Usage
Ethamsylate is prescribed for the prevention and treatment of capillary bleeding, including:
- Menorrhagia: Abnormally heavy or prolonged menstrual bleeding.
- Dysfunctional Uterine Bleeding (DUB): Vaginal bleeding that is irregular and unrelated to normal menstruation.
- Perioperative Bleeding: Bleeding during, before, or after surgical procedures, especially delicate surgeries.
- Other Capillary Bleeding: Such as epistaxis (nosebleeds), hematuria (blood in urine), and bleeding from small blood vessels.
Pharmacological Classification: Hemostatic agent, antifibrinolytic.
Mechanism of Action: Ethamsylate works by enhancing platelet adhesion and improving capillary resistance, which helps to control and reduce bleeding from small blood vessels. It is thought to inhibit the biosynthesis and action of certain prostaglandins that contribute to platelet disaggregation, vasodilation, and increased capillary permeability.
Alternate Names
- International Nonproprietary Name (INN): Etamsylate
- Brand Names: Dicynone, Cyclonamine, Alstat, and various others.
How It Works
Pharmacodynamics: Ethamsylate primarily acts by enhancing primary hemostasis. It increases platelet adhesiveness and strengthens capillary walls, thereby reducing capillary fragility and permeability. It does not affect the normal coagulation cascade or alter prothrombin time, fibrinolysis, or platelet count.
Pharmacokinetics:
- Absorption: Well-absorbed after oral administration. Peak plasma levels are reached within approximately 1 hour.
- Metabolism: Limited information is available regarding the specific metabolic pathways of ethamsylate.
- Elimination: Primarily excreted in the urine, with about 85% of the administered dose eliminated within the first 24 hours. The plasma half-life is approximately 2 hours.
Mode of Action: While the precise mechanism is not fully elucidated, it appears to promote interaction between platelets and the vascular endothelium, improving the formation of the platelet plug. Its anti-inflammatory properties may also contribute to its hemostatic effects. It does not have adrenergic or vasoconstrictor activity.
Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Ethamsylate’s mode of action does not primarily involve receptor binding, direct enzyme inhibition, or neurotransmitter modulation. It primarily affects platelet function and capillary resistance.
Dosage
Standard Dosage
Adults:
- Oral: 250-500 mg every 4-6 hours as needed.
- Intravenous (IV) or Intramuscular (IM): 250-500 mg every 4-6 hours as needed.
Children:
- Dosage should be reduced based on weight or age. Typically, half the adult dose is recommended.
- Neonates: 10 mg/kg body weight IV/IM every 6 hours.
Pediatric safety should be carefully considered, and treatment is usually initiated within 2 hours of birth in neonates requiring this medication.
Special Cases:
- Elderly Patients: Dosage adjustments may be needed based on renal function.
- Patients with Renal Impairment: Dose reduction may be required depending on the degree of impairment.
- Patients with Hepatic Dysfunction: No specific dosage adjustments are typically recommended.
- Patients with Comorbid Conditions: Use with caution in patients with porphyria, bronchial asthma, or hypotension.
Clinical Use Cases:
- Intubation: Can be used to minimize bleeding risk.
- Surgical Procedures: Prophylactically before, during, or after surgery to control capillary bleeding.
- Mechanical Ventilation: May be beneficial in reducing bleeding complications.
- Intensive Care Unit (ICU) Use: For managing active bleeding or preventing bleeding risks.
- Emergency Situations: IV/IM administration for acute capillary hemorrhage.
Dosage Adjustments:
Dose modifications are often necessary in patients with renal impairment, depending on the level of kidney function. For hepatic dysfunction, no specific dosage adjustments are usually required.
Side Effects
Common Side Effects:
- Headache
- Nausea
- Skin rash
- Dizziness
- Injection site reactions (pain, redness) with parenteral administration
Rare but Serious Side Effects:
- Severe allergic reactions (anaphylaxis)
- Severe hypotension (especially with IV administration)
Long-Term Effects:
Limited information is available on the long-term effects of ethamsylate use.
Adverse Drug Reactions (ADR):
Anaphylaxis, although rare, requires immediate medical intervention. Severe hypotension, particularly with IV administration, can also be a serious ADR.
Contraindications
- Hypersensitivity to ethamsylate or any component of the formulation.
- Porphyria
- Bronchial asthma (especially when using formulations containing sulfites)
Drug Interactions
- Anticoagulants (e.g., warfarin, heparin): May increase the risk of bleeding.
- Antiplatelet agents (e.g., aspirin, clopidogrel): May potentiate the anticoagulant effect.
- Thiamine (Vitamin B1): Intravenous ethamsylate formulations containing sulfites may inactivate thiamine.
- Dextran: If co-administration is necessary, ethamsylate should be administered first.
Pregnancy and Breastfeeding
- Pregnancy: Limited data are available regarding the safety of ethamsylate in pregnancy. Use only if the potential benefit outweighs the risk to the fetus. Not recommended during the first trimester.
- Breastfeeding: It is unknown whether ethamsylate is excreted in breast milk. Avoid use during breastfeeding or discontinue breastfeeding while taking this medication.
Drug Profile Summary
- Mechanism of Action: Enhances platelet adhesion, strengthens capillary walls, and inhibits some prostaglandins involved in bleeding.
- Side Effects: Headache, nausea, skin rash, dizziness. Rarely, severe allergic reaction or hypotension.
- Contraindications: Hypersensitivity, porphyria, bronchial asthma.
- Drug Interactions: Anticoagulants, antiplatelet agents, thiamine, dextran.
- Pregnancy & Breastfeeding: Use with caution in pregnancy; avoid during breastfeeding.
- Dosage: Adults: 250-500 mg PO/IV/IM every 4-6 hours; Children: Reduced dose; Neonates: 10 mg/kg IV/IM every 6 hours.
- Monitoring Parameters: Bleeding time, blood pressure.
Popular Combinations
Ethamsylate is sometimes used in combination with tranexamic acid, another antifibrinolytic agent, to manage heavy menstrual bleeding or other bleeding disorders.
Precautions
- General Precautions: Assess for any history of hypersensitivity, porphyria, or bronchial asthma. Monitor blood pressure, especially with IV administration.
- Specific Populations: Use with caution in pregnancy, avoid during breastfeeding, and reduce the dose in children and patients with renal impairment.
- Lifestyle Considerations: No specific lifestyle restrictions are generally associated with ethamsylate use.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ethamsylate?
A: Adults: 250-500 mg orally, IV, or IM every 4-6 hours. Children: Half the adult dose. Neonates: 10 mg/kg IV/IM every 6 hours.
Q2: How does Ethamsylate work to stop bleeding?
A: It increases platelet adhesiveness, reinforces capillary walls, and inhibits prostaglandins that promote bleeding.
Q3: What are the common side effects of Ethamsylate?
A: Headache, nausea, skin rashes, dizziness, and injection site reactions (for IV/IM administration).
Q4: Is Ethamsylate safe during pregnancy?
A: Limited data are available. Use with caution and only if the potential benefits outweigh the risks to the fetus. Avoid use during the first trimester.
Q5: Can I take Ethamsylate while breastfeeding?
A: It’s generally recommended to avoid ethamsylate during breastfeeding.
Q6: What are the contraindications for Ethamsylate use?
A: Hypersensitivity to ethamsylate, porphyria, and bronchial asthma.
Q7: Does Ethamsylate interact with any other medications?
A: Yes, it can interact with anticoagulants, antiplatelet drugs, thiamine, and dextran.
Q8: What should I do if I miss a dose of Ethamsylate?
A: Take the missed dose as soon as you remember unless it’s close to the time for your next dose. Don’t double the dose to catch up.
Q9: How is Ethamsylate administered?
A: It can be taken orally, intravenously (IV), or intramuscularly (IM), depending on the clinical situation.
