Usage
Sovateltide is prescribed for the treatment of acute cerebral ischemic stroke (ACIS) in adults. It is classified as a neuroprotective agent and a selective endothelin B receptor agonist. Sovateltide’s mechanism of action involves stimulating neural progenitor cells, promoting neurovascular remodeling (forming new neurons and blood vessels), increasing blood flow, demonstrating anti-apoptotic activity, and protecting and enhancing neural mitochondria biogenesis.
Alternate Names
Sovateltide is also known as PMZ-1620 and IRL-1620. It is marketed under the brand name Tyvalzi in India.
How It Works
Pharmacodynamics: Sovateltide primarily acts as an agonist at endothelin B (ETB) receptors in the brain. This leads to neuroprotection, neurogenesis (formation of new neurons), and improved cerebral blood flow. It protects neural mitochondria and enhances their biogenesis.
Pharmacokinetics: Sovateltide is administered intravenously. Following IV administration, the drug rapidly distributes to tissues. In vitro metabolism studies have revealed 83–85% protein binding. The drug is primarily excreted through the urine.
Mode of Action: Sovateltide selectively binds to and activates ETB receptors. This activation triggers a cascade of intracellular events promoting neuronal survival, growth, and repair. The specific downstream pathways and molecular mechanisms involved are still being elucidated.
Receptor binding, enzyme inhibition, or neurotransmitter modulation: Sovateltide is a selective ETB receptor agonist. Current research does not indicate direct enzyme inhibition or neurotransmitter modulation.
Elimination pathways: Sovateltide is primarily eliminated through renal excretion.
Dosage
Standard Dosage
Adults:
0.3 µg/kg body weight per dose, administered as an intravenous bolus over one minute. Three doses are given per day, at intervals of 3 hours ± 1 hour. The treatment is initiated within 24 hours of stroke onset, with repeat doses on days 3 and 6, for a total of nine doses.
Children:
The safety and efficacy of sovateltide in pediatric patients have not been established.
Special Cases:
- Elderly Patients: No specific dose adjustments are mentioned for elderly patients, but clinical experience is limited.
- Patients with Renal Impairment: Dosage modifications may be required; consult current research for specific recommendations.
- Patients with Hepatic Dysfunction: Dosage modifications may be required; consult current research for specific recommendations.
- Patients with Comorbid Conditions: Exercise caution in patients with severe cardiovascular diseases or uncontrolled hypertension.
Clinical Use Cases
Specific dosage guidelines for intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations are not currently defined. The drug’s primary indication is for acute ischemic stroke within 24 hours of onset.
Dosage Adjustments
Adjustments may be needed based on individual patient response and tolerability. Refer to the latest research for specific clinical recommendations.
Side Effects
Common Side Effects
Headache, dizziness, nausea, fatigue.
Rare but Serious Side Effects
Hypotension, allergic reactions (rash, itching, swelling, severe dizziness, difficulty breathing), abdominal discomfort, vomiting.
Long-Term Effects
Long-term effects are not yet fully characterized due to the drug’s relatively recent introduction.
Adverse Drug Reactions (ADR)
Severe allergic reactions (anaphylaxis), significant hypotension requiring intervention.
Contraindications
Hypersensitivity to sovateltide or its components. Pregnancy and breastfeeding (safety not established). Severe cardiovascular diseases, uncontrolled hypertension. Active bleeding or bleeding disorders. Recent major surgery or trauma. Concurrent participation in other therapeutic clinical trials. Any life-threatening condition that would prevent study completion or where sovateltide would be contraindicated or harmful.
Drug Interactions
Drug interactions are still under investigation. Caution is advised with medications affecting blood pressure or vascular tone (antihypertensives, vasodilators, vasoconstrictors), NSAIDs, and drugs impacting renal function. Patients should disclose all concomitant medications, including OTC drugs and supplements.
Pregnancy and Breastfeeding
Sovateltide is contraindicated during pregnancy and breastfeeding due to insufficient safety data.
Drug Profile Summary
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Mechanism of Action: Selective endothelin B receptor agonist, promoting neuroprotection, neurogenesis, and cerebral blood flow.
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Side Effects: Headache, dizziness, nausea, fatigue, hypotension, allergic reactions.
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Contraindications: Hypersensitivity, pregnancy, breastfeeding, severe cardiovascular disease, uncontrolled hypertension, bleeding disorders.
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Drug Interactions: Potential interactions with drugs affecting blood pressure, renal function, and NSAIDs.
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Pregnancy & Breastfeeding: Contraindicated.
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Dosage: 0.3 µg/kg IV bolus, three doses per day on days 1, 3, and 6, initiated within 24 hours of stroke onset.
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Monitoring Parameters: Blood pressure, heart rate, neurological status, signs of allergic reactions.
Popular Combinations
Combinations with other stroke therapies are still being investigated. Standard supportive care is usually provided alongside Sovateltide.
Precautions
Standard pre-screening for allergies and organ dysfunction. Close monitoring of blood pressure and other vital signs during and after administration. Caution in patients with pre-existing cardiovascular conditions. Safety in children, pregnant/breastfeeding women not established. No data on effects on driving ability.
FAQs
Q1: What is the recommended dosage for Sovateltide?
A: 0.3 µg/kg body weight/dose IV bolus over one minute, three doses/day at (3 ± 1) hour intervals, on days 1, 3, and 6. Treatment should be initiated within 24 hours of stroke onset.
Q2: What is the mechanism of action of Sovateltide?
A: Sovateltide is a selective endothelin B receptor agonist that stimulates neural progenitor cells, improves cerebral blood flow, and reduces neuronal cell death.
Q3: What are the common side effects of Sovateltide?
A: Headache, dizziness, nausea, and fatigue are the most common side effects.
Q4: Is Sovateltide safe for use in pregnant or breastfeeding women?
A: No. Sovateltide is contraindicated in pregnancy and breastfeeding as its safety has not been established in these populations.
Q5: Are there any known drug interactions with Sovateltide?
A: Interactions with medications affecting blood pressure, renal function, and NSAIDs are possible. Patients should inform their physician about all concomitant medications.
Q6: What are the contraindications for Sovateltide?
A: Hypersensitivity to the drug, pregnancy, breastfeeding, severe cardiovascular diseases, uncontrolled hypertension, active bleeding, recent major surgery or trauma are contraindications.
Q7: How is Sovateltide administered?
A: Sovateltide is administered as an intravenous bolus over one minute.
Q8: What is the role of Sovateltide in acute ischemic stroke management?
A: Sovateltide is indicated for improving neurological recovery and reducing the incidence of disability following acute ischemic stroke.
Q9: When should Sovateltide treatment be initiated after stroke onset?
A: Sovateltide treatment should be initiated within 24 hours of the onset of stroke symptoms.
Q10: What monitoring parameters should be considered when administering Sovateltide?
A: Close monitoring of vital signs, particularly blood pressure, and neurological status is essential. Be vigilant for signs of allergic reactions.
