Endocrine stuff Flashcards
First line drug for Type II DM?
Metformin (Biguanide)
Main ADRs for Biguanide?
GI! NVD, bloating, anorexia…… Macrocystic Anemia B12 Deficiency
What Class are the follwing drugs?
Glyburide
Glypizide
Glimepiride
Sulfonylureas (2nd gen)
Mechanism of Sulfonylureas? (glypizide, glyburide)
Insulin Secretagogues!
Does Sulfonylureas target ppBG or FBG or both?
BOTH; sulfonylureas target both ppBG and FBG
Which Sulfonylurea has the highest incidence of Hypoglycemia?
Glyburide
Glypizide
Glimepiride
Glyburide has the highest incidence of hypoglycemia. (avoid in elderly)
Most common ADR of Sulfonylureas?
Hypoglycemia
Weight Gain
Which Sulfonylurea is the safest in pts with renal impairment?
Glyburide
Glypizide
Glimepiride
Glipizide is the safest sulfonylurea in pts with renal impairment.
What class are the following drugs?
Canagliflozin
Dapagliflozin
Empagliflozin
Sodium-Glucose Cotransporter 2 Inhibitors
SGLT2 Inhibitors
Mechanism of SGLT2 inhibitors
Reduces reabsorption of filtered glucose
lowers renal threshold for glucose, increases urinary glucose excretion
Most common ADR of SGLT2 inhibitors?
-gliflozins
UTI and Candidiasis
What class are the following drugs?
Liraglutide Exenatide Albiglutide Dulaglutide Lixisenatide
GLP 1 Agonisits
-tide
MOA of GLP 1 Agonists?
Exenatide, Liraglutide
Binds to/activates GLP-1 Receptor.
(Increases Insulin release from functioning Beta-cells)
(Decreases Glucagon release after meals)
(Decreases Hepatic Glucose production)
Use and Generic name of VICTOZA?
Liraglutide
Weight Loss
Contraindications for GLP 1 Agonists?
Exenatide, Liraglutide, Albiglutide
Gastroparesis
Pancreatitis
(ESRD - Exenatide)
(Thyroid CA - Liraglutide)
ADR of GLP 1 Agonists?
GI problems (they decrease over time though) May delay absorption of other drugs (take 1 hr before or 3 hrs after eating)
What class are the following?
(-gliptin)
Sitagliptin
Saxagliptin
Linagliptin
AlogliptinDPP-4 inhibitors (-gliptin)
What Pathway do GLP 1 Agonists and DPP 4 Inhibitors affect?
INCRETIN pathway
MOA of DPP-4 inhibitors? (-gliptin) Sitagliptin Saxagliptin Linagliptin Alogliptin
Prevents degradation and prolongs 1/2 life of GLP-1.
GLP-1 increases glucose-mediated insulin secretion, suppress glucagon secretion
(Glucose-dependent)
CI of DPP-4 inhibitors?
Pancreatitis hx (just like GLP-1 agonists)
DKA
Type 1 DM
Warnings for Saxagliptin (DPP-4 inhibitor)
Saxagliptin is more likely to decrease absolute lymphocyte counts…. increase incidence of CHF
ADRs for DPP-4 inhibitors? (-gliptin)
Requires adjustment for renal patients.
Alogliptin: pancreatitis, hepatotoxicity, SJS/TEN
DPP-4 inhibitors are WEIGHT NEUTRAL and do not cause Hypoglycemia as montherapy!
DPP-4 inhibitors lower A1C by 0.7%
Saxagliptin is metabolized by liver via P450!
Sitagliptin is not extensively metabolized (DPP-4 inhib)
How much do GLP-1 Agonits lower A1C?
Exenatide, Liraglutide, Albiglutide
1-1.5%
What class do Rosiglitazone and Pioglitazone belong?
-glitazone
Thiazolidinediones (-glitazone)
MOA of Thiazolidinediones?
Rosiglitazone
Pioglitazone
PPARg agonist
Increases Insulin sensitivity in Peripheral Tissues (fat, muscle, liver)
Decreases hepatic glucose output
Thiazolidinediones are endogenous insulin-dependent
Pt must be making insulin for process to work (Early type 2 DM)
How much can Thiazolidinediones lower A1C?
Rosiglitazone
Pioglitazone
0.8-1.5%
CI for Thiazolidinediones?
CHF Avoid in class 3 and 4 HR
CHF!
ADRs for Thiazolidinediones?
Rosiglitazone
Pioglitazone
Weight Gain
Anemia
Edema
CHF
potentialy bladder cancer for Pioglitazone
potentially MI for Rosiglitazone
Things to monitor when using Thiazolidinedons?
Rosiglitazone (Avandia)- increase LDL, TG, MI, Edema, HF, fractures
Pioglitazone (Actos)- increase HDL, Edema, HF, fx
decrease LDL, TG
Monitor LFTs!!! with both drugs
What class do the following belong?
Repaglinide
Nateglinide
Meglitinides (-glinide)
MOA of Meglitinides? (-glinide)
Repaglinide
Nateglinide
Stimulate insulin secretion from functioning Beta-cells
Glucose-Dependent stimulation of insulin secretion
How much do Meglintindes lower A1C?
0.5-1.5% (Repaglinide, Nateglinide)
Do Meglintinides target ppBG or FBG?
ppBG! (skip meal = skip dose) (add meal = add dose)
Repaglinide
Nateglinide
ADRs of Meglintinides (Repaglindie, Nateglinide)
Hypoglycemia
Weight gain
What class doe the following belong?
Acarbose
Miglitol
Alpha-Glucosidase Inhibitors
Acarbose, Miglitol
MOA of Alpha-Glucosidase Inhibitors?
Acarbose, Miglitol
Delay the breakdown and absorption of complex CHOs and sucrose.
Decrease ppBG
How much does Alpha-Glucosidase Inhibitors lower A1C?
0.5-1%
Acarbose, Miglitol
CI for Alpha-Glucosidase Inhibitors?
Bowel Stuff
(Inflammatory Bowel Dz, Short-bowel syndrom, Colonic ulceration, Partial Intestional Obstruction, Disorders of digestion/absorption)
Also Cirrhosis
ADRs of Alpha-Glucosidase Inhibitors?
Acarbose, Miglitol
GI stuff (diarrhea, abd pain, FARTS!) Elevated serum transaminases
Can you use sucrose (soft drinks, candy) to treat Hypoglycemia on a patient taking Acarbose or Miglitol? (Alpha-Glucosidase Inhibitors)
NO!
Use a glucose tablet or gel, or fructose or lactose instead.
Pramlintide belongs to what class of Diabetes meds?
Amylin Analog
Pramlintide
MOA of Amylin Analog (Pramlintide)
Works w/ insulin to suppress postprandial glucagon secretions and slow gastric emptying.
(Reduces food intake -> weight loss)
Can Pramlintide be used in T1DM?
amylin analog
Yes!
Can also be used in T2DM as adjunct therapy
Which Amylin Analog:
Reduces A1C by 0.5-0.7%
Reduces ppBG in Type 1 DM
Weight loss by 1-1.5kg over 6 months
Pramlintide
the only Amylin Analog we have learned about.
CI of Amylin Analog (Pramlintide)
Gastroparesis
Hypoglycemia unawarness
A1c > 9% (must be used early)
Pt unwilling to self monitor sugars
T/F you must lower insulin dose by 30-50% before giving Pramlintide to T1DM.
(Amylin Analog)
True
ADRs of Amylin Analog (Pramlintide)
Nausea, Vomiting, Anorexia, Hypoglycemia
Caution using Pramlintide (Amylin Analog) in renal insufficiency.
BTW Its an injection into the abdomen or thigh.
Colesevelam is a drug… whats it about?
Colesevelam lowers hepatic glucose production…. but its really used for cholesterol.
Whats Bromocriptine about?
Bromocriptine improves glucose and energy metabolism….. but it’s really a dopamine agonist.
How do you calculate average glucose from A1c?
(A1c - 2) x 30
Classes of Diabetes drugs that Increase Insulin Sensitivity (2)
- Metformin
2. Thiazolidinediones
Classes of Diabetes drugs that Increase Insulin Secretion (4)
- Sulfonylureas
- GLP-1 Agonists
- DPP-4 Inhibitors
- Meglitinides
Classes of Diabetes drugs that decrease Hepatic Glucose Production (3)
- Metformin
- GLP-1 Agonist
- Thiazolidinediones
Classes of Diabetes drugs that decrease glucagon secretion (3)
- GLP-1 Agonist
- DPP-4 Inhibitors
- Alpha-Glucosidase Inhibitors
Classes of Diabetes drugs that reduce reabsorption of glucose in Kidneys (1)
SGLT2 Inhibitors
Classes of Diabetes drugs that Delay breakdown/absorption of complex carbs & sucrose (1)
Alpha-Glucosidase Inhibitors
What kinds of Insulins are these?
Aspart
Lispro
Glulisine
RAPID acting
Aspart, Lispro, Glulisine
What kind of Insulins are these?
- Regular U-100
- Regular U-500
SHORT acting
- Orange cap (Novolin R)
- Brown cap (Humulin R)
What kind of Insulin is this?
Neutral Protamine Hagedorn (NPH)
INTERMEDIATE acting
Humulin N, Novolin N
What kind of Insulins are these?
- Glargine
- Detemir
- Degludec
LONG acting
How are Short and Intermediate acting insulins produced?
Novolins and Humulins
Genetically altered E. Coli produce Human insulin.
What is the name of T4?
Thyroxine (T4)
What must most thyroid hormone (99%) be carried by?
Binding/Carrier Protein (Mostly TBG)
What are the following drugs used to Treat?
Liothyronine
Thyroid USP
Levothyroxine
Hypothyroidism
What are the following drugs used to Treat?
Methimazole
Propylthiouracil
B-Blockers
Hyperthyroidism
Name a drug that is:
Synthetic T3
more stimulating than T4 (can be overstimulating)
Avoided in Pregnacy
Used to treat hypothyroidism
Liothyronine (Cytomel)
Name a drug that is:
Desiccated pig thyroid
Contains T4, T3, T2, T1
Use to treat hypothyroidism
Thyroid USP (Armour Thyroid)
Name a drug that is:
1st line tx for Hypothyroidism
Nearly bioidentical to native T4
Can be used in young healthy pts, preggers, and thyroid CA pts
Levothyroxine
What are the ADRs for all hypothyroid drugs?
Liothyronine
Thyroid USP
Levothyroxine
Palpitations, Insomnia, Nervousness Iatrogenic Hyperthyroidism (Heart, Bone, Psych issues)
Make sure to evaluate pt’s taking Levothyroxine at 5-6 week intervals until TSH normalizes.
Avoid Liothyronine (Cytomel) in pregnancy
Name a drug that:
Blocks new thyroid hormone production
1st line in pts with Hyperthyroidism
Avoided in pregnancy/lactation
Can cause Rash, GI upset, arthralgias, HA
Methimazol (MMI)
What is important to monitor in pts taking MMI?
Methimazol
LFTs, CBCs, TSH
Also stop drug if WBC is low (agranulocytosis)
Name a drug that is:
Less effective than Methimazol (MMI)
Blocks thyroid hormone cnoversion and peripheral conversion of T4 to T3
Used EMERGENTLY for pts in thyroid storm who cannot tolerate MMI
Use during 1st trimester of pregnancy and lactation
Propylthiouracil (PTU)
Warning with Propylthiouracil?
FDA warning due to liver failure.
Name 4 beta-blockers that are used to treat Hyperthyroidism related Cardiac stuff.
Propanolol
Atenolol
Metoprolol
Nadolol
Which beta-blocker helps the most with tremors associated with Hyperthyroidism.
Propanolol
Atenolol
Metoprolol
Nadolol
Propanolol
all decrease heart rate and tremors to some extent
What must you be careful for when giving Beta-Blockers to pts with hyperthyroidism…. or any pt really
Beta-blockers affect the heart and Lung beta receptors (non-selective)…. be careful in heart and lung dz pts.
(-olol)
What class do the following drugs belong?
Carbergoline
Bromocriptine
Dopamine Agonists
Used to treat Hyperprolactinemia and Acromegaly
MOA of Cabergoline
Selective for Dopamine D2 receptors
Direct inhibiotry effect on prolactin secretion
Reduces serum prolactin 80-90%
ADR of Carbegoline (Dostinex)
NV, Constipation, NA, Cardiac Valvulopathy (tricusp regurg)
Half Life of Carbegoline?
65 hrs
2 classes used to treat GH excess?
Somatostatin Analogue
GH Receptor Antagonist
Octreotide and Lanreotide Autogel belong to what class of drug?
Somatostatin Analogue
used to treat GH excess (Acromegaly)
Name the only GH receptor antagonist we learned about.
Pegvisomant (Somavert)
MOA of Pegvisomant (Somavert)
Blocks GH effect of target tissues. Elevates GH concentration, lowers IGF-1. (Insulin-like growth factor)
Most Effective…. Expensive
Name the drug used to treat GH deficiency.
Somatropin (humatrope, Genotropin, Nutropin)
MOA of Somatropin?
GH replacement
ADR of Somatropin? (GH replacement)
Intracranial tumors, glucose intolerance, diabetic retinopathy, fluid retension, intracranial HTN.
What drug is used to treat ADH deficiency?
Diabetes insipidus
Desmopressin DDAVP
MOA of Desmopressin DDAVP
Synthetic ADH analog (sub Q injectable)
ADR of ADH deficiency treatment (Desmsopressin)
Nausea, Headache, Abd cramps, hyponatremia, thrombosis.
Drug used to treat Pheochromocytoma while pt is waiting for 1st line tx which is surgical removal of tumor?
Phenoxybenzamine
Phenoxybenzamin MOA?
Long acting Alpha Adrenergic Blocker
Increases blood flow
Lowers BP
ADRs of Phenoxybenzain?
Hypotension, tachycardia, miosis, nasal congestion, ED
Drug used to treat Adrenal Insufficiency Output?
Low cortisol levels
Hydrocortisone!
remember to stress dose!
3 drugs used to treat Hypoparathyroidism?
- Calcium Gluconate
- Calcitriol
- Natpara (injection)
MOA of Calcium Gluconate?
Raises Ca2+
used for calcium deficiency and black widow bites…
MOA of Calcitriol?
Synthetic analog of Vit D3 (most potent), regulates Ca2+ absorption & utilization
(used after thyroid surgery hypocalcemia, dialysis)
Indications of Natapara?
Hypocalcemia due to hypoarathyroidism
Last Line! - must use with Ca2+ and Vit D
ADR of Calcitriol?
Hypercalcemia, Hypercalciuria, Hyperphosphatemia
Vit D intoxication
