Olmesartan Up-regulates the Vitamin D Receptor and Resolves Neurological Symptoms Related to Lyme Disease Meg Mangin, RN Non-resolving inflammation may be initiated when cell-wall-deficient bacteria invade nucleated cells and use strategies to evade destruction.

One of those strategies appears to be down-regulation of the 1,25(OH)2D-activated vitamin D receptor (VDR). This is suggested by the presence of elevated calcitriol in many inflammatory diseases.

Normally, renal production of 1,25(OH)2D is tightly self-regulated, with the end product down-regulating its own further production. But production in extra-renal cells is not controlled by a feedback mechanism.

Case Report-Inflammation Therapy

The result is sustained inflammation, inflammatory symptoms and eventual tissue damage.

Molecular modeling indicates olmesartan medoxomil (Benicar®) has a high affinity for the vitamin D receptor, which modulates the immune system via 1,25(OH)2D.

Olmesartan, an angiotensin receptor blocker (ARB), when administered at higher than standard anti-hypertension doses, appears to be an agonistic VDR ligand which up-regulates the bacterially-inhibited VDR.

37 year old female with post-treatment Lyme disease syndrome. Neurological symptoms improved during Inflammation Therapy. She had no improvement with previous oral Levaquin and IV Rocephin.

Following olmesartan administration, a reduction in elevated 1,25(OH)2D suggests restored renal control of calcitriol production. In addition, olmesartan is the only ARB that reduces the level of angiotensin II. Significantly, 1,25(OH)2D also reduces angiotensin II (by repressing renin genetic expression).

Olmesartan appears to improve immune system function to eliminate intracellular bacteria and extracellular co-infections. This is evidenced by a gradual resolution of inflammatory symptoms.

Inflammation Therapy ● Olmesartan 20 mg q6-8h ● Very gradual introduction of low-dose, oral antibiotics: ● Minocycline 25-100 mg qod ● Azithromycin 31-125 mg q10days ● Clindamycin 37-150 mg qod ● No immunosuppressive agents ● Maintain 25(OH)D below 30 ng/mL to avoid immunosuppression

Conclusion Extra-renal production of 1,25(OH)2D may be stimulated by intracellular bacteria. Elevated 1,25(OH)2D suggests the immune system recognizes the presence of pathogens and is making a futile attempt to increase transcription of antimicrobial peptides (AMPs) to combat them.

Up-regulation of the VDR is evidenced by Jarisch-Herxheimer reactions (a temporary increase in inflammatory symptoms in response to dying bacteria). This suggests increased AMP transcription and elimination of pathogens.

Intracellular bacteria may down-regulate the VDR and reduce immune system function which allows extracellular pathogens (e.g, borrelia, bartonella, etc.) to persist. Olmesartan appears to enhance VDR expression and, along with low-dose oral antibiotics, eliminate offending pathogens. Patients with post-treatment Lyme disease syndrome have been treated successfully with this activation immunotherapy.

Reference Mangin M, Sinha R, Fincher K. Inflammation and vitamin D: the infection connection. Inflamm Res. Oct 2014;63(10):803-19.

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