Monosemicarbazone Adrenochrome

Approved Uses:

• Control and prevention of capillary bleeding in conditions such as:
• Epistaxis (nosebleed)
• Hematuria
• Hemorrhagic purpura
• Bleeding from wounds, gums, or minor injuries
• Post-surgical bleeding (including dental and ENT surgeries)
• Adjunctive treatment during surgery to reduce intraoperative and postoperative bleeding from capillary sources.

Off-label (Clinically Accepted) Uses:

• Management of hyphaema following ocular trauma or surgery.
• Supportive treatment for capillary fragility syndromes such as hereditary hemorrhagic telangiectasia.
• Reduction of bruising and bleeding in certain dermatologic procedures or minor trauma.

Adults:

• Oral tablets:
  4 to 12 tablets daily in divided doses.
  Preferably taken 1 hour before meals.
• Injection (IM, SC, or slow IV):
  1.5 to 5 mg, given on the evening before surgery and repeated approximately 30 minutes prior to the procedure.

Pediatrics:

• Not well studied; limited safety and efficacy data.
• Use with caution and under direct medical supervision in pediatric patients.
• In neonates or infants, doses should not exceed 0.3 mL of a 5 mg/mL injectable solution.

Elderly:

• No specific dosing adjustments, but cautious use is recommended due to possible age-related organ function decline.

Renal or Hepatic Impairment:

• No clear guidelines available.
• Use cautiously; monitor for adverse effects.
• Dose adjustments may be considered based on clinical response.

Administration Route:

• Oral: Tablets should be swallowed whole with water.
• Injection: Administered intramuscularly, subcutaneously, or by slow intravenous injection.

Monosemicarbazone Adrenochrome is a synthetic derivative of adrenochrome that acts as a hemostatic agent. It works primarily by stabilizing capillary walls and promoting vasoconstriction of small blood vessels, which reduces capillary permeability and microvascular bleeding. It does not exhibit systemic vasopressor effects. The drug exerts its effect locally by enhancing platelet aggregation and improving clot formation, thus reducing bleeding time in capillary beds without affecting the larger vascular system.

• Absorption: Orally administered drug is well absorbed; onset of action is relatively rapid.
• Distribution: Likely localized to vascular and interstitial compartments; specific protein-binding data unknown.
• Metabolism: Presumed hepatic metabolism, but detailed enzymatic pathways are not well established.
• Excretion: Believed to be excreted primarily through the kidneys; elimination half-life and exact clearance values remain undocumented.
• Onset of Action: Generally within minutes for injectable forms; oral forms may take 30–60 minutes.

• Pregnancy:
  Safety in pregnancy has not been adequately established. Use only if clearly needed and when potential benefits outweigh potential risks to the fetus.
• Lactation:
  It is not known whether the drug is excreted in human milk. Caution is advised when administered to breastfeeding women. Monitor infants for any signs of adverse effects if use during lactation is necessary.

• Primary Class: Hemostatic Agent
• Subclass: Capillary Stabilizing/Vasoconstrictor Agent (Non-Sympathomimetic)

• Known hypersensitivity to Monosemicarbazone Adrenochrome or any component of the formulation.
• Patients with severe hypertension.
• Patients with closed-angle glaucoma.
• Presence of thromboembolic disorders.
• Use in patients with significant hepatic or renal dysfunction without close monitoring.

• Use with caution in elderly patients due to the potential for organ sensitivity and reduced clearance.
• Monitor for signs of hypersensitivity reactions including rash, pruritus, or anaphylaxis.
• Avoid use in patients with cardiovascular diseases such as severe hypertension or arrhythmias, due to potential vascular reactivity.
• Injection use requires medical supervision, especially in patients with bleeding disorders or altered coagulation profiles.
• Instruct patients to report any unusual bleeding, dizziness, or signs of clot formation.

Common Side Effects:

• Headache
• Dizziness
• Nausea
• Mild abdominal discomfort
• Injection site pain or irritation

Serious but Rare Side Effects:

• Hypersensitivity reactions (rash, angioedema, anaphylaxis)
• Hypertensive episodes (especially with injection)
• Palpitations or arrhythmias
• Local thrombosis or hematoma at injection site

Severity and Timing:

• Most side effects are mild and transient.
• Injection-related effects occur immediately or within 30 minutes.
• Oral side effects may appear within 1–2 hours of dosing.

• With anticoagulants or antiplatelet drugs: May alter efficacy due to vascular effects; caution advised.
• With antihypertensives: Theoretical antagonistic effect; monitor blood pressure closely.
• With monoamine oxidase inhibitors (MAOIs): Potential additive vasoconstriction; avoid co-administration.
• No well-documented interactions with food or alcohol.
• Enzyme system interactions (e.g., CYP450) are not clearly established.

• No recent changes in global regulatory status.
• No new safety alerts or black box warnings issued.
• No major updates from FDA, WHO, or EMA on indication or dosing.
• Remains in use primarily in certain countries for minor surgical and capillary bleeding applications.

• Temperature: Store below 25°C; ideal storage at 20–25°C.
• Light and Moisture: Protect from light and humidity; store in original container.
• Handling: Keep tightly closed. Do not freeze.
• Injectables: Use immediately after opening; discard any unused portion per standard disposal procedures.
• Tablets: No refrigeration needed. Store in a cool, dry place out of reach of children.