insulin glulisine (Apidra, Apidra Solostar)

Dosing and uses of Apidra (insulin glulisine)

• Adult
• Pediatric

 

Adult dosage forms and 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

 

Pediatric dosage forms and 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)

 

Apidra (insulin glulisine) adverse (side) 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

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

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Considered safe during breastfeeding

 

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 of Apidra (insulin glulisine)

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)