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Pharmacology: The hormonal components of Lusienne inhibit ovulation by suppressing gonadotropin release. Secondary mechanisms which may contribute to the effectiveness of Lusienne as a contraceptive include changes in the cervical mucus (which increase the difficulty of sperm penetration) and in the endometrium (which reduce the likelihood of implantation).
Pharmacokinetics: Ethinyl estradiol and Gestodene (Lusienne) are rapidly and almost completely absorbed from the gastrointestinal tract.
Peak plasma levels of each drug are reached within 1-2 hours. Post maximum concentration curves show 2 phases with half-lives of 1 and 15 hours in the case of Gestodene (Lusienne) and 1-3 and approximately 24 hours in the case of ethinyl estradiol.
After oral administration, Gestodene (Lusienne), unlike ethinyl estradiol is not subject to first-pass metabolism. Following oral administration, Gestodene (Lusienne) is completely bioavailable, ethinyl estradiol about 40%.
Gestodene (Lusienne) is extensively plasma protein bound to sex hormone binding globulin (SHBG). Ethinyl estradiol is bound in plasma to albumin and enhances the binding capacity of SHBG.
The elimination half-life of ethinyl is approximately 25 hours. It is primarily metabolized by aromatic hydroxylation but a wide variety of hydroxylated and methylated metabolites are formed, and these are present both free and as conjugates with glucuronide and sulfate. Conjugated ethinyl estradiol is excreted in bile and subject to enterohepatic recirculation. About 40% of the drug is excreted in the urine and 60% is eliminated in the feces.
The elimination half-life of Gestodene (Lusienne) is approximately 16-18 hours after multiple oral doses. The drug is primarily metabolized by reduction of the A ring followed by glucuronidation. About 50% of Gestodene (Lusienne) is excreted in the urine and 33% is eliminated in the feces.
Cycle Control in Clinical Trials: In clinical trials with Lusienne including 14,281 cycles of treatment, the overall incidence of spotting was 5% and breakthrough bleeding was 0.7%.
Amenorrhea (absence of expected withdrawal bleeding), occurred in 68 of 14,281 treatment cycles, an incidence of 0.5%.
Influence of Missed Tablets: Table 2 shows that the rate of intermenstrual bleeding is increased by intake errors, ie when one or more tablets are omitted.
Lusienne is an amphetamine that stimulates neurons to release or maintain high levels of a particular group of neurotransmitters known as catecholamines; these include dopamine and norepinephrine. High levels of these catecholamines tend to suppress hunger signals and appetite. Lusienne (through catecholamine elevation) may also indirectly affect leptin levels in the brain. It is theorized that diethylpropion can raise levels of leptin which signal satiety. It is also theorized that increased levels of the catecholamines are partially responsible for halting another chemical messenger known as neuropeptide Y. This peptide initiates eating, decreases energy expenditure, and increases fat storage.
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Information checked by Dr. Sachin Kumar, MD Pharmacology
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