Dimethyl Sulfoxide (Dr. JP’s)

Dimethyl Sulfoxide (Dr. JP’s)

Product Name: Диметилсульфоксид, Dimethyl sulfoxide, Dimethylsulfoxid, Dimetilsulfóxido, Diméthylsulfoxyde, ثنائي ميثيل سلفوكسيد, ไดเมทิลซัลฟอกไซด์, Диметилсульфоксид, Диметилсульфоксид, Dimetilsulfoksid, Диметилсулфоксид, Dimetilsulfoksid, Диметилсулфоксид, Dimetilsulfoksid, Диметилсульфоксид, דימתיל סולפוקסיד

Main Indications for Use of Dimethyl Sulfoxide: Interstitial cystitis, extravasation of cytostatics, complex regional pain syndrome type I with thermal phenotype, cutaneous amyloidosis (lichen, macular), chronic trophic skin ulcers, herpes zoster in combination with idoxuridine, superficial basal cell skin carcinoma in combination with ascorbic acid, chronic bedsores.

Indications for Use of Dimethyl Sulfoxide as Part of Therapeutic Complexes: Degenerative osteoarthritis, systemic scleroderma with digital ulcers, traumatic brain injury with intracranial hypertension, invasive breast carcinoma, squamous cell skin carcinoma, soft tissue sarcoma, inflammatory joint diseases of rheumatoid etiology, malignant skin lymphomas.

Main Pharmacological Properties of Dimethyl Sulfoxide: anti-inflammatory, analgesic, antioxidant, antimicrobial, immunomodulatory, antiplatelet, vasodilatory, antipruritic, cryoprotective, penetrating (transdermal), antitumor (experimental).

Composition of Dimethyl Sulfoxide: Dimethyl sulfoxide

Functions of the Components in Dimethyl Sulfoxide.

Dimethyl sulfoxide: primary pharmacologically active component, provides anti-inflammatory, analgesic, and antioxidant action, used as a cryoprotectant, as well as a universal solvent and transdermal conductor for other medicinal substances.

Product Form of Dimethyl Sulfoxide: Solution in a 100 ml bottle, containing 100% dimethyl sulfoxide; mass of active substance in one bottle is 100 g.

Dosage of Dimethyl Sulfoxide

Interstitial Cystitis: For adult patients, intravesical instillation of the solution is used. Use 50 ml of 50% dimethyl sulfoxide, introduced via catheter into the bladder cavity. The solution is retained for 15–20 minutes, then evacuated. Procedures are performed once every 2 weeks, the course consists of 6–8 instillations.

Extravasation of Cytostatics (anthracyclines, mitomycin, actinomycin D): Applied topically to the skin. Use a 99% dimethyl sulfoxide solution. Apply topically in a volume of approximately 4 drops per 10 cm² of affected skin surface. Treatment is performed every 8 hours for 7–14 consecutive days.

Complex Regional Pain Syndrome Type I with Thermal Phenotype: External applications of a 50% dimethyl sulfoxide solution are used. Compresses are applied to the affected area 4–5 times per day. Therapy course – not less than 2 months.

Cutaneous Amyloidosis (lichen, macular): Local applications of a 50–70% dimethyl sulfoxide solution are used. Applied to affected skin areas 2 times a day. Treatment duration ranges from several weeks to clinical improvement.

Herpes Zoster in Combination with Idoxuridine: External application of the preparation is used. Use a 30–50% dimethyl sulfoxide solution as a solvent and transport carrier for idoxuridine. Cream or solution is applied to the eruptions up to 4 times a day until complete epithelialization.

Superficial Basal Cell Skin Carcinoma (in combination with ascorbic acid): External applications of a dimethyl sulfoxide solution with dissolved ascorbic acid are used. Dimethyl sulfoxide concentration – 50–70%. Applied to the affected area daily, the course is determined by a dermato-oncologist depending on tumor regression.

Chronic Trophic Ulcers and Bedsores: A 50% dimethyl sulfoxide solution is used for applications to the ulcer area. Impregnated sterile gauze is applied 2 times a day. The treatment course may continue for several weeks until granulation tissue forms.

Degenerative Osteoarthritis: For external use, 25–50% dimethyl sulfoxide solutions have been used as compresses on affected joints. Compresses are applied for 30–60 minutes 2–3 times a day in courses of 2–4 weeks. Moderate reduction in pain syndrome and stiffness is noted.

Systemic Scleroderma with Digital Ulcers: Local applications of a 70% dimethyl sulfoxide solution on ulcerative defects are used. An impregnated sterile napkin is applied 2 times a day until epithelialization begins. The total duration of therapy can be several weeks.

Traumatic Brain Injury with Intracranial Hypertension (experimental regimens): Intravenous infusions of dimethyl sulfoxide have been used at a dosage of 1 g/kg body weight by drip over 30–60 minutes. Rapid reduction of intracranial pressure was noted. Use is limited to experimental protocols, requires strict monitoring.

Invasive Breast Carcinoma (experimental): Intraperitoneal administrations of dimethyl sulfoxide in mice at a dose of 0.5–1 g/kg body weight were used to modulate the tumor microenvironment. Data in humans are limited to laboratory studies; no clinical protocols for systemic use exist.

Squamous Cell Skin Carcinoma (experimental): Topical application of dimethyl sulfoxide as a solvent for photosensitizers (5-aminolevulinic acid) increased the effectiveness of photodynamic therapy. Preparation concentration – 20–50%, frequency of application is determined by the PDT scheme.

Soft Tissue Sarcoma (experimental): In sarcoma models, administration of dimethyl sulfoxide was used to modulate the antitumor response in doses of 0.5–1 g/kg in laboratory animals. No clinical regimens exist for humans; use is possible only as an adjunct within experimental protocols.

Inflammatory Joint Diseases of Rheumatoid Etiology: External compresses with a 50% dimethyl sulfoxide solution on affected joints 2–3 times a day have been used. Course – from 2 weeks to 1 month. Reduction in the severity of pain syndrome and inflammatory reaction was noted.

Malignant Skin Lymphomas (experimental): Dimethyl sulfoxide was used as a carrier for cytostatics and photosensitizers in local therapy of cutaneous lymphomas. Concentrations – 30–50%, applied locally to lesions as part of combined schemes. Data are limited to individual studies.

Preventive Dosage of Dimethyl Sulfoxide: Preventive use is limited to external applications of 10–30% solutions for chronic degenerative joint diseases, rheumatic arthralgias, in elderly patients with chronic soft tissue pain syndromes. Applications are performed once a day at night for 10–14 days with the possibility of repeating the course after 1–2 months. Data on preventive systemic intake in humans have not been registered.

Contraindications of Dimethyl Sulfoxide: Severe liver dysfunction, severe kidney dysfunction, severe cardiovascular diseases in the decompensation stage, individual intolerance. Scientifically reliable data on contraindications during pregnancy, lactation, and in children have not been registered.

Side Effects of Dimethyl Sulfoxide: Registered side effects: local skin irritation, erythema, itching, burning sensation, metallic or garlic-like taste in the mouth, specific odor of exhaled air, nausea, dizziness, diarrhea. Overdose may intensify all listed effects.

Storage Conditions for Dimethyl Sulfoxide: Store in tightly closed container at temperatures from +15 °C to +25 °C, in a light-protected place. Keep away from sources of electromagnetic radiation. Crystallization at temperatures below +18.5 °C is allowed, with subsequent restoration upon warming to room temperature. Shelf life in the bottle – up to 3 years. After opening, use within 12 months provided it is sealed and protected from moisture.

Dosage of Dimethyl Sulfoxide in Creams, Ointments, and Applications of Various Preparations

Use of Dimethyl Sulfoxide in Creams and Ointments: Dimethyl sulfoxide is widely used in topical pharmaceutical forms at concentrations from 5% to 30% as an auxiliary component. Its main task is to enhance the penetration of active substances through the stratum corneum and increase their bioavailability in the deep layers of the skin and underlying tissues. When manufacturing creams and ointments, dimethyl sulfoxide is incorporated into an oil-water or gel-like base, into which the active medicinal substance is preliminarily introduced. Depending on the pharmacological task, the cream or ointment may contain 5–10% dimethyl sulfoxide for mild dermatological agents or up to 25–30% for preparations intended for treating chronic inflammatory joint and soft tissue diseases.

Use of Dimethyl Sulfoxide in Applications of Medicinal Substances: Dimethyl sulfoxide is used as a solvent and transport carrier in applications. The most effective use is in the form of impregnated gauze dressings applied to the affected area. The solution concentration is selected in the range of 20% to 70% depending on the medicinal substance that needs to be delivered through the skin. The application lasts for 20–30 minutes, after which the dressing is removed. Repeat procedures are possible 2–3 times a day in courses of 10–14 days.

Use of Dimethyl Sulfoxide with Methylene Blue: Methylene blue is a water-soluble dye with pronounced antimicrobial and antiseptic properties. When combined with dimethyl sulfoxide, a significant enhancement of methylene blue penetration into the deep layers of the skin and soft tissues is observed. For applications, solutions of methylene blue at 1–2% concentration, prepared in a 30–50% dimethyl sulfoxide solution, are used. A gauze pad is impregnated with the solution and applied to the affected skin surface or to the area of a chronic ulcer for 15–20 minutes. Repeat procedures are performed 1–2 times a day until the therapeutic effect is achieved. This method is particularly useful in the treatment of infected trophic ulcers, fungal skin infections, and in preparing the skin surface for surgical interventions.

Creams and Ointments with Dimethyl Sulfoxide and Herbal Components: Dimethyl sulfoxide is included in phytotherapeutic topical agents at concentrations of 10–25%. Standardized extracts or essential oils of medicinal plants are used as active components. Such a combination provides a synergistic effect: DMSO enhances the penetration of phytochemical substances through the skin, and the plant components provide anti-inflammatory, antimicrobial, and reparative action.

Examples of Herbal Combinations for Creams and Ointments with Dimethyl Sulfoxide:

• Curcuma longa (turmeric) – curcumin has antioxidant and anti-inflammatory action; included in the ointment as a 1–5% extract in combination with 15% DMSO.
• Arnica montana (arnica) – flower extract reduces soft tissue inflammation and accelerates hematoma resorption; added to the ointment at a concentration of 3–10% on a fatty base with 20% DMSO.
• Calendula officinalis (calendula) – provides antiseptic and reparative action; 5–10% extract is combined with 10% DMSO in a cream base.
• Aloe vera (aloe) – aloe gel enhances tissue repair and hydration; used at a concentration of 20–30% with the addition of 15% DMSO.
• Melaleuca alternifolia (tea tree oil) – strong antimicrobial action; added to the ointment at a concentration of 2–3% in combination with 10% DMSO.

Applications of Herbal Preparations with Dimethyl Sulfoxide: The method involves preparing solutions of active plant components on a water-alcohol or oil base with the addition of DMSO. Gauze pads are impregnated with the composition and applied to the affected area for 20–30 minutes.

Examples:

• Hypericum perforatum (St. John's wort) – 5% oil extract + 20% DMSO for applications on inflammatory skin foci and joints.
• Symphytum officinale (comfrey) – 10% water-alcohol extract + 15% DMSO for applications in osteoarthritis and myalgias.
• Glycyrrhiza glabra (licorice) – 5% aqueous extract + 10% DMSO for applications in chronic dermatoses.
• Camellia sinensis (green tea) – 2% alcohol extract of catechins + 15% DMSO for applications in skin photoaging and superficial inflammatory processes.

Use of Dimethyl Sulfoxide with Methylene Blue and Herbal Preparations: In applications, dimethyl sulfoxide can be used simultaneously with methylene blue (1–2%) and plant extracts (e.g., calendula, arnica). Such a combination enhances antimicrobial action, stimulates the healing of chronic ulcers and bedsores, reduces bacterial load and inflammation. Optimal DMSO concentration – 20–30%. Applications are performed 1–2 times a day for a course of 7 to 14 days.

Method for Preparing Creams and Ointments:

• Prepare the base (emulsion or gel-like).
• Dissolve water or alcohol plant extracts in the aqueous phase, oils in the lipid phase.
• In a separate container, mix the required volume of DMSO with part of the aqueous phase.
• Combine the phases with constant stirring, add the phyto-components.
• Bring the mass to a homogeneous state, package into tubes or jars.

Pharmacological Significance of Using Dimethyl Sulfoxide in Creams and Applications:

• Ensures rapid and effective penetration of active substances.
• Reduces local inflammation and pain due to its own analgesic effect.
• Reduces microbial contamination thanks to its own antiseptic activity.
• Accelerates reparative processes in chronic ulcers and wound surfaces.

Memo: What Absolutely Must Not Be Done with Concentrated Dimethyl Sulfoxide (DMSO 98–99%)

• Do not apply the concentrate directly to the skin. Dimethyl sulfoxide instantly passes through the skin into the bloodstream, carrying with it everything on the surface – microbes, dirt, toxins, residue from creams. This can lead to poisoning or infection.
• Do not use on mucous membranes (eyes, mouth, nose, genitals). Concentrated solution causes severe irritation and chemical burns. Contact with eyes can result in vision damage.
• Do not use without dilution. For medical and research purposes, solutions from 10% to 50% are used. The 98–99% concentrate is not suitable for these purposes.
• Do not think that "a little bit won't hurt". Even a small amount of concentrate can cause burning, itching, a metallic or garlic-like taste in the mouth, headache, and nausea.
• Do not drink dimethyl sulfoxide and do not use it for enemas. Oral intake or rectal administration of the concentrate is dangerous for the liver, kidneys, and gastrointestinal tract. Such experiments can end in severe poisoning and hospitalization.

How to Use Safely. Used only in diluted form, typically 10–50%, exclusively on clean skin, without creams, ointments, or damage. Use is possible only in accordance with medical protocols or under the supervision of a specialist.

Summary Dimethyl sulfoxide is a powerful pharmacological tool, but the 98–99% concentrate must not be drunk, used for enemas, applied to mucous membranes, or applied to the skin without dilution. Such use will lead not to treatment, but to severe complications.

Toxicity and Biosafety – Dimethyl Sulfoxide

Dimethyl sulfoxide has low acute toxicity compared to most organic solvents. Experimental studies on animals show the following LD₅₀ values:

• Orally, rats: LD₅₀ ≈ 14.5 g/kg body weight
• Orally, mice: LD₅₀ ≈ 28.3 g/kg body weight
• Intravenously, rats: LD₅₀ ≈ 2.5 g/kg body weight
• Dermal, rabbits: LD₅₀ > 40 g/kg body weight

These data indicate that dimethyl sulfoxide belongs to substances with relatively low acute toxicity. However, its peculiarity lies in its ability to rapidly penetrate the skin and biological membranes, which can enhance the toxic effects of impurities and concomitant compounds carried into the body.

With chronic exposure, changes in the liver, kidneys, and reproductive organs have been noted in laboratory animals at high doses. In cell culture studies, signs of cytotoxicity have been identified at concentrations above 1–2% in the medium.

The modeled cumulative toxicity for the preparation consisting exclusively of dimethyl sulfoxide (without additional components) corresponds to the presented experimental data. When used at concentrations of 10–50% for topical use, toxicity is significantly reduced, but the risk of systemic action remains with prolonged use or application to large skin areas.

Thus, dimethyl sulfoxide is characterized as a relatively safe compound when properly diluted and used, but requires strict quality control and exclusion of contaminants due to its pronounced ability to carry foreign substances through biological barriers.

Synergy – Dimethyl Sulfoxide

Dimethyl sulfoxide is a unique compound demonstrating pronounced pharmacological synergy with a wide range of biologically active substances of various origins. Numerous studies have noted that dimethyl sulfoxide can potentiate the activity of antimicrobial agents by enhancing the penetration of molecules through cellular and tissue barriers by increasing membrane permeability and altering the lipid microenvironment composition. When combined with anti-inflammatory compounds such as curcumin, resveratrol, or green tea polyphenols, dimethyl sulfoxide exhibits additive and potentiating effects on the inhibition of inflammatory mediators, including tumor necrosis factor-α and the cyclooxygenase cascade. In vivo experiments have demonstrated enhanced antioxidant activity when combining dimethyl sulfoxide with vitamins C and E, which is associated with a joint increase in overall antiradical capacity and additional protective action on cell membranes.

Of particular importance is the synergy of dimethyl sulfoxide with photosensitizers, such as 5-aminolevulinic acid and methylene blue. In these combinations, dimethyl sulfoxide increases intracellular accumulation of active forms and promotes deeper tissue-specific action upon light activation. In preclinical models, it has been established that the combined use of dimethyl sulfoxide and immunomodulatory phytochemicals, such as licorice saponins or astragalus triterpenes, leads to a modulating effect on the T-cell response and interleukin production. Cell culture studies have shown that dimethyl sulfoxide at low concentrations can protect protein structures from denaturation and potentiate the action of cytoskeleton stabilizers, thereby enhancing additive cellular anti-stress action.

The nature of the interaction of dimethyl sulfoxide with most compounds can be described as potentiating and modulating: it facilitates transdermal and intracellular delivery, enhances the severity of the active substance's effect, and reduces its required effective concentration. Collectively, the data indicate systemic synergy of dimethyl sulfoxide with anti-inflammatory, antioxidant, antimicrobial, and immunomodulatory taxa, confirmed in vitro, in vivo, and partially in clinical practice.

References: PubMed, PMC, ScienceDirect, SpringerLink, Wiley, Semantic Scholar.

Pharmacodynamics of Dimethyl Sulfoxide

Dimethyl sulfoxide possesses a wide range of pharmacodynamic effects confirmed by experimental and clinical studies. At the level of the nervous system, it exerts an analgesic action associated with the inhibition of pain impulse transmission and stabilization of neuronal membrane potentials. This action is linked to effects on ion channels and partial modulation of the NMDA receptor cascade. Regarding the immune system, dimethyl sulfoxide exhibits a pronounced anti-inflammatory effect by inhibiting the activation of the transcription factor NF-κB and suppressing the production of pro-inflammatory cytokines. A reduction in cyclooxygenase-2 expression and suppression of prostaglandin formation is also observed, forming a systemic anti-inflammatory effect.

At the level of the vascular and hematopoietic system, dimethyl sulfoxide exerts vasodilatory and antiplatelet effects, reducing platelet aggregation and improving microcirculation. Regarding the skin and underlying tissues, dimethyl sulfoxide significantly increases the permeability of the epidermal barrier, facilitating the transdermal delivery of both low-molecular-weight and macromolecular compounds. This effect is the primary reason for using dimethyl sulfoxide as a pharmacological penetration enhancer.

Antioxidant action is realized through direct binding of free radicals and prevention of lipid peroxidation. At the cellular level, dimethyl sulfoxide can stabilize membranes, protect protein structures from denaturation, and reduce DNA damage under oxidative stress. In endocrine and metabolic systems, its influence on the regulation of the oxylipin profile and modulation of signaling pathways associated with inflammation and apoptosis has been noted.

Thus, the pharmacodynamics of dimethyl sulfoxide are characterized as multi-faceted: analgesic, anti-inflammatory, antioxidant, vasodilatory, antiplatelet, and penetrating. Local action is realized through improved delivery of active substances and modulation of inflammatory processes, systemic – through antioxidant and membrane-stabilizing influence at the cellular and tissue levels.

References: PubMed, PMC, ScienceDirect, SpringerLink, Wiley, WHO.

Pharmacokinetics of Dimethyl Sulfoxide

Dimethyl sulfoxide is characterized by high absorption capacity via various routes of administration. With transdermal application, the substance rapidly penetrates the epidermal barrier, reaching the systemic bloodstream within a short time, which is associated with its low molecular weight and high polarity. Oral administration is accompanied by rapid absorption in the gastrointestinal tract with subsequent distribution to organs and tissues. Administration via mucous membranes results in accelerated absorption due to high solubility in aqueous environments and ability to diffuse through intercellular barriers. The inhalational route of administration also ensures entry into the systemic bloodstream due to high volatility and solubility in biological fluids.

After absorption, dimethyl sulfoxide is evenly distributed in most body tissues, including the liver, kidneys, lungs, and skin. Its ability to cross the blood-brain barrier and accumulate in the cerebrospinal fluid is noted. Interaction with plasma proteins is relatively weak, facilitating free distribution of the substance.

Metabolism of dimethyl sulfoxide occurs primarily in the liver. The main metabolic transformations include oxidation to dimethyl sulfone and partial reduction to dimethyl sulfide. These metabolites possess their own biological activity, explaining the complexity of the pharmacodynamic effects. Cytochrome P450 enzyme systems and associated oxidoreductases are involved in the metabolic processes.

Excretion occurs mainly through the kidneys in the form of dimethyl sulfoxide and dimethyl sulfone; a portion is also excreted via exhaled air as dimethyl sulfide, which causes the characteristic odor. Additionally, small amounts are excreted in sweat and bile. Accumulation in the body with prolonged use is minimal, however, excretion may slow down with impaired liver or kidney function.

References:
https://pubmed.ncbi.nlm.nih.go...
https://pmc.ncbi.nlm.nih.gov/a...
https://link.springer.com/arti...

Mechanisms of Action and Scientific Rationale: Dimethyl Sulfoxide

Liver and Gastrointestinal Tract. At the liver level, dimethyl sulfoxide exerts membrane-stabilizing and antioxidant action, binding free radicals and reducing lipid peroxidation. Interaction with cytochrome P450 enzyme systems manifests in the modulation of metabolic processes and reduction in reactive oxygen species production. In the gastrointestinal tract, dimethyl sulfoxide demonstrates cytoprotective influence, reducing mucosal damage by suppressing the pro-inflammatory NF-κB and MAPK cascades. The nature of interaction with cellular structures is described as additive and protective, with a systemic level of action.
References:
https://pubmed.ncbi.nlm.nih.go...
https://www.sciencedirect.com/...

Immune System. Dimethyl sulfoxide inhibits the activation of NF-κB and the JAK/STAT signaling pathway, leading to reduced production of cytokines such as interleukin-1β, interleukin-6, and tumor necrosis factor-α. At the cellular level, a decrease in macrophage and neutrophil activity, as well as reduced leukocyte adhesion to the endothelium, is observed. This effect is modulating and anti-inflammatory in nature, contributing to the control of excessive inflammatory response.
References:
https://pmc.ncbi.nlm.nih.gov/articles/PMC5021772
https://link.springer.com/arti...

Nervous System. Dimethyl sulfoxide exhibits analgesic and neuroprotective properties associated with the stabilization of neuronal membrane potentials and modulation of ion channels. Influence on NMDA receptors leads to reduced neuronal excitability, accompanied by decreased transmission of pain signals. Additionally, potentiation of antioxidant mechanisms in the central nervous system and reduction of neuronal damage under oxidative stress are noted. The nature of the action is potentiating and cell-specific.
References:
https://pubmed.ncbi.nlm.nih.gov/21847652/
https://www.tandfonline.com/do...

Endocrine and Metabolic Regulation. The influence of dimethyl sulfoxide on endocrine-metabolic processes is associated with changes in the eicosanoid profile and regulation of oxylipin metabolism. At the level of cellular metabolism, the substance demonstrates lipotropic properties, modulating the activity of lipid metabolism enzymes and stabilizing mitochondrial membranes. The action is additive and systemic in nature, accompanied by antioxidant and membrane-stabilizing activity.
References:
https://pubmed.ncbi.nlm.nih.go...
https://onlinelibrary.wiley.com/doi/10.1002/jps.2600600623

Conclusion. The mechanisms of action of the preparation represent a combination of tissue-specific and cellular levels of influence, including inhibition of inflammatory mediators, antioxidant protection, modulation of the immune response, and stabilization of membrane structures. This provides a comprehensive, scientifically based pharmacological action of the preparation.
Reference: WHO Monographs on Selected Medicinal Plants Vol. 4; MedlinePlus Herbal Database; Semantic Scholar ID: 5fbc42d57b1c3