Pharmacology of the Selected Endocrine Drugs

2005

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Fig. 10.10

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Fig. 10.17

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Fig. 10.19

Endocrine Medications
Hormonal replacement

Endocrine Medications
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

Endocrine Medications
Therapeutic Indications 1. Hormonal replacement 2. Used in diagnostic procedure 3. Used to control the hemorrhage in variceal bleeding 4. Treatment of enuresis

Endocrine Medications
Used in DI 1. Desmopressin and Lypressin intranasally 2. Pitressin IntraMuscularly

Endocrine Medications
Anti-diuretic hormones 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

Thyroid Medications
Thyroid hormones Levothyroxine (Synthroid) Liothyroxine (Cytomel) Thyroid dessicated Liotrix (Thyrolar)

Thyroid Medications
Thyroid hormones: Actions Replaces both T3 and T4 Increases metabolic rate

Thyroid Medications
Thyroid hormones: Actions Increase the metabolic rate Increase O2 consumption Increase HR, RR, BP

Thyroid Medications
Thyroid hormones: Indications Hypothyroidism Diagnostic suppression test

Thyroid Medications
Thyroid hormones Side-effects 1. Nausea and Vomiting 2. Signs of increased metabolism= tachycardia, hypertension, cardiac arrhythmias, anxiety, headache, tremors, palpitations

Thyroid Medications
Thyroid hormones : Nursing responsibility

1. Monitor weight, VS 2. Instruct client to take daily medication the same time each morning WITHOUT FOOD Monitor blood tests to check the activity of thyroid

Thyroid Medications
Thyroid hormones: Nursing responsibility

3. Advise to report palpitation, tachycardia, and chest pain 4. Instruct to avoid foods that inhibit thyroid secretions like cabbage, spinach and radishes

ANTI-Thyroid Medications
ANTI-THYROID medications The thyroid becomes oversaturated with iodine and stop producing thyroid hormone

ANTI-Thyroid Medications
ANTI-THYROID medications Drugs used to BLOCK the thyroid hormones and treat hyperthyroidism Inhibit the synthesis of thyroid hormones

ANTI-Thyroid Medications
ANTI-THYROID medications 1. Methimazole (Tapazole) 2. PTU (prophylthiouracil) 3. Iodine solution- SSKI and Lugols solution

ANTI-Thyroid Medications
ANTI-THYROID medications: Indications 1. Graves dosease 2. Thyrotoxicosis

ANTI-Thyroid Medications
ANTI-THYROID medications: Absorption is good orally

ANTI-Thyroid Medications
ANTI-THYROID medications Side-effects of thionamides
N/V, drowsiness, lethargy, bradycardia, skin rash GI complaints Arthralgia, myalgia AGRANULOCYTOSIS
Most important to monitor

ANTI-Thyroid Medications
ANTI-THYROID medications 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

ANTI-Thyroid Medications
ANTI-THYROID medications Nursing responsibilities 1. Monitor VS, T3 and T4, weight 2. The medications WITH MEALS to avoid gastric upset

ANTI-Thyroid Medications
ANTI-THYROID medications Nursing responsibilities

3. Instruct to report SORE THROAT or unexplained FEVER 4. Monitor for signs of hypothyroidism.
Instruct not to stop abrupt medication

ANTI-Thyroid Medications
ANTI-THYROID medications 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

STEROIDS

These drugs enter the cells and bind to receptors They inhibit the enzyme phospholipase

STEROIDS
Corticosteroids are used topically and locally to achieve the desired anti-inflammatory effects at a particular site Examples: Prednisone Bethamethasone Prednisolone Fludrocortisone

STEROIDS
Side-effects HYPERglycemia Increased susceptibility to infection (immunosuppression) Hypokalemia Edema Peptic ulceration

STEROIDS
Side-effects If high dosesosteoporosis, growth retardation, peptic ulcer, hypertension, cataract, mood changes, hirsutism, and fragile skin

STEROIDS

Nursing responsibilities 1. Monitor VS, electrolytes, glucose 2. Monitor weight edema and I/O

STEROIDS
Nursing responsibilities 3. Protect patient from infection 4. Handle patient gently 5. Instruct to take meds WITH MEALS to prevent gastric ulcer formation

STEROIDS
Nursing responsibilities 6. Caution the patient NOT to abruptly stop the drug 7. Drug is tapered to allow the adrenal gland to secrete endogenous hormones

STEROIDS
Evaluation: The drugs are effective if there is: 1. Relief of signs and symptoms of inflammation 2. Return of adrenal function to normal

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.

DRUG THERAPY and MANAGEMENT

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.

Diabetes Mellitus
DRUG THERAPY and MANAGEMENT TYPE 2 DM may have decreased insulin production, ORAL agents that stimulate insulin production are usually employed.

Diabetes Mellitus
PHARMACOLOGIC INSULIN This may be grouped into several categories according to: 1. Source- Human, pig, or cow 2. Onset of action- Rapid-acting, short-acting, intermediate-acting, long-acting and very long acting

Diabetes Mellitus
PHARMACOLOGIC INSULIN This may be grouped into several categories according to: 3. Pure or mixed concentration 4. Manufacturer of drug

Diabetes Mellitus
GENERALITIES 1. Human insulin preparations have a shorter duration of action than animal source

Diabetes Mellitus
GENERALITIES 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

Diabetes Mellitus

3. ONLY Regular insulin can be used INTRAVENOUSLY!

Diabetes Mellitus
4. Insulin are measured in INTERNATIONAL UNITS or iu 5. There is a specified insulin injection calibrated in units

Diabetes Mellitus
Mixed insulin are also available The msot 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 Type ULTRA-acting RAPID acting Intermediate acting Long Acting Example Lispro Regular Insulin NPH and Lente Ultra-lente Onset
15 minutes 1 hour 1 to 2 hrs 4-8 hrs

PEAK
1 hour 2-4 hrs 6-8 hrs to 12 hrs 10-20 hrs

Diabetes Mellitus
RAPID ACTING INSULIN Lispro (Humalog) and Insulin Aspart (Novolog) Produces a more rapid effect and with a shorter duration than any other insulin preparation

Diabetes Mellitus
RAPID ACTING INSULIN ONSET- 5-15 minutes PEAK- 1 hour DURATION- 3 hours Instruct patient to eat within 5 to 15 minutes after injection

Diabetes Mellitus
REGULAR INSULIN Also called Short-acting insulin R Usually Clear solution administered 30 minutes before a meal

Diabetes Mellitus

REGULAR INSULIN ONSET- 30 minutes to 1 hour PEAK- 2 to 4 hours DURATION- 4 to 6 hours

Diabetes Mellitus

INTERMEDIATE ACTING INSULIN Called NPH or LENTE Appears white and cloudy

Diabetes Mellitus

INTERMEDIATE ACTING INSULIN ONSET- 2-4 hours PEAK- 4 to 6-12 hours DURATION- 16-20 hours

Diabetes Mellitus

LONG- ACTING INSULIN UltraLENTE Referred to as peakless insulin

Diabetes Mellitus

LONG- ACTING INSULIN ONSET- 6-8 hours PEAK- 12-16 hours DURATION- 20-30 hours

Diabetes Mellitus

HEALTH TEACHING Regarding Insulin SELFAdministration 1. Insulin is administered at home subcutaneously

Diabetes Mellitus
HEALTH TEACHING Regarding Insulin SELF- Administration 2. Cloudy insulin should be thoroughly mixed by gently inverting the vial or ROLLING between the hands

Diabetes Mellitus
HEALTH TEACHING Regarding Insulin SELF- Administration 3. Insulin NOT IN USE should be stored in the refrigerator, BUT avoid freezing/extreme temperature

Diabetes Mellitus

4. Insulin IN USE should be kept at room temperature to reduce local irritation at the injection site

Diabetes Mellitus

5. INSULIN may be kept at room temperature up to 1 month

Diabetes Mellitus

6. Select syringes that match the insulin concentration. U-100 means 100 units per mL

Diabetes Mellitus
7. Instruct the client to draw up the REGULAR (clear) Insulin FIRST before drawing the intermediate acting (cloudy) insulin

Diabetes Mellitus

8. 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

Diabetes Mellitus
9. The four main areas for insulin injection areABDOMEN, UPPER ARMS, THIGHS and HIPS

Diabetes Mellitus
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.

Diabetes Mellitus
10. Alcohol may not be used to cleanse the skin 11. Utilize the subcutaneous injection techniquecommonly, a 45-90 degree angle.

Diabetes Mellitus

12. No need to instruct for aspirating the needle 13. Properly discard the syringe after use.

Diabetes Mellitus
T-I-E Test blood Inject insulin food

Eat

Diabetes Mellitus
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!

Diabetes Mellitus
ORAL HYPOGLYCEMIC AGENTS There are several agents: Sulfonylureas Biguanides Alpha-glucosidase inhibitors Thiazolidinediones Meglitinides

Diabetes Mellitus
ORAL HYPOGLYCEMIC AGENTS 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

Diabetes Mellitus
ORAL HYPOGLYCEMIC AGENTS General Nursing Consideration 1. Observe for manifestations of hypoglycemia 2. Assess for allergic reaction 3. Instruct to take the medication at the same time each day 4. Caution to avoid taking other drugs without consultation with physician

Diabetes Mellitus
ORAL HYPOGLYCEMIC AGENTS General Nursing Consideration 5. THESE medications SHOULD NEVER be given to pregnant women, so rule out pregnancy 6. Instruct to wear sunscreen 7. Advise to bring simple sugar to be taken when hypoglycemic episodes occur

Diabetes Mellitus

SULFONYLUREAS MOA- stimulates the beta cells of the pancreas to secrete insulin Classified as to generations- first and second generations

Diabetes Mellitus
SULFONYLUREAS FIRST GENERATIONAcetoheximide, Chlorpropamide, Tolazamide and Tolbutamide SECOND GENERATION- Glipizide, Glyburide, Glibenclamide, Glimepiride

Diabetes Mellitus: Sulfonylureas

The most common side effects of these medications are Gastrointestinal upset and dermatologic reactions. HYPOGLYCEMIA is also a very important side-effect Given 30 minutes before mealsbreakfast

Diabetes Mellitus: Sulfonylureas

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

Diabetes Mellitus
BIGUANIDES MOA- Facilitate the action of insulin on the peripheral receptors These can only be used in the presence of insulin

Diabetes Mellitus
BIGUANIDES= formin They have no effect on the beta cells of the pancreas Metformin (Glucophage) and Phenformin are examples

Diabetes Mellitus: Biguanides

The most important side effect is LACTIC ACIDOSIS! These are not given to patient with renal impairment

Diabetes Mellitus: Biguanides

These drugs are usually given with a sulfonylurea to enhance the glucose-lowering effect more than the use of each drug individually

Diabetes Mellitus
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

Diabetes Mellitus
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

Diabetes Mellitus
Side-effect if used with other drug is HYPOGLYCEMIA Note that sucrose absorption is impaired and IV glucose is the therapy for the hypoglycemia

Diabetes Mellitus

THIAZOLIDINEDIONES MOA- Enhance insulin action at the receptor site They do not stimulate insulin secretion

Diabetes Mellitus
THIAZOLIDINEDIONES Examples- Rosiglitazone, Pioglitazone These drugs affect LIVER FUNCTION Can cause resumption of OVULATION in peri-menopausal anovulatory women

Diabetes Mellitus

MEGLITINIDES MOA- Stimulate the secretion of insulin by the beta cells Examples- Repaglinide and Nateglinide

Diabetes Mellitus
MEGLITINIDES They have a shorter duration and fast action Should be taken BEFORE meals to stimulate the release of insulin from the pancreas

Diabetes Mellitus

MEGLITINIDES 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 include ESTROGENS, PROGESTINS and ovarian hormones Male hormones include ANDROGENS and anabolic steroids

Reproductive Hormones
The GENERAL Mechanism of Action These hormones interfere with the normal cycle of hormone balance

Reproductive Hormones
INDICATIONS 1. FEMALE: Hormonal replacement therapy, oral contraception, treatment of infertility and management of some tumors 2. MALE: replacement therapy, metabolic stimulators and treatment of some tumors

Reproductive Hormones
Estrogens Conjugated estrogen Estradiol Ethinyl estradiol Diethylstilbesterol (DES) Clomiphene

Reproductive Hormones
Progestins Medroxyprogesterone acetate (Provera) Megestrol Norethindrone Levonorgestrel (Norplant) Norgestrel Norethindrone acetate

Reproductive Hormones
Androgens Testosterone cypionate Methyltestosterone Fluoxymesterone Aqueous testosterone

Reproductive Hormones
Oral Contraceptive Pills Two types are available: Combination estrogen and progesterone AND progestins only

Reproductive Hormones
Oral Contraceptive Pills: 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

Reproductive Hormones
Oral Contraceptive Pills: Indicators Suppression of ovulation for prevention of pregnancy Regulation of menstrual cycle and management of dysfunctional bleeding Treatment of endometriosis

Reproductive Hormones
Oral Contraceptive Pills: Kinetics Easily absorbed orally NORPLANT provides 5 years of contraception Provera provides 3 months of protection Metabolized and excreted in liver

Reproductive Hormones
Oral Contraceptive Pills: 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

Reproductive Hormones
Oral Contraceptive Pills: Drug Interaction Rifampicin, penicillin and tetracycline REDUCE effectiveness of contraception Benzodiazepines decrease the levels of OCP

Reproductive Hormones
Oral Contraceptive Pills: Side effects CNS: headache CV: Thromboembolic disease, MI, hypertension and pulmonary edema NAUSEA and cholestatic JAUNDICE Breast tenderness, weight gain, edema, breakthrough bleeding, acne

Reproductive hormones
Nursing Considerations 1. Assess for risk factors and the ability to comply with medications 2. 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

Reproductive hormones
Nursing Considerations 3. Teach the common side-effects and reassure that these will decrease in time 4. Instruct to use other means of contraception if antibiotics and anticonvulsants are also taken 5. WARNT 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

Clomiphene
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

Viagra (Sildenafil)
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

Viagra (Sildenafil)
Nursing consideration Assess for risk factors Instruct to take the drug ONE hour before sexual act Drug is taken orally