Ischelium Dihydroergotoxine Methanesulfonate Sustained‑Release Tablets

1. Indications and Usage
Dihydroergotoxine Methanesulfonate Sustained-Release Tablets are indicated for the treatment of:
Cerebrovascular disease sequelae.
Mild vascular dementia in elderly patients.
2. Dosage and Administration
Standard Dose: The usual dosage is one tablet (2.5 mg) taken orally twice daily (morning and evening).
Administration: Should be taken after meals. As this is a sustained-release formulation, the tablet must be swallowed whole and should not be chewed, crushed, or split.
Elderly Patients: Due to potentially higher plasma concentrations in elderly patients, dosage adjustment may be necessary based on physician guidance.
3. Mechanism of Action
Metabolic Improvement: The drug improves neuronal metabolism by inhibiting ATPase and adenylate cyclase activity, reducing ATP breakdown, and improving cellular energy balance. It facilitates the shift from anaerobic to aerobic glucose metabolism, increasing neuronal energy and improving microcirculation.
Neurotransmitter Modulation: It directly acts on central nervous system dopamine and 5-hydroxytryptamine (serotonin) receptors, enhancing neurotransmitter release and improving neural transmission.
Vasodilation: It blocks alpha-adrenergic receptors, relieving vascular spasms and reducing vascular resistance, thereby increasing cerebral blood flow and oxygen utilization.
4. Safety and Warnings
Contraindications: This medication is contraindicated in patients with hypersensitivity to the product, hypotension, severe bradycardia, organic heart disease, impaired renal function, and pregnant women.
Warnings:
Must be used under strict medical supervision. It is not indicated for any acute or chronic psychiatric conditions.
Fibrosis Risk: There are reported cases of fibrotic reactions (e.g., pulmonary interstitial fibrosis, myocardial fibrosis, heart valve fibrosis, and retroperitoneal fibrosis) associated with 5-HT2β receptor agonism. Patients at risk for fibrosis should use this product with caution.
Pediatric Use: Contraindicated in children due to unestablished safety and efficacy.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: The drug is generally well-tolerated. During the initial phase of treatment, patients may experience transient nausea, gastric discomfort, vomiting, and facial flushing.
Cardiovascular Effects: Postural hypotension may occur; blood pressure monitoring is recommended.
Serious Adverse Reactions: Rare but severe fibrotic reactions (as noted in warnings) and symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain, and peripheral vasoconstriction).
6. Drug Interactions
Anticoagulants and Antihypertensives: Concomitant use may enhance the activity of this product.
Other Ergot Alkaloids: Concurrent administration with other ergot alkaloid derivatives may exacerbate adverse reactions.
7. Pharmaceutical Information
Active Ingredient: Dihydroergotoxine Methanesulfonate (a mixture of equal parts dihydroergocornine, dihydroergocristine, and dihydroergocryptine mesylates).
Strengths: 2.5 mg sustained-release tablets.
Appearance: White tablets with a score line on one side.
Storage: Store in a tightly sealed container, protected from light.
Shelf Life: 24 months.