This monograph describes a medication approved for use in Canada by the Therapeutic Products Directorate, a division of Health Canada’s Health Products and Food Branch. The medication is not approved by the United States Food and Drug Administration; however, a similar formulation carrying a different generic or brand name might be available in the US.
luteinizing hormone-releasing hormone (LHRH) analogues
- Subcutaneous injection– Initial and maintenance palliative treatment of advanced hormone-dependent prostate cancer (usually given with an anti-androgen).
- Nasal solution– Maintenance palliative treatment of advanced hormone-dependent prostate cancer (usually given with an anti-androgen).
- Nasal solution– Non-surgical treatment of endometriosis (course of treatment 6–9 mo).
Acts as a synthetic analog of endogenous gonadotropin-releasing hormone (GnRH/LHRH). Chronic use results in inhibited secretion of gonadotropin release and gonadal steroid production. The overall effect is due to down-regulation of pituitary LHRH receptors. In males, testosterone synthesis and release is decreased. In females, secretion of estrogen in decreased.
- Decreased spread of advanced prostate cancer.
- Decreased sequelae of endometriosis (pain, dysmenorrhea).
Absorption: Subcut– 70%; intranasal– 1–3%; implant– drug is slowly absorbed over 2–3 mo.
Distribution: Accumulates in liver, kidneys and anterior pituitary lobe; enters breast milk in small amounts.
Metabolism and Excretion: Metabolized in liver, kidneys and by enzymes on membranes in the pituitary gland.
Half-life: Subcut– 80 min; intranasal– 1–2 hr; implant– 20–30 days.
|prostate cancer †||7 days||4 mos||until discontinuation|
|endometriosis ‡(intranasal)||unknown||unknown||duration of treatment|
- Non-hormonal-dependent prostate cancer or previous orchiectomy;
- Females with undiagnosed vaginal bleeding;
- OB: Pregnancy (avoid use);
- Lactation: Avoid breast feeding (small amounts enter breast milk; injection contains benzyl alcohol).
Use Cautiously in:
- Prostate cancer with urinary tract obstruction or spinal lesions;
- Pedi: Safety and effectiveness not established (injection contains benzyl alcohol).
Adverse Reactions/Side Effects
CNS: depression, dizziness
Endo: glucose intolerance
Local: injection site reactions
MS: osteoporosis (long-term use
Misc: transient exacerbation of metastatic prostate cancer or endometriosis
CNS: headache (nasal solution)
EENT: nasal irritation (nasal spray)
GU: ↓ libido, impotence
Derm: hot flushes
Endo: gynecomastia, testosterone flair
MS: bone pain
CNS: headache, weakness, insomnia
GI: constipation, gastrointestinal disorders, nausea
GU: ↓ libido, vaginal dryness, menorrhagia
Derm: hot flushes, acne
Endo: supression of ovulation
MS: back pain
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Risk of serious arrhythmias may be↑ by concurrent amiodarone, disopyramide, dofetilide, flecainide ibutilide, propafenone quinidine, sotalol, antipsychotics (including chlorpromazine) antidepressants (including amitrypline and nortriptyline ), opioids (including methadone ), macrolide anti-infectives (including azithromycin, erythromycin and clarithromycin ), fluoroquinolones (including moxifloxacin ), azole antifungals, 5-HT3 antagonists (including ondansetron ), beta-2 receptor agonists (including salbutamol ), pentamidine, and quinine .
SC (Adults) Initial treatment– 500 mcg every 8 hr for 7 days, Maintenance treatment– 200 mcg daily.
Intranasal (Adults) Maintenance treatment– 400 mcg (200 mcg in each nostril) 3 times daily.
Subcut implant: (Adults) 6.3 mg every 2 mo or 9.45 mg every 3 mo.
Intranasal (Adults) 400 mcg (200 mcg in each nostril) 3 times daily. Treatment is usually continued for 6 mo; not to exceed 9 mo.
Solution for subcutaneous injection (contains benzyl alcohol): 1000 mcg/mL
Intranasal Solution : 1000 mcg/mL (delivers 100 mcg per actuation)
Subcutaneous implant (depot): 6.3 mg (2–mo implant), 9.45 mg (3–mo implant)
- Monitor patients with vertebral metastases for increased back pain and decreased sensory/motor function.
- Monitor intake and output ratios and assess for bladder distention in patients with urinary tract obstruction during initiation of therapy.
- Assess for signs and symptoms of endometriosis before and periodically during therapy. Amenorrhea usually occurs within 8 wk of initial administration and menses usually resume 8 wk after completion.
Lab Test Considerations: Monitor serum testosterone levels every 3 mo during treatment with male patients. When treatment begins, testosterone levels can temporarily markedly ↑ and patients may need another medication to ↓ levels.
- Monitor blood glucose in patients with diabetes frequently; may affect blood glucose levels.
- Verify negative pregnancy test before starting therapy for women.
- Sexual dysfunction
- Disturbed body image
- SC Only use syringes that come with kit for accurate dose. Inject into fatty tissue of abdomen, arm, or leg 3 times/day for 7 days; then daily during maintenance.
- Intranasal When used as maintenance, begin nasal spray in each nostril 3 times daily. If patient also receives decongestant nasal spray, wait 30 minutes to give buserelin spray before or after the decongestant.
- Implant is inserted in subcut tissue of upper abdominal wall every 28 days. Local anesthesia may be used before injection.
- If the implant needs to be removed for any reason, it can be located by ultrasound.
- Intranasal One spray in each nostril 3 times daily for 6–9 mo.
- Inform male patients that they may experience breast swelling and tenderness, decreased libido, hot flashes and sweats, impotence and weight gain. Notify health care professional if these symptoms occur.
- Inform female patients that they may experience decreased libido, constipation, painful sexual intercourse, menopausal symptoms, changes in hair growth. Notify health care professional if these symptoms occur.
- Caution both male and female patients to use contraception while taking this drug. Advise female patient to inform health care professional if pregnancy is suspected. Buserelin can be harmful to a fetus.
- SC Instruct patient in proper technique for self-injection, care and disposal of equipment. Use only syringes included in kit. Instruct patients that syringes may only be used once, and then discarded.
- Intranasal Instruct patient on proper nasal spray technique. Prime pump before use.
- Advise patients that the nasal spray can cause nose bleeds, and may change smell and taste senses.
- Decrease in the spread of prostate cancer.
- Decrease in lesions and pain in endometriosis.
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