Lecture 5 Flashcards
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
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
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
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
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
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
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
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
9
Q
Scheduling of peak effects for benzodiazepines
A
- 2 to 4 hours
10
Q
Benzodiazepines and other sleep medications are associated with?
A
- fall risk, trauma
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
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
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
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
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
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
Antipsychotics
- 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
Antipsychotics: Extrapyramidal Symptoms: Tardive dyskinesia
- 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
Antipsychotics: Extrapyramidal Symptoms: Psuedoparkinsonism
- 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
Antipsychotics: Extrapyramidal Symptoms: Akathisia
- Motor restlessness, an inability to sit or lie still
- Agitation
- Insomnia
- Successfully treated by changing the dose
- Can also use a beta blocker
29
Antipsychotics: Extrapyramidal Symptoms: Other
- Dyskinesia
- Dystonia
- Neuroleptic malignant syndrome
30
Antipsychotics: Nonmotor effects
- 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
Importance of Antipsychotic drugs
- 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
