Bremelanotide / Oxytocin / Tadalafil Troche
Overview of Bremelanotide / Oxytocin / Tadalafil Troche
Dosage Strength1 mg/100 IU/10 mg
2 mg/100 IU/20 mg
Bremelanotide is an injectable agonist of the melanocortin receptor. It is injected subcutaneously and is approved for the treatment of Hypoactive Sexual Desire Disorder (HSDD), or poor sexual desire, in premenopausal females. It has a distinct method of action that aids in the activation of brain circuits involved in appropriate sexual responses. Safety and efficacy were established in premenopausal females aged 19 to 56 years old with HSDD that causes significant distress or interpersonal difficulty and is NOT due to a co-existing medical or psychiatric condition, relationship problems, or the effects of a medication or other drug substance. Bremelanotide is not approved to treat HSDD in postmenopausal women, men, or to improve sexual performance. In clinical trials, around 25% of patients treated with bremelanotide exhibited an increase of 1.2 or more in their sexual desire score (rated on a scale of 1.2 to 6, with higher values indicating stronger sexual desire), compared to approximately 17% of those taking placebo. Bremelanotide is used “as needed” before to expected sexual activity; women are not required to take the medication on a daily basis. 1
Endogenous oxytocin is a hormone released by the hypothalamic supraoptic and paraventricular nuclei and stored in the posterior pituitary. It promotes uterine smooth muscle contraction during pregnancy and causes milk ejection after milk has been produced in the breast. Mating, parenting, and social behaviors have all been linked to oxytocin. Because oxytocin is released during intercourse in both men and women, it is thought to be important in sexual bonding. The hormone is thought to facilitate the emotional attachment between mother and child in addition to assisting nursing and the birthing process. 2 Oxytocin has also been investigated in autism and may be related to the social and developmental deficits associated with the disorder. 3 In clinical practice, oxytocin is most commonly administered to induce and intensify labor and to reduce postpartum bleeding. Intranasal oxytocin formulations, which were used to increase postpartum milk ejection, are no longer made in the United States. The FDA authorized oxytocin in 1962.
Tadalafil, like sildenafil and vardenafil, is a selective phosphodiesterase (PDE) type 5 inhibitor. It is used orally and is used to treat male erectile dysfunction (ED), pulmonary arterial hypertension (PAH), benign prostatic hypertrophy (BPH), or both erectile dysfunction and BPH. Tadalafil does not suppress prostaglandins like certain impotence medications (e.g., alprostadil). Visual problems have not been recorded with tadalafil, which is more selective for PDE5 than PDE6 in the retina, unlike sildenafil. Tadalafil appears to have a longer duration of action (up to 36 hours) than sildenafil and vardenafil for the treatment of ED. Because PDE inhibitors only enhance erections in the presence of sexual stimulation, tadalafil’s longer duration of action allows for greater spontaneity in sexual engagement. Oral phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are regarded first-line medication in ED treatment guidelines. 4 Tadalafil was in phase II studies for the treatment of female sexual dysfunction, but further research was halted. In November 2003, the FDA approved it for the treatment of male erectile dysfunction (ED), then in January 2008, it was approved for once-daily usage without respect to sexual activity timing. Tadalafil (Adcirca) was approved by the FDA in May 2009 for the treatment of pulmonary arterial hypertension (PAH). Tadalafil-treated participants in clinical studies with pulmonary arterial hypertension (PAH) had greater exercise capacity and less clinical deterioration compared to placebo. Tadalafil was approved by the FDA in October 2011 for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH) as well as the combined treatment of erectile dysfunction and BPH.
1.Vyleesi (bremelanotide) injection package insert. Waltham, MA: AMAG Pharmaceuticals, Inc.; 2020 Oct.
2.Cabanac M, Pfaff DW, Ogawa S, et al. Neural oxytocinergic systems as genomic targets for hormones and as modulators of hormone-dependent behaviors. Results Probl Cell Differ 1999;26:91-105.
3.Modahl C, Green L, Fein D, et al. Plasma oxytocin levels in autistic children. Biol Psychiatry 1998;43:270-277.
4.Montague DK, Jarow JP, Broderick GA, et al. Chapter 1: The management of erectile dysfunction: an AUA update. J Urol 2005;174:230-9.
5.American College of Obstetrics and Gynecology (ACOG). ACOG Practice Bulletin Number 10: Clinical Management Guidelines for Obstetrician-Gynecologists. Induction of labor. Washington, DC: American College of Obstetricians and Gynecologists; November 1999.
6.Cialis (tadalafil) package insert. Indianapolis, IN: Lilly ICOS, LLC; 2011 Oct.
7.Adcirca (tadalafil) package insert. Indianapolis, IN: Lilly ICOS, LLC; 2011 Apr.
8.Mangesi L, Dowswell T. Treatments for breast engorgement during lactation. Cochrane Database Syst Rev. 2010;9:CD006946.
9.Burnett AL, Bivalacqua TJ. Priapism: current principles and practice. Urol Clin N Am 2007;34:631-642.
10.Bortolotti M, Mari C, Giovannini M, et al. Effects of sildenafil on esophageal motility of normal subjects. Dig Dis Sci 2001;46:2301-2306.
11.Pitocin (oxytocin) package insert. Rochester, MI: JHP Pharmaceuticals, LLC; 2014 Sept.
12.Curless RV, Beaumont DM, Sinar EJ, et al. Subarachnoid hemorrhage mimicking acute water intoxication during labour augmented by oxytocin infusion. Br J Clin Pract 1990;44(12):637-638.
13.Padma-Nathan H, McMurray JG, Pullman WE, et al. On-demand IC351 (Tadalafil) enhances erectile function in patients with erectile dysfunction. Int J Impot Res 2001;13:2-9.
14.Pomeranz HD, Bhavsar AR. Nonarteritic ischemic optic neuropathy developing soon after use of sildenafil (Viagra): a report of seven new cases. J Neuroophthalmol 2005;25:9-13.
15.Escaravage GK Jr, Wright JD Jr, Givre SJ. Tadalafil associated with anterior ischemic optic neuropathy. Arch Ophthalmol 2005;123(3):399-400.
16.Bollinger K, Lee MS. Recurrent visual field defect and ischemic optic neuropathy associated with tadalafil rechallenge. Arch Ophthalmol 2005;123(3):400-1.
17.Peter NM, Singh MV, Fox PD. Tadalafil-associated anterior ischaemic optic neuropathy. Eye 2005;19(6):715-7.
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