Usage
Ergoloid mesylates are prescribed for the symptomatic management of age-related cognitive decline, including conditions like vascular dementia, Alzheimer’s disease, and primary progressive dementia. It is important to note that ergoloid mesylates do not cure these conditions, but rather aim to alleviate some of the associated symptoms like confusion, memory loss, and mood changes.
It is classified as an ergot alkaloid derivative but lacks the vasoconstrictor properties of the naturally occurring ergot alkaloids. It is also considered a “metabolic enhancer” although the exact mechanism remains unclear. It is believed to potentially improve blood flow and metabolism in the brain.
Alternate Names
- Generic: Ergoloid Mesylates
- Brand Name: Hydergine, Gerimal, Hydergine LC
- Chemical Name: a mixture of dihydroergocornine, dihydroergocristine, and dihydroergocryptine
How It Works
Pharmacodynamics:
Ergoloid mesylates’ precise mechanism of action is not fully understood. However, it’s believed to work through multiple pathways, including interactions with neurotransmitter systems in the brain, particularly the dopaminergic, serotonergic, and adrenergic systems. This modulation may help balance neurotransmitter levels, leading to improved cognitive function, mood, and motivation. It might also increase blood flow and cerebral metabolism in the brain.
Pharmacokinetics:
- Absorption: Rapid but incomplete after oral administration.
- Metabolism: Extensively metabolized in the liver, primarily by CYP3A4 enzymes.
- Elimination: Primarily eliminated through hepatic (liver) routes with a half-life of approximately 2.6 to 5.1 hours. The metabolites then undergo renal excretion.
Cellular/Molecular Level:
Ergoloid mesylates are thought to act as partial agonists or antagonists at various receptor sites, including dopamine D2 receptors and serotonin (5-HT1 and 5-HT2) receptors. Its effects on cerebral blood flow, although not fully understood, are believed to contribute to its therapeutic effects.
Dosage
Standard Dosage
Adults:
The standard oral dosage is 1 mg three times daily. Clinical improvement may not be observed for 3-4 weeks. Higher doses (up to 9mg/day split into three doses) have been studied, but haven’t shown significantly increased efficacy.
Children:
The safety and efficacy of ergoloid mesylates in children have not been established. Therefore, its use is not recommended in pediatric populations.
Special Cases:
- Elderly Patients: Start with the standard adult dose and monitor closely for adverse effects. Dose adjustment may be necessary based on individual patient response and tolerance. This medication is noted in the Beers Criteria as a potentially inappropriate medication for use in patients 65 and older due to lack of efficacy.
- Patients with Renal Impairment: No dosage adjustment is typically needed.
- Patients with Hepatic Dysfunction: Use with caution as the drug undergoes extensive hepatic metabolism. Monitor closely and adjust the dose as needed.
- Patients with Comorbid Conditions: Close monitoring and dosage adjustments may be necessary, especially in patients with cardiovascular disease or other conditions.
Clinical Use Cases
The clinical use of ergoloid mesylates is limited to managing the symptoms of age-related cognitive decline. It is not indicated for specific medical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dosage adjustments may be required based on individual patient response, tolerability, and the presence of renal or hepatic impairment. Drug interactions, particularly with CYP3A4 inhibitors and inducers, should be carefully considered and appropriate dosage modifications made.
Side Effects
Common Side Effects:
Nausea, vomiting, dizziness, drowsiness, flushing, loss of appetite, stomach upset, blurred vision, stuffy or runny nose, lightheadedness, and irritation under the tongue (with sublingual tablets).
Rare but Serious Side Effects:
Slow heartbeat, low blood pressure, fainting, allergic reactions (rash, itching, hives, swelling), breathing difficulty.
Long-Term Effects:
The long-term effects of ergoloid mesylates are not well established. However, chronic use might lead to dependence.
Adverse Drug Reactions (ADR):
Clinically significant ADRs include severe hypotension, bradycardia, and allergic reactions requiring immediate medical attention.
Contraindications
- Hypersensitivity to ergoloid mesylates or other ergot alkaloids.
- Acute or chronic psychosis.
- Concurrent use with potent CYP3A4 inhibitors (azole antifungals, some macrolide antibiotics, HIV protease inhibitors).
- Severe bradycardia (Canadian labeling).
- Severe hypotension (Canadian labeling).
Drug Interactions
Ergoloid mesylates can interact with numerous medications, including:
- CYP3A4 Inhibitors: These can significantly increase ergoloid mesylate levels, increasing the risk of side effects. Examples include azole antifungals (ketoconazole, itraconazole), macrolide antibiotics (clarithromycin, erythromycin), HIV protease inhibitors (ritonavir).
- CYP3A4 Inducers: These can decrease ergoloid mesylate levels, potentially reducing its efficacy.
- Triptan Migraine Medications: Concurrent use can increase the risk of serious side effects like vasospasm. Doses should be separated.
- Vasoconstrictors (e.g., pseudoephedrine): Combined use can synergistically increase blood pressure and risk of peripheral ischemia.
- Other ergot alkaloids: Avoid concurrent use due to the risk of additive effects and ergotism.
Also, avoid concurrent use with tobacco due to increased risk of vasoconstriction.
Pregnancy and Breastfeeding
- Pregnancy: Ergoloid mesylates are generally not recommended during pregnancy due to potential risks to the fetus, including vascular disruption. Limited data is available, but other ergot alkaloids are known to be harmful during pregnancy.
- Breastfeeding: Ergoloid mesylates are not recommended during breastfeeding as their excretion in breast milk is unknown. Other ergot alkaloids are known to be excreted in breast milk and can cause adverse effects in infants.
Drug Profile Summary
- Mechanism of Action: Modulates neurotransmitter systems (dopaminergic, serotonergic, adrenergic), possibly increases cerebral blood flow and metabolism. Exact mechanism unclear.
- Side Effects: Nausea, vomiting, dizziness, drowsiness, flushing, loss of appetite, stomach upset, slow heartbeat, hypotension, allergic reactions.
- Contraindications: Hypersensitivity, psychosis, concurrent use with potent CYP3A4 inhibitors, severe bradycardia/hypotension.
- Drug Interactions: CYP3A4 inhibitors/inducers, triptans, vasoconstrictors, other ergot alkaloids.
- Pregnancy & Breastfeeding: Not recommended.
- Dosage: 1 mg orally three times daily. Maximum 9 mg/day.
- Monitoring Parameters: Blood pressure, heart rate, cognitive function, mood, adverse effects.
Popular Combinations
There are no widely recognized or recommended drug combinations involving ergoloid mesylates. Given its potential for numerous drug interactions and limited efficacy evidence, combining it with other medications for cognitive decline is not typically practiced.
Precautions
- General Precautions: Assess patient’s medical history, including allergies, cardiovascular disease, hepatic/renal impairment, and psychosis. Monitor blood pressure and heart rate.
- Specific Populations: Avoid in pregnancy and breastfeeding. Use with caution in the elderly and those with hepatic impairment.
- Lifestyle Considerations: Avoid smoking and limit alcohol intake as these can exacerbate certain side effects. Advise patients against driving or operating machinery until the drug’s effects are known.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ergoloid Mesylates?
A: The standard adult dosage is 1 mg orally three times a day. The maximum recommended dose is 9 mg/day, though benefits at doses exceeding 3 mg/day have not been demonstrated.
Q2: How long does it take to see results from Ergoloid Mesylates?
A: It may take 3-4 weeks to see improvements in cognitive function after initiating treatment.
Q3: What are the common side effects of Ergoloid Mesylates?
A: Common side effects include nausea, vomiting, dizziness, drowsiness, flushing, loss of appetite, stomach upset, blurred vision, and nasal congestion.
Q4: Is Ergoloid Mesylates safe for pregnant or breastfeeding women?
A: Ergoloid mesylates are generally not recommended for pregnant or breastfeeding women due to limited safety data and the potential risks to the fetus or infant.
Q5: What are the contraindications for Ergoloid Mesylates?
A: Ergoloid mesylates are contraindicated in patients with hypersensitivity to the drug or other ergot alkaloids, acute or chronic psychosis, and concurrent use with potent CYP3A4 inhibitors. Severe hypotension and bradycardia are also contraindications.
Q6: How does Ergoloid Mesylates interact with other medications?
A: Ergoloid mesylates can interact with many medications, including CYP3A4 inhibitors and inducers, triptan migraine medications, and vasoconstrictors. It’s crucial to review a patient’s medication list and screen for potential drug interactions before prescribing ergoloid mesylates.
Q7: Can Ergoloid Mesylates cure dementia?
A: No, Ergoloid mesylates does not cure dementia or other neurodegenerative conditions. It primarily aims to manage symptoms and improve cognitive function, but the efficacy is questionable. The medication is listed in the Beers Criteria as a potentially inappropriate medication for use in patients 65 and older due to lack of efficacy.
Q8: What should patients do if they miss a dose of Ergoloid Mesylates?
A: If a dose is missed, take it as soon as possible. If it’s almost time for the next dose, skip the missed dose and resume the regular dosing schedule. Do not double the dose to catch up.
Q9: Can Ergoloid Mesylates be used with other medications for cognitive impairment?
A: The use of ergoloid mesylates in combination with other medications for cognitive impairment should be done with extreme caution given its potential interactions and limited efficacy evidence. Consult with a specialist and carefully assess the risks and benefits before combining it with other treatments.
Q10: What patient education should be provided regarding Ergoloid Mesylates?
A: Patients should be informed about potential side effects, drug interactions, and the importance of adhering to the prescribed dosage. Advise patients to report any new or worsening symptoms to their doctor promptly. Patients should also be aware that it may take several weeks to see improvements in their condition. Additionally, advise them to avoid smoking and limit alcohol intake as these can worsen certain side effects. Caution patients against driving or operating heavy machinery until they know how the drug affects them.
