Week 16: Endocrine Meds Flashcards
How fast does rapid acting insulin take to work
10-15 minutes
How long do long acting insulins work
at least 24 hours
Endocrine drugs are generally used to do what things
- Supply addtl hormone because glands are not producing enough
- prevent release of addtl hormone because the gland produced too much (negative feedback mechanisms)
Prototype Endocrine Drugs
- ACTH (crticotropin)
- Vasopressin (ADH, pitressin)
- Oxytocin (Pitocin)
- Vitamin D (Hytakerol)
- Calcitonin (Calcimar)
- Alendronate (Fosamax)
- Levothyroxine (Synthroid)
- Sodium iodide 131
- Insulin
- metformin (Glucophage)
- Pioglitazone (Actos)
- Cortisone
- Testosterone
- Progesterone
- Estrogen
Corticotropin (ACTH) Classification
Hormone, Anterior Pituitary
Action fo Cortiotropin
stimulates the cortex of the adrenal gland - when stimulated it produced cortisol
What is the reason corticotropin is often given
Usually to diagnose adrenal insufficiency
Helps us figure out if the gland is not working or if there is not enough hormone being made
What does it mean if, after giving corticotropin, the cortisol levels fail to rise? What does it mean if the cortisol levels would rise?
If cortisol levels fail to rise then it is primary adrenal insufficiency
If cortisol levels do rise that means the anterior pituitary is not making enough ACTH
ADRs of Corticoptropin (ACTH)
Same as those for cortisone
Vasopressin (Pitressin, ADH) Classification
Post Pituitary Hormone
Action of Vasopressin
- Fxns as ADH - enhances water permeability of tubular epitherlial membranes of distal convoluting ducts and collecting ducts so water can be absorbed by osmotic flow - PROMOTES RENAL CONSERVATION OF WATER ( HOLD ONTO WATER)
- Causes contraction of smooth muscle of vascular beds enhancing motility and tone of GI tract (2nd action less strong)
ADRs of Vasopressin
- EXCESSIVE VASOCONSTRICTION (2ndary effect)
- WATER RETENTION AND INTOXIFICATION
Other: arrhythmias, decreased CO, intestinal and uterine cramps, marked facial pallor (from cutaneous vasoconstriction), allergic rxns
What is vasopressin used to treat
- Diabetes Insipidus - loss of /urinating large amounts og dilute urine
- Gaseous Distention - rarer use - increases GI tone
Oxytocin (Pitocin, Syntocinon) Classification
Posterior Pituitary Hormone
Action of Oxytocin
Stimulate uterine smooth muscle though non pregnant uterus is relatively insensitive
Does have SOME VASOPRESSOR ACTIVITY (some contracture of vasculature)
Stimulates let down reflex - milk
Has limited ADH effect (may hold some water) - get baby out but a non pregnant uterus does not act like that
Absorption/Route of Oxytocin
Mostly IV infusion, IM, Subcutaneous, Intranasal, Buccal (NOT ORAL)
ADRs of Oxytocin
- WATER INTOXICATION (with large doses over long periods)
- ALLERGIC RXNs INJUDICIOUS USE
Other: uterine rupture, HTN crisis (high BP from vasoconstriction), cerebral hemorrhage, pelvic hematomas, bradycardia, arrhythmias
Oxytocin is often used in what situations
Stop postpartum bleeding
Induction of labor
Cholecalciferol and Ergocalciferol Classification
Parathyroid:
Vitamind D (Modified Form)
Cholecalciferol - D3
Ergocalciferol - D2
(MORE A HORMONE THAN VITAMIN)
Action of Cholecalciferol and Ergocalciferol
- Stimulate intestinal Ca absorption
- Decrease Ca excretion
- Bone Ca mobilization (resorption) in absence of parathyroid hormoen and fxning renal tissue - analog of Vitamin D
Vitamin D
“Sunshine Vitamin”
Can get from food or sun
Stimulates calcium absorption in the intestines and decreases Calcium excretion
Cholecalciferol/Ergocalciferol may be used when a person…
has low aprathyroid hormone
What is unique about the metabolism of Cholecalciferol/Ergocalciferol
It is activated in the liver AND kidneys
Kidney is pretty unique (plays a big part in bones)
What happens with Cholecalciferol/Ergocalciferol if there is no kidney function
No kidney function –> cannot activate Vitamin D –> Renal Osteodystrophy (bad kidneys means bad bones)
ADRs of Cholecalciferol/Ergocalciferol
- Hypercalcemia
* Hypercalcemia causes - anorexia, NV, weakness, constipation, lethargy, depression, amnesia, disorientation, hallucination, syncope, diarrhea, vertigo, HA, polyuria, thirst ataxia*
Calcitrol
Drug for renal patients on dialysis with hypocalcemia
Increase GI absorption of Ca when you have renal disease
It is already activated Vitamin D since the kidneys would normally do this
Calcitonin-Salmon (MIacalcin, Calcimar) Classification
(Fish Form)
Hypocalcemic Hormone (from thyroid)
Action of Calcitonin-Salmon
Direct inhibition of osteoclasts
Decreases tubular resorption leading to increased excretion of Ca
When is calcitonin-salmon used
in diseases like osteoporosis, Pagets disease, or Hypercalcemia
It is going to save the bones and inhibit resorption/osteroclast breakdown
Parathyroid Hormone v Calcitonin
PH will pull Ca from bone while Calcitonin keeps it in the bone
ADRs of Calcitonin Salmon
- HYPOCALCEMIA (with tetany)
Other: NV, allergy, tenderness and swelling of hands, flushing
What is the max amount of calcitonin-salmon given IM and SubQ?
IM - no more than 2 cc per site
SubQ - no more than 1 cc
Alendronate Sodium (Fosamax) Classification
Bone resorption inhibitor, Biphosphonate
Action of Alendronate Sodium
Inhibits osteoclast activity
Absorption/Route of Alendronate Sodium
Oral
FOOD GREATLY DELAYS ABSORPTION
Biphosphonates
class fo drugs inhibiting osteoclast activity
ex: Alendronate Sodium
ADRs of Alendronate Sodium
- MOST ARE MILD - MAY HAVE SOME MILD GI DISTRESS, ULCERS, ESOPHAGITIS/ESOPHAGUS ULCER
- BRONJ ? JAW NECROSIS
Other: A fib concerns (may be correlation not causation
BRONJ
Biphosphonate related osteonecrosis of the jaw
There is concern with a higher incidence of bone death in the jaw / jaw necrosis with dental procedures when taking alendronate sodium
When is alendronate sodium taken
AT LEAST 30 minutes before FIRST intake of the day
Taken with a full glass of water
What must not be done up to 30 minutes after taking alendronate sodium
you must not lay down (prevent esophagus ulcers)
What is the Alendronate Sodium drug holiday
This drug can stay in bones for a long time so sometimes people can take breaks from taking it
Levothyroxine Sodium (Synthroid, Levothroid) Classification
Thyroid Hormone
Synthetic T4 (which converts to T3 in the body)
Action of Levothyroxine Sodium
- Regulate growth/dev through control of PROTEIN SYN
- Calorigenic effect - increase metabolic rate
- Metabolic - increase metabolic rate by various modes
- Inhibition of thyrotropin secretion by pituitary
Absorption/Route of Levothyroxine Sodium
Oral
Food delays absorption - give on empty stomach
When is levothyroxine sodium given
it is used as hypothyroidism hormone replacement therapy
treatment for this is lifelong
ADRs of Levothyroxine Sodium
(Look like Hyperthyroidism)
- CNS - Nervous, insomnia
- CV - arrhythmia, palpitation
- GI - WEIGHT LOSS, cramp, diarrhea
- GU - menstrual irregularities
OVERDRIVE OF SNS
Levothyroxine sodium will enhance the effect of oral ____
anticoagulants
Caution using levothyroxine sodium in what patients
patients with heart disease, esp. coronary insufficiency
patients with diabetes
patients on tricyclic antidepressants
Levothyroxine cannot be taken within 4 hours of taking…
calcium carbonate (TUMS and other local antacids)
How big are the Levothyroxine Sodium doses
thyroid hormone is given in mcg (tiny doses)
If there is not enough T4 being made and a patient needs levothyroxine sodium, what lab value will be different?
TSH (Thyroid Stimulating Hormone) will be high
Iodine 131 Classification
Radioactive Thyroid Hormone
Action of Iodine 131
Destroy thyroid tissue mainly through Beta rats
Goal to produce clinical remission without complete thyroid destruction - in hyperthyroidism/Graves dx
ADRs of Iodine 131
- DELAYED HYPOTHYROIDISM (10% a year after)
Other: Depressed hematopoietic system, anemia, thyroiditis
What is another, more uncommmon use, of Iodine 131
since it is uptook by the thyroid gland it can be given in miniscule non damaging amounts for diagnostic purposes
Iodine 131 should not be used on what patients
Pregnant Patients
children
lactating patients
Insulin
drug used for management of hyperglycemia by promoting cellular uptake of glucose
varies in onset peak and duration of action
What are the routes of insulin administration
Mostly IV, SubQ, IM - does have inhaled version but iffy rn
___ Units/mL are the most common form for SubCu insulin
100
Action of Insulin
increase cellular uptake of amino acids, glucose, and other monosaccharides
What is important to know about the absorption of insulin
It is inactivated by gastric enzymes so must be given subcu or IV
ADRs of Insulin
- HYPOGLYCEMIA (most common)
- ALLERGIC MANIFESTATIONS (if from an animal rather than synthetic source)
- INSULIN RESISTANCE DEVELOPMENT
Why does insulin resistance develop in some diabetics taking insulin
it will only occur in Type 2 diabetics probably due to development of antibodies
The only insulin that can be given IV is ___ insulin since it is unbound
regular
Always use insulin syringes measured by ____
units
Can pregnant women have insulin
yes, it does not cross membranes
Too much insulin causes ____
hypoglycemia
Too little insulin causes ___
hyperglycemia
Rapid insulins work in 10-15 minutes so they are oftne called
mealtime insulins
Regular insulin is ___ acting and ___ lasting
fast acting and short lasting
NPH
intermediate acting insulin
works in 8-10 hours
appears as a cloudy / milky suspension
Long Acting Insulins
Insulin Glargine/Detemir
Not a real peak, a flat level in the body
given once daily and never mixed with other insulins
Metformin (Glucophage) Classification
Biguanide Oral Hypoglycemic
Action of metformin
decreases hepatic glc production and intestinal absorption of glucose
also increases peripheral glucose intake
Absorption of Metformin
Oral Route - ER form absorbed v slowly
Often given in 1500-2550 mg PO in divided doses
ADRs of metformin
- GI EFFECTS (Metal Taste, NV, Abdominal pain, Mod Weight Loss)
- LACTIC ACIDOSIS
Other: Cognitive decline?
Why does lactic acidosis occur with metformin
if someone has a kidney issue and getting dye studied, they can end up with renal impairment and lactic acidosis
So metformin should cease 48 hours prior to dye study and resume 48 hours after
Black Box Warning of Metformin
Lactic Acidosis in Dye Studied Renal Impairment if Metformin not discontinued 48 hours prior and 48 hours after
Does metforming cause hypoglycemia
NO in most cases
Pioglitazone (Actos) Classification
Insulin Sensitizer, Antidiabetic Agent, Thiazolidinedione (TZD)
-glitazone means
part of the TZD/Thiazolidinedione family
Action of pioglitazone
increases ability of target cells to respond to insulin (DECREASES INSULIN RESISTANCE)
Absorption /Route of Pioglitazone
Oral - rapidly absorbed
Food may increase absorption!!!
ADRs of Pioglitazone
Nothing to dreadful!:
URI, HA, Sinusitis, Myalgia, lower TG levels, Raised LDL AND HDL
IN THE BACK OF THE MIND KEEP LIVER AND HEART CONCERNS
Why were some other glitazone (TZD) drugs like Rosiglitazone and Troglitazone taken off the market
Rosiglitazone was not recommended because of risk of MI and CVA
The first ever glitazone was troglitazone and causes hepatic failure
Pioglitazone is indicated for _____ diabetes only
type-2
Cortisone and Hydrocortisone Classification
Corticosteroid (Glucocorticoids)
Glucocorticoids
release in the stress response
role in inflammation, immune response, protein, fat and carbohydrate metabolism
-isone / -asone means
glucocorticoid (corticosteroid)
What are the 8 actions of corticosteroids like cortisone and hydrocortisone
- Anti Inflammatory
- Maintenance of normal BP
- Carbohydrate and Protein Metabolism
- Fat Metabolism
- Immunosuppressive
- Stress Effects
- Anti-diuretic
- CNS effects
Anti-inflammatory action of corticosteroids
stabilize lysosomal membrane to inhibit proteolytic enzyme release during inflammaation
MAJOR anti inflammatory group
Maintenance of normal BP action of corticosteroids
potentiate vasoconstrictor action of NEP - help keep vessels constricted
MINOR EFFECT
Carbohydrate and Protein Metabolism action of corticosteroids
Facilitate muscle and extrahepatic tissue breakdown increasing plasma AA levels
Increase AA trapping by liver and deaminate them
Increase enzyme activity important to gluconeogenesis and inhibit glycolytic enzymes
MAJOR: BREAKDOWN MUSCLES LEADING TO AA RELEASE TO FORM GLUCOSE - THIS IS WHY GLUCOCORTICOIDS LEAD TO INCREASED GLUCOSE LEVEL WITH MUSCLE ATROPHY IN LONG TERM USE
Fat Metabolism Action of Corticosteroids
Promote mobilization of FA from adipose tissue
Long term therapy will redistribute fat to neck, back, face, supraclavicular area, and decrease it in extremeties
Immunosuppressive action of corticosteroids
Thymolytic, Lymphocytic, and eosinopenia actions - as well as atrophy of thymus and decrease # of lymphocytes, plasma cells, and eosinophils in blood
Decrease rate of conversion of lymphocytes into antibodies
This and the anti inflammatory action make them GREAT IMMUNOSUPPRESSANTS AND ANTI ALLERGENICS
Stress effect action of corticosteroids
during stress, acute release of corticosteroids occurs leading to synergistic action of catecholamines
Antidiuretic Effect of corticosteroids
Not as strong as a mineralo-corticoid (aldosterone)
Acts on distal tubules of kidney (ENHANCE REABSORPTION OF Na from TUBULAR FLUID)
INCREASE URINARY EXCRETION OF BOTH K AND H IONS - not as strong as aldosterone but you retain fluid
CNS Action of corticosteroids
AFFECTS MOOD (euphoria, excitation, depression)
Potential steroid psychosis (eager, active, hungry, hyper)_
Route of Cortisone/Hydrocortisone
Oral, IM, IV Topical
Cortisone/Hydrocortisone can be used as replacement therapy in …
adrenal deficiency
Cortisone/Hydrocortisone are very important in _____ and ____ therapy
anti-inflammatory and immunosuppressant therapy
Prednisone
the most common long term corticosteroid
What is important to know about corticosteroid ADRs
THEY ARE HUGE
Common for systemic symptoms from long time use but can even occur in shorter term use where chronic issues appear
ADRs of Corticosteroids
Delay in wound healing (Immunosuppression)
GI Ulceration and Perforation (disrupts lining)
Amenorrhea
Disorders of calcium metabolism (long term use suppresses bone formation and boosts resorption)
Cushings Syndrome/Hypercortisolism (Hump back, moon face, hirsutism, acne, water and Na retention, edema, restlessness, insomnia, euphoria, manic states)
Decreased resistance to infection
Masking of symptoms of inflammation and infection
Weakness
Striae
Thin Friable Skin
Lyte imbalances
Increased lymphoma (cancer) changes
higher cataract incident
can precipitate diabetes in the susceptible
Withdrawal issues
Resp issues in premautre infants
Can corticosteroids be used in pregnant women
no they cross the BBB
Sometimes steroids can be used as …
anti rejection drugs
Why is withdrawal a big issue with corticosteroids
adrenal gland wont be ready to go back to making cortisol leading to severe adrenal insufficiency
Diabetics on corticosteroids are at high risk for what after surgery
infection, dehiscence, and evisceration
What is important to know about corticosteroids compared to aldosterone
the effect on Na retention and K excretion is much less than aldosterone
Testosterone Classification
Androgen Hormone (Primary Male Sex Hormone)
Action of Testosterone
fxns as a stimulator to promote and maintain male secondary sex characteristics
Powerful anabolic agent- stimulates formation and maintenance of muscular and skeletal protein and nitrogen retention
Absorption/Route of Testosterone
Oral - rapid absorption - but actively inactivated by the liver - SO NOT GIVEN ORALLY
Sublingual will bypass the liver
Is testosterone a scheduled drug
yes it is schedule III
Why is it important to keep testosterone gel away from children
they can have masculazation rapidly and easy
ADRs of Testosterone
- LIVER TOXICITY
- HYPERCALCEMIA
- CHOLESTEROL ELEVATION
Other: Retention of Na and water, Nausea, Lipid disorder, HTN from water and Na
What are some ADRs in females taking testosterone that are unique to the gender
deepening of voice
hirsutism
flushing
acne
regression of breasts
enlargement of clitoris
general masculinization
How does testosterone impact calcium levels
it decreases secretion of Ca so the levels of Ca are rising
It is important to monitor what when on testosterone
liver function
When is testosterone contraindicated
prostate cancer
serious cardiorenal dysfunction
pregnancy
Progesterones (Provera-Medroxyprogesterone) Classification
Progestin Hormone
“The Hormone of Pregnancy”
Action of Progesterones
Exact mechanism not completely known but it does bind to cell receptors and causes reproductive effects
What are the reproductive effects of progesterones
- INHIBIT OVULATION (decrease LH and FSH release)
- Induce biochem changes in endometrium in prep for fert egg implant
- CAUSE CERVICAL MUCUS TO BECOME STICKY AND VISCOUS
- decrease sensitivity of uterus to oxytocin
- facilitate dev of secretory apparatus in mammary glands
- increase body temp
- elevate basal insulin levels and potentiate response to glc
- promote hepatic glycogen storage and ketogenesis
- decrease plasma levels of AA
In essence, what is progesterone doing
it is preparing the endometrium for implantation
it also is decreasing uterine contractions to maintain the endometrium and making thick sticky mucus
Progesterone has extensive..
first pass
Route of Progesterone
Parenteral - but too rapid to maintain efficiency
Oral - less effective
ADRs of Progesterone are also known as …
Hormonal ADRs
ADRs of Progesterone
drowsiness GI Symptoms HA Dizziness Allergic Response Irregular Vaginal Bleeding Photosensitivity Retinal Damage CV Complications
Prolonged High Dose: Edema, Weight gain via fluid retention, vertigo, oligomenorrhea, breast congestion, hirsutism, rash, depression, migraine
Most of progesterone adminsitered is used…
as a part of contraception with estrogen
Can also be sued for amenorrhea, threatened abortion, dysmenorrhea, endometriosis
What is the major non contraceptive use of progesterone
to counteract the adverse estrogen effects
stimulation of the uterus via estrogen replacement could cause endometrial cancer if uterus is still present so this will counteract it
Progestins
Synthetic Progesterone Like
For deficiencies, dysfunctional uterine bleeding, an amenorrhea
If combined with estrogen it will help prevent endometrial cancer BUT increase breast, and ovarian cancer risk and heart disease risk
Sodium estrogen Sulfate (Premarin) Classification
Estrogen Hormone
Comes from urine of pregnant mare
ER
estrogen replacement
Action of Estrogen
Stimulate Female Characteristics
- Reproductive
- Metabolic
- Blood coagulation
Reproductive Actions of Estrogen
- FACILITATE OVULATION (increase LH release)
- DECREASE RELEASE OF FSH (through negative feedback)
- Stimulate development of endometrium
- promote growth and cornification of vaginal epithelium
- increase sensitivity of uterus to oxytocin
- promote development of duct system in mammary glands
Metabolic Actions of Estrogen
- DECREASE BONE RESORPTION RATE (DECREASES BREAKDOWN SO WOMEN ARE NOT AS PRONE TO OSTEOPOROSIS UNTIL AFTER MENOPAUSE)
- Increase protein synthesis
- accelerate closure of epiphyses
- increase serum triglycerides, and HDL
- decrease serum cholesterol and LDL
- enhance sodium and water retention
- increase blood glucose (anti insulin action)
Blood Coagulation Action of Estrogen
- INCREASES LEVELS OF VITAMIN K DEPENDENT CLOTTING FACTORS
- PROBABLY INCREASES PLATELET AGGREGATION
- PROMOTES FORMATION OF BLOOD CLOTS
Routes of Estrogen
Oral - prompt and complete
Also parenteral, topical, or vaginal
ADRs of Estrogen
HORMONAL ADR: (Similar to progesterone):
Nausea, Anorexia (like morning sickness), Increased feminine characteristics, fluid retention, break through bleeding, changes in menstrual flow, breast tenderness, irritability, depression, HTN, HA, Cancer (ovarian and breast fed by estrogen), gallbladder disease
STRONG RELATIONSHIP TO EMBOLIC DISEASE (BLOOD CLOT ISSUES LIKE STROKE OR MI)
Estrogen Can be used to control…
menopausal symptoms or dysfunctional uterine bleeding
Contraindications of Estrogen
Estrogen Dependent Cancers (Breast, Ovarian, anything with estrogen receptors)
Undiagnosed Vaginal Bleeding (could be endometrial cancer)
Thrombus or Thromboembolic Dissorders (estrogen already promotes blood clots)
What is the big concern of using estrogen without progestin
in post menopausal women this increases risk for uterine cancer because it will thicken the endometriumd leading to cancer
If a patient is changed to lispro insulin (Humalog) you will teach him to administer it when:
A. 1 hour before meals
B. 1 hour after meals
C. 10-15 minutes before a meal
D. only at bedtime
C. 10-15 min before a meal
Regular insulin has its peal in approximately:
A. 3-4 hours
B. 8-12 hours
C. 24 hours
D. more than 36 hours
A. 3-4 hours
What is the most dangerous colmplication of prednisone therapy:
A. GI Ulceration
B. Hyperglycemia
C. Immune System Compromise
D. Vertigo
C. Immune System Compromise
