L-Acetylcarnitine

Absorption

Acetylcarnitine supplements are absorbed in a similar manner to L-carnitine.

Description

L-Acetylcarnitine is a endogenous substance, synthesized in the mitochondria, that increases cellular oxidative metabolism and cholinergic activity. It has a good penetration in the CNS when administered orally and intravenously, and no side effects have been observed.
L-Acetylcarnitine has a large variety of interesting pharmacological properties:
It is a cholinergic agent because it promotes the synthesis and freeing of acetylcholine.
It reduces oxidation processes, thus reducing lipofuscin deposits in the brain.
It acts on the hypothalamic-hypophyseal-adrenal axis, antagonizing the existing downregulation (Carta and Calvani 1991).
In a 1-year study of 130 patients with AD (63 in treatment with L-acetylcarnitine and 67 with placebo), an improvement in the cognitive decline measured through neuropsychiatric batteries was observed (Spagnoli et al. 1991).

The Uses of L-Acetylcarnitine

Acetylcarnitine may be a useful for treatment of male infertility caused by low quantities of immobile sperm.
Acetyl-L-carnitine (ALC) is produced naturally in humans, and can be found in the brain, liver, and kidneys. ALC is also available as a dietary supplement. ALC has been studied for its potential use in slowing the progression of age-related memory loss and Alzheimer’s disease. ALC may also have a potential use in the treatment of neuropathy (nerve pain) associated with diabetes and HIV disease.

What are the applications of Application

Acetyl-L-Carnitine is an acetylated form of L-carnitine.

Indications

Acetylcarnitine is not approved for any indication in the United states and Canada, but it is approved and indicated in Italy for cerebrovascular disorders, mental function disorders, peripheral nerve disorders, diabetic neuropathy, and nutritional supplementation; Portugal for mental function disorders; Argentina for cerebral vasculopathy, nutritional supplementation, and peripheral neuropathy; Chile for dementia; Philippines for cerebrovascular disorders and mental function disorders; Australia for nutritional supplementation; and India for nutritional supplementation to increase sperm count. Acetylcarnitine also has several potential therapeutic indications for which it is still being investigated: in Norway, acetylcarnitine is in a phase IV trial for prophylactic treatment of migraines; in Italy acetylcarnitine is in a phase II trial for use in patients with type 2 Diabetes Mellitus, a phase III trial for alleviating fatigue in patients with chronic hepatitis C, and for use in patients with Minimal Hepatic Encephalopathy; in the United States acetylcarnitine is in a phase II trial for the neurodegenerative disorder Progressive Supranuclear Palsy, a phase II and III trial for reducing peripheral neuropathy in cancer patients as an adjunct to chemotherapy, a phase I and II trial for treating patients in septic shock, a phase II trial for bipolar depression, a phase II trial to reduce oxidative stress in patients with Sickle Cell disease, a phase I and II trial for chronic fatigue syndrome, and a study for preventing nerve damage in HIV patients; in China acetylcarnitine is in a phase III trial for reducing peripheral neuropathy in cancer patients as an adjunct to chemotherapy; in the United Kingdom acetylcarnitine is being investigated for preventing nerve damage in HIV patients; and in Israel acetylcarnitine is being studied for the treatment of male infertility.

Background

Acetylcarnitine is an investigational drug in the United states, Italy, United Kingdom, China, Israel, and Norway, and it is approved in Italy, Portugal, Argentina, Chile, Philippines, Australia, and India. Acetylcarnitine can be synthesized, but it is also naturally found in adequate amounts in healthy humans. In human plasma and tissues, acetylcarnitine is the most predominant acylated ester of carnitine, which is an amino acid derivative that is made in the kidney, liver, and brain from lysine and methionine. The main role of acetylcarnitine is to help transport fatty acids into the mitochondrial matrix where fatty acid metabolism occurs.

Definition

ChEBI: An O-acyl-L-carnitine where the acyl group specified is acetyl. It facilitates movement of acetyl-CoA into the matrices of mammalian mitochondria during the oxidation of fatty acids.

Pharmacokinetics

The complete physiological effects of acetycarnitine are still being studied. What has been discovered so far is that acetylcarinitine has positive effects on mental fatigue, neurodegenerative disorders, cognitive functions, peripheral neuropathy, and sperm motility. Specifically, in one study involving patients with HIV, patients on acetylcarnitine supplementation had increased CD4 cells, decreased lymphocyte apoptosis, improved polyneuropathy and cardiovascular damage, and decreased triglyceride and TNF alpha levels in the blood. Another study showed that acetylcarnitine increased glucose disposal in type 2 diabetic patients through possibly increasing the activity of glycogen synthase.

Metabolism

Not Available