anxiolytic, tranquilizing, and muscle relaxant medications

what is a tranquilizer?

• medication that produces emotional calming, reduces anxiety, tension, agitation, and other related emotional states

• major: antipsychotics

• minor: anxiolytics

• clinical effects: anxiolytic, sedative, hypnotic, myorelaxant

what is an anxiolytic?

reduces/relieves anxiety, fear, apprehension

what are sedatives?

general slowing down of cognitive function, reduction of restlessness, impairment of memory formation

what is a hypnotic?

induction of sleep

what is a myorelaxant?

causing relaxation of the muscles

what are antiepileptic/anticonvulsants?

• used to treat epilepsy/convuslions

• preferred term: antiseizure medication

what is the problem with barbiturates?

• have the highest risk of overdose death due to respiratory depression

• scheduled medications with a high potential for abuse

what are benzodiazepines?

• azo, azep, azepam, azolam

• generally safer: less respiratory depression/toxicity than barbiturates (except when mixed with alcohols)

what is the MOA of benzodiazepines?

bind to GABA neurons and enhance inhibitory effects

what is buspirone (buspar)?

• antianxiety agent with no potential for misuse: not a controlled substance

• has an advantage over barbiturates and benzodiazepines

what is the MOA of buspirone (buspar)?

no direct effect on GABA receptors, high affinity for serotonin receptors (5-HT1A agonist), and moderate affinity for dopamine receptors

what are the adverse effects of skeletal muscle relaxants?

anticholinergic effects

what are non-benzodiazepine antiseizure medications?

• azepines

• carbamazepine: seizure disorders, bipolar disorders, neuropathic pain

• oxcarbazepine, eslicarbazepine

what is a BBW for all non-benzodiazepine antiseizure medications?

increased risk of suicidal thoughts/behavior

what are the contraindications/precautions of carbamazepine?

• bone marrow suppression: anemia, low WBC count

• severe rash: Stevens-Johnson syndrome, toxic epidermal necrolysis (Asian ancestry: HLA-B*1502 allele)

what are non-benzodiazepine (BZD) receptor agonists (NBRAs)?

• Z drugs: zolpidem, zaleplon, eszopiclone

• sedative-hypnotics

• enhance GABA activity by binding to BZD-1 receptors: no effect on BZD-2

• C-IV: potential for misuse, tolerance, dependence

what are the warnings/precautions of NBRAs?

• complex sleep behaviors

• may worsen depression

• caution with sleep apnea, COPD

what is ramelteon (rozerem)?

• melatonin receptor agonist

• indicated for sleep onset insomnia

• no concern for misuse

• adverse effects: headache, dizziness, somnolence

what is low-dose doxepin (silenor)?

• tricyclic antidepressant (TCA): at low doses, acts as an antihistamine

• indicated for sleep maintenance in insomnia

• no concern for misuse: but can be fatal in overdose

• adverse effects: drowsiness, headache, dry mouth

what is carisoprodol (soma)?

• C-IV substance: potential for misuse, tolerance, dependence

• skeletal muscle relaxant