Supprelin LA 50mg Implantkit

Manufacturer ENDO Active Ingredient Histrelin Implant (CPP)(his TREL in) Pronunciation His-TREL-in
It is used to delay puberty in children who are maturing too early.If your child has been given this drug for some other reason, talk with the doctor about the benefits and risks. Talk with the doctor if you have questions or concerns about giving this drug to your child.
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Drug Class
Gonadotropin-releasing hormone (GnRH) analog
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Pharmacologic Class
GnRH receptor agonist
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Pregnancy Category
Category X
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FDA Approved
May 2007
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Supprelin LA is a small implant placed under the skin of the arm. It contains a medicine called histrelin, which helps to stop early puberty in children. It works by telling the body to slow down the production of hormones that cause puberty. The implant stays in for 12 months and then needs to be replaced.
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How to Use This Medicine

Proper Administration of This Medication

To ensure your child receives this medication correctly, follow the instructions provided by their doctor and read all accompanying information carefully. The medication is inserted under the skin in the upper arm through a minor surgical procedure, which will be performed by your child's doctor.

Post-Procedure Care

After the medication is inserted, keep the upper arm dry for 24 hours to promote healing. Avoid bathing or swimming during this time. Do not remove any surgical strips, as they will fall off on their own within a few days.

Activity Restrictions

For 7 days after the procedure, have your child avoid heavy play or exercise that involves the affected arm to prevent complications.

Storage and Disposal

If you need to store this medication at home, consult with your child's doctor, nurse, or pharmacist for guidance on proper storage procedures.

Missed Dose

If you miss a dose, contact your child's doctor immediately to determine the best course of action.
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Lifestyle & Tips

  • Maintain regular follow-up appointments with the endocrinologist to monitor treatment effectiveness and overall health.
  • Report any new or worsening symptoms, especially signs of continued puberty or implant site issues.
  • Ensure proper care of the implant site as instructed by the healthcare provider.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Not indicated for adults for central precocious puberty (CPP).
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: One 50 mg implant subcutaneously, replaced once every 12 months. For central precocious puberty (CPP).
Adolescent: One 50 mg implant subcutaneously, replaced once every 12 months. For central precocious puberty (CPP).
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Dose Adjustments

Renal Impairment:

Mild: No dose adjustment recommended.
Moderate: No dose adjustment recommended.
Severe: No dose adjustment recommended.
Dialysis: No specific recommendations; not expected to be significantly affected by dialysis.

Hepatic Impairment:

Mild: No dose adjustment recommended.
Moderate: No dose adjustment recommended.
Severe: No dose adjustment recommended.

Pharmacology

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Mechanism of Action

Histrelin is a synthetic nonapeptide analog of naturally occurring gonadotropin-releasing hormone (GnRH). It acts as a potent agonist at GnRH receptors in the anterior pituitary. Chronic administration of histrelin leads to desensitization and downregulation of GnRH receptors, resulting in a profound decrease in the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This, in turn, suppresses gonadal steroidogenesis (estradiol in females, testosterone in males), thereby arresting the progression of central precocious puberty.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (from implant)
Tmax: Initial peak within 24 hours, then sustained release with relatively stable concentrations over 12 months.
FoodEffect: Not applicable (implant).

Distribution:

Vd: Not well characterized for implant; distributes into systemic circulation.
ProteinBinding: Not extensively protein bound.
CnssPenetration: Limited

Elimination:

HalfLife: Parent compound has a short half-life (approx. 3-4 hours) but the implant provides sustained release for 12 months.
Clearance: Not precisely quantified for implant; primarily via peptidase degradation.
ExcretionRoute: Metabolites excreted via renal and hepatic pathways.
Unchanged: Minimal
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Pharmacodynamics

OnsetOfAction: Initial transient increase (flare) in LH, FSH, and sex steroids within the first few days, followed by suppression within 2-4 weeks.
PeakEffect: Sustained suppression of LH, FSH, and sex steroids achieved within 4 weeks and maintained for 12 months.
DurationOfAction: 12 months

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If your child exhibits any of the following symptoms, contact their doctor or seek immediate medical attention:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Seizures
Behavior and mood changes, including:
+ Aggressive behavior
+ Crying
+ Depression
+ Emotional ups and downs
+ Restlessness
+ Feeling angry and irritable
+ Suicidal thoughts or actions
Raised pressure in the brain, which may cause:
+ Headache
+ Dizziness
+ Upset stomach
+ Ringing in the ears
+ Eye pain
+ Eyesight problems, such as blurred vision, double vision, or loss of vision

Other Possible Side Effects

Like all medications, this drug may cause side effects. While many people experience no side effects or only mild ones, it's essential to monitor your child's condition. If your child experiences any of the following side effects or if they persist or worsen, contact their doctor:

Irritation at the implant site
If your child is taking this medication to delay puberty, they may experience short-term body odor or signs of puberty, such as:
+ Vaginal bleeding
+ Enlarged breasts
+ Increased pubic hair
+ These symptoms usually occur during the first month of treatment and may be temporary. However, if they persist or are severe, consult your child's doctor.

Reporting Side Effects

This list is not exhaustive, and your child may experience other side effects. If you have questions or concerns, consult your child's doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Signs of continued puberty (e.g., new breast development, menstrual bleeding, testicular enlargement, rapid growth spurt)
  • Severe pain, redness, swelling, or discharge at the implant site
  • Fever
  • Headaches or vision changes
  • Mood swings or behavioral changes
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Before Using This Medicine

Before Giving This Medication to Your Child: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies your child may have to this medication, its components, or other substances, including foods and drugs. Describe the allergic reaction and its symptoms.
Your child's age, particularly if they are under 2 years old, as this medication is not recommended for children younger than 2 years.
If your child is pregnant or may become pregnant, as this medication should not be given during pregnancy.
If your child is breastfeeding or plans to breastfeed, as you should discuss the potential risks and benefits with your doctor.

Additionally, this medication may interact with other medications or health conditions. Therefore, it is crucial to:

Inform your doctor and pharmacist about all medications your child is taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss your child's health problems and any potential interactions with this medication.
Ensure it is safe to give this medication with your child's other medications and health conditions before proceeding.
Never start, stop, or change the dose of any medication your child is taking without first consulting with your doctor.
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Precautions & Cautions

Important Information for Patients Taking This Medication

It is crucial that all of your child's healthcare providers, including doctors, nurses, pharmacists, and dentists, are informed that your child is taking this medication. In rare instances, the implant may dislodge from its original placement site. If this occurs, promptly contact your child's doctor.

Adhere to the follow-up schedule as advised by your child's doctor. Additionally, have your child's blood work checked as directed by their doctor, and discuss any concerns or questions with them.

Please note that this medication may interfere with certain laboratory tests. Therefore, it is essential to inform all of your child's healthcare providers and laboratory personnel that your child is taking this medication.

In some cases, this medication may affect growth in children and teenagers. As a result, they may require regular growth assessments. Consult with your child's doctor to discuss this potential effect.

Special Considerations for Pregnant Patients

If your child is pregnant or becomes pregnant while taking this medication, it is vital to contact their doctor immediately. This medication may pose a risk to the unborn baby if taken during pregnancy.
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Overdose Information

Overdose Symptoms:

  • Overdose with the implant is unlikely due to its controlled release mechanism. Acute overdose symptoms with GnRH agonists are generally not well-defined but could theoretically include an exaggeration of pharmacological effects (initial flare followed by profound suppression).

What to Do:

In case of suspected overdose, contact a poison control center (e.g., 1-800-222-1222) or seek immediate medical attention. Management is supportive and symptomatic.

Drug Interactions

Monitoring

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Baseline Monitoring

Height and Weight

Rationale: To establish baseline growth velocity and monitor treatment efficacy.

Timing: Prior to implant insertion.

Bone Age

Rationale: To assess skeletal maturation and monitor treatment efficacy.

Timing: Prior to implant insertion.

Tanner Staging

Rationale: To assess pubertal development and monitor treatment efficacy.

Timing: Prior to implant insertion.

Basal LH and FSH levels

Rationale: To confirm diagnosis of CPP and establish baseline.

Timing: Prior to implant insertion.

GnRH stimulation test (LH response)

Rationale: To confirm diagnosis of CPP and establish baseline pituitary sensitivity.

Timing: Prior to implant insertion.

Sex steroid levels (Estradiol in girls, Testosterone in boys)

Rationale: To confirm diagnosis of CPP and establish baseline gonadal activity.

Timing: Prior to implant insertion.

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Routine Monitoring

Height and Weight

Frequency: Every 3-6 months

Target: Decreased growth velocity appropriate for chronological age.

Action Threshold: Continued accelerated growth velocity or signs of puberty progression.

Bone Age

Frequency: Every 6-12 months

Target: Stabilization or deceleration of bone age advancement.

Action Threshold: Continued rapid bone age advancement.

Tanner Staging

Frequency: Every 3-6 months

Target: Regression or stabilization of pubertal signs.

Action Threshold: Progression of pubertal signs.

Basal LH levels

Frequency: Every 3-6 months (or as clinically indicated)

Target: Suppressed to prepubertal levels (< 4 mIU/mL or as per lab specific prepubertal range).

Action Threshold: LH levels not suppressed to prepubertal range.

GnRH stimulation test (LH response)

Frequency: Periodically, if basal LH is not sufficiently suppressed or clinical progression occurs.

Target: Peak LH response to GnRH stimulation suppressed to prepubertal levels (< 4 mIU/mL or as per lab specific prepubertal range).

Action Threshold: Peak LH response not suppressed to prepubertal range.

Sex steroid levels (Estradiol in girls, Testosterone in boys)

Frequency: Every 3-6 months (or as clinically indicated)

Target: Suppressed to prepubertal levels.

Action Threshold: Sex steroid levels not suppressed to prepubertal range.

Implant site inspection

Frequency: At each visit

Target: No signs of infection, irritation, or extrusion.

Action Threshold: Redness, swelling, pain, discharge, or extrusion.

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Symptom Monitoring

  • Signs of continued pubertal progression (e.g., breast development, testicular enlargement, pubic hair growth, menstrual bleeding)
  • Headaches
  • Mood changes
  • Hot flashes
  • Vaginal bleeding (in girls, especially during the initial flare)
  • Symptoms of implant site reaction (pain, redness, swelling, itching, infection)

Special Patient Groups

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Pregnancy

Contraindicated in pregnancy. Histrelin can cause fetal harm when administered to a pregnant woman. It is expected to cause adverse effects on pregnancy and fetal development based on its pharmacological action.

Trimester-Specific Risks:

First Trimester: High risk of fetal harm due to hormonal effects.
Second Trimester: High risk of fetal harm due to hormonal effects.
Third Trimester: High risk of fetal harm due to hormonal effects.
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Lactation

Contraindicated during lactation. It is not known whether histrelin is excreted in human milk. Due to the potential for serious adverse reactions in the breastfed infant, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Infant Risk: High (L5) - Potential for serious adverse effects on the infant due to hormonal disruption.
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Pediatric Use

Supprelin LA is specifically indicated for the treatment of central precocious puberty in pediatric patients. Efficacy and safety have been established in this population.

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Geriatric Use

Not indicated for geriatric patients. Central precocious puberty is a pediatric condition.

Clinical Information

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Clinical Pearls

  • Supprelin LA is a long-acting GnRH agonist implant, providing 12 months of continuous therapy for CPP, which can improve adherence compared to daily injections.
  • An initial 'flare' phenomenon (transient increase in LH, FSH, and sex steroids) may occur during the first few weeks of treatment, potentially leading to a temporary worsening of pubertal signs or vaginal bleeding in girls. Patients/parents should be counseled about this.
  • Proper surgical technique for insertion and removal is crucial to ensure efficacy and minimize complications (e.g., infection, extrusion, difficulty locating implant).
  • Regular monitoring of clinical signs of puberty, growth velocity, bone age, and hormonal levels (LH, FSH, sex steroids) is essential to confirm suppression and guide treatment decisions.
  • Treatment with GnRH agonists for CPP is typically continued until the appropriate chronological age for the onset of puberty, or until growth potential is optimized, usually around 11-12 years of age for girls and 12-13 years for boys, but individualized based on clinical judgment.
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Alternative Therapies

  • Leuprolide acetate (e.g., Lupron Depot-PED, Fensolvi, Eligard)
  • Triptorelin (e.g., Trelstar, Triptodur)
  • Other GnRH agonists (e.g., goserelin)
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Cost & Coverage

Average Cost: Very high (e.g., tens of thousands USD) per implant
Insurance Coverage: Specialty Tier (requires prior authorization, often subject to high co-pays/coinsurance)
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General Drug Facts

If your child's symptoms or health issues persist or worsen, it is essential to contact their doctor promptly. To ensure safe use, never share your child's medication with others, and do not administer someone else's medication to your child. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.

Proper disposal of unused or expired medications is crucial. Unless instructed otherwise, do not dispose of medications by flushing them down the toilet or pouring them down the drain. Instead, consult with your pharmacist to determine the best disposal method. Many communities offer drug take-back programs, which provide a safe and environmentally responsible way to dispose of unwanted medications.

For comprehensive information about your child's medication, refer to the accompanying patient information leaflet, if available. If you have questions or concerns about the medication, consult with your child's doctor, nurse, pharmacist, or other healthcare provider. They can provide personalized guidance and support.

In the event of a suspected overdose, immediate action is necessary. Contact your local poison control center or seek medical attention right away. Be prepared to provide critical information, including the name of the medication, the amount taken, and the time of ingestion, to ensure prompt and effective treatment.