Exploring the Benefits of Benfotiamine, The Fat-Soluble form of B1

Common complaints such as insomnia, irritability, fatigue, and brain fog can be symptoms of a thiamin deficiency.  While conducting extensive research through PubMed and Cochrane databases for supplements that may serve as valuable adjunctive therapies for chemo-induced neuropathy, benfotiamine emerged as a promising option in a number of peer-reviewed papers. In this article, we will delve into the extensive benefits of benfotiamine, a synthetic fat-soluble derivative of vitamin B1 (thiamine) that not only provides nerve support but also offers a range of other health benefits.

Thiamin and its historical context

Thiamin deficiency symptoms have been recorded in ancient Chinese texts, but a dietary connection wasn’t documented until 1884 when a Japanese physician noticed that Japanese sailors were getting ill when spending months at sea, eating a limited diet of rice.  Thaimin, the natural form of benfotiamine, can be found in foods such as pork, fish, beans, lentils, green peas, sunflower seeds, yogurt, and enriched/fortified foods such as breakfast cereals, breads, noodles, and rice.

Scientific Foundation of Benfotiamine

Now, let's look into the scientific basis that underpins benfotiamine's role in promoting health and preventing disease:

1. Enhanced Bioavailability: Unlike traditional thiamine supplements, Benfotiamine is fat-soluble, enabling better absorption and tissue penetration, a crucial factor for its clinical effectiveness.  Interestingly, recent pharmacokinetic data suggest a five-fold enhancement in bioavailability.¹
2. Anti-Inflammatory Properties: Benfotiamine has demonstrated anti-inflammatory effects by inhibiting the activation of inflammatory signaling pathways.² This makes it valuable in managing conditions with underlying inflammation, which is implicated in most chronic illnesses.
3. Neuroprotection: Benfotiamine promotes nerve health and regeneration, making it a promising therapy for neuropathic conditions and neurological disorders.

Clinical Applications of Benfotiamine Supplementation

1. Neuropathy Management: Benfotiamine's neuroprotective properties are particularly beneficial in managing neuropathic conditions. It has shown promise in alleviating symptoms associated with diabetic neuropathy, alcoholic and chemo-induced neuropathy, as well as sciatica and nerve impingement syndromes. ²
2. Diabetes Care/Improved Blood Sugar Control: Patients with diabetes often face challenges related to glucose metabolism and nerve health. Benfotiamine offers a double whammy to improve glucose control and reduce the risk of diabetic complications, such as retinopathy and nephropathy. ^3,4
3. Cardiovascular Health: Benfotiamine's anti-inflammatory and vascular protective effects contribute to improved cardiovascular health. It may be used to complement treatments for conditions like atherosclerosis and hypertension.⁵ It certainly beats drugs and surgical interventions.
4. Mental Health: Nerve health extends to mental well-being. Benfotiamine's support for nerve function may have implications for conditions like depression and anxiety. ⁶
5. Alzheimer's Disease: While research is ongoing, benfotiamine's neuroprotective properties may have potential applications in the management or prevention of neurodegenerative diseases, such as Alzheimer's disease. ⁷

Dosing

Recommended dosing in the literature ranges from 100 milligrams (mg) to 600mg per day, oral administration. Pay close attention to the ingredients. Some products contain harmful additives such as silicon dioxide (or other chemicals) to prolong shelf life. Taking benfotiamine with a nut butter or other fat-containing food will facilitate absorption.

Side Effects

WebMD suggests benfotiamine is "likely safe at doses of up to 600 mg daily for up to 24 weeks."  Side effects are rare, but some have reported stomach problems and skin rashes.

Case Example

Mrs. Johnson, a 60-year-old female diagnosed with triple-negative breast cancer, is currently undergoing chemotherapy. She has developed chemotherapy-induced peripheral neuropathy (CIPN), causing her significant pain, numbness, and tingling in her hands and feet.  Her neuropathy symptoms have become so severe that they are affecting her daily life and quality of life. Specifically, she has trouble driving, and her balance is affected due to the CIPN, especially with her eyes closed when showering. Benfotiamine was recommended at 300mg per day in addition to acupuncture with microcurrent application.  After seven acupuncture treatments over a four-week period in addition to supplementation, her discomfort has dropped from a pain scale of eight out of ten down to two out of ten, and she has resumed driving.

Benfotiamine supplementation offers a promising approach to managing neuropathic conditions, diabetes-related complications, cardiovascular health, and more. However, its use should be guided by patient assessment, individualized treatment plans, and ongoing monitoring. When integrated thoughtfully into your clinical practice, benfotiamine supplementation can be a valuable tool in improving patient health and quality of life.

References:

1. Loew D. Pharmacokinetics of thiamine derivatives, especially of benfotiamine. International Journal of Clinical Pharmacology and Therapeutics. 1996 Feb;34(2):47-50. PMID: 8929745.
2. Shoeb M, Ramana K, Anti-inflammatory effects of benfotiamine are mediated through the regulation of the arachidonic acid pathway in macrophages, Free Radical Biology and Medicine, 2012; 52(1):182-190, ISSN 0891-5849.
3. Winkler G, Pál B, Nagybéganyi E, et al. Effectiveness of different benfotiamine dosage regimens in the treatment of painful diabetic neuropathy. Arzneimittelforschung. 1999 Mar;49(3):220-4. doi: 10.1055/s-0031-1300405. PMID: 10219465.
4. Beltramo E, Berrone E, Tarallo S, Porta M. Effects of thiamine and benfotiamine on intracellular glucose metabolism and relevance in the prevention of diabetic complications. Acta Diabetol. 2008 Sep;45(3):131-41. doi: 10.1007/s00592-008-0042-y. Epub 2008 Jun 26. PMID: 18581039.
5. Stirban A, Monica Negrean M, Bernd Stratmann B, et al. Benfotiamine Prevents Macro- and Microvascular Endothelial Dysfunction and Oxidative Stress Following a Meal Rich in Advanced Glycation End Products in Individuals with Type 2 Diabetes. Diabetes Care 1 September 2006; 29 (9): 2064–2071.
6. Katare R, Oikawa A, Cesselli D, et al. Boosting the pentose phosphate pathway restores cardiac progenitor cell availability in diabetes. Cardiovasc Res. 2013 Jan 1;97(1):55-65. doi: 10.1093/cvr/cvs291. Epub 2012 Sep 20. PMID: 22997160; PMCID: PMC3619276.
7. Markova N, Bazhenova N, Anthony D, et al. Thiamine and benfotiamine improve cognition and ameliorate GSK-3β-associated stress-induced behaviours in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2017 Apr 3;75:148-156. doi: 10.1016/j.pnpbp.2016.11.001. Epub 2016 Nov 5. PMID: 27825907.
8. Gibson, G. et al. ‘Benfotiamine and Cognitive Decline in Alzheimer’s Disease: Results of a Randomized Placebo-Controlled Phase IIa Clinical Trial’. 1 Jan. 2020 : 989 – 1010.