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Leuprorelin; Uses, Dosage, Side Effects, Interactions, Pregnan

Leuprolide is a synthetic nonapeptide analogue of gonadotropin-releasing hormone. Leuprolide binds to and activates gonadotropin-releasing hormone (GnRH) receptors. Continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production. This agent reduces testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression.

Leuprorelin is a manufactured version of a hormone used to treat prostate cancer, breast cancer, endometriosis, uterine fibroids, and early puberty.It is given by injection into a muscle or under the skin.Leuprolide belongs to the general class of drugs known as hormones or hormone antagonists. It is a synthetic 9 residue peptide analog of gonadotropin releasing.

Mechanism of Action of Leuprorelin

Leuprorelin acts as an agonist at pituitary GnRH receptors. By interrupting the normal pulsatile stimulation of, and thus desensitizing, the GnRH receptors, it indirectly downregulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels regardless of sex.Leuprolide provides a medical castration for the patient and deprives hormonally-dependent tumors of testosterone or estrogen. During short-term or intermittent therapy, leuprolide has the same stimulatory action as GnRH, but long-term therapy suppresses gonadotropin release from the pituitary gland and reduces steroidogenesis in the ovaries and testicles. Normally, GnRH is released in a pulsatile fashion, but the sustained activity of leuprolide leads to downregulation of the receptor and decreased production of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). In the male, this activity stops testosterone production in the testis. In the female, it stops estrogen production in the ovaries. In patients with endometriosis, this reversible hypoestrogenic state produces symptomatic relief of the pain of endometriosis and decreases the number of endometriotic lesions. Initially, there is a surge of FSH and LH, which can cause a flare reaction in prostate or breast carcinoma. Eventually, the flare reaction will diminish. Total castration can be expected in 1—2 weeks.

Initial stimulation of gonadotropins form the anterior pituitary is followed by prolonged suppression. Gonadotropin release from the anterior pituitary transiently increases estrone and estradiol concentrations in females. However, continuous administration of leuprolide in the treatment of endometriosis produces a fall in estrogens to postmenopausal levels. As a consequence of suppression of ovarian function, both normal and ectopic endometrial tissues become inactive and atrophic. As a result, amenorrhea occurs.

Indications of Leuprorelin

Female infertility
Precocious puberty
Breast cancer, adjuvant
Endometriosis
Hirsutism
Prostate cancer
Uterine fibroids
Uterine leiomyomata
Advanced prostate cancer
Cancer, Breast
Central precocious puberty
Endometriosis
Infertilities
Paraphilia
Uterine Leiomyomas
Symptom recurrence
Treatment of prostate cancer, endometriosis, uterine fibroids, and premature puberty
Treatment of congenital hypogonadotropic hypogonadism
Leuprolide is indicated for the palliative treatment of advanced prostatic cancer, especially as an alternative to orchiectomy or estrogen administration.
Leuprolide is indicated for the management of endometriosis, including pain relief and reduction of endometriotic lesions.

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Contra-Indications of Leuprorelin

Spread of cancer to the spinal column
Diabetes
High cholesterol
Low amount of magnesium in the blood
Low amount of potassium in the blood
Overweight
Depression
High blood pressure
Heart attack
prolonged QT interval on EKG
Chronic heart Failure
Abnormal EKG with QT changes from Birth
Stroke
Liver Problems
Decreased calcification or density of bone
Seizures
High blood sugar
Pregnancy
A Mother who is producing milk and breastfeeding
Obstruction of any part of the urinary tract
Tobacco smoking
Increased cardiovascular event risk

Dosages of Leuprorelin

Strengths: 22.5 mg/3 months; 7.5 mg/month; 45 mg/6 months; 30 mg/4 months; 65 mg; 11.25 mg/month; 15 mg/month; 3.75 mg/month; 11.25 mg/3 months; 30 mg/3 months; 5 mg/mL; 1 mg/0.2 mL; 7.5 mg; 3.75 mg

Prostate Cancer

1 mg injection subcutaneously once a day or
7.5 mg depot IM or depot subcutaneously once a month or
22.5 mg depot IM once every 3 months or
30 mg depot IM once every 4 months or
45 mg subcutaneous injection every 6 months or
65 mg subcutaneous implant once every 12 month

Endometriosis

3.75 mg IM once a month for up to 6 months or 11.25 mg depot every 3 months

Uterine Leiomyomata

3.75 mg IM once a month for up to 6 months or 11.25 mg depot every 3 months

Pediatric Precocious Puberty

Depot injection

Body weight: Less than or equal to 25 kg: 7.5 mg IM once a month
Body weight: Greater than 25 kg to 37.5 kg: 11.25 mg IM once a month
Body weight: Greater than 37.5 kg: 15 mg IM once a month

Uterine fibroids

Adult: As depot preparations: In combination with iron therapy for women with anaemia due to uterine fibroids, 3.75 mg every mth given as a single IM/SC inj or 11.25 mg every 3 mth as IM Inj. Treatment duration: Usually up to 3 mth.

Precocious puberty

Child:

As aqueous soln inj: Initial: 50 mcg/kg daily by SC inj, may be titrated upwards by 10 mcg/kg/day if total down-regulation is not achieved.
As depot preparations: Initial: 0.3 mg/kg/dose (minimum dose: 7.5 mg) given every 4 wk via IM inj; which equates to children ≤25 kg: 7.5 mg; >25-37.5 kg: 11.25 mg and >37.5 kg: 15 mg given every 4 wk.
Maintenance: May titrate dose upwards in steps of 3.75 mg every 4 wk if down-regulation is not achieved. Consider discontinuing therapy before age 11 (females) and age 12 (males).

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Side Effects of Leuprorelin

The most common

More common

Fast or irregular heartbeat
appetite loss
changes in nails
constipation
fatigue
fever
Back pain
dizziness
headache
increased cough
Acid or sour stomach
decreased appetite
Agitation
chest congestion
chest pain
cold sweats
confusion
decreased sexual ability or desire
stomach or abdominal cramps, gas, or pain
trouble sleeping

Less common

bleeding gums
blood in the urine or stools
chest pain
diarrhea
Burning, crawling, itching, numbness, prickling, “pins and needles“, or tingling feelings
difficulty in moving
muscle stiffness
redness of the face, neck, arms and occasionally, upper chest
lack or loss of strength
muscle spasm
difficult or labored breathing
dry mouth
headache
irritability
lack or loss of strength
loose stools
loss of interest or pleasure
muscle stiffness
night sweats
passing gas
stomach discomfort, upset, or pain
swollen joints
trouble concentrating
increased blood pressure

Drug Interactions of Leuprorelin

Leuprolide may interact with following drugs, supplements & may decrease the efficacy of the drug

alpha blockers (e.g., alfuzosin, doxazosin, silodosin, tamsulosin)
anticancer medications (e.g., cabazitaxel, docetaxel, doxorubicin, etoposide, ifosfamide, irinotecan, vincristine)
“azole” antifungal medications (e.g., fluconazole, itraconazole, ketoconazole)
beta-blockers (e.g., atenolol, propranolol, metoprolol)
barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
benzodiazepines (e.g., chlordiazepoxide, clonazepam, diazepam, lorazepam)
calcium channel blockers (e.g., nifedipine, diltiazem, verapamil, amlodipine, felodipine)
bupropion
estrogen and estrogen-containing birth control (women)
medications that promote loss of bone density (e.g., prednisone)
testosterone and androgens (men)
corticosteroids (e.g., dexamethasone, prednisone, methylprednisolone)
cyclosporine
“gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
losartan
macrolide antibiotics (e.g., azithromycin, clarithromycin, erythromycin)
metronidazole
montelukast
norfloxacin
ondansetron
carbamazepine
phenytoin
proton pump inhibitors (PPIs; e.g., esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole)
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine,paroxetine, sertraline)
sildenafil
“statin” anticholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
tadalafil
tamoxifen
tetracycline
theophylline
tocilizumab
tolterodine
tramadol
other selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, sertraline)
5-HT3 antagonists (e.g., granisetron, ondansetron)
tamsulosin
tapentadol
thiazide diuretics (e.g., hydrochlorothiazide, indapamide)
tramadol
tricyclic antidepressants (e.g., nortriptyline, amitriptyline, imipramine,
trimethoprim
other tyrosine kinase inhibitors (e.g., dasatinib, imatinib, nilotinib, sunitinib)
tetracycline
tocilizumab

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Pregnancy & Lactation of Leuprorelin

FDA Pregnancy Category X

Pregnancy

Leuprolide should not be used during pregnancy. A non-hormonal method of birth control (e.g., condom, diaphragm, IUD) should be used during treatment. If you become pregnant during treatment, notify your doctor as soon as possible.

Lactation

It is not known if leuprolide passes into breast milk. Women should not breast-feed while receiving leuprolide treatment due to risk of harm to the infant.