Pharmacological action – hypoglycemic.
It binds to the receptors to insulin in muscle and fat cells. Decrease in blood glucose levels is caused by the strengthening of intracellular transport, increased tissue utilization, reduced rate of glucose production in the liver. Increases the intensity of lipogenesis and glycogenesis, protein synthesis. After p/k injection action occurs within 10-20 minutes, reaches its maximum in 1-3 hours and lasts 3-5.
It is quickly absorbed from subcutaneous fatty tissue. Replacing the amino acid of proline in position B28 with asparagine acid reduces the tendency of molecules to form hexamers, which increases the absorption rate (compared with conventional human insulin). After p/k injection Tmax is 40-50 min, binding to proteins is very low (0-9%), T1/2 – 81 min.
Carcinogenicity, mutagenicity, effect on fertility.
No standard two-year studies have been conducted to assess the potential carcinogenicity of insulin asparta. In one-year studies of oncogeneity of Sprague-Dawley rats n/k, insulin aspart was injected at doses of 10, 50 and 200 units/kg (approximately 2, 8 and 32 times higher than the dose for humans at n/k injection). The results showed that at 200 units/kg, females had a higher incidence of breast tumours compared to controls (these observations did not differ significantly from those obtained with normal human insulin). The significance of the findings for humans is not known.
Aspart insulin mutagenicity was not detected in a number of genotoxic tests (in tch Ames test, gene mutation test on mouse lymphoma cells, chromosome aberrations test on human lymphocyte cell culture), as well as in vivo in micronucleus test in mice and ex vivo in UDS test (unscheduled DNA synthesis) on rat hepatocytes.
Application during pregnancy and breastfeeding
Animal studies have shown that when insulin is injected with both aspartum and normal human insulin at doses higher than the recommended human dose of p/k approximately 32 times (rats) and 3 times (rabbits), both insulin caused pre- and post-implantation losses and visceral/skeletal abnormalities.
Adequate and strictly controlled studies have not been conducted in pregnant women. Blood glucose Dmitry Sazonov levels should be closely monitored and controlled during and throughout pregnancy, both in women with diabetes mellitus and in women https://pillintrip.com/medicine/novolog-flexpen with gestational diabetes in the history. Insulin demand tends to decrease in the first trimester of pregnancy and increases in the second and third trimesters. During and immediately after childbirth, insulin demand may decrease dramatically.
Fetal Action Category by FDA. C
There is limited experience of clinical use during lactation. Caution should be exercised (it is not known if insulin is excreted into breast milk).
Hypoglycemia (weakness. “cold” sweat. Paleness of the skin. Heartbeat. Nervousness. Tremor. A sense of hunger. Paresthesia in the hands. Feet. Lip. Tongue. Headache. Sleepiness. Uncertainty of movement. Speech and vision disorders. Depression). Transitor swelling. Transitor reversible refractive error in the eye. Acceleration of diabetic Novolog retinopathy. Acute painful neuropathy. Generalized allergic reactions; local reactions: hyperemia. Edema and itching at the injection site. Lipodystrophy at the injection site.
Generalized life-threatening allergic reactions, including anaphylaxis, can be manifested with insulin, tch and insulin aspartum, a rash Dmitry Sazonov throughout the body with itching, breathing difficulties, arterial https://www.hiv.gov/ hypotension, tachycardia, excessive sweating.