Synonym |
Exenatide |
Species |
Human |
Protein Accession |
P43220 |
Purity |
≥98% |
Endotoxin Level |
<1.0 EU per 1 μg of protein |
Biological Activity |
The ED50 for this effect is typically 0.06-0.2 μg/ml. |
Expression System |
Escherichia coli |
Fusion Tag |
None |
Predicted Molecular Mass |
5.0 kDa |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20mM Citrate, pH 4.0 |
Reconstitution |
Centrifuge vial before opening. Reconstitute in 10mM HCl to a concentration of 0.1-1.0 mg/ml.
|
Storage & Stability |
Store at -20°C. Stable for at least 2 years when stored at -20°C. |
FAQ
What is Exenatide Acetate and how does it work for diabetes management?
Exenatide Acetate is an
injectable medication used to manage blood sugar levels in individuals with type 2 diabetes. It belongs
to a class of drugs known as incretin mimetics or GLP-1 receptor agonists. These medications mimic the
action of incretin hormones that the body naturally produces. Incretins increase insulin secretion in
response to meals and decrease the amount of glucose the liver produces. They also slow down gastric
emptying and help control appetite, which can contribute to weight loss. Exenatide Acetate is not an
insulin replacement but is used in conjunction with other diabetes medications, as well as diet and
exercise, to improve glycemic control.
The mechanism of Exenatide Acetate involves its action on
the GLP-1 receptor, a receptor that plays a crucial role in glucose metabolism. When exenatide binds to
GLP-1 receptors on pancreatic beta cells, it triggers a cascade of intracellular events that increase
the synthesis and release of insulin. One of the unique advantages of exenatide is that it tends to
stimulate insulin secretion only when blood-sugar levels are high, thus reducing the risk of
hypoglycemia compared to some other anti-diabetic agents. Additionally, exenatide reduces the secretion
of glucagon, another hormone produced by the pancreas that raises blood-sugar levels, thus further
contributing to lowering post-meal glucose spikes.
Importantly, Exenatide Acetate also influences
gastric emptying by slowing it down, which can lead to users feeling fuller longer and reduce appetite.
This effect is advantageous for individuals with type 2 diabetes who are often overweight, although it’s
worth noting that not everyone using exenatide will experience significant weight loss. Because of these
multiple mechanisms, Exenatide Acetate is considered an effective option for people whose blood sugar
levels are not adequately controlled with oral medications alone.
What are the potential side
effects of using Exenatide Acetate?
Exenatide Acetate, like any medication, comes with a spectrum of
potential side effects. Not everyone who uses Exenatide Acetate will experience these side effects, and
some people may experience side effects not listed here. The most common side effects experienced by
individuals taking Exenatide Acetate are gastrointestinal in nature. These include nausea, vomiting,
diarrhea, and sometimes constipation. Nausea is often the most frequently reported side effect and may
decrease over time as the body becomes accustomed to the medication.
Another set of potential
side effects includes reactions at the injection site such as redness, swelling, or itching. These are
generally mild and resolve without intervention. However, more severe hypersensitivity reactions can
occur, and symptoms like a rash, difficulty breathing, or severe dizziness should be addressed
immediately by seeking medical attention.
Additionally, Exenatide Acetate may be associated with
more serious side effects such as pancreatitis. Symptoms of pancreatitis include persistent abdominal
pain that may radiate to the back, nausea, and vomiting. If pancreatitis is suspected, the medication
should be discontinued immediately, and medical care should be sought. There are also concerns
surrounding potential thyroid C-cell tumors. In animal studies, some GLP-1 receptor agonists have been
linked to increased rates of thyroid tumors, but the relevance of these findings to humans remains
uncertain. Nonetheless, it is recommended that individuals with a personal or family history of
medullary thyroid carcinoma or Multiple Endocrine Neoplasia syndrome type 2 avoid the use of
exenatide.
Finally, although the risk of hypoglycemia (low blood sugar) is considered lower with
Exenatide Acetate compared to insulin or sulfonylureas, the risk increases if exenatide is used in
combination with such medicines. It's crucial for individuals to recognize the symptoms of hypoglycemia,
which include shakiness, sweating, confusion, and palpitations. Those taking a combination of diabetes
medications should frequently monitor their blood glucose levels as advised by their healthcare
provider.
While Exenatide Acetate is effective for many individuals in managing type 2 diabetes,
it’s important to have an open dialogue with healthcare providers to weigh the benefits against the
potential risks of any medication. Should side effects occur, they should be reported to a healthcare
professional to address any concerns that may arise during the treatment course.
How should
Exenatide Acetate be stored and handled safely?
Proper storage and handling of Exenatide Acetate are
vital to ensure its efficacy and safety for the managing of type 2 diabetes. Exenatide Acetate is
provided in a pre-filled pen, which must be stored in a refrigerator at a temperature between 36°F to
46°F (2°C to 8°C) until the first use. It's crucial that users do not freeze Exenatide Acetate or store
it near the freezer compartment, as freezing can degrade the product and render it ineffective. If the
medication becomes frozen, it should be disposed of properly and not used.
Before using, allowing
the medication to warm up to room temperature can help reduce discomfort at the injection site. After
the first use, the Exenatide Acetate pen can be stored at room temperature not exceeding 77°F (25°C) for
up to 30 days. Keeping the pen cool and protected from both direct sunlight and heat sources will
preserve its potency. It is important to keep the pen cap closed when not in use to prevent
contamination and protect the solution from light exposure.
Handling Exenatide Acetate also
requires attention to hygiene and accuracy. Users should always wash their hands thoroughly before
administering the injection. Selecting a different injection site for each dose is recommended to
minimize the risk of site reactions or lipodystrophy, a condition that changes the way insulin is
absorbed due to repeated injections in the same area. The pen should be inspected visually for any
particulate matter or discoloration before use. If particulate matter or a change in color is observed,
the medication should not be used, as these could indicate contamination or degradation.
For
individuals using Exenatide Acetate, maintaining a routine schedule for injections is important,
typically administered twice daily within 60 minutes before the morning and evening meals. Missing a
dose should be managed according to healthcare provider instructions but typically involves taking the
missed dose only if it's close to the dosing time, avoiding double dosing. All used needles should be
disposed of in a proper, FDA-cleared sharps disposal container to prevent injury and contamination.
In summary, meticulous attention to the storage and handling of Exenatide Acetate supports the
medication's efficacy in managing diabetes and mitigates potential safety risks. Ensure to follow any
additional storage or handling guidance provided by a healthcare professional or pharmacist, as these
can be tailored to individual patient needs and circumstances.
Can Exenatide Acetate be used
alongside other medications and treatments?
Exenatide Acetate is often used in combination with
other medications for managing type 2 diabetes, such as metformin, sulfonylureas, and insulin. However,
the compatibility and potential interactions with other medications must be meticulously considered to
ensure safety and effectiveness in blood sugar management. It’s essential to create a comprehensive plan
under the guidance of a healthcare provider when incorporating Exenatide Acetate with other treatments,
as interactions could influence how medications work or heighten the risks of side
effects.
Regarding the use alongside insulin, care should be taken as combining Exenatide Acetate
with insulin can increase the risk of hypoglycemia. When starting Exenatide Acetate, a healthcare
provider may adjust the dose of concurrent antidiabetic agents to reduce this risk. The provider will
usually suggest more frequent blood sugar monitoring to assess individual response and correct
dosing.
Additionally, Exenatide Acetate can slow gastric emptying, which may affect the
absorption and effectiveness of oral medications. Patients should discuss with their healthcare provider
how to time the administration of other oral medications concerning their Exenatide Acetate injections
to mitigate any absorption issues. For example, oral contraceptives or antibiotics might need to be
taken at least an hour before the Exenatide Acetate to ensure full effectiveness.
Notably,
Exenatide Acetate may not be suitable for people taking medications that require rapid gastrointestinal
absorption. Since Exenatide Acetate may interfere with the absorption of such medications, adjusting
these treatments could be crucial for maintaining their therapeutic efficacy. Tailoring the medication
regimen to individual needs often involves a careful review of all medications being taken, including
over-the-counter drugs and supplements.
Finally, lifestyle interventions such as diet and
physical activity are integral parts of diabetes management and should complement Exenatide Acetate
therapy. A coordinated approach involving a registered dietitian or diabetes educator can optimize the
overall treatment outcomes. They can work closely with healthcare providers to develop a comprehensive
and individualized management plan.
In conclusion, while Exenatide Acetate provides flexibility
when used with other diabetes treatments, coordination and open communication with healthcare providers
are key to safe and effective therapy. Monitoring, adjustments, and personalized education about
interactions can mitigate risks and contribute to optimal blood glucose control for individuals with
type 2 diabetes.
What are the benefits of Exenatide Acetate beyond blood glucose control?
Exenatide Acetate offers several benefits beyond its primary role in blood glucose regulation for
individuals with type 2 diabetes. One of the significant advantages is its potential to contribute to
weight loss. Many patients with type 2 diabetes are overweight, and excess weight can exacerbate insulin
resistance and complicate management of the condition. Exenatide Acetate can promote modest weight loss
by mimicking the hormone GLP-1, which slows gastric emptying and helps users feel fuller for longer
periods, subsequently reducing caloric intake and fostering weight loss. This effect not only aids in
better glycemic control but also in achieving more favorable cardiovascular outcomes.
Moreover,
weight loss associated with Exenatide Acetate use may improve other metabolic parameters, including
lipid profiles and blood pressure, by reducing obesity-related health risks. Clinical studies have shown
improvements in triglycerides, HDL cholesterol, and blood pressure with weight loss, contributing to an
overall reduction in cardiovascular risk, which is crucial for individuals with type 2 diabetes at
higher risk for heart disease.
Additionally, Exenatide Acetate can have a positive impact on the
preservation of pancreatic beta-cell function. The enhanced secretion of insulin in response to meals
provided by Exenatide may help delay the progression of beta-cell failure that typically characterizes
type 2 diabetes, potentially altering the disease's natural progression over time. While more
longitudinal studies are needed to fully understand this benefit, the potential long-term preservation
of beta-cell function is a promising aspect of Exenatide Acetate therapy.
Exenatide Acetate may
also offer benefits related to improvements in quality of life. By modulating appetite and contributing
to weight loss, patients might experience an empowerment and confidence in managing their weight and
diabetes. This psychological benefit, although intangible, can critically impact adherence to diabetes
management plans and lifestyle changes, fostering a more proactive approach toward health.
Beyond
the physical benefits, the twice-daily dosing regimen of Exenatide Acetate offers a routine that is
practical and fits into many patients’ daily schedules. These multiple benefits illustrate that
Exenatide Acetate serves as a multifaceted treatment option, providing value that extends beyond blood
glucose control, enhancing overall metabolic health and quality of life for patients with type 2
diabetes. However, it remains paramount that the use of Exenatide Acetate and its benefits be
continuously assessed in consultation with healthcare providers to maximize outcomes while minimizing
risks.
Are there any considerations or contraindications to be aware of before starting
Exenatide Acetate?
Before initiating treatment with Exenatide Acetate, there are several important
considerations and contraindications that healthcare providers typically review with patients to ensure
safe and effective use. One of the primary contraindications is a history of severe hypersensitivity
reactions to exenatide or any components of the formulation. If a patient is aware of an allergy to
similar medications or any components in Exenatide Acetate, it is categorized as a
contraindication.
More notably, Exenatide is contraindicated in patients with a personal or
family history of medullary thyroid carcinoma or those with Multiple Endocrine Neoplasia syndrome type 2
(MEN 2) due to concerns raised from animal studies demonstrating increased rates of C-cell tumors with
GLP-1 receptor agonists, though the human relevance is still being studied. Therefore, patients with
these backgrounds typically avoid using Exenatide to remove potential risks.
It's crucial to
consider underlying health conditions, such as severe renal impairment or end-stage renal disease, where
the use of Exenatide is not recommended, as it is eliminated by the kidneys, and compromised renal
function could lead to its accumulation and increased risk of side effects. Furthermore, cases of acute
pancreatitis have been reported in patients treated with Exenatide. Hence, caution is advised in
patients with a history of pancreatitis. Patients are educated to report any unexplained severe
abdominal pain to their healthcare provider.
Concomitant gastrointestinal diseases such as
gastroparesis or severe gastrointestinal disease also warrant caution when prescribing Exenatide, given
its influence on gastric emptying. Additionally, it’s important to assess the patient’s understanding of
injection techniques and the ability to manage an injectable medication. Training is often provided to
ensure that patients can administer Exenatide correctly and consistently while managing areas like
proper storage, dose timing and handling emergencies like hypoglycemia.
Finally, the
comprehensive patient medication profile should be considered, involving drug-drug interaction
assessments. Exenatide may affect the absorption and efficacy of oral medications due to its slowing
effect on gastric emptying, and adjustments may need to be considered.
In summary, beginning
Exenatide Acetate therapy should involve an in-depth assessment of medical history, concurrent
conditions, and patient-specific factors, guided by healthcare professionals to optimize therapeutic
benefits while minimizing potential risks.