DT-Web

DB06751 - Drotaverine


Identification
Name Drotaverine
Accession Number DB06751
Type small molecule
Description Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects. Drotaverine has been shown to possess dose-dependant analgesic effects in animal models. One small study has shown drotaverine to be eliminated mainly non-renally.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 397.5072
Groups approved
Monoisotopic Weight 397.225308485
Pharmacology
Indication Used in the treatment of functional bowel disorders and alleviating pain in renal colic.
Mechanism of action Drotaverine inhibits phosphodiesterases hydrolysing cAMP, thereby increasing cAMP concentration, decreasing Ca uptake of the cells and changing the distribution of calcium among the cells. It may also have minor allosteric calcium channel blocking properties.
Absorption Bioavailability is highly variable
Protein binding 80 to 95%
Biotransformation Hepatic
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Name cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Gene Name PDE4A
Pharmacological action yes
Actions inhibitor
References
  • Muravyov AV, Yakusevich VV, Chuchkanov FA, Maimistova AA, Bulaeva SV, Zaitsev LG: Hemorheological efficiency of drugs, targeting on intracellular phosphodiesterase activity: in vitro study. Clin Hemorheol Microcirc. 2007;36(4):327-34. - Pubmed
  • Romics I, Molnar DL, Timberg G, Mrklic B, Jelakovic B, Koszegi G, Blasko G: The effect of drotaverine hydrochloride in acute colicky pain caused by renal and ureteric stones. BJU Int. 2003 Jul;92(1):92-6. - Pubmed
  • Pareek A, Chandurkar NB, Patil RT, Agrawal SN, Uday RB, Tambe SG: Efficacy and safety of aceclofenac and drotaverine fixed-dose combination in the treatment of primary dysmenorrhoea: a double-blind, double-dummy, randomized comparative study with aceclofenac. Eur J Obstet Gynecol Reprod Biol. 2010 Sep;152(1):86-90. Epub 2010 Jun 15. - Pubmed
DTHybrid score Not Available
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 inhibitor
References
  • Tomoskozi Z, Finance O, Aranyi P: Drotaverine interacts with the L-type Ca(2+) channel in pregnant rat uterine membranes. Eur J Pharmacol. 2002 Aug 2;449(1-2):55-60. - Pubmed
  • Romics I, Molnar DL, Timberg G, Mrklic B, Jelakovic B, Koszegi G, Blasko G: The effect of drotaverine hydrochloride in acute colicky pain caused by renal and ureteric stones. BJU Int. 2003 Jul;92(1):92-6. - Pubmed
DTHybrid score 0.1998

Predictions


Id Partner name Gene Name Score
2358 cAMP-specific 3',5'-cyclic phosphodiesterase 4D PDE4D 0.1603
541 cAMP-specific 3',5'-cyclic phosphodiesterase 4B PDE4B 0.1527
4109 cAMP-specific 3',5'-cyclic phosphodiesterase 4C PDE4C 0.1057
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.084
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0768
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0724
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.065
485 cGMP-inhibited 3',5'-cyclic phosphodiesterase A PDE3A 0.0499
268 Adenosine A2b receptor ADORA2B 0.0442
1178 Adenosine A2a receptor ADORA2A 0.0414
16 Adenosine A1 receptor ADORA1 0.041
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0387
4512 Cytochrome P450 3A4 CYP3A4 0.0372
4200 Cytochrome P450 1A2 CYP1A2 0.0337
695 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A PDE10A 0.0326
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0326
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0325
750 Voltage-dependent calcium channel gamma-1 subunit CACNG1 0.0293
204 cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A 0.0292
691 cAMP-specific 3',5'-cyclic phosphodiesterase 7B PDE7B 0.026
3806 cGMP-dependent 3',5'-cyclic phosphodiesterase PDE2A 0.0253
779 High-affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A PDE7A 0.025
1588 Multidrug resistance protein 1 ABCB1 0.0238
4160 Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2 0.0219
4118 Cytochrome P450 3A5 CYP3A5 0.0214
1108 Calpastatin CAST 0.0211
1089 Cartilage oligomeric matrix protein COMP 0.0211
6048 Troponin C, skeletal muscle TNNC2 0.0201
4122 Histone deacetylase 2 HDAC2 0.0193
4119 Cytochrome P450 2D6 CYP2D6 0.019
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0187
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0187
4757 Cytochrome P450 2C9 CYP2C9 0.0187
6107 Cytochrome P450 3A7 CYP3A7 0.0173
465 Calmodulin CALM1 0.0166
1830 5'-nucleotidase NT5E 0.0162
3957 Adenosine deaminase ADA 0.0156
6045 Voltage-dependent calcium channel subunit alpha-2/delta-3 CACNA2D3 0.0152
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0143
4924 Cytochrome P450 2C8 CYP2C8 0.014
6013 Cytochrome P450 2E1 CYP2E1 0.0137
6216 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A PDE8A 0.0128
6217 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B PDE8B 0.0128
6024 Cytochrome P450 1A1 CYP1A1 0.0125
6143 Solute carrier family 22 member 7 SLC22A7 0.0121
2132 Protein S100-B S100B 0.0117
5718 Cytochrome P450 2A6 CYP2A6 0.0115
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0113
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0107
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0104
6136 Multidrug resistance-associated protein 5 ABCC5 0.0104
2164 Multidrug resistance-associated protein 4 ABCC4 0.01
1792 Tissue-type plasminogen activator PLAT 0.01
6030 Cytochrome P450 2B6 CYP2B6 0.0099
751 Potassium channel subfamily K member 6 KCNK6 0.0098
241 Calcium-transporting ATPase type 2C member 1 ATP2C1 0.0095
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.0095
737 Mineralocorticoid receptor NR3C2 0.0093
527 Prostacyclin receptor PTGIR 0.0093
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0092
6016 Cytochrome P450 2C19 CYP2C19 0.0091
172 Potassium channel subfamily K member 1 KCNK1 0.009
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0086
492 Histamine H1 receptor HRH1 0.0085
73 Prostaglandin E2 receptor, EP1 subtype PTGER1 0.0085
6040 6-phosphogluconate dehydrogenase, decarboxylating PGD 0.0083
6160 Solute carrier organic anion transporter family member 3A1 SLCO3A1 0.0081
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.008
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.008
6152 Solute carrier organic anion transporter family member 2A1 SLCO2A1 0.008
6220 Aryl hydrocarbon receptor AHR 0.0073
6046 Voltage-gated calcium channel beta 1 subunit splice variant CavB1d CACNB1 0.0067
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0065
3970 Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B 0.0063
789 Alpha-1D adrenergic receptor ADRA1D 0.0052
632 Alpha-1B adrenergic receptor ADRA1B 0.0046
233 Potassium channel subfamily K member 2 KCNK2 0.0046
3923 Cholinesterase BCHE 0.0045
556 Alpha-1A adrenergic receptor ADRA1A 0.0041
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0041
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0037
1898 Cytochrome P450 1B1 CYP1B1 0.0035
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0034
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0033
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0033
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0033
831 D(2) dopamine receptor DRD2 0.0032
295 Carbonic anhydrase 1 CA1 0.003
378 Alpha-2C adrenergic receptor ADRA2C 0.0026
629 Alpha-2B adrenergic receptor ADRA2B 0.0026
193 Beta-1 adrenergic receptor ADRB1 0.0025
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0024
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0023
318 Alpha-2A adrenergic receptor ADRA2A 0.0023
392 Voltage-dependent P/Q-type calcium channel subunit alpha-1A CACNA1A 0.0021
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0021
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0021
103 Muscarinic acetylcholine receptor M1 CHRM1 0.002
587 Serum albumin ALB 0.0019
6148 Multidrug resistance-associated protein 7 ABCC10 0.0016
6106 Cytochrome P450 2C18 CYP2C18 0.0015
833 Organic cation/carnitine transporter 1 SLC22A4 0.0015
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0015
776 Bile salt export pump ABCB11 0.0014
824 Sodium-dependent serotonin transporter SLC6A4 0.0014
862 Multidrug resistance-associated protein 1 ABCC1 0.0013
118 Organic cation/carnitine transporter 2 SLC22A5 0.0013
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0013
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0013
6145 Solute carrier family 22 member 1 SLC22A1 0.0012
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0012
↑