Drugs For Diabetes Dr. Konorev

Question 1

Insulin activates what 2 things

Answer 1

Glycolysis + Glycogen synthase

Question 2

2 drug classes that can treat T1D

Answer 2

Insulins + Amylin Analog

Question 3

Rapid Acting Insulins

1. 3 of them
2. Clinical use + administration
3. Duration

Answer 3

1. Aspart, Lispro, Glulisine
2. Postprandial hyperglycemia (Take before meal, IV)
3. 1hr-3hr

Question 4

Short Acting Insulins

1. 1 of them
2. Clinical use + administration
3. Duration

Answer 4

1. Regular Insulin
2. Base insulin regulation + Postprandial hyperglycemia (IV 45min before meal) + Overnight coverage
3. 3hr-5hr

Question 5

Intermediate Acting Insulins

1. 1 of them
2. Clinical use + administration
3. Duration

Answer 5

1. NPH (Neutral Protamine Hagerdorn) use is declining = protamine + Zn insulin
2. Maintenance + overnight
3. 10hr-12hr

Question 6

Long Acting Insulins

1. 2 of them
2. Clinical use + administration
3. Duration

Answer 6

1. Detemir (Lys 29, rapid absorption + binds to albumin) + Glargine (low pH solvable insulin)
2. Maintenance + overnight
3. 24hr, inject 1-2 times a day

Question 7

Insulin is used also in what besides DM

Answer 7

Hyperkalemia sever, (Insulin + glucose) = takes long time

Loop Diuretics also given for immediate elimination of K+

Question 8

Artificial or bionic pancreas

Answer 8

Insulin delivery system )glucose sensor + microchip controlling + insulin pump
= NON invasive, placed over BVs on skin to measure blood glucose with electromagnetic waves

Question 9

Adverse effects insulin

Answer 9

1. Hypoglycemia
2. Lipodystrophy : hypertrophy of SubQ fat at injection site
3. IgG against insulin = resistance
4. Allergic reaction rare
5. Hypokalemia*

Question 10

Hypoglycemia is usually caused with during insulin tx

Answer 10

1. Delay of meals or missed meal
2. Exercises
3. Insulin overdose

Question 11

Hypoglycemia SX

Answer 11

1. CNS, confusion, coma,
2. Tachy, sweating, tremor, palpitations, hunger, N,
   TX = give glucagon or sucrose/glucose

Question 12

Amylin Analog

1. What is it
2. MOA

Answer 12

1. Pancreatic H made by B-cells
2. Enhance insulin action by (inhibiting glucagon secretion, lower gastric emptying for more absorption time, increase satiety)

Question 13

Amylin Analog:

1. 1 drug
2. Clinical use
3. Duration

Answer 13

1. Parmlintide SUB Q* administration
2. T1D**, T2D with mealtime insulin, (injected with insulin before meals when there is no insulin in the pt)
3. 3hr

Question 14

Pramlintide side effects

Answer 14

1. N, V, Hypoglycemia, Constipation

Question 15

Glucose to insulin release happens how

Answer 15

1. Glucose binds GLUT 4
2. K+ channel closes = increases ATP
3. Depolarization happens
4. Ca+ goes into cell (when PKA is phosphorylation)
5. Insulin leaves cell

Question 16

Drug types increasing Gs (more insulin) and drugs increasing Gi (lowerring insulin)

Answer 16

1. Gs: B2 agonist (isoproterenol) + GLP-1 agonist (incretin)
2. Gi : Somatostatin + a2 agonist + B Blockers

Question 17

GLP-1 role and and reason it is not as useful

Answer 17

1. Increase insulin, lower glucagon, B-cell proliferation

2. Very short half-life (1-2min) due to DPP-4 cleaving it

Question 18

Incretin drugs that are useful

Answer 18

1. Long-Acting GLP1 receptor agonist

2. DPP-4 inhibitors (keeps GLP-1 from being cleaved)

Question 19

Long-Acting GLP1 receptor agonist

1. 2 drugs
2. Clinical use

Answer 19

1. Exenatide (from Gila monster saliva 2.4hr) + Lirglutide (binds to albumin 11-15hr)
2. T2D patients that are not adequately controlled by metformin , Sulfonylurea, Thiazolidinediones + oral drug

Question 20

Long-Acting GLP1 receptor agonist SIDE EFFECTS

Answer 20

Hypoglycemia (lower then insulin + Sulfonylurea) , N,V, D

Question 21

DPP4 inhibitors

1. 4 Drugs
2. MOA
3. Clinical use

Answer 21

1. Sitagliptin, Linagliptin, Saxagliptin, Alogliptin
2. Increase GLP levels due to not cleaving it
3. Adjunct to diet and exercise in T2D, can be taken with metformin and he other drugs

Question 22

Sulfonylureas :

1. 1st gen drugs
2. 2nd gen drugs
3. 2 nonsulfonylureas drugs (Meglitinides)

Answer 22

1. Chlorpropamide + Tolbutamide + Tolazamide
2. Glipizide + Glyburide + Glimepiride
3. Nateglinide + Repaglinide

Question 23

Sulfonylureas :

1. MOA
2. Half-life
3. Clinical use

Answer 23

1. K ATP channel Blockers (bind to SUR1. +Kir6.2 to block)

2. T2D main drug , Meglitinides are short (before eating)

Question 24

Sulfonylureas 1st gen

Answer 24

Infrequent use , ,used in high doses

Question 25

Sulfonylureas 2nd gen

Answer 25

``` Higher potency (lower dose) , lower adverse effects = used more ```

Question 26

Sulfonylureas side effects

Answer 26

1. Hypoglycemia**** | 2. Increased weight gain from insulin increase *

Question 27

Sulfonylureas drug interactions *

Answer 27

1. NSAIDS, alcohol, anti-fungal = enhance hypoglycemia | 2. B-blockers, CCB, hepatic CYP enzymes = increase glucose in blood lower Sulfonylureas effectiveness

Question 28

Meglitinides 1. MOA 2. Clinical use

Answer 28

1. K + blocker (similar to Sulfonylurea) | 2. Short half-life, so before eating

Question 29

METFORMIN 1. MOA 2. Clinical use 3. Advantages

Answer 29

1. AMP-activated protein kinase activator (increase ATP uptake processes and decrease ATP consumption) = lowering glucose 2. 1st line for T2D, oral (purpose to get glucose levels and A1C levels right) 3. Does not cause hypoglycemia, does not cause weight gain, decrease macro and micro vascular complications in DM

Question 30

METFORMIN 1. Half-life 2. Adverse effects

Answer 30

1. 1.5hr-3hr (no drug-drug interactions) 2. = GI N,D, ABD pain = Lactic acidosis (esp if renal or hepatic insufficiency) = contraindications in HF, COPD, renal failure, chronic alcoholism, cirrhosis (tissue hypoxia)

Question 31

Thiazolidinediones 1. 2 drugs 2. MOA

Answer 31

1. Pioglitazone + Rosiglitazone | 2. PPAR-gamma nuclear R in muscle, liver, fat, endothelium (activated cause peroxisome proliferations) = INCREASE GLUT4

Question 32

Thiazolidinediones 1. Administration 2. Clinical use 3. Adverse effects

Answer 32

1. Oral, full effect after 1-3mo 2. Safe in pt what renal insufficiency + T2D, DELAYS PRE-DM to DM + no hypoglycemia (makes insulin for sensitive, lowering resistance) 3. Weight gain, edema (increased vascular permeability, increase NA and water reabsorption =edema, CONTRAindicated in HF) + suppress MSCs into osteoblasts = osteoporosis esp in women

Question 33

Euglycemic drugs (does not cause hypoglycemia) however lower blood glucose to normal level

Answer 33

Thiazolidinediones + Metformin (not insulin and K+ blockers)

Question 34

Gliflozins : 1. MOA 2. 3 drugs

Answer 34

1. Na+/Glucose cotransporter 2 inhibitor (SGLT2 inhibitors) = reduce reabsorption of glucose in Proximal Tubule 2. Canagliflozin+ Dapagliflozin + Empagliflozin

Question 35

Gliflozins 1. Clinical use 2. Adverse effects

Answer 35

1. NEW drug, no hypoglycemia, T2D lower glucose in blood , REDUCE BP (improve Cardiac and renal problems and future probs) orally before 1st meal 2. WL, lower uric acid, osmotic diuresis (dehydration)

Question 36

Gliflozins contraindications in and serous adverse effects

Answer 36

1. Hypotension | 2. Hypovolemia (orthostatic hypotension, dizziness, syncope) + UTI, genital infection

Question 37

A-glycosides inhibitors 1. 2 drugs 2. MOA 3. Clinical use

Answer 37

1. Acarbose + Miglitol 2. Inhibit GI absorption of glucose to blood 3. Lower postprandila hyperglycemia ( you dont need that much insulin)

Question 38

A-glycosidase inhibtors 1. Advantages 2. Adverse effects

Answer 38

1. No hypoglycemia, no WG, T2D before meals | 2. Malabsorption, d, flatulence, bloating