Term
|
Definition
1. Nonopiod +/- adjuvant
2. opiod for mild to moderate pain +/- nonopiod +/- adjuvant
3. opiod for moderate to severe pain +/- nonopiod +/- adjuvant |
|
|
Term
| first line agents for neuropathic pain |
|
Definition
• Anticonvulsants (e.g., gabapentin, pregabalin)
• Antidepressants (e.g., duloxetine, venlafaxine, amitriptyline) |
|
|
Term
| second-line agents for neuropathic pain |
|
Definition
• Lidocaine patch
• Capsaicin
• Tramadol |
|
|
Term
|
Definition
| NSAIDS, anticonvulsants, antidepressants, topical agents, opiods, others |
|
|
Term
| other medications for pain |
|
Definition
• Local anesthetics
• Bisphosphonates
• Calcitonin
• Capsaicin
• Calcium channel blockers
• Baclofen
• Antidepressants
• Anticonvulsants
• Corticosteroids |
|
|
Term
|
Definition
- Lidocaine (Lidoderm®) patch
• Local anesthetic
• Minimal systemic absorption
• 12 hours on, 12 hours off- Capsaicin
• Depletes substance P from nociceptive nerve fibers
• Causes burning, stinging, erythema |
|
|
Term
| Musculoskeletal Pain agents |
|
Definition
- Spasmolytics
• Baclofen
• Tizanidine
• Cyclobenzaprine (Flexeril®)
• Methocarbamol (Robaxin®)
• Carisoprolol (Soma®)
• Metaxalone (Skelaxin®) |
|
|
Term
|
Definition
• Reduce spasticity (increased basal muscle tone with muscle weakness)
• Avoid in elderly (BEERS criteria drugs)
• Valium (diazepam) most effective benzodiazepine to treat spasticity |
|
|
Term
| Spasmolytics: Baclofen MOA |
|
Definition
| GABAb agonist, facilitates spinal inhibition of motor neurons |
|
|
Term
| has SE: sedation, weakness, constipation. At high doses/intrathecal administration, sudden cessation can precipitate a potentially fatal withdrawal syndrome |
|
Definition
| Baclofen. Can administer intrathecally to reduce dose and hence reduce adverse effects |
|
|
Term
| Spasmolytics: Zanaflex (Tizanidine) MOA |
|
Definition
| Alpha-2 adrenergic agonist in the spinal cord |
|
|
Term
| Has S/E: weakness, sedation, hypotension, xerostomia, bradycardia. Monitor LFTs, caution with psychiatric illness (hallucinations). Reduce dose in renal impairment. Avoid in hepatic impairment |
|
Definition
|
|
Term
| Spasmolytics: Flexeril, Amrix (Cyclobenzaprine) MOA |
|
Definition
| inhibits muscle stretch reflex in spinal cord |
|
|
Term
| Has S/E: drowsiness, dizziness, xerostomia, confusion, hallucinations. Avoid extended-release cap in hepatic impairment, elderly |
|
Definition
| Spasmolytics: Flexeril, Amrix (Cyclobenzaprine) |
|
|
Term
| Spasmolytics: Soma (Carisoprodol) C-IV MOA |
|
Definition
| central depressant, active metabolite meprobamate has anxiolytic and sedative properties |
|
|
Term
| Has S/E: drowsiness, dizziness, headache. Use caution in renal or hepatic impairment. Avoid use >2–3 weeks due to lack of evidence supporting long-term efficacy |
|
Definition
Spasmolytics:
Soma (Carisoprodol) C-IV |
|
|
Term
| Spasmolytics: Robaxin (Methocarbamol) MOA |
|
Definition
| skeletal muscle relaxation by general CNS depression |
|
|
Term
| Has S/E: bradycardia, hypotension, dizziness, drowsiness. Reduce dose in hepatic impairment |
|
Definition
| Spasmolytics: Robaxin (Methocarbamol) |
|
|
Term
| Spasmolytics: Skelaxin (Metaxalone) MOA |
|
Definition
| disrupts spasm-pain-spasm cycle likely through general CNS depression |
|
|
Term
| Has S/E: dizziness, drowsiness, irritability, blood dyscrasias. Avoid in renal and hepatic impairment |
|
Definition
| Spasmolytics: Skelaxin (Metaxalone) |
|
|
Term
| ADD/ADHD medication therapy |
|
Definition
1st line: • Stimulants (effect size ~ 0.9
2nd line:
• Atomoxetine (Strattera®) (effect size ~ 0.6)
• Guanfacine (Intuniv®) (effect size ~ 0.5)
• Clonidine (Kapvay®) (effect size ~ 0.5)
3rd line:
• Bupropion (Wellbutrin®)
• Modafinil (Provigil®) |
|
|
Term
| Common Adverse Effects of stumulants |
|
Definition
• Decreased appetite • Weight loss
• Headache
• Insomnia
• Abdominal pain
• Dizziness
• Nervousness
• Emotional lability
• Dry mouth |
|
|
Term
| Risks Associated with Excessive Use of stimulants |
|
Definition
• Cardiovascular failure
• Irregular heartbeat
• Hypertension
• Paranoia
*Risk increases significantly when used IV or intranasally |
|
|
Term
| has MOA blockade of dopamine transporters (minimal effects on norepinephrine) |
|
Definition
|
|
Term
has MOA Stimulate release of dopamine, norepinephrine
(and serotonin at higher doses) |
|
Definition
| Amphetamines, Dextroamphetamine and mixed amphetamine salts |
|
|
Term
| short-acting methylphenidate agents |
|
Definition
|
|
Term
| intermediate-acting methylphenidate agents |
|
Definition
Ritalin SR®
Metadate ER®
Methylin ER® |
|
|
Term
| long-acting methylphenidate agents |
|
Definition
Metadate CD®
Ritalin LA®
Concerta®
Daytrana®
Quillivant XR®
Quillichew ER®
Aptensio XR® |
|
|
Term
| Dexmethylphenidate agents |
|
Definition
|
|
Term
• 12-hour duration
• Tablet shell eliminated in stool
• Can be taken with or without food
• Cannot crush or chew (less likely to be snorted)
• Late release may cause insomnia |
|
Definition
|
|
Term
• 50/50 mixture of delayed release and IR beads • Contents can be sprinkled on applesauce
• Release is pH dependent (avoid antacids/acid suppressants) • Time to first peak quicker than Concerta® |
|
Definition
|
|
Term
• 70/30 mixture of extended-release and IR beads • Should be taken in the morning before breakfast
• Contents can be sprinkled on applesauce
• Approximately 7-hour duration to cover school day |
|
Definition
|
|
Term
• 60/40 mixture of extended-release and IR beads • 12-hour duration
• Contents can be sprinkled on applesauce |
|
Definition
|
|
Term
• Extended release oral liquid
• 80/20 mixture of extended-release and IR components
• Oral suspension does not require refrigeration • Stable for four months after reconstitution
• 12-hour duration |
|
Definition
|
|
Term
• Long-acting chewable
• 70/30 mixture of extended-release and IR components
• 8-hour duration |
|
Definition
|
|
Term
• Transdermal patch
• Not bioequivalent with oral dosage forms
• Patch can be removed any time to customize stimulant exposure • 2-hour delay in effect after application
• Wear no longer than nine hours per day • Apply to hip, do not cut patches
• May have more insomnia, anorexia, and tics than oral forms |
|
Definition
|
|
Term
• D-threo enantiomer of racemic methylphenidate
• Dose is half of typical methylphenidate doses
• Available in IR (Focalin® ) and extended-release
(Focalin XR®) formulations
• FocalinXR® release is pH dependent: avoid antacids, proton pump inhibitors, and H2 blockers
• FocalinXR® caps can be opened, sprinkled on applesauce |
|
Definition
|
|
Term
|
Definition
| Adzenys XR, Dyanavel, Evekeo |
|
|
Term
|
Definition
| Dexedrine, Dexedrine Spansule |
|
|
Term
| Mixed Amphetamine Salts agents |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| amphetamines, dextroamphetamine, mixed amphetamine salts, lisdexamfetamine |
|
|
Term
| Amphetamine clinical pearls |
|
Definition
• Adzenys XR: first ODT, 50/50 delayed-release and IR particles (similar PK to Adderall XR)
• Dynavel XR: oral suspension, mixture of IR and ER particles
• Vitamin C/fruit juice decreases amphetamine absorption
• Sodium bicarbonate increases absorption |
|
|
Term
| Dextroamphetamine (IR and SR) clinical pearls |
|
Definition
| • IR:Forage>3years;SR:>6years • IR available in liquid |
|
|
Term
| Mixed amphetamine salts (IR and ER) clinical pearls |
|
Definition
• Decreased sense of fatigue, mild euphoria, increased motor activity
• IR:Forage>3years;SR:>6years
• IR can be crushed; ER can be opened and put in
applesauce
• ER: 50:50 mix of IR and ER beads |
|
|
Term
| Lisdexamfetamine clinical pearls |
|
Definition
• Oral prodrug converted to dextroamphetamine
• Transformation to active drug in gut prevents
snorting/injecting
• Longest duration of action of amphetamines
• Amphetamine uptake slower: less euphoric effects
• Capsule can be opened and dissolved in water |
|
|
Term
| Atomoxetine (Strattera®) MOA |
|
Definition
| Selective norepinephrine reuptake inhibitor |
|
|
Term
• Less effective than stimulants
• Slower onset of effect (1–4 weeks)
• Longer treatment duration increases probability of response
• Generic became available recently (2017) |
|
Definition
|
|
Term
has S/E:• Nausea/vomiting, abdominal pain
• Weight loss, ↓ appetite
• Tachycardia
• Headache
• Insomnia
• Hepatotoxicity
• Myocardial infarction
• Priapism |
|
Definition
|
|
Term
Reasonable option for the following populations:
• Patient does not respond to or tolerate stimulants
• Families who want to avoid controlled substances
• Patients or families with history of substance abuse |
|
Definition
|
|
Term
|
Definition
| Guanfacine ER, clonidine ER |
|
|
Term
| Guanfacine ER, clonidine ER MOA |
|
Definition
Inhibit presynaptic norepinephrine release and increase blood flow to
prefrontal cortex (alpha-2 agonists) |
|
|
Term
|
Definition
• Longer half-life and duration of action for guanfacine (18 hrs) compared to clonidine (12 hrs)
• Less sedation and dizziness with guanfacine |
|
|
Term
• Not as effective as stimulants for monotherapy
• May be used to reduce disruptive behavior, control aggression, insomnia, tics |
|
Definition
| Guanfacine ER, clonidine ER. Alpha-2 Agonists |
|
|
Term
|
Definition
| Dopamine reuptake inhibitor |
|
|
Term
| Has ADE: nausea/vomiting, rash, seizure |
|
Definition
|
|
Term
• Delayed onset:~two weeks
• No abuse potential, good for comorbid depression |
|
Definition
|
|
Term
• Wake-promoting stimulant
• Effective in treatment of ADHDsymptoms
• Not approvable letter from FDA due to skin reactions (including Stevens Johnson Syndrome) |
|
Definition
|
|
Term
|
Definition
• Stimulants
• Insomnia from extended medication effects
vs. rebound of ADHD symptoms when meds wear off
• Atomoxetine and alpha-2 agonists usually sedating
• Evaluate sleep quality and type of disturbance
• Change stimulant formulation
• Change medication
• Rule out comorbid sleep apnea or restless legs
• Add sleep agent |
|
|
Term
|
Definition
| • Rarely reported with atomoxetine and methylphenidate |
|
|
Term
| adverse effects have been associated with stimulant treatment? |
|
Definition
| Appetite suppression, tachycardia, tics |
|
|
Term
ADHD and Conduct Disorder/Oppositional Defiant
Disorder management |
|
Definition
• Stimulants have anti-aggressive effects • 2nd line: Behavioral therapy followed by
antipsychotics/VPA/Lithium |
|
|
Term
| ADHD and Bipolar Disorder management |
|
Definition
| • Treat bipolar 1st with mood stabilizer • If ADHD sxs continue, add stimulant |
|
|
Term
| ADHD and Major Depressive Disorder management |
|
Definition
• Treat most disabling condition first
• Depression: CBT, SSRIs, venlafaxine |
|
|
Term
| ADHD and anxiety disorders treatment |
|
Definition
• CBT before or with ADHD treatment
• Consider stimulant or atomoxetine
• Add SSRI if symptoms continue |
|
|
Term
| ADHD and Tic disorders treatment |
|
Definition
• Consider methylphenidate or atomoxetine
• Alpha agonists can improve tics and ADHD sxs |
|
|
Term
| ADHD and substance use disorders treatment |
|
Definition
• 1st: Treat active substance abuse • Can treat both concomitantly
• Use stimulant with low abuse potential or consider non-stimulant |
|
|
Term
|
Definition
• Methylphenidate and amphetamines inhibit monoamine
oxidase->avoid MAOIs
• Methylphenidate can increase blood levels of tricyclic
antidepressants
• CYP2D6 inhibitors increase levels of amphetamine and
atomoxetine
• Combination of stimulants and serotonergic agents (antidepressants/tramadol) may increase seizure or
serotonin syndrome risk
• Use caution co-administering alpha agonists with other
blood pressure lowering medications |
|
|
Term
| Dopamine Mesocortical pathway |
|
Definition
Important for “higher order” cognitive
functions (motivation,
impulse control, emotion) |
|
|
Term
| Dopamine Mesolimbic pathway |
|
Definition
|
|
Term
| Dopamine Nigrostriatal pathway |
|
Definition
|
|
Term
| Dopamine Tubero- infundibular pathway |
|
Definition
|
|
Term
Dopamine Receptor
Antagonist affects |
|
Definition
Mesocortical (prefrontal cortex)
Worsening negative symptoms (anhedonia)
Mesolimbic (basal ganglia)
Relief of positive symptoms (hallucinations)
Nigrostriatal (substantia nigra)
Extrapyramidal symptoms
Tuberoinfundibular (hypothalamus)
Increased prolactin release |
|
|
Term
Dopamine Receptor
Agonist affects |
|
Definition
Mesocortical (prefrontal cortex)
Theorized improvement in negative symptoms
Mesolimbic (basal ganglia)
Reward pathway (addiction), psychosis
Nigrostriatal (substantia nigra)
Target of action for relief of movement disorders in Parkinson’s
Tuberoinfundibular (hypothalamus)
Decrease in prolactin release |
|
|
Term
First Generation Antipsychotics (FGAs)
• MOA |
|
Definition
Blockade of post- synaptic D2 receptors in brain
• Other receptors may be affected, which accounts for differences in side effects
• Ex: Histaminergic, muscarinic, adrenergic |
|
|
Term
| First gen antipsychotic agents |
|
Definition
| Haloperidol, Thiothixene (thio thick scene), Chloropromazine (chlorine pro maze), Thioridazine (thio rid of magazines), Trifluoperazine (try flower pie magazines), Perphenazine (perfect hen magazine), Fluphenazine (floop hen mazagine) |
|
|
Term
Has ADE: • Blockade of D2 receptors in other areas leads to variety of adverse effects
• Nigrostriatal -> movement disorders
• Tuberoinfundibular ->hyperprolactinemia
• Mesocortical ->worsening negative symptoms |
|
Definition
| first generation antipsychotic agents |
|
|
Term
Black box warning for ALL
antipsychotics |
|
Definition
| Increased death associated with treatment in patients with dementia-related psychosis |
|
|
Term
| Has AVE: sedation, EPS, Anticholinergic, Cardiovascular |
|
Definition
| First generation antipsychotics |
|
|
Term
| Chlorpromazine indicxation |
|
Definition
schizophrenia, bipolar disorder (mania), N/V
*Also indicated for treatment of acute intermittent porphyria, presurgical apprehension, intractable hiccoughs, problem behavior (severe), tetanus |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| Trifluoperazine indication |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
Second Generation Antipsychotics (SGAs)
• MOA |
|
Definition
| Post-synaptic D2 and 5HT2A blockade |
|
|
Term
|
Definition
has a unique mechanism of action
• Partial agonist at D2 and 5HT1A receptors • Antagonist at 5HT2A
• High affinity for D2, D3, and 5HT2A /1A |
|
|
Term
| Second generation antipsychotic agents |
|
Definition
| Aripiprazole (abilify), brexpiprazole (rexulti)- break pipe razor, clozapine (clozaril)- closet pine, olanzapine (zyprexa), quetiapine (seroquel), risperidone (risperdal), paliperidone (invega)- palpate dome, lurasidone (latuda), iloperidone (fanapt)- little parrot dome, asenapine (saphris)- aspen pine |
|
|
Term
| 2D6 second generation antipsychotics |
|
Definition
| ariprazole, iloperidone, risperidone (converted to active metabolite paliperidone) |
|
|
Term
| 1A2 second generation antipsychotics |
|
Definition
| Asenazpine, Clozapine, Olanzapine |
|
|
Term
| 3A4 second generation antipsychotics |
|
Definition
| aripiprazole, lurasidone, quetiapine, ziprasidone *Two-thirds of ziprasidone metabolism occurs via aldehyde oxidase and one- third by CYP450 system (3A4). |
|
|
Term
|
Definition
• 1A2
• Smoking induces this enzyme by 20–30%
• May need to adjust dose if changes in smoking status
• Watch for 1A2 inhibitors like fluvoxamine
• 2D6
• Genetic variations between PM, UM, RM*
• 2D6 inhibitors: paroxetine, fluoxetine, and bupropion
• If patient is taking risperidone + 2D6 inhibitor, may not get full effect of antipsychotic
• 3A4
• Many medications are metabolized through this enzyme
• Watch for strong inhibitors such as azole class of antifungals |
|
|
Term
Has ADE: • Metabolicabnormalities(lipidsandglucose)
• Weight gain
• QTc prolongation
• Prolactin elevation
• Sedation
• Akathisia
• Anticholinergic effect
• Orthostatic hypotension |
|
Definition
| second generation antipsychotics |
|
|
Term
|
Definition
|
|
Term
|
Definition
| D2 blockade in nigrostriatal pathway |
|
|
Term
| second generation drugs and weight gain side effect from most likely to least likely to cause |
|
Definition
| Clozapine, Olanzapine -> Quetiapine, Iloperidone -> Risperidone, Paliperdone -> Arpiprazole, Lurasidone, Ziprasidone |
|
|
Term
| second gen antipsychotics and prolactin elevation most likely to cause to least likely to cause |
|
Definition
| Risperidone, Paliperidone -> Lurasidone ,Ziprasidone -> Iloperidone, Olanzapine ,Asenapine -> Quetiapine, Aripiprazole |
|
|
Term
| second gen antipsychotics and sedation SE most likely to cause to least likely to cause |
|
Definition
| Clozapine -> Olanzapine ,Quetiapine ,Ziprasidone -> Asenapine, Risperidone, Lurasidone -> Aripiprazole, Iloperidone, Paliperidone |
|
|
Term
| Antipsychotics and Qtc Prolongation, agents most likely to cause |
|
Definition
| Thioridazine, Ziprasidone |
|
|
Term
|
Definition
| Bipolar Disroder, MDD, Schizophrenia, Autism disorder |
|
|
Term
| Brexpiprazole indicaitons |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Bipolar Disorder, MDD (in combo w fluoxetine), schizophrenia |
|
|
Term
|
Definition
| bipolar disorder, MDD, Schizophrenia |
|
|
Term
|
Definition
| bipolar disorder, Schizophrenia, autism disorder |
|
|
Term
|
Definition
|
|
Term
|
Definition
| bipolar disorder, schizophrenia |
|
|
Term
|
Definition
|
|
Term
|
Definition
| bioplar disorder, schizophrenia |
|
|
Term
| SGA Prescribing Considerations |
|
Definition
• Risperidone
• Clinicalmaxof6–8mg
• >8mgbeginsactingsimilartotypicalantipsychotics • Paliperidone
• DoseadjustmentrequiredwhenCrCl<80mL/min
• Quetiapine
• Highlyanticholinergicmetabolite
• Doses<100mg/dayprimaryactionatH1receptorà no real antipsychotic effect
• Effectonmood:200–400mg/day
• Antipsychoticdoses:500–800mg/day
• Clozapine generally reserved for treatment refractory cases
• Requires registering with clozapine REMS program
• Aripiprazole and lurasidone have higher incidence of akathisia
• Cost to patients |
|
|
Term
|
Definition
• Reservedfortreatmentrefractorycases
• Generallyafterfailureof>twoadequatetrialsof antipsychotics
• Requirespatient,pharmacy,andphysician registration with clozapine REMS program
• Priortoinitiationandthroughouttimeon clozapine, blood draws are required due to risk of neutropenia
• Fiveblackboxwarnings(BBW)associatedwith clozapine |
|
|
Term
| Clozapine: BBW and Adverse Effects |
|
Definition
| myocarditis (mostly in 1st 8 weeks), agranulocytosis (ANC >1500), orthostatic hypotension (slowly titrate dose to minimize), seizure, death in dementia-related psychosis |
|
|
Term
Has ADE: • Highlyanti-cholinergicmedication
• Tachycardia
• Constipation
• Prescribe sufficient bowel regimen!
• Cholinergic agonist at M4 receptors in mouth • Excessivesalivation
• Stronghistaminergiceffect • Sedating
• Weightgain |
|
Definition
|
|
Term
| Clozapine: Prescribing Considerations |
|
Definition
• Consider in patients who have failed adequate doses and trials of other agents
• May not be appropriate in patients with adherence issues
• Dose will need to be re-titrated from initial 25 mg QHS if patient missed > 48 hours of dose
• Patient will need to travel for blood work • Weekly for 1st six months
• Biweekly for 2nd six months • Then monthly for life |
|
|
Term
| Which of the following is the most common form of extrapyramidal symptoms (EPS)? |
|
Definition
|
|
Term
| You have a patient stable on clozapine 600 mg QHS. You diagnose him with OCD and wish to start treatment. Which SSRI should you avoid? |
|
Definition
|
|
Term
|
Definition
• Group of potentially serious adverse effects associated with antipsychotic medications or metoclopramide
• Antagonize D2 receptors in nigrostriatal pathway (substantia nigra) |
|
|
Term
|
Definition
| Repetitive, involuntary, purposeless body or facial movements Ex: Lip smacking, tongue movements, finger movements |
|
|
Term
|
Definition
| Occurs after longer duration of use, may be permanent |
|
|
Term
|
Definition
| Extreme form of internal or external restlessness, inability to sit still, urge to move constantly |
|
|
Term
|
Definition
| Muscle tension disorder -> strong muscle contractions, unusual twisting of parts of body, especially neck |
|
|
Term
|
Definition
| Mask-like facies, resting tremor, cogwheel rigidity, shuffling gait, bradykinesia |
|
|
Term
| antipsychotics with high risk for EPS |
|
Definition
| haloperidole, thiothixene, fluphenazine, paliperidone, risperidone |
|
|
Term
| antipsychotics with low risk for EPS |
|
Definition
• Chlorpromazine
• Aripiprazole
• Brexpiprazole
• Clozapine
• Iloperidone • Olanzapine
• Quetiapine • Ziprasidone |
|
|
Term
|
Definition
• HistoricallyassociatedwithFGAs>SGAs
• Generaltreatment:
• Diphenhydramine(Benadryl):25–50mgpoorIM
(prn or scheduled)
• Benztropine(Cogentin):0.5–4mgpo • Typically divided into BID dosing
• Propranololmayhelpwithtreatmentofakathisia
• Anticholinergics may worsen Parkinsonian symptoms or tardive dyskinesia |
|
|
Term
| Tardive Dyskinesia Clinical features: |
|
Definition
Oral, Facial, Lingual Dyskinesia:
• Abnormal movements of the tongue
• Facial grimacing
• Lip puckering, smacking, pouting
• Bulging of cheeks
• Chewing movements
Limbs and Trunk
• Twisting, spreading of fingers
• Foot tapping
• Dyskinesia of neck
• Shoulder shrugging
• Rocking/swaying
• Tremor (rare) |
|
|
Term
| Tardive Dyskinesia Treatment |
|
Definition
No standard treatment approach has been established:
Discontinue medication • Low response rate
Switch to less potent dopamine
antagonist
• FGA -> SGA
Adjunctive agents
• Clonazepam, gingko biloba, amantadine
• VMAT2 inhibitors? |
|
|
Term
| Valbenazine (Ingrezza®) MOA |
|
Definition
| Reversibly inhibits VMAT2 transporter->regulates uptake of monoamine from cytoplasm to synaptic vesicle for storage/release (↓ monoamine levels in synapse) |
|
|
Term
| Valbenazine (Ingrezza®) indication |
|
Definition
|
|
Term
| Has ADE: Drowsiness, fatigue, sedation |
|
Definition
|
|
Term
| Long-Acting Injectable Antipsychotics |
|
Definition
• Noncompliance to antipsychotic medications may lead to relapsing psychiatric illness.
• Worsening psychiatric symptoms
• Need for emergent treatment or admission
• Readmission rate with schizophrenia is 20–46% in one year
• The monthly or bimonthly administration of long-acting injectable (LAI) antipsychotics may improve treatment adherence.
• Conflicting evidence regarding impact on hospital readmission rate |
|
|
Term
| Available LAI Antipsychotics |
|
Definition
First-Generation Antipsychotics:
Fluphenazine decanoate
Prolixin Decanoate®
Haloperidol decanoate
Haldol Decanoate®
Second-Generation Antipsychotics:
Aripiprazole lauroxil
Aristada®
Aripiprazole monohydrate
Abilify Maintena®
Olanzapine pamoate
Zyprexa Relprevv®
Paliperidone palmitate
Invega Sustenna®, Invega Trinza®
Risperidone
Risperdal Consta® |
|
|
Term
| Oral Antipsychotic Overlap w LAI |
|
Definition
**Tolerability to oral formulation should be established prior to administration of LAI antipsychotic. **
Fluphenazine
Varies depending on oral dose (next slide)
Haloperidol
Based on clinical effect with goal to discontinue oral
within 1 month
Aripiprazole
Abilify Maintena®: Continue oral medication for 14 days Aristada®: Continue oral medication for 21 days
Olanzapine
May begin tapering oral medication immediately after first injection
Paliperidone
May begin tapering oral medication immediately after first injection
Risperidone
Continue oral medication for 3 weeks |
|
|
Term
| Monitoring Recommendations for LAI antipsychoitics |
|
Definition
Metabolic Effects
Weight gain
Weight and BMI
Monthly x 3 months, then quarterly
Central obesity
Waist circumference
Annually
Diabetes
Fasting glucose or HgbA1c
3 months, then annually
Hyperlipidemia
Fasting lipid profile
3 months
Neurologic Effects
EPS
Involuntary movements
Every visit
Sedation
Daytime somnolence
Every visit
Cardiovascular Effects
QT prolongation
QT interval on EKG
With addition of other QT prolonging drugs |
|
|
Term
|
Definition
| Ketorolac, Diclofenac, Ibuprofen, Indomethacin, Nabumetone, Aspirin, Naproxen |
|
|
Term
|
Definition
|
|
Term
|
Definition
• Osteoarthritis, rheumatoid arthritis
• Ankylosing spondylitis
• Migraine
• Analgesia |
|
|
Term
| has toxicities of • Liver function test abnormalities |
|
Definition
|
|
Term
Has toxicities of:
• Rare
• Aseptic meningitis
• Agranulocytosis
• Aplastic anemia |
|
Definition
|
|
Term
|
Definition
• Potential inhibition of:
• Phospholipase A/C
• Decreased neutrophil migration
• Decreased T/B cell proliferation |
|
|
Term
|
Definition
• Inflammatory/rheumatoid disorders
• Closure of patent ductus arteriosus • Acute gouty arthritis
• Many off-label trials |
|
|
Term
Has toxicities:
• Pancreatitis
• Headache (15–25%)
• Dizziness, confusion, depression
• Renal papillary necrosis |
|
Definition
|
|
Term
|
Definition
|
|
Term
Has toxicities:
• Headache
• Injection site pain
• GI bleeding (>5 days of therapy)
• Renal function abnormality
-maximum duration in therapy is 5 days |
|
Definition
|
|
Term
|
Definition
|
|
Term
Has Toxicities:
rare:
• Pseudoporphyria
• Photosensitivity |
|
Definition
|
|
Term
|
Definition
• Osteoarthritis, rheumatoid arthritis
• Analgesia
• Acute gouty flare
• Migraine
• Ankylosing spondylitis |
|
|
Term
Has toxicities:
• Upper GI bleeding
- Rare:
• Allergic pneumonitis
• Leukocytoclastic vasculitis
• Pseudoporphyria |
|
Definition
|
|
Term
|
Definition
• Osteoarthritis
• Rheumatoid arthritis
• Acute pain
• Ankylosing spondylitis |
|
|
Term
has side effects/toxicities:
• Associated with fewer ulcers
• Does not inhibit platelet aggregation
• Toxicities - Rash |
|
Definition
| Celecoxib (COX-2 selective) |
|
|
Term
| Indications for Meloxicam |
|
Definition
Osteoarthritis, rheumatoid arthritis
• Note: preferential selection for COX-2 vs. COX-1 |
|
|
Term
|
Definition
• Weak COX-1 and COX-2 inhibitors
• Block prostaglandin synthesis in the CNS
• No significant anti-inflammatory effects
• Major metabolites
- Nontoxic sulfate and glucoronide
- Reactive: N-acetyl-p-benzoquinone |
|
|
Term
Has Toxicities:
Therapeutic doses
• Mild hepatic enzyme elevations
Larger doses
• Dizziness
• Excitement
• Disorientation
>15grams
• Severe hepatotoxicity
• Acute renal tubular necrosis
• Death |
|
Definition
|
|
Term
| APAP/Acetaminophen: Toxicity Timeline |
|
Definition
Stage 1 (Days 0–1)
N/V
Abdominal pain
Sweating
General discomfort
Pale color
Stage 2 (Days 1– 3)
Liver injury develops
Upper right quadrant pain
Rise in LFTs
Stage 3 (Days 3– 5)
Hepatotoxicity peak
Rapid/severe liver failure
Glucose, lactate, phosphate abnormalities
Coma and death |
|
|
Term
| Considerations for choosing an NSAID |
|
Definition
• Similar efficacy
• Key considerations
• Toxicities
- Indomethacin, ketorolac, diclofenac
- Celecoxib, meloxicam
• Cost-effectiveness |
|
|
Term
|
Definition
• Progressive immunologic disease
• Outcomes
-Systemic effects (joint)
- Shortens lifespan
- Reduces mobility and quality of life |
|
|
Term
| Treatment for Rheumatoid arthritis |
|
Definition
|
|
Term
| Rheumatoid arthritis MOA diagram |
|
Definition
[image]
In rheumatoid arthritis, we have a pretty complicated system occurring. So first, we have some type of antigen, hypothesized, maybe a microbe. It's going to be going and attaching to the CD4 T cell. That CD4 T cell will go on to have B cell activation, macrophage activation, as well as activation of the endothelial lining. Ultimately, a series of cascading events will occur with cytokine activation, formation of auto-antibodies. Ultimately, bottom line, we're going to have pannus formation in the joints. We're going to have destruction of the bone occurring at that joint, as well as cartilage, fibrosis, as well as ankylosis occurring.
We want to prevent that from occurring. This is where our DMARDs come in, the first being methotrexate. By far, it's probably the first agent that will be prescribed by rheumatologists for the management of rheumatoid arthritis. |
|
|
Term
|
Definition
AICAR inhibits intracellular AMP deaminase ->
Increased AMP levels ->
AMP exits cell -> adenosine ->
Adenosine = inhibits inflammation
• Secondary effects on PMN chemotaxis
• Immune-inflammatory cells
- Inhibitory effects on proliferation - Increased apoptosis
• Inhibits proinflammatory cytokines |
|
|
Term
| Methotrexate: Indications |
|
Definition
• Rheumatoid arthritis
• Juvenile chronic arthritis • Psoriasis
• PA
• AS
• Polymyositis
• SLE |
|
|
Term
Has toxicities:
- Hematologic
• Anemia • Leukopenia
- Gastrointestinal
• Nausea • Mucosal ulcers • GI ulcerations • Stomatitis
- Hepatic
• Elevated liver function tests • Cirrhosis (rare)
- Pulmonary
• Hypersensitivity-like reaction |
|
Definition
|
|
Term
|
Definition
| Methotrexate, Azathioprine (a wrath of pine), Cyclosporine, Leflunomide (Left in time), Sulfasalazine, Tofacitinib (Total kit of bibs) |
|
|
Term
|
Definition
• Major metabolite = 6-thioguanine
• 6-thioguanine suppresses:
- Inosinic acid synthesis
- B-/T-cell function
- Immunoglobulin production
-IL-2 secretion |
|
|
Term
| Azathioprine: Indications |
|
Definition
• Rheumatoid arthritis
• Prevention of organ transplant rejection
• PA
• Reactive arthritis
• Polymyositis
• SLE |
|
|
Term
Has toxicities:
- Bone marrow suppression
- GI disturbances
- Rare
• Acute allergic reactions with: • Fever • Rash • Hepatoxicity |
|
Definition
|
|
Term
|
Definition
• Inhibits IL-1 and IL-2 receptor production
• Secondarily inhibits:
- Macrophage-T-cell interaction - T-cell responsiveness
• Impairs T-cell-dependent B-cell function |
|
|
Term
| Cyclosporine: Indications |
|
Definition
• Rheumatoid arthritis
• SLE
• Polymyositis
• Juvenile chronic arthritis • Solid organ transplant |
|
|
Term
Has Toxicities:
• Hematologic
- Leukopenia - Thrombocytopenia - Anemia
• Cardiotoxic
• Infertility |
|
Definition
|
|
Term
|
Definition
• Active metabolite: A77-1726
• Inhibits: dihydroorotate dehydrogenase •-Decreased ribonucleotide synthesis - Arrests cell growth in stimulated cells
• Inhibits T-cell proliferation
• Decreases production of autoantibodies by B-cells
- Secondary effects:
• Increases in IL-10 receptor mRNA
• Decreased IL-8 receptor type A mRNA
• Decreased TNF-alpha dependent nuclear factor kappa B activation |
|
|
Term
|
Definition
|
|
Term
Has Toxicities:
• Diarrhea
• Elevated LFTs
• Mild alopecia
• Weight gain
• Increased blood pressure
• Leukopenia, thrombocytopenia
• Contraindications: pregnancy |
|
Definition
|
|
Term
|
Definition
• Active agent: sulfapyridine
• Suppresses T-cell response to concanavalin
• In-vitro studies show inhibition of:
- B-cell proliferation
- Inflammatory cytokine release from monocytes and macrophages |
|
|
Term
| Sulfasalazine: Indications |
|
Definition
• Rheumatoid arthritis
• Juvenile chronic arthritis
• Psoriatic arthritis
• IBD |
|
|
Term
Has Toxicities:
• Nausea/vomiting • Headache
• Rash
• Rare
- Hemolytic anema
- Methemoglobinemia
- Neutropenia
- Thrombocytopenia |
|
Definition
|
|
Term
|
Definition
Inhibits Janus kinase (JAK) enzymes
- JAK stimulates: • Hematopoiesis • Immune cell function
- Reduced cytokine or growth factor mediated gene expression
- Reduced intracellular immune cell activity
• Includes: CD15/56+, NK cells, serum IgG, IgM, IgA, CRP |
|
|
Term
|
Definition
• Rheumatoid arthritis
• IBD
• Spondyloarthritis • Psoriasis
• Dry eyes |
|
|
Term
Has toxicities:
• Increased infection risk
• Malignancy
- Lymphoma, lung, breast cancer
• Lipid panel changes
• Neutropenia, anemia |
|
Definition
|
|
Term
|
Definition
T-cell modulation, B-cell cytotoxic, Anti-IL-6 Receptor Antibody, IL-1 Inhibition, TNF-a Blockade
Generally, there's five different categories of biologic DMARDs. And what are biologic DMARDs compared to non-biologic? Well, generally, these medications are large protein molecules that are often produced by recombinant DNA technology. |
|
|
Term
|
Definition
[image]
T-cell modulator
The first medication class is the T-cell modulators. Here the medication is Abatacept. It's a pretty unique mechanism of action. So here we have an antigen presenting cell in the bottom left-hand corner.
It has a major histocompatibility receptor in its cell surface, as well as CD80/86 receptor. In the upper right-hand corner, we have the T-cell. It has a T-cell receptor as well as a CD28 receptor.
When these two cells combine, well, the overall result is activation, proliferation, and production of inflammatory mediators. We do not want this to occur in our rheumatoid arthritis patients. So this is where Abatacept comes in.
Abatacept will bind with CD80/86 receptor. What happens here is blockade of this activation, proliferation, and production of inflammatory mediators, just exactly what we wanted. We don't want that T-cell to be activated. |
|
|
Term
|
Definition
• Rheumatoid arthritis
• PJIA
• Psoriatic arthritis |
|
|
Term
|
Definition
• Increased risk of infection
• Infusion related reactions
• Hypersensitivity reactions
• Increased lymphoma risk |
|
|
Term
|
Definition
B-cell cytotoxic
Targets CD20 B lymphocytes ->
1. Cell-mediated/complement mediated cytoxicity
2. Stimulation of cell apoptosis ->
Reduced inflammation |
|
|
Term
|
Definition
• Rheumatoid arthritis (moderate-severe)
• Granulomatosis with polyangitis
• Vasculitis |
|
|
Term
|
Definition
• Rash
• Increased risk of infection
• Hepatitis B reactivation
• Hematologic - Cytopenias |
|
|
Term
|
Definition
Anti-IL-6 Receptor Antibody
• Binds to soluble/membrane bound IL-6 receptors
• IL-6 = proinflammatory cytokine
- Physiologic processes: • T-cell activation • Hepatic acute-phase protein synthesis • Stimulation of inflammatory processes |
|
|
Term
|
Definition
• Rheumatoid arthritis
• SJIA (Systemic juvenile idiopathic arthritis)
• PJIA (Polyarticular juvenile idiopathic arthritis ) |
|
|
Term
Has Toxicities:
• Increased risk of serious infections
• Hematologic - Neutropenia, thrombocytopenia
• Lipid panel abnormalities
• Common - Headache - Hypertension - Elevated LFTs |
|
Definition
|
|
Term
|
Definition
TNF-a Blockade (biggest group)
• Fully humanized IgG anti-TNF monoclonal antibody
- Prevents TNF interaction with p55 and p75 cell receptors
• End Result
- Downregulation of macrophage and T-cell
function |
|
|
Term
|
Definition
• Rheumatoid arthritis
• Plaque psoriasis
• Ulcerative colitis
• Crohn disease
• Ankylosing spondylitis |
|
|
Term
|
Definition
TNF-a Blockade (biggest group)
• Recombinant fusion protein comprised of:
- Two soluble TNF p75 receptor moieties
- Fc portion of human IgG
• Binds to TNF-α and inhibits lymphotoxin α |
|
|
Term
|
Definition
• Rheumatoid arthritis
• Plaque psoriasis
• Ankylosing spondylitis
• Psoriatic arthritis |
|
|
Term
|
Definition
TNF-a Blockade (biggest group)
• Chimeric IgG1 monoclonal antibody:
- Binds with high affinity to TNF-α
- Prevents TNF interaction with p55 and p75 cell receptors |
|
|
Term
|
Definition
• Rheumatoid arthritis
• Crohn disease
• Plaque psoriasis
• Psoriatic arthritis
• Ulcerative colitis |
|
|
Term
Has Toxicities:
• Bacterial infections
• Activation of latent TB
• Reactivation of HBV
• Increased risk of skin cancer • SLE
• Antidrug antibodies
• Injection site reactions
• GI ulcers, bowel perforation |
|
Definition
| TNF-α Blockers (Adalimumab- a day of mobs, Etanercept- etan intercept, Infliximab- inflict a mob) |
|
|
Term
|
Definition
Binds to intracellular tubulin in neutrophils ->
Prevents polymerization into microtubules ->
Inhibits activation, degranulation, migration, and phagocytosis ->
Reduced inflammation |
|
|
Term
|
Definition
• Gout
• Flare treatment: 1.2 mg once followed by 0.6 mg one hour later
• Prophylaxis: 0.6 mg daily, twice daily • Maximum 1.2 mg/day
• Familial Mediterranean fever(FMF)
• Pericarditis(off-label)
• Postpericariotomy syndrome(off-label) |
|
|
Term
Has Toxicities:
- Gastrointestinal
• Diarrhea, nausea, vomiting, abdominal pain
- Rare
• Hematologic
• Hepatic necrosis
• Acute renal failure • Peripheral neuritis • Myopathy |
|
Definition
|
|
Term
|
Definition
• Inhibits reabsorption of uric acid in the proximal renal tubule
• Increased excretion of uric acid
• Reduced urate pool
- Reabsorption of tophaceous deposits |
|
|
Term
|
Definition
• Gout (under excretion of uric acid)
• Prolong penicillin serum levels |
|
|
Term
Has Toxicities:
• Acute gouty flare
• GI irritation
• Hematologic - Anemias - Leukopenia
• Rash
• Nephrotic syndrome • Hepatic necrosis |
|
Definition
|
|
Term
|
Definition
[image]
Allopurinol is a very popular option in the management of gout. So first off, we have allopurinol being metabolized by xanthine oxidase into alloxanthine. Then further below you'll see hypoxanthine being converted by xanthine oxidase to xanthine, which then gets further metabolized into uric acid. Well, allopurinol will come in and will block this final step of xanthine oxidase converting xanthine into uric acid. And again, alloxanthine, that's going to be the metabolite of allopurinol and the active agent that's ultimately blocking that uric acid formation. |
|
|
Term
|
Definition
• Chronic gout
• Cancer-induced hyperuricemia |
|
|
Term
Has Toxicities:
• Acute gouty flare
• GI intolerance
• Hypersensitivity reaction -Drug rash
• Hepatic toxicity
• Interstitial nephritis |
|
Definition
|
|
Term
|
Definition
• Inhibits prostaglandin synthase
• Inhibits urate crystal phagocytosis |
|
|
Term
| Indomethacin: Indications |
|
Definition
• Gout
• Inflammatory/rheumatoid disorders
• Bursitis/tendonitis of the shoulder
• Acute pain |
|
|
Term
Has Toxicities:
• Standard NSAIDs toxicities
• Pancreatitis
• Headache (15–25%)
• Dizziness, confusion, depression
• Renal papillary necrosis |
|
Definition
|
|
Term
|
Definition
| supraspinal, spinal, incx2 respiratory depression, reduce gi motility, euphoria/sedation, incx2 physical dependence |
|
|
Term
|
Definition
| spinal, inc respiratory depression, incx2 gi motility, antidepressant |
|
|
Term
|
Definition
| spinal, peripheral, inc respiratory depression, dysphoria/sedation, inc x2 physical dependence |
|
|
Term
|
Definition
|
|
Term
|
Definition
- Pupillary miosis
• Pupillary constriction occurs at therapeutic opioid doses
• A central effect of the oculomotor nerve
• Chronic users will continue to have constricted pupils
- Itching
• Secondary to histamine release
- Constipation
• Reduced GI motility
• Tolerance will NOT develop to this side effect
• Patients on long-term opiates should be on a bowel regimen
- Nausea/vomiting |
|
|
Term
| opioid severe adverse effects: |
|
Definition
- Respiratory depression
• Respiratory control centers in brain
• Occurs in a dose-dependent manner
• Potentially life threatening
- Hypotension
• Caused by histamine releaseàvasodilation
- Bradycardia
• Direct effect on cardiac pacemaker cells
- True allergy:
• Bronchospasm
• Very low blood pressure/shock
• Angioedema |
|
|
Term
| Opioids: Contraindications |
|
Definition
• Significant respiratory disease
• Comatose patients (unless used for palliative care for a dying patient)
• Hypersensitivity to structurally similar opioid medications |
|
|
Term
|
Definition
• Bowel obstruction
• CNS depression
• Delirium tremens
• Head trauma
• Renal impairment (for renally cleared opioids)
• Respiratory disease (COPD, cor pulmonale, etc.)
• Seizure disorders |
|
|
Term
| full agonist opioid agents |
|
Definition
| fentanyl, heroin, hydrocodone, hydromorphone, methadone, morphine, oxycodone, oxymorphone |
|
|
Term
| partial agonist opioid agents |
|
Definition
|
|
Term
|
Definition
|
|
Term
| codeine metabolism and excretion |
|
Definition
• Metabolism:hepatic
• Glucuronidation to codeine-6-glucuronide • CYP 2D6 to morphine (active)
• CYP 3A4 to norcodeine
- Excretion:viaurine |
|
|
Term
| has fatal side effect for kids after tonsillectomy |
|
Definition
|
|
Term
| hydromorphone immediate release vs extended release |
|
Definition
| immediate release- dilaudid, extended release- Exalgo |
|
|
Term
| oxycodone + acetaminophen |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| roroxycodone (weakly active) |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| hydrocodone + acetaminophen |
|
Definition
|
|
Term
• Extremely potent, NOT for opioid naïve
• Least cardiovascular effects |
|
Definition
|
|
Term
• Analgesia
• Potent opioid μ-receptor agonist
• Blocks NMDA receptor
• Inhibits monoaminergic reuptake
• Adult dose (oral, opioid naïve): 2.5 mg every 8 hours
• Useful for detoxification and treatment of opioid abuse • Highly regulated
• Drug interactions (CYP 3A4 and 2B6)
• QTc prolongation, seizures |
|
Definition
|
|
Term
• Centrally acting synthetic analgesic
• Multiple mechanisms:
- Opioid receptor agonist
- Increased release of serotonin
- Inhibition of serotonin and norepinephrine reuptake
• Available in combination with acetaminophen (Ultracet®)
• Metabolism: hepatic
-CYP 3A4, 2B6, glucuronidation: inactive metabolites
-CYP 2D6: O-desmethyl tramadol (active)
• Excretion: via urine
• Greatest seizure potential |
|
Definition
|
|
Term
| Opioids: Pearls for Prescribing |
|
Definition
• Extended release products should never be crushed or chewed
- Abuse potential
• Dangerous drug interactions
- All: CNS depressants (alcohol, benzodiazepines, barbiturates)
- Some: CYP 3A4 inhibitors (protease inhibitors, macrolides, calcium channel blockers, azole antifungals, grapefruit juice)
- Some: CYP 2D6 inhibitors (antidepressants, ritonovir, quinidine)
• Bowel regimen
- Stimulant laxative + stool softener (senna + docusate) |
|
|
Term
• Sublingual, transdermal patch (Butrans®), IV/IM (Buprenex®)
• Analgesic ceiling
• Reduced potential for abuse (but still possible)
• Treatment of opioid dependence
- Buprenorphine/naloxone (Suboxone®) • Highly regulated |
|
Definition
| Partial Agonists: Buprenorphine (C-III) |
|
|
Term
| What has an active metabolite that accumulates in renal impairment? |
|
Definition
|
|
Term
| Schedule I Controlled Substances |
|
Definition
• No currently accepted medical use in treatment in the United States
• Lack of safety for use under medical supervision
• High potential for abuse
• Illegal to prescribe these substances in the vast majority of cases
• Examples:heroin, lysergic acid diethylamide (LSD), marijuana, methylene-dimethoxy- methamphetamine (ecstasy) |
|
|
Term
| Schedule II Controlled Substances |
|
Definition
• High potential for abuse
• Associated with severe psychological or physical dependence
• Legal to prescribe but with strict federal regulations*
• Examples: morphine,oxycodone,oxymorphone, methadone, meperidine, fentanyl, hydrocodone, cocaine, pentobarbital |
|
|
Term
| Schedule II Prescribing Laws (Federal) |
|
Definition
• No refills may be prescribed on any schedule II controlled substance.
• There is no federal time limit for the filling of a schedule II prescription (i.e., does not expire).
- However—pharmacists are encouraged to use clinical judgment.
• A signed hard copy must be presented to the pharmacy prior to dispensing of the controlled substance.
- Prescriptions may be faxed only if the hard copy is presented to the pharmacist prior to the physical dispensing of the drug.
• Only one prescription may be written per prescription blank.
• Exceptions to the requirement for hard copy prescriptions:
- In emergency situations, an emergency supply may be called into the pharmacy for only the minimum quantity required during that period.
- Prescriptions to be compounded for direct administration by parenteral, IV, IM, SubQ, or intraspinal infusion may be faxed.
- Prescriptions for residents of long-term care facilities may be faxed.
- Prescriptions for patients enrolled in a hospice care program certified and/or paid for by Medicare may be faxed.
• No refills? No problem!
- Federal law allows for issuance of multiple prescriptions for up to a 90-day supply.
- Each prescription must contain all the required elements of a schedule II prescription.
- Each prescription must have clear instructions indicating the earliest date on which a pharmacy may fill them.
• This practice is not recommended for all patients.
- It is at the discretion of the provider to ensure this does not create undue risk of diversion or abuse.
- Provider must assess on a patient-by-patient basis. |
|
|
Term
| Schedule II Prescribing Laws (Connecticut) |
|
Definition
• Original and continuing orders placed in a hospital, infirmary, or clinic are limited to a maximum of 7 days from order entry.
• Prescribers may extend the order for 7 days at a time. |
|
|
Term
|
Definition
• High potential for abuse, but less than that of a schedule I or II substance
• Examples: ketamine, dronabinol, codeine (> 90 mg per dosage unit) |
|
|
Term
|
Definition
• Lower potential for abuse relative to schedule III
• Examples: benzodiazepines (alprazolam, lorazepam, etc.) |
|
|
Term
|
Definition
• Lower potential for abuse relative to schedule IV
• Examples: codeine (< 200 mg/100 mL or 100 g) |
|
|
Term
| Schedule III–V Prescribing Laws (Federal) |
|
Definition
• Permitted modes of transmission:
- Telephone, written, fax
- All required elements for a valid controlled substance prescription must be provided regardless of method used
• Refills:
- Maximum of five refills may be prescribed
• Expiration:
- Prescriptions expire six months after the date of issue |
|
|
Term
| Schedule III–V Prescribing Laws (Connecticut) |
|
Definition
• Original and continuing orders placed in a hospital, infirmary, or clinic are limited to a maximum of 30 days from order entry.
• Faxed prescriptions are only valid if they contain the statement: “This prescription is valid only if transmitted by means of a facsimile machine.” |
|
|
Term
| General Controlled Substance Prescribing Laws (Connecticut) |
|
Definition
• Public Act No. 16-43
• When issuing a prescription for an opioid drug to an adult for the first time for outpatient use, the prescriber shall not issue greater than a 7-day supply.
• Prescribers shall not issue a prescription for greater than a 7-day supply of opioid drug to a minor at any time.
• If, in the professional medical judgment of the prescriber, more than a 7-day supply of an opioid is required to treat a patient’s acute medical condition, or is necessary for treatment of chronic pain, then the prescriber may issue a prescription for the quantity required to treat the condition.
- This condition must be documented in the patient’s medical record, and the prescriber must document that an alternative drug was not appropriate to address the medical condition. |
|
|
Term
| How many refills may be prescribed for a Schedule IV controlled substance? |
|
Definition
|
|
Term
|
Definition
repeated dosing has reduced effect
• 2–3 weeks
• Develops to analgesic, sedating, respiratory, cardiovascular, and emetic effects
• Does NOT develop to constipation or miosis
• Cross-tolerance possible |
|
|
Term
| Opioids: Dependence and Withdrawal |
|
Definition
• Dependence:discontinuationleadsto withdrawal
• μ-agonismindirectlyincreasesdopaminein mesolimbic regionè“reward”
• Opioidwithdrawal
- Rhinorrhea, lacrimation, yawning, chills, goosebumps, hyperventilation, mydriasis, muscular aches, diarrhea, anxiety, hostility
- Onset depends on half-life
- Naloxone can precipitate withdrawal |
|
|
Term
| Symptoms of Opioid Overdose |
|
Definition
• Respiratory depression (slow breathing or apnea, cyanosis)
• Hypotension, bradycardia
• Depressed mental status
• Miosis (pinpoint pupils)
• Hyporeflexia |
|
|
Term
| Naloxone: Opioid Withdrawal |
|
Definition
• Blocking opioids from binding to receptors will precipitate withdrawal in opioid-dependent patients.
• If this occurs, allow symptoms of withdrawal to diminish.
• If necessary ,provider can administer additional lower doses of naloxone.
• Caution: significant nausea/vomiting may occur.
- Risk of aspiration
- Consider pretreatment with an antiemetic |
|
|
Term
| Opioid Withdrawal Symptoms |
|
Definition
• Diaphoresis
• Rhinorrhea
• Irritability
• Anxiety
• Diarrhea
• Tremor
• Anorexia
• Nausea
• Vomiting
• Muscle spasms |
|
|
Term
| antidote for an opioid overdose |
|
Definition
|
|
Term
| Prostaglandin Endoperoxides |
|
Definition
• Two unique cyclooxygenases (COX) isozymes convert AA into prostaglandin endoperoxides
• COX-1 (PGH synthase-1) • Expressed in most cells
• COX-2 (PGH synthase-2)
• Expression dependent on stimulus |
|
|
Term
|
Definition
• Generates prostanoids for • “housekeeping” functions
- Gastric epithelial cytoprotection |
|
|
Term
|
Definition
-Immediate response upregulated by:
• Sheer stress
• Growth factors
• Tumor promoters • Cytokines
- Major source in inflammation
- Endothelial COX-2 primary source of vascular prostacyclin (PGI2)
- Renal COX-2 important for renal development and function |
|
|
Term
| physiology of prostaglandins diagram |
|
Definition
|
|
Term
| NSAID pharmacodynamics diagram |
|
Definition
|
|
Term
| pharmacodynamics of Non-selective NSAIDS vs.selective COX-2 |
|
Definition
• COX-2: Platelet function not affected at usual doses
- Equivalent efficacy with non-selective NSAIDS
- GI safety may be improved with selective COX-2
• COX-2: increase the incidence of edema, hypertension, and possibly myocardial infarction
- Celecoxib: FDA Black Box warning concerning CV risk |
|
|
Term
| non-selective NSAID agents and notes |
|
Definition
| Aspirin (antiplatelet effects), Diclofenac, Etodolac, Ibuprofen, Indomethacin, Nabumetone, Naproxen, Ketorolac |
|
|
Term
|
Definition
|
|
Term
|
Definition
• All NSAIDs, including aspirin, equally efficacious with few exceptions
• Differentiated based on toxicity and cost-effectiveness
- Ketorolac: IV and limited to five days
- Indomethacin and tolmetin: associated with greatest toxicity
- Aspirin and ibuprofen: least toxic
• Renal insufficiency: nonacetylated salicylates may be preferential
• LFT abnormalities: diclofenac and sulindac associated with more abnormalities
• GI bleeding
- Celecoxib probably safest for high-risk patients for GI bleeding, but has
greatest risk for CV toxicity |
|
|
Term
|
Definition
• Undergoes glucuronidation (40–60%) and sulfation (20–40%) and is excreted in the urine
• Alternative cytochrome P450-dependent GSH conjugation pathway accounts for remaining 5–8%
- Potential production in hepatotoxic metabolite N-acetyl-p-benzoquinone imine (NAPQI)
- Pathway becomes extremely important during toxicity |
|
|
Term
| Stages of Tylenol Toxicity |
|
Definition
|
|
Term
|
Definition
| sheer stress, growth factors, and cytokines. |
|
|
Term
| Diuretic Effects on Calcium |
|
Definition
Thiazide Diuretics ↑ Ca Increase in bone density causes a reduction in incidence of hip fractures (less sodium will be going into the cell so less Ca will leave)
Loop Diuretics ↓ Ca Decrease in bone density and increase risk of hip fractures (dec Na, K, Cl into cell, divalent ion loss) |
|
|
Term
| Bisphosphonates MOA Monitoring |
|
Definition
• MOA: inhibit bone resorption by suppressing osteoclasts
• Monitoring: BMD, calcium level
• Avoid in renal failure
• Oral bisphosphonates irritate gastrointestinal mucosa— patients should take on an empty stomach and must stay upright for at least 30–60 minutes after dose and until first meal of the day
• Space out from calcium supplements |
|
|
Term
| bisphosphonate agents and comments |
|
Definition
| Fosamax (alendronate-i draw on nate, Actonel (risedronate- rice drawn on nate), Boniva (ibandronate- iBand on nate)- only approved for postmenopausal females), Reclast (zoledronate- zoey desconele or nate) only IV + least frequent administration, mostly for post menopausal females except reclas |
|
|
Term
| Miacalcin (Calcitonin) MOA Monitoring |
|
Definition
for postmenopausal females
• MOA:similartoendogenouscalcitonin,inhibits osteoclasts, decreases renal absorption of calcium, phosphate, magnesium, potassium
• Monitoring: BMD, serum calcium, phosphorus |
|
|
Term
| Recombinant Parathyroid Hormone agent |
|
Definition
| Forteo (teriparatide- terrible party time) |
|
|
Term
| Forteo (teriparatide) MOA Monitoring |
|
Definition
• MOA: recombinant parathyroid hormone, which stimulates osteoblasts, increases GI absorption of calcium, renal reabsorption of calcium
• Monitoring: BMD, serum calcium, phosphorus, uric acid, blood pressure
• Administer first dose with patient sitting or laying down due to risk of orthostasis |
|
|
Term
| Selective Estrogen Receptor Modulators agent |
|
Definition
| Evista (Raloxifene- ralph ox if needed) |
|
|
Term
| Evista (Raloxifene) MOA Monitoring |
|
Definition
| • MOA: inhibits bone resorption through modulation of some estrogen receptors• Monitoring: BMD, lipid profile |
|
|
Term
| Hormones agents and comments |
|
Definition
Forteo (teriparatide- terrible party time) Hypercalcemia and hypercalciuria;
osteosarcoma reported in animals; administer first dose with patient sitting or laying down (risk of orthostasis)
Miacalcin (calcitonin) Rhinitis with nasal spray
Evista (raloxifene- ralph ox if needed) Peripheral edema, rare venothromboembolism |
|
|
Term
| Rank Ligand Inhibitor agent |
|
Definition
| Prolia (Denosumab- dens are for mobs) |
|
|
Term
| Prolia (Denosumab) MOA Monitoring |
|
Definition
• MOA: monoclonal antibody which prevents RANKL- stimulated osteoclast differentiation and function
• Monitoring: BMD, SCr, serum calcium, phosphorus, magnesium, chronic back pain
• Use caution in severe renal impairment (CrCl <30ml/min) |
|
|
Term
| Monoclonal Antibodies agent and comments |
|
Definition
| Prolia (denosumab- dens are for mobs) Monoclonal antibody; dermatologic reactions |
|
|
Term
|
Definition
• Historically used as an anabolic agent for treatment of postmenopausal osteoporosis
• MOA:
• Stimulate osteoblast activity and increase bone formation
-narrow therapeutic window |
|
|
Term
AE:
• Long-term toxicities:
• Skeletal fluorosis
• Abnormal bone mineralization
• Treatment of osteoporosis with monotherapy fluoride does not reduce fracture risk |
|
Definition
|
|
Term
| Medication-Induced Bone Loss |
|
Definition
• Corticosteroids
• Selective serotonin release inhibitors (SSRI)
• Enzyme-inducing anticonvulsants (e.g., phenytoin)
• Proton pump inhibitors (PPI)
• Aluminum
• Lithium
• Calcineurin inhibitors
• Methotrexate
• Thiazolidinediones (e.g. pioglitazone) |
|
|
Term
| Initiation of osteoporosis treatment |
|
Definition
• Osteopenia or history of hip or vertebral fractures (including asymptomatic)
• T-score • Postmenopausal women or men over 50 years old with T- score -1 to -2.5 at femoral neck, total hip or lumbar spine as measured by DXA who have a 10-year hip fracture probability of at least 3% or a 10-year major osteoporosis-related fracture probability of at least 20%
• Use US-adapted WHO absolute fracture risk model (FRAX®):www.NOF.org |
|
|
Term
| Which medication below is the most effective treatment for osteoporosis as measured by the relative increase in lumbar spine bone mineral density? |
|
Definition
| Teriparatide (terrible party time) |
|
|
Term
| • Adverse effects: dyspepsia, arthralgia, back pain, adynamic bone, rare osteonecrosis and fractures |
|
Definition
Bisphosphonates
Fosamax (alendronate, Actonel (risedronate), Boniva Fosamax (alendronate-i draw on nate, Actonel (risedronate- rice drawn on nate), Boniva (ibandronate- iBand on nate)- only approved for postmenopausal females), Reclast (zoledronate- zoey desconele or nate) only IV + least frequent administration, mostly for post menopausal females except reclas |
|
|
Term
| • Adverseeffects:nausea,flushing,rhinitiswith nasal spray |
|
Definition
|
|
Term
| • Adverse effects: dizziness, insomnia, depression, nausea, arthralgia, weakness, rhinitis, hypercalcemia, hypercalciuria, orthostasis, osteosarcoma reported in animals |
|
Definition
| Forteo (teriparatide- terrible party time) |
|
|
Term
| • Adverse effects: peripheral edema, hot flashes, arthralgia, rare venous thromboembolism |
|
Definition
| Evista (Raloxifene- ralph ox if needed) |
|
|
Term
• Adverse effects: dermatitis, eczema, rash, arthralgia, may increase risk of infection, rare osteonecrosis
of the jaw |
|
Definition
| Prolia (Denosumab- dens are for mobs) |
|
|
Term
| Tricyclic Antidepressants (TCAs) MOA |
|
Definition
| Non-selective inhibitors of NE and 5-HT reuptake transporters |
|
|
Term
|
Definition
Amitriptyline (am i right to pry a little)
Elavil
Imipramine (im a prime mime)
Tofranil
Clomipramine (claim a prime mine)
Anafranil
Doxepin (doxy pin)
Sinequan
Nortriptyline (notorize prime line)
Pamelor
Desipramine (despirate mime)
Norpramin
Trimipramine (try to prime mime)
Surmontil
Protriptyline (pro trip prime line)
Vivactil
Amoxapine (a moxy pine)
Asendin
Maprotiline (my prototype line)
Ludiomil |
|
|
Term
|
Definition
a1- orthostatic hypotension
muscarinin- dry mouth, blurry vision, confusion ,constipation, urinary retention
H1 and 5HT2C- weight gain
H1- sedation |
|
|
Term
| QTc prolongation meds from least to most (TCAs) |
|
Definition
| Doxepin, Amoxepine, Nortriptyline, Chlomipramine, Amitriptyline, Imipramine |
|
|
Term
|
Definition
• Ex: imipramine, amitriptyline
• Significant side effect profile due to increased α1, H1, and M1 blockade |
|
|
Term
|
Definition
• Ex: desipramine, nortriptyline
• Increased tolerability with minimal α1, H1, and M1 blockade |
|
|
Term
May benefit in treatment of chronic pain, polyneuropathy, and migraines
Additional sedating properties |
|
Definition
|
|
Term
| May benefit in treatment of myofascial pain and neuralgia |
|
Definition
|
|
Term
| Additional benefit in treatment of neuropathic pain |
|
Definition
| Imipramine, Desipramine (TCA) |
|
|
Term
| May be used as sleep aid at low doses |
|
Definition
|
|
Term
Monoamine Oxidase Inhibitors
• Mechanism of action |
|
Definition
Non-specific irreversible inhibition of monoamine
oxidase
• MAO is responsible for metabolism of 5HT, NE, and DA |
|
|
Term
|
Definition
Phenelzine (Nardil) (fencing in line)
Diet restriction required
Tranylcypromine (Parnate) (trying to cycle promise)
Diet restriction required
Isocarboxazid (Marplan) (iso carbs and acid)
Diet restriction required
Selegiline patch (Emsam) (sell a guy's line)
Tyramine-diet restriction unnecessary unless daily
dose > 6 mg
Two active metabolites: amphetamine/
methamphetamineàurine tox may be (+) |
|
|
Term
Has ADE:
• Sedation
• Insomnia
• Weight gain
• Changes in blood pressure |
|
Definition
|
|
Term
| MAOI Diet Recommendations |
|
Definition
• Foods to avoid
• Aged cheeses, dried meats, red wine, tap beers, sauerkraut, raw yeast, legumes
• Foods to limit
• Caffeinated beverages, chocolate, figs, meat tenderizers, raisins
• Very important to counsel patients
on how to successfully follow low tyramine diet! |
|
|
Term
|
Definition
• Resulting from significant tyramine levels
• Usually develops 20–60 minutes after ingestion of the interacting food or drug
• Can lead to CVA or death
• Clinical presentation: nausea, vomiting, sweating, headache, stiff neck, chest pain, hypertension, palpitations |
|
|
Term
| Serotonin Syndrome presentation |
|
Definition
| Abdominal pain, diarrhea, sweating, fever, tachycardia, delirium, hyperreflexia, clonus, irritability |
|
|
Term
|
Definition
Inhibit presynaptic serotonin reuptake by inhibition of the 5-HT
transporter
• Increased 5-HT in synaptic cleft |
|
|
Term
| Has ADE GI, HE, Insomnia/Sedation, Anxiety, Sexual dysfuncion, SIADH, Discontinuation synderome |
|
Definition
|
|
Term
|
Definition
Citalopram (Celexa®)
Dose-related risk of QT prolongation
Max doses for >65 y/o, hepatic impairment, or
with concomitant 2C19 inhibitors
Escitalopram (Lexapro®)
Dose-related risk of QT prolongation
S-enantiomer of citalopram
Fluoxetine (Prozac®)
↓ Dose by 50%
Activating 2D6 inhibitor
Active metabolite
(norfluoxetine) with long half-life (7–9
days), taper not required
Paroxetine (Paxil®)
Dry mouth, drowsiness, fatigue
More anti-cholinergic adverse effects
High risk of
discontinuation syndrome with abrupt d/c
due to short half-life 2D6 inhibitor
Sertraline (Zoloft®)
GI side effects (diarrhea, nausea, vomiting) common
->start with lower dose and titrate slowly
Active metabolite N- desmethylsertraline (half-
life 60–80 hours)
Fluvoxamine (Luvox®)
Potent 1A2 enzyme inhibitor
Generally only used in OCD |
|
|
Term
| SSRIs: Prescribing Considerations |
|
Definition
•
SSRIs: Prescribing Considerations
Consider unique features to narrow selection
• Drug-drug interactions
• Renal adjustments are generally not necessary
Paroxetine
Strong anticholinergic effectsàmay benefit in appetite stimulation and weight gain
Sertraline
Most GI side effects
Fluoxetine
Longest half-life
Citalopram/Escitalopram
May prolong QTc
• • •
Monitor for response and titrate as tolerated
May require 4–6 weeks for full antidepressant effect |
|
|
Term
|
Definition
All SSRIs are pregnancy category C
• Exception: Paroxetine (cardiac defects)->category D |
|
|
Term
|
Definition
Inhibition of the 5HT and NE transporters ->
increased neurotransmitters in synaptic cleft |
|
|
Term
|
Definition
• Venlafaxine (Effexor®) (venmo the fax machine)
• Desvenlafaxine (Pristiq®) (dat venmo the fax machine)
• Levomilnacipran (FetzimaTM) (levitate mili ants with pam)
• Duloxetine (Cymbalta®) (dull ox for time) |
|
|
Term
|
Definition
• Venlafaxine
• Doses < 150 mg primarily inhibits 5HT-reuptake à higher doses provide dual NE and 5HT blockade
• Hypertension (dose-related) • <100 mg/day: 3%
• >300 mg/day: Up to 13%
• Desvenlafaxine
• Active metabolite of venlafaxine (CYP 2D6)
• Levomilnacipran
• NE > 5HT reuptake inhibition
• Duloxetine
• Equal affinity for 5HT and NE reuptake transporters |
|
|
Term
|
Definition
Duloxetine- Monitor liver function
Venlafaxine IR and ER- Dose-related increase in blood pressure
Doses >150 mg required to get dual NE and 5HT transporter inhibition
Desvenlafaxine- Active metabolite of venlafaxine
Requires 2D6 for metabolism
$$$$
Levomilnacipran- BP and HR elevations can occur
NE > 5HT reuptake inhibitor |
|
|
Term
| SNRIs: Prescribing Considerations |
|
Definition
• Consider unique features to narrow selection of SNRI
• All SNRIs are approved for treatment of depression
• Venlafaxine is also indicated for panic disorder/anxiety, neuropathic pain
• Dose-related increases in blood pressure
• Duloxetine has evidence in treatment of anxiety, fibromyalgia, and musculoskeletal pain
• Non-antidepressant properties may be evident within 1– 2 weeks of starting therapy
• Monitor for response and titrate as tolerated
• All SNRIs are pregnancy category C |
|
|
Term
| Mirtazapine (Remeron®) MOA |
|
Definition
• Presynaptic α-2 antagonist
• Increases synaptic concentration of 5HT
and NE
• Antagonist at 5HT2 and 5HT3 |
|
|
Term
Has ADE: • Increased appetite (17%)
• Weight gain (7.5%: >7% ↑ in BW)
• Constipation (13%) • Sedation (54%) |
|
Definition
|
|
Term
| Has unique features: Often scheduled at night for sedating and appetite-stimulating effects |
|
Definition
|
|
Term
| Bupropion (Wellbutrin®) MOA |
|
Definition
| NE and DA reuptake blockade with no 5HT effects |
|
|
Term
Has ADE: • Headache (25–34%) • Insomnia (11–20%)
• Dizziness (6–11%)
• Xerostomia (17–26%)
• Tachycardia (11%)
• Weight loss (14–23%)
• Agitation (2–9%) • Anxiety (5–7%)
• Seizures (0.1–0.4%) |
|
Definition
|
|
Term
Has unique features: Activating (useful with fatigue, poor concentration) CYP 2B6 (major pathway), strong CYP2D6 inhibitor
No sexual dysfunction |
|
Definition
|
|
Term
Has ADE:• Dose-related seizure (0.1–0.4%)
• Maximum dose depends on formulation |
|
Definition
|
|
Term
| Bupropion (Wellbutrin®) contraindication |
|
Definition
| history of seizures, history of anorexia/bulimia, abrupt disontinuation of EtOH, BDZ, barbituates antiepileptics, AVS malformation in CNS, severe head injurey stoke CNS tumor |
|
|
Term
|
Definition
| Weak 5HT reuptake inhibitor Significantly blocks H1 and α1 receptors |
|
|
Term
Has ADE: • Sedation (46%)
• Headache (33%)
• Dizziness (25%)
• Fatigue (15%)
• Dry mouth (25%)
• Nausea (21%)
• Constipation (8%) |
|
Definition
|
|
Term
| Used commonly as sleep aid, rarely as antidepressant |
|
Definition
|
|
Term
| Nefazodone (Serzone®) MOA |
|
Definition
| 5HT2A antagonist with moderate inhibition of 5HT and NE reuptake |
|
|
Term
Has ADE: • Dry mouth (25%)
• Sedation (25%)
• Nausea (22%)
• Dizziness (17%)
• Blurred vision (16%) |
|
Definition
|
|
Term
Not usually prescribed due to rare incidence of
hepatotoxicity |
|
Definition
|
|
Term
| Vilazodone (Viibryd®) MOA: |
|
Definition
• Inhibition of presynaptic 5HT transporter
• 5HT1A partial agonist |
|
|
Term
Has ADE: • Diarrhea (28%)
• Nausea (23%)
• Vomiting (5%) |
|
Definition
|
|
Term
| Vortioxetine (Trintellix®) MOA |
|
Definition
• Inhibition of 5HT reuptake
• 5HT3 antagonist
• 5HT1A agonist |
|
|
Term
HAs ADE: • Nausea (10–20%)
• Diarrhea (7–10%)
• Dry mouth (6–8%)
• Sexual dysfunction (males: 16–29%, females:
22–34%) |
|
Definition
| Vortioxetine (Trintellix®) |
|
|
Term
| Pregnancy category C metabolized by CYP2D6 $$$$ |
|
Definition
| Vortioxetine (Trintellix®) |
|
|
Term
| Sedation, increased appetite, weight gain |
|
Definition
|
|
Term
| 2nd and 3rd Generation SNRI Prescribing Considerations |
|
Definition
• Consideruniquefeaturestonarrowselection
• Mirtazapinesupportsincreasedappetite,weight gain, and sedation with possible benefit as an antiemetic
• Trazodoneiscommonlyusedasasleepaidbuthas increased anticholinergic effects
• Newer atypical antidepressants have higher cost with no superior benefit over traditional agents
• Non-antidepressanteffectsmaybeevident within days of starting therapy
• Monitor for response and titrate as tolerated |
|
|
Term
| Due to its 5HT3 receptor blockade, mirtazapine lacks which of the following adverse effects? |
|
Definition
| Nausea and vomiting (causes Weight gain Sedation Constipation) |
|
|
Term
| For which of the following patients would bupropion be an acceptable option to treat MDD? |
|
Definition
| 36 y/o M with comorbid cocaine use disorder and borderline personality disorder |
|
|
Term
|
Definition
• Used historically to treat anxiety
• Phenobarbital, secobarbital, primidone
• Current use: sedative-hypnotic, anticonvulsant
• Rarely used due to toxicity, dependence, development of tolerance
• Over sedation
• Impaired cognitive function
• High doses: anesthesia, coma, death
• First benzodiazepine available in 1950s |
|
|
Term
Benzodiazepines (BZPs)
• MOA |
|
Definition
| Bind to the gamma subunit of the GABAA receptor -> allosteric modification of receptor -> GABA binds -> increased frequency of channel opening -> increase in chloride ion conductance and inhibition of the action potential |
|
|
Term
|
Definition
• Categories based on elimination half-life
• Most hepatically metabolized via CYP system
Ultra-short acting (Midazolam, clorazepate)- middle of the lamb, chlorine pete, Short acting (Triazolam)- try a lamb, Intermediate-acting agents (Alprazolam, estazolam, temazepam, oxazepam, lorazepam)- alpine lamb, esta lamb, team lamb, ox lamb, lauel lamb, Long-acting agents (Flurazepam, diazepam, quazepam, clonazepam)- fluffy lamb, die a lamb, quazi lamb, clone lamb |
|
|
Term
| Alprazolam (Xanax) indications |
|
Definition
|
|
Term
| chlordiazepoxide (Librium) indication |
|
Definition
| anxiety, pre-op anx, alcohol withdrawal |
|
|
Term
| clonazepam (Klonopin) indications |
|
Definition
|
|
Term
| diazepam (valium) indications |
|
Definition
| anxiety, pre-op anx, panic, alcohol withdrawal, seizure |
|
|
Term
| lorazepam (ativan) indications |
|
Definition
| anxiety, seizure, insomnia |
|
|
Term
| oxazepam (serax) indications |
|
Definition
| anxiety, alcohol withdrawl, insomnia |
|
|
Term
| estazolam (prosom) indications |
|
Definition
|
|
Term
| flurazepam (dalmane) indicaxitons |
|
Definition
|
|
Term
| temazepam (restoril) indications |
|
Definition
|
|
Term
Has ADE: • Impaired psychomotor performance
• Amnesia
• Sedation, somnolence, fatigue
• Dependence, withdrawal- More likely when treated with BZDs with shorter half-lives
• Rebound anxiety
• Cognitive dysfunction, confusion |
|
Definition
|
|
Term
|
Definition
• Most intentional ingestions involve coingestant (ex: alcohol)
• Slurred speech
• Ataxia
• Altered mental status
• Respiratory compromise->much more likely with concomitant ingestion of sedatives |
|
|
Term
| BZDs: Prescribing Considerations |
|
Definition
• Elimination half-life
• Slow taper to avoid potential for seizures
• Generally safe when used alone - Present a fall risk for elderly patients!
• Potential for physiological and psychological dependence
• Reserve for short-term therapy
• Preferred agents in elderly or with poor hepatic
function: lorazepam, oxazepam, temazepam |
|
|
Term
|
Definition
| Hydroxyzine (atarax), gabapentin (neurotin), pregabalin (lyrica), buspirone (buspar) |
|
|
Term
|
Definition
| Binds to H1 receptors for skeletal muscle relaxing, antihistamine, antiemetic effects |
|
|
Term
| has ADE: Xerostomia, somnolence |
|
Definition
|
|
Term
| gabapentin (neurotonin) MOA |
|
Definition
| Structurally related to GABA, does not bind to GABAA or GABAB receptors |
|
|
Term
| has ADE: Sleepiness (25%), dizziness (23%), ataxia (20%), nystagmus, headache, fatigue, peripheral edema |
|
Definition
|
|
Term
|
Definition
Not completely understood
GABA analog à binds to alpha2-delta site |
|
|
Term
| Has ADE: Weight gain, peripheral edema, constipation, xerostomia, ataxia, dizziness, headache, fatigue, disturbance in thinking/SI |
|
Definition
|
|
Term
|
Definition
| Unknown, high affinity for 5-HT1A receptors and moderate affinity for D2 receptors |
|
|
Term
| Has ADE: Nausea, dizziness, somnolence, headache |
|
Definition
|
|
Term
| Physiologic Changes With Aging |
|
Definition
• Decreased total body water
• Decreased muscle mass • Decreased organ volume • Increased body fat |
|
|
Term
| Drugs With Increased Bioavailability in the Elderly Statins |
|
Definition
Statins
Atorvastatin 14%
Lovastatin 5%
Pravastatin 17-34%
Simvastatin 5% |
|
|
Term
| Drugs With Increased Bioavailability in the Elderly Beta blockers |
|
Definition
Labetalol 30-65%
Metoprolol 50-70%
Propranolol 30-70% |
|
|
Term
| Drugs With Increased Bioavailability in the Elderly TCAs |
|
Definition
Amitriptyline 30-60%
Desipramine 33-51%
Imipramine 22-77% |
|
|
Term
| Drugs With Increased Bioavailability in the Elderly CNS drugs |
|
Definition
levodopa 30-60%
morphine 20-40% |
|
|
Term
|
Definition
• Oxidation and reduction via cytochrome (CYP) P450 enzyme system
• Inconsistent changes in elderly • Some 2C19 reductions
• No change 2D6
• Inconsistent: 1A2, 2C9, 2E1, 3A4
• Largest change in frail elderly |
|
|
Term
|
Definition
• Examples:
• Glucuronidation • Acetylation
• Sulfation
• No major change in activity with aging |
|
|
Term
| Phase I cardiovascular agents |
|
Definition
• Atorvastatin • Simvastatin
• Propranolol |
|
|
Term
| Phase II cardiovascular agents |
|
Definition
|
|
Term
| Phase I hypnbotic agents, sedatives |
|
Definition
• Benzodiazepines • Diphenhydramine
• “Z” drugs |
|
|
Term
| phase II hypnotic agents, sedatives |
|
Definition
|
|
Term
|
Definition
• Ibuprofen
• Meperidine
• Tramadol |
|
|
Term
| phase II analgesic agents |
|
Definition
|
|
Term
|
Definition
• Tricyclic antidepressants
• Selective Serotonin Receptor Inhibitors |
|
|
Term
• Barbiturates
• Carbamazepine
• Phenytoin
• Risperidone • Theophylline
phase??? |
|
Definition
|
|
Term
|
Definition
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Term
| Cockcroft-Gault (CG) Equation controversies |
|
Definition
• Weight (actual, lean body, adjusted, ideal)
• Underpredicts:
- Patients who weigh less than their IBW
• Overpredicts:
- Patients who weigh more then their IBW (i.e. obese) |
|
|
Term
| Drugs With Altered Renal Excretion and Dose Adjustments, Antibiotics |
|
Definition
• Aminoglycosides -hearing loss, ATN
• Carbapenems- Seizures
• Penicillins-CNS stimulation, seizures
• Sulfonamides - crystalluria
• Tetracycline- azotemia, renal damage
• Vancomycin- ototoxicity, nehrotoxicity |
|
|
Term
| Drugs With Altered Renal Excretion and Dose Adjustments, antivviral agents |
|
Definition
• Acyclovir, Valacyclovir • Famciclovir
-seizures, confusion, renal failure |
|
|
Term
| Drugs With Altered Renal Excretion and Dose Adjustments,cardiovascular agents |
|
Definition
• Atenolol • Digoxin
• Telmisartan
potential toxicity: • Bradycardia, hypotension • Heart block, confusion
• Renal failure |
|
|
Term
| Drugs With Altered Renal Excretion and Dose Adjustments,, CNS agents |
|
Definition
• Gabapentin • Lithium
• Pregabalin
potential toxicity: • Somnolence, confusion
• Sedation, confusion, tremors
• Confusion, blurred vision |
|
|
Term
| Pharmacodynamic Changes and Aging |
|
Definition
| altered receptor number and affinity, signal transduction, homeostatic mechanisms -> increased drug sensitivity |
|
|
Term
| Pharmacodynamic Changes: Cardiovascular w age |
|
Definition
• Beta-blockers
• Increased response
• Increased risk of orthostatic hypotension • Decreased arterial compliance
• Decreased baroreceptor reflex
• Medications
• TCAs, antipsychotics, diuretics, ACEIs • Direct vasodilators, opioids |
|
|
Term
| Gamma-aminobutyric acid (GABA) neurotransmitter system changes w age |
|
Definition
• Increased sensitivity to benzodiazepines
• Toxicities • Ataxia
• Sedation
• Cognitive impairment |
|
|
Term
| Managed Care Plans (Part C) |
|
Definition
• Medicare Advantage Plan
• Private companies that contract with Medicare to provide Part A, B, and D coverage
• Examples include:
• Health Maintenance Organizations (HMOs) • Preferred Provider Organizations (PPOs)
• Cover all Medicare services
• Most plans offer extra coverage
• Rules
• Medicare pays insurance company fixed monthly amount
• Plans can charge different out-of-pocket costs • Set different rules on how to get services |
|
|
Term
|
Definition
• Voluntary prescription drug insurance coverage
-All Medicare patients are eligible
• Hundreds of privately-insured subsidized plans are offered
• Late enrollment penalty
-Applied if not purchased when first eligible for Medicare |
|
|
Term
|
Definition
• State run health insurance program for low income and disabled individuals
• Must enroll in a PDP
• PDP pays first then Medicaid covers remainder
• Participants responsible for small co-payment • Nursing home patients pay $0 |
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