MIDAZOLAM

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Created Jul 2020 | Updated Nov 2020

MIDAZOLAM

  • [VERSED]
  • [NAYZILAM]

DEA CODE 2884: Schedule 4

Midazolam injection is used to produce sleepiness or drowsiness and relieve anxiety before surgery or certain procedures. When midazolam is used before surgery, the patient will not remember some of the details about the procedure. Midazolam injection is also used as an anesthesia to produce loss of consciousness before and during surgery. Midazolam injection is also used to treat status epilepticus, a severe type of seizure where there is more than one seizure within 5 minutes. Midazolam is a benzodiazepine. Benzodiazepines belong to the group of medicines called central nervous system (CNS) depressants, which are medicines that slow down the nervous system. This medicine is given only by or under the direct supervision of your doctor.

Pediatric:
Appropriate studies have not been performed on the relationship of age to the effects of midazolam in children below 6 months of age.

Safety and efficacy have not been established.

Geriatric:
Appropriate studies have not been performed on the relationship of age to the effects of midazolam in the geriatric population.

Safety and efficacy have not been established.

Other Interactions:

  • Ethanol
  • Grapefruit Juice

Other Medical Problems:
Make sure you tell your doctor if you have any other medical problems, especially:

  • Apnea (temporary stopping of breathing)
  • Heart disease
  • Hypoventilation (slow breathing)
  • Infections
  • Lung disease, severe
  • Lung or airway blockage- Use with caution. May increase risks for more serious side effects
  • Congestive heart failure
  • Kidney disease
  • Liver disease - Use with caution. The effects may be increased because of slower removal of the medicine from the body
  • Glaucoma, acute narrow-angle - Should not be used in patients with this condition

Prescribed for:
    What Conditions does it Treat?
  • Induce temporary amnesia
  • Anxious
  • Anxiety associated with an operation
  • Additional medication for calming
  • Calming of pediatric patient by sedative administration
  • Sedation with ability to respond to stimulation or speech
  • Additional agent to induce general anesthesia

Uses:
This medication is used in children before a procedure or anesthesia to cause drowsiness, decrease anxiety, and cause forgetfulness of the surgery or procedure.

It should be used while the child is under the care of a health professional.

It is not for home or long-term use.

Midazolam belongs to a class of medications called benzodiazepines, which produce a calming effect on the brain and nerves (central nervous system). It is thought to work by increasing the effect of a certain natural chemical (GABA) in the brain.

Before using:
Tell your doctor or pharmacist your medical history, especially of:

  • Kidney disease
  • Liver disease
  • Breathing problems (e.g., chronic obstructive pulmonary disease-COPD, sleep apnea)
  • Heart disease (e.g., congestive heart failure)
  • Glaucoma (open-angle)
  • Personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol)
Consult your doctor or pharmacist if you have:
  • glaucoma (narrow-angle)

Precautions:

  • This drug may make you dizzy or drowsy
  • Alcohol or marijuana (cannabis) can make you more dizzy or drowsy
  • Do not drive, use machinery, or do anything that needs alertness until you can do it safely.
  • Avoid alcoholic beverages.
  • Talk to your doctor if you are using marijuana (cannabis).

WARNINGS:
Midazolam has rarely caused very serious breathing problems (such as rapid/slow/shallow breathing, trouble breathing), especially if used with other medications that cause drowsiness (including opioid medications such as morphine). This medication should be used only in a hospital or medical office under the care of a health professional.

Read Reviews (8):
https://www.webmd.com/drugs/drugreview-16685-midazolam-oral.aspx?drugid=16685&drugname=midazolam-oral

IMPORTANT WARNING:
Midazolam may cause serious or life-threatening breathing problems such as shallow, slowed, or temporarily stopped breathing. Your child should only receive this medication in a hospital or doctor's office that has the equipment that is needed to monitor his or her heart and lungs and to provide life-saving medical treatment quickly if his or her breathing slows or stops. Your child's doctor or nurse will watch your child closely after he or she receives this medication to make sure that he or she is breathing properly. Tell your child's doctor if your child has a severe infection or if he or she has or has ever had any airway or breathing problems or heart or lung disease. Tell your child's doctor and pharmacist if your child is taking any of the following medications: antidepressants; barbiturates such as secobarbital (Seconal); droperidol (Inapsine); medications for anxiety, mental illness, or seizures; narcotic medications for pain such as fentanyl (Actiq, Duragesic, Sublimaze, others), morphine (Avinza, Kadian, MS Contin, others), and meperidine (Demerol); sedatives; sleeping pills; or tranquilizers.

Dravet syndrome:
Midazolam is a benzodiazepine that is given to children before a medical procedure to relieve anxiety. It also is used as the first-line treatment of status epilepticus in children. Status epilepticus is when seizures last longer than five minutes, or multiple seizures occur close together without the patient recovering between them. Children with Dravet syndrome often experience status epilepticus, which can be life-threatening. Midazolam is a so-called rescue medicine that can be used to stop a seizure before it progresses to a medical emergency.

Dentistry (1993 Article):
Introduction: Much interest has been focused on the use of midazolam (Versed~Roche Laboratories of Hoffman LaRoche, Nutley, NJ) for conscious sedation in pediatric dentistry. The drug has been used as a preanesthetic sedative in adults and more recently in children. However, studies are lacking concerning its use in pediatric dentistry. The purpose of this paper is to review the pharmacokinetics of midazolam in children and its routes of administration including intravenous, oral rectal, and nasal routes.

Summary: Midazolam is a short-acting, water-soluble benzodiazepine. It has anxiolytic, sedative, hypnotic, anticonvulsant, muscle-relaxant, and anterograde amnesic effects. The drughas been used as a preanesthetic sedative in adults, andmore recently in children. This paper reviewed the pharmacokinetics of midazolam and its routes of administration in children. Intranasal administration was found tohave many advantages including rapid onset of sedation, ease of administration, and safety. The use of intranasal midazolam together with nitrous oxide/oxygen for conscious sedation of children during dental treatment should be investigated.

AAPD PDF Midazolam

Anesthesia:
A recent article from the California Society of Anesthesiologists BULLETIN underscored the danger of respiratory depression, morbidity, and mortality while using the remarkably effective and very useful drug, midazolam. This letter asks all anesthesiologists to be personally vigilant when using midazolam and to inform colleagues (endoscopist, dentists, etc.) concerning the appropriate dosage and potential hazards of midazolam.

Epilepsy:
Midazolam is a rescue medication that is approved for use:

  • For short-term treatment of increased or frequent seizures called seizure clusters or acute repetitive seizures.
  • In children over 12 years old and in adults.
  • It is not supposed to be taken daily.
  • This medicine does not take the place of your daily seizure medicine.

Nayzilam (midazolam) nasal spray Used to treat
Absence Seizures, Atonic Seizures, Atypical Absence Seizures, Clonic Seizures, Focal Impaired Awareness or Complex Partial Seizures, Febrile Seizures, Myoclonic Seizures, Secondarily Generalized Seizures or Bilateral Tonic Clonic Seizure, Focal Aware or Simple Partial Seizure, Tonic Seizures, Tonic-clonic Seizures, Unknown Onset

UCB PDF Midazolam

Breastfeeding:

Summary of Use During Lactation:
The small amounts of midazolam excreted into breastmilk would not be expected to cause adverse effects in most breastfed infants.

Two expert panels advocates waiting for at least 4 hours after a single intravenous dose of midazolam (e.g., for endoscopy) before resuming nursing.

However, after a single dose of diazepam, as for sedation before a procedure or for a seizure, there is usually no need to wait to resume breastfeeding, although with a newborn or preterm infant, a cautious approach would be to wait a period of 6 to 8 hours before resuming nursing. After general anesthesia, breastfeeding can be resumed as soon as the mother has recovered sufficiently from general anesthesia to nurse. When a combination of anesthetic agents is used for a procedure, follow the recommendations for the most problematic medication used during the procedure.

With prolonged use (days) of intravenous therapy, an active metabolite can accumulate in the mother and might affect the infant, but data in breastfeeding are lacking.

Drug Levels:
Midazolam is about 36% bioavailable orally in adults. It is metabolized to 1-hydroxymidazolam (60 to 70%) and 4-hydroxymidazolam (5%) which are about equipotent to midazolam. The half-life of 1-hydroxymidazolam is about 12 hours in adults and can accumulate with prolonged or repeated doses or in renal impairment.

Alternate Drugs to Consider:

Versed Pharmacokinetics:

  • Absorption:
    Absorption after I.M. administration appears to be 80% to 100% and after oral administration 40% to 50%.
  • Distribution:
    Drug has a large volume of distribution and is about 97% protein-bound. Drug crosses the placental barrier and enters fetal circulation.
  • Metabolism:
    Metabolized in the liver.
  • Excretion:
    Metabolites are excreted in urine. Half-life of drug is 1 1/4 to 12 1/3 hours. Half-life is prolonged in obese patients, the elderly, and seriously ill neonates.

Midazolam
Duration:

A common hypnotic, sedative and anxiolytic benzodiazepine. High doses may cause amnesia and loss of inhibitions. Unusually, it is water soluble, and commonly used as a premedication for sedation as the solubility makes it better for IV use than other benzodiazepines.

RouteOnsetDurationAfter Effects
Tripsit Factsheets
IM:10-20 minutes4-8 hours1-12 hours
IV:0-1 minutes4-8 hours1-12 hours
Rectal:15-25 minutes4-8 hours1-12 hours
Insufflated: 1-5 minutes4-8 hours1-12 hours
Oral:10-40 minutes4-8 hours1-12 hours
Midazolam Duration
Avoid:
All other CNS depressants.
Effects:
Anxiolytic, Sedative, Muscle Relaxant, Amnesia, Dystaxia, Hypnotic.


Midazolam, previously marketed under the trade name Versed, is a medication used for anesthesia, procedural sedation, trouble sleeping, and severe agitation. Midazolam is a short-acting benzodiazepine central nervous system (CNS) depressant. Pharmacodynamic properties of midazolam and its metabolites, which are similar to those of other benzodiazepines, include sedative, anxiolytic, amnesic and hypnotic activities. Benzodiazepine pharmacologic effects appear to result from reversible interactions with the y-amino butyric acid (GABA) benzodiazepine receptor in the CNS, the major inhibitory neurotransmitter in the central nervous system. The action of midazolam is readily reversed by the benzodiazepine receptor antagonist, flumazenil. Data from published reports of studies in pediatric patients clearly demonstrate that oral midazolam provides safe and effective sedation and anxiolysis prior to surgical procedures that require anesthesia as well as before other procedures that require sedation but may not require anesthesia. The most commonly reported effective doses range from 0.25 to 1 mg/kg in children (6 months to <16 years). The single most commonly reported effective dose is 0.5 mg/kg. Time to onset of effect is most frequently reported as 10 to 20 minutes. The effects of midazolam on the CNS are dependent on the dose administered, the route of administration, and the presence or absence of other medications.

How Does Execution Drug Midazolam Work?
States can still use the sedative drug midazolam in lethal injections, according to today's Supreme Court decision. But how exactly does the drug work, and why do some say that it's unreliable? In a 5-to-4 vote, the court ruled that using midazolam does not violate the Eighth Amendment, which prohibits "cruel and unusual punishment." In executions, the drug has been used to induce unconsciousness before other drugs are administered to stop an inmate's breathing and stop the heart. However, midazolam was involved in several botched executions last year, including the case of Clayton Lockett from Oklahoma, who lived for about 45 minutes after he was administered drugs for lethal injection, and was seen convulsing and writhing before dying of a heart attack. (It was later determined that the IV line used to deliver the drugs in Lockett's execution was not properly placed.) In another controversial execution in Ohio, which also used midazolam, the inmate seemed unconscious at first, but then made loud snorting and choking noises before being pronounced dead, according to the New York Times. The combination of drugs used in the Ohio case had not previously been used in an execution.
- https://www.livescience.com/51384-execution-drug-midazolam-effect.html

Midazolam hydrochloride
Maximum Dosage:
Prescribers Digital Reference
Adults:1 spray (5 mg)/dose intranasal up to 2 doses/episode for acute repetitive seizures. Specific maximum dosage information for other routes or indications is not available; the dose required is dependent on route of administration, indication for therapy, and clinical response.
Geriatric:1 spray (5 mg)/dose intranasal up to 2 doses/episode for acute repetitive seizures. Specific maximum dosage information for other routes or indications is not available; the dose required is dependent on route of administration, indication for therapy, and clinical response.
Adolescents:1 mg/kg PO (Max: 20 mg/dose) for procedural sedation; a total dose up to 5 mg IV may be necessary for amnesia induction; 1 spray (5 mg)/dose intranasal up to 2 doses/episode for acute repetitive seizures; specific maximum dosage information for other routes or indications is not available; the dose required is dependent on route of administration, indication, and clinical response.
Children:12 years: 1 mg/kg PO (Max: 20 mg/dose) as a single dose for procedural sedation; a total dose up to 0.4 mg/kg IV (Usual Max: 10 mg) may be necessary for amnesia induction; 1 spray (5 mg)/dose intranasal up to 2 doses/episode for acute repetitive seizures; specific maximum dosage information for other routes or indications is not available; the dose required is dependent on route of administration, indication, and clinical response.
Children:6 to 11 years: 1 mg/kg PO (Max: 20 mg/dose) as a single dose for procedural sedation; a total dose up to 0.4 mg/kg IV (Usual Max: 10 mg) may be necessary for amnesia induction; specific maximum dosage information for other routes or indications is not available; the dose required is dependent on route of administration, indication, and clinical response.
Children:1 to 5 years: 1 mg/kg PO (Max: 20 mg/dose) as a single dose for procedural sedation; a total dose up to 0.6 mg/kg IV (Usual Max: 6 mg) may be necessary for amnesia induction; specific maximum dosage information for other routes or indications is not available; the dose required is dependent on route of administration, indication, and clinical response.
Infants:6 to 11 months: 1 mg/kg PO (Max: 20 mg/dose) as a single dose for procedural sedation; a total dose up to 0.6 mg/kg IV (Usual Max: 6 mg) may be necessary for amnesia induction; specific maximum dosage information for other routes or indications is not available; the dose required is dependent on route of administration, indication, and clinical response.
Infants:1 to 6 months: Specific maximum dosage information is not available; the dose required is dependent on route of administration, indication, and clinical response.
Neonates:Specific maximum dosage information is not available; the dose required is dependent on route of administration, indication, and clinical response.

Midazolam (Rx)
Black Box Warnings:
Respiratory depression/arrest has been associated with use, especially when used for sedation in noncritical care settings

Use lower end of dosing range in debilitated patients, including the elderly

Do not administer by rapid IV injection in neonates (hypotension and seizures reported, especially when used concomitantly with fentanyl)

Respiratory depression, airway obstruction, desaturation, hypoxia, and apnea, particularly when used with concomitant CNS depressants (eg, opioids), have been reported

Should be used only in settings (eg, hospital, ambulatory care settings, including physicians' or dentists' offices) that can provide continuous monitoring of respiratory and cardiac function; immediate availability of resuscitative drugs and age- and size-appropriate equipment for ventilation and intubations, as well as personnel trained in their use and skilled in airway management, should be ensured

For deeply sedated patients, a dedicated individual other than the practitioner performing the procedure should monitor the patient throughout the procedure

Use of the 1 mg/mL formulation or dilution of the 1 mg/mL or 5 mg/mL formulation is recommended to facilitate slower injection

Adult dosing

  • The initial IV dose for sedation in adult patients may be as little as 1 mg but should not exceed 2.5 mg in a normal, healthy adult; lower doses are necessary for older (>60 years) or debilitated patients and for patients receiving concomitant narcotics or other CNS depressants; the initial dose and all subsequent doses should always be titrated slowly; administer over at least 2 minutes and allow an additional 2 or more minutes to fully evaluate the sedative effect

Pediatric dosing

  • Doses of sedative medications in pediatric patients must be calculated on a mg/kg basis, and initial doses and all subsequent doses should always be titrated slowly; the initial pediatric dose of midazolam for sedation/anxiolysis/amnesia is age, procedure, and route dependent.

Neonates

  • Midazolam should not be administered by rapid injection in the neonatal population; severe hypotension and seizures have been reported following rapid IV administration, particularly with concomitant use of fentanyl

General anesthetics and sedation drugs in young children and pregnant women

  • Brain development
    • Prolonged or repeated exposure may result in negative effects on fetal or young children's brain development
    • Caution with use during surgeries or procedures in children younger than 3 yr or in pregnant women during their third trimester
    • Assess the risk:benefit ratio in these populations, especially for prolonged procedures (ie, >3 hr) or multiple procedures

Midazolam Injection (midazolam)
Side Effects:
RxList
Common side effects of Midazolam include:
  • headache
  • nausea
  • vomiting
  • cough
  • drowsiness
  • hiccups
  • "oversedation
  • injection site reactions (pain, swelling, redness, stiffness, blood clots, and tenderness)

Liver:
Midazolam therapy has not been associated with serum aminotransferase elevations and has not been linked to cases of clinically apparent liver injury.

Midazolam Hepatotoxicity:
Midazolam, like other benzodiazepines, is rarely associated with serum ALT elevations. Clinically apparent liver injury from midazolam has not been reported and must be extremely rare, if it occurs at all. Cases of clinically apparent liver injury have been reported with other benzodiazepines including alprazolam, chlordiazepoxide, clonazepam, diazepam, flurazepam and triazolam. The clinical pattern of acute liver injury from benzodiazepines is typically cholestatic, but hepatocellular patterns of injury have been reported with chlorazepate and clotiazepam. The injury is usually mild to moderate in severity with a time to onset of 1 to 6 months. Fever and rash are uncommon as is autoantibody formation.

E Likelihood score: E (unlikely cause of clinically apparent liver injury).


Important Information:

Midazolam can slow or stop your breathing, especially if you have recently used a narcotic (opioid) medication. Midazolam is given in a hospital, dentist office, or other clinic setting where your vital signs can be watched closely.

You should not take midazolam if you have narrow-angle glaucoma, if you are allergic to cherries, or if you are allergic to midazolam or similar medicines (Valium, Xanax, Ativan, and others).

Do not drink alcohol for at least 24 hours after taking midazolam.

Do not drink alcohol for at least 24 hours after taking midazolam. This medication can increase the effects of alcohol, which could be dangerous.

Grapefruit and grapefruit juice may interact with midazolam and lead to potentially dangerous effects. Avoid the use of grapefruit products while taking midazolam.

Midazolam injection can cause extreme drowsiness that may last for 24 hours after you have received the medication. Older adults may feel sleepy for even longer.

Avoid driving or doing anything that requires you to be awake and alert until the effects of midazolam have worn off completely.

Interactions:

Drug Interactions (461) Alcohol/Food Interactions (2) Disease Interactions (12)


What other drugs will affect Midazolam?
Shortly after you take midazolam, taking other drugs that make you sleepy or slow your breathing can cause dangerous side effects. Tell your doctor if you regularly use a sleeping pill, narcotic pain medicine, prescription cough medicine, a muscle relaxer, or medicine for anxiety, depression, or seizures. Many drugs can interact with midazolam. Not all possible interactions are listed here. Tell your doctor about all your current medicines, especially:
  • antifungal medicine
  • an antibiotic
  • an antidepressant
  • heart or blood pressure medicine
  • antiviral medicine to treat hepatitis C or HIV/AIDS
  • seizure medication
  • tuberculosis medication
This list is not complete and many other drugs can interact with midazolam. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Give a list of all your medicines to any healthcare provider who treats you.

A total of 461 drugs are known to interact with Midazolam.

  • 31 major drug interactions
  • 391 moderate drug interactions
  • 39 minor drug interactions

Caymanchem PDF Midazolam

History:
Midazolam is among about 35 benzodiazepines currently used medically, and was synthesized in 1975 by Walser and Fryer at Hoffmann-LaRoche, Inc in the United States. Owing to its water solubility, it was found to be less likely to cause thrombophlebitis than similar drugs. The anticonvulsant properties of midazolam were studied in the late 1970s, but not until the 1990s did it emerge as an effective treatment for convulsive status epilepticus. As of 2010, it is the most commonly used benzodiazepine in anesthetic medicine. In acute medicine, midazolam has become more popular than other benzodiazepines, such as lorazepam and diazepam, because it is shorter lasting, is more potent, and causes less pain at the injection site. Midazolam is also becoming increasingly popular in veterinary medicine due to its water solubility.

Midazolam can be given by mouth, intravenously, or injection into a muscle, by spraying into the nose, or through the cheek. When given intravenously, it typically begins working within five minutes; when injected into a muscle, it can take fifteen minutes to begin working. Effects last for between one and six hours. Side effects can include a decrease in efforts to breathe, low blood pressure, and sleepiness. Tolerance to its effects and withdrawal syndrome may occur following long-term use. Paradoxical effects, such as increased activity, can occur especially in children and older people. There is evidence of risk when used during pregnancy but no evidence of harm with a single dose during breastfeeding. Midazolam was patented in 1974 and came into medical use in 1982.

  
Midazolam 1 Mg/Ml In Sodium Chloride, Iso-Osmotic Intravenous Solution Benzodiazepines-Injectable - Uses, Side Effects, and More - Infants and children younger than 3 years using anesthesia or drugs for sedation (including midazolam) for procedures/surgeries may be at risk for slower brain growth. Talk to the doctor about the ...
Tuesday May 10, 2022 - webmd.com

Night-Time Use of Sedative Increases Heart Damage Risk - A new research study has found that midazolam – a sedative used before surgery to make patients relaxed and sleepy – is associated with a greater risk of heart damage when used at night.
Friday February 03, 2023 - technologynetworks.com

Midazolam - Indications, Dosage, Side Effects and Precautions - Latest prescription information about Midazolam. Learn how to pronounce the drug's name, its indications, dosage, how to take, when to take, when not to take, side effects, special precautions ...
Sunday August 16, 2020 - medindia.net

Midazolam/Ginkgo Biloba Interactions - Consult your healthcare professional before taking or discontinuing any drug or commencing any course of treatment. Let your healthcare professionals (e.g. doctor or pharmacist) know that you are ...
Wednesday July 24, 2019 - webmd.com

Thousands of doses of fentanyl stolen from Fenton hospital; feds investigating - More than three thousand vials of liquid fentanyl have been stolen from SSM Health St. Clare Hospital in Fenton. The drug — almost two gallons worth of it — went missing alongside more than 700 vials ...
Thursday January 26, 2023 - msn.com

Midazolam HCl Market Research on Present State and Future Growth Prospects of Key Players, Forecast by 2023 To 2028 - Midazolam hydrochloride is the hydrochloride salt of midazolam. It has a role as an anticonvulsant, an antineoplastic agent, an anxiolytic drug, an apoptosis inducer, a central nervous system ...
Wednesday January 25, 2023 - marketwatch.com

Top Tennessee prison officials fired after report finds ‘shocking’ issues with death penalty drugs - Two top Tennessee corrections officials have been fired, following a report that found “shocking” issues with the state’s death penalty protocols. Debra Inglis, general counsel at the Tennessee ...
Monday January 23, 2023 - msn.com

Status Epilepticus: Clinical Analysis of a Treatment Protocol Based on Midazolam and Phenytoin - Eighty-three patients were excluded because of pretreatment with another antiepileptic medication (37), treatment with midazolam bolus directly followed by continuous midazolam (without prior ...
Thursday January 26, 2023 - medscape.com

A Prospective Observational Cohort Pilot Study of the Association Between Midazolam Use and Delirium in Elderly Endoscopy Patients - Background: Midazolam is a benzodiazepine commonly used in procedural sedation and general anaesthesia. Current anaesthetic guidelines advise the avoidance of benzodiazepines in elderly patients ...
Tuesday March 16, 2021 - medscape.com

Top Tennessee pair fired after damning review of state’s execution protocol - The report also found that the three drugs used in the state’s protocol – midazolam to sedate the person, vecuronium bromide to paralyze the person and potassium chloride to stop their heart ...
Saturday January 21, 2023 - theguardian.com

  
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