Testosterone Lozenges

Testosterone replacement therapy is advised to hypogonadal men who manifests severe symptoms of testosterone deficiency. It is imperative to mention that testosterone replacement helps a great deal at restoring normal hormonal balance, but in some cases side-effects may outweigh the potential benefits of therapy. The severity of side-effects can be managed by monitoring hormonal levels in the serum by choosing different formulations of testosterone.  

What Are Testosterone Lozenges?

Testosterone hormone replacement therapy (TRT) when consumed by transbuccal or oral route is referred to as testosterone lozenges. The bioavailability of testosterone via buccal route is fairly high, due to direct absorption in the blood stream via mucous membrane of the mouth.

The lozenges are kept underneath the tongue or against the gums for maximum oral absorption. There are two sides of the lozenge formulation of testosterone – the flat side is placed against the cheek and the rounded side is aligned against the gum. Please note that testosterone lozenges are not for chewing or swallowing purposes.

Dosing Schedule

The lozenges can be consumed twice daily, first dose in the morning and second dose in the evening. Lozenges stays in the mouth (while melting slowly to release small but consistent doses of testosterone) and should be replaced after 12 hours. The lozenges should be rotated to alternate sides of the mouth with each application (3).

Indications And Uses

Testosterone is a male sex hormone which is advised to men who are not capable of synthesizing the hormone naturally in the body.

One common indication of TRT is male hypogonadism (congenital or acquired), either due to a primary lack of male sex hormone production from the testis, or due to problems in the release of stimulatory hormones from the higher brain centers (hypothalamus or pituitary). Also, testosterone levels tends to decline with age, and at times, should be supplied from the exogenous sources to restore optimal sexual functions.

Available Products And Costs

The only FDA-Cleared testosterone lozenge available in the US is sold under the brand name ‘Striant’ (produced by Endo Pharmaceuticals Inc.) It is prescribed in a twice daily regimen; each lozenge has 30 mg testosterone. The prescription details are provided with the product. The monthly cost of Striant is about $350.

Alternate Forms Of Testosterone

Testosterone medication comes in various forms for instance gels, topical solutions, injections, transdermal patches (applied beneath the skin), and pellets (implanted under the skin).

Advantages Of Testosterone Lozenges

• Lower risk of liver toxicity: Testosterone lozenges are less likely to cause liver damage since buccal route eliminates the first pass metabolism by liver. Absorption through mucous membranes of gums is also associated with higher bioavailability and steady testosterone levels (3).
• Easier dose modifications: Proper dosing can be ensured as the regimen can be modified easily.

Disadvantages Of Testosterone Lozenges

• These lozenges needs to be placed for a long time (12 hours) and there is inconvenience in removing and replacing the medicine on a daily basis. Most people would rather prefer once a week/ month testosterone injection.
• Due to long hours of use, testosterone lozenges can cause gum irritation or inflammation.
• The drug traces can be transferred from the user to another person via saliva.

Side Effects

Following are some adverse effects that are very frequently associated with testosterone lozenges:

• Gum/mouth irritation and bitter taste/taste perversion
• Edema, pain or tenderness in the gums. Users are advised to inspect their gums regularly for any ulceration or sores.
• Recurrent episodes of headache

Contraindications

• Men with breast cancer or suspicion of prostate cancer should avoid testosterone.
• It is also contraindicated during pregnancy and lactation as there is high risk of damage to the fetus.
• Safety and efficacy in people younger than 18 years is not established.

Monitoring Serum Levels Of Testosterone

Testosterone levels should be measured 1-3 months after the commencement of therapy and periodically thereafter. In case levels are abnormally high, discontinue the drug and seek medical attention.

References

1. Slater, C. C., Souter, I., Zhang, C., Guan, C., Stanczyk, F. Z., & Mishell, D. R. (2001). Pharmacokinetics of testosterone after percutaneous gel or buccal administration. Fertility and sterility, 76(1), 32-37.

2. Mechlin, C. W., Frankel, J., & McCullough, A. (2014). Coadministration of anastrozole sustains therapeutic testosterone levels in hypogonadal men undergoing testosterone pellet insertion. The journal of sexual medicine, 11(1), 254-261.

3. Rathbone, M. J., Şenel, S., & Pather, I. (2015). Design and Development of Systemic Oral Mucosal Drug Delivery Systems. In Oral Mucosal Drug Delivery and Therapy (pp. 149-167). Springer US.