Bloxiverz 1mg/1ml Inj, 10ml
It is used to treat myasthenia gravis. It is used to get back function in muscles after surgery.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Reversal agent for non-depolarizing neuromuscular blocking agents
Pharmacologic Class
Acetylcholinesterase inhibitor
Pregnancy Category
Category C
FDA Approved
May 2013
DEA Schedule
Not Controlled
Overview
What is this medicine?
Neostigmine is a medication given by injection, usually in a hospital setting, to help reverse the effects of muscle relaxants used during surgery. It helps your muscles regain their strength and allows you to breathe on your own after anesthesia.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all guidelines provided. This medication is administered via injection.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
In the event that you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
In the event that you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
Lifestyle & Tips
- This medication is typically administered in an acute care setting (e.g., operating room, recovery room) and does not require specific lifestyle modifications from the patient.
- Patients should report any unusual symptoms or discomfort to their healthcare provider immediately after administration.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
0.03-0.07 mg/kg IV, typically administered with an anticholinergic agent (e.g., glycopyrrolate 0.2 mg for every 1 mg neostigmine) to counteract muscarinic effects. Total dose not to exceed 5 mg.
Dose Range:
0.03 - 0.07 mg
Condition-Specific Dosing:
reversal_of_neuromuscular_blockade:
0.03-0.07 mg/kg IV, maximum total dose 5 mg. Administer slowly over at least 1 minute. Should be given after signs of spontaneous recovery from neuromuscular blockade are evident (e.g., 2-3 twitches on TOF).
Pediatric Dosing
Neonatal:
Not established for routine use in neonates for NMB reversal. Use with extreme caution if at all.
Infant:
0.025-0.07 mg/kg IV, maximum total dose 2.5 mg. Administer with an anticholinergic.
Child:
0.025-0.07 mg/kg IV, maximum total dose 2.5 mg. Administer with an anticholinergic.
Adolescent:
0.03-0.07 mg/kg IV, maximum total dose 5 mg. Administer with an anticholinergic.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but monitor closely.
Moderate:
Consider dose reduction (e.g., 50% of usual dose) and extend dosing interval. Monitor closely for signs of cholinergic crisis.
Severe:
Significant dose reduction (e.g., 25-50% of usual dose) and extended dosing interval. Monitor closely for signs of cholinergic crisis. Avoid if possible.
Dialysis:
Neostigmine is partially removed by hemodialysis. Administer after dialysis or consider dose adjustment based on post-dialysis assessment.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
Use with caution. No specific dose adjustment guidelines, but monitor for prolonged effects.
Severe:
Use with caution. No specific dose adjustment guidelines, but monitor for prolonged effects. Consider lower doses.
Pharmacology
Mechanism of Action
Neostigmine is a reversible anticholinesterase agent. It inhibits the hydrolysis of acetylcholine by acetylcholinesterase, resulting in an accumulation of acetylcholine at cholinergic synapses. This increased concentration of acetylcholine at the neuromuscular junction competes with neuromuscular blocking agents, thereby reversing their effects. It also has direct cholinomimetic effects on skeletal muscle.
Pharmacokinetics
Absorption:
Bioavailability:
100% (IV)
Tmax:
Immediate (IV)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
0.7-1.4 L/kg
ProteinBinding:
15-25%
CnssPenetration:
Limited
Elimination:
HalfLife:
0.5-2.1 hours (average ~1 hour)
Clearance:
Not readily available as a single value, primarily renal excretion.
ExcretionRoute:
Renal (urine)
Unchanged:
Approximately 50% (renal excretion)
Pharmacodynamics
OnsetOfAction:
1-10 minutes (IV)
PeakEffect:
5-15 minutes (IV)
DurationOfAction:
25-60 minutes (dose-dependent, patient-dependent)
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Muscle weakness
Twitching
Swelling in the arms or legs
Fever
Flushing
Shivering
Chest pain
Abnormal heartbeat (fast, slow, or irregular)
Shortness of breath
Severe dizziness or fainting
Seizures
Excessive sleepiness
Changes in vision
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Dizziness or headache
Upset stomach or vomiting
Dry mouth
Trouble sleeping
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor for medical advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Muscle weakness
Twitching
Swelling in the arms or legs
Fever
Flushing
Shivering
Chest pain
Abnormal heartbeat (fast, slow, or irregular)
Shortness of breath
Severe dizziness or fainting
Seizures
Excessive sleepiness
Changes in vision
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Dizziness or headache
Upset stomach or vomiting
Dry mouth
Trouble sleeping
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor for medical advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Difficulty breathing or shortness of breath
- Slow heartbeat or feeling faint
- Excessive sweating or salivation
- Abdominal cramps or diarrhea
- Muscle weakness or twitching
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Bowel blockage
+ Peritonitis (inflammation of the lining of the abdominal cavity)
+ Difficulty urinating
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Bowel blockage
+ Peritonitis (inflammation of the lining of the abdominal cavity)
+ Difficulty urinating
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so.
Precautions & Cautions
It is essential to inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you are 65 years of age or older, exercise caution when using this drug, as you may be more susceptible to experiencing side effects. Additionally, if you are pregnant, planning to become pregnant, or are currently breast-feeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Cholinergic crisis: severe muscle weakness (including respiratory muscles), bradycardia, hypotension, excessive salivation, lacrimation, miosis, bronchospasm, abdominal cramps, diarrhea, nausea, vomiting.
What to Do:
Immediate medical attention is required. Treatment involves discontinuing neostigmine, maintaining a patent airway, providing ventilatory support if needed, and administering atropine to counteract muscarinic effects. Call 911 or poison control (1-800-222-1222).
Drug Interactions
Contraindicated Interactions
- Patients with known hypersensitivity to neostigmine or bromides.
- Mechanical intestinal or urinary obstruction.
Major Interactions
- Succinylcholine (prolongs depolarizing block)
- Other neuromuscular blocking agents (non-depolarizing: antagonizes effects; depolarizing: prolongs effects)
- Anticholinergic agents (e.g., atropine, glycopyrrolate: used to counteract muscarinic effects, but excessive doses can reduce neostigmine's effectiveness)
- Corticosteroids (may reduce neostigmine's effect in myasthenia gravis, not typically relevant for NMB reversal)
- Aminoglycoside antibiotics (e.g., gentamicin, tobramycin: may potentiate neuromuscular blockade, requiring higher neostigmine doses)
Moderate Interactions
- Local anesthetics (may interfere with neuromuscular transmission)
- Magnesium salts (may potentiate neuromuscular blockade)
- Beta-blockers (increased risk of bradycardia)
- Cardiac glycosides (e.g., digoxin: increased risk of bradycardia/AV block)
- Quinidine (may antagonize neostigmine's effect)
Minor Interactions
- Not readily available for minor interactions specific to acute NMB reversal.
Monitoring
Baseline Monitoring
Neuromuscular function (e.g., Train-of-Four, TOF)
Rationale: To assess the degree of neuromuscular blockade and confirm readiness for reversal (e.g., 2-3 twitches present).
Timing: Immediately prior to administration of neostigmine.
Vital Signs (Heart Rate, Blood Pressure, SpO2)
Rationale: To establish baseline and monitor for adverse effects like bradycardia or hypotension.
Timing: Pre-administration.
Respiratory status (tidal volume, respiratory rate)
Rationale: To assess ventilatory adequacy before and after reversal.
Timing: Pre-administration.
Routine Monitoring
Neuromuscular function (TOF)
Frequency: Every 5-10 minutes until full recovery (TOF ratio >0.9)
Target: TOF ratio >0.9
Action Threshold: If TOF ratio <0.9 after adequate time, consider re-dosing or alternative reversal strategy.
Vital Signs (Heart Rate, Blood Pressure, SpO2)
Frequency: Every 5 minutes initially, then as clinically indicated until stable.
Target: Within patient's normal physiological range.
Action Threshold: Bradycardia (<50 bpm), hypotension (MAP <60-65 mmHg), or desaturation (<92%) requires immediate intervention.
Respiratory status (respiratory rate, depth, end-tidal CO2)
Frequency: Continuously until extubation and stable spontaneous ventilation.
Target: Adequate spontaneous ventilation, normal EtCO2.
Action Threshold: Hypoventilation, hypercapnia, or signs of respiratory distress require ventilatory support.
Symptom Monitoring
- Bradycardia
- Hypotension
- Bronchospasm
- Increased bronchial secretions
- Salivation
- Lacrimation
- Miosis
- Abdominal cramps
- Diarrhea
- Nausea
- Vomiting
- Muscle fasciculations
- Muscle weakness (cholinergic crisis)
Special Patient Groups
Pregnancy
Category C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks. Use only if clearly needed.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm, but data are limited. Avoid if possible.
Second Trimester:
Use with caution, monitor fetal heart rate if administered.
Third Trimester:
May cause uterine irritability and premature labor. Can also cause cholinergic effects in the neonate (e.g., muscle weakness, bradycardia). Use with extreme caution near term.
Lactation
L3 (Moderately Safe). Neostigmine is poorly absorbed orally, so infant exposure via breast milk is likely low. Monitor breastfed infant for signs of cholinergic effects (e.g., diarrhea, bradycardia, increased salivation).
Infant Risk:
Low risk of adverse effects due to poor oral absorption by the infant. Monitor for cholinergic symptoms.
Pediatric Use
Dosing is weight-based. Infants and children may be more susceptible to muscarinic side effects. Close monitoring of vital signs and neuromuscular function is essential. Max dose is lower than adults.
Geriatric Use
No specific dose adjustment based on age alone, but elderly patients may have reduced renal function, necessitating dose adjustment based on creatinine clearance. More susceptible to cardiovascular side effects (bradycardia). Monitor closely.
Clinical Information
Clinical Pearls
- Always administer neostigmine with an anticholinergic agent (e.g., glycopyrrolate or atropine) to mitigate muscarinic side effects like bradycardia, salivation, and bronchospasm.
- Ensure adequate spontaneous recovery from neuromuscular blockade (e.g., 2-3 twitches on TOF) before administering neostigmine for optimal reversal and to avoid prolonged weakness.
- Monitor neuromuscular function (TOF) closely after administration to confirm adequate reversal (TOF ratio >0.9) before extubation.
- Be prepared to manage cholinergic crisis (severe muscle weakness, bradycardia, secretions) with atropine and ventilatory support.
- Neostigmine is ineffective for reversal of succinylcholine-induced blockade and may prolong it.
Alternative Therapies
- Sugammadex (Bridion) - specifically for reversal of rocuronium and vecuronium, offers faster and more complete reversal in some cases, but is more expensive.
- Pyridostigmine (Mestinon) - primarily used for myasthenia gravis, not typically for acute NMB reversal due to slower onset and longer duration.
Cost & Coverage
Average Cost:
Varies, typically $10-$50 per 10ml vial (1mg/ml) per 10ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (generic injectable, widely covered by most insurance plans for hospital use)
General Drug Facts
If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed to someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or pour them down the drain. If you are unsure about the proper disposal method, consult your pharmacist for guidance. Many communities have drug take-back programs, which your pharmacist can help you locate. Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken to ensure prompt and effective treatment.