Neurologic agents Flashcards
alprazolam
Brand - Xanax
Class - C-IV, Benzodiazepine (short/intermediate acting)
Indication - Anxiety, panic disorder
Contraindications - Narrow-angle glaucoma, concurrent ketoconazole/itraconazole
Pregnancy - Data suggests Risk
Black Box - Concurrent use w/ opioids
Counseling - Drowsiness? Avoid alcohol, driving, crushing XR
MoA - Enhances the effect of GABA
amitriptyline
Brand - Elavil
Class - Tricyclic antidepressant
Indication - Depression
Contraindications - MAOI use in last 2w, during acute recovery period after MI, use of cisapride
Black Box - Suicidality; not approved for children <12y
Counseling - Avoid alcohol & CNS depressants, avoid sudden discontinuation, improvement may not be seen for weeks
MoA - Blocks reuptake of 5-HT & NE, subsequent downreg of adrenergic receptors
aripiprazole
Brand - Abilify
Class - Antipsychotic
Indication - Bipolar (mania), schizophrenia, depression (w/ antidepressant), Tourette syn, irritability (w/ autism)
Black Box - Dementia, sucidality
Counseling - Avoid discontinuation, alcohol. May impact mental alertness/coordination, impair heat regulation, lower seizure threshold. Report increased seizure activity, depression, thots of suicide, hyperglycemia, extrapyamidal effects, neuroleptic malignant syndrome.
MoA - Quinolinone derivative, partial agonist at DA2,3 & 5-HA1a receptors and antagonist at 5-HA2a
atomoxetine
Brand - Strattera
Class - NE reuptake inhibitor, CNS stimulant
Indication - ADHD
Contraindications - MAOIs use within 2w, narrow-angle glaucoma, pheochromocytoma, severe cardiovascular disorders where increases in BP/HR is dangerous
Pregnancy - Risk
Black Box - Suicidality in children/adolescents
Counseling - Beware mental alertness, monitor growth/weight in children for dose, report new psychiatric problems, chest pain, palpitations, dyspena, cardiac dysrhythmias, MI, or cerebrovascular accidents. Do not open capsules (dust irritates eyes).
MoA - Selective NE reuptake inhibitor for ADHD
bupropion
Brand - Wellbutrin (SR, XL), Aplenzin
Class - Monocyclic antidepressant
Indication - Depression, SAD, smoking cessation
Contraindications - Seizures, anorexia/bulimia, MAOI use within 2w, undergoing abrupt discontinuation of alcohol, benzodiazepines, barbituarates, or antiepileptics
Black Box - Suicidality, neuropsychiatric reactions
Counseling - Avoid alcohol, CNS depressants, activities w/ mental alertness. Tk at the same time (at bedtime). XL tab shell visible in stool.
MoA - Mild DA & NE uptake inhibitor, no direct effect on 5-HT receptors or MAO
buspirone
Brand - BuSpar
Class - Antianxiety
Indication - Anxiety
Counseling - Realize mental alertness, improvement may not be seen for weeks, avoid sudden discontinuation. Tk w/wo food but consistently. Avoid alcohol, grapefruit juice, and MAOI.
MoA - Selective 5-HT1a receptor partial agonist. Acts on DA2 autoreceptors and can DR B-adrenergic receptors. Does not have amnestic, anticonvulsant, muscle relaxant, or hypnotic effects like a benzodiazepines.
carbamazepine
Brand - Tegretol
Class - Anticonvulsant
Indication - Epilepsy, trigeminal neuralgia
Contraindications - Bone marrow depression, MAOIs, nefazodone
Black Box - Agranulocytosis, aplastic anemia, dermatological reactions (esp Asians), screen for HLA-B*15:02
Counseling - May decrease effectiveness of oral contraceptives (use condom), take with food but not alcohol or grapefruit, avoid abrupt discontinuation, realize mental alertness
MoA - Blocks firing of AP, decreases excitatory NT
carbidopa / levodopa
Brand - Rytary, Duopa
Class - Antiparkinsonian
Indication - Parkinson disease
Contraindications - Narrow-angle glaucoma, concurrent MAOI or linezolid
Pregnancy - Risk (carbidopa)
Counseling - Place disintegrating tablets on tongue
MoA - Carbidopa (does not cross BBB) allows more levodopa to reach CNS before decarboxylating so less is required and less side effects occur, levodopa turns into DA
citalopram
Brand - Celexa
Class - SSRI antidepressant
Indication - Depression
Contraindications - Concomitant use of pimozide or MAOIs
Pregnancy - Risk
Black Box - Suicidal ideation, not approved for children
Counseling - Realize mental alertness. Improvement may not be seen for several weeks, avoid abrupt discontinuation. Do not drink alcohol or use NSAIDs, report worsening depression or unusual bleeding.
MoA - Bicyclic selective/potent inhibitor of 5-HT reuptake
clonazepam
Brand - Klonopin
Class - C-IV, Benzodiazepine
Indication - Panic disorder, seizure
Contraindications - Liver disease, narrow-angle glaucoma
Black Box - Concurrent use w/ opioids, abuse/addiction
Counseling - May cause drowsiness, avoid alcohol. Allow disintegrating tab to dissolve on tongue.
MoA - Enhances the effect of GABA
dexmethylphenidate
Brand - Focalin
Class - C-II, CNS Stimulant
Indication - ADHD
Contraindications - MAOI use, drug dependence, glaucoma, tics or Tourette syn
Black Box - Abuse & dependence
Counseling - Avoid late doses (insomnia), may pour on applesauce and swallow whole if needed.
MoA - Increases CNS activity by inhibiting reuptake of NE & DA
dextroamphetamine
Brand - Dexedrine, {Adderall is dextroamphetamine&hetamine salt}
Class - C-II, CNS Stimulant
Indication - ADHD, Narcolepsy
Contraindications - HSN, HTN, Advanced arteriosclerosis, Hyperthyroidism
Black Box - Cardiac events including sudden death, Abuse & dependence
Counseling - May cause anorexia, Report vocal or motor tics, Caution pt w/ history of seizure, Do not give at bedtime (insomnia), Report irregular HR
MoA - Amphetamines cause release of DA and NE at presynaptic nerve terminals and may block reuptake of NE and DA by competitive inhibition.
diazepam
Brand - Valium
Class - C-IV, Benzodiazepine
Indication - Alcohol withdrawal syndrome, anxiety, seizure
Contraindications - Narrow-angle glaucoma, severe liver disease, myasthenia gravis, sleep apnea, respiratory insufficiency, kids <6mo
Pregnancy - Risk
Black Box - Concurrent use w/ opioids
Counseling - May cause drowsiness, avoid alcohol, avoid driving.
MoA - Enhanced effect of GABA
divalproex Na+
Brand - Depakote
Class - Anticonvulsant
Indication -Seizures, manic bipolar disorder, migraine prophylaxis
Contraindications - Hepatic disease, urea cycle disorders
Pregnancy - Risk
Black Box - Hepatotoxicity, teratogenicity, pancreatitits, patients w/ mitochondrial disease
Counseling - May cause dizziness or somnolence, look for signs of liver dysfunction during first 6 mo, tk w/ food to avoid GI upset, do not discontinue abruptly, avoid alcohol
MoA - Sodium valproate/valproic acid increases GABA by inhibiting metabolism and limits repetitive neuronal firing through sodium channels
donepezil
Brand - Aricept
Class - Central cholinesterase inhibitor
Indication - Alzheimer disease, dementia
Contraindications - Hypersensitivity to piperidine derivatives
Counseling - Take at bedtime, allow tab to dissolve on tongue and follow w/ water. Report GI bleeding. Adverse effects tend to resolve w/ continued use.
MoA - Enhances ACe by reversibly inhibiting AChE (that hydrolyzes it), it is highly selective for the CNS, so less peripheral side effects
duloxetine
Brand - Cymbalta
Class - SNRI antidepressant
Indication - Anxiety, Depression, Diabetic peripheral neuropathy pain/fibromyalgia/musculoskeletal pain
Contraindications - MAOI, TCA, linezolid use, uncontrolled glaucoma
Pregnancy - Risk
Black Box - Suicidality, not approved for children
Counseling - Report withdrawal, may cause hepatoxicity and increased risk of bleeding, require several weeks for depression improvement, avoid alcohol.
MoA - Selectively inhibits reuptake of 5-HT & NE
escitalopram
Brand - Lexapro
Class - SSRI antidepressant
Indication - Depression, Generalized anxiety disorder
Contraindications - Concurrent MAOI use
Pregnancy - Risk
Black Box - Suicidality
Counseling - Improvement may not be seen for 6w, report worsening depression, avoid abrupt ddiscontinuation, do not drink alcohol or use NSAIDs
MoA - S-enatiomer of citaloprom and selective inhibitor of 5-HT reuptake
fluoxetine
Brand - Prozac
Class - SSRI antidepressant
Indication - Depression, OCD, Panic Disorder, Bulimia nervosa, Premenstrual dysphoric disorder
Contraindications - Concomitant pimozide, thiordazine, or MAOIs
Pregnancy - Risk
Black Box - Suicidality, approved children >7y
Counseling - Take before breakfast, do not drink alcohol or use NSAIDs, improvement may not be seen for several weeks, while adverse effects present in the first week, report worsening depression.
MoA - Bicyclic selective & potent inhibitor of 5-HT reuptake
guanfacine
Brand - Intuniv
Class - Alpha2-adernergic agonist
Indication - ADHD (extended release), HTN (immediate release)
Counseling - Avoid alcohol, CNS depressants, caution driving, report signs of hypotension, hepatic dysfunction, edema; avoid abrupt discontinuation
MoA - Stimulates alpha receptors in the CNS by activating inhibitory neurons to decrease sympathetic outflow
lamotrigine
Brand - Lamictal
Class - Phenyltriazine anticonvulsant
Indication - Bipolar I disorder, partial seizure
Black Box - Serious skin reactions
Counseling - Seek PCP if blistering rash, yellowing of skin/eyes, unusual bleeding, shortness of breath, or suicidal thoughts occur; avoid alcohol
MoA - Inhibits voltage Na+ channels, stabilizing membranes and reducing release of excitatory NT like glutamate and aspartate
levetiracetam
Brand - Keppra (XR)
Class - Anticonvulsant
Indication - Myoclonic/partial/tonic-clonic seizure
Pregnancy - Risk
Counseling - Realize mental alert, report mood swings, agitation, avoid sudden discontinuation of drug
MoA - Pyrrolidine derivative that is unrelated to other AEDs
lisdexamfetamine [dimestylate]
Brand - Vyvanse
Class - C-II, amphetamine
Indication - ADHD, binge eating disorder
Contraindications - hypersensitivity/idiosyncrasy to sympthomimetic amines; MAOIs; CV disease/advanced arteriosclerosis; mod-severe HTN; hyperthyroidism, glaucoma, agitated states, history of drug dependence
Pregnancy - Risk
Black Box - Risk of abuse/misuse/diversion
Counseling - Tk in morning; monitor growth rate/weight in children, report new psych problems, chest pain, palpitations, dyspnea, signs of cardiac dysrhythmia, AMI, cerebrovascular accident
MoA - Prodrug of dextroamphetamine > release DA & NE and block reuptake by competitive inhibition
lithium
Brand - Eskalith (CR), Lithobid
Class - Antimanic
Indication - Bipolar disorder (maintenance or manic episode)
Contraindications - Severe debilitation, dehydration, Na+ depletion, CV disease, renal impairment, concomitant diuretic therapy
Pregnancy - Risk
Black Box - Lithium levels required
Counseling - Dispense medication guide. Maintain fluid and salt intake. Report signs of toxicity (diarrhea, vomiting, tremor, ataxia, drowsiness, muscle weakness, lack of coordination, giddiness, blurred vision, tinnitus, or large volumes of dilute urine.
MoA - Alters action of several second-messenger systems, cation transport across cell membrane and influence reuptake of 5-HT and/or NE, inhibited phosphatidylinositol cycle messangers
lorazepam
Brand - Ativan
Class - C-IV, Benzodiazepine (short or intermediate act)
Indication - Anxiety, Insomnia (due to situational stress)
Contraindications - Narrow-angle glaucoma
Pregnancy - Risk
Black Box - Concurrent use w/ opioids
Counseling - Drowsiness, avoid alcohol, avoid driving
MoA - Enhance the effect of GABA
memantine
Brand - Namenda
Class - NMDA receptor antagonist
Indication - Alzheimer disease
Pregnancy - Weigh risks/benefits
Counseling - Administer oral solution w/ dosing device
MoA - Noncompetitive antagonist of NMDA receptors normally activated by glutamate
methylphenidate
Brand - Ritalin, Concerta
Class - C-II, CNS Stimulant
Indication - ADHD, narcolepsy
Contraindications - Anxiety, agitation, cocurrent MAOIs, drug dependence, glaucoma, tics or Tourette, HTN, angina, heart failure, concurrent halogenated anesthetics
Pregnancy - Moderate risk
Black Box - Abuse/dependence potential
Counseling - Avoid late doses (insomnia), avoid abrupt discontinuation. Patch: apply same time each day, alt hips, remove after 9 h.
MoA - Increases CNS activity by inhibiting reuptake of NE & DA
mirtazapine
Brand - Remeron
Class - alpha2-antagonist, antidepressant
Indication - Depression
Contraindications - MAOIs use within 2w, linezolid or IV methylene blue use
Pregnancy - Moderate Risk
Black Box - Sucidality; not for use in children
Counseling - Take prior to sleep. Dissolve on tongue. Avoid alcohol. Report worsening depression. Realize mental alertness.
MoA - Antagonizes alpha2-adrenergic auto/heteroreceptors that release NE & 5-HT to increase activity with minimal adverse effects
nortriptyline
Brand - Pamelor
Class - Tricyclic antidepressant
Indication - Depression
Contraindications - MAOI use within 2w, use during acute recovery period after MI, use of linezolid or IV methylene blue
Black Box - Sucidality
Counseling - May cause somnolence/dizziness. Report worsening depression or unusual bleeding. Avoid abrupt discontinuation, avoid alcohol.
MoA - Demethylated metabolite of amitriptyline, heterocyclic AD that blocks reuptake of NE and DR adrenergic receptors (not much activity on 5-HT).
oxcarbazepine
Brand - Trileptal
Class - Dibenzazepine Carboxamide, anticonvulsant
Indication - Partial seizure
Pregnancy - Risk
Counseling - Tk w/ food, avoid alcohol and grapefruit. Shake well and prep dose immediately. Report signs of serious dermatologic reactions, myelosuppression, or hepatotoxicity. Avoid abrupt discontinuation, realize mental alertness.
MoA - 10-keto analogue of carbamezepine that works through an active 10-monohydroxy metabolite
paroxetine
Brand - Paxil (CR)
Class - SSRI antidepressant
Indication - Depression, generalized/social anxiety or panic disorder, OCD, PTSD, premenstrual synd, menopause (vasomotor symp)
Contraindications - Concomitant use of thioridazine, MAOIs
Pregnancy - Contraindicated
Black Box - Suicidality
Counseling - Do not drink alcohol, caution w/ NSAIDs, avoid abrupt discontinuation, improvement may not be seen for weeks, realize mental alert. Shake suspension well, do not crush CR tabs.
MoA - Highly selective/potent inhibitor of 5-HT reuptake
phenobarbital
Brand - Luminal
Class - C-IV, Long-acting Barbiturate
Indication - Epilepsy, Daytime sedation
Contraindications - Liver impairment, dyspnea/res obstruction, history of hypnotic addiction, family history of acute intermittent porphyria
Pregnancy - Risk
Counseling - May cause dizziness/somnolence, avoid alcohol, CNS depressants, driving, sudden discontinuation. Many drug interactions, check with HCP for new OTC.
MoA - Depresses CNS (sedation»_space; gen anesthesia)
phenytoin
Brand - Dilantin
Class - Hydantoin Anticonvulsant
Indication - Seizure
Contraindications - Sinus bradycardia, AV block
Black Box - Hypotension and arrhythmias (w/ IV admin)
Counseling - Report signs of pancytopenia, hepatotoxicity, systemic lupus erythematosus, or skin reaction. Many drug interactions, check w/ HCP for new OTC. Do not drink alcohol, realize mental alert, shake suspension well, do not crush XR tabs.
MoA - Suppresses spread of seizure by inhibiting synaptic posttetanic potentiation and blocking propagation of electric discharge (might decrease Na+ transport and block Ca2+ channels)
pramipexole H2Cl2
Brand - Mirapex (ER)
Class - Dopamine agonist, Antiparkinson
Indication - Parkinson, Restless leg synd
Counseling - Tk w/ food if nausea, rise slowly from a sitting/lying position. Report new urges to gambling, sex, compulsive eating or buying, or worsening dyskinesia. Realize mental alertness, avoid alcohol and other CNS depressants. Do not discontinue abruptly (emergent hyperpyrexia/confusion)
MoA - Selective DA2,3 agonist but no activity at DA1. (DA2 important in Parkinson)
pregabalin
Brand - Lyrica
Class - Anticonvulsant, Analgesic
Indication - Neuropathic pain, fibromyalgia, partial seizure, postherpetic neuralgia
Pregnancy - Moderate risk
Counseling - Solution must be used in 45d, avoid sudden discontinuation, alcohol, CNS depressants; realize mental alertness
MoA - GABA analogue binds to alpha2-delta site in CNS, reduces Ca2+ dependent release of NT
quetiapine
Brand - Seroquel (XR)
Class - (atypical) Antipsychotic
Indication - Bipolar, Schizophrenia, Major Depressive disorder (w/ antidepressant)
Black Box - Mortality in dementia, suicidality, not approved for kids <10y
Counseling - Caution w/ increase temp. Tk w/ food, avoid alcohol and coordination activities. Rise slowly from sitting. Report signs of hyperglycemia, bradycardia, arrhythmia, tardive dyskinesia, neuroleptic malignant syndrome.
MoA - Antagonist of 5-HT1a,2; DA1,2; H1; A1,2. Combo of DA2 and 5-HT2 > bipolar/schizophrenia
risperidone
Brand - Risperdal
Class - Benzisoxazole, Antipsychotic
Indication - Schizophrenia, Bipolar (acute manic/mixed), Autism (irritability)
Contraindications - Agents that increase QTc interval
Black Box - Mortality in dementia, DRESS?
Counseling - Tk w/ food. Caution w/ increasing core temp. Rise slowly from sitting. Report signs of hyperglycemia, arrhythmia, tardive dyskinesia, neuroleptic malignant syndrome. Realize mental alertness. Place on tongue and dissolve. Solution may be mixed w/ water/coffee/OJ/milk but not soda/tea.
MoA - Potent 5-HT2 and weak DA2 antagonist.
ropinirole
Brand - Requip (XL)
Class - Dopamine agonist
Indication - Parkinson, Restless legs syndr
Pregnancy - Risk
Counseling - Tk w/ food (nausea). Rise slowly from sit, avoid sudden discontinuation, alcohol, other CNS depressant. Report dyskinesia, BP changes, fainting, or new urges. Realize mental alertness.
MoA - Higher specificity to DA3 than DA2&4, moderate affinity for opioid receptors (stimulates postsynaptic DA2 receptor in Parkinson)
sertraline
Brand - Zoloft
Class - SSRI antidepressant
Indication - Depression, OCD, Premenstrual dyphoric disorder, Panic/PTSD/Social phobia disorders
Contraindications - Concomitant use of pimozide, thiordiazine, or MAOIs
Pregnancy - Risk
Black Box - Suicidality, not approved for kids (depression), must be >6y for OCD
Counseling - Improvement may not be seen for weeks, avoid abrupt discontinuation, report worsening depression or unusual bleeding. Avoid alcohol & NSAIDs. Realize mental alertness.
MoA - SSRI, indirectly DR Beta-adrenergic receptors.
temazepam
Brand - Restoril
Class - C-IV, Benzodiazepine
Indication - Insomnia
Contraindications - Narrow-angle glaucoma, pregnancy
Black Box - Concurrent use w/ opioids
Counseling - Tk 30 min before bed. Causes drowsiness, avoid alcohol, driving. Sleepwalking has been reported!
MoA - Metabolite of diazepam, enhances effect of GABA
topiramate
Brand - Topamax
Class - Anticonvulsant
Indication - Seizure (partial or tonic-clonic), migraine prophylaxis
Contraindications - For ER formulation: Alcohol use within 6 hours before/after
Pregnancy - Risk
Counseling - May cause dizziness, somnolence, diplopia, nervousness, confusion, decrease sweating (avoid hot temps), kidney stones (drink wawa), decrease oral contaceptives (use condom). Avoid alcohol and other CNS depressants, if more than 1 missed dose, consult HCP. Realize mental alertness.
MoA - Might block voltage Na+ channel, augment the activity of GABA-A receptor, and antagonize/inhibit other stuff
trazodone
Brand - Desyrel
Class - Antidepressant
Indication - Depression
Contraindications - Use of MAOI within 2ws
Black Box - Suicidal ideation, not for kids
Counseling - May cause dizziness/somnolence, realize mental alert, report signs of pripism ASAP. Avoid alcohol, other CNS depressants, and sudden discontinuation.
MoA - Inhibits reuptake of 5-HT, and blocks H1 and alpha1-adrenergic receptors.
venlafaxine
Brand - Effexor (XR)
Class - SNRI antidepressant
Indication - Generalized anxiety, depression, panic, and social anxiety disorders
Contraindications - MAOIs
Pregnancy - Risk
Black Box - Suicidal ideation
Counseling - Tk w/ food, no alcohol. Improvement may not be evident for weeks, do not discontinue. May cause dizziness/somnolence. Do not chew ER tabs.
MoA - Potent 5-HT & NE reuptake inhibitor
zolpidem
Brand - Ambien, Intermezzo
Class - C-IV, Hypnotic (nonbarbiturate)
Indication - Insomnia (short-term)
Contraindications - History of sleepwalking
Pregnancy - Risk
Black Box - Risk of sleepwalking
Counseling - Tk on empty stomatch immediately before bedtime. May cause daytime drowsiness, avoid driving, alcohol, other CNS depressants. Warn patient of sleep-walking, partner should monitor irregular respiration.
MoA - Binds to benzodiazepine receptor somehow, increases chloride conductance and inhibition of AP
