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Ergoloid Mesylates

( Dihydrogenated Ergot Alkaloids ; Dihydroergotoxine )

Pronunciation: err-GO-loyd MEH-suh-lates
Class: Psychotherapeutic agent

Trade Names

Gerimal
- Tablets, oral 1 mg
- Tablets, sublingual 0.5 mg
- Tablets, sublingual 1 mg

Hydergine
- Liquid 1 mg/mL
- Tablets, oral 1 mg
- Tablets, sublingual 0.5 mg
- Tablets, sublingual 1 mg

Pharmacology

Unknown; may increase brain metabolism, possibly increasing cerebral blood flow.

Slideshow: Flashback: FDA Drug Approvals 2013

Pharmacokinetics

Absorption

Approximately 25% is absorbed; approximately 50% is removed by the first-pass metabolism. T max is 1.5 to 3 h.

Distribution

Excreted in breast milk.

Metabolism

Undergoes first-pass metabolism.

Elimination

The t ½ is approximately 2.6 to 5.1 h (unchanged ergoloid in the plasma).

Indications and Usage

Treatment of age-related decline in mental capacity, primary progressive dementia, Alzheimer dementia, multi-infarct dementia and senile onset.

Contraindications

Hypersensitivity to ergoloid mesylates or other ergot alkaloids; acute or chronic psychosis.

Dosage and Administration

Adults

PO/SL 1 to 2 mg 3 times daily (up to 12 mg/day has been used).

General Advice

Instruct patient to allow SL tablets to completely dissolve under tongue; do not allow patient to swallow, crush, or chew tablet.

Storage/Stability

Store in tightly closed, light-resistant container at room temperature.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Orthostatic hypotension; bradycardia.

Dermatologic

Rash.

GI

Transient nausea; GI disturbances; sublingual irritation.

Precautions

Pregnancy

Pregnancy category undetermined.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hepatic Function

Elimination of drug may be affected.

Special Risk Patients

Administer drug with caution to patients with history of bradycardia or hypotension.

Overdosage

Symptoms

Headache, flushing, anorexia, nausea, vomiting, abdominal cramps, nasal congestion, impaired vision, dizziness, fainting.

Patient Information

  • Teach patient how to decrease effects of orthostatic hypotension by rising slowly from supine position and dangling feet for few min before standing.
  • Instruct patient to avoid alcohol consumption, which may enhance hypotensive effect.
  • Caution patient not to take OTC cough, cold and allergy preparations that contain alcohol.
  • Instruct patient to avoid excessive exposure to cold since temperature regulation may be impaired.
  • Instruct patient to notify health care provider if adverse reactions occur.
  • Advise patient/family that it may require 3 to 4 wk and up to 6 mo to determine clinical effectiveness of drug.

Copyright © 2009 Wolters Kluwer Health.

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