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Pharmacology > Drugs for Diabetes Mellitus 1 > Flashcards

Drugs for Diabetes Mellitus 1 Flashcards

1
Q

Insulin preparations - MoA

A

Binds to insulin receptors (mainly skeletal muscles, liver and adipose tissue) activating tyrosine kinase –> phosphorylation of insulin receptor substrate proteins (ISP). Alters enzymes for metabolism. Also increased glucose transporter molecules in membranes (GLUT4) (muscle & fat tissue)

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2
Q

Insulin preparations - Clinical use

A

Used for ALL patients with DM1, and 1/3 of DM2

Gestational diabetes

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3
Q

Insulin preparations - Administration

A

Adm subcut (injection or infusion), inhalation

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4
Q

Insulin preparations - Adverse effects

A

Lipodystrophy at injection site

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5
Q

Rapid-acting insulin - Clinical use

A

Postprandial glycemia

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6
Q

Rapid-acting insulin - Special considerations

A

Onset: 10-20 min, peak at 1h. Duration: <3h

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7
Q

Rapid-acting insulins/ human insulin analogues

A

Insulin lispro
Insulin aspart
Insulin glulisine

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8
Q

Short-acting insulin

A

Regular insulin

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9
Q

Regular insulin - MoA

A

Consists of insulin hexamers crystallized around a zinc molecule.

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10
Q

Regular insulin - Clinical use

A

Diabetic ketoacidosis (IV)

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11
Q

Regular insulin - Special considerations

A

Onset: 30-60 min after injection.
Duration: 5-8h
NOT suitable for postprandial glycemia.

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12
Q

Intermediate-acting insulin

A

Isophane insulin aka neutral protamine Hagedorn (NPH)

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13
Q

Isophane insulin aka neutral protamine Hagedorn (NPH) - MoA

A

Consists of particles of insulin combined with zinc and protamine

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14
Q

Isophane insulin aka neutral protamine Hagedorn (NPH) - Clinical use

A

DM2

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15
Q

Isophane insulin aka neutral protamine Hagedorn (NPH) - Special considerations

A

More prone to erratic absorption and intrapatient variations than long-acting insulins
Low-cost alternative

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16
Q

Long-acting insulins

A

Insulin glargine
Insulin detemir
Insulin degludec

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17
Q

Long-acting insulin - MoA

A

Provide basal levels of insulin and facilitate control of glycemia throughout the day.

18
Q

Long-acting insulin - Special considerations

A

Slow release of insulin – basal level

Diabetic pt started on lower dose.

19
Q

Insulin glargine - MoA

A

Amino acid substitutions in the A and B chains –> released slowly

20
Q

Insulin glargine - Clinical use

A

DM1 & DM2

21
Q

Insulin glargine - Special considerations

A

No peak effect. Often in combo with rapid-acting insulin

Adm 1-2 x daily

22
Q

Insulin detemir - MoA

A

Reversibly binds to albumin in ECF & plasma

23
Q

Ultralong-acting insuilin

A

Insulin degludec

24
Q

Inhaled insulin - Clinical use

A

Postprandial glycemia DM1

25
Q

Inhaled insulin - Special considerations

A

Alternative to short- or rapid-acting insulin esp if injection site reactions, needle aversion, difficulty injecting.
Also effective when injected

26
Q

Hypoglycemic drugs - MoA and Clinical use

A

Increases insulin secretion

DM2

27
Q

Hypoglycemic drugs - groups

A

Sulfonylurea drugs and Meglitinide drugs

28
Q

Sulfonylurea drugs - MoA

A

1) Inh ATP-sensitive potassium channels, preventing K+-efflux and causing Ca2+-influx and activation of pulsatile insulin secretion. No effect on basal insulin secretion.
2) Decreasing glucagon secretion by increasing insulin and increasing pancreatic somatostatin secretion.
3) Increase insulin sensitivity in DM2

29
Q

Sulfonylurea drugs - Clinical use

A

DM2 (without other drugs or dietary restrictions, exercise, weight reduction).
Combo therapy with metformin

30
Q

Sulfonylurea drugs - Special considerations

A

1st generation of these drugs are no longer used!
Advise pt to limit alcohol to 60 ml daily.
Therapy starts with low doses

Adm orally

31
Q

Sulfonylurea drugs - Adverse effects

A

Weight gain
Hypoglycemia (skipped meals, inadequate carbohydrate intake, excessive doses, renal/hepatic diseases), skin rashes,
nausea, vomiting,
cholestasis,
hematologic reactions (leukopenia, thrombocytopenia, hemolytic anemia)

32
Q

Sulfonylurea drugs - Interactions

A

Decreased effectiveness when given with: Thiazide diuretics, corticosteroids, estrogens, thyroid hormones, and phenytoin

Increases hypoglycemic effect when given with:
Angiotensin-converting enzyme inhibitors, sulfonamides, salicylates, NSAIDs, gemfibrozil, alcohol

Alcohol: disulfiram-like reaction

33
Q

Sulfonylurea drugs

A

Tolbutamide - not used
Glimepiride
Glipizide
Glyburide (glibenclamide)

34
Q

Glipizide - Special considerations

A

Absorption is decreased by food. Given 30 min before breakfast.

35
Q

Meglitinide drugs

A

Repaglinide

Nateglinide

36
Q

Meglitinide drugs - MoA

A

Inh ATP-sensitive potassium channels, preventing K+-efflux and causing Ca2+-influx and activation of pulsatile insulin secretion. No effect on basal insulin secretion.

37
Q

Meglitinide drugs - Clinical use

A

Postprandial glycemia (short duration of action)
DM2 (1st line)
Comb with metformin

38
Q

Meglitinide drugs - Special considerations

A

Should not be used with other oral antidiabetic drugs or insulin. Can be used with metformin.
Taken before meals

39
Q

Meglitinide drugs - Adverse effects

A

Hypoglycemia

40
Q

Contraindication for DIA 1 patients

A

Beta blockers: mask hypoglycemic symptoms

Pharmacology (55 decks)

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