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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 |