Insulin-glulisine

Glulisine is a biosynthetically produced human insulin (Kasper 2015) and is one of the rapid-acting insulin analogues (Robinson 2006). It has been approved since 2004 (Danne 2016).

Pharmacodynamics

By varying the amino acid sequence (exchanging the amino acids proline and lysine at position B 28 and B 29 [Siegenthaler 2006]), the subcutaneous formation of hexamers is prevented in insulin glulisine. This causes the more rapid absorption (Herold 2018).

Glulisine exhibits intrinsic stability and ensures rapid release of insulin monomers (Becker 2007).

Indication

Glulisine is an insulin approved for children, adolescents, and adults (Garnock- Jones 2009) that can be used for therapy of type 1 diabetes or type 2 diabetes (Prinz 2012) such as in:

• SIT (supplemental insulin therapy)
• Intensified insulin therapy (both ICT and insulin pump therapy [Herold 2020]).
• Basic bolus concept (Alawi 2019).

Dosage and method of administration

Insulin glulisine is applied s. c.. It is not approved for i.v. application (Weihrauch 2020).

It can be injected into the abdominal wall (faster absorption) and into the front or outer thigh (slower absorption).

(Schubert 2009)

Injection sites should be changed constantly to avoid lipohypertrophy (Marischler 2020).

Insulin glulisine can be injected shortly before (< 10 min) or shortly after a meal (Kasper 2015)

Advantages

• less frequent occurrence of postprandial hypoglycemia, (especially since the decay of the effect of insulin corresponds to the postprandial decline in plasma glucose levels [Kasper 2015])
• in most cases it is possible to do without snacks in between meals
• no or short injection-meal interval
• postprandial injection possible (Herold 2018)
• HbA1c- value:

In both type 1 diabetes and type 2, insulin glulisine lowers the HbA1c- value better than human insulin (Garg 2005). The reduction already reaches a similar level after 12 weeks as e.g. human insulin or insulin lispro after 26 weeks (Robinson 2006).

After 12 months of treatment, a drop in type 1 diabetics from 8.36 to 7.53 and in type 2 diabetics from 8.3 to 7.29 occurs.

Of type 1 diabetics, 50% achieved their individual HbA1c- target while on glulisine therapy, and 45% of type 2 diabetics (Hubert 2019).

• Patient-friendly handling through cartridges or ready-to-use pens (Ebenbichler 2010).

Disadvantages

• need for exact dosage of basal insulin supply
• Duration of action may be too short with slowly absorbed carbohydrates (Herold 2018)

Adverse effects

• Hypoglycemia (only rarely see "Advantages" above [Kasper 2015])
• Lipodystrophy at the injection sites
• allergic reaction
• Insulin resistance (Dellas 2018)

Contraindication

Absolute contraindications:

• Hypoglycemia
• Insulinoma (Flake 2021)

Preparations

• Insulin Glulisine

The drug is commercially available under the name "Apidra". The onset of action occurs after 10 min, and the duration of action is approximately 3.5 h (Herold 2018).

Insulin glulisine may be freshly mixed in a syringe with NPH insulin only and should be injected immediately thereafter (Frankincense 2020).

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