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Endocrine Week 1 > Diabetes Drugs > Flashcards

Diabetes Drugs Flashcards

1
Q

What is the main difference between treatment of Type I and Type II diabetes?

A

Type I diabetes can only be managed via insulin (and adjuvant low carb diet) while Type II diabetes management incorporates diet, exercise, and oral hypoglycemic drugs as well as insulin

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2
Q

What are the three principal types of insulin preparations?

A

–Short acting: rapid onset of action, short half-life

–Intermediate acting: slower onset, longer half-life

–Long acting: longest half-life, largest crystals

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3
Q

Describe short-acting insulin. AEs?

A

These bind quickly (no LAG) to insulin receptors

–Soluble, clear, crystalline zinc-insulin

–Called Regular Insulin, the only preparation that can be injected IV. All others SC or IM

–All other preparations have been modified to provide prolonged action and are dispensed as turbid suspensions

can be used for both Type I AND II diabetes

AEs: hypoglycemia, lipodystrophy, rare hypersensitivity

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4
Q

Describe Intermediate-acting insulin

A

–NPH insulin [Neutral, Protamine, Hagedorn] (Isophane®)

–Lente insulins [mixture of 30% semilente (short-acting) and 70% ultralente (long-acting) zinc insulin crystals

–Long-acting = large crystals = slow absorption

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5
Q

When is insulin given to a diabetic typically?

A

Short acting AND a NPH/Lente at breakfast and these two again at dinner

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6
Q

When should BG levels be measured daily?

A

4 times BEFORE each meal

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7
Q

Blood glucose before lunch reflects the efficacy of what insulin dose?

Blood glucose before supper reflects the efficacy of what insulin dose?

A

morning regular insulin dose

the morning NPH insulin dose

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8
Q

Blood glucose before bedtime reflects the efficacy of what insulin dose?

A

the evening regular insulin dose

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9
Q

Blood glucose before breakfast reflects the efficacy of what insulin dose?

A

the evening NPH insulin dose

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10
Q

What are some additional strategies developed to improve insulin replacement regimens?

A
  • Inhaled insulin- Exubera® (human insulin inhalation power) Micronized powder administered into the lungs by an inhaler. (Pfizer stopped marketing this preparation in October 2007. It has not been taken off the market.)
  • Insulin pump- Mechanical pump administers insulin through a catheter into abdominal fat. These are very useful for young children
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11
Q

How are the recombinant human insulin products made?

A

–Humulin R® (Lilly) is made using recombinant DNA to produce the hormone in bacteria or yeast.

–Novolin R ® (Novo Nordisk) is also made this way.

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12
Q

What does the R in Humulin R mean?

A

R stands for Regular, not recombinant! R means soluble at room temperature and neutral pH

NOTE: Humulin N and Novolin N are NPH treated products to increase crystal size and increase half-life.

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13
Q

How do Human insulin analogs circulate through the body?

A

Insulin in circulation forms hexamers with Zn2+, but hexamers don’t bind the insulin receptor until dissoc.

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14
Q

What is Insulin lispro (Humalog)?

A

Insulin lispro (Humalog®) is a rapid acting analogue of Humulin® in which the normal Proline B28 and Lysine B29 are switched. Switching is done by mutations of hrDNA. Insulin lispro doesn’t form hexamers. (Exists in circulation as monomer only.)

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15
Q

How are the pharmacokinetics of lispro different than insulin?

A

Humalog® has a faster onset of action and shorter half-life than Regular Insulin.

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16
Q

How is Insulin aspart (NovoLog) different from insulin?

A

Insulin aspart (NovoLog®) as another rapid acting insulin analog (Asp substituted for Pro). It also exists only as a monomer.

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17
Q

How is Insulin glulisine (Apidra) different from insulin?

A

still another rapid-acting insulin analogue that differs from human insulin in that the asparagine at position B3 is replaced by lysine and the lysine in position B29 is replaced by glutamic acid. It also does not form hexamers.

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18
Q

NOTE: Insulin lispro, insulin aspart and insulin glulisine all have the same pharmacokinetic properties–faster onset of action and shorter onset of action. Why?

A

because they exist in the monomeric state

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19
Q

What is Insulin glargine (Lantus)

A

A long-acting recombinant human insulin analog for use as an injection.

•Insulin glargine differs from human insulin - in amino acid Asparagine 21 is replaced by glycine and two arginines are added to the C-terminus of the B-chain.

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20
Q

How do Insulin glargine and insulin detemir work?

A

•Long-acting (up to 24-hour duration of action)

  • When injected, the acidic solution is neutralized, causing crystals to precipitate = slow absorption= long-acting.
  • Can be injected once a day.

Low peak insulin concentration decreases chances of nocturnal hypoglycemia

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21
Q

What is insulin degludec?

A
  • (Tresiba®) is a modified human insulin that has one aa deleted and is conjugated to hexadecanedioic acid via gamma-glutamyl spacer at the amino acid lysine at position B29. This modification allows hexamer formation subcutaneously.
  • No peak concentration; slow absorption.
  • Can be mixed with other insulins.
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22
Q
A
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23
Q

What is Exubera?

A

A short acting human insulin from rDNA in the form of micron-sized particles (dry powder) administered by inhalation into lungs through an inhaler that may be used for either type I or type II diabetics

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24
Q

What are the uses of Exubera?

A

Not a complete replacement for insulin therapy; could replace meal-time injections

•Less difficult but more expensive than injected insulin

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25
Q

Note about hypoglycemia comas. Tx?

A

–Usually caused by INSULIN OVERDOSE

–So common that all comatose patients are given glucose first while blood glucose is being measured.

–Treatment: Glucose

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26
Q

What is a main treatment for severe hypoglycemia?

A

recombinant human glucagon

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27
Q

Describe endogenous glucagon

A

Glucagon is a 29 a.a. peptide secreted by a-cells of the pancreas that is elevated in times of fasting to liberate glucose and raise BG.

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28
Q

What are some indications that hypoglycemia may be occurring?

A

Confusion, shakiness, and feeling of light-headedness. This may cause trembling, sweating, anxiety, and tachycardia

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29
Q

What are some signs that hypoglycemia is progressing and becoming more severe?

A

The development of pounding HA, poor coordination and concentration, numbness in the mouth and tongue, and nightmares

30
Q

What are some oral drugs available for hyperglycemia?

A

Sulfonylureas

Meglitinides

Biguanides

Thiazolidinediones

a-Glucosidase Inhibitors

SGLT-2 Inhibitors

Amylin analogs

DDP-4 inhibitors

31
Q

Describe sulfonylureas

A

These are developed from ABX having hypoglycemic properties and tonically close the ATP dependent K+ channel in B cells to promote insulin secretion. These initially increase insulin release, may decrease insulin metabolism by the liver, and increase insulin sensitivity by enhancing the effect of insulin on glucose uptake.

32
Q

How are sulfonylureas metabolized?

A

These are rapidly absorbed from the GI tract, extensively protein bound, metabolized in liver, and excreted by kidney.

NOTE: Second generation drugs are 10-100x more potent

33
Q

What are the first-gen sulfonylureas? AEs?

A

Chlorpropamide (long half-life), tolbutaminde, and Diabinese

AEs: weight gain, disulfiram-like effects

34
Q

What are the second-gen sulfonylureas? AEs?

A

Glyburide (Micronase),

Glipizide (Glucotrol),

Gliclazide (Diabend), and

Glimepiride (Amaryl)

AEs: hypoglycemia only

35
Q

______ enhance the hypoglycemic action of sulfonylureas.

A

NSAIDs

NOTE: Sulfonylureas require some insulin action and thus are useless in Type I diabetes

36
Q

Describe Meglitinides

A

Benzoic acid derivatives not related to sulfonylureas that stimulate postprandial insulin secretion by binding to K+ channels on B-cell membranes (not the same site as sulonfylureas)

37
Q

What are some Meglitinides?

A

Repaglinide (Prandin)

Nateglinide (Starlix)

38
Q

Describe the pharmokinetics of meglitinides

A

Very rapid GI absorption and has a short half-life before metabolzied by the liver.

39
Q

When should be meglitinides be taken? Uses?

A

Taken before each meal to control post-prandial glucose level.

Use: Used as monotherapy in type II diabetes or combined with metformin

40
Q
A
41
Q

How do Biguanides decrease BG?

A

Their exact mechanism is unknown but they decrease hepatic gluconeogenesis and enhance peripheral insulin sensitvity (in contrast to the other oral hypoglycemics that increase insulin secretion)

42
Q

How are Biguanides metabolized?

A

Absorbed from the GI and have little metabolism

43
Q

Types of Biguanides?

A

Metformin (Glucophase)

Metformin + glyburide (Glucovance)

44
Q

How do Thiazolidinediones work? Metabolism?

A

Bind specifically to Peroxisome Proliferator-Activated Receptor-g (PPARg) to increase insulin sensitivity and adiponectin levels

Little metabolism

45
Q

Types of Thiazolidinediones? Uses?

A

Rosiglitazone (Avandia)

Pioglitazone (Actos)

Rosiglitazone+ metformin (Avandamet)

Glipizide+ metformin (Metaglip)

Uses: Monotherapy in type II diabetes or combined. Safe in renal impairment

46
Q

How do a-Glucosidase Inhibitors work? Uses?

A

These reduce intestinal absorption of starch and disaccharides by inhibiting brush border a-glucosidase which reduces uptake of carbohydrate and reduces post-prandial glucose rise.

•Usually used in combination with other hypoglycemic drugs and/or insulin in Type II diabetes

47
Q

What are some a-Glucosidase Inhibitors?

A

Acarbose (Precose)

Miglitol (Glyset)

48
Q

Describe somatostatin and its action

A

This is a peptide secreted by D cells of pancreatic islets (also some from GI and the brain) that inhibits release of TSH and GH from the pitutiary, as well as inhibiting release of insulin AND glucagon

49
Q

What are some therapeutic uses of somatostatin or its analog drug octreotide (Sandostatin)?

A

-inhibition of insulin from insulinomas or glucagon release from glucagonomas

50
Q

What is the half-life of somatostatin?

A

3-6 min

51
Q

What is Diazoxide?

A

An Antihypertensive antidiuretic that has potent hyperglycemic actions by inhibiting insulin secretion (but does not inhibit insulin synthesis) causing insulin to build up in b-cells.

Diazoxide (Proglycem®) used to treat various forms of hypoglycemia. Used for inoperable insulinomas.

52
Q

What are the effects of GLP-1 (and their drug analogs)? AEs?

A

It increases glucose-dependent insulin secretion/synthesis, inhibits glucagon-stimulated glycogenolysis in the liver, slows gastric emptying, decreases appetite, and decreases glucagon secretion all in order to decrease postprandial blood gluose

AEs: N/V, pancreatitis, weight loss

53
Q

How does GLP-1 affect the heart?

A

provides cardioprotection and increases CO

54
Q

What are incretins?

A

The incretins are hormones that can increase insulin secretion. They were discovered after it was observed that there is more insulin secreted in response to oral glucose versus intravenous glucose.

55
Q

What are the two main incretin hormones in humans?

A

GIP (glucose-dependent insulinotropic peptide; also known as gastric inhibitory peptide) and GLP-1 (glucagon-like peptide-1). Both hormones are secreted by endocrine cells that are located in the epithelium of the small intestine

56
Q

What are some exogenous GLP-1 analogs? Uses?

A

Exanatide (Byetta)

Liraglutide (Victoza) (SC)

Uses: Type II diabetes

57
Q

Describe Exenatide

A

•a synthetic peptide of 39 aa (the natural peptide is exendin-4 isolated from Gila monster venom) inhibits glucagon-stimulated glycogenolysis in the liver. May preserve or increase production of new beta-cells in the pancreas.

This is more potent than endogenous GLP-1

58
Q

How does Sitagliptin phosphate work?

A

(Januvia ®) is an inhibitor of dipeptidyl peptidase-4 (DPP-4), the enzyme that inactivates incretin hormones.

59
Q

What are some others Dipeptidyl peptidase-4 inhibitors? Uses? AEs?

A

Saxagliptin (Onglyza), Linagliptin (Tradjenta)

Uses: Type II Diabetes

AEs: mild urinary or respiratory infections; weight neutral

60
Q

What is Pramlintide Symlin?

A

An analogue of amylin, a peptide hormone released by β-cells of the pancreas along with insulin, after a meal. Like insulin, amylin is deficient in individuals with type 1 diabetes.

61
Q

What are the effects of Pramlintide Symlin?

A

By augmenting endogenous amylin, pramlintide aids in the absorption of glucose by slowing gastric emptying and promoting satiety via hypothalamic receptors (different receptors than for GLP-1), and inhibiting inappropriate secretion of glucagon

62
Q

What is Symlin approved for?

A

Approved for use by the FDA by type 1 and type 2 diabetics who use insulin.

63
Q

What are the effects of Symlin?

A

Symlin® treatment results in weight loss, allows patients to use less insulin, lowers average blood glucose, and substantially reduces the postprandial glucose rise.

64
Q

What are SGLTs?

A

They are a family of glucose transporters found in intestinal mucosal cells (SGLT1) and the proximal tubule of the nephron (SGLT2).

65
Q

What is the role of SGLT2?

A

SGLT2 is responsible for renal glucose reabsorption. 100% of filtered glucose (through glomerulus) must be reabsorbed in the tubules.

In Type 1 diabetes glucose is excreted in the urine (glucosuria) beause SGLT is saturated.

66
Q

What is an approved SGLT2 inhibitor? Others?

A

Canagliflozin (Invokana®)‎ is recently FDA approved for Type 2 diabetes treatment by decreasing reabsorption

Others: Dapagliflozin, Empagliflozin

67
Q

What are the AEs of SGLT2 inhibitors?

A

UTIs, vaginal yeast infections, hyperkalemia, orthostatic hypotension, hypoglycemia, and elevated LDL levels

68
Q

What are some contraindications for SGLT2 inhibitors?

A

–Severe renal impairment

–End stage renal disease

–Patients on dialysis

69
Q

Use of Bile Acid sequestrants in diabetes treatment

A

Colesevelam hydrochloride was developed to lower blood cholesterol and is now approved for Type 2 diabetes patients who are taking other medications. (2 grams/day)

•It lowers HbA1c 0.5% and lowers LDL cholesterol 15%.

70
Q

How is Colesevelam hydrochloride thought to work?

A

Assumed to interrupt enterohepatic cycling and lower Farnesoid X Receptor activation.

71
Q

AEs of bile acid sequestrants?

A

GI related disturbances

Endocrine Week 1 (20 decks)

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