Anti-Anxiety/Benzos Flashcards
alprazolam (Xanax)
Indication: Generalized Anxiety Disorder; Panic Disorder
Dose: GAD: 0.25mg-0.5mg TID, increase by 0.25-0.5mg daily every 3-4 days; MAX=4mg daily
Panic: 0.5mg TID, increasing by no more than 1mg increments every 3-4 days; MAX=10mg
XR: 0.5-1mg daily; increase by 1mg/d every 3-4d; MAX 3-6mg daily
Monitoring: No routine monitoring required
Mechanism: Binds to benzodiazepine receptors to enhance GABA effects.
Advantages: effective almost immediately
Disadvantages: high dependence potential (though research shows people with panic disorder rarely increase their dose once effective); short duration of action contributes to breakthrough symptoms; Schedule IV
ADEs: sedation; somnolence; memory impairment; slurred speech incoordination; dependence; SERIOUS: anterograde amnesia; increase fall risk in elderly; paradoxical reactions (irritability); respiratory depression (use in extreme caution with concomitant opioids and sleep apnea)
Off-Label: Insomnia; Acute Mania; Catatonia; Other Anxiety Disorders
Fun Facts: Street Names: Bars, Z-Bars; Zannies; Footballs; Blues; Blue Footballs
buspirone (BuSpar)
Indication: Generalized Anxiety Disorder
Dose: Start 7.5mg BID (or 5mg TID); increase by 5mg/d every 2-3d to target dose of 20-30mg daily in divided doses; MAX=20mg TID
Monitoring: No monitoring required.
Mechanism: Serotonin 5HT1A receptor partial agonist (presynaptic)
Advantages: non-sedating, non-habit-forming alternative to benzodiazepines; serotonin effect can potentiate antidepressant effects
Disadvantages: response is not particularly robust; only found effective in GAD; requires several weeks to reach benefit and no particular PRN benefits
ADEs: dizziness; nervousness; nausea; headache; jitteriness
Off-Label: Treatment-resistant depression; anxiety symptoms in depression
Fun Facts: Other 5HT1A partial agonists: aripiprazole, ziprasidone, vilazodone
clonazepam (Klonopin)
Indication: Seizure Disorders; Panic Disorder
Dose: Anxiety: 0.5mg BID; MAX=6mg daily
Insomnia: 0.25mg at bedtime; MAX=2mg
Monitoring: No routine monitoring required
Mechanism: Binds to benzodiazepine receptors to enhance GABA effects.
Advantages: long half-life reduces breakthrough symptoms
Disadvantages: has active metabolites that accumulate; effects of a dose are not evidence for a few days due to the need for metabolite accumulation; dependence (Schedule IV)
ADEs: daytime grogginess; sedation; confusion; ataxia; SERIOUS: anterograde amnesia; increase fall risk in elderly; paradoxical reactions (irritability)-primarily in elderly and pediatric populations; respiratory depression (use in extreme caution with concomitant opioids and sleep apnea)
Off-Label: Insomnia; Acute Mania; Catatonia; Other Anxiety Disorders
Fun Facts: “K-pins” on the street ($5 per tablet)
diazepam (Valium)
Indication: Generalized Anxiety Disorder; Alcohol Withdrawal; Seizure Disorders; Muscle Spasms
Dose: Anxiety: 2-5mg BID; increase by 2-5mg daily every 4d; MAX=40mg daily
Monitoring: No routine monitoring required
Mechanism: Binds to benzodiazepine receptors to enhance GABA effects.
Advantages: long half-life reduces breakthrough symptoms
Disadvantages: has active metabolites that accumulate; effects of a dose are not evidence for a few days due to the need for metabolite accumulation; tolerance to the sedative effects occurs before the tolerance to anti-anxiety effect; dependence (Schedule IV); highest abuse potential because it is the most lipid solubility and has rapid distribution into the CNS which creates a “rush.”
ADEs: somnolence; dizziness; weakness; ataxia; SERIOUS: anterograde amnesia; increase fall risk in elderly; paradoxical reactions (irritability)-primarily in elderly and pediatric populations; respiratory depression (use in extreme caution with concomitant opioids and sleep apnea)
Off-Label: Insomnia; Acute Mania; Catatonia; Other Anxiety Disorders
Fun Facts: Often glorified in song (“little yellow pill;” “Mother’s Little Helper;” “Walk on the Wild Side”)
lorazepam (Ativan)
Indication: Generalized Anxiety Disorder; abortive for status epilepticus (in IV form)
Dose: Anxiety: 1mg BID initially; increase by 0.5-1mg daily every 2-4 d; MAX=10mg daily
Insomnia: 0.5mg-1mg at bedtime; MAX=4mg
Monitoring: No routine monitoring required.
Mechanism: Binds to benzodiazepine receptors to enhance GABA effects.
Advantages: no active metabolites that accumulate
Disadvantages: dependence within the first 2-4 weeks; disrupts sleep architecture (Schedule IV); withdrawal seen on the first day after abrupt discontinuation; need lower doses in elderly
ADEs: somnolence; dizziness; weakness; ataxia; SERIOUS: anterograde amnesia; increase fall risk in elderly; paradoxical reactions (irritability)-primarily in elderly and pediatric populations; respiratory depression (use in extreme caution with concomitant opioids and sleep apnea)
Off-Label: Insomnia; Acute Mania; Catatonia; Other Anxiety Disorders
Fun Facts: Early Ativan marketing was direct to consumer: “The Ativan Experience can be yours” (in 1977) and “In a world where certainties are few…prescribed by so many caring clinicians” (in 1987).
prazosin (Minipress)
Indication: Hypertension (rarely used anymore for its original indication)
Dose: PTSD (nightmares): 1mg at bedtime for three days, increase by 1mg every 4d; dose can be up to 20mg at bedtime; consider BID dosing for PTSD-associated arousal symptoms
Monitoring: Blood pressure
Mechanism: alpha-1 adrenergic receptor antagonist
Advantages: no particular advantages
Disadvantages: mixed evidence; caution with PDE5 inhibitors or other antihypertensives
ADEs: somnolence; dizziness; headache; weakness; orthostasis; syncope; prolonged erections/priapism
Off-Label: nightmares; urinary hesitancy in BPH; alcohol dependence
diphenhydramine (Benadryl)
Indication: Insomnia (12+); Motion Sickness; Antiparkinsonism; Allergies
Dose: 25-50mg at bedtime (can be as low at 6.25mg)
Monitoring: No routitine monitoring required
Mechanism: Histamine-1 (H1) Antagonist
Advantages: non-habit forming
Disadvantages: non-selective H1 antagonist with negative effects
ADEs: dry mouth; ataxia; urinary retention; constipation; drowsiness; memory problems; blurred vision; tachycardia
Off-Label: morning sickness; EPS
Benzodiazepine Equivalents
Triazolam (Halcion): 0.25mg
Alprazolam (Xanax): 0.5mg
Clonazepam (Klonopin): 0.25-0.5mg
Estazolam (ProSom): 1mg
Lorazapam (Ativan): 1mg
Diazepam (Valium): 5mg
Clorazepate (Tranxene): 7.5mg
Oxazepam (Serax): 15mg
Temazepam (Restoril): 15mg
Flurazepam (Dalmane): 15mg
Quazepam (Doral): 15mg
Chlordiazepoxide (Librium): 25mg
Benzodiazepine Metabolism
(chlordiazepoxide/Librium) –> +1 –> +1 –> Desmethyldiazepam –> (oxazepam/Serax) –> Glucuronides
–
(flurazepam/Dalmane) –> +1 –> N-desalkylflurazepam –> Glucuronides
–
(quazepam/Doral) –> +1 –> N-desalkylflurazepam –> Glucuronides
–
(triazolam/alprazolam : Halcion/Xanax) –> +1 –> Glucuronides
(lorazepam/temazepam : Ativan/Restoril) –> Glucuronides
propranolol (Inderal)
Indication: hypertension; angina; post-MI cardioprotection; atrial fibrillation; migraine prophylaxis; essential tremor
Dose: Performance Anxiety: 10mg one hour before even; usual dose 10-40mg
Tremor: 10mg BID; can go up to 30-120mg divided daily (BID or TID); LA up to 60-80mg daily
Akathisia: 10mg BID; up to 30-90mg divided (BID/TID)
Monitoring: Periodic BP and pulse
Mechanism: non-selective beta-1 and beta-2 adrenergic receptor antagonist; reduces the somatic effects of anxiety (i.e., sweating,
Advantages: no cognitive effects (like with benzodiazepines)
Disadvantages: no particular disadvantages
ADEs: dizziness; fatigue; bradycardia; hypotension
Off-Label: performance anxiety; tremor due to medications (esp. Lithium); akathisia
