Derivatives of oxoacids RnE(=O)OH in which the hydroxy group is replaced by an amino group and the oxo group is replaced by =NR. Amidines include carboxamidines, sulfinamidines and phosphinamidines.
DrugDrug NameDrug Indication
DB00148CreatineFor nutritional supplementation, also for treating dietary shortage or imbalance.
DB00217BethanidineFor the treatment of hypertension.
DB00226GuanadrelUsed to treat and control hypertension.
DB00501CimetidineFor the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
DB00536GuanidineFor the reduction of the symptoms of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert. It is not indicated for treating myasthenia gravis.
DB00558ZanamivirFor the prevention and treatment of influenza A and B.
DB00629GuanabenzFor management of High blood pressure
DB00738PentamidineFor the treatment of pneumonia due to Pneumocystis carinii.
DB00878ChlorhexidineFor reduction of pocket depth in patients with adult periodontitis, used as an adjunct to scaling and root planing procedures. Also for prevention of dental caries, oropharyngeal decontamination in critically ill patients, hand hygiene in health-care personnel, general skin cleanser, and catheter site preparation and care.
DB00914PhenforminFor the reatment of type II diabetes mellitus.
DB01018GuanfacineFor use alone or in combination with other classes of antihypertensive agents in the management of hypertension. Has also been used for the treatment of attention deficit hyperactivity disorder (ADHD) in pediatric patients.
DB01131ProguanilFor the causal prevention and suppression of malaria caused by susceptible strains of P. falciparum and other species of Plasmodium found in some geographical areas of the world.
DB01170GuanethidineFor the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.
DB02727N-Butyl-N'-HydroxyguanidineNot Available
DB03127BenzamidineNot Available
DB03608DiminazeneNot Available
DB04778SC45647Not Available
DB04830BuforminNot Available
DB05217GMX1777Intended for the treatment of solid tumors and lymphomas.
DB06468CariporideInvestigated for use/treatment in cardiac surgery.
DB06532PafuramidineInvestigated for use/treatment in pneumonia, trypanosomiasis, malaria, HIV infection, and infectious and parasitic disease (unspecified).
DB06598BrostallicinInvestigated for use/treatment in solid tumors.
DB06614PeramivirIndicated for the treatment of acute uncomplicated influenza in patients 18 years and older who have been symptomatic for no more than two days.[label]
DB06704IobenguaneDetection of primary and metastatic pheochromocytoma or neuroblastoma
DB06762PinacidilNot Available
DB08838AgmatineAgmatine is being studied experimentally for several indications such as cardioprotection, diabetes, decreased kidney function, neuroprotection (stroke, severe CNS injuries, epilepsy, glaucoma, and neuropathic pain), and psychiatric conditions (depression, anxiety, schizophrenia, and cognition). As an investigational drug, agamatine is being studied in a non-blinded prospective case study in the United States looking at patients who have been diagnosed with small fiber peripheral neuropathy.
DB11409FebantelNot Available
DB11888Laninamivir octanoateNot Available
DB12277PolihexanideNot Available
DB12314ChlorproguanilNot Available
DB12598NafamostatUsed as an anticoagulant in patients with disseminative blood vessel coagulation, hemorrhagic lesions, and hemorrhagic tendencies. It prevents blood clot formation during extracorporeal circulation in patients undergoing continuous renal replacement therapy and extra corporeal membrane oxygenation.
DB12692GusperimusNot Available
DB12791LaninamivirNot Available
DB12831GabexateNo approved indication.
DB12967MitoguazoneNot Available
DB12980CHS-828Not Available
DB12991DeoxyspergualinNot Available
DB13191PhosphocreatinePhosphocreatine is a naturally occuring substance that is found predominantly in the skeletal muscles of vertebrates. Its primary utility within the body is to serve in the maintanence and recycling of adenosine triphosphate (ATP) for muscular activity like contractions. Given this utility of phosphocreatine to recycle ATP, the most plausible therapeutic potentials for its use involve conditions caused by energy shortage or by increased energy requirements - such as in ischemic stroke and other cerebrovascular diseases. It is important to note however that relatively little clinical research has been done to significantly further the evidence for any such indications, although it is administered intravenously for cardiovascular conditions in some countries. Additionally, because phosphocreatine is not regulated as a controlled substance it is taken as a supplement by some professional athletes as a means to perhaps increase short bursts of muscle strength or energy for professional athletics.
DB13211GuanoxanNot Available
DB13296PropamidineNot Available
DB13410GuanoxabenzNot Available
DB13548DibrompropamidineNot Available
DB13604GuanazodineNot Available
DB13697AmbazoneNot Available
DB13726SulfaguanidineNot Available
DB13729CamostatNot Available
DB13779GuanoclorNot Available
DB14191DiphenylguanidineDiphenylguanidine is approved for use within allergenic epicutaneous patch tests which are indicated for use as an aid in the diagnosis of allergic contact dermatitis (ACD) in persons 6 years of age and older.
DB00331Metformin**Metformin tablet** Metformin is indicated as an adjunct to diet and exercise to increase glycemic control in _adults and pediatric patients_ 10 years of age and older diagnosed with type 2 diabetes mellitus [FDA label]. **Metformin extended-release tablet (XR)** The extended-release form is indicated as an adjunct to diet and exercise to improve glycemic control in only _adults_ with type 2 diabetes mellitus. Safety in children has not been determined to this date [FDA label].
DB03808HexamidineNot Available
DB05383PimagedineInvestigated for use/treatment in diabetic kidney disease.
DB14753HydroxystilbamidineUsed in the treatment of nonprogressive blastomycosis of the skin and other mycoses.
DB14763CycloguanilNot Available
DB12997BrilacidinNot Available
DrugDrug NameTargetType
DB00148CreatineSodium- and chloride-dependent creatine transporter 1target
DB00148CreatineGuanidinoacetate N-methyltransferasetarget
DB00148CreatineCreatine kinase M-typetarget
DB00148CreatineCreatine kinase U-type, mitochondrialtarget
DB00148CreatineCreatine kinase B-typetarget
DB00148CreatineCreatine kinase S-type, mitochondrialtarget
DB00148CreatineSolute carrier family 22 member 5transporter
DB00217BethanidineAlpha-2 adrenergic receptorstarget
DB00217BethanidineATP-sensitive inward rectifier potassium channel 1target
DB00217BethanidineBeta adrenergic receptortarget
DB00226GuanadrelSodium-dependent noradrenaline transportertarget
DB00501CimetidineHistamine H2 receptortarget
DB00501CimetidineCytochrome P450 1A2enzyme
DB00501CimetidineCytochrome P450 2D6enzyme
DB00501CimetidineCytochrome P450 2C19enzyme
DB00501CimetidineCytochrome P450 3A4enzyme
DB00501CimetidineCytochrome P450 3A5enzyme
DB00501CimetidineCytochrome P450 3A7enzyme
DB00501CimetidineMultidrug resistance protein 1transporter
DB00501CimetidineSolute carrier family 22 member 2transporter
DB00501CimetidineSolute carrier family 22 member 1transporter
DB00501CimetidineSolute carrier family 22 member 3transporter
DB00501CimetidineSolute carrier family 22 member 5transporter
DB00501CimetidineSolute carrier family 22 member 6transporter
DB00501CimetidineSolute carrier family 22 member 8transporter
DB00501CimetidineMultidrug and toxin extrusion protein 1transporter
DB00501CimetidineSolute carrier family 22 member 4transporter
DB00501CimetidineSolute carrier family 22 member 11transporter
DB00501CimetidineSolute carrier family 22 member 7transporter
DB00501CimetidineCytochrome P450 11B1, mitochondrialenzyme
DB00501CimetidineCytochrome P450 2C8enzyme
DB00501CimetidineCytochrome P450 2C9enzyme
DB00501CimetidineCytochrome P450 2E1enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00501CimetidineBile salt export pumptransporter
DB00501CimetidineMultidrug and toxin extrusion protein 2transporter
DB00536GuanidineRibonuclease pancreatictarget
DB00536GuanidineDNAtarget
DB00536GuanidineDisks large homolog 4target
DB00536GuanidineLysozymetarget
DB00536GuanidineAldehyde dehydrogenase, mitochondrialtarget
DB00536GuanidineArgininosuccinate synthasetarget
DB00536GuanidineGuanidinoacetate N-methyltransferasetarget
DB00536GuanidineArginasetarget
DB00536GuanidineSolute carrier family 22 member 2transporter
DB00536GuanidineSolute carrier family 22 member 1transporter
DB00536GuanidineSolute carrier family 22 member 3transporter
DB00536GuanidineSolute carrier family 22 member 5transporter
DB00536GuanidineSolute carrier family 22 member 8transporter
DB00536GuanidineSolute carrier family 22 member 4transporter
DB00536GuanidineMultidrug and toxin extrusion protein 1transporter
DB00536GuanidineMultidrug and toxin extrusion protein 2transporter
DB00558ZanamivirNeuraminidasetarget
DB00558ZanamivirNeuraminidasetarget
DB00558ZanamivirSialidase-2target
DB00629GuanabenzAlpha-2A adrenergic receptortarget
DB00629GuanabenzCytochrome P450 1A2enzyme
DB00629GuanabenzAlpha-2B adrenergic receptortarget
DB00738PentamidineDNAtarget
DB00738PentamidineCytochrome P450 2C19enzyme
DB00738PentamidinetRNA (cytosine(38)-C(5))-methyltransferasetarget
DB00738PentamidineCytochrome P450 2C8enzyme
DB00738PentamidineCytochrome P450 2D6enzyme
DB00738PentamidineCytochrome P450 1A1enzyme
DB00738PentamidineCytochrome P450 3A5enzyme
DB00738PentamidineCytochrome P450 4A11enzyme
DB00878ChlorhexidineBacterial outer membranetarget
DB00878ChlorhexidineHistamine N-methyltransferaseenzyme
DB00878ChlorhexidineChloramphenicol acetyltransferaseenzyme
DB00914Phenformin5'-AMP-activated protein kinase catalytic subunit alpha-1target
DB00914PhenforminCytochrome P450 2D6enzyme
DB00914PhenforminSolute carrier family 22 member 2transporter
DB00914PhenforminSolute carrier family 22 member 1transporter
DB00914PhenforminATP-sensitive inward rectifier potassium channel 8target
DB01018GuanfacineAlpha-2A adrenergic receptortarget
DB01018GuanfacineCytochrome P450 2C19enzyme
DB01018GuanfacineCytochrome P450 3A4enzyme
DB01018GuanfacineAlpha-2B adrenergic receptortarget
DB01131ProguanilBifunctional dihydrofolate reductase-thymidylate synthasetarget
DB01131ProguanilDihydrofolate reductasetarget
DB01131ProguanilCytochrome P450 2C19enzyme
DB01131ProguanilCytochrome P450 2D6enzyme
DB01131ProguanilCytochrome P450 2C9enzyme
DB01131ProguanilCytochrome P450 2E1enzyme
DB01131ProguanilCytochrome P450 3A4enzyme
DB01170GuanethidineSodium-dependent noradrenaline transportertarget
DB01170GuanethidineCytochrome P450 3A4enzyme
DB02727N-Butyl-N'-HydroxyguanidineNitric oxide synthase, braintarget
DB03127BenzamidineUrokinase-type plasminogen activatortarget
DB03127BenzamidineTrypsin-1target
DB03127BenzamidineCasein kinase II subunit alphatarget
DB03127BenzamidineKallikrein-6target
DB03127BenzamidineTrypsin-2target
DB03127BenzamidineTrypsin-3target
DB03127BenzamidineCopper transport protein ATOX1target
DB03127BenzamidineEnoyl-CoA delta isomerase 1, mitochondrialtarget
DB03127BenzamidineTrypsintarget
DB03127BenzamidineSuppressor of tumorigenicity 14 proteintarget
DB03127BenzamidineKallikrein-1target
DB03608DiminazenePeroxiredoxin-5, mitochondrialtarget
DB03608DiminazeneHTH-type transcriptional regulator QacRtarget
DB03608DiminazeneTrypsin-1target
DB03608DiminazeneAmiloride-sensitive amine oxidase [copper-containing]target
DB04830BuforminSolute carrier family 22 member 1transporter
DB05217GMX1777Nicotinamide phosphoribosyltransferasetarget
DB06468CariporideSodium/hydrogen exchanger 1target
DB06468CariporideMyeloperoxidaseenzyme
DB06614PeramivirNeuraminidasetarget
DB06614PeramivirNeuraminidasetarget
DB06614PeramivirNeuraminidasetarget
DB06704IobenguaneSodium-dependent noradrenaline transportertransporter
DB06762PinacidilCytochrome P450 3A4enzyme
DB08838AgmatineSolute carrier family 22 member 1transporter
DB08838AgmatineSolute carrier family 22 member 2transporter
DB08838AgmatineSolute carrier family 22 member 3transporter
DB08838AgmatineAlpha-2C adrenergic receptortarget
DB08838AgmatineNischarintarget
DB08838AgmatineAcetylcholine receptor subunit alphatarget
DB08838AgmatineGlutamate receptor ionotropic, NMDA 1target
DB08838AgmatineATP-sensitive inward rectifier potassium channel 1target
DB08838AgmatineVoltage-dependent N-type calcium channel subunit alpha-1Btarget
DB08838AgmatineAcid-sensing ion channel 3target
DB08838AgmatineY+L amino acid transporter 1transporter
DB08838AgmatineCytochrome P450 3A4enzyme
DB12598NafamostatIntercellular adhesion molecule 1target
DB12598NafamostatTrypsin-1target
DB12598NafamostatKallikrein-1target
DB12598NafamostatProthrombintarget
DB12598NafamostatCoagulation factor Xtarget
DB12598NafamostatCoagulation factor XIItarget
DB12598NafamostatSolute carrier family 22 member 1transporter
DB12598NafamostatSolute carrier family 22 member 2transporter
DB12831GabexateTrypsin-1enzyme
DB12831GabexateComplement C1s subcomponentenzyme
DB12831GabexateComplement C1r subcomponentenzyme
DB12831GabexatePlasma kallikreintarget
DB12831GabexateProthrombintarget
DB12831GabexatePlasminogentarget
DB13191PhosphocreatineGuanidinoacetate N-methyltransferasetarget
DB13191PhosphocreatineSodium- and chloride-dependent creatine transporter 1target
DB13191PhosphocreatineCreatine kinase M-typetarget
DB13191PhosphocreatineCreatine kinase U-type, mitochondrialtarget
DB13191PhosphocreatineCreatine kinase S-type, mitochondrialtarget
DB13191PhosphocreatineCreatine kinase B-typetarget
DB00331Metformin5'-AMP-activated protein kinase subunit beta-1target
DB00331MetforminSolute carrier family 22 member 2transporter
DB00331MetforminSolute carrier family 22 member 1transporter
DB00331MetforminMultidrug and toxin extrusion protein 1transporter
DB00331MetforminEquilibrative nucleoside transporter 4transporter
DB00331MetforminSolute carrier family 22 member 3transporter
DB00331MetforminMultidrug and toxin extrusion protein 2transporter
DB00331MetforminMitochondrial complex Itarget
DB00331MetforminGlycerol-3-phosphate dehydrogenase [NAD(+)], cytoplasmictarget
DB03808HexamidineHTH-type transcriptional regulator QacRtarget
DB03808HexamidineHTH-type transcriptional regulator QacRtarget
DB05383PimagedineNitric oxide synthase, inducibletarget
DB05383PimagedineAldose reductasetarget
DB05383PimagedineMetalloproteinase inhibitor 3target
DB05383PimagedineSolute carrier family 22 member 2transporter
DB14753HydroxystilbamidineDNAtarget