Pharmacology- Cns Drugs Ii

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Drugs used to calm patient and help them sleep:

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sedative-hypnotics

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2 main types of sedative-hypnotics:

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benzodiazepines

others

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Uses for benzodiazepines:

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sedative-hypnotic
epilepsy
muscle relaxant
antianxiety

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Pharmacokinetics of sedative-hypnotics:

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administered orally
distributed fairly evenly
may have reservoir effects
metabolized in liver
excreted through kidneys

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Example of a sedative-hypnotic benzodiazepine:

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flurazepam (Dalmane)

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Mechanism of benzodiazepine:

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binds to GABAa receptor, increasing GABA's inhibitory effects

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Benefit of benzodiazepines:

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less chance of lethal overdose than barbiturates

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Problems assoc. with benzodiazepines:

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residual effects
risk of tolerance
physical dependence

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Barbiturates uses:

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general anesthesia*
promote sleep
antiseizure

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Mechanism of barbiturates:

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binds to GABAb receptor, increasing GABA's inhibitory effects

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At low doses, barbiturates primarily affect:

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reticular formation
limbic system

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At high doses, barbiturates primarily affect:

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spinal cord
other areas of brain

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Problems with barbiturates:

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low TI
risk of dependence and abuse
risk of fatal overdose

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zolpidem (Ambien) mechanism:

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affects GABA a1 receptor...causes sedation

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Benefits of Ambien:

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effective as benzodiazepines, with fewer side effects and less risk of dependence

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Residual effects of sedative-hypnotics:

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drowsiness
decreased motor performance the next day

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2 types of antianxiety drugs:

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benzodiazepines

others (antidepressants, seratonin agonists, beta blockers)

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Prototypical antianxiety benzodiazepine:

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diazepam (Valium)

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PT implications for sedative-hypnotics and antianxiety meds:

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do PT @ peak effect or not?
increased falls risk
may be able to decrease need for these meds (breathing, exercise, massage, yoga)

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2 typical presentations of affective disorders:

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major depressive disorder

bipolar disorder

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Pathophysiology of depression:

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thought to be a problem with amine NT metabolism or reuptake

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3 types of antidepressants:

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tricyclics
MAO inhibitors
second-generation drugs (SSRIs)

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Goal of antidepressants:

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increase amine neurotransmission

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Pharmacokinetics of antidepressants:

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administered orally
metabolized in liver

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Antidepressants can also be used as adjunct tx in...

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chronic pain
(neuropathic, fibromyalgia, LBP)

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Mechanism of tricyclics:

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block reuptake of amine NTs into presynaptic terminal

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Example of a tricyclic:

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Elavil

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Problems with tricyclics:

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sedation
central and periph anticholinergic effects (confusion, cardiac)
highest potential for suicidal use

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Mechanism of MAO inhibitors:

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inhibit MAO, the enzyme that metabolizes amine NTs in the nerve ending

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Use MAO inhibitors when...

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other antidepressants aren't effective
other antidepressants have intolerable side effects

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MAO inhibitor interactions:

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cheese/wine/other drugs--increase in sympathetic activity

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Problems with MAO inhibitors:

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restlessness
irritability
confusion
cardiac
hypertensive crisis

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Mechanism of SSRIs

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selectively block serotonin reuptake

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Examples of SSRIs:

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fluoxetine (Prozac)
sertraline (Zoloft)

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Often the initial drug prescribed for depression:

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SSRI

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Side effects with SSRIs

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generally fewer than others
GI
insomnia
seratonin syndrome (shivering, restlessness, dystonia)

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Goal of bipolar tx:

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stop mania from beginning
lessen mood swings

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Treatments for bipolar:

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lithium
valproic acid (antiseizure)
risperidone (antipsychotic)

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Mechanism of lithium:

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may compete with other + charged ions, influencing neural excitability

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Pharmacokinetics of lithium:

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absorbed easily from GI tract
excreted by kidneys

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Rehab concerns for antidepressants:

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depression could be related/unrelated to reason for PT

may help pt take a more active role in PT

side effects can be troublesome

effects take a few weeks to kick in

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Psychoses definition:

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group of mental d/os
marked thought disturbance
impaired perception of reality
delusions, hallucinations, grossly disorganized thinking

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Types of psychoses:

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schizophrenia
psychotic depression
severe paranoid disorders
bipolar (sometimes)

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2 types of antipsychotics (neuroleptics):

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traditional

atypical

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Purpose of antipsychotics:

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normalize thinking and behavior

prevent recurrence

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Other uses of antipyschotics:

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during manic phase of bipolar
to decrease psychotic sx in PD or Alzheimers

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Pathophysiology of schizophrenia:

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overactivity of dopamine pathways in the limbic system?

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Most antipsychotics block...

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central dopamine receptors

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Example of a traditional antipsychotic:

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haloperidol (Haldol)

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Example of an atypical antipsychotic:

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risperidone (Risperdal)

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Why are atypical antipsychotics often the first choice?

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fewer side effects
less involved in motor fx
less pt to pt variability
better at preventing relapse

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Problems/rehab concerns with antipsychotics:

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extrapyramidal sx (tardive dyskinesia, pseudoparkinsonism, restlessness, neuroleptic malignant syndrome

sedation

OH

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Pharmacokinetics of ethanol:

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absorbed quickly
metabolized in gut and liver

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Pharmacodynamics of ethanol:

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increases effects of vasodilators and oral hypoglycemic agents

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Major goals of alcohol withdrawal syndrome:

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prevent seizures, DTs, arrhythmias

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DTs:

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delirium tremens--total disorientation, hallucinations, marked abnormal vital signs