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ENDOCRINE

PHARMACOLOGY

Drugs Affecting the Pituitary


Gland
1.

Anterior Pituitary Gland

2.

Conditions treated are those of abnormal growth,


specifically:
* Dwarfism
* Acromegaly
* Gigantism

Anterior Pituitary Drugs

Dwarfism

Somatrem (protropin)
Somatropin (hymatrope)
Both are similar to endogenous growth hormone
Side effects include:
* Pain
* Redness at injection site

Anterior Pituitary Drugs


1.

Acromegaly & Gigantism

2.

Treatment of choice is surgical removal of the tumor


Octreotide (sandostatin)
* Synthetic drug similar to somatostatin.
* Inhibits the release of growth hormone
* Side effects include: bradycardia, diarrhea and
stomach distress

3.

Posterior Pituitary Drugs

Two posterior hormones are oxytocin and


antidiuretic hormone.
Antidiuretic analogues are used to treat diabetes
insipidus, nocturnal enuresis (bedwetting).
ADH can cause vasoconstriction and increased
BP.
Other names: Vasopressin (pitressin),
desmopressin (stimate), lypressin (diapid)

Drugs Affecting the Parathyroid &


Thyroid Glands

Parathyroid glands regulate calcium levels.


Thyroid gland produces thyroid hormones. Play
a role in regulating growth, maturation, and
metabolism.
Hyperparathyroidism, results from a tumor and
treatment is surgical removal of all or part of the
glands.

Hypothyroidism

Treatment is aimed at thyroid hormone


replacement.
Prototype drug: levothyroxine (Synthroid)
No significant side effects in therapeutic doses.
Overdose could lead to thyrotoxicosis or thyroid
storm.

Goiter

Not common in developed countries.


AKA Hashimotos disease
Chronic autoimmune disease
Treatment is aimed at supplementing the
inadequate iodine.

Hyperthyroidism

Typically a result of tumors


Most common cause is Graves Disease
Treatment is typically surgical removal of all or
part of the gland.
Radioactive iodine may be given
Propylthiouracil (PTU), may be given alone or in
conjunction with radiation

Drugs Affecting the Adrenal


Cortex
1.

Adrenal cortex secretes 3 classes of


hormones:

2.

Glucocorticoids
Mineralocorticoids
Androgens

3.
4.

5.

Two diseases associated with the adrenal


cortex:

6.

Cushings Disease
Addisons disease

7.

Cushings Disease
1.
2.

3.
4.

Treatment is typically surgical.


Pharmacologic intervention with a
antihypertensives:
Spironolactone (Aldactone)
ACE inhibitors Captopril (Capoten)

Addisons Disease

Therapy is aimed at replacement therapy.


Cortisone (cortistan) and hydrocortisone
(solucortef) are the drugs of choice.
Fludrocortisone (florinef acetate) is a
mineralocorticoid that is also available for use

Drugs Affecting the Pancreas

Insulin Preparations
Three Sources:
Beef
Pork
Human

Differ primarily in their onset and duration of


action and incidence of allergic reaction.
Preparations may be short acting, intermediate
acting or long acting. (table 9-10)

Insulin Preparations

Also classified as nature (regular) or modified.


Natural insulins are used as they occur in
nature.
Insulin can also be modified to increase their
duration of action, decreasing the number of
administrations necessary

Insulin Preparations

Modified insulin preparations include:

Neutral Protamine Hagedorn (regular insulin attached


to a large protein to delay absorption)
Lente (attached to zinc)

Insulin preparations derived from beef or pork,


lentes, may lead to allergic reactions.
Natural human insulin preparations do not
have allergic reactions.

Oral Hypoglycemic Agents


1.

2.
3.
4.
5.
6.

Used to stimulate insulin secretion from the


pancreas is patients with NIDDM.
Four Pharmacologic classes:
Sulfonylureas
Biguanides
Alpha-glucosidase inhibitors
Thiazolidinediones

Sulfonylureas

First class of oral hypoglycemics.


Drugs include:
Tolbutamide (Orinase)
Chlorpropamide (Diabinese)
Glipizide (Glucotrol)
Glyburide (Micronase)

Increase insulin secretion from the pancreas.


Side effect: hypoglycemia

Biguanide

Metformin (Glucophage)
Decreases glucose synthesis and increases
glucose uptake.
Does not stimulate release of insulin.
Side effects: nausea, vomiting, decreased
appetite

Alpha-glucosidase Inhibitors

Acarbose (precose)
Miglitol (glyset)
Delay carbohydrate metabolism
Side effects: flatulence, cramps, diarrhea,
abdominal distention

Thiazolidinediones

New class of oral hypoglycemic agents.


Troglitazone (Rezulin)
Promotes tissue response to insulin, making
available insulin more effective
Has no major side effects

Hyperglycemic Agents

Two agents:

Glucagon
Diazoxide (proglycem)

Increase blood glucose levels.

Glucagon

Given IM when IV live is unobtainable


Converts glycogen stores into glucose
Side effects: N/V, allergic reactions (rare)

Diazoxide

Inhibits insulin release


Typically used for patient with hyperinsulin
secretion from pancreatic tumors
Not indicated for treating diabetes-induced
hypoglycemia

D50

Sugar solution given intravenously for acute


hypoglycemia.
Primary side effect is local tissue necrosis if
infiltration occurs

DEXTROSE 50%

Generic Name:

Dextrose 50%

Brand Name:

None

Classification:

Hyperglycemic

DEXTROSE 50%
Actions

Rapidly increases serum glucose levels


Provides short-term osmotic diuresis

DEXTROSE 50%
Indications

Coma of unknown origin


Hypoglycemia
Status Epilepticus

DEXTROSE 50%
Contraindications

Intracranial hemorrhage
Delirium tremens
Use with caution in acute alcoholism - ineffective
without thiamine; may make thiamine deficiency
more severe
Severe pain (paradoxical excitement may occur)
Know or suspected CVA unless hypoglycemia is
documented

DEXTROSE 50%
Adverse Reactions

Extravasation leads to tissue necrosis

DEXTROSE 50%
Dose:

Adult:

25-50 g IV bolus

Pediatric:

25% dextrose, 2-4 ml/kg IV


bolus

DEXTROSE 50%
Incompatible Reactions

Sodium bicarbonate
Coumadin

DEXTROSE 50%
Notes

Onset:
Peak:
Duration:

Immediate
Variable
Variable

GLUCOSE

Generic Name:

Glucose (oral)

Brand Name:

Glucola, Insta-Glucose

Classification:

Hyperglycemic

GLUCOSE
Actions

A quickly absorbed form of glucose to


increase blood glucose levels

GLUCOSE
Indications

Hypoglycemia
Conscious patients

GLUCOSE
Contraindications:

Decreased level of consciousness


Nausea/vomiting

GLUCOSE
Precautions:

Assure that the airway is patent

GLUCOSE
Dose:

ADULT: sipped slowly by the patient until


a feeling of improvement is reported. It is
not essential to administer the entire
bottle.
PEDIATRIC: Same as adult

GLUCOSE
Notes:

Onset:
Peak:
Duration:

Minutes
Variable
Variable

Glucola - 300 ml bottles


Glucose pastes and gels also available in
various forms

GLUCAGON

Generic Name:

Glucagon

Brand name:

None

Classification:

Hyperglycemic

GLUCAGON
Actions

Protein secreted by the alpha cells of the


pancreas (islets of Langerhans)
Causes a breakdown of stored glycogen
to glucose (glycogenesis); increases
circulating blood glucose
Unknown mechanism of stabilizing cardiac
rhythm in beta-blocker overdose

Actions

Positive inotropic and chronotropic


Decreases GI motility and secretions,
pancreatic secretions, and blood pressure

GLUCAGON
Indications

Hypoglycemia
Beta-blocker overdose

GLUCAGON
Contraindications

Hyperglycemia
Known hypersensitivity

GLUCAGON
Adverse Reactions

Hypersensitivity (protein-based drug)


Nausea/vomiting

GLUCAGON
Precautions

Caution with administration to patients


with a history of cardiovascular or renal
disease

GLUCAGON
Dose

ADULT: 0.5-1.0 mg IV; repeat 1-2 times if


no response within 20 minutes
PEDIATRIC: Not used

GLUCAGON
Incompatible/Reactions

Incompatible in solution with most other


substances

GLUCAGON
Notes

Onset:
1 minute
Peak:
30 minutes
Duration:
Variable
Should always be used in conjunction with
D5W
Must be reconstituted before
administration. Must be used or
refrigerated after reconstitution.

THIAMINE

Generic Name

Thiamine (Vitamin B)

Brand Name

Betalin

Classification

Vitamin

THIAMINE
Actions

Required for carbohydrate metabolism


Deficiency leads to anemia, polyneuritis,
Wernickes encephalopathy,
cardiomyopathy
Administration may reverse symptoms of
deficiency, but effects are dependent upon
duration of illness and severity of disease

THIAMINE
Indications

Coma of unknown origin, especially if


alcohol may be involved
Delirium tremens
Other thiamine deficiency syndromes

THIAMINE
Contraindications

Known hypersensitivity

THIAMINE
Adverse Reactions

Rare

THIAMINE
Dose

ADULT: 100 mg
PEDIATRIC: Rarely used

THIAMINE
Incompatible/Reactions

Alkaline solutions
Barbiturates
Bicarbonate
Cephalosporins
Other antibiotics

THIAMINE
Notes

Onset:
Hours
Peak:
3-5 days
Duration:
Unavailable
Any comatose patient, especially those
who are suspected to be alcoholic, should
receive IV thiamine prior to the
administration of D50 or Narcan

INSULIN

Generic Name:

Insulin

Brand Name:

Classification:

Regular Insulin,
Humulin R
Antidiabetic

INSULIN
Actions

Protein secreted by beta cells of the Islets


of Langerhans
Responsible for promoting the uptake of
glucose by the cells (muscle, cardiac,
CNS, and all other tissue)
Necessary for carbohydrate, fat and
protein metabolism
Converts glycogen to fat

Actions

Allows glucose storage in the liver


Promotes fat and protein synthesis while
antagonizing fat breakdown
Produces intracellular shift of potassium
and magnesium to reduce elevated serum
levels of those electrolytes

INSULIN
Indications

Rarely used in the field - blood glucose


levels are necessary before administering
in an emergency situation
In-hospital use: diabetic ketoacidosis or
other hyperglycemic state
Hyperkalemia

INSULIN
Contraindications

Hypoglycemia
Hypokalemia

INSULIN
Adverse Reactions

Hypokalemia
Hypoglycemia

INSULIN
Dose

ADULT: Adjusted to relative blood sugar


levels. Standard dose for diabetic coma is
10-25 units Regular Insulin IV bolus
PEDIATRIC: Adjusted to relative blood
sugar levels

INSULIN
Incompatible/Reactions

Incompatible in solution with all other


drugs
Antagonizes actions of epinephrine,
steroids, estrogens, thyroid hormones,
diazoxide, dilantin

INSULIN
Notes
ONSET
Regular:
NPH/Lente:
Ultralente:
PEAK
Regular:
NPH/Lente:
Ultralente:

Minutes
Minutes
Minutes
1 hour
2 hours
6 hours

INSULIN
Notes
DURATION
Regular
NPH/Lente
Ultralente

12 hours
24 hours
36 hours

INSULIN
Notes

Usually refrigerated
Oral hypoglycemics, such as Orinase,
Diabinese and Dymelor, are not
substitutes for insulin, they stimulate the
release of insulin from a sluggish
pancreas

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