Agmatine and it’s Potential Role in the Treatment of Glaucoma

What is Agmatine?

Agmatine is a naturally occurring byproduct of the bacterial metabolism of L-Arginine. L-Arginine is an amino acid found in dietary proteins. Agmatine can be found in many fermented foods such as wine, beer, and sake.[1] It is even produced by our own gut bacteria.

Although readily absorbed by the gut[2], if taken with large amounts of protein its absorption will be decreased. This is because L-Arginine competes with Agmatine for gut absorption.[3] Once absorbed into the bloodstream Agmatine is rapidly removed from the bloodstream by the kidneys.[4] However, Agmatine does cross the blood-brain barrier.[5] Once in the brain it appears to stay there for a while.[6]

Evidence that Agmatine can be effective in the treatment of Glaucoma

In animal models Agmatine has been shown to both protect retinal ganglion cells from injury[7] as well as lower the intraocular pressure (IOP).[8] Additionally, there are multiple studies supporting its role as a neuroprotective agent.[9] Unfortunately, there are no published human studies evaluating its potential glaucoma benefit.

Potential Side Effects and Risks of Agmatine:

Agmatine appears to be relatively safe when taken in dosages commonly available in over-the-counter supplements. The only reported side effect is that of mild gastrointestinal discomfort.[10] Agmatine should not, however, be taken along with alcohol as it may worsen alcohol-induced stomach ulceration.[11]

Potential Drug Interactions

Anti-Diabetes Medications

Agmatine may lower blood glucose. In those whose blood sugar is not well-controlled this could be a good thing.  However, care should be taken when used along with other antidiabetes drugs such as glimepiride (Amaryl), glyburide (DiaBeta, Glynase PresTab, Micronase), insulin, metformin (Glucophage), pioglitazone (Actos), and rosiglitazone (Avandia).

Anti-Hypertensive (Blood Pressure) Medications

At least in rats, Agmatine lowers blood pressure.[12] In humans with high blood pressure this could be a good thing. However, care should be taken when used along with other blood-pressure lowering medications such as captopril (Capoten), enalapril (Vasotec), losartan (Cozaar), valsartan (Diovan), diltiazem (Cardizem), amlodipine (Norvasc), hydrochlorothiazide (HydroDIURIL), furosemide (Lasix), as well as many others.

Recommended Dosage

As no human glaucoma studies have been done looking at the role of Agmatine in the treatment of glaucoma, it is not possible to recommend a proper dosage.

References

1) Galgano F, et al. Focused review: agmatine in fermented foods. Front Microbiol. (2012)

2) Haenisch B, von Kügelgen I, Bönisch H, Göthert M, Sauerbruch T, Schepke M, Marklein G, Höfling K, Schröder D, Molderings GJ (2008). Regulatory mechanisms underlying agmatine homeostasis in humans. Am. J. Physiol. Gastrointest. Liver Physiol. 295 (5): G1104–10. doi:10.1152/ajpgi.90374.2008. PMID 18832451

3) Molderings GJ, et al. Gastrointestinal uptake of agmatine: distribution in tissues and organs and pathophysiologic relevance. Ann N Y Acad Sci. (2003)

4) Huisman H, Wynveen P, Nichkova M, Kellermann G (2010). Novel ELISAs for screening of the biogenic amines GABA, glycine, beta-phenylethylamine, agmatine, and taurine using one derivatization procedure of whole urine samples. Anal. Chem. 82 (15): 6526–33. doi:10.1021/ac100858u. PMID 20586417

5) Piletz JE, et al. Agmatine crosses the blood-brain barrier. Ann N Y Acad Sci. (2003)

6) Roberts JC, et al. Pharmacodynamic and pharmacokinetic studies of agmatine after spinal administration in the mouse. J Pharmacol Exp Ther. (2005)

7) Hong S, et al. Agmatine protects retinal ganglion cells from hypoxia-induced apoptosis in transformed rat retinal ganglion cell line. BMC Neurosci. (2007)

8) Hong S, et al. Ocular hypotensive effects of topically administered agmatine in a chronic ocular hypertensive rat model. Exp Eye Res. (2010)

9) Wang CC, et al. Beneficial effect of agmatine on brain apoptosis, astrogliosis, and edema after rat transient cerebral ischemia. BMC Pharmacol. (2010)

Agmatine reduced the expressions of nitric oxide synthase and peroxynitrite formation in rat cerebral cortex after transient global cerebral ischemia

Kim JH, et al. Agmatine attenuates brain edema through reducing the expression of aquaporin-1 after cerebral ischemia. J Cereb Blood Flow Metab. (2010)

Lee WT, et al. Neuroprotective effects of agmatine on oxygen-glucose deprived primary-cultured astrocytes and nuclear translocation of nuclear factor-kappa B. Brain Res. (2009)

Kim JH, et al. Agmatine reduces infarct area in a mouse model of transient focal cerebral ischemia and protects cultured neurons from ischemia-like injury. Exp Neurol. (2004)

Feng Y, Piletz JE, Leblanc MH. Agmatine suppresses nitric oxide production and attenuates hypoxic-ischemic brain injury in neonatal rats. Pediatr Res. (2002)

10) Keynan O, et al. Safety and Efficacy of Dietary Agmatine Sulfate in Lumbar Disc-associated Radiculopathy. An Open-label, Dose-escalating Study Followed by a Randomized, Double-blind, Placebo-controlled Trial. Pain Med. (2010)

11) Utkan T, et al. Investigation on the mechanism involved in the effects of agmatine on ethanol-induced gastric mucosal injury in rats. Life Sci. (2000)

12) Schäfer U, et al. Effects of agmatine on the cardiovascular system of spontaneously hypertensive rats. Ann N Y Acad Sci. (1999)

Sun MK, Regunathan S, Reis DJ. Cardiovascular responses to agmatine, a clonidine-displacing substance, in anesthetized rat. Clin Exp Hypertens. (1995)

Don’t delay getting checked for glaucoma.

Make an appointment with an eye doctor in your area now.  If you live in the greater Los Angeles area and would like Dr. Richardson to evaluate your eyes for glaucoma call 626-289-7856 now. No referral required. Same day or next day appointments are available, Tuesday through Saturday.

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