Histamine is a biological mediator used in physiological and pathological processes. Histamine plays an important role in inflammation, gastric acid secretion, immune responses, smooth muscle contractions and as a neurotransmitter. Endogenous histamine is synthesized in all tissues and is stored primarily in the granules of mast cells or basophils. Historically histamine is best known as a mediator of allergic reactions and inflammation, but it's function as a immunostimulant is being further investigated. Histamine dihydrochloride is a topical analgesic used for minor aches and pains of muscles and joints. It is also being researched as an orphan drug for the adjunctive treatment of acute myeloid leukemia or malignant melanoma.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Topical Administration
-Apply a thin layer to pain site and massage into skin until thoroughly absorbed.
-Wash hand before and after applying, unless hands are a treated area.
-Do not apply to open skin wounds, infections, or exfoliative dermatitis.
-Do not bandage tightly or use with a heating pad.
If a rash (unspecified) occurs while using histamine dihydrochloride, discontinue use and consult your healthcare professional.
Do not apply histamine dihydrochloride to areas with skin abrasion, skin irritation, skin infection, wounds or otherwise ldamaged skin due to the potential for enhanced absorption. Do not tightly wrap or bandage the treated area or use with a heating pad. Ophthalmic administration should be avoided; rinse thoroughly if ocular exposure occurs.
The effects of histamine dihydrochloride during pregnancy are not known. The manufacturer recommends discussing the use of this product with your healthcare professional if you are pregnant or wish to become pregnant.
The effects of histamine dihydrochloride during breast-feeding are not known. The manufacturer recommends discussing the use of this product with your healthcare professional if you are breast-feeding.
For the treatment of mild aches and mild pain of muscles (myalgia) and joints (arthralgia) associated with arthritis, uncomplicated backaches, strains, and bruises:
Topical dosage:
Adults and Adolescents: Apply to the affected area 3 to 4 times daily. Gently massage until the medication is thoroughly absorbed into the skin. Discontinue use and consult a health care provider if condition worsens, if symptoms persist more than 7 days, or if symptoms clear up, and then recur within a few days.
Maximum Dosage Limits:
-Adults
4 topical applications/day.
-Geriatric
4 topical applications/day.
-Adolescents
4 topical applications/day.
-Children
Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Histamine Dihydrochloride products.
Histamine is a ubiquitous biogenic amine that is synthesized by mast cells, basophils, platelets, and enterochromaffin cells, where it is stored in intracellular granules and is secreted on stimulation. There are four known G protein-coupled receptors (GPCR) found on target cells in various tissues for histamine to bind, H1, H2, H3, and H4. Each receptor exerts a different response to the body, including vasodilation, tachycardia, endothelial permeability, increased mucus secretion, smooth muscle constriction, increased gastric acid secretion, neurotransmitter release and possibly immunostimulatory effects. Histamine dihydrochloride, when applied topically, causes vasodilation at the site of application allowing for more blood to reach the site, enabling the body to heal more effectively. There is limited scientific evidence supporting this claim.
Histamine dihydrochloride is administered topically. Pharmacokinetic data after topical administration of histamine is not available from the manufacturer.
-Route-Specific Pharmacokinetics
Topical Route
Pharmacokinetic data after topical administration of histamine dihydrochloride is not available from the manufacturer.