Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Endocrine > 186. Diabetic Pharmacology > Flashcards

186. Diabetic Pharmacology Flashcards

1
Q

2 arginines at C terminus of B chain
Aspragine at position 21 of A chain

Acidic - forms microprecipitates at physiologic pH
- does not readily go into circulation

When injected subcutaneously, aggregation results in slower absorption

Onset: 1-4 hours
Duration: 20-24 hours
Duration = Peakless

A

Glargine insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Adverse effects:

  • genetical mycotic and urinary tract infections (d/t increased sugars in urine)
  • Increased risk of amputations
  • diuresis and volume depletion –> CHF
  • abnormalities in renal function

Interacts with gatifloxacin

A

SGLT-2 inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Increases dopaminergic activity in the hypothalamus

  • mechanism for effects on blood glucose is unknown
  • decreases post-prandial glucose without increasing insulin

Orally effective

Adverse effects:

  • nausea and vomiting
  • HAs, fatigue, orthostatic hypotension
  • weak effect
A

Dopaminergic agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Structurally related to sulfonamide antibiotics

Primary effect is to increase secretion of insulin from pancreatic beta-cells

  • used for type 2 DM
  • block K+ channel => Ca2+ channels opening => insulin secretion

Rapidly absorbed after oral administration
- absorption can be reduced by food

Plasma half life of 3-5 hours, but 24 hours duration of hypoglycemic action

Hepatic metabolism - CYP2C9

Renal excretion

A

Sulfonylureas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Natural molecule that associates as hexamers in solution at neutral pH

Onset: 30-60 min
Peak: 2-3 hours
Duration: 5-8 hours

A

Regular insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Coleseyelam

Primary use is in the treatment of hypercholesterolemia

  • lowers plasma glucose in patients with Type 2 DM
  • lowers A1c

Minimally orally absorbed

Adverse effects:

  • constipation, dyspepsia, abdominal pain, nausea
  • increased plasma TGs

Interferes with absorption of many commonly used drugs and fat-soluble vitamins

A

Bile-binding resin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Glargine or determir before breakfast or bedtime with preprandial injections of short-acting insulin

A

Basal/bolus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Act on beta-cell potassium channels
- some overlap in binding sites with sulfonylureas

Very rapid onset with oral administration; stimulate insulin over the period of meal digestion

Metabolized in the liver - CYP3A4
- some renal metabolism

Drug interactions with gemfibrozil

A

Meglitinides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Lysine and proline are reverse which results in a rapid dissociation upon injection (aggregates less)

Onset: 5-15 min
Peak: 30-90 min
Duration: 3-5 hours

A

Lispro insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Bind to PPAR-gamma, which interacts with retinoid X receptors
- promotes transcription of insulin-sensitive genes in liver, muscle, and adipose tissue

Orally effective
Metabolized in liver by several CYPs

A

Thiazolidinediones

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Pre-breakfast and pre-supper injection of a mixture of short- and long-acting insulins

A

Split-mixed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

If A1c is not at target (<7% after 3-4 months) what do you do? (first time)

A

Add another drug to metformin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Biguanide

A

Metformin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Neutral protamine hagedorn (isophane)
- protamine slows absorption in circulation

Onset: 1-4 hours
Peak: 6-10 hours
Duration: 10-16 hours

A

NPH insulin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Acts on a receptor in the proximal tubule

  • functions in reabsorption of glucose which is then returned to the circulation via GLUT-1 and GLUT-2
  • causes glucosuria when the transporter is mutated

Orally effective, peak at 1-2 hours
Metabolized, undergoes fecal and renal excretion

A

SGLT-2 inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Most commonly used oral agent
- first line for type 2 DM

Activates AMP kinase

  • decreases hepatic glucose production
  • suppresses gluconeogenesis
  • increases glycogen storage in muscle
  • less likely to cause hypoglycemia than other agents
A

Metformin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

2 short-acting insulins used in pumps for continuous subcutaneous insulin infusion

A

Aspart and glulisine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Glimepiride
Glipizide
Glyburide

A

Sulfonylureas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

A thiazide drug but has no diuretic effects

Interacts with beta cell K+ channels - opens it (active)
- decreases insulin secretion

Adverse effects:

  • nausea
  • vomiting
  • Na+ and fluid retention
  • thrombocytopenia
  • leukopenia
A

Diazoxide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Inhibit DPP-4 that inactivates GLP-1

Increase glucose-mediated insulin secretion
- decrease glucagon

Orally effective, renally excreted

Adverse effects:

  • HAs
  • allergy
  • nasopharyngitis

CYP3A4 metabolism

A

DPP-4 Inhibitors

21
Q

High affinity for alpha-glucosidases on the brush border of epithelial cells

Delays absorption of glucose, interfering with hydrolysis of disaccharides

Minimally absored, renally excreted

Adverse effects:

  • abdominal pain
  • flatulence
  • weak effects

Interacts with digoxin

A

Alpha-glucosidase inhibitors

22
Q

__ injection is used for patients undergoing diabetic ketoacidosis

A

IV

23
Q

Adverse effects:

  • weight gain, edema
  • macular edema
  • bone fractures
  • possibly bladder cancer
  • increase in CHF

Interacts with rifampin

A

Thiazolidinediones

24
Q

Side effect of insulin that is not hypoglycemia

A

Weight gain (enlargement of subcutaneous fat depots)

25
Q

Binds to the amylin receptor in the hindbrain
- mimics physiological effects of amylin

Slows gastric emptying, decreases post-prandial glucose concentrations

  • anoretic effect
  • inhibits glucagon release

Used as an adjunct in Type 1 or Type 2 DM

A

Amylin analog

26
Q

Risk of hypoglycemia d/t insulin injection is higher in __

A

Children

27
Q

Example of a SGLT-2 inhbitor

A

Canagliflozin

28
Q

Act through GPCRs –> cAMP/PKA activity

Promote glucose-dependent insulin secretion
- only effective in Type 2 DM

Also decrease hepatic glucose production, decrease glucagon secretion, delay gastric emptying, and promote satiety

Can result in weight loss

A

GLP-1 mimetics

29
Q

Regular insulin
Lispro
Aspart
Glulisine

A

Short-acting insulins

30
Q

Example of a meglitinide

A

Repaglinide

31
Q

Aspartic acid replaces proline at B28 which results in a rapid dissociation upon injection (aggregates less)

Onset: 5-15 min
Peak: 30-90 min
Duration 3-5 hours

A

Aspart insulin

32
Q

Pump provides a continuous basal rate, with mealtime bolus injections based on the size and nature of meals

Problems include abscesses, cellulitis, pump failures

A

CSII

33
Q

Example of a dopaminergic agonist

A

Bromocryptine

34
Q

Example of an amylin analog

A

Pramlintide

35
Q

GLP-1 mimetics (2 of them)

A

Exenatide, liraglutide

36
Q

Example of a thiazolidinedione

A

Pioglitazone

37
Q

Acts through GPCRs and cAMP

Increases hepatic glucose production

Adverse effects:

  • nausea
  • vomiting
A

Glucagon

38
Q

Adverse effects:

  • hypoglycemia - elderly and pts w/ renal and hepatic impairments
  • weight gain
  • nausea, vomiting
  • cholestatic jaundice
  • agranulocytosis, aplastic and hemolytic anemia
  • allergic reaction
  • interference with alcohol metabolism (disulfiram-like)
  • Possible CV effects
A

Sulfonylureas

39
Q

NPH insulin
Glargine
Detemir

A

Longer-acting insulins

40
Q

Rapidly absorbed after sc injection

  • exenatide: peaks at 2 hours, not significantly metabolized, excreted by kidneys
  • liraglutide: peaks at 8-12 hours

Adverse effects:

  • nausea, vomiting, abdominal pain, pancreatitis
  • contraindicated in patients with thyroid medullary carcinoma

Drug interactions:

  • antibiotics
  • alcohol
  • oral contraceptives (exenatide)
A

GLP-1 mimetics

41
Q

If A1c is still not at target after an additional 3-4 months then ..

A

Add 2 oral agents or insulin to metformin regimen

42
Q

Regional blood flow, which affects insulin absorption, is affected by (3 things)

A

Exercise
Temperature
Smoking

43
Q

Not metabolized, renal excretion

Adverse effects:

  • indigestion, cramps, diarrhea
  • decreased Vit B12 absorption
  • lactic acidosis

Cationic drugs can increase bioavailability

A

Metformin

44
Q

Administered subcutaneously, prior to meals

Renal metabolism and excretion

Adverse effects:

  • nausea
  • increases insulin hypoglycemic risk
  • contraindicated in patients with disorder of GI motility
A

Amylin analog

45
Q

Example of alpha-glucosidase inhibitor

A

Acarbose

46
Q

DPP-4 inhibitor

A

Sitagliptin

47
Q

Myristoyl fatty acid side chain on B29

Aggregates and binds to albumin (slows down kinetics)

Onset: 1-4 hours
Duration: 20-24 hours
Duration = Peakless

A

Detemir insulin

48
Q

Glutamic acid at B29, lysine at B23 which results in a rapid dissociation upon injection (aggregates less)

Onset: 5-15 min
Peak: 30-90 min
Duration 3-5 hours

A

Glulisine insulin

Endocrine (26 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions