Proanthocyanidin + Tranexamic Acid

Usage

This combination medication is primarily used in the treatment of hyperpigmentation (melasma), a condition characterized by darkened patches of skin due to increased melanin production. It is also used to manage heavy menstrual bleeding (menorrhagia).

• Pharmacological Classification: Proanthocyanidin is classified as a phytochemical, antioxidant, and anti-inflammatory agent. Tranexamic acid is an antifibrinolytic agent.

• Mechanism of Action: Proanthocyanidin inhibits tyrosinase, an enzyme crucial for melanin synthesis, and suppresses melanocyte activity, thereby reducing melanin production. Tranexamic acid prevents the breakdown of blood clots, which reduces bleeding. This combination also promotes collagen synthesis and improves skin quality.

Alternate Names

Several brand names exist for this combination, including Oxifine-TX, Qtvit-TX, Melano-TX, Triolite, Nucell-TX, Praxamic, Gse+tx, and Tyrodin Plus. It’s sometimes referred to as Pine Bark Extract + Tranexamic Acid.

How It Works

• Pharmacodynamics: Proanthocyanidin exerts antioxidant and anti-inflammatory effects, protecting blood vessels and promoting collagen and elastin production in the skin. Tranexamic acid, by inhibiting plasminogen activation and subsequent fibrinolysis, stabilizes blood clots and reduces bleeding.

• Pharmacokinetics: The pharmacokinetic profile of the combined formulation isn’t well-defined. Tranexamic acid is readily absorbed orally, with peak plasma levels reached in approximately 3 hours. It is primarily excreted renally. Proanthocyanidin absorption and metabolism data are limited, although it is believed to be well-absorbed after oral administration.

• Mode of Action: Proanthocyanidin targets melanocytes by inhibiting tyrosinase, thus reducing melanin synthesis. Tranexamic acid binds to plasminogen, preventing its conversion to plasmin, the enzyme responsible for dissolving fibrin clots.

• Elimination Pathways: Tranexamic acid is predominantly eliminated unchanged through renal excretion. Information on proanthocyanidin elimination is limited.

Dosage

Dosage information for the combination product is limited. Dosing for tranexamic acid is better defined and will be supplied. Proanthocyanidin dosing is less clear but typical dosages are provided. Always consult with a healthcare professional for personalized dosing recommendations.

Standard Dosage

Adults:

• Tranexamic Acid:

  • For heavy menstrual bleeding: 1000-1500 mg orally three times a day, for up to five days during menstruation. Start taking as soon as bleeding begins.
  • Other bleeding conditions: Consult a physician for appropriate dosing.

• Proanthocyanidin:

  • Typical dosage: 75-150 mg twice daily.

Children:

Use in children is not routinely recommended. Consult a pediatrician if considering use in children. Dosage should be weight based if prescribed, at 25mg/kg per dose at adult frequencies.

Special Cases:

• Elderly Patients: No dose reduction is necessary for tranexamic acid unless renal impairment is present. For proanthocyanidin, dosage adjustments may be needed based on individual health status.
• Patients with Renal Impairment: Dose reduction of tranexamic acid is recommended in patients with renal impairment. Consult specific dosing guidelines based on creatinine clearance.
• Patients with Hepatic Dysfunction: Caution is advised with tranexamic acid in patients with hepatic impairment, although specific dosage adjustments may not be required. Limited information is available regarding proanthocyanidin.
• Patients with Comorbid Conditions: Exercise caution in patients with cardiovascular disease, thromboembolic disorders, or a history of seizures.

Clinical Use Cases

Dosing recommendations for clinical use cases, other than heavy menstrual bleeding, should be determined by a physician based on the specific condition and patient factors.

Dosage Adjustments

Dose modifications may be required based on renal function, hepatic function, and other patient-specific factors. Always consult with a healthcare professional for personalized dosage recommendations.

Side Effects

Common Side Effects

Nausea, vomiting, diarrhea, headache, dizziness, muscle pain, fatigue, stuffy nose, sinusitis.

Rare but Serious Side Effects

Visual disturbances, severe allergic reactions (anaphylaxis), blood clots (thromboembolic events such as deep vein thrombosis or pulmonary embolism), decreased blood pressure.

Long-Term Effects

Chronic complications from prolonged use are rare but may include vision changes and increased risk of thromboembolic events.

Adverse Drug Reactions (ADR)

Serious ADRs include visual changes, angioedema, and thromboembolic complications.

Contraindications

Active intravascular clotting, thrombosis, hypersensitivity to tranexamic acid, subarachnoid hemorrhage, severe renal impairment, color vision impairment, history of thromboembolic events.

Drug Interactions

Tranexamic acid may interact with hormonal contraceptives, clotting factor concentrates, fibrinolytic medications, and some acne medications. Concurrent use of other drugs that increase the risk of thrombosis should be avoided. Consult drug interaction resources for detailed information.

Pregnancy and Breastfeeding

The safety of this combination during pregnancy and breastfeeding is not well-established. Caution is advised. Consult a physician before use during pregnancy or breastfeeding.

Drug Profile Summary

• Mechanism of Action: Proanthocyanidin inhibits melanin synthesis; tranexamic acid inhibits fibrinolysis.
• Side Effects: Nausea, vomiting, diarrhea, headache, dizziness, visual disturbances, thromboembolic events.
• Contraindications: Active clotting disorders, hypersensitivity, subarachnoid hemorrhage, severe renal impairment.
• Drug Interactions: Hormonal contraceptives, clotting factors, fibrinolytics.
• Pregnancy & Breastfeeding: Consult a physician.
• Dosage: Varies depending on indication and patient factors.
• Monitoring Parameters: Menstrual blood loss, signs of thrombosis, vision changes.

Popular Combinations

This combination is typically prescribed as a standalone therapy. Other medications may be added to address specific symptoms or underlying conditions.

Precautions

Screen patients for allergies, bleeding disorders, and renal/hepatic impairment before initiating therapy. Caution is advised in patients with a history of thromboembolic events. Avoid alcohol consumption as it may exacerbate dizziness.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Proanthocyanidin + Tranexamic Acid?

A: The dosage varies based on indication and patient factors. For heavy menstrual bleeding, tranexamic acid is typically dosed at 1000-1500 mg three times daily for up to five days. Proanthocyanidin is typically dosed at 75-150 mg twice daily. Consult a physician for personalized dosing recommendations.

Q2: What are the common side effects?

A: Common side effects include nausea, vomiting, diarrhea, headache, and dizziness.

Q3: Is this combination safe during pregnancy?

A: The safety during pregnancy isn’t well-established. Consult a physician before using this medication during pregnancy.

Q4: Are there any drug interactions I should be aware of?

A: Yes, tranexamic acid can interact with hormonal contraceptives, clotting factors, and fibrinolytic medications. Consult a comprehensive drug interaction resource for a complete list.

Q5: What are the contraindications for this medication?

A: Contraindications include active clotting disorders, hypersensitivity to tranexamic acid, subarachnoid hemorrhage, and severe renal impairment.

Q6: How does Proanthocyanidin work for hyperpigmentation?

A: It inhibits tyrosinase, a key enzyme in melanin synthesis, and reduces melanocyte activity.

Q7: How should I monitor patients on this medication?

A: Monitor for changes in menstrual blood loss (if applicable), signs and symptoms of thrombosis (e.g., leg pain, swelling, shortness of breath), and any vision changes.

Q8: Can this combination be used in children?

A: It’s not routinely recommended for children. If considering its use, consult a pediatrician for appropriate dosing and safety information.

Q9: How long can a patient take this medication for heavy menstrual bleeding?

A: Tranexamic acid should be taken for a maximum of five days during each menstrual cycle.

Q10: What should patients do if they miss a dose?

A: Take the missed dose as soon as remembered unless it’s almost time for the next dose. Do not double the dose to catch up.