Delivery route choices for PROGESTERONE: Topical /Epithelial delivery via rectum

(Using hormonal cream/gel)

Epithelial tissue forms the covering or lining of all internal and external body surfaces

Rectal delivery of PROGESTERONE using suppositories/pessaries is the PREFERRED supplementation choice for MEN

Avoids hormonal build-up in fat cells.   This improvement to PROGESTERONE delivery method avoids the hormonal build-up in fat cells that occurs with the transdermal method. Dr. Jonothon Wright, another pioneer in bio-identical hormone supplementation (in addition to the now deceased Dr. John Lee), uses this method in his clinics.

The rectum has a mucosal epithelial surface similar to the vagina.  Chakmakjian et al found that RECTAL administration of micronized PROGESTERONE in normally menstruating women (during the follicular phase) yielded increased under-the-curve areas of serum PROGESTERONE compared to doses of sublingual, oral or vaginal micronized PROGESTERONE .

Chakmakjian ZH, ZachariahNY. Bioavailability of PROGESTERONE with different modes of administration. J Reprod Med 1987;32:443- 448. [PubMed]

Suppositories / Pessaries may make rectal application of the hormone a little easier, but it does make it messier.   PROGESTERONE is usually combined with a highly saturated fat, such as cocoa butter.   This will harden at cooler temperatures, but melt at body temperature. 

Rectal PROGESTERONE administration has a wide range of absorbability

Blood drainage from the lower end of the rectum is directly into systemic circulation via the vena cava.     Drainage is via both venous blood capillaries and lymphatic vessels. When an active component is absorbed in the lower portion of the rectum (via the inferior hemorrhoidal veins) it reaches the general circulation directly - bypassing the hepatic first-pass elimination.

RitschelWA. Targeting in the gastrointestinal tract: new approaches. Methods Find Exp CUn Pharmacol 1991;13:313-336. [PubMed]

-   However, if the compounds are absorbed by the upper part of the rectum (superior rectal ampulla) they will reach the portal circulation (via the superior hemorrhoidal vein).    Thus the liver gets the “first pass” at the PROGESTERONE with the inherent problems seen in oral administration.

de Boer AG, Moolcnaar F, de Lecdc LG, Breimcr DD. Rectal drug administration: clinical pharmacokinetic considerations. Clin Pharmacokinct 1982;7:285-311.[PubMed]

Drawbacks of rectal administration

Defecation affecting absorption;

Lack of patient acceptability.