Histamine H2 Antagonists

Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
DrugDrug NameDrug Description
DB00501CimetidineA histamine H2 receptor antagonist used to manage GERD, peptic ulcer disease, and indigestion.
DB00585NizatidineAn H2 receptor antagonist used to treat GERD and a variety of ulcers.
DB00863RanitidineA histamine H2 antagonist used to treat duodenal ulcers, Zollinger-Ellison syndrome, gastric ulcers, GERD, and erosive esophagitis.
DB00927FamotidineA histamine H2 receptor antagonist used to treat duodenal ulcers, benign gastric ulcers, GERD, and Zollinger-Ellison syndrome.
DB08805MetiamidePotential in the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
DB08806Roxatidine acetateFor the treatment of disorders of the upper gastro-intestinal region that are due to an excess of hydrochloric acid in the gastric juice, i.e. duodenal ulcers, benign gastric ulcers. Also...
DB12770LafutidineLafutidine has been investigated in Peptic Ulcer, Community-acquired Pneumonia, and Gastroesophageal Reflux Disease (GERD).
DB12884LavoltidineLavoltidine has been used in trials studying the diagnostic of Reflux, Gastroesophageal and Gastroesophageal Reflux Disease.
DB13760NiperotidineNot Annotated
DB01142DoxepinA psychotropic agent used for the treatment of depression, anxiety, manic-depressive disorder, and insomnia.
DB00751EpinastineAn H1 receptor antagonist used to prevent itching in allergic conjunctivitis.
DB06216AsenapineAn atypical antipsychotic used to treat patients with bipolar I disorder and patients with schizophrenia.
DB00940MethanthelineFor the treatment of peptic ulcer disease, irritable bowel syndrome, pancreatitis, gastritis, biliary dyskinesia, pylorosplasm, and reflex neurogenic bladder in children.
DB00334OlanzapineAn antipsychotic drug used in the management of schizophrenia, bipolar 1 disorder, and agitation associated with these disorders.
DB01069PromethazineA first-generation antihistamine used for the treatment of allergic conditions, nausea and vomiting, and motion sickness.
DrugDrug NameTargetType
DB00501CimetidineHistamine H2 receptortarget
DB00501CimetidineCytochrome P450 1A2enzyme
DB00501CimetidineCytochrome P450 2D6enzyme
DB00501CimetidineCytochrome P450 2C19enzyme
DB00501CimetidineCytochrome P450 3A4enzyme
DB00501CimetidineCytochrome P450 3A5enzyme
DB00501CimetidineP-glycoprotein 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
DB00585NizatidineHistamine H2 receptortarget
DB00585NizatidineP-glycoprotein 1transporter
DB00585NizatidineCholinesteraseenzyme
DB00863RanitidineHistamine H2 receptortarget
DB00863RanitidineCytochrome P450 1A2enzyme
DB00863RanitidineCytochrome P450 2D6enzyme
DB00863RanitidineSolute carrier family 22 member 1transporter
DB00863RanitidineP-glycoprotein 1transporter
DB00863RanitidineSolute carrier family 22 member 8transporter
DB00863RanitidineCytochrome P450 3A4enzyme
DB00863RanitidineAcetylcholinesterasetarget
DB00863RanitidineSolute carrier family 22 member 2transporter
DB00863RanitidineCholinesterasetarget
DB00863RanitidineCholinesteraseenzyme
DB00927FamotidineHistamine H2 receptortarget
DB00927FamotidineSolute carrier family 22 member 2transporter
DB00927FamotidineSolute carrier family 22 member 8transporter
DB08805MetiamideHistamine H2 receptortarget
DB08806Roxatidine acetateHistamine H2 receptortarget
DB01142DoxepinSodium-dependent serotonin transportertarget
DB01142DoxepinSodium-dependent noradrenaline transportertarget
DB01142DoxepinHistamine H1 receptortarget
DB01142DoxepinHistamine H2 receptortarget
DB01142DoxepinCytochrome P450 2D6enzyme
DB01142DoxepinMuscarinic acetylcholine receptor M1target
DB01142DoxepinMuscarinic acetylcholine receptor M2target
DB01142DoxepinMuscarinic acetylcholine receptor M3target
DB01142DoxepinMuscarinic acetylcholine receptor M4target
DB01142DoxepinMuscarinic acetylcholine receptor M5target
DB01142DoxepinAlpha-1A adrenergic receptortarget
DB01142Doxepin5-hydroxytryptamine receptor 1Atarget
DB01142Doxepin5-hydroxytryptamine receptor 2Atarget
DB01142DoxepinCytochrome P450 2C19enzyme
DB01142DoxepinCytochrome P450 2C9enzyme
DB01142DoxepinCytochrome P450 1A2enzyme
DB01142DoxepinP-glycoprotein 1transporter
DB01142Doxepin5-hydroxytryptamine receptor 2Btarget
DB01142Doxepin5-hydroxytryptamine receptor 2Ctarget
DB01142DoxepinAlpha-1B adrenergic receptortarget
DB01142DoxepinAlpha-1D adrenergic receptortarget
DB01142DoxepinCytochrome P450 3A4enzyme
DB01142Doxepin5-hydroxytryptamine receptor 6target
DB01142DoxepinHistamine H4 receptortarget
DB01142DoxepinPotassium voltage-gated channel subfamily H member 2target
DB01142DoxepinSerum albumincarrier
DB01142DoxepinAlpha-1-acid glycoprotein 1carrier
DB00751EpinastineHistamine H1 receptortarget
DB00751EpinastineHistamine H2 receptortarget
DB00751EpinastineAlpha-1A adrenergic receptortarget
DB00751EpinastineAlpha-2A adrenergic receptortarget
DB00751Epinastine5-hydroxytryptamine receptor 2Atarget
DB00751Epinastine5-hydroxytryptamine receptor 7target
DB00751EpinastineP-glycoprotein 1transporter
DB00751EpinastineCytochrome P450 2B6enzyme
DB00751EpinastineCytochrome P450 2D6enzyme
DB00751EpinastineCytochrome P450 3A4enzyme
DB06216Asenapine5-hydroxytryptamine receptor 1Atarget
DB06216Asenapine5-hydroxytryptamine receptor 1Btarget
DB06216Asenapine5-hydroxytryptamine receptor 2Atarget
DB06216Asenapine5-hydroxytryptamine receptor 2Btarget
DB06216Asenapine5-hydroxytryptamine receptor 2Ctarget
DB06216Asenapine5-hydroxytryptamine receptor 6target
DB06216Asenapine5-hydroxytryptamine receptor 7target
DB06216AsenapineAlpha-2A adrenergic receptortarget
DB06216AsenapineAlpha-2B adrenergic receptortarget
DB06216AsenapineAlpha-2C adrenergic receptortarget
DB06216AsenapineAlpha-1A adrenergic receptortarget
DB06216AsenapineDopamine D1 receptortarget
DB06216AsenapineDopamine D2 receptortarget
DB06216AsenapineDopamine D3 receptortarget
DB06216AsenapineDopamine D4 receptortarget
DB06216AsenapineHistamine H1 receptortarget
DB06216AsenapineHistamine H2 receptortarget
DB06216AsenapineCytochrome P450 1A2enzyme
DB06216AsenapineCytochrome P450 2D6enzyme
DB06216Asenapine5-hydroxytryptamine receptor 5Atarget
DB06216AsenapineUDP-glucuronosyltransferase 1-4enzyme
DB06216AsenapineCytochrome P450 3A4enzyme
DB06216AsenapineBeta-1 adrenergic receptortarget
DB06216AsenapineBeta-2 adrenergic receptortarget
DB06216AsenapineSerum albumincarrier
DB06216Asenapinealpha1-acid glycoproteincarrier
DB00940MethanthelineMuscarinic acetylcholine receptor M1target
DB00940MethanthelineHistamine H2 receptortarget
DB00334OlanzapineDopamine D1 receptortarget
DB00334OlanzapineMuscarinic acetylcholine receptor M1target
DB00334OlanzapineMuscarinic acetylcholine receptor M3target
DB00334Olanzapine5-hydroxytryptamine receptor 2Atarget
DB00334OlanzapineDopamine D4 receptortarget
DB00334OlanzapineHistamine H1 receptortarget
DB00334OlanzapineMuscarinic acetylcholine receptor M4target
DB00334OlanzapineMuscarinic acetylcholine receptor M2target
DB00334OlanzapineDopamine D2 receptortarget
DB00334Olanzapine5-hydroxytryptamine receptor 2Ctarget
DB00334OlanzapineDopamine D3 receptortarget
DB00334OlanzapineAlpha-1B adrenergic receptortarget
DB00334OlanzapineCytochrome P450 1A2enzyme
DB00334Olanzapine5-hydroxytryptamine receptor 3Atarget
DB00334Olanzapine5-hydroxytryptamine receptor 6target
DB00334OlanzapineAlpha-1A adrenergic receptortarget
DB00334OlanzapineDopamine D5 receptortarget
DB00334OlanzapineSerum albumincarrier
DB00334OlanzapineAlpha-1-acid glycoprotein 1carrier
DB00334OlanzapineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00334OlanzapineCytochrome P450 2D6enzyme
DB00334OlanzapineP-glycoprotein 1transporter
DB00334OlanzapineCytochrome P450 2C19enzyme
DB00334OlanzapineD(1) dopamine receptortarget
DB00334OlanzapineBeta adrenergic receptortarget
DB00334Olanzapine5-hydroxytryptamine receptor 1target
DB00334OlanzapineGABA-A receptor (benzodiazepine site)target
DB00334OlanzapineCytochrome P450 2C9enzyme
DB00334OlanzapineUDP-glucuronosyltransferase 1-4enzyme
DB00334OlanzapineCytochrome P450 3A4enzyme
DB00334OlanzapineCYP3Aenzyme
DB01069PromethazineDopamine D2 receptortarget
DB01069PromethazineHistamine H1 receptortarget
DB01069PromethazineMuscarinic acetylcholine receptor M4target
DB01069PromethazineMuscarinic acetylcholine receptor M1target
DB01069PromethazineMuscarinic acetylcholine receptor M5target
DB01069PromethazineAlpha-1A adrenergic receptortarget
DB01069Promethazine5-hydroxytryptamine receptor 2Atarget
DB01069PromethazineMuscarinic acetylcholine receptor M2target
DB01069PromethazineMuscarinic acetylcholine receptor M3target
DB01069PromethazineCalmodulintarget
DB01069PromethazineCytochrome P450 2D6enzyme
DB01069PromethazineCytochrome P450 2B6enzyme
DB01069PromethazineP-glycoprotein 1transporter
DB01069PromethazineCytochrome P450 2C9enzyme
DB01069PromethazineHistamine H2 receptortarget