histrelin (Rx)

Brand and Other Names:Supprelin LA, Vantas
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

implant

  • 50mg (Vantas)
  • Vantas delivers ~50mcg/day

Palliative Treatment of Advanced Prostate Cancer

Vantas: 1 implant SC q12Months (50 mg/implant [delivers ~50 mcg/day])

Renal Impairment

CrCl: 15-60 mL/min: Dose adjustment not necessary

Porphyria (Orphan)

Treatment of acute intermittent porphyria, hereditary coproporphyria, and variegate porphyria

Orphan indication sponsor

  • Anderson, Karl E., M.D.; University of Texas Medical Branch at Galveston, Route J-09, 700 The Strand; Galveston, TX 77550

Administration

Insert SC in inner aspect of upper arm

When removing, confirm that the entire implant has been removed

Dosage Forms & Strengths

implant

  • 50mg (Supprelin LA)
  • Supprelin LA delivers ~65mcg/day

Central Precocious Puberty

Supprelin LA: 1 implant SC q12Months (50 mg/implant [delivers 65 mcg/day])

Administration

Insert SC in inner aspect of upper arm

When removing, confirm that the entire implant has been removed

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Adverse Effects

>10%

Hot flashes (65.5%)

1-10%

Fatigue

Headache

Insomnia

Constipation

Weight gain

Decreased libido

Erectile dysfunction

Gynecomastia

Testicular atrophy

Anemia

Hepatic disorder

Implant site reaction

Renal impairment<2% (important only)

  • Fluid retention, peripheral edema, palpitations, ventricular extrasystoles
  • Various pain
  • Renal calculi

Postmarketing Reports

Cases of pituitary apoplexy (a clinical syndrome secondary to infarction of the pituitary gland) have been reported after the administration of gonadotropin-releasing hormone agonists

Severe liver injury reported; toxicity was reversible with the removal of the implant

General disorders and administration site conditions: Implant breakage

Nervous system disorders: Seizures

Psychiatric Disorders: Emotional lability, including crying, irritability, impatience, anger, and aggression; depression, including rare reports of suicidal ideation and attempt, in children treated for central precocious puberty

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Warnings

Contraindications

Hypersensitivity

Women who may become or are currently pregnant, children

Cautions

Hyperglycemia and an increased risk of developing diabetes have been reported in men receiving GnRH agonists

Cases of spinal cord compression, which may contribute to weakness or paralysis with or without fatal complications, have been reported with GnRH agonists

Convulsions reported in patients receiving GnRH agonists; reports with GnRH agonists have included patients with a history of seizures, epilepsy, cerebrovascular disorders, central nervous system anomalies or tumors, and patients on concomitant medications that have been associated with convulsions such as bupropion and SSRIs; convulsions also reported in patients in the absence of any of the conditions listed

Psychiatric events reported in patients taking GnRH agonists; postmarketing reports with this class of drugs include symptoms of emotional lability, such as crying, irritability, impatience, anger, and aggression; monitor for development or worsening of psychiatric symptoms during treatment

Reports of MI, sudden cardiac death, and stroke in men treated with GnRH agonists

QT prolongation

  • Androgen deprivation therapy may prolong the QT/QTc interval; consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities, and in patients taking drugs known to prolong the QT interval
  • Electrolyte abnormalities should be corrected
  • Consider periodic monitoring of ECG and electrolytes
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Pregnancy & Lactation

Pregnancy

Contraindicated during pregnancy since expected hormonal changes that occur with treatment increase risk for pregnancy loss; the limited data with histrelin use in pregnant women are insufficient to determine a drug-associated risk for major birth defects or adverse developmental outcomes

Reproductive potential

  • Based on findings in animals and mechanism of action, therapy may impair fertility in males of reproductive potential

Animal data

  • Consistent with mechanism of action, animal reproduction studies showed an increase in fetal loss at clinically relevant exposures

Lactation

There are no data on presence of drug in human or animal milk, effects on breastfed infant, or on milk production; absorption and systemic activity are not expected from potential exposure to drug, in breast milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed child from drug or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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Pharmacology

Mechanism of Action

Synthetic nonapeptide analog & agonist of luteinizing hormone-releasing hormone/gonadotropin-releasing hormone (LHRH/GnRH); desensitizes response to endogenous LHRH

Pharmacokinetics

Release Rate: 50-60 mcg/day (Vantas); 65 mcg/day (Supprelin LA)

Peak Plasma: 1.1±0.375 ng/mL

Vd: 58.4±7.86 L (following 500 mcg bolus)

Bioavailability: 92% (adults

Duration: 1 year

Clearance: 174±56.5 mL/min

Protein binding: 70% ± 9%

Half-Life, terminal: 3.9±1 hr

Metabolism: Likely peptide hydrolysis

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Images

BRAND FORM. UNIT PRICE PILL IMAGE
Supprelin LA implant
-
50 mg (65 mcg/day) kit
Vantas implant
-
50 mg (50 mcg/day) kit

Copyright © 2010 First DataBank, Inc.

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Patient Handout

Patient Education
histrelin implant

HISTRELIN - IMPLANT

(HISS-treh-lin)

COMMON BRAND NAME(S): Supprelin LA, Vantas

USES: Histrelin is used in men to treat advanced prostate cancer. It is not a cure. Most types of prostate cancer need the male hormone testosterone to grow and spread. Histrelin works by reducing the amount of testosterone that the body makes. This helps slow or stop the growth of cancer cells and helps relieve symptoms such as painful/difficult urination. Talk to your doctor about the risks and benefits of treatment.Histrelin is also used by children to treat early puberty (central precocious puberty). It helps to slow abnormally fast bone development so that height and growth rate are near normal and to stop or reverse signs of early puberty (such as breast/pubic hair growth in girls, pubic hair growth in boys). Histrelin works by reducing the amount of testosterone in boys and estrogen in girls. This medication is used until the doctor decides it is time for puberty to resume.

HOW TO USE: Read the Medication Guide and, if available, the Patient Information Leaflet that comes with the histrelin implant. If you have any questions, ask your doctor.Your doctor will surgically place the medicated implant under the skin of your upper arm. The implant releases histrelin into your blood slowly and continuously over 12 months. After 12 months, your doctor will remove the implant and replace it with a new one. Consult your doctor for details.It is very important to keep the bandage in place for several days until the surgical incision heals. Keep the incision clean and dry. Avoid bathing and swimming for 24 hours after the procedure. Also avoid any heavy lifting, bumping of the incision site, or physical activity for 7 days after the procedure.When you first start this medication, new or worsening symptoms may occur. This is a normal response by your body to this drug. Such symptoms should get better after the first month of treatment. Girls being treated for early puberty may notice vaginal bleeding or an increase in breast size or pubic hair. Boys being treated for early puberty may notice an increase in pubic hair. Tell the doctor if the symptoms persist or worsen after 1 month.New or worsening symptoms may also occur at the beginning of treatment for prostate cancer. Tell your doctor right away if you experience any of the following serious side effects: bone pain, numbness/tingling/weakness of the arms/legs, blood in the urine, painful/difficult urination, unusual weakness, inability to move. If you have prostate cancer that has spread to the spine or caused problems urinating due to blockage, you may require closer monitoring by your doctor, especially when you first start treatment.

SIDE EFFECTS: Irritation at the implant site (such as bruising, pain, redness), mood swings, or headache may occur. In men using this medication for prostate cancer, hot flashes (flushing), increased sweating, night sweats, tiredness, swelling of the ankles/feet, or constipation may occur. In girls using this medication for early puberty, breast tenderness or abnormal vaginal bleeding may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Rarely, breast tenderness/swelling may occur in men and boys as a result of lowered testosterone levels. Shrinking of the testicles and reduced sexual interest/ability may also occur in men. Talk to your doctor if these effects occur.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.If you are a man using this medication for prostate cancer, tell your doctor right away if you have any serious side effects, including: new/worsening bone pain, easily broken bones, increased thirst/urination.Get medical help right away if you have any very serious side effects, including: chest/jaw/left arm pain, fast/irregular heartbeat, severe dizziness, fainting, weakness on one side of the body, trouble speaking, seizures.Rarely, a very serious problem with the pituitary gland (pituitary apoplexy) has been reported with similar drugs, usually in the first 2 weeks after starting treatment. Get medical help right away if any of these very serious side effects occur: sudden severe headache, sudden severe mental/mood changes (e.g., severe confusion, difficulty concentrating), vision changes, severe vomiting, fainting.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using histrelin, tell your doctor or pharmacist if you are allergic to it; or to similar drugs (e.g., leuprolide); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, heart disease (such as heart attack), stroke, high cholesterol, seizures.If you are a man using this medication for prostate cancer, histrelin may weaken your bones and increase your risk for bone loss (osteoporosis) if used for a long time. Before using this medication, tell your doctor or pharmacist if you have osteoporosis or if you have any of the following risk factors for osteoporosis: long-term alcohol use, smoking, family history of osteoporosis and broken bones, use of certain medications (including corticosteroids such as prednisone, certain anti-seizure drugs such as phenytoin).Histrelin may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using histrelin, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using histrelin safely.Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).This medication must not be used during pregnancy. It may harm an unborn baby. Discuss the use of reliable forms of birth control (such as condoms, birth control pills) with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

OVERDOSE: This implant may be harmful if swallowed. If someone has swallowed it and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Laboratory and/or medical tests (such as blood testosterone level, PSA blood test if using for prostate cancer, blood testosterone/estradiol level, height, bone age if using for early puberty, blood glucose) should be performed periodically to monitor your progress. Consult your doctor for more details.If you have radiology tests (X-rays, MRI), the histrelin implant will not be affected or affect the results of these tests. This implant does not show up on X-ray examination. However, make sure radiology personnel and all your doctors know you use this product.

MISSED DOSE: Rarely, the implant can come out of the upper arm. If this occurs or you suspect that this has occurred, call your doctor. Keep all appointments so your doctor can make sure the implant is in place and working.To help prevent a missed dose, mark your calendar to keep track of when to schedule the placement of your next implant.

STORAGE: Before implantation, the product should be refrigerated. Protect from light and do not freeze.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.