Ch: 34 & 35: Sedative-Hypnotic Drugs Flashcards
Benzodiazepines
Mechanism: GABA which is an inhibitory neurotransmitter in CNA
- bind to GABA receptors and enhance effects of GABA in brain
uses: anziety, insomnia, seizure disorders, muscle spasm, alcohol withdrawl and perioperative applications
Adverse: CNS depression, anterograde amnesia, sleep driving, paradoxical effects, resp. depression, abuse
- use in prego and lactation: highly lipid soluble, cross placenta barrier
interactions: CNS depressants, ETOH
Tolerance: with prolonged use; can cause physicial dependence
Benzodiazepines: Acute toxicity
- oral overdose: drowsiness, lethargy, and confusion
- intravenous: life-threatening reactions, profound hypotension, resp. arrest, and cardiac arrest
- general treatment: gastric lavage, activated charcoal, saline cathartic and dialysis
- treatment with flumazenil: competeive receptor antagonist; reverse sedative effects
Barbiturates
- cause tolerance and dependence
- higher potential for abuse
- multiple drug interactions
- powerful resp. depressants
- 3 classifications: ultrashort-acting, short-to-intermediate acting, and long-acting
- mechanism of action: bind to GABA receptor-Cl- channel complex
- cause CNS depression, CV effects, induce hepatic drug-metabolizing enxymes
- tolerance: develops to many but little develops to resp. depression
- uses: seizure disorders, induce anesthesia, insomnia
Barbiturates: Interactions and Adverse
- CNS depressants
- adverse: resp. depression, suicide and abuse
Barbiturates: Toxicity
- symptoms: resp. depression, coma, pinpoint pupils
- treat: activated charcoal; maintain oxygen supply to brain; maintain body heat, suppot BP
- admin: oral, IV, IM
Insomnia: Drugs used
- benzodiazepines, or like drugs: Zolpidem, zaleplon, and eszopiclone
- ramelteon
- antidepressants
- antihistamines: tolerance develops quickly and daytime drowsiness and anticholinergic effects
- melatonin
Ramelteon
- melatonin agonist
- activates melatonin receptors
- used for chronic insomnia: difficult with sleep onset but not with sleep maintenance
- rapid onset (30mins)
Zaleplon (Sonata)
- short-term management of insomnia
- prolonged use does not cause tolerance
- side effects: headache, nausea, drowsiness, dizzy, myalgia, and ab pain
Generalized Anxiety Disorder
- uncontrollable worrying that lasts 6 months or longer (not situational)
- treatment: non-drug approaches: cognitive behavioral therapy, supportive therapy
Generalized Anxiety Disorder: Buspirone (BuSpar)
- not a CNS depressant
- no abuse potential
- does not intensify effects of CNA depressants
- well absorbed after oral admin
- adverse: dizziness and nausea, headache, nervousness, sedation, lightheaded, excitement
- interactions: erythromycin and grapefruit juice
- tolerance: no withdrawl symptoms
Antidepressants
- venlafaxine (Effexor XR):
- short and long term use
- nausea is most common side effect; headache, anorexia, nervousness, sweating, insomnia and hypertension
Panic Disorder
- palpitations, punding heart, chest pain or discomfort, short of breath, dixxy/light headed, nausea, fear of losing control or dying, numbness in hands, and chills or flushes
- treat: cognitive behavioural therapy
- drug therapy: antidepressants and benzodiazepines
OCD
- treat: behavioural therapy
- drug therapy: selective serotonin reuptake inhibitors
SSRIs
- used for OCD
- first line of defense
Social Anxiety Disorder
- intense and irrational fear that one will be scrutinized by others
- treat: psychotherapy
- drug therapy: SSRIs, paroxetine, and sertraline
