tresibafill

tresibafill Uses, Dosage, Side Effects, Food Interaction and all others data.

The primary activity of insulin, including tresibafill, is regulation of glucose metabolism. Insulin and its analogues lower blood glucose by stimulating peripheral glucose uptake, especially by skeletal muscle and fat, and by inhibiting hepatic glucose production. Insulin also inhibits lipolysis and proteolysis, and enhances protein synthesis. tresibafill forms multihexamers when injected into the subcutaneous tissue resulting in a subcutaneous insulin degludec depot. The protracted time action profile of tresibafill is predominantly due to delayed absorption of insulin degludec from the subcutaneous tissue to the systemic circulation and to a lesser extent due to binding of insulin degludec to circulating albumin.

Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, the pancreas produces a continuous supply of low levels of basal insulin along with spikes of insulin following meals. Increased insulin secretion following meals is responsible for the metabolic changes that occur as the body transitions from a postabsorptive to absorptive state. Insulin promotes cellular uptake of glucose, particularly in muscle and adipose tissues, promotes energy storage via glycogenesis, opposes catabolism of energy stores, increases DNA replication and protein synthesis by stimulating amino acid uptake by the liver, muscle and adipose tissue, and modifies the activity of numerous enzymes involved in glycogen synthesis and glycolysis. Insulin also promotes growth and is required for the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis). Insulin detemir is a long-acting insulin analogue with a flat and predictable action profile. It is used to mimic the basal levels of insulin in diabetic individuals. The onset of action of insulin detemir is 1 to 2 hours and its duration of action is up to 24 hours. Interestingly, it has a lower affinity (30%) for the insulin receptor than human insulin.

tresibafill
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	tresibafill
Generic	Insulin Degludec
Insulin Degludec Other Names	Insulin degludec, Insulina degludec
Weight	100iu/ml
Type	Solution
Formula	C₂₇₄H₄₁₁N₆₅O₈₁S₆
Weight	6103.97 Da
Protein binding	The affinity of insulin degludec to serum albumin corresponds to a plasma protein binding of >99% in human plasma. The results of the in vitro protein binding studies demonstrate that there is no clinically relevant interaction between insulin degludec and other protein bound drugs.
Groups	Approved
Therapeutic Class	Long Acting Insulin
Manufacturer	Novo Nordisk
Available Country	Saudi Arabia
Last Updated:	September 19, 2023 at 7:00 am

Uses

tresibafill is used for once-daily treatment of adults with diabetes mellitus to improve glycemic control. tresibafill is not recommended for the treatment of diabetic ketoacidosis.

tresibafill is also used to associated treatment for these conditions: Diabetes Mellitus, Type 1 Diabetes Mellitus, Type 2 Diabetes Mellitus

How tresibafill works

Insulin detemir binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor autophosphorylates and phosphorylates numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. Activation of these proteins leads to the activation of downstream signalling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC), both of which play critical roles in metabolism and catabolism.

Dosage

tresibafill dosage

tresibafill is ultra long-acting basal insulin for once-daily at any time of the day, preferably at the same time every day.

Patients with type 2 diabetes mellitus: The recommended daily starting dose is 10 units followed by individual dosage adjustments.

Patients with type 1 diabetes mellitus: tresibafill is to be used once-daily with meal-time insulin and requires subsequent individual dosage adjustments.

In patients with type 2 diabetes mellitus,tresibafill can be administered alone or in any combination with oral anti-diabetic medicinal products, GLP-1 receptor agonists and bolus insulin. In type 1 diabetes mellitus, tresibafill must be combined with short-/rapid-acting insulin to cover mealtime insulin requirements. On occasions when administration at the same time of the day is not possible, tresibafill allows for flexibility in the timing of insulin administration. A minimum of 8 hours between injections should always be ensured. Patients who forget a dose, are advised to take it upon discovery and then resume their usual once-daily dosing schedule.

Side Effects

Nasopharyngitis, Severe hypoglycemic episode, Upper respiratory tract infection, Headache, Diarrhea, Sinusitis, Gastroenteritis, Injection site reactions, Peripheral edema

Toxicity

Observe for signs and symptoms of hypoglycemia, hypokalemia, and fluid retention and heart failure with concomitant use of Thiazolidinediones. Pregnancy Category C

Precaution

tresibafills must not be injected into a vein (intravenously) or a muscle (intramuscularly) and must not be used in infusion pumps.

There is no experience with tresibafill in children and adolescents under 18 years of age.

Interaction

Decreased hypoglycaemic effect with corticosteroids, danazol, diazoxide, diuretics, glucagon, isoniazid, phenothiazine derivatives, somatropin, sympathomimetic agents, thyroid hormones, oestrogens, progestins (e.g. in oral contraceptives), protease inhibitors and atypical antipsychotic (e.g. olanzapine and clozapine). Increased hypoglycaemic effect with oral antidiabetic agents, ACE inhibitors, disopyramide, fibrates, fluoxetine, MAOIs, pentoxifylline, propoxyphene, salicylates and sulfonamide antibiotics. Decreased insulin resistance with octreotide and lanreotide. Increased risk of wt gain and peripheral oedema with pioglitazone, rosiglitazone. Decreased effect of sermorelin.

Food Interaction

Avoid alcohol. Alcohol may impair blood glucose control.

Elimination Route

In patients with type 1 diabetes, after 8 days of once daily subcutaneous dosing with 0.4 U/kg, maximum degludec concentrations of 4472 pmol/L were attained at a median of 9 hours (tmax). After the first dose of, median onset of appearance was around one hour. The glucose lowering effect lasted at least 42 hours after the last of 8 once-daily injections. Insulin degludec concentration reach steady state levels after 3-4 days.

Half Life

The half-life after subcutaneous administration is determined primarily by the rate of absorption from the subcutaneous tissue. On average, the half-life at steady state is approximately 25 hours independent of dose.

Clearance

The mean apparent clearance of insulin degludec is 0.03 L/kg (2.1 L/h in 70 kg individual) after single subcutaneous dose of 0.4 units/kg.

Pregnancy & Breastfeeding use

Pregnant Women: There is no clinical experience from well-controlled studies with Insulin degludec in pregnant women. Animal reproduction studies have not revealed any differences between insulin degludec and human insulin regarding embryotoxicity and teratogenicity. Animal reproduction studies are not always predictive of human response; therefore, Insulin degludec should not be used during pregnancy unless the potential benefits to the mother justify the potential risks to the fetus

Nursing Women: There is no clinical experience from well controlled studies with Insulin degludec during breast-feeding. It is unknown whether insulin degludec is excreted in human milk. In rats, insulin degludec was secreted in milk; the concentration in milk was lower than in plasma.