Leuprolide dosage

Several randomized trials have demonstrated that leuprolide and goserelin are effective agents when used alone in patients with advanced prostate cancer.19 Response rates around 80% have been reported, with a lower incidence of adverse effects compared with estrogens.19 There are no direct comparative trials of the currently available LHRH agonists or the dosage formulations, but a recent meta-analysis reported that there is no difference in efficacy or toxicity between leuprolide and goserelin. Therefore, the choice between the two usually is made based on cost and patient and physician preference for a dosing schedule. 

Treatment can be carried out with injections of leuprolide or nasal application of nafarelin. Leuprolide treatment is usually initiated at a dosage of 0.05 mg/kg body weight injected subcutaneously daily and then adjusted on the basis of the clinical response. Pediatric depot preparations of leuprolide are also available. The recommended initial dosage of nafarelin for central precocious puberty is 1.6 mg/d. This is achieved with two-unit dose sprays (each spray contains 0.1 mL, 0.2 mg) into each nostril twice daily. Treatment with a GnRH agonist is generally continued to age 11 in females and age 12 in males. 

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). 

In this section, the pharmacokinetics of clinically important peptide/protein drugs, such as insulin, EPO, G-CSF, interferon, growth hormone, leuprolide, desmopressin, and antibodies, are described in relation to their administration routes and formulations (i.e., dosage forms). 

In the 1980s numerous impediments were overcome to provide controlled-release peptide dosage forms, which has changed the paradigm of drug delivery for many of these important drugs, i.e., particularly leuprolide for treatment of prostate cancer. Over the last 10 years, numerous impediments to controlled-release of proteins have been similarly identified, and several solutions demonstrated, as evidenced by the marketed Nutropin Depot formulation for growth hormone, and some of the examples described... 

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