Testosterone is a sex hormone from the androgen group. In women, endogenous androgens are responsible for the maintenance of the female genital system: nipples, labia majora, and the clitoris.
Intranasally administered testosterone may increase sexual stimulation and motivation.
Testosterone is commonly compounded as a 0.6mg/spray solution for intranasal administration.
In women, endogenous androgens are responsible for the maintenance of the female genital system (nipples, labia majora, and in particular the clitoris), maintenance of bone density, muscle size and strength, mood, and the health of the cardiovascular system. The daily production of testosterone in young healthy women approximates 250mcg, an amount that is 20-30 times lower than what is produced in men. Half of the testosterone comes from the conversion of DHEA and androstenedione in fat and skin tissues, one-fourth is made by the ovaries, and another fourth is made by the adrenal glands.
The decrease of testosterone in women occurs earlier than in men, and initially at a greater rate as well. The average testosterone blood level in women of age 40 is low, less than half of that in women of 21 years of age. Based on the known effects of androgens, it is likely that long-term testosterone deficiency predisposes women to depression, anxiety, joint disorders, osteoporosis, atherosclerosis, loss of libido, and impaired sexual function.
Age-related decline in androgen levels may also be associated with decreased amygdala reactivity, which is a part of a larger emotion circuitry important for the identification of the emotional significance of stimuli, the generation of an affective response, and emotion regulation.
Testosterone administered intranasally may activate central sexual mechanisms thereby increasing salience of sexual stimuli, which affects central sexual stimulation and can thereby increase sexual motivation.
Intranasal testosterone has been studied for use in females with:
- Female Organismic Disorder (FOD).2,3,4
When comparing intranasal route versus intravenous route administration of testosterone, Banks, et al, found that intranasal administration delivers testosterone systemically, including the brain, especially the olfactory bulb, hypothalamus, striatum, and hippocampus. Whole brain testosterone levels were twice as high with via intranasal than intravenous.1
In a study by van Gorsel, et al, patients treated with intranasal testosterone had significantly higher vaginal pulse amplitude (VPA) response as soon as 30 minutes following administration in FOD patients.3
In a Phase II clinical trial by Laan, et al, intranasal testosterone was studied for Hyposexual Desire Disorder (HSDD) and Female Orgasmic Disorder (FOD) in 59-patients. Of the patients diagnosed with FOD and treated with intranasal testosterone, 40% of the treatment group reported experiencing an orgasm or sensations indicative of an orgasm. Women treated with intranasal testosterone reported more intense feelings of sexual arousal after stimulation and showed an increased genital response.4
Testosterone dosed intranasally has been studied at doses ranging from 0.6mg – 1.8mg daily to three times daily.3,4
Testosterone nasal spray may be used 30-minutes to 4.5-hours before sexual activity.
Vaginal pulse amplitudes are found to increase in as little as 30 minutes after administration in higher dosed groups as compared to 4.5h in lower dosed groups in women suffering from female orgasmic disorder.3
General: Headache, rhinorrhea, epistaxis, nasal discomfort, nasopharyngitis, bronchitis, upper respiratory tract infection, sinusitis, or nasal scabbing.
Secondary sexual side effects: Facial hair, acne, voice changes, clitoral enlargement
Skin and appendages: Hirsutism, male pattern baldness, and acne
Fluid and electrolyte disturbances: Retention of sodium, chloride, water, potassium, calcium and inorganic phosphates
Gastrointestinal: Nausea, cholestatic jaundice, alterations in liver tests, rare hepatocellular neoplasm and peliosis hepatis
Hematologic: Suppression of clotting factors II, V, VII, and X, bleeding in patients on concomitant anticoagulation therapy, and polycythemia
Vascular disorders: Venous thrombosis
Miscellaneous: Rarely anaphylactic reactions
A possible increased risk of heart attack, stroke, or death has been reported. Edema, with or without congestive heart failure, may occur in patients with preexisting cardiac, renal or hepatic disease; discontinuation and diuretic therapy may be required.
Increased risk of hypercalcemia and associated hypercalciuria in cancer patients; monitoring recommended Dyslipidemia may occur; monitoring recommended; dosage adjustment or discontinuation may be warranted.
Venous thromboembolic events, including DVT and pulmonary embolism, have been reported; monitoring recommended; discontinue use if suspected.
Polycythemia may occur; monitoring recommended and dose adjustment may be warranted.
Osteolysis may be stimulated by periods of immobilization and can result in hypercalcemia.
A possible increased risk of heart attack, stroke, or death has been reported with testosterone use.
Secondary exposure in children may result in virilization, inappropriate changes in genital size, and other serious adverse effects; discontinue use until cause of virilization is determined.
Use is not recommended in patients with mucosal inflammatory disorders, sinus disease, or a history of nasal disorders, nasal or sinus surgery, nasal fracture (within last 6 months), or nasal fracture resulting in deviation of the anterior nasal septum. Increased risk of sleep apnea in patients with obesity or chronic lung diseases.
Pregnancy: Testosterone is a Category X medication. It should not be prescribed to pregnant women, or women planning to become pregnant.
Breastfeeding: Infant risk has been demonstrated with testosterone use. Avoid breastfeeding.
- Undiagnosed Vaginal Bleeding
- Breast Cancer
- Pretreatment endogenous levels >40ng/dl
Androgens may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may require reduction in order to maintain satisfactory therapeutic hypoprothrombinemia.
In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, insulin requirements.
Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone.
Circulating testosterone is chiefly bound in the serum to sex hormone binding globulin (SHBG) and albumin. The albumin-bound fraction of testosterone easily dissociates from albumin and is presumed to be bioactive. The amount bound to SHBG is not considered to be biologically active. SHBG binding capacity is high in pre-pubertal children, declines during puberty and adulthood, and increases again during the later decades of life. Approximately 40% of testosterone in plasma is bound to SHBG, 2% remains unbound (free) and the rest is bound to albumin and other proteins.
About 90% of the dose of testosterone is excreted renally as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6 percent of a dose is excreted in feces, mostly in the unconjugated form. Inactivation of testosterone occurs primarily in the liver. Testosterone is metabolized to various 17-keto steroids through 2 different pathways.
There are considerable variations of the half-life as reported in the literature, ranging from 10-100 minutes.
- Keep tightly closed after each use.
- Keep out of reach from children.
- Store in a cool and dry place.
- Banks WA, Morley JE, Niehoff ML, Mattern C. Delivery of testosterone to the brain by intranasal administration: comparison to intravenous testosterone. J Drug Target. 2009;17(2):91-97. doi:10.1080/10611860802382777
- Both S. Recent Developments in Psychopharmaceutical Approaches to Treating Female Sexual Interest and Arousal Disorder. Curr Sex Health Rep. 2017;9(4):192-199. doi:10.1007/s11930-017-0124-3
- Gorsel H, Laan, Tkachenko NM, Dickstein J, Kreppner W. Pharmacokinetics and pharmacodynamic efficacy of testosterone intranasal gel in women with hypoactive sexual desire disorder and anorgasmia. J Sex Med. 2012;9(3):162–180.
- Laan E, Nievaart M, Tkachenko NM, Dickstein J, Kreppner W, Lunsen RHW. Randomized, placebo controlled, five-arm parallel group study to assess efficacy of TBS-2 intranasal gel using vibrotactile stimulation combined with visual sexual stimulation in women with anorgasmia. J Sex Med. 2013;10:165–166.
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