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Endocrine Agents

Drugs Affecting Endocrine System


A. Hypothalamic Hormone Agents
B. Pituitary Agents
C. Posterior Pituitary Hormones
D. Adrenocortical Agents
E. Thyroid Agents
F. Parathyroid Agents
G. Agents to Control Blood Glucose Level
• Therapeutic Actions and Indications
-Hypothalamic agents can inhibit or stimulate the release of hormones from the anterior pituitary using hormones or factors.
However, not all of these hormones are available for pharmacological use.
-not all of the hypothalamic hormones are used as pharmacological agents.
-Tesamorelin, is used to stimulate GH and its lipolytic effects helping to decrease the excess abdominal fat in HIV- infected patients
with lipodystrophy
-Agonists: Goselein,Histrelin, Leuprolide, and Nafarelin are analogues of GnRH.
-Antagonist: Degarelix and Ganirelix acetate a
• Pharmacokinetics
-these drugs are absorbed slowly when given IM , subcutaneously, or in depot form.
-they tend to have very long half-lives of days to weeks.
-Most of these drugs are secreted in the urine.
-Nafarelin is given in a nasal form.
• Contraindications and Cautions
- known hypersensitivity to any component of the drug
-pregnancy ad lactation
-renal impairment
-peripheral vascular disorders
-rhinitis
• Adverse Effects
--stimulation or blocking of regular hormone control.
-Agonist: can lead to increased release of sex hormones,leading to ovarian overstimulation, flushing,
increased temperature and appetite, and fluid retention.
-Antagonist: can lead to a decrease in female sex hormones, leading to lack of menstruation,fluid and
electrolyte changes,insomnia, and irritability.
• Nursing Considerations for Patients
-monitor for adverse effects
-periodic radiograph of the long bones
-monitoring for blood sugar levels and electrolytes
B. Pituitary Agents

1. Growth Hormone Agonists:


– Therapeutic Actions and Indications
- acceleration of wound healing, activation of immune cells, and action on the
central nervous system. As GHRH might function as a growth factor, we
examined effects of GHRH agonists on tumors.
-GH is responsible for linear skeletal growth, the of internal organs,protein
synthesis, and the stimulation of many other processes that are required for
normal growth
-Hypopituitarism -is seen in as GH deficiency, may occur as a result of
developmental abnormalities or congenital defects of the pituitary, circulatory
disturbances like hemorrhage,infarction,acute or chronic inflammation of the
pituitary and pituitary tumors.
-GH deficiency in children results in short stature (Dwarfism).
-Somatropin and Somatropin rDNA origin.
– Pharmacokinetics
-Somatropin is injected and reaches peak levels within 7 hours.
-excretion occurs through the urine and feces
-patients with liver or renal dysfunction may experience reduced clearance and
increased concentrations of the drug.
– Contraindications and Cautions
-Somatropin is contraindicated with any known allergy
-presence of closed epiphyses or with underlying cranial lesions
-abdominal surgery and acute illness
-caution in pregnancy and lactation
– Adverse Effects
-development of antibodies to GH
-sign of inflammation and autoimmune-type reactions: swelling and joint pain
– Nursing Considerations for Patients
-assess history of allergy ,height,weight,thyroid function tests,glocuse tolerance tests
and GH level
-Monitor patient response to the drug, adverse effects,teaching
-Monitor effectiveness of comfort measures and compliance with the regimen
2. Growth Hormone Antagonists:
– Therapeutic Actions and Indications
-GH antagonists block the action of GH at the GH receptor in the liver. GH is a protein. The substitution of one amino acid
converts endogenous GH into an antagonist.
-Somatostatin is an inhibitory factor released from the hypothalamus.
-it is not used to decrease GH levels
-analogues of Somatostatin, Ocreotide acetate and Lanreotide are considerably more potent in inhibiting GH release with
less of an inhibitory effect on insulin release.
-Bromocriptine, a semisynthetic ergot alkaloid, is a dopamine agonist frequently used to treat acromegaly.
-Lanreotide, which acts like somatostatin, is given as a monthly depot subcutaneous injection.
-Pegvisomant, is a GH analogue that was approved for the treatment of acromegaly in patients who do not respond to other
therapies.

– Pharmacokinetics
-Octreotide and Ianreotide must be admistered subcutaneously.
-Octreotide , rapidly absorbed and widely distributed throughout the body and metabolized in the tissues with about 30%
excreted unchanged in the urine.
-Lanreotide , a depot in the suncutaneous tissue and is slowly released into circulation with a half-life of 25 to 30 days.
-Bromocriptine - is administered orally and effectively absorbed from the GI tract.
-Pegvisomant - is given by subcutaneous injection and its slowly absorbed, reaching peak effects in 33 to 77 hours.
– Contraindications and Cautions
-Bromocriptine, should not used during pregnancy or lactation
-any known allergy
-caustiously used in the presence of any other endocrine disorders
– Adverse Effects
- GI complains
-Octreotide and Ianreotide have also been associated with the development of acute
cholecystitis, cholestatic jaundice, biliary tract obstruction and pancreatitis.
-Ianreotide is associated with changes in blood glucose level.
-Bromocriptine is also associated with GI disturbances.
– Nursing Considerations for Patients
-Assess history of allergy ,height,weight,orientation,affect and reflexes,thyroid function
tests,glocuse tolerance tests and GH level
-Monitor patient response to the drug, adverse effects,teaching ,
-Monitor effectiveness of comfort measures and compliance with the regimen
C. Posterior Pituitary Hormones
• Therapeutic Actions and Indications
- The posterior pituitary hormones, oxytocin and vasopressin (also known as antidiuretic hormone), regulate myometrial and myoepithelial
contractions in the female and water balance in both genders, respectively.
-Vasopressin (also called antidiuretic hormone) regulates the amount of water excreted by the kidneys and is therefore important in maintaining water
balance in the body.
-These activites reduce plasma osmolarity and increase blood volume.
• Pharmacokinetics
-Desmopressin -is available for oral ,IV,subcutaneous,and nasal administration
-Tolvaptan-is given orally,is readily absorbed, and has a half-life of 12 hours.
-Conivaptan-is given by continous IV infusion, the half-life of the drug is 5 hours
• Contraindications and Cautions
-any known allergy
-with severe renal dysfunction , vascular disease , asthma, and hyponatremia
-not used during pregnancy and lactation
• Adverse Effects
-Water intoxication (drowsiness,light-headededness,headache,coma,convulsions)
-Hangover effect: tremor , sweating, vertigo and headache
-Local reaction at injection sites
• Nursing Considerations for Patients
-Assess history of allergy ,height,weight,orientation,affect and reflexes,skin lessions
-Monitor patient fluid volume and patients with vascular disease for any sign of exacerbation
D. Adrenocortical Agents
1. Glucocorticoids
– Therapeutic Actions and Indications
-Glucocorticoids are powerful medicines that fight inflammation and work with your immune system to treat wide range of
health problems. Your body actually makes its own glucocorticoids.
- These hormones have many jobs, such as controlling how your cells use sugar and fat and curbing inflammation.
- Hydrocortisone ,Cortisone, and Prednisone
-indicated for the short-term treatment of many inflammatory disorders
– Pharmacokinetics
-Glucocorticoids inhibit many inflammation-associated molecules such as cytokines, chemokines, arachidonic acid
metabolites, and adhesion molecules. In contrast, anti-inflammatory mediators often are up-regulated by glucocorticoids.
-Beclomethasone and Flunisolide
-Betemethasone
-Bedesonide
-Cortisone
– Contraindications and Cautions
- any known allergy
-presence of acute infection and lactation
-Caution should be used in patients with diabettes, acute peptic ulcers, and with other endocrine disorders
– Adverse Effects
-Methylprednisolone is associated with increased toxicity
-children are at risk for growth retardation
-local inflammations and infections as well as burning and stinging
sensations
– Nursing Considerations for Patients
-Assess history of allergy ,height,weight,orientation
-use the minimal dose for the minimal amount of time
-taper doses when discontinuing from high doses or from long-term
therapy
-arrange for increased dose when the patient is under stress
-use alternate day maintenance therapy with short-acting drugs when
ever possible
2. Mineralocorticoids
– Therapeutic Actions and Indications
- Mineralocorticoids are a class of steroid hormones that regulate salt and water balances.
-Aldosterone is the primary mineralocorticoid.
-Mineralocorticoids promote sodium and potassium transport, usually followed by changes in water
balance. This function is essential to life.
-These drugs are indicated in combination with glucocorticoid for replacement therapy in primary and
secondary adrenal insufficiency
-indicated for the treatment of salt-wasting adrenogenital syndrome
– Pharmacokinetics
-these drugs are absorbed slowly and distributed throughout the body.
-they undergo hepatic metabolism to inactive forms
– Contraindications and Cautions
-known allergy
-with severe hypertension,heart failure, or cardiac disease
-lactation and pregnancy
-presence of any infection
-with high sodium intake
– Adverse Effects
-increased fluid volume seen with sodium and water retention
-possible hypokalemia

– Nursing Considerations for Patients


-Assess history of allergy ,height,weight,orientation
-use only in conjunction with appropriate glucocorticoid
- increase dose in timess of stress
-monitor for hypokalemia
- discontinue if signs of overdose
(like excessive
weightgain,edema,hypertension,cardiomegaly)
E. Thyroid Agents
1. Thyroid Hormones:
– Therapeutic Actions and Indications
-Thyroid hormone, in the form of triiodothyronine (T3), acts by modifying gene transcription in virtually all tissues to alter
rates of protein synthesis and substrate turnover.
- These actions are the net result of the presence of T3 and of multiple other factors that amplify or reduce its action
-these hormones replace the low or absent levels of natural thyroid hormone and supress the overproduction of TSH by
the pituitary
-Levothyroxine (Synthroid,Levoxyl,Levothyroid) -a synthetic salt of T4, is the most frequently used replacement hormone
-Desiccated thyroid (Armour thyroid,and others) is prepared from died animal thyroid glands and contains both T3 and T4
– Pharmacokinetics
-Oral absorption of thyroid hormone can be erratic (T4 up to 80%; T3 up to 95%) and decreases with age.
-The time for peak serum levels is 2-4 hours. The onset of action for oral administration is 3-5 days and 6-8 hours for IV
administration.
-These drugs are well absorbed from the GI tract and bound to serum proteins
-thyroid replacement therapy should not be discontinued during pregnancy
– Contraindications and Cautions
-any known allergy
-during acute thyrotoxicosis
-during acute myocardial infaction
- pregnancy and lactation
-hypoadrenal conditions
– Adverse Effects
-These side effects include rash, itching, abnormal hair loss, and fever.
-Less common side effects include nausea, swelling, heartburn, muscle and joint aches,
numbness, and headache.
– Nursing Considerations for Patients
-Assess history of allergy ,height,weight,orientation
-administer a single daily dose before breakfast each day
-administer with a full glass of water
-monitor periodically of the blood test of thyroid functions
2. Antithyroid Agents:
– Therapeutic Actions and Indications
-Antithyroid medications inhibit the formation and coupling of iodotyrosines in thyroglobulin. Because
these processes are necessary for thyroid hormone synthesis, this inhibition induces a gradual
reduction in thyroid hormone levels over 2-8 weeks or longer.
-Thioamides - lower thyroid hormone levels by preventing the formation of thyroid hormone in the
thyroid cells. These drugs are indicated fo the treatment of hyperthyroidism.
-Iodine Solutions- low doses of iodine are needed in the body for the formation of thyroid hormone. High
doses, block thyroid function.This drug is used to treat hyperthyroidism.

– Pharmacokinetics
-Antithyroid agents comprise a diverse group of substances used to reduce thyroid hormone synthesis
and/or secretion in treating hyperthyroidism, the most common cause of which is Graves' disease.
-Thioamides- these drugs are well absorbed from the GI tract and are then concentrated in the thyroid
gland. Methimazole has na onset of action of 30 and 40 minutes and peaks in about 60 minutes.
-Iodine solution- these drugs are rapidly absorbed from the GI tract and widely distributed throughout
the body fluids.
– Contraindications and Cautions
-any known allergy
-during preganncy and lactation
-pulmonary edema and tuberculosis
– Adverse Effects
-Thiomides: most commonly seen are
drowsiness,lethargy,bradycardia,nausea,skin rash and so on.
-Iodine solution: most common adverse effect is
hypothyroidism,iodism(metallic taste and burning in the mouth,sore
teeth and gums,diarrhea,cold symptoms and stomach upset, staining
of teeth, skin rash , and the development of goiter.)
– Nursing Considerations for Patients
-Assess history of allergy ,height,weight,orientation
-adminiter propylthiouracil 3 times a day, around the clock
-give iodine solution through a straw
-monitor patient receiving iodine solution for any of iodism
F. Parathyroid Agents
1. Antihypocalcemic Agents:
• Therapeutic Actions and Indications
-Antihypocalcemic agents are indicated for the following medical conditions: Management of hypocalcemia in
patients on chronic renal dialysis. Management of hypocalcemia associated with hypoparathyroidism and with
sustained systemic glucocorticoids therapy.
-vitamin D compounds regulate the absorption of calcium and phosphate from the small intestine,mineral
resorption in bone , and reabsorption of phosphate from the renal tubules.
• Pharmacokinetics
-Calcitriol , is well absorbed from the GI tract and widely distributed throughout the body. It is stored in the
liver,fat.muscle,skin, and bones. It has a half-life of approximately 5 to 8 hours and a duration of action of 3 to 5
days.
-Parathyroid hormone is given as a daily subcutaneous injection.
• Contraindications and Cautions
-any known allergy
-hypercalcemia or vitamin d toxicity
-history of renal stone
• Adverse Effects
-related to GI effects: metallic taste,nausea,vomoting,dry
mouth,constipation and anorexia.
-CNS effect
• Nursing Considerations for Patients
-Assess history of allergy ,height,weight,orientation
-Assess for hypercalcemia,vitamin toxicity,renal stone and pregnancy
and lactation.
-monitor serum calcium concentration
-arrange nutritional consultation if GI effects
2. Antihypercalcemic Agents:
• Therapeutic Actions and Indications
-Antihypercalcemic agents are drugs used to treat PRH excess or hypercalcemia.
-These agents include bisphosphonates and calcitonin salmon.
-These drugs act on the serum levels of calcium and do not suppress the parathyroid gland
or PTH.
-Bisphosphonates, act to slow or block bone resorption by doing this they help to lower
serum calcium levels but they do not inhibit normal bone formation and mineralization.
- Bisphosphonates drugs are used to treat Paget’s disease and of postmenopausal
osteoporosis in women and Alendronate is also used to treat osteoporosis in men.
-Calcitonin, are hormones secreted by the thyroid gland to balance the effects of PTH.This
hormone inhibits bone resorption.
• Pharmacokinetics
-Bisphosphonates-these drugs are well absorbed from the small intestine and do not
undergo metabolism.
-Calcitonin- these drugs are metabolized in the body tissue to inactive fragments, which are
excreted by the kidney.
• Contraindications and Cautions
-Bisphosphonates-not be used in the presence of
hypocalcemia,history of allergy,during pregnancylactation
-Calcitonin-can be used in pregnancy only if benefits to the mother
clearly outweights, not be used in lactation,known allergy,renal
dysfunction or pernicious anemia
• Adverse Effects
-Bisphosphonates’commnly seen are headache,nausea,and diarrhea
-Calcitonin commonly seen are flushing of the face and hands. skin
rash,nausea and vomiting, urinary frequency and local inflammation
• Nursing Considerations for Patients
-Assess history of allergy ,height,weight,orientation
-ensure adequate hydration
-arrange for concominant vitamin D, calcium supplements, and
hormone replacement theray
-rotate injection sites
G. Agents to Control Blood Glucose Level

1. Insulin:
– Therapeutic Actions and Indications
-Insulin therapy is indicated in patients with newly diagnosed diabetes and severe hyperglycemia
(plasma glucose level greater than 250 mg per dL), recent significant weight loss, and ketonuria.
– Pharmacokinetics
-The pharmacokinetics of insulin comprise the absorption process, the distribution including binding to
circulating insulin antibodies, if present, and to insulin receptors, and its ultimate degradation and
excretion.
- The distribution and metabolism of absorbed insulin follow that of endogenous insulin.
-At a cellular level in most tissues, insulin degradation is initiated by the hormone binding to specific
receptors.
-The hormone-receptor complex is processed, including internalization and degradation of at least
some of the hormone-receptor complexes.
– Contraindications and Cautions
- episodes of hypoglycemia
-insulin does not cross the placenta
-insulin does enter breast milk
– Adverse Effects
- initial weight gain as the cells start to take in glucose ,blood sugar that drops
too low , or hypoglycemia, rashes, bumps, or swelling at an injection site.
-hypoglycemia and ketoacidosis
-lipodystrophy
-cough and throat pain or irritations
– Nursing Considerations for Patients
-Assess for contraindications or cautions
-any known to allergy
-Assess for history of ashma and COPD
-assess for any sign of skin lessions and nutritional intake
-obtain blood glucose levels as ordered and monitor results
-ensure pt is following a dietary and exercise regimen
-monitor for sign of hypoglycemia
-use caution in mixing types of insulin
-store insulin in a cool place away from the direct sunlight
-monitor pt sensory losses
2. Sulfonylureas:
– Therapeutic Actions and Indications
-These drugs exert their hypoglycaemic effects by stimulating insulin
secretion from the pancreatic beta-cell.
-Their primary mechanism of action is to close ATP-sensitive K-
channels in the beta-cell plasma membrane, and so initiate a chain of
events which results in insulin release.
-type II diabetes, a drug of choice for patients where metformin is
contraindicated (or who cannot tolerate metformin) can be added in
combination with other hypoglycemic drugs or insulin.
-Chlorpropamide
– Pharmacokinetics
-Sulfonylureas are structurally related to sulfonamide antimicrobials.
-They are absorbed rapidly (although the rate of absorption is reduced
when taken with food), are highly protein-bound and are metabolised
– Contraindications and Cautions
-Contraindications to the use of sulfonylureas include hypersensitivity
to sulfonylureas and drugs that have similar structures (see earlier)
and pregnancy.
-Caution should be exercised in cases of reduced renal or hepatic
function. Patients with ketoacidosis should receive insulin, not an oral
antihyperglycemic agent.
-these drugs are not for use during pregnancy and lactation
– Adverse Effects
-What is the major adverse effect of the sulfonylureas?
-Sulfonylureas are usually well tolerated.
-The most common side effect is hypoglycemia, more common with
long-acting sulfonylureas such as chlorpropamide and glibenclamide .
However, all sulfonylureas may cause hypoglycemia, usually due to
an excessive dosage.
3. Other Antidiabetic Agents:
– Common antidiabetic agents include:
-alpha-glucosidase inhibitors (acarbose, miglitol)
-amylin analogs (pramlintide)
-dipeptidyl peptidase 4 inhibitors (alogliptan, linagliptan,
saxagliptin, sitagliptin)
-incretin mimetics (albiglutide, dulaglutide, exenatide, liraglutide,
lixisenatide)
-insulin.
4. Glucose-Elevating Agents:
– Therapeutic Actions and Indications
-Glucose-elevating agents are indicated for the following medical conditions:
Diazoxide is an oral management of hypoglycemia; intravenous use for
management of severe hypertension.
-Glucagon is used to counteract severe hypoglycemic reactions.
– Pharmacokinetics
-Glucose-elevating agents raise blood level of glucose when severe
hypoglycemia occurs at <40 mg/dL.
-The desired and beneficial action of glucose-elevating agents is increasing
blood glucose by decreasing insulin release and accelerating the breakdown of
glycogen in the liver to release glucose.
– Contraindications and Cautions
-Diazoxide is contraindicated with known allergies to sulfonamides or thiazides.
-Pregnancy and lactation.
– Adverse Effects
-Glucagon is associated with GI upset, nausea, and vomiting.
-Diazoxide is associated with vascular effects, including
hypotension, headache, cerebral ischemia, weakness, heart
failure, and arrhythmias.
References:

• Karch, A. M., & Karch. (2011). Focus on nursing


pharmacology. Wolters Kluwer Health/Lippincott Williams
& Wilkins.

• Katzung, B. G. (2017). Basic and clinical pharmacology.


McGraw-Hill Education.

• Gersch,C.(2017).Pharmacology Made Incredibly


Easy.Wolters Kluwer Health/Lippincott Williams & Wilkins.

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