Fatty Acid Binding Proteins (FABPs) are Intracellular Carriers for Δ9-Tetrahydrocannabinol (THC) and Cannabidiol (CBD).

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“Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) occur naturally in marijuana (Cannabis) and may be formulated, individually or in combination in pharmaceuticals such as Marinol or Sativex.

Recent reports suggest that CBD and THC elevates the levels of the endocannabinoid anandamide (AEA) when administered to humans, suggesting that phytocannabinoids target cellular proteins involved in endocannabinoid clearance.

Fatty acid binding proteins (FABPs) are intracellular proteins that mediate AEA transport to its catabolic enzyme fatty acid amide hydrolase (FAAH).

By computational analysis and ligand displacement assays, we show that at least three human FABPs bind THC and CBD and we demonstrate that THC and CBD inhibit the cellular uptake and catabolism of AEA by targeting FABPs.

Furthermore, we show that in contrast to rodent FAAH, CBD does not inhibit the enzymatic actions of human FAAH, and thus FAAH inhibition cannot account for the observed increase in circulating AEA in humans following CBD consumption.

Using computational molecular docking and site-directed mutagenesis we identify key residues within the active site of FAAH that confer the species-specific sensitivity to inhibition by CBD.

Competition for FABPs may in part or wholly explain the increased circulating levels of endocannabinoids reported after consumption of cannabinoids.

These data shed light on the mechanism of action of CBD in modulating the endocannabinoid tone in vivo and may explain, in part, its reported efficacy towards epilepsy and other neurological disorders.”

http://www.ncbi.nlm.nih.gov/pubmed/25666611

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Medicinal Cannabis Does Not Influence the Clinical Pharmacokinetics of Irinotecan and Docetaxel

“For the past 4,000 years, patients and doctors of each era have resorted to cannabis when conventional treatments were ineffective or lacking. Indeed, in oncology beneficial effects have been reported for cancer-associated anorexia, chemotherapy-induced nausea and vomiting, and palliation…

The only U.S. Food and Drug Administration (FDA)-approved medicinal cannabis products are an oral formulation containing dronabinol (Marinol®)… the synthetic version of delta9-tetrahydrocannabinol (THC), the main pharmacologically active cannabinoid, and capsules containing nabilone, an analog of dronabinol (Cesamet®)…

…many patients claim (subjectively) that a whole or partially purified extract of Cannabis sativa L. offers advantages over a single isolated ingredient…

We anticipated an increased use of medicinal cannabis concurrent with anticancer drugs, and undertook a drug-interaction study to evaluate the effect of concomitant medicinal cannabis on the pharmacokinetics of irinotecan and docetaxel…

Conclusion. Coadministration of medicinal cannabis, as herbal tea, in cancer patients treated with irinotecan or docetaxel does not significantly influence the plasma pharmacokinetics of these drugs. The evaluated variety of medicinal cannabis can be administered concomitantly with both anticancer agents without dose adjustments.”

Full text: http://theoncologist.alphamedpress.org/content/12/3/291.long

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Dronabinol for supportive therapy in patients with malignant melanoma and liver metastases.

“Loss of appetite and nausea can reduce the quality of life of patients with malignant melanoma and liver metastases. Often established antiemetic drugs fail to bring relief. Tetrahydrocannabinol (THC, Marinol), which is the active agent of Indian hemp, has been used successfully in this situation for other malignant tumors.

PATIENTS AND METHODS:

We treated 7 patients with hematogenous metastatic melanoma and liver metastases suffering from extensive loss of appetite and nausea supportively with dronabinol (Marinol. All of these patients had previously received standard antiemetic therapy without adequate relief. Dronabinol is a synthetic Delta-tetrahydrocannabinol. The drug was administered in capsule form. We evaluated the palliative effects of dronabinol with a special patient evaluation form, which was filled out at the beginning of the therapy and again after 4 weeks.

RESULTS:

The majority of patients described a significant increase in appetite and decrease in nausea. These effects remained for some weeks, but then decreased as metastases progressed and the general condition worsened. All of the patients experienced slight to moderate dizziness, but it was not sufficiently troubling to cause interruption or termination of therapy.

CONCLUSION:

Loss of appetite and nausea due to liver metastases of malignant melanoma can be treated in individual cases supportively with Dronabinol.”

http://www.ncbi.nlm.nih.gov/pubmed/16408219

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Marijuana is helping to treat parkinson’s

“My sister, who lives in Holland, is a Parkinson’s patient who is treating her condition with marijuana – or derivatives of it. In the last couple of months, Dutch doctors have been allowed to prescribe marijuana-based medication for Parkinson’s, and my sister has taken advantage of this change in the law.

Several products are available, including Marinol, a synthetic form of THC (tetrahydrocannabiol), the active ingredient of marijuana. This US-made product is expensive – 10 capsules cost 86 euros (£60) – and is not yet approved for Parkinson’s. It has so far been tested only on AIDS and MS patients.

Nonetheless, my sister has started to show spectacular results. She now has clarity of mind, she can turn around in bed by herself and doesn’t have to wake her husband to help her get out of bed. Her stiffness has gone and she is no longer an invalid…”

http://www.wddty.com/marijuana-is-helping-to-treat-parkinson-s.html

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