Pharmacology Flashcards
Synthetic aldosterone is called _________
Fludrocortisone
Blocks conversion of cholesterol to pregnenolone
Aminoglutethimide
Potent, nonselective inhibitor of adrenal and gonadal steroid synthesis and anti-fungal
ketoconazole
Nonselective cytotoxic action on adrenal cortex and DDT analog
Mitotane
Relatively selective inhibitor of 11-hydroxylation, interferes with cortisol and corticosterone synthesis
Metyrapone
Tx for cushing’s
Dx for adrenal insufficiency
Progesterone receptor antagonist; GR antagonist at high concentrations
Mifepristone (RU-486)
Binds to somatostatin receptorand blocks release of ACTH from corticotropes
treatment for cushings and acromegaly
Pasireotide
Which type of thyroid converting enzyme is expressed in the kidney and liver? (D1/ D2/ D3)
D1
Which type of thyroid converting enzyme does the majority of conversion? (D1/ D2/ D3)
D2
Which type of thyroid converting enzyme is expressed in the brain and skin? (D1/ D2/ D3)
D3
How does Iodine get into the follicular cells of the thyroid gland?
The Sodium-Iodide symporter
What are 2 ways that the Sodium-Iodide symporter can be affected and cause disease
- gene mutations -> congenital hypothyroidism
2. Autoimmune Dz -> Hashimoto’s thyroiditis
What is the synthetic T4 replacement?
Levothyroxone
What is the synthetic T3 replacement?
Liothyronine
What is the 4:1 mix of T4:T3?
Liotrix
Readjustments to thyroid medication should be made ____ weeks after beginning therapy
4-6 weeks
Which thyroid medication can be give IV in an emergency?
Liothyronine
What are the 3 drugs that inhibit thyroid hormone synthesis?
- Propylthiouracil, PTU
- Methimazole
- Carbimazole
What step in thyroid hormone synthesis do Propylthiouracil, Methimazole and Carbimazole work?
organification of iodine
and coupling of iodotyrosine
Which is the pro-drug? What is it’s active form? (Propylthiouracil/ Methimazole/ Carbimazole)
Carbimazole —-> Metimazole
What are the 3 major side effects of Propylthiouracil, Methimazole and Carbimazole?
- agranulocytosis
- Hepatitis
- Lupus-like reaction
Which is best used in pregnancy? (Propylthiouracil/ Methimazole/ Carbimazole)
Propylthiouracil,
crosses placenta less,
lower conc in breast milk,
but high risk of agranulocytosis
How does 1,25(OH)2D increase serum calcium?
By increasing efficiency of intestinal absorption
Lithium therapy leads to (increased/ decreased) calcium levels
increased
Thiazide diuretics cause (increased/ decreased) serum calcium levels
increased
Loop diuretics (increased/ decreased) serum calcium levels
decrease
What are the 5 bisphosphonates that reduce osteoclastc bone resorption?
- Alendronate
- Risedronate
- Ibandronate
- Pamidronate
- Zoledronic acid
Which bisphosphonates cause fever and flu like reactions?
- Alendronate
- Risedronate
- Ibandronate
- Pamidronate
- Zoledronic acid
Pamidronate and Zoledronic acid
Which bisphosphonates cause esophageal irritation?
- Alendronate
- Risedronate
- Ibandronate
- Pamidronate
- Zoledronic acid
Alendronate
Risedronate
Ibandronate
Why can’t calcitonin be used long term for lowering serum calcium?
Osteoclasts will down-regulate their receptors
How do hydrocortisone and prednisone lower serum calcium?
decrease production of 1,25 vitamin D
Synthetic PTH, used for osteoporosis
Teriparatide
Why does high potassium increase aldosterone?
it indicates that H2O volume is low
What are the 2 most powerful regulators of aldosterone release?
- Potassium
- Angiotensin II
Other factors:
ACTH, Sodium deficiency
synthetic mineralocorticoid: Binds aldosterone receptor (AR) which increases Na+K+ATPase expression and increase epithelial sodium channel expression
Fludrocortisone
for chronic adrenal insufficiency
in primary adrenal insufficiency there is hyperpigmentation due to increased _____, a bi-product of ACTH production from POMC
MSH, melanocyte-stimulating hormone
Chronic primary adrenal insufficiency is called ______ ______
Addison’s disease
Acute primary adrenal insufficiency is most often caused by ______ ______ ______
Waterhouse–Friderichsen syndrome
The MC cause of Congenital adrenal hyperplasia is deficiency in the enzyme __________
21-hydroxylase
In congenital adrenal hyperplasia there is an excess production of _______ (steroids) and a lack of ______
excess of sex steroids, lack of cortisol
hypercortisolism is also called ________ syndrome
cushings syndrome
Dx: Acute adrenal insufficiency
Rx: _________?
- dexamethasone, won’t interfere with blood measurments
2. cortisol, works but will interfere
Dx: Congential adrenal hyperplasia w/ 21-hydroxylase def.
Rx: _________?
- replace glucocorticoids (cortisol)
2. replace Mineralocorticoids (fludrocortisone)
What drugs are used to treat cushing’s syndrome?
- Ketoconazole - antifungal, blocks hormone synth
- Mitotane- cytotoxic to adrenal
- Metyrapone- blocks cortisol synth
- Aminoglutethimide- blocks conversion of choles to preg
- Mifpristone- creates cortisol resistance
- Pasireotide- blocks release of ATCH
Dx: Aldosteronism
Rx: ________?
- Spironolactone
2. Eplerenone
This drug is a PTH analog
Teriparatide
Insulin is necessary for (T1/T2) diabetes, as needed for (T1/T2) diabetes
necessary for T1
as needed for T2
In the endocrine pancreas, alpha cells secrete _________, beta cells secrete _______
Alpha cells: glucagon
Beta cells: insulin
The metabolic hormones that increase in the amount of insulin released from pancreatic beta cells are called ______
Incretin hormones
The most important incretin in humans is ________
GLP-1, glucagon like peptide 1
GLP-1, glucagon like peptide 1 is made by the _______
L cells of the ileum and colon, response to meal
GLP-1 is degraded by ______
DPP-4, dipeptidyl peptidase-4
At the time of T2DM diagnosis, first line therapy is _______
Metformin
What is the mech of action of metformin?
Activates AMP kinase, inhibits mitochondrial isoform of glycerophosphate dehydrogenase
Reduces gluconeogenesis from the liver
when you put you patient on metformin, you must monitor their _____ level
B12
What are the 4 sulfonylureas for Diabetes?
- Glyburide
- Glipizide
- Glaclazide
- Glimepiride
Which drug decreases hepatic glucose production?
Metformin, a Biguianide
Which drug closes Katp channels on beta cell plasma membranes?
- Sulfonylureas
2. Meglitinides
Which drugs increase insulin secretion?
- Sulfonylureas
2. Meglitinides
What are the 2 Meglitinides?
- Repaglinide
2. Nateglinide
Which drugs that increase insulin secretion work faster? (Sulfonylureas/ Meglitinides)
Meglitinides
Which drug activates PPAR-gamma?
- Pioglitazone
- Rosiglitazone
the thiazolidinedione
Which drugs increase peripheral insulin sensitivity?
Thiazolidinediones: e.g. Pioglitazone
What are the intestinal α-glucosidase inhibitors?
- Acarbose
2. Miglitol
Which drugs slows intestinal carbohydrate metabolism? (Sulfonylureas/ Meglitinides/thiazolidinedione/ GLP-1 receptor agonists/ α-glucosidase inhibitors)
α-glucosidase inhibitors
What are the (4) GLP-1 receptor agonists/activators?
- Exenatide, variable
- Liraglutide, daily
- Albiglutide, weekly
- Dulaglutide, weekly
Which diabetes drugs cause weight gain? weight loss?
Gain:
Sulfonylureas
Meglitinides
thiazolidinedione
Neutral:
Biguanides
α-glucosidase inhibitors
DPP-4 inhibitors
Loss:
GLP-1 receptor agonists
SGLT-2 inhibitors
What are the DPP-4 inhibitors (incretin enhancers)?
- Sitagliptin
- Alogliptin
- Saxagliptin
- Linagliptin
What are the SGLT-2 inhibitors?
- Canaliflozin
- Dapagliflozin
- Empagliflozin
Which class of drugs lower serum glucose by reducing glucose reabsorption in proximal tubule?
SGLT-2 inhibitors
Which to Diabetes drugs most frequently result in hypoglycemia?
- insulin
2. sulfonylureas
Patients at risk for hypoglycemia should carry both glucose tablets and _______ _______
glucagon injection
What is the peptide released with insulin from beta cells that SLOWS GASTRIC EMPTYING and suppresses glucagon?
Amylin
What is the injectable drug analog of amylin?
Pramlintide
Glucagon causes the liver to convert stored ______ into glucose
glycogen
What are the (3) Rapid Insulin therapies?
- Lispro 2. Aspart 3. Glulisine
What are the (3) Intermediate Insulin therapies?
The neutral protamine w/ zinc:
- NPH
- NPL
- NPA
What are the long acting insulin therapies?
- Dentemir DoA: 6-24hrs
2. Glargine DoA: 24-30hrs
What is the best insulin for maintaining a basal level of insulin throughout the day?
Glargine
What is the ultra long acting insulin?
Degludec, DoA 42 hrs
What cells have GLUT-1 receptors that do not require insulin for uptake of glucose?
- RBC’s
- Brain
- Cornea
- Placenta
repeatedly injecting insulin in the same place can lead to __________
lipohypertrophy
What are the 3 defining characteristics of hyperosmolar hyperglycemic state, HHS
- hyperglycemia
- hyperosmolality
- dehydration
The 4 major counter regulatory hormones that increase serum glucose are:
- glucagon
- cortisol
- growth hormone
- Epinephrine
What are the 3 defining characteristics of DKA?
- Hyperglycemia
- Metabolic Acidosis
- Ketone Production
Insulin (promotes/prevents) fatty acid oxidation
prevents
winter’s formula is that PaCO2 =
1.5 * HCO3 +8
An octapeptide that mimics natural somatostatin is called ________
octreotide
In an adrenal crisis there is hyperkalemia and hyponatremia due to increased ______
ADH
What are the 3 phosphate binders for secondary hyperparathyroidism from renal failure?
- Selavemer 2. Calcium carbonate 3. Calcium acetate
What is the calcimimetic, reduced PTH and serum calcium level?
Cinacalcet
This is a mAb that targets RANKL to inhibit osteoclast maturation
Denosumab