Synonym |
DGlu-His-Trp-Ser-Tyr-D-Ser(TBu)-Leu-Arg-Pro -Lys-Pro-D-Ala-Phe-NH2 |
Species |
Human |
Protein Accession |
P01137 |
Purity |
≥ 95% |
Endotoxin Level |
< 1 EU/μg |
Biological Activity |
Fully biologically active when compared to standard |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
1805.3 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in water to a concentration of 0.1-1.0 mg/ml.
Do not vortex. |
Storage & Stability |
Store at -20°C. Stable for 12 months from the date of receipt. |
FAQ
What is (Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH and what does it
do?
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH is a synthetic peptide analog of the naturally
occurring gonadotropin-releasing hormone (GnRH), which plays a crucial role in the regulation of
reproduction. This analog is designed to interact with the pituitary gland in a manner similar to
natural GnRH but with modified properties that enhance its therapeutic potential. The primary function
of (Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH is to regulate the secretion of two critical hormones,
luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which are vital for reproductive
function in both males and females. In clinical settings, such peptides are often developed to treat
hormone-sensitive conditions such as prostate cancer, breast cancer, and precocious puberty by
modulating the production of sex hormones.
The synthetic nature of this peptide allows for
increased stability, potency, and selectivity in its action compared to the endogenous hormone. By
altering specific amino acids in its sequence, (Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH is
engineered to resist enzymatic degradation, which typically limits the duration of action of natural
peptides in the body. This means that when administered for medical purposes, it can have longer-lasting
effects, reducing the frequency with which it needs to be administered.
Additionally, by
adjusting the molecular structure, this analog can exhibit agonistic or antagonistic properties based on
the therapeutic needs. An agonistic version might be used to initially stimulate the production of sex
hormones, while an antagonistic version can suppress the hormone levels by continuous administration,
leading to downregulation of the pituitary response. This dual potential allows for versatile
applications in managing hormone-related disorders.
It's also noteworthy that due to its targeted
mechanism of action, (Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH can offer a more focused approach
compared to broader hormonal therapies, potentially reducing side effects. However, like any potent
pharmaceutical agent, its use must be closely monitored by healthcare professionals to tailor the
treatment to individual patient needs and minimize possible side effects.
How is
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH administered and what should be expected during
treatment?
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH is typically administered via injection,
either subcutaneously or intramuscularly, depending on the specific clinical application and
formulation. The route of administration is chosen based on the desired speed and duration of action, as
well as patient convenience and compliance. Before starting the treatment, a healthcare provider will
conduct a comprehensive evaluation to determine the appropriate dosage and frequency, tailored to the
patient’s specific condition and physiological responses.
Upon administration, patients may
observe a temporary flare-up effect, especially in cases where the peptide acts initially as a GnRH
agonist. This means there may be a transient increase in hormone levels before a subsequent decline,
particularly when used to manage hormone-sensitive cancers like prostate or breast cancer. During this
period, patients might experience a worsening of symptoms, which should be communicated to and monitored
by their healthcare provider. In patients for whom such responses are contraindicated, concurrent
medications such as anti-androgens may be prescribed to counteract these effects.
Throughout the
course of treatment, regular monitoring is essential. This would commonly include blood tests to
evaluate hormone levels and assess the efficacy of the treatment. Patients should attend all scheduled
check-ups and immediately report any adverse symptoms or significant changes in health status to their
healthcare providers. Side effects can vary but may include injections site reactions, mood swings, hot
flashes, or other symptoms related to hormonal fluctuations. These should be managed under the guidance
of a healthcare professional.
Furthermore, the treatment plan is likely to be adjusted over time
based on the patient’s response and progress. This dynamic approach helps ensure the treatment remains
effective and aligned with the evolving needs of the patient. Therefore, it is important for patients to
maintain open and ongoing communication with their healthcare providers throughout the treatment
process. Additionally, educational resources and support groups can be valuable for patients to better
understand their treatment and how to manage their condition effectively.
What potential side
effects or adverse reactions should be aware of when using
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH?
Like any medical treatment,
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH comes with the potential for side effects and adverse
reactions. It is important for patients and healthcare providers to be aware of and actively monitor for
these potential issues to ensure safe and effective use of the medication. Common side effects are often
related to its action on hormone levels and might include hot flashes, sweating, mood alterations,
decreased libido, and fatigue. These symptoms are typically due to the intended effects of lowering sex
hormone levels, which mimic some aspects of menopause or andropause.
Injection site reactions
such as pain, swelling, or redness are also possible. These are usually mild to moderate in severity and
resolve without intervention. However, any severe or persistent injection site reactions should be
brought to the attention of a healthcare provider as they may require specific management or changes in
injection technique.
More serious, albeit less common, side effects could include cardiovascular
issues such as palpitations, hypertension, or changes in lipid profile. Patients with pre-existing
cardiovascular conditions should be monitored closely. In some instances, the treatment can also lead to
bone density loss, increasing the risk of osteoporosis over long-term use. This is due to the reduced
levels of sex hormones, which play a critical role in bone health. Supplementary calcium and vitamin D,
alongside weight-bearing exercises, may be recommended to mitigate this risk, but specific strategies
should be tailored by healthcare providers.
Moreover, patients with hormone-sensitive cancers may
initially experience a tumor flare during the first few weeks of treatment, which can transiently worsen
symptoms. This is particularly relevant in prostate cancer treatments, where patients might experience
increased bone pain or other related symptoms. Prophylactic measures, such as the use of anti-androgens,
might be employed to manage these effects.
It's critical for patients to have a comprehensive
understanding of these potential risks and to work closely with their healthcare team to promptly
address any side effects. Regular follow-up appointments are crucial for monitoring health status and
hormone levels to adjust treatment as needed. Patients should never hesitate to reach out to their
healthcare provider if they suspect they are experiencing side effects, as early intervention can
prevent complications and improve overall treatment outcomes.
How does
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH treatment affect long-term health?
The long-term
effects of (Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH treatment are primarily dependent on its
mechanism of action, which involves the modulation of hormone levels. Over extended periods, the
suppression of sex hormones such as testosterone and estrogen can have several systemic effects. One of
the most significant long-term health considerations is bone health, as chronic hormone suppression can
lead to decreased bone density. This increases the risk of osteoporosis and related fractures,
particularly in populations already vulnerable to bone loss, such as postmenopausal women and older
men.
Patients undergoing long-term treatment should have their bone density monitored
periodically. Preventive strategies might include dietary supplementation with calcium and vitamin D, as
well as engaging in regular weight-bearing exercises to strengthen bones. In some cases, additional
medications like bisphosphonates may be prescribed to protect bone health, especially in individuals
with a high risk of osteoporosis.
Long-term hormone suppression can also affect muscle mass and
strength, potentially leading to sarcopenia, a condition characterized by the loss of muscle tissue.
This can be mitigated through resistance training exercises, which help maintain muscle integrity and
function. Regular physical activity should be encouraged as part of the management plan to support
overall physical health and well-being.
Another long-term consideration is the potential impact
on cardiovascular health. Changes in lipid profiles and an increased risk of metabolic syndrome have
been observed with prolonged hormone treatment. Patients should be monitored for changes in blood
pressure, cholesterol levels, and glucose metabolism. Lifestyle modifications addressing diet, exercise,
and smoking cessation are critical to managing these risks. In some cases, pharmacological interventions
may be necessary to address significant alterations in cardiovascular health
markers.
Psychological effects over the long term should not be overlooked. Hormonal changes can
affect mood and cognitive function, and patients may experience issues such as depression or memory
changes. Mental health support, whether through counseling or pharmacotherapy, may be beneficial and
should be considered as part of comprehensive treatment planning.
Patients and healthcare
providers should work collaboratively to monitor for and address these long-term effects, adjusting
treatment as necessary to balance the therapeutic benefits with potential risks. Regular evaluations and
personalized care plans are essential to mitigate these risks, ensuring that patients maintain a good
quality of life while benefiting from the therapeutic effects of the treatment.
Are there any
contraindications or special precautions that should be considered before starting
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH therapy?
Before initiating treatment with
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH, it is essential to evaluate any contraindications or
special precautions to ensure patient safety and therapeutic efficacy. This involves a thorough medical
assessment by a healthcare provider, including a review of the patient's medical history, current health
status, and any existing medical conditions.
The primary contraindication for this treatment is
pregnancy. As the medication can significantly alter hormone levels, it may adversely affect fetal
development, making it imperative that women of childbearing potential have a confirmed negative
pregnancy test prior to starting therapy. Effective contraception should be used before, during, and
after treatment as advised by a healthcare provider to prevent pregnancy.
Another key
consideration is the presence of any hypersensitivity or allergic reactions to the components of
(Des-Gly10,D-His2,D-His(Bzl)6,Pro-NHEt9)-LHRH or similar analogs. Patients with a known history of
allergic reactions to peptide therapies should inform their healthcare provider, as alternative
treatments may be necessary.
Patients with pre-existing cardiovascular conditions should be
assessed carefully, as the treatment can influence cardiovascular health markers. Regular monitoring for
changes in blood pressure, heart rate, and lipid levels is essential. Additionally, individuals with a
history of osteoporosis or other bone health issues should be evaluated for the risk of bone density
loss, with preventive strategies put in place to minimize this risk.
Hepatic and renal function
should also be considered, as these organs play a role in the metabolism and excretion of many
medications. Impaired liver or kidney function may necessitate adjustments to dosing or frequency of
administration, ensuring that the treatment remains safe and effective.
Furthermore,
psychological assessments may be warranted, particularly for patients with a history of mood disorders
or cognitive impairments, as these conditions can be exacerbated by hormonal changes. Supportive mental
health care should be integrated into the treatment plan if necessary.
Personalized treatment
considerations, including the patient's overall health, lifestyle, and treatment goals, should guide the
approach. Open communication between the patient and healthcare provider is vital to address any
concerns, enabling proactive management of potential complications and ensuring optimal outcomes
throughout the treatment journey. Regular follow-ups and a comprehensive care plan can further support
patients in managing these precautions effectively.