Pharma Mod 13 PDF - C-NCM 106 Pharmacology - University of the Assumption - AY 2024-2025

COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Module 13: Drugs Affecting the Endocrine System...

COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Module 13: Drugs Affecting the Endocrine System Time Frame: Three (3hours) BSN 2 ABCD Mapped Learning Outcomes and Course Content for C-NCM 106 Pharmacology, Module 13 Target Learning Outcomes Content and Activities Hour (At the close of the period allotted, Online Session Offline Session students should have :) 3hours 1. Describe the physiology of the A. Overview of the Endocrine Self – directed Learning endocrine system particularly System Activities: on the effects of the hormones B. Pituitary, Thyroid, that are secreted by the organs. Parathyroid, and Adrenal 2. Discuss the salient information Disorders and Drugs NOTE: Rubrics provided at related the drugs that affects C. Antidiabetic Agents the end of the module. the endocrine system. 3. Identify the nursing responsibilities before, during and after the administration of the medication. 4. Apply the information learned from the module in answering the case scenario. 1. Content / Discussion / Learning Resources / Link A. Overview of the Endocrine System Ø Consists of ductless glands that secrete hormones into the bloodstream. Ø Hormones è chemical substances synthesized from amino acids and cholesterol that act on body tissues and organs and affect cellular activity. Ø Two categories a.) Steroids Hormones from the adrenal glands (adrenal cortex) Sex hormones are classified as steroids b.) Proteins or protein derivatives All other hormones except from the above mentioned Ø Hypothalamus links the endocrine system with the nervous system to maintain homeostasis in the body by producing, releasing, and inhibiting hormones; these hormones control the production of other hormones throughout the body Ø The action of the glands is mostly regulated by a negative feedback loop. Faculty: David Merrick B. Soriano, RN Page 1 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Major Organs 1. Pituitary Gland (Hypophysis) Located at the base of the brain Master gland because it secretes hormones that stimulate the release of most other hormones. Two Lobes Anterior Pituitary Gland (adenohypophysis) Ø Amount of each hormone secreted from the anterior pituitary gland is regulated by a negative feedback system. Ø If excess hormone is secreted from the target gland, hormonal release from the anterior pituitary gland is suppressed. Ø If there is a lack of hormone secretion from the target gland, there will be an increase in that particular anterior pituitary hormone Thyroid-Stimulating Hormone Secreted anterior pituitary gland in response to thyroid-releasing hormone (TRH) from the hypothalamus. TSH, or thyrotropic hormone, stimulates the release of triiodothyronine (T3) and thyroxine (T4) from the thyroid gland Adrenocorticotropic Hormone Secretion of ACTH occurs in response to corticotropin-releasing hormone (CRH) from the hypothalamus. ACTH from the anterior pituitary gland stimulates the release of glucocorticoids (cortisol), mineralocorticoids (aldosterone), and androgen from the adrenal cortex (adrenal glands). Elevated serum hormone levels from the adrenal cortex inhibit ACTH and CRH release. Faculty: David Merrick B. Soriano, RN Page 2 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 When the hormone level is low, ACTH secretion is stimulated, which in turn stimulates the adrenal glands (adrenal cortex and adrenal medulla) to release more of its hormones: cortisol, aldosterone, catecholamines, and androgens (sex hormones). Gonadotropic Hormones The gonadotropic hormones regulate hormone secretion from the ovaries and testes (the gonads). The anterior pituitary gland secretes the gonadotropic hormones FSH, LH, and PRL. FSH promotes the maturation of follicles in the ovaries and initiates sperm production in the testes. LH combines with FSH in follicle maturation and estrogen production and promotes secretion of testosterone from the testes. PRL stimulates milk formation in the glandular breast tissue after childbirth. Growth Hormone GH, or somatotropic hormone (STH), acts on all body tissues, particularly the bones and skeletal muscles. The amount of GH secreted is regulated by GH-releasing hormone (GH-RH) and GH inhibiting hormone (GH-IH, or somatostatin) from the hypothalamus. Sympathomimetics, serotonin, and glucocorticoids can inhibit the secretion of GH. Prolactin Necessary for breast milk production. Posterior Pituitary Gland (neurohypophysis) Ø Secretes ADH (vasopressin) and oxytocin Ø Interconnecting nerve fibers (the pituitary stalk) between the hypothalamus and the posterior pituitary gland allow ADH and oxytocin to be synthesized in the hypothalamus and stored in the posterior pituitary gland. Ø ADH increases the reabsorption of water from the renal tubules, returning it to the systemic circulation Ø Secretion of ADH is regulated by the serum osmolality (concentration of the vascular fluid). Ø é Serum osmolalityè é release of ADH from the posterior pituitary gland; more water is then reabsorbed from the renal tubules to dilute the vascular fluid (excess ADH è fluid overload in vascular system) Ø ê Serum osmolality è ê the release of ADH, promoting more water excretion (é urine formation) from the renal tubules. Ø Oxytocin stimulates contraction of the smooth muscle of the uterus; 2. Thyroid Gland Secretes three hormones, triiodothyronine (T3), thyroxine (T4), and to a lesser extent calcitonin T3 and T4 affect nearly every tissue and organ by controlling their metabolic rate and activity. Calcitonin helps with the regulation of serum calcium levels, opposes the action of parathyroid gland é T3 and T4 levels result è é in cardiac output, oxygen consumption, carbohydrate use, protein synthesis, and breakdown of fat (lipolysis) Thyroid hormone levels in the blood are regulated by negative feedback Anterior pituitary gland secretes TSH, which stimulates the thyroid gland to produce T3, T4, calcitonin Faculty: David Merrick B. Soriano, RN Page 3 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 é Amount of circulating thyroid hormones suppresses the release of TSH, and ê amount increases the release of TSH by the adenohypophysis 3. Parathyroid Glands Parathyroid glands secrete parathormone, or parathyroid hormone (PTH), which regulates calcium levels in the blood. A decrease in serum calcium stimulates the release of PTH, and PTH increases calcium levels Calcitonin, a hormone produced primarily by the thyroid gland and to a lesser extent by the parathyroid and thymus glands, inhibits calcium reabsorption by bone and increases renal excretion of calcium. Calcitonin counteracts the action of PTH. 4. Adrenal Glands Located at the top of each kidney and consist of two separate sections: a.) adrenal medulla (inner section) and adrenal cortex (section that surrounds the adrenal medulla) Releases the catecholamines, epinephrine and norepinephrine, and is linked with the SNS. Adrenal cortex produces two major types of hormones (corticosteroids), glucocorticoids and mineralocorticoids Principal glucocorticoid is cortisol, and the principal mineralocorticoid is aldosterone. The adrenal cortex also produces small amounts of androgen, estrogen, and progestin. 5. Pancreas The pancreas, located to the left of and behind the stomach, is both an exocrine and an endocrine gland. The exocrine section of the pancreas secretes digestive enzymes into the duodenum The endocrine section has cell clusters called islets of Langerhans. Alpha islet cells produce glucagon, which breaks glycogen down to glucose in the liver Beta cells secrete insulin, which regulates glucose metabolism Insulin, an antidiabetic agent, is used to control diabetes mellitus B. Pituitary, Thyroid, Parathyroid, and Adrenal Disorders and Drugs PITUITARY GLAND ***ANTERIOR PITURITARY GLAND a.) Growth Hormone 1. Drug Therapy: Growth Hormone Deficiency Somatropin o Growth hormone used to treat growth failure in children because of GH deficiency o Product that has the identical amino acid sequence as human growth hormone (HGH) o Contraindication: pediatric patients who have growth deficiency due to Prader-Willi syndrome, severely obese, severe respiratory impairment (death may occur) o Drug interaction: Faculty: David Merrick B. Soriano, RN Page 4 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 a.) Corticosteroids can inhibit the effects of somatropin è NOT be taken concurrently b.) Enhance the effects of antidiabetics and can cause hypoglycemia. o Side effects: paresthesia, arthralgia, myalgia, peripheral edema, weakness, cephalgia, flulike symptoms and hyperpigmentation of skin o Adverse reactions: seizures, intracranial hypertension, and secondary malignancy (e.g., leukemia) o Metabolic complications: glucose fluctuations, hypothyroidism, and hematuria 2. Drug Therapy: Growth Hormone Excess ² Gigantism, excessive growth during childhood, and acromegaly, excessive growth after puberty ² If the tumor cannot be destroyed by radiation, the following maybe given: a.) GH receptor antagonists (e.g., pegvisomant) b.) Somatostatin analogues (e.g., lanreotide, octreotide) c.) Dopamine agonists (e.g., bromocriptine) ² Mechanism of action: act by either blocking GH receptor sites or by inhibiting secretion of GH Pegvisomant o Blocks GH receptor sites è preventing abnormal growth by normalizing insulin-like growth factor 1 (IGF-1) level o Side effects: hyperhidrosis, cephalgia, and fatigue o Adverse effects: chest pain, hypertension, and elevated hepatic transaminases. Lanreotide o Analogue of somatostatin that has actions similar to those of endogenous somatostatin o Effects of reduced GH are dose related, duration of at least 28 days after a single injection, injections given every 4 weeks o Available in depot formulation and is administered deep in the subcutaneous layer CTTO: https://pharmacy.nirmauni.ac.in/wp-content/uploads/sites/17/2019/04/Parenteral-Depot-Formulation-1.jpg o Common side effects: mild GI symptoms è diarrhea, abdominal pain, nausea, vomiting, constipation, weight loss, and flatulence. Octreotide o Synthetic somatostatin-inhibiting secretion of GH o It is available in immediate release (given TID SQ) and depot formulations (given once monthly) o Common side effects: GI upsets such as nausea, bloating, and flatus o Adverse effects: cardiac toxicity, such as bradycardia and arrhythmia Bromocriptine o Dopamine agonist, inhibits the secretion of GH caused by pituitary adenomas o Available in oral form; fewer side effects: GI symptoms (e.g., nausea, anorexia, dyspepsia, and xerostomia) Faculty: David Merrick B. Soriano, RN Page 5 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 o Adverse effects: cardiac toxicity (e.g., hypertension, myocardial infarction [MI], and angina) and cerebrovascular toxicity (e.g., stroke and seizure) o Discontinued if hypertension occurs due to pregnancy (e.g., preeclampsia, eclampsia, or pregnancy- induced hypertension) b.) Thyroid Stimulating Hormone ² TSH stimulates the thyroid gland to release thyroxine (T4) and triiodothyronine (T3, or liothyronine). ² Excess TSH secretion àhyperthyroidism, TSH deficit à hypothyroidism Thyrotropin o Purified extract of TSH for thyroid cancer o Indication: diagnostic agent to differentiate between primary and secondary hypothyroidism o Side effects: symptoms of hyperthyroidism, urticaria, rash, pruritus, and flushing. c.) Adrenocorticotropic Hormone ² ACTH and cortisol secretion is higher in the early morning and then decreases throughout the day. ² Hypocortisolism, or adrenal insufficiency, can occur and may be due to inadequate secretion of ACTH or dysfunction of the adrenal glands. Cosyntropin (synthetic ACTH) o Administered to establish the endocrine gland responsible for the inadequate serum cortisol o Only approved for diagnostic purposes and is less potent and less allergenic than corticotropin o Mechanism of action: stimulates the production and release of cortisol, corticosterone, and androgens from the adrenal cortex. o Administered via IM or intravenous (IV) routes o Plasma cortisol concentrations should be measured just before (basal) and 30 to 60 minutes after administration; normal response is the doubling of the basal cortisol level o Caution: administering cosyntropin in patients receiving diuretics (increase electrolyte loss) o Drug interaction: estrogens can have an abnormal decreased response to the ACTH stimulation test o Side effects and adverse effects: bradycardia, hypertension, sinus tachycardia, and peripheral edema. Corticotropin (exogenous ACTH) o Indication: diagnose adrenal gland disorders, treat multiple sclerosis (MS), and treat infantile spasms; it is rarely used for corticosteroid-responsive disorders o Available as repository corticotropin injection (RCI); administered via IM or SQ o Mechanism of action: controls the synthesis of ACTH from cholesterol, which stimulates adrenal glands in releasing its hormones; effects of RCI are primarily due to the glucocorticoid from the adrenal cortex o Decreases the symptoms of MS during its exacerbation phase o Tapered over a 2-week period for infantile spasms to avoid adrenal insufficiency o Drug interaction: o Diuretics and anti-Pseudomonas penicillins, such as piperacillin à ê the serum potassium level o If the patient is taking a digitalis preparation and hypokalemia is present, digitalis toxicity can result. o Phenytoin, rifampin, and barbiturates é the metabolic rate, which can ê the effect of the ACTH drug. ² DM may need increased insulin and oral antidiabetic (hypoglycemic) drugs because ACTH stimulates cortisol secretion, which increases the blood glucose level Faculty: David Merrick B. Soriano, RN Page 6 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 d. Prolactin ² PRL deficiency (hypoprolactinemia) is generally without symptoms except during breastfeeding ² Excess PRL (hyperprolactinemia) produces symptoms in both males and females. ² Males may develop excess breast tissue (gynecomastia) and may lactate (galactorrhea), and excess PRL decreases sperm production. ² Females with excess PRL can experience lactation that is not pregnancy related, or they can develop amenorrhea ² Excess PRL can be treated with dopamine agonists (e.g., bromocriptine, cabergoline). ² Cabergoline à better tolerated, longer half-life, and offers more convenient dosing ***POSTERIOR LOBE ² Secretes antidiuretic hormone (ADH) and oxytocin. ² ADH promotes water reabsorption from the renal tubules to maintain water balance in the body fluids ² Deficiency of ADH, large amounts of water are excreted by the kidneys è Diabetes insipidus ² Management: monitoring of fluid and electrolyte balance and ADH replacement ² Example: vasopressin and desmopressin acetate Desmopressin o Indication: bleeding disorders due to hemophilia A or von Willebrand disease type 1 o Does not induce the release of ACTH, nor does it increase serum cortisol level o Available as a nasal spray, oral tablet, and in parenteral formulation o Contraindication: moderate to severe renal disease, hyponatremia o Side effects and adverse reaction: hyponatremia, cephalgia, dyspepsia, diarrhea, nausea, and vomiting, seizures related to hyponatremia, hypotension and tachycardia can occur due to hypovolemia ² Excessive secretion of ADH à most common cause is small cell carcinoma of the lung, other malignancies, and stressors (e.g., pain, infection, anxiety, trauma) à excessive amount of water retention expanding the intracellular and intravascular volume known as syndrome of inappropriate antidiuretic hormone (SIADH) ² é fluid volume causes enhanced glomerular filtration and decreased tubular sodium reabsorption ² Natriuresis, excretion of urinary sodium, can occur and can cause hyponatremia. ² Management: fluid restrictions, hypertonic saline, drugs such as demeclocycline, conivaptan, and tolvaptan Demeclocycline o Tetracycline antibiotic that can induce nephrogenic DI within 5 days of starting treatment that is reversed in 2 to 6 days following cessation of treatment o Most common complaint: photosensitivity, dental discoloration and enamel hypoplasia Vaptans (e.g., conivaptan and tolvaptan) o Vasopressin receptor antagonists o Indication: treatment of euvolemic hyponatremia in SIADH o Its effects increase serum sodium and free water clearance. o Conivaptan is contraindicated in patients with corn allergy o Complications: injection site reactions (phlebitis, pain, edema, and pruritus) à administered only in large veins, and rotation of infusion sites every 24 hours o Side effects and adverse reactions: orthostatic hypotension, syncope, hypertension, atrial fibrillation, and electrolyte imbalances. o Tolvaptan given PO o Black-box warnings for patients with alcoholism, hepatic disease, and malnutrition (avoided) Faculty: David Merrick B. Soriano, RN Page 7 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 o Common side effects and adverse reactions: related to loss of fluids (e.g., thirst, dry mouth, constipation, hyperglycemia, dizziness, and weakness) à monitor fluid and serum electrolytes o Contraindications of vaptans: hypovolemia o Fluid restrictions should be avoided during therapy to prevent too rapid an increase in serum sodium THYROID GLAND ² 3 Hormones produced and secreted by the thyroid gland are triiodothyronine (T3), thyroxine (T4) that helps with metabolism, and to a lesser extent calcitonin for regulating serum calcium. ² A majority of thyroid hormone is synthesized as T4, which is then converted to T3 to act on target cells. ² Iodide, an inorganic form of iodine, is needed for the synthesis of T3 and T4. ² These are carried in the blood by thyroxine-binding globulin (TBG) and albumin, which protect the hormones from being degraded. ² T3 is more potent than T4, and only unbound (free) T3 and T4 have biologic actions and produce a hormonal response ² Negative feedback mechanisms regulate hormone secretion from the thyroid gland. ² Hypothalamus releases thyrotropin-releasing hormone (TRH), which stimulates the release of TSH from the pituitary gland. TSH stimulates the synthesis and release of T3 and T4 from the thyroid gland. ² Excess free T3 and T4 è ê TRH and TSH secretion. ² Too low of an amount of T3 and T4 è é TRH and TSH secretion. Hypothyroidism ê T4 and é TSH levels indicate primary hypothyroidism; the causes of which are acute or chronic inflammation of the thyroid gland, radioiodine therapy, excess intake of antithyroid drugs, or surgical removal of the thyroid gland. Myxedema è severe hypothyroidism in the adult In children, congenital onset that can cause delayed physical and mental growth (cretinism) or onset may be prepubertal (juvenile hypothyroidism). Drugs that contain T3 and T4, alone or in combination, are used to treat hypothyroidism Exogenous thyroid hormones are contraindicated in patients with thyrotoxicosis, acute myocardial infarction (AMI), and adrenal insufficiency Because thyroid hormones are catabolized by the hepatic system, drugs with hepatic enzyme–inducing properties (e.g., carbamazepine, hydantoins, rifabutin) should be used with caution Thyroid Drugs Levothyroxine sodium o Drug of choice for replacement therapy for the treatment of primary hypothyroidism o Mechanism of action: increases the levels of T4 and metabolically is deiodinated to T3 o Indication: treat simple goiter and chronic lymphocytic (Hashimoto) thyroiditis Liothyronine o Synthetic T3 with a biologic t1/2 of 2.5 days with rapid onset of action (within a few hours) o Indication: replacement or supplemental treatment for hypothyroidism of any etiology o Does not need to be deiodinated, which increases the availability for use by the body tissues o Better absorbed from the GI tract (over 95%) than levothyroxine Faculty: David Merrick B. Soriano, RN Page 8 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 o Rapid onset of action and short half-life, it is frequently used as initial therapy for treating myxedema o Route of administration: PO or IV Desiccated thyroid o Naturally occurring thyroid hormone from porcine thyroid glands o Contains both levothyroxine and liothyronine o Indication: used to treat hypothyroidism due to thyroid atrophy, thyroid hormone deficiency, and goiter o Liotrix is a mixture of levothyroxine sodium and liothyronine sodium in a 4-to-1 ratio by weight, Hyperthyroidism é in circulating T3 and T4 levels, which usually results from an overactive thyroid gland or excessive output of thyroid hormones from one or more thyroid nodules Grave’s disease, or thyrotoxicosic è caused by hyperfunction of the thyroid gland Management: surgical removal of a portion of the thyroid gland (subtotal thyroidectomy), radioactive iodine therapy, or antithyroid drugs, which inhibit either synthesis or release of thyroid hormone. Any of these treatments can cause hypothyroidism. Propranol è block beta receptors that can control cardiac symptoms that result from hyperthyroidism, such as palpitations and tachycardia Antithyroid Drugs Purpose: reduce the excessive secretion of thyroid hormones by inhibiting thyroid secretion The use of surgery (subtotal thyroidectomy) and radioiodine therapy frequently leads to permanent hypothyroidism; these patients will need to be on thyroid replacement therapy Thiourea derivatives (thioamides) Drugs of choice used to decrease thyroid hormone production Mechanism of action: interferes with synthesis of thyroid hormone; do not destroy thyroid tissue, rather they block thyroid action Examples: Propylthiouracil (PTU) and methimazole Indication: control overactive thyroid due to Grave’s disease, toxic nodular goiter, or multinodular goiter; they are also used prior to radioiodine treatment or thyroid surgery Drug Interactions a.) With oral anticoagulants (e.g., warfarin), they can cause an increase in the anticoagulation effect b.) Thyroid drugs decrease the effect of insulin and oral antidiabetics; c.) Digoxin and lithium increase the action of thyroid drugs d.) Phenytoin increases serum T3 level. Methimazole o Does not inhibit peripheral conversion of T4 to T3 as does PTU o 10 times more potent; longer half-life than PTU; euthyroid state is achieved in 2 to 4 months. o Preferred antithyroid because of the less severe side effects o Rapidly absorbed from the GI tract o Prolonged use of thioamides may cause goiter related to é TSH secretion and inhibited T4 and T3 synthesis PARATHYROID GLANDS Secrete parathyroid hormone (PTH), or parathormone, which regulates serum calcium levels a.) It enhances the release of calcium from the bones. b.) It enhances calcium reabsorption in the renal tubules. c.) It enhances calcium absorption in the intestines by increasing the production of activated vitamin D Faculty: David Merrick B. Soriano, RN Page 9 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 A decrease (negative feedback) in serum calcium stimulates the release of PTH Calcitonin, one of three thyroid hormones, decreases serum calcium levels by promoting osteoclast activity in bones and calcium excretion by the kidneys and intestines. PTH deficiencyè use of PTH analogues Hyperparathyroidism è surgical removal (parathyroidectomy) Calcimimetic drugs, which mimic calcium in the blood, prevent the parathyroid gland from releasing PTH Hypoparathyroidism The action of PTH is to promote calcium absorption from the GI tract, promote reabsorption of calcium from the renal tubules, and activate vitamin D. Calcitriol o Vitamin D analogue that promotes calcium absorption from the GI tract and promotes secretion of calcium from bone to the bloodstream. Hyperparathyroidism Partial or full parathyroidectomy is the most common treatment for primary hyperparathyroidism. Calcitonin-salmon o Prevents bone loss and fractures, increases bone density, and alleviates pain due to fractures and bone metastasis o Not as effective as other drugs for hyperparathyroidism o Contraindication: patients with allergy to fish o Side effects: allergic reactions, GI symptoms (e.g., nausea and vomiting), cephalgia, and hypocalcemia o Adverse reactions due to severe hypocalcemia (e.g., tetany and seizures) can also occur Cinacalcet o Calcimimetics o Indication: patients with hyperparathyroidism due to chronic renal disease and parathyroid cancer, unable to undergo parathyroidectomy o Mechanism of action: mimics calcium in circulation, increasing the sensitivity of the calcium-sensing receptors of the cells of the parathyroid gland, thereby reducing PTH secretion è ê serum calcium è slows the progression of bone disease o Contraindication: hypocalcemia Bisphosphonates (e.g., alendronate, etidronate, ibandronate, and risedronate) o Mechanism of action: block osteoclast activities, thereby inhibiting mineralization or resorption of the bone, which may lessen osteoporosis caused by hyperparathyroidism o Prior to treatment bone mineral density measurements, serum calcium concentration is obtained at baseline and periodically thereafter and hypocalcemia must be corrected o Adequate intake of calcium and vitamin D is essential during therapy o Contraindication: patients who are unable to sit or stand upright for at least 30 minutes after administration or who have esophageal strictures o During therapy, transient hypocalcemia and hypophosphatemia can occur o Side effects include abdominal and musculoskeletal pain, GI upsets, hypotension, and fever. ADRENAL GLANDS Adrenal cortex produces two types of steroid hormones, glucocorticoids (cortisol) and mineralocorticoids (aldosterone), and to a lesser extent the adrenal androgens and estrogens. ê Serum steroid levels (hypocortisolism) é corticotropin-releasing factor (CRF) and ACTH secretions from the hypothalamus and anterior pituitary gland, respectively; stimulate the adrenal glands to secrete and release steroids Faculty: David Merrick B. Soriano, RN Page 10 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 é serum steroid level (hypercortisolism) inhibits the HPA axis, resulting in fewer steroids being released. Adrenal hyposecretion (Addison disease) è decrease in steroid Adrenal hypersecretion (Cushing syndrome) è increase in steroid secretion Patient Safety Do not confuse… Calcitonin with calcitriol or calcium Levothyroxine with liothyronine Somatropin with somatostatin or sandostatin Glucocorticoids Most potent natural cortisol produced by the body and influenced by ACTH Indications for glucocorticoid therapy: trauma, surgery, inflammation, emotional upsets, and anxiety Most cortisone drugs are synthetically produced. Administered deep IM, SQ is NOT recommended Indications: a.) Inflammatory conditions è autoimmune disorders (MS, rheumatoid arthritis, myasthenia gravis); ulcerative colitis; glomerulonephritis; shock; ocular and vascular inflammation; polyarteritis nodosa; and hepatitis b.) Allergic è asthma, drug reactions, contact dermatitis, and anaphylaxis c.) Debilitating conditions are mainly caused by malignancies d.) Organ transplant recipients may require glucocorticoids to prevent organ rejection. Dexamethasone o Indication: treatment of severe inflammatory responses that result from head trauma or allergic reactions o Potent glucocorticoid, interacts with many drugs a.) Phenytoin, theophylline, rifampin, barbiturates, and antacids decrease the action of dexamethasone, whereas estrogen and NSAIDs such as aspirin increase its action b.) Dexamethasone decreases the effects of oral antidiabetics Prednisone o An inexpensive glucocorticoid frequently prescribed Side effects and adverse reactions: result from high doses or prolonged use include increased blood glucose, abnormal fat deposits in the face and trunk (so-called moon face and buffalo hump), decreased extremity size, muscle wasting, edema, sodium and water retention, hypertension, euphoria or psychosis, thinned skin with purpura, increased intraocular pressure (glaucoma), peptic ulcers, and growth retardation. Long-term use of glucocorticoid drugs can cause adrenal atrophy (loss of adrenal gland function), severe muscle weakness Tapering of dose is needed to allow the adrenal cortex to produce cortisol and other corticosteroids Abrupt withdrawal of the drug can result in severe adrenocortical insufficiency. Drug Interactions a.) Glucocorticoids increase the potency of drugs taken concurrently, including aspirin and NSAIDs, thus increasing the risk of GI bleeding and ulceration b.) Use of potassium-wasting diuretics (e.g., furosemide) with glucocorticoids increases potassium loss, resulting in hypokalemia Faculty: David Merrick B. Soriano, RN Page 11 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 c.) Barbiturates, phenytoin, and rifampin decrease the effect of prednisone because they increase glucocorticoid metabolism. Larger doses of glucocorticoids may be required to achieve the desired effect. Glucocorticoids can increase blood glucose levels, so insulin or oral antidiabetic drug dosage may need to be increased. Drug interaction: a.) With diuretics or anti-Pseudomonas penicillin preparations, the serum potassium level may decrease b.) Herbal products like cascara sagrada, yellow dock, and licorice can potentiate the effects of corticosteroids, which can worsen potassium depletion. Mineralocorticoids Promote sodium retention and potassium and hydrogen excretion in the renal tubules. Primary mineralocorticoid is aldosterone which is controlled by the renin-angiotensin-aldosterone system When hypovolemia (a decrease in circulating fluid) occurs, more aldosterone is secreted to increase sodium and water retention, thereby restoring fluid balance. With sodium reabsorption, potassium is lost and hypokalemia (potassium deficit) can occur. Some glucocorticoid drugs also contain mineralocorticoid properties: cortisone and hydrocortisone. Severe ê in the mineralocorticoid leads to hypotension and vascular collapse, as seen in Addison disease Mineralocorticoid deficiency usually occurs with glucocorticoid deficiency, frequently called corticosteroid deficiency. Fludrocortisone o Oral mineralocorticoid that can be given with a glucocorticoid o Mechanism of action: mimics the actions of endogenous aldosterone, facilitating sodium resorption and promoting hydrogen ion and potassium excretion o In larger doses, it can inhibit endogenous hormone secretions of adrenal cortex and pituitary gland, causing a negative nitrogen balance; therefore, a high-protein diet is usually indicated o Need to monitor potassium level since potassium is excreted o Other adverse effects: fluid imbalance, fluid overload, and hypertension (indicative of overdosage è discontinue then resume at lower dose) o Hypokalemia may cause metabolic alkalosis that can cause GI symptoms (nausea and vomiting), orthostatic hypotension, cardiac rhythm changes, weakness, anorexia, and myalgia C. Antidiabetic Ø Used primarily to control diabetes mellitus, a chronic disease that affects carbohydrate metabolism Ø Two groups: insulin and oral hypoglycemic (antidiabetic) drugs 1. Insulin è a protein secreted from the beta cells of the pancreas, is necessary for carbohydrate metabolism and plays an important role in protein and fat metabolism 2. Oral hypoglycemic drugs (oral antidiabetic drugs) Diabetes Mellitus Diabetes mellitus, a chronic disease that results from deficient glucose metabolism, is caused by insufficient insulin secretion from the beta cells. This results in high blood glucose (hyperglycemia); characterized by the three p’s: polyuria (increased urine output), polydipsia (increased thirst), and polyphagia (increased hunger) Faculty: David Merrick B. Soriano, RN Page 12 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Types of Diabetes Mellitus CTTO: https://www.scielo.br/img/revistas/abo/v71n6s0/18t1.gif Insulin Released from the beta cells of the islets of Langerhans in response to an increase in blood glucose Oral glucose load is more effective in raising the serum insulin level than an intravenous (IV) glucose load Insulin promotes the uptake of glucose, amino acids, and fatty acids and converts them to substances that are stored in body cells. Glucose is converted to glycogen in the liver and muscle for future glucose needs, thereby lowering the blood glucose level. Normal range for fasting blood glucose is 70 to 99 mg/dl Blood glucose level is > 180 mg/dL è glycosuria—glucose in the urine—can occur é blood glucose acts as an osmotic diuretic causing polyuria Blood glucose level that remains elevated (>200 mg/dL) è diabetes mellitus Hemoglobin A1c (HbA1c), a derivative of the interaction of glucose with hemoglobin in red blood cells (RBCs), is used for the diagnosis of diabetes à reflects blood glucose level for up to 3months Goal of treatment: keep the diabetic patient’s HbA1c below 7% Diagnostic purposes, an HbA1c level of 6.5% or greater indicates a diagnosis of diabetes mellitus. Commercially Prepared Insulin Early insulin preparations utilized pancreas tissue extracted from animals—either pigs or cattle. Insulins are currently manufactured biosynthetically using recombinant DNA technology. Human insulin duplicates insulin produced by the pancreas of the human body; examples of human insulin include Humulin R and Novolin N Use of human insulin has a low incidence of both allergic effects and insulin resistance Human insulin analogues are modifications of human insulin with alterations in onset and duration of action è examples: Insulin lispro and insulin aspart Insulins are usually administered SQ; abdominal injections are absorbed faster than those at other body sites and have been found to be more consistent Newly diagnosed patients with insulin-dependent diabetes are usually prescribed human insulin. Faculty: David Merrick B. Soriano, RN Page 13 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Patients in whom hyperglycemia develops during pregnancy or who already have diabetes and become pregnant are usually prescribed human insulin. Concentration of insulin is 100 units/mL or 500 units/mL (U100/mL or U500/mL, respectively), and the insulin is packaged in a 10-mL vial. Insulin in 500 units/mL is only available in short-acting regular insulin. Insulin in 500 units/mL is seldom used except in emergencies and for patients with serious insulin resistance (>200 U/day). Insulin syringes are typically marked in units of 100 U/mL or 50 U/0.5 mL for insulin U100. Insulin syringes must be used for accurate dosing. To prevent dosage errors, the nurse must be certain that there is a match of the insulin concentration with the calibration of units on the insulin syringe. Before use, the patient or nurse must roll—not shake—cloudy insulin bottles to ensure that the insulin and its ingredients are well mixed Shaking a bottle of insulin can cause bubbles, which can lead to an inaccurate dose. Insulin requirements vary; usually less insulin is needed with increased exercise, and more insulin is needed with infections and high fever. Administration of Insulin It is administered subcutaneously. 90- degrees angle is made by raising the skin and fatty tissue, and the insulin is injected into the pocket between the fat and the muscle. In a thin person with little fatty tissue, use 45- to 60-degree angle Regular insulin è ONLY type that can be administered intravenously. Site and depth of insulin injection affect absorption. Insulin absorption is greater when given in the abdomen than when given in the thigh or buttocks. Heat and massage could increase subcutaneous absorption, and cooling the subcutaneous area can decrease absorption Usually given in the morning before breakfast, and it can be given several times a day Insulin injection rotated to prevent LIPODYSTROPHy, TISSUE ATROPHY or HYPERTROPHY, which can interfere with insulin absorption. Lipoatrophy, tissue atrophy è depression under the skin surface that primarily occurs in women and children Lipohypertrophy, tissue hypertrophy è raised lump or knot on the skin surface; more common in men It is frequently caused by repeated injections into the same site. Develop a “site rotation pattern” to avoid lipodystrophy and to promote insulin absorption There are various insulin rotation programs, such as an 8-day rotation schedule in which insulin is given at a different site each day. The ADA suggests that insulin be injected daily at a chosen site for 1 week. Injections should be 1.5 inches (a knuckle length) apart each day. When a patient requires two insulin injections a day, morning and evening, one site should be chosen on the right side (morning) and one on the left side (evening) A record of injection area sites and dates administered should be kept. Illness and stress increase the need for insulin, so doses should not be withheld during illness, including infections and stress. Hyperglycemia and ketoacidosis may result from insufficient insulin. Faculty: David Merrick B. Soriano, RN Page 14 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 CTTO: https://i.pinimg.com/originals/8b/28/f1/8b28f13d5ff65723b0beaac685a9b8d8.png Types of Insulin Type Example Characteristics Rapid Insulin lispro Clear solutions Insulin aspart Administered within 10 to 15 minutes before mealtime (food Insulin glulisine should be present before administration) Human oral inhalation insulin Short Regular Insulin Clear solutions (Humulin R, Novolin R) Onset of action of 30 minutes Intermediate Isophane insulins like NPH Cloudy, may contain protamine (prolongs the action) or zinc contain protamine, a protein that (slows the onset of action and prolongs the duration of prolongs the action of insulin activity) (Humulin N, Novolin N) Long Acting Insulin glargine Insulin glargine with onset of 1 to 1.5 hours Insulin detemir Evenly distributed over a 24-hour duration of action; thus it is administered OD, usually HS Incidence of nocturnal hypoglycemia is not as common as with other insulins because of its continuous sustained release First long acting rDNA-origin human insulin for patients with types 1 and 2 diabetes. Insulin detemir peaks in 6 to 8 hours and lasts for 24 hours Insulin degludec onset of 1 hour, peaks at 12 hours, and lasts for 42 hours Glargine was the Glargine, detemir, and degludec are available in a prefilled cartridge for the OptiPen insulin pen device Combination NPH 70/regular 30 and NPH Combinations are widely used. The NPH 70/regular 30 is 50/regular 50. available in vials or as prefilled disposable pens. Faculty: David Merrick B. Soriano, RN Page 15 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 It can be stored at room temperature for up to 10 days. However, some patients need less than 25% or 30% regular insulin and more intermediate-acting insulin These patients need to mix the two insulins in the prescribed proportions. Regular insulin can be mixed with other insulin in the same syringe. However, mixing insulin can alter the absorption rate. Insulin Resistance Antibodies develop over time in persons taking animal insulin This can slow the onset of insulin action and extend its duration of action Antibody development can cause insulin resistance and insulin allergy, and obesity can also be a causative factor for insulin resistance Skin tests with different insulin preparations may be performed to determine allergic effect Human and regular insulins produce fewer allergens. Storage of Insulin Unopened insulin vials are refrigerated until needed. Once an insulin vial has been opened, it may be kept at room temperature for 1 month or in the refrigerator for 3 months; insulin is less irritating to the tissues when injected at room temperature. Insulin vials should not be put in the freezer, nor should they be placed in direct sunlight or in a high- temperature area. Prefilled syringes should be stored in the refrigerator and should be used within 1 to 2 weeks. Opened insulin vials lose their strength after approximately 3 months. Pharmacokinetics All insulins can be administered subcutaneously, but only regular insulin can be given intravenously. Pharmacodynamics Signs and symptoms of hypoglycemic reaction: nervousness, tremors, confusion, sweating, and éPR Give orange juice, sugar-sweetened beverages, or hard candy if with hypoglycemia If the patient is unable to ingest fast-acting carbohydrates, glucagon may be given Glucagon promotes the breakdown of glycogen in the liver and raises blood glucose within 10 minutes Regular insulin can be given several times a day, especially during the regulation of insulin dosage Intermediate- and long-acting insulins are usually administered OD Regular insulin can be mixed with intermediate-acting NPH insulin, especially if rapid onset of action is needed When switching from one type of insulin to another, the patient may require a dose adjustment because human insulin has a shorter duration of action Faculty: David Merrick B. Soriano, RN Page 16 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Sliding-Scale Insulin Coverage Insulin may be administered in adjusted doses that depend on individual blood glucose test results. When the diabetic patient has extreme variances in insulin requirements—such as with stress from hospitalization, surgery, illness, or infection—adjusted dosing or sliding-scale insulin coverage provides a more constant blood glucose level Blood glucose testing is performed several times a day at specified intervals, usually before meals. A preset scale usually involves directions for the administration of rapid- or short-acting insulin. CTTO: https://i.pinimg.com/originals/df/a6/f9/dfa6f956aab65a54b7061b4b41955f5b.jpg Drug Interactions Drugs such as thiazide diuretics, glucocorticoids (cortisone preparations), thyroid agents, and estrogen é blood glucose, therefore the insulin dosage may need adjustment Drugs that ê insulin needs are tricyclic antidepressants (TCAs), monoamine oxidase inhibitors (MAOIs), aspirin products, and oral anticoagulants. Side Effects and Adverse Reactions: Hypoglycemic Reactions and Ketoacidosis More insulin is administered than is needed for glucose metabolism, a hypoglycemic reaction, or insulin shock è exhibit nervousness, trembling, and lack of coordination; have cold and clammy skin; and complain of a headache. Ä Management: giving sugar PO or IV é the use of insulin, and the symptoms disappear immediately. Somogyi effect è response to an excessive dose of insulin; a hypoglycemic condition that usually occurs in the predawn hours of 2:00 am to 4:00am wherein a rapid decrease in blood glucose during the nighttime hours stimulates a release of hormones (cortisol, glucagon, and epinephrine) to increase blood glucose by lipolysis, gluconeogenesis, and glycogenolysis Ä Management of the Somogyi effect involves monitoring blood glucose between 2:00 am and 4:00 am and reducing the bedtime insulin dosage. Dawn Phenomenon è hyperglycemia on awakening; patient usually awakens with a headache and reports night sweats and nightmares Ä Management of the dawn phenomenon involves increasing the bedtime dose of insulin. With an inadequate amount of insulin, sugar cannot be metabolized, and fat catabolism occurs. The use of fatty acids (ketones) for energy causes ketoacidosis (diabetic acidosis or diabetic coma). Insulin Pen Injectors An insulin pen resembles a fountain pen but contains a disposable needle and a disposable insulin filled cartridge. Insulin pens come in two types, prefilled and reusable, and are considered to deliver a more accurate dose than the traditional 100- unit syringe and vial. To operate the insulin pen, the insulin dose is obtained by turning the dial to the number of insulin units needed. Insulin pens available on the market include the NovoLog FlexPen (Novo Nordisk), Humalog KwikPen (Lilly), Apidra SoloSTAR (Sanofi- Faculty: David Merrick B. Soriano, RN Page 17 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Aventis), Lantus SoloSTAR (Sanofi), and Levemir FlexPen (Novo Nordisk). CTTO: https://www.drugs.com/cg/images/en3190797.jpg Insulin Pumps (Continuous subcutaneous insulin infusion) Alternative to daily insulin injections used in association with blood glucose monitoring and carbohydrate counting Computerized devices have an insulin reservoir and programming capacity to deliver continuous rapid- acting insulin in varying amounts at different times throughout a 24-hour period. Surgically implanted in the abdomen and delivers both basal infusion (continuous release of a small amount of insulin) and bolus (additional) doses with meals. It is administered intraperitoneally. Needle is inserted into the abdomen, upper thigh, or upper arm. CTTO: https://assets.aboutkidshealth.ca/akhassets/IMD_insulin_pump_function_EN.jpg?RenditionID=19 Infusions are programmed by the patient The patient pushes a button to deliver a bolus dose at meals. Only rapid-acting insulin is used; modified (NPH) insulins are not used because of unpredictable control of blood glucose. An alarm sounds so the patient can take appropriate action when insulin is not delivered or when there is an oncoming low or high. Newer pumps have an automatic shutoff for 1 to 2 hours during periods of low blood glucose Pump can be disconnected from the insertion site for bathing, swimming, and other activities; however, it is recommended that it not be discontinued for longer than 1 to 2 hours. Insulin Jet Injectors Insulin jet injectors shoot insulin, without a needle, directly through the skin into the fatty tissue. Because the insulin is delivered under high pressure, stinging, pain, burning, and bruising may occur. This method of insulin insertion is not indicated for children or older adults. This type of device is also expensive, costing approximately 2 to 10 times as much as the subcutaneous dose. CTTO: https://insujet.com/wp-content/uploads/InsuJet_V5.0_wLF- 2.jpg Oral Antidiabetic (Hypoglycemic) Drugs 1. First- and Second-Generation Sulfonylureas Patients with type 2 diabetes have some degree of insulin secretion by the pancreas. Group of antidiabetics chemically related to sulfonamides but lacking antibacterial activity, stimulate pancreatic beta cells to secrete more insulin. This increases the insulin cell receptors, which increases the ability of the cells to bind insulin for glucose metabolism. Faculty: David Merrick B. Soriano, RN Page 18 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 First-generation sulfonylureas o Short-, intermediate-, and long-acting antidiabetic o Tolbutamide is a first-generation, short-acting sulfonylurea; tolazamide is a first-generation, intermediate-acting sulfonylurea o Chlorpropamide is a first-generation, long-acting sulfonylurea Second-generation sulfonylureas o Increase the tissue response to insulin and decrease glucose production by the liver. o Greater hypoglycemic potency than the first-generation sulfonylureas Longer duration of action, lower effective dose, fewer side effects. Less displacement potential from protein binding sites by other highly protein-bound drugs, such as salicylates and warfarin, than do first generation drugs Not be used when liver or kidney dysfunction is present Examples: glimepiride and glipizide, which directly stimulate the beta cells to secrete insulin, thus decreasing the blood glucose level Glimepiride improves postprandial glucose levels and may be used in combination with insulin in persons with type 2 diabetes. Side effects: GI disturbances such as nausea, vomiting, diarrhea, and abdominal pain. Side Effects, Adverse Reactions, and Contraindications The side effects of most oral antidiabetic drugs are similar to those of insulin. Taking antidiabetic drugs without adequate food can lead to an insulin reaction with signs and symptoms such as nervousness, tremors, and confusion. Adverse reactions include hematologic disorders such as aplastic anemia, leukopenia, and thrombocytopenia, weight gain, seizures, and coma may also occur. Contraindication: type 1 diabetes (no functioning beta cells), diabetic ketoacidosis, pregnancy, and lactation and during stress, surgery, or severe infection. Major side effect: hypoglycemia. Drug Interactions Aspirin, oral anticoagulants, MAOIs, sulfonamides, cimetidine, and some nonsteroidal antiinflammatory drugs (NSAIDs) can increase the action of sulfonylureas, especially first generation ones, by binding to plasma proteins and displacing sulfonylureas. Because this causes increased free sulfonylurea, an insulin reaction can result Concurrent administration of thiazide diuretics, isoniazid, phenytoin, and corticosteroids + sulfonylureas è decrease effect of sulfonylureas Alcohol + sulfonylurea è alcohol increases the half-life, and a hypoglycemic reaction can result. 2. Nonsulfonylureas Examples: metformin and acarbose use different methods to control serum glucose levels following a meal. Affect the hepatic and GI production of glucose a.) Biguanides: Metformin Mechanism of action: acts by decreasing hepatic production of glucose from stored glycogen Diminishes the increase in serum glucose following a meal and blunts the degree of postprandial hyperglycemia. Does not produce hypoglycemia or hyperglycemia, although it can cause GI disturbances. It does not undergo hepatic metabolism and is eliminated unchanged in the urine. Not recommended for patients with renal impairment. Faculty: David Merrick B. Soriano, RN Page 19 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Metformin therapy should be withheld for 48 hours before and after administration of IV contrast because lactic acidosis or acute renal failure may develop. b.) Alpha-Glucosidase Inhibitors: Acarbose and Miglitol Mechanism of action: acts by inhibiting the digestive enzyme in the small intestine that is responsible for the release of glucose from complex carbohydrates in the diet By inhibiting alpha glucosidase, absorption of complex carbohydrates is delayed. It does not cause a hypoglycemic reaction. Acarbose is intended for use in patients who do not achieve results with diet alone. This drug will not cause hypoglycemia, but if taken with a sulfonylurea or insulin, hypoglycemia could occur. c.) Thiazolidinediones Examples: Pioglitazone and rosiglitazone Contraindication: class III and IV heart failure due to dose-related fluid retention. Prescribed as monotherapy or combined with other oral antidiabetic drugs Drugs do not induce hypoglycemic reactions if taken alone; they decrease insulin resistance and improve blood glucose control. d.) Meglitinides Examples: Repaglinide and nateglinide Mechanism of action: stimulate the beta cells to release insulin Used alone or in combination with metformin for patients with type 2 diabetes mellitus Short-acting antidiabetic drugs Contraindication: patients with liver dysfunction because of a possible decreased liver metabolism rate; more of the drug could remain in the body, which could cause a hypoglycemic reaction. e.) Incretin Modifier (dipeptidyl peptidase 4 (DPP-4) inhibitors and gliptins) Examples: sitagliptin phosphate and saxagliptin Mechanism of action: é level of incretin hormones, increase insulin secretion, and decrease glucagon secretion to reduce glucose production. Adjunct treatment with exercise and diet to reduce both fasting and postprandial plasma glucose levels. Guidelines for Oral Antidiabetic (Hypoglycemic) Therapy for Type 2 Diabetes Criteria for the use of oral antidiabetic drugs: 1. Onset of diabetes mellitus at age 40 years or older 2. Diagnosis of diabetes within the past 5 years 3. Normal weight or overweight 4. Fasting blood glucose of 200 mg/dL or less 5. Fewer than 40 units of insulin required per day 6. Normal renal and hepatic function Other Antidiabetic Agents Incretin Mimetics (glucagon-like peptide 1 (GLP-1) agonists) Examples: Exenatide and liraglutide o Mechanism of action: improve beta-cell responsiveness, enhance insulin secretion è improves glucose control with type 2 DM, suppress glucagon secretion, slow gastric emptying, reduce food intake Faculty: David Merrick B. Soriano, RN Page 20 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 o NOT a substitute for insulin o Contraindication: type 1 DM, diabetic ketoacidosis, severe renal dysfunction, or severe GI disease Exenatide o Administered by injectable prefilled pens in twice-a-day dosing and has significantly improved HbA1c levels and weight loss in many patients o Adverse effects: headache, dizziness, jitteriness, nausea, vomiting, and diarrhea Liraglutide o Given SQ, OD Amylin Analogue Pramlintide acetate o For adults with type 1 and type 2 diabetes mellitus. o Primary purpose of pramlintide is to improve postprandial glucose control in diabetic patients who are using insulin but are unable to achieve and maintain glucose control o Mechanism of action: suppress glucagon secretion, slow gastric emptying, and modulate appetite by inducing satiety o Suppression of glucagon secretion reduces postprandial hepatic glucose for approximately 3 hours. o By slowing gastric emptying, the absorption rate of glucose is reduced; satiety promotes reduced food intake o Adverse effects: dizziness, anorexia, nausea, vomiting, and fatigue. o Administered by SQ before meals in the abdomen or thigh; it is never given in the arm Hyperglycemic Drugs Glucagon Hyperglycemic hormone secreted by alpha cells of the islets of Langerhans in the pancreas Glucagon increases blood glucose by stimulating glycogenolysis (glycogen breakdown) in the liver. It protects the body cells, especially those in the brain and retina, by providing the nutrients and energy needed to maintain body function. Glucagon is available for parenteral use (subcutaneous, intramuscular [IM], and IV). It is used to treat insulin-induced hypoglycemia when other methods of providing glucose are not available. Patients with diabetes who are prone to severe hypoglycemic reactions (insulin shock) should keep glucagon in the home, and family members should be taught how to administer subcutaneous or IM injections during an emergency hypoglycemic reaction. The blood glucose level begins to increase within 10 minutes after administration. Diazoxide Oral diazoxide, which is chemically related to thiazide diuretics, increases blood glucose by inhibiting insulin release from the beta cells and stimulating release of epinephrine from the adrenal medulla. Contraindication: hypoglycemic reaction, rather it is used to treat hypoglycemia cause: hyperinsulinism. Diazoxide has a long half-life and is highly protein bound. Faculty: David Merrick B. Soriano, RN Page 21 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 2. Assessment of Learning This section will enable you to do self-check of your progress in the discussion. During the self-evaluation, you are expected to practice the virtue of honesty. A score equivalent to 75% will enable you to proceed to the assignment section. A separate sheet will be utilized to answer the questions in this section. You may repeat answering the questions until the required score equivalent is acquired. Matching Type Match Column A with Column B Column A Column B ____ 1. Monitor vital signs. A. Cortisone increases sodium retention and increases blood ____ 2. Monitor weight after taking a cortisone preparation pressure. for more than 10 days. B. Adrenal crisis may occur if cortisone is abruptly stopped. ____ 3. Monitor laboratory values, especially blood C. Glucocorticoid drugs promote loss of potassium. glucose and electrolytes. D. Weight gain occurs with cortisone use as a result of water ____ 4. Instruct the patient to take the cortisone with food. retention. ____ 5. Advise the patient to eat foods rich in potassium. E. Glucocorticoid drugs promote sodium retention, potassium ____ 6. Instruct the patient not to abruptly discontinue the loss, and increased blood glucose. cortisone preparation. F. Cortisone promotes loss of muscle tone and loss of calcium ____ 7. Report changes in muscle strength and signs of from bone. osteoporosis. G. Glucocorticoid drugs may cause moon face, puffy eyelids, ____8. Teach the patient to report signs and symptoms of edema in the feet, dizziness, and menstrual irregularity at high drug overdose. doses. H. Glucocorticoid drugs can irritate the gastric mucosa and may cause peptic ulcer. Column A Column B ____ 12. NPH insulin A. Oral hypoglycemic drug group ____ 13. Lipoatrophy B. Hyperglycemic hormone that stimulates glycogenolysis ____ 14. Sulfonylureas C. Intermediate-acting insulin ____ 15. Glucagon D. Long-acting insulin ____ 16. Lispro insulin E. Tissue atrophy F. Rapid-acting insulin Multiple Choices Select the best answer from the given choices 1. A patient is receiving the drug somatropin. The nurse understands that the action of this drug is to do what? A. Act as an antiinflammatory agent B. Increase metabolic rate and oxygen consumption C. Stimulate growth in long bones at epiphyseal plates D. Promote water reabsorption from the renal tubules 2. A patient is given desmopressin acetate. The nurse knows that this drug is used to treat which of the following conditions? A. Gigantism B. Diabetes mellitus C. Diabetes insipidus D. Adrenal insufficiency Faculty: David Merrick B. Soriano, RN Page 22 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 3. A patient is taking levothyroxine. For which adverse effect would the nurse monitor? A. Tachycardia B. Drowsiness C. Constipation D. Weight gain 4. A patient has just begun taking calcitriol. Which is a nursing implication of this drug? A. Monitor the patient’s weight. B. Monitor serum calcium levels. C. Teach side effects of alopecia and petechiae. D. Instruct the patient to avoid persons with respiratory infections. 5. A patient is given corticotropin. The nurse knows to monitor the patient for which condition? A. Weight gain B. Hyperkalemia C. Hypoglycemia D. Dehydration 6. A nurse is administering prednisone to a newly admitted patient who is taking multiple other drugs. The nurse should consider which drug interactions with prednisone? (Select all that apply.) A. Cardiac and central nervous system actions are increased when drug is taken with an adrenergic agent. B. Potassium-wasting diuretics increase potassium loss, resulting in hypokalemia. C. Risk for gastrointestinal bleeding and ulceration increases when drug is taken with aspirin or other nonsteroidal antiinflammatory drugs (NSAIDs). D. The action of prednisone is decreased when taken with phenytoin because phenytoin increases glucocorticoid metabolism. E. Risk for dysrhythmias and digitalis toxicity increase when drug is taken with cardiac glycosides. F. Dosage of antidiabetic agents may need to be decreased when taken concurrently with glucocorticoids. 7. The nurse is administering vasopressin to a patient. Which of the following nursing interventions are indicated when administering vasopressin? (Select all that apply.) A. Record urinary output. B. Observe the patient’s weight, and note edema. C. Monitor the patient for decreased blood pressure D. Closely monitor the patient’s blood glucose levels. E. Monitor the patient’s pulse for increased heart rate. F. Record the patient’s daily calcium levels. 8. A patient is diagnosed with type 2 diabetes mellitus. The nurse is aware that which statement is true about this patient? A. The patient is most likely a teenager. B. The patient is most likely a child younger than 10 years. C. Heredity and obesity are major causative factors. D. Viral infections contribute most to disease development. 9. Antidiabetic drugs are designed to control signs and symptoms of diabetes mellitus. The nurse primarily expects a decrease in which? A. Blood glucose B. Fat metabolism C. Glycogen storage D. Protein mobilization Faculty: David Merrick B. Soriano, RN Page 23 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 10. A patient is to receive insulin before breakfast, and the time of breakfast tray delivery is variable. The nurse knows that which insulin should not be administered until the breakfast tray has arrived and the patient is ready to eat? A. NPH B. Lispro C. Glargine D. Regular 11. A patient is receiving a daily dose of NPH insulin at 7:30 am. The nurse expects the peak effect of this drug to occur at what time? A. 8:15 am B. 10:30 am C. 5:00 pm D. 11:00 pm 12. A patient is prescribed glipizide. The nurse knows that which side effects and adverse effects may be expected? (Select all that apply.) A. Tachypnea B. Tachycardia C. Increased alertness D. Increased weight gain E. Visual disturbances F. Hunger 13. A nurse is teaching a patient how to recognize symptoms of hypoglycemia. Which symptoms should be included in the teaching? (Select all that apply.) A. Headache B. Nervousness C. Bradycardia D. Sweating E. Thirst F. Sweet breath odor 14. A patient is newly diagnosed with type 1 diabetes mellitus and requires daily insulin injections. Which instructions should the nurse include in the teaching of insulin administration? A. Teach family members how to administer glucagon by injection when the patient has a hyperglycemic reaction. B. Instruct the patient about the necessity for compliance with prescribed insulin therapy. C. Teach the patient that hypoglycemic reactions are more likely to occur at the onset of action time. D. Instruct the patient in the care and handling of the insulin container and syringe. 15. What is/are contraindication(s) for the use of oral antidiabetic drugs? (Select all that apply.) A. Breastfeeding B. Pregnancy C. Renal dysfunction D. Severe infection E. Type 2 diabetes 3. Evaluation of Learning For the evaluation of learning for Module 13, a scheduled quiz will be assigned in the Google Classroom and will be taken before the start of the next Module during the Synchronous Class. Faculty: David Merrick B. Soriano, RN Page 24 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 Activities for Self-Directed Learning 1. Interview of a Client with Diabetes (Written Output) A. Learning Outcomes 1. Apply appropriate nursing concepts and actions holistically and comprehensively 2. Based on the activity (Interview) Assess with the client Institute health education and appropriate corrective actions to prevent or minimize harm arising from adverse effects B. Description of the Activity § Interview a client who is diagnosed with diabetes Guide Concepts 1. Type of Diabetes Mellitus 2. Medications Given (Include the Frequency, Dosage) 3. Aside from Medications what are the other interventions done to the client § Prepare a written output following the format A. Brief description about diabetes Mellitus B. Management of Diabetes Mellitus Ideal Management Actual Management C. Medications Given Name of the Medication Frequency / Dosage Classification D. Health Education to the Client Include here brief description of the health education you have done E. Documentation Faculty: David Merrick B. Soriano, RN Page 25 of 26  COLLEGE OF NURSING AND PHARMACY C-NCM 106 – PHARMACOLOGY First Semester | AY 2024-2025 C. Rubrics for Grading Output RUBRIC – WRITTEN OUTPUT CRITERIA Does Not Meet Expectations Meets Expectations Exceeds Expectations SCORE (1-3points) (4-7points) (8-10points) Content Content is not explained. Explained content within Explained content thoroughly, Explained content but out of the context / in-depth and fully supported and justified in a context /incorrect/ in detain / clearly / in an way that adds to the audience’s oversimplified way or with no analytical way. Supported understanding and appreciation analysis explanation with reason and of the topic or subject content. evidence Organization and Unable to convey different Organized ideas logically Organized and delivered the Format perspectives of the content and presented in a polished presentation in a refined and way. Partially followed educated way. Followed Document is formatted instructions and limitations instructions and limitations poorly and lacks a quality precisely. precisely. cover page and index Formatting of the document Formatting of the document is is generally consistent and professional and includes a adequate, includes a good professional cover page quality cover page Mechanics Sentences are poorly written; Sentences are generally Sentences are well-written; there are numerous incorrect well-written; there are a few there are no incorrect word word choices and errors in incorrect word choices and choices and the text is free of grammar, punctuation and errors in grammar, errors in grammar, punctuation spelling. punctuation and spelling. and spelling Documentation Failed to correctly document Most sources are correctly All sources are correctly and any sources or to utilize documented; appropriate thoroughly documented; appropriately citation forms. citation forms are generally appropriate citation forms are utilized. utilized throughout. Time Timely submission = 5 Submitted 1 day after the deadline = 3; Submitted 2 days after the deadline = 2 Failure to submit 2 days after the deadline = Output will not be accepted but it should still be done as part of the portfolio for this module References Burchum, Jacqueline Rosenjack, Rosenthal Laura D. Lehne’s Pharmacology for Nursing. 10th Edition. (2018). Elsevier Inc. St. Louis, Missouri USA. Kee, Joyce LeFever, Hayes, Evelyn R., McCuistion, Linda E. Pharmacology: A Patient-Centered Nursing Process Approach. 8th Edition. (2015). Elsevier Pte. Ltd. Singapore. McCuistion, Linda, Vuljoin-DiMaggio, Kathleen, Winton, Mary, Yeager, Jennifer. Pharmacology: A Patient-Centered Nursing Process Approach. 9th Edition. (2018). Elsevier Inc. St. Louis, Missouri USA. Pacitti, Diane, Smith, Blaine T. (editor). Pharmacology for Nurses. 2nd Edition. (2020). Jones & Bartlett Learning. Burlington, MA. Congratulations for having completed this C-NCM 106 Module 13! See you in the next Module Faculty: David Merrick B. Soriano, RN Page 26 of 26