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ANTIGLYCEMICS
Biguanides
Uses:
1. Monotherapy in the treatment of type 2 diabetes or secondary diabetes where
there is capacity for pancreatic insulin production
2. Combination therapy in the treatment of type 2 diabetes.
Adverse Effects:
1. Abdominal discomfort and diarrhea
2. metallic taste, agitation, sweating and headache.
Precautions:
1. Contraindicated in clients with hepatic or renal dysfunction, a history of
alcoholism, or binge alocohol ingestion, or CHF.
2. Should be temporarily withheld in situations that predispose to acute renal
dysfunction.
3. Not recommended for individuals >80 years ild unless renal function is assessed.
4. use cautiously in persons with dehydration, hypoxia, or pituitary or thyroid
dysfunction.
5. Contraindicated in clients with renal dysfunction manifested with a serum
creatinine ≥1.4 mg/dL; 1.5 mg/dL in males; and ≥ 1.4 mg/dL in females
Alpha-Glucosidase Inhibitor
Act primarily by inhibiting alpha-glucosidase enzymes in the small intestine and alpha
amylase in the pancreas. This decreases the rate of complex carbohydrate metabolism.
The result is a reduced rate of glucose absorption postprandially (after a meal).
Uses:
1. Most effective in clients with type 2 NIDDM (Non Insulin Dependent Diabetes
Mellitus) who demonstrate a significant post meal hyperglycemia.
Adverse Effects:
1. Flatulence, bloating, and diarrhea.
2. Reductions in hematocrit have been observed, but are not associated with
congruent change in hemoglobin.
Precautions:
1. Not intended for use during pregnancy, lactation or by children.
2. Contraindicated with cirrhosis of the liver.
3. Contraindicated in clients with inflammatory bowel disease, chronic intestinal
disorders, or obstructive bowel disorders.
4. Hypoglycemia may occur if taken in combination with other hypoglycemic agents
5. Used with caution in clients with renal dysfunction manifested with a serum
creatinine >2.0 mg/dL.
Thiazolidinediones
Functions primarily by enhancing insulin action at the cell receptor and post receptor site
and decreases insulin resistance.
Uses:
1. Monotherapy in the treatment of Type 2 NIDDM or secondary diabetes where
there is capacity for pancreatic insulin production
2. Combination therapy in the treatment of Type 2 NIDDM.
Adverse Effects:
1. Can cause injury to the liver
2. Weight gain may occur.
3. Lower extremity edema.
4. GI discomfort.
5. Increase in plasma volume with associated decrease in hemoglobin and
hematocrit
Precautions:
1. Not intended for use during pregnancy, lactaion, or by children
2. May inhibit effectiveness of oral contraceptives.
3. May cause and increase in HDL and LDL.
4. At risk for hypoglycemia when taken in combination with other diabetes
medications.
ANTITHYROID AGENTS
S/S:
1. Tachycardia
2. Dysrhythmias
3. Restlessness
4. Insomia
5. Weak skeletal muscles
6. Increased body temperature
7. Weight loss despite increased foor intake.
Thyroid Crisis of “Storm”
– extremely high serum levels of thyroid hormone
– life threatening as it can lead to heart failure and coma.
Uses:
1. Suppress thyroid hormones synthesis and prevent the conversion of T4
(triiodothyronin) (contains 3 atoms of iodine) to T3 (thyroxine) (contains 4 atoms
of iodine).
2. Uses of thiomides in the treatment of hyperthyroidism:
a. Treatment of Grave’s disease
b. Suppression of thyroid hormone synthesis until radiation destroys thyroid
tissue.
c. Suppression of thyroid hormone synthesis before thyroid surgery to reduce
risk of thyroid crisis.
d. Treatment of thyroid crisis.
3. Radioactive iodine used to:
a. Destroy part of the thyroid tissue in Grave’s disease.
b. Treat some types of thyroid cancer.
c. Diagnose various thyroid disorders
4. Iodine preparations are used to :
a. Suppress thyroid function before surgery for hyperthyroidism.
b. Treat Grave’s disease
c. Treat thyroid crisis
d. Prevent thyroid damage resulting from exposure to radiation
Adverse Effects:
1. Excessive suppression of hormone-hypothyroidism
2. A/E of Thiomides: Rash, nausea, muscle aches, headache, dizziness, paresthesia.
3. Most harmful A/E: blood dyscrasias, agranulocytosis
a. Rare
b. Occurs in first 2 months of therapy
c. Early symptoms: sore throat and fever.
Precautions:
1. Contraindicates during pregnancy and lactation because the thyroid function of
the fetus/infant will be suppressed.
2. Periodic blood counts to detect agranulocytosis
3. Radioactive agents are contraindicated during pregnancy and lactaion
CORTICOSTEROIDS
- necessary for life
- accelerates rapidly in response to stress
- produced by the adrenal cortex
Physiologic Functions:
Glucocorticoids
- maintain adequate serum glucose for brain metabolism by
stimulating glucogenesis, promoting glycogen storage and
reducing peripheral glucose use.
- Promote breakdown of fats
- Inhibit synthesis of protein
- Maintain normal capillary permeability and vasomotor tone
- Maintain function of skeletal muscle
- Affect excitability of the CNS and moods
- Increase RBC’c
Example: Cortisol
Mineralocorticoids
- maintain fluid and electrolyte balance by increasing the renal
absorption of sodium and water and promoting the excretion of
potassium anf hydrogen
Example: Aldosterone
Disorders:
Cushing’s syndrome: adrenocortical hormone excess
Addison’s disease: adrenocortical hormone deficiency
Uses:
1. Physiologic dose is relatively low and intended to restore normal levels.
2. Pharmacologic dose is high and is used to treat a variety of non-endocrine
disorders.
3. Physiologic doses of corticosteroids are used for replacement therapy when there
is insufficiency such as Addison’s disease.
4. Pharmacologic dosages are used to treat:
a. inflammatory diseases
- rheumatoid arthritis
- chronic ulcerative colitis
- ocular inflammations
- nephritic syndromes
- liver disorder
b. allergic conditions
- status asthmaticus
- bronchial asthma
- allergic reactions
c. neoplastic diseases
- leukemias
- Hodgkin’s disease
5. Brain injured victims (suppress edema)
6. Skin conditions:
a. psoriasis
b. dermatitis
7. Opthalmic conditions (Topical ophthalmic preparations)
a. allergic conjunctivitis
b. corneal injury
c. suppression of graft rejection
d. prevention of post-op inflammation.
Adverse Effects:
1. Safe for short term treatment
2. Topical corticosteroids can have systemic effect and even toxicity with significant
absorption through the skin or mucus membrane.
3. Adverse effects of pharmacologic doses:
a. Increased risk of infection
b. Muscle weakness
c. Osteoporosis
d. Abnormal fat distribution (buffalo hump” “moon face” “potbelly”)
e. Mood swings
f. Water and sodium retention
Precautions:
1. Use cautiously with:
a. pregnancy
b. lactation
c. children
d. osteoporosis, peptic ulcer disease, cardiac or renal failure
2. Drug interactions
a. Hypokalemia with potassium depleting diuretics
b. Increased risk of digitalis toxicity with hypokalemia
c. Increased risk of gastric ulcers with NSAID’s
Examples:
1. Systemic:
a. Cortisone (Cortone)
b. Prednisone (Deltasone)
c. Betamethasone (Celestone)
2. Topical: Hydrocortisone
3. Inhaled: Beclomethasone (Vanceril)
4. Opthalmic: Prednisolone (AK-Pred)
Client Education:
1. All clients on corticosteroid therapy
a. always wear a medical alert tag noting that you take corticosteroids.
b. Always have an emergency supply of medication with you
c. Never stop taking medication without medical supervision
d. Take oral medications with food or milk to minimize GI irritation
e. Notify physician of the following:
- any sign of infection
- weight gain, edema
- blurred or cloudy vision
- pregnancy
- dark or tarry stools, abd’l pain
HORMONES
- the neurologic and endocrine systems maintain homeostasis.
Neurologic responses are generally rapis in onset and brief in
duration, whereas the endocrine system responds more slowly
and produces a long lasting effect.
Hormones which are secreted by the anterior pituitary produce the following effect:
- growth hormone: stimulates growth and by body tissues.
- Corticotrophin: stimulation of adrenal cortex
- Thyroid stimulating hormone: stimulation of thyroid gland
- Luteinizing hormone: stimulation of hormone production by
gonads
- Follicle stimulating hormone: stimulates growth of ovarian
follicles
- Prolactin: plays a role in milk production
- Melanocyte stimulating hormone: affect skin pigmentation
Hormones which are stored and released by the posterior pituitary and produce the
following effect:
- Antidiuretic: plays a role in water balance
- Oxytocin: initiates uterine contractions and causes milk to move
to the nipples
Uses:
1. Hormone replacement therapy for post menopausal women.
a. Prevents urogenital atrophy
b. Maintain bone mass
c. May protect against coronary artery disease and colon cancer
d. Suppresses vasomotor symptoms (hot flashes)
2. Promotion of normal sexual dev’t and function in girls with estrogen deficiency.
3. Androgen suppression in men with prostate cancer.
4. Oral contraception by inhibition of ovulation
Adverse Effects:
1. Risk for endometrial hyperplasia and carcinoma if used without progestin.
2. The use of estrogen with progestin may increase the risk of breast cancer.
3. The most common adverse effects of estrogen therapy are nausea, fluid retention,
and breast tenderness.
4. Less common adverse effects associated with high dosage:
a. headache
b. dizziness
c. depression
Precautions:
1. Estrogens are contraindicated with:
a. pregnancy and lactation
b. undiagnosed vaginal bleeding
c. estrogen-dependent cancers
d. coronary artery disease
e. breast carcinoma
f. liver tumors
Important Drugs:
1. Estrogen preparations PO, IM, IV, transdermal, and intravaginal use
2. Some common forms of estrogens used for HRT (hormone replacement therapy)
are:
a. Conjugated estrogens, equine
b. Conjugates estrogens, synthetic
c. DES (Diethylstilbestrol)
d. Estradiol
e. Estrone
Progesterone
- a progestin that plays a vital role in reproduction.
- Ovarian hormone
Uses:
1. Oral contraception
2. HRT (hormone replacement therapy)
3. Ovarian suppression to treat endometriosis, dysmenorrheal and uterine bleeding.
Adverse Effects:
1. Irregular vaginal bleeding
2. Teratogenic during the first four months of pregnancy
3. Nausea
4. Impaired glucose tolerance
5. Depression
6. Drowsiness
7. Insomia
8. Edema
9. Weight gain
Precautions:
1. Contraindicated with:
a. pregnancy
b. undiagnosed vaginal bleeding
c. cancer of the breast or reproductive organs
d. severe liver disease
Client Education:
1. Take oral progesterone with food or milk to decrease nausea
2. If pregnancy is suspected, STOP
3. Report: weight gain, pain and tenderness in legs, chest pain, mental depression
Androgens
- male sex hormones that are produces by the testes, the ovaries
and the adrenal cortex.
- Classes: Testosterone and testosterone esters, 17-alpha alkylates
androgens, danazol
- Testosterone most important androgen
Effects in Males:
1. Enlargement of testes, penis and scrotum
2. Increased body hair
3. Growth of bone and skeletal muscle
4. Enlargement of the larynx
5. Increased number of sebaceous glands
6. Beard development
7. Spermatogenesis
In Females:
1. Influence clitoral growth
2. Maintain normal libido
3. Have masculine effects (virilization), but only in the presence of ovarian
dysfunction
Uses:
1. In males to treat:
a. hypogonadism
b. cryptorchidism (undescended testes)
c. erectile dysfunction
2. In females to treat:
a. endometriosis
b. fibrocystic breast disease
c. hereditary angioedema
d. some menopausal symptoms
Adverse Effects:
1. Virilization is the most common adverse effect
a. Adult males normal testosterone secretion may experience:
i. increased sexual desire
ii. reduce sperm count
iii. prostate enlargement
iv. priapism
b. Woman may experience:
i. deepening of the voice
ii. increased hair growth
iii. menstrual irregularities
c. In prepubertal boys:
i. premature sexual development may occur
ii. premature epiphyseal closure may occur, decreasing adult height.
d. Masculinization of the female fetus
2. Decreased HDL; increased LDL
3. Hepatotoxicity (jaundice, hepatitis, liver cancer) has occurred with some
androgens
4. Edema
5. Gynecomaastia in males
Precautions:
1. Contraindicated during pregnancy and with prostate enlargement.
2. Children must have bone growth evaluated every six months
Antiandrogens
- tumor cells in prostate cancer are dependent on androgenic
stimulation. Antiendrogens blocks the receptors in tumor cells
which deny the cells of androgenic stimulation.
- Used in combination with other therapies that prevent or
suppress androgen secretion
- This can be achieved by:
1. orchiectomy (surgical castration)
2. Gonadotropin-releasing hormone agonists inhibit the testes
from producing antiandrogens
Uses:
1. Used in combination with surgical or chemical castration to treat advanced
prostate cancer.
2. Treat advanced breast cancer in postmenopausal women.
Adverse Effects:
1. Gynecomastia can occur with all androgen blockers
2. Serious diarrhea (Bicalutamide)
3. Hot flashes
4. Visual disturbances and delayed adaption to dark
5. Constipation
6. Nausea
7. Bicalutamide and Hilutamide may cause loss of hair
Client Education:
1. Nilutamide:
a. if you miss a dose do noy double up when the next doe is due to be taken
b. be aware that it will take longer for your eyes to adapt to changes in
lighting
c. this can be taken with or without food
2. Bicalutamide:
a. notify physician for severe or persistent diarrhea
3. Monitor liver function test
HYPERGLYCEMIC HORMONES
- produced in the alpha sellc of the pancreas. Serum blood glucose
level is raised by breaking down stored glycogen in the liver and
muscles and synthesis of glucose. Hormones are secreted
normally in response to hypoglycemia for the concurrent release
of insulin and cathecolamines
Uses:
1. The emergency treatment of severe hypoglycemia when:
a. the client is unconscious or uncooperative
b. it is not possible for emergency personnel to treat hypoglycemia with 50%
dextrose
c. IV access is not available and a client is unconscious.
Adverse Effects:
1. Nausea and vomiting
2. Generalized allergic reaction manifested as urticaria, respiratory distraa and
hypotension.
Precautions:
1. Safety during pregnancy and lactation
2. May interact with oral anticoagulants and thus increase risk of bleeding
3. Protect the airway of the unconscious client
4. Dosage is dependent on age and clinical condition
Example: Glucagon
Client Education:
1. Report repeated episodes of hypoglycemia.
2. Carry emergency identification
3. Perform self blood glucose testing on a regular basis.
Hypoglycemics
- naturally occurring hormones such as insulin or oral medication
aimed at lowering blood glucose levels.
- Insulin is produced and secreted from the beta cells in the islet of
Langerhans in the pancreas. Elevated blood glucose levels
stimulate the secretion of insulin.
Insulin
- facilitates the passage of glucose into cells for energy. It
suppresses excess production of sugar in the liver and muscles as
well as the breakdown of fat for energy.
Uses:
1. All ind’l with Type I IDDM (Insulin Dependent Diabetes
Mellitus)
2. Some ind’ls with Type 2 NIDDM
3. Women with gestational diabetes if dietary therapy is not
effective.
4. Some clients receiving parenteral nutrition therapy:
Adverse Effects:
1. Hypoglycemia
2. Weight gain
Important Drugs:
1. Insulin are classified by their effect and duration
a. Rapid –acting
- Insulin Lispro (Humalog)
- Insulin Aspart (NovoLog)
- start working in 10-20 minutes
- peaks in 30-90 minutes
- therapeutic duration: 3-5 hrs.
b. Short-acting
- Regular (R)
- starts working in 30-60 minutes
- peaks in 2-4 hrs
- therapeutic duration:6-8 hrs.
c. Intermediate-acting
- NPH (N)
- Lente (L)
- starts working 1-4 hrs
- peaks in 6-12 hrs
- therapeutic duratiom: 24 hrs.
d. Long-acting
- Ultralente (U)
- starts working in 4-6 hrs.
- peaks in 18-20 hrs.
- therapeutic duration 24-36 hrs.
e. Premixed
- NPH and Regular Insulin mixed together in one bottle (70/30 &
50/50)
- starts working in 30 minutes
- peaks in 8-12 hrs.
-therapeutic duration:16-24 hrs.
Client Education:
1. Perform self blood glucose testing
2. Carry an emergency source of carbohydrate to treat hypoglycemia
3. Carry emergency identification the identifies you as diabetic.
4. To reduce irritation, never inject cold insulin
5. Carry insulin and supplies when traveling
6. Inject insulin SC and rotate injection site
7. Do not massage injection sites
Sulfonylureas
- classified as 1st or 2nd generation
- act to increase insulin from the pancreas
- enhance performance and the number of insulin receptors on
muscles and fat cells
- facilitate glucose transport into cells and decreases hepatic
glucose production
Uses:
1. Monotherapy or combination therapy in the treatment of
Type 2 NIDDM
2. Treatment of secondary diabetes if there is a potential for
insulin secretion
Adverse Effects:
1. Hypoglycemia
2. Skin Rash
3. Weight gain
4. GI disturbances
5. Photosensitivity
6. Agranulocytosis
Precautions:
1. Not intended for use during pregnancy, lactation or by children
2. First generation agents are not recommended in the elderly or those with hepatic
and renal dysfunction.
Important Drugs:
1. First-Generation agents
a. Tolbutamide (Orinase)
b. Acetohexamide (Dymelor)
c. Tolazamide (Tolinase)
d. Chlorpropamide (Diabinase)
2. Second-Generation agents