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Betahistine dihydrochloride

Betahistine dihydrochloride
Betahistine dihydrochloride structure
CAS No.
5579-84-0
Chemical Name:
Betahistine dihydrochloride
Synonyms
PT-9;Serc;Betaserc;Microser;SinMenier;BetahistineHCl;Betahistine 2 hcl;Betahistine Di HCl;Betahistine dihydroc;BETAHISTINE HYDROCHLORIDE
CBNumber:
CB8390055
Molecular Formula:
C8H14Cl2N2
Formula Weight:
209.12
MOL File:
5579-84-0.mol

Betahistine dihydrochloride Properties

Melting point:
150-154 °C
storage temp. 
2-8°C
solubility 
Very soluble in water, soluble in ethanol (96 per cent), practically insoluble in 2propanol.
form 
powder
CAS DataBase Reference
5579-84-0(CAS DataBase Reference)
EWG's Food Scores
1
FDA UNII
49K58SMZ7U
SAFETY
  • Risk and Safety Statements
Safety Statements  24/25
WGK Germany  3
RTECS  UT2969000
HS Code  29333990
NFPA 704
1
2 1

Betahistine dihydrochloride price More Price(41)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich B4638 Betahistine dihydrochloride ≥98% 5579-84-0 5g $69.5 2021-12-16 Buy
Sigma-Aldrich Y0000391 Betahistine dihydrochloride European Pharmacopoeia (EP) Reference Standard 5579-84-0 $190 2021-12-16 Buy
Sigma-Aldrich 1065618 Betahistine hydrochloride United States Pharmacopeia (USP) Reference Standard 5579-84-0 200mg $366 2021-12-16 Buy
Cayman Chemical 27602 Betahistine (hydrochloride) 5579-84-0 10g $75 2021-12-16 Buy
Cayman Chemical 27602 Betahistine (hydrochloride) 5579-84-0 5g $56 2021-12-16 Buy

Betahistine dihydrochloride Chemical Properties,Uses,Production

Description

Betahistine dihydrochloride (BH.2HCl) is an orally active histamine analog which has been used to control vertigo, lack of hearing and tinnitus related to Ménière’s disease. The mechanism of BH.2HCl is to reduce the pressure of the membranous labyrinth that results in enhancement of the microvasculature circulation and improves the signs of Ménière’s disease. Peroral administration undergoes extensive first-pass metabolism and gastric irritation in patients with peptic ulcer. In treatment of vertigo, a uniform and constant supply of drug is required in order to maintain steady-state concentration of the drug in the body. Unfortunately, BH.2HCl possesses a short half-life of about 3–4 h and requires frequent administration of the drug,12–15 thereby making it an ideal candidate for controlled release preparations.

Chemical Properties

white to light yellow crystalline powder

Uses

Betahistine is belongs to a group of medications used to treat vertigo associated with Ménière's disease. Vertigo is a condition that causes sufferers to have a sensation of rotation or movement of themselves or their surroundings. Ménière's disease is a disorder of the inner ear that causes vertigo in addition to symptoms such as ringing in the ears, headache, and loss of hearing.
Betahistine is used to reduce the number of episodes of vertigo associated with Ménière's disease. It is believed to work by decreasing the pressure in the ear. This pressure is believed to contribute to the sense of dizziness, nausea, and ringing in the ears and hearing loss that people with Ménière's disease experience.

Uses

therapeutic for thrombocytopenia, effective against idiopathic thrombocytopenic purpura and cirrhosis due to hepatitis C.

brand name

Serc (Unimed).

General Description

Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards

Pharmacokinetics

Absorption:
Betahistine dihydrochloride is readily and almost completely absorbed after oral administration from all parts of the gastro-intestinal tract, and peak plasma concentrations of 14C-labelled betahistine dihydrochloride are attained one hour after oral administration to fasting subjects.After absorption, the drug is rapidly and almost completely metabolized into 2-pyridylacetic acid. Plasma levels of betahistine are very low. Pharmacokinetic analyses are therefore based on 2-PAA measurements in plasma and urine.
Under fed conditions Cmax is lower compared to fasted conditions. However, total absorption of betahistine is similar under both conditions, indicating that food intake only slows down the absorption of betahistine.
Distribution:
The percentage of betahistine that is bound by blood plasma proteins is less than 5 %.
Biotransformation:
After absorption, betahistine is rapidly and almost completely metabolized into 2-PAA (which has no pharmacological activity). After oral administration of betahistine the plasma (and urinary) concentration of 2-PAA reaches its maximum 1 hour after intake and declines with a half-life of about 3.5 hours.
Excretion:
2-PAA is readily excreted in the urine. In the dose range between 8 and 48 mg, about 85% of the original dose is recovered in the urine. Renal or faecal excretion of betahistine itself is of minor importance.
Betahistine dihydrochloride is eliminated by the kidney with 85 - 90% of the radioactivity of an 8 mg dose appearing in the urine over 56 hours. Maximum excretion rates are reached within 2 hours of administration. Plasma levels of the parent drug are below the limits of detection of the assay.
Bioavailability has therefore been assessed from urinary excretion of its main metabolite, 2-pyridylacetic acid.
There is no evidence for presystemic metabolism. Biliary excretion is not important as a route of elimination of either the drug or its metabolites in the rat and is unlikely to be so in man.
Linearity:
Recovery rates are constant over the oral dose range of 8 – 48 mg indicating that the pharmacokinetics of betahistine are linear, and suggesting that the involved metabolic pathway is not saturated.

Side effects

Stomach upset, nausea, and headache may occur. This medication may also rarely cause drowsiness. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including:
rash
itching/swelling (especially of the face/tongue/throat)
severe dizziness
trouble breathing
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Mode of action

Betahistine acts both as a partial histamine H1-receptor agonist and histamine H3-receptor antagonist also in neuronal tissue, and has negligible H2-receptor activity. Betahistine increases histamine turnover and release by blocking presynaptic H3-receptors and inducing H3-receptor downregulation.
Betahistine dihydrochloride is a histamine-like drug in which pharmacological activity can be attributed to a specific effects and/or more direct influences on recovery mechanisms the vestibular nuclei. It has weak agonist activity at histamine H1 receptors and moderate antagonist activity at H3; receptors. The antagonist action of betahistine dihydrochloride at the H3: receptor can be expected to potentiate the release of presynaptic histamine in vivo by blocking the auto-inhibitory feedback at histaminergic terminals, its action on medial vestibular nucleus cells is to significantly reduce their responsiveness to histamine. This action of betahistine dihydrochloride occurs at post-synaptic H1 receptors, since betahistine dihydrochloride lacks any effect at H2 receptors. The effects of betahistine dihydrochloride are thus consistent with a partial agonist action at these receptors, with betahistine dihydrochloride having little excitatory action on its own but reducing the excitatory responses to histamine by occupying H1 receptor sites.

Betahistine dihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products


Betahistine dihydrochloride Suppliers

Global( 270)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Hefei TNJ Chemical Industry Co.,Ltd.
+86-0551-65418679
86-0551-65418697 info@tnjchem.com China 3000 55
career henan chemical co
+86-0371-55982848
sales@coreychem.com China 29954 58
Shenzhen Nexconn Pharmatechs Ltd
15013857715
admin@nexconn.com CHINA 3004 58
Hebei Guanlang Biotechnology Co., Ltd.
+8619930503282
sales3@crovellbio.com China 5941 58
Wuhan Chemwonders Technology Inc.
027-85778276
027-85778276 info@chemwonders.com CHINA 176 58
Xiamen AmoyChem Co., Ltd
+86 592-605 1114
sales@amoychem.com CHINA 6369 58
Shandong chuangyingchemical Co., Ltd.
18853181302
sale@chuangyingchem.com CHINA 5917 58
Shanghai Longyu Biotechnology Co., Ltd.
+8615821988213
+86 15821988213 info@longyupharma.com China 2500 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 37282 58

View Lastest Price from Betahistine dihydrochloride manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2022-01-18 Betahistine dihydrochloride
5579-84-0
US $0.00 / KG 100g 98%+ 100kg WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
2021-12-23 Betahistine dihydrochloride
5579-84-0
US $0.00 / KG 1g 99% 100kg WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
2021-10-20 Betahistine dihydrochloride
5579-84-0
US $58.00-42.00 / KG 1KG 99% 9000kg/per week Hebei Lingding Biological Technology Co., Ltd

Betahistine dihydrochloride Spectrum


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