Lecture 5 Flashcards

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1
Q

Sedative-Hypnotic Drugs: Benzodiazepines

A
  • Share the same basic chemical structures and pharmacological effects
  • Indicated for sleep, anxiety, or both
  • Less chance for lethal overdose
  • boosting the effect of GABA
    • pam or lam endings
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2
Q

Sedative - Hypnotic drugs: Nonbenzodiazepines: Barbiturates

A
  • CNS depressants with common chemical origin of barbituric acid
  • Addictive
  • Prolonged use often leads to drug abuse
  • Occasionally used for hypnotic / sleep properties
    • can be used in general anesthesia
    • barbital ending
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3
Q

Sedative - Hypnotic drugs: Nonbenzodiazepines: Other

A
  • GABA receptors
  • As effective as benzodiazepines in promoting sleep with fewer side effects - shorter duration of action
  • Other drugs that facilitate sleep: Antihistamines, Antidepressants, Antipsychotics, Anticonvulsants, Opioid analgesics
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4
Q

Sedative - Hypnotic drugs: Pharmacokinetics

A
  • Highly lipid soluble, so reach CNS easily
  • Typically administered orally
  • Distribution fairly uniform throughout the body
  • Metabolized by oxidative enzymes in the liver
  • Excretion through the kidney
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5
Q

Side effects of Sedative-Hypnotic drugs

A
  • Residual effects: Drowsiness, poor motor performance
  • Tolerance and physical dependence
  • Complex behaviors
  • Other: GI discomfort, dry mouth, sore throat, muscular incoordination. Cardiovascular and respiratory depression in overdose
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6
Q

Antianxiety Drugs: Benzodiazepines

A
  • Share the same basic chemical structures and pharmacological effects
  • Indicated for sleep, anxiety, or both
  • Less chance for lethal overdose
  • boosting the effect of GABA
  • Increase inhibition in the spinal cord to produce skeletal muscle relaxation
    • pam or lam endings
  • Side effects: sedation, addiction, abuse, and withdrawal
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7
Q

Antianxiety Drugs: Buspirone

A
  • Serotonin agonist that stimulates specific receptors
  • Less motor and sedation side effects than benzodiazepines
  • Lower risk for tolerance, dependence, and abuse
  • Only moderately effective
  • May be helpful in neurological issues that are influenced by serotonin
  • Side effects: Dizziness, headache, nausea, restlessness
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8
Q

Antianxiety Drugs: Other

A
  • First line anxiety medications: fewer side effects, lower risk for tolerance, dependence, and abuse than benzodiazepines
  • beta blockers
  • Antipsychotics
  • Anticonvulsants
  • Antihistamines
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9
Q

Scheduling of peak effects for benzodiazepines

A
  • 2 to 4 hours
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10
Q

Benzodiazepines and other sleep medications are associated with?

A
  • fall risk, trauma
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11
Q

Antidepressant drugs - SSRIs

A
  • Selective serotonin reuptake inhibitors
  • Blocking the reuptake of serotonin in the presynaptic terminal
  • Allows serotonin to remain in the synaptic cleft and exert effects for longer
    • often first choice
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12
Q

Antidepressant drugs - SNRIs

A
  • Serotonin-norepinephrine reuptake inhibitors (SNRIs)
  • Decreasing serotonin and norepinephrine reuptake without an appreciable effect of dopamine synapses
  • good for chronic pain, osteoarthritis, peripheral neuropathies, and fibromyalgia
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13
Q

Side effects of SSRIs and SNRIs

A
  • GI symptoms
  • Less sedation than tricyclic antidepressants and other drugs
  • Low incidence of cardiovascular problems and anticholinergic effects
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14
Q

Antidepressant drugs - Tricyclics

A
  • share a common 3-ring structure
  • blocking the reuptake of amine neurotransmitters in the presynaptic terminal
  • No very selective in effects, tend to affect synapses in all 3 primary amines (serotonin, norepinephrine, and dopamine)
  • More interactions with other drugs
  • Usually when people have failed to respond to other antidepressants
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15
Q

Side effects of tricyclics

A
  • Major problem is sedation
  • significant anticholinergic effect
  • Increased incidence of orthostatic hypotension
  • Increased seizure risk
  • Highest potential for lethal overdose from an antidepressant: cardiac arrhythmias
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16
Q

Antidepressant drugs - Monoamine oxidase (MAO) inhibitors

A
  • Allow more neurotransmitter to remain in the synaptic cleft and continue to exert an effect
  • High incidence of side effects and can be dangerous if taken with food that contains tyramine such as avocade
  • Phenelzine, Trimipramine
  • Side effects: CNS excitation, Anticholinergic effects, increased blood pressure
17
Q

Other compounds for treating depression

A
  • Trazadone ( Desyrel) and nefazodone (Serzone) block serotonin receptors while simultaneously inhibit serotonin reuptake
  • May help normalize serotonin influence in the brain
  • Trazodone: used “off label” for insomnia, anxiety, chronic pain, sexual dysfunction, and eating disorders
18
Q

Bupropion (Wellbutrin)

A
  • Work primarily as a dopamine and norepinephrine reuptake inhibitor
19
Q

Pharmacokinetics of Antidepressants

A
  • Usually taken orally
  • Dose usually started low and ramped up
  • Metabolized in the liver, excreted by kidneys
20
Q

Antidepressants and chronic pain

A
  • chronic pain syndromes improve with antidepressant
  • evidence of helping even when no depressive symptoms are present
  • affect pain through actions on CNS monoamine neurotransmitters
21
Q

Duloxetine (Cymbalta)

A
  • only antidepressant that is FDA approved to treat pain
22
Q

Lithium: Treating Bipolar Disorder

A
  • Mood stabilizer
  • Primary drug for bipolar disorder
  • orally, absorbed in the GI tract, eliminated in urine
  • high dose for acute manic episode
  • Not metabolized: accumulation can be a problem
  • Adverse effects: can accumulate in the body and lead to lithium toxicity
23
Q

Anti-seizure and Antipsychotic medications

A
  • can prevent neuronal excitation, stabilized mood, and prevent manic symptoms
24
Q

Psychosis

A
  • severe forms of mental illness
  • Schizophrenia: 1% of the population
  • Delusions, Hallucinations, disorganized speech, grossly disorganized or catatonic behavior
25
Q

Antipsychotics

A
  • Block dopamine
  • Normalize dopamine and serotonin in the brain
  • Mainly orally, but can be intramuscularly
  • Metabolized in the liver
  • can be used as antiemetics
  • can be used in dementia
26
Q

Antipsychotics: Extrapyramidal Symptoms: Tardive dyskinesia

A
  • May be irreversible
  • Involuntary sucking noises
  • can lead to dysphagia
  • 20 to 25% of people on “traditional” antipsychotics
  • Risk Factors: increased age, genetic predisposition, affective mood disorders, diabetes, history of alcohol abuse, using the drug more than 6 months
  • maybe caused by “disuse supersensitivity” of the dopamine receptor
  • Treated by lowering the dose, changing the medication
27
Q

Antipsychotics: Extrapyramidal Symptoms: Psuedoparkinsonism

A
  • Antipsychotics block dopamine receptors
  • Motor symptoms of Parkinson disease are caused by deficiency in dopamine transmission in the basal ganglia
  • Parkinson-like symptoms: Resting tremor, Bradykinesia, Rigidity
  • Elderly patients more susceptible
28
Q

Antipsychotics: Extrapyramidal Symptoms: Akathisia

A
  • Motor restlessness, an inability to sit or lie still
  • Agitation
  • Insomnia
  • Successfully treated by changing the dose
  • Can also use a beta blocker
29
Q

Antipsychotics: Extrapyramidal Symptoms: Other

A
  • Dyskinesia
  • Dystonia
  • Neuroleptic malignant syndrome
30
Q

Antipsychotics: Nonmotor effects

A
  • Metabolic effects: Weight gain, Increased plasma lipids, Diabetes
  • Sedation effects: Do not enhance the antipsychotic efficacy of the drug
  • Anticholinergic effects
  • Orthostatic hypotension in the first few days
  • Withdrawal effects when coming off the medication
31
Q

Importance of Antipsychotic drugs

A
  • Drugs tend to “normalize” patient behavior
  • Drugs improve confusion and paranoia
  • Serious side effects can be first to notice in changes in posture, balance, mood, motor function
  • Orthostatic hypotension when drug first administered