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Pharmacology BAS208 > Diabetes Drugs > Flashcards

Diabetes Drugs Flashcards

1
Q

Lispro (Humalog)

A

Onset: 10-15 min
Peak: 15-120 min
Duration: <5 hr

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2
Q

Glulisine (Apidra)

A

Rapid acting
Onset: 10-15 min
Peak: 15-120 min
Duration: <5 hr

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3
Q

Aspart (Novolog)

A

Rapid acting
Onset: 10-15 min
Peak: 15-120 min
Duration: <5 hr

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4
Q

Regular (R)

A

Rapid acting
Onset:30-60 min
Peak: 2-3 hr
Duration: 6-8 hr

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5
Q

NPH (N)

A

Intermediate acting
Onset: 2-4 hr
Peak: 6-10 hr
Duration: 10-16 hr

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6
Q

Glargine (Lantus)

A

long acting
onset 2-4 hours
no peak action
effective duration 20-24 hours

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7
Q

Determin (Levimir)

A

long acting
onset: 1 hours
no peak action
effective duration 20-24 hours

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8
Q

70%/30% Aspart protamine/aspart

A

Mixed intermediate/short acting
Onset: 30 min
Peak: 2-12 hr
Duration: 10-16 hr

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9
Q

50%/50% NPL/Lispro

A

Mixed intermediate/short acting
Onset: 30 min
Peak: 3-5 hr
Duration: 10-16 hr

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10
Q

75%/25% NPL/Lispro

A

Mixed intermediate/short acting
Onset: 15 min
Peak: 30-90 min
Duration: 10-16 hr

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11
Q

*Active profiles of insulin analogues

A 
insulin lispro aspart, glulisine
regular
NPH
Detemir
Glargine
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12
Q

Insulin effects on glucose levels

A

Insulin lispro, aspart
Regular
NPH or lente
Ultralente or glargine

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13
Q

How Insulin pump works

A

Insulin in reservoir
Travels to cannula inserted in body
needle held by infusion set, adhesive patch

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14
Q

Difficulties of Insulin Pump

A

Physical activity
Insulin or battery could run out
kink in tube

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15
Q

Inhaled Insulin (exubera)

A

rapid acting dry powder
need larger dose
9% of insulin lingered in lungs long after 12 hr
accumulation problems and increase in lung cancer (not statistically sig)
Pulled from market due to lack of interest and cumbersome with restrictions

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16
Q

Inhaled Insulin (Afrezza)

A 
rapid acting
waiting approval
No lingering insulin in lung
smaller apparatus
lower incidence of hypoglycaemia
fewer restrictions
no weight gain
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17
Q

Drugs the decrease the hypoglycaemic effect

A

AIDS antivirals, Albuterol, Oral contraceptives, corticosteroids, diltiazem, diuretics, epinephrine, estrogen, lithium, morphine sulfate, niacin, phenothiazines, thyroid hormones

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18
Q

Drugs that increase the hypoglycaemic effect

A

Alcohol, ACE inhibitors, antidiabetics, beta-blockers, calcium, clonidine, lithium, MAOIs, Salicyclates, Sulfonamides, Tetracycline

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19
Q

Oral Hypoglycemic Agents

A 
Biguanide
Thiazolidinediones
Sulphonlureas
Meglitinides
Alpha-glucosidase inhibitors
Incretin mimetics
DPP inhibitors
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20
Q

Biguanide MoA

A

↓ Hepatic gluconeogenesis
↑ Peripheral insulin sensitivity
Slows intestinal abs. of sugars

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21
Q

Biguanide

metformin

A 
Only oral hypoglycaemic proven to decrease CV mortality
Does NOT cause hypoglycaemia
Decreases HgA1C by 1.5-2%
Modest benefit to lipid profile
Taken with meals
Modest weight loss (loss of appetite)
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22
Q

Biguanide Adverse Effects

A 
LACTIC ACIDOSIS
GI discomfort
DIARRHEA
metallic taste
nausea
anorexia
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23
Q

Biguanide Contraindications

A

Renal Disease

CHF, metabolic acidosis, patients over 80, lactation

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24
Q

Biguanide precautions

A

During surgery with use of contrast dyes

contrast dies can cause kidney failure increasing risk of lactic acidosis

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25
Q

Biguanide Interactions

A

Cimetidine, furosemide (compete for excretion)

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26
Q

Biguanide Drug Interactions

A

Interfere with abs of B12
Alcohol
Cimetidine, furosemide, nifedipine

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27
Q

Biguanide use

A

2-3x/day
no result after 4 weeks add sulfonylurea
extended-release formulation 1x/day with evening meal

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28
Q

Thiazolidinediones (TZD)

A 
Enhance insulin sensitivity
Glitazones
pioglitazone
rosiglitazone
troglitazone (liver toxicity)
Can be used in patients with renal insufficiency and the elderly
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29
Q

MOA thiazolidinediones?

A

Bind to PPAR-gamma receptor site without increasing insulin secretion from beta cells
Inc insulin sensitivity in liver, muscle, adipose tissue.

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30
Q

Thiazolidinediones PK

A

High serum albumin binding
Extensive P450 metabolism
Active metabolites excreted through urine
Parent drug excreted in bile

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31
Q

Thiazolidinedione advantages

A 
May be taken irrespective of meals
does not cause hypoglycaemic events
Reduces TG, blood sugar, insulinemia, HbA1C
Safe in renal failure
Expansion of subcutaneous fat
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32
Q

Thiazolidinediones warning

A

Congestive Heart Failure

cause or exacerbate

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33
Q

Thiazolidinedione Adverse Effects

A 
Weight gain
Osteopenia
Effects on Cholesterol
Fluid retention
Watch for hepatotoxicity
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34
Q

Thiazolidinediones Interactions

A

Oral contraceptives

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35
Q

Thiazolidinediones Contraindications

A

Severe heart failure

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36
Q

Thiazolidinediones Precautions

A

Edema, CVD, liver or kidney disease

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37
Q

Thiazolidinedione Use

A

w or w/o food

eat within 30 min of dose or hypoglycaemia

38
Q

MOA of Insulin secretagogues (sulfonylureas/meglitinides)

A
  • binds to sulfonylurea receptor in beta cells (pancreas)
  • K+ closes
  • Ca2+ opens
  • Ca2+ STIMULATES RELEASE OF INSULIN
    extra-pancreatic effect:
    -reduces serum glucagon
    -inc binding of insulin to target tissues and receptors
39
Q

Insulin Secretagogues: Sulfonylureas, meglitinides, phenylalanine derivatives

A

increase basal and/or postprandial insulin levels
Decrease A1C 1-2%
Depend on function of beta cells

40
Q

Insulin Secretagogues: Sulfonylureas, meglitinides, phenylalanine derivatives Adverse Effects

A

HYPOGLYCEMIA
weight gain
rare allergy

41
Q

Sulfonylureas dosing

A

1-2x/day

42
Q

Meglitinides dosing

A

tid-qid

43
Q

phenylalaninederivative dosing

A

tid-qid

44
Q

Sulfonylureas PK

A

Serum protein binding
LV metabolized
LV or KI excretion

45
Q

What are the adverse effects of sulphonylureas?

A
  1. DISULFURAM REACTION
  2. Stimulates appetite => weight gain
  3. Hypoglycaemia (esp in hepatic/renal insufficiency)
  4. GI upsets
  5. Rash
  6. COQ10 deficiency
  7. MANY DRUG INTERACTIONS
  8. can traverse placenta and deplete insulin in fetal pancreas
46
Q

Sulphonylureas Contraindications

A

LV/KI insufficiency, obesity, concurrent alcohol use

47
Q

What does a sulphur allergy do to Sulphonylruea choice?

A

Use Meglitinide (repaglinide)

48
Q

Sulphonylurea drug interactions increase hypoglycaemic effect

A 
Anticoagulants, clofibrate
chloramphenicol, fluconazole, sulfonamides
H2 receptor antagonist
methyldopa, MAOIs, TCAs
salicyclates
49
Q

Which Drug Interferes with B12 Absorption?

A

Biguanide

Metformin

50
Q

Which drug can cause CoQ10 deficiency?

A

Sulphonylureas

51
Q

MOA of meglitinides

A

stimulate insulin release from B cells by closing K+ channels and opening Ca2+ channels

52
Q

Meglitinides efficacy

A

decrease HgA1C 0.6-1%

53
Q

Meglitinides PK

A

Fast onset, short half life
taken before each meal
LV metabolized by P450 3A4

54
Q

Meglitinides Adverse Reactions

A

URT infection, back pain, hypoglycaemia
Nateglinide- flu like symptoms
Repaglinide- arthralgia, headache, nausea, diarrhea

55
Q

Meglitinides Precautions

A

LV/KI disease

56
Q

Meglitinides Use

A

Repaglinide- 15min before meal can be taken immediately or up to 30 minutes before meal
Nateglinide- up to 30 min before meal
If skip a meal, skip dose
If add a meal, add dose

57
Q

alpha-glucosidase inhibitor (Acarbose) MOA

A

Inhibit glycoside hydrolases needed to digest carbohydrates - decreases postprandial increase in glucose levels

alpha-glucosidase in brush border of small intestine and pancreatic alpha-amylase

58
Q

Acarbose (alpha-glucoside inhibitor) Adverse effects

A

Flatulence
Diarrhea
Abd. cramps
Increase liver enzymes (rare)

59
Q

Alpha glucosidase inhibitor cautions and contraindications

A

Avoid:
Patients with GI disorderes such as ulcerative colitis, Crohn’s disease,bowel obstruction, and short bowel syndrome, Cirrhosis

60
Q

Alpha-glucosidase inhibitor precautions

A

renal impairment, preexisting GI problems

61
Q

Alpha-glucosidase inhibitor Interactions

A

digestive enzymes

62
Q

Alpha-glucosidase inhibitor Use

A

Must be taken with first bite of meal
3x/day
ease in with low dose once daily and gradually increase to minimize GI effects

63
Q

Bile Acid sequestrants

A

Colesevelam

Targets fasting plasma glucose

64
Q

Which drug targets fasting plasma glucose

A

Bile acid sequestrates

65
Q

Amylin Analog

A

Pramlintide
regulates glucose appearance in bloodstream
slows gastric emptying and promotes satiety
suppresses postprandial glucagon secretion

66
Q

Which drug targets post-pradial levels?

A

Pramlintide

amylin analogue

67
Q

Amylin Analogue Adverse Effects

A 
headache
nausea
anorexia
vomiting
hypoglycemia
68
Q

Which drugs cause hypoglycaemia?

A 
Sulphonylureas
Meglitinides
Amylin Analogue
GLP-1 Receptor Agonist
DPP-4 Inhibitors
69
Q

Amylin Analog Interactions

A

Drugs that affect GI motility

Drugs that inhibit nutrient absorption

70
Q

Amylin analog Contraindications

A

Gastroparesis

Hypoglycemia unawareness

71
Q

Amylin Analog Use

A

Subcutaneously immediately prior to meal
can increase dose if patent not experience nausea for 3 days
cannot be mixed with insulin for injecting
Separate from insulin injection site

72
Q

Agents affecting GLP-1 levels

A

Incretins

DPP inhibitors

73
Q

Incretins Role

A

Amplify beta cell insulin response to food

74
Q

GLP-1 receptor agonist

A

Increases insulin and satiety, decreases glucagon and gastric emptying
NO hypoglycemia
Only injectable, GI complaints, possible pancreatitis and medullary cancer, and expensive

75
Q

GLP-1 Receptor Agonist Adverse Reactions

A 
Nausea
vomiting
diarrhea
constipation
dizziness
hypoglycemia
injection site reactions
76
Q

GLP-1 Receptor Agonist Interactions

A

Other anti diabetic drugs
Exenatide- digoxin warfarin, oral antibiotics and contraceptives
Liraglutide- digoxin, griseofulvin, atorvastatin

77
Q

GLP-1 receptor agonist Liraglutide use

A

subcutaneously once daily

Anytime of day, w or w/o food

78
Q

GLP-1 receptor agonist Exenatide use

A

subcutaneously twice daily, within 60 min before morning and evening meal

79
Q

What are the actions of DPP-4 inhibitors?

A

Prevent breakdown of incretin hormones: Increase insulin secretion, decrease glucagon release

80
Q

DPP-4 Inhibition use

A

oral therapy
1-2x/day
w or w/o food

81
Q

DPP-4 inhibitors adverse reactions

A

Nasopharyngitis

hypoglycemia

82
Q

Which drugs have site of action in pancreas

A

Sulphonylureas
Meglitinides
Incretins

83
Q

Which drugs affect glucagon secretion

A

Incretins

amylin analogue

84
Q

Which drug has site of action in gut

A

Alpha-glucosidase inhibitors
Amylin Analogue
Bile acid sequestrant

85
Q

Which drug has site of action in muscle

A

Metformin

TZDs

86
Q

Which drugs have site of action in liver

A

Metformin

TZDs

87
Q

Which drugs affect appetite control

A

Incretins

Amylin Analogue

88
Q

Hyperglycemic herbs

A 
Coffee
cola seeds
ephedra
gotu kola
rosemary leaves
89
Q

What naturopathic medicines can be used with Metformin?

A

Guar gum

B12 and folic acid

90
Q

Naturopathic medicines for Diabetes

A

Licorice
stinging needle (above ground parts)
glucomannan

91
Q

Which drugs are controversial

A

Advantia (TZD) causes CHF, MI, angina

Beyatta (incretin) from lizard spit

Pharmacology BAS208 (5 decks)

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