Betahistine: A retrospective synopsis of safety data

Drug Safety

Volumn 29, Issue 11, 2006, Pages 1049-1059

  Jeck Thole, Sabine ^a   Wagner, Wolfgang ^a  

^a Solvay Pharmaceuticals GmbH   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ALCOHOL; ASCORBIC ACID; BETAHISTINE; CELECOXIB; CETIRIZINE; HISTAMINE; OMEPRAZOLE; PLACEBO; POTASSIUM BICARBONATE; POTASSIUM CHLORIDE; PROCHLORPERAZINE; ROFECOXIB; TERFENADINE;

ABDOMINAL PAIN; ANAPHYLAXIS; ANGIONEUROTIC EDEMA; ASTHMA; BALANCE DISORDER; BENIGN TUMOR; BLOOD DISEASE; BREAST DISEASE; BRONCHOSPASM; BURNING SENSATION; CONGENITAL DISORDER; CONNECTIVE TISSUE DISEASE; COUGHING; DIZZINESS; DRUG ABSORPTION; DRUG EFFECT; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG INTOXICATION; DRUG METABOLISM; DRUG OVERDOSE; DRUG SAFETY; DRUG WITHDRAWAL; DYSPNEA; EAR DISEASE; EDEMA; ENDOCRINE DISEASE; ERYTHEMA; EYE DISEASE; FACE EDEMA; FAMILIAL DISEASE; FATALITY; GASTRIC ULCER BLEEDING; GASTROINTESTINAL DISEASE; GASTROINTESTINAL HEMORRHAGE; GASTROINTESTINAL SYMPTOM; GENETIC DISORDER; GENITAL SYSTEM DISEASE; GYNECOLOGIC DISEASE; HEADACHE; HEART DISEASE; HEMATEMESIS; HEPATOBILIARY DISEASE; HUMAN; HYPESTHESIA; IMMUNOPATHOLOGY; IMPATIENCE; INFECTION; INFESTATION; INNER EAR DISEASE; INSOMNIA; IRRITABILITY; KIDNEY DISEASE; LIVER FAILURE; LYMPHATIC SYSTEM DISEASE; MACULOPAPULAR RASH; MALIGNANT NEOPLASTIC DISEASE; MEDIASTINUM DISEASE; MENIERE DISEASE; MENTAL DISEASE; METABOLIC DISORDER; MIGRAINE WITHOUT AURA; MOUTH EDEMA; MUSCULOSKELETAL DISEASE; NAUSEA AND VOMITING; NEOPLASM; NEUROLOGIC DISEASE; NONHUMAN; NUTRITIONAL DISORDER; OCULAR PRURITUS; PAPULAR RASH; PARESTHESIA; PERIPHERAL EDEMA; PERSONALITY DISORDER; PHEOCHROMOCYTOMA; POSTMARKETING SURVEILLANCE; PREGNANCY DISORDER; PRIORITY JOURNAL; PRURITUS; RASH; RECOMMENDED DRUG DOSE; RECTUM HEMORRHAGE; RESPIRATORY TRACT DISEASE; RESTLESSNESS; REVIEW; SIDE EFFECT; SKIN ALLERGY; SPONTANEOUS ABORTION; STEVENS JOHNSON SYNDROME; SWELLING; TENSION HEADACHE; THORAX DISEASE; TONGUE SWELLING; TREMOR; UNSPECIFIED SIDE EFFECT; URTICARIA; URTICARIA PIGMENTOSA; VASCULAR DISEASE; VERTIGO; VESTIBULAR DISORDER; WEIGHT REDUCTION; WHEEZING;

ADVERSE DRUG REACTION REPORTING SYSTEMS; BETAHISTINE; DRUG INTERACTIONS; HUMANS; MENIERE'S DISEASE; PRODUCT SURVEILLANCE, POSTMARKETING; RETROSPECTIVE STUDIES; VERTIGO;

EID: 33845494270     PISSN: 01145916     EISSN: None     Source Type: Journal    
DOI: 10.2165/00002018-200629110-00004     Document Type: Review

References (38)

1. Sheldon CH, Horton BT. Treatment of Meniere's disease with histamine administered intravenously. Proc Staff Meet Mayo Clin 1940; 15: 17-21
2. Hill SJ, Ganellin CR, Timmerman H, et al. International Union of Pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev 1997; 49: 253-77
3. 4) expressed in bone marrow. Mol Pharmacol 2001; 59: 420-6
4. Arrang JM, Garbarg M, Quach TT, et al. Actions of betahistine at histamine receptors in the brain. Eur J Pharmacol 1985; 111: 73-84
5. Ganellin CR. Chemistry structure-activity relationship of drugs acting at histamine receptors. In: Ganellin CP, Parsons ME, editors. Pharmacology of histamine receptors. Bristol: Wright PSG, 1982: 10-102
6. 2 receptors for histamine. Agents Actions 1986; 18: 342-50
7. Curwain BP, Holton P, Spencer J. The effect of betahistine on gastric acid secretion and mucosal blood flow in conscious dogs. Br J Pharmacol 1972; 46: 351-4
8. Woodward DF, Ledgard SE. Histamine induced microvascular permeability increases in hamster skin: a response predominantly mediated by H2-receptors. Agents Actions 1986; 18: 504-7
9. West RE, Zweig A, Shih NY, et al. Identification of two H3-histamine receptor subtypes. Mol Pharmacol 1990; 38: 610-3
10. Laurikainen EL, Miller JM, Nuttall AL. The vascular mechanism of action betahistine in the inner ear of the guinea pig. Eur Arch Otorhinolaryngol 1998; 255: 119-23
11. Dziadziola JK, Laurikainen EL, Rachel JD. Betahistine increases vestibular blood flow. Otolaryngol Head Neck Surg 1999; 120: 400-5
12. Soto E, Chávez H, Valli P, et al. Betahistine produces post-synaptic inhibition of the excitability of the primary neurons in the vestibular endorgans. Acta Otolaryngol Suppl 2001; 545: 19-24
13. Lacour M, Sterkers O. Histamine and betahistine in the treatment of vertigo: elucidation of mechanisms of action. CNS Drugs 2001; 15 (11): 853-70
14. Tighilet B, Trottier S, Mourre C, et al. Betahistine dihydrochloride interaction with the histaminergic system in the cat: neurochemical and molecular mechanisms. Eur J Pharmacol 2002; 20: 63-73
15. Botta L, Mira E, Valli S, et al. Effects of betahistine and of its metabolites on vestibular sensory organs. Acta Otorhinolaryngol Ital 2001; 21 (3 Suppl. 66): 24-30
16. Chen XY, Zhong DF, Duan JL, et al. LC-MS-MS analysis of 2-pyridylacetic acid, a major metabolite of betahistine: application to a pharmacokinetic study in healthy volunteers. Xenobiotica 2003; 33: 1261-71
17. Reilly MA, Schayer RW. Further studies on histamine catabolism in vivo. Br J Pharmacol 1971; 43: 349-58
18. Colletti V. Medical treatment in Meniere's disease: avoiding vestibular neurectomy and facilitating postoperative compensation. Acta Otolaryngol 2000, Suppl. 544: 27-33
19. Mira E, Guidetti G, Ghilardi PL, et al. Betahistine dihydrochloride in the treatment of peripheral vestibular vertigo. Eur Arch Otorhinolaryngol 2003 Feb; 260 (2): 73-7. Epub 2002 Sep 11
20. Albera R, Ciuffolotti R, Di Cicco M, et al. Double-blind, randomized, multicentre study comparing the effect of betahistine and fluranizine on the Dizziness Handicap in patients with recurrent vestibular vertigo. Acta Otolaryngol 2003, 260: 73-7
21. Gordon CR, Shupak A. Prevention and treatment of motion sickness in children. CNS Drugs 1999, 12: 369-81
22. Chistyakova VR. The role of betaserk in combined treatment of neurosensory hypoacusis and vestibulopathy in childhood. Bulletin of otorhinolaryngology 2004, 2: 9-12
23. Code of Federal Regulations. Title 21, Chapter 1. Food and Drug Administration, Department of Health and Human Services. Part 312.32. IND Safety Reports: revised 1 April 2002
24. WHO Collaborating Centre for Drug Statistics Methodology [online]. About the ATC/DDD system. Available from URL: http://www.whocc.no/atcddd/atcsystem. html [Accessed 2006 Mar 18]
25. Beeley L, Cunningham H, Brennan A. Betahistine and terfenadine. In: Stockley IH. Drug interactions. 5th Ed. London: Pharmaceutical Press, 2000: 779
26. CIOMS. Guidelines for preparing core clinical safety information on drugs. Report from CIOMS working group III. Genf WHO, 1995
27. Wilson AM, Thabane L, Holbrook A. Application of data mining techniques in pharmacovigilance. Br J Clin Pharmacol 2003; 57: 127-34
28. Biriell C, Edwards R. Reasons for reporting adverse drug reactions: some thoughts based on an international review. Pharmacoepidemiol Drug Saf 1997; 6: 21-6
29. ICH Harmonised Tripartite Guideline. Clinical safety data management: definitions and standards for expedited reporting E2A [online]. Available from URL: http://www.ich.org/LOB/media/MEDIA436.pdf [Acessed 2006 Mar 18]
30. Davies AG, Stonier PD. Development of medicines: full development. In: Griffin JP, O'Grady J, editors. The textbook of pharmaceutical medicine. London: BMJ, 2003: 395-420
31. de Abajo FJ, Montero D, Madurga M, et al. Acute and clinically relevant drug-induced liver injury: a population based case-control study. Br J Clin Pharmacol 2004; 58: 71-80
32. Dendorfer A, Fitschen M, Raasch W, et al. Mechanisms of bradykynin-induced catecholamine release in pithed spontaneously hypertensive rats. Immunopharmacology 1999; 44: 99-104
33. Prys-Roberts C. Phaeochromocytoma: recent progress in its management. Br J Anaesth 2000; 85: 44-57
34. Schneider D, Kießling B, Wieczorek M, et al. Influence of 3 antivertiginous medications on the vigilance of healthy volunteers. Int J Clin Pharmacol Ther 2003; 41: 171-81
35. Waggoner WC. Pharmacology and toxicology of Serc (betahistine hydrochloride). Report Unimed Inc Feb. 1970
36. Betts T, Harris D, Gadd E. The effect of two anti-vertigo drugs (betahistine and prochlorperazine) on driving skills. Br J Pharmacol 1991; 32: 455-8
37. Kohno S, Nakao S, Ogawa K, et al. Possible participation of histamine H3-receptors in the regulation of anaphylactic histamine release from isolated rat peritoneal mast cells. Jpn J Pharmacol 1994; 66: 173-80
38. Chistyakova VR. The role of betaserk in combined treatment of neurosensory hypoacusis and vestibulopathy in childhood. Vestn Otorinolaringol 2004; 2: 9-12