Usage
- Ozagrel is prescribed for the treatment of acute ischemic stroke and improvement of cerebrovascular spasms and associated symptoms of cerebral ischemia after subarachnoid hemorrhage surgery. It is also used to improve movement disorders associated with acute cerebral thrombosis. Additionally, some formulations are used for the treatment of bronchial asthma.
- Pharmacological classification: Ozagrel is classified as a selective thromboxane A2 synthase inhibitor and an antiplatelet agent.
- Mechanism of action: Ozagrel inhibits thromboxane A2 synthase, the enzyme responsible for the production of thromboxane A2, a potent vasoconstrictor and platelet aggregator. This inhibition leads to decreased platelet aggregation and improved blood flow in ischemic areas. It also promotes prostacyclin production, a vasodilator and inhibitor of platelet aggregation, thereby contributing to the balance of these two mediators.
Alternate Names
- International Nonproprietary Name (INN): Ozagrel
- Other Names: Ozagrel sodium, Ozagrel hydrochloride, Ozagrel hydrochloride hydrate
- Brand names: Examples include Pulmoza, Strozagel, Ozaflo (India), OZAC (various regions). Brand names can vary regionally.
How It Works
- Pharmacodynamics: Ozagrel primarily acts by inhibiting thromboxane A2 synthase. This leads to a decrease in thromboxane A2 levels and reduced platelet aggregation, promoting vasodilation and improving blood flow, especially in ischemic areas.
- Pharmacokinetics: Ozagrel is available in both oral (for asthma) and intravenous formulations. Following intravenous administration, the drug reaches peak plasma concentrations rapidly. The elimination half-life is approximately 2 hours, with primarily renal excretion within 24 hours. After oral administration for asthma, it is rapidly absorbed, and its metabolism does not produce pharmacologically active metabolites. It achieves peak plasma concentration within 2 hours. The elimination half-life is around 2 hours, with primarily renal excretion.
- Mode of action: Ozagrel selectively targets thromboxane A2 synthase, inhibiting the conversion of prostaglandin H2 to thromboxane A2. It does not directly inhibit cyclooxygenase (COX) enzymes.
- Receptor binding, enzyme inhibition, or neurotransmitter modulation: Ozagrel specifically inhibits thromboxane A2 synthase. It does not directly affect other prostanoid receptors or pathways.
- Elimination pathways: Ozagrel is primarily eliminated through renal excretion.
Dosage
Standard Dosage
Adults:
- Intravenous (for stroke/cerebral ischemia): 80 mg twice daily, infused over 2 hours, or 80 mg infused over 24 hours (dosing may vary depending on the indication). Treatment duration typically ranges from 1 to 2 weeks.
- Oral (for asthma): 200mg twice daily after breakfast and before bedtime. Treatment duration is determined based on individual patient response and clinical judgment.
Children:
- The safety and efficacy of ozagrel have not been established in children. Use with extreme caution if benefits outweigh risks, and under strict medical supervision.
Special Cases:
- Elderly Patients: Use with caution due to potential age-related decline in renal function. Dosage adjustment may be necessary. Close monitoring of renal function is recommended.
- Patients with Renal Impairment: Dosage adjustment is required based on the degree of impairment. Close monitoring of renal function is necessary.
- Patients with Hepatic Dysfunction: Exercise caution in patients with hepatic dysfunction as drug clearance might be affected. Close monitoring of liver function tests is recommended. Dosage adjustments may be required.
- Patients with Comorbid Conditions: Careful consideration and potential dosage adjustments are necessary for patients with bleeding disorders, cardiovascular disease, or other relevant comorbidities.
Clinical Use Cases
- Intubation: Not specifically indicated for intubation.
- Surgical Procedures (Post-subarachnoid hemorrhage): 80mg twice daily, infused over 2 hours, or 80mg infused over 24 hours. The treatment duration is typically 1-2 weeks.
- Mechanical Ventilation: Not specifically indicated for mechanical ventilation.
- Intensive Care Unit (ICU) Use: Administered in the ICU setting for patients with stroke, cerebral ischemia following subarachnoid hemorrhage, or cerebral thrombosis. The dosage is typically 80mg twice daily, infused over 2 hours, or 80mg infused over 24 hours. The duration is typically 1-2 weeks, based on clinical judgment.
- Emergency Situations: Data for specific emergency situations are limited.
Dosage Adjustments
- Dose modifications are necessary for patients with renal or hepatic impairment, based on the severity of the dysfunction.
- Close monitoring of coagulation parameters and possible dosage adjustments are necessary when co-administered with anticoagulants or antiplatelet agents.
Side Effects
Common Side Effects
- Nausea, vomiting, gastrointestinal discomfort, diarrhea, headache, dizziness, rash, itching, injection site reactions.
Rare but Serious Side Effects
- Bleeding (including gastrointestinal bleeding, intracranial bleeding, skin bleeding), thrombocytopenia, allergic reactions (including anaphylaxis), acute renal failure, liver dysfunction, jaundice.
Long-Term Effects
- Limited data are available on long-term effects. Chronic complications with prolonged use are possible but not extensively studied.
Adverse Drug Reactions (ADR)
- Severe allergic reactions (anaphylaxis), significant bleeding, acute renal failure, severe liver dysfunction require immediate medical attention.
Contraindications
- Hypersensitivity to ozagrel or its components.
- Active bleeding or history of bleeding disorders (e.g., hemorrhagic stroke, peptic ulcer).
- Severe hepatic or renal impairment.
- Pregnancy and breastfeeding (unless absolutely necessary and after careful risk-benefit assessment).
Drug Interactions
- Anticoagulants and antiplatelet agents: (e.g., warfarin, heparin, aspirin) Increased risk of bleeding. Close monitoring of coagulation parameters is crucial.
- NSAIDs: (e.g., ibuprofen, naproxen) Increased risk of gastrointestinal bleeding.
- Drugs affecting liver enzyme activity: (e.g., rifampin, ketoconazole) Altered metabolism of ozagrel.
Pregnancy and Breastfeeding
- Ozagrel is generally not recommended during pregnancy and breastfeeding due to limited safety data. It should only be used if the potential benefits clearly outweigh the risks to the fetus or infant. There are no adequate and well-controlled studies on pregnant women. Its presence in breastmilk and potential effects on the infant are unknown. Consultation with a physician is necessary if its use during pregnancy or breastfeeding is being considered.
Drug Profile Summary
- Mechanism of Action: Thromboxane A2 synthase inhibitor.
- Side Effects: Nausea, vomiting, headache, dizziness, rash, itching, bleeding.
- Contraindications: Hypersensitivity, active bleeding, severe hepatic/renal impairment.
- Drug Interactions: Anticoagulants, antiplatelet agents, NSAIDs.
- Pregnancy & Breastfeeding: Not recommended unless absolutely necessary. Consult a physician.
- Dosage: IV: 80 mg twice daily or 80mg once daily, Oral: 200mg twice daily.
- Monitoring Parameters: Liver function tests, renal function, bleeding signs, complete blood count (especially platelet count).
Popular Combinations
- Specific popular combinations are not widely established. Clinicians may combine ozagrel with other therapies based on individual patient needs and specific clinical scenarios.
Precautions
- General Precautions: Assess for allergies, bleeding disorders, hepatic/renal function before initiating therapy. Monitor for bleeding and other adverse effects during treatment.
- Specific Populations: Use cautiously in elderly patients, pregnant/breastfeeding women (only if absolutely necessary). Pediatric use not established.
- Lifestyle Considerations: Alcohol consumption should be limited due to unknown interactions. Smoking cessation is advisable as it can affect drug metabolism and exacerbate underlying respiratory conditions.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ozagrel?
A: For adults with stroke/cerebral ischemia, the recommended intravenous dosage is 80 mg twice daily, infused over 2 hours, or 80 mg infused over 24 hours. For bronchial asthma, the oral dose is 200mg twice daily. Pediatric dosing is not established.
Q2: What are the main contraindications to using Ozagrel?
A: Ozagrel is contraindicated in patients with hypersensitivity to the drug, active bleeding, severe hepatic or renal impairment.
Q3: How does Ozagrel interact with other antiplatelet medications?
A: Co-administration with other antiplatelet drugs or anticoagulants can increase the risk of bleeding. Close monitoring of coagulation parameters and potential dosage adjustments are required.
Q4: Can Ozagrel be used during pregnancy or breastfeeding?
A: Ozagrel is generally not recommended during pregnancy or breastfeeding unless absolutely necessary and the benefits clearly outweigh the potential risks to the fetus/infant.
Q5: What are the common side effects associated with Ozagrel?
A: Common side effects include nausea, vomiting, gastrointestinal discomfort, headache, dizziness, rash, and itching.
Q6: What is the mechanism of action of Ozagrel?
A: Ozagrel selectively inhibits thromboxane A2 synthase, reducing thromboxane A2 production and thereby inhibiting platelet aggregation and promoting vasodilation.
Q7: How is Ozagrel eliminated from the body?
A: Ozagrel is primarily eliminated through renal excretion.
Q8: What should be monitored in patients receiving Ozagrel?
A: Monitor for signs of bleeding, changes in liver and kidney function, and complete blood count, especially platelet count.
Q9: Are there any specific dietary recommendations for patients taking Ozagrel?
A: While there are no specific dietary restrictions, general healthy dietary practices are recommended, especially for patients with cardiovascular conditions. Limit alcohol intake.
Q10: What are the alternative treatment options if Ozagrel is contraindicated?
A: Alternative antiplatelet agents or other treatment strategies should be considered based on the patient’s specific condition and clinical judgment. Consult with a specialist.
