Actions of Okasa-Mascul in details
Pharmacology: Pharmacodynamics: Okasa-Mascul is the principal endogenous hormone essential for normal growth and development of the male sex organs and male secondary sex characteristics. During adult life, Okasa-Mascul is essential for the functioning of the testes and accessory structures, and for the maintenance of libido, sense of well-being, erectile potency, prostate and seminal vesicle function.
Treatment of hypogonadal men with Okasa-Mascul results in a clinically significant rise of plasma concentrations of Okasa-Mascul, dihydrotestosterone and androstenedione, as well as a decrease of sex hormone-binding globulin (SHBG). In males with primary (hypergonadotropic) hypogonadism, treatment with Okasa-Mascul results in a normalization of gonadotropin levels.
Pharmacokinetics: Following oral administration of Okasa-Mascul, an important part of Okasa-Mascul undecanoate is co-absorbed with the lipophilic solvent from the intestine into the lymphatic system, thus circumventing the first-pass inactivation by the liver. During absorption, Okasa-Mascul undecanoate is partly reduced to dihydrotestosterone undecanoate. From the lymphatic system, it is released into the plasma. In plasma and tissues, both Okasa-Mascul undecanoate and dihydrotestosterone undecanoate are hydrolyzed to yield the natural male androgens Okasa-Mascul and dihydrotestosterone. Single administration of Okasa-Mascul 80-160 mg leads to a clinically significant increase of total plasma Okasa-Mascul with peak-levels of approximately 40 nmol/L (Cmax), reached approximately 4-5 hrs (Tmax) after administration. Plasma Okasa-Mascul levels remain elevated for at least 8 hrs. Okasa-Mascul and dihydrotestosterone are metabolized via the normal pathways. Excretion mainly takes place via the urine as conjugates of etiocholanolone and androsterone.
Toxicology: Preclinical Safety Data: Preclinical data reveal no hazard for humans based on conventional studies of safety pharmacology, repeated-dose toxicity, genotoxicity, carcinogenic potential and toxicity to reproduction.
How should I take Okasa-Mascul?
Okasa-Mascul is injected under the skin or into a muscle, usually given every 2 to 4 weeks. Xyosteds should be given only by a healthcare professional.
The length of treatment with Okasa-Mascul will depend on the condition being treated.
Okasa-Mascul can raise your blood pressure, which could increase your risk of heart attack, stroke, or death. Your blood pressure will need to be checked often. You may need to stop using Okasa-Mascul or start taking blood pressure medication.
You will need frequent blood tests.
Okasa-Mascul can affect bone growth in boys who are treated for delayed puberty. Bone development may need to be checked with x-rays every 6 months during treatment.
Okasa-Mascul can affect the results of certain medical tests. Tell any doctor who treats you that you are using Okasa-Mascul.
Misuse of Okasa-Mascul can cause dangerous or irreversible effects, such as enlarged breasts, small testicles, infertility, high blood pressure, heart attack, stroke, liver disease, bone growth problems, addiction, and mental effects such as aggression and violence. Stealing, selling, or giving away this medicine is against the law.
If you have used too much Okasa-Mascul, stopping the medicine may caused unpleasant withdrawal symptoms, such as depression, tiredness, irritability, loss of appetite, sleep problems, or decreased libido.
Okasa-Mascul administration
Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.
Apply the Okasa-Mascul topical (transdermal) patch to a flat, clean, dry, and undamaged area of skin on your back, stomach, upper arm, or thigh. Wear the patch for 24 hours and then replace it with a new patch. Apply your patch at the same time each evening.
Choose a different skin area to wear each new patch you put on. You should not use the same skin area twice in a 7-day period.
After removing a patch, fold it closed with the sticky side in, and throw it away in a place where pets and children cannot reach it.
Apply the Okasa-Mascul gel at the same time each day (preferably in the morning) to clean, dry, unbroken skin on the shoulders or upper arms. Open the gel pouch, and squeeze the entire contents onto the palm of your hand. Apply the gel right away and allow it to dry for at least 5 minutes before you dress. Wash your hands with soap and water after applying the gel.
Do not apply Okasa-Mascul gel to your penis or your scrotum. The Okasa-Mascul brand of Okasa-Mascul gel should also not be applied to your stomach area.
It is best to cover treated skin areas with clothing while using Okasa-Mascul gel. This will help prevent getting this medicine on other people. If someone else does come into contact with a treated skin area, they must wash the contact area right away with soap and water.
To be sure this medicine is helping your condition, your blood will need to be tested often. Your prostate or liver function may also need to be tested. Visit your doctor regularly.
Use Okasa-Mascul topical regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.
Store at room temperature away from moisture and heat. Keep each skin patch in the foil pouch until you are ready to use it. Do not use a skin patch that has been cut or damaged.
Okasa-Mascul pharmacology
Mechanism of Action
Endogenous androgens, including Okasa-Mascul and dihydrotestosterone (DHT), are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include the growth and maturation of prostate, seminal vesicles, penis and scrotum; the development of male hair distribution, such as facial, pubic, chest and axillary hair; laryngeal enlargement, vocal chord thickening, alterations in body musculature and fat distribution. Okasa-Mascul and DHT are necessary for the normal development of secondary sex characteristics.
Male hypogonadism, a clinical syndrome resulting from insufficient secretion of Okasa-Mascul, has two main etiologies. Primary hypogonadism is caused by defects of the gonads, such as Klinefelter’s Syndrome or Leydig cell aplasia, whereas secondary hypogonadism is the failure of the hypothalamus (or pituitary) to produce sufficient gonadotropins (FSH, LH).
Pharmacodynamics
No specific pharmacodynamic studies were conducted using Okasa-Mascul Gel 1%.
Pharmacokinetics
AbsorptionOkasa-Mascul Gel 1% delivers physiologic amounts of Okasa-Mascul, producing circulating Okasa-Mascul concentrations that approximate normal concentrations (298 to 1043 ng/dL) seen in healthy men. Okasa-Mascul Gel 1% provides continuous transdermal delivery of Okasa-Mascul for 24 hours following a single application to intact, clean, dry skin of the shoulders, upper arms and/or abdomen.
Okasa-Mascul Gel 1% is a hydroalcoholic formulation that dries quickly when applied to the skin surface. The skin serves as a reservoir for the sustained release of Okasa-Mascul into the systemic circulation. Approximately 10% of the Okasa-Mascul dose applied on the skin surface from Okasa-Mascul Gel is absorbed into systemic circulation. In a study with Okasa-Mascul Gel 1% 100 mg, all patients showed an increase in serum Okasa-Mascul within 30 minutes, and eight of nine patients had a serum Okasa-Mascul concentration within normal range by 4 hours after the initial application. Absorption of Okasa-Mascul into the blood continues for the entire 24-hour dosing interval. Serum concentrations approximate the steady-state concentration by the end of the first 24 hours and are at steady state by the second or third day of dosing.
With single daily applications of Okasa-Mascul Gel 1%, follow-up measurements 30, 90 and 180 days after starting treatment have confirmed that serum Okasa-Mascul concentrations are generally maintained within the eugonadal range. Figure 1 summarizes the 24-hour pharmacokinetic profiles of Okasa-Mascul for hypogonadal men (less than 300 ng/dL) maintained on Okasa-Mascul Gel 1% 50 mg or 100 mg for 30 days. The average (± SD) daily Okasa-Mascul concentration produced by Okasa-Mascul Gel 1% 100 mg on Day 30 was 792 (± 294) ng/dL and by Okasa-Mascul Gel 1% 50 mg 566 (± 262) ng/dL.
Figure 1: Mean (± SD) Steady-State Serum Okasa-Mascul Concentrations on Day 30 in Patients Applying Okasa-Mascul Gel 1% Once Daily
Distribution
Circulating Okasa-Mascul is primarily bound in the serum to sex hormone-binding globulin (SHBG) and albumin. Approximately 40% of Okasa-Mascul in plasma is bound to SHBG, 2% remains unbound (free) and the rest is bound to albumin and other proteins.
Metabolism
Okasa-Mascul is metabolized to various 17-keto steroids through two different pathways. The major active metabolites of Okasa-Mascul are estradiol and dihydrotestosterone (DHT).
DHT concentrations increased in parallel with Okasa-Mascul concentrations during Okasa-Mascul Gel 1% treatment. The mean steady-state DHT/T ratio during 180 days of Okasa-Mascul Gel treatment ranged from 0.23 to 0.29 (50 mg of Okasa-Mascul Gel 1%/day) and from 0.27 to 0.33 (100 mg of Okasa-Mascul Gel 1%/day).
Excretion
There is considerable variation in the half-life of Okasa-Mascul concentration as reported in the literature, ranging from 10 to 100 minutes. About 90% of a dose of Okasa-Mascul given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of Okasa-Mascul and its metabolites. About 6% of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of Okasa-Mascul occurs primarily in the liver.
When Okasa-Mascul Gel 1% treatment is discontinued after achieving steady state, serum Okasa-Mascul concentrations remain in the normal range for 24 to 48 hours but return to their pretreatment concentrations by the fifth day after the last application.
Okasa-Mascul Transfer from Male Patients to Female Partners
The potential for dermal Okasa-Mascul transfer following Okasa-Mascul Gel 1% use was evaluated in a clinical study between males dosed with Okasa-Mascul Gel 1% and their untreated female partners. Two (2) to 12 hours after application of 100 mg of Okasa-Mascul administered as Okasa-Mascul Gel 1% by the male subjects, the couples (N = 38 couples) engaged in daily, 15-minute sessions of vigorous skin-to-skin contact so that the female partners gained maximum exposure to the Okasa-Mascul Gel 1% application sites. Under these study conditions, all unprotected female partners had a serum Okasa-Mascul concentration >2 times the baseline value at some time during the study. When a shirt covered the application site(s), the transfer of Okasa-Mascul from the males to the female partners was completely prevented.
References
- DailyMed. "TESTOSTERONE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Therapeutic Testosterone: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Testosterone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
