Anti-DM Drugs Flashcards
What is the renal glucose threshold?
180mg/dL
What is the effect of Incretin in type 2 DM?
Decreased bcos Incretin —> Increases secretion of Insulin
What are the hormones released by the gut in response to food intake?
GLP-1
GIP: glucose dependent insulonotropic polypeptide
What are the 3 pathophysiologies involved in egregious eleven?
- presence of abnormal microbiota
- Immune dysregulation/inflammation
- increased rate of glucose absorption in the stomach/small intestine
What are the treatment goals of adults w/ DM?
<7.0%
Tx should be individualized
Pre-meal blood glucose: 80-130mg/dL
Post-meal blood glucose: <180mg/dL
What are the different non-insulin DM medications?
Biguanides: Metformin, Buformin
GLP-1 receptor agonists: Exenatide, Liraglutide, Lixisenatide, Semeglutide, Dulaglutide, Albiglutide
SGLT-2 inhibitors: Dapagliflozin, Canagliflozin, Empaglifozin, Luseogliflozin
DPP-4 inhibitors: Sitagliptin, Viladagliptin, Saxagliptin, Linagliptin, Tenegliptin, Gemigliptin, Alogliptin —> “-LIPTIN”
A-Glucosidase inhibtors: Acarbose, Voglibose, Miglitol
Thiazolidinediones: Pioglitazone, Rosiglitazone
Sulfonylurea: Glyburide/Glibenclamide, Gliclazide, Gilmepiride, Glipizide, Gliquidone
Other insuline secretagogudees: Repaglinide, Nateglinide
Bile acid sequestrants: Colesevelam
Amilyn agonists: Pramlintide
Dopamine agonists: Bromocriptine QR
Combined GLP-1 & GIP Agonist: Tirzepatide
What is the only locally available Bugianide?
Metformin
What are the MOA of metformin/Biguanide?
DEC gluconeogenesisis, DEC lipogenesis, DEC insulin secretion, INC Glucagon secretion
What are the adverse effects of Metformin (a BIguanide)?
GI: Nausea, metallic taste, dyspepsia, diarrhea
Vitamin B12 Deficiency -> remember
Lactic acidosis
What are the C/I of Metformin?
If there is renal impairment, avoid when GFR is <30mL/min
What are the different SGLT-2 Inhibitors?
“-liflozin”
DapagLIFLOZIN
EmpagLIFLOZIN
CanagLIFLOZIN
LuseogLIFLOZIN
What are the addition benefits of SGLT2 inihibtor administration?
Weight loss
BP improvement
Renal protective & CV benefits
What are the different indications of SGLT2 inhibitors?
T2DM
ASCVD (indicator for high risk of this)
Heart failure
CKD
What are important AEs of SGLT2 inhibitors?
Female genital mycotic infection &UTI = bcos of glucosuria; proper hygiene
Nasopharyngitis
Dehydration
What are warnings of SGLT2 inhibtors (where u cant give it to them)?
Hypotension due to osmotic diuresis
Increased LDL-C
What is the DOC out of all SGLT2 inhibitors?
Empagliflozin
What cells secrete Incretin?
L cells and K cells
What is the MO Aof GLP1 receptor agonists?
Stimulate Incretin receptors —> INC insuline secretion & DEC glucagon secretion
What glucagon-like polypeptide receptor agonist has a high efficacy of weight loss?
Semaglutide —> very high efficacy
Dulaglutide —> high efficacy
What are drugs approved for weight loss among px without DM?
LIRAGLUTIDE (Saxenda)
SEMAGLUTIDE (Wegovy)
What drug is given in ASCVD or px high0risk?
Liraglutide
What is given for glucose control & weight loss?
Dulaglutide & Semaglutide
What is needed by Semaglutide to enhance absorption in the stomach ?
SNAC
What GLP-1 receptor agonist is the only one that is not indicated if Creatinine Clearance is <30mL/min?
ExaTINIDE
What are the 8 non-insulin drug class for DM?
Biguanides
SGLT2 inhibitor
GLP-1 receptor agonist
DPP-4 agonist
TZD
Sulfonylureas
Alpha glucosidase inhibitors
What are the different Dipeptidyl Peptidase-4 inhibtors?
SitagLIPTIN
VildagLIPTIN
SaxagLIPTIN
LinagLIPTIN
TenegLIPTIN
GemigLIPTIN
AlogLIPTIN
What is the MOA of Dipeptidyl Peptidase-4 inihbitors?
INC circulating levels of native GLP-1 & GIP —> INC glucose-mediated insulin secreiton —> DEC Glucoagon levels —> DEC hepatic gluconeogenesis —> DEC glucose production
What is an AE of DPP4 inhibitors in long term use?
Bullous pemphigoid
Other AEs: INC rate of infections (UTI, nasopharyngitis), headaches, peripheral edema, hypoglycemia
Does DPP4 inhibitor have hypoglycemic effect, and weight loss? What are other important to take note of DPP4inhibitors?
No
Renal
- dose adjustment is necessary
- effective in reducing albuminuria
Cardiac
- INC hospitalizations for HG w/ Alogliptin & Saxagliptin
What is the only Thiazolidinediones available in PH?
PiogLITAZONE
What is the MOA of thiazolidinediones?
Inhibtor of lipolysis
Promotes glucose uptake, utilization, modulation of synthesis of lipid hormones or cytokines
Reduces hepatic glucose production & INC hepatic glucose uptake
What are the AEs of Thialozidinediones?
Fluid retention
INC risk of HG
DEC bone mineral density
Bladder cancer
What are the C/Is of Thiazolidinediones?
Significant liver disease?
Pregnancy and lactation
What is the summary profile of thiazidinediones?
Weigh gain
No effect to induce hypoglycemia
Moderate risk in px who have CHF
Reduce risk in px with stroke risk or transient ischemic attack
What are the diff 2nd generation Sulfonylureas?
Glyburide/Glibenclamide
Glimepiride
Gliclazide
Glipizide
Gliquidone
What is the MOA of Sulfonylureas?
Stimualtes B cells to secrete Insulin
Binds to sulfonylurea-receptor —> inhibits K efflux —> depolarization —> Ca influx —> release of Insulin
What are the important AEs of S ulfonylureas?
Hypoglycemia
Weight gain
INC CV events => adrenergic symptoms
Epinephrine can cause palpitations, starvation, cold sweat, tremors
Disulfram-like rxn with alcohol
What is the only sulfonylurea that has the most favorable CV safety?
Gliclazide
What Sulfonylurea has the longest half life?
Gliclazide —> 10.4 hrs
Others:
Glyburide: ~10 hrs
Glipizide: 2-4hrs
Glimepiride: 5 hrs
What is the summary profile of Sulfonylureas?
Moderate/severe hypoglycemia
Weight gain
Neutral in terms of HF
Possible ASCVD risk
What is the MOA of alpha-glucosidase inhibitors?
Delays digestion and absorption of starch & disaccharides in the gut
What are the alpha-glucosidase inhibitors?
AcarBOSE
VogliBOSE
Miglitol
What is the AE of alpha-glucosidase inhibitors?
Flatulence, diarrhea, abdominal pain
What other non-insulin medications are not available locally?
Glinides/Mglitinides
Bile acid sequestrants
Amylin analog
Bromcriptine quick release
Tirzepatide
What is a Glinides that is a short-acting insulin releasing secretagogues? What are its AE?
Repaglinide/Nateglinide
AEs: hypoglycemia, weight gain
What is a bile acid sequestrant that is a cholesterol-lowering drug?
Colesevelam
What is the MOA of Amylin analog & its AEs?
Suppresses Glucagon release, delays gastric emptying
AEs: hypoglycemia, N/V, anorexia
What is the MOA & AE of Bromocriptine quick release?
hyperprolactinemia
AE: N/V, fatigue, dizziness, headache
What is the MOA of Tirzepatide?
DEC appetite, food intake & bone reabsorption
INC: wt loss, Insulin secretion & synthesis, beta-cell survival, lipolysis, cardioprotection, lipogenesis
What is the basal period?
Required insulin production even w/o eating
For what is a regular insulin given intravenously?
Diabetic ketoacidosis
For how long until you feel the effects of regular insulin?
30-60mins
What are the diff short-acting insulins?
Aspart
Gluisine
Lispro
Regular
What are the diff long-acting insulins?
Degludec
Detemir
Glargine
NPH
What hormone is given upon waking and during dinner?
Neutral protamine hagedorn (NPH)
What are newe
‘
What happens when hyperglycemia crises occur?
Diabetic keotacidosis
Hyperglycemic hyperosomolar state
Which of the ff medications for the tx of diabetes acts directly on the pancreatic alpha cells to decrease glucagon secretion?
A. Dapagliflozin
B. Semaglutide
C. Gliclazide
D. Sitagliptin
B
GLP-1 receptor agonists such as semaglutide stimulate the incretin receptors on the pancreatic alpha and beta cells to dec glucagon secretion & increase insulin secretion
Which of the ff medications for the tx of diabetes increases pancreatic beta cells secretion of insulin?
A. Canagliflozin
B. Pioglitazone
C. Insulin
D. Gliclazide
D
MOA is to INC beta-cell secretion of insulin. Insulin does not promote beta cell production of insulin
Which of the ff medications for the tx of diabetes prolongs the half-life of endogenous.native GLP-1?
A. Insulin
B. Linagliptin
C. Metformin
D. Liraglutide
B
DPP4 enzyme that degrades GLP-1. DPP4i like Linagliptin prolong half-life of GLP-1
A diabetic patient was prescribed pioglitazone. What adverse effect should she be advised to watch out for?
A. Dyspepsia
B. Fluidretention
C. Hypoglycemia
D. Mycoticgenitalinfections
B
Fluid retention or edema is associated with TZDs (e.g., Pioglitazone)
A diabetic patient was prescribed gliclazide. What adverse effect should she be advised to watch out for?
A. Dyspepsia
B. Fluidretention
C. Hypoglycemia
D. Mycoticgenitalinfections
C
Hypoglycemia is associated with sulfonylureas (e.g., Gliclazide) and insulin.
What drugs can cause mycotic genital infections?
SGLT2 inhibitors
EmpagLIFLOZIN
DapagLIFLOZIN
A diabetic patient developed a hip fracture. Which of the following medications that she is taking is associated with an increased risk for fracture?
A. Insulin
B. Pioglitazone
C. Sitagliptin
D. Liraglutide
B
Pioglitazone is a thiazolidinedione (TZD), which is the only drug group that has an adverse effect of fractures. Insulin, Sitagliptin (DPP-4i), and Liraglutide (GLP1-RA) are all bone neutral agents.
What drug class of medications should be added to metformin among patients with heart failure regardless of baseline HbA1c?
A. GLP-1RAs
B. DPP4inhibitors
C. Thiazolidinediones
D. SGLT2inhibitors
D
Based on current guidelines in the management of heart failure and diabetes mellitus, SGLT2 inhibitors are added.
What medication used in the treatment of diabetes mellitus is associated with cobalamin deficiency?
A. Metformin
B. Gliclazide
C. Sitagliptin
D. Insulin
A
Metformin is associated with Vitamin B12 (Cobalamin) deficiency.
In a patient who requires the addition of insulin for glycemic control, which of the following insulins should be initiated first?
A. Glulisine
B. Regular
C. Lispro
D. Glargine
D
A basal insulin should be initiated first to promote glycemic control throughout the day
What type of insulin is given in postprandial phase?
Short-acting insulin
What type of insulin is given in basal phase?
Long-acting: should first induce basal phase to last the whole day
What electrolyte abnormality may be expected among patients on continuous intravenous insulin infusion?
A. Hyponatremia
B. Hypokalemia
C. Hypocalcemia
D. Hypomagnesemia
B
Physiologically, remember that insulin causes potassium to shift intracellularly, thereby causing transient hypokalemia. Hence, it is one of the treatments used in treating severe hyperkalemia.
“Insulin is the key to the cell, K+ goes in once the door is open.”
A patient with type 1 diabetes mellitus will not be allowed to eat breakfast on the morning of his eye surgery. He is maintained on insulin glargine 30 units once a day at bedtime and insulin glulisine 10 units 3x/day before meals. How should he be advised regarding his insulin doses?
A. Do not inject insulin glargine the night before surgery and insulin glulisine on the morning before surgery
B. Do not inject insulin glargine the night before surgery
C. Do not inject insulin glulisine on the morning before surgery
D. Do not inject insulin glulisine for all meals on the day of surgery
C
Only his pre-breakfast short-acting insulin (glulisine) should be withheld
After how many minutes of injecting regular insulin may a patient start his meal?
A. 5
B. 20
C. 30
D. 15
C
Onset of regular insulin is at 30 minutes. Other short-acting insulins, such as Lispro, Aspart, and Glulisine have an onset at 15
Which of the following insulins has a duration of action of up to 24 hours when administered subcutaneously?
A. NPH
B. Regular
C. Glargine
D. Aspart
C
Glargine = 20-24 hrs
NPH = 10-16 hrs
Regular = 3-6 hrs
Aspart = 2-4hrs
