Dosing & Uses
Dosage Forms & Strengths
injectable solution (as 10 mL vial and 3 mL cartridge for OptiClick SC device)
- 100 units/mL
prefilled 3 mL pen (Solostar)
- 100 units/mL
Diabetes Mellitus Type I or II
Indicated to improve glycemic control in adults and children with diabetes mellitus
Dosing considerations
- Equipotent to regular human insulin (ie, elicits same glucose lowering effects on unit per unit basis) when administered IV
- Insulin glulisine has a more rapid onset of action and a shorter duration of action than regular human insulin
- Dosage must be individualized; blood glucose monitoring is essential in all patients receiving insulin therapy
- Total daily insulin requirement may vary and is usually between 0.5-1 unit/kg/day
- Insulin requirements may be altered during stress, major illness, or with changes in exercise, meal patterns, or coadministered drugs
SC injection
- Administer within 15 minutes before a meal or within 20 minutes after starting a meal
- When administered by SC injection, insulin glulisine should generally be used in regimens with an intermediate- or long-acting insulin
- Administered by SC injection in the abdominal wall, thigh, or upper arm
- Injection sites should be rotated within the same region (abdomen, thigh or upper arm) from one injection to the next to reduce the risk of lipodystrophy
Continuous SC injection (insulin pump)
- May be administered by continuous SC infusion in the abdominal wall
- Do not dilute or mix with any other insulin
- Infusion sites should be rotated within the same region to reduce the risk of lipodystrophy
- Insulin in the reservoir must be changed at least q48hr
- Do not expose to temeratures >98.6 F (37 C)
- Initial programming of the external insulin infusion pump should be based on the total daily insulin dose of the previous regimen
- Malfunction of the insulin pump or infusion set, or handling errors or insulin degradation can rapidly lead to hyperglycemia, ketosis and diabetic ketoacidosis
- See prescribing information for compatible insulin pumps
IV administration
- May be administered IV while under medical supervision for glycemic control with close monitoring of blood glucose and serum potassium to avoid hypoglycemia and hypokalemia
- When administered IV, use concentrations of 0.05-1 unit/mL in infusion systems using PVC bags
- Stable only in 0.9% NaCl (normal saline)
- Inspected visually for particulate matter and discoloration prior to administration
- Do not administer insulin mixtures IV
Dosage Forms & Strengths
injectable solution (as 10 mL vial and 3 mL cartridge for Opticlick SC device)
- 100 units/mL
prefilled 3 mL pen (Solostar)
- 100 units/mL
Type 1 Diabetes Mellitus
Indicated to improve glycemic control in adults and children with diabetes mellitus
Dosage of human insulin, which is always expressed in USP units, must be based on the results of blood and urine glucose tests and must be carefully individualized to optimal effect
<4 years: Safety and efficacy not established
4-17 years: May require 0.8-1.2 units/kg/day SC during growth spurts; otherwise use adult dosing (0.5-1 unit/kg/day)
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
Frequency Not Defined
Hypoglycemia
Insulin resistance
Lipodystrophy
Lipohypertrophy
Local allergic rxn
Hypokalemia
Warnings
Contraindications
During episodes of hypoglycemia
Documented hypersensitivity
Cautions
Adjust dosage and monitoring when medically warranted
Decreased insulin requirements: Diarrhea, N/V, malabsorption, hypothyroidism, renal impairment, hepatic impairment
Increased insulin requirements: fever, hyperthyroidism, trauma, infection, surgery
Hypoglycemia is the most common adverse reaction
May cause a shift in potassium from extracellular to intracellular space, possibly leading to hypokalemia; caution when coadministered with potassium-lowing drugs or conditions that may decrease potassium
Frequent glucose monitoring and insulin dose reduction may be required with renal or hepatic impairment
Thiazolidinediones are peroxisome proliferator-activated receptor (PPAR)-gamma agonists and can cause dose-related fluid retention, particularly when used in combination with insulin; fluid retention may lead to or exacerbate heart failure, monitor for signs and symptoms of heart failure and treat accordingly and consider discontinuing thiazolidinediones
Never share a pen between patients even if the needle is changed
Patients using vials must never share needles or syringes with another person
Changes in insulin, insulin strength, manufacturer, type, or method of administration may affect glycemic control and predispose to hypoglycemia or hyperglycemia; changes should be made cautiously and only under close medical supervision and frequency of blood glucose monitoring should be increased; for patients with type 2 diabetes, dosage adjustments in concomitant oral anti-diabetic treatment may be needed
Accidental mix-ups between insulin products reported; to avoid medication errors between APIDRA and other insulins, instruct patients to always check insulin label before each injection
If hypersensitivity reactions occur, discontinue therapy; treat per standard of care and monitor until symptoms and signs resolve; drug is contraindicated in patients who have had a hypersensitivity reaction to it or any of its excipients
Do not mix SC injection with insulin preparations other than NPH insulin
SC insulin infusion
- Do not dilute or mix with any other insulin
- Insulin in the reservoir must be changed at least every 48 hr
- Do not expose to temperatures >98.6 F (37 C)
- Malfunction of the insulin pump or infusion set, or handling errors or insulin degradation can rapidly lead to hyperglycemia, ketosis and diabetic ketoacidosis; prompt identification and correction of cause of hyperglycemia or ketosis necessary; patients using continuous subcutaneous insulin infusion pump therapy must be trained to administer insulin by injection and have alternate insulin therapy available in case of pump failure
Pregnancy & Lactation
Pregnancy
Available pharmacovigilance data have not established an association with insulin glulisine use during pregnancy and major birth defects, miscarriage or adverse maternal or fetal outcomes; there are risks to mother and fetus associated with poorly controlled diabetes in pregnancy
Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, still birth, and macrosomia related morbidity
Animal data
- Animal reproduction studies have been conducted with insulin glulisine in rats and rabbits using regular human insulin as a comparator; insulin glulisine was given to female rats throughout pregnancy at subcutaneous doses up to 10 units/kg/day (2 times the average human dose, based on body surface area comparison) and to rabbits during organogenesis at subcutaneous doses up to 1.5 units/kg/day (0.5 times the average human dose, based on body surface area comparison); effects did not differ from those observed with subcutaneous regular human insulin
Lactation
Available data from published literature suggest that human insulin products are transferred into human milk; there are no adverse reactions reported in breastfed infants in literature; there are no data on effects of exogenous human insulin products, on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant or from underlying maternal condition
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Protein hormone
Insulins lower blood glucose by stimulating peripheral glucose uptake by skeletal muscle and fat, and by inhibiting hepatic glucose production
Absorption
Bioavailability: 70% following SC
Onset: 20 min (SC abdominal or deltoid injection); 30 min (SC femoral injection)
Peak Plasma Time: 1 hr
Peak Plasma Concentration: 83 microUnits/mL
Duration of action: 5 hr
Distribution
Protein Bound: 5% (not bound to serum binding-protein, but present as a monomer in plasma)
Vd: 13 L
Metabolism
Liver >50%; kidney 30%; adipose tissue/muscle 20%
Elimination
Half-Life: 13 minutes (IV); 42 min (SC)
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Formulary
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