Actually, liraglutide is an old friend of endocrinologists, since it has been used for years in the treatment of type 2 diabetes, although it is not usually a primary therapy. The drug acts on the regulation of appetite, reducing the desire to eat. It is a human analog of the peptide similar to glucagon type 1 (GLP-1) which stimulates the secretion of insulin and can be said to have a physiological satiating effect. This mechanism of action, has nothing to do with those of the sibutramine, which in different ways, acted on neurotransmission processes. Saxenda joins orlistat on the market, the only medication approved for the treatment of obesity, which is available with and without a prescription in pharmacies and which acts by blocking the absorption of a percentage of the fat.
Although no studies have directly compared them, there is several evidences that the results achieved with liraglutide are superior to those achieved with orlistat. In any case, medical supervision is recommended when taking either drug. Saxenda is aimed at people with a body mass index (BMI) equal to or greater than 30 kg/m2, as well as those with a BMI greater than 27 kg/m2, who also present some additional risk factor, such as hypertension or high cholesterol levels. In any case, the medication should always be indicated together with a low-calorie diet and an exercise plan.
One of the largest studies to test the effectiveness of the drug was conducted by Columbia University where a total of 2500 individuals were studied and given a daily dose of 3 mg of liraglutide, while another 1244 people with significant weight problems were similarly given a safe substance. None of them had diabetes at the beginning of the study. After one year of follow-up, the researchers found that the people who had undergone Saxenda treatment had lost an average of 18 lbs, while the other group had lost an average of 7 lbs. They also observed that 63% of those who received liraglutide managed to lose at least 5% of their body weight, compared to 27% who did so after receiving a placebo.
Furthermore, the experts also saw that Saxenda therapy was associated with a greater reduction in cardiometabolic risk factors, such as abdominal circumference, blood pressure or a number of inflammatory markers, and with better blood sugar control regardless of whether or not the individuals tested had previously suffered from pre-diabetes. It has been found that liraglutide is a real hope for many patients with obesity and that it helps those who have difficulty in losing weight or maintaining losses over time. The most common side effects detected in the aforementioned experiment were gastrointestinal and dehydration. There are already results of studies two or more years old that have been published and that have found nothing alarming against human health.
Liraglutide therapy consists of 3mg injections during the first weeks, then the patient's doctor will be in charge of increasing the doses as required. Each injection is a pre-filled pen with the medication that is administered subcutaneously once a day, at any time of the day, regardless of meal times. It should be injected into the abdomen, thigh or upper arm. It is very important to follow the doctor's instructions in terms of diet and regular exercise to complement the therapy, in addition to the need for periodic tests. The greatest benefits of Saxenda found in patients who have undergone this treatment, are that it has been proven to be effective in reducing appetite and increasing the feeling of satiety, which makes it much easier to achieve positive results. Weight losses of 5% were found in the first 12 weeks of treatment in most patients. Therapy with liraglutide 3mg. is also associated with a significant improvement in glycemic parameters, reduction in cardiometabolic risk factors, reduction in waist circumference and significant reduction of sleep apnea.
Although liraglutide is one of the most effective drugs in the treatment of obesity, without compromising the patient's health in order to obtain results, and it is good news to have a new therapeutic alternative for overweight patients, we must not forget that drugs are not the whole solution to the problem. Since a large percentage of the population suffers from overweight, it is not feasible to think that such a large number of people can be persuaded to eventually make responsible decisions about their health. The key is to change life habits, make cities healthier and build consumption models that really help society as a whole to fight obesity.
Liraglutide is a GLP-1 analog with 97% sequence homology to human GLP-1 that binds to and activates the GLP-1 receptor, an endogenous incretin that enhances glucose dependent insulin secretion in pancreatic beta cells. Unlike regular GLP-1, liraglutide has a human pharmacodynamic profile suitable for once-daily administration. After subcutaneous administration, its delayed-action profile is based on three mechanisms: self-association, which results in slow absorption; binding to albumin; and enzymatic stability superior to dipeptidyl peptidase 4 and the neutral endopeptidase enzyme, which results in a plasma half-life.
The action of liraglutide is through a specific interaction with GLP-1 receptors, which produces an increase in cyclic adenosine monophosphate. Liraglutide stimulates insulin secretion in a glucose-dependent manner. Simultaneously, liraglutide decreases the secretion of inadequately elevated glucagon. So, when blood glucose is high, insulin secretion is stimulated and glucagon secretion is inhibited. In contrast, during hypoglycemia, liraglutide decreases insulin secretion and does not affect glucagon secretion. The hypoglycemic mechanism also involves a slight delay in gastric emptying.
Liraglutide reduces body weight and body fat mass through mechanisms involving a reduction in appetite and caloric intake. After subcutaneous administration of liraglutide, its absorption is slow, reaching a maximum concentration 8-12 hours after administration. The estimated maximum concentration of liraglutide is 9.4 nmol per liter after a single subcutaneous dose of 0.6 mg of liraglutide. With doses of 1.8 mg of liraglutide, the concentration is approximately 34 nmol per liter. In terms of chronic toxicity studies, two-year experiments were conducted in which non-lethal tumors were observed in thyroid C cells in rats and mice at all doses used. These tumors were not observed in monkeys treated for 20 months. The relevance in humans is low but cannot be completely excluded.
Liraglutide is indicated in the treatment of patients over 10 with type 2 diabetes mellitus to achieve glycemic control as monotherapy or in combination with metformin or a sulfonylurea, or in combination with metformin and a thiazolidindione. It has also been approved for weight control, its administration is subcutaneous and is presented below:
Children over 10 years old and adults: the initial dose is 0.6 mg of liraglutide per day. After at least one week, the dose should be increased to 1.2 mg. These doses may be increased in some patients to 1.8 mg. Daily doses higher than 1.8 mg are not recommended. It is possible to add liraglutide to an existing treatment with metformin or to a combined therapy of metformin and a thiazolidindione. The doses of metformin and thiazolidindione used at this time may be kept unchanged. Liraglutide may also be added to an existing treatment with a sulfonylurea or to a combined therapy of metformin and a sulfonylurea. When liraglutide is added to a sulfonylute combination therapy, consideration should be given to lowering the dose of the sulfonylute to reduce the risk of hypoglycemia.
Patients with renal insufficiency: no dose adjustment is necessary in patients with mild renal insufficiency (creatinine clearance 60-90 ml/min). Therapeutic experience in patients with moderate renal failure (creatinine clearance 30-59 ml/min) is very limited and there is no therapeutic experience in patients with severe renal failure (creatinine clearance below 30 ml/min). The use of liraglutide is not recommended in patients with moderate and severe renal dysfunction, including patients with end-stage renal disease. Currently the therapeutic experience in patients with any degree of liver failure is too limited to recommend use in patients with mild, moderate, or severe liver failure. Therefore, unless the doctor approves the use of liraglutide in the individual, the best advice is not to use it.
Some cautions are that Liraglutide is contra-indicated in patients with hypersensitivity to the drug or any of its components. Liraglutide should not be used in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis. The use of liraglutide is associated with transitory gastrointestinal adverse reactions, such as nausea, vomiting and diarrhea. On the other hand, experience with liraglutide in patients with inflammatory bowel disease and diabetic gastroparesis is limited, and its use is not recommended.
The use of GLP-1 analogues has been associated with the risk of pancreatitis, although in the case of liraglutide no cases of acute pancreatitis have been reported. If symptoms such as ongoing abdominal pain appear, the patient should discontinue treatment with liraglutide and any other medication that is thought to be a possible cause. Thyroid adverse events have been reported in clinical trials including increased blood calcitonin, goiter, and thyroid neoplasm in patients with pre-existing
thyroid disease. Patients given liraglutide in combination with a sulfonylurea may experience episodes of hypoglycemia, necessitating dose reduction of oral antidiabetic. Patients who do not have a medical history of diseases such as those mentioned above are not at risk for adverse events, although medical supervision should always be involved in liraglutide therapies.
SAXENDA FOR WEIGHT LOSS
Liraglutide is very similar to a hormone (GLP-1 analog) that the human body makes. Under physiological conditions, this hormone is produced in the intestine in response to food to signal the brain that the person has eaten enough, thus suppressing the appetite, decreasing anxiety about food, and causing greater satiety after eating. How is it used? It is given as a subcutaneous injection once a day. The use of these drugs is approved to treat obesity in adults when sufficient weight loss is not achieved with the usual treatment. They should always be used in conjunction with diet and exercise, under medical supervision. The indication for Saxenda is made taking into account the body mass index (BMI).
Consequently, liraglutide could be used in the following cases:
- People with a BMI of 30 or more (obesity)
- People with a BMI of between 27 and 30 (overweight) but who also suffer from some complication related to excess weight: for example, diabetes, hypercholesterolemia or hypertriglyceridemia, high blood pressure or obstructive sleep apnea.
- People who do not have or have had pancreatic or liver disease.
Is it safer to take natural medicines? These products are not real medicines and therefore have not been proven to be effective in scientific studies. The worst thing is that in most cases they have not even proved to be really safe. It is necessary to understand that natural does not mean safe! There are an endless number of cases in which natural products have had negative consequences for health. For example, natural diuretics, besides only making the patient lose fluid, can cause a cardiac arrhythmia due to potassium loss in the urine. Other products cause serious liver and kidney problems or, in the best of cases, annoying symptoms and a useless economic expense.
Saxenda therapies have been carried out with patients up to 65 years old, with the same doses prescribed for healthy adults and no adverse results have ever been reported. Also, Liraglutide is originally used to regulate blood glucose in patients aged 10 and older without side effects. People over 65 and under 10 years of age are not candidates for this treatment. Generally, the side effects of Saxenda are vomiting and diarrhea during the first days of use, symptoms that gradually disappear in almost all patients.
How much weight can a person lose by using Liraglutide? It is difficult to establish an exact figure since the effectiveness is very variable and depends above all on the treatment that accompanies the drugs, that is to say, on the diet and exercise, as well as the discipline of the patient. It also depends on the moment in which the weight loss is measured, since the effectiveness decreases with time (some patients regain their lost weight). Normally in scientific studies, 4 to 8% of the weight has been lost, which represents 11 to 22 lbs. after a few weeks of treatment. To correctly interpret these results, it must be recognized that not all the weight lost is due to drugs, but also to diet and exercise.
The patient should take these considerations in mind before starting to use Saxenda:
- This medication should never be the first treatment before trying an intensive habit change. The treatment of choice will always be diet and exercise.
- Neither will it prevent the patient from dieting and exercising since even using these drugs, changing habits is essential to achieve good results.
- It is not an adequate treatment if the person does it just to try it, but it must be in the context of a real attempt to lose weight, and this, requires a lot of effort.
- The result will depend on the effort and on the patient being able to change the lifestyle that led to the overweight. If he does not change, he will not manage to lose weight.
In summary, Liraglutide is extremely effective for helping to lose weight, and is one of the safest medicines on the market, there is no doubt about that. But its effect is not a miracle, it will not do all the work for the patient, if the patient doesn't commit to follow the diet and exercise before, during and after the treatment. So, the person who takes this therapy will have excellent results and will avoid in the long term regaining the weight lost, especially if he takes advantage of the weight loss process to change his lifestyle intensively. This would really be taking advantage of the treatment, if the patient decides to use it as support to change his life.