Oral antidiabetic drugs are classified into several classes based on their mechanism of action: (1) Sulfonylureas (first generation: tolbutamide, chlorpropamide; second generation: glibenclamide, glimepiride, glipizide) and meglitinides (repaglinide, nateglinide) block ATP-sensitive potassium channels in pancreatic beta cells to increase insulin secretion, with adverse effects including hypoglycemia and cholestatic jaundice; (2) DPP4 inhibitors (gliptin class: sitagliptin, saxagliptin, vildagliptin, linagliptin) increase insulin secretion and decrease glucagon levels; (3) Biguanides (metformin) decrease hepatic gluconeogenesis and increase insulin sensitivity without stimulating insulin secretion, with adverse effects including diarrhea, metallic taste, and lactic acidosis; (4) Thiazolidinediones (PPAR gamma agonists: rosiglitazone, pioglitazone) increase insulin sensitivity at the receptor level, causing weight gain and edema; (5) Alpha-glucosidase inhibitors (acarbose, voglibose, miglitol) decrease glucose absorption in the intestine, causing diarrhea and flatulence; (6) SGLT2 inhibitors (dapagliflozin, canagliflozin, empagliflozin) increase glucose excretion through urine, causing urinary tract infections; (7) GLP-1 analogs (exenatide) decrease glucagon release and delay gastric emptying, causing weight loss and nausea.
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D- 331 | Oral Antidiabetic Drugs - Pharmacology | Rapid revision notes #PharmacologyAdded:
Hello DI Students Welcome back to the GDC Classes. So DI students, welcome all of you once again to GDC's YouTube channel. And today in this digestive series we are going to talk about the mechanism of action and adverse effects of the oral anti-diabetic drug or we can say oral hypoglycemic agent.
Listen to me very carefully, children. The classification of these oral hypoglycemic agents, their mechanism of action, and their basic adverse effects are very, very, very important. Because you always get to see questions from them. So please don't take it lightly. So we have already read the classification many times. Today it is the turn of its mechanism. So first of all, if we talk about our oral hypoglycemic agents, we divide them into different classes.
See why diabetes occurs? Because the secretion of insulin either decreases which we call insulin dependent diabetes mellitus. Or insulin is being secreted but that insulin is not able to bind to its receptor.
Resistance is happening. So there we call it non-insulin dependent diabetes mellitus. And for these, our drugs come in different classes.
So our first class is the drugs which enhance the insulin secretion. That is, which increases the secretion of insulin.
Now our drugs that increase insulin secretion fall into three classes.
First are sulfonyl ureas which block ATP sensitive potassium channels. It comes in two classes which we call first generation and second generation.
In the first generation, tolbutamide, chloropropamide, in the second generation, glibenclamide, glimepiride, glizide, glipizide, all these drugs come in sulfonyl form. Then there's another class that is called the meglitinide class of drugs. And these meglitinide class drugs also inhibit our ATP sensitive potassium channels.
And this includes two of our drugs.
In Megletinide, we call Repaglinide and Nataglenide as Megletinide. And next comes DPP4 inhibitor i.e. dipeptidyl peptidase 4 enzyme inhibitor where gliptin class drugs come.
Sitagliptin Saxagliptin Weldagliptin Lena Gagliptin All drugs belong to the gliptin class. Then comes the second class which does not increase the secretion of insulin but increases the sensitivity of insulin, in which our biguanides, activators of AMP, come, metformin, phenformin and the second one comes thiazolidine diagonase derivatives which are PP AR i.e. peroxisome proliferated activator receptor gamma agonists, where we talk about drinking a little bit every day, i.e. rosiglitazone, pioglitazone. Then we have some other classes. Like we talk about reducing glucose absorption, that is, our absorption should not happen at all, where alpha glucosidase inhibitor is used, where we talk about accarose voglivoz miglitol.
Then sir, the glucose should be excreted out through urine, that is, it should not be reabsorbed, that is called the sodium glucose to transporter inhibitor dapagliflozin canagliflozin empagliflozin, all these are our drugs.
Similarly, we also have a glucagon like peptide i.e. GLP one analog exenatide.
What are all these drugs that we have? It belongs to the oral hypoglycemic agent class of drugs.
Now this is not your question today's digester. Today's digest is what is their mechanism of action? For example, if we talk about it, the first class that comes to our mind is Sulfonyl Urea. We talked about how it works? Sir, it increases the release of insulin and how does it do so? Because it blocks ATP sensitive potassium channels.
Last year, this question was also seen in AIIMS. Apart from that, we talked about it increasing the release of insulin. Yes sir. And what will happen if you increase the release of insulin? Sir, if insulin increases then obviously its action will increase by binding to its receptor.
This will increase tissue sensitivity.
But if we talk about adverse effects, if there is more secretion then there will be hypoglycemia, cholestatic jaundice and yes disulfiram like action, especially in chlorpropamide we will see disulfiram like action, so remember this does not happen in everyone but in the chlorpropamide that we come with, disulfiram like action is seen.
Our second class is Meglitinide. This is also an ATP sensitive potassium channel blocker. Repaglinide and nateglenide. It also increases the release of insulin from pancreatic beta cells. And their adverse effect is also hypoglycemia.
Class III glucagon-like peptides, where we talked about exenatide, and this will be about exenatide.
What is their work? Decreases glucagon release. Because it is a glucagon like peptide. Now that glucagon is already in the blood, glucagon will not be released.
So it delays the gastric emptying and decreases the peptide, which will reduce our hunger and reduce the glucose in our body.
But the adverse effect will be weight loss because you will feel less hungry. Vomiting, diarrhea, nausea, as well as hemorrhagic pancreatitis may occur with the GLP1 analog ecanatide. If we talk here about our dipeptyl peptidase 4 inhibitor i.e. DPP 4 inhibitor, in which we talked about gliptin class drugs, these also increase the secretion of insulin. Decreases glucagon levels and also reduces aptite. So wait, the same adverse effect will occur in this, sir.
Headache, allergy and increased incidence of UTI will be discussed. Next we talk about our bigvanoid. Well, it is a non-drug. It is used a lot. Metformin, especially phenformin, has been reduced in use due to its potential for lactic acidosis. has been discontinued. But metformin is very useful. What does she do? Does it increase insulin secretion? No sir. Then what does she do? Decreases hepatic gluconeogenesis. That means it will not allow glucose to increase in the blood. That means if it reduces blood glucose, it will increase glycogenesis. It will also increase our glycolysis.
Decreases glycogenolysis, decreases gluconeogenesis.
All of this is done by our AMP activator, the biguanide metformin. Now if we talk about its adverse effect, then yes sir, it has an adverse effect that what does it do to us? Sir, it helps in weight loss and we remember it by the name of Most. That is, metformin is given to obese patients and sulfonyl urea is given to thin patients. So sir, its major adverse effects will be diarrhea, metallic taste and lactic acidosis.
Next we'll talk about thiazodiine diazepam, which are PPAR gamma agonists.
So this is a PPR gamma agonist. It also decreases hepatic gluconeogenesis and increases insulin sensitivity at the receptor. Its adverse effect will also be weight gain. Sir, there is edema, CCF, risk of hepatotoxicity, these will be its major adverse effects.
What other classes do we have? Sir, we said alpha glucoside is an inhibitor. The boss never gives a toll. So decreases glucose absorption. Now if glucose absorption decreases then can you tell me further sir what will happen? Yes sir, it can be diarrhea.
Abdominal distension may occur.
Flotulence gas can be formed here with the alpha glucosidase inhibitor. Amlin analog comes in Pramylinite, nausea, vomiting, anorexia, especially anorexia. Its major adverse effect is what it does, it reduces the release of glucagon, reduces gastric emptying, delays and decreases peptide.
Next, it is a sodium glucose transporter inhibitor. Its major adverse effect is that what it does in urine is it sends glucose for urination, due to which UTI is a major reason for this and urine frequency also increases.
Inhibits sodium to glucose transporter in kidney increase glucose excretion. Will increase the excretion of glucose. These are our major oral hypoglycemic agents and their mechanisms as well as adverse effects we have seen here. So now let us see which questions have come from these topics.
First, the mechanism of action of the accaro. What do carbs do?
Inhibits the alpha glucosidase enzyme, preventing glucose absorption.
So alpha glucosidase inhibitor yahan pe b answer aayega alpha glucosidase inhibitor.
Which one of these is not insulin secretagogues Which drug does not cause insulin secretion. Now what you just saw sir is our sulfonyl urea, meglitinide, DPP4 inhibitor. All these increase the secretion of insulin.
Now here you have Repaglinide, Nataglinide and here we have Sulfonyl Urea but Sir, what is our Miglitol Sir? It is an alpha glucosidase inhibitor. Will this increase insulin secretion?
No sir, in one line. Choose the pair of PPR gamma receptor agonists. And we said PPR gamma receptor, drink a little bit every day, that is, daily glitazone and PO glitazone, what are these two of ours?
Biguanite is a class of drug. What do these two have to do with us? It is a sulfonylurea class drug. And what are these two of ours?
Alpha glucosidase inhibitors are class of drugs. The next question is one of the following does not belong to the category of DPP4 inbiter?
Look gliptin gliptin gliptin are all DPP four inhibitors. But repaglinide nateglinide is our meglitinide class drug. This is not a DPP four-inbiter. Which of the following is peroxisomal proliferated activated receptor gamma agonist i.e. PPR gamma agonist i.e. meglitinide. Here we will talk about thiazolidine dienes. Where the answer to rosiglitazone and pioglitazone will come. SGLT to work by V mechanism what do they do? Sodium inhibits the glucose transporter. Drug transport without a stimulation of insulin secretion from the pancreatic facilitates active transport of glucose into the bloodstream? No sir first take transportation to inbit. Written in salt but you will get it by meaning elimination.
What is the mechanism of action of the sulfonyl urea? Now what is the mechanism of action of sulfonyl urea? Sulfonyl urea is so sir will block ATP sensitive potassium channels.
Increases insulin sensitivity Stimulates insulin release by closing the ATP sensitive potassium channel in the beta cell Does not reduce perfect glucose absorption Does not reduce gluconeogenesis from GIT Sir, our answer will come here Insulin secretagogue consist of Right now we have said the same thing again and again It is sulfonyl urea It is meglitinide It is biguanide It will not come Sir It increases insulin sensitivity not secretion Aminoglycoside has no role here and sulfonyl urea is fine. Bignide will not come here. So our correct answer will come. Which among the following statements is correct with respect to their mechanism of anti- diabetic action? Antidiabetic action: Dapagliflozin, canagliflozin, sodium glucose transporter inhibitor.
Glipizide Glilazite DPP For Inhibitor There should be gliptin. Linagliptin Albogliptin Activator of AMP is wrong sir. This is our DPP four inbiter. Ekbose Voglibose ATP Sensitive Potassium Channel Only our first combination is going right.
Everything else is wrong. Which among the following statements is correct with respect to their mechanism of action? Let me tell you.
Sitaglipine Vitagliptin is a DPP4 inhibitor. Yes sir. Dapagliflozin is not an activator of canagliflozin AMP.
Glibenclamide Glimepiride Not a glucosidase inhibitor. Both the cars in the form of a car are not of the same class. So we will get only our first answer. The story of DPP4 Inbiter will come. Which antidiabetics work through the amplification of the incretin pathway.
And glucagon-like peptide is responsible for working through the incretin pathway.
We will talk about Acnatide. Metformin acts by two mechanisms. How does metformin work? So increases insulin secretion not metformin secretion sir.
Inhibiting alpha glucosidase decreasing hepatic glucose production. Increasing insulin action in the muscles and fat i.e. R and S. Please mark your answer as P and Q are wrong. Which of the following drugs is an alpha glucosidase inhibitor? So Bose never pays toll. We'll find alpha glucosidase inhibitors. The following drug increases insulin secretion? When it comes to insulin secretion, sulfonyl urea will be the most perfect answer. It blocks our ATP-sensitive potassium channels and causes insulin secretion.
Ok? So next question. Biguanide acts by the following mechanism except Biguanide increases glycolysis Increases insulin release from the pancreas Decreases gluconeogenesis Increases insulin binding to its receptor Perfect hai yeh jyank yahan pe sulfonyl urea kaam karti baaki nahi An anti diabetic drug pioglitazone used in type 2 diabetes acts by which me kaam karengi sir PPR gamma means it will increase the sensitivity of insulin Decreases uptake will not inhibit intestinal glucosidase sir Stimulating insulin secretion will increase the sensitivity. A 50-year-old obese patient with type 2 diabetes mellitus and a history of alcoholism probably should not receive metformin because it can increase the risk of lactic acidosis.
Because our Bignite contains Phenformin which causes the most lactic acidosis.
But metformin also has a little mechanism of action of pioglitazone acts as an agonist to the nuclear receptor called pioglitazone where sir? Peroxisome proliferated activated receptor gamma agonist will come. Which of the following is a sodium glucose transporter inhibitor? It is a gliflozin class of drug. So our answer is the same. What is metformin sir? It is a biguanide class drug. We will get this answer.
So here are our previously asked questions from the topic that is the mechanism of action and adverse effects of the oral anti-diabetic drug. and The Oral Hypoglycemic Agent from We Can. How did you like this digest? How is our hard work looking? Please give your love and comments on this video. We'll see you in the next video with some new and fun content. Till then keep learning with the JDC.
Thank you so much to all.
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