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346 Cards in this Set
- Front
- Back
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Thyrotopin classification
|
thyroid stimulating hormone from bovine anterior pituitary
|
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Therapeutic use of Thyrotropin
|
hypothyroidism diagnosis
differentiate between 1' and 2' hypothyroidism thyroid carcinoma enhances uptake of 131 I by thyroid gland |
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important side effects of Thyrotropin
|
N/V
headache fever sinus tachycardia atrial fibrillation |
|
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what type of effects do sympathomimetics have on Thyrotropin?
|
additive effects
|
|
|
what type of effects does hepatic enzyme inducers such as Barbs, rifampin, carbamazepine have on Thyrotropin?
|
decrease plasma concentration
|
|
|
T/F
Estrogens increase the level of TBG. |
True
|
|
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when is the use of Thyrotropin contraindicated?
|
Coronary artery disease
adrenal insufficency |
|
|
What is recombinant TSH used for?
|
Hypothyroidism diagnosis
thyroid carcinoma diagnosis |
|
|
what are side effects of recombinant TSH?
|
N/V
headache sinus tachycardia atrial fibrillation |
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what drug has improved the quality of thyroid scans?
|
Recombinant TSH
|
|
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what is Levothyroxine sodium?
|
thyroid hormone class of drug
|
|
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what do you use Levothyroxine sodium for?
|
HYPOthyroidism
TSH suppression (Hashimoto's thyroiditis, familial goiter, surgical removal) |
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is Levothyroxine sodium T4 or T3?
|
T4
must be converted to T3 for clinical effect |
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how long does it take to see a clinical effect of Levothyroxine sodium?
|
4-6 weeks to achieve a steady plasma state
|
|
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how should Levothyroxine be administered?
|
take on an empty stomach bc this helps increase absorption
|
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Side effects of Levothyroxine sodium
|
headache, insomnia, tremors, fever
Cardiac arrhythmias, tachycardia, diarrhea, weight loss, amenorrhea |
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what type of drug interactions does Lecothyroxine sodium (T4) and Liothyronine (T3) have?
|
Increase anticoagulant activity of warfarin
Drug interactions with TBG: increase binding: estrogens, tomoxifen Decrease binding: ASA, phenytoin, furosemide, androgens, carbazaepine, Hepatic enzyme inducers: Barbs, rifampin, carbamazepine |
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when is Liothyronine contraindicated?
|
adrenal insufficiency and cardiac disease
|
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what is Liothyronine used for?
|
T3, thyroid hormone
used to treat HYPOthyroidism and TSH suppression |
|
|
what is Liotrix
|
T3/T4: combination of thyroid hormone
|
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|
Liotrix
|
combination of T3/T4
used to treat HYPOthyroidism and TSH suppression |
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If you have a patient that has hypothyroidism and is pregnant what should you do to the dose of Levothyroxine sodium or Liothyronine they are taking?
|
increase the dose because in pregnancy there is an increased TBG
|
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Propythiouracil
|
Thioureylene: class of anti-thyroid drug
|
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what is the DOC for thyroid storm?
|
Propylthiouracil
|
|
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how does Propythiouracil work?
|
inhibits peripheral conversion of T4 to T3
does NOT affect conversion in brain or pituitary |
|
|
what is Propythiouracil used to treat?
|
HYPERthyroidism:
Graves disease Hyperfunctioning thyroid nodules Thyroid storm (DOC) |
|
|
adverse reactions to Propythiouracil?
|
headache
vertigo edema N/V Rash: urticaria, pruritus, alopecia |
|
|
what is the DOC for HYPERthyroidism in pregnancy?
|
propythiouracil
|
|
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if your patient is on an oral anticoagulant while taking Propythiouracil what must be monitored?
|
Pro-time closely
|
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Methimazole
|
antithyroid drug
thiourylene |
|
|
what is Methimazole used to treat?
|
HYPERthyroidism:
Graves disease Hyperfunctioning thyroid nodules thyroid storm |
|
|
how is Methimazole administered?
|
Once per day
|
|
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what is a side effect of Methimazole that is not seen in Propylthiouracil ?
|
Agranylocytosis (reversible)
Aplastic anemia |
|
|
how do the anti-thyroid drugs work?
|
inhibit thyroid peroxidase mediated iodination (primary)
|
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Lugol's solution
|
Strong Iodide solution
|
|
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what is Lugol's solution used for?
|
tx HYPERthyroidism: preoperative period in preparation for surgery
thyroid storm |
|
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adverse side effects of Lugol's solution?
|
N/V
diarrhea Acneiform rash HSR Type III Angioedema, hemorrhage Induction of goiter and myxedema |
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|
T/F
Lugol's solution alters free Lithium concentrations. |
True
|
|
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Ipodate
|
Contrast agent for oral administration used in HYPERthyroidism and thyroid storm
|
|
|
what is the mechanism of action of Ipodate?
|
inhibits conversion of T4 to T3
|
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|
Ipanoic acid
|
contrast agent
oral administration used in HYPERthyroidism and thyroid storm |
|
|
Diatrizoate
|
IV administration of contrast agent used in HYPERthyroidism and thyroid storm
|
|
|
Potassium Iodide
|
iodide solution
HYPERthyroidism: preoperative period in preparation for surgery thyroid storm |
|
|
what type of rash can Potassium Iodide cause?
|
Acneiform rash
|
|
|
what are the side effects associated with Potassium Iodide?
|
N/V
diarrhea Acneiform rash TYPE III HSR Angioedema, hemorrhage, induction of goiter and myxedema |
|
|
131-I
|
radioactive iodide
|
|
|
what is radioactive iodide used for?
|
HYPERthyroidism: poor surgical subjects.
Additional treatment when subtotal thyroidectomy ineffective Toxic nodular goiter |
|
|
what are the adverse side effects of radioactive iodide?
|
high incidence of delayed HYPOthyroidism
Long treatment period |
|
|
T/F
radioactive iodide is contraindicated in pregnancy? |
True
|
|
|
what is radioactive iodide contraindicated in pregnancy?
|
deposits in the fetal thyroid
|
|
|
describe MOA of radioactive iodide?
|
deposits in follicle > acts exclusively on parenchymal cells > destroys thyroid gland without damaging surrounding tissue
|
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|
Gonadorelin
|
GnRH classification
|
|
|
therapeutic use of Gonadorelin.
|
central amenorrhea
Idiopathic hypogonadotropic hypodonadism |
|
|
important side effects of Gonadorelin.
|
ovarian hyperstimulation
anaphylaxis |
|
|
how is Gonadorelin administered?
|
IV infusion > mimics normal pattern of hormone release better than SC administration
|
|
|
Leuprolide
|
GnRH analog
LONG acting |
|
|
therapeutic use of Leuprolide
|
Ovulation suppression
Prostatic/breast cancer Endometriosis Idiopathic precocious puberty |
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side effects of Leuprolide
|
androgen like effects
|
|
|
contraindication of Leuprolide.
|
pregnancy and lactation
osteoporosis |
|
|
Goserelin
|
LONG acting GnRH analog
|
|
|
therapeutic uses of Goserelin
|
ovulation suppression
prostatic/breast cancer endometriosis idiopathic precocious puberty |
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|
route of administration of Goserelin.
|
SC implant for hormonal suppression
|
|
|
route of administration of Nafarelin
|
nasal spray of GnRH analog
|
|
|
Nafarelin
|
Long acting GnRH analog administered with nasal spray
|
|
|
primary use of Nafarelin
|
ovulation suppression
prostatic/breast cancer Endometriosis Idiopathic precocious puberty |
|
|
is Nafarelin used in the treatment of Cryptochoridism?
|
YES
used in short term tx of Cryptochordism with no anatomical blockage |
|
|
describe the mechanism of action of the long acting GnRH analogs.
|
Leuprolide, Goserelin, Nafarelin
- used to suppress LH surge in assisted fertility - variety of endocrine disorders - usually takes 2 weeks to see GnRH suppression |
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|
Abarelix
|
GnRH antagonist
|
|
|
primary use of Abarelix.
|
Controlled ovarian hyperstimulation
|
|
|
adverse effects of Abrarelix.
|
abdominal pain, headache, ovarian hyperstimulation syndrome
contraindicated in pregnancy/lactation |
|
|
describe the MOA of Abrarelix.
|
antagonist activity at GnRH receptor
timed induced ovulation > prevent premature LH surge (IVF procedures) NO CYP metabolism |
|
|
Sermorelin
|
GHRH analog
|
|
|
primary use of Sermorelin
|
GHRH analog
Growth hormone deficiency Growth hormone deficiency diagnosis |
|
|
adverse effects of Sermorelin.
|
facial flushing, nausea, vomiting
|
|
|
what substances inhibit Sermorelin?
|
agents that affect secretion of GH: insulin, glucocorticoids, NSAIDS
|
|
|
what agents increase GH levels?
|
clonidine
levadopa |
|
|
what agents decrease response to GHRH, therefore decrease response to Sermorelin?
|
Antimuscarinic drugs
|
|
|
what type of feedback is observed on Sermorelin from insulin growth factor-1?
|
negative feedback
|
|
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how is Sermorelin administered?
|
IV administration
|
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Octreotide
|
somatostatin analog
- inhibits secretion of pituitary and GI hormones |
|
|
primary use of Octreotide.
|
acromegaly
hyperfunctioning endocrine tumors: GH-secreting tumors, Carcinoid syndrome, VIP-secreting tumors |
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side effects of Octreotide.
|
Suppression of insulin release
Gallstone formation GI effects: abdominal pain, N/V, diarrhea |
|
|
what type of drug interactions are seen with Octreotide?
|
decreased bioavailability of cyclosporine
additive effects of b-blockers, CCBs |
|
|
T/F
SC administration of Octreotide is more selective for GH? |
True
|
|
|
Bromocriptine
|
Dopamine D2 receptor agonist
inhibits prolactin release mammary gland site of action |
|
|
Bromocriptine primary use
|
Hyperprolactinemia
Acromegaly parkinson's disease suppression of lactation normal ovulation |
|
|
important side effects of Bromocriptine.
|
ORTHOSTATIC hypotension
N/V dizziness Seizures arrhythmias stroke |
|
|
is Bromocriptine teratogenic?
|
YES
|
|
|
what is a contraindication for Bromocriptine administration?
|
severe ischemic disease
HTN Pregnancy |
|
|
T/F
Antihypertensive drugs have an additive effect when administered with Bromocriptine. |
True
may cause orthostatic hypotension |
|
|
Human chorionic gonadotropin
|
Gonadotropin prep produced by placenta and isolated in urine from pregnant woman (primarily contains LH)
|
|
|
what is HCG used for?
|
infertility: induce ovulation
HYPOgonadism |
|
|
potential side effects of HCG?
|
Ovarian enlargement
hyperstimulation Thromboembolism |
|
|
what are side effects of Abarelix (GnRH antagonist)?
|
hot flashes, sleep disturbances, constipation, peripheral edema
|
|
|
Menotropin(s)
|
Gonadotropin prep isolated in urine from menopausal women (contains FSH & LH)
|
|
|
what are Menotropins used for?
|
Infertility: induce ovulation
Hypogonadism |
|
|
adverse effects of Menotropins.
|
ovarian enlargement
hyperstimulation thromboembolism |
|
|
T/F
Menotropins are only effective if administered IM |
true
|
|
|
why is the half life of FSH so much longer than LH?
|
because of decrease hepatic clearance of FSH
|
|
|
Urofollitropin
|
ultra pure FSH preparation
|
|
|
primary use of Urofollitropin.
|
induced ovulation in women with polycystic ovary syndrome
|
|
|
Somatropin
|
recombinant growth hormone
|
|
|
primary use of somatropin
|
replacement therapy in GH deficiency
Turner's syndrome in girls AIDS wasting or cachexia |
|
|
adverse side effects of Somatropin.
|
headache
intracranial HTN muscle pain mild hyperglycemia ANTIBODY PRODUCTION TO GH Leukemia |
|
|
when is Somatropin contraindicated?
|
onces the epiphysis close
|
|
|
how is Somatropin administered?
|
IM/SC administration
IGF levels peak at 20 hours |
|
|
does Somatropin induce the CYP450 system?
|
YEs
metabolized by the liver and kidneys |
|
|
Somatrem
|
recombinant growth hormone analog (GH analog)
|
|
|
primary use of Somatrem
|
replacement therapy in GH deficiency
Turner's syndrome in girls AIDS wasting/cachexia |
|
|
is the GH analog or recombinant hormone more antigenic?
|
Somatrem (GH analog) is more antigenic than Samatropin (recombinant GH)
|
|
|
T/F
Corticosteroids retard bone growth. |
true
|
|
|
Pegvisomant
|
growth hormone antagonist
|
|
|
primary use of Pegvisomant
|
directly blocks effects of GH and reduces plasma levels of IGF
|
|
|
Pegvisomant used to treat?
|
acromegaly, especially resistant to somatostatin analog- degraded in the liver and kidneys
|
|
|
Arginine Vasopressin
|
posterior pituitary hormone (ADH)
|
|
|
route of administration of Arginine Vasopressin.
|
IM/SC
|
|
|
primary use for Arginine Vasopressin
|
Diabetes insipidus
hemophilia A von Willebrand's disease Enuresis |
|
|
adverse effects of Arginine Vasopressin.
|
Water intoxication
Vasoconstriction |
|
|
Potentiators of Arginine Vasopressin
|
Carbamazepine
Chlorpropamide Tricyclic Antidepressants |
|
|
Inhibitors of Arginine Vasopressin
|
Lithium
heparin Epinephrine Ethanol |
|
|
Does Desmopressin or Arginine Vasopressin have a longer duration of action?
|
Desmopressin
|
|
|
when treating a patient for diabetes insipidus that already has pre-existing CAD, what medication would you use?
|
Desmopressin
|
|
|
how can you administer desmopressin?
|
SC/IV
Oral/Intranasal |
|
|
what are the different routes of administration of Oxytocin used for?
|
IV: induce/enhance uterine contractions
IM: prevent post partum hemorrhage Nasal: stimulate milk letdown |
|
|
where is oxytocin produced?
|
posterior pituitary
|
|
|
contraindications of administration of oxytocin?
|
abnormal fetal presentation
prematurity cephalopelvic diproportion |
|
|
T/F
T3 has a longer half-life than T4 |
false
|
|
|
T/F
T3 is more potent than T4 |
True
|
|
|
T/F
T4 is converted to T3 by oxidation in the pancreas |
false
|
|
|
T/F
T4 is more expensive |
false
|
|
|
Identify the corticosteroid with the highest relative mineralcorticoid activity.
dexammethasone predinsone methylprednisone cortisol |
Cortisol
|
|
|
Glucocorticoid synthesis inhibitors which block the RLS in all steroid synthesis inhibit which enzyme?
- Aromatase - P45011b - P450 scc - 3B-hydroxysteroid dehydrogenase |
P450scc
if you want to block everything block the side chain |
|
|
which estrogen ring is important for high affinity estrogen binding?
A B C D |
A
|
|
|
Selective estrogen receptor modulators van be used to treat?
|
osteoporosis
tx at risk patients for invasive breast cancer |
|
|
substitution on which carbon # will increase the effective half-life of methyltestosterone?
|
C-17
|
|
|
Which formation has the longest duration of action?
Insulin aspart Insulin lispro Isophane Insulin detemir |
insulin detemir
|
|
|
what is the duration of action of insulin aspart and insulin lispro?
|
fast acting
|
|
|
what is the duration of action of isophane?
|
intermediate acting insulin
|
|
|
biphosphonates do which of the following therapeutically?
inhibit bone reabsorption increase the activity of bone marrow inhibit the activity of PTH cause decreased plasma levels of vitamin D |
inhibit bone reabsorption
|
|
|
what inhibits the activity of PTH?
|
vitamin D
|
|
|
T/F
Bisophosphanates cause decreased plasma levels of vitamin D. |
False
little to no effect on serum vitamin D |
|
|
what is the alternate day treatment with Glucocorticoids in theory suppose to do?
|
minimize HPA-suppression
minimize reduction in bone growth minimize risk of Cushing's syndrome (hypercortisolism) |
|
|
What is the classification of Cortisol and Hydorcortisone?
|
Short acting Glucocorticoid
|
|
|
What is the classification of Prednisone?
|
intermediate acting glucocorticoid
|
|
|
what is the classification of prednisolone?
|
intermediate acting glucocorticoid
|
|
|
classification of methyl-prednisolone?
|
intermediate acting glucocorticoid
|
|
|
Dexamethasone
|
Long acting glucocorticoid
|
|
|
Betamethasone
|
long acting glucocorticoid
|
|
|
Metyrapone
|
long acting glucocorticoid
|
|
|
Mifepristone
|
glucocorticoid antagonist
|
|
|
primary use of Mifepristone.
|
Hypercorticism
|
|
|
MOA of Mifepristone.
|
blocks glucocorticoids receptors which leads to increase in ACTH and Cortisol
antiprogestrin |
|
|
primary use of Metyrapone
|
can be used in place of dexamethasone in the DST
may offer improved diagnosis in verifying cause of Cushing's syndrome (pituitary dysfunction > increased ACTH secretion) |
|
|
when being used for diagnostic purposes how does Metyrapone help in the diagnosis of Cushings disease?
|
may result in prolonged suppression of the HPA and resulting in reduction in cortisol response
|
|
|
what glucocorticoid agents are best used for ACUTE treatment?
|
Dexamethasone or Betamethasone
|
|
|
what will produce the maximum anti-inflammatory effect in septic shock/brain edema?
|
Dexamethasone
|
|
|
why do you not prescribe Betamethasone or Dexamethasone for long term chronic treatment?
|
growth suppression
bone demineralization |
|
|
what glucocorticoids produce the maximum amount of anti-inflammatory reaction?
|
Dexamethasone/Betamethasone
long acting glucocorticoids |
|
|
what glucocorticoid is used in the treatment of SLE?
|
prednisolone
|
|
|
What type of diseases are prednisolone and prednisone used to treat?
|
SLE: collagen disease
Vasculitis Chron's disease Ulcerative colitis Glomerulonephritis Bronchial asthma COPD |
|
|
what is the first choice of glucocorticoid for treatment of chronic inflammation?
|
prednisone
|
|
|
how is prednisone administered?
|
orally
|
|
|
what has the highest MR activity?
|
Cortisol
|
|
|
Hypofunction of adrenal gland
|
Addison's disease
|
|
|
Hyperfunction of adrenal gland
|
Cushings
Congenital Adrenal hyperplasia |
|
|
Fludrocortisone
|
mineralcorticoid agonist
|
|
|
primary use of Fludrocortisone (mineralcorticoid agonist)
|
hypo-aldosteronism
1' adrenal insufficiency diabetic hypo-renin hypoaldosteronism Salt losing Congenital adrenal hypoplasia orthostatic hypotension |
|
|
what is the greatest salt retaining steroid?
|
Fludrocortisone
|
|
|
what type of DOA does Fludrocortisone have?
|
short DOA
|
|
|
Spironolactone
|
mineralcorticoid antagonist
- only antagonist available in the US |
|
|
primary uses of Spironolactone
|
HYPER-aldosteronism
- adrenal adenomas - bilateral adrenal hyperplasia - refractory edema associated with 2' aldosteronism |
|
|
MOA of spironolactone
|
inhibits formation of MR-ALDO complex - no AIP formation - greater the aldosterone the greater the effect
|
|
|
Aminoglutethimide
|
mineralcorticoid synthesis inhibitor
|
|
|
aminoglutethimide primary use
|
Cushing's (hyper-secretion of ACTH)
Breast cancer |
|
|
side effects of Aminoglutetimide
|
GI distess
adrenal insufficiency |
|
|
what does Aminogluetethimide inhibit?
|
inhibits P450-scc - rate limiting for all physiological steroids
|
|
|
Ketoconazole
Fluconazole |
mineralcorticoid synthesis inhibitor
|
|
|
what is the most effective treatment of Cushing's syndrome?
|
Ketoconazole
|
|
|
if Ketoconazole interacts with a 2nd generation antihistamine, what might occur?
|
prolonged QT interval causing a PVC
|
|
|
Trilostane
|
mineralcorticoid synthesis inhibitors
|
|
|
Trilostane primary use
|
Cushing's
|
|
|
MOA Trilostane.
|
blocks pregnelone > progestrone
- prevents formation of Cortisol and Aldosterone |
|
|
Mitotane
|
mineralcorticoid synthesis inhibitor
|
|
|
what mineralcorticoid synthesis inhibitor is used in the treatment of adenocortical carcinoma?
|
Mitotane
|
|
|
MOA Mitotane.
|
attacks adrenal cortical cells
|
|
|
what are potential side effects of Mitotane?
|
anorexia
nausea lethargy |
|
|
why can Estradiol not be administered orally?
|
because it has extensive first pass metabolism
|
|
|
what is the classification of Estradiol?
|
natural estrogen
|
|
|
what is Estradiol used for?
|
postmenopausal HRT
Osteoporosis |
|
|
what are common side effects associated with Estradiol?
|
nausea
vomiting breast tenderness |
|
|
List the side effects associated with all estrogens and synthetic estrogens?
|
Inhibits metabolism of cyclosporine, tricyclic antidepressants
increases risk of liver toxicity Dantolene, methotrexate increases hepatic synthesis of Vitamin K clotting factors which may lead to thromboembolism decreases warfarin |
|
|
how is Estrone administered?
|
IM injection of aqueous suspension
|
|
|
how is Estradiol valerate administered?
|
IM injection
|
|
|
how is Estradiol cypoinate administered?
|
IM injection
|
|
|
Estradiol valerate and Estradiol cypionate are both administered through IM injection, how does this effect their duration of action?
|
provides 2-3 weeks of estrogenic effect
|
|
|
why can Estrone equilin sulfate esters and plant derived be administered to a patient orally?
|
the sulfation and esterification produces less of a first pass metabolic effect
|
|
|
what is the advantage of Medroxyprogesterone being added to an Estrogen?
|
MPA limits endometrial hyperplasia
|
|
|
If your patient has had a hysterectomy, does your patient need to have progesterone administered with her estrogen?
|
NO
|
|
|
what are the synthetic steroids of estrogen?
|
Ethinyl estradiol
Mestranol |
|
|
How is Ethinyl estradiol and Mestranol administered?
|
Oral administration
|
|
|
what is the only drug approved for postpartum breast engorgement?
|
Chlorotrianisene
|
|
|
what is the classification of Chlorotrianisene?
|
synthetic NONsteriod
|
|
|
T/F
Ethinyl estradiol is used primarily in OCPs. |
True
|
|
|
Where is the Ethinyl added to estrogen to make it have less first pass effect?
|
Carbon 17
|
|
|
Megestrol Hydroxyprogestrone caproate
|
Ester Progestrins
|
|
|
what is the common clinical use of Megestrol Hydroxyprogesterone caproate?
|
primarily used in birth control medications/devices
|
|
|
what are signs of progesterone excess ?
|
acne
fatigue libido change weight changes |
|
|
What drugs are in the synthetic progestins Estrane class?
|
Norethindrone and Norethynodrel
|
|
|
primary use of:
Norethindrone Norethynodrel |
primarily used in birth control medications/devices
|
|
|
what drugs are in the synthetic progestrins Gonane class?
|
L-norgestrel
Desogestrel Norgestimate |
|
|
primary use of:
L-norgestrel Desogestrel Norgestimate |
primarily used in birth control medications/devices
|
|
|
Raloxifene
|
Selective estrogen receptor modulator (SERM)
|
|
|
what is the primary use of Raloxifene?
|
osteoporosis
|
|
|
what are side effects associated with Raloxifene?
|
HOT flashes
|
|
|
Does Raloxifene help with the vasomotor symptoms of menopause?
|
NO
|
|
|
What are the actions of Raloxifene at the breast and uterine tissues?
|
Raloxifene (SERM) acts as an Estrogen antagonist in the breast and uterine tissue
|
|
|
where can estrogen induce tumors at?
|
breast
uterus bone testis kidney etc. |
|
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Classification of:
Clomiphene Tamoxifen Toremifene Leuprolide |
Antiestrogens
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which antiestrogen is a racemic mixture of cis and trans configured molecules?
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Clomiphene
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what is the primary use of clomiphene?
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Infertility: induces ovulation in anovulatory female with an INTACT HP-O axis.
Female must have adequate endogenous estrogens |
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what is a significant side effect of Clomiphene?
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Ovarian enlargement
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T/F
Clomiphene is teratogenic. |
True
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how does Clomiphene work?
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binds competitively to estrogen receptors
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T/F
Tamoxifen is the pure trans isomer. |
True
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T/F
Tamoxifen is used for treatment of Breast cancer that is ERC +. |
True
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how does Tamoxifen work?
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slows cell cycling
decreases insulin-like-growth-factor-1 |
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what is a significant side effect of Tamoxifen?
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HYPERlipidemia
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how long does it take for Tamoxifen to reach a steady state in the plasma?
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3-4 weeks
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What is Toremifene a derivative of?
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Tamoxifen
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what is one benefit of Toremifene that is not seen with Tamoxifen?
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Increases HDL
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how is the GnRH analog Leuprolide an antiestrogen?
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it is used to assist fertilization techniques by suppressing the preovulatory LH surge
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T/F
Leuprolide does NOT help control ovulation. |
False
it assists in controlling ovulation by suppressing the preovulatory LH surge |
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what disease found in a man can Leuprolide be used to treat?
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Prostate cancer
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why is Gabarelix, a GnRH antagonist a better option of treatment for assisted fertilization than Leuprolide?
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Gabarelix is a GnRH antagonist, which is faster acting than Leuprolide because you do not have to wait for downregulation of GnRH receptors.
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primary use of Gacarelix.
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Assisted fertilization techniques to suppress the preovulatory LH surge.
Prostate cancer Endometriosis Idiopathic precocious puberty |
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List the aromatase inhibitors and the differences between them.
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Anastrozole: reversible/non-steroidal
Exemestane: irreversible/steroidal |
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what are aromatase inhibitors used to treat?
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Advanced breast cancer in Postmenopausal Women ONLY
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what are potential side effects of the aromatase inhibitors: Anastrazole and Exemestane
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GI disturbances
Fatigue, headache, hot flashes, edema, weight gain |
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when is Anastrazole/Exemestane commonly used in the treatment of breast cancer?
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In postmenopausal women when Tamoxifen treatment has failed
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Mechanism of action of Anastrazole.Exemestane
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Aromatase inhibitors
inhibits the final steps of estrogen synthesis in PM women > suicide inhibitor > reduces circulating estrogen |
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Mifepristone
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Antiprogestin that is not currently approved in the US
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what androgens are used for the treatment of HYPOgonadism?
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Testosterone
DHT Transdermal testosterone |
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what is the best route of administration of testosterone?
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transdermal or IM injection
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what are potential side effects of Testosterone, DHT, or transdermal testosterone,
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General: N/V, diarrhea, altered libido, DECREASED HDL/LDL ratio, jaundice, cholestatic hepatitis, may lead to Hepatic Adenocarcinoma
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what type of testosterone is most likely to lead to hepatic adenocarcinoma?
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alkyl substituted androgens
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what is Testosterone cypionate?
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Ester derivative of testosterone
IM injection |
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what drugs are testosterone derivatives?
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Fluoxymesterone
Methyltestosterone Oxandrolone |
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what is the primary use of Fluoxymestreone?
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Hereditary Angioneurotic Edema
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what is the primary use of Methyltestosterone?
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Hereditary Angioneurotic edema
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what does methylating testosterone do?
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increases the half life of the drug
makes it so that it can be administered orally |
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what is the DOC for Nitrogen balance and muscle development?
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Oxandrolone
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what is the only drug approved for cachexia?
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Oxandrolone
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what is Danazol?
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synthetic testosterone
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primary use of Danazol.
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hereditary angioneurotic edema
endometriosis symptomatically tx fibrocystic breast disease |
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what is the DOC for endometriosis?
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Danazol
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what drug can be given for the symptomatic treatment of fibrocystic breast disease?
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Danazol
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what is DHEA?
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precursor to testosterone
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primary use of DHEA?
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SLE and DM type II
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where is DHEA converted to testosterone and estrogen?
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in the peripheral tissue
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what is Fluasterone?
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derivative of DHEA
used to treat SLE and DM type II |
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Leuprolide
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GnRH analog
inhibitor of androgen synthesis used in the tx of Advanced Prostate cancer |
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Ketoconazole
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antifungal agent that is inhibitor of androgen synthesis
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primary use of Ketoconazole
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advanced prostate cancer
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side effects of Ketoconazole
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GI effects
Impotence hepatotoxicty |
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Finasteride
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5-alpha-reductase inhibitor
androgen synthesis inhibitor treatment of mild BPH |
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primary use of Finasteride
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Benign prostatic hyperplasia
male pattern baldness |
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what are the contraindications for Finasteride?
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women
category X pregnancy drug- women should not handle |
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potential side effects of Finasteride?
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impotence
decreased libido Gynecomastia |
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how long does it take for clinical effects to be seen with Finasteride?
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3-6 months
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what are the Androgen antagonist?
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Flutamide
Bicalutamide Nilutamide |
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which androgen antagonist is irreversible?
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Nilutamide
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when administering Flutamide or Bicalutamide, what are they combined with?
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GnRH antagonist for treatment of metastatic prostatic carcinoma
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which androgen antagonist is administered to patient for metastatic prostatic carcinoma in combination with orchiectomy?
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Nilutamide
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which androgen antagonist is a potent antagonist of DHT?
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Nilutamide
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Potential side effects of Nilutamide and Flutamide?
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hepatitis, anemia, leucopenia, GI effects
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potential side effects of Bicalutamide.
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GI effects
anemia |
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what is the classification of
Insulin lispro Insulin aspart Insulin glulisine |
RAPID acting insulin
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what is the classification of
Human insulin "regular insulin" |
SHORT acting insulin
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what is the classification of
Isophane insulin |
Intermediate acting insulin
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Classification of
Insulin glargine Insulin detemir |
LONG acting insulin
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what is the name of the inhaled insulin formulation?
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Human insulin liquid
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put the different types of insulin in order according to shortest duration of action to longest duration of action.
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Rapid: Insulin Lispro, Aspart, Glulisine
Short: Human insulin Intermediate: Isophane insulin Long: Insulin Glargine, Detemir |
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what is a potential side effect of insulin therapy?
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HYPOglycemia
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what are the different types of insulin used for treatment of?
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Type I DM
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which type of DM is insulin dependent?
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Type I DM
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what does insulin prevent in Type I DM?
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DKA
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what are sulfonylureas used to treat?
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Type II DM
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what type of drug is Chlorpropamide?
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1st generation sulfonylurea
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does Chlorpropamide have an active metabolite?
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YES
it is not readily available it must be metabolized Sulfonylurea |
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Chlorpropamide administration.
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administered prior to meal > increases insulin receptor release from b-cells
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what is the most severe side effect of Chloropropamide?
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HYPOglycemia
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what are the 2nd generation Sulfonylureas?
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Glipizide
Glyburide Glymepiride |
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Does Glipizide/Glyburide/Glymepiride have an active metabolite?
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NO active metabolite
longer half life than chloropropamide |
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Repaglinide
Nateglinide |
Meglitinide classification
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MOA on Repaglinide/Nateglinide
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NO direct action on insulin exocytosis
Can be used with metformin Regulates K+ efflux on b-cells Controls post prandial glucose rise |
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Metformin classification
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Biguanide
ANTIHYPERglycemic |
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potential side effect of Metformin.
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nausea and diarrhea
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how does Metformin work?
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no metabolism of drug
increases glucose metabolism > increases insulin action in peripheral tissues > anti-HYPERglycemic |
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what is a possible treatment advantage of Troglitazone, Risoglitazone, Pioglitazone, in treating Type II DM?
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Avoid HTN and Hyperlipidemia
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what is the main mechanism of action of the Thiazolidinediones?
(Troglitazone/Risoglitazone/Pioglitazone) |
Increase insulin effects on target tissues
increase number of insulin receptors and GLUT-4 receptors |
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what is the primary effect of the alpha-glucosidase inhibitors?
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HYPERglycemic
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Acarbose
Miglitol |
alpha-glucosidase inhibitors
primary agent acts only on intestine |
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potential side effects of Acrabose/Miglitol
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malabsorption
flatulence abdominal bloating |
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describe the mechanism of action of Acarbose/Miglitol
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alpha-glucosidase inhibitors
- enzymatic degradation of starch and dissacharides to glucose > BLUNT post prandial rise in glucose |
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Exenatide
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Incretin mimetic
- resists DDP-4 degradation |
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Is Exenatide anithyperglycemic or antihypoglycemic?
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Anti-HYPERglycemic
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what drug has improved hbA1c when administered with metformin?
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Exenatide
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Sitagliptin
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competitive antagonist of DDP-4 activity
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Does Sitagliptin cause HYPOglycemia?
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NO
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what drug may produce a cancer risk due to DDP-4 inhibitors?
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Sitagliptin
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Pramlintide
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amylin analog
co-secreted with glucose anti-HYPERglycemic |
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what is Pramlintide used for the treatment of?
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type I and II DM
- slows gastric emptying and reduces glucagon secretion reduces rise in plasma glucose |
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is there a risk for hypoglycemia with Pramlintide?
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a slight risk
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Does Pramlintide effect the total glucose absorption?
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NO
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what is Glucagon used for?
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severe HYPOglycemia
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Ergocalciferol
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Vitamin D2
cheapest activated form/slower onset of action than Calcitrol |
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primary use of Ergocalciferol
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Nutritional & metabolic rickets
Osteoporosis Osteomalacia |
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what is potential side effect of Ergocalciferol?
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hypercalcemia: potentially fatal
Hyperphosphatemia |
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Dihydrotachysterol
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Analog of Vitamin D2
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why is Dihydrotachysterol a greater advantage than Calcitrol?
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faster onset
shorter DOA greater effect on bone mineralization |
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what is the DOC for HYPOparathyroidism?
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Dihydrotachysterol
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Doxercalciferol
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analog of vitamin D2
Treatment of HYPERparathyroidism - produces highest level of Vitamin D which will suppress PTH |
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Calcifediol
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active form of Vitamin D3
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what is the only approved therapeutic use of Calcifediol?
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HYPOcalcemia
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Calcitriol
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active vitamin D3
used in the treatment of HYPERparathyroidism |
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Salmon calcitonin
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Calcitonin hormone
used in tx: Hypercalcemia, Paget's disease, osteoporosis |
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what is used for the long term treatment of Paget's disease?
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Salmon Calcitonin
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what are possible side effects of Salmon Calcitonin?
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HSRs
GI disturbances HYPOcalcemia Rhinitis, headache, nose bleeds: intranasal administration |
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how does Salmon Calcitonin work in the tx of osteoporosis?
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inhibits bone loss by decreasing bone reabsorption
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MOA of Salmon Calcitonin in treatment of Paget's disease.
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prevents abnormal bone turnover
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What are Raloxifene and Conjugated estrogens used in the treatment of for bone disorders?
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osteoporosis
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what might a 1st generation bisphosphonate cause that a 2nd generation will not?
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osteomalacia
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Etidronate
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1st generation bisphosphonate
primary use: HYPERcalcemia, Paget's disease adverse effects: osteomalacia, GI disturbances, rash, M/S pain |
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what reduces the absorption of all bisphosophonates?
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NSAIDS
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Pamidronate
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2nd generation Bisphosphonate
IV administration only tx: HYPERcalcemia, Paget's disease side effects: GI disturbances, rash, M/S pain |
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T/F
2nd generation bisphosphonates have higher potency anda decrease effect on mineralization. |
True
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which has a higher potency?
Etidronate Pamidronate |
pamidronate
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classification of Risedronate
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2nd generation bisphosphonate
oral administration |
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what is Risedronate used in the treatment of?
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paget's disease
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Alendronate
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bisphosphonate
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which bisphosphonate is used in the treatment of osteoporosis and osteoporosis prophylaxis?
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Alendronate
- increases bone density by decreasing bone reabsorption |
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tiludronate
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bisphosphonate
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which two bisphosphonates can be used in the treatment of HYPERcalcemia?
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Etidronate
Pamidronate |
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Plicamycin
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antibiotic used in the tx of HYPERcalcemia
IV administration |
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adverse side effect of Plicamycin
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Bone marrow suppression
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how do thiazide diuretics help with the treatment of osteoporosis?
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Hydrochlorothiazide and Chlorothiazide reduce urinary excretion of calcium
lower doses are used in tx of osteoporosis oral administration |
