psychopharmacology Flashcards
What are psychoactive drugs also known as?
Psychotropic drugs
They act on the central nervous system and generate physical, cognitive, and behavioral changes.
What are the two categories of antipsychotic drugs?
First generation and second generation
What are first-generation antipsychotics also known as?
Traditional and conventional antipsychotics
Name two examples of first-generation antipsychotics.
- Chlorpromazine (Thorazine)
- Haloperidol (Haldol)
What symptoms are first-generation antipsychotics more effective in treating?
Positive symptoms
How do first-generation antipsychotics primarily exert their therapeutic effects?
By blocking dopamine (especially D2) receptors
What are the three categories of major side effects of first-generation antipsychotics?
- Anticholinergic side effects
- Extrapyramidal side effects
- Neuroleptic malignant syndrome
What are anticholinergic side effects most likely associated with?
Low potency FGAs
List some examples of anticholinergic side effects.
- Dry mouth
- Blurred vision
- Urinary retention
- Constipation
- Tachycardia
What are extrapyramidal side effects most likely associated with?
High-potency FGAs
Name some extrapyramidal side effects.
- Parkinsonism
- Dystonia
- Akathisia
- Tardive dyskinesia
What is tardive dyskinesia?
A potentially life-threatening side effect characterized by involuntary, rhythmic movements
What treatment options are available for tardive dyskinesia?
- Gradually withdrawing the drug
- Administering a benzodiazepine
- Switching to a second-generation antipsychotic
What is neuroleptic malignant syndrome (NMS)?
A rare life-threatening side effect of antipsychotics
What are some symptoms of neuroleptic malignant syndrome?
- Muscle rigidity
- High fever
- Autonomic dysfunction
- Altered mental state
What should be done at the first sign of neuroleptic malignant syndrome symptoms?
Stop taking the drug and provide supportive therapy
What are second-generation antipsychotics also known as?
Atypical antipsychotics
Name two examples of second-generation antipsychotics.
- Clozapine (Clozaril)
- Risperidone (Risperdal)
How do second-generation antipsychotics primarily alleviate positive symptoms?
By blocking dopamine (especially D3 and D4) receptors
How do second-generation antipsychotics alleviate negative and cognitive symptoms?
By blocking serotonin receptors
What is a significant advantage of second-generation antipsychotics over first-generation antipsychotics?
Less likely to cause extrapyramidal side effects
What is metabolic syndrome associated with second-generation antipsychotics?
Substantial weight gain, high blood pressure, insulin resistance, hyperglycemia, increased risk for diabetes mellitus and heart disease
What dangerous conditions can clozapine and other SGAs cause?
Neutropenia and agranulocytosis
What is required for patients taking clozapine?
Regular blood tests
Fill in the blank: Clozapine is the only FDA-approved antipsychotic for _______.
treatment-resistant schizophrenia
What are the major types of antidepressants?
The major antidepressants include:
* SSRIs
* SNRIs
* NDRIs
* TCAs
* MAOIs
These classes of antidepressants are differentiated by their mechanisms of action and side effect profiles.
What are SSRIs and what do they primarily treat?
SSRIs are selective serotonin reuptake inhibitors used primarily to treat:
* Major depressive disorder
* Persistent depressive disorder
* Premenstrual dysphoric disorder
* OCD
* Panic disorder
* Generalized anxiety disorder
* PTSD
* Bulimia nervosa
* Premature ejaculation
Common SSRIs include fluoxetine, fluvoxamine, paroxetine, sertraline, and citalopram.
How do SSRIs exert their therapeutic effects?
SSRIs exert their therapeutic effects by blocking the presynaptic reuptake of serotonin, increasing its availability in the synaptic cleft.
This mechanism classifies SSRIs as serotonin agonists or indirect agonists.
What are some advantages of SSRIs over TCAs?
Advantages of SSRIs over TCAs include:
* Fewer side effects
* Safer in overdose
* Safer for older adults
SSRIs are less cardiotoxic and have a better safety profile.
What are common side effects of SSRIs?
Common side effects of SSRIs include:
* Mild anticholinergic effects
* Gastrointestinal disturbances
* Insomnia
* Anxiety
* Sexual dysfunction
Abrupt cessation can lead to discontinuation syndrome.
What is serotonin syndrome and what causes it?
Serotonin syndrome is a potentially fatal condition caused by:
* Combining an SSRI with an MAOI, lithium, or other serotonergic drugs.
Symptoms include extreme agitation, confusion, autonomic instability, and seizures.
What is tachyphylaxis in the context of SSRIs?
Tachyphylaxis, or antidepressant tolerance, occurs when a patient loses a previously effective antidepressant response despite staying on the same drug and dosage.
Common signs include apathy, fatigue, and sleep disturbances.
What are SNRIs and what conditions do they treat?
SNRIs include venlafaxine, duloxetine, and desvenlafaxine, treating:
* Major depressive disorder
* Social anxiety disorder
* Neuropathic pain
SNRIs inhibit the reuptake of serotonin and norepinephrine.
What are the side effects of SNRIs?
Side effects of SNRIs are similar to those of SSRIs and can include:
* Discontinuation syndrome
* Serotonin syndrome
* Elevated blood pressure
Caution is advised for patients with hypertension.
What are NDRIs and their primary uses?
NDRIs, such as bupropion, are used to treat:
* Major depressive disorder
* Smoking cessation
They inhibit the reuptake of norepinephrine and dopamine.
What are the advantages of bupropion?
Advantages of bupropion include:
* Few anticholinergic effects
* No sexual dysfunction
* Not cardiotoxic
It’s energizing, suitable for low energy patients.
What are TCAs and how are they categorized?
TCAs are tricyclic antidepressants categorized as:
* Tertiary amines (e.g., amitriptyline)
* Secondary amines (e.g., nortriptyline)
They inhibit the reuptake of serotonin and norepinephrine.
What are common side effects of TCAs?
Common side effects of TCAs include:
* Cardiovascular effects
* Anticholinergic effects
* Sedation
* Weight gain
* Sexual dysfunction
Secondary amines generally have fewer side effects.
What are MAOIs and their primary use?
MAOIs, such as phenelzine and tranylcypromine, are used for:
* Treatment-resistant depression
* Atypical depression
They inhibit the enzyme monoamine oxidase, increasing norepinephrine, serotonin, and dopamine levels.
What are potential side effects of MAOIs?
Potential side effects of MAOIs include:
* Anticholinergic effects
* Orthostatic hypotension
* Sedation
* Sexual dysfunction
They can cause hypertensive crisis with certain foods or medications.
What are the categories of psychoactive drugs mentioned?
Sedatives, Hypnotics, and Anxiolytics; Narcotic-Analgesics (Opioids); Beta-Blockers
These categories encompass various drugs used for different therapeutic purposes.
Name three examples of benzodiazepines.
Diazepam (Valium), Alprazolam (Xanax), Lorazepam (Ativan)
Benzodiazepines are primarily used to treat anxiety, insomnia, seizures, and alcohol withdrawal.
What is the primary action of benzodiazepines?
Increase GABA activity
GABA is an inhibitory neurotransmitter that helps reduce neuronal excitability.
List common side effects of benzodiazepines.
- Drowsiness
- Sedation
- Weakness
- Unsteadiness
- Impaired memory and concentration
- Anticholinergic effects
- Sexual dysfunction
- Disorientation and confusion in older adults
These side effects can vary in severity depending on the individual.
What can chronic use of benzodiazepines lead to?
- Tolerance
- Dependence
- Withdrawal symptoms
Withdrawal symptoms may include rebound anxiety, depression, anorexia, delirium, and seizures.
What is the importance of gradual tapering when discontinuing benzodiazepines?
To prevent symptom reemergence and severe withdrawal symptoms
The tapering schedule depends on factors like the benzodiazepine dose and half-life.
True or False: Combining benzodiazepines with alcohol can be lethal.
True
The combination creates a synergistic depressant effect.
Name three examples of barbiturates.
Thiopental (Pentothal), Amobarbital (Amytal), Secobarbital (Seconal)
Barbiturates enhance GABA activity and are used in various medical treatments.
What are the side effects of barbiturates?
- Drowsiness
- Dizziness
- Confusion
- Ataxia
- Cognitive impairment
- Paradoxical excitement
These effects can impact a person’s ability to function normally.
What is the function of azapirones, and name one example.
Used to treat generalized anxiety disorder; Example: Buspirone (BuSpar)
Azapirones do not cause sedation, dependence, or tolerance.
What are narcotic-analgesics, and what do they mimic?
They mimic the effects of the body’s natural analgesics (endorphins and enkephalins)
These drugs are used for pain relief and anesthesia.
List examples of natural and synthetic narcotic-analgesics.
- Natural: Opium, Morphine, Heroin, Codeine
- Synthetic: Methadone, Oxycodone, Hydrocodone, Fentanyl
Methadone is also used for heroin detoxification.
What are common side effects of narcotic-analgesics?
- Dry mouth
- Nausea
- Pupil constriction
- Postural hypotension
- Drowsiness
- Dizziness
- Constipation
- Respiratory depression
Overdose can lead to convulsions, coma, and death.
What are initial withdrawal symptoms from narcotic-analgesics similar to?
The flu
Symptoms include runny nose, watery eyes, nausea, and muscle aches.
What is the role of beta-blockers?
Inhibit the activity of the sympathetic nervous system
They are used to treat various conditions including hypertension and anxiety.
Give an example of a beta-blocker and its side effects.
Propranolol (Inderal); Side effects include hypotension, decreased sex drive, insomnia
Propranolol is noted for alleviating somatic symptoms of anxiety.
What happens if beta-blockers are abruptly discontinued?
Can cause rebound hypertension, tremors, headaches, confusion, and cardiac arrhythmia
Gradual tapering is recommended to avoid these effects.
What are mood stabilizers used to treat?
Bipolar disorder
Mood stabilizers include lithium and anticonvulsant medications.
What is the first-line drug for acute mania and classic bipolar disorder?
Lithium (Eskalith, Lithobid)
Lithium is effective for euphoric mania without rapid cycling.
List common side effects of lithium.
- Nausea
- Vomiting
- Diarrhea
- Metallic taste
- Increased thirst
- Weight gain
- Hand tremor
- Fatigue
- Impaired memory and concentration
Regular monitoring of lithium levels is necessary to avoid toxicity.
What can lithium toxicity cause?
- Seizures
- Coma
- Death
Lithium levels must be regularly checked.
What are the anticonvulsant drugs used for treating bipolar disorder?
Carbamazepine (Tegretol) and valproic acid (Depakene)
These are used for acute mania and mixed episodes.
List common side effects of anticonvulsant drugs.
- Nausea
- Dizziness
- Sleepiness
- Lethargy
- Ataxia
- Tremor
- Visual disturbances
- Impaired concentration
Blood levels must be monitored to avoid serious side effects.
What drugs are used to treat Alzheimer’s disease?
Cholinesterase inhibitors and NMDA receptor antagonist
These drugs slow the progression of Alzheimer’s disease.
Name some cholinesterase inhibitors used for Alzheimer’s disease.
- Tacrine (Cognex)
- Donepezil (Aricept)
- Rivastigmine (Exelon)
- Galantamine (Razadyne)
All four are approved for mild and moderate Alzheimer’s disease.
Which cholinesterase inhibitor is also approved for severe Alzheimer’s disease?
Donepezil (Aricept)
Tacrine is not commonly prescribed due to serious side effects.
What is the role of the NMDA receptor antagonist memantine in Alzheimer’s treatment?
Regulates the activity of glutamate
Memantine (Namenda) is approved for moderate to severe Alzheimer’s disease.
What are the first-line pharmacological treatments for ADHD?
Psychostimulants
Include methylphenidate, pemoline, and amphetamine-dextroamphetamine.
List some common side effects of psychostimulants used for ADHD.
- Insomnia
- Nervousness
- Decreased appetite
- Weight loss
- Abdominal pain
These drugs can suppress growth in children but can be reversed with drug holidays.
What is a potential issue with using stimulant drugs in college students and adults without ADHD?
They may not improve reading comprehension and fluency
Evidence suggests negative effects on working memory and academic performance.
Name some second-line medications for ADHD.
- Atomoxetine (Strattera)
- Guanfacine (Intuniv)
- Clonidine (Kapvay)
These are prescribed when patients cannot tolerate stimulants or have significant comorbidities.
What is atomoxetine’s mechanism of action?
Norepinephrine reuptake inhibitor
It is the most commonly prescribed nonstimulant for ADHD.
What are the third-line pharmacological treatments for ADHD?
- Tricyclic desipramine (Norpramin)
- NDRI bupropion (Wellbutrin)
These also increase dopamine and norepinephrine levels.
Which drugs are used to treat alcohol use disorder?
- Disulfiram (Antabuse)
- Naltrexone (ReVia)
- Acamprosate (Campral)
- Topiramate (Topamax)
Disulfiram causes unpleasant symptoms when combined with alcohol.
What is the action of naltrexone in treating alcohol use disorder?
Reduces pleasurable effects and craving for alcohol
Acamprosate primarily reduces craving.
What types of medications are used to treat tobacco use disorder?
- Nicotine replacement therapy (NRT)
- Bupropion
- Varenicline
NRT helps prevent withdrawal symptoms.
What is the FDA-approved treatment for cocaine use disorder?
None
Research has not strongly supported any particular drugs for effectiveness.
Which drugs have shown some evidence of effectiveness for increasing abstinence in cocaine use disorder?
- Bupropion
- Topiramate
- Psychostimulants (e.g., modafinil, dextroamphetamine)
A recent meta-analysis suggested these may be helpful.
What is the main active ingredient of cannabis?
Tetrahydrocannabinol (THC)
THC stimulates the release of dopamine in the ventral striatum.
What psychoactive effects does THC exert?
Stimulating the release of dopamine in the ventral striatum
This is part of the brain’s mesolimbic dopaminergic reward pathway.
What is Dronabinol oral solution (Syndros) approved for?
Treatment of anorexia and weight loss for patients with AIDS and chemotherapy-induced nausea and vomiting
Approved by the U.S. FDA.
Which two psychedelic drugs have received breakthrough therapy designations from the FDA?
- A form of LSD for generalized anxiety disorder
- Psilocybin for major depressive disorder and treatment-resistant depression
What is the role of serotonin in the action of psychedelic drugs?
Psychedelic drugs are serotonin agonists, increasing the effects of serotonin
LSD also increases the effects of dopamine, while psilocybin alters glutamate levels.
What is the definition of drug half-life?
The time needed for the blood level of the drug to decrease to 50% of its peak level.
How does drug half-life affect dosing intervals?
Short half-life drugs require shorter dosing intervals, and longer half-life drugs require longer intervals.
What should be considered when prescribing drugs to older adults?
Start low and go slow
This means starting at a low dose and gradually increasing it.
What is drug tolerance?
A gradual reduction in a drug’s effects requiring higher doses to achieve the same effect.
What is cross-tolerance?
Tolerance to one drug resulting in tolerance to other drugs in the same class.
What does the therapeutic index (TI) measure?
A drug’s safety.
How is therapeutic index calculated in animal studies?
LD50 divided by ED50 (LD50/ED50).
What do LD50 and ED50 represent?
- LD50: Lethal dose for 50% of the test sample
- ED50: Effective dose for 50% of the test sample.
What is the significance of a narrow therapeutic window?
TI equals 1.0 or less, indicating the drug is not very safe and requires close monitoring.
What characterizes a drug with a wide therapeutic window?
ED50 is lower than LD50 or TD50, making it safer.