Overview of Semaglutide
Obesity is a key factor in the development and progression of type 2
diabetes mellitus, obesity is also associated with increase in cardiovascular
disease risks as well as uncontrolled diabetes.
Semaglutide
is an anti-diabetic drug of the class Glucagon-like peptide 1 analogue “GLP-1
analogues”, Semaglutide was approved for the treatment of type 2 diabetes mellitus, Semaglutide is also
associated with significant weight reduction and semaglutide now has been approved
by FDA for weight loss in diabetic patients.
Semaglutide drug class:
Glucagon-like peptide 1 analogue “ GLP-1
analogue”.
Semaglutide mechanism of action
Semaglutide is an analogue of glucagon-like peptide 1 and it provide its
actions by several different mechanisms such increasing insulin secretion from
beta cells of pancreas, reducing secretion of glucagon hormone form alpha cells
of pancreas and it’s also slows down gastric emptying rate (GER).
Semaglutide mechanism of weight reduction
It is believed that Semaglutide affects mainly the appetite of the patients who are taking it, it promote less appetite and reduces food cravings, thus decreasing the food intake.
Semaglutide therapeutic uses
Semaglutide is used concomitantly with exercise and diet for management
of type 2 diabetes mellitus, either as monotherapy when metformin is not
tolerated or in combination with other anti-diabetic drugs.
Semaglutide is now also approved by FDA for weight loss (reduction of
obesity).
The beneficial effects of semaglutide on cardiovascular and renal systems
The cardiovascular risks was significantly reduced with Semaglutide.
The risk of nephropathy associated with diabetes is significantly reduced in patients taking semaglutide.
Semaglutide pharmacokinetics
- The bioavailability of SC route is about 89% and peak plasma levels is reached with 1-3 days.
- The bioavailability of oral route is about 0.4-1% and peak plasma levels is reached with 1 hour.
- The estimated volume of distribution “ Vd” of Semaglutide is about 8 L for oral route and is about 12.5 L for SC route.
- Semaglutide is highly bounded to plasma proteins. It is bounded by more than 99% to albumin.
- Semaglutide is metabolized mainly by cleavage of the peptide backbone followed by beta oxidation of the fatty acid chain of the drug.
- The half-life of Semaglutide is about 7 days, this long half-life may be attributed to its high plasma protein binding.
- Semaglutide is primarily excreted in the urine and feces.
Semaglutide contraindications
- Semaglutide is contraindicated in patients with personal of family history of medullary thyroid carcinoma (MTC).
- Semaglutide is also contraindicated in patients with multiple endocrine neoplasia syndrome type 2.
- Semaglutide is contraindicated in patients with known hypersensitivity to it.
Semaglutide in pregnancy
- Semaglutide should be used only if the benefits outweigh the potential risks on the fetus.
- Semaglutide should be discontinued in women at least 2 months before planning to be pregnant.
Semaglutide in lactation
No available data shows that semaglutide is excreted in human milk, has
effects on breastfed infant or has effects on milk production.
Semaglutide adverse effects
The adverse effects of Semaglutide include loss of appetite, diarrhea or
constipation, abdominal pain, vomiting and nausea.
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