05 CNS Update Dopheide Flashcards by Chris Clark

What side effect is often caused by Risperidone?

Muscle stiffness and tremor. Blocks D2 postsynaptically (atypical), leading to pseudoparkinsonism and muscle stiffness

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Why should anticholinergics (eg. Benztropine (Cogentin)) be avoided in people with dementia?

Could exacerbate the dementia (Worsen memory problems)

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What are some common Alzheimers medications?

Donepezil (Aricept), Galantamine (Razadyne), Rivastigmine (Exelon), Memantine (Namenda)

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How does Memantine (Namenda) differ from the other Alzheimer drugs?

Memantine is an NMDA receptor antagonist while the others are ACh Esterase Inhibitors (inhibit breakdown of ACh)

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What are some special considerations for Donepezil (Aricept)?

Most prescribed. Less GI upset vs. Rivastigmine. Long t1/2. Can be combined with Namenda

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What are some special considerations for Galantamine (Razadyne)?

Metabolized 2D6, 3A4. Must TITRATE Q4-6 weeks. Butylcholinesterase activity

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What are some special considerations for Rivastigmine (Exelon)?

Least drug interactions. Short t1/2. Nicotinic receptor activity

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What are some special considerations for Memantine (Namenda)?

Renal impairment: half dose. Constipation. For moderate/severe disease

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What are the common ADRs with the ACh Esterase Inhibitors?

GI upset, HA, Bradycardia (d/t increased ACh which can act on the heart to slow rate, Muscarinic stimulation can also cause nausea)

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How does Risperidone cause dizziness and feeling of lightheadedness?

Through orthostasis. Alpha-1-Adrenergic blockade (blocking the post synaptic alpha receptors in the periphery can cause blood pooling, lower BP)

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What are some considerations with Fluoxetine (Prozac)?

Most activating. Most drug interactions (inhibits 2D6)

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What are some considerations with Sertraline (Zoloft)?

Well-studied for anxiety d/o. Give with foot to increase absorption

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What are some considerations with Paroxetine (Paxil)?

More sleepiness than activation. Anticholinergic. Worse withdrawal

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What are some considerations with Escitalopram (Lexapro) and Citalopram (Celexa)?

Less drug interactions. 2C19 substrates

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What are some considerations with Fluvoxamine (Luvox)?

Approved for OCD. Drug interactions w/ caffeine. Give at bedtime

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Why do Fluvoxamine and Paxil have the worst withdrawals?

No active metabolites, have the worst type of serotonin withdrawal (get more restless, anxious, insomnia)

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What is Citalopram’s (Celexa) new dosing range and why?

20-40 (was 60) d/t unexpected QTc prolongation w/ higher doses

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How can Risperidone worsen osteoporosis?

Blocks dopamine in tubule infundibular track which will elevate Prolactin which can lead to osteoporosis and soft brittle bones and lactation (and gynecomastia in men)

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Why are antipsychotic doses lower in older adults?

Dopamine receptors decrease over time, less dopamine blocking drug needed to cause pseudoparkinson’s and tardive dyskinesia (which can be irreversible). There is an increased risk of death with antipsychotics in elderly

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What are some considerations with Risperidone (Risperdal)?

Highest increase in EPSE and increased prolactin risk of all antipsychotics; substrate of 2D6

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What are some considerations with Olanzapine (Zyprexa)?

Highest metabolic ADRs, high sedation. LAI, Q2-4 weeks

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What are some considerations with Quetiapine (Seroquel)?

Very sedating. Minimal risk of EPSE

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What are some considerations with Aripiprazole (Abilify)?

Minimal metabolic ADRs, activating

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What are some considerations with Paliperidone (Invega, Sustenna)?

Active metabolite of Risperidone. Monthly injection

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Which Antipsychotic(s) cause Orthostasis?

Risperidone

Which Antipsychotic(s) cause QTc prolongation?

Ziprasidone (Geodon)

Which Antipsychotic(s) has the least metabolic ADRs?

Ziprasidone (Geodon)

What is required for Schizophrenia diagnosis?

Needs 6 months of symptoms w/ 1 month active phase and rule out drug causation

What medication is usually used for the First Episode of Schizophrenia, stage 1?

Start with a second generation agent (RISP, OLAN, QUET, ZIPR, ARIP)

What medication is usually used for the Schizophrenia, stage 2 (partial or no response to SGA)?

Switch to alternate SGA or FGA

What medication is usually used for the Schizophrenia, stage 3 (partial or no response to trial of 2nd agent (either SGA or FGA))?

Clozapine (one of the best antipsychotics we have, but lots of ADRs

What are some considerations with Haloperidol (Haldol)?

Liquid. Monthly depot. Levels: 4-12 ng/mL

What are some considerations with Chlorpromazine (Thorazine)?

Poor tolerability long term, very sedating (never start with this drug)

Which 1st Gen Antipsychotics have High EPSE?

Haloperidol (Haldol) and Fluphenazine (Prolixin)

Which 1st Gen Antipsychotic has the highest orthostasis?

Chlorpromazine (Thorazine)

What are 1st Gen Antipsychotics best for?

Treating positive symptoms (hallucinations, delusions). Not as effective for cognitive symptoms

Which antipsychotic is available in a long-acting injectable medication that can be taken monthly?

Paliperidone (Invega) - SGA

Which antipsychotic has a very fast onset of action?

Olanzapine

What do most bipolar patients need?

Antipsychotic and Mood Stabilizer

What are the advantages of Lamotrigine over Lithium?

No weight gain, no tremor, no blood levels needed, good for bipolar depression. Works mainly for depressed phase with bipolar as well as maintenance

What is the first choice as a mood stabilizer in bipolar disorder used with an Antimanic?

Lamotrigine

What are the PROs of Lithium?

It works for all stages of Bipolar disorder, can draw levels to see therapeutic levels (0.8-1.5)

What is the recommended dosing and titration schedule for Lithium?

Start (for 150lb person) 300mg BID, then get level and adjust dose accordingly

What is the recommended dosing and titration schedule for Lamotrigine?

25mg for at least 2 weeks, then increase to 50mg for two weeks, and eventually 100mg (can take up to 8 weeks to get to therapeutic level). Slowly titrated to prevent SJS with LMG (increased risk if used with Valproate)

What are the main Anticonvulsants used?

Carbamazepine. Phenytoin. Valproate. Lamotrigine. Levetiracetam

What are the main side effects found with Anticonvulsants?

Sedation

Which Anticonvulsant is an enzyme inducer?

Carbamazepine (Tegretol) and Phenytoin (Dilantin)

Which dosage form of Phenytoin is preferred?

Extended release preferred, dose in evening

What is a warning with Valproate (Depakene, Depakote)?

Teratogenic

Which Anticonvulsant is renally eliminated and has the least drug interactions?

Levetiracetam (Keppra)

What is a concern with Carbamazepine and Risperidone taken together?

Carbamazepine causes Risperidone blood levels to go down to where it is no longer effective (enzyme induction)

What are the main Benzos used for Anxiety?

Alprazolam (Xanax). Lorazepam (Ativan). Clonazepam (Klonopin). Diazepam (Valium). Not benzo, but used for anxiety: Buspirone (Buspar)

Which Anti-Anxiety medication is difficult to withdrawal?

Alprazolam (Xanax) d/t its short duration and fast onset

Which Anti-Anxiety medication has a rapid onset and high abuse potential?

Diazepam (Valium)

Which Anti-Anxiety medication has no abuse potential and no sexual side effects?

Buspirone (Buspar)

What are some of the main medications used for Insomnia?

Zaleplon (Sonata). Zolpidem (Ambien). Eszopiclone (Lunesta). Triazolam (Halcion). Temazepam (Restoril)

Which Z-hypnotic has the longest half-life?

Eszopiclone (Lunesta: 5 hours)

Which Insomnia agent needs to be taken on an empty stomach?

Eszopiclone (Lunesta)

Which Insomnia agent has a fast onset but can cause rebound insomnia?

Triazolam (Halcion)

What are stimulants first line for?

ADHD

Which stimulants are most well-studied and less likely to exacerbate tics?

Methylphenidate/Dexmethylphenidate: Ritalin LA, Metadate CD, Concerta, Focalin XR

Which stimulants are more potent, with slightly longer duration of action?

Dextroamphetamine, Mixed Amphetamine salts: Dexedrine, Adderall, Adderall XR, Vyvanse

What are the side effects with Stimulants?

Upset stomach (give on full stomach, lower dose, titrate slow). Insomnia (dose early in day). HA (tolerance over time, APAP). Tics (lower dose, change drugs). Dysphoria, irritability (reassess diagnosis, decrease dose, change drugs). Hallucinations (d/c drug). Over-focused, zombie-like (lower dose)

What is Atomoxetine (Strattera)?

Selective NE reuptake inhibitor. Approved for ADHD in children > 6 years, adolescents and adults

What are the advantages Atomoxetine (Strattera)?

No abuse potential, less insomnia, less growth effects, effective if Tourette's disorder or anxiety

What are the disadvantages with Atomoxetine (Strattera)?

Longer onset of therapeutic benefit (2-4 weeks) vs. stimulants, less effective

What are the ADRs for Atomoxetine (Strattera)?

Similar to stimulants, urinary hesitation/retention, more sedation, slightly more increased heart rate

What are some special considerations with Venlafaxine (Effexor)?

Monitor BP. Take with food. Treats refractory patients

What are some special considerations with Duloxetine (Cymbalta)?

Effective for pain. Caution in hepatic disease!

What are some special considerations with Bupropion (Wellbutrin)?

No sexual side effects, not for anxiety. CI: seizure disorder, eating disorder, EtOH or BZD withdrawal

What are some special considerations with Mirtazapine (Remeron)?

No sexual side effects. Check lipid panels

What are some special considerations with Trazodone (Desyrel)?

Used mainly as adjunct for insomnia. Anticholinergic effects

How do Zolpidem peak blood levels and AUC differ in females and elderly?

Levels higher in females, as well as elderly. Elderly females have the highest peak and AUC