• Drugs that depress the CNS function
• Primarily used to treat anxiety and insomina
• Antianxiety agents or anxiolytics
• Distniction between antianxiety effects and hypnotic effects if often a matter of dosage
• Benzodiazepines
• Benzodiazepine-like drugs
• Barbiturates

• DOC to treat insomnia and anxiety
• Used to induce general anesthesia
• Used to manage seizure disorders, muscle spasm, panic disorder, and withdraw from alcohol
• Most familiar member-diazepam (Valium)
• Safer than general CNS depressant due to the decreased risk of causing respiratory depression at therapeutic doses
• Lower potential for abuse
• Produce less tolerance and physical dependence
• Fewer drug interactions despite being metabolized in the liver
• Pharmacologic effects
• CNS depressant  
• Cardiovascular depressant
• Respiratory system depressant
• 75-90% absorption
• Well distributed throughout the body
• Metabolized in the liver
• Short acting with half lives ranging from 2-6 hrs
• Prescribed as "Take as needed"
• Therapeutic Uses
• Anxiety
• Insomnia
• Seizure disorders
• Muscle spasm
• Alcohol withdrawal
• Panic Disorder
• Perioperative disorders
• Adverse Effects:
• CNS depression
• Anterograde amnesia
• Sleep driving
• Paradoxial effects: Very rare
• Respiratory depression: Rare and generally not seen in therapeutic doeses
• Abuse: Patients feel good and calm
• Use in pregnancy and lactation is not recommended
• Drug Interactions: CNS depressants
• Tolerance with prolonged use.  Tolerance develops to some effects but not others
• Can cause physical dependence but the incidence of substantial dependence is low
• Acute Toxicity:
• Oral Overdose
• IV toxicity
• General Treatment Measures
• Antidote: Treatment with Flumazenil
• Can be given orally, IM, IV
• Increase frequency of GABA channel opening

Benzodiazpines

• Relative Safety: High
• Maximal ability to depress CNS function: Low
• Respiratory depressant ability: Low  
• Suicide Potential: Low
• Ability to cause physical dependence: Low
• Although dependence is lost in most patients, significant dependence can develop with long term high dose use
• Ability to cause tolerance: Low
• Abuse potential: Low
• Ability to induce hepatic drug metabolism: Low

Barbiturates

• Relative Safety: Low
• Maximal ability to depress CNS function: High
• Respiratory depressant ability: High 
• Suicide Potential: High
• Ability to cause physical dependence: High 
• Ability to cause tolerance: High
• Abuse potential: High
• Ability to induce hepatic drug metabolism: High

• Zolpidem (Ambien)
• Sedative-hypnotic
• Short-term management of insomnia- tolerance develops
• Zaleplon (Sonata)
• New class of hypnotics
• Pyrazolopyrimidines
• Short term management of insomnia
• Prolonged use does not appear to cause tolerance
• Eszopiclone (Lunesta)
• Is the s-isomer of zopiclone
• Treatment of insomnia
• No limitation on how long it can be used  

• Melatonin Agonist
• Brand name: Rozerem
• Relatively new hypnotic
• Activation of melatonin receptors
• Approved for chronic insomnia-difficulty with sleep onset  

• Three Classifications:
• Ultrashort acting: Tiopental
• Short to intermediate acting: secobarbital
• Long-acting: Phenobarbital
• Binds to the GABA receptor-Cl channel complex: Increases duration GABA cannel is open  
• Pharamcologic Effects:
• CNS depression
• Cardiovascular effects
• Induction of hepatic drug metabolizing enzymes
• Tolerance develops to many but not all of the CNS effects
• Very little tolerance develops to respiratory depression
• By increasing the synthesis of porphyrin, barbiturates increase the production of cytochrome p450
• Rapid onset and brief duration
• Lipid soluble
• Therapeutic Uses:
• Seizure disorders
• Induction of anesthesia
• Insomnia
• Adverse Effects:
• Respiratory depression which can lead to death
• Suicide
• Abuse
• Not recommened in pregnant women
• Exacerbation of intermittent porophyria
• Hangover
• Paradoxical excitment
• Hyperalgesia
• Acute Toxicity
• Respiratory depression
• Coma
• Pinpoint pupils
• Treatment is removal of barbiturate from the body and maintenance of an adequate oxygen supply to the brain
• Admin is oral, IV, IM

• Nonselevtive CNS despressants
• Actions similiar to those os barbiturates
• Acute overdose resembles poisoning with barbiturates
• Avoid during pregnancy and lactation
• Chloral Hydrate
• Meprobamate
• Paraaldehyde  

• REM
• NREM:
• I: Light sleep
• II: Light sleep
• III: Deep sleep
• IV: Deep sleep  

Benzodiazepines

Benzodiazepine-like Drugs

Trazodone

Antihistamines

Alternative medicine

• An uncomfortable state wtih psychologic and physical components
• Characterized by fear, apprehension, dread, and uneasiness
• Among the MC psychiatric illnesses 

• Generalized anxiety disorder
• Panic Disorder
• OCD
• Social anxiety disorder-social phobia
• PTSD 

• Uncontrollable worrying that last 6 (+) months
• Treatment:
• Supportive therapy
• Cognitive behavioral therapy
• Biofeedback
• Relaxation training
• Benzodiazepines
• Buspirone (BuSpar)
• Antidepressants
• Venlafaxine (Effexor XR)
• Paroxetine (Paxil) short and long term
• Escitalopram (Lexapro)

• Non CNS depressant
• Does not cause sedation
• Has no abuse potential
• Does not intensify the effects of the CNS depressants
• Anxiolytic effects develop slowly
• Well abs following oral admin
• Adverse Effects:
• Dizziness
• Nausea
• Headache
• Nervousness
• Lightheadedness
• Excitment
• Drug and Food Interactions
• Ketoconazole
• Erythromycin
• Grapefruit juice
• No withdrawal symptoms have been observed

• Palpitations, pounding heart, racing heartbeat
• Chest pain or discomfort
• Sensation of SOB
• Feeling of choking
• Dizziness
• Lightheadedness
• Nausea, or abdominal disomfort
• Fear of losing control
• Fear of dying
• Tingling or numbness in the hands
• Flushes or chills
• Treatment:
• Cognitive behavioral therapy (CBT)
• Antidepressants: SSRIs, Tricyclics, MAOIs
• Benzodiazepines- First line Drug  

• Potentially disabling condition
• Persistent obsession and compulsions
• Treatment:
• Behavioral therapy
• SSRIs
• First line drug
• Citalopram
• Escitalopram
• Fluxetine
• Fluvoxamine
• Paroxetine
• Sertaline
• Clompramine (Anafranil)
• Less tolerated
• Second line Drug  

Social Anxiety Disorder

Social Phobia

• Intense irrational fear that one might be scrutinized by others
• Can be generalized or nongeneralized
• Very debilitating
• One of the MC psychiatric disorders
• Treatment:
• Psychotherapy
• Drug Therapy 

• Develops following a traumatic event
• Re-experiencing the event
• Avoiding reminders of the event
• Persistent state of hyperarousal
• Treatment
• Psychotherapy with drugs
• Psychotherapy alone