The intravenous (IV) route of DCA has a number of therapeutic advantages, including:
1) higher blood levels because pulsed IV dosing can achieve a higher concentration than is feasible with an oral dosage
2) a longer washout period to reduce the potential for neurotoxicity
3) a bypassing of the digestive system, which is particularly significant for advanced-stage cancer patients.
I want to collect here all the details about the intravenous DCA. Below, I wrote out all the information on the doses and schedule of intravenous DCA in published treatment reports.
1. A Novel Form of Dichloroacetate Therapy for Patients With Advanced Cancer: A Report of 3 Cases
http://alternative-therapies.com/at/web_pdfs/s202khan.pdf
https://www.ncbi.nlm.nih.gov/pubmed/25362214
Case 1: A 79-year-old male sought therapy for metastatic colon cancer
The first dose of 3000 mg (41 mg/kg) of IV DCA was administered on December 22, 2011, together with 50 g of IVC. The second DCA infusion was given 6 days later at a dose of 3500 mg (48 mg/kg) together with 35 g of IVC. A third DCA infusion at a dose of 3700 mg (50 mg/kg) and 50 g of IVC were given 8 days after the second dose.
Case 2: A 43-year-old male sought therapy for metastatic angiosarcoma of the right femur.
IV DCA was started at a dose of 3000 mg (47 mg/kg) weekly and escalated in a 2-week period to 5000 mg (47 mg/kg) twice per week. No side effects were observed. Following a total of 4 months of IV DCA therapy, an MRI demonstrated stability.
2. Long-term stabilization of stage 4 colon cancer using sodium dichloroacetate therapy
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5067498/
A 57 years old female.
The plan consisted of addition of high dose oral vitamin D at 10000 international units per day, a change of oral vitamin C to vitamin C 50 g intravenous (i.v.) weekly, and addition of dichloroacetate sodium (DCA) 3000 mg i.v. (49 mg/kg) weekly (manufacturer: Tokyo Chemical Industry, United States). To reduce the risk of DCA side effects, 3 natural supplements were prescribed: Alpha lipoic acid (racemic) 500 mg i.v. with each DCA dose, oral R-alpha lipoic acid 150 mg 3 times a day, oral acetyl L-carnitine 500 mg 3 times a day, and oral benfotiamine 80 mg twice a day.
DCA was increased to 4000 mg i.v. (66 mg/kg) weekly. The only side effect noted at the higher DCA dose was mild post-infusion sedation.
…DCA i.v. was continued, and the dose was increased to 4500 mg i.v. weekly.
3. Pharmacokinetics and pharmacodynamics of dichloroacetate in patients with cirrhosis
https://ascpt.onlinelibrary.wiley.com/doi/full/10.1053/cp.1999.v66.a101340
http://sci-hub.tw/https://ascpt.onlinelibrary.wiley.com/doi/pdf/10.1053/cp.1999.v66.a101340
Stock dichloroacetate solution (100 mg/mL) was prepared by dissolving sodium dichloroacetate (>99%, TCI America, Portland, Ore) in 0.45% sodium chloride under aseptic conditions, sterilized by 0.22 micron filtration, and tested for sterility and pyrogenicity before use. It was stored at 4°C, where it is stable for >1 year. Purity and stability were verified by negative chemical ionization gas chromatography—mass spectroscopy (NCI-GC/MS, models 5890/5989A, Hewlett-Packard, Pleasanton, Calif) as described previously. Stock dichloroacetate solution was diluted in 0.9% sodium chloride to a final dichloroacetate concentration of 60 mg/mL on the morning of the infusion protocol.
Intravenous dichloroacetate, 35 mg/kg, was infused for 30 minutes. This dichloroacetate dose was chosen for a near-maximal response of plasma lactate concentration without the somnolence commonly associated with larger doses, even in healthy volunteers. After completion of the stable isotope infusion protocol, subjects were allowed to eat and drink for the duration of the study. All subjects were discharged and sent home 24 hours after the single dichloroacetate administration.
4. Preparation and Stability of Intravenous Solutions of Sodium Dichloroacetate (DCA)
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Unfortunately, I can not find any more information on how to prepare an intravenous DCA solution.
I found a ready-made DCA solution, but still can not find where to buy it.
If you have any information about intravenous DCA, share it!
1) higher blood levels because pulsed IV dosing can achieve a higher concentration than is feasible with an oral dosage
2) a longer washout period to reduce the potential for neurotoxicity
3) a bypassing of the digestive system, which is particularly significant for advanced-stage cancer patients.
I want to collect here all the details about the intravenous DCA. Below, I wrote out all the information on the doses and schedule of intravenous DCA in published treatment reports.
1. A Novel Form of Dichloroacetate Therapy for Patients With Advanced Cancer: A Report of 3 Cases
http://alternative-therapies.com/at/web_pdfs/s202khan.pdf
https://www.ncbi.nlm.nih.gov/pubmed/25362214
Case 1: A 79-year-old male sought therapy for metastatic colon cancer
The first dose of 3000 mg (41 mg/kg) of IV DCA was administered on December 22, 2011, together with 50 g of IVC. The second DCA infusion was given 6 days later at a dose of 3500 mg (48 mg/kg) together with 35 g of IVC. A third DCA infusion at a dose of 3700 mg (50 mg/kg) and 50 g of IVC were given 8 days after the second dose.
Case 2: A 43-year-old male sought therapy for metastatic angiosarcoma of the right femur.
IV DCA was started at a dose of 3000 mg (47 mg/kg) weekly and escalated in a 2-week period to 5000 mg (47 mg/kg) twice per week. No side effects were observed. Following a total of 4 months of IV DCA therapy, an MRI demonstrated stability.
2. Long-term stabilization of stage 4 colon cancer using sodium dichloroacetate therapy
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5067498/
A 57 years old female.
The plan consisted of addition of high dose oral vitamin D at 10000 international units per day, a change of oral vitamin C to vitamin C 50 g intravenous (i.v.) weekly, and addition of dichloroacetate sodium (DCA) 3000 mg i.v. (49 mg/kg) weekly (manufacturer: Tokyo Chemical Industry, United States). To reduce the risk of DCA side effects, 3 natural supplements were prescribed: Alpha lipoic acid (racemic) 500 mg i.v. with each DCA dose, oral R-alpha lipoic acid 150 mg 3 times a day, oral acetyl L-carnitine 500 mg 3 times a day, and oral benfotiamine 80 mg twice a day.
DCA was increased to 4000 mg i.v. (66 mg/kg) weekly. The only side effect noted at the higher DCA dose was mild post-infusion sedation.
…DCA i.v. was continued, and the dose was increased to 4500 mg i.v. weekly.
3. Pharmacokinetics and pharmacodynamics of dichloroacetate in patients with cirrhosis
https://ascpt.onlinelibrary.wiley.com/doi/full/10.1053/cp.1999.v66.a101340
http://sci-hub.tw/https://ascpt.onlinelibrary.wiley.com/doi/pdf/10.1053/cp.1999.v66.a101340
Stock dichloroacetate solution (100 mg/mL) was prepared by dissolving sodium dichloroacetate (>99%, TCI America, Portland, Ore) in 0.45% sodium chloride under aseptic conditions, sterilized by 0.22 micron filtration, and tested for sterility and pyrogenicity before use. It was stored at 4°C, where it is stable for >1 year. Purity and stability were verified by negative chemical ionization gas chromatography—mass spectroscopy (NCI-GC/MS, models 5890/5989A, Hewlett-Packard, Pleasanton, Calif) as described previously. Stock dichloroacetate solution was diluted in 0.9% sodium chloride to a final dichloroacetate concentration of 60 mg/mL on the morning of the infusion protocol.
Intravenous dichloroacetate, 35 mg/kg, was infused for 30 minutes. This dichloroacetate dose was chosen for a near-maximal response of plasma lactate concentration without the somnolence commonly associated with larger doses, even in healthy volunteers. After completion of the stable isotope infusion protocol, subjects were allowed to eat and drink for the duration of the study. All subjects were discharged and sent home 24 hours after the single dichloroacetate administration.
4. Preparation and Stability of Intravenous Solutions of Sodium Dichloroacetate (DCA)
Solutions for injection (100 mg/ml) were prepared by weighing DCA in a laminar flow hood and, using autoclaved utensils, dissolving it in 0.9% (154 mEq sodium chloride per liter) saline solutions. The solution was filtered through a sterile 0.2 u,m nylon Posidyne filter into a sterile pyrogen-free evacuated container. The solution was then transferred asepticaliy to commercially obtained sterile pyrogen-free vials.
______________________
Unfortunately, I can not find any more information on how to prepare an intravenous DCA solution.
I found a ready-made DCA solution, but still can not find where to buy it.
If you have any information about intravenous DCA, share it!
