Karakteristik Insulin

(NPH, Glargine, Determir dan Degludeg)

Kelompok 2
052115153001 Nur Aini Indah Febriyanti 052115153006 Surya Dwiyatna
052115153002 Aulia Tamara 052115153007 Rifdah Atikah Safitri
052115153003 Nabila A.Y. Kuswandi 052115153008 Naning Ni’mawati
052115153004 Ade Giriayu Anjani 052115153009 Ahmad Nasir
052115153005 Fauziah Hasdin 052115153010 Nelly Kurniawati
 Profil
NPH GLARGINE DETEMIR DEGLUDEG
Deskripsi Human Insulin, DNA Analog human insulin Analog human insulin, DNA Analog Human Insulin
recombinant pada E.Coli recombinant pada
atau Saccharomyces Saccharomyces Cerevisiae
Cerevisiae
Human insulin Substitusi glisin A21 dg B30 dihapus, + 14 Asam lemak B30 dihapus, + Asam
Struktur Aspargin, + 2 arginin di Myristol pd B29  terikat dg lemak 16 C di rantai B29
rantai B30 albumin
Pemerian Suspensi (cloudy) Jernih Jernih Jernih, tidak berwarna
pH 7-7,5 4 7,4 7,6
Dosis 0,1 -0,2 U/kg/hari 0,5-1,5 U/kg/hari 1dd1/2dd1 0,4U/kg/hari
15 min sebelum atau 1dd1 atau 2dd1, Diinjeksikan sore hari atau
segera setelah makan diinjeksikan pada jam menjelang tidur
yang sama setiap hari
Sediaan U100 vial, U100 prefilled U100 vial, U100 prefilled U100 vial, U100 prefilled pen U100 prefilled pen
pen pen U200 prefilled pen
U300 prefilled pen
Rute SC SC SC SC
 Farmakokinetik
NPH GLARGINE GLARGINE DETEMIR DEGLUDEG
100U/ml 300 U/ml
Onset 1,5 – 4 jam 1,5 jam 3-4 jam 30-90 menit
Durasi 5 -12 jam Hingga 24 jam > 24 jam 6-23 jam 42 jam
tmax 6 – 12 jam 8-12 jam Close to 6 – 8 jam 9 jam
peakless
Ikatan 5% 98% ≥ 99%
protein
t1/2 4,4 jam 12 jam 19 jam 25,1 jam
Steady state 3-5 hari
Vd 0,15 L/Kg 0.1 L/Kg 0,7 L/Kg
49 L BB 70kg post
dosis 0,4U/kg sc
CL 0,03L/kg BB 70kg post
dosis 0,4U/kg sc
 NPH GLARGINE DETEMIR DEGLUDEG
terdepo di subcutan pH 4 diinjeksikan di pH 7,4 Terdapat rantai samping Hexadecanedioic acid
Penyebab membentuk presipitasi di asam lemak (14-C Fatty sebagai halangan
lamanya tempat injeksi (sc) depo Acid) yang mendorong sterik memperlambat
 dilepas perlahan pembentukan unit kerusakan
durasi multiheksamer dan multihexamer oleh ezim
(Mekanisme berikatan dengan albumin protease
Kerja)  kerja insulin lebih
panjang

Membentuk komplek Variabilitas antar individu Resiko hipoglikemi

Kelebihan dengan protamin sehingga tidak se signifikan insulin nocturnal rendah
memperlambat absorbsi NPH
(meningkatkan durasi)
Kekurangan Profil PK basal paling tidak Belum bisa menyamai Harga lebih mahal
ideal insulin fisiologis, dosis
Hipoglikemia tidak bisa rendah durasi action tidak
diprediksi sampai 24 jam

Contoh Merk Humulin N®, Novolin N® Lantus® Levemir® Tresiba®

PROFIL FARMAKOKINETIKA
Struktur Human Insulin (NPH)
BACK
 Mekanisme Kerja
Human Insulin (NPH) Mekanisme Kerja Glargine
Mekanisme Kerja Detemir
 Mekanisme Kerja Degludeg

BACK
Profil Farmakokinetik (Cheng et al., 2021)
Perbandingan IDeg dengan Insulin Basal Lain (NPH, IGLAR, IDEG)

NPH Iglar Ideg

(Woo, et al., 2020)

 Profil Farmakokinetik (Jaronsiki et al., 2021)

Profil insulin degludec selama 24 jam memiliki kurva yang datar dan fluktuasi paling
minimal dibandingkan jenis insulin basal lainnya (Jaronsiki et al., 2021)
 DAFTAR PUSTAKA
• Atkin, S., Javed, Z. & Fulcher, G., 2015. Insulin Degludec and insulin aspart: novel insulins for the management of diabetes
mellitus. Therapeutic Advances in Chronic Disease, 6(6), pp. 375-388.
• Hanne dan Haise, 2014, A Review of the Pharmacological Properties of Insulin Degludec and Their Clinical Relevance, Clin
Pharmacokinet, Vol. 53, pp. 787-800.
• Jennifer G, Christoph , K Jeremy P, Tim H, 2017, Understanding how pharmacokinetic and pharmacodynamic differences of
basal analog insulins influence clinical practice, Taylor and Francis, Vol 1, pp. 1-27.
• Goldman Jennifer [et al.] Understanding how pharmacokinetic and pharmacodynamic differences of basal analog insulins
influence clinical practice [Journal]. - [s.l.] : Current Medical Research and Opinion, 2017. - 1473-4877.
• Sanofi-aventis Product Monograph Lantus [Online] // sanofi-aventis Canada Inc., . - sanofi-aventis Canada Inc., Oktober
19, 2017. - November 1, 2021. - https://pdf.hres.ca/dpd_pm/00041813.PDF.
• Gualandi, A. & Giorgi, G., 2001. Insulin Formulation Review. European Review for Medical and Pharmacological Sciences,
Volume 5, pp. 73-83.
• Hirsch, I., 2005. Drug Therapy: Insulin Analogues. The New England Journal of Medicine, Volume 352, pp. 174-183.
• Trujillo, J. & Haines, S., 2020. Diabetes Mellitus. In: J. Dipiro, G. Yee & L. Posey, eds. Pharmacotherapy: . United State: Mc
Graw Hill, pp. 7700-7727.
 DAFTAR PUSTAKA
Jonassen I, Havelund S, Hoeg-Jensen T, Steensgaard DB,Wahlund PO, Ribel U. Design of the novel protraction mechanism of insulin degludec, an ultra-long-acting
basal insulin. Pharm Res.2012;29:2104-2114.
Hanne dan Haise, 2014, A Review of the Pharmacological Properties of Insulin Degludec and Their Clinical Relevance, Clin Pharmacokinet, Vol. 53, pp. 787-800.
Heise, T dan Mathieu, C.2017. Impact of the mode of protraction of basal insulin therapies on their pharmacokinetic and pharmacodynamic properties and
resulting clinical outcomes. Diabetes, Obesity, Metabolism, 19(1), pp.3-12.
Jennifer G, Christoph , K Jeremy P, Tim H, 2017, Understanding how pharmacokinetic and pharmacodynamic differences of basal analog insulins influence clinical
practice, Taylor and Francis, Vol 1, pp. 1-27.
Jaronsinski, M, Dhayalan, B., Chen, Y.S., Chatterjee,D., Varas, N., Weiss, M.A.2021. Structural principles of insulin formulation and analog design :
A century of Inovation.Molecular Metabolism, Vol. 52, pp. 1-18
Donner, Thomas; Sarkar, Sudipa, 2019, Insulin Pharmacology therapeutic Regimens and Principles of Intensive Insulin Therapy,South Darmouth :
MDText.cim.Inc
American Diabetes Association. (2017). Pharmacologic approaches to glycemic treatment. Sec. 8. In Standards of Medical Care in Diabetes. ADA (American
Diabetes Asscociation): 40(Suppl. 1):S64–S74.
Cheng, Ran. Taleb, Nadine. Dubois-stainforth, Meggie. Lhoret-Rabasa, Remi. (2021). The Promising Future of Insulin Therapy in Diabetes Mellitus. American
Journal of Physiology Endocrinology and Metabolism 320: E886-E890.
Davis, Sondra. Friece, Chad. Roderman, Nicki. Newcomer, Darrel. Castaneda, Evangelina. (2017). Comparison of Insulin Detemir and Insulin Glargine for
Hospitalized Patients on a Basal-Bolus Protocol. MDPI Pharmacy.
King, Allen B. Poon, Kitty. (2010). Glargine and Detemir: Safety and Efficacy Profiles of the Long-acting Basal Insulin Analogs. Drug, Healthcare and Patient
Safety 2010:2 213-223: Dove medical Press Ltd.
Petznick, Allison. (2011). Insulin Management of Type 2 Diabetes Mellitus. American Academy of Family Physicians Volume 84, Number 2.