Sexual Dysfunction in Women
Sexual Dysfunction in Women
The prostaglandin alprostadil has been studied in a topical formulation for treatment of FSD. Alprostadil is indicated for male erectile dysfunction as an intracavernous injection or urethral suppository. In females, topical alprostadil has been shown to increase blood flow to the vaginal area by producing smooth muscle relaxation and vasodilation. Adverse reactions of vaginal burning and irritation have been reported.
Apomorphine is a nonselective dopamine receptor agonist that works in the central nervous system (CNS) and is thought to enhance sexual response due to stimuli. For the treatment of FSD, a sublingual dose of 2 to 3 mg is being studied. Reported adverse reactions include nausea, vomiting, headache, and dizziness.
Bremelanotide stimulates melanocortin-4 receptors in the CNS, which increases sexual arousal and desire. Bremelanotide is a synthetic analogue of melanocyte stimulation hormone (MSH). MSH is commonly associated with development of skin pigmentation, protecting the dermis from ultraviolet radiation, and appetite control. The agent is being tested in dosages of 1.25 and 1.75 mg for SC injection. Originally, it was formulated as a nasal spray but in clinical trials was found to increase blood pressure. Adverse reactions associated with SC use include nausea, headache, and flushing.
Bupropion has been shown to improve sexual function in premenopausal women with HSDD, as reported in two studies. Bupropion sustainedrelease 150 mg daily and 300 to 400 mg daily yielded satisfactory responses in these studies. Women reported that they were satisfied with the treatment and that bupropion increased sexual arousal, orgasm completion, and sexual satisfaction. The mechanism of action of bupropion has not been clearly defined, but it is thought to facilitate dopamine and norepinephrine neurotransmission, possibly by inhibiting the reuptake of neurotransmitters.
DHEA and its sulfate ester DHEA-S are steroid hormones produced in the adrenal glands, liver, and testes in men. DHEA is metabolized to androstenedione, the precursor to androgen and estrogen. Levels of DHEA usually decline with age. DHEA is available as an OTC supplement and has been reported to increase libido in postmenopausal women. DHEA supplementation is believed to change the circulating androgen-estrogen ratio in a gender-specific manner. Therefore, the supplementation of DHEA in women increases the concentration of testosterone more than estrogen.
Oral administration of DHEA has been studied with variable results for the treatment of vaginal atrophy and HSDD. An oral dosage of 50 to 1,600 mg daily has been studied with mixed results. An intravaginal 0.25% to 1% cream is being evaluated because oral dosages have been linked with acne and hirsutism.
Pharmacists should be aware of adverse effects associated with DHEA, especially since it is available as an OTC supplement as tablets or capsules in strengths of 25 and 50 mg. A daily dosage of 50 mg is associated with mildto- low side effects. Dosages of 200 mg per day or greater are linked to various adverse effects such as acne, hirsutism, hair loss, voice deepening, insulin resistance, changes in menstrual pattern, hepatic dysfunction, abdominal pain, and hypertension.
PDE5 inhibitors such as sildenafil, tadalafil, and vardenafil have been successful for treatment of male erectile dysfunction. The use of PDE5s for treatment of sexual dysfunction in women has not been as favorable. PDE5s may be efficacious in women with FSD secondary to the use of SSRIs and may additionally be effective in women diagnosed with sexual interest/arousal disorder.
Pipeline Drugs
Alprostadil
The prostaglandin alprostadil has been studied in a topical formulation for treatment of FSD. Alprostadil is indicated for male erectile dysfunction as an intracavernous injection or urethral suppository. In females, topical alprostadil has been shown to increase blood flow to the vaginal area by producing smooth muscle relaxation and vasodilation. Adverse reactions of vaginal burning and irritation have been reported.
Apomorphine
Apomorphine is a nonselective dopamine receptor agonist that works in the central nervous system (CNS) and is thought to enhance sexual response due to stimuli. For the treatment of FSD, a sublingual dose of 2 to 3 mg is being studied. Reported adverse reactions include nausea, vomiting, headache, and dizziness.
Bremelanotide
Bremelanotide stimulates melanocortin-4 receptors in the CNS, which increases sexual arousal and desire. Bremelanotide is a synthetic analogue of melanocyte stimulation hormone (MSH). MSH is commonly associated with development of skin pigmentation, protecting the dermis from ultraviolet radiation, and appetite control. The agent is being tested in dosages of 1.25 and 1.75 mg for SC injection. Originally, it was formulated as a nasal spray but in clinical trials was found to increase blood pressure. Adverse reactions associated with SC use include nausea, headache, and flushing.
Bupropion
Bupropion has been shown to improve sexual function in premenopausal women with HSDD, as reported in two studies. Bupropion sustainedrelease 150 mg daily and 300 to 400 mg daily yielded satisfactory responses in these studies. Women reported that they were satisfied with the treatment and that bupropion increased sexual arousal, orgasm completion, and sexual satisfaction. The mechanism of action of bupropion has not been clearly defined, but it is thought to facilitate dopamine and norepinephrine neurotransmission, possibly by inhibiting the reuptake of neurotransmitters.
Dehydroepiandrosterone (DHEA)
DHEA and its sulfate ester DHEA-S are steroid hormones produced in the adrenal glands, liver, and testes in men. DHEA is metabolized to androstenedione, the precursor to androgen and estrogen. Levels of DHEA usually decline with age. DHEA is available as an OTC supplement and has been reported to increase libido in postmenopausal women. DHEA supplementation is believed to change the circulating androgen-estrogen ratio in a gender-specific manner. Therefore, the supplementation of DHEA in women increases the concentration of testosterone more than estrogen.
Oral administration of DHEA has been studied with variable results for the treatment of vaginal atrophy and HSDD. An oral dosage of 50 to 1,600 mg daily has been studied with mixed results. An intravaginal 0.25% to 1% cream is being evaluated because oral dosages have been linked with acne and hirsutism.
Pharmacists should be aware of adverse effects associated with DHEA, especially since it is available as an OTC supplement as tablets or capsules in strengths of 25 and 50 mg. A daily dosage of 50 mg is associated with mildto- low side effects. Dosages of 200 mg per day or greater are linked to various adverse effects such as acne, hirsutism, hair loss, voice deepening, insulin resistance, changes in menstrual pattern, hepatic dysfunction, abdominal pain, and hypertension.
Phosphodiesterase Type 5 (PDE5) Inhibitors
PDE5 inhibitors such as sildenafil, tadalafil, and vardenafil have been successful for treatment of male erectile dysfunction. The use of PDE5s for treatment of sexual dysfunction in women has not been as favorable. PDE5s may be efficacious in women with FSD secondary to the use of SSRIs and may additionally be effective in women diagnosed with sexual interest/arousal disorder.
