Chemical: Drug
midazolam

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PharmGKB has no annotated drug labels with pharmacogenomic information for this . If you know of a drug label with PGx, send us a message.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for midazolam

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP3A4 *1 N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *22 N/A N/A N/A
No VIP available CA VA CYP3A5 *1A N/A N/A N/A
No VIP available CA VA CYP3A5 *3A N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1045642 NC_000007.13:g.87138645A>G, NC_000007.14:g.87509329A>G, NG_011513.1:g.208920T>C, NM_000927.4:c.3435T>C, NP_000918.2:p.Ile1145=, rs10239679, rs11568726, rs117328163, rs17210003, rs2229108, rs386513066, rs60023214, rs9690664
A > G
SNP
I1145I
No VIP available CA VA
rs1057868 NC_000007.13:g.75615006C>T, NC_000007.14:g.75985688C>T, NG_008930.1:g.75587C>T, NM_000941.2:c.1508C>T, NP_000932.3:p.Ala503Val, NW_003871064.1:g.3514924C>T, XM_005250459.1:c.1508C>T, XM_005250460.1:c.1205C>T, XM_005250461.1:c.932C>T, XM_005277600.1:c.1508C>T, XM_005277601.1:c.1205C>T, XM_005277602.1:c.932C>T, XP_005250516.1:p.Ala503Val, XP_005250517.1:p.Ala402Val, XP_005250518.1:p.Ala311Val, XP_005277657.1:p.Ala503Val, XP_005277658.1:p.Ala402Val, XP_005277659.1:p.Ala311Val, rs17840495, rs17846082, rs17859083, rs3198400, rs57699079
C > T
SNP
A503V
No VIP available CA VA
rs11568820 NC_000012.11:g.48302545C>T, NC_000012.12:g.47908762C>T, NG_008731.1:g.1270G>A, rs17883968, rs56977367, rs60432410
C > T
SNP
No VIP available No Clinical Annotations available VA
rs12721613 NC_000003.11:g.119526176C>T, NC_000003.12:g.119807329C>T, NG_011856.1:g.31846C>T, NM_003889.3:c.79C>T, NM_022002.2:c.196C>T, NM_033013.2:c.79C>T, NP_003880.3:p.Pro27Ser, NP_071285.1:p.Pro66Ser, NP_148934.1:p.Pro27Ser, XM_005247866.1:c.-87C>T, rs45456591, rs56553122, rs58844532, rs61151865
C > T
SNP
P27S
No VIP available CA VA
rs12721627 NC_000007.13:g.99366093G>C, NC_000007.14:g.99768470G>C, NG_008421.1:g.20716C>G, NM_001202855.2:c.554C>G, NM_017460.5:c.554C>G, NP_001189784.1:p.Thr185Ser, NP_059488.2:p.Thr185Ser, XM_011515841.1:c.554C>G, XM_011515842.1:c.554C>G, XP_011514143.1:p.Thr185Ser, XP_011514144.1:p.Thr185Ser, rs28371754, rs56915287
G > C
SNP
T185S
No VIP available No Clinical Annotations available VA
rs1464602 NC_000003.11:g.119526372G>A, NC_000003.12:g.119807525G>A, NG_011856.1:g.32042G>A, NM_003889.3:c.197+78G>A, NM_022002.2:c.314+78G>A, NM_033013.2:c.197+78G>A, XM_005247866.1:c.32+78G>A
G > A
SNP
No VIP available No Clinical Annotations available VA
rs1464603 NC_000003.11:g.119526349G>A, NC_000003.12:g.119807502G>A, NG_011856.1:g.32019G>A, NM_003889.3:c.197+55G>A, NM_022002.2:c.314+55G>A, NM_033013.2:c.197+55G>A, XM_005247866.1:c.32+55G>A
G > A
SNP
No VIP available CA VA
rs1544410 NC_000012.11:g.48239835C>T, NC_000012.12:g.47846052C>T, NG_008731.1:g.63980G>A, NM_000376.2:c.1024+283G>A, NM_001017535.1:c.1024+283G>A, NM_001017536.1:c.1174+283G>A, XM_006719587.2:c.1024+283G>A, XM_011538720.1:c.1024+283G>A, XR_944903.1:n.-763C>T, rs386536760, rs56495123, rs56911380
C > T
SNP
No VIP available No Clinical Annotations available VA
rs2740574 NC_000007.13:g.99382096C>T, NC_000007.14:g.99784473C>T, NG_008421.1:g.4713G>A, NM_001202855.2:c.-392G>A, NM_017460.5:c.-392G>A, XM_011515841.1:c.-392G>A, XM_011515842.1:c.-392G>A, rs3176920, rs36231114, rs59393892
C > T
SNP
No VIP available CA VA
rs35599367 NC_000007.13:g.99366316G>A, NC_000007.14:g.99768693G>A, NG_008421.1:g.20493C>T, NM_001202855.2:c.522-191C>T, NM_017460.5:c.522-191C>T, XM_011515841.1:c.522-191C>T, XM_011515842.1:c.522-191C>T, rs45581939, rs62471940
G > A
SNP
No VIP available CA VA
rs4516035 NC_000012.11:g.48299826T>C, NC_000012.12:g.47906043T>C, NG_008731.1:g.3989A>G, NM_000376.2:c.-1172A>G, NM_001017535.1:c.-1294A>G, NM_001017536.1:c.-1413A>G, XM_006719587.2:c.-1091A>G, XM_011538720.1:c.-1213A>G, rs17396597, rs17882742, rs58063668
T > C
SNP
rs776746 NC_000007.13:g.99270539C>T, NC_000007.14:g.99672916T>C, NG_007938.1:g.12083G=, NG_007938.1:g.12083G>A, NM_000777.4:c.219-237A>G, NM_000777.4:c.219-237G>A, NM_001190484.2:c.219-237A>G, NM_001190484.2:c.219-237G>A, NM_001291829.1:c.-253-1A>G, NM_001291829.1:c.-253-1G>A, NM_001291830.1:c.189-237A>G, NM_001291830.1:c.189-237G>A, NR_033807.2:n.717-1A>G, NR_033807.2:n.717-1G>A, NR_033808.1:n.689-1G>A, NR_033809.1:n.581-237G>A, NR_033810.1:n.689-1G>A, NR_033811.1:n.321-1G>A, NR_033812.1:n.321-1G>A, XM_005250169.1:c.189-237G>A, XM_005250170.1:c.-357-1G>A, XM_005250171.1:c.-253-1G>A, XM_005250172.1:c.-254G>A, XM_005250173.1:c.-331-237G>A, XM_005250198.1:c.806-4288C>T, XM_006715859.2:c.219-237A>G, XM_011515843.1:c.-254A>G, XM_011515844.1:c.-229-237A>G, XM_011515845.1:c.-463-1A>G, XM_011515846.1:c.-331-237A>G, XM_011515847.1:c.-571-1A>G, XR_927383.1:n.344-237A>G, XR_927402.1:n.1466+48736T>C, rs10361242, rs11266830, rs386613022, rs58244770
C > T
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Dea No. 2884
  • Midazolam Base
  • Midazolam Hcl
  • Midazolamum [INN-Latin]
Trade Names
  • Dormicum
  • Versed
Brand Mixture Names

PharmGKB Accession Id

PA450496

Type(s):

Drug

Description

A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH. PubChem Midazolam is a schedule IV drug in the United States.

Source: Drug Bank

Indication

For use as a sedative perioperatively.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

It is thought that 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 brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines bind to the benzodiazepine site on GABA-A receptors, which potentiates the effects of GABA by increasing the frequency of chloride channel opening.

Source: Drug Bank

Pharmacology

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 (gamma)-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.

Source: Drug Bank

Food Interaction

Grapefruit juice slows the product's absorption and significantly increases its bioavailability.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, (alpha)-hydroxymidazolam, and 4-hydroxymidazolam.

Source: Drug Bank

Protein Binding

97%

Source: Drug Bank

Absorption

Rapidly absorbed after oral administration (absolute bioavailability of the midazolam syrup in pediatric patients is about 36%, and intramuscular is greater than 90%).

Source: Drug Bank

Half-Life

2.2-6.8 hours

Source: Drug Bank

Toxicity

LD 50=825 mg/kg (Orally in rats). Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs.

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, alpha-hydroxymidazolam, followed by glucuronidation of the alpha-hydroxyl metabolite which is present in unconjugated and conjugated forms in human plasma. The alpha- hydroxymidazolam glucuronide is then excreted in urine. No significant amount of parent drug or metabolites is extractable from urine before beta-glucuronidase and sulfatase deconjugation, indicating that the urinary metabolites are excreted mainly as conjugates.

Source: Drug Bank

Volume of Distribution

Chemical Properties

Chemical Formula

C18H13ClFN3

Source: Drug Bank

Isomeric SMILES

Cc1ncc2n1-c3ccc(cc3C(=NC2)c4ccccc4F)Cl

Source: OpenEye

Canonical SMILES

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

Source: Drug Bank

Average Molecular Weight

325.767

Source: Drug Bank

Monoisotopic Molecular Weight

325.078203343

Source: Drug Bank

SMILES

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

Source: Drug Bank

InChI String

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

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
GABRA1 (source: Drug Bank)
GABRA2 (source: Drug Bank)
GABRA3 (source: Drug Bank)
GABRA4 (source: Drug Bank)
GABRA5 (source: Drug Bank)
GABRA6 (source: Drug Bank)
GABRB1 (source: Drug Bank)
GABRB2 (source: Drug Bank)
GABRB3 (source: Drug Bank)
GABRD (source: Drug Bank)
GABRE (source: Drug Bank)
GABRG1 (source: Drug Bank)
GABRG2 (source: Drug Bank)
GABRG3 (source: Drug Bank)
GABRP (source: Drug Bank)
GABRQ (source: Drug Bank)
GABRR1 (source: Drug Bank)
GABRR2 (source: Drug Bank)
GABRR3 (source: Drug Bank)

Drug Interactions

Interaction Description
amprenavir - midazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
amprenavir - midazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
aprepitant - midazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
atazanavir - midazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
atazanavir - midazolam Increases the effect and toxicity of benzodiazepine (source: Drug Bank)
carbamazepine - midazolam Reduces the effect of the benzodiazepine (source: Drug Bank)
carbamazepine - midazolam Reduces the effect of the benzodiazepine (source: Drug Bank)
cimetidine - midazolam Increases the effect of the benzodiazepine (source: Drug Bank)
cimetidine - midazolam Increases the effect of the benzodiazepine (source: Drug Bank)
clarithromycin - midazolam The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
clarithromycin - midazolam The macrolide increases the effect of the benzodiazepine (source: Drug Bank)
clozapine - midazolam Increased risk of toxicity (source: Drug Bank)
clozapine - midazolam Increased risk of toxicity (source: Drug Bank)
delavirdine - midazolam The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
delavirdine - midazolam The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
diltiazem - midazolam The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
diltiazem - midazolam The calcium channel blocker increases the effect and toxicity of the benzodiazepine (source: Drug Bank)
docetaxel - midazolam The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
docetaxel - midazolam Midazolam may increase the serum levels and toxicity of docetaxel. (source: Drug Bank)
erythromycin - midazolam The macrolide increases the efect of the benzodiazepine (source: Drug Bank)
erythromycin - midazolam The macrolide increases the efect of the benzodiazepine (source: Drug Bank)
fluconazole - midazolam Increases the effect of the benzodiazepine (source: Drug Bank)
fluconazole - midazolam Increases the effect of the benzodiazepine (source: Drug Bank)
fosamprenavir - midazolam Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
fosamprenavir - midazolam Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
fosphenytoin - midazolam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
indinavir - midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
indinavir - midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
itraconazole - midazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
itraconazole - midazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
ketoconazole - midazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
ketoconazole - midazolam The imidazole increases the effect of the benzodiazepine (source: Drug Bank)
midazolam - amprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - amprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - aprepitant Aprepitant increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - atazanavir Atazanavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - atazanavir Atazanavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - carbamazepine Carbamazepine reduces the effect of the benzodiazepine (source: Drug Bank)
midazolam - carbamazepine Carbamazepine reduces the effect of the benzodiazepine (source: Drug Bank)
midazolam - cimetidine Cimetidine increases the effect of benzodiazepine (source: Drug Bank)
midazolam - cimetidine Cimetidine increases the effect of benzodiazepine (source: Drug Bank)
midazolam - clarithromycin The macrolide increases the effect of benzodiazepine (source: Drug Bank)
midazolam - clarithromycin The macrolide increases the effect of benzodiazepine (source: Drug Bank)
midazolam - clozapine Increased risk of toxicity (source: Drug Bank)
midazolam - clozapine Increased risk of toxicity (source: Drug Bank)
midazolam - delavirdine The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - delavirdine The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - diltiazem The calcium channel blocker increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - diltiazem The calcium channel blocker increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - docetaxel The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
midazolam - docetaxel Midazolam may increase the serum levels and toxicity of docetaxel. (source: Drug Bank)
midazolam - efavirenz The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - efavirenz The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - erythromycin The macrolide increases the effect of benzodiazepine (source: Drug Bank)
midazolam - erythromycin The macrolide increases the effect of benzodiazepine (source: Drug Bank)
midazolam - ethotoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
midazolam - fluconazole Fluconazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - fluconazole Fluconazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - fosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
midazolam - indinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - indinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - itraconazole The imidazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - itraconazole The imidazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - josamycin The macrolide increases the effect of benzodiazepine (source: Drug Bank)
midazolam - ketoconazole The imidazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - ketoconazole The imidazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
midazolam - mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
midazolam - nelfinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - nelfinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - omeprazole Omeprazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - omeprazole Omeprazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
midazolam - phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
midazolam - quinupristin This combination presents an increased risk of toxicity (source: Drug Bank)
midazolam - rifampin Rifampin increases the effect of benzodiazepine (source: Drug Bank)
midazolam - rifampin Rifampin increases the effect of benzodiazepine (source: Drug Bank)
midazolam - ritonavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - ritonavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - saquinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - saquinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
midazolam - telithromycin Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank)
midazolam - verapamil The calcium channel blocker increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - verapamil The calcium channel blocker increases the effect and toxicity of benzodiazepine (source: Drug Bank)
midazolam - voriconazole The imidazole increases the effect of benzodiazepine (source: Drug Bank)
midazolam - voriconazole The imidazole increases the effect of benzodiazepine (source: Drug Bank)
nelfinavir - midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir - midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
omeprazole - midazolam Omeprazole increases the effect of benzodiazepine (source: Drug Bank)
omeprazole - midazolam Omeprazole increases the effect of benzodiazepine (source: Drug Bank)
phenytoin - midazolam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
phenytoin - midazolam Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank)
quinupristin - midazolam This combination presents an increased risk of toxicity (source: Drug Bank)
rifampin - midazolam Rifampin decreases the effect of benzodiazepine (source: Drug Bank)
rifampin - midazolam Rifampin decreases the effect of benzodiazepine (source: Drug Bank)
telithromycin - midazolam Telithromycin increases the effect/toxicity of the benzodiazepine (source: Drug Bank)
telithromycin - midazolam Telithromycin may reduce clearance of Midazolam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Midazolam if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
tipranavir - midazolam Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Midazolam. Concomitant therapy is contraindicated. (source: Drug Bank)
triprolidine - midazolam The CNS depressants, Triprolidine and Midazolam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
triprolidine - midazolam The CNS depressants, Triprolidine and Midazolam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
verapamil - midazolam Verapamil may increase the serum concentration of Midazolam by decreasing its metabolism. Avoid concomitant therapy if possible or consider a dose reduction in the initial dose of Midazolam. (source: Drug Bank)
voriconazole - midazolam Voriconazole may increase the serum concentration of midazolam by decreasing its metabolism. Monitor for midazolam toxicity if voriconazole is initiated or dose increased. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to midazolam: 61

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Variability in Expression of CYP3A5 in Human Fetal Liver. Drug metabolism and disposition: the biological fate of chemicals. 2015. Vyhlidal Carrie A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Progressive decline in tacrolimus clearance after renal transplantation is partially explained by decreasing CYP3A4 activity and increasing hematocrit. British journal of clinical pharmacology. 2015. de Jonge Hylke, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Impact of visceral leishmaniasis and curative chemotherapy on cytochrome P450 activity in Brazilian patients. British journal of clinical pharmacology. 2015. Lanchote Vera Lucia, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Ritonavir is the best alternative to ketoconazole as an index inhibitor of cytochrome P450-3A in drug-drug interaction studies. British journal of clinical pharmacology. 2015. Greenblatt David J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Neurotoxicity of generic anesthesia agents in infants and children: an orphan research question in search of a sponsor. JAMA. 2015. Psaty Bruce M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Midazolam microdose to determine systemic and pre-systemic metabolic CYP3A activity in humans. British journal of clinical pharmacology. 2015. Hohmann Nicolas, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The CYP3A4*22 C>T single nucleotide polymorphism is associated with reduced midazolam and tacrolimus clearance in stable renal allograft recipients. The pharmacogenomics journal. 2014. de Jonge H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Evaluation of felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions. European journal of clinical pharmacology. 2014. Snyder Ben D, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP3A5*3 and bilirubin predict midazolam population pharmacokinetics in Asian cancer patients. Journal of clinical pharmacology. 2013. Seng Kok-Yong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effect of CYP3A5 Expression on the Inhibition of CYP3A-Catalyzed Drug Metabolism: Impact on CYP3A-Mediated Drug-Drug Interactions. Drug metabolism and disposition: the biological fate of chemicals. 2013. Shirasaka Yoshiyuki, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effect of the CYP3A inhibitor ketoconazole on the PXR-mediated induction of CYP3A activity. European journal of clinical pharmacology. 2013. Fuchs Ines, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of POR*28 on the clinical pharmacokinetics of CYP3A phenotyping probes midazolam and erythromycin. Pharmacogenetics and genomics. 2013. Elens Laure, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP3A4 intron 6 C>T SNP (CYP3A4*22) encodes lower CYP3A4 activity in cancer patients, as measured with probes midazolam and erythromycin. Pharmacogenomics. 2013. Elens Laure, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of P450 oxidoreductase: implications in drug metabolism and therapy. Pharmacogenetics and genomics. 2012. Hu Lei, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Sulforaphane is not an effective antagonist of the human pregnane X-receptor in vivo. Toxicology and applied pharmacology. 2012. Poulton Emma Jane, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Intestinal CYP3A4 and midazolam disposition in vivo associate with VDR polymorphisms and show seasonal variation. Biochemical pharmacology. 2012. Thirumaran Ranjit K, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition. Pharmacological reviews. 2012. Michaud Veronique, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Complex Drug Interactions of HIV Protease Inhibitors 1: Inactivation, Induction and Inhibition of Cytochrome P450 3A by Ritonavir or Nelfinavir. Drug metabolism and disposition: the biological fate of chemicals. 2011. Kirby Brian J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Induction of CYP3A4 by vinblastine: Role of the nuclear receptor NR1I2. The Annals of pharmacotherapy. 2010. Smith Nicola F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Substrate-specific modulation of CYP3A4 activity by genetic variants of cytochrome P450 oxidoreductase. Pharmacogenetics and genomics. 2010. Agrawal Vishal, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP2B6. Pharmacogenetics and genomics. 2010. Thorn Caroline F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
A Phenotype-Genotype Approach to Predicting CYP450 and P-Glycoprotein Drug Interactions With the Mixed Inhibitor/Inducer Tipranavir/Ritonavir. Clinical pharmacology and therapeutics. 2010. Dumond J B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clinical pharmacology and therapeutics. 2010. Mathias A A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Individualizing dosing of irinotecan. Clinical cancer research : an official journal of the American Association for Cancer Research. 2010. Ratain Mark J, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The P450 oxidoreductase genotype is associated with CYP3A activity in vivo as measured by the midazolam phenotyping test. Pharmacogenetics and genomics. 2009. Oneda Beatrice, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Association of genotypes of the CYP3A cluster with midazolam disposition in vivo. The pharmacogenomics journal. 2009. Miao J, et al. PubMed
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Functional characterization of CYP3A4.16: catalytic activities toward midazolam and carbamazepine. Xenobiotica; the fate of foreign compounds in biological systems. 2009. Maekawa K, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Benzodiazepine metabolism: an analytical perspective. Current drug metabolism. 2008. Mandrioli Roberto, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacokinetics/genotype associations for major cytochrome P450 enzymes in native and first- and third-generation Japanese populations: comparison with Korean, Chinese, and Caucasian populations. Clinical pharmacology and therapeutics. 2008. Myrand S P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of pregnancy on CYP3A and P-glycoprotein activities as measured by disposition of midazolam and digoxin: a University of Washington specialized center of research study. Clinical pharmacology and therapeutics. 2008. Hebert M F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Contribution of the N-glucuronidation pathway to the overall in vitro metabolic clearance of midazolam in humans. Drug metabolism and disposition: the biological fate of chemicals. 2008. Klieber Sylvie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Prediction of pharmacokinetic drug-drug interactions using human hepatocyte suspension in plasma and cytochrome P450 phenotypic data. II. In vitro-in vivo correlation with ketoconazole. Drug metabolism and disposition: the biological fate of chemicals. 2008. Lu Chuang, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Influence of CYP3A5 genotype on the pharmacokinetics and pharmacodynamics of the cytochrome P4503A probes alfentanil and midazolam. Clinical pharmacology and therapeutics. 2007. Kharasch E D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of daily ingestion of cranberry juice on the pharmacokinetics of warfarin, tizanidine, and midazolam--probes of CYP2C9, CYP1A2, and CYP3A4. Clinical pharmacology and therapeutics. 2007. Lilja J J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Development of the "Inje cocktail" for high-throughput evaluation of five human cytochrome P450 isoforms in vivo. Clinical pharmacology and therapeutics. 2007. Ryu J Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ABCB1 and cytochrome P450 genotypes and phenotypes: influence on methadone plasma levels and response to treatment. Clinical pharmacology and therapeutics. 2006. Crettol Séverine, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Sex differences in CYP3A activity using intravenous and oral midazolam. Clinical pharmacology and therapeutics. 2006. Chen Maylee, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Human pregnane X receptor: genetic polymorphisms, alternative mRNA splice variants, and cytochrome P450 3A metabolic activity. Journal of clinical pharmacology. 2006. He Ping, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Low hepatic cytochrome P450 3A activity is a risk for corticosteroid-induced osteonecrosis. Clinical pharmacology and therapeutics. 2006. Kaneshiro Yasunori, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Factors influencing midazolam hydroxylation activity in human liver microsomes. Drug metabolism and disposition: the biological fate of chemicals. 2006. He Ping, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genotype-phenotype associations of cytochrome P450 3A4 and 3A5 polymorphism with midazolam clearance in vivo. Clinical pharmacology and therapeutics. 2005. He Ping, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The benzodiazepine site of the GABAA receptor: an old target with new potential?. Sleep medicine. 2004. Bateson Alan N. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genotype-phenotype associations for common CYP3A4 and CYP3A5 variants in the basal and induced metabolism of midazolam in European- and African-American men and women. Pharmacogenetics. 2003. Floyd Michael D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug metabolism and disposition: the biological fate of chemicals. 2003. Patki Kiran C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Human extrahepatic cytochromes P450: function in xenobiotic metabolism and tissue-selective chemical toxicity in the respiratory and gastrointestinal tracts. Annual review of pharmacology and toxicology. 2003. Ding Xinxin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The role of peripheral benzodiazepine receptors (PBRs) in CNS pathophysiology. Current medicinal chemistry. 2002. Lang Senyang. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mapping of the benzodiazepine recognition site on GABA(A) receptors. Current topics in medicinal chemistry. 2002. Sigel Erwin. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Co-regulation of CYP3A4 and CYP3A5 and contribution to hepatic and intestinal midazolam metabolism. Molecular pharmacology. 2002. Lin Yvonne S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
New insights into the role of the GABA(A)-benzodiazepine receptor in psychiatric disorder. The British journal of psychiatry : the journal of mental science. 2001. Nutt D J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants. Pharmacogenetics. 2001. Zhang J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression. Nature genetics. 2001. Kuehl P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Two linked mutations in transcriptional regulatory elements of the CYP3A5 gene constitute the major genetic determinant of polymorphic activity in humans. Pharmacogenetics. 2000. Paulussen A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica; the fate of foreign compounds in biological systems. 1998. Tassaneeyakul W, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The benzodiazepine binding site of GABAA receptors. Trends in pharmacological sciences. 1997. Sigel E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Benzodiazepines, anxiety and immunity. Pharmacology & therapeutics. 1997. Zavala F. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Expression of enzymatically active CYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of 1alpha,25-dihydroxyvitamin D3. Molecular pharmacology. 1997. Schmiedlin-Ren P, et al. PubMed
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O-demethylation of epipodophyllotoxins is catalyzed by human cytochrome P450 3A4. Molecular pharmacology. 1994. Relling M V, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0574-0150-04
DrugBank:
DB00683
KEGG Compound:
C07524
KEGG Drug:
D00550
PubChem Compound:
4192
PubChem Substance:
183492
46507611
Drugs Product Database (DPD):
2240286
BindingDB:
21363
ChemSpider:
4047
Therapeutic Targets Database:
DAP000241
FDA Drug Label at DailyMed:
0be63f63-6a93-4782-8f9c-d13ca5ae44bd

Clinical Trials

These are trials that mention midazolam and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, PubChem.