Plenaxis

abarelix

(a-ba-re-lix) ,

Plenaxis

(trade name)

Classification

Therapeutic: antineoplastics
Pharmacologic: gnrh antagonist
Pregnancy Category: X

Indications

Advanced prostate cancer when LHRH agonists are inappropriate or surgical castration is refused and there is risk of neurologic compromise from metastatic disease, ureteral/bladder obstruction due to local/metastatic disease or severe metastatic bone pain unresponsive to adequate opioid analgesia.

Action

Directly and competitively blocks pituitary GnRH receptors, thereby suppressing production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This results in decreased production of testosterone by the testes, which is not accompanied by an initial increase in testosterone.

Therapeutic effects

Suppressed spread of metastatic prostate cancer, with decreased neurologic complications, bladder outlet obstruction and need for opioid analgesics.

Pharmacokinetics

Absorption: Well absorbed following IM administration.
Distribution: Extensively distributed.
Protein Binding: 96–99%.
Metabolism and Excretion: Metabolized by hydrolysis of peptide bonds; 13% excreted unchanged in urine.
Half-life: 13.2 days.

Time/action profile (decrease in testosterone levels)

ROUTEONSETPEAKDURATION
IM2 days3 days (blood level)1 mo*
*Testosterone levels at mo reflect medical castration

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Adult females or children.
Use Cautiously in: Patients with pre-existing QTc prolongation or concurrent use of Class IA antiarrhythmics (amiodarone, sotalol); Weight >225 pounds (decreased effectiveness over time).

Adverse Reactions/Side Effects

Central nervous system

  • dizziness (most frequent)
  • fatigue (most frequent)
  • headache (most frequent)
  • sleep disturbances (most frequent)

Cardiovascular

  • peripheral edema (most frequent)
  • prolonged QTc interval

Gastrointestinal

  • constipation (most frequent)
  • diarrhea (most frequent)
  • nausea (most frequent)
  • increased transaminases

Genitourinary

  • dysuria (most frequent)
  • urinary frequency (most frequent)

Dermatologic

  • hot flushes (most frequent)

Endocrinologic

  • breast enlargement/nipple tenderness (most frequent)

Musculoskeletal

  • back pain (most frequent)

Miscellaneous

  • allergic reactions
  • decreased bone mineral density

Interactions

Drug-Drug interaction

None noted.

Route/Dosage

Intramuscular (Adults) 100 mg on Day 1, 15, and 29 and then every 4 wk thereafter.

Availability

Sterile powder for suspension (requires reconstitution): 113 mg/vial (yields 100 mg/2 mL dose)

Nursing implications

Nursing assessment

  • Observe patient for at least 30 min following injection for immediate-onset systemic allergic reactions (urticaria, pruritus, hypotension, syncope). Treat symptomatically; if hypotension or syncope occur measures such as leg elevation, oxygen, IV fluids, antihistamines, corticosteroids, and epinephrine should be used. Risk of reaction increases with duration of treatment.
  • Lab Test Considerations: Measure serum total testosterone concentrations just prior to administration on Day 29 and every 8 wk thereafter. Overall effectiveness may decrease with increased duration of therapy.
    • May cause ↑ serum AST and ALT levels. Monitor serum transaminase levels prior to and periodically during therapy.
    • Monitor serum PSA levels periodically during therapy.
    • May cause slight ↓ in hemoglobin.
    • May cause ↑ in serum triglycerides.
    • May cause ↓ in bone mineral density.

Potential Nursing Diagnoses

Chronic pain (Side Effects)

Implementation

  • Abarelix should be prescribed only by physicians enrolled and qualified by the Plenaxis User Safety Program.
  • Intramuscular: Prior to reconstitution, shake vial. Hold vial at 45° angle and tap lightly on table to break up any caking. Using enclosed 18 gauge needle and 3 cc syringe, withdraw 2.2 mL of 0.9% NaCl. Discard remaining diluent. With vial upright, insert needle all the way into vial and inject diluent quickly. Before withdrawing needle, remove 2.2 mL of air. Shake vial immediately for approximately 15 seconds. Allow vial to stand for approximately 2 min. Tap vial to reduce foaming and swirl vial occasionally. Do not reinject air into vial. Locate a second injection spot on stopper and insert the 18 gauge needle. Invert vial and draw up some of the suspension into syringe and reinject into remaining solids in vial without removing needle. Repeat until all solids are dispersed. Swirl vial before withdrawal and withdraw entire contents (at least 2 mL) by positioning needle in vial at a 45° angle. Pull the plunger back to recover residual suspension in needle, then exchange needle with the enclosed 22 gauge 1 1/2 inch injection needle. Administer the entire reconstituted suspension IM immediately. Must be administered within 1 hr of reconstitution.

Patient/Family Teaching

  • Inform patient of purpose and risks of abarelix.
  • May cause dizziness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
  • Advise patient to notify physician immediately if symptoms of immediate-onset systemic allergic reaction occur.

Evaluation/Desired Outcomes

  • Decreased serum testosterone levels resulting in suppressed spread of metastatic prostate cancer, with decreased neurologic complications, bladder outlet obstruction and need for opioid analgesics.

Plenaxis

a trademark for abarelix.
References in periodicals archive ?
Plenaxis is a novel product - it is the first in a new class of hormonal products (the GnRH blockers) and it is used to treat advanced and metastatic prostate cancer.
In May, IURTC leaders honored Roger Roeske, professor in the Department of Biochemistry and Molecular Biology at the IU School of Medicine in Indianapolis, for research that led to Plenaxis, a drug therapy for prostate cancer patients.
Protein drug candidates (a) Drug brand name Drug manufacturer/ (generic name) developer, location Plenaxis (Abarelix-Depot, Praecis Pharmaceuticals, PPI-149) Inc.
Results from the clinical trial supporting this indication were presented at the 2001 Annual Meeting of the American Society of Clinical Oncology, and suggest that patients, when placed on Plenaxis therapy, were able to avoid surgical castration (orchiectomy), the study's primary clinical goal (endpoint).
The Food and Drug Administration previously rejected Praecis' application to market Plenaxis, a prostate cancer drug that was developed in conjunction with Amgen.
Product Innovations/Introductions II-66 Speciality European Pharma Introduces Plenaxis II-66 Actavis Unveils Bicalutamide Tablets for Prostate Cancer in the European Markets II-66 Artemis to Introduce IGRT II-66 Immunomedics Introduces Immunotoxin for Treatment of Prostate and Lung Cancer II-66 Barr Unveils Generic Version of Proscar[R] Tablets II-67 IRX Therapeutics to Develop Vaccine for Prostate Cancer II-67 Actavis Introduces New Generic Drugs in Europe II-67 Robot-Assisted Radical Prostatectomy for Treatment of Prostate Cancer II-67
Product Innovations/Introductions II-66 Speciality European Pharma Introduces Plenaxis II-66 Actavis Unveils Bicalutamide Tablets for Prostate Cancer in the European Markets II-66 Artemis to Introduce IGRT II-66 Immunomedics Introduces Immunotoxin for Treatment of Prostate and Lung Cancer II-66 Barr Unveils Generic Version of Proscar(R) Tablets II-67 IRX Therapeutics to Develop Vaccine for Prostate Cancer II-67 Actavis Introduces New Generic Drugs in Europe II-67 Robot-Assisted Radical Prostatectomy for Treatment of Prostate Cancer II-67 7.
On stopping treatment with Plenaxis, testosterone levels rapidly recover while disease activity remains under control for some time.
to develop Plenaxis, an experimental treatment for prostate cancer.
Avodart, Zoladex, Proscar, Casodex, Taxotere, Satraplatin, Plenaxis, EULEXIN, Trelstar Depot, Trelstar LA, Viadur, Gleevec, Avastin, Herceptin, Atrasentan, Acapodene, Actimid, OSI-461, Revimid, Eladem, GTI-2501, ILX-651, calcitrol, Genasense, Provenge , GVAX, SGN-15, Thalomid, Velcade, Lupron Depot, Histrelin, Eligard, ILX651, Vitaxin, J591, CG7870, BBR-3576, PCK3145, Leuvectin, Leuprolide, ProMaxx-100, Osaterone, Prinomastat, BLP25, Metaret, Chimax, Drogenil, Flutamide, EULEXIN, Onconase, IM862, MDX-010, Erbitux, Eladem, GTI-2040, Apomine, Eflornithine, Doxil, GTI-2501, Thalidomide, TG4010, KRX-0401, Yondelis, TRICOM Vaccine, Zarnestra
On December 6, 2004, Praecis provided an update on the Company's commercialization of Plenaxis in the United States.
The complaint alleges that Praecis misrepresented or failed to disclose the following facts: that the distribution of Plenaxis had been severely restricted by the FDA; that Praecis had failed to establish effective messaging to educate physicians about Plenaxis' indication and the appropriate patient population; and that despite impressive enrollment numbers in the PLUS program, Praecis had difficulties convincing physicians to prescribe Plenaxis due to uncertainty over its use and concerns over reimbursement.