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Identification
NameMagnesium Sulfate
Accession NumberDB00653  (APRD01080)
Typesmall molecule
Groupsapproved
Description

A small colorless crystal used as an anticonvulsant, a cathartic, and an electrolyte replenisher in the treatment of pre-eclampsia and eclampsia. It causes direct inhibition of action potentials in myometrial muscle cells. Excitation and contraction are uncoupled, which decreases the frequency and force of contractions. (From AMA Drug Evaluations Annual, 1992, p1083)

Structure
Thumb
Synonyms
SynonymLanguageCode
Magnesium sulphateNot AvailableNot Available
SaltsNot Available
Brand namesNot Available
Brand mixturesNot Available
Categories
CAS number7487-88-9
WeightAverage: 120.368
Monoisotopic: 119.936771076
Chemical FormulaMgO4S
InChI KeyCSNNHWWHGAXBCP-UHFFFAOYSA-L
InChI
InChI=1S/Mg.H2O4S/c;1-5(2,3)4/h;(H2,1,2,3,4)/q+2;/p-2
IUPAC Name
magnesium(2+) ion sulfate
SMILES
[Mg++].[O-]S([O-])(=O)=O
Mass SpecNot Available
Taxonomy
KingdomInorganic Compounds
SuperclassMixed Metal/Non-metal Compounds
ClassAlkaline Earth Metal Oxoanionic Compounds
SubclassAlkaline Earth Metal Sulfates
Direct parentAlkaline Earth Metal Sulfates
Alternative parentsOrganic Sulfuric Acids and Derivatives
Substituentssulfuric acid derivative
Classification descriptionThis compound belongs to the alkaline earth metal sulfates. These are inorganic compounds in which the largest oxoanion is sulfate, and in which the heaviest atom not in an oxoanion is an alkaline earth metal.
Pharmacology
IndicationUsed for immediate control of life-threatening convulsions in the treatment of severe toxemias (pre-eclampsia and eclampsia) of pregnancy and in the treatment of acute nephritis in children. Also indicated for replacement therapy in magnesium deficiency, especially in acute hypomagnesemia accompanied by signs of tetany similar to those of hypocalcemia. Also used in uterine tetany as a myometriat relaxant.
PharmacodynamicsMagnesium sulfate is a small colorless crystal used as an anticonvulsant, a cathartic, and an electrolyte replenisher in the treatment of pre-eclampsia and eclampsia. It causes direct inhibition of action potentials in myometrial muscle cells. Excitation and contraction are uncoupled, which decreases the frequency and force of contractions. Magnesium sulfate is gaining popularity as an initial treatment in the management of various dysrhythmias, particularly torsades de pointes, and dyrhythmias secondary to TCA overdose or digitalis toxicity.
Mechanism of actionMagnesium is the second most plentiful cation of the intracellular fluids. It is essential for the activity of many enzyme systems and plays an important role with regard to neurochemical transmission and muscular excitability. Magnesium sulfate reduces striated muscle contractions and blocks peripheral neuromuscular transmission by reducing acetylcholine release at the myoneural junction. Additionally, Magnesium inhibits Ca2+ influx through dihydropyridine-sensitive, voltage-dependent channels. This accounts for much of its relaxant action on vascular smooth muscle.
AbsorptionNot Available
Volume of distributionNot Available
Protein binding25-30%
Metabolism

None

Route of eliminationMagnesium is excreted solely by the kidney at a rate proportional to the serum concentration and glomerular filtration.
Half life43.2 hours (for newborns)
ClearanceNot Available
ToxicityLD50 = 1200 mg/kg (rat, subcutaneous). May be harmful if swallowed. May act as an irritant. Adverse reactions include hypotension, ECG changes, diarrhea, urinary retention, CNS depression and respiratory depression.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.7487
Blood Brain Barrier + 0.9646
Caco-2 permeable - 0.6267
P-glycoprotein substrate Non-substrate 0.9137
P-glycoprotein inhibitor I Non-inhibitor 0.9194
P-glycoprotein inhibitor II Non-inhibitor 0.9904
Renal organic cation transporter Non-inhibitor 0.9521
CYP450 2C9 substrate Non-substrate 0.8775
CYP450 2D6 substrate Non-substrate 0.8213
CYP450 3A4 substrate Non-substrate 0.7007
CYP450 1A2 substrate Non-inhibitor 0.7767
CYP450 2C9 substrate Non-inhibitor 0.7602
CYP450 2D6 substrate Non-inhibitor 0.9115
CYP450 2C19 substrate Non-inhibitor 0.7547
CYP450 3A4 substrate Non-inhibitor 0.9759
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9577
Ames test Non AMES toxic 0.5773
Carcinogenicity Carcinogens 0.8111
Biodegradation Ready biodegradable 0.943
Rat acute toxicity 2.4160 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.7988
hERG inhibition (predictor II) Non-inhibitor 0.9446
Pharmacoeconomics
Manufacturers
  • Abraxis pharmaceutical products
  • Hospira inc
Packagers
Dosage forms
FormRouteStrength
LiquidIntramuscular
LiquidIntravenous
LiquidOral
PelletOral
PowderOral
SolutionIntramuscular
SolutionIntravenous
Solution / dropsOral
Prices
Unit descriptionCostUnit
Elliotts b solution ampule4.71USDml
Magnesium Sulfate 50% Solution 2ml Vial0.92USDvial
Magnesium sulfate powder0.29USDg
Magnesium-ns 6 g/50 ml bag0.29USDml
Magnesium-ns 4 g/50 ml bag0.27USDml
Magnesium-ns 3 g/50 ml bag0.26USDml
Magnesium sulfate-ns 2 gm bag0.25USDml
Magnesium sulfate-ns 1 gm bag0.24USDml
Magnesium-d5w 1 gm/100 ml soln0.07USDml
Magnesium-lr 20 g/500 ml0.03USDml
Magnesium-lr 40 g/500 ml bag0.03USDml
Magnesium-lr 50 g/500 ml bag0.02USDml
Epsom salt 100% powder0.01USDg
Magnesium sulf 4% iv soln0.01USDml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point1124 °C (decomposition)Not Available
water solubility710 mg/mLNot Available
logP-0.91Not Available
Predicted Properties
PropertyValueSource
logP-0.84ChemAxon
pKa (strongest acidic)-3ChemAxon
physiological charge-2ChemAxon
hydrogen acceptor count4ChemAxon
hydrogen donor count0ChemAxon
polar surface area80.26ChemAxon
rotatable bond count0ChemAxon
refractivity11.53ChemAxon
polarizability5.81ChemAxon
number of rings0ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterNoChemAxon
Veber's ruleNoChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Shinichi Yamamoto, Akifumi Sekitani, “BASIC MAGNESIUM SULFATE GRANULE, AND PROCESS FOR PRODUCTION THEREOF.” U.S. Patent US20110042297, issued February 24, 2011.

US20110042297
General Reference
  1. Blitz M, Blitz S, Hughes R, Diner B, Beasley R, Knopp J, Rowe BH: Aerosolized magnesium sulfate for acute asthma: a systematic review. Chest. 2005 Jul;128(1):337-44. Pubmed
  2. Yokoyama K, Takahashi N, Yada Y. Prolonged maternal magnesium administration and bone metabolism in neonates. Early Hum Dev. 2010;86(3):187-91. Epub 2010 Mar 12.
  3. Wedig KE, Kogan J, Schorry EK et al. Skeletal demineralization and fractures caused by fetal magnesium toxicity. J Perinatol. 2006; 26(6):371-4.
  4. Nassar AH, Sakhel K, Maarouf H, et al. Adverse maternal and neonatal outcome of prolonged course of Magnesium Sulfate tocolysis. Acta Obstet Gynecol Scan. 2006;85(9):1099-103.
  5. Malaeb SN, Rassi A, Haddad MC. Bone mineralization in newborns whose mothers received magnesium sulphate for tocolysis of premature labor. Pediatr Radiol. 2004;34(5):384-6. Epub 2004 Feb 18.
  6. Matsuda Y, Maeda Y, Ito M, et al. Effect of Magnesium Sulfate treatment on neonatal bone abnormalities. Gynecol Obstet Invest. 1997;44(2):82-8.
  7. Schanler RJ, Smith LG, Burns PA. Effects of long-term maternal intravenous Magnesium Sulfate therapy on neonatal calcium metabolism and bone mineral content. Gynecol Obstet Invest. 1997;43(4):236-41.
  8. Santi MD, Henry GW, Douglas GL. Magnesium Sulfate treatment of preterm labor as a cause of abnormal neonatal bone mineralization. J Pediatr Orthop. 1994;14(2):249-53.
  9. Holcomb WL, Shackelford GD, Petrie RH. Magnesium tocolysis and neonatal bone abnormalities: a controlled study. Obstet Gynecol. 1991; 78(4):611-4.
  10. Cumming WA, Thomas VJ. Hypermagnesemia: a cause of abnormal metaphyses in the neonate. Am J Roentgenol. 1989; 152(5):1071-2.
  11. Lamm CL, Norton KL, Murphy RJ. Congenital rickets associated with Magnesium Sulfate infusion for tocolysis. J Pediatr. 1988; 113(6):1078-82.
  12. McGuinness GA, Weinstein MM, Cruikshank DP, et al. Effects of Magnesium Sulfate treatment on perinatal calcium metabolism. II. Neonatal responses. Obstet Gynecol. 1980;56(5): 595-600.
  13. Riaz M, Porat R, Brodsky NL, et al. The effects of maternal Magnesium Sulfate treatment on newborns: a prospective controlled study. J Perinatol. 1998;18(6 pt 1):449-54.
External Links
ResourceLink
KEGG DrugD01108
PubChem Compound24083
PubChem Substance46508411
ChemSpider23226
ChEBI32599
ChEMBLCHEMBL1200456
Therapeutic Targets DatabaseDAP000201
PharmGKBPA450302
Drug Product Database602264
RxListhttp://www.rxlist.com/cgi/generic3/mgso4.htm
Drugs.comhttp://www.drugs.com/cdi/magnesium-sulfate.html
WikipediaMagnesium_Sulfate
ATC CodesA06AD04A12CC02B05XA05D11AX05V04CC02
AHFS Codes
  • 84:92.00
  • 56:12.00
  • 40:12.00
  • 28:12.92
  • 92:02.00*
PDB EntriesNot Available
FDA labelNot Available
MSDSshow(72.1 KB)
Interactions
Drug Interactions
Drug
AtazanavirThis gastric pH modifier decreases the levels/effects of atazanavir
DihydrocodeineMay enhance CNS depressant effects of CNS depressants. It is recommended to monitor therapy.
EltrombopagLevels of eltrombopag are decreased due to GI inhibition. Separate administration by at least 4 hours.
TiludronateThe divalent cation of oral Magnesium sulfate may significantly decrease the absorption of Tiludronate by forming a nonabsorbable chelate. Oral dosing should be separated by at least 2 hours.
TriprolidineThe CNS depressants, Triprolidine and Magnesium sulfate, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
TrovafloxacinMagnesium may decrease the absorption of orally administered Trovafloxacin. Administer Trovafloxacin 2 hours before or 6 hours after a dose of the magnesium containing agent to minimize the interaction.
Food InteractionsNot Available

Targets

1. Voltage-dependent calcium channel gamma-1 subunit

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Voltage-dependent calcium channel gamma-1 subunit Q06432 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

2. Voltage-dependent calcium channel subunit alpha-2/delta-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Voltage-dependent calcium channel subunit alpha-2/delta-1 P54289 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

3. Voltage-dependent L-type calcium channel subunit alpha-1C

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit alpha-1C Q13936 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

4. Voltage-dependent L-type calcium channel subunit beta-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit beta-1 Q02641 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

5. Voltage-dependent L-type calcium channel subunit beta-2

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit beta-2 Q08289 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

6. Voltage-dependent L-type calcium channel subunit alpha-1S

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Voltage-dependent L-type calcium channel subunit alpha-1S Q13698 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on March 14, 2014 14:50