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PharmTest2

Pharm

QuestionAnswer
BARBITUATES Phenobarbital, Pentobarbital, Thiopental; GABA(a) receptor agonist; @ low = increases GABA-induced opening; @ high = directly activates & opens; NEVER GIVE CNS STIMULANTS
Phenobarbital Long-acting barb; enhance GABA(a) receptor; USE = daytime sedative, antiseizure (tonic-clonic & partial); AE = hypothermia, hyoptension, bradypnea, bradycardia, rapid weak thready pulse, cold/cyanotic skin
Pentobarbital Mid-acting barb; enhance GABA(a) receptor; USE = hypnotic (insomnia), preop sedative; AE = hypothermia, hyoptension, bradypnea, bradycardia, rapid weak thready pulse, cold/cyanotic skin
Thiopental Short-acting barb; enhance GABA(a) receptor; USE = induction of anesthesia; AE = hypothermia, hyoptension, cardiac/resp depression, cold/cyanotic skin
BENZODIAZEPINES Alprazolam, Chlordiazepoxide, Clonazepam, Diazepam, Flurazepam, Lorazepam, Midazolam, Temazapam; GABA(a) receptor agonists; No effect without GABA; NEVER GIVE ALCOHOL
Alprazolam Mid-acting benzo; enhance GABA(a) receptors; USE = anxiety; AE = sedation, altered sleep pattern, anterograde amnesia
Chlordiazepoxide Mid-acting benzo; enhance GABA(a) receptors; USE = anxiety, anesthetic; AE = sedation, altered sleep pattern, anterograde amnesia
Clonazepam Long-acting benzo; enhance GABA(a) receptors; USE = seizures, mania, muscle spasticity; AE = sedation, altered sleep pattern, anterograde amnesia
Diazepam Long-acting benzo; enhance GABA(a) receptors; USE = anxiety, status epilepticus, muscle spasticity, anesthetic; AE = sedation, altered sleep pattern, anterograde amnesia
Flurazepam Long-acting benzo; enhance GABA(a) receptors; USE = insomnia; AE = sedation, altered sleep pattern, anterograde amnesia
Lorazepam Mid-acting benzo; enhance GABA(a) receptors; USE = anxiety, status epilepticus, anesthetic; AE = sedation, altered sleep pattern, anterograde amnesia
Midazolam Short-acting benzo; enhance GABA(a) receptors; USE = anesthetic (amnestic/anxiolytic); AE = sedation, altered sleep pattern, anterograde amnesia
Temazapam Mid-acting benzo; enhance GABA(a) receptors; USE = insomnia; AE = sedation, altered sleep pattern, anterograde amnesia
Flunitrazepam benzodiazepine (used as a date rape)
Zolpidem Binds @ BZ1 site of GABA(a); USE = hypnotic (insomnia); AE = headache, bitter aftertaste (1st week), morning sedation (if taken too late), sleep-walking/eating
Zaleplon Binds @ BZ1 site of GABA(a); USE = hypnotic (insomnia); AE = headache, bitter aftertaste (1st week), morning sedation (if taken too late), sleep-walking/eating
Eszopiclone Binds @ BZ1 site of GABA(a); USE = hypnotic (insomnia); AE = headache, bitter aftertaste (1st week), morning sedation (if taken too late), sleep-walking/eating
Flumazenil Competitive GABA antagonist; USE = benzo overdose; AE = agitation, confusion, risk of seizure
Melatonin 5-HT derivative from pineal (controlled by light); USE = promote sleep (from jet lag)
Ramelteon MT1/2 agonist (in SCN); USE = hypnotic (promotes falling asleep); AE = hyperprolactinemia, hypogonadism, infertility, osteoporosis, decreased testosterone
Doxylamine H1 receptor antagonist (also anticholinergic & anti-alpha adrenergic); USE = hypnotic; AE = daytime sedation, dry mouth, urinary retention
Diphenhydramine H1 receptor antagonist (also anticholinergic & anti-alpha adrenergic); USE = hypnoti, dystoniasc; AE = daytime sedation, dry mouth, urinary retention
Alcohol
Sodium Oxybate GABA(b) agonist (made into GABA @ high conc); USE = narcolepsy; AE = resp/cv depression, LOC, seizures, urinary incontinence, dizziness
GHB GABA(b) agonist (made into GABA @ high conc); USE = date rape; AE = resp/cv depression, LOC, seizures, urinary incontinence, dizziness
Modafinil Inhibit DAT/NET (stimulant); USE = narcolepsy, excessive sleepiness (from apnea, shift-work); AE = headache
SPASMOLYTICS Baclofen, Tizanidine, Dantrolene, Diazepam, Clonazepam; USE = MS, ALS, spinal transection, cerebral palsy
Baclofen GABA(b) agonist; AE = drowsiness, seizures
Tizanidine alpha2-agonist; AE = drowsiness, hypotension, dry mouth
Dantrolene Decrease Ca+2 release from SR; AE = muscle weakness (NOT used in ALS), hepatotoxicity
Carbamazepine Inhibits Na+ channels; USE = partial & generalized tonic-clonic seizures, mania (bipolar); AE = liver damage (need LFTs), aplastic anemia, agranulocytosis, hyponatremia, teratogen; OTHER = induced own metabolism (CYP450)
Phenytoin Inhibits Na+ channels; USE = partial & generalized tonic-clonic seizures, status epilepticus; AE = gingival hyperplasia, hirsuitism, teratogen, nystagmus; OTHER = monitor thyroid function, induces CYP450
Lamotrigine Inhibits Na+ channels & glutamate release; USE = partial & generalized tonic-clonic seizures, Lennox-Gastaut (<16), bipolar (maintenance); AE = toxic epidermal necrolysis, DIC, hypersensitivity
Valproate Inhibits Na+ & T-type Ca+2 channels, inhibits GABA-T, stimulates GAD; USE = all seizures, mania (bipolar); AE = hepatotoxicity (LFTs needed), NTDs, pancreatitis, thrombocytopenia; OTHER = highly protein bound
Topiramate Inhibit Na+ channel, enhance GABA, AMPA/KA antagonist; USE = partial seizures; AE = metabolic acidosis, renal calculi, myopia, hyperthermia, language dysfunction
Gabapentin Decrease Ca+2 influx (little NE, Glu), increased GABA; USE = partial seizures; AE = peripheral edema, behavor disorders
Ethosuximide Inhibits T-type Ca+2 channels; USE = absence seizures; AE = blood dyscrasias, skin rxn's, photophobia
Fosphenytoin USE = status epilepticus
Corticotropin USE = infantile spasms (before 1st yr)
Prednisone USE = infantile spasms (before 1st yr)
Absence seizures Ethosuxomide, Valproate, Lamotrigine
Partial Seizures Carbamazepine, Phenytoin, Lamotrigine, Valproate, Topiramate, Gabapentin, Phenobarbital (infants)
Tonic-Clonic Seizures Valproate, Phenytoin, Carbamazepine, Lamotrigine, Phenobarbital (infantile)
Status Epilepticus Lorazepam, Diazepam, Fosphenytoin
Infantile Spasms Corticotropin, Prednisone
IV Anesthetics Thiopental (barbiturates), Etomidate, Propofol, Opioids, Ketamine, Midazolam (Benzo)
Inhaled Anesthetics Halothane, Isoflurane, Desflurane, Sevoflurane, Nitrous Oxide
Local Anesthetics Esters (cocaine, procaine, tetracaine, benzocaine) [plasma cholinesterase] & amides (lidocaine, bupivocaine) [CYP450]; given with Epinephrine to decrease rate of absorption
Halothane GABA(a) agonist; USE = induction/maintenance of anesthesia; AE = malignant hyperthermia (w/ succinylcholine), myocardial depression, arrhythmias
Isoflurane GABA(a) agonist; USE = induction/maintenance of anesthesia; AE = airway irritation, increased HR
Desflurane GABA(a) agonist; USE = induction/maintenance of anesthesia; AE = airway irritation, increased HR
Sevoflurane GABA(a) agonist; USE = induction/maintenance of anesthesia; AE = decreased CO, risk of renal failure (fluoride toxicity)
Nitrous Oxide GABA(a) agonist; USE = induction/maintenance of anesthesia (incomplete anesthetic); AE = Increase ICP
Propofol Potentiate GABA(a); USE = induction/maintenance of anesthesia, anti-emetic; AE = repiratory depression, dec in MAP
Etomidate Potentiate GABA(a); USE = induction of anesthesia; AE = myoclonus, post-op nausea/vomit, adrenal suppression
Ketamine NMDA receptor antagonist; USE = minor surgical procedures; AE = inc cerebral flow, cardiac stimulant (leads to depression)
Injectible Local Anesthetics Procaine, Lidocaine, Bupivocaine
Skin/MM Local Anesthetics Benzocaine, Lidocaine, Cocaine
Ophthalmological Local Anesthetic Proparacaine
Cocaine Inhibit monoamine uptake; USE = topical anesthesia; AE = cardiomegaly, paranoia, psychosis, nasal septum damage, withdrawal (increased appetite, ahedonia, depression)
Procaine Block Na+ channels (intra); USE = infiltration anesthesia, diagnostic nerve blocks; AE = hypersensitivity rxn's due to PABA
Benzocaine Block Na+ channels (intra); USE = topical to wounds/ulcers
Lidocaine Block Na+ channels (intra); USE = intermediate local, antiarrhythmic
Bupivocaine USE = minor surgical procedures; AE = CV depression (hypotension)
Tetradotoxin/Saxitoxin Blocks Na+ channel (outer pore)
Parkinson's Tx Levodopa, carbidopa, bromocriptine, ropinirole, pramipexole, rotigotine, amantadine, rasagiline, selegiline, propranolol, benztropine, trihexyphenidyl, entacapone
Alzheimer's Tx donepezil, rivastigmine, galantamine, memantine
Levodopa Converted into dopamine (acts @ D2 to inhibit GABA & cholinergic); USE = Parkinsons; AE = nausea, orthostatic hypotension, arrhythmias, psychosis, dyskinesia, "on-off" phenomena; OTHER = don't give w/ MAOIs (HTN crisis) or antipsychotics (antagonistic)
Carbidopa DOPA-decarboxylase inhibitor (periphery); USE = adjunct to levodopa; AE = less side effects due to less need for high L-dopa
Rasagiline MAO B inhibitor (CNS); USE = Parksinson's
Selegiline MAO B inhibitor (CNS - older); USE = Parkinson's
Entecapone COMT inhibitor (prevent further L-dopa breakdown in periphery); USE = Parkinson's; AE = HTN @ high doses
Bromocriptine Partial D2 agonist; USE = adjunct in Parksinson's (reduce "on-off" incidence); AE = nausea, orthostatic HoTN, hallucinations, dyskinesias
Ropinirole D2 agonist; USE = early stage Parkinsons; AE = nausea, orthostatic HoTN, hallucinations, dyskinesias
Pramipexole D2 agonist; USE = early stage Parkinsons; AE = nausea, orthostatic HoTN, hallucinations, dyskinesias
Rotigotine D2 agonist; USE = early stage Parkinsons; AE = nausea, orthostatic HoTN, hallucinations, dyskinesias; OTHER = transdermal
Benztropine/Trihexyphenidyl Muscarinic cholinergic antagonist; USE = very early stage parksinson's, dystonias; AE = dry mouth, blurred vision, urinary retention
Amantadine Displaces dopamine from nerve terminals; USE = early stage parkinson's; AE = hallucinations
Donepezil AChE inhibitor; USE = Alzheimers; AE = NVD, anorexia, abdominal pain
Rivastigmine AChE inhibitor; USE = Alzheimers; AE = NVD, anorexia, abdominal pain
Galantamine AChE inhibitor; USE = Alzheimers; AE = NVD, anorexia, abdominal pain
Memantine NMDA receptor antagonist; USE = Alzheimers (slows progression)
Albuterol Short-acting beta2-agonists, transcellular shift K+ into cell; USE = acute, severe asthma (bronchodilator), hyperkalemia
Tiotropium Long-acting M3 competitive antagonist; USE = asthma (intolerant to Beta-agonists); AE = urinary retention, tachycardia, dry mouth, loss of accomodation
Ipratropium Short-acting M3 competitive antagonist; USE = asthma (intolerant to Beta-agonists); AE = urinary retention, tachycardia, dry mouth, loss of accomodation
Theophylline Inhibit phosphodiesterase, adenosine receptor antagonist; USE = asthma; AE = arrhythmias, tachycardia, arousal, tremor; OTHER = macrolides cause major buildup
Fluticasone Inhibit cytokine production & PLA2 activity, potentiate beta-agonists; USE = asthma (anti-inflammatory); AE = cataracts, decreased bone density, oral candidiasis, wt gain, Cushingoid syndrome, adrenal suppression
Montelukast Reversible inhibitor of Cysteinyl leukotriene-1 receptor (block LTC4/D4/E4); USE = prevent aspirin/exercise induced asthma; AE = abnormal LFTs
Cromolyn Inhibit delayed chloride channels & IgE production; USE = prophylaxis for exercise induced asthma; AE = throat irritant, cough, dry mouth, chest tightness
Omalizumab Removing unbound IgE (prevent interaction with mast cells); USE = asthma prevention
Fomepizole Inhibits alcohol dehydrogenase (ADH); USE = methanol or ethylene glycol poisoning
Ethanol Inhibit NMDA receptor, potentiate GABA-mediated inc in Cl- conductance, CB1 agonist (decreased LHRH); AE = tachycardia, arrhythmia, euphoria, dehydration, gastritis, pancreatitis, hepatitis, teratogen
Disulfuram Inhibitis acetaldehyde DH; USE = alcohol cessation (negative feedback); AE = nausea, emesis, cutaneous vasodilation, jaundice
Alcohol Dependence Signs/Symptoms Tremors, hyper-reflexia, sweating, hallucinations, delirium tremens (3-4 days after), hyperthermia, Wernicke-Korsakoff, pellagra, tonic-clonic seizures, decreased appetite (7kcals/g), GI problems, erectile dysfunction, testicular atrophy
Naltrexone opiate antagonist (reduces reinforcing effects in Nac); USE = alcohol dependence
Acamprosate Inhibit NMDA receptor (reduces craving); USE = alcoholism
MAOIs Tranylcypromine
TCAs Imipramine, desipramine, amitriptyline, nortriptyline
SSRIs fluoxetine, sertraline, venlafaxine, duloxetine
Antidepressants (ALL) MAOIs, SSRIs, TCAs, trazodone, bupropion, mirtazapine
Bipolar (Manic) Antipsychotics (haloperidol, olanzipine, quetiapine, aripiprazole), benzos (lorazepam, diazepam, clonazepam), antiseizure (valproate, carbamazepine, lamotrigine)
Bipolar (Depression) olanzapine & fluoxetine, lamotrigine, quetiapine
Bipolar lithium, antiseizure (valproate, carbamazepine, lamotrigine)
ADHD D-amphetamine, methylphenidate, atomoxetine
Tranylcypromine Irreversibly inhibit MAO A & B; USE = antidepressant, panic disorder, phobias; AE = orthostatic HoTN, insomnia, hypomania, agitation, sexual dysfunction, serotonin syndrome (w/ SSRIs); OTHER = avoid tyramine (cheese, red wine)
Imipramine Tertiary amine; blocks 5HT/NE reuptake, also muscarinic, H1, a1; USE = depression, migraine, ADHD, chronic pain, OCD; AE =sedation, orthostatic HoTN, conduction block, arrhythmias, dry mouth, confusion, increased appetite
Desipramine Secondary amine; blocks 5HT/NE(primary) reuptake, also muscarinic, H1, a1; USE = depression, migraine, ADHD, chronic pain, OCD; AE =sedation, orthostatic HoTN, conduction block, arrhythmias, dry mouth, confusion, increased appetite
Amitriptyline Tertiary amine; blocks 5HT/NE reuptake, also muscarinic, H1, a1; USE = depression, migraine, ADHD, chronic pain, OCD; AE =sedation, orthostatic HoTN, conduction block, arrhythmias, dry mouth, confusion, increased appetite
Nortriptyline Secondary amine; blocks 5HT/NE(primary) reuptake, also muscarinic, H1, a1; USE = depression, migraine, ADHD, chronic pain, OCD; AE =sedation, orthostatic HoTN, conduction block, arrhythmias, dry mouth, confusion, increased appetite
Fluoxetine Block 5HT reuptake; USE = panic disorders, OCD, eating disorders, depression; AE = headache, Gi upset, sexual dysfunction, serotonin syndrome (w/ MAOIs)
Sertaline Block 5HT reuptake (& some DA block); USE = panic disorders, OCD, eating disorders, depression; AE = headache, Gi upset, sexual dysfunction, serotonin syndrome (w/ MAOIs)
Venlafaxine Block 5HT/NE reuptake; USE = panic disorders, OCD, eating disorders, depression; AE = headache, Gi upset, sexual dysfunction, serotonin syndrome (w/ MAOIs)
Duloxetine Block 5HT/NE reuptake; USE = panic disorders, OCD, eating disorders, depression; AE = headache, Gi upset, sexual dysfunction, serotonin syndrome (w/ MAOIs)
Trazodone Inhibit 5HT/NE reuptake, 5HT2A antagonist; USE = antidepressant; AE = sedation, orthostatic HoTN, nausea, priapism
Bupropion Inhibit DAT/NET, nicotinic antagonist; USE = antidepressent, smoking cessation; AE = dry mouth, nausea
Mirtazapine alpha2 & 5HT2/3 antagonist; USE = antidepressant; AE = sedation, wt gain, increased appetite
Lithium Inhibits IP3 metabolism; USE = bipolar (maintenance), schizoaffective disorder; AE = tremor, edema, nephrogenic DI, DI irritation, NVD, mental confusion, aphasia
Methylphenidate Inhibits NE/DA/5HT reuptake; USE = narcolepsy, ADHD
D-amphetamine Stimulates release of monoamine from vesicles via displacement & inhibits MAO (most active enantiomer); USE = ADHD; AE = insomnia, decreased appetite
Atomoxetine NET inhibitor; USE = ADHD; AE = drowsiness, sexual dysfunction, suicidal tendencies
Naloxone/Naltrexone Opiate antagonist; USE = opioid overdose (will elicit withdrawal)
Morphine Opiate agonist @ mu receptor; USE = analgesic (not useful anesthetic)
Codeine Opiate agonist; USE = analgesis (weak), cough suppressant
Heroin Gets metabolized to morphine (effects similar to morphine)
Hydromorphone More potent than morphine
Methadone Equipotent to morphine; USE = analgesic, opioid addiction (ease withdrawal without producing 'high')
Meperidine Opiate agonist (older); less potent & shorter duration than morphine
Oxycodone Opiate agonist; USE = analgesic for mild pain (weak like codeine)
Fentanyl Opiate agonist; USE = anesthetic/analgesic (skin patch)
Loperamide USE = anti-diarrheal (does not enter CNS so no analgesia)
Buprenorphine Partial opiate agonist; USE = treatment of opiate addiction (antagonizes heroin/morphine)
Dextromethophan NMDA antagonist; USE = cough suppressant
Clonidine Alpha2 agonist; USE = reduces withdrawal severity in opiate dependence
Cocaine Blocks NET/DAT/SERT; USE = some minor surgeries (ophthalmogic); AE = cardiomegaly, nasal septum damage, inc BP & HR, euphoria, depression
THC CB1/2 receptor agonist; USE = chemotherapy-induced emesis, glaucoma, pain relief; AE = tachycardia, euphoria, relaxation/sedation, dry mouth, hunger, amotivational syndrome; OTHER = 9-COOH is metabolite detected in urine (24hr)
LSD/mescaline Partial agonist 5HT2; AE = dizziness, pupil dilation, burred vision, hallucinations, mood swings, aggressive (contrast to THC)
PCP/Ketamine Non-competitive NMDA antagonist; AE = staggering gait, blank stare, catatonia, hypersalivation, sweating, memory deficitis, aggression
Hallucinogens PCP, LSD, atropine, scopolamine, salvinorum A
Methotrexate USE = antibiotic, DMARD; AE = anorexia, vomiting, bone marrow suppression, lymphomas
Leflunomide Inhibits dyhyrdoorotate DH (lymph prolif); USE = DMARD; AE = allergic rxn's, serious infections, increase in malignancies
Etanercept TNF-alpha antagonist (dimeric protein); USE = DMARD; AE = allergic rxn's, serious infections, increase in malignancies
Infliximab TNF-alpha monoclonal Ab (Fc of human IgG + Fab of rat anti-TNF Ab); USE = DMARD; AE = allergic rxn's, serious infections, increase in malignancies
Abatacept Reduces TNF-alpha; USE = DMARD; AE = allergic rxn's, serious infections, increase in malignancies
Rituximab Anti-CD20 monoclonal Ab; USE = DMARD; AE = allergic rxn's, serious infections, increase in malignancies
Anakinra IL-1 receptor antagonist; USE = DMARD; AE = allergic rxn's, serious infections, increase in malignancies
Aspirin irreversible COX inhibitor; USE = analgesic, anti-inflammatory, antiplatelet, antipyretic, dysmenorrhea; AE = risk of hemorrhage, ulcers, Reye syndrome, respiratory alkalosis (low), metabolic/rep acidosis (high); OTHER = deacetylated to salicylate
Indomethacin Reversible COX inhibitor; USE = anti-inflammatory, analgesic, antipyretic, close PDA; AE = GI bleed, ulcer, renal damage
Ibuprofen Reversible COX inhibitor; USE = antipyretic, analgesic, anti-inflammatory, no antiplatelet; AE = risk of hemorrhage, ulcers, renal damage/failure
Naproxen Reversible COX inhibitor; USE = antipyretic, analgesic, anti-inflammatory; AE = risk of hemorrhage, ulcers, renal damage/failure
Acetaminophen weak COX inhibitor; USE = antipyretic (varicella, flu), analgesic, anti-inflammatory; AE = risk of hemorrhage, ulcers, hepatotoxicity (due to NAPQ1 & loss of GSH), renal tubular necrosis
Celecoxib COX-2 inhibitor; USE = analgesic (dental pain & osteoarthritis); AE = GI upset, interstitial nephritis (impaired renal development), thromboses
Allopurinol Inhibits xanthine oxidase; USE = prevent further gouty attacks; AE = GI upset, hypersensitivity
Colchicine Induces microtubular depolymerization (decreased leukocyte migration); USE = acute gout attack; AE = diarrhea, bone marrow suppression
Probenecid Decreased uric acid reabsorption; USE = prevent further gouty attacks; AE =GI upset
Want to close a PDA? NSAIDs
Chlorpromazine D2, alpha & cholinergic antagonist; USE = 'positive' symptoms of schizophrenia, manic phave of bipolar; AE = orthostasis, hyperprolactinemia, sedation, parkinsonism, dystonias, akathisias, tardive dyskinesia (treat neuro with benztropine)
Haloperidol D2 antagonist; USE = 'positive' symptoms of schizophrenia; AE = orthostasis, hyperprolactinemia, sedation, parkinsonism, dystonias, akathisias, tardive dyskinesia (treat neuro with benztropine)
Clozapine D4>D2 antagonist, block 5HT2A; USE = schizoprenia; AE = agranulocytosis, mild extrapyramidal
Risperidone D2 & 5HT2A antagonist; USE = 'negative' & 'positive' symptoms of schizophrenia, manic phave of bipolar; AE = hyperprolactinemia, extrapyramidal (@ high)
Olanzapine D2=D4 antagonism, block 5HT2A; USE = schizophrenia, manic phase & depression of bipolar; AE = some extrapyramidal & some prolactin excess
Quetiapine Blocks 5HT2A > D2, blocks H1; USE = schizophrenia, manic phave of bipolar; AE = modest elevation in prolactin & extrapyramidal
Ziprasidone Blocks 5HT2A > D2, blocks H1; USE = schizophrenia, manic phave of bipolar; AE = modest elevation in prolactin & extrapyramidal
Aripiprazole Partial agonist D2 & 5HT1A, antagonist at 5HT2A; USE = antipsychotic, manic phave of bipolar; AE = minimal
Created by: lamsonma