Sedatives and Hypnotics

importance of sedative-hypnotic agents

• epilepsy

• muscle relaxation

• reduce anxiety

• decreased alertness

• insomnia (affects 10-15% of population)

pharmacokinetic properties for an ideal hypnotic

• rapid absorption

• no active metabolites

• optimal half-life

pharmacoknetic effects of an ideal hypnotic

• rapid sleep induction

• physiological sleep pattern

• mechanism other than general CNS depression

• sleep maintenance

• improved daytime function

side effects of an ideal hypnotic

• no residual sedation

• no respiratory depression

• no ethanol interaction

• no tolerance

• no physical dependence

• no rebound insomnia

• no effect on memory

benzodiazepines

= GABA+ agonist effect → act on GABA receptors

• hyperpolarize chloride currents

rohypnol

7-10x stronger than valium and effective in 20-30 mins, roofie

xanax generic name

alprazolam

valium generic name

diazepam

klonopin generic name

clonazepam

ativan generic name

lorazepam

halcion generic name

triazolam

doral generic name

quazepam

restoril generic name

temazepam

side effects of alprazolam that are a concern to PTs

• memory problems

• confusion

• hallucination

• seizures

• weakness

• problems with coordination

short acting benzos and the elderly

• not converted to active intermediates → metabolized directly into inactive products

• elderly have a reduced ability to metabolize long-acting benzos

benzo withdrawal timeline

• first sx in 6-12 hours

• peaks after 2 weeks and then begins to subside

• need to be titrated off of these so withdrawal isn’t bad

signs of withdrawal

• muscle spasms

• seizures

• aches/pains

• anxiety

benzos with alcohol

alcohol multiplies the effects of benzos

nonbenzos-barbituates

• small therapeutic index

• 10x therapeutic dose can be fatal

• very addictive

sodium thiopental or pentothal

= higher cortical function is suppressed making you chatty and cooperative

effects on CNS → benzos

• with increasing doses, benzodiazpines can progressively cause sedation, then hypnosis and then stupor

• does not cause general anethesia since awareness persists

• have anti-anxiety/sedative-hypnotic properties

• some are mm relaxants, most aren’t

effects on CNS → barbiturates

• depress respiratory drive

• at doses 3x higher than required, neurogenic is abolished and the hypoxic respiratory drive is reduced and the chemoreceptor drive is attenuated

• at even higher doses, the hypoxic drive is abolished

what suffix = barbiturates

barbital

ambien

= sleeping pill

• takes 12 hours to get out of your system → not processing things, slow reaction times, increased risk of falls

• don’t drink alcohol or effects increase

GABA effects

binding with the synapse to open channels and inhibit anxiety effects of nerve connections

hormones

= serotonin, norepinephrine, dopamine

• act as neurotransmitters in the nervous system

depression

a result of deficiency in cortical and limbic serotonin, norepinephrine, and dopamine

dopamine

reward, attention, emotional regulation

norepinephrine

fight or flight → arousal and alertness

MAO Inhibiters

inhibit the breakdown of hormones

tricyclics and second-generation drugs

inhibit the reuptake of hormones

tricyclic hormones

block other hormones from binding to the next synapse

SSRI

= selective serotonin reuptake inhibitors

SNRI

= serotonin and norepinephrine reuptake inhibitors

tricyclic common side effects

• tremors

• indigestion

• headache

• dry mouth

• drowsiness

• elevated HR

SSRI common side effects

• sweating

• indigestion and nausea

• headache

• dry mouth

• drowsiness

• sexual side effects

SNRIs common side effects

• tremors

• nausea

• headache

• dry mouth

• blurred vision

• increased BP

• sexual side effects

• nervousness

• dizziness

MAOIs common side effects

• insomnia

• muscle aches

• low BP

• dry mouth

• sexual side effects

• nervousness

• dizziness

• avoid decongestants and certain foods

adverse effects of SSRIs

“S-S-S”

• stomach upset

• sexual dysfunction

• serotonin syndrome

SSRI drugs

“Effective For Sadness, Panic, and Compulsions”

• Escitalopram

• Fluoxetine, Fluvoxamine

• Sertroline

• Paroxetine

• Ciralopram

serotonin syndrome

when there’s TOO much serotonin in body

• changes to mental state

• dry mouth

• sweating or fever

• hypothermia and shock

• diarrhea or nausea

• tremors or reflex changes

• muscle rigidity

• mixing meds

common sx of SSRI discontinuation syndrome

• dizziness

• nausea

• headaches

• irritability

• insomnia

do antidepressants affect weight

yes → 21% increase in risk of >5% weight gain

do antidepressants affect fx rates

yes, higher risk of fx

SSRI and risk of fx with perimenopausal women

• fx rate 76% higher with SSRIs 1 year after starting tx

• 73% higher after 2 years

• 67% higher after 5 years