Identification
Name Magnesium Sulfate
Accession Number DB00653 (APRD01080)
Type small molecule
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
Categories (*)
Molecular Weight 120.368
Groups approved
Monoisotopic Weight 119.936771076
Pharmacology
Indication Used 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.
Mechanism of action Magnesium 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.
Absorption Not Available
Protein binding 25-30%
Biotransformation None
Route of elimination Magnesium is excreted solely by the kidney at a rate proportional to the serum concentration and glomerular filtration.
Toxicity LD50 = 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
Interactions
Drug Interactions
Drug Mechanism of interaction
Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
Dihydrocodeine May enhance CNS depressant effects of CNS depressants. It is recommended to monitor therapy.
Eltrombopag Levels of eltrombopag are decreased due to GI inhibition. Separate administration by at least 4 hours.
Tiludronate The 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.
Triprolidine The CNS depressants, Triprolidine and Magnesium sulfate, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Trovafloxacin Magnesium 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 Interactions Not Available
Voltage-dependent calcium channel gamma-1 subunit
Name Voltage-dependent calcium channel gamma-1 subunit
Gene Name CACNG1
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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
DTHybrid score 0.419
Voltage-dependent calcium channel subunit alpha-2/delta-1
Name Voltage-dependent calcium channel subunit alpha-2/delta-1
Gene Name CACNA2D1
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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
DTHybrid score 0.5122
Voltage-dependent L-type calcium channel subunit alpha-1C
Name Voltage-dependent L-type calcium channel subunit alpha-1C
Gene Name CACNA1C
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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
DTHybrid score 0.5628
Voltage-dependent L-type calcium channel subunit beta-1
Name Voltage-dependent L-type calcium channel subunit beta-1
Gene Name CACNB1
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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
DTHybrid score 0.3123
Voltage-dependent L-type calcium channel subunit beta-2
Name Voltage-dependent L-type calcium channel subunit beta-2
Gene Name CACNB2
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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
DTHybrid score 0.4583
Voltage-dependent L-type calcium channel subunit alpha-1S
Name Voltage-dependent L-type calcium channel subunit alpha-1S
Gene Name CACNA1S
Pharmacological action unknown
Actions Not Available
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • 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
DTHybrid score 0.4648
Id Partner name Gene Name Score
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.3477
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.161
4512 Cytochrome P450 3A4 CYP3A4 0.1596
4160 Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2 0.148
4118 Cytochrome P450 3A5 CYP3A5 0.1438
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.133
6107 Cytochrome P450 3A7 CYP3A7 0.125
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.1136
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.1125
1588 Multidrug resistance protein 1 ABCB1 0.1039
4119 Cytochrome P450 2D6 CYP2D6 0.0935
4200 Cytochrome P450 1A2 CYP1A2 0.0788
6045 Voltage-dependent calcium channel subunit alpha-2/delta-3 CACNA2D3 0.0745
4757 Cytochrome P450 2C9 CYP2C9 0.0719
751 Potassium channel subfamily K member 6 KCNK6 0.0707
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0678
4924 Cytochrome P450 2C8 CYP2C8 0.0644
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.0643
172 Potassium channel subfamily K member 1 KCNK1 0.0639
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.0565
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.0565
3970 Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B 0.0549
737 Mineralocorticoid receptor NR3C2 0.0499
5718 Cytochrome P450 2A6 CYP2A6 0.0465
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0464
465 Calmodulin CALM1 0.0462
831 D(2) dopamine receptor DRD2 0.0441
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0437
6016 Cytochrome P450 2C19 CYP2C19 0.0432
6048 Troponin C, skeletal muscle TNNC2 0.0423
6220 Aryl hydrocarbon receptor AHR 0.0419
4604 Liver carboxylesterase 1 CES1 0.0409
6024 Cytochrome P450 1A1 CYP1A1 0.0405
6013 Cytochrome P450 2E1 CYP2E1 0.0401
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.04
6030 Cytochrome P450 2B6 CYP2B6 0.0389
502 5-hydroxytryptamine 2A receptor HTR2A 0.0374
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0369
6046 Voltage-gated calcium channel beta 1 subunit splice variant CavB1d CACNB1 0.0334
1971 cAMP-specific 3',5'-cyclic phosphodiesterase 4A PDE4A 0.0332
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0298
233 Potassium channel subfamily K member 2 KCNK2 0.0266
789 Alpha-1D adrenergic receptor ADRA1D 0.0244
632 Alpha-1B adrenergic receptor ADRA1B 0.0218
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0216
1108 Calpastatin CAST 0.0211
1089 Cartilage oligomeric matrix protein COMP 0.0211
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0209
574 Branched-chain-amino-acid aminotransferase, cytosolic BCAT1 0.0199
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0196
556 Alpha-1A adrenergic receptor ADRA1A 0.0194
16 Adenosine A1 receptor ADORA1 0.0189
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0188
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.017
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0159
378 Alpha-2C adrenergic receptor ADRA2C 0.015
629 Alpha-2B adrenergic receptor ADRA2B 0.0147
295 Carbonic anhydrase 1 CA1 0.0144
193 Beta-1 adrenergic receptor ADRB1 0.0142
318 Alpha-2A adrenergic receptor ADRA2A 0.0132
392 Voltage-dependent P/Q-type calcium channel subunit alpha-1A CACNA1A 0.0124
2132 Protein S100-B S100B 0.0117
587 Serum albumin ALB 0.0112
3923 Cholinesterase BCHE 0.0099
241 Calcium-transporting ATPase type 2C member 1 ATP2C1 0.0095
6148 Multidrug resistance-associated protein 7 ABCC10 0.0094
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0086
6106 Cytochrome P450 2C18 CYP2C18 0.0086
833 Organic cation/carnitine transporter 1 SLC22A4 0.0084
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0084
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0084
776 Bile salt export pump ABCB11 0.008
824 Sodium-dependent serotonin transporter SLC6A4 0.0079
2164 Multidrug resistance-associated protein 4 ABCC4 0.0078
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0076
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0074
862 Multidrug resistance-associated protein 1 ABCC1 0.0074
118 Organic cation/carnitine transporter 2 SLC22A5 0.0074
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0073
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0072
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0071
6145 Solute carrier family 22 member 1 SLC22A1 0.007
492 Histamine H1 receptor HRH1 0.0069
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0068