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Effects of Psychoactive Drugs - Agonists
produce effects similar to those produced by a neurotransmitter.
Direct agonists exert their effects by mimicking the effect of a neurotransmitter at a receptor site, while indirect agonists attach to a binding site on a receptor cell (a site other than the one used by the neurotransmitter) and facilitate the action of the neurotransmitter.
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Effects of Psychoactive Drugs - Inverse Agonists
produce an effect opposite the effect produced by a neurotransmitter or an agonist.
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Effects of Psychoactive Drugs - Partial agonists
produce effects that are similar (but less than) the effects produced by a neurotransmitter or an agonist
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Effects of Psychoactive Drugs - Antagonists
produce no activity in the cell on their own but, instead, reduce or block the effects of a neurotransmitter or agonist.
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Drugs on older adults
Medication-related problems are a common cause of hospital admissions for people over 65.
Changes in sensitivity are due to age-related changes in drug absorption, distribution, metabolism, and excretion.
General rule for prescribing to older people is start low and go slow.
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Drugs and Race/Ethnicity
Some ethnic dissimilarities in drug response have been linked to differences in metabolism - Asian and to a lesser degree blacks are slower and poorer metabolizers than whites making them more sensitive to therapeutic and side effects of drugs.
begin with a low dose and gradually titrate upward until desired effect
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Name the class of drug - Chlorpromazine
Thorazine - conventional antipsychotic
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Name the class of drug - Fluphenazine
Prolixin - conventional antipsychotic
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Name the class of drug - Thiothixene
Narvane - conventional antipsychotic
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Name the class of drug - Haloperidol
Haldol - conventional antipsychotic
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Name the class of drug - Clozapine
Clozaril - Atypical antipsychotic
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Name the class of drug - Risperidone
Risperdal - Atypical antipsychotic
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Name the class of drug - Olanzapine
Zyprexa - Atypical antipsychotic
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Name the class of drug - Quetiapine
Seroquel - Atypical antipsychotic
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Name the class of drug - Amitriptyline
Elavil, Endep - Tricyclic antidepressant
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Name the class of drug - Doxepin
Sinequan, Adapin - Tricyclic antidepressant
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Name the class of drug - Imipramine
Trofranil - Tricyclic antidepressant
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Name the class of drug - Clomipramine
Anafranil - Tricyclic antidepressant
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Name the class of drug - Nortriptyline
Pamelor - Tricyclic antidepressant
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Name the class of drug - Fluoxetine
Prozac - SSRI
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Name the class of drug - Fluvoxamine
Faverin, Luvox - SSRI
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Name the class of drug - Paroxetine
Paxil - SSRI
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Name the class of drug - Sertraline
Zoloft - SSRI
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Name the class of drug - Isocarboxazid
Marplan - MAOI
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Name the class of drug - Phenelzine
Nardil - MAOI
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Name the class of drug - Tranylcypromine
Parnate - MAOI
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Name the class of drug - Diazepam
Valium - Anxiolytic (benzodiazepine)
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Name the class of drug - Alprazolam
Xanax - Anxiolytic (benzodiazepine)
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Name the class of drug - Oxazepam
Serax - Anxiolytic (benzodiazepine)
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Name the class of drug - Triazolam
Halcion - Anxiolytic (benzodiazepine)
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Name the class of drug - Chlordiazepoxide
Librium - Anxiolytic (benzodiazepine)
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Name the class of drug - Lorazepam
Ativan - Anxiolytic (benzodiazepine)
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Antipsychotic Drugs - Traditional (Conventional) Antipsychotic Drugs - Use
Effective for alleviating psychotic symptoms and are most often prescribed as a treatment for schizophrenia. Also used to treat acute mania, delusions and hallucinations associated with MDD, and organic psychoses.
Much less effective for negative symptoms
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Antipsychotic Drugs - Traditional (Conventional) Antipsychotic Drugs - Mode of Action
Exert their effects by blocking dopamine receptors in the brain (especially D2 receptors).
Led to the dopamine hypothesis - schizophrenia = overactivity of dopamine receptors due to oversensitivity or excessive levels
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Antipsychotic Drugs - Traditional (Conventional) Antipsychotic Drugs - Side Effects
anticholinergic, extrapyramidal, and neuroleptic malignant syndrome
anticholinergic effects - dry mouth, blurred vision, urinary retention, constipation, tachycardia, and delayed ejaculation. Usually develop tolerance within a few weeks or months.
Extrapyramidal effects - Parkinsonism (rigidity, tremors, and bradykinesia), akathisia (extreme motor restlessness), acute dystonia (muscle spasms in the mouth, face, and neck), and tardive dyskinesia (most serious)
neuroleptic malignant syndrome - characterized by a rapid onset of motor, mental, and autonomic symptoms including muscle rigidity, tachycardia, hyperthermia, and alter consciousness. Must stop drug or could be fatal
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Atypical (Novel) Antipsychotic Drugs - Use
Used to treat schizophrenia and other disorders with psychotic symptoms. Clozapine has been found useful for treating Bipolar Disorder that has not responded to a mood stabilizer, depression and suicidality, alcohol and drug addiction, hostility, and the motor symptoms of Huntington's disease, Parkinson's disease, and other movement disorders.
Can alleviate positive and negative symptoms but have a slower onset of therapeutic effects than traditional antipsychotics
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Atypical (Novel) Antipsychotic Drugs - Mode of Action
Act of D4 and other dopamine receptors as well as receptors for other neurotransmitters including serotonin and glutamate
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Atypical (Novel) Antipsychotic Drugs - Side Effects
include anticholinergic effects (blurred vision, dry eyes/mouth, constipation, urinary retention), lowered seizure threshold, and sedation.
Extrapyramidal side effects are much less common (except akathisia [an inability to remain still]); and less likely to cause tardive dyskinesia
Can cause agranulocytosis (a marked decrease in certain white blood cells) and requires careful blood monitoring
Can also cause neuroleptic malignant syndrome
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Several terms are used to describe the effects of the psychoactive drugs: For example, _______ produce effects similar to those produced by a neurotransmitter, while ________ produce no activity on their own but reduce or block the effects of a neurotransmitter. Because of the increased risk for adverse side effects, a general rule when prescribing drugs for older adults and members of some ethnic minority groups is to __________
agonists
antagonists
start low and go slow
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The traditional antipsychotic drugs are used primarily as a treatment for ________ and are especially effective for alleviating its _________ symptoms such as delusions and hallucinations.
schizophrenia
positive
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Research on the effects of the traditional antipsychotic drugs provides support for the dopamine hypothesis, which attributes schizophrenia to __________ to dopamine or excessive dopamine levels. These drugs are associated with several undesirable side effects including ________ effects (dry mouth, constipation, blurred visions, etc.) and extrapyramidal symptoms. Of the latter, _______ is the most serious side effect, but its symptoms may eventually decrease if the drug is _________. Neuroleptic __________ is characterized by a rapid onset of muscle rigidity, tachycardia, hyperthermia, and altered consciousness.
oversensitivity
anticholinergic
tardive dyskinesia
gradually withdrawn
malignant syndrome
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The atypical antipsychotic drugs (e.g., clozapine) are associated with several advantages. They alleviate both the _________ symptoms of schizophrenia and are often effective when traditional drugs have failed. In addition, they are less likely to produce ________ and other extrapyramidal side effects (except akathisia). However, they can cause _________ or other blood dyscrasias.
positive and negative
tardive dyskinesia
agranulocytosis
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Antidepressant Drugs - Tricyclics (TCAs) - Use
Most effective for depressions that involve decreased appetite and weight loss, early morning awakening and other sleep disturbances, psychomotor retardation, and anhedonia.
Particularly useful for alleviating the vegetative, somatic symptoms of depression.
Take 2-4 weeks to work so ECT is sometimes preferred
Also used for panic disorder, agoraphobia, bulimia, OCD (clomipramine), enuresis in children and adolescents (imipramine), and neuropathic pain.
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Antidepressant Drugs - Tricyclics (TCAs) - Mode of Action
block the reuptake of norepinephrine, serotonin, and/or dopamine at nerve synapses.
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Antidepressant Drugs - Tricyclics (TCAs) - Side Effects
anticholinergic but the most serious are cardiotoxic, producing such cardiovascular symptoms as tachycardia, palpitations, hypertension, severe hypotension, and cardiac arrhythmia.
Must be used with caution with people suffering from heart disease.
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Antidepressant Drugs - SSRIs - Use
used to treat depression and are particularly effective for melancholic depression. Several SSRIs are also prescribed for OCD, bulimia, panic disorder, and PTSD
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Antidepressant Drugs - SSRIs - Mode of Action
Block the reuptake of serotonin
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Antidepressant Drugs - SSRIs - Side Effects
gastrointestinal disturbances, insomnia, anxiety, headache, dizziness, anorexia, tremor, frequent urination, sexual dysfunction
Less cardiotoxic, safer in overdose, and are less likely to produce cognitive impairment
Mixing with an MAOI may result in serotonin syndrome and can cause coma or death
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Antidepressant Drugs - MAOIs - Use
most effective for treating non-endogenous and atypical depressions that involve anxiety, reversed vegetative symptoms, and interpersonal sensitivity
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Antidepressant Drugs - MAOIs - Mode of Action
inhibit the enzyme monoamine oxidase, which is involved in deactivating dopamine, norepinephrine and serotonin
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Antidepressant Drugs - MAOIs - Side Effects
The most dangerous is hypertensive crisis, which can occur when an MAOI is taken with barbiturates, amphetamines, antihistamines, or certain other drugs or foods containing tyramine
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Mood Stabilizing Drugs - Lithium - Use
Considered the drug of choice for Bipolar disorder. It reduces manic symptoms and suppresses mood swings
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Mood Stabilizing Drugs - Lithium - Mode of Action
related to the reuptake of serotonin and norepinephrine
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Mood Stabilizing Drugs - Lithium - Side Effects
gastrointestinal, fine hand tremor and shakiness, fatigue, restlessness, polyuria, and polydipsia
The major danger is toxicity, which result from doses that are too high and levels must be closely monitored
must avoid fluctuations in salt intake, caffeine, alcohol, and other diuretics.
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Mood Stabilizing Drugs - Carbamazepine - Use
effective treatment for Bipolar when not responding to lithium. May be more beneficial than lithium for mood swings and dysphoric mania
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Mood Stabilizing Drugs - Carbamazepine - Mode of Action
believed to affect serotonin levels
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Mood Stabilizing Drugs - Carbamazepine - Side Effects
dizziness, ataxia, visual disturbances, anorexia, nausea, and rash, but tolerance develops quickly.
slight risk for agranulocytosis so blood monitoring is required.
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The antidepressants include the TCAs, SSRIs, and MAOIs. The TCAs exert their effect by blocking the reuptake of _________, serotonin, and/or dopamine. There effects on the former supper the _______ hypothesis. Undesirable effects include _________ effects (e.g., blurred vision, dry mouth, constipation), weight gain, drowsiness, and confusion. These drugs are also _________ and can cause hypertension, extreme hypotension, and tachycardia.
norepinephrine
catecholamine
anticholinergic
cardiotoxic
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The SSRIs are particularly effective for _________ depression. They are less cardiotoxic than the TCAs, and safer in _______ and are less likely to produce ___________ impairments. The SSRIs exert their effects by blocking the reuptake of _______. The MAOI is most effective for ________ depression. The most dangerous side effect is hypertensive crisis, which can occur when an MAOI is taken in conjunction with certain drugs and foods containing ________.
melancholic
overdose
cognitive
serotonin
non-endogenous and atypical
tyramine
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Lithium is the drug of choice for classic __________. To avoid toxicity when taking this drug, patients must be careful to avoid fluctuations in their ______ intake and to avoid caffeine, alcohol, and other diuretics. Carbamazepine is an _________ drug that has been found to have similar effects on manic symptoms as lithium and may be more beneficial than lithium for people who experience ________ or who have dysphoric mania
bipolar disorder
salt
anticonvulsant
frequent mood swings
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Sedative-Hypnotics - Barbiturates - Use
In the past, frequently used as sedative and anesthetic agents but, due to recognition of their lethal effects and the development of safer and more effective drugs, they are now infrequently prescribed
Effects range from mild sedation to anesthesia, coma, and death.
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Sedative-Hypnotics - Barbiturates - Mode of Action
interrupt impulses to the reticular activating system
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Sedative-Hypnotics - Barbiturates - Side Effects
slurred speech, nystagmus (eyes make repetitive, uncontrolled movements), dizziness, irritability, and impaired motor and cognitive performance. An overdose can produce ataxia, confusion, agitation, respiratory depression, and death.
Chronic use results in tolerance and psychological and physical dependence.
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Sedative-Hypnotics - Benzodiazepines - Use
primarily used for anxiety relief but also can be used for sleep disturbances, seizures, cerebral palsy, and other disorders involving muscle spasms, and alcohol withdrawal
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Sedative-Hypnotics - Benzodiazepines - Mode of Action
stimulate the inhibitory action of GABA
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Sedative-Hypnotics - Benzodiazepines - Side Effects
Most common are drowsiness, dizziness, lethargy, slurred speech, ataxia, and impaired psychomotor ability
Can create psychological dependence and chronic use can create physical dependence
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Sedative-Hypnotics - Azapirone
the first anxiolytic that reduces anxiety without sedation. It appears non-addictive, non-habit forming, and not subject to abuse.
Must be taken for several weeks before it is effective.
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Beta-Blockers - Use
Used to treat high blood pressure, angina, and other cardiovascular disorders; tremors; migraine headache, and glaucoma.
Been found useful to reduce symptoms of anxiety
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Beta-Blockers - Mode of Action
block beta-adrenergic receptors, which respond to epinephrine and norepinephrine
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Beta-Blockers - Side Effects
bradycardia, shortness of breath, arterial insufficiency (usually of the Raynaud's type), nausea, diarrhea, depression, dizziness, sexual dysfunction, trouble sleeping, and numbness or tingling in the fingers and tows.
Can be lethal for people with respiratory problems
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Narcotic-Analgesics (opioids) - Use
Primarily pain relief
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Narcotic-Analgesics (opioids) - Mode of Action
bind with opioid receptors in the brain
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Narcotic-Analgesics (opioids) - Side Effects
constricted pupils, decreased visual acuity, increased perspiration, constipation, nausea, vomiting, and respiratory depression
Overdose can produce slow and shallow breathing, muscle rigidity, catalepsy, clammy skin, decreased blood pressure and pulse rate, convulsions, coma, and death
Chronic use creates tolerance and dependence
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Psychostimulant - Use
Amphetamines are used to treat narcolepsy and ADHD and methylphenidate is used to treat ADHD in children and adults
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Psychostimulant - Mode of Action
potentiate the release of norepinephrine and dopamine and block their reuptake
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Psychostimulant - Side Effects
amphetamines - restlessness, insomnia, poor appetite, tremor, palpitations, and cardiac arrhythmia. Creates tolerance and dependence and prolonged use can lead to a psychotic state
methylphenidate - decreased appetite, insomnia, dysphoria, abdominal pain, and tachycardia. Symptoms quickly return when drug is stopped
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Anti-Alcohol Drugs - Use
To prevent alcohol use
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Anti-Alcohol Drugs - Mode of Action
Disulfiram (Antabuse) inhibits alcohol metabolism, causing an accumulation of acetaldehyde and unpleasant reactions (severe nausea, vomiting, sweating, headache, tachycardia, and hypotension)
Naltrexone - an opioid receptor antagonist that blocks the craving for and reinforcing effects of alcohol.
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The sedative-hypnotics are generalized ________ depressants that include the barbiturates and anxiolytics. The effects of the sedative0hypnotics are synergistic, and they also produce cross-________. The barbiturates are now rarely prescribed because of their adverse effects. Their use causes a decrease in REM sleep, and abrupt cessation can produce REM _________ and nightmares.
CNS
tolerance
rebound
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The benzodiazepines are the most commonly prescribed anxiolytic. They are associated with several adverse side effects including drowsiness, lethargy, slurred speech, and _______ (lack of muscle coordination). The euphoric feelings produced by the benzodiazepines results in psychological dependence, and chronic use can result in the development of ________ and physical dependence. Withdrawal can produce rebound ________.
ataxia
tolerance
hyperexcitability
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Propranolol and other beta-blockers are used to treat cardiovascular disease, tremor, and migraine headache and have been found useful for reducing the ________ symptoms of anxiety. Propranolol and other beta blockers should not be discontinued ________ because doing so can cause sweating, headache, tremulousness, and cardiac arrhythmia.
physical
abruptly
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The narcotic-analgesics have both sedative and analgesic effects. Research on the effects of these drugs led to the discovery of natural _________ receptors in the spinal cord and brain. Chronic use results in tolerance and _________ dependence.
opioid
psychological and physical
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Amphetamines are currently used to treat _______ and ADHD, while methylphenidate is used to treat the latter disorder. Common side effects of methylphenidate include decreased ________, insomnia, and dysphoria. Higher doses of methylphenidate may cause ________ suppression, but occasional _______ can help minimize this effect. Methylphenidate is contraindicated for people with pre-existing motor tics or a family history of _________.
narcolepsy
appetite
growth
drug holidays
Tourette's Disorder
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Disulfiram and naltrexone are both used to prevent alcohol use. Disulfiram does so by causing _________ that deter and individual from drinking, while naltrexone blocks the ________ and reinforcing effects of alcohol.
unpleasant reactions (symptoms)
cravings
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Practical (or pragmatic) clinical trials (PCTs) are conducted to determine the effectiveness of interventions in typical ________. They tend to be large, ________ trials with hundreds, if not thousands, of participants. Therapeutic Drug Monitoring (TDM) is used in clinical practice to optimize medication regimens by maintaining a specific ______ level in the bloodstream. Three main types of genetic screening techniques are utilized to identify any abnormalities in chromosome structure, protein sequences, or DNA structure: cytogenetic, biochemical, and ________
community settings
simple
concentration
molecular
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Which of the following is most likely to be useful for treating Obsessive-Compulsive Disorder?
A.A drug that blocks the reuptake of serotonin
B.A drug that increases cholinergic activityC.
A drug that blocks the release of GABA
D.A drug that increases the availability of cortisol
A
SSRIs have been found to be effective in treating OCD. The SSRIs block the reuptake of serotonin at nerve synapses.
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A 72-year-old man is prescribed lithium for Bipolar Disorder. In terms of side effects, the man can most likely expect which of the following?
A.Shuffling gait
B.Visual disturbances
C.Shortness of breath
D.Fine hand tremor
D
Fine hand tremor is a common side effect of lithium, especially for older adults. Other common side effects of lithium include gastrointestinal symptoms, shakiness, fatigue, restlessness, polyuria, and polydipsia.
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In comparison to the tricyclics, fluoxetine and other SSRIs:
A.Are more likely to cause cognitive impairment
B.Are less cardiotoxic
C.Have a slower onset of therapeutic effects
D.Are more harmful in overdose.
B
Overall, SSRIs are associated with fewer side effects than the tricyclics. An important advantage of the SSRIs is that they are less cardiotoxic than the tricyclics.
Answer A: The SSRIs are less likely to cause cognitive impairment compared to the tricyclics.
Answer C: The SSRIs have a slightly more rapid onset of therapeutic effects, although both SSRIs and tricyclics can produce an improvement within two to four weeks.
Answer D: The SSRIs are actually safer in overdose.
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The atypical neuroleptic Clozapine (Clozaril):
A.Has a slower onset of therapeutic effects than traditional neuroleptics
B.Is less effective than the traditional neuroleptics for negative symptoms
C.Is more likely than the traditional neuroleptics to produce tardive dyskinesia
D.Does not produce anticholinergic side effects
A
For the exam, you should be familiar with the differences between traditional and atypical neuroleptic (antipsychotic) drugs. A disadvantage of Clozapine and other atypical antipsychotics is that they have a slower onset of effects than the traditional antipsychotics.
Answer B: An advantage of the atypical drugs is that they alleviate both the positive and negative symptoms of Schizophrenia.
Answer C: The atypical drugs are less likely to produce tardive dyskinesia.
Answer D: Anticholinergic side effects are common for atypical antipsychotics
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Drugs that block the activity of _______ produce dry mouth, blurred vision, postural hypotension, urinary retention, and tachycardia.
A.5-HT
B.Glycine
C.ACh
D.Glutamate
C
Acetylcholine (ACh) is one of the neurotransmitters classified as "cholinergic." Drugs that block ACh activity produce anticholinergic effects, including the symptoms listed in the question.
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Therapeutic drug monitoring relies on measuring specific drugs to maintain a concentration in the patient's bloodstream for what purpose?
A.Prevent individuals with substance use disorders from overdosing on illicit substances
B.Optimize dosage regimens
C.Reduce undesired side-effects of medications
D.Identify chromosomal abnormalities that may be affected by specific drugs
B
Therapeutic drug monitoring operates on the assumption that there is a connection between the concentration of a drug in a patient's bloodstream and the therapeutic effects that patient experiences.
Answers A and C: These may occur as a result of therapeutic drug monitoring, but they are not the main goal, thus these are not the best answer choices.
Answer D: Identifying chromosomal abnormalities would occur through genetic testing, not therapeutic drug monitoring.
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