Synonym |
Des-Cys1,Cyclo(Ser2-Asu7))-Calcitonin (eel), Elc |
Species |
Synthetic |
Protein Accession |
NA |
Purity |
> 95% |
Endotoxin Level |
< 1.0 EU per µg protein |
Biological Activity |
Not specified |
Expression System |
Synthetic |
Fusion Tag |
None |
Predicted Molecular Mass |
Approximately 3466.0 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Centrifuge vial before opening. Reconstitute in sterile deionized water to a concentration of
0.1-1.0 mg/ml. |
Storage & Stability |
Store lyophilized product at -20°C. Reconstituted product is stable for 3 months at -20°C. |
FAQ
What is Des-Cys1,c yclo(Ser2-Asu7))-Calcitonin (eel), Elc, and how does it work in the
body?
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc, is a synthetic analogue of the naturally
occurring hormone calcitonin found in the eel. Calcitonin is a hormone that plays a crucial role in
calcium and bone metabolism. It is produced by the parafollicular cells of the thyroid gland in humans
and helps regulate calcium levels in the blood by inhibiting osteoclast activity. Osteoclasts are cells
that break down bone tissue, releasing calcium into the bloodstream. By inhibiting these cells,
calcitonin effectively reduces calcium levels in the blood and helps maintain bone density and
strength.
The synthetic version, Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc, has been
designed to mimic the effects of human calcitonin but with improved stability and potency. It's used
primarily in conditions where calcium regulation is disrupted, such as in the management of
osteoporosis, Paget's disease of bone, and hypercalcemia of malignancy. By maintaining calcium balance,
it helps prevent bone loss and can alleviate bone pain and other symptoms associated with bone
disorders.
The mechanism through which Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc acts
involves binding to specific receptors on the osteoclasts. When the hormone binds to these receptors, it
triggers a cascade of events that result in reduced activity of the osteoclasts. Consequently, bone
resorption is decreased, and the rate at which calcium is released into the bloodstream is significantly
lowered. This process helps in preserving bone mass and reducing the risk of fractures, which is
particularly beneficial in postmenopausal women and the elderly, who are at higher risk of developing
osteoporosis.
Furthermore, Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc has shown potential
in alleviating pain by acting on central nervous system pathways. It may modulate how pain signals are
processed, providing an added benefit for individuals suffering from chronic bone pain. This dual action
on bone metabolism and pain management makes it a valuable therapeutic agent in the treatment of various
bone-related conditions.
Despite its benefits, it's important to note that the effectiveness of
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc can vary among individuals, and its use should be
carefully managed by healthcare professionals to ensure optimal results and minimize potential side
effects. Regular monitoring of calcium levels and bone density tests are often a part of the therapeutic
regimen to assess the drug's impact and adjust dosages accordingly.
What are the typical uses of
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc in
medicine?
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc, is used in the medical field for its
ability to replicate the action of human calcitonin, particularly in managing and treating conditions
that involve hypercalcemia and bone metabolism disorders. Its primary clinical applications include the
treatment of osteoporosis, Paget's disease of bone, and hypercalcemia due to malignancy.
In
osteoporosis, a condition characterized by weakened bones, Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel),
Elc is useful because it can slow bone loss and maintain bone density. Osteoporosis is a significant
concern, especially among postmenopausal women and the elderly, as it leads to a higher risk of
fractures. By inhibiting osteoclast activity, the drug helps mitigate bone degradation, thereby
strengthening the skeletal structure and reducing the likelihood of fractures.
In the context of
Paget's disease, where there is abnormal bone remodeling leading to bone expansion and weakening,
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc can help normalize the process of bone turnover. It
reduces the excessive and disorganized bone resorption, allowing for healthier bone formation and
consequently lessening the pain and deformities associated with this condition. Early intervention and
treatment with this calcitonin analogue can be crucial in managing symptoms effectively and preventing
complications that arise from unchecked bone remodeling.
In cases of hypercalcemia associated
with malignancy, which can occur when cancer causes either primary or secondary increases in bone
resorption, Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc offers a therapeutic approach by promptly
lowering calcium levels in the blood. This is vital not only in a palliative sense to relieve symptoms
but also in emergency situations to prevent the life-threatening effects of extreme hypercalcemia. By
controlling elevated calcium levels, the treatment also plays a role in preserving kidney function,
which can be compromised in prolonged hypercalcemic states.
Another potential, although less
common, use of Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc is in the management of chronic bone
pain. There is evidence to suggest that it can have analgesic effects, making it a supplementary therapy
for individuals suffering from persistent pain syndromes linked to bone conditions. This can improve
overall quality of life and functional ability for patients who are dealing with chronic
discomfort.
As with any medication, the use of Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc
should be tailored to the individual patient, taking into account the specific disorder, severity, and
patient-specific factors such as concurrent medical conditions and overall treatment goals. Close
monitoring and adjustment by healthcare professionals are important to ensure that the drug is both
effective and safe for long-term use.
What are the potential side effects of using
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc?
The use of
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc, while beneficial in managing conditions related to
bone metabolism and calcium regulation, can also come with a range of potential side effects. As with
any pharmacological treatment, it's critical for healthcare providers and patients to weigh the
therapeutic benefits against possible adverse effects.
One of the frequently reported side
effects is nausea, which occurs in some patients shortly after administration. The mechanism behind this
side effect is not entirely clear, but it's believed to involve the central nervous system and
gastrointestinal tract interactions. In most cases, the nausea is mild and transient, often resolving
without the need for intervention. However, in some patients, it may persist, necessitating the use of
anti-nausea medications or dose adjustments.
Flushing and a sensation of warmth are also common,
primarily due to the vasodilatory effects of the drug. This is typically mild and does not usually
require medical attention, although it can cause discomfort for some individuals. Managing such symptoms
can include ensuring a comfortable ambient temperature and dressing in layers to help control heat
intolerance.
Another potential side effect is allergic reactions, which can range from mild skin
rash to more severe symptoms such as anaphylaxis. Patients with known hypersensitivity to calcitonin or
fish products (since the drug is derived from eel calcitonin) should use it cautiously. Severe allergic
reactions, although rare, require immediate medical attention and discontinuation of the
drug.
Patients may also experience an increase in urinary frequency or volume. This side effect
is related to the hormone's role in calcium regulation, which can subsequently affect the balance of
electrolytes and fluid excretion by the kidneys. Monitoring of kidney function and electrolytes may be
necessary for those showing significant changes in urination patterns.
Headaches have been noted
as another side effect, although the incidence is not particularly high. These headaches can be
tension-type or migraine-like, and in some cases, they can be managed with over-the-counter pain relief
medications. Persistent or severe headaches should be evaluated to rule out other causes and to
determine if they are indeed related to the use of Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel),
Elc.
Importantly, long-term use of this calcitonin analogue has been associated with a slightly
increased risk of malignancies. This potential risk has prompted discussions in the medical community
about the balance between the benefits of reducing fracture risk and improving calcium homeostasis
against the possibility of developing cancer. It's a consideration that should be part of the long-term
management and decision-making process.
While the drug has a well-documented safety profile when
used as directed, any signs of adverse effects should be promptly reported to a healthcare provider to
allow for timely interventions and adjustments to the treatment plan. As with all medications, patient
education on potential side effects and clear communication with healthcare providers play critical
roles in ensuring safe and effective use.
How does Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel),
Elc compare to other treatments for osteoporosis?
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel),
Elc, offers a unique approach in treating osteoporosis, distinct from other available therapies which
include bisphosphonates, selective estrogen receptor modulators (SERMs), and parathyroid hormone-related
drugs. Each class of osteoporosis medication has a specific mechanism, and the choice of treatment often
involves considering efficacy, side effects, and patient-specific factors such as tolerability and
comorbid conditions.
In comparison to bisphosphonates, which are the most commonly prescribed
drugs for osteoporosis, Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc is generally considered when
patients cannot tolerate oral bisphosphonates due to gastrointestinal side effects, or when intravenous
administration is impractical. Bisphosphonates work by directly adhering to the bone matrix and
inhibiting osteoclast activity more aggressively. They are known for their bone mineral density
improvements and significant reduction in fracture risk. However, prolonged use has been linked to
atypical femoral fractures and osteonecrosis of the jaw, concerns that have led to treatment holidays
and reevaluations after a few years of use.
On the other hand,
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc provides not only anti-resorptive activity but also
potential analgesic effects, which can be beneficial for patients with osteoporosis who experience bone
pain—a feature not provided by bisphosphonates. This might make it an appealing option for older
patients who prioritize pain management alongside bone protection.
Selective estrogen receptor
modulators (SERMs) like raloxifene offer another alternative. They mimic estrogen's bone-preserving
properties without the hormone's other effects. While SERMs are typically more effective in reducing
vertebral fractures than non-vertebral fractures, they do not directly alleviate pain associated with
osteoporosis as Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc might. However, SERMs can increase the
risk of venous thromboembolism, making calcitonin a potentially safer option for patients at risk for
such conditions.
Parathyroid hormone-related therapies, like teriparatide, actually stimulate
osteoblastic activity, leading to new bone formation, contrasting with the anti-resorptive mechanism of
calcitonin. These are typically prescribed for more severe osteoporosis cases, particularly when
bisphosphonates have been ineffective or contraindicated. The use of
Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc over anabolic treatments might be more appropriate in
patients with less severe bone density loss, or where they're particularly at risk for an imbalance in
calcium homeostasis.
When comparing Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc to these
other treatments, its role often aligns with a more targeted patient population—those who may benefit
from its safety profile, unique dual benefits, or those who require a different strategy due to
contraindications or intolerance to other therapies. As always, treatment choice should be
individualized, guided by a comprehensive assessment of the patient's overall health, osteoporosis
severity, risk factors, and their personal treatment goals, while continually reassessing the efficacy
and safety throughout the course of the therapy.
What is the recommended administration route and
dosage for Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc?
The administration route and dosage
of Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc should be meticulously followed as prescribed by
healthcare providers, ensuring that patients receive the maximum benefit while minimizing the risk of
adverse effects. This calcitonin analogue is typically administered via injection or nasal spray, with
the chosen method often depending on the condition being treated, the patient’s ability to adhere to the
treatment regimen, and their preference.
For the treatment of osteoporosis, the nasal spray is a
common form of administration due to its convenience and ease of use. Patients are usually directed to
use one spray, typically delivering 200 International Units (IU), in one nostril per day, alternating
nostrils each day to reduce the risk of local irritation. This form of delivery is especially practical
for patients who may have difficulty with injections or who are on multiple oral medications, offering a
non-invasive option that fits easily into daily routines.
In contrast, for conditions that
require more immediate or aggressive intervention, such as conditions causing acute hypercalcemia, an
injectable form may be used. In such cases, Des-Cys1,cyclo(Ser2-Asu7))-Calcitonin (eel), Elc is
administered subcutaneously or intramuscularly, with initial doses generally ranging from 4 to 8 IU/kg
every 6 to 12 hours, depending on the severity of the condition and the patient’s response. This method
allows for quick adjustments to dosing and administration frequency based on therapeutic needs and
calcium levels monitored closely.
Paget's disease treatment can also make use of either route
depending on the severity and response expected. Initially, 100 IU a day administered subcutaneously or
intramuscularly for a period can be prescribed, with adjustments made based on patient response and
tolerance. The injectable route ensures a consistent delivery of the drug, particularly important in
managing intensive bone remodeling characteristic of the disease.
It is important to
comprehensively follow the instructions provided with nasal spray products, ensuring that the spray pump
is primed before use and that patients understand the importance of alternating nostrils with each dose.
For injections, patients or caregivers who administer the medication at home should be taught proper
injection techniques, site rotation to prevent local irritation, and to monitor any adverse
reactions.
Regular follow-ups and bone density assessments are crucial to evaluate the ongoing
appropriateness of the treatment and adjust dosages if necessary. In some treatments, particularly for
osteoporosis, long-term benefits should be weighed against the potential risks; thus, periodic reviews
and discussions with healthcare professionals are necessary.
Ultimately, the chosen route and
dosage should balance effectiveness with the patient's lifestyle, ability to administer or receive the
medication consistently, safety considerations, and specific therapeutic goals. This patient-centered
approach ensures individualized care that aligns with both medical standards and the patient's personal
circumstances and preferences.