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Ball-and-stick model of cimetidine, the prototypical H 2 receptor antagonist. H 2 antagonists, sometimes referred to as H2RAs [1] and also called H 2 blockers, are a class of medications that block the action of histamine at the histamine H 2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid.
Famotidine, sold under the brand name Pepcid among others, is a histamine H 2 receptor antagonist medication that decreases stomach acid production. [4] It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. [4]
Since Tums is an over-the-counter drug, it is not considered a pharmaceutical-grade treatment (does not require a prescription). Prescription strength acid reflux medications often contain proton-pump inhibitors (PPI) or histamine H 2 receptor blockers (H 2 blockers, H 2 antagonists).
Both enantiomers are involved in antagonism of the H 1 and α 2-adrenergic receptors, [9] [91] although the (S)-(+) enantiomer is the stronger antihistamine. [ 92 ] Although not clinically relevant, mirtazapine has been found to act as a partial agonist of the κ-opioid receptor at high concentrations ( EC 50 = 7.2 μM).
Proton-pump inhibitors have largely superseded the H 2-receptor antagonists, a group of medications with similar effects but a different mode of action, and heavy use of antacids. [3] A potassium-competitive acid blocker (PCAB) revaprazan was marketed in Korea as an alternative to a PPI.
Ranitidine has 10% of the affinity that cimetidine has to CYP450, so it causes fewer side effects, but other H 2 blockers famotidine and nizatidine have no CYP450 significant interactions. [ 131 ] Ranitidine was introduced in 1981, and was the world's biggest-selling prescription drug by 1987. [ 132 ]
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Heart failure may be worsened with nondihydropyridine calcium channel blockers, the alpha blocker doxazosin, and the alpha-2 agonists moxonidine and clonidine. On the other hand, β-blockers, diuretics, ACEis, ARBs, and aldosterone receptor antagonists have been shown to improve outcome. [67] Pregnancy. Although α-methyldopa is generally ...