Pharmacology Unit 4 - Endocrine Pt. 3 Flashcards
which sulfonylurea has the lowest incidence of hypoglycemia?
nateglinide (D-phenylalanine derivative)
what pharmacologic agent is the first line therapy for DM II
metformin
black box warning of metformin
lactic acidosis
due to the black box warning with metformin, it is c/i in who?
- any renal dz
- etoh-ism
- hepatic disease
- any condition that predisposes to tissue anoxia
which anti-diabetic agent is described as a “euglycemic agent” due to less fasting, and less postprandial hyperglycemia, and hypoglycemia?
metformin
MOA of biguanides (metformin)
reduces hepatic glucose production through the activation of AMP-activated protein kinase
_____________ is an antidiabetic agent that is excreted by the kidneys as the active compound
meformin
1/2 life of metformin
1.5-3 hours
toxicity of metformin
- lactic acidosis
- vitamin B12 deficiency
- GI: anorexia, N/V/D, abdominal pain
if a patient presents for contrast study on metformin, the drug should be stopped ________ days prior
2-3
which antidiabetic agents are thiazolidinediones
“-glitazone”
- rosiglitazone (Avandia)
- Piogllitazone (Actos)
toxicity of thiazolidinediones
- fluid retention
- edema
- weight gain
- anemia
- bone fractures in women
c/i of thiazolidinediones
- CHF
- hepatic disease
what is the biggest contraindication with Rosiglitazone (avandia)?
heart disease, d/t it worsening the condition
Thiazolidinediones MOA
- regulates gene expression by binding to PPAR-Y
- reduces insulin resistance in T2DM
Thiazolidinediones are long acting oral antidiabetic agents. Effects last > __________ hours
24
which meds are alpha glucosidase inhibitors
Acarbose and Miglitol
which type of oral antidm agents reduce the post meal excursion by delaying the digestion and absorption of starch and disaccharides?
alpha glucosidase inhibitors (Acarbose & miglitol)
why must hypoglycemia secondary to alpha-glucosidase inhibitors have to be treated with glucose?
bc the metabolism of sucrose might be blocked
which oral anti-dm agent is a bile acid sequestrant?
colesevelam HCL
what is the MOA of bile-acid sequestrants (colesevelam hcl) in the tx of dm?
unknown
bile acid sequestrants like colesevelam hcl are approved as a _______________ antihyperglycemic therapy
DMII
pharmacological effect of glucagon
increases cAMP –> catabolism of stored glycogen, increases gluconeogenesis, and ketogenesis
glucagon has potent ____________ and ____________ effects on the heart
inotropic; chronotropic
what are the clinical uses of glucagon
- hypoglycemia
- dx of endocrine d/o
- B-blocker OD
- radiological procedure of the bowel
why is glucagon used in radiological procedures of the bowel
it relaxes the intestines.
what are the 3 primary hormones for Ca and Phos homeostasis
- Fibroblast Growth Factor 23 (FGF23)
- PTH
- Vitamin D
which hormone for Ca and Phos homeostasis is considered a “prohormone,” meaning it requires further metabolism to gain biologic activity
Vitamin D
Net effect of PTH on serum levels
increased calcium, decreased phos
net effect of FGF23 of serum levels
decreased phos
net effect of Vitamin D on serum levels
increased Calcium and Phos
________________ and ____________ regulate bone formation and resorption, BOTH are capable of stimulating both processes
PTH; vitamin D
osteoblasts = ___________________
bone forming cells
Vitamin D is produced in the ______________ when stimulated by __________
kidney; PTH
what inhibits the production of Vitamin D
FGF 23
Vitamin D inhibits the production of ______________ and stimulates the release of _________________
PTH; FGF23
____________________ is the principal regulator of intestinal Ca nd P absorption
Vitamin D
what are 2 of the most important minerals for general cellular function?
Ca and Phos
Ca and P enter the body from the ________________
intestine
Ca and P are excreted via _______________, which balances the intestinal absorption
kidneys
Actions of Calcitonin
- lowers serum Ca and P through bone and kidney action
- inhibits osteoclastic bone resorption
- reduces Ca and P reabsorption in the kidney
Calcitonin is used the tx of
- pagets Dz
- hypercalcemia
- osteoporosis
Glucocorticoid effect on Calcium levels
- antagonizes Vitamin D stimulated intestinal calcium transport
- stimulates calcium excretion in the kidneys
- blocks bone formation
_______________ prevents accelerated bone loss during the post menopausal period
estrogen
what are your non-hormonal agents that affect bone mineral homeostasis
- Bisphonates
- RANK lingand inhibitors
- Calcium receptor agonists
- Thiazide diuretics
- Plicamycin
bisphonate drugs end in ?
”- dronates”
MOA of bisphonates
- inhibit bone resorption (decreases serum calcium which stimulates PTH –> increased serum calcium and decreased phos)
- inhibits secondary bone formation
what type of drug is Denosumab
a RANK-L inhibitor
MOA of Denosumab
interferes with RANK-L fx –> inhibition of osteoclast formation and activity
Cinacacet is what type of drug
calcium receptor agonist
what is the MOA of Cincalcet
activates Ca receptors of the PTH gland which inhibits the release of PTH
Cinacalcet is approved for the treatment of ?
- secondary hyperparathyroidism
- secondary CKD
- parathyroid carcinoma
how do thiazide diuretics affect calcium homeostasis
increases the reabsorption of Calcium, thus increasing serum calcium levels
Plicamycin is a ____________________, which is (rarely) used in the tx of _____________ & ________________
cytotoxic Abx; pagets dz; hypercalcemia
major causes of hypercalcemia
- hyperparathyroidism
- Cancer with or without bone mets
___________________ can lead to CNS depression, which can lead to coma without treatement
hypercalcemia
Tx of hypercalcemia
- 500-1L/h saline + lasix
- bisphonates
- calcitonin
- gallium nitrate
- plicamycin
- IV phosphate
- glucocorticoids
what is the fastest and surest way to reduce serum calcium levels?
IV phosphate
if IV phosphate is administered too fast, what can happen?
deplete calcium –> arrhythmias and cardiac arrest
__________________ IV will lower serum calcium substantially within 24-48 hours; however, it is not the drug of choice because of toxicity
plicamycin
s/sx of hypocalcemia
- tetany
- parasthesias
- muscle cramps
- seizures
- LARYNGOSPASM
causes of hypocalcemia
- hypoparathyroidism
- Vitamin D deficiency
- CKD
- malabsorption
Tx of hypocalcemia
- Calcium (IV, IM, PO)
- Vitamin D (calcitrol)
_________________ takes 24-48 hours to increase serum calcium levels
Vitamin D (Calcitrol)
________________ delivers 3x more elemental calcium than _____________
CaCl; Ca-gluconate
what is the benefit of Calcium gluconate in the tx of hypocalcemia
less irritating to veins
_________________ is a common complication of renal failure
hyperphosphatemia
tx of hyperphosphatemia
- dietary restrictions
- phosphate binders: sevelamer
- calcium supplements
causes of hypophosphatemia
- primary hyperparathyroidisim (increased PTH = dec P)
- vitamin D deficiency (dec Vit D = dec P)
- idiopathic hypercalciuria
- increased FGF23 (inc FGF23 = dec P)
- renal phosphate wasting (Fanconi’s syndrome)
- over use of phosphate binder
- TPN with inadequate phosphate content
conditions that cause increase in FGF23 –> decreased phos
- rickets
- tumor induced osteomalacia
acute hypophosphatemia can decrease ________________, which decreases _________________, causing a ________________ shift in the oxyhgb dissociation curve –> ______________
ATP; 2,3 DPG, left; rhabdomyolysis
what is the primary tx of symptomatic primary hyperparathyroidism with hypercalcemia?
surgical tx
CKD will cause retention of _________ and excretion of ______________
phosphorus; ionized calcium
tx of secondary hyperparathyroidism of CKD
calcitrol analogs (doxercalciferol and paricacitol)
s/sx of chronic adrenocortical insufficiency (addisons dz)
- weakness
- fatigue
- wt loss
- hypotn
- hyperpigmentation
- inability to maintain blood glucose during fasting
congenital adrenal hyperplasia is a defect in the synthesis of __________
cortisol
in congenital adrenal hyperplasia there will be a __________ cortisol level that is equal to a ____________ in ACTH levels
decrease; increase
if you know a fetus has congenital adrenal hyperplasia, ______________ can be given to the mom to prevent the baby being born in acute crisis
decadron
tx of congenital adrenal hyperplasia
- stress dose glucocorticoids
- stabilization doses of glucocorticoids and mineralcorticoids
causes of cushings syndrome
- bilateral adrenal hyperplasia (ACTH secreting pituitary adenoma)
- chronic, excessive glucocorticoids
tx for cushings
- surgical removal of ACTH or cortisol producing tumor
- irradiation of adrenal gland(s)
with surgical tx of cushings syndrome, large doses of ______________ must be administered before and after surgery
cortisol (up to 300 mg of hydrocortisone)
what is chrousos syndrome?
a genetic inactivating mutation of the GR gene which causes primary generalized glucocorticoid resistance
chrousos syndrome the HPA compensates causing _________ ACTH, __________ cortisol, ___________ androgens, and ___________ mineracorticoid activity
increased; increased; increased; increased
how do you tx chrousos syndreom
dexmethasone
HPA compensation with increased ACTH will cause what s/sx
- htn
- potassium imbalance
- hyperandrogenism (male characteristics)
tx for aldosteronism
spironolactone
______________ is responsible for 50% production of aldosterone, and ____________ is responsible for the other 50%
ACTH; Angiotensin
aldosterone has a negative feedback effect on _____________
ACTH
MOA of mineralcorticoid drugs
bind to mineralcorticoid receptors in the cytoplasm of target cells in the DCT and CD
aldosterone increases Na reabsorption in what cells?
- CD and DCT of kidney
- sweat and salivary glands
- GI mucosa
- across cell membranes
increased aldosterone results in…
- hypokalemia
- metabolic alkalosis
- increased plasma volume
4 HTN
mineralcorticoids are metabolized in the _______________
liver
what are your mineralcorticoid drugs? (i.e. aldo agonists)
- deoxycorticosterone (DOC)
- fludrocortisone
__________________ is mineralocorticoid that is a precursor of aldosterone
dexoxycorticosterone
which mineralcorticoid drug is endogenous
deoxycorticosterone
which mineralcorticoid drug is exogenous
fludrocortisone
which drug is used to tx adrenocortical insuffciency
fludrocortisone
which mineralcorticoid agonist has a potent salt retaining activity
fludrocortisone
what is aldosteronism
excessive production of aldosterone via adrenal adenoma causing HTN and Hypok
what are your adrenocortical antagonist drugs
- steroid synthesis inhibitors
- glucocorticoid antagonists
- mineralcorticoid antagonists
which drugs are your steroid synthesis inhibitors (adrenocortical antagonists)
- aminoglutethimide
- ketoconazole
- arbiraterone
which drugs are your glucocorticoid antagonists
Mifepristone
1/2 life of mifepristone
20 hours
mifepristone has a high affinity for the _____________ Receptor, and has extensive binding to _______________
glucocorticoid; albumin
Mifepristone is only recommended for tx of ___________________ or ____________ that have failed other tx
ACTH secretion; adrenal cancer
what are your mineralcorticoid antagonists
spironolactone and epleronone
which mineralcorticoid antagonist drug is more selective
epleronone
which mineralcorticoid antagonist also fx as an androgen antagonists
spironolactone
action of spironolactone lasts ___________ days
2-3
adverse effects of estrogen therapy
- thromboemboli
- MI
- HTN
- HA
- peripheral edema
- nausea
what are the steps of rational prescribing?
- make a specific diagnosis
- consider the pathophysiologic implications of the Dx
- select a specific therapeutic objective
- select a drug of choice
- determine the appropriate dosing regimen
- devise a plan for monitoring the drugs action
- determine an endpoint of therapy
- plan a program of patient education
what are the 17 elements that must be included on an outpatient prescription?
- prescriber name
- prescriber license classification
- prescribers address
- prescribers telephone number
- date script is written
- patients name
- patients address
- name of the medication
- strength of the medication (metric units)
- quantity to be dispensed
- complete directions for use
- number of refills and expiration date of script
- waiver of the requirement for childproof containers
- additional instructions/warnings
- prescribers signature
- prescribers national provider identification number
- state licensce number
which elements are required for an inpatient prescription
- date script is written
- name of medication
- strength of medication
- quantity to be dispensed
- compete directions for use
- prescribers signature
with inpatient computer prescription writing (charting); ______________ must be present for the order to be valid
all elements
if the duration of therapy or the number of total doses is not specified, the medication is continued until….
- prescriber discontinues the order
- order is terminated per matter of policy
what are common omissions with prescription writing ?
- not D/C prior med when new one has begun
- not stating whether regular or long acting form should be used
- fail to specify a strength or notation for long acting forms
- “PRN” but fail to state what conditions justify the needs
“resume pre-op meds”; “continue present IV fluids”; “continue eye drops”
these are all what type of prescribing erros
omission of information
when writing prescriptions, these rules should be followed to prevent errors:
- always precede decimal points with a zero
- do not follow whole numbers with a zero
- “units” should always be written out
- “micrograms” should always be written out
- Avoid acronyms and drug abbreviations
which is appropriate in prescription writing?
A. “one ampule of furosemide”
B. Furosemide 40 mg
B - 40 mg furosemide
T/F: “OD” is often mistaken for QD therefore you should write out “for right eye only”
true
which is appropriate in prescription writing?
A. QD
B. Q.D.
C. once daily
C - write out once daily
how do inappropriate drug prescriptions get written?
- failure to recognize C/i from other conditions the patient has
- failure to obtain information about the other drugs the patient is taking
- failure to recognize possible physiochemical incompatibilities between drugs
how do you avoid errors in prescribing like: inappropriate drug prescriptions
- do a thorough H & P
- check physicians desk reference
- consult handbook of injectable drugs
what is the electronic flow of information with E-prescribing
Prescriber <–> Intermediary <–> Pharmacy <–> Health insurance
components of E-prescribing
- must be HIPAA compliant
- prescribers have information readily available
- prescriptions are clearly written
- renewals can be processed electronically
what is the disadvantage to e prescribing
pull down drugs lists create new errors (wrong drug, wrong dose, regimen)
what are the 4 ways a patient be noncompliant with meds?
- patient fails to obtain the medication
- patient fails to take the medication as prescribed
- patient prematurely D/Cs the medication
- patient (or someone else) takes the medication inappropriately
ways to improve medication compliance
- communication
- assess personal, social, and economic conditions
- assist in the development of a routine for taking medications
- mailing refill reminders
factors which encourage medication noncompliance
- dz with no sx
- changing medications in hopes of finding one that works better
- multiple doses per day
- living alone
- packaging
- transportation
- social or personal beliefs
what schedule drug is there no accepted medical use, and is there lack of accepted safety as a drug?
I
this schedule of drug has current accepted medical use, high potential for abuse, and abuse may lead to psychological and/or physical dependence
II
T/F: all generic drugs are the equivalent to the trade name (proprietary) drug
False
what is the benefit to generic drugs
- offer flexibility in filling an order
- cost reduction
“________________” must be written on the prescription or the generic drug will be used
dispense as written
what is a generic substitution
when the pharmacist substitutes the generic drug for the trade
what is a therapeutic substitution
when a drug within the same class is substituted for the prescribed drug. pharmacist must have permission of the provider to do this.
under what condition can a pharmacist make a therapeutic substitution without the approval of the prescriber?
in managed care organizations with a specific formulary
T/F: Herbal and dietary supplements are regulated by the FDA
false
herbal and dietary supplements are considered __________________, not _____________
part of the diet; medications
WHO estimated in 2011 that ___________% of the worlds population is still dependent on herbal meds
80
ASA recommends that patients discontinue all herbal medications _____________ weeks prior to surgery
2-3
T/F: herbals are legally considered medications/drugs
false
T/F: FDA approval is required prior herbals being sold
false
T/F: there is no proof of efficacy or safety prior to marketing of herbals
true
common s/e attributed to herbal medicines
- CV instability
- Electrolyte disturbances
- coagulation d/o
- endocrine effects
- hepatotoxicity
- renal failure
T/F: herbals are available without a prescription
true
_____________________ was established to reaffirm that herbals and dietary supplements were a part of the diet, and prohibit manufactures from making false claims (i.e. est of good manufacturing practice [GMP])
Dietary supplement health and Education Act 1994 (DSHEA)
in 2006, the ______________________________ Act requires mandatory reporting by manufacturers, packers, and distributors, to the FDA of serious adverse events
Dietary Supplement and non-prescription drug consumer protection act
what was the goal of the 2006 Dietary supplement & non-prescription drug consumer protection act
to identify trends to alert the public to potential safety issues with supplements
What are examples of serious events that were now required to be reported d/t the 2006 Dietary supplement and non-prescription drug consumer protection act
- death
- life threatening event
- hospitalization
- persistent disability or incapacity
- congenital anomaly or birth defect
- adverse event requiring medical or surgical intervention
what year did the FDA release the final Good manufacturing Practice (GMP) standards for supplements?
2007
________________ is a botanical supplement that should not be used longer than 10-14 days d/t immunosuppression
Echinacea
What are the uses of Echinacea ?
- immune modulation
- Anti-inflammatory
- Antibacterial
- antifungal
- antiviral
- antioxidant
