Pharm Neuro IV Flashcards
Chlorpromazine
Typical antipsychotic D2 antagonist low potency Schizophrenia (+ symp.) psychosis, acute mania, Tourette syndrome Side effects: ANS (dry mouth), sedation, hypotension
Haloperidol
Typical antipsychotics D2 antagonist High potency Schizophrenia (+ symp.), Huntington’s Side effects: EPS tardive dyskinesia Neuroleptic malignant syndrome
Clozapine
Atypical antipsychotics D2/5HT2A antagonist (low ratio) Schizophrenia (- symp) SE: weight gain, *agranulocytosis*, seizures, prolonged QT
Olanzapine
Atypical antipsychotics D2/5HT2A antagonist (low ratio) Schizophrenia (- symp) SE: weight gain, prolonged QT
Quetiapine
Atypical antipsychotics D2/5HT2A antagonist (low ratio) Schizophrenia: (- symp) SE: weight gain, prolonged QT, some sedation
Risperidone
Atypical antipsychotics D2/5HT2A antagonist (low ratio) Schizophrenia (- symp) SE: increased prolactin (lactation and gynecomastia) irregular menstruation and fertility issues, DM type II, prolonged QT
Aripiprazole
Atypical antipsychotics D2 and 5HT1A Partial agonist, 5HT2A antagonist high potency Schizophrenia (- symp) SE: weight gain, headache, anxiety, insomnia, nausea, constipation, lightheadedness
Ziprasidone
Atypical antipsychotics D2/5HT2A antagonist (low ratio)
Paroxetine
SSRI Block SERT SE: sedation, constipation, weight gain, dry mouth, serotonin syndrome, SIADH, sexual dysfunction, withdrawal symptoms (
Sertraline
SSRI Block SERT SE: *GI distress*, activation insomnia, constipation, dry mouth, weight gain, serotonin syndrome, SIADH, sexual dysfunction, withdraw symptoms (
Citalopram
SSRI Block SERT SE: fewest of the SSRIs
Escitralopram
SSRI Block SERT SE: fewest of the SSRIs
Bupropion
NE DA reuptake inhibitor (NDRI) Depression (Wellbutrin), smoking cessation (Zyban) SE: insomnia/agitation, stimulant effects, headache, *seizures at high dose* no sedation, no addiction, no tolerance and no sexual SE no interaction with EtOH
Venlafaxine
SNRI SERT and NET blocker Depression, anxeity, panic, PTSD SE: Hypertension, anxeity, nausea, withdrawal symptoms, sexual dys., sedation
Duloxetine
SNRI SERT and NET blocker Depression, Diabetic peripheral neuropathy SE: Hypertension, anxeity, nausea, withdrawal symptoms, sexual dys., sedation
Trazodone
Mixed serotonin receptor and alpha 1 receptor blocker Insomnia, High doses for depression SE: sedation, nausea, priapism (trazo*bone*), postural hypotension
Mirtazapine
Alpha-2 adrenergic antagonist increase release of NE and 5HT 5HT2 and 3 receptor antagonist depression, insomnia SE: sedation, increase appetite, weight gain, dry mouth
Amitriptyline
TCADs NET/SERT reuptake block Major depression, peripheral neuropathy, chronic pain, migraine prophylaxis SE: Sedation, antimuscarinic (Amitriptyline >Desipramine), orthostatic hypotension, Convulsions, Coma, Cardiotoxicity (arrhythmias), respiratory depression
Nortriptyline
TCADs NET/SERT reuptake block Major depression, peripheral neuropathy, chronic pain, migraine prophylaxis SE: Sedation, antimuscarinic, orthostatic hypotension, Convulsions, Coma, Cardiotoxicity (arrhythmias), respiratory depression
Imipramine
TCADs NET/SERT reuptake block Major depression, enuresis SE: Sedation, antimuscarinic, orthostatic hypotension, Convulsions, Coma, Cardiotoxicity (arrhythmias), respiratory depression
Desipramine
TCADs NET reuptake block Major depression, peripheral neuropathy, chronic pain, migraine prophylaxis SE: Sedation, antimuscarinic (Amitriptyline >Desipramine), orthostatic hypotension, Convulsions, Coma, Cardiotoxicity (arrhythmias), respiratory depression
Clomipramine
TCADs (NET)/SERT reuptake block Major depression, OCD, peripheral neuropathy, chronic pain, migraine prophylaxis SE: *Sedation*, antimuscarinic , orthostatic hypotension, Convulsions, Coma, Cardiotoxicity (arrhythmias), respiratory depression
Phenelzine
MAOI Atypical depression, anxeity SE: Hypertensive crisis (tyramine), CNS stimulation, Serotonin syndrome
Fluoxetine
SSRI Block SERT SE: Hypertension, anxeity, nausea, withdrawal symptoms (lower risk with fluox), sexual dys., sedation
Selegiline
MAOI Parkinson’s SE: Hypertensive crisis (tyramine), CNS stimulation, Serotonin syndrome
Lithium
mechanism unknown (inhibition of phosphoinositol cascade) Mood stabilizer for bipolar blocks relapse and acute manic events SE: narrow therapeutic index (monitoring) LMNOP Movement (tremor) Nephrogenic Diabetes Insipitus O-hypOthyroid Pregnancy problems (Ebstein anomaly) polyuria (diabetes insipitus),
Carbamazepine
Antimanic agent
Alprazolam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening short acting, high potency acute management of anxiety. (situational anxiety) ,SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Flurazepam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening Anxiety, spasticity, detox, night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxant), insomnia SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Diazepam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening longer half life acute management of anxiety. (situational anxiety) SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Oxazepam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening; short acting anxiety, insomnia, withdraw from EtOH SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Triazolam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening; short acting Insomnia SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Lorazepam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening short half life, high potency acute management of anxiety. (situational anxiety) good for elderly SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Midazolam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening; short acting anesthesia (adjunct), anxiety, insomnia SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Temazepam
Benzodiazepine agonist intensify GABA effects (binding alpha 1 and 2-5) Increase freq. of Cl- channel opening insomnia, anxiolytic, anticonvulsant, muscle relaxant SE: Dependence, additive depressant effects w/ EtOH, anterograde amnesia, abuse
Flumazenil
Benzodiazepine receptor ANTagonist used for OD of Benzo
Zolpidem
Non-BDZ Activate BZ1 subtype of GABA receptor Insomnia SE: Ataxia, headache, confusion less dependence risk, less amnesia
Eszopiclone
Non-BDZ Activate BZ1 subtype of GABA receptor Insomnia SE: Ataxia, headache, confusion less dependence risk, less amnesia
Zaleplon
Non-BDZ Activate BZ1 subtype of GABA receptor (GABA Cl- channel) Insomnia SE: Ataxia, headache, confusion less dependence risk, less amnesia
Pentobarbital
Barbiturates increase *duration* of GABA CL- channel opening Anxiety, seizures, insomnia, anesthesia (thiopental) SE: Respiratory and CV depression! CNS depression (worse w/ EtOH), dependence, DDI (P-450 inducer)
Phenobarbital
Barbiturates increase *duration* of GABA CL- channel opening Anxiety, seizures, insomnia, anesthesia (thiopental) SE: Respiratory and CV depression! CNS depression (worse w/ EtOH), dependence, DDI (P-450 inducer)
Ramelteon
Melatonin Receptor Agonist
Buspirone
5HT1A partial agonist (D2 antagonist) Anxiety
Chloral hydrate
Enhance GABA receptor sedative-hyponitic class Short term insomnia treatment
Cocaine
DAT (+SERT, NET) Stimulant
Amphetamines
DAT (+SERT, NET) stimulant
MDMA
ecstasy SERT>DAT, NET stimulants
Nicotine
nicotinic receptor Stimulants
Stimulants
Nicotine Cocaine Meth MDMA (ecstasy)
Depressants
Alcohol Barbiturates Benzodiazepines
Barbiturates
increase GABA-A, decrease NMDA
Benzos
Increase GABA-A only antagonist: flumazenil
Dissociative Anesthetics
Phencyclidine (PCP) Ketamine
Phencyclidine
NMDA receptor antagonist
Ketamine
NMDA receptor antagonist
Opioid analgesics
Morphine heroin fentanyl meperidine
Morphine
Mu-opioid receptor (Gi/o) agonist treat w/ naloxone
Heroin
Mu-opioid receptor (Gi/o) agonist treat w/ naloxone
Fentanyl
Mu-opioid receptor (Gi/o) agonist treat w/ naloxone
Meperidine
Mu-opioid receptor (Gi/o) agonist treat w/ naloxone
Cannabinoids
CB-1 receptor (Gi/o) agonist
Hallucinogens
Lysergic acid diethyl amide (LSD) Mescaline (peyote)
LSD
5HT-2A receptor (Gq) partial agonist
Methadone
Treat opioid dependence binds Mu receptor agonist and NMDA antagonist
Buprenorphine
partial mu agonist (avoid respiratory depression) Treat opioid addiction
Nicotine
Help stop smoking Nicotinic receptors
Varenicline
treat nicotine addiction agonist of nicotinic receptors
Clonidine
Alpha 2 agonist treat withdrawal from EtOH, Opioids, smoking
Disulfiram
Antabuse blocks enzyme acetaldehyde dehydrogenase treat alcoholism SE: metallic taste, headache, drowsiness, optic neuritis, peripheral neuropathy, hepatitis Contraindications: Risk MI, CVA, pregnant or if cognitively
Naltrexone
antagonists at μ-opioid receptor, the κ-opioid receptor (KOR) to a lesser extent reverses effects of opioids and EtOH SE: Nausea, Headaches, anxiety, sedation If on opiates or heroin will go into withdrawal
d-Amphetamine
Adderall Inhibits or reverses the transporter proteins for the monoamine Increases releases of monoamines Inhibits breakdown of monoamines
Methylphenidate
Ritalin Blocks the dopamine transporter and norepinephrine transporter more remains in synaptic cleft
-ipramine
TCA
-etine
SSRI
-triptyline
TCA
-zepam
Benzo
-zolam
Benzo
-barbital
Barbiturate
-azine
Typical antipsychotics
Nitrous Oxide
Gaseous anesthetics low potency, good analgesic paired with barbiturates or opioids rapid onset and recovery Problems: Concentration effect (faster uptake) Diffusion hypoxia (not enough O2) Second gas effect (more of paired GA)
Volatile anesthetics
Desflurane Enflurane Halothane Isoflurane Sevoflurane
Desflurane
Volatile anesthetics induce and maintain surgical anesthesia low blood and fatty tissue solubility (fast onset and recovery) Con: smells bad Do NOT use with pts w/ Family history of malignant hyperthermia
Enflurane
Volatile anesthetics Maintenance of GA in adults Good analgesic and muscle relaxant fast induction and recovery Con: can trigger seizures
Halothane
Volatile anesthetics mod to high potency; poor analgesic Three issues: -Respiratory and CV failure -Hepatotoxicity (metabolized in liver) -Malignant Hyperthermia
Isoflurane
Volatile anesthetics most widely used Pros: more potent, less hepatotoxicity, less risk of seizure, good muscle relaxant Con: bad odor can lead to coughing
Sevoflurane
Volatile anesthetics pleasant odor used for induction Con: releases fluoride ions–>renal toxicity
IV anesthetics
Propofol Etomidate Thiopental
Propofol
IV anesthetic Potentiates GABA-A receptor activity rapid onset, faster recovery than thiopental less nausea post-op
Etomidate
IV anesthetic non-barbiturate hypnotic potentiates GABA-A no analgesia minimal depression of CV and respiratory function (larger safety margin) Con: can cause involuntary movements, lots of nausea and vomiting and pain on injection.
Thiopental
Barbiturate (short acting) Potentiates GABA-A IV anesthetic Induction and short surgical procedures High potency, high lipid solubility, rapid entry into brain
IV adjuncts for GA
Diazepam Ondansteron (anti-emetic) Fentanyl (analgesic) Glycopyrrolate (Anticholinergic) Ketamine (NMDA antagonist) Morphine Neuromuscular blocking agents Dantrolene (Ca2+ channel blocker)
Diazepam
Valium Benzo–potentiates GABA-A used pre-op for induction and *sedative* purposes
Ondansteron
5-HT3 receptor antagonist Anti-emetic reduces post-op nausea and vomiting
Fentanyl
Mu receptor agonist Analgesics
Glycopyrrolate
Anticholinergic drug reduce GA-induced hypotension, bradycardia, and excess salivations (prevent choking)
Ketamine
NMDA receptor antagonist IV anesthetic–produces dissociative anesthesia (catatonia, amnesia, analgesia)
Morphine
Mu receptor agonist Analgesics
Neuromuscular blocking agents
Vecuronium Relax skeletal muscle (esp for abdominal surgeries)
Dantrolene
prevents release of Ca2+ from sarcoplasmic reticulum of skeletal muscle Malignant hyperthermia and neuroleptic malignant syndrome
Phenytonin
Grand mal