Drug information of Ergoloid Mesylate

Mechanism of effect

The general mechanism of action of ergoloid mesylate is the dual action of partial agonism/antagonism of adrenergic, dopaminergic and serotonergic receptors. The pharmacological activity is determined by the degree of activity of each component at the receptor site.

Pharmacodynamic

It is thought that it increases both the blood flow and cerebral metabolism. Some studies have shown a significant improvement in alertness and memory, as well as a decline in confusion while some other benefits have shown a lack of effect.

Pharmacokinetics

Absorption: The maximal plasma concentration of the components of the mixture of ergoloid mesylates is approximately 0.04mcg/l. The analysis of the concentration of the major metabolites of each component indicates that all ergoloid mesylate are rapidly transformed after absorption.

Volume of distribution: The volume of distribution is about 2 L/kg.

Protein binding: Ergoloid mesylate presents a very large plasma protein binding that accounts for 81% of the administered dose.

Metabolism

Most of the metabolism of ergoloid mesylate is hepatic and it is performed very rapidly after absorption. After exposition in vitro, the major metabolites identified are hydroxy-dihydroergocornine, hydroxy-dihydroergocryptine and hydroxy-dihydroergocristine.

Route of elimination

The ergoloid mesylate mixture is mainly excreted via bile in feces. The ratio of the eliminated dose via urine after intravenous and oral administration is 8.4% and 2% respectively.

Half life

The reported plasma half-life of ergoloid mesylate is 3.5 hours while the terminal half-life is of 13 hours.

Indication

For the treatment of symptoms of an idiopathic decline in the mental capacity not related to a potentially reversible condition.

Dosage

1 mg PO 3 times per day. Clinical improvement may take 3 to 4 weeks after initiating therapy.

Drug contraindications

Ergoloid mesylates are contraindicated in patients with sensitivity to ergoloid mesylates or in patients with known ergot alkaloid hypersensitivity.
Ergoloid mesylates are also contraindicated in patients with acute or chronic psychosis, regardless of etiology; dopamine agonist activity may exacerbate pre-existing psychosis.

Side effects

Blurred vision , severe bradycardia

Severe:
bradycardia / Rapid / Incidence not known Moderate:
orthostatic hypotension / Delayed / Incidence not known
hypotension / Rapid / Incidence not known
blurred vision / Early / Incidence not known

Interactions

Expectorant , Almotriptan , Diethylpropion , nelfinavir , eletriptan , lisdexamfetamine , Amyl Nitrite , Efavirenz , Tipranavir , Xylometazoline , Propylhexedrine , acrivastine+pseudoephedrine , Erythromycin , Itraconazole , Voriconazole , Ketoconazole , Clarithromycin , Benzphetamine

Some products that may interact with this drug include: azole antifungals (e.g., ketoconazole, itraconazole, voriconazole), cobicistat, delavirdine, macrolide antibiotics (e.g., erythromycin, clarithromycin, troleandomycin), nefazodone, HIV protease inhibitors (e.g., indinavir, nelfinavir, ritonavir, saquinavir), telithromycin.
If you also take "triptan" migraine drugs (e.g., sumatriptan, rizatriptan), you will need to separate your "triptan" dose from your dose of this medication to reduce the risk of serious side effects. Ask your doctor how long you should wait between your doses of these drugs.

Alerts

Before taking ergoloid mesylates, tell your doctor or pharmacist if you are allergic to them; or to other ergot alkaloids (e.g., dihydroergotamine, ergotamine); or if you have any other allergies.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: a certain mental/mood disorder (psychosis).

Ergoloid mesylates are extensively metabolized by the liver. Therefore, ergoloid mesylates should be used with caution in patients with hepatic disease, since hepatic impairment could limit drug elimination mechanisms.

Points of recommendation

Before using this medication, tell your doctor or pharmacist your medical history, especially of: other behavior problems, blood pressure problems, heart problems, liver disease.

This drug may make you dizzy or drowsy or blur your vision. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness or clear vision until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Pregnancy level

Although specific data are lacking for ergoloid mesylates, natural ergot alkaloids are considered contraindicated (pregnancy risk category X) during pregnancy due to their oxytocic and uterine stimulant properties.

Related drugs

Memantine