ENDOCRINE DRUGS

ENDOCRINE MEDICATIONS
General indications of Endocrine Drugs Hormonal replacement Contraception Miscellaneous Cancer treatment

Side-effects of thionamides N/V, drowsiness, lethargy, bradycardia, skin rash GI complaints Arthralgia, myalgia AGRANULOCYTOSIS Most important to monitor Side-effects of Iodine solutions Lugols Most common adverse effects is HYPOTHYROIDISM Iodism= metallic taste, burning in the mouth, sore teeth and gums, diarrhea, stomach upset Lugols Solution Used to decrease the vascularity and size of the thyroid (in preparation for thyroid surgery) T3 and T4 production diminishes Given per orem, can be diluted with juice, administered WITH foods Use straw to decrease staining Monitor iodism STEROIDS Replaces the steroids in the body Cortisol, cortisone, betamethasone, and hydrocortisone These drugs enter the cells and bind to receptors They inhibit the enzyme phospholipase Corticosteroids are used topically and locally to achieve the desired anti-inflammatory effects at a particular site Examples: 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

ANTI-DIURETIC HORMONES Enhance re-absorption of water in the kidneys Increases water permeability in the renal collecting ducts Also stimulates VASOCONSTRICTION and increases the blood pressure Therapeutic Indications Hormonal replacement Used in diagnostic procedure Used to control the hemorrhage in variceal bleeding Treatment of enuresis Used in DI 1. Desmopressin and Lypressin intranasally 2. Pitressin IntraMuscularly SIDE-effects Flushing and headache Water intoxication CVS: heart block, MI Renal: hyponatremia Gangrene due to vasoconstriction

THYROID MEDICATIONS
THYROID HORMONES These products are used to treat the manifestations of hypothyroidism Replace hormonal deficit in the treatment of HYPOTHYROIDSM Levothyroxine (Synthroid) Liothyroxine (Cytomel) Thyroid dessicated Liotrix (Thyrolar) Actions Replace both T3 and T4 Increase metabolic rate Increase O2 consumption Increase HR, RR, BP Indications Hypothyroidism Diagnostic suppression test Side-effects Nausea and Vomiting Signs of increased metabolism= tachycardia, hypertension, cardiac arrhythmias, anxiety, headache, tremors, palpitations ANTI-THYROID medications 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 1. Methimazole (Tapazole) 2. PTU (prophylthiouracil) 3. Iodine solution- SSKI and Lugols solution Indications Graves dosease Thyrotoxicosis Absorption is good orally

DM DRUG THERAPY
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 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 This may be grouped into several categories according to: 1. 2. 3. 4. 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 1. Human insulin preparations have a shorter duration of action than animal source 2. 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 3. ONLY Regular insulin can be used INTRAVENOUSLY! 4. Insulin are measured in INTERNATIONAL UNITS or iu 5. There is a specified insulin injection calibrated in units Mixed insulin are also available The most common of which is the 70-30 insulin Made up of 70% NPH and 30% regular insulin in the vial

8. 9.

10. 11. 12. 13.

Comparison of Insulin Peak action

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 areABDOMEN, 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 techniquecommonly, 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

RAPID ACTING INSULIN Lispro (Humalog) and Insulin Aspart (Novolog) Produces a more rapid effect and with a shorter duration than any other insulin preparation ONSET - 5-15 minutes PEAK - 1 hour DURATION - 3 hours REGULAR INSULIN Also called Short-acting insulin R Usually Clear solution administered 30 minutes before a meal ONSET - 30 minutes to 1 hour PEAK - 2 to 4 hours DURATION - 4 to 6 hours INTERMEDIATE ACTING INSULIN Called NPH or LENTE Appears white and cloudy ONSET - 2-4 hours PEAK - 4 to 6-12 hours DURATION - 16-20 hours LONG ACTING INSULIN UltraLENTE Referred to as peakless insulin ONSET - 6-8 hours PEAK - 12-16 hours DURATION - 20-30 hours

ORAL HYPOGLYCEMIC AGENTS These may be effective when used in TYPE 2 DM that cannot be treated with diet and exercise These are NEVER used in pregnancy! There are several agents: Sulfonylureas Biguanides Alpha-glucosidase inhibitors Thiazolidinediones Meglitinides These drugs are given per orem and are effective only in type 2 DM Common adverse effects include: Hypoglycemia Diarrhea, jaundice, nausea and heartburn Anemia , photosensitivity SULFONYLUREAS MOA - stimulates beta cells of the pancreas to secrete insulin Classified as to generations- first and second generations FIRST GENERATION Acetoheximide Chlorpropamide Tolazamide Tolbutamide SECOND GENERATION Glipizide Glyburide Glibenclamide Glimepiride

HEALTH TEACHING Regarding Insulin SELF- Administration 1. Insulin is administered at home subcutaneously 2. Cloudy insulin should be thoroughly mixed by gently inverting the vial or ROLLING between the hands 3. Insulin NOT IN USE should be stored in the refrigerator, BUT avoid freezing/extreme temperature 4. Insulin IN USE should be kept at room temperature to reduce local irritation at the injection site 5. INSULIN may be kept at room temperature up to 1 month 6. Select syringes that match the insulin concentration. U-100 means 100 units per mL 7. Instruct the client to draw up the REGULAR (clear) Insulin FIRST before drawing the intermediate acting (cloudy) insulin

The most common side effects of these medications are Gastro-intestinal upset and dermatologic reactions. HYPOGLYCEMIA is also a very important side-effect Given 30 minutes before meals- breakfast Chlorpropamide has a very long duration of action. This also produces a disulfiram-like reaction when taken with alcohol Second generation drugs have shorter duration with metabolism in the kidney and liver and are the choice for elderly patients

BIGUANIDES MOA - Facilitate the action of insulin on the peripheral receptors These can only be used in the presence of insulin BIGUANIDES= formin They have no effect on the beta cells of the pancreas Metformin (Glucophage) and Phenformin are examples The most important side effect is LACTIC ACIDOSIS These are not given to patient with renal impairment These drugs are usually given with a sulfonylurea to enhance the glucose-lowering effect more than the use of each drug individually

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 Examples of AGI are Acarbose and Miglitol They are not absorbed systemically and are very safe They can be used alone or in combination with other OHA Side-effect if used with other drug is HYPOGLYCEMIA Note that sucrose absorption is impaired and IV glucose is the therapy for the hypoglycemia THIAZOLIDINEDIONES MOA - Enhance insulin action at the receptor site They do not stimulate insulin secretion Examples- Rosiglitazone, Pioglitazone These drugs affect LIVER FUNCTION Can cause resumption of OVULATION in perimenopausal anovulatory women MEGLITINIDES MOA - Stimulate the secretion of insulin by the beta cells Examples- Repaglinide and Nateglinide They have a shorter duration and fast action Should be taken BEFORE meals to stimulate the release of insulin from the pancreas Principal side-effect of meglitinides- hypoglycemia Can be used alone or in combination Reproductive Hormones Gonadal hormones include agents that affect the female and male reproductive cycle Female hormones: ESTROGENS, PROGESTINS and ovarian hormones Male hormones: ANDROGENS and anabolic steroids The GENERAL 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 Estrogens Conjugated estrogen Estradiol Ethinyl estradiol Diethylstilbesterol (DES) Clomiphene Progestins Medroxyprogesterone acetate (Provera) Megestrol Norethindrone Levonorgestrel (Norplant) Norgestrel Norethindrone acetate Androgens Testosterone cypionate Methyltestosterone Fluoxymesterone Aqueous testosterone MALE Replacement therapy, metabolic stimulators and treatment of some tumors

Oral Contraceptive Pills Two types are available: Combination estrogen and progesterone AND progestins only OCP 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 OCP INDICATORS Suppression of ovulation for prevention of pregnancy Regulation of menstrual cycle and management of dysfunctional bleeding Treatment of endometriosis OCP KINETICS Easily absorbed orally NORPLANT provides 5 years of contraception Provera provides 3 months of protection Metabolized and excreted in liver o Oral Not to be used in patients with history of, hypertension, thromboemoblic or CVA disease o Not given in certain cancers o Contraindicates in pregnancy o SMOKING should be avoided under therapy OCP DRUG INTERACTION Rifampicin, penicillin and tetracycline REDUCE effectiveness of contraception Benzodiazepines decrease the levels of OCP 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 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 can be: 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