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2 vertin

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2 vertin

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2 vertin

  1. 1. 1 MANAGEMENT OF VERTIGO
  2. 2. 2 Management of vertigo Pharmacotherapy Adaptation exercises Surgery
  3. 3. 3 A Vertigo Patient I WANT .. Fewer attacks every month Attacks should not be as bad as before Attacks should not last long
  4. 4. 4 Pharmacotherapy (Antivertigo drugs) Vasodilators Antiemetics Labyrinthine sedatives Anxiolytics Diuretics
  5. 5. 5 Anti- emetics Antihistamines Anti Phenothiazines Miscellaneous Cholinergics Large overlap between the effects produced by antihistamines, anticholinergics and phenothiazines.
  6. 6. 6 Phenothiazines (Prochlorperazine, Thiethylperazine) Prochlorperazine is less sedating than some other phenothiazines but drowsiness still occurs Also causes hypotension, Parkinsonian side effects --Betts T et al, Brit. J. Clin. Pharmac, 1991, 32, 455-8, --Curley JWA, E N T Journal, 1984, 65, 555-560 “The drug which most commonly causes parkinsonism in general practice is Prochlorperazine” --Chaplin S, Geriatric Medicine, 1989, Feb, 13-14
  7. 7. 7 Anxiolytics (Tranquilizers) (Benzodiazepines such as diazepam, Lorazepam) No effect on the underlying vertigo Helps patient endure the symptoms by allaying anxiety Many side effects drowsiness and sedation, dependence and addiction abuse potential, psychomotor impairment, memory loss, interactions with alcohol Harris T, Ear Nose Throat J, 1984, 65, 551-5
  8. 8. 8 Diuretics (e.g. Furosemide, Hydrochlorthiazide) Used in vertigo and meniere’s disease Reduce the volume of endolymph by promoting urine flow and reducing fluid retention. Use mainly associated with electrolyte imbalance Ludman H, Brit. Med. J., 1981, 282, 454-457, Harris T, Ear Nose Throat J, 1984, 65, 551-5
  9. 9. 9 Cinnarizine, Collin Dollery Therapeutic Drugs, C240-3, Godfraind T et al, Drugs of Today, 1982, XVIII(1), 27-42, Venkataraman S, Neurosciences Today, 1997, Vol. I, 3&4, 205-6, Norre M E, Crit Rev. Phy. Rehab. Med., 1990, 2,2,101-20 Antihistamines Cinnarizine, Flunarizine, Cyclizine Drowsiness and blurred vision (Difficult for patients who drive or operate machinery) Delay normal vestibular compensation process Cinnarizine and Flunarizine act via calcium antagonism, unspecific action may cause side effects Weight gain & depression (serotonergic effects) Extrapyramidal symptoms (dopaminergic effects) G.I. upset
  10. 10. 10 * SOLVAY PHARMA INDIA LTD. Betahistine 8, 16 & 24 mg tablets
  11. 11. 11 Betahistine The original research product of Solvay Available Worldover as Betaserc® Serc® Vasomotal® Urutal® Available in India as Vertin *
  12. 12. 12 Data on file Betahistine Trusted therapy for more than 41 million Vertigo patients worldwide
  13. 13. 13 BETAHISTINE CHEMISTRY & PHARMACOKINETICS
  14. 14. 14 Betahistine - Chemistry Histamine Betahistine N N H CH2CH2NH2 N CH2CH2NHCH3 Histamine analogue, can be given orally with no histamine like side effects Van Cauwenberge P B, et al, Acta Otolaryngol, 1997, suppl. 526, 43-6, Venkataraman S, Neurosciences Today, 1998, II, 1 & 2, 56-8
  15. 15. 15 Betahistine : Pharmacokinetics Oral administration Rapid and complete absorption Mean plasma half life :- 3-4 Hrs. Complete excretion via urine in 24 hours Very low plasma protein binding One metabolite (2-aminoethyl pyridine) is found to be active
  16. 16. 16 BETAHISTINE PHARMACOLOGY MODE OF ACTION
  17. 17. 17 Betahistine : Mode of Action Vascular Effects Neurological Effects (in inner ear & brain) (in brain)
  18. 18. 18 H3-AUTORECEPTORS … CONTROLLING THE RELEASE OF HISTAMINE Adapted Van Cauweneberge PB, Acta Otolaryngol, 1997, suppl. 526, 43-6, Venkataraman S, Neurosciences Today, 1998, II, 1 & 2, 56-8 H1 H2 H3 autoreceptor Histaminergic Neuron
  19. 19. 19 Venkataraman S, Neurosciences Today, 1998, II (1 & 2), 56-8 EFFECTS OF BETAHISTINE
  20. 20. 20 Betahistine - Vascular Effects H3 autoreceptors antagonist H1 agonist Inhibits autoregulation of histamine release Venkataraman S, Neurosciences Today, 1998, II (1 & 2), 56-8 Improves cochlear microcirculation Improves cerebral / vertebrobasilar blood flow
  21. 21. 21 Blocks H3 heteroreceptors Increases release of other neurotransmitters e.g. serotonin Regulates firing activity of vestibular nuclei Venkataraman S, Neurosciences Today, 1998, II (1 & 2), 56-8, Biswas A, Ind. J. Otolaryngol H N S, 1997, 49(2), 179-81 Betahistine - Neurological Effects
  22. 22. 22 Betahistine : Mode of action Blocks H3 heteroreceptors H3 autoreceptors stimulates release of other neurotransmitter e.g. serotonin Stimulates release of histamine Regulatory effect on vestibular nuclei H1 receptor Symptomatic relief of vertigo Prophylactic effect of vertigo improvement of cochlear & cerebral blood flow direct stimulatory effect
  23. 23. 23 BETAHISTINE Therapeutic Indications Vertigo Meniere’s Syndrome Dosage Recommendations 24-48 mg /day
  24. 24. 24 Betahistine -Tolerance No sedation No gastric side effects No anticholinergic effects No extrapyramidal side effects Bradoo RA et al, Ind. J. Otolaryngol HNS, 2000, 52(2), 151-8, Biswas A, Ind. J. Otolaryngol H N S, 1997, 49(2), 179-81
  25. 25. 25 Betahistine: No affinity for H2 receptors H2 receptors predominate in stomach and control gastric secretion Betahistine has no effect on H2 receptors. Betahistine is generally free of gastric side effects Betahistine, Collin Dollery Therapeutic Drugs, B 62-5 Van Cauwenberge PB, Acta Otolaryngol, 1997, Suppl. 526, 43-6
  26. 26. 26 Betahistine Contraindications - Not known Precaution / Caution for use Betahistine, being a histamine analogue, should be used with caution in patients with pheochromocytoma, peptic ulcer, bronchial asthma, concurrent use of antihistamines Bradoo RA et al, Ind. J. Otolaryngol HNS, 2000, 52(2), 151-8
  27. 27. 27 Betahistine No antagonistic effect on H1 receptors Antihistamines block H1 receptors in brain, causing sedation or drowsiness Betahistine, stimulates H1 receptors Betahistine, does not slow down vestibular compensation, unlike antihistamines. Hence is suitable for use with vestibular habituation therapy. Kirtane MV, Ind. J. Otolaryngol HNS, 1999, 51(2),27-36
  28. 28. 28 Betahistine - Summary Pharmacokinetics: Rapid and complete absorption after oral route Pharmacology: It is a H1 agonist and H3 receptor antagonist. It increases cochlear and cerebral blood flow and regulates firing activity of vestibular nuclei. Dose: 24-48 mg /day Indication: vertigo, meniere’s syndrome Contraindications: not known Precaution for use: pheochromocytoma, peptic ulcer, bronchial asthma

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