Which side effect is most common for midazolam

Midazolam is a short-acting injectable benzodiazepine with rapid onset that is commonly used in seizures, anesthesia and anxiety disorders.

Brand NamesGeneric NameMidazolamDrugBank Accession NumberDB00683Background

Midazolam is a short-acting hypnotic-sedative drug with anxiolytic, muscle relaxant, anticonvulsant, sedative, hypnotic, and amnesic properties. It belongs to a class of drugs called benzodiazepines. This drug is unique from others in this class due to its rapid onset of effects and short duration of action. Midazolam is available by oral, rectal, intranasal, intramuscular (IM), and intravenous (IV) routes and has been used in various biomedical applications, including dentistry, cardiac surgery, and endoscopic procedures as pre-anesthetic medication, and as an adjunct to local anesthesia.

This drug was initially approved by the US FDA in 1985, and has been approved for various indications since. In late 2018, the intramuscular preparation was approved by the FDA for the treatment of status epilepticus in adults. In May 2019, the nasal spray of midazolam was approved for the acute treatment of distinctive intermittent, stereotypic seizure episodes in patients 12 years of age and older. Midazolam is considered a schedule IV drug in the United States due to the low potential for abuse and low risk of dependence.

TypeSmall MoleculeGroupsApproved, IllicitStructure

WeightAverage: 325.767
Monoisotopic: 325.078203343Chemical FormulaC18H13ClFN3SynonymsExternal IDs

• Dea No. 2884
• Ro 21-3981/001
• Ro 21-3981/003

Intravenous

Indicated for promoting preoperative sedation, anxiolysis, anesthesia induction, or amnesia.

Intramuscular

Indicated for the treatment of status epilepticus in adults.

Nasal

Indicated for the acute treatment of intermittent, stereotypic episodes of frequent seizure activity (i.e., seizure clusters, acute repetitive seizures) that are distinct from a patient’s usual seizure pattern in patients with epilepsy 12 years of age and older.

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Associated ConditionsAssociated Therapies

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Pharmacodynamics

General effects

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 benzodiazepine drugs, include sedative, anxiolytic, amnestic, muscle relaxant, as well as hypnotic activities. Benzodiazepines enhance the inhibitory action of the amino acid neurotransmitter gamma-aminobutyric acid (GABA). Receptors for GABA are targeted by many important drugs that affect GABA function and are commonly used in the treatment of anxiety disorder, epilepsy, insomnia, spasticity, and aggressive behavior.

Sedation and memory

The onset of sedation after intramuscular administration in adults is 15 minutes, with maximal sedation occurring 30-60 minutes after injection. In one study of adults, when tested the following day, 73% of the patients who were administered midazolam intramuscularly had no recollection of memory cards shown 30 minutes following drug administration; 40% had no recollection of the memory cards shown 60 minutes after drug administration. Onset time of sedative effects in pediatric patients begins within 5 minutes and peaks at 15-30 minutes depending upon the dose administered. In the pediatric population, up to 85% had no memory of pictures shown after receiving intramuscular midazolam compared to 5% of the placebo control group.

Sedation in both adult and pediatric patients is reached within 3 to 5 minutes post intravenous (IV) injection. The time of onset is affected by the dose administered and the simultaneous administration of narcotic pre-medication. Seventy-one (71%) percent of the adult patients in clinical endoscopy studies had no memory of insertion of the endoscope; 82% of the patients had no memory of withdrawal of the endoscope.

Anesthesia induction

When midazolam is administered intravenously (IV) for anesthetic induction, induction of anesthesia occurs in about 1.5 minutes when narcotic pre-medication has been given and in 2 to 2.5 minutes without narcotic pre-medication/ other sedative pre-medication. Impairment in a memory test was observed in 90% of the patients.

Mechanism of action

The actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the central nervous system. Benzodiazepines increase the activity of GABA, thereby producing a sedating effect, relaxing skeletal muscles, and inducing sleep, anesthesia, and amnesia. Benzodiazepines bind to the benzodiazepine site on GABA-A receptors, which potentiates the effects of GABA by increasing the frequency of chloride channel opening. These receptors have been identified in different body tissues including the heart and skeletal muscle, although mainly appear to be present in the central nervous system.

Absorption

Oral Absorption: Rapidly absorbed after oral administration. The absolute bioavailability, if given intramuscularly (IM), is greater than 90% . Due to first pass metabolism, only 40-50% of the administered oral dose reaches the circulation. The absolute bioavailability of the midazolam syrup in pediatric patients is about 36%.

Intramuscular Absorption: The mean peak concentration (Cmax) and time to peak (Tmax) following the IM dose was 90 ng/mL (20% CV) and 0.5 hour (50% CV).

Rectal administration: After rectal administration midazolam is absorbed rapidly. Maximum plasma concentration is reached within 30 minutes. The absolute bioavailability is approximately 50%.

Intranasal Administration: Midazolam is absorbed rapidly after intranasal administration. Mean peak plasma concentrations are reached within 10.2 to 12.6 minutes. The bioavailability is between 55 and 57%.

Volume of distribution

Female gender, old age, and obesity may increase the volume of distribution. Midazolam may also cross the placenta and has been detected in human milk and cerebrospinal fluid.,

Intravenous administration

1.24 to 2.02 L/kg [pediatric patients (6 months to <16 years) receiving 0.15 mg/kg IV midazolam] 1 to 3.1 L/kg [midazolam intravenously administered, healthy adults].

Intramuscular administration

The mean apparent volume of distribution of midazolam after a single IM dose of 10 mg midazolam in healthy adults was 2117 (±845.1) mL/kg.

Protein binding

Midazolam is approximately 97% bound to plasma protein, mainly albumin, in adults. The 1-hydroxy metabolite is approximately 89% bound to plasma protein.

Metabolism

Midazolam is primarily metabolized in the liver and gut by CYP3A4 to its pharmacologic active metabolite, alpha-hydroxymidazolam (also known as 1-hydroxy-midazolam), and 4-hydroxymidazolam (which makes up 5% or less of the biotransformation products). This metabolite likely contributes to the pharmacological effects of midazolam. Midazolam also undergoes N-glucuronidation via UGT1A4 after the process of hepatic oxidation by cytochrome enzymes.

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Route of elimination

The α-hydroxymidazolam glucuronide conjugate of midazolam is excreted in urine. No significant amount of parent drug or metabolites is found in urine before beta-glucuronidase and sulfatase deconjugation, suggesting that the urinary metabolites are excreted mainly as conjugates. The amount of midazolam excreted unchanged in the urine when given intravenously is less than 0.5%. 45% to 57% of the dose was excreted in the urine as 1-hydroxymethyl midazolam conjugate.

Plasma clearance of midazolam is higher in patients that remain in supine position, because of a 40-60 percent increase in hepatic blood flow during supination. Pregnancy may also increase the metabolism of midazolam.

Half-life

Intravenous: healthy adults = 1.8 to 6.4 hours (mean of 3 hours).

Intramuscular: Following IM administration of 10 mg midazolam, mean (±SD) elimination half-life was 4.2 (±1.87) hours.

Clearance

Intramuscular: apparent total body clearance, 367.3 (±73.5) mL/hr/kg. Intravenous: total clearance (Cl), 0.25 to 0.54 L/hr/kg

Adverse Effects

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Toxicity

LD50=215 mg/kg, in rats.

Overdose

Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs. Serious cardiorespiratory adverse reactions have occurred, sometimes ending in death or permanent neurologic effects, after the administration of midazolam.

A note on cardiac and respiratory depression

After administration of midazolam, continuous monitoring of respiratory and cardiac function is recommended until the patient is in stable condition. Serious and life-threatening cardiorespiratory adverse reactions, including hypoventilation, airway obstruction, apnea, and hypotension have been reported with the use of midazolam. Patients should be monitored in a setting with immediate access to resuscitative drugs if they are required. Resuscitation equipment and personnel trained in their use and skilled in airway management should be available when midazolam is administered.

The usual recommended intramuscular pre-medicating doses of midazolam do not depress the ventilatory response to carbon dioxide stimulation to a clinically significant extent in adults. Intravenous induction doses of midazolam depress the ventilatory response to carbon dioxide stimulation for at least 15 minutes longer than the duration of ventilatory depression following administration of thiopental in adults. Impairment of ventilatory response to carbon dioxide is more severe in adult patients diagnosed with chronic obstructive pulmonary disease (COPD).

A note on dependence

When midazolam is used in long-term sedation in the ICU (intensive care unit) or other settings, physical dependence on midazolam may develop. The risk of dependence increases with dose and duration of treatment; this risk is also greater in patients with a medical history of substance abuse.

Special caution should be exercised when administering midazolam in the following populations

High-risk patients include adults over 60 years of age, chronically ill or debilitated patients, which may include patients with chronic respiratory insufficiency, patients with chronic renal failure, impaired hepatic function or with impaired cardiac function, pediatric patients (especially those with cardiovascular instability). These high-risk patients require lower dosages and should be monitored on a continuous basis for early signs of alterations of vital functions, so that appropriate management may be administered.

Mutagenesis

Midazolam was negative for genotoxicity during in vitro and in vivo assays.

Impairment of Fertility

When midazolam (0, 1, 4, or 16 mg/kg) was given orally to male and female rats before and during mating and continuing in females throughout gestation and lactation, no adverse effects on male or female fertility were observed. Midazolam plasma exposures (AUC) at the highest dose tested were approximately 6 times that in humans at the recomended human dose.

PathwaysNot AvailablePharmacogenomic Effects/ADRsNot Available

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

DrugInteraction

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1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Midazolam is combined with 1,2-Benzodiazepine.AbacavirMidazolam may decrease the excretion rate of Abacavir which could result in a higher serum level.AbametapirThe serum concentration of Midazolam can be increased when it is combined with Abametapir.AbataceptThe metabolism of Midazolam can be increased when combined with Abatacept.AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Midazolam.AbirateroneThe serum concentration of Midazolam can be increased when it is combined with Abiraterone.AcalabrutinibThe serum concentration of Midazolam can be increased when it is combined with Acalabrutinib.AceclofenacAceclofenac may decrease the excretion rate of Midazolam which could result in a higher serum level.AcemetacinAcemetacin may decrease the excretion rate of Midazolam which could result in a higher serum level.AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Midazolam.

Food Interactions

• Avoid grapefruit products.

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Product IngredientsInternational/Other BrandsAnquil (General Pharma) / Benzosed (Pharmaceutical) / Dalam (Richmond) / Damizol (Specifar) / Demizolam (Dem Ilaç) / Doricum (Roche) / Dormicum (Roche) / Dormid (Scott) / Dormipron (Chalver) / Dormire (Cristália) / Dormitol (Square) / Dormixal (Demo) / Dormonid (Roche) / Drimnorth (Northia) / Epistatus (IFET) / Flormidal (Galenika) / Fulsed (Ranbaxy) / Fulsed Injection (Terapia) / Garen (Bio-Pharma) / Gobbizolam (Gobbi) / Hipnazolam (EMS) / Hipnoz (Pharos) / Hypnofast (Incepta) / Hypnovel (Roche) / Ipnovel (Roche) / Nocturna (Lafi) / Setam (Rimsa) / Talentum (Fisiopharma) / Terap (Sanitas) / Versed (Roche)Brand Name Prescription ProductsNameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImageBuccolamSolution10 mgBuccalLaboratorios Lesvi S.L.2016-09-08Not applicableEUBuccolamSolution2.5 mgBuccalLaboratorios Lesvi S.L.2016-09-08Not applicableEUBuccolamSolution5 mgBuccalLaboratorios Lesvi S.L.2022-05-04Not applicableEUBuccolamSolution7.5 mgBuccalLaboratorios Lesvi S.L.2016-09-08Not applicableEUBuccolamSolution10 mgBuccalLaboratorios Lesvi S.L.2022-05-04Not applicableEUBuccolamSolution2.5 mgBuccalLaboratorios Lesvi S.L.2022-05-04Not applicableEUBuccolamSolution5 mgBuccalLaboratorios Lesvi S.L.2016-09-08Not applicableEUBuccolamSolution7.5 mgBuccalLaboratorios Lesvi S.L.2022-05-04Not applicableEUMidazolam HClInjection, solution1 mg/1mLIntravenousCantrell Drug Company2013-06-28Not applicableUSMidazolam HClInjection, solution0.5 mg/1mLIntravenousCantrell Drug Company2014-09-03Not applicableUSGeneric Prescription ProductsNameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImageApo-midazolam Injectable 1 mg/mlLiquid1 mg / mLIntramuscular; IntravenousApotex Corporation2001-04-102013-08-02CanadaApo-midazolam Injectable 5 mg/mlLiquid5 mg / mLIntramuscular; IntravenousApotex Corporation2001-04-102013-08-02CanadaMidazolamInjection1 mg/1mLIntramuscular; IntravenousHikma Pharmaceuticals USA Inc.2000-06-20Not applicableUSMidazolamInjection1 mg/1mLIntramuscular; IntravenousCardinal Health2000-06-20Not applicableUSMidazolamInjection, solution1 mg/1mLIntramuscular; IntravenousFresenius Kabi USA, LLC2000-07-14Not applicableUSMidazolamInjection, solution1 mg/1mLIntramuscular; IntravenousSagent Pharmaceuticals2012-03-192016-04-01USMidazolamInjection, solution5 mg/1mLIntramuscular; IntravenousGeneral Injectables and Vaccines, Inc.2020-11-12Not applicableUSMidazolamInjection5 mg/1mLIntramuscular; IntravenousA-S Medication Solutions2000-06-20Not applicableUSMidazolamInjection, solution10 mg/2mLIntramuscular; IntravenousFresenius Kabi USA, LLC2014-10-03Not applicableUSMidazolamInjection, solution5 mg/1mLIntramuscular; IntravenousThe Medicines Company2000-07-142015-09-30USUnapproved/Other ProductsNameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImageMidazolam HClMidazolam hydrochloride (1 mg/1mL)Injection, solutionIntravenousCantrell Drug Company2013-06-28Not applicableUSMidazolam HClMidazolam hydrochloride (0.5 mg/1mL)Injection, solutionIntravenousCantrell Drug Company2014-09-03Not applicableUSMIDOLAM 15 MG/3 ML IM/IV REKTAL COZELTI ICEREN AMPUL, 5 ADETMidazolam (15 mg/3ml)InjectionIntramuscular; IntravenousPHARMADA İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkeyMIDOLAM 5 MG/1 ML IM/IV REKTAL COZELTI ICEREN AMPUL, 5 ADETMidazolam (5 mg/1ml)InjectionIntramuscular; IntravenousPHARMADA İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkeyMIDOLAM 50 MG/10 ML IM/IV REKTAL COZELTI ICEREN AMPUL, 5 ADETMidazolam (50 mg/10ml)InjectionIntramuscular; IntravenousPHARMADA İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkeyMILOZ 5 MG/5ML 10 AMPULMidazolam (5 mg)Injection, solutionIntravenousBİEM İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkeyMKH Dose PackMidazolam (3 mg/1) + Hydroxyzine hydrochloride (10 mg/1) + Ketamine hydrochloride (25 mg/1)TrocheSublingualImprimis Njof, Llc2019-03-04Not applicableUSMKO MeltMidazolam (3 mg/1) + Ketamine hydrochloride (25 mg/1) + Ondansetron hydrochloride dihydrate (2 mg/1)TrocheSublingualImprimis Njof, Llc2018-12-012019-03-04USMKO Melt Dose PackMidazolam (3 mg/1) + Ketamine hydrochloride (25 mg/1) + Ondansetron hydrochloride (2 mg/1)TrocheSublingualImprimis Njof, Llc2019-03-04Not applicableUS

ATC CodesN05CD08 — MidazolamChemical TaxonomyProvided by ClassyfireDescriptionThis compound belongs to the class of organic compounds known as imidazo[1,5-a][1,4]benzodiazepines. These are compounds containing an imidazole ring and a 1,4-benzodiazepine ring system, both sharing one nitrogen atom.KingdomOrganic compoundsSuper ClassOrganoheterocyclic compoundsClassBenzodiazepinesSub Class1,4-benzodiazepinesDirect ParentImidazo[1,5-a][1,4]benzodiazepinesAlternative ParentsFluorobenzenes / 1,4-diazepines / N-substituted imidazoles / Aryl fluorides / Aryl chlorides / Heteroaromatic compounds / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds / Organofluorides / Organochlorides / Hydrocarbon derivatives show 3 moreSubstituentsAromatic heteropolycyclic compound / Aryl chloride / Aryl fluoride / Aryl halide / Azacycle / Azole / Benzenoid / Fluorobenzene / Halobenzene / Heteroaromatic compound / Hydrocarbon derivative / Imidazo[1,5-a][1,4]benzodiazepine / Imidazole / Imine / Ketimine / Monocyclic benzene moiety / N-substituted imidazole / Organic 1,3-dipolar compound / Organic nitrogen compound / Organochloride / Organofluoride / Organohalogen compound / Organonitrogen compound / Organopnictogen compound / Para-diazepine / Propargyl-type 1,3-dipolar organic compound show 16 moreMolecular FrameworkAromatic heteropolycyclic compoundsExternal Descriptorsdiazepine (CHEBI:6931)Affected organisms

UNIIR60L0SM5BCCAS number59467-70-8InChI KeyDDLIGBOFAVUZHB-UHFFFAOYSA-NInChI

InChI=1S/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3

IUPAC Name

12-chloro-9-(2-fluorophenyl)-3-methyl-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene

SMILES

CC1=NC=C2CN=C(C3=CC=CC=C3F)C3=C(C=CC(Cl)=C3)N12

Synthesis ReferenceGeneral References

1. Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. [Article]
2. Isojarvi JI, Tokola RA: Benzodiazepines in the treatment of epilepsy in people with intellectual disability. J Intellect Disabil Res. 1998 Dec;42 Suppl 1:80-92. [Article]
3. Garratt JC, Gent JP, Feely M, Haigh JR: Can benzodiazepines be classified by characterising their anticonvulsant tolerance-inducing potential? Eur J Pharmacol. 1988 Jan 5;145(1):75-80. [Article]
4. Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. [Article]
5. Vermeeren A: Residual effects of hypnotics: epidemiology and clinical implications. CNS Drugs. 2004;18(5):297-328. [Article]
6. Nordt SP, Clark RF: Midazolam: a review of therapeutic uses and toxicity. J Emerg Med. 1997 May-Jun;15(3):357-65. [Article]
7. Jembrek MJ, Vlainic J: GABA Receptors: Pharmacological Potential and Pitfalls. Curr Pharm Des. 2015;21(34):4943-59. [Article]
8. Siegel GJ, Agranoff BW, Albers RW et al. (1999). Basic Neurochemistry: Molecular, Cellular and Medical Aspects (6th ed.). Lippincott Williams.
9. Drug Scheduling: United States Drug Enforcement Administration (DEA) [Link]
10. DailyMed: Midazolam [Link]
11. NAYZILAM® (midazolam) nasal spray - FDA Label [Link]
12. Intravenous Midazolam FDA label [File]
13. MedSafe NZ: Midazolam Inj [File]

Human Metabolome DatabaseHMDB0014821KEGG DrugD00550KEGG CompoundC07524PubChem Compound4192PubChem Substance46507611ChemSpider4047BindingDB213636960ChEBI6931ChEMBLCHEMBL655ZINCZINC000095626706Therapeutic Targets DatabaseDAP000241PharmGKBPA450496Guide to PharmacologyGtP Drug PagePDBe Ligand08JRxListRxList Drug PageDrugs.comDrugs.com Drug PageWikipediaMidazolamPDB Entries3u5k / 5te8FDA labelMSDS

Clinical Trials

Manufacturers

• Apothecon inc div bristol myers squibb
• App pharmaceuticals llc
• Astrazeneca pharmaceuticals lp
• Baxter healthcare corp anesthesia and critical care
• Baxter healthcare corp anesthesia critical care
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Packagers

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• Pharmedium
• Physicians Total Care Inc.
• Ranbaxy Laboratories
• Roxane Labs
• Wockhardt Ltd.

Dosage FormsFormRouteStrengthLiquidIntramuscular; Intravenous1 mg / mLSolutionIntramuscular; Intravenous1 mgSolutionBuccal10 mgSolutionBuccal2.5 mgSolutionBuccal5 mgSolutionBuccal7.5 mgSolutionOral10 MGSolutionOral2.5 MGSolutionOral5 MGSolutionOral7.5 MGSolutionIntramuscular; IntravenousInjection, solutionIntramuscular; Intravenous; RectalInjectionIntravenousInjectionIntramuscular; Intravenous15 MGInjectionIntramuscular; Intravenous5 mg/mlInjectionIntramuscular; Intravenous5 MGInjectionIntramuscular; IntravenousSolutionIntramuscular; Intravenous; Rectal1 mgInjection, solutionParenteralInjectionIntramuscular; Intravenous; Rectal15 MG/3MLSolutionIntramuscular; Intravenous; Rectal5 MG/5MLInjectionIntramuscular; Intravenous; Rectal5 MG/MLTablet, film coatedOral15 mgTabletOral7.5 MGSolutionIntramuscular; Intravenous15 mgInjection, solutionInjectionIntramuscular; Intravenous15 mg/3mlInjection, solutionIntramuscular; Intravenous; Rectal5 mgInjectionIntramuscular; Intravenous1 mg/mLInjection, solutionIntramuscular; IntravenousInjection, solutionIntramuscular; Intravenous10 mg/2mLInjection, solutionIntramuscular; Intravenous2 mg/2mLSolutionParenteral15 mgSolutionIntramuscular; Parenteral15 mgSolutionIntramuscular; Intravenous50 mgSolutionIntravenousTablet, coatedOral7.5 mgTablet, film coatedOral7.5 mgInjection, solutionParenteral; Rectal1 MG/MLInjection, solutionRectal5 MG/MLInjection, solutionIntravenous0.5 mg/1mLInjection, solutionIntravenous1 mg/1mLInjectionIntramuscular; Intravenous1 mg/1mLInjectionIntramuscular; Intravenous10 mg/2mLInjectionIntramuscular; Intravenous2 mg/2mLInjectionIntramuscular; Intravenous5 mg/1mLInjection, solutionIntramuscular; Intravenous1 mg/1mLInjection, solutionIntramuscular; Intravenous5 mg/1mLSyrupOral10 mg/5mLSyrupOral2 mg/1mLInjection, solution5 MG/MLInjection, solutionIntramuscular; Intravenous; Rectal5 MG/MLLiquidIntramuscular; Intravenous5 mg / mLSolutionIntramuscular; Intravenous1 mg / mLSolutionIntramuscular; Intravenous5 mg / mLSolutionIntravenous1 mg / mLSolutionIntravenous5 mgSolutionIntramuscular; Intravenous5 mgInjection, solutionParenteral1 mg/mlSolutionTablet, film coatedOralInjection, solutionIntramuscular; Intravenous; Rectal1 mg/mLInjectionIntravenous1 mg/mlInjectionParenteral1 MG/MLInjection, solutionParenteral2 mg/mlInjectionIntravenous5 mg/mlInjection, solutionParenteral5 mg/mlInjectionParenteral5 MG/MLSolutionIntravenous50 mgInjectionIntramuscular; Intravenous50 mg/10mlInjectionInjection, solutionIntravenous5 mgTrocheSublingualInjection, solutionIntramuscular10 mg/0.7mLSprayNasal5 mg/0.1mLSolutionOral2 MG/MLSolutionOralSolutionIntramuscular; Intravenous; RectalInjection, solutionIntramuscular5 mg/1mLSolutionIntramuscular; Intravenous; Rectal5 mg/mLSolutionIntramuscular; Intravenous; Rectal1 mg/mLPricesUnit descriptionCostUnitMidazolam 5 mg/ml3.9USDmlMidazolam-nacl 2 mg/ml inj2.31USDmlMidazolam hcl 5 mg/ml vial1.18USDmlMidazolam-nacl 1 mg/ml inj1.13USDmlMidazolam hcl 2 mg/ml syrup1.08USDmlMidazolam 1 mg/ml isecure syr0.73USDmlMidazolam hcl 1 mg/ml vial0.26USDml

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PatentsPatent NumberPediatric ExtensionApprovedExpires (estimated)RegionUS9289432No2016-03-222028-01-18USUS9687495No2017-06-272028-01-18USUS8217033No2012-07-102028-01-18USUS8809322No2014-08-192028-01-18USUS10966990No2021-04-062038-06-20US

StateSolidExperimental PropertiesPropertyValueSourcemelting point (°C)161-164MSDSboiling point (°C)497MSDSwater solubilitysolubleFDA labelPredicted PropertiesPredicted ADMET FeaturesPropertyValueProbabilityHuman Intestinal Absorption+1.0Blood Brain Barrier+0.9724Caco-2 permeable+0.8866P-glycoprotein substrateNon-substrate0.5074P-glycoprotein inhibitor IInhibitor0.5587P-glycoprotein inhibitor IIInhibitor0.8388Renal organic cation transporterInhibitor0.7476CYP450 2C9 substrateNon-substrate0.7366CYP450 2D6 substrateNon-substrate0.9116CYP450 3A4 substrateSubstrate0.7194CYP450 1A2 substrateInhibitor0.8586CYP450 2C9 inhibitorInhibitor0.7132CYP450 2D6 inhibitorNon-inhibitor0.6887CYP450 2C19 inhibitorInhibitor0.6554CYP450 3A4 inhibitorNon-inhibitor0.5214CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9001Ames testNon AMES toxic0.8024CarcinogenicityNon-carcinogens0.7703BiodegradationNot ready biodegradable1.0Rat acute toxicity3.1488 LD50, mol/kgNot applicablehERG inhibition (predictor I)Weak inhibitor0.9827hERG inhibition (predictor II)Non-inhibitor0.7379

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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