Regonol

REGONOL- pyridostigmine bromide injection, solution
Sandoz Inc

Rx Only

CONTAINS BENZYL ALCOHOL

THIS DRUG SHOULD BE ADMINISTERED BY ADEQUATELY TRAINED INDIVIDUALS FAMILIAR WITH ITS ACTIONS, CHARACTERISTICS, AND HAZARDS.

DESCRIPTION

REGONOL® (pyridostigmine bromide injection, USP) is an active cholinesterase inhibitor chemically designated as 3-hydroxy-1-methylpyridinium bromide dimethyl-carbamate.

Its structural formula is:

chemical-structure
(click image for full-size original)

REGONOL® is supplied as a sterile, isotonic, nonpyrogenic solution for injection. Each mL contains 5 mg of pyridostigmine bromide USP as active, 10 mg BENZYL ALCOHOL NF as preservative WHICH IS NOT INTENDED FOR USE IN NEWBORNS, 0.23 mg sodium citrate dihydrate USP and 0.1 mg anhydrous citric acid USP as buffering agent, pH adjusted with sodium hydroxide NF and anhydrous citric acid USP if necessary and water for injection USP.

CLINICAL PHARMACOLOGY

REGONOL® (pyridostigmine bromide injection, USP) an analogue of neostigmine, facilitates the transmission of impulses across the myoneural junction by inhibiting the destruction of acetylcholine by cholinesterase. Currently available data indicate that pyridostigmine may have a significantly lower degree and incidence of bradycardia, salivation and gastrointestinal stimulation than does neostigmine. Animal studies using the injectable form of pyridostigmine and human studies using the oral preparation have indicated that pyridostigmine has a longer duration of action than does neostigmine measured under similar circumstances.1,2 REGONOL® is effective in reversing the neuromuscular blocking effects of nondepolarizing muscle relaxants.

Anticholinesterase agents such as REGONOL® and neostigmine may produce depolarization block when administered at doses above their recommended therapeutic ranges. The therapeutic index of REGONOL® (ratio of reversal dose to blocking dose) is approximately 1:6 (see OVERDOSAGE).3

The antagonism of neuromuscular blockade by anticholinesterase agents may be influenced by the degree of spontaneous recovery achieved when the reversal agent is administered, by the particular relaxant administered, acid-base balance, body temperature, electrolyte imbalance, concomitant medications such as potent inhalational anesthetics, antibiotics or other drugs which enhance or antagonize the action of nondepolarizing muscle relaxants.4 The use of peripheral nerve stimulation to determine the degree of neuromuscular blockade is recommended in evaluating the effects of the reversal agents.

Failure of anticholinesterase agents to produce prompt (within 30 minutes) reversal of neuromuscular blockade may occur in the presence of extreme debilitation, carcinomatosis, and with concomitant use of certain broad-spectrum antibiotics, or anesthetic agents and other drugs which enhance neuromuscular blockade or cause respiratory depression through their own pharmacologic actions.

As with other anticholinesterase agents, the administration of REGONOL® may be associated with muscarinic and nicotinic side effects, notably bradycardia and excessive bronchial secretions; the use of glycopyrrolate or atropine sulfate simultaneously with or prior to administration of REGONOL® is recommended to counteract these side effects (see DOSAGE AND ADMINISTRATION).5

Pharmacokinetics

It has been postulated that the clearance of pyridostigmine is almost equally dependent on metabolism and on urinary elimination of the unchanged drug.6 Other studies in man indicated that approximately 75 percent of the plasma clearance of pyridostigmine is dependent on renal excretion and the remainder on nonrenal mechanisms.7

INDICATIONS AND USAGE

REGONOL® (pyridostigmine bromide injection, USP) is indicated as a reversal agent or antagonist to the neuromuscular blocking effects of nondepolarizing muscle relaxants.

CONTRAINDICATIONS

Known hypersensitivity to anticholinesterase agents; intestinal and urinary obstructions of mechanical type.

WARNINGS

NOT FOR USE IN NEONATES

REGONOL® (pyridostigmine bromide injection, USP) should be used with particular caution in patients with bronchial asthma or cardiac dysrhythmias. Transient bradycardia may occur and be relieved by atropine sulfate. Atropine sulfate should also be used with caution in patients with cardiac dysrhythmias. When large doses of pyridostigmine bromide are administered, as during reversal of muscle relaxants, prior or simultaneous injection of atropine sulfate or an equipotent dose of glycopyrrolate is advisable. Because of the possibility of hypersensitivity in an occasional patient, atropine and antishock medication should always be readily available.

When used as an antagonist to nondepolarizing muscle relaxants, adequate recovery of voluntary respiration and neuromuscular transmission must be obtained prior to discontinuation of respiratory assistance, and there should be continuous patient observation. Satisfactory recovery may be judged by adequacy of skeletal muscle tone, respiratory measurements, and by observation of the response to peripheral nerve stimulation. A patent airway should be maintained and manual or mechanical ventilation should be continued until complete recovery of normal respiration is assured.

Exposure to excessive amounts of benzyl alcohol has been associated with toxicity (hypotension, metabolic acidosis), particularly in neonates, and an increased incidence of kernicterus, particularly in small preterm infants. There have been rare reports of deaths, primarily in preterm infants, associated with exposure to excessive amounts of benzyl alcohol. The amount of benzyl alcohol from medications is usually considered negligible compared to that received in flush solutions containing benzyl alcohol. Administration of high dosages of medications containing this preservative must take into account the total amount of benzyl alcohol administered. The amount of benzyl alcohol at which toxicity may occur is not known. If the patient requires more than the recommended dosages or other medications containing this preservative, the practitioner must consider the daily metabolic load of benzyl alcohol from these combined sources (see PRECAUTIONS: Pediatric Use).

PRECAUTIONS

THE USE OF A PERIPHERAL NERVE STIMULATOR TO MONITOR RECOVERY OF NEUROMUSCULAR FUNCTION WILL MINIMIZE THE POSSIBILITY OF EXCESS DOSING OR INADEQUATE REVERSAL.

Inadequate reversal of the neuromuscular blockade induced by nondepolarizing (curariform) muscle relaxants is possible. This can be managed by manual or mechanical ventilation until recovery is judged adequate. The administration of additional doses of anticholinesterase reversal agents is not recommended since excessive dosages of such drugs may produce depolarizing block through their own pharmacologic actions.

Pyridostigmine is mainly excreted unchanged by the kidney.2,7,8 Therefore, lower doses may be required in patients with renal disease, and treatment should be based on titration of drug dosage to effect.2,7

Drug Interactions

Concomitant administration of REGONOL® (pyridostigmine bromide injection, USP) and 4-aminopyridine has been reported to delay the onset of action of REGONOL®.9

Antibiotics

Parenteral administration of high doses of certain antibiotics may intensify or produce neuromuscular block through their own pharmacologic actions. The following antibiotics have been associated with various degrees of paralysis: aminoglycosides (such as neomycin, streptomycin, kanamycin, gentamicin, and dihydrostreptomycin); tetracyclines; bacitracin; polymyxin B; colistin; and sodium colistimethate. If these or other newly introduced antibiotics are used in conjunction with nondepolarizing neuromuscular blocking drugs during surgery, unexpected prolongation of neuromuscular block or resistance to its reversal should be considered a possibility.

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