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161 Cards in this Set
- Front
- Back
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What is Prozac?
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Fluoxetine (SSRI)
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What is Paxil?
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Paroxetine (SSRI)
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What is Zoloft?
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Sertraline (SSRI)
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What is Luvox?
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Fluvoxamine (SSRI)
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What is Cipralex?
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Escitalopram (SSRI)
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What is Celexa?
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Citalopram (SSRI)
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Name 6 selective serotonin reuptake inhibitors (SSRIs):
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Fluoxetine
Paroxetine Sertraline Citalopram Escitalopram Fluvoxamine |
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What is Wellbutrin?
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BupropIon - NDRI (norepinephrine/dopamine reuptake inhibitor)
In addition to Wellbutrin for MDD, buproprion also marketed as Zyban for smoking cessation |
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How long does it typically take to start seeing results with SSRIs?
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4-6 weeks
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What are common side effects of SSRIs?
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Psych: Can cause activation (mania, anxiety, insomnia) OR sedation, increased risk of suicide in young patients
Dizziness/headache Nausea/vomiting Sexual dysfunction Serotonin syndrome Discontinuation syndrome |
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What is Haldol?
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Trade name for haloperidol, typical neuroleptic
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What is flupentixol?
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Typical neuroleptic
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What is Zyprexa?
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Trade name for olanzapine, atypical neuroleptic
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What is clozapine?
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Atypical neuroleptic
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What is Risperdal?
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Risperidone, atypical neuroleptic
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What is clozapine and what chemical is it related to structurally?
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Atypical neuroleptic, closely related to olanzapine
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What is Seroquel?
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Trade name for quetiapine, atypical neuroleptic
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What is Abilify?
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Aripiprazole, atypical neuroleptic
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What is Valium?
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Diazepam, benzodiazepine
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What is Ativan?
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Lorazepam, a quick-onset, short acting benzodiazepine
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What is Thorazine?
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Chlorpromazine, typical neuroleptic
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What are "tranquilizers"?
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Imprecise term referring to tranquility-inducing drugs
Minor tranquilizers: anxiolytics Major tranquilizers: neuroleptics (antipsychotics) Antimanic agents can also be considered tranquilizers |
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Name 8 typical neuroleptics:
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1) Chlorpromazine (thorazine)
2) Fluphenazine 3) Methotrimeprazine 4) Perphenazine 5) Loxapine 6) Pimozide 7) Haloperidal 8) Flupentixol |
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What is fluphenazine?
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Typical neuroleptic (antipsychotic)
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What is methotrimeprazine?
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Low potency typical neuroleptic with strong analgesic and antiemetic properties
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What is loxapine?
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Typical neuroleptic
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What is perphenazine?
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Typical neuroleptic
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What is pimozide?
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Typical neuroleptic
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What is Haldol?
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Haloperidal, typical neuroleptic
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What is flupentixol?
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Typical neuroleptic
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Name 8 atypical neuroleptics:
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The "typical" atypicals:
1) Clozapine 2) Olanzapine 3) Risperidone 4) Quetiapine The "atypical" atypicals: 5) Aripiprazole (Abilify) 6) Amisulpride 7) Paliperidone (Invega) 8) Ziprasidone (Zeldox, Geodon) |
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What is Invega?
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Paliperidone, "atypical" atypical neuroleptic
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What is a depot injection and which atypical neuroleptic is available in this form?
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Injection of pharmacological agent which releases its active compound in a consistent way over a long period of time
Risperidone |
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Which antipsychotic is associated with agranulocytosis?
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Clozapine
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What is the mechanism of action of typical neuroleptics?
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Dopamine blockade (D2 receptor antagonism)
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What is an agonist?
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Chemical that binds to the receptor of a cell and triggers a response by that cell
Agonists often mimic the action of naturally occurring substances |
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What is an antagonist?
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Chemical that does not provoke a biological response itself upon binding to a receptor but rather blocks or dampens the affect of an agonist
In other words, antagonists bind to receptors, thus "blocking" the effect that an agonist might have on that receptor |
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What is an inverse agonist?
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Chemical that binds to the same receptor as an agonist but provokes the opposite affect as the agonist
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What is an agonist-antagonist?
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Simply a chemical that has some properties of an agonist and some properties of an antagonist
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What are the major dopaminergic pathways in the brain?
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1) Mesocortical pathway - Ventrotegmental area to frontal cortex
2) Mesolimbic pathway - ventrotegmental area (VTA) to the nucleus accumbens (NA) in the ventral striatum 3) Nigrostriatal pathway - substantia nigra (SN) to the 4) Tuberoinfundibular pathway |
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What is Epival?
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Trade name for valproate semisodium (valproic acid), a mood stabilizer and anticonvulsant.
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What drugs can lithium react with to tip patients into toxicity?
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ACE inhibitors, diuretics, NSAIDS can increase lithium levels
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Is lithium safe for pregnant women?
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NO!!!
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What is the dose of valproic acid for long-term mood stabilization?
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750-3000 mg
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What blood levels of valproic acid are safe and therapeutic for long term mood stabilization?
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350-750 mmol/L
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What is Depakene?
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Trade name for valproic acid
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What are the psychiatric indications for valproic acid?
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Acute mania
Long term mood stabilization Agitation Aggression Borderline Personality Disorder |
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Is valproic acid safe to use during pregnancy?
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NO!!!
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What effect does valproic acid have on liver enzymes?
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Inhibits hepatic enzymes, slows down hepatic metabolism
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What anticonvulsants are used as mood stabilizers?
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Valproate, carbamazepine, lamotrigine
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What effect does carbamazepine have on liver enzymes and other drugs?
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Induces liver enzymes (speeds them up), lowers levels of other drugs
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What effect does carbamazepine have on oral contraceptives?
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Lowers their efficacy
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What is Stevens-Johnson syndrome?
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Hypersensitivity reaction that results in life threatening rash, separation of epidermis from dermis.
Severe potential side effect of lamotrigine (Lamictal) |
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Which atypicals are associated with the most weight gain? The least?
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Moste: Clozapine, olanzapine
Least: Risperidone, quetiapine |
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What are the effects of hyperprolactinemia?
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Women: amenorrhea, galactorrhea, sexual problems
Men: gynecomastia |
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Which atypicals are the most sedative/hypnotic?
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Olanzapine, quetiapine
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What is the therapeutic dosage of quetiapine (Seroquel) for psychosis?
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300-600 mg daily
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What is Geodon?
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Ziprasidone, an "atypical atypical," also marketed as Zeldox
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What is the severe potential side effect of ziprasidone (Zeldox)?
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Arrhythmia, prolonged QT interval
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What is the advantage of aripiprazole? The disadvantage?
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Advantage: less EPS and TD than typicals, less metabolic problems than atypicals
Disadvantages: none yet... |
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What is the therapeutic dose of aripiprazole (Abilify)?
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10-15 mg daily, maximum 30 mg
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Which are the "atypical" atypicals? What's so atypical about them?
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Ziprasidone (Geodon)
Aripiprazole (Abilify) Paliperidone (Invega) Amisulpride Have less EPS and TD like other atypicals, but also have less metabolic side effects |
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When are neuroleptics indicated/used for other than for psychosis?
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Mania (after mood stabilizers, benzos tried)
Treatment resistant OCD Agitation in demented patients Nausea in cancer patients after Gravol Tourette's Syndrome Borderline Personality Disorder Augmentation in Personality Sedation? No, try hypnotic or benzo because of risk of TD |
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How do you manage EPS?
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Anticholinergics:
Benztropine (Cogentin) Diphenhydramine (Benadryl) |
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What is Valium?
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Diazepam
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What kind of receptor is the GABA receptor, and what does ligand binding to this receptor accomplish?
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Ionotropic receptor (ligand-gated ion channel attached to receptor)
Binding causes chloride channel to open, chloride ions to enter cell, and hyperpolarization to occur In other words, activation of the GABA receptor causes an inhibitory postsynaptic potential (IPSP) |
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What is Ativan?
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Trade name for lorazepam, benzodiazepine
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What are the clinical uses of benzodiazepines?
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Psych:
Anxiolytic (to reduce anxiety) Hypnotic (to induce sleep) Sedative/tranquilizer (to reduce agitation) Neuro: Anticonvulsant MSK: Muscle relaxant |
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What is Valium?
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Trade name for diazepam, benzodiazepine
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Name 6 benzodiazepine drugs:
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1) Diazepam
2) Clonazepam 3) Chlordiazepoxide 4) Lorazepam 5) Oxazepam 6) Temazepam |
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What is Librium?
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Chlordiazepoxide, a longer-acting benzodiazepine drug
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Benzodiazepines work great. What are their drawbacks and limitations?
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1) Patients can become addicted and abuse benzodiazepines
2) Patients can develop dependence with severe withdrawal symptoms Because of this, benzos should only be used short term (days, weeks, months) and be tapered down slowly Benzos only mask symptoms, they don't cure the problem |
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What is the mechanism of action of benzodiazepine drugs?
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GABA A receptor agonists (hyperpolarize neuron by opening chloride channels)
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What are the difference between the various benzodiazepines?
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1) Differences in how quickly they start to work (onset of action)
2) Differences in how long they work for (duration) 3) Differences in their potential for abuse/dependence |
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Name three intermediate to long acting benzodiazepines:
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Diazepam, clonazepam, chlordiazepoxide
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What is Rivotril?
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Clonazepam, long acting benzodiazepine
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Name 3 short-to-intermediate-acting benzodiazepines:
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Lorazepam, oxazepam, temazepam
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What are the three "Z drugs," what is their mechanism of action, and what is their clinical indication?
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Zolpidem
Zopiclone Zaleplon These drugs are non-benzodiazepine GABA receptor agonists that bind to the same receptor site as benzos. Clinical indication: hypnotics for insomnia (i.e. to catch some zzzs) |
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What are the symptoms of benzodiazepine withdrawal?
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Anxiety, insomnia, agitation
Severe: seizures |
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What are barbiturates? What is their mechanism of action? Where does their name come from?
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Barbiturates are derivatives of barbituric acid.
Barbituric acid was discovered by Adolf von Baeyer in 1864. Possibly named for Saint Barbara, possibly for a waitress named Barbara whose urine he used to get the urea for the synthesis of barbituric acid. Barbiturates are GABA receptor agonists. They bind to a site on the receptor that is different than the site for GABA and benzodiazepines. The effect, however, is similar. They cause opening of the ion channel, chloride influx and an overall inhibitory effect on the postsynaptic neuron. |
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Why have benzodiazepines effectively replaced barbiturates in clinical practice?
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Lower risk of lethal overdose
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What are some of the more colourful uses of barbiturates?
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Euthanasia and capital punishment
Truth serum |
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What is the clinical indication for buspirone?
What is its MOA? |
Anxiolytic used especially in GAD
Partial serotonin receptor agonist |
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What are the advantages of buspirone over benzos for anxiety?
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Non-sedating
Little chance of dependency/abuse |
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What is the dosage of buspirone?
How long does it take buspirone to start working? |
5-30 mg daily, sometimes more, 1-2 week lag time
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What drug is indicated for benzodiazepine overdose?
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Flumazenil
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What is lorazepam mostly used as? What about clonazepam?
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Lorazepam mainly used as hypnotic, clonazepam as axiolytic
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What two kinds of stimulants are used to treat ADHD/ADD?
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Dextro-amphetamine (DEX) based products (e.g. Adderall)
Methylphenidate (MPH) based products (e.g. Ritalin, Concerta) |
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What is Adderall?
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Trade name for dextroamphetamine salts-based medication
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What is Vyvanse? What are the advantages of Vyvanse?
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Lisdexamfetamine, prodrug that is converted to DEX, may see less abuse because onset of action is delayed
Lasts 13-14 hours |
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What are the methylphenidate (MPH)-based stimulants used in managing ADHD? What are the differences between them?
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Ritalin
-5,10, 20 mg tablets -immediate release -lasts around 3 hours Ritalin SR -20 mg -slow release -lasts 4-8 hours Concerta - 18, 27, 36, 54 mg -22% immediate release, 78% delayed release -lasts 10-12 hours -generic Concerta has different release formula Biphentin -10, 15, 20, 30, 40... -40% immediate release, 60% delayed release -lasts 10-12 hours -can sprinkle on food |
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Theoretically, how do stimulants help relieve symptoms of ADHD?
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Not well understood, though it's thought that these drugs stimulate those areas of the frontal lobe responsible for inhibiting impulses
I.e. they enhance executive function |
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What are the side effects of stimulants?
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Anorexia
Restlessness, irritability, insomnia Strokes, MI, and sudden death reported with all stimulatns in adults and in children Dysphoria or sadness Headache |
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What is PCP?
What is another street name for PCP? |
Phencyclidine
OR 1-(1-phenylcyclohexyl)piperidine) OR Angel dust |
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What is a releasing agent (RA)?
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Drug that induces the release of a neurotransmitter from the presynaptic neuron into the synaptic cleft
Also known simply as a releaser |
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What percentage of children with ADHD will see improvement with treatment with MPH or DEX stimulants?
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70-80% if different stimulants are tried in a systematic way
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What natural alkaloid are amphetamines similar to structurally?
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Ephedrine, derived from various plants of the genus Ephedra
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What is tryptamine? What is the structural heart of tryptamine?
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Tryptamine is a monoamine alkaloid found in many plants, fungi, and animals.
The structural heart of tryptamine is the indole ring. Besides being a neurotransmitter/neuromodulator itself, tryptamine is the biological backbone for a number of other molecules, including serotonin and melatonin, that are collectively called the tryptamines. |
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What is indigo dye?
What is the etymology of indigo? Who was the first to synthesize indigo, and when? What is the relationship of indigo to indole? |
Indigo dye is an organic compound with a distinctive blue colour, originally only available from the plant Indigofera tinctoria. It is the blue of blue jeans.
Indigo originally came from India, hence its name. Adolf von Baeyer first synthesized it in 1878, revolutionizing the trade in indigo. Von Baeyer was also the first to synthesize indole, using indigo as a substrate. The two chemicals are related etymologically for this reason. |
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Describe the structure of indole:
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Bicyclic aromatic compound
Composed of a six-membered benzene ring fused to a five-membered nitrogen-containing pyrrole ring In other words, it's a benzene ring fused to a pyrrole ring |
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What is the mechanism of action of dextroamphetamine and methylphenidate stimulants?
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MA releasing agents (DA, NA, 5-HT)
MA reuptake inhibitors (DA, NA, 5-HT) Reversal of MA transporter action Inhibition of MAO Pretty much everything except an MA receptor agonist The net effect is to increase the synaptic concentrations of dopamine, norepinephrine, and serotonin. Because of their effects on norepinephrine, amphetamines are sympathomimetic |
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What is the mechanism of action of MDMA?
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Similar to that of other amphetamines and methylphenidates:
MA releasing agent (DA, NA, 5-HT) MA reuptake inhibitor (DA, NA, 5-HT) MAO inhibitor The net effect is to increase the synaptic concentrations of dopamine, norepinephrine, and serotonin. Because of its effects on norepinephrine, MDMA is sympathomimetic |
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What is the MOA of cocaine?
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MA reuptake inhibition leading to increased synaptic levels of DA, NA, and 5-HT
Sympathomimetic because of its inhibitory effect on NA reuptake |
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What is the mechanism of action of phencyclidine?
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NMDA receptor antagonist
Sigma receptor antagonist |
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What is the function of sigma receptors? Which ligands are known to bind to these receptors?
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Originally thought to be a type of opiod receptor but not any more. Function currently unknown
DMT and phencyclidine both bind to this receptor |
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What is Effexor?
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Trade name for venlaxafine, an SNRI
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What is Cymbalta?
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Trade name for duloxetine, an SNRI
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What is the mechanism of action of bupriopion (Wellbutrin)?
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NDRI (noradrenaline/dopamine reuptake inhibitor)
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Give the generic and trade names of two SNRIs:
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1) Venlaxafine (Effexor)
2) Duloxetine (Cymbalta) |
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What is Zeldox?
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Trade name for ziprasidone, atypical neurolpetic
Also marketed as Geodon |
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What is clomipramine?
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TCA
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What is amitryptiline?
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TCA
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What is nortryptaline?
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TCA
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What is desipramine?
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TCA
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Name 5 tricyclic antidepressants:
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1) Clomipramine
2) Nortryptaline 3) Amitryptiline 4) Imipramine 5) Desipramine |
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What is imipramine?
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TCA
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What is the downside of tricyclic antidepressants?
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Risky side effect profile, lethal in overdose, cardiotoxic
Blocks alpha 1 adrenergic receptors Blocks muscarinic cholinergic receptors Blocks H1 histamine receptors A bit of a blunt hammer, in other words |
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What is the mechanism of action of tricyclic antidepressants?
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In effect, TCAs are SNRIs, inhibiting the reuptake of both NA and 5-HT
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In addition to NA and 5-HT reuptake inhibition, which 3 receptors do TCAs notoriously block to cause side effects? What side effects do they cause?
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Alpha 1 adrenergic receptors
-postural hypotension Muscarinic cholinergic receptors -blurred vision, dry mouth, constipation, urinary retention H1 histamine receptors -sedation |
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What is Valdoxan?
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Agomelatine, a melatonin receptor agonist and antidepressant
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What are the clinical uses of TCAs?
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2nd line therapy for depression
Enuresis Neuropathic pain |
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What does NaSSA stand for?
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Noradrenergic and specific serotonergic antidepressant (e.g. mirtazapine)
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What class does mirtazapine belong to?
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NaSSAs (noradrenergic and specific serotonergic antidepressants)
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What is Remeron?
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Mirtazapine, NaSSA
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What is the mechanism of action of NaSSAs?
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NaSSAs like mirtazapine (Remeron) work by antagonising specific noradrenergic (alpha 2) and serotonin (5-HT2 and 5-HT3) receptors
Antagonism of the alpha 2 receptor prevents an inhibitory effect on 5-HT transmission Antagonism of the 5-HT2 and 5-HT3 receptors reduces the side effect profile |
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What's the typical dosage for mirtazapine?
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15-45 mg/day
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What is the advantage of NaSSAs over SSRIs?
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Less sexual side effects, less nausea
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Name 5 drug classes considered first line treatment for depression:
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1) SSRIs (e.g. escitalopram)
2) SNRIs (e.g. duloxetine) 3) NDRIs (e.g. bupropion 4) NaSSAs (e.g. mirtazapine) 5) Melatonin-receptor agonists (e.g. agomelatine) |
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What is agomelatine?
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Melatonin receptor agonist used to treat depression, marketed as Valdoxan
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What is moclobemide?
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Reversible monoamine oxidase inhibitor
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What is phenelzine?
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Irreversible monoamine oxidase inhibitor
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Name a reversible monoamine oxidase inhibitor:
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Moclobemide
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Name an irreversible monoamine oxidase inhibitor:
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Phenelzine
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What drugs are used to treat Alzheimer's Dementia?
How much improvement will people see? |
Cholinesterase inhibitors:
Donepezil (5-10mg) -Aricept Rivastigmine (1.5 - 6 mg BID) -Exelon Galantamine (8-24 mg) -Reminyl ER Very |
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What is Aricept?
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Donepezil, cholinesterase inhibitor
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What are the side effects of cholinesterase inhibitors for AD?
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Neuro: headache, dizziness, syncope
GI: nausea/vomiting, diarrhea, anorexia Nasal congestion Nightmares |
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What are the symptoms of cholinergic crisis? In other words, describe the cholinergic toxidrome.
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Severe nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression
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What is memantine?
What is its MOA? |
Memantine is an NMDA receptor antagonist.
It is used in combination with cholinesterase inhibitors to treat AD. |
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What are the serious long term complications of lithium therapy?
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Renal dysfunction (metabolized by kidney)
Thyroid dysfunction - hypothyroidism Benign WBC elevation Cardiac disturbances: arrhythmias (rare) |
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What work up do you want to do before starting someone on lithium?
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1) Pregnancy test
2) TSH 3) Kidney function tests 4) CBC (lithium can raise leukocyte levels) 5) Baseline EKG (lithium can cause arrhythmias) |
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What are the common acute side effects of lithium?
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Weight gain
Nausea/vomiting Tremor |
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What is the workup before putting someone on valproic acid?
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Pregnancy test
LFTs CBC (can cause thrombocytopenia) |
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What is the starting dose of Epival?
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250 BID
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What are the side effects of Epival?
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Weight gain
Hepatotoxicity Thrombocytopenia |
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What's the advantage of lamotrigine over lithium and Epival?
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Less weight gain
Very good at reducing depressive symptoms and as a prophylactic, not effective in treating acute mania |
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What are the mood stabilizers, in order of use (i.e. first line, second line, etc...)
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1) Lithium
2) Epival 3) Lamotrigine 4) Carbamazepine |
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Which atypicals have high quality evidence in treating acute mania?
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Olanzapine, quetiapine, risperidone
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What are the first line treatments for acute mania?
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Lithium
Epival Atypicals: olanzapine, quetiapine, risperidone |
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What is Epival?
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Divalproex sodium, an anticonvulsant and mood stabilizer
Active component: valproic acid |
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How do you treat bipolar depression?
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Lithium first line
Antidepressants can be used, but watch out for flips into mania, not as effective as lithium |
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What is Reminyl?
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Galantamine, an acetylcholinesterase inhibitor used to treat dementia
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What's the first line pharmacotherapy for Tourette's?
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Neuroleptics
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Name a common side effect of methylphenidate:
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Tics
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What is Reminyl?
What is it used for? How does it work? |
Galantamine
Used to treat mild to moderate Alzheimer's Galantamine is an acetylcholinesterase inhibitor, increases synaptic acetylcholine concentration |
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What is Ebixa?
What is it used for? How does it work? |
Memantine
Used to treat dementia NMDA receptor antagonist (blocks glutamate binding to NMDA receptor) |
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What is Cogentin?
What is it used for? How does it work? |
Cogentin is the trade name for benztropine, or benzatropine
Benztropine is an anticholinergic drug that works in a similar fashion to atropine. It is a muscarinic receptor antagonist |
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What is Benadryl?
What is it used for in psychiatry? |
Benadryl is the trade name for diphenhydramine
Diphenhydramine is an anticholinergic drug that works similar to atropine and benztropine. It works as a muscarinic receptor antagonist. Diphenydramine (Benadryl) is used to treat the EPS side effects of antipsychotics. |
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How are the extrapyramidal symptoms (EPS) of antipsychotic medications managed?
Name two drugs used to treat EPS: |
Anticholinergic drugs.
So far I haven't figured out why. Antipsychotics themselves may have anticholinergic side effects, so I'm not sure why introducing an anticholinergic would help with symptoms Two drugs used: Benztropine (Cogentin) Diphenhydramine (Benadryl) These drugs are muscarinic receptor antagonists similar to atropine |
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Name three classes of drugs used in psychiatry that have potent anticholinergic effects:
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1) Antipsychotics
-the weaker the antipsychotic, the greater the anticholinergic effects 2) Anticholinergics used to treat EPS -Benztropine and diphenhydramine 3) Tricyclic antidepressants |
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Sum up the relationship between the potency of antipsychotic drugs and their anticholinergic side effects
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More potent antipsychotics (those with greater D2 receptor affinity) have fewer anticholinergic side effects
Less potent antipsychotics (those with less affinity for the D2 receptor) have greater anticholinergic side effects More potent antipsychotics cause more EPS but have less anticholinergic side effects. These are the most likely to have to be supplemented with anticholinergics (benztropine, dephenhydramine) to control EPS |
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Describe the anticholinergic toxidrome:
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Delirium
Mydriasis Flushing Dry mucous membranes Tachycardia Decreased GI motility Urinary retention "Mad as a hatter, blind as a bat, hot as hare, red as a beet, dry as a bone" |
