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Sulfonylureas compounds Sulfonylureas.. Alert secretion of insulin from the beta cells in the pancreas

Sulfonylureas compounds Sulfonylureas

These medicines have been discovered by accident after it was noted that sulfa drugs antibacterial which has been used to treat typhoid caused a drop in blood sugar in patients. After that was the construction of several sulfonylureas drugs by changing the chemical form of the sulfa drug and these drugs are still used to this day. The first two drugs are used to treat patients with type II diabetes Altolbyautamad and Alklorbrupamid.

Common to all vehicles sulfonylureas either first-or second-generation building on the same basic chemical compounds sulfa, and therefore the patients who may suffer from allergic to sulfa drugs will have the same degree of sensitivity for compounds sulfonylureas.

These drugs are taken by mouth and have the ability to alert the secretion of insulin from the beta cells in the pancreas. For good control of blood sugar it is necessary to take these medicines before eating the duration of 20-30 minutes. Most patients can be dealt drugs sulfonylureas for 7-10 years before they lose their effectiveness. And give those drugs with a small amount of insulin or with other medications such as sugar-lowering metformin or vehicles Althiazouliden debt can prolong the duration of effect. In fact there are currently a mixture of Algelebjurajd with metformin in a single disc has proved its effectiveness. Has been encouraged by the study worked in 2000 on patients with severe diabetes of the second type, where showed that study that giving insulin with Alklorbrupamid or Algelebeizaid (two different types of drugs sulfonylureas) led to control well in the level of sugar in the blood compared to use long to insulin alone.

The compounds are classified sulfonylureas into two main groups according to stages of development and effectiveness:

The first generation First Generation

The drugs include first generation Altolbyautamad, and Alklorbrupamid, and Alosatohecsamed, and Altollazamed.

Second generation Second Generation

Include second-generation drugs Aljlaepioarad, Algelebeizaid, and Algelimbraad. These medicines have been constructed after about twenty-five years of construction and use of drugs The first generation Of sulfonylureas. It works Drugs with the same mechanism of action of first-generation drugs, but more effective doses less may be a lot of inaccuracies in the union with receptors on the various members of the body, compared with the first generation of drugs sulfonylureas.

Mechanism of action of drugs sulfonylureas

Working sulfonylureas drugs whether first-or second-generation mainly by altering the secretion of insulin from the beta cells in the pancreas. Thus, these drugs have no place in the treatment of patients with type I diabetes, or diabetics who rely on insulin treatment. For this to work successfully it is necessary medicines and there is about 30% of the beta cells in a healthy state.

Consequently, those drugs are useful in the early stages of infection type II diabetes. In order to operate drugs sulfonylureas well it's best to use at the same time every day. And can be used with metformin or with drugs debt Althiazouliden.

And the short-acting drugs such as Aljlaepjurajd Algelebeizaid usually taken twice a day, Before breakfast and dinner.

The drugs are effective long can be taken once a day, either before dinner when noting the high level of sugar in the blood when bedtime or before breakfast when there is good care to control the blood sugar level throughout the day so be sure of the safety of daily dose.

And all drugs sulfonylureas whether first-or second-generation work the same way to reduce the level of sugar in the blood. Although the mechanism of action of these drugs is not known precisely.

Does sulfonylureas reduce insulin resistance?

Prolonged sulfonylurea administration decreases insulin resistance and increases insulin secretion in non-insulin-dependent diabetes mellitus: evidence for improved insulin action at a postreceptor site in hepatic as well as extrahepatic tissues. Diabetes Care. 1984 May-Jun;7 Suppl 1:89-99.

What mechanism stimulates the release of insulin from pancreatic beta cells?

Insulin is secreted by the β-cells of the pancreatic islets of Langerhans in response to elevation of the intracellular Ca2+ concentration ([Ca2+]i). This is produced by an influx of extracellular Ca2+ via voltage-dependent Ca2+ channels, whose activity, in turn, is regulated by the β-cell membrane potential.

What is the mechanism of Sulphonylurea?

Mechanism of action

Sulfonylureas bind to and close ATP-sensitive K+ (KATP) channels on the cell membrane of pancreatic beta cells, which depolarizes the cell by preventing potassium from exiting. This depolarization opens voltage-gated Ca2+ channels.

How does sulfonylurea stimulate insulin secretion?

Sulfonylureas are widely used to treat type 2 diabetes because they stimulate insulin secretion from pancreatic β-cells. They primarily act by binding to the SUR subunit of the ATP-sensitive potassium (KATP) channel and inducing channel closure.

What is the mechanism of action of sulfonylureas drugs in lowering blood glucose levels?

Sulfonylureas and meglitinides directly stimulate release of insulin from pancreatic beta cells and thereby lower blood glucose concentrations. Because they work by stimulating insulin secretion, they are useful only in patients with some beta cell function. Adverse effects may include weight gain and hypoglycemia.

Use drugs sulfonylureas with insulin

Sulfonylureas drugs as we not only stimulate the secretion of insulin from the beta cells, but also increases the sensitivity of peripheral tissue response to insulin. And therefore the use of these drugs will reduce the total dose of insulin needed to control high blood sugar level. At present, the available information to give those drugs with insulin still limited with regard to the total cost of material in the event description sulfonylureas drugs with insulin for patients with type II diabetes. In any case, patients who do not respond to more than 100 units per day of insulin, it may prefer to give each of the drugs sulfonylureas with insulin rather than continuing to increase the total dose of insulin.

How do sulfonylureas increase insulin sensitivity?

Do sulfonylureas improve insulin sensitivity?

Hypoglycemia is a major clinical concern with the use of sulfonylureas. Also, improving insulin sensitivity is a primary objective for the prevention and treatment of diabetes due to the rise in prevalence of obesity which is associated with insulin resistance. Sulfonylureas do not improve insulin sensitivity.

Can sulfonylureas be used with insulin?

Combining insulin and sulfonylurea is usually not endorsed, as they have similar mechanisms of action (providing more insulin), and the same glucose-lowering effect can usually be achieved with a modestly higher dose of insulin alone.

Which drug increases the tissue sensitivity to insulin?

Rosiglitazone is an insulin sensitizer with a major effect in stimulating glucose uptake in skeletal muscle and adipose tissue. It lowers plasma insulin levels. Rosiglitazone is used for treatment of type 2 diabetes associated with insulin resistance and may benefit polycystic ovary syndrome (PCOS) patients.

Which classification of oral hypoglycemic drugs decreases hepatic glucose production and increases insulin sensitivity and peripheral glucose uptake?

Pioglitazone–Actos. Pioglitazone is an oral antidiabetic agent that decreases insulin resistance in adipose tissue, liver and muscles which action is mediated by its link to PPAR-γ, which improves insulin sensitivity, decreases hepatic glucose production, and increases glucose uptake in the peripheral tissues.

What is the function of sulfonylureas?

What medications are sulfonylureas?

Sulfonylureas are oral medications that help lower blood sugar (glucose) levels in people living with Type 2 diabetes. All sulfonylureas are available in generic versions, making them relatively affordable. They include medications like glipizide, glimepiride, and glyburide.

Effectiveness and safety of drugs sulfonylureas.. Possible increased risk of death due to heart disease as a result of the use of these drugs

A report issued by the university group sugar program (University Group Diabetes Program) In 1970 to increase the number of deaths due to heart disease in diabetics who are treated with a drug Altolbyautamad compared with those patients who were treated by injecting insulin.

There is still a contradiction to this day about the validity of this conclusion due to the presence of notes on how to design the study.

Thus, the relationship between the death of patients resulting from heart disease and drugs sulfonylureas did not prove clear and strong evidence.

For this reason, the sulfonylureas drugs still to this day are widely used for the treatment of patients with type II diabetes.

However in 1984 committed the Department of Nutrition and Drug Administration (FDA) Manufacturers of drugs sulfonylureas should be written warning about the possibility of increased risk of death due to heart disease as a result of the use of these drugs.

Contraindications drugs sulfonylureas.. Of type I diabetes. Failure and liver and kidney function. Allergic to sulfa compounds

** Patients with type I diabetes.

* Patients who suffer from failure and liver and kidney function.

** Allergies to sulfa compounds.

* Not recommended to use these drugs in nursing women or during pregnancy. And do not use these drugs during pregnancy not only because of these medications may cause birth defects of the embryos, but may not lead to a reduction in the level of sugar in the blood is the desired shape in pregnant women.In addition, these drugs can pass through the placenta.

This has caused a sharp drop in blood sugar when the fetus. And usually uses insulin to control the level of sugar in the blood during pregnancy being a naturally occurring hormone and safe and does not cause a congenital malformations of the fetus.

* Patients who suffer from severe pressure.

Failure sulfonylureas drugs and the lack of response from the body.. Shortcomings in the response to the beta cells in the pancreas

Sulfonylureas drugs failed to continue to maintain a good response to these drugs at the beginning of use is one of the evils Sulfonylureas drugs in the treatment of type II diabetes. Although the inability to hold the attendance diet may be responsible for many cases, it is likely that the use of multiple doses, which yields high levels of drugs long-acting sulfonylureas may result in failure to respond beta cells in the pancreas.

Gelebjurajd	Gelebeizaid	Gelimbraad
Absorption Metabolism Metabolic products Half-life (hours) Effect (hours) Output Borders dose (mg) The number of doses / day	Good Yes Effective weak Less than 3 12-24 Urine and bile 2.5-20 1	Good Yes Ineffective 2-4 10-16 Urine 2.5-40 1-2	Good Yes Ineffective 5-9 12-24 Urine 1-8 1

Mechanism of action of drugs sulfonylureas.. Alert secretion of insulin from the beta cells in the pancreas

This is the basis for the mechanism of action of all drugs sulfonylureas. And be alert insulin secretion from beta cells by the union of these drugs with future T. beta cells. The union of these drugs in this way prevents potassium ions exit through the channels and result in the demise of polarization depolarization .This in turn opens calcium channels and lead to calcium entry and exit of insulin ready within cells. And confirms the validity of this theory that these drugs is not effective in patients who lack the presence of insulin, or even animals that have been the destruction of beta cells using chemical Alluxan alloxan .

Mechanism of action of drugs sulfonylureas.. Reducing the concentration of glucagon Glucagon In the blood

Use drugs sulfonylureas in the long term in patients with type II diabetes leads to reduced levels T. glucagon in the blood, This may contribute to lower blood sugar by these drugs. The mechanism of action of these drugs To reduce glucagon levels are not entirely clear, but may be due to an indirect effect by increasing the start of both insulin and somatostatin somatostatin And who in turn يثبطون secretion of a cell (A cells ) In the pancreas. In the absence of beta cells, as is the case for patients with type I diabetes, as well as updated in experimental animals have sugar using AlstrepettosasanStreptozacin , The sulfonylureas drugs in fact lead to a slight increase in the secretion of glucagon.

Mechanism of action of drugs sulfonylureas.. Increase the effect of insulin on the tissue

Characterized patients with type II diabetes low number of insulin receptors, which may explain the weakness of the effect of insulin in these patients or what is called insulin resistance. And there are studies that suggest that chronic use of these drugs increases the correlation with insulin receptor tissue by increasing the number of receptors on the walls of the cells of the liver, and therefore increases the effectiveness of insulin released from the beta cells in these patients or insulin given by injection. In any case, the mechanism has not been proven correct after as giving drugs sulfonylureas in patients with type I diabetes and who do not have insulin, this did not improve the level of sugar in their blood, and also did not lead these drugs to increase the effectiveness of insulin given by injection, or increase the number of receptors that are associated with insulin.

Possible side effects of the drugs sulfonylureas.. Sharp drop in blood sugar. Overweight. Blood poisoning. Reservation of water in the body

Is usually possible sulfonylureas drugs by patients well. Side effects include:

** Sharp drop in blood sugar.

Although the drugs sulfonylureas less serious than insulin in causing the sharp drop in blood sugar but that the sharp drop in blood sugar resulting from drugs sulfonylureas may be long and at the same time may pose a risk to the patient. And when you start using drugs sulfonylureas, the risk of a decline in the level of sugar in the blood is greater during the first few days and even the first four months of use. And therefore it should be emphasized to the patient should be drawn to the blood sugar level during this period.

And also must make sure that the level of sugar in the blood continuously when practicing sports and increased activity or in the case of not taking the meal. And must be alert and to emphasize to patients the importance of eating breakfast, lunch, and snack before going to sleep every day, as not eating or delay a meal can lead to a sharp drop in blood sugar using these drugs. And the risk of a sharp drop in blood sugar due to the use of Sulfonylureas drugs from the second generation, like Algelimbraad, equivalent to 1/10 that updated by sulfonylureas drugs from the first generation.

* Weight gain causes increased appetite and this is undesirable in obese patients with diabetes.

** Drugs may occur redness of the face, especially when use Alklorbrupamid with alcohol.

** Can cause drug Alklorbrupamid reservation of water in the body. And is similar in effect This Alvasupersen hormone Vasopressin Inhibitor to urinate. This leads to a low level of sodium in the blood and the occurrence of water intoxication.

** Blood poisoning and this rare could occur in less than 1% of patients.

** Can occur slightly dangerous drugs on the heart.

** Nausea and a metallic taste or change in taste in 1-3% of patients.

** Sulfonylureas drugs Combine with blood proteins, And being metabolized and disposal by the liver, and therefore drugs that compete with centers correlation drugs sulfonylureas with blood proteins, or drugs that affect the metabolism in the liver can interact with drugs sulfonylureas and increase or irresistible force-reducing sugar in the blood.

Increase the effectiveness of drugs sulfonylureas drugs in reducing the level of sugar in the blood.. Non-steroidal anti-inflammatory. Pill. Some anti-fungal drugs

* Non-steroidal anti-inflammatory (NSAIDS) - Like Sulaiceli, and sulfa compounds, and Alorfarin - Displaces sulfonylureas drugs and increase its concentration in the blood and cause a sharp drop in blood sugar. And sulfonylureas drugs from the second generation is characterized by first-generation drugs against their union with blood proteins, and thus bring about a sharp decline in the level of sugar in the blood due to drug interactions with blood proteins infrequent with sulfonylureas drugs from the second generation.

** Pills containing estrogen can increase the effect of sulfonylureas drugs in causing a sharp fall in the level of sugar in the blood.

* Some anti-fungal drugs such as Filokonazel Fluconazole And antibiotics such as chloramphenicol chloramphenicol could lead to a sharp drop in blood sugar when used with sulfonylureas drugs This occurs due to inhibition of digestive enzymes to sulfonylureas drugs by these drugs and also because of competition with blood proteins or with the output.

** Anti-congestion medications can increase the risk of low blood sugar when used with sulfonylureas drugs.

** When taking Alcohol with drugs sulfonylureas, it increases the risk of a sharp drop in blood sugar.

Reduce the effectiveness of drugs sulfonylureas drugs in reducing the level of sugar in the blood.. Vehicles steroids. Diuretics. Drugs that induce liver enzymes

** Compounds steroids Corticosteroids , And convoys beta receptors (beta blockers), And niacin (niacin), And Alreeten - a (Retin-A) Can reduce the effect of sulfonylureas compounds and lead to a rise in the level of sugar in the blood.

** Diuretics such as thiazide compounds Thiazide And Alvuorizmaid Furosemide Can reduce the effect of sulfonylureas drugs.

** Drugs that induce liver enzymes such as phenytoin Phenytoin , And phenobarbital Phenobarbital, And other irresistible force of blood sugar-reducing drugs sulfonylureas.

Second-generation sulfonylureas drugs.. Caution in patients who suffer from heart disease or in older patients

Drugs should be used sulfonylureas powerful second-generation effect like Aljlaepjurajd, and Algelebeizaid, and Algelimbraad caution in patients who suffer from heart disease or in older patients who are more vulnerable to the sharp drop in blood sugar.

Diabetics with type II diabetes who have not responded to treatment with Altolbyautamad or Altollazamed can respond to treatment with the most powerful vehicles from the first generation of drugs sulfonylureas (like Alklorbrupamid), or a second-generation drugs.

Tolbyautamad	Asatohecsamed	Tollazamed	Chlorpropamide
Absorption Metabolism Metabolic products Half-life (hours) Effect (hours) Output Borders dose (mg) The number of doses / day	Good Yes Ineffective 4-5 6-8 (short) Urine 500-3000 2-3	Good Yes Effective 6-8 10-16 (average) Urine 250-1500 1-2	Slow Yes Effective 7 12-14 (average) Urine 100-1000 1-2	Good Yes, but slowly Ineffective 32 20-60 (long) Urine 100-500 1-2

Advantages sulfonylureas drugs that are taken by mouth compared to injected insulin

1 - ease of administration - where the administration of sulfonylureas drugs by mouth is no doubt that it is easier and less expensive than giving insulin injections.

2 - Give sulfonylureas drugs by mouth stimulates the secretion of insulin from the beta cells in the pancreas and is therefore similar physiological scientific terms that insulin released from the pancreas by these drugs first reaches the liver and affect the exit of glucose from the liver. In contrast, the insulin given by injection will result in the accumulation of insulin in peripheral tissues before it reaches the liver.

3 - sulfonylureas drugs are less likely to cause insulin sensitivity because of insulin that is given by injection private extracted from animal source or persons who have no antibodies to insulin.

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Sulfonylureas compounds Sulfonylureas.. Alert secretion of insulin from the beta cells in the pancreas