Download to read offline
2008-antianxiety.ppt Pdf ppt for the study of
- 1. Anxiolytics & Hypnotics bySue Henderson
- 2. Therapeutic actions 1. Hypnotic 2.Anxiolytic 3. Anticonvulsant 4. Amnestic 5. Myorelaxant • In what medical circumstances might the amnestic properties of benzodiazepines be useful?
- 3. Indications • Why are benzodiazepines usefulin the treatment of alcohol detoxification? • Can they be used in the long term to prevent further alcohol abuse?
- 4. Anti-Anxiety & Hypnotics Anti-Anxiety •Benzodiazepine e.g. Diazepam • Non Benzodiazepine e.g. Buspirone Hypnotics: Sedatives • Benzodiazepine e.g. Temazepam • Non Benzodiazepine e.g. Zopiclone
- 5. Differentiate • What isthe difference between an anti-anxiety medication and a hypnotic?
- 6. Antidepressants for anxiety Clomipramine(TCA) OCD Fluvoxamine (SSRI) OCD Paroxetine (SSRI) OCD, panic disorder, social phobia Sertraline (SSRI) OCD, panic dis, PTSD Venlafaxine (SNRI) GAD Fluoxetine (SSRI) OCD
- 7. Benzodiazepines • Used mostlyin primary care rather than psychiatry. • Often prescribed for problems that are more effectively managed with non-drug therapies. • Temazepam in 10 most frequently prescribed up until 2001.
- 8. Benzodiazepines • Should notbe 1st line therapy in mental health & sleep management. • Limit use to less than 2 weeks. • Only benefit of continued use is avoiding withdrawal effects (NPS, 1999). • All equally effective but differ in metabolism, speed of onset & half life
- 9. 2004-05 National HealthSurvey • 5% of Australians had used a benzodiazepine for anxiety management in the 2 weeks prior to the survey. • Benzodiazepine use was higher in women and in older age groups (mostly due to sleeping tablets). • Overall use has fallen since 80’s but total use remains high (ABS, 2006).
- 10. Anxiolytic/hypnotic (% ofpop all age groups) 0 2 4 6 8 10 12 Temazepam Diazepam Other benzodiazepines Oxazepam
- 11. MCQ Benzodiazepines can safelybe prescribed during pregnancy. • A. True • B. False
- 12. Indications Drug Anxiolytic Diazepam,Alprazolam, Bromazepam, Lorazepam, Oxazepam, Buspirone* Muscle relaxant Diazepam Pre-med Diazepam, Lorazepam Alcohol withdrawal Diazepam, Oxazepam, Panic disorder Alprazolam, Clonazepam. Anti-convulsant Clobazam, Clonazepam, Diazepam, Lorazepam Hypnotic Flunitrazepam, Nitrazepam Temazepam, Zolpidem, Zopiclone*
- 13. Dose Equivalents Drug Dailyrange mg Equiv 5mg diazepam. Duration (½ life) alprazolam 1 – 4 0.5 - 1 Short/Intermediate bromazepam 6 – 9 3 – 6 Short/Intermediate clobazam 30 – 80 10 Intermediate clonazepam 4 – 8 0.5 Intermediate diazepam 5 – 20 5 Long flunitrazepam 0.5 – 2 1 – 2 Intermediate lorazepam 2 – 4 1 Short/Intermediate nitrazepam 5 – 20 5 – 10 Intermediate oxazepam 45 – 90 15 – 30 Short temazepam 10 – 30 10 - 20 Short triazolam 0.125 - 0.25 0.25 Short buspirone* 15 – 30 - Short zopiclone* 3.75 - 7.5 - Short
- 14. Short Acting: 3- 8 hrs • Oxazepam • Temazepam • Triazolam • Buspirone* • Zopiclone*
- 15. Intermediate Acting: 10- 20 hours • Alprazolam • Bromazepam • Clobazam • Clonazepam • Flunitrazepam • Lorazepam • Nitrazepam
- 16. Hypnotics • Explain thebenefit of using Temazepam over Nitrazepam for assisting with sleep. • Why should hypnotics be used for a limited time to assist with sleep?
- 17. Long Acting 1-3 days: Diazepam X X X
- 18. Addiction • Why areshort acting benzodiazepines more of a problem with addiction than the long acting ones?
- 19. Dependency cycle of benzodiazepines Green,1996, p. 88 Use of benzodiazepine Reduced anxiety Effect wears off Even more anxious
- 20. Benzodiazepines: Action • CNSdepressant • Enhance the effect of GABA. • GABA is a neurotransmitter that inhibits neuronal activity i.e. reduces the firing rate of neurones.
- 21. Agonist = Facilitate •Benzodiazepines bind to a site near the GABA binding site thus facilitating the action of GABA
- 22. Death Increasing dose of drug Coma General Anaesthesia Sleep Sedation Disinhibition Relief fromanxiety No effect •(Julien, 2001)
- 23.
- 24. Contra-indications • Myasthenia gravis. •Severe respiratory impairment e.g sleep apnoea, COAD.
- 25. Avoid (if possible) •Pregnancy • Lactation
- 26. Adverse Effects • Physicaldependence occurs in about 1 in 3 patients. • History substance abuse > risk dependence • Increased accident risk. • Tolerance & rebound insomnia. • Alcohol & CNS depressants potentiate adverse effects.
- 27. Adverse effects • 60y+> vulnerability to confusion, memory impairment, over sedation (most common S/E) & falls. • Adverse mood effects: depression, emotional anaesthesia, aggression, increased suicide risk in elderly.
- 28. Withdrawal from Benzodiazepines • Abruptcessation: > seizures • Withdrawal symptoms may occur between doses during continuous use (inter-dose withdrawal). Patients may think these symptoms are due to the original problem. • Withdrawal symptoms: increased anxiety, sleep disorder, aching limbs, nervousness & nausea.
- 29. Withdrawal from Benzodiazepines • Withdrawalexperienced by 45% of patients discontinuing low dose benzodiazepines & 100% patients on high doses. • Short half life benzodiazepines are associated with more acute & intense withdrawal symptoms. • Long half life benzodiazepines - milder, more delayed withdrawal (NPS, 1999).
- 30. Withdrawal from benzodiazepines • Benzodiazepinesshould not be ceased abruptly. • Dose reduced by 10-20% per week. • Patient allowed to stabilise between each reduction. • Admission for high dose users, history of seizures or psychosis, or for more rapid withdrawal.
- 31. Withdrawal from benzodiazepines • Implementrelaxation/cognitive techniques. • If necessary referral: • Drug & Alcohol Services • Self Help group TRANX www.tranx.org.au • Psychologist (for CBT)
- 32. Overdose Benzodiazepines • Generallysafe in overdose unless mixed with alcohol/CNS depressants. • Symptoms overdose: hypotension, respiratory depression & coma. • Treatment: Supportive • Flumazenil rarely indicated
- 33. IV Flumazenil • Dangerousto use if mixed overdose (e.g benzodiazepine + tricyclics, amphetamines, other pro-convulsants) - Result in uncontrolled seizure • In dependent individuals severe withdrawal • Flumazenil has a shorter half life ( one hour) than all benzodiazepines Therefore, repeat doses of flumazenil may be required to prevent recurrent symptoms of overdosage once the initial dose of flumazenil wears off.
- 34. Flumazenil is a benzodiazepineAntagonist = Blocker Flumazenil binds to GABA receptor displacing benzodizepine
- 35. Non benzodiazepines Anxiolytic: Buspirone(Buspar) • Different action to bzd. • Not a CNS depressant. • Partial agonist (stimulant) of dopaminergic & serotoninergic receptors. • No sedation, anti-convulsant or muscle relaxant properties - just anxiolytic. • Delayed action (1-2 weeks) • Effect reduced if benzodiazepine used in last 3/12
- 36. Comparison of benzodiazepine& buspirone Benzodiazepine Rapid onset Can cause sedation May impair performance Additive effects with alcohol May cause dependence & withdrawal Pharmacokinetic change with age Associated with falls in elderly (Keltner & Folks, 2001) Buspirone Delayed onset (cannot be used PRN) Does not cause sedation Does not impair performance No additive effect with alcohol Non addictive No pharmacokinetic change with age Does not cause falls in elderly Expensive (Not on PBS)
- 37. Presentation: Buspar • Whitescored • 5 mg & 10 mg tabs
- 38. Buspirone: Agonist =Mimic • Buspirone attaches to serotonin receptor mimicking serotonin.
- 39. Non benzo Hypnotic: Zopiclone(Imovane) • Similar action, side effects & contraindications to benzo’s.
- 40. Benzodiazepines key points •Should not be used in patients with liver disease, history of substance abuse, severe respiratory distress, performing hazardous tasks • Avoid during pregnancy/lactation if possible • Assess for over sedation • Cease slowly • Monitor elderly (cognition, falls) • Be aware they raise seizure threshold, and • Potentiate CNS depressants (alcohol)
- 41. Hypnotic key points •Advise re rebound insomnia when medications ceased • Should not be used in sleep apnoea • Avoid alcohol • Hangover effect (impairing performance) • Monitor in elderly (falls, double dosing)
- 42. References • Australian Bureauof Statistics. (2006). National health survey 2004-05: Summary of results. Canberra: Australian Bureau of Statistics. • Fortinash, K. M., & Holoday-Worret, P. A. (2000). Psychiatric mental health nursing ( 2nd ed.). St. Louis: Mosby. • Galbraith, A., Bullock, S. & Manias, E. (2001). Fundamentals of pharmacology (3rd ed.). Melbourne: Prentice Hall.
- 43. References • Julien, R.M. (2001). A primer of drug action: A concise, non- technical guide to the actions, uses, and side effects of psychoactive drugs. New York: W. H. Freeman and Co. • Keltner, N. L., & Folks, D. G. (2001). Psychotropic drugs (3rd ed.). St. Louis: Mosby. • National Prescribing Service. (1999). Helping patients withdraw. National Prescribing Service Newsletter, No. 4 June. • National Prescribing Service. (1999). Benzodiazepines reviewing long term use: A suggested approach. Prescribing Practice Review, No. 4 July.
Editor's Notes
- #2 Insomnia – induce sleep Anxiety: panic disorders, phobias, agitated psychosis Convulsions, seizures Muscle relaxant, relieve spasms Pre surgical operations, sedation for minor surgical procedures (twilight - amnestic) Sedation/anticonvulsant for alcohol withdrawal Answer: Unpleasant surgical or test procedures e.g. colonoscopy
- #3 Alcohol and benzodiazepines are both CNS depressants. Benzo’s can be gradually tapered off preventing rebound CNS over excitability. They cannot be used in the long term because they are addictive. People addicted to alcohol have cross addiction with benzodiazepines.
- #5 Hypnotics induce sleep. Hypnotics at lower doses cause sedation (anti-anxiety effect) Anti-anxiety drugs result in a reduction in anxiety but can induce sleep in higher doses
- #6 Clomipramine (TCA) Anafranil, Clopram, Placil Fluvoxamine (SSRI) Faverin, Luvox Paroxetine (SSRI) Aropax, Oxetine, Paxtine Sertraline (SSRI) Zoloft Venlafaxine (SNRI) Efexor Fluoxetine (SSRI) Auscap, Fluohexal, Lovan, Prozac, Zactin
- #10 Anxiolytic/hypnotics Temazepam 9.8 Diazepam 5.6 Other benzodiazepines 4.9 Oxazepam 2.6
- #11 Benzodiazepines may cause hypotonia, respiratory depression and hypothermia in the newborn infant if used in high doses during labour. Withdrawal symptoms in newborn infants have been reported with prolonged use of this class of drugs. Category C (TGA) Drugs which, owing to their pharmacological effects, have caused or may be suspected of causing, harmful effects on the human fetus or neonate without causing malformations. These effects may be reversible. Accompanying texts should be consulted for further details.
- #12 * = Non benzodiazepine
- #13 * Non benzodiazepine
- #14 Non benzodiazepine
- #16 Temazepam is short acting and will induce sleep but not cause a hangover effect. Prolonged use of benzodiazepines can result in tolerance (more drug needed to induce same effect)
- #18 Drugs with short half lives are cleared from the bloodstream fairly quickly and may induce withdrawal effects such as rebound excitement and insomnia. Those with longer half lives are cleared less quickly resulting in a decrease in withdrawal effects. The resulting slow drop in blood levels allows the body to adjust to the lack of drug more effectively
- #20 Potentiate other CNS depressants: Alcohol, anti-histamines, analgesics, anti-convulsants, anti-psychotics, hypnotics, barbiturates, anaesthetics. Combination will lead to sedation and may lead to unconsciousness and death.
- #21 Benzodiazepines bind to a site near the GABA binding site thus facilitating the action of GABA Drug binds to a site near the binding site for the endogenous transmitter facilitating binding. Also an agonist action.
- #22 Death if mixed with other CNS depressants. Rare if taken on own.
- #34 Attaches to the benzodiazepine binding site but does not facilitate action of GABA. Competes with any benzodiazepine that is present, displacing the benzodiazepine from the receptor and reversing the action of the benzodiazepine
- #36 Gradual improvement in 1 to 2 weeks, maximum effect in 4 to 6 weeks
- #38 Buspirone attaches to Serotonin 1A receptor and activates it mimicking serotonin action on the receptor, which results in an anti-anxiety action. Drug mimics action of the transmitter = Agonist Green symbolises “Go”