Anxiety management Flashcards
Generalized Anxiety Management
- SSRIs (DOC) & Venlafaxine
- Benzos - are used at the start to produce short-term relief while the AD take 2-4 weeks. Tapered over 4-12 weeks.
- Buspirone (2nd line)
- Hydroxyzine & Pregabalin ( Alternatives)
Panic Disorder Management
- SSRI (DOC) OR TCA/ MAOI if SSRI is ineffective
- Benzos- Concomitantly with AD or Monotherapy for acute relief
NB: Alprazolam is widely used but may cause rebound anxiety, withdrawal syndrome & seizures
Social Anxiety Management
- SSRI (DOC)
Obsessive Compulsive Disorder Management
- Clomipramine
- Fluoxetine
- Fluvoxamine
- Paroxetine
- Sertraline
NB: Add a BENZO or AP for highly anxious OCD pts.
Post-traumatic Stress Disorder Management
- SSRI (DOC)
- Venlafaxine, TCAs & MAOIs - more AE
- Sertraline & Paroxetine (Acute management)
NB: Sertraline is also approved for long-term management
Performance Anxiety Management
- B-blockers - Propranolol & Nadolol
AE: hypotension
NB: b-blockers w/ higher lipophilicity is used
Benzodiazepine MOA
Binds to the GABAa receptors –> Opens Cl channel –> Cl influx
- +ve allosteric modulator –> Dec EC50
- Inc. FREQUENCY of channel opening
GABAa receptor & the binding sites
- A2B2y pentameric structure
- GABA binding site = between adjacent A&B subunits
- Benzo binding site = between adjacent A&Y subunits
NB: Benzo receptors in the CNS are BZ1 & BZ2
Actions of Benzos
- Anxiety management - Clonazepam, Lorazepam, Alprazolam & Diazepam
- Sedative & hypnotic - Temazepam & Triazolam
- Anticonvulsant - Clonazepam (epilepsy), Midazolam, Lorazepam & Diazepam ( Status epilepticus)
- Muscle relaxant - Diazepam
- Alcohol withdrawal
- Anesthesia
Pharmacokinetics of Benzos
- Onset of action= 30-60 mins (varying half-life)
- Lipophilic
- Rapidly & completely absorbed
- Oral
Benzos (names) based on duration of action
Long acting - Clonazepam - Diazepam - Flurazepam Intermediate acting - Alprazolam - Lorazepam - Oxazepam - Temazepam Short acting - Midazolam - Triazolam
Metabolism of Benzos
Adverse effects of Benzos
- Drowsiness & confusion
- Ataxia
- Cognitive impairment
- Paradoxical effects (rare)- anxiety, irritability, hostility, rage, paranoia, depression & suicidal ideation
- Dependence & withdrawal syndrome - Confusion, anxiety, agitation, restlessness, insomnia & tension
Benzo Overdose Management
FLUMAZENIL (Only Benzo receptor antagonist)
- rapid onset & short duration (1hr)
- reverse CNS depressant effects
- blocks effects of Benzos & Z-drugs
- may cause seizures if benzo was used for seizure control
- may precipitate withdrawal syndrome
Barbiturates MOA
- +ve GABAa receptor allosteric modulators
- Inc. DURATION of Cl- channel opening
- High dose - Directly activate Cl channels
- Block Glutamate receptors
- Inhibits voltage-activated Na & Ca channels
Actions of Barbituates
CNS depression
- Low dose - Sedation
- High dose - Hypnosis, Anesthesia, Coma & Death
RESP. depression
- Suppress the Hypoxic & Chemoreceptor response to CO2
ENZYME induction
- Induce P450 enzymes
Uses of Barbituates
- Anesthesia (short-acting barbiturates used IV)
Anticonvulsants - Phenobarbital - Tonic-clonic seizures & Status epilepticus
Phenobarbital & Thiopental - Status epilepticus
Adverse effects of Barbiturates
- Drowsiness & impaired concentration
- Paradoxical excitement
- Hypersensitivity
- Hangover
- Respiratory depression
- Pain
- Dependence & Severe withdrawal syndrome
- Poisoning- severe Resp. & central CV depression
Non-benzodiazepine Benzodiazepine Receptor Agonists (NBBRA)/ Z-Drugs (names)
- Zolpidem
- Zaleplon
- Eszopiclone
NBBRA/ Z-drugs MOA
- +ve GABAa receptor modulator
- Acts on BZ1
- ONLY used as hypnotics
- Little/ No tolerance & AEs - FLUMAZENIL reverses effects
Uses of NBBRA
Only approved for HYPNOTICS INSOMNIA w/ - problems initiating sleep = Zolpidem - problems of sleep onset & maintenance = Zolpidem ER - short term management = Zaleplon
- Minimal muscle relaxing & anti-convulsant effects
Z-drugs properties (onset, DOA, HL & uses)
Melatonin Receptor Agonists (Name & MOA)
RAMELTEON
- MT1 & MT2 agonist
- Can be used long term bc of minimal abuse potential
Uses of Melatonin Receptor Agonist (Remelteon)
Insomnia characterized by difficulty with sleep onset
Adverse effects of Melatonin Receptor Agonist
- Dizziness
- Somnolence
- Fatigue
- Endocrine changes
- Dec in Testosterone
- Inc in Prolactin
Orexin Receptor Antagonist (names & MOA)
SUVOREXANT & LEMBOREXANT
- Dual OX1R & OX2R Receptor Antagonist (DORA)
NB: Orexin A & B promote wakefulness by activating OX1 & OX2
Uses of Orexin Receptor Antagonist
Insomnia characterized by difficulties w/ sleep onset and/or sleep maintenance
Adverse effects & Contraindications of Orexin Receptor Antagonist
- Daytime somnolence
- Worsening of depression/ Suicidal Ideation
Contraindicated in Narcolepsy
Beta blockers (names, uses)
PROPRANOLOL
- Dec autonomic symptoms of specific phobias
- USED to control performance anxiety (stage fright)
Anti-histaminic (names, class, uses)
Doxepin (TCA)
- Insomnia w/ difficulty of sleep maintenance
- H1 antagonism
Hydroxyzine
- Symptomatic relief of anxiety
- Antiemetic propertied
Diphenhydramine & Doxylamine (non-prescription)
- Mild types of insomnia
5HT1A Partial Agonist (Name, uses, onset, MOA, interactions)
BUSPIRONE
- Anxiety & GAD (2nd line)
- ONLY anxiolytic properties
- Onset = 2-3 weeks
- MOA- same as Antidepressants
- No interaction w/ alcohol or benzos or other sedative-hypnotics, rebound anxiety, withdrawal signs, dependence & less psychomotor impairment than BZ
