Histamine diphosphate: Full Drug Profile

Histamine diphosphate - General Information

Histamine stimulates gastric gland secretion, causing an increased secretion of gastric juice of high acidity. This action is probably due mainly to a direct action on parietal and chief gland cells.

Pharmacology of Histamine diphosphate

Histamine stimulates gastric gland secretion, causing an increased secretion of gastric juice of high acidity. This action is probably due mainly to a direct action on parietal and chief gland cells.

Additional information about Histamine diphosphate

Histamine diphosphate Indication

Histamine phosphate is indicated as a diagnostic aid for evaluation of gastric acid secretory function.

Mechanism Of Action

Histamine acts directly on the blood vessels to dilate arteries and capillaries; this action is mediated by both H 1- and H 2-receptors. Capillary dilatation may produce flushing of the face, a decrease in systemic blood pressure, and gastric gland secretion, causing an increased secretion of gastric juice of high acidity. Increased capillary permeability accompanies capillary dilatation, producing an outward passage of plasma protein and fluid into the extracellular spaces, an increase in lymph flow and protein content, and the formation of edema. In addition, histamine has a direct stimulant action on smooth muscle, producing contraction if H 1-receptors are activated, or mostly relaxation if H 2-receptors are activated. Also in humans, the stimulant effect of histamine may cause contraction of the intestinal muscle. However, little effect is noticed on the uterus, bladder, or gallbladder. Histamine has some stimulant effect on duodenal, salivary, pancreatic, bronchial, and lacrimal glands.

Generic Name

Histamine Phosphate

Drug Category

Diagnostic aid

Drug Type

Small Molecule; Approved

Other Brand Names containing Histamine Phosphate

Histamine; Histamine biphosphate; Histamine dihydrogen phosphate; Histamine diphosphate;

Absorption

Readily absorbed after parenteral administration

Toxicity (Overdose)

LD₅₀=807 mg/kg (mouse, oral). Side effects can lead to hypertension, hypotension, headache, dizziness, nervousness and tachycardia. Large overdoses can lead to seizures.

Biotransformation

Primarily hepatic. Histamine is rapidly metabolized by methylation and oxidation. Methylation involves ring methylation and catalyzation by the enzyme histamine-N-methyltransferase, producing N-methylhistamine, which is mostly converted to N-methyl imidazole acetic acid. 2 to 3% excreted as free histamine, 4 to 8% as N-methylhistamine, 42 to 47% as N-methyl imidazole acetic acid, 9 to 11% as imidazole acetic acid, and 16 to 23% as imidazole acetic acid riboside

Dosage Forms of Histamine diphosphate

Liquid Subcutaneous

Chemical IUPAC Name

2-(3H-imidazol-4-yl)ethanamine; phosphoric acid

Chemical Formula

C5H15N3O8P2

Organisms Affected

Humans and other mammals