Usage
This combination is primarily prescribed for the treatment of melasma and hyperpigmentation. Melasma presents as brown patches, mostly on the face, while hyperpigmentation refers to any darkening of the skin due to increased melanin production. Additionally, this combination may be used for general skin brightening and anti-aging purposes. This drug’s pharmacological classifications include antioxidant, skin lightening agent, and antifibrinolytic.
The mechanism of action involves multiple pathways: Tranexamic acid inhibits plasminogen activation, thereby reducing inflammation and melanin production. Ascorbic acid (Vitamin C) acts as an antioxidant, protecting against UV damage and promoting collagen synthesis. Glutathione, also an antioxidant, helps to detoxify the skin and further inhibit melanin production. These combined actions result in a synergistic effect on skin lightening and overall improvement in skin health.
Alternate Names
No specific alternate names exist for this particular combination. It may be referenced by its constituent ingredients.
Brand names under which this combination is marketed include Tenxima 3D Glow and Bloomberg Forte.
How It Works
Pharmacodynamics: Tranexamic acid exerts its effect by inhibiting plasminogen activator, which reduces inflammation and melanogenesis. Both L-Ascorbic acid and glutathione act as potent antioxidants, scavenging free radicals and protecting against UV-induced skin damage. Ascorbic acid also contributes to collagen synthesis, improving skin texture and elasticity. Glutathione aids in skin detoxification.
Pharmacokinetics: Ascorbic acid is readily absorbed orally, and any excess is excreted renally. Glutathione, when taken orally, has limited bioavailability but can be administered intravenously for better absorption. Tranexamic acid is also well-absorbed orally and is primarily excreted unchanged in the urine. It’s metabolized in the liver via hydrolysis to inactive metabolites. More research is needed to fully elucidate the pharmacokinetics of this specific combination.
Mode of Action: Tranexamic acid targets the plasminogen activation system, which is involved in inflammation and melanogenesis. Ascorbic acid stimulates collagen synthesis and protects against oxidative stress. Glutathione, acting as an antioxidant, aids in detoxification pathways and inhibits tyrosinase, an enzyme involved in melanin production.
Elimination Pathways: Tranexamic acid is primarily eliminated through renal excretion. Ascorbic acid and its metabolites are also eliminated renally. Glutathione is metabolized within cells and ultimately excreted as various metabolites.
Dosage
Standard Dosage
Children: Use in children below 12 years of age is generally not recommended unless specifically prescribed by a pediatrician.
Special Cases:
- Elderly Patients: Dosage adjustments may be necessary based on renal function.
- Patients with Renal Impairment: Dose reduction may be needed in moderate to severe renal impairment.
- Patients with Hepatic Dysfunction: Caution is advised, and dosage adjustments may be required.
- Patients with Comorbid Conditions: Use with caution in patients with thromboembolic disorders, bleeding or clotting disorders, or seizure disorders.
Clinical Use Cases
The combination is typically not used in clinical settings like intubation, surgical procedures, mechanical ventilation, or the ICU. Its primary use is for dermatological purposes.
Dosage Adjustments
Dose adjustments may be necessary in patients with renal or hepatic impairment, or those with other comorbid conditions as described above.
Side Effects
Common Side Effects
Nausea, diarrhea, abdominal cramps or pain, headache, dry skin, rash, redness, itching.
Rare but Serious Side Effects
Allergic reactions (rash, itching, swelling, difficulty breathing), severe stomach pain, seizures (rarely), thromboembolic events.
Long-Term Effects
The long-term effects of this specific combination require further investigation, although prolonged use of high doses of ascorbic acid could potentially increase the risk of kidney stones.
Adverse Drug Reactions (ADR)
Clinically significant ADRs include allergic reactions, seizures, and thromboembolic events.
Contraindications
Hypersensitivity to any of the components, active intravascular clotting disorders, severe renal failure, history of seizures, thromboembolic disorders, color vision disorders, subarachnoid bleeding, and current or planned pregnancy.
Drug Interactions
Limited data is available on drug interactions with this specific combination. However, tranexamic acid may interact with anticoagulants and hormonal contraceptives. Ascorbic acid can increase the absorption of iron and interact with certain chemotherapy drugs. Caution should be used when combining with other antioxidants, iron supplements, and anticancer agents.
Pregnancy and Breastfeeding
The safety of this combination during pregnancy and breastfeeding has not been established. It is recommended to avoid use during these periods unless the potential benefits clearly outweigh the risks.
Drug Profile Summary
- Mechanism of Action: Tranexamic acid inhibits plasminogen activation, reducing inflammation and melanogenesis; Ascorbic acid and Glutathione act as antioxidants and inhibit melanin production; Ascorbic acid also promotes collagen synthesis.
- Side Effects: Nausea, diarrhea, abdominal cramps, headache, dry skin, rash, itching (common); Allergic reactions, severe stomach pain, seizures, thromboembolic events (rare but serious).
- Contraindications: Hypersensitivity, active intravascular clotting, severe renal failure, seizure history, thromboembolic disorders.
- Drug Interactions: Limited data, potential interactions with anticoagulants, hormonal contraceptives, iron supplements, and some chemotherapy drugs.
- Pregnancy & Breastfeeding: Avoid unless benefits outweigh risks.
- Dosage: Typically, one tablet/capsule daily; adjust for renal/hepatic impairment.
- Monitoring Parameters: Monitor for signs of allergic reactions, thromboembolic events, and changes in renal function.
Popular Combinations
This combination itself is a popular choice for addressing hyperpigmentation.
Precautions
Screen for allergies, renal/hepatic dysfunction, and bleeding disorders before prescribing. Advise patients about potential side effects and drug interactions. Caution is needed in patients with a history of seizures, thromboembolic disorders, and renal impairment. Avoid alcohol consumption after taking the medicine. Use cautiously in pregnant or breastfeeding individuals and children.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for L Ascorbic acid + L Glutathione Reduced + Tranexamic Acid?
A: The typical dosage is one tablet or capsule daily, usually taken with a meal. Dosage may be adjusted based on individual response and tolerance under the supervision of a healthcare professional.
Q2: What are the primary uses of this combination therapy?
A: Primarily used for the treatment of melasma and hyperpigmentation, and as an adjunct in skin brightening and anti-aging regimens.
Q3: How does tranexamic acid contribute to skin lightening?
A: Tranexamic acid inhibits plasmin, reducing inflammation and the subsequent stimulation of melanocytes, which produce melanin.
A: Ascorbic acid acts as a potent antioxidant, scavenging free radicals, promoting collagen synthesis, and contributing to skin brightening.
Q5: How does glutathione work to improve skin health?
A: Glutathione acts as an antioxidant, detoxifies the skin, and inhibits tyrosinase, an enzyme involved in melanin production.
Q6: Are there any specific contraindications for this combination?
A: Yes, contraindications include hypersensitivity to any of the components, active intravascular clotting disorders, severe renal failure, history of seizures, and pregnancy.
Q7: What are the potential side effects patients should be aware of?
A: Common side effects include nausea, diarrhea, abdominal discomfort, headache, dry skin, rash, itching. Rare but serious side effects include allergic reactions, thromboembolic events, and seizures.
Q8: Can this combination be used during pregnancy or breastfeeding?
A: It’s generally recommended to avoid use during pregnancy and breastfeeding due to limited safety data, unless benefits clearly outweigh the risks.
Q9: Is this medication suitable for all age groups?
A: It’s generally not recommended for children under 12 years old unless specifically prescribed by a pediatrician. Dosage adjustments may be necessary for elderly patients.