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Pharm_Sedatives
Sedatives, Anxiolytics, Hypnotic Medication
| Question | Answer |
|---|---|
| Sedatives: | drugs that: - decrease neural activity, - moderate excitement and - calm the person taking the drug |
| Anxiolytics: | drugs intended to reduce anxiety or tension at doses which do not cause sedation or sleep. |
| Hypnotics: | drugs that produce drowsiness and facilitate the onset and maintenance of sleep |
| Benzodiazepines: Mechanism of Action | increase responses to GABA by binding to the allosteric site, which widens the Cl- channel |
| Benzodiazepines: Pharmacokinetics | - rapid onset of action - lipid-soluble > cross BBB - persist longer in fat people than old people - abuse possibility |
| Flumazenil (Romazicon) | (antagonist) Antidote for benzodiazepine overdose |
| Benzodiazepines: effects & uses | - Sedation and Sleep - Anxiety and Aggression reduction - Muscle Spasm Relaxants - Anticonvulsant Effects - Amnesia |
| Insomnia | |
| OTL | (metabolized) (O)utside (T)he (L)iver = OxAZEPAM, TemAZEPAM, LorAZEPAM |
| Benzodiazepine drug names | mostly AZEPAM (Medazepam, Diazepam, Clonazepam, Temazepam, Nordazepam, Oxazepam, Lorazepam) and AZOLAM (Triazolam, Alrpazolam, Midazolam) and ChlorAZEPATE and ChlordiAZEPOXIDE |
| MedAZEPAM > … | … > DiAZEPAM |
| DiAZEPAM > … | … > NordAZEPAM |
| ChlorAZEPATE > … | ... > NordAZEPAM |
| NordAZEPAM > … | ... > OxAZEPAM |
| TemAZEPAM > … | ... > OxAZEPAM |
| LorAZEPAM = … | … = Ativan |
| DiAZEPAM = … | … = Valium |
| ChlordiAZEPOXIDE = … | … = Librium |
| Benzodiazepine Side Effects: | psychotic slowing, risk of physical dependence (alcoholics) |
| Benzodiazepines used to treat insomnia: | EstAZOLAM, TriAZOLAM, FlurAZEPAM, QuAZEPAM TemAZEPAM, |
| FlurAZEPAM (info): | ↓sleep induction time, ↓ awakenings, ↑sleep duration, works for <4weeks, peaks in 2-3 nights of use (long ½ life) |
| TemAZEPAM (info): | ↓freq. wakening, intermediate acting, short term use (7-10d), peak: 2-3 h |
| TriAZOLAM (info): | induces sleep in insomniacs, short acting, peak: 1-2h, use <2-4 wks, tolerance within days, withdrawal=rebound insomnia & amnesia, risk for severe allergic reaction |
| D/C benzodiazepines > insomnia ? | ↑potent & ↑rapidly eliminated = ↑withdrawal |
| NONBenzodiazepines for insomnia: | ZolpiDEM, EzopiCLONE, ZalepLON (all very similar in action & effects) |
| ZolpiDEM = ... | ... = Ambien |
| ZolpiDEM (info): | 1st choice for insomnia, rapid onset, short acting hypnotic agent (↑GABA by binding to benzodiazepine receptor) as effective as benzodiazepines but safer, similar to ZalepLON & EzopiCLONE |
| EzopiCLONE = … | … = Lunesta |
| EzopiCLONE (info): | similar to ZolpiDEM & ZalepLON but mechanism unknown |
| ZalepLON = … | … = Sonata |
| ZalepLON (info): | similar to ZolpiDEM & EzopiCLONE, mechanism unknown, ultra-short acting so great for those who wake up at night, non-drowsy, risk of sever allergy |
| Barbiturates: | mostly obsolete for insomnia due to wide spectrum CNS depression, side effects: risk of abuse, drowsiness, nausea, vertigo, tremors, ↑hepatic enzymes (P450), therapeutic range ↓with duration of use (tolerance), TOXICITY |
| Benzodiazepines vs. Barbiturates | duration of action of Benzo > Barbi; toxicity Benzo (Diazepam) vs. < Barbi (Phenobarbital) |
| Ramelteon (info) | melatonin receptor agonist, action ~melatonin, used to help falling asleep, works within 7-10d, metabolized by P450 into active metabolite, well tolerated, no risk of abuse, ↓testosterone, ↑ prolactin |
| Melatonin agonists: | RamelTEON, TasimelTEON, AgoMELATINE |
| Sedatives-Hypnotics use: | treat insomnia and anxiety thru depression of CNS activity |
| Anxiolytics use: | control anxiety |
| Anxiety: | psychological SX: abnormal “fear of fear” ; physical SX: tachycardia, palpitations, trembling, dry mouth, sweating, weakness, fatigue, shortness of breath |
| Types of Anxiety: | 1. Generalized Anxiety (GAD), 2. Panic Disorders, 3. OCD, 4. Phobias, 5. PTSD, Acute Stress Disorder |
| Benzos for GAD: | Alprazolam, Chlordiazepoxide, Clorazepate, Diazepam, Lorazepam, Oxazepam |
| SSRIs for GAD: | Paroxetine, Escitalopram |
| SNRIs for GAD: | Duloxetine, Benlafaxine |
| Other drugs for GAD: | Buspirone |
| Benzos for Panic Disorder: | Alprazolam, Clonazepam, Lorazepam |
| SSRIS for Panic Disorder: | Paroxetine, Sertraline |
| SSRIs for OCD: | Citalopram, Escitalopram, Paroxetine, Fluoxetine, Fluvoxamine, Sertraline |
| SSRIs for SAD: | Paroxetine, Sertraline |
| SSRIs for PTSD: | Paroxetine, Sertraline |
| Alprazolam = … | … = Xanax |
| Alprazolam (Xanax) (info): | use panic disorders (short/long), metabolized by hepatic enzymes (P450), 70% protein bound, abuse risk |
| Chlordiazepoxide = … | … = Librium |
| Clorazepate = … | … = Tranxene |
| Diazepam = … | … = Valium |
| Diazepam (Valium) (info) | long acting (1-3d), hepatic metabolism > active metabolite, orally, treats ANXIETY & STATUS EPILEPTICUS |
| Halazepam = … | … = Paxipam |
| Lorazepam = … | … = Ativan |
| Lorazepam (Ativan): | short acting (exception), rapidly absorbed, IM/PO/IV |
| Oxazepam = … | … = Serax |
| Prazepam = … | … = Centrax |