Professional Drug Information > Ergoloid Mesylates

Ergoloid Mesylates (Systemic)

VA CLASSIFICATION
Primary: CN900

Commonly used brand name(s): Gerimal; Hydergine; Hydergine LC.

Another commonly used name is
dihydrogenated ergot alkaloids .
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Dementia symptoms treatment adjunct—

Indications

Accepted

Dementia, early (treatment adjunct)—Ergoloid mesylates has been used to treat symptoms of an idiopathic decline in mental capacity (such as cognitive and interpersonal skills, mood, self-care, and apparent motivation) related to aging or to an underlying dementing condition such as primary progressive dementia, Alzheimer's dementia, or senile-onset multi-infarct dementia. ^{05} Careful diagnosis is recommended prior to use to rule out other causes of the presenting symptoms. ^{{05} {08}}
—The role of this medication in the therapy of dementia is controversial. ^{10} A recent controlled study in patients with Alzheimer's disease found no advantage to the use of ergoloid mesylates as compared to placebo ^{06}, and suggested that ergoloid mesylates may worsen scores on certain cognitive and behavioral rating scales. ^{06} More study is needed to determine the risk-benefit profile of ergoloid mesylates in the treatment of dementia.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    Dihydroergocornine mesylate: 659.80
    Dihydroergocristine mesylate: 707.84
    Dihydro-alpha-ergocryptine mesylate: 673.82
    Dihydro-beta-ergocryptine mesylate: 673.82

Mechanism of action/Effect:

Not established with regard to indications. Ergoloid mesylates acts centrally to decrease vascular tone and slow the heart rate, and acts peripherally to block alpha-receptors. ^{03} Another possible mechanism is the effect of ergoloid mesylates on neuronal cell metabolism, possibly resulting in improved oxygen uptake and improved cerebral metabolism, which in turn may normalize depressed neurotransmitter levels. ^{09}

Absorption:

Ergoloid mesylates is rapidly but incompletely (approximately 25%) absorbed from the gastrointestinal tract. ^{{11} {16}} Approximately 50% of an absorbed dose is removed by first-pass metabolism. ^{{11} {16}}

Biotransformation:

Hepatic. ^{02}

Half-life:

2 to 5 hours. ^{02}

Onset of action:

Clinical improvement may not be apparent for 3 to 4 weeks or longer. ^{{04} {11} {12} {13} {14} {15} {16} {17}}

Time to peak plasma concentration

1 to 2 hours. ^{11}


Precautions to Consider

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
» Bradycardia^{04}{17} or
» Hypotension^{04}{17}    (may be exacerbated)


Hepatic function impairment    (impaired elimination and possible toxicity)


» Psychosis, acute or chronic^{{11}{12}{13}{14}{15}{16}{17}}    (bradycardia reported; dopamine agonist activity may aggravate existing psychosis)


Sensitivity to ergoloid mesylates or other ergot alkaloids^{{11}{12}{13}{14}{15}{16}{17}}

Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):

Blood pressure and
Pulse count    (determinations recommended prior to initiation of therapy and at periodic intervals during therapy ^{04})






Side/Adverse Effects

Note: At recommended dosage, side effects usually are rare. Incidence and severity of side effects tend to be related to dose and duration of treatment and are usually reversible after therapy is discontinued.
Ergot alkaloids have been reported to precipitate attacks of acute intermittent porphyria in susceptible patients.

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence less frequent or rare
    
Bradycardia^{03}{04}{17} (drowsiness; slow heartbeat)
    
orthostatic hypotension (dizziness^{03}{04}{17} or lightheadedness when getting up from a lying or sitting position)
    
skin rash^{04}{17}



Those indicating need for medical attention only if they continue or are bothersome
Incidence less frequent or rare
    
Soreness under tongue —with sublingual use^{{03}{11}{12}{14}{15}{16}{17}}

Incidence dose-related
—possible symptoms of overdose^{17}    
Blurred vision^{04}
    
dizziness^{04}
    
fainting^{04}
    
flushing^{04}
    
headache^{04}
    
loss of appetite^{04}
    
nausea or vomiting^{03}{04}{11}
    
stomach cramps^{04}
    
stuffy nose^{04}





Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Ergoloid Mesylates (Systemic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to ergoloid mesylates

Other medical problems, especially bradycardia, hypotension, or acute or chronic psychosis

Proper use of this medication
» Importance of not using more or less medication than the amount prescribed

Proper administration of sublingual tablet: Dissolving tablet under tongue; not eating, drinking or smoking while tablet is dissolving

» Proper dosing
Missed dose: Not taking missed dose; not doubling doses; checking with physician if two or more doses in a row are missed

» Proper storage

Precautions while using this medication
Importance of regular monitoring by physician

» May require several weeks before clinical response is noted; checking with physician before discontinuing medication


Side/adverse effects
Signs of potential side effects, especially bradycardia, orthostatic hypotension, and skin rash


General Dosing Information
Clinical improvement may not be apparent for 3 to 4 weeks or longer. ^{{04} {11} {12} {13} {14} {15} {16} {17}} Continued clinical evaluation of the patient during ergoloid mesylates therapy is required to determine whether there is any initial benefit of the medication and if the benefits continue with time. ^{05}

If marked bradycardia or hypotension occurs, it is recommended that therapy with ergoloid mesylates be permanently withdrawn.

Ergoloid mesylates does not have the vasoconstrictor properties of the natural ergot alkaloids. ^{{11} {12} {13} {14} {15} {17}}


Oral Dosage Forms

ERGOLOID MESYLATES CAPSULES

Usual adult dose
Dementia symptoms treatment adjunct
Oral, 1 ^{{11} {12} {13} {14} {15} {16}} to 2 mg three times a day.


Strength(s) usually available
U.S.—


1 mg (Rx) [Hydergine LC (methyl paraben) (propyl paraben) (sorbitol)]

Note: 0.333 mg each of dihydroergocornine mesylate, dihydroergocristine mesylate, and dihydroergocryptine mesylate, per capsule.


Canada—
Not commercially available.

Packaging and storage:
Store below 30 °C (86 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. Protect from light.


ERGOLOID MESYLATES ORAL SOLUTION USP

Usual adult dose
See Ergoloid Mesylates Capsules .

Strength(s) usually available
U.S.—


1 mg per mL (Rx) [Hydergine (alcohol 28.5%) (glycerin) (propylene glycol) (purified water)]

Note: 0.333 mg each of dihydroergocornine mesylate, dihydroergocristine mesylate, and dihydroergocryptine mesylate, per mL.


Canada—
Not commercially available.

Packaging and storage:
Store below 30 °C (86 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight, light-resistant container. Protect from freezing.


ERGOLOID MESYLATES TABLETS USP

Usual adult dose
See Ergoloid Mesylates Capsules .

Strength(s) usually available
U.S.—


0.5 mg (Rx)[Generic]


1 mg (Rx) [Gerimal] [Hydergine (lactose)][Generic]

Canada—


1 mg (Rx) [Hydergine (scored)]

Note: An equal quantity of dihydroergocornine mesylate, dihydroergocristine mesylate, and dihydroergocryptine mesylate (that is, 0.167 or 0.333 mg of each) per tablet.


Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight, light-resistant container.



Sublingual Dosage Forms

ERGOLOID MESYLATES TABLETS (SUBLINGUAL) USP

Usual adult dose
Dementia symptoms treatment adjunct
Sublingual, 1 ^{{11} {12} {14} {15} {16}} to 2 mg three times a day.


Strength(s) usually available
U.S.—


0.5 mg (Rx) [Gerimal] [Hydergine (sucrose)][Generic]


1 mg (Rx) [Gerimal] [Hydergine (sucrose)][Generic]

Note: An equal quantity of dihydroergocornine mesylate, dihydroergocristine mesylate, and dihydroergocryptine mesylate (that is 0.167 or 0.333 mg of each) per tablet.


Canada—
Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight, light-resistant container.

Auxiliary labeling:
   • Dissolve under the tongue.
   • Do not swallow tablets whole.

Revised: 04/16/1993

References

Note: References used in the development and earlier revisions of this monograph have not yet been incorporated into the computer database and, therefore, are not listed below. Citations for information not yet referenced in the monograph will be provided upon request.

1. Hydergine package insert (Sandoz—US), 10/31/83.
   

2. Schran HF, McDonald S, Lehr R. Pharmacokinetics and bioavailability of ergoloid mesylates. Biopharmaceutics and Drug Disposition 1988; 9: 349-61.
   

3. AMA DE, 3rd ed.
   

4. Long: The essential guide to prescription drugs.
   

5. Hydergine package insert (Sandoz—US), Rev 6/1/90.
   

6. Thompson TL, Filley CM, Mitchell WD, Culig KM, LoVerde M, Byyny RL. Lack of efficacy of Hydergine in patients with Alzheimer's disease. N Engl J Med 1990 Aug 16; 323 (7): 445-8.
   

7. Posner JD, Landsberg L. Lack of efficacy of Hydergine in Alzheimer's disease. N Engl J Med 1991 Jan 17; 324 (3): 197-8.
   

8. Panel comment, 5/91.
   

9. Personal communication, 5/17/91.
   

10. Panel consensus, 5/91.
    

11. Hydergine package insert (Sandoz—US), 10/1/85.
    

12. Ergoloid mesylates oral tablets package insert (Bolar—US), 4/88.
    

13. Ergoloid mesylates sublingual tablets package insert (Bolar—US), 4/88.
    

14. Nyloric package insert (B.F. Ascher—US), 11/87.
    

15. Ergoloid mesylates sublingual tablets package insert (Lederle—US), 4/87.
    

16. Ergoloid mesylates sublingual tablets package insert (KV Pharmaceutical—US), Rev 2/88, Rec 3/89.
    

17. Hydergine (Sandoz—Canada) product monograph, CPS 1989: 459.
    

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