Sedative and Hypnotic Drugs Flashcards
What is the effect of lower doses of S and H drugs?
- Calming effect, pacify patient
2. Decrease anxiety – anxiolytic properties (w/ or w/o sedation)
What is the effect of higher doses of S and H drugs?
- Produce drowsiness
- Initiate relatively normal state of sleep – hypnosis
- General anestesia (highest doses)
What is the general action of S and H drugs?
CNS depressant actions
- epilepsy
- muscle relaxation
What are the uses for S and H drugs?
- Insomnia - 10-15% of people
2. Anxiety
What are the categories of sedative-hypnotic agents?
- For use facilitating sleep
1. Benzodiazepines
2. Non-benzodiazepine hypnotics
MOA: bind to GABA receptors and hyper polarize neurons by helping GABA open chloride ion channels (potentiate effects of GABA);
Used to treat anxiety and produce sedation (Depends on drug and dose); ADRs: Residual effects the next day, Tolerance and physical dependence
Benzodiazepines
- Generally safer than non-benzodiazepine drugs (overdose)
- decrease excitation, resulting in relaxation and sleep facilitation
MOA: potentiate cations of GABA; Act in RF and limbic system to produce general anesthesia; Small therapeutic window – 10X therapeutic dose; Addicting: Prolonged use can be a problem with regards to drug abuse
Barbituates
What are some nonbenzodiazepine drugs that have a hypnotic effect?
- Zolpidem (Ambien)
- Zaleplon (Sonata)
- As effective as benzodiazepines in promoting sleep, but lower risk of adverse effects and difficulties during withdrawal
What are the pharmacokinetics of S and H drugs?
- Most are highly lipid soluble
A – usually oral
D – fairly uniform throughout body – enter CNS because they are lipid soluble
M – Liver
E – Metabolic breakdown;
builds up in fatty tissue, can slowly leak out and produce low levels of sedation, hangover like feelings reported the day after; Kidneys after metabolism by liver
ADRs of S and H
- Residual effects
- Tolerance and Physical Dependence
- Additive actions with other drugs (sedative drugs)
- Alcohol, Antihistamines, Anticholinergic drugs, Antiseizure medications, Opioid analgesics, TCA - Residual effects
- N & V
- Dry mouth
- Sore throat
- Muscular incoordination
- last 4 fairly uncommon
Occur the day after the drug is used to induce sleep; Drowsiness; Decreased motor performance; Anterograde amnesia; Can be resolved by using a smaller dose or a drug with a shorter half-life (newer drug)
Residual effects
What can be done other than drugs that can help reduce stress and promote relaxation?
- Mental imagery
- Biofeedback (exercise)
- Massage
- Relaxation techniques
What drugs are used to treat anxiety?
- Benzodiazepine - frontline drug
- Buspirone (general anxiety)
- Antidepressants (not used for acute anxiety)
- Beta-blockers (block symptoms NS for physical effects)
Serotonin agonist (5 HT recepts); Better side effects than traditional drugs; Less sedation and psychomotor impairment; Smaller risk of tolerance and dependence; Only moderate efficacy and may not act as quickly
Buspirone
ADR: Dizziness, headache, nausea, restlessness
What are ADRs of anti anxiety drugs?
- Sedation
- Psychomotor impairment – particularly in activities which require a person to be mentally alert – driving
- Benzodiazepines: Addiction, abuse, dependence and withdrawal (rebound anxiety)
