Enlon

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Enlon

Classes

Myasthenia Gravis Agents

Administration

For storage information, see the specific product information in the How Supplied section.
 
NOTE: Atropine sulfate and resuscitation equipment should always be available during the administration of edrophonium.

Injectable Administration

Edrophonium is usually administered intravenously; but is approved to be administered intravenously or intramuscularly. The subcutaneous route has also been used to treat pediatric patients (e.g., infants).
During administration, frequently monitor pulse, respiratory rate, blood pressure, and neurologic status. Monitor ECG during intravenous administration.
Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.

Intravenous Administration

Inject undiluted solution intravenously using a tuberculin syringe.

Intramuscular Administration

Inject into a large muscle. Aspirate prior to injection to avoid injection into a blood vessel.

Subcutaneous Administration

Inject subcutaneously taking care not to inject intradermally.

Adverse Reactions
Severe

seizures / Delayed / Incidence not known
bradycardia / Rapid / Incidence not known
respiratory arrest / Rapid / Incidence not known
cardiac arrest / Early / Incidence not known
laryngospasm / Rapid / Incidence not known

Moderate

dysphagia / Delayed / Incidence not known
conjunctival hyperemia / Early / Incidence not known
dysphonia / Delayed / Incidence not known
dysarthria / Delayed / Incidence not known
respiratory depression / Rapid / Incidence not known
hypotension / Rapid / Incidence not known

Mild

diarrhea / Early / Incidence not known
vomiting / Early / Incidence not known
nausea / Early / Incidence not known
abdominal pain / Early / Incidence not known
hypersalivation / Early / Incidence not known
miosis / Early / Incidence not known
lacrimation / Early / Incidence not known
diplopia / Early / Incidence not known
diaphoresis / Early / Incidence not known
bronchial secretions / Early / Incidence not known
weakness / Early / Incidence not known
increased urinary frequency / Early / Incidence not known

Common Brand Names

Enlon

Dea Class

Rx

Description

Parenteral cholinesterase inhibitor
Used for diagnosing myasthenia gravis, assessing cholinesterase inhibitor therapy, differentiating cholinergic and myasthenic crises, and reversing effects of nondepolarizing neuromuscular blockers after surgery; adjunct to atropine for treating respiratory depression associated with curare overdosage
Drug of choice for diagnosing myasthenia gravis because of rapid action and short duration of effect

Dosage And Indications
For myasthenia gravis diagnosis. Intravenous Dosage Adults

Initially 2 mg IV over 15 to 30 seconds. If a cholinergic reaction occurs, discontinue test and administer 0.4 to 0.5 mg atropine IV. If no response occurs within 45 seconds, inject another 8 mg of edrophonium. Test may be repeated in 30 minutes or more to test a positive cholinergic reaction.

Children weighing > 34 kg

2 mg IV given over 1 minute; if no response occurs after 45 seconds, give 1 mg every 30 to 45 seconds until response seen. Maximum total dose: 10 mg.

Children <= 34 kg

1 mg IV given over 1 minute; if no response occurs after 45 seconds, give 1 mg every 30 to 45 seconds until response seen. Maximum total dose: 5 mg.

Infants

0.5 mg IV once.

Intramuscular Dosage

NOTE: All cholinergic or myasthenic signs that appear with the IV route appear with the IM route, except there is a delay of 2—10 minutes before any reaction may be seen with the IM route.

Adults

Initially 10 mg IM. Subjects who demonstrate hyperreactivity to this injection (cholinergic reaction), should be retested after 30 minutes with 2 mg IM edrophonium to rule out false negative results.

Children > 34 kg

5 mg IM.

Children <= 34 kg

2 mg IM.

Infants

0.5 to 1 mg IM.

Subcutaneous Dosage† Infants

0.5 to 1 mg subcutaneously.

For the assessment of cholinesterase inhibitor therapy in patients with myasthenia gravis. Intravenous Dosage Adults

1 to 2 mg IV, given 1 hour after oral intake of the cholinesterase inhibitor being used in treatment. A transient increase in muscle strength indicates undermedication with the cholinesterase inhibitor.

Children

0.04 mg/kg IV, given 1 hour after oral intake of the cholinesterase inhibitor being used in treatment. A transient increase in muscle strength indicates undermedication with the cholinesterase inhibitor.

For use to differentiate a myasthenic crisis from a cholinergic crisis (e.g., myasthenic crisis diagnosis). Intravenous Dosage Adults

Initially, 1 mg IV. May repeat dose after 1 minute. NOTE: This test should only be done if adequate airway protection, ventilation, and cardiac monitoring are established.

For use in nondepolarizing neuromuscular blockade reversal.
NOTE: Neostigmine plus atropine is usually the preferred treatment.
Intravenous Dosage Adults

10 mg IV given over 30 to 45 seconds. May follow with 10 mg IV every 5 to 10 minutes, until a total of 40 mg has been given. If large doses of edrophonium (e.g., 15 mg) are required, they should be preceded by IV atropine.

For the treatment of paroxysmal supraventricular tachycardia (PSVT)† or diagnosis of supraventricular arrhythmias†. Intravenous Dosage Adults

10 mg IV as a single dose.

†Indicates off-label use

Dosing Considerations
Hepatic Impairment

Specific guidelines for dosage adjustments in hepatic impairment are not available.

Renal Impairment

Specific guidelines for dosage adjustments in renal impairment are not available.

Drug Interactions

Ambenonium Chloride: (Major) Other cholinesterase inhibitors can produce additive pharmacodynamic effects if used concomitantly with ambenonium chloride. Because ambenonium has a more prolonged action than other antimyasthenic drugs, simultaneous administration with other cholinergics is contraindicated except under strict medical supervision. The overlap in duration of action of several drugs complicates dosage schedules. Therefore, when a patient is to be given ambenonium, suspend the administration of all other cholinergics until the patient has been stabilized. In most instances, the myasthenic symptoms are effectively controlled by ambenonium use alone.
Amifampridine: (Moderate) Coaministration of amifampridine and edrophonium may increase the risk for adverse reactions due to additive cholinergic effects. Monitor patients closely for new or worsening side effects such as headache, visual disturbances, watery eyes, excessive sweating, shortness of breath, nausea, vomiting, diarrhea, bradycardia, loss of bladder control, confusion, or tremors.
Amitriptyline: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Amitriptyline; Chlordiazepoxide: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Amoxapine: (Major) Amoxapine may antagonize some of the effects of parasympathomimetics. However, bethanechol has occasionally been used therapeutically to offset some of the adverse antimuscarinic effects of cyclic antidepressants. Due to their anticholinergic actions, some cyclic antidepressants, such as amoxapine, may potentially antagonize the therapeutic actions of edrophonium. Consider alternatives if concurrent therapy is needed.
Articaine; Epinephrine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Atropine: (Major) Coadministration of Atropine and Edrophonium Chloride can produce mutually antagonistic effects.
Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Major) Coadministration of Atropine and Edrophonium Chloride can produce mutually antagonistic effects. (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of hyoscyamine.
Atropine; Difenoxin: (Major) Coadministration of Atropine and Edrophonium Chloride can produce mutually antagonistic effects.
Atropine; Diphenoxylate: (Major) Coadministration of Atropine and Edrophonium Chloride can produce mutually antagonistic effects.
Atropine; Edrophonium: (Major) Coadministration of Atropine and Edrophonium Chloride can produce mutually antagonistic effects.
Atropine; Hyoscyamine; Phenobarbital; Scopolamine: (Major) Coadministration of Atropine and Edrophonium Chloride can produce mutually antagonistic effects. (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of hyoscyamine. (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of scopolamine.
Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of hyoscyamine.
Benzonatate: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Benztropine: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of benztropine. Benztropine might also antagonize some of the effects of edrophonium.
Bupivacaine Liposomal: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Bupivacaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Bupivacaine; Lidocaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary. (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used; dosage adjustments of the cholinesterase inhibitor may be necessary. In addition, inhibitors of CYP1A2, such as tacrine, could theoretically reduce lidocaine metabolism and increase the risk of toxicity when given concurrently. Also, rivastigmine is an acetylcholinesterase inhibitor and therefore is likely to exaggerate muscle relaxation under general anesthetics.
Chloroprocaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Cholinergic agonists: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Clomipramine: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Cocaine: (Major) cholinesterase inhibitors reduce the metabolism of cocaine, therefore, prolonging cocaine's effects or increasing the risk of toxicity. It should be taken into consideration that the cholinesterase inhibition caused by echothiophate, demecarium, or isoflurophate may persist for weeks or months after the medication has been discontinued. Additionally, local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Dosage adjustment of the cholinesterase inhibitor may be necessary to control the symptoms of myasthenia gravis.
Desipramine: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Dextromethorphan; Quinidine: (Major) Disopyramide possesses anticholinergic properties. It is unclear if disopyramide can interfere with the cholinomimetic activity of edrophonium. Procainamide and quinidine also have anticholinergic properties, albeit somewhat less than disopyramide. Edrophonium may not terminate paroxysmal supraventricular tachycardias in patients receiving quinidine, disopyramide or procainamide, although data are limited. These antiarrhythmics should be used cautiously in patients with myasthenia gravis.
Dicyclomine: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of dicyclomine and vice-versa.
Digoxin: (Moderate) The increase in vagal tone induced by some cholinesterase inhibitors may produce bradycardia, hypotension, or syncope. The vagotonic effect of these drugs may be increased when given with other medications known to cause bradycardia such as digoxin. In one study involving multiple doses of galantamine at 24 mg/day with digoxin at a dose of 0.375 mg/day, there was no effect on the pharmacokinetics of digoxin, except one healthy subject was hospitalized due to second and third degree heart block and bradycardia.
Disopyramide: (Moderate) Disopyramide possesses clinically significant antimuscarinic properties and these appear to be dose-related. It is possible that disopyramide could antagonize the muscarinic actions cholinesterase-inhibitors, such as edrophonium.
Doxepin: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Etomidate: (Moderate) Muscle relaxation produced by succinylcholine can be prolonged when the drug is administered with a cholinesterase inhibitor. If used during surgery, extended respiratory depression could result from prolonged neuromuscular blockade. Other neuromuscular blockers may interact with cholinesterase inhibitors in a similar fashion. Cholinesterase inhibitors are therefore also likely to exaggerate muscle relaxation under general anesthetics.
Fospropofol: (Moderate) Muscle relaxation produced by succinylcholine can be prolonged when the drug is administered with a cholinesterase inhibitor. If used during surgery, extended respiratory depression could result from prolonged neuromuscular blockade. Other neuromuscular blockers may interact with cholinesterase inhibitors in a similar fashion. Cholinesterase inhibitors are therefore also likely to exaggerate muscle relaxation under general anesthetics.
Glycopyrrolate: (Minor) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of glycopyrrolate.
Glycopyrrolate; Formoterol: (Minor) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of glycopyrrolate.
Halogenated Anesthetics: (Moderate) Muscle relaxation produced by succinylcholine can be prolonged when the drug is administered with a cholinesterase inhibitor. If used during surgery, extended respiratory depression could result from prolonged neuromuscular blockade. Other neuromuscular blockers may interact with cholinesterase inhibitors in a similar fashion. Cholinesterase inhibitors are therefore also likely to exaggerate muscle relaxation under general anesthetics.
Homatropine; Hydrocodone: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of homatropine.
Hyoscyamine: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of hyoscyamine.
Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of hyoscyamine.
Imipramine: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Indacaterol; Glycopyrrolate: (Minor) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of glycopyrrolate.
Ketamine: (Moderate) Muscle relaxation produced by succinylcholine can be prolonged when the drug is administered with a cholinesterase inhibitor. If used during surgery, extended respiratory depression could result from prolonged neuromuscular blockade. Other neuromuscular blockers may interact with cholinesterase inhibitors in a similar fashion. Cholinesterase inhibitors are therefore also likely to exaggerate muscle relaxation under general anesthetics.
Levobupivacaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Lidocaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used; dosage adjustments of the cholinesterase inhibitor may be necessary. In addition, inhibitors of CYP1A2, such as tacrine, could theoretically reduce lidocaine metabolism and increase the risk of toxicity when given concurrently. Also, rivastigmine is an acetylcholinesterase inhibitor and therefore is likely to exaggerate muscle relaxation under general anesthetics.
Maprotiline: (Major) Maprotiline may antagonize some of the effects of edrophonium.
Mepivacaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Mepivacaine; Levonordefrin: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of hyoscyamine.
Methocarbamol: (Major) The effects of cholinesterase inhibitors may be inhibited by methocarbamol. Therefore, methocarbamol should be used with caution in patients with myasthenia gravis receiving cholinesterase inhibitors.
Methscopolamine: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of methscopolamine.
Neostigmine: (Major) Edrophonium and neostigmine are both parasympathomimetics. Coadministration results in additive effects and should be done cautiously.
Neuromuscular blockers: (Major) Cholinesterase inhibitors may be used to reverse the actions of nondepolarizing neuromuscular blockers; however, cholinesterase inhibitors may also prolong the neuromuscular blocking effects if given with depolarizing neuromuscular blockers, as these drugs are metabolized by acetylcholinesterase. In addition, neuromuscular blocking agents can antagonize the effects of the cholinesterase inhibitors; temporary dosage adjustment following surgery may be necessary.
Nonsteroidal antiinflammatory drugs: (Moderate) NSAIDs may cause additive pharmacodynamic GI effects with cholinesterase inhibitors, leading to gastrointestinal intolerance. Patients receiving concurrent NSAIDs should be monitored closely for symptoms of active or occult gastrointestinal bleeding. While NSAIDs appear to suppress microglial activity, which in turn may slow inflammatory neurodegenerative processes important for the progression of Alzheimer's disease (AD), there are no clinical data at this time to suggest that NSAIDs alone or as combined therapy with AD agents result in synergistic effects in AD.
Nortriptyline: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Oxybutynin: (Moderate) Oxybutynin is an antimuscarinic; the muscarinic actions of edrophonium chloride could be antagonized when used concomitantly with oxybutynin.
Perphenazine; Amitriptyline: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Physostigmine: (Major) Edrophonium and physostigmine are both parasympathomimetics. Coadministration results in additive effects and should be done cautiously.
Prilocaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Prilocaine; Epinephrine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Procainamide: (Moderate) Procainamide has anticholinergic properties and may interfere with the cholinomimetic activity of edrophonium.
Procaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Propantheline: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of propantheline.
Propofol: (Moderate) Muscle relaxation produced by succinylcholine can be prolonged when the drug is administered with a cholinesterase inhibitor. If used during surgery, extended respiratory depression could result from prolonged neuromuscular blockade. Other neuromuscular blockers may interact with cholinesterase inhibitors in a similar fashion. Cholinesterase inhibitors are therefore also likely to exaggerate muscle relaxation under general anesthetics.
Protriptyline: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Pyridostigmine: (Major) Edrophonium and pyridostigmine are both parasympathomimetics. Coadministration results in additive effects and should be done cautiously.
Quinidine: (Major) Disopyramide possesses anticholinergic properties. It is unclear if disopyramide can interfere with the cholinomimetic activity of edrophonium. Procainamide and quinidine also have anticholinergic properties, albeit somewhat less than disopyramide. Edrophonium may not terminate paroxysmal supraventricular tachycardias in patients receiving quinidine, disopyramide or procainamide, although data are limited. These antiarrhythmics should be used cautiously in patients with myasthenia gravis.
Quinine: (Major) The actions of quinine on skeletal muscle are pharmacologically opposite to those of cholinesterase inhibitors. Therefore, quinine may interfere with the actions of cholinesterase inhibitors in treating such conditions as myasthenia gravis. This represents a pharmacodynamic interaction with cholinesterase inhibitors rather than a pharmacokinetic interaction.
Ropivacaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine.
Scopolamine: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of scopolamine.
Tetracaine: (Moderate) Local anesthetics can antagonize the effects of cholinesterase inhibitors by inhibiting neuronal transmission in skeletal muscle, especially if large doses of local anesthetics are used. Also, local anesthetics interfere with the release of acetylcholine. Dosage adjustment of the cholinesterase inhibitor may be necessary.
Tricyclic antidepressants: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.
Trihexyphenidyl: (Major) The muscarinic actions of edrophonium chloride can antagonize the antimuscarinic actions of trihexyphenidyl.
Trimipramine: (Moderate) Tricyclic antidepressants may antagonize some of the effects of parasympathomimetics, such as edrophonium, due to their anticholinergic activity.

How Supplied

Enlon Intramuscular Inj Sol: 1mL, 10mg
Enlon Intravenous Inj Sol: 1mL, 10mg

Maximum Dosage
Adults

10 mg/dose IV.

Geriatric

10 mg/dose IV.

Adolescents

> 34 kg: 10 mg IV.

Children

> 34 kg: 10 mg IV.
<= 34 kg: 5 mg IV.

Infants

0.5 mg IV.

Mechanism Of Action

Edrophonium competes with acetylcholine for its binding site on acetylcholinesterase. By interfering with enzymatic destruction of acetylcholine, edrophonium potentiates the action of acetylcholine on both the skeletal muscle (nicotinic receptor) and the GI tract (muscarinic receptor). It also can stimulate cholinergic responses in the eyes (causing miosis) if directly applied. Different muscle groups exhibit different levels of response to cholinesterase inhibitors, and doses that stimulate one muscle group can weaken, through overdose, another.
 
Specific responses to cholinesterase inhibitors include: increased skeletal muscle tone (nicotinic); increased gastric motility and GI tone (muscarinic); bradycardia (muscarinic); ureteral constriction (muscarinic); stimulation of the sweat and salivary glands (muscarinic); and constriction of the bronchi (muscarinic). Few of these actions are seen with edrophonium, however, due to its short duration of action.
 
In myasthenia gravis, edrophonium increases the amount of acetylcholine in the neuromuscular junction, which is deficient of acetylcholine receptors at the motor endplate. This action allows for a greater number of the depleted acetylcholine receptors to be bound with acetylcholine. This binding can be clinically evaluated as an increase in the patient's muscular strength and can establish the diagnosis of myasthenia gravis in 90—95% of those suspected of having the disease. Edrophonium is not used in the treatment of myasthenia gravis, however, due to its short duration of action.

Pharmacokinetics

Edrophonium is administered parenterally. The distribution of edrophonium is poorly understood, but the drug does not cross the placenta. Similarly, the metabolic fate and excretion of edrophonium are not known. Duration of action ranges from 5—10 minutes when given IV and 5—30 minutes when given IM.

Intravenous Route

Edrophonium has a rapid onset of action, occurring 30—60 seconds after IV administration.

Intramuscular Route

Edrophonium has a rapid onset of action, occurring 2—10 minutes after IM administration.

Pregnancy And Lactation
Pregnancy

The manufacturer warns that the safe use of edrophonium during breast-feeding has not been established. However, the drug's effect is manifested within 30 to 60 seconds after injection and lasts an average of 10 minutes. Edrophonium is ionized at physiological pH and is therefore not believed to be excreted in breast milk. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.