Tocolytic Agents

Drugs that prevent preterm labor and immature birth by suppressing uterine contractions (TOCOLYSIS). Agents used to delay premature uterine activity include magnesium sulfate, beta-mimetics, oxytocin antagonists, calcium channel inhibitors, and adrenergic beta-receptor agonists. The use of intravenous alcohol as a tocolytic is now obsolete.
DrugDrug NameDrug Indication
DB00328IndometacinOral indometacin is indicated for symptomatic management of moderate to severe rheumatoid arthritis including acute flares of chronic disease, moderate to severe ankylosing spondylitis, moderate to severe osteoarthritis, acute painful shoulder (bursitis and/or tendinitis) and acute gouty arthritis.[A177871,Label] Intravenous indometacin is indicated to induce closure of a hemodynamically significant patent ductus arteriosus in premature infants weighing between 500 and 1750 g when after 48 hours usual medical management (e.g., fluid restriction, diuretics, digitalis, respiratory support, etc.) is ineffective.[F4600]
DB00653Magnesium sulfateUsed 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.
DB00816OrciprenalineFor the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema.
DB00867RitodrineFor the treatment and prophylaxis of premature labour
DB00871TerbutalineFor the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible, obstructive airway disease, as well as symptomatic management of reversible bronchospasm associated with bronchitis and emphysema. Also used acute IV and sub-Q therapy in selected women to inhibit uterine contractions in preterm labor (tocolysis) and prolong gestation when beneficial.
DB01001SalbutamolSalbutamol is indicated for (i) the symptomatic relief and prevention of bronchospasm due to bronchial asthma, chronic bronchitis, reversible obstructive airway disease, and other chronic bronchopulmonary disorders in which bronchospasm is a complicating factor, and/or (ii) the acute prophylaxis against exercise-induced bronchospasm and other stimuli known to induce bronchospasm [FDA Label, F3265, F3268].
DB01115NifedipineFor the management of vasospastic angina, chronic stable angina, hypertension, and Raynaud's phenomenon. May be used as a first line agent for left ventricular hypertrophy and isolated systolic hypertension (long-acting agents).
DB01288FenoterolFenoterol is used for the treatment of asthma.
DB06152NylidrinNylidrin is mainly indicated in conditions like arteriosclerosis, cerebrovascular disease, peripheral vascular disease, Raynaud's disease, thrombo-angitis obliterans, and thrombophlebitis [L2285]. It may sometimes be used in the treatment of peripheral vascular disorders in addition premature labor (however, the drug is not approved for premature labor)[A32531].
DB08941IsoxsuprineNot Available
DB08957HexoprenalineNot Available
DB09059AtosibanAtosiban is indicated for use in delaying imminent pre-term birth in pregnant adult women with: - regular uterine contractions of at least 30 s duration at a rate of at least 4 per 30 min - a cervical dilation of 1-3cm (0-3cm for nulliparas) and effacement of at least 50% - a gestational age of 24-33 weeks - a normal fetal heart rate
DrugDrug NameTargetType
DB00328IndometacinProstaglandin G/H synthase 1target
DB00328IndometacinProstaglandin G/H synthase 2target
DB00328IndometacinCytochrome P450 2C19enzyme
DB00328IndometacinUDP-glucuronosyltransferase 1-9enzyme
DB00328IndometacinPhospholipase A2, membrane associatedtarget
DB00328IndometacinProstaglandin reductase 2target
DB00328IndometacinLactoylglutathione lyasetarget
DB00328IndometacinProstaglandin D2 receptor 2target
DB00328IndometacinPeroxisome proliferator-activated receptor gammatarget
DB00328IndometacinSerum albumincarrier
DB00328IndometacinCanalicular multispecific organic anion transporter 2transporter
DB00328IndometacinMultidrug resistance-associated protein 4transporter
DB00328IndometacinMultidrug resistance-associated protein 6transporter
DB00328IndometacinMultidrug resistance protein 1transporter
DB00328IndometacinMultidrug resistance-associated protein 1transporter
DB00328IndometacinSolute carrier organic anion transporter family member 1A2transporter
DB00328IndometacinSolute carrier family 22 member 6transporter
DB00328IndometacinSolute carrier family 22 member 8transporter
DB00328IndometacinCanalicular multispecific organic anion transporter 1transporter
DB00328IndometacinATP-binding cassette sub-family C member 11transporter
DB00328IndometacinSolute carrier family 22 member 11transporter
DB00328IndometacinSodium/bile acid cotransportertransporter
DB00328IndometacinSolute carrier family 22 member 7transporter
DB00328IndometacinCytochrome P450 2C9enzyme
DB00328IndometacinUDP-glucuronosyltransferase 1-1enzyme
DB00328IndometacinLiver carboxylesterase 1enzyme
DB00328IndometacinUDP-glucuronosyltransferase 2B7enzyme
DB00328IndometacinPeroxisome proliferator-activated receptor alphatarget
DB00328IndometacinAldo-keto reductase family 1 member C3target
DB00328IndometacinSolute carrier organic anion transporter family member 1B1transporter
DB00328IndometacinBile salt export pumptransporter
DB00653Magnesium sulfateVoltage-dependent calcium channel gamma-1 subunittarget
DB00653Magnesium sulfateVoltage-dependent calcium channel subunit alpha-2/delta-1target
DB00653Magnesium sulfateVoltage-dependent L-type calcium channel subunit alpha-1Ctarget
DB00653Magnesium sulfateVoltage-dependent L-type calcium channel subunit beta-1target
DB00653Magnesium sulfateVoltage-dependent L-type calcium channel subunit beta-2target
DB00653Magnesium sulfateVoltage-dependent L-type calcium channel subunit alpha-1Starget
DB00816OrciprenalineBeta-2 adrenergic receptortarget
DB00867RitodrineBeta-2 adrenergic receptortarget
DB00867Ritodrine6-phosphogluconate dehydrogenase, decarboxylatingenzyme
DB00871TerbutalineBeta-2 adrenergic receptortarget
DB00871TerbutalineCholinesteraseenzyme
DB00871TerbutalineBeta-3 adrenergic receptortarget
DB00871TerbutalineBeta-1 adrenergic receptortarget
DB01001SalbutamolBeta-2 adrenergic receptortarget
DB01001SalbutamolBeta-1 adrenergic receptortarget
DB01001SalbutamolCytochrome P450 3A4enzyme
DB01001SalbutamolBeta-3 adrenergic receptortarget
DB01115NifedipineVoltage-dependent calcium channel subunit alpha-2/delta-1target
DB01115NifedipineCytochrome P450 3A4enzyme
DB01115NifedipineCytochrome P450 2E1enzyme
DB01115NifedipineCytochrome P450 2D6enzyme
DB01115NifedipineCalmodulintarget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit alpha-1Dtarget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit alpha-1Starget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit alpha-1Ctarget
DB01115NifedipineVoltage-dependent L-type calcium channel subunit beta-2target
DB01115NifedipinePotassium voltage-gated channel subfamily A member 1target
DB01115NifedipineVoltage-dependent T-type calcium channel subunit alpha-1Htarget
DB01115NifedipineCytochrome P450 1A2enzyme
DB01115NifedipineCytochrome P450 2A6enzyme
DB01115NifedipineCytochrome P450 2C8enzyme
DB01115NifedipineCytochrome P450 3A5enzyme
DB01115NifedipineCytochrome P450 3A7enzyme
DB01115NifedipineCanalicular multispecific organic anion transporter 2transporter
DB01115NifedipineMultidrug resistance protein 1transporter
DB01115NifedipineCanalicular multispecific organic anion transporter 1transporter
DB01115NifedipineCytochrome P450 1A1enzyme
DB01115NifedipineCytochrome P450 2B6enzyme
DB01115NifedipineNuclear receptor subfamily 1 group I member 2target
DB01115NifedipineSolute carrier organic anion transporter family member 1B1transporter
DB01115NifedipineBile salt export pumptransporter
DB01288FenoterolBeta-2 adrenergic receptortarget
DB01288FenoterolBeta-1 adrenergic receptortarget
DB01288FenoterolBeta-3 adrenergic receptortarget
DB06152NylidrinCatechol O-methyltransferaseenzyme
DB06152NylidrinVoltage-dependent T-type calcium channel subunit alpha-1Itarget
DB06152NylidrinInterferon alpha/beta receptor 2target
DB06152NylidrinCytochrome P450 3A4enzyme
DB09059AtosibanOxytocin receptortarget
DB09059AtosibanVasopressin V1a receptortarget
DB09059AtosibanVasopressin V1b receptortarget
DB09059AtosibanVasopressin V2 receptortarget