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Pharm II Test 3 > Diabetes Mellitus Type 2 > Flashcards

Diabetes Mellitus Type 2 Flashcards

1
Q

Biguanides- Available Drugs

A

Metformin

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2
Q

Metformin- Mech of Action

A

INHIBIT COMPLEX I OF MITOCHONDRIAL OXIDATIVE PHOSPHORYLATION–> INCREASE AMP/ATP RATIO–> ACTIVATE AMP DEPENDENT KINASE (AMPK)–> REDUCE HEPATIC GLUCONEOGENESIS/INCREASE IN INSULIN SENSITIVITY IN MUSCLE AND ADIPOSE–> INCREASE GLUCOSE UTILIZATION–> LOWER FASTING PLASMA GLUCOSE

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3
Q

Metformin- Kinetics

A

HbA1c decrease= 1.5%

duration= 6 hr

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4
Q

Metformin- Clinical Use

A

DOC FOR ALL TYPE II DM THAT ISN’T CONTROLLED BY DIET AND EXERCISE ALONE

LOWERS FASTING GLUCOSE

requires the presence of insulin for its effects
improves lipid profiles (decreases FFA, TGs, LDL, increases HDL)

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5
Q

Metformin- Side Effects/Contraindications

A

DOES NOT CAUSE WEIGHT GAIN

generally well tolerated
can inhibit absorption of B12

POTENTIALLY FATAL LACTIC ACIDOSIS (DEEP, RAPID BREATHING, VOMITING, ABDOMINAL PAIN, WEAKNESS OF LEGS AND ARMS)–> USUALLY SEEN IN RENAL INSUFFICIENCY, CHF, MI, HYPOXIC STATE

CONTRAINDICATED in: 
pregnancy
IMPAIRED LIVER OR RENAL FUNCTION
elderly
patients taking iodinated contrast agent
other conditions predisposing to lactic acidosis- CHF, MI, shock, septicemia, hypoxic/ischemic state, serious illness
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6
Q

Thiazolidinediones- Available Drugs

A

Pioglitazone

Rosiglitazone

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7
Q

Pioglitazone, Rosiglitazone- Mech of Action

A

AGONIST FOR PPAR-G TRANSCRIPTION FACTOR–> INCREASE GLUT4 EXPRESSION, ADIPONECTIN, FFA UPTAKE, ADIPOSE REMODELING AND DECREASE TNF-A/RESISTIN–> INCREASE INSULIN SENSITIVITY IN ADIPOSE, MUSCLE, LIVER–> INCREASE GLUCOSE UTILIZATION

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8
Q

Pioglitazone, Rosiglitazone- Kinetics

A

HbA1c decrease= 0.5%

duration= weeks

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9
Q

Pioglitazone, Rosiglitazone- Clinical Use

A

LOWERS FASTING GLUCOSE
lowers TGs

monotherapy or in combination with metformin, sulfonylureas, or insulin for DM 2

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10
Q

Pioglitazone, Rosiglitazone- Side Effects/Contraindications

A

SUB-Q WEIGHT GAIN

FLUID RETENTION–>PERIPHERAL EDEMA–>RISK OF HEART FAILURE

ROSIGLITAZONE CAN CAUSE MI AND CARDIOVASCULAR DEATH = not on the market anymore

decrease bone density–> fracture risk in women
hepatotoxicity

CONTRAINDICATED IN LIVER DISEASE, HEART FAILURE, CVD, preganancy

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11
Q

Sulfonylureas- Available Drugs

A

2nd Gen:
Chlorpropamide
Tolbutamide

3rd Gen:
Glimepiride
Glyburide
Glipizide

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12
Q

Sulfonylureas- Mech of Action

A

INHIBIT K CHANNELS IN B-CELLS–> INCREASED [K]INTRACELLULAR–> MEMBRANE DEPOLARIZATION–> OPEN CA CHANNEL–> INCREASE [CA]INTRACELLULAR–> INCREASE SECRETION OF INSULIN

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13
Q

Sulfonylureas- Kinetics

A

LONG DURATION OF ACTION
metabolized by liver and excreted in kidney

HbA1c decrease= 1.5%
duration= 14-24 hrs

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14
Q

Sulfonylureas- Clinical Use

A

LOWERS FASTING GLUCOSE

dependent on B-cell function- most effective in patients that have had diabetes for less than 10 years, still have functional B cells

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15
Q

Sulfonylureas- Side Effects/Contraindications

A

HYPOGLYCEMIA especially in liver/renal dysfunction and the elderly

weight gain

CONTRAINDICATED IN:
IMPAIRED RENAL/HEPATIC FUNCTION
elderly
DM 1
pregnancy
lactation
sulfa allergies
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16
Q

Sulfonylureas- Drug Rxns

A

High protein binding- interaction with other protein binders (Salicylates, B-blockers, warfarin, fibrates)

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17
Q

Meglitinides- Available Drugs

A

Nateglinide

Repaglinide

18
Q

Nateglinide, Repaglinide- Mech of Action

A

INHIBIT K CHANNELS IN B-CELLS–> INCREASED [K]INTRACELLULAR–> MEMBRANE DEPOLARIZATION–> OPEN CA CHANNEL–> INCREASE [CA]INTRACELLULAR–> INCREASE SECRETION OF INSULIN

19
Q

Nateglinide, Repaglinide- Kinetics

A

SHORTER ACTING, FASTER ONSET

HbA1c decrease= 1-1.5%
duration= 2-4 hrs

20
Q

Nateglinide, Repaglinide- Clinical Use

A

CONTROL POSTPRANDIAL GLUCOSE ELEVATIONS

should be taken with or shortly before meal

21
Q

Nateglinide, Repaglinide- Side Effects/Contraindications

A

Hypoglycemia, weight gain

CONTRAINDICATED IN:
LIVER DISEASE
pregnancy

22
Q

GLP-1 Homologs- Available Drugs

A

Exenatide

Liraglutide

23
Q

Exenatide, Liraglutide- Mech of Action

A

BIND GLP-1 RECEPTOR ON PANCREATIC B-CELLS–> INCREASE GLUCOSE INDUCED INSULIN RELEASE/DECREASE GLUCAGON RELEASE/INCREASE B-CELL REGENERATION/INCREASE SATIETY

24
Q

Exenatide, Liraglutide- Kinetics

A

injected SubQ twice daily

HbA1c decrease= 0.5-1%
duration= 6-15 hrs

25
Exenatide, Liraglutide- Clinical Use
DECREASE FASTING GLUCOSE DECREASE POSTPRANDIAL GLUCOSE promotes weight loss alternative to starting insulin in patients not controlled with metformin, sulfonylurea, or both
26
Exenatide, Liraglutide- Side Effects/Contraindications
Frequent nausea, vomiting, diarrhea Little chance of hypoglycemia BLACK BOX WARNING FOR RARE PANCREATITIS
27
DPP-IV Inhibitors- Available Drugs
Sitagliptin | Saxagliptin
28
Sitagliptin, Saxagliptin- Mech of Action
INACTIVATES DPP-IV, THE GLP-1 PEPTIDASE= INCREASES ACTIONS OF GLP-1
29
Sitagliptin, Saxagliptin- Kinetics
PO once daily HbA1c decrease= 0.48-0.61% duration= 24 hrs
30
Sitagliptin, Saxagliptin- Clinical Use
DECREASE FASTING GLUCOSE DECREASE POSTPRANDIAL GLUCOSE monotherapy or adjuvant with metformin or thiazolidinedione
31
Sitagliptin, Saxagliptin- Side Effects/Contraindications
little risk of hypoglycemia | BLACK BOX WARNING FOR RARE PANCREATITIS
32
Alpha-glucosidase Inhibitors- Available Drugs
Acarbose | Miglitol
33
Acarbose, Miglitol- Mech of Action
INHIBIT A-GLUCOSIDASE-->PREVENT DIGESTION OF CARBOHYDRATES--> DECREASE GLUCOSE ABSORPTION
34
Acarbose, Miglitol- Kinetics
HbA1c decrease= 0.5-0.8% | duration= 3-4 hrs
35
Acarbose, Miglitol- Clinical Use
DECREASE POSTPRANDIAL GLUCOSE less potent than other drugs- not considered a first line drug
36
Acarbose, Miglitol- Side Effects/Contraindications
no risk of hypoglycemia abdominal pain, flatulence CONTRAINDICATED IN: IBD CHRONIC INTESTINAL DISEASE COLONIC ULCERATION OR OBSTRUCTION
37
Amylin Mimetic- Available Drugs
Pramlintide
38
Pramlintide- Mech of Action
MIMIC ENDOGENOUS AMYLIN--> CONTRIBUTE TO POSTPRANDIAL GLUCOSE CONTROL- DECREASE GLUCAGON RELEASE, DECREASE HEPATIC GLUCONEOGENESIS, SLOW GASTRIC EMPTYING, INCREASE SATIETY
39
Pramlintide- Kinetics
injected HbA1c decrease= 0.5-0.7% duration= 2-3 hrs
40
Pramlintide- Clinical Use
adjuvant to insulin for DM type 1 or type 2 DECREASE POSTPRANDIAL GLUCOSE promote weight loss
41
Pramlintide- Side Effects/Contraindications
nausea | hypoglycemia, especially with insulin- need to reduce insulin dose 50%

Pharm II Test 3 (9 decks)

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