Insulin For Injection

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Contents 1 More Specific Terms 2 Introduction 3 Indications 4 Contraindications 5 Dosage 6 Dosage-adjustment-in-renal-failure 7 Pharmacokinetics 8 Adverse-effects 9 Drug-interactions 10 Mechanism-of-action 11 More General Terms 12 Additional Terms 13 Internet Database 14 References

More Specific Terms

• neutral protamine Hagedorn (NPH) insulin

Introduction

• Tradenames: Iletin, Novolin, Humilin.

Indications

• diabetes mellitus, hyperglycemia, diabetic ketoacidosis
• severe hyperkalemia

Contraindications

• Pregnancy_category: B
• Safety in lactation: +

Dosage

• maintenance 0.5-1 unit/kg/day (doses vary)
• no maximum dose [11]
• severe hyperkalemia: 5-10 units regular plus concurrent IV dextrose
• profound hyperglycemia/ diabetic ketoacidosis ( DKA):

• 0.1 units regular/kg IV bolus

• infusion 100 units regular in 500 mL of normal saline (0.2 units/ mL), at 0.1 units/kg/ hr [allow 100 mL to drain & prime tubing prior to hook-up] 70 kg: 7 units/ hr (35 mL/ hr)
• see insulin sliding scale
• conventional SQ dosing: insulin 70/30 (70% NPH/30% regular) 2/3 in AM, 1/3 in PM
• intensified SQ therapy

• regular insulin 1/4 of daily dose TID before meals
• NPH or Lente 1/4 of daily dose QHS
• mealtime dosage adjusted by patient using fingerstick glucose according to algorithm
• adjustments of +/- 10% of mealtime & QHS insulin based on 3 day trends.

• NPH given QHS selectively reduces fasting hypoglycemia & minimizes weight gain [4]
• avoid injection of > 2.5 mL SQ at any one site [11]

• Injection: 100 units/ mL (10 mL)
• Inhalation:

• dry insulin for inhalation (Exubera) [5,8].

Dosage-adjustment-in-renal-failure

*  creatinine clearance          dose 
*    10-50 mL/min                 75% 
*     < 10 mL/min              25-50%

Pharmacokinetics

* Preparation     Onset (hr)   Peak (hr)  Duration (hr)    Class 
* Lispro           15-30 min    0.5-2.5     3-6.5 
* Aspart           10-20 min    1-3         3-5            rapid 
* Glulisine        10-15 min    1-1.5       3-5 
* Regular          0.5-1        2.5-5       6-8            short 
* Semilente        1-1.5        5-10        12-16 
* NPH (isophane)   1-1.5        4-12        24      intermediate 
* Lente            1-2.5        7-15        24 
* PZI              4-8          14-24       36 
* Ultralente       4-8          10-20       24-28           long 
* Glargine         1.1          none        24 
* Detemir           ?           6-8         12-24 
* Novolin* 70/30    0.5-1.0     4-12        18-24 
* Humulin* 50/50    0.5         2-5.5       18-24        mixture 
* Novolog# 70/30   <0.5-1.0     1-4         15-18 
* Humalog% 75/25   <0.5-1.0     1.6.5       10-16 
* Exubera          10-20 min    0.5-1.5     6         inhalation

• * NPH/regular; Also Humulin 70/30
• # Novolog 70/30 is Aspart 30%/ Aspart protamine 70%
•  % Humalog 75/25 is Lispro 25%/ Lispro protamine 75%

Adverse-effects

• not common (1-10%)

• hypoglycemia*, perspiration, palpitations, tachycardia, tingling of fingers, tremors, confusion, fatigue, loss of consciousness, headache, urticaria, anaphylaxis, hypothermia, hunger, pallor, nausea, numbness of mouth, itching, redness, swelling, stinging, warmth at injection site, atrophy or hypertrophy of subcutaneous fat tissue, muscle weakness, transient presbyopia, blurred vision

• other

• transient edema [4]

• * Caution: avoid exercise within 4 h of regular insulin.
  

• drug adverse effects of hypoglycemic agents

Drug-interactions

• agents that increase hypoglycemic effect

• alcohol
• beta-blockers
• salicylates
• tetracycline
• alpha blockers
• MAO inhibitors

• agents that decrease hypoglycemic effect

• corticosteroids
• oral contraceptives
• tobacco smoke
• thiazide diuretics
• thyroid hormone
• niacin
• diltiazem
  

• drug interaction(s) of fluoroquinolones with hypoglycemic agents

Mechanism-of-action

• via insulin receptor
• improved pancreatic islet beta cell function
• decreased insulin resistance

More General Terms

• parenteral hypoglycemic agent

Additional Terms

• anti-insulin antibody
• insulin analog (synthetic insulins, recombinant insulins)
• insulin device (device for administering insulin)
• insulin in serum
• insulin receptor antagonist (insulin antagonist)
• insulin receptor; IR; (INSR)
• insulin resistance
• insulin sliding scale (ISS)

Internet Database

Prosite: [1]
OMIM: 176730
Entrez gene: 3630
PubChem: 196300
PubChem: 3082397

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
4. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
5. Journal Watch 21(5):44, 2001 Cefalu WT et al; Inhaled Insulin Study Group. Inhaled human insulin treatment in patients with type 2 diabetes mellitus. Ann Intern Med. 2001 Feb 6;134(3):203-7. PMID: [2]
   - Nathan DM. Inhaled insulin for type 2 diabetes: solution or distraction?. Ann Intern Med. 2001 Feb 6;134(3):242-4. No abstract available. PMID: [3]
6. Locus Link [4]
7. Insulins Prescriber's Letter 10(8):41 2004 Detail-Document#: [5] (subscription needed) [6]
8. Prescriber's Letter 12(9): 2005 Diabetes Drugs on the Horizon Detail-Document#: [7] (subscription needed) [8]
9. Prescriber's Letter 13(3): 2006 Detail-Document#: [9] Comparison of Insulins (subscription needed) [10]
10. Prescriber's Letter 15(11): 2008 Insulin Use in Patients With Type 2 Diabetes Detail-Document#: [11] (subscription needed) [12]
11. Prescriber's Letter 16(1): 2009 COMMENTARY: How Much Insulin Is Too Much? CHART: Comparison of Insulins Detail-Document#: [13] (subscription needed) [14]
12. Prescriber's Letter 16(8): 2009 COMMENTARY: Is Lantus Associated With An Increased Risk of Cancer? CHART: Comparison of Insulins Detail-Document#: [15] (subscription needed) [16]
13. Prescriber's Letter 16(10): 2009 CHART: How to Switch Between Insulin Products CHART: Initiation and Adjustment of Insulin Regimens for Type 2 Diabetes CHART: Comparison of Insulins Detail-Document#: [17] (subscription needed) [18]
14. National Guideline Clearinghouse Best practice guideline for the subcutaneous administration of insulin in adults with type 2 diabetes ngc-guideline: [19]

insulin for injection (Novolin, Humilin, Lente, Semilente, Ultralente, Iletin, NPH (isophane), PZI, INS)