form thyroglobulin)
– Control rate of cellular metabolism, linear growth, brain
function, dentition, bone development and neural
development
Physiologic Effects of
Thyroid Hormones

– Inhibition of pituitary release of TSH


– Increassesd fat metabolism
– Increased carbohydrate metabolism
– Increased heart rate, force of contraction and cardiac
output
– Increase rate of cellular metabolism and oxygen
consumption
Hypothyroidism

– Common causes include: Hashimoto’s thyroiditis,


secondary to treatment for hyperthyroidism
– Treatment with amiodarone, lithium or iodine preparations
– Congenital—cretinism
– Myxedema –can progress to coma
Signs and Symptoms of
hypothyroidism
 Bruising
 Decreased cardiac output
 Decreased heart rate
 Cardiomegaly
 ASHD
 Apathy, lethargy
 Forgetfulness
 Drowsiness
 Cold intolerance
 Constipation
 Fatigue
 Puffiness
 Increased susceptibility to infections
 Increased sensitivity to narcotics, barbiturates, anesthetics
Hyperthyroidism

– Excessive production of thyroid hormone


– Associated with Graves Disease, nodular goiter, thyroiditis,
overtreatment with thyroid drugs, pituitary adenoma or
thyroid cancer
– Subclinical=reduced TSH but normal T3/T4
Can result in osteoporosis
– Thyroid storm aka thyrotoxicosis
– Have been reported cases of iodine-induced
hyperthyroidism
Signs and Symptoms of
Hyperthyroidism
 Tachycardia
 Increased cardiac output
 Increased BP
 Dysrhythmias
 Heart failure
 Nervousness, restlessness, insomnia
 Heat intolerance
 Weight loss
 Diarrhea
 Weakness
 Tremors
 Amenorrhea
 Increased susceptibility to infection
 exophthalmos
Drugs for Hypothyroidism

– Prototype and drug of choice is Synthroid, Levothroid


(levothyroxine)
– Maximum absorption if taken on empty stomach
– Is T4
– TSH (0.5 to 4.2 microunits/L) desired level
– Goal is euthyroid with TSH level
– Most drugs given will have prolonged effect
– Lifelong therapy is indicated
Drugs for Hyperthyroidism

– Thioamide derivatives-- Propylthiouracil and methimazole.


Used before radioactive iodine therapy
– Results may not be apparent for 3 months or longer
Combination therapy
before Surgery

 Thioamide preparation to achieve euthyroid state


 Then Iodine preparations—Lugol’s and SSKI
 Iodine preparations may be used to reduce size and
vascularity of thyroid before surgery
 Can cause: goiter, hyperthyroidism, benefits are temporary
 Radioactive iodine cannot be used effectively for prolonged
time in those who have received iodine preparations
(insufficient uptake thereafter)
 OK TO GIVE THIOAMIDE THEN IODINE PREPARATION BUT
NOT IODINE THEN THIOAMIDE
Special Populations

– Thyroid disorders change metabolism of other drugs


– Children w/congenital hypothyroidism, tx should be
started within 6 weeks of birth
– Drug of choice is levothyroxine
– Monitor ht. and wt.
– If hyperthyroid, can use PTU or methimazole, discourage
radioactive iodine in children
Special Populations

– s/s of thyroid disorders may mimic other disorders in older


adults
– Thorough PE and diagnostic workup
– Levothyroxine is appropriate
– Start with small doses, may increase in small increments
monthly
– Monitor vitals closely
– For hyperthyroidism, use PTU or methimazole. May use
radioactive iodine.
– Thyrotoxicosis manage in intensive care
Thank You!

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