Reviewer Endocrine PDF

**Week 10** **Endocrine Drugs** 1. **Antidiuretic Hormones** (RIVc) - Enhance re-absorption of water in the kidneys - Increases water permeability in the renal collecting ducts - Stimulates VASOCONSTRICTION and increases the blood pressure **Therapeutic Indications** (CHED) - Used to...

**Week 10** **Endocrine Drugs** 1. **Antidiuretic Hormones** (RIVc) - Enhance re-absorption of water in the kidneys - Increases water permeability in the renal collecting ducts - Stimulates VASOCONSTRICTION and increases the blood pressure **Therapeutic Indications** (CHED) - Used to control the hemorrhage in variceal bleeding - Hormonal replacement - Treatment of enuresis (Inability to control urination) - Used in diagnostic procedure **Route** (essin) - Intranasal (DL) - Desmopressin - Lypressin - Intramuscular (P) - Pitressin **Side Effects** (FWHHG) - Flushing and headache - Water intoxication - CVS: heart block, MI - Renal: *hyponatremia* (low NA in blood) - Gangrene due to vasoconstriction 2. **Thyroid Hormones** - To **treat** the manifestations of hypothyroidism - **Replace hormonal deficit** in the treatment of HYPOTHYROIDSM **Actions** (everything e**LEV**ate; VSOMR) - Replace both T3 and T4 - Thyroxine - Triiodothyronine - Increase metabolic rate - Increase O2 consumption - Increase HR, RR, BP **Therapeutic Indication** - Hypothyroidism - Diagnostic suppression test **Examples** - **Lev**o**thy**roxine (**Syn**throid) - Elevates thyroid - Synthetic thyroid - S/E: diarrhea, cramps, tremors, nervousness/palpitation, insomnia, h/a, wt. loss, tachycardia, hypertension, thyroid crisis - Liothyroxine (Cytomel) - Thyroid desiccated - Liotrix (Thyrolar) **Side effect** - Nausea and Vomiting - Signs of increased metabolism - tachycardia, hypertension, cardiac arrhythmias, anxiety, headache, tremors, palpitations **Nursing Implication** - Monitor weight, VS - Instruct client to take daily medication the same time **[each morning WITHOUT FOOD]** - Monitor blood tests to check the **activity of thyroid** - Advise to report palpitation, tachycardia, and chest pain (hyperthyroidism) - Instruct to avoid foods that inhibit thyroid secretions like cabbage, spinach and radishes 3. **Anti-thyroid Hormones** - The thyroid becomes oversaturated with iodine and stop producing thyroid hormone - Drugs used to BLOCK the thyroid hormones and treat hyperthyroidism - Inhibit the synthesis of thyroid hormones - Absorption is good orally **Therapeutic Indication** (GT) - Grave's disease - Thyrotoxicosis - Methimazole (Tapazole) - Inhibit secretion of thyroid hormone - **\*M**elts away hormones - First line - PTU (prophylthiouracil) - PTU also inhibits peripheral conversion of T4 to T3 - **\*P**revents **T**hyroid from building **U**p - First line - Preferred drug during pregnancy; does not cross placenta - Iodine solution- SSKI - Lugol's solution - - - - - **Adverse effects** - - **Side-effects of thionamides** - N/V, drowsiness, lethargy, bradycardia, skin rash - GI complaints - Arthralgia, myalgia - AGRANULOCYTOSIS - Most important to monitor **Nursing Implication** - Monitor VS, T3 and T4, weight - The medications [WITH MEALS] to avoid gastric upset - Instruct to report SORE THROAT or unexplained FEVER - Monitor for signs of hypothyroidism. - Instruct not to stop abrupt medication **Adrenal Cortex** - **Mineralocorticoids** (aldosterone and deoxycortisone) - Regulate fluids and electrolytes - Help adjust blood pressure and blood volume - **Glucocorticoids** (e.g. cortisone) - Regulate metabolism and resistance to stress - **Androgens** - Promote libido in females and are converted to estrogen, also stimulate growth of axillary and pubic hairs in boys and girls and contribute to the prepubertal growth spurt **Adrenal Medulla** - - 4. **Steroids** - - - - - **Actions** (sone; asone, ide; BFPP) - Prednisone - Bethamethasone - Prednisolone - Fludrocortisone **Side-effects** - HYPERglycemia - Increased susceptibility to infection (immunosuppression) - Hypokalemia - Edema - Peptic ulceration - If high doses- osteoporosis, growth retardation, peptic ulcer, hypertension, cataract, mood changes, hirsutism, and fragile skin **Nursing Implication** - Monitor VS, electrolytes, glucose - Monitor weight edema and I/O - Protect patient from infection - Handle patient gently - Instruct to take meds WITH MEALS to prevent gastric ulcer formation - Caution the patient NOT to abruptly stop the drug - Drug is tapered to allow the adrenal gland to secrete endogenous hormones **Evaluation** The drugs are effective if there is: - Relief of signs and symptoms of inflammation - Return of adrenal function to normal **Glucocorticoids** - Prednisone, Dexamethasone - Used to treat many diseases including inflammatory conditions, allergy and many debilitating conditions - S/E: hyperglycemia, deposition of fats in the face & trunk, Na and water retention, glaucoma, osteoporosis, peptic ulcer, growth retardation **Clinical Notes of Dexamethasone** - Has a rapid onset of action and shorter duration of action - Must be prescribed in a shorter frequency - 6 mg IM every 12 H X 4 doses **Adverse Reaction** - insomnia - nervousness - increased appetite - headache - hypersensitivity reaction - arthralgia **Corticosteroid Therapy** **Mechanism of Action** - Accelerates lung maturation **Therapeutic Uses** - PTL to decrease the incidence of RD - Betamethasone (Celestone) - When PTL occurs before the 33rd AOG, corticosteroid therapy with betamethasone may be prescribed, 12 mg IM every 24 H X 2 doses **Adverse Reactions** - seizures - headache - vertigo - edema - hypertension - increased sweating - petechiae - ecchymoses - facial erythema **Nursing Implication** - Shake the suspension well. Avoid exposing to excessive heat or light. - Inject into large muscle, but not to deltoid, avoid local atrophy. - Monitor maternal V/S. - Maintain accurate I & O. - Check blood glucose if used for client with diabetes. **Dexamethasone** - Has a rapid onset of action and shorter duration of action - Must be prescribed in a shorter frequency - 6 mg IM every 12 H X 4 doses **Adverse Reaction** - insomnia - nervousness - increased appetite - headache - hypersensitivity reaction - arthralgia 5. **Diabetes Drug Therapy** Diabetes Mellitus - Disorder of metabolism and chronic hyperglycemia - - - Produce glucagons, which increase blood glucose levels when it falls below normal - - Produce insulin, helps lower blood glucose levels when it is high **Diagnosis** Blood glucose values are normally maintained in a very narrow range, usually 70-120 ml/dL. The diagnosis of diabetes is established by noting elevation of blood glucose by any of three criteria - **A random glucose** - 200mg/dL, with classical signs and symptoms - **Fasting glucose** - 126 mg/dL on more than 1 occasion - An abnormal **oral glucose tolerance test**, in which glucose is \> 200 mg/dL 2 hours after a standard carbohydrate load 1. **Carbohydrates (CHO)** - **Glucose (Serum/Plasma)** - **Fasting Blood Glucose (FBG/FBS)** - DM and DM therapy monitoring; 6-8Hr fast - NV 70-105mg/dL if \>60y/o 80-115 - **2-hr Post-Prandial (PP)** - Simple glucose loading test (meal or 75g load) - NV \140mg/dL - **Other Blood CHO Metabolism Tests** - **Insulin** - NV 6-24 uU/mL - Evaluates fasting hypoglycemia and insulinoma - **C-Peptide** - NV 0.78-1.89ng/mL - Detects factitious fasting hypoglycemia and endogenous insulin secretion - **Glycated Hemoglobin** - Index of long-term (2-3 month) glucose control - NV 5.3-7.5% of total hemoglobin - Fructosamine -- 2-3 week glucose control - **Glucose Methods** - **Glucose Hexokinase Coupled Enzyme Reaction** - Reference method and most frequently performed - Virtually no interference - **Glucose Oxidase O2 Consumption** - Glucose meter testing; no interference - **Glucose Oxidase Coupled Enzyme Reaction (Trinder)** - Whole blood and urine rapid strip testing - **CHO Metabolism Methods** - **Insulin Immunoassays** - Interference: exogenous insulin and insulin antibody - **C Peptide Immunoassays** - Interference: cross-react with pro-insulin - **Glycated Hemoglobin Affinity Chromatography** - **Uses whole blood (Hemolysate)** **Adult Non-Pregnant Testing**  **Adult, Pregnant O'Sullivan Criteria** **Drug Therapy and Management** - Usually, this type of management is employed if diet modification and exercise cannot control the blood glucose level. - These agents are employed to control the blood glucose level - They can be insulin and oral agents - These are given to replace the hormone in the body - If hormone is still present BUT decreased, Oral agents are given **Diabetes Mellitus** **Drug Therapy and Management** - Because the patient with TYPE 1 DM cannot produce insulin, exogenous insulin must be administered for life - TYPE 2 DM may have decreased insulin production, ORAL agents that stimulate insulin production are usually employed. **Pharmacologic Insulin** - - Source- Human, pig, or cow - Onset of action- Rapid-acting, short-acting, intermediate acting, long-acting and very long acting - - Pure or mixed concentration - Manufacturer of drug **Generalities** - Human insulin preparations have a shorter duration of action than animal source - Animal sources of insulin have animal proteins that may trigger allergic reaction and they may stimulate antibody production that may bind the insulin, slowing the action - ONLY Regular insulin can be used INTRAVENOUSLY! - Insulin is measured in INTERNATIONAL UNITS or "iu" - There is a specified insulin injection calibrated in units - Mixed insulin is also available - The most common of which is the 70-30 insulin - Made up of :70% NPH and 30% regular insulin in the vial **Comparison of Insulin Peak action**  **Insulin Products** - Purified Animal Insulins (porcine, bovine) purified by gel filtration, single peak purity, few contaminants - Recombinant human insulins (Humulin) - Extremely low-risk of insulin allergy - "Designer Insulins" -- biochemical modifications of human insulins altering their absorption profile, duration of action a. **Bolus-Basal Insulin Dosing (Type 1 Diabetes)** - The goal of this strategy is to mimic the normal physiologic pattern of insulin secretion. - Rapid-acting insulins (Lispro, Aspart) or Regular insulin are given prior to meals to manage post-prandial glucose levels - Isophane insulin (NPH) or long-acting insulins (insulin glargine, insulin detemir) provide basal insulin coverage b. **Insulin Pumps** - A continuous subcutaneous delivery device that most closely mimics physiologic secretory patterns - The programmable pump delivers bolus and basal insulin doses based on blood glucose monitoring. Basal levels are usually relatively constant; bolus doses vary based on food consumption. - Pumps use rapid acting insulins (lispro or aspart) or regular insulins. 1. **Rapid Acting Insulin** - - - - - - - 2. **Regular Insulin** - - - - - - - 3. **Intermediate Acting Insulin** - - - - - - 4. **Long- Acting Insulin** - - - - - - - **Administration** - Before injection insulin should be at room temperature - Roll vial in between the palm to redistribute insulin particles - Inject air into the insulin bottle - Draw up the regular insulin first - Administer insulin at a 45 to 90 ° angle - Rotate the site of injection - Store vials of insulin in current use at room temperature, other vials not in used should be refrigerated. - Regarding Insulin SELF- Administration - Insulin is administered at home subcutaneously - Cloudy insulin should be thoroughly mixed by gently inverting the vial or ROLLING between the hands - Insulin NOT IN USE should be stored in the refrigerator, BUT avoid freezing/extreme temperature - Insulin IN USE should be kept at room temperature to reduce local irritation at the injection site - INSULIN may be kept at room temperature up to 1 month - Select syringes that match the insulin concentration. - U-100 means 100 units per mL - Instruct the client to draw up the REGULAR (clear) Insulin FIRST before drawing the intermediate acting (cloudy) insulin - Pre-filled syringes can be prepared and should be kept in the refrigerator with the needle in the UPRIGHT position to avoid clogging the needle - The four main areas for insulin injection are- ABDOMEN, UPPER ARMS, THIGHS and HIPS - Insulin is absorbed fastest in the abdomen and slowest in the hips - Instruct the client to rotate the areas of injection, but exhaust all available sites in one area first before moving into another area. - Alcohol *may not* be used to cleanse the skin - Utilize the subcutaneous injection technique- commonly, a 45--90-degree angle. - No need to instruct for aspirating the needle - Properly discard the syringe after use. - T-I-E Test blood Inject insulin Eat food **Complications of Insulin Therapy** - Local allergic reactions - Lipodystrophy - Edema - Hypoglycemia c. **Oral Hypoglycemic Agents** - Test blood- insulin- eat food - These may be effective when used in TYPE 2 DM that cannot be treated with diet and exercise - These drugs are given per Orem and are effective only in type 2 DM - These are NEVER used in pregnancy! - Hypoglycemia - Diarrhea, jaundice, nausea and heartburn - Anemia, photosensitivity d. **Sulfonylureas** - MOA- stimulates the beta cells of the pancreas to secrete insulin **Classification** **FIRST GENERATION** - **SECOND GENERATION** - Glipizide, Glyburide, Glibenclamide, Glimepiride - - - - - e. **Biguanides** (formin) - - - - **Side Effect** - - - f. **Alpha-Glucosidase Inhibitors** - MOA- Delay the absorption of glucose in the GIT - Result is a lower post-prandial blood glucose level - They do not affect insulin secretion or action! - **Side-effect** - DIARRHEA and FLATULENCE - Acarbose, Miglitol - They are not absorbed systemically and are very safe - They can be used alone or in combination with other OHA - HYPOGLYCEMIA - Note that sucrose absorption is impaired and IV glucose is the therapy for the hypoglycemia g. **Thiazolidinediones** - MOA- Enhance insulin action at the receptor site - They *do not* stimulate insulin secretion - Rosiglitazone, Pioglitazone - These drugs affect LIVER FUNCTION - *Can cause resumption of OVULATION in peri-menopausal anovulatory women* h. **Meglitinides** - - - - - hypoglycemia - Can be used alone or in combination **General Consideration** - Observe for manifestations of hypoglycemia - Assess for allergic reaction - Instruct to take the medication at the same time each day - Caution to avoid taking other drugs without consultation with physician - THESE medications SHOULD NEVER be given to pregnant women, so rule out pregnancy - Instruct to wear sunscreen - Advise to bring simple sugar to be taken when hypoglycemic episodes occur 6. **Reproductive Hormones** - Gonadal hormones include agents that affect the female and male reproductive cycle - Female hormones include ESTROGENS, PROGESTINS and ovarian hormones - Male hormones include ANDROGENS and anabolic steroids **Mechanism of Action** - These hormones interfere with the normal cycle of hormone balance **Indications** - FEMALE: Hormonal replacement therapy, oral contraception, treatment of infertility and management of some tumors - MALE: replacement therapy, metabolic stimulators and treatment of some tumors 1. **Estrogens** - Conjugated estrogen - Estradiol - Ethinyl estradiol - Diethylstilbesterol (DES) - Clomiphene 2. **Progestins** - Medroxyprogesterone acetate (Provera) - Megestrol - Norethindrone - Levonorgestrel (Norplant) - Norgestrel - Norethindrone acetate 3. **Androgens** - Testosterone cypionate - Methyltestosterone - Fluoxymesterone - Aqueous testosterone 4. **Oral Contraceptive Pills** - Combination estrogen and progesterone - progestins only **Dynamics** - Inhibits OVULATION by altering the hypothalamus and gonadotropin axis - Alters the MUCUS to prevent sperm entry - Alters the uterine endometrium to prevent implantation - Suppresses the ovaries **Indicators** - Suppression of ovulation for prevention of pregnancy - Regulation of menstrual cycle and management of dysfunctional bleeding - Treatment of endometriosis **Kinetics** - Easily absorbed orally - NORPLANT provides 5 years of contraception - Provera provides 3 months of protection - Metabolized and excreted in liver **Contraindication** - Not to be used in patients with history of, hypertension, thromboemoblic or CVA disease - Not given in certain cancers - Contraindicates in pregnancy - SMOKING should be avoided when under therapy **Drug Interaction** - Rifampicin, penicillin and tetracycline REDUCE effectiveness of contraception - Benzodiazepines decrease the levels of OCP **Side effects** - CNS: headache - CV: Thromboembolic disease, MI, hypertension and pulmonary edema - NAUSEA and cholestatic JAUNDICE - Breast tenderness, weight gain, edema, breakthrough bleeding, acne **Nursing Considerations** - Assess for risk factors and the ability to comply with medications - Determine the type of OCP used - Monophasic pills provide constant dosing of BOTH estrogen and progestin - Biphasic pills provide constant estrogen but varying progestin doses - Triphasic pills provide varying Estrogen and Progesterone - Teach the common side-effects and re-assure that these will decrease in time - Instruct to use other means of contraception if antibiotics and anticonvulsants are also taken - *WARN the client to avoid smoking because this will increase the risk for embolic episodes* **Clomiphene** - A synthetic, non-steroidal estrogen - Increases the secretion of gonadotropins and initiates the secretion of FSH and LH - OVULATION will occur - Used in the treatment of infertility - Readily absorbed orally **Side effects** - Risk for Multiple pregnancy - Nausea, breast discomfort, headache and GI disturbances - Visual disturbances - Enlargement of the ovaries **Viagra (Sildenafil)** - A medication used for penile erectile dysfunction - Selectively inhibits receptors and enzyme *Phosphodiesterase E* - This increases the nitrous oxide levels allowing blood flow into the corpus cavernosum **Contraindicated** - in patients with bleeding disorders and with penile implants - Caution: Coronary Artery Disease and concomitant use of nitrates **Side-effects** - PRIAPISM, headache, flushing, dyspepsia, UTI, diarrhea and dizziness **Nursing consideration** - Assess for risk factors - Instruct to take the drug ONE hour before sexual act - Drug is taken orally **Week 9** **Gastrointestinal Medication** 1. **Antacid Medication (**hydroxides/ carbonates) **Acid-Related Pathophysiology** **The stomach secretes:** - Hydrochloric acid (HCl) - Bicarbonate - Pepsinogen - Intrinsic factor - Mucus - Prostaglandins **Glands of the Stomach** - Cardiac - Pyloric - Gastric\* **Cells of Gastric Gland** **Parietal** - Produce and secrete HCl - Primary site of action for many acid-controller drugs - Hydrochloric Acid - Maintains stomach at a pH of 1 to 4 - Secretion stimulated by: - Large, fatty meals - Excessive amounts of alcohol - Emotional stress **Chief** - Secrete pepsinogen, a proenzyme - Pepsinogen becomes PEPSIN when activated by exposure to acid - Pepsin breaks down proteins (proteolytic) **Mucoid** - Mucus-secreting cells (surface epithelial cells) - Provide a protective mucous coat - Protects against self-digestion by HCl \*The gastric glands are the largest in number **Acid-Related Diseases** - Caused by imbalance of the three cells of the gastric gland and their secretions - **Most common:** - Hyperacidity - **Most harmful:** - Peptic ulcer disease (PUD) - Layman's terms for overproduction of HCl by the parietal cells: indigestion, sour stomach, heartburn, acid stomach **Antacids: Mechanism of Action** **Promote the gastric mucosal defense mechanisms** Secretion of: - **Mucus**: Protective barrier against HCl - **Bicarbonate**: Helps buffer acidic properties of HCl - **Prostaglandins**: Prevent activation of proton pump - Antacids DO NOT prevent the overproduction of acid. - Acids DO neutralize the acid once it's in the stomach. --------------------------------------------- --------------- ----------------------------------- **Anti-ulcer drugs** **Prototype** **Best time to give** Histamine (H2) receptor antagonist/blockers Cimetidine With FOOD or 1 hour after ANTACID Antacids AlOH & MgOH Usually after meals Proton pump inhibitors Omeprazole BEFORE MEALS Mucosal protectants Sucralfate BEFORE MEALS Prostaglandin analog Misoprostol WITH MEALS --------------------------------------------- --------------- ----------------------------------- **Drug Effects of Antacids** **Reduction of pain associated with acid-related disorders** - Raising gastric pH from 1.3 to 1.6 neutralizes 50% of the gastric acid. - Raising gastric pH 1 point (1.3 to 2.3) neutralizes 90% of the gastric acid. **OTC formulations available as:** - Capsules and tablets - Powders - Chewable tablets - Suspensions - Effervescent granules and tablets a. **Salts** a. **Aluminum salts** - Forms: carbonate, hydroxide, phosphate - Have **constipating effects** - Often used with magnesium to counteract constipation - Example: aluminum carbonate (Basaljel) b. **Magnesium salts** - Forms: carbonate, hydroxide, oxide, trisilicate - Commonly cause a **laxative effect** - \*Magnesium moves bowels - Usually used with other agents to counteract this effect - Dangerous when used with renal failure---the failing kidney cannot excrete extra magnesium, resulting in accumulation - magnesium hydroxide (MOM); combination products such as Maalox, Mylanta (aluminum and magnesium) c. **Calcium salts** - Forms: many, but carbonate is most common - **May cause constipation** - Their use may result in kidney stones - Long duration of acid action may cause increased gastric acid secretion (**hyperacidity rebound**) - Often advertised as an extra source of dietary calcium - Example: Tums (calcium carbonate) d. **Sodium bicarbonate** - Highly soluble - Quick onset, but short duration - May cause **metabolic alkalosis** - Sodium content may cause problems in patients with CHF, hypertension, or renal insufficiency **Anti-flatulent** - used to relieve the painful symptoms associated with gas - Several agents are used to bind or alter intestinal gas, and are often added to antacid combination products. **OTC Anti-flatulent** - activated charcoal - simethicone - Alters elasticity of mucus-coated bubbles, causing them to break. - Used often, but there are limited data to support effectiveness. **Side Effects** - Minimal, and depend on the compound used - Aluminum and calcium - Constipation - Magnesium - Diarrhea - Calcium carbonate - Produces gas and belching; often combined with simethicone **Drug Interactions** - **Chelation** - Chemical binding, or inactivation, of another drug - **Chemical inactivation** - Produces insoluble complexes - **Result:** reduced drug absorption - **Increased stomach pH** - Increased absorption of basic drugs - Decreased absorption of acidic drugs - **Increased urinary pH** - Increased excretion of acidic drugs - Decreased excretion of basic drugs **Nursing Implications** - Assess for allergies and preexisting conditions that may restrict the use of antacids, such as: - Fluid imbalances - Renal disease - CHF - Pregnancy GI obstruction - Patients with CHF or hypertension should use low-sodium antacids - Riopan, - Maalox - Mylanta II. - Use with caution with other medications due to the many drug interactions. - Most medications should be given 1 to 2 hours after giving an antacid. - Antacids may cause premature dissolving of enteric-coated medications, resulting in stomach upset. - Be sure that chewable tablets are chewed thoroughly, and liquid forms are shaken well before giving. - Administer with at least 8 ounces of water to enhance absorption (except for the "rapid dissolve" forms). - Caffeine, alcohol, harsh spices, and black pepper may aggravate the underlying GI condition. - Monitor for **side effects**: - Nausea, vomiting, abdominal pain, diarrhea - With calcium-containing products: constipation, acid rebound - Monitor for **therapeutic response**: - Notify heath care provider if symptoms are not relieved. b. **H~2~ Antagonist Medications** **H~2~ Antagonists** (tidine) - Reduce acid secretion - All available OTC - Most popular drugs for treatment of acid-related disorders - **cimetidine** (Tagamet) - famotidine (Pepcid) - nizatidine (Axid) - ranitidine (Zantac) **Mechanism of Action** - Block histamine (H~2~) at the receptors of acid-producing parietal cells - Production of hydrogen ions is reduced, resulting in decreased production of HCl **Drug Effect** - Suppressed acid secretion in the stomach **Therapeutic Uses** - Shown to be effective for: - Gastric ulcer - Gastroesophageal reflux disease (GERD) - Upper GI Duodenal ulcer (with or - bleeding without H. pylori) - May be effective for: - Stress ulcers - Peptic esophagitis - Prevention and management of allergic conditions, when used with H~1~ blockers **Side Effects** - Overall, less than 3% incidence of side effects - **Cimetidine** may induce impotence and gynecomastia **Drug interaction** - **Cimetidine** - Binds with P-450 microsomal oxidase system in the liver, resulting in inhibited oxidation of many drugs and increased drug levels - All H~2~ antagonists may inhibit the absorption of drugs that require an acidic GI environment for absorption - SMOKING has been shown to decrease the effectiveness of H~2~ blockers **Nursing Implications** - Assess for allergies and impaired renal or liver function. - Use with caution in patients who are confused, disoriented, or elderly. - Take 1 hour before or after antacids. - Ranitidine may be given intravenously; follow administration guidelines. - \*Take tidine before you dine c. **Proton Pump Inhibitor Medications** - The parietal cells release positive hydrogen ions (protons) during HCl production. - This process is called the "proton pump." - H~2~ blockers and antihistamines do not stop the action of this pump. - \*PPI Pause acid pump production **Mechanism of Action** **Irreversibly bind to H+/K+ ATPase enzyme.** - This bond prevents the movement of hydrogen ions from the parietal cell into the stomach. - Result: Achlorhydria---ALL gastric acid secretion\ is blocked. (low acid- **p**otential infection) - In order to return to normal acid secretion, the parietal cell must synthesize new H+/K+ ATPase. **Drug Effect** (**p**razole) - Total inhibition of gastric acid secretion - lansoprazole (Prevacid) - omeprazole (Prilosec) - rabeprazole (Aciphex) - pantoprazole (Protonix) - esomeprazole (Nexium) **Therapeutic Uses** - GERD maintenance therapy - Erosive esophagitis - Short-term treatment of active duodenal and benign gastric ulcers - Zollinger-Ellison syndrome - Treatment of H. **py**lori-induced ulcers - Safe for short-term therapy - Incidence low and uncommon - Assess for allergies and history of liver disease - **Pantoprazole** is the only proton pump inhibitor available for **parenteral** administration, and can be used for patients who are unable to take oral medications - May increase serum levels of diazepam, phenytoin, and cause increased chance for bleeding with warfarin - Instruct the patient taking omeprazole: - It should be taken **before meals**. (prior meals) - The capsule should be swallowed whole, not crushed, opened or chewed. - It may be given with antacids. - Emphasize that the treatment will be short-term. (**po**rous spongy bones) d. **Other Medications** - **sucralfate (Carafate)** - Cytoprotective agent - Used for stress ulcers, erosions, PUD - Attracted to and binds to the base of ulcers and erosions, forming a protective barrier over these areas - Protects these areas from pepsin, which normally breaks down proteins (making ulcers worse) - Little absorption from the gut - May cause constipation, nausea, and dry mouth - May impair absorption of other drugs, especially tetracycline - Binds with phosphate; may be used in chronic renal failure to reduce phosphate levels - Do not administer with other medications - **misoprostol (Cytotec)** - Synthetic prostaglandin analogue - Prostaglandins have cytoprotective activity: - Protect gastric mucosa from injury by enhancing local production of mucus or bicarbonate - Promote local cell regeneration - Help to maintain mucosal blood flow - Used for prevention of NSAID-induced gastric ulcers - Doses that are therapeutic enough to treat duodenal ulcers often produce abdominal cramps, diarrhea 2. **Anti-Diarrheal Medications** - Abnormal frequent passage of loose stools or - Abnormal passage of stools with increased frequency, fluidity, and weight, or with increased stool water excretion - **Acute Diarrhea** - Sudden onset in a previously healthy person - Lasts from 3 days to 2 weeks - Self-limiting - Resolves without sequelae - Bacteria - Viral - Drug-induced hyperthyroidism - Nutritional Protozoal - - **Chronic Diarrhea** - Lasts for over 3 to 4 weeks - Associated with recurring passage of diarrheal stools, fever, loss of appetite, nausea, vomiting, weight loss, and chronic weakness - Tumors - Diabetes - Addison's disease - Irritable bowel syndrome ---------------------------- ------------------------------- -------------------------------------------------------------------------------------- **Type** **Prototype** **Action** **Local reflex inhibitor** Bismuth subsalicylate Locally coats the lining of the GIT to *soothe irritation* **Local anti-motility** Loperamide Directly inhibits the intestinal muscle activity to *[SLOW peristalsis]* **Central acting agent** Opium derivatives (paregoric) *Stops GIT spasm by CNS action* ---------------------------- ------------------------------- -------------------------------------------------------------------------------------- **Mechanism of Action** a. **Adsorbents** - Coat the walls of the GI tract - Bind to the causative bacteria or toxin, which\ are then eliminated through the stool - bismuth subsalicylate (Pepto-Bismol) - kaolin-pectin, activated charcoal - attapulgite (Kaopectate) b. **Anticholinergics** - Decrease intestinal muscle tone and peristalsis of GI tract - Result: slowing the movement of fecal matter through the GI tract - belladonna alkaloids (Donnatal) - atropine - hyoscyamine **Side effects** (BHUD) - Urinary retention, hesitancy, impotence - Headache, dizziness, confusion, anxiety, drowsiness - Dry skin, rash, flushing - Blurred vision, photophobia, increased\ intraocular pressure c. **Intestinal Flora Modifiers** - Bacterial cultures of Lactobacillus organisms\ work by: - Supplying missing bacteria to the GI tract - Suppressing the growth of diarrhea-causing bacteria - Lactobacillus acidophilus (Lactinex) d. **Opiates** - Decrease bowel motility and relieve rectal spasms - Decrease transit time through the bowel, allowing more time for water and electrolytes to be absorbed - paregoric, - opium tincture - codeine - loperamide - diphenoxylate **Side Effects** - Drowsiness, sedation, dizziness, lethargy - Nausea, vomiting, anorexia, constipation - Respiratory depression - Bradycardia, palpitations, hypotension - Urinary retention - Flushing, rash, urticaria **Interactions** - **Adsorbents** decrease the absorption of many agents, including digoxin, clindamycin, quinidine, and hypoglycemic agents - **Adsorbents** cause increased bleeding times when given with anticoagulants - Antacids can decrease effects of anticholinergic antidiarrheal agents **Nursing Implications** - Obtain thorough history of bowel patterns, general state of health, and recent history of illness or dietary changes, and assess for allergies. - DO NOT give bismuth subsalicylate to children under age 16 or teenagers with chicken pox because of the risk of Reye's syndrome. - Use adsorbents carefully in elderly patients or those with decreased **bleeding time, clotting disorders, recent bowel** **surgery,\ or confusion**. - Anticholinergics should not be administered to patients with a history of glaucoma, BPH, urinary retention, recent bladder surgery, cardiac problems, or myasthenia gravis - Teach patients to take medications exactly as prescribed and to be aware of their fluid intake and dietary changes. - Assess fluid volume status; intake and output; and mucous membranes before, during, and after initiation of treatment - Teach patients to notify their physician immediately if symptoms persist. - Monitor for therapeutic effect. 3. **Laxative Medications** **Constipation** - Abnormally infrequent and difficult passage of feces through the lower GI tract. - Symptom, not a disease - Disorder of movement through the colon and/or rectum - Can be caused by a variety of diseases\ or drugs **Causes** a. **Metabolic and endocrine disorders** - Diabetes, hypothyroidism, pregnancy b. **Neurogenic** - Autonomic neuropathy, multiple sclerosis, spinal cord lesions, Parkinson's disease, CVA c. **Adverse drug effects** - Analgesics, anticholinergics, iron supplements, opiates, aluminum antacids, calcium antacids d. **Lifestyle** - Poor bowel movement habits: voluntary refusal to defecate resulting in constipation - Diet: poor fluid intake and/or low-residue (roughage) diet, or excessive consumption of dairy products - Physical inactivity - Psychological factors: stress, anxiety, hypochondria **Laxatives Mechanism of Action** a. **Bulk-forming** - High fiber - Absorbs water to increase bulk - Distends bowel to initiate reflex bowel activity - psyllium (Metamucil), - methylcellulose (Citrucel), - polycarbophil - Acute and chronic constipation\ irritable bowel syndrome - Diverticulosis - Impaction and fluid overload b. **Emollient** - Stool softeners and lubricants - Promote more water and fat in the stools - Lubricate the fecal material and intestinal walls - Stool softenerdocusate salts Colace, Surfak - Lubricants: mineral oil - Acute and chronic constipation - Softening of fecal impaction - Facilitation of BMs in anorectal conditions - Skin rashes - Decreased absorption of vitamins c. **Hyperosmotic** - Increase fecal water content - Result: bowel distention, increased peristalsis,\ and evacuation - polyethylene glycol (GoLYTELY), - sorbitol - glycerin - lactulose (Chronulac) - Chronic constipation - Diagnostic and surgical preps - Abdominal bloating, rectal irritation d. **Saline** - Increase osmotic pressure within the intestinal tract, causing more water to enter the intestines - Result: bowel distention, increased peristalsis, and evacuation - magnesium sulfate (Epsom salts) - magnesium hydroxide (MOM) - magnesium citrate - sodium phosphate (Fleet Phospho-Soda) - Constipation - Diagnostic and surgical preps - Removal of helminths and parasites - Magnesium toxicity (with renal insufficiency) - Cramping - Diarrhea - increased thirst e. **Stimulant** - Increases peristalsis via intestinal nerve stimulation - castor oil - senna - cascara - bisacodyl **Therapeutic Uses** - Acute constipation - Diagnostic and surgical\ bowel preps - Nutrient malabsorption - Skin - Rashes - gastric irritation - rectal irritation - **All laxatives can cause electrolyte imbalances!!!** ------------------------------ ---------------------- --------------------------------------------------------------------------------------- **Type** **Prototype** **Action** Chemical stimulants Bisacodyl (Dulcolax) Direct stimulation of the GIT nerves Irritant laxatives Mechanical (bulk) stimulants Lactulose Increased fluid content of the fecal material causing stimulation of the local reflex Lubricants Docusate Lubricating the intestinal material to promote passage through the GIT Mineral oil ------------------------------ ---------------------- --------------------------------------------------------------------------------------- **Nursing Implications** - Obtain a thorough history of presenting symptoms, elimination patterns, and allergies. - Assess fluid and electrolytes before\ initiating therapy. - Patients should not take a laxative or cathartic if they are experiencing nausea, vomiting, and/or abdominal pain. - A healthy, high-fiber diet and increased\ fluid intake should be encouraged as an alternative to laxative use. - Long-term use of laxatives often results in decreased bowel tone and may lead to dependency. - All laxative tablets should be swallowed whole, not crushed or chewed, especially\ if enteric-coated. - Patients should take all laxative tablets with 6 to 8 ounces of water. - Patients should take bulk-forming laxatives as directed by the manufacturer with at least 240 mL (8 ounces) of water. - Bisacodyl and cascara sagrada should be given with water due to interactions with milk, antacids, and H2 blockers. - Patients should contact their physician if they experience severe abdominal pain, muscle weakness, cramps, and/or dizziness, which may indicate possible fluid or electrolyte loss. - Monitor for therapeutic effect 4. **Emetics & Anti-Emetics Medications** a. **Emetic Agent** - Prototype: Syrup of Ipecac **Pharmacodynamics** - Ipecac syrup irritates the GI mucosa locally, resulting to stimulation of the vomiting center - It acts within 20 minutes - **Clinical Use of ipecac** - To induce vomiting as a treatment for drug overdose and certain poisonings - **Contraindications** - Ingestion of CORROSIVE chemicals - Ingestion of petroleum products - Unconscious and convulsing patient **Side effects** - Nausea - Diarrhea - GI upset - Mild CNS depression - *[CARDIOTOXICITY if large amounts are absorbed in the body]* **Nursing Implications** **Assessment** - Nursing History- elicit the exact nature of poisoning - Physical Examination- CNS status and abdominal exam **Implementation** - Administer to *[conscious patient only]* - Administer ipecac as soon as possible - Administer with a *[large amount of water]* - Vomiting should occur within 20 minutes of the first dose*. Repeat the dose and expect vomiting to occur with 20 minutes* - Provide comfort measures like ready access to bathroom, assistance with ambulation - Offer support **Evaluation** - Evaluate patient response within 20 minutes of drug ingestion - Monitor for adverse effects - Evaluate effectiveness of comfort measures and teaching plan b. **Anti-emetics** - These are agents used to manage nausea and vomiting - They act either locally or centrally - In general, they may inhibit the chemoreceptor trigger zone in the medulla by blocking DOPAMINE receptor - Others act by decreasing the sensitivity of the vestibular apparatus ------------------------------------ -------------------------------------- ------------------------------------------------------------------------------------------------- --------------------------------------------------- **Anti-emetic types** **Common examples** **Pharmacodynamics** **Clinical Use** Phenothiazines Prochlorperazine, Promethazine Centrally block the vomiting center in the medulla N/V associated w/ anesthesia, intractable hiccups Non-phenothiazines Metoclopramide Reduces the responsiveness of the nerve cell in the medulla; also blocks the dopamine receptors N/V associated w/ chemical stimulation Anticholinergics & Antihistaminics Meclizine, buclizine Block the transmission of the impulses to the medulla N/V associated w/ motion sickness Serotonin Receptor blockers *["setron"-]* dolasetron Centrally and locally inhibits the serotonin receptors N/V associated w/ chemo Miscellaneous Dronabinol, hydroxyzine Act in the CNS , either in the medulla or in the cortex N/V associated with chemo ------------------------------------ -------------------------------------- ------------------------------------------------------------------------------------------------- --------------------------------------------------- **Indications** - Prevention and treatment of vomiting - Motion sickness **Contraindications** - Severe CNS depression - Severe liver dysfunction **Pharmacokinetics** - Oral absorption is good if vomiting is not present - IV drugs can be given if vomiting is active - Most drugs are metabolized in the liver excreted in the kidneys - PHOTHOSENSITIVITY - Drowsiness, dizziness, weakness and tremors and DEHYDRATON - Phenothiazines= autonomic [anti-cholinergic effects] like dry mouth, nasal congestion and urinary retention - Metoclopramide= EPS due to dopamine receptor blockage **Nursing Implications** **Assessment** - History- elicit allergy, impaired hepatic function and CNS depression - Physical Examination- CNS status and abdominal examination - Laboratory test- Liver function studies **Nursing Diagnosis** - Alteration in comfort: pain - High risk for injury - Knowledge deficit **Implementation** - Assess patient's intake of other drugs that may cause dangerous drug interaction - Emphasize that this is given on a short term basis - Provide comfort and safety measures - Advise to change position slowly - Avoid hazardous activities - Provide mouth care and ice chips - Monitor for dehydration and offer fluids if it occurs - Protect from sun exposure - Sunscreens - Protective covering - Provide health teaching **Evaluation** - Monitor for the drug effectiveness - Relief of nausea and vomiting - Monitor for adverse effects - Evaluate effectiveness of comfort measures and teaching plan