Psych/neuro Flashcards
Benzodiazepines *
Drugs- alprazolam (Xanax), clonazepam (klonopin), diazepam (Valium), estazolam, flurazepam, lorazepam (Ativan), midazolam, oxazepam, quazepam (doral), temazepam (restoril), Triazolam (halcyon), chlordiazepoxide (librium), clorazepate (tranxene)
Controlled substance
MOA- enhanced GABA effect
Uses- reduction in anxiety although not DOC, sedative, hypnotic, Anticonvulsants, anterograde amnesia, muscle relaxant, muscular skeletal spasms
Not recommended in pregnancy or nursing infants
Dependence!
ADE- drowsiness, confusion, ataxia, cognitive impairment, use in caution with liver patients and alcohol use patients can enhance CNS depression, avoid with opioids can cause death
Benzodiazepines antagonist *
Drugs- flumazenil
MOA- anatagonize GABA, reverse effects of benzos for toxicity or OD
IV only
Short half life may need multiple doses
ADE- seizures if benzo was used to control; or pt is taking TCAs or antipsychotic concurrently, n/v, agitation
Antidepressants for anxiety *
SSRIs like escitalopram, paroxetine
SNRIs like venlafexine or duloxetine
Alone or in combo with benzos
4-6 weeks for effects
Buspirone *
Uses- GAD
MOA- mediated by serotonin receptors and potentially dopamine-serotonin receptors
Similar efficacy as benzo but not for acute anxiety and lacks anticonvulsant and muscle relaxant properties
ADE- HA, dizziness, nervousness, nausea, lightheartedness, minimal sedative effects
Barbiturates
Drugs- amobarbital (amytal), methohexital (brevital), pentobarbital (nembutal), phenobarbital, secobarbital (seconal)
Controlled substance
MOA- GABA enhancement receptor site different from benzos, blocks glutamate receptors
Uses- anesthesia, anticonvulsant, sedative hypotonic, can cause CNS/RESPIRATORY DEPRESSION
Do not give in pregnancy/breast feeding
ADE- drowsiness, impaired concentration, mental and psychomotor impairment, CNS depression worsens with alcohol, hangover feeling
D-D- CYP450
Contraindicated in acute intermittent porphyria
do not abrupt withdrawal can cause cardiac arrest
Death can occur from OD
No reversal agent
Zolpidem (ambien) *
Uses- hypnotic agent for about 5 hrs
MOA- binds to GABA, relative selectivity as benzos but anticonvulsant or muscle relaxant properties
Controlled substance
Few withdrawal effects
ADE- HA, dizziness, anterograde amnesia, next morning impairment, sleep walking , sleep driving
D-D- CYP450
Zaleplon (sonata) *
Oral non benzo hypnotic similar to zolpidem
Fewer residual side effects on psychomotor or cognitive function
Rapid elimination
For this have difficulty falling asleep
CYP3A4 metabolite
Eszopiclone (lunesta)*
Non benzo hypnotic
Effective for insomnia for 6 months
Rapid absorption
CYP450 metabolite
ADE- anxiety, dry mouth, HA, peripheral edema, somnolence, unpleasant taste
Melatonin receptor agonist *
Drugs- ramelteon (rozerem), tasimelteon (hetlioz)
MOA- selective agonist in MT 1 and 2, for melatonin a natural circadian rhythm hormone
Minimal potential for abuse
Uses- insomnia due to difficult falling asleep, non 24 hour sleep wake disorder
ADE- increase prolactin levels, HA, abnormal dreams, increase in LFT, URI
D-D- CYP1A2 and CYP3A4 metabolite
Antihistamine *
Drugs- diphenhydramine (Benadryl), hydroxyzine, doxylamine
Uses- mild insomnia
Sedating Antidepressants *
Doxepin- TCA
Trazodone-TCA
Quetiapine- antipsychotic
Both used for insomnia
Orexin receptor antagonist *
Drug- suvorexant (belsomra), lemborexant (dayvigo)
MOAa antagonist for OX1R and 2, ore in is a neuro peptide that promote wakefulness
ADE- nacrolepsy like, sleep paralysis, cataplexy, hypnogogic and hypnopompic hallucinations, daytime sommolence, SI
D-D- CYP3A4 metabolite
SSRIs*
Drugs- citalopram (celexa), escitalopram (lexapro), fluoxetine (Prozac), fluboxamine (Luvox), paroxetine (Paxil), sertraline (zoloft)
MOA- block reuptake of serotonin leading to increased concentrations
Takes 2-12 weeks for max benefit
Uses- MDD, anxiety, OCD, panic disorder, GAD, PTSD, social anxiety, PMDD, bulimia (Prozac only)
ADE- HA, sweating, anxiety, agitations, hyponatremia, n/v/d, weakness, fatigue, sexual dysfunction, sleep disturbances, prolong QT
Use caution in children/adolescents
Withdrawal symptoms
DOC for MDD
SNRIs*
Drugs- desvenlafaxine (pristiq), duloxetine (cymbalta), levomilnacipron (fetzima), venlafexine (effexor); milnacipran (savella)
MOA- dual inhibition of serotonin and norepinephrine reuptake
Uses- pain syndromes (savella) , depression, anxiety
ADE- nausea, HA, sexual dysfunction, dizziness, insomnia, sedations, constipation, increase in BP/HR at high doses max, sweating
Withdrawal effects
Brexanolone (zulresso)
Atypical antidepressant
MOA- positive allosteric modulator if GABA
Uses -PPD
IV
ADE- excessive sedation, loss of consciousness, hypoxia
Monitoring required
Bupropion (Wellbutrin)*
Atypical antidepressant
MOA- weak dopamine and norepinephrine reuptake inhibitor
Uses- depression, smoking cessation
ADE- dry mouth, sweating, nervousness, tremor, seizures
Low instance of sexual dysfunction
Low D-D interactions
Avoid in seizure patients and those with history of anorexia or bulimia
Esketamine (spravato)
Atypical antidepressant
MOA- S enantiomer of racemic ketamine, non selective, non competitive antagonist of N methyl D aspartate
Faster acting
Uses- adjunct therapy for treatment resistant MDD, or MDD with SI or behavior
ADE- sedative- must be monitored for 2 hours post admin; n/v, dissociation, hallucinations, elevated BP
Controlled substance for misuse
Mirtazapine (remeron)*
Atypical antidepressant
MOA- enhances serotonin and norepinephrine, antibody for alpha receptors
ADE- Sedation, increased appetite, dry mouth, weight gain
Nefazodone and trazodone *
Atypical antidepressant
MOA- weak inhibitors of serotonin and norepinephrine reuptake. Antagonist of 5HT receptor
Sedating effect
D-D-CYP3A4
ADE- priaprism, hepatotoxicity, orthostatics, dizziness, nausea, dry mouth
Vilazodone (viibryd)*
Atypical antidepressant
MOA- serotonin reuptake inhibit and 5HT receptor partial agonist
D-D CYP3A4
ADE-similar to SSRIs
Withdrawal syndrome
Vortioxetine (trintellix)*
Atypical antidepressant
MOA- serotonin reuptake inhibitor inhibition, 5HT 1 agonism, 5HT 3 and 5HT7 anatagonist
ADE- nausea; constipation, sexual dysfunctions
TCAs*
Drugs- amitriptyline, amoxapine, clomipramine (anafranil), doxepin (silenor), imipramine (tofranil), maprotiline, nortriptyline (pamelor), protriptyline, trimipramine (surmontil)
MOA- inhibit norepinephrine and serotonin reuptake, affect several other receptors like 5HT2, dopamine, histamine-more side effects than SSRIs
Uses- MDD moderate to severe, panic disorders, nocturnal enuresis, migraines, chronic pain, insomnia
ADE- blurred vision, xerostomia, urinary retention; sinus tachycardia, constipation, aggregation of angle closure glaucoma, exacerbate arrhythmia, orthostatic hypotension, dizziness, sedation, weight gain, sexual dysfunction
Uses in caution in BPD - may case a switch to manic behavior
narrow therapeutic index
Monitor those with depression and suicidal ideations
Many D-D interactions
MAOIs*
Drugs- isocarboxazid (marplan), phelelzine (nardil), selegiline (emsam), tranylcypromine (parnate)
MOA- increased stores on norepinephrine, serotonin, dopamine, inhibit MOA which catalyzes oxidation delaminating of drugs and tyramine containing foods
Uses- depression, usually intolerant or unresponsive to other agents
Many D-D interactions - no SSRIs, pseudoephedrine
Food interactions - must avoid tyramine containing foods like cheese, wine, aged meats, liver, picked or smoked fish- can cause large amounts of catecholamines to release cause hypertensive crisis, arrhythmia, cardiac arrest
ADE- drowsiness, hypotension, blurred vision, dry mouth, constipation
Serotonin-dopamine antagonist *
Second generation antipsychotic
Drugs- aripiprazole, brezipiorazole, quetiapine
MOA- block serotonin and dopamine receptors
Adjunct therapy for antidepressants
Mania and BPD*
-Lithium salt- for mania and hypomania; MOA not fully understood; therapeutic index low, monitor serum concentration; ADE- HA, dry mouth, polydipsia, polyuria, polyphagia, GI distress, tremor, dizziness, fatigue, skin reactions, sedation; signs of toxicity-ataxia, slurred speech, tremors, confusion, seizures;associated with nephrogenic diabetes insipidus, monitor thyroid function; use caution in renal patients
-valproate- also anti seizure, for maniac, not effective for MDD used as secondary agent, less toxic, monitor blood levels, no liver disease, pregnancy or mitochondrial disorders, ADE/ n/d; tremor, sedation, elevated LFTs, HA, rash, low platelet
-others-
-carbamazepine/oxabarazepine- acute maniac no blood level needed, ADE- n/v, constipation, dizziness. Rash, monitor level with cabramazepine, also WBC can cause agranulocytosis
divakproex, haloperidol, chlororpromazine, atypical antipsychotic like risperidone, olanzapine, quetiapine
-lamotrigine (not acute), unknown MOA, folic acid issues try not to use in pregnancy, ADE- HA, dry mouth, rash, DRESS
First generation antipsychotics *
Drugs- chlororomazine, thioridazine (low potency), fluphenazine, haloperidol (haldol), loxapine, molindone, perphenazine, pimozide (orap), prochlorperazine (compro, procomp), thiothixene, trifluoperazine
(High potency)
MOA- competitive inhibitors of variety of receptors mainly dopamine
More like to have EPS and movement disorders
Second generation antipsychotic *
Drugs- aripiprazole (abilify), asenapine (saphiris, secuado), brexipiprazole (rexulti), cariprazine (vraylar), clozapine (clozaril), lloperidone (fanapt), lumateperone (caplyta), lurasidine (latuda), olanzapine (zyprexa), paliperidone (invega), pimavanserin (nuplazid), quetiapine (seroquel), risperidone (risperdal), ziprasidone (geodon)
MOA- blockage of both serotonin and 5HT 2 and dopamine
Lower incidence of EPS,
Uses- first line for schizophrenic, antiemetic affects, agitation and disruptive behavior in other disorders like autism, tics
ADE- EPS, TD, neuroleptic malignant syndrome, anticholinergic effects, drowsiness, sedation, gynecomastia prolong QT, higher risk for DM, HLD, weight gain
May lower seizure threshold
BBW INCREASED RISK OF MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA
Methylxanthines *
Drugs- theophylline (elixophyllin), theobromine, caffeine
Tea, cola, energy drinks, chocolate, cocoa, coffee
MOA-translocation of extra cellular calcium, increased cyclic adenosine and cyclic guanosine, inhibition of phosphodiesterase and adenosine receptors
Actions- on CNS can decrease fatigue and increased mental alertness, 1.5 grams or more can product anxiety or tremors, spinal cord is stimulated at very high doses. On CV- inotropic or chronotropic effects, diuretic. In GI- avoid in peptic ulcer stimulates gastric secretions.
Uses- asthma, migraines
Tolerance and withdrawal symptoms
ADE- insomnia, anxiety, agitation, emesis and convulsions at toxic doses, lethal dose is 10 grams (100 cups of coffee), cardiac arrhythmias
Nicotine *
Drugs- nicoderm, nicorette, nicotrol
MOA- ganglion stimulation, CNS stimulant, can produce euphoria, arousal or relaxation, improve attention; increase BP, increase vasoconstriction including coronary arteries
High doses can lead to respiratory paralysis and hypotension
Uses- not therapeutic unless weaning from cigarettes
ADE- irritability, tremors, cramps, diarrhea, increased HR, BP, increased rate of drug metabolism
Addition and withdrawal
Varenicline (chantix)*
MOA- partial agonist of nicotinic receptors in CNS, less euphoric than nicotine
Uses- weaning from cigarette, adjunct therapy
Monitor for SI, vivid nightmares, mood changes
Cocaine *
Highly addictive, schedule 2
MOA- blockade of reuptake of norepinephrine, serotonin, dopamine
Potentials and prolongs CNS and peripheral actions, and pleasure system
Chronic use can deplete stores of dopamine creating craving
Death usually due to hyperthermia
When used with etoh causes cocaethylene which further causes cardiac issues
Amphetamines *
Drugs- dextroamphetamine (Dexedrine, zenzedi), lisdexamfetamine (vyvanse) methamphetamine (speed), methylenedioxymethamohetamine (MDMA)
MOA- elevation of catecholamines and neurotransmitters in space; inhibit reuptake, similar to cocaine, decreases appetite, insomnia, CNS stimulant
Uses- some are schedule1/2, ADHD, narcolepsy, appetite suppression
ADE- at high doses psychosis and convulsions can occur, insomnia, irritability, weakness, dizziness, confusion, delirium, panic, SI, amphetamine psychosis in long term abuse, dependence, arrhythmias, CHF, cardiac arrest
Methylphenidate (concerta, cotempla, daytrana, Ritalin) *
MOA- dopamine and norepinephrine transport inhibitor
Uses- ADHD
Schedule 2
ADE- abdominal pain, nausea, anorexia, insomnia, nervousness, fever, cardiac issues similar to amphetamines, increase seizures in epilepsy
Modafinil (provigil) and armodafinil (nuvigil)*
MOA- unclear, promotes more wakefulness but less psychoactive or euphoric effects
Uses- 1st line for narcolepsy
ADE- HA, nausea, nervousness, some potential for abuse and dependence
Controlled substance
Levodopa and carbidopa*
MOA- metabolic precursors of dopamine, enhanced synthesis of dopamine
Uses- PD
ADE-anorexia, nausea, vomiting, orthostatic hypotension, tachycardia, ventricle extrasystole, arrhythmia, blood dycrasias, hallucinations, abnormal involuntary movements, mood changes
D-D vitamin pyridoxine B6, MAOIs
Selegiline (eldepryl, zelapar), rasagiline (azilect), safinamide (xadago)
MOA- selectively inhibits MAO type B the metabolite of dopamine, increases dopamine levels, Amphetamine like actions
Uses- PD
ADE- hypertensive crisis. Insomnia, nausea, serotonin syndrome, HA, confusion
Catechol -o- methyltransferase inhibitors
Drugs- entacapone (comtan), opicapone (ongentys), tolcapone (tasmar)
Uses- PD
MOA- selection inhibits COMT for increased 3 I methyldopa a levodopa metabolite
ADE- similar to levodopa-diarrhea, postural hypotension, nausea, anorexia, dyskinesia, hallucinations, sleep disorders
Monitor LFTs
Dopamine receptor agonist *
Drugs- bromicriptine(parlodel), Ropinirole (requip), pranipexole (mirapex), rotigotine neupro), apomorphine (apokyn, kynmobi)
MOA- dopamine agonist, Longer DOA than levodopa, not effective for those who have not responded to levodopa
Uses- PD complicated by motor function and dyskinesia
ADE- nausea, vomiting, somnolence, postural hypotension, loss of impulse control-uncontrolled spending, increased libido, binge eating, hallucinations, mental conditions can worsen, pulmonary fibrosis (bromocriptine)
Amantadine (gocovri)*
Antiviral by nature but has PD uses
MOA- releases dopamine, blocks cholinergic receptors, inhibits NMDA
ADE- restlessness, agitation, confusion, hallucinations, high doses can induce psychosis, orthostatic hypotension, urinary retention, edema, dry mouth
Antimuscarinic drugs
Drugs- benztropine (congentin), trihexyphenidyl
Uses- PD
MOA-Blockage of cholinergic transmission, helps correct dopamine and acetylcholine balance
ADE- mood changes, confusion, zerostomia, constipation, visual problems
Adenosine receptor antagonist *
Drugs- istradefyllibe (nourianz)
MOA- antagonist for adenosine A2A receptor
Uses- PD, adjunct therapy with levodopa/carbidopa
ADE- dyskinesia, nausea, constipation; hallucinations, insomnia, loss of impulse control
Acetylcholinesterase inhibitors *
Drugs- donepezil (aricept), galantamine (razadyne), rivastigmine (exelon)
Uses- Alzheimer’s
MOA- inhibits acetlycholinesteraae which improves selectivity for acetylcholine transmission
ADE-nausea, diarrhea, vomiting, anorexia, tremors, bradycardia, muscle cramps
NMDA receptor antagonist *
Drug- memantine (namenda)
Uses- Alzheimer’s
MOA- antagonist for NMDA which is thought to accelerate apoptosis
Well tolerate some ADE include confusion, agitation and restlessness
Often used in combo with acetlychonlinesteraae
Aducanumab (aduhelm)
Class- amyloid beta directed monoclonal antibody
Uses- Alzheimer’s
MOA- reduces amyloid plaques in the brain uncertain if it delays progression
ADE- Brain edema, micro hemorrhage, HA, diarrhea
Sphingosine 1 phosphate receptor modulators
Drugs- fingolimod (gilenya), ozanimod (zeposia), ponesimod (ponvory), siponimod (mayzent)
Uses-MS
MOA-alter lymphocyte migration by modulating sphingosine 1 phosphate receptors, reduce lymphocytes in CNS
ADE- bradycardia, macular edema, PML, increased risk for OI
Teriflunomide (aubagio)
MOA- pyrimidine synthesis inhibitor and decreased lymphocytes in CNS
Uses-MS
ADE- elevated LFTs, avoid in pregnancy
Nuclear factor like 2 activators
Drugs-Dimethyl fumarate (tecfidera), diroximel fumarate (vumerity), mono methyl fumarate (bafiertam)
MOA- activated nuclear factor like 2 antioxidant pathway
Uses- MS
ADE- OI, PML, liver injury
Brivaracetam (briviact)*
Uses- treatment of focal seizures in adults
MOA- high and selective affinity for synaptic vesicle protein, exact MOA unknown
D-D CYP450