Red-line Drugs 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
Quetiapine
Atypical antipsychotics
D2/5HT2A antagonist (low ratio)
Schizophrenia: (- symp)
SE: weight gain, prolonged QT, some sedation
Paroxetine
SSRI Block SERT
SE: sedation, constipation, weight gain, dry mouth, serotonin syndrome, SIADH, sexual dysfunction, withdrawal symptoms
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
Trazodone
Mixed serotonin receptor and alpha 1 receptor blocker
Insomnia, High doses for depression
SE: sedation, nausea, priapism (trazo*bone*), postural hypotension
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
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),
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), status epileticus
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, status epilepticus
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
Phenobarbital
Barbiturates increase *duration* of GABA CL- channel opening
Anxiety, seizures, insomnia, anesthesia (thiopental)
Seizures: partial and generalized tonic-clonic
SE: Respiratory and CV depression! Sedation!
CNS depression (worse w/ EtOH), dependence, DDI (P-450 inducer)
Ramelteon
Melatonin Receptor Agonist
Buspirone
5HT1A partial agonist (D2 antagonist)
Anxiety
Cocaine
DAT (+SERT, NET) Stimulant
Amphetamines
DAT (+SERT, NET) stimulant
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
Opioid analgesics
Morphine heroin fentanyl meperidine
Heroin
Mu-opioid receptor (Gi/o) agonist treat w/ naloxone
Cannabinoids
CB-1 receptor (Gi/o) agonist
Hallucinogens
Lysergic acid diethyl amide (LSD) Mescaline (peyote)
Methadone
Treat opioid dependence binds Mu receptor agonist and NMDA antagonist
Buprenorphine
partial mu agonist (avoid respiratory depression) Treat opioid addiction
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
Halothane
Volatile anesthetics mod to high potency; poor analgesic
Three issues: -Respiratory and CV failure -Hepatotoxicity (metabolized in liver) -Malignant Hyperthermia
IV anesthetics
Propofol Etomidate Thiopental
IV adjuncts for GA
Diazepam Ondansteron (anti-emetic) Fentanyl (analgesic) Glycopyrrolate (Anticholinergic) Ketamine (NMDA antagonist) Morphine Neuromuscular blocking agents Dantrolene (Ca2+ channel blocker)
Dantrolene
prevents release of Ca2+ from sarcoplasmic reticulum of skeletal muscle
Malignant hyperthermia and neuroleptic malignant syndrome
Ethosuximide
Blocks thalamic T-type Ca2+ channels
Absence seizures
SE: EFGHIJ
Ethosuximide causes
Fatigue
GI distress
Headache
Itching
steven-Johnson syndrome
Diazepam
Benzodiazepime
Increased GABA-A action–increased frequency of Cl- channel opening
Status Epliepticus
SE:Sedation, tolerance dependence, respiratory depression
Lorazepam
Benzodiazepime
Increased GABA-A action–increased frequency of Cl- channel opening
Status Epliepticus
SE:Sedation, tolerance dependence, respiratory depression
Midazolam
Benzodiazepime
Increased GABA-A action–increased frequency of Cl- channel opening
Status Epliepticus
SE:Sedation, tolerance dependence, respiratory depression
Phenytoin
increase Na+ channel inactivation
zero order kinetics, Induction of P450
Not as popular anymore but used for Partial seizures and generalized tonic-clonic seizures
Prophylaxis for status epilepticus
SE: Nystagmus, diplopia, ataxia, sedation (high dose), rash, gingival hyperplasia, hirsutism, megaloblastic anemia, peripheral neuropathy
Carbamazepine
Increase Na+ channel inactivation
First line for Partial and Tonic clonic (also trigeminal neuralgia)
SE: diplopia, ataxia, blood dyscrasias (agranuloctosis and aplastic anemia), teratogenesis
Induction of P450
SIADH, Steven-Johnson syndrome
Valproic Acid
Inhibits GABA transminase (increasing [GABA]) (Increases Na+ channel inactivation)
Use: first line in Generalized Tonic-Clonic
also for absance and partial
SE: GI destress, possible hepatotoxicity, neural tube defects, tremor, weight gain, bad for pregnancy
DDI: alcohol/CNS depressants, anticonvulsants, aspirin/warfarin
Phenobarbital
Increase GABA-A action
CYP450 inducer (many DDI)
Partial seizures and generalized tonic-clonic
- excessive sedation limits use*
- S*E:sedation, tolerance, dependence, cardiorespiratory depression
Levetiracetam
unknown MOA
First line for Tonic-clonic
SE: somnolence, dizziness, fatigue
NO P450 effect
Lamotrigine
Blocks VSSC
partial, generalized and absance
SE: dizziness, ataxia, diplopia, sedation, rashes, nausea
(less than phenytoin)
Divalproex
Inhibits GABA transminase (increasing [GABA]) (Increases Na+ channel inactivation)
Use: first line in Generalized Tonic-Clonic
also for absance and partial
SE: GI destress, possible hepatotoxicity, neural tube defects, tremor, weight gain, bad for pregnancy
DDI: alcohol/CNS depressants, anticonvulsants, aspirin/warfarin
