Leuprolide acetate depot

In a randomized, placebo-controlled study in women who received leuprolide acetate depot 11.25 mg intramuscularly with tibolone 2.5 mg/day (n = 36), leuprolide acetate depot 11.25 mg with placebo (n = 37), or a placebo injection with placebo tablets (n = 39), irritable bowel syndrome related to the menstrual cycle improved in those who received leuprolide (5). There were hot flushes in those who took leuprolide compared with placebo no data were given about the frequency of hot flushes, but there were no withdrawals because of this symptom. Amenorrhea also occurred. Both flushing and amenorrhea are expected adverse effects of leuprolide. 

The use of gonadorelin analogues is commonly associated with reduced bone mineral density. In 50 premenopausal women with uterine leiomyomas who received leuprolide acetate depot 3.75 mg every 28 days for 18 cycles with raloxifene 60 mg/day, there was a reduction in leiomyoma size with no significant change in bone mineral density or markers of bone metabolism [86],... 

Premenopausal women who received leuprolide acetate depot 3.75 mg every 28 days for 6 cycles had slightly but statistically significant higher concentrations of total cholesterol, FDL-cholesterol, and HDL-cholesterol, and increased insulin resistance (64). Whether these changes are clinically significant is not known. 

Hornstein MD, Surrey ES, Weisberg GW, Casino LA. Leuprolide acetate depot and hormonal add-back in endometriosis A 12-month study. Lupron Add-Back Study Group. Obstet Gynecol 1998 91 16-24. 

Those treatments, like the leuprolide acetate depot, will also likely spin premenopausal women right into pseudomenopause. But are the side effects similar ... 

There are no comparative trials of LHRH agonists, so the choice is usually based on cost (Table 65-1) and on patient and physician preference. Leuprolide acetate is administered daily. Leuprolide depot and goserelin acetate implant can be administered monthly, or every 12 or 16 weeks. 

Lupron Depot PLA Leuprolide acetate Prostate cancer, endometreosis... 

Add-back estrogen replacement reduces the frequency and severity of these symptoms without apparently compromising the effectiveness of gonadorelin in women with endometriosis (19,27). In a randomized, multicenter, double-blind comparison of intranasal nafarelin twice daily and depot leuprolide acetate monthly for 6 months in 192 young women with endometriosis, nafarelin caused fewer hypoestrogenic symptoms, although the... 

In 47 children treated with depot leuprolide acetate for precocious puberty for 2 years, bone mineral density decreased significantly and markers of bone turnover increased significantly during treatment but were normal for age 2 years after treatment was withdrawn (54). 

Neely, E.K. Hintz, R.L. Parker, B. Bachrach, L.K. Cohen, P. Olney, R. Wilson, D.M. Two-year results of treatment with depot leuprolide acetate for central precocious puberty. J. Pediatr. 1992, 121 (4), 634—640. 

Leucovorin Wellcovorin -GlaxoSmithkIine, and others) Leuprolide acetate (Lupron, Lupron Depot - TAP, and others)... 

Leuprolide acetate, a synthetic nonapeptide, is prescribed for the treatment of metastatic prostate cancer and endometriosis. Leuprolide acetate is presented in a number of injectable dosage forms including Lupron sterile solution for subcutaneous administration (1 and 5 mg mL 1) and Lupron depot controlled release formulation for intramuscular injection (3.75 and 7.5 mg). Zheng and Fulu [106] have evaluated the in vivo effect of leuprolide loaded micro emulsions on the genital organs of the male and female rats. In the preliminary pharmacokinetic studies, oral microemulsions of leuprolide administration resulted in 10-fold higher plasma levels of leuprolide as compared to that of saline solution (Fig. 9.4). 

Polymeric micropsheres, particularly those prepared from the biodegradable polylactide/ polyglycolide polymers, have been widely investigated as a means to achieve sustained parenteral drug delivery. The advantage of formulating the polymeric matrix as microspheres is the ability to administer them via a conventional needle and syringe as a suspension formulation, rather than as an implant (see below). Lupron depot formulations are available which can provide therapeutic blood levels of leuprolide acetate for up to four months. These products are presented as lyophilized polylactic acid microspheres which are reconstituted to form a suspension prior to administration. 

Leuprolide acetate/poly(DL-lactide-co-glycolide) Lupron Depot , Takeda Chemical Industries Endometriosis... 

Implantable delivery systems offer a number of advantages over more traditional delivery routes, particularly for biological macromolecules (including peptides, proteins, and oligonucleotides). Some specific delivery mechanisms to date include polymer depots (e.g., Gliadel Wafer, prolifeprosan 20 with carmustine implant) and osmotic pumps (e.g., Viadur leuprolide acetate implant). 

The W /0/W emulsion technique has been also employed to encapsulate variety of drug compounds, including adriamycin and tobramycin, leuprolide acetate (Lupron Depot )15,20, nucleotides, thyrotropin-releasing hormone, growth hormone, RNA, and calcitonin. ... 

Microsphere PLA Lupron Depot Leuprolide acetate Peptide hormone cancer and Alzheimer s... 

Leuprolide acetate (S) Lupron Depot Takeda-Abbott... 

Okada and co-workers (1988,1989,1991) and Ogawa etal. (1988) have also described a 75 25 PLGA microencapsulated 30-day release system for the delivery of another LHRH analog leuproUde acetate [(D-Leu , Pro NEt)-LHRH Lupron Depot , Takeda-Abbott], Their results indicate that a single injection of microcapsules maintains constant and effective serum levels of the analog for one month. Sufficient therapeutic efficacy in the treatment of advanced prostatic cancer has also been shown for leuprolide acetate, and the product has recently been approved for use by the U.S. Food and Drug Administration (Lupron Depot , 7.5mg PDR, 1994). This treatment has also shown to cause a dramatic regression of... 

Controlled Release of Peptides and Proteins. Sustained release applications are especially useful for proteins/peptides because of their short half-lives (62). This concept was first utilized commercially in Lupron Depot, which was introduced as a sustained release formulation of a lutenizing hormone-releasing hormone (LHRH), leuprolide acetate, with poly(lactic acid) as the polymer (63). Following the success of Lupron Depot, other sustained release formulations of LHRH analogues have also been commercialized, including Zoladex wherein the LHRH peptide is encapsulated in PLA-extruded rods, and Trelstar depot wherein the peptide is encapsulated in PLGA polymer matrices. 

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