Neostigmine (Injection)

Neostigmine is used to treat myasthenia gravis and to improve muscle function after surgery, and is administered via an injection into skin, muscle, or a vein.

Overview

Neostigmine is commonly administered to patients with myasthenia gravis, a chronic muscle disease which causes severe muscle weakness. It is often used after surgery, too, to reverse the effects of other drugs given to stop muscles from moving. Sometimes the drug is also given to prevent or treat certain intestinal or kidney problems. It is a type of drug known as a cholinesterase inhibitor, and essentially it works to help muscles function more effectively.

Injectable neostigmine is only available with a doctor's prescription. Usually it is administered by a doctor, nurse, or other healthcare professional in a hospital or other clinical environment. In the US, its brand name is Bloxiverz.

Conditions Treated?

Type Of Medicine?

  • Cholinesterase inhibitor

Side Effects

Along with its wanted effects, neostigmine can cause unwanted side effects, some of which can be very serious. Familiarize yourself with all potential side effects in order that you can recognize when it is necessary to speak to your doctor. It is unlikely that all of these side effects will occur.

The following are serious side effects which should be reported to your doctor or nurse immediately:

  • More common:

O Blurred vision

O Loss of vision

O Dizziness, lightheadedness or fainting

O Dizziness, faintness, or lightheadedness when arising

O Confusion

O Unusual tiredness or weakness

O Chest pain, tightness, or discomfort

O Difficult or labored breathing

O Fast, slow, pounding, or irregular heartbeat

O Twitches of muscle visible under skin

O Sweating

  • Incidence unknown

O Changes in speech patterns or rhythms

O Slurred speech

O Difficulty speaking

O Difficulty swallowing

O Cough

O Fast, slow, shallow, or irregular breathing

O Noisy breathing

O Loss of consciousness

O No pulse or blood pressure

O Stopping of the heart

O Difficulty moving

O Seizures

O Muscle cramps and spasms

O Muscle pain or stiffness

O Joint pain

O Double vision

O Tunnel vision

O Disturbed color perception

O Halos around eyes

O Overbright appearance of lights

O Night blindness

O Itching

O Rash

O Hives

O Puffiness or swelling of eyelids, face, lips or tongue

O Pale or blue lips, fingernails or skin

The following side effects are minor and do not usually require medical attention unless they become very severe or persistent. If you have concerns about them, you should talk to your doctor or nurse.

  • More common

O Problems at injection site, such as:

  • Bleeding
  •  Blistering
  •  Hives
  •  Rash
  •  Discoloration of skin
  •  Redness
  •  Stinging
  •  Burning
  •  Warmth
  •  Coldness
  •  Numbness
  •  Tingling
  •  Tenderness
  •  Swelling
  •  Ulceration
  •  Infection
  • O Drowsiness

O Nausea

O Vomiting

O Headache

O Sore throat

O Sleeplessness

O Trouble sleeping

O Increased watering of the mouth

  • Incidence unknown

O Bloating

O Excess gas in stomach or intestines

O Full feeling

O Passing gas

O Stomach cramps

O Diarrhea

O Passing urine more often

O Dry mouth

O Increased mucous from lungs

O Feeling of warmth

O Redness of skin

O Redness of face, neck, arms, and sometimes upper chest

O Skin rash

This may not necessarily be an exhaustive list of all side effects which could occur with the use of neostigmine. If you notice any others, tell your doctor or nurse immediately. You could also report them to the FDA, or your healthcare provider may do this on your behalf.

Overdose

Get immediate help if you notice any of the following signs of overdose:

  • Constipation
  • Difficult urination
  • Dry mouth
  • Enlarged pupils
  • Muscle weakness (new or worsened)

Dosage

A doctor, nurse, or other healthcare professional will administer neostigmine injections to you. A doctor will determine the appropriate dose based on a range of factors, such as the condition being treated and your medical history. You may have to undergo tests to assess your neuromuscular function before neostigmine is administered to you. It may also be necessary to administer other medicines at the same time as neostigmine to ensure it works correctly.

Neostigmine can be injected into the muscle, under the skin, or into the veins. If you experience pain, warmth, burning, stinging, bleeding, or other problems at the injection site, you could mention them to your doctor or nurse. Usually, these problems quickly dissipate, but if they persist long after the injection, or you think you may have developed an infection, speak to your doctor.

Interactions

You should tell your doctor about all the medicines you are currently taking, including those prescribed to you, those purchased over the counter, and any herbal supplements or multivitamins that you take. Some medicines may interact with neostigmine and cause harmful effects.

The following medicines are not recommended for concurrent use with neostigmine, and if possible your doctor may avoid prescribing neostigmine or they may change some of the current medicines you take. If both drugs are deemed important, however, they may continue to prescribe both and make dosage adjustments.

  • Bupropion (Aplenzin, Buproban, Forfivo XL, Wellbutrin, Zyban, Budeprion)
  • Donepezil (Aricept)

The following medicines can increase the risk of certain side effects when taken at the same time as neostigmine. However, if both drugs are necessary, your doctor may continue to prescribe both, possibly with dosage adjustments or with closer monitoring of your condition.

  • Succinylcholine (Anectine, Quelicin)

Warnings

Interactions with preexisting medical conditions

It is vital that patients give their doctor their full medical history before neostigmine is prescribed. Be sure to mention all the medical conditions you currently have, as well as those you have suffered from in the past. The medical conditions listed below pose the most risk, but there may be others which doctors should also be aware of when considering administering neostigmine.

People with the following conditions should not be given neostigmine injections:

  • Urinary tract blockage
  • Intestinal blockage (bowel)
  • Peritonitis (swelling of the lining of the stomach or abdomen)

The following conditions may be worsened by neostigmine:

  • Coronary artery disease
  • Recent heart attack
  • Heart rhythm problems
  • Hypotension (low blood pressure)
  • Bradycardia (slow heartbeat)
  • Asthma
  • Seizures
  • Stomach ulcer

Kidney disease can cause neostigmine to be removed from the body at a much slower rate than normal. If the drug is in the body for longer, it can have more powerful effects than expected and increase the risk or severity of side effects. If you have kidney disease, you may still be able to have neostigmine injections, but doctors may prescribe lower dosages. Doctors may want to assess your kidney function before administering neostigmine.

Allergy

If you have ever had an allergic reaction to neostigmine in the past, or to drugs like it, you may not be able to have future neostigmine injections. Be sure to tell your doctor the nature of the reaction and the symptoms you experienced.

It is also important that your doctor know about any other allergies you suffer from in case you are allergic to any of the ingredients in neostigmine. Be sure to mention food, pollen, dye, chemical, drug, and animal allergies.

If you notice symptoms of allergic reaction after having neostigmine injections, such as rash, hives, swelling of the eyes, face, lips, tongue, or throat, or breathing problems, tell your doctor or nurse immediately.

Pediatric use

Studies into neostigmine have not demonstrated any problems that would limit the efficacy of the drug for pediatric patients. However, infants and very young children may be more sensitive to its effects than older children. Doctors therefore exert caution when prescribing the drug to children, and they may administer lower doses.

Geriatric use

Studies have demonstrated that neostigmine can be just as safe and effective when administered to elderly patients as it is in younger adults. However, age-related kidney problems are more likely in elderly patients, which means doctors are more cautious when prescribing it to this population. Additional tests may need to be performed to assess kidney function before the drug is administered, and lower doses may be given initially.

Pregnancy and breastfeeding

There have been very few controlled studies into the effects of neostigmine upon pregnant women and their fetuses. For this reason, the drug should be used with caution in pregnant women. Generally, it should only be administered if absolutely necessary and the potential benefits of the drug outweigh potential risks. Patients who think they could be pregnant should tell their doctor before neostigmine is administered.

It is not known whether neostigmine is excreted in breast milk, but many similar drugs are. It is not clear what effects the drug could have on nursing infants. Nursing mothers should decide whether to discontinue breastfeeding, or avoid taking the drug.

Storage

Since neostigmine is administered by doctors or nurses in a clinical environment, patients are not expected to have to store the medicine at home.

Summary

Neostigmine is commonly given to patients following surgery to help restore muscle function, and to patients with myasthenia gravis, a chronic muscle disease. It may also be given to treat or prevent some intestinal problems or kidney problems. The injectable dosage form is administered only in hospital or clinical settings, and should be given by a doctor, nurse, or other healthcare professional.

Sometimes neostigmine can cause irritation, pain, or discomfort at the injection site, as well as drowsiness, headache, sleeping problems, bloating and excess gas, diarrhea, and flushing of the skin. These effects are usually nothing to be concerned about unless they become very severe. If patients notice changes to their vision, faintness, changes to heartbeat, breathing problems, or chest pain they should tell their doctor or nurse right away.

People with urinary tract blockage, bowel blockage, or peritonitis should not take neostigmine. Asthma, seizures, stomach ulcer, coronary heart disease, recent heart attack, heart rhythm problems, and low blood pressure may be worsened by neostigmine. The drug is suitable for children, but it is used with caution in infants and very young children who tend to be more sensitive to its effects. The drug is not recommended for use during pregnancy, and women are advised to avoid breastfeeding after being given neostigmine injections.