Peringatan Keamanan

An excess of insulin relative to food intake, energy expenditure, or both may lead to severe and sometimes prolonged and life-threatening hypoglycemia and hypokalemia see Warnings and Precautions (5.3, 5.6). Mild episodes of hypoglycemia usually can be treated with oral glucose.L42375 Lowering the insulin dosage, and adjustments in meal patterns, or exercise may be needed. More severe episodes with coma, seizure, or neurologic impairment may be treated with a glucagon product for emergency use or concentrated intravenous glucose.L42375 Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs and symptoms of hypoglycemia include difficulty concentrating, lethargy/weakness, confusion, drowsiness, vision changes, difficulty speaking, headache, and dizziness.L42375Individuals may become unconscious in severe cases of hypoglycemia. Injection site reactions may also occur. Symptoms include: redness, inflammation, bruising, swelling and itching at the injection site.L42375 After apparent clinical recovery from hypoglycemia, continued observation and additional carbohydrate intake may be necessary to avoid recurrence of hypoglycemia. Hypokalemia must be corrected appropriately.L42375

Insulin detemir

DB01307

biotech approved

Deskripsi

Insulin detemir is a long-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes.A2358, A2359, A2360, A44 Insulin is typically prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promotes glucose metabolism.A2358, A2359, A2360, A44 Insulin is released from the pancreas following a meal to promote the uptake of glucose from the blood into internal organs and tissues such as the liver, fat cells, and skeletal muscle.A2358, A2359, A2360, A44 The absorption of glucose into cells allows for its transformation into glycogen or fat for storage.A2358, A2359, A2360, A44 Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis among many other functions.A2358, A2359, A2360, A44

Insulin is an important treatment in the management of Type 1 Diabetes (T1D) which is caused by an autoimmune reaction that destroys the beta cells of the pancreas, resulting in the body not being able to produce or synthesize the insulin needed to manage circulating blood sugar levels.A2358, A2359, A2360, A44 As a result, people with T1D rely primarily on exogenous forms of insulin, such as insulin detemir, to lower glucose levels in the blood.A2358, A2359, A2360, A44 Insulin is also used in the treatment of Type 2 Diabetes (T2D), another form of diabetes mellitus that is a slowly progressing metabolic disorder caused by a combination of genetic and lifestyle factors that promote chronically elevated blood sugar levels.A2358, A2359, A2360, A44 Without treatment or improvement in non-pharmacological measures such as diet and exercise to lower blood glucose, high blood sugar eventually causes cellular resistance to endogenous insulin, and in the long term, damage to pancreatic islet cells.A2358, A2359, A2360, A44 Insulin is typically prescribed later in the course of T2D, after several oral medications such as DB00331, DB01120, or DB01261 have been tried, when sufficient damage has been caused to pancreatic cells that the body is no longer able to produce insulin on its own.A2358, A2359, A2360, A44

Marketed as the brand name product Levemir, insulin detemir has a duration of action of 16-24 hours allowing for once-daily dosing, typically at bedtime.A2358, A2359, A2360, A44 Due to its duration of action, Levemir is considered "basal insulin" as it provides low concentrations of background insulin that can keep blood sugar stable between meals or overnight.A2358, A2359, A2360, A44 Basal insulin is often combined with short-acting "bolus insulin" such as DB00046, DB01309, and DB01306 to provide higher doses of insulin required following meals.A2358, A2359, A2360, A44 Use of basal and bolus insulin together is intended to mimic the pancreas' production of endogenous insulin, with a goal of avoiding any periods of hypoglycemia.A2358, A2359, A2360, A44

Insulin detemir is produced using recombinant DNA technology in yeast cells.A2358, A2359, A2360, A44 This insulin analogue has a 14-C fatty acid, myristic acid, bound to the lysine amino acid at position B29. The myristoyl side chain increases self-association and albumin binding.A2358, A2359, A2360, A44 This along with slow systemic absorption from the injection site prolongs distribution of the hormone into tissues and results in a long duration of action. A2358, A2359, A2360, A44

Without an adequate supply of insulin to promote absorption of glucose from the bloodstream, blood sugar levels can climb to dangerously high levels and can result in symptoms such as fatigue, headache, blurred vision, and increased thirst.A2358, A2359, A2360, A44 If left untreated, the body starts to break down fat, instead of glucose, for energy which results in a build-up of ketone acids in the blood and a syndrome called ketoacidosis, which is a life-threatening medical emergency. In the long term, elevated blood sugar levels increase the risk of heart attack, stroke, and diabetic neuropathy.A2358, A2359, A2360, A44

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) After subcutaneous administration in patients with type 1 diabetes, insulin detemir has a terminal half-life of 5 to 7 hours depending on dose.[L42375]
Volume Distribusi Insulin detemir has an apparent volume of distribution of approximately 0.1 L/kg.[L42375]
Klirens (Clearance) The apparent clearance (CL/F) was fairly consistent among different patients population with type 1 diabetes. It was estimated to be 3.43 ± 1.36 L/min·kg in 6 to 12 years old patients, 3.74 ± 0.98 L/min·kg in 13 to 17 years old, and 3.41 ± 1.00 L/min·kg in adult patients (18-65 years old).[A43]

Absorpsi

After subcutaneous injection of LEVEMIR in healthy subjects and in patients with diabetes, insulin detemir serum concentrations had a relatively constant concentration/time profile over 24 hours with the maximum serum concentration (Cmax) reached between 6-8 hours post dose.L42375 When single dose of 0.5 units/kg of insulin detemir was given to adult type 1 diabetes patients, the maximum serum concentration (Cmax) was 4,641 ± 2,299 pmol/L.L42375,A43Insulin detemir was more slowly absorbed after subcutaneous administration to the thigh where AUC0-5h was 30 40% lower and AUC0-? was 10% lower than the corresponding AUCs with subcutaneous injections to the deltoid and abdominal regions.L42375 Insulin detemir has a slow and prolonged absorption and a relatively constant concentration/time profile over 24 hours with no pronounced peak. The median time to maximum serum insulin concentration was 12 hours after injection. On average, serum insulin concentrations declined to baseline by approximately 24 hours.L42375,A2358 The absolute bioavailability of insulin detemir is approximately 60%.L42375

Metabolisme

The liver and kidney play the major role in metabolizing insulin.A231654However, while the liver predominantly metabolizes endogenous insulin, exogenous insulin is primarily metabolized due to the kidney since it is not directly delivered into the portal system.A231654

Rute Eliminasi

30 to 80% of circulating insulin is removed by the kidney.A249935

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol may impair blood glucose control.
  • 2. Take with food. Once daily administration should be given with the evening meal or prior to bedtime.

Interaksi Obat

791 Data
Liraglutide Liraglutide may increase the hypoglycemic activities of Insulin detemir.
Metreleptin Metreleptin may increase the hypoglycemic activities of Insulin detemir.
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Insulin detemir.
Pioglitazone The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin detemir.
Pramlintide Pramlintide may increase the hypoglycemic activities of Insulin detemir.
Rosiglitazone The risk or severity of congestive heart failure can be increased when Insulin detemir is combined with Rosiglitazone.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Insulin detemir.
Edetic acid Edetic acid may increase the hypoglycemic activities of Insulin detemir.
Esmolol Esmolol may increase the hypoglycemic activities of Insulin detemir.
Landiolol Landiolol may increase the hypoglycemic activities of Insulin detemir.
Gatifloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Gatifloxacin.
Moxifloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Moxifloxacin.
Enoxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Insulin detemir can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Cinoxacin.
Norfloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Sparfloxacin.
Fleroxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Insulin detemir can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Insulin detemir can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Insulin detemir can be increased when used in combination with Pipemidic acid.
Grepafloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Grepafloxacin.
Lomefloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Lomefloxacin.
Temafloxacin The therapeutic efficacy of Insulin detemir can be increased when used in combination with Temafloxacin.
Methyclothiazide The risk or severity of hypoglycemia can be increased when Methyclothiazide is combined with Insulin detemir.
Chlorthalidone The risk or severity of hypoglycemia can be increased when Chlorthalidone is combined with Insulin detemir.
Bendroflumethiazide The risk or severity of hypoglycemia can be increased when Bendroflumethiazide is combined with Insulin detemir.
Metolazone The risk or severity of hypoglycemia can be increased when Metolazone is combined with Insulin detemir.
Benzthiazide The risk or severity of hypoglycemia can be increased when Benzthiazide is combined with Insulin detemir.
Hydroflumethiazide The risk or severity of hypoglycemia can be increased when Hydroflumethiazide is combined with Insulin detemir.
Indapamide The risk or severity of hypoglycemia can be increased when Indapamide is combined with Insulin detemir.
Chlorothiazide The risk or severity of hypoglycemia can be increased when Chlorothiazide is combined with Insulin detemir.
Hydrochlorothiazide The risk or severity of hypoglycemia can be increased when Hydrochlorothiazide is combined with Insulin detemir.
Trichlormethiazide The risk or severity of hypoglycemia can be increased when Trichlormethiazide is combined with Insulin detemir.
Polythiazide The risk or severity of hypoglycemia can be increased when Polythiazide is combined with Insulin detemir.
Quinethazone The risk or severity of hypoglycemia can be increased when Quinethazone is combined with Insulin detemir.
Cyclopenthiazide The risk or severity of hypoglycemia can be increased when Cyclopenthiazide is combined with Insulin detemir.
Epitizide The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Epitizide.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Insulin detemir.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Insulin detemir.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Insulin detemir.
Amineptine Amineptine may decrease the hypoglycemic activities of Insulin detemir.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Insulin detemir.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Insulin detemir.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Insulin detemir.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Insulin detemir.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Insulin detemir.
Opipramol Opipramol may decrease the hypoglycemic activities of Insulin detemir.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Insulin detemir.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Insulin detemir.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Insulin detemir.
Melitracen Melitracen may decrease the hypoglycemic activities of Insulin detemir.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Insulin detemir.
Iprindole Iprindole may decrease the hypoglycemic activities of Insulin detemir.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Insulin detemir.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Insulin detemir.
Imipramine Imipramine may decrease the hypoglycemic activities of Insulin detemir.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Insulin detemir.
Doxepin Doxepin may decrease the hypoglycemic activities of Insulin detemir.
Desipramine Desipramine may decrease the hypoglycemic activities of Insulin detemir.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Insulin detemir.
Dapagliflozin The risk or severity of hypoglycemia can be increased when Insulin detemir is combined with Dapagliflozin.
Canagliflozin The risk or severity of hypoglycemia can be increased when Insulin detemir is combined with Canagliflozin.
Leuprolide The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Goserelin.
Torasemide The risk or severity of hypoglycemia can be increased when Torasemide is combined with Insulin detemir.
Nelfinavir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Nelfinavir.
Indinavir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Indinavir.
Ziprasidone The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Ziprasidone.
Etonogestrel The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Etonogestrel.
Desogestrel The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Desogestrel.
Olanzapine The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Olanzapine.
Megestrol acetate The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Megestrol acetate.
Clozapine The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Clozapine.
Levonorgestrel The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Levonorgestrel.
Progesterone The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Progesterone.
Chlorpromazine The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Chlorpromazine.
Haloperidol The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Haloperidol.
Ritonavir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Ritonavir.
Piperazine The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Piperazine.
Medroxyprogesterone acetate The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Medroxyprogesterone acetate.

Target Protein

Insulin receptor INSR
Insulin-like growth factor 1 receptor IGF1R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17881328
    Kurtzhals P: Pharmacology of insulin detemir. Endocrinol Metab Clin North Am. 2007 Aug;36 Suppl 1:14-20.
  • PMID: 18034591
    Morales J: Defining the role of insulin detemir in Basal insulin therapy. Drugs. 2007;67(17):2557-84.
  • PMID: 17901036
    Tibaldi J: Actions of insulin beyond glycemic control: a perspective on insulin detemir. Adv Ther. 2007 Jul-Aug;24(4):868-82.
  • PMID: 14578244
    Danne T, Lupke K, Walte K, Von Schuetz W, Gall MA: Insulin detemir is characterized by a consistent pharmacokinetic profile across age-groups in children, adolescents, and adults with type 1 diabetes. Diabetes Care. 2003 Nov;26(11):3087-92.
  • PMID: 18715209
    Owens DR, Bolli GB: Beyond the era of NPH insulin--long-acting insulin analogs: chemistry, comparative pharmacology, and clinical application. Diabetes Technol Ther. 2008 Oct;10(5):333-49. doi: 10.1089/dia.2008.0023.
  • PMID: 25905175
    Donner T, Sarkar S: Insulin - Pharmacology, Therapeutic Regimens, and Principles of Intensive Insulin Therapy .
  • PMID: 22267935
    Morello CM: Pharmacokinetics and pharmacodynamics of insulin analogs in special populations with type 2 diabetes mellitus. Int J Gen Med. 2011;4:827-35. doi: 10.2147/IJGM.S26889. Epub 2011 Dec 12.
  • PMID: 29512653
    Scapin G, Dandey VP, Zhang Z, Prosise W, Hruza A, Kelly T, Mayhood T, Strickland C, Potter CS, Carragher B: Structure of the insulin receptor-insulin complex by single-particle cryo-EM analysis. Nature. 2018 Apr 5;556(7699):122-125. doi: 10.1038/nature26153. Epub 2018 Feb 28.
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Contoh Produk & Brand

Produk: 33 • International brands: 1
Produk
  • Levemir
    Implant • 14.2 mg/1mL • Soft tissue • US • Approved
  • Levemir
    Injection, solution • 14.2 mg/1mL • Subcutaneous • US • Approved
  • Levemir
    Injection • 14.2 mg/1mL • Subcutaneous • US • Approved
  • Levemir
    Injection • 14.2 mg/1mL • Subcutaneous • US • Approved
  • Levemir
    Injection, solution • 100 [iU]/1mL • Subcutaneous • US • Approved
  • Levemir
    Injection • 14.2 mg/1mL • Subcutaneous • US • Approved
  • Levemir
    Injection, solution • 100 [iU]/1mL • Subcutaneous • US • Approved
  • Levemir
    Injection, solution • 100 [iU]/1mL • Subcutaneous • US • Approved
Menampilkan 8 dari 33 produk.
International Brands
  • Levemir FlexPen — Novo Nordisk

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