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Pharm_Sedatives

Sedatives, Anxiolytics, Hypnotic Medication

QuestionAnswer
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
Created by: Flubzy
Popular Pharmacology sets

 

 



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