Betahistine
JFDA label: Betastin 16mg Tab
Mechanism of Action
Antagonist of Histamine H3 receptor — Histamine H3 receptor antagonist; Agonist of Histamine H1 receptor — Histamine H1 receptor agonist
| Target | Action | Gene / class |
|---|---|---|
| Histamine H1 receptor efficacy | AGONIST | HRH1 |
| Histamine H3 receptor efficacy | ANTAGONIST | HRH3 |
Indications
Approved
- Ménière disease
Contraindications
Source: Lexicomp
- Hypersensitivity to betahistine or any component of the formulation Absolute
- pheochromocytoma Absolute
- presence or history of active peptic ulcer disease Absolute
Adverse Reactions
Cardiac disorders (3)
Not Known Hypotension (including orthostatic and postural hypotension) · tachycardia · ventricular premature contractions (case reports)
Nervous system disorders (6)
Common Headache
Not Known Confusion · convulsions · drowsiness (case reports) · hallucination · paraesthesia
Immune system disorders (3)
Not Known Anaphylaxis · angioedema · hypersensitivity reaction
Gastrointestinal disorders (7)
Common dyspepsia · Nausea
Not Known Abdominal distension · abdominal pain · bloating · peptic ulcer (including exacerbation of previous disease) · vomiting
Skin and subcutaneous tissue disorders (4)
Not Known Pruritus · skin rash · Stevens-Johnson syndrome · urticaria
Respiratory, thoracic and mediastinal disorders (1)
Not Known Dyspnea
Dosing
Source: Lexicomp
Warnings & Precautions
Source: Lexicomp
Asthma
Use with caution; clinical intolerance has been reported in a few asthmatic patients.
Cardiovascular disease
Use with caution in patients with cardiovascular disease; post-market cases of ventricular extrasystoles, hypotension, and tachycardia have been reported during use.
Hepatic impairment
Use with caution; primarily undergoes hepatic metabolism.
Peptic ulcer
Exacerbation of symptoms has been observed in patients with a history of peptic ulcer; use is contraindicated in the presence or history of peptic ulcer.
Pregnancy & Lactation
Pregnancy
Adverse events were observed in some animal reproduction studies.
Lactation
It is not known if betahistine is present in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Chemistry & Properties
| Formula | C8H12N2 |
|---|---|
| Molecular weight | 136.2 g/mol |
| IUPAC name | N-methyl-2-pyridin-2-ylethanamine |
| CAS | 5638-76-6 |
| PubChem CID | 2366 |
| InChIKey | UUQMNUMQCIQDMZ-UHFFFAOYSA-N |
| logP | 0.84 (XLogP 0.4) |
| Polar surface area | 24.92 Ų |
| H-bond acceptors / donors | 2 / 1 |
| Drug-likeness (QED) | 0.67 |
| Lipinski violations | 0 |
SMILES
CNCCc1ccccn1Biology & Pharmacokinetics
Pharmacokinetics
| BBB penetrant | Yes (logBB -0.3) |
|---|
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP2C19 | Substrate | — |
| CYP2D6 | Substrate | — |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Registered Products (41)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Vasoserc | Tablet 8 mg | 30 tab | Sun Set Drug Store | 2.130 |
| Joswe Mezan | Tablet 8 mg | 30 tab pack varies | Jordan Sweden Medical & Sterilization Co. | 2.270 |
| Vertiloc | Tablet 16.00 mg | 20 tab pack varies | Itqan Pharmaceutical Industries/Jordan | 2.620 |
| Vasoserc BID | Tablet 24 mg | 30 tab | Sun Set Drug Store | 2.940 |
| Vasoserc Forte | Tablet 16 mg | 30 tab | Sun Set Drug Store | 2.940 |
| Anatax | Tablet 24 mg | 30 tab | UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN | 3.500 |
| Betastin | Tablet 16 mg | 30 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 3.600 |
| Lavistina | Tablet 16.0 mg | 40 tab | Sukhtian Group | 3.610 |
| Joswe Mezan | Tablet 16 mg | 30 tab pack varies | Jordan Sweden Medical & Sterilization Co. | 3.720 |
| Anatax | Tablet 8 mg | 60 tab | UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN | 3.740 |
| Vertiloc | Tablet 24.00 mg | 30 tab pack varies | Itqan Pharmaceutical Industries/Jordan | 3.740 |
| Joswe Mezan | Tablet 8 mg | 60 tab pack varies | Jordan Sweden Medical & Sterilization Co. | 4.320 |
| Verotec | Tablet 8 mg | 60 tab pack varies | THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN | 4.460 |
| Verotec | Tablet 8 mg | 1500 tab pack varies | THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN | 4.460 |
| Vertiloc | Tablet 8 mg | 60 tab pack varies | Itqan Pharmaceutical Industries/Jordan | 4.570 |
| Plantine | Tablet 8 mg | 60 tab | Dar Al Dawa Development and Investment Co Ltd/Jordan | 4.900 |
| Lavistina | Tablet 8.0 mg | 100 tab | Sukhtian Group | 5.230 |
| Verotec | Tablet 16 mg | 50 tab pack varies | THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN | 5.840 |
| Verotec 24 | Tablet 24 mg | 50 tab | THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN | 5.840 |
| Betastin | Tablet 16 mg | 50 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 6.000 |
| Betastin | Tablet 24 mg | 50 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 6.000 |
| Anatax | Tablet 16 mg | 60 tab | UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN | 6.130 |
| Vertiloc | Tablet 16.00 mg | 50 tab pack varies | Itqan Pharmaceutical Industries/Jordan | 6.240 |
| Vertiloc | Tablet 24.00 mg | 50 tab pack varies | Itqan Pharmaceutical Industries/Jordan | 6.240 |
| Vertiloc | Tablet 8 mg | 100 tab pack varies | Itqan Pharmaceutical Industries/Jordan | 6.250 |
| BE-Stedy | Tablet 16 mg | 100 tab | AL Rahma Drug Store | 6.400 |
| BE-STEDY | Tablet 8 mg | 100 tab | AL Rahma Drug Store | 6.500 |
| Dizivert | Tablet 16.0 mg | 60 tab | SAVVY PHARMA/JORDAN | 6.640 |
| Dizivert | Tablet 8.0 mg | 100 tab | Savvy Pharms | 6.750 |
| Betastin | Tablet 16 mg | 60 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 6.850 |
| Betastin | Tablet 24 mg | 60 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 6.850 |
| Joswe Mezan | Tablet 16 mg | 60 tab pack varies | Jordan Sweden Medical & Sterilization Co. | 7.080 |
| Betaserc Tab | Tablet 8 mg | 100 tab | Abu Sheikha Drug Store | 7.390 |
| Vertiloc | Tablet 16.00 mg | 60 tab pack varies | Itqan Pharmaceutical Industries/Jordan | 7.490 |
| Plantine | Tablet 16 mg | 60 tab | Dar Al Dawa Development and Investment Co Ltd/Jordan | 8.040 |
| Dizivert | Tablet 24.0 mg | 60 tab | SAVVY PHARMA/JORDAN | 9.230 |
| Betaserc Tab | Tablet 16 mg | 60 tab | Abu Sheikha Drug Store | 10.510 |
| Betastin | Tablet 16 mg | 100 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 11.420 |
| Betastin | Tablet 24 mg | 100 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 11.420 |
| BE-STEDY | Tablet 24 mg | 100 tab | AL Rahma Drug Store | 12.880 |
| Verotec | Tablet 16 mg | 900 tab pack varies | THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN | 90.400 |