Histamine H2 Antagonists

Name
Histamine H2 Antagonists
Accession Number
DBCAT000933  (DBCAT002400, DBCAT002656, DBCAT003361, DBCAT003696)
Description

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.

ATC Classification
Drugs
DrugDrug Description
CimetidineA histamine H2 receptor antagonist used to manage GERD, peptic ulcer disease, and indigestion.
NizatidineAn H2 receptor antagonist used to treat GERD and a variety of ulcers.
RanitidineA histamine H2 antagonist used to treat duodenal ulcers, Zollinger-Ellison syndrome, gastric ulcers, GERD, and erosive esophagitis.
FamotidineA histamine H2 receptor antagonist used to treat duodenal ulcers, benign gastric ulcers, GERD, and Zollinger-Ellison syndrome.
MetiamidePotential in the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
Roxatidine 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...
LafutidineLafutidine has been investigated in Peptic Ulcer, Community-acquired Pneumonia, and Gastroesophageal Reflux Disease (GERD).
LavoltidineLavoltidine has been used in trials studying the diagnostic of Reflux, Gastroesophageal and Gastroesophageal Reflux Disease.
NiperotidineNot Annotated
DoxepinA psychotropic agent used for the treatment of depression, anxiety, manic-depressive disorder, and insomnia.
EpinastineAn H1 receptor antagonist used to prevent itching in allergic conjunctivitis.
AsenapineAn atypical antipsychotic used to treat patients with bipolar I disorder and patients with schizophrenia.
MethanthelineFor the treatment of peptic ulcer disease, irritable bowel syndrome, pancreatitis, gastritis, biliary dyskinesia, pylorosplasm, and reflex neurogenic bladder in children.
OlanzapineAn antipsychotic drug used in the management of schizophrenia, bipolar 1 disorder, and agitation associated with these disorders.
PromethazineA first-generation antihistamine used for the treatment of allergic conditions, nausea and vomiting, and motion sickness.
ViloxazineA selective norepinephrine reuptake inhibitor indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in adults in children.
Drugs & Drug Targets
DrugTargetType
CimetidineHistamine H2 receptortarget
CimetidineCytochrome P450 1A2enzyme
CimetidineCytochrome P450 2D6enzyme
CimetidineCytochrome P450 2C19enzyme
CimetidineCytochrome P450 3A4enzyme
CimetidineCytochrome P450 3A5enzyme
CimetidineP-glycoprotein 1transporter
CimetidineSolute carrier family 22 member 2transporter
CimetidineSolute carrier family 22 member 1transporter
CimetidineSolute carrier family 22 member 3transporter
CimetidineSolute carrier family 22 member 5transporter
CimetidineSolute carrier family 22 member 6transporter
CimetidineSolute carrier family 22 member 8transporter
CimetidineMultidrug and toxin extrusion protein 1transporter
CimetidineSolute carrier family 22 member 4transporter
CimetidineSolute carrier family 22 member 11transporter
CimetidineSolute carrier family 22 member 7transporter
CimetidineCytochrome P450 11B1, mitochondrialenzyme
CimetidineCytochrome P450 2C8enzyme
CimetidineCytochrome P450 2C9enzyme
CimetidineCytochrome P450 2E1enzyme
CimetidineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
CimetidineDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
CimetidineBile salt export pumptransporter
CimetidineMultidrug and toxin extrusion protein 2transporter
CimetidineSerum albumincarrier
NizatidineHistamine H2 receptortarget
NizatidineP-glycoprotein 1transporter
NizatidineCholinesteraseenzyme
RanitidineHistamine H2 receptortarget
RanitidineCytochrome P450 1A2enzyme
RanitidineCytochrome P450 2D6enzyme
RanitidineSolute carrier family 22 member 1transporter
RanitidineP-glycoprotein 1transporter
RanitidineSolute carrier family 22 member 8transporter
RanitidineCytochrome P450 3A4enzyme
RanitidineAcetylcholinesterasetarget
RanitidineSolute carrier family 22 member 2transporter
RanitidineAcetylcholinesteraseenzyme
FamotidineHistamine H2 receptortarget
FamotidineSolute carrier family 22 member 2transporter
FamotidineSolute carrier family 22 member 8transporter
FamotidineMultidrug and toxin extrusion protein 1transporter
FamotidineCytochrome P450 1A2enzyme
FamotidineSolute carrier family 22 member 6transporter
MetiamideHistamine H2 receptortarget
Roxatidine acetateHistamine H2 receptortarget
NiperotidineHistamine H2 receptortarget
DoxepinSodium-dependent serotonin transportertarget
DoxepinSodium-dependent noradrenaline transportertarget
DoxepinHistamine H1 receptortarget
DoxepinHistamine H2 receptortarget
DoxepinCytochrome P450 2D6enzyme
DoxepinMuscarinic acetylcholine receptor M1target
DoxepinMuscarinic acetylcholine receptor M2target
DoxepinMuscarinic acetylcholine receptor M3target
DoxepinMuscarinic acetylcholine receptor M4target
DoxepinMuscarinic acetylcholine receptor M5target
DoxepinAlpha-1A adrenergic receptortarget
Doxepin5-hydroxytryptamine receptor 1Atarget
Doxepin5-hydroxytryptamine receptor 2Atarget
DoxepinCytochrome P450 2C19enzyme
DoxepinCytochrome P450 2C9enzyme
DoxepinCytochrome P450 1A2enzyme
DoxepinP-glycoprotein 1transporter
Doxepin5-hydroxytryptamine receptor 2Btarget
Doxepin5-hydroxytryptamine receptor 2Ctarget
DoxepinAlpha-1B adrenergic receptortarget
DoxepinAlpha-1D adrenergic receptortarget
DoxepinCytochrome P450 3A4enzyme
Doxepin5-hydroxytryptamine receptor 6target
DoxepinHistamine H4 receptortarget
DoxepinPotassium voltage-gated channel subfamily H member 2target
DoxepinSerum albumincarrier
DoxepinAlpha-1-acid glycoprotein 1carrier
EpinastineHistamine H1 receptortarget
EpinastineHistamine H2 receptortarget
EpinastineAlpha-1A adrenergic receptortarget
EpinastineAlpha-2A adrenergic receptortarget
Epinastine5-hydroxytryptamine receptor 2Atarget
Epinastine5-hydroxytryptamine receptor 7target
EpinastineP-glycoprotein 1transporter
EpinastineCytochrome P450 2B6enzyme
EpinastineCytochrome P450 2D6enzyme
EpinastineCytochrome P450 3A4enzyme
Asenapine5-hydroxytryptamine receptor 1Atarget
Asenapine5-hydroxytryptamine receptor 1Btarget
Asenapine5-hydroxytryptamine receptor 2Atarget
Asenapine5-hydroxytryptamine receptor 2Btarget
Asenapine5-hydroxytryptamine receptor 2Ctarget
Asenapine5-hydroxytryptamine receptor 6target
Asenapine5-hydroxytryptamine receptor 7target
AsenapineAlpha-2A adrenergic receptortarget
AsenapineAlpha-2B adrenergic receptortarget
AsenapineAlpha-2C adrenergic receptortarget
AsenapineAlpha-1A adrenergic receptortarget
AsenapineDopamine D1 receptortarget
AsenapineDopamine D2 receptortarget
AsenapineDopamine D3 receptortarget
AsenapineDopamine D4 receptortarget
AsenapineHistamine H1 receptortarget
AsenapineHistamine H2 receptortarget
AsenapineCytochrome P450 1A2enzyme
AsenapineCytochrome P450 2D6enzyme
Asenapine5-hydroxytryptamine receptor 5Atarget
AsenapineUDP-glucuronosyltransferase 1-4enzyme
AsenapineCytochrome P450 3A4enzyme
AsenapineBeta-1 adrenergic receptortarget
AsenapineBeta-2 adrenergic receptortarget
AsenapineSerum albumincarrier
Asenapinealpha1-acid glycoproteincarrier
MethanthelineMuscarinic acetylcholine receptor M1target
MethanthelineHistamine H2 receptortarget
MethanthelineMuscarinic acetylcholine receptor M2target
MethanthelineMuscarinic acetylcholine receptor M3target
MethanthelineMuscarinic acetylcholine receptor M4target
MethanthelineMuscarinic acetylcholine receptor M5target
MethanthelineAcetylcholinesteraseenzyme
OlanzapineDopamine D1 receptortarget
OlanzapineMuscarinic acetylcholine receptor M1target
OlanzapineMuscarinic acetylcholine receptor M3target
Olanzapine5-hydroxytryptamine receptor 2Atarget
OlanzapineDopamine D4 receptortarget
OlanzapineHistamine H1 receptortarget
OlanzapineMuscarinic acetylcholine receptor M4target
OlanzapineMuscarinic acetylcholine receptor M2target
OlanzapineDopamine D2 receptortarget
Olanzapine5-hydroxytryptamine receptor 2Ctarget
OlanzapineDopamine D3 receptortarget
OlanzapineAlpha-1B adrenergic receptortarget
OlanzapineCytochrome P450 1A2enzyme
Olanzapine5-hydroxytryptamine receptor 3Atarget
Olanzapine5-hydroxytryptamine receptor 6target
OlanzapineAlpha-1A adrenergic receptortarget
OlanzapineDopamine D5 receptortarget
OlanzapineSerum albumincarrier
OlanzapineAlpha-1-acid glycoprotein 1carrier
OlanzapineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
OlanzapineCytochrome P450 2D6enzyme
OlanzapineP-glycoprotein 1transporter
OlanzapineCytochrome P450 2C19enzyme
OlanzapineD(1) dopamine receptortarget
OlanzapineBeta adrenergic receptortarget
Olanzapine5-hydroxytryptamine receptor 1target
OlanzapineGABA(A) Receptor Benzodiazepine Binding Sitetarget
OlanzapineCytochrome P450 2C9enzyme
OlanzapineUDP-glucuronosyltransferase 1-4enzyme
OlanzapineCytochrome P450 3A4enzyme
OlanzapineCytochrome P450 3A Subfamilyenzyme
PromethazineDopamine D2 receptortarget
PromethazineHistamine H1 receptortarget
PromethazineMuscarinic acetylcholine receptor M4target
PromethazineMuscarinic acetylcholine receptor M1target
PromethazineMuscarinic acetylcholine receptor M5target
PromethazineMuscarinic acetylcholine receptor M2target
PromethazineMuscarinic acetylcholine receptor M3target
PromethazineCalmodulintarget
PromethazineCytochrome P450 2D6enzyme
PromethazineCytochrome P450 2B6enzyme
PromethazineP-glycoprotein 1transporter
PromethazineCytochrome P450 2C9enzyme
PromethazineHistamine H2 receptortarget
PromethazineAlpha adrenergic receptortarget
PromethazineP2 Purinoceptorstarget
PromethazineVoltage-gated sodium channel alpha subunittarget
PromethazineVoltage-gated Potassium Channelstarget
PromethazineCanalicular multispecific organic anion transporter 2transporter
PromethazineMultidrug resistance-associated protein 4transporter
PromethazineSerum albumincarrier
ViloxazineSodium-dependent noradrenaline transportertarget
ViloxazineCytochrome P450 1A2enzyme
ViloxazineCytochrome P450 2D6enzyme
ViloxazineUDP-glucuronosyltransferase 1-9enzyme
ViloxazineUDP-glucuronosyltransferase 2B15enzyme
ViloxazineCytochrome P450 2B6enzyme
ViloxazineCytochrome P450 3A4enzyme
ViloxazineCytochrome P450 3A5enzyme
ViloxazineMultidrug and toxin extrusion protein 1transporter
Viloxazine5-hydroxytryptamine receptor 2Btarget
Viloxazine5-hydroxytryptamine receptor 2Ctarget
ViloxazineAlpha-1B adrenergic receptortarget
ViloxazineBeta-2 adrenergic receptortarget
ViloxazineAmine oxidase [flavin-containing] Atarget
ViloxazineAmine oxidase [flavin-containing] Btarget
ViloxazineHistamine H1 receptortarget
ViloxazineHistamine H2 receptortarget
ViloxazineMuscarinic acetylcholine receptor M1target
ViloxazineMuscarinic acetylcholine receptor M2target
ViloxazineMuscarinic acetylcholine receptor M3target
ViloxazineMuscarinic acetylcholine receptor M4target