Tirzepatide MOUNJARO Mechanism precautions let us discuss one of the new topic, triphatite. How this drug acts, what are the important precautions, side effects, dosage, all these things we will discuss. Food is the important source of energy which is going to be converted into very small molecules, glucose.
These glucose levels, when they are within the limits, they supply the energy for daily activities. But when these glucose levels are excessively increased and they are out of control, we can observe elevated levels of glucose. But still in this condition, few of the mediators can act to control the glucose levels in healthy people. One of the important protein is the insulin which can control the glucose levels by increasing the glucose uptake into the cells as well as increase the glucose utilization.
Apart from the insulin, few of the other mediators can also control the glucose. Among them, one of the important mediator is the GLP1. Glycogone like peptide one. This peptide is structurally similar to glucogone, but it reduce the glucose levels by promoting the insulin secretion. This GLP1 can also control the glucose levels by various types of actions. Similarly, another mediator is the GIP.
Tirzepatide MOUNJARO Mechanism precautions
This is the glucose dependent insulinotropic polypeptide. This GIP can also control the glucose levels based on the elevated levels of glucose. So apart from insulin, GLP1 and GIP can also control the glucose. And these two mediators are well known as incretins. We have many of the antibiotic drugs which increase the insulin secretion, but one category of drugs are going to increase the actions of these incretins. So here we have one of the drug, trizopetide. This is one of the new anti diabetic agents that acts by dual action.
This drug can increase the activity of GLP 1 as well as GAP. So the actions of ingr itin’s are promoted by tripsetide, which is the new anti diabetic agent with proved activity on controlling the glucose levels in those patients with type 2 diabetes mellitus. On the pancreatic beta cells, GLP1 receptors are present as well as GLP 1 receptor receptors are present, as well as GLP receptor are expressed.
Now GLP 1 as well as GLP can act on their corresponding receptorsto increase the insulin secretion. These are the natural incretines which are controlling the excessive glucose levels. Now, titropeptide is one of the new anti diabetes case agentswhich can act as a gunist on these two receptors.
Thereby, it can increase the insulin secretion. That’s why this drug can be used in the treatment of type 2 diabetes mellitus. Along with diet control and proper exercise, this titropeptide can be used in the patients with type 2 diabetes mellitus. But at the same time, this drug is having few of the limitations. This drug is contraindicated in the patients with any history of pancreatitis. Even this drug is not suitable for the treatment of type 1 diabetes mellitus.
Now, let us the chemical nature of this drug. Trizopetide is one of the polypeptide made up of 39 amino acids. And within this structure, structural modifications are done in order to increase the bioavailability as well as decreased degradation within the body. In this polypeptide chain, at the 20th amino acid, lycin is going to be introduced. And this lycin is connected with a linker chain which is further attached with a C 20 fatty acid.
The linker is responsible for the flexibility of this polypeptide such that it is physiologically stable. And the C 20 fatty acid gives the long binding of this drug to the corresponding receptors, thereby, it produce long duration of action. This drug trizopetide can bind to serum albumin by which it is less metabolized and duration of action is further increased.
Similarly, the amino acids at the second position and 13th position are again replaced, and these amino acids are replaced with noncoding amino acids. So at the second and 13th position, alpha amino isobutic acid is introduced, which is a noncoding amino acid. Thereby, this polypeptide cannot be cleaved by DPP4 enzyme, dipeptidylpepidase 4 enzyme.
This enzyme is naturally cle the incretins like GLP1 and GIP. Even terzopetide acts as agonist on these receptors, but still it is not cleaved by DPP4 enzyme because of modification of amino acids at second and the 10th position. That’s why this drug is long acting as well as more stable, and it can stimulate the actions of both GLP1 as well as GIP. Thereby, it can increase the insulin secretion and control the glucose levels.
Now, let us see how this drug acts. Just we have a seen that tiger phthalate can act by several mechanisms. One of its primary action is on the pancreas. From the pancreas, this drug can promote the insulin secretion. Insulin can be released by two phases. Now, tiger phthalate can increase the first phase of the insulin secretion, as well as it can also increase the second phase of insulin secretion.
The first phase is the peak insulin secretion, which is observed within few minutes of intake of food. And after 30 minutes to 1 hour, the second phase of insulin secretion is going to be initiated, which is a basal insulin secretion. Now, titrate peptide can increase both first phase as well as second phase insulin secretion.
Thereby, it can control the elevation of post p randial glucose after a food intake. This drug can also act on the pancreas to reduce the glucagon secretion, by which again, it can control the glucose levels. Apart from this action on the pancreas, this drug can also produce delayed gastric emptying. Thereby, the glucose absorption is somewhat reduced. So post p randial glucose levels are reduced by triphatide.
Finally, this drug can also act on the appetite centers within the CNS. Thereby, it can reduce the appetite, leading to decreased food intake. By all of these actions, this drug can reduce the glucose levels as well as it can also reduce the appetite. Thereby, it can produce some weight loss. That’s why this drug may also reduce the body weight in the patients with obesity as well as diabetes. Now, on the phthalate beta cells, GLP1 receptors are expressed, which are G protein couple of receptor s coupled with alpha, beta, gamma subunits.
Similarly, GIP receptors are also expressed on these beta cells, which are again G protein couple receptors. Now, titrate appetite can act on both of these receptors. It can bind to GLP1 receptor as agonist, such that it can activate the adenylal cyclase system. This adenylal cyclate can convert the ATP into one of the important secondary messenger, CYCLA KMP.
Similarly, trigipitide can also act on the GIP receptors, which are the receptors for glucose dependent insulinotropic polypeptide, GIP. By activation of these receptors, again, it releases the CYCLA KMP, so both of these receptors can increase the cycle KMP levels within the beta cells, which then promotes the action of protein kinase A. Protein kinase A is a group of fast volatility enzymes which can control the different types of ion channels. One of the ion channels are ATP sensed to potassium channels.
And second one is voltage gated calcium channels. And third one is again, voltage gated sodium channels. The activity of all these channels is controlled by protein kinase A. It can inhibit the activity of ATP sensed to potassium channels so that potassium cannot go outside. Instead, it can activate the voltage gated calcium channels so that calcium can enter into the beta cells, leading to depolarization.
This protein kinase A can also activate the voltage gated sodium channels so that sodium ions are also entered, which finally results in the depolarization and release of the insulin from the beta cells. In this way, triphatide can activate both GLP1 receptors as well as GIP receptors. Thereby, it can promote the insulin secretion.
At the same time, it can reduce the glucagon secretion, and it can produce delayed gastric emptying, which resists in the decreased glucose absorption. Apart from these actions, it can also inhibit the appetite centers within the CNS. Thereby, it can control the appetite, resulting in the decreased food intake in the patients. Now, let us the precautions of this try.
With the use of tinger phthalate, the patient may observe some abdominal pain, which may be mild, but in some conditions, it may produce some severe abdominal pain which is frequent and persisting for longer periods. This severe abdominal pain may be associated with other symptoms like vomiting. In such conditions, any development of pancreatitis may be suspected in the patients. So if these symptoms are developed, then immediately test should be done to check any development of pancreatitis as trizopetriate can increase the risk of pancreatitis.
In such conditions, this drug should not be used to reduce the further complications with pancreatitis. Second important precaution is that this drug can increase the other.
