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
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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
more...

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 Category: X

Lactation: excretion in milk unknown; contraindicated

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.

more...
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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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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

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.