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Which Insulins have a rapid OOA/DOA?
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Which Insulins have a short OOA/DOA?
Regular insulin
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Which Insulins have an intermediate OOA/DOA?
NPH
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Which Insulins have a long OOA/DOA?
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What additive does NPH have to help create a suspension rather than a solution?
Protamine
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Which Insulin is cloudy?
NPH
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A cloudy vs. a clear Insulin indicates what?
- Cloudy: Suspension
- Clear: Solution
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What is a rapid OOA/DOA for insulin?
- OOA: 5-15 minutes
- DOA: 3-5 hrs
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What is a Short OOA/DOA for insulin?
- OOA: 30-60 minutes
- DOA: 5-8 hrs
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What is an intermediate OOA/DOA for insulin?
- OOA: 2-4 hours
- DOA: 10-16 hours
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What is a long OOA/DOA for insulin?
- OOA: 2-6 hours
- DOA: 8-24 hours
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What is the mechanism that gives Detimir its long OOA and DOA?
- Bound to Myristic acid, which make it highly albumin bound
- Must remove Myristic acid and be released from albumin to be active = slow process
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What is the mechanism that gives Glargine its long OOA and DOA?
- 2 arginines added to end of B chain
- Enhances crystal formation at physiological pH, which is slow to dissolve
- Stored at pH 4
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What is the mechanism that gives Insulin Lispro and Aspart their rapid OOA and DOA?
The amino acids are switched at 29 and 28 on the B chain
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Which insulin is sometimes called peakless?
Glargine
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What is the goal fasting glucose for a diabetic?
70-130 mg/dL
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What is the goal for postprandial glucose in a diabetic?
<180 mg/dL
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What is the goal fr Hb A1c for diabetics?
<7%
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What are the Adverse effects of Insulin?
- Hypoglycemia
- Weight gain
- Local reactions – itching, rash, lipohypertrophy
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Which hypoglycemic drugs are Insulin sensitizers?
- Biguanide
- Thiazolidinediones
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Which hypoglycemic drugs are Insulin releasers?
Sulfonylureas and Meglitinides
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Which hypoglycemic drugs are Glucose absorption inhibitors?
Alpha Glucosidase inhibitors
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Which hypoglycemic drugs mimic endogenous incretins?
Incretin drugs
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Which hypoglycemic drugs are Dipeptidyl peptidase – IV inhibitors that prevent the breakdown of endogenous incretins?
Gliptins
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Which hypoglycemic drugs are Amylin analogues?
Pramlintide
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Which hypoglycemic drugs increase glucose excretion?
Na glucose co-transporter 2 inhibitors
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What groups of Hypoglycemic drugs are PO?
Sulfonylureas and Meglitinides, Biguanide, Thiazolidinediones, Alpha Glucosidase Inhibitors, Gliptins, Na+-glucose co-transporter 2 inhibitors
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What groups of Hypoglycemic drugs are IV?
Incretin drugs and Pramlintide
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Sulfonylureas and Meglitinides differ in what way?
- Pharmacokinetics
- Sulfonylureas: Given 1 or 2x per day = Fast OOA (1 hr) and very long DOA
- Meglitinides: Given before meals = Very Rapid OOA (20 min) and short DOA (2-3 hrs)
- Metabolites: Sulfonylureas have active ones and Meglitinides do not
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What is the OOA and DOA of Glipizide?
- OOA: 1 hr
- DOA: 10-20 hours
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What type of drug is Glipizide?
Sulfonylurea
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What type of drug is Repaglinide?
Meglitinide
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What is the OOA and DOA of Repaglinide?
- OOA: 20 minutes
- DOA: 2-3 hours
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What are the 2nd Gen Sulfonylureas?
Glyburide, Glipizide and Glimepiride
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What are the Meglitinides?
Repaglinide and Nateglinide
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Does Glipizide have active liver metabolites?
No
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Does Repaglinide have active liver metabolites?
No
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What is the MOA of Sulfonylurea and Meglitinides?
- Stimulate release of Insulin from B-cells
- By: Blocking ATP sensitive K+ channels and depolarizing B-cells
- May increase sensitivity of muscle and fat cells to insulin
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Which drug can be used in patients with Sulfa allergies, Sulfonylureas or Meglitinides?
Meglitinides
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Which drug can be used in patients with renal impairment, Sulfonylureas or Meglitinides?
Meglitinides – not excreted by the kidneys
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What are the Adverse effects of Sulfonylureas or Meglitinides?
- Excessive hypoglycemia
- Sulfa allergy (Sulfonylureas)
- Weight gain
- Loss of effectiveness/secondary failure
- Sulfonylureas cautioned in renal failure
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