FA Neuro & Psych Drugs Flashcards
MoA: dec aqueous humor synthesis
Use: glaucoma
alpha-agonists
alpha-agonist used for glaucoma
ADRs: mydriasis, stinging; C/I in closed-angle
Epinephrine
alpha-agonist used for glaucoma
[ADRs: no pupillary/vision changes]
Brimonidine
MoA: dec aqueous humor secretion
Use: glaucoma
[ADRs: no pupillary/vision changes]
beta-blockers
beta-blocker used for glaucoma
Timolol
beta-blocker used for glaucoma
Betaxolol
beta-blocker used for glaucoma
Carteolol
MoA: dec aqueous humor secretion (dec bicarb)
Use: glaucoma
[ADRs: no pupillary/vision changes]
Acetazolamide
MoA: inc aqueous humor outflow by contracting ciliary muscle & opening trabecular meshwork
ADRs: miosis, cyclospasm
Cholinomimetics
Direct cholinomimetic used in glaucoma
Use: glaucoma emergencies (v. effective)
Pilocarpine
Direct cholinomimetic used in glaucoma
Carbachol
Indirect cholinomimetic used in glaucoma
Physostigmine
Indirect cholinomimetic used in glaucoma
Echothiphate
MoA: PGF_2alpha, inc outflow of aqueous humor
Use: glaucoma
ADRs: darkens iris color (browining)
Latanoprost
MoA: agonist at opioid-R (esp mu) –> open K+ channels & close Ca2+ channels to dec synaptic transmission & inhibit release of ACh, NE, 5-HT, glutamate, & substance P
Use: pain
ADRs: Respiratory depression, pinpoint pupils, additive CNS depression, addiction, constipation (no tolerance to miosis & constipation)
Opioid Analgesics
Opioid-R antagonist
Use: opioid OD
Naloxone
Opioid-R antagonist
Use: opioid OD
Naltrexone
Opioid analgesic
Use: general anesthesia (w/ other CNS depressants); acute pul edema for relief of anxiety (not 1st line)
Morphine
Opioid analgesic
Use: general anesthesia (w/ other CNS depressants)
Fentanyl
Opioid analgesic
Codeine
Opioid analgesic
Heroin
Opioid analgesic
Use: maintenance programs for addicts
Methadone
Opioid analgesic
Meperidine
Opioid analgesic
Use: cough suppression
Dextromethorphan
Opioid analgesic
Use: diarrhea
Dipheoxylate
Opioid analgesic
Use: diarrhea
Loperamide
MoA: partial opioid mu-R agonist, agonist at opioid kappa-R
Use: pain
ADRs: less respiratory depression than nl opioids; withdrawal if on full opioid agonist
Butorphanol
MoA: weak opioid agonist; inhibits 5-HT & NE reuptake
Use: chronic pain
ADRs: like opioid; dec seizure threshold
Tramadol
Carbamazepine
DOC for simple partial seizures
Carbamazepine
DOC for complex partial seizures
Carbamazepine, phenytoin, valproic acid
DOC for tonic-clonic generalized seizures
Ethosuximide
DOC for absence generalized seizures
Prophylaxis: phenytoin
Acute: benzodiazepines (diazepam/lorazepam)
DOC for status epilepticus
Carbamazepine
DOC for trigeminal neuralgia
Phenobarbital
DOC for seizures in pregnant women & children
1st line: MgSO4
2nd line: benzodiazepines (diazepam/lorazepam)
DOC for seizures of eclampsia
MoA: inc Na+ channel inactivation (use-dependent) –> inhibits glutamate release from pre-synaptic neuron
Use: partial & tonic-clonic seizures (1st line for TC), status epilepticus prophylaxis (1st line); also class 1B anti-arrythmic
ADRs: nystagmus, ataxia, diplopia, sedation, drug-induced lupus, teratogenic; chronically –> gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia
PK: fosphenytoin –> parenteral; induces P450
Phenytoin
MoA: inc Na+ channel inactivation
Use: partial & tonic-clonic seizures (1st line for all), trigenminal neuralgia
ADRs: diplopia, ataxia, agranulocytosis or aplastic anemia, liver tox, SIADH, Stevens-Johnson Syndrome, teratogenesis
PK: induces P450
Carbamazepine
MoA: blocks V-gated Na+ channels
Use: partial & tonic-clonic seizures
ADRs: Stevens-Johnson Syndrome
Lamotrigine
MoA: inhibits HVA Ca2+ channels, GABA analog
Use: partial & tonic-clonic seizures, peripheral neuropathy, bipolar disorder
ADRs: sedation, ataxia
Gabapentin
MoA: blocks Na+ channels, inc GABA action
Use: partial & tonic-clonic seizures
ADRs: mental dulling, sedation, kidney stones, weight loss
Topiramate
MoA: inc Na+ channel inactivation, inc GABA concentration
Use: partial, tonic-clonic, absence, & myoclonic seizures (1st line for TC)
ADRs: GI distress, neural tube defects in fetus (C/I in preg), tremor, wt gain, rare but fatal hepatotoxicity
Valproic acid
MoA: blocks thalamic T-type Ca2+ channels
Use: absence seizures (1st line)
ADRs: GI distress, fatigue, headache, urticaria, Stevens-Johnson Syndrome
Ethosuximide
MoA: inhibits GABA reuptake
Use: partial seizures
Tiagabine
MoA: irrev inhibits GABA transaminase –> inc GABA
Use: partial seizures
Vigabatrin
MoA: may modulate GABA/glutamate release
Use: partial & tonic-clonic seizures
Levetiracetam
MoA: inc freq of Cl- channel opening –> facilitate GABA action; dec REM sleep
Use: anxiety, spasticity, detoxification (esp delirium tremens ass’d w/ alcohol), night terrors, sleepwalking, general anesthetic, insomnia
ADRs: sedation, tolerance & dependence, additive CNS depression (w/ EtOH), less respiratory depression/coma risks
Benzodiazepines
MoA: competitive GABA BZD-R antatonist
Use: BZD overdose
Flumazenil
Benzodiazepine
Use: status epilepticus
PK: Long-acting (lower addictive potential)
Diazepam
Benzodiazepine
Use: status epilepticus
PK: Long-acting (lower addictive potential)
Lorazepam
Benzodiazepine
PK: Short-acting (higher addictive potential)
Triazolam
Benzodiazepine
PK: Long-acting (lower addictive potential)
Temazepam
Benzodiazepine
PK: Short-acting (higher addictive potential)
Oxazepam
Benzodiazepine
Use: IV anesthetic for endoscopy (w/ inhaled anesthetics & narcotics
ADRs: severe post-op resp depression, dec BP, amnesia
PK: Short-acting (higher addictive potential)
Midazolam
Benzodiazepine
PK: Long-acting (lower addictive potential)
Chlordiazepoxide
Benzodiazepine
PK: Long-acting (lower addictive potential)
Alprazolam
MoA: inc GABA action by inc duration of Cl channel opeining –> dec neuron firint
Use: (sedative) anxiety, seizures, insomnia
ADRs: sedation, tolerance, dependence, additive CNS depression (w/ alcohol), resp/CV depression
OD Tx: symptom management (respiration, inc BP)
PK: induces P450
Barbituates
Barbituate
Use: partial & tonic-clonic seizures, esp in pregnancy
Phenobarbital
Barbituate
Pentobarbital
Barbituate
Use: induction of anesthesia, short surgical procedures
PK: high potency (high lipid solubility), rapid CNS entry; dec cerebral blood flow; Fx terminated by redistribution into tissue/fat
Thiopental
Barbituate
Secobarbital
MoA: act at BZ1-R subtype; reversible by flumazenil
Use: insomnia
ADRs: ataxia, headaches, confusion; lower dependence risk than BZDs, only modest day-after psychomotor depression, few amnestic Fx (short duration)
Non-BZD hypnotic
Non-BZD hypnotic
Zolpidem
Non-BZD hypnotic
Zaleplon
Non-BZD hypnotic
Eszopiclone
MoA: unknown
Fx: myocardial & respiratory depression, N/V, inc cerebral blood flow
Inhaled anesthetics
Inhaled anesthetic
ADR: hepatotoxicity
Halothane
Inhaled anesthetic
ADR: proconvulsant
Enflurane
Inhaled anesthetic
Isoflurane
Inhaled anesthetic
Sevoflurane
Inhaled anesthetic
ADR: nephrotoxicity
Methoxyflurane
Inhaled anesthetic
ADR: expansion of trapped gas
Nitrous Oxide
MoA: PCP analogs –> block NMDA-R, inc cerebral bloodflow
Use: dissociative anesthetics
ADRs: cardiovascular stimulant, disorientation, hallucination, bad dreams
Arylcyclohexylamines
Arylcyclohexylamine
Ketamine
MoA: potentiates GABA
Use: rapid anesthesia induction, short procedures
ADRs: less post-op nausea than thiopental
Propofol
MoA: bind to intracellular portion of Na+ channels (penetrate = uncharged; bind = charged); use-dependent (prefer activated Na+ channels)
Use: minor surgical procedures, spinal anesthesia
PK: more needed in infected (acidic) tissue; usually given w/ vasoconstrictors (except cocaine)
ADRs: CNS excitation, HTN/hypotension
Local anesthetics
Ester local anesthetic
ADRs: allergy (give amide)
Procaine
Ester local anesthetic
ADRs: allergy (give amide), arrythmias
Cocaine
Ester local anesthetic
ADRs: allergy (give amide)
Tetracaine
Amide local anesthetic
Lidocaine
Amide local anesthetic
Mepivacaine
Amide local anesthetic
ADRs: severe CV tox (arrythmias, hypotension) if given IV
Bupivacaine
MoA: Compete w/ ACh for motor nicotinic receptor
Use: muscle paralysis in surgery or mechanical ventilation
Reverse blockade w/ cholinesterase inhibitors
Nondepolarizing neuromuscular blocking drugs
MoA: depolarizing neuromuscular blocking drug; Phase I = prolonged depolarization (no antidote), Phase II = repolarized but blocked (use cholinesterase-I)
Use: muscle paralysis in surgery or mechanical ventilation (quicker onset than non-depol)
ADRs: hypercalcemia, hyperkalemia
Succinylcholine
Nondepolarizing neuromuscular blocker
Tubocurarine
Nondepolarizing neuromuscular blocker
Atracurium
Nondepolarizing neuromuscular blocker
Mivacurium
Nondepolarizing neuromuscular blocker
Pancuronium
Nondepolarizing neuromuscular blocker
Vecuronium
Nondepolarizing neuromuscular blocker
Rocuronium
MoA: prevent Ca2+ release from skeletal muscle sarcoplasmic reticulum
Use: malignant hyperthermia (from inhalation anesthetics + succinylcholine), neuroleptic malignant syndrome (from antipsychotics)
Dantrolene
MoA: agonize Dopamine receptors
Use: Parkinson’s disease
Dopamine agonists
Ergot Dopamine agonist
Bromocriptine
Non-ergot (preferred) Dopamine agonist
Pramipezole
Non-ergot (preferred) Dopamine agonist
Ropinirole
MoA: may inc dopamine release
Use: Parkinson’s Disease, influenza A, rubella
ADRs: ataxia
Amantadine
MoA: inc dopamine in brain (L-dopa crosses BBB & is converted to dopamine)
Use: Parkinsonism
ADRs: N/V w/o constipation, arrhythmias (due to peripheral conversion); long-term: dyskinesia w/ admin, akinesia b/w doses; dec ADRs w/ carbidopa
L-dopa/carbidopa
MoA: selective MAO-B inhibitor –> inc dopamine availability
Use: Parkinson’s disease (adjunctive Tx), depression, anxiety, hypochondriasis
ADRs: may enhance L-dopa ADRs; hypertensive crisis (w/ tyramine or beta-agonists), CNS stimulation, C/I w/ SSRIs/meperidine
Selegiline
MoA: prevent L-dopa degradation –> inc dopamine
Use: Parkinson’s disease
COMT inhibitors
MoA: anti-muscarinic
Use: Parkinson’s disease (for tremor & rigidity, no Fx on bradykinesia)
Avoid if: Hx of GI/GU obstruction –> can exacerbate Sx
Benztropine
MoA: NMDA-R antagonist –> prevents excitotoxicity
Use: Alzheimer’s Disease
ADRs: dizziness, confusion, hallucinations
Memantine
MoA: indirect cholinomimetic
Use: Alzheimer’s disease
ADRs: Nausea, dizziness, insomnia
Acetylcholinesterase Inhibitors
Acetylcholinesterase Inhibitor used in Alzheimer’s
Donepezil
Acetylcholinesterase Inhibitor used in Alzheimer’s
Galantamine
Acetylcholinesterase Inhibitor used in Alzheimer’s
Rivastigmine
MoA: amine-depleting
Use: Huntington’s Disease (HD shows inc dopamine)
Reserpine
MoA: amine-depleting
Use: Huntington’s Disease (HD shows inc dopamine)
Tetrabenazine
MoA: dopamine-R antagonist
Use: Huntington’s Disease (HD shows inc dopamine)
Haloperidol
MoA: 5-HT_1B/1D agonist –> vasoconstiction, inhibition of trigeminal activation, & vasoactive peptide release
Use: acute migraine, cluster headache attacks
ADRs: coronary vasospasm, mild tingling; C/I in CAD or Pinzmetals’ angina
Sumatriptan
benzodiazepines
Treatment for alcohol withdrawal
SSRIs
Treatment for bulimia
Acute: benzodiazepines
Chronic: buspirone, SSRIs
Treatment for anxiety
Methylphenidate
Amphetamines
Treatment for ADHD
MAO-Is/SSRIs
Treatment for Atypical depression
“Mood Stabilizers” –> lithium, valproic acid, carbamazepine
Atypical antipsychotics
Treatment for Bipolar Disorder
SSRIs, SNRIs
TCAs (less)
Treatment for Depression
Mirtazapine
Treatment for Depression w/ insomnia
SSRIs
Clomipramine
Treatment for OCD
SSRIs, TCAs, BZDs
Treatment for Panic Disorder
SSRIs
Treatment for PTSD
Antipsychotics (atypicals 1st))
Treatment for Schizophrenia
Antipsychotics (haloperidol, risperidone)
Treatment for Tourette’s Syndrome
SSRIs
Treatment for Social Phobias
MoA: inc catecholamines at synaptic cleft (esp NE & dopamine)
Use: ADHD, narcolepsy, appetite control)
CNS stimulants
CNS stimulant
Methylphenidate
CNS stimulant
Dextroamphetamine
CNS stimulant
Mixed amphetamine salts
MoA: block dopamine D2-R (inc cAMP)
Use: Schizophrenia (pos Sx), psychosis, acute mania, Tourette’s Syndrome
ADRs: Extrapyramidal sys side Fx, Neuroleptic malignant Syndrome, Tardive Dyskinesia, endocrine side Fx (e.g. hyperprolactinemia), dry mouth/constipation (anti-muscarinic), hypotension (anti-alpha), & sedation (anti-histamine)
Anti-psychotics
Neuroleptic malignant syndrome –> rhabdomyolysis -> rigidity & myoglobinuria; autonomic instability, hyperpyrexia
Tx: dantroline, D2 agonists
Pt presents w/ fever, encephalopathy, unstable vitals, elevated enzymes, & muscle rigidity (as ADR)
High-potency anti-psychotic
ADRs: more neurological –> extrapyramidal Sx, tardive dyskinesia
Haloperidol
High-potency anti-psychotic
ADRs: more neurological –> extrapyramidal Sx, tardive dyskinesia
Trifluoperazine
High-potency anti-psychotic
ADRs: more neurological –> extrapyramidal Sx, tardive dyskinesia
Fluphenazine
Low-potency anti-psychotic
ADRs: more non-neurological –> anticholinergic, antihistamine, & alpha-blockade; retinal deposits
Thioridazine
Low-potency anti-psychotic
ADRs: more non-neurological –> anticholinergic, antihistamine, & alpha-blockade; corneal deposits
Chlorpromazine
MoA: Fx on 5-HT, dopamine, alpha, & H1 receptors
Use: schizophrenia (pos & neg Sx)
ADRs: fewer EPs & anti-cholinergic side Fx
Atypical Antipsychotics
Atypical Antipsychotic
Use: OCD, anxiety disorder, depression, mania, Tourette’s Syndrome
ADRs: weight gain
Olanzapine
Atypical Antipsychotic
ADRs: weight gain, seizures, agranulocytosis
Clozapine
Atypical Antipsychotic
Quetiapine
Atypical Antipsychotic
ADR: hyperprolactinemia (DA-antag)
Risperidone
Atypical Antipsychotic
Aripiprazole
Atypical Antipsychotic
ADR: QT prolongation
Ziprasidone
MoA: unclear, possibly phosphoinositol cascade inhibition
Use: bipolar disorder (mood stabilizer –> blocks relapse & acute manic events); SIADH (ADH antag)
ADRs: MNOP –> Movement (tremor), Nephrogenic diabetes insipidus, hypOthyroidism, Pregnancy problems (cardiac defects –> Ebstein anomaly & malformation of great vessels); also sedation, edema, heart block,
Lithium
MoA: stimulates 5-HT receptors
Use: generalized anxiety disorder
[ADRs: no sedation, addiction, tolerance, or additive CNS depression w/ EtOH]
Buspirone
MoA: block NE & serotonin reuptake
Use: major depression, fibromyalgia
ADRs: sedation, alpha-blockade, atropine-like (tachycardia, urinary retention, C/I in glaucoma)
OD: 3C: Convulsions, Coma, Cardiotoxicity; also resp depression, hyperpyrexia; elderly –> confusion & halucinations
OD Tx: NaHCO3 for cardiotox
Tricyclic antidepressants
Tricyclic antidepressant
ADR: tertiary –> more anticholinergic Fx
Amitriptyline
Tricyclic antidepressant
ADR: secondary –> fewer anticholinergic Fx (better in elderly)
Nortriptyline
Tricyclic antidepressant
Use: bedwetting
Imipramine
Tricyclic antidepressant
ADRs: lower seizure threshold, least sedating
Desipramine
Tricyclic antidepressant
Use: OCD
Clomipramine
Tricyclic antidepressant
Doxepin
Tricyclic antidepressant
Amoxapine
MoA: serotonin-specific reuptake inhibitors
Use: depression, OCD good for suicidal pts
SSRIs
Serotonin syndrome: due to interaction of 2 drugs that increase serotonin, e.g. SSRIs, MAO-I, meperidine (MC –> SSRI + MAO-I)
Tx: cyproheptadine (5-HT-R antagonist)
Depressed pt presenting w/ hyperthermia, myoclonus, hypotension, flushing, diarrhea, seizures
SSRI
Fluoxetine
SSRI
Paroxetine
SSRI
Sertraline
SSRI
Citalopram
MoA: inhibit serotonin & NE reuptake
Use: depression
ADRs: MC inc BP; stimulant Fx, sedation, nausea
SNRIs
SNRI
Use: generalized anxiety disorder
Venlafaxine
SNRI (greater NE effect)
Use: diabetic peripheral neuropathy
Duloxetine
MoA: nonselective MAO inhibition, inc amine neurotransmitter levels (NE, serotonin, dopamine)
Use: atypical depression, anxiety, hypochondriasis
ADRs: Hypertensive crisis (w/ tyramine or beta-agonists), CNS stimulation; C/I w/ SSRIs or meperidine
MAO-I
MAO-I
Tranylcypromine
MAO-I
Phenelzine
MAO-I
Isocarboxazid
MAO-I
Use: also alkylating agent used in cancer chemoTx)
Procarbazine
MoA: inc NE & dopamine (unknown mech)
Use: atypical antidepressant; smoking cessation
ADRs: stimulant Fx (tachycardia, insomnia), headache, seizures in bulimic pts [no sexual side Fx]
Bupropion
MoA: alpha2-antag –> inc NE & 5-HT release; potent 5-HT2 & 5-HT3 antag
Use: atypical antidepressant
ADRs: sedation, inc appetite, weight gain, dry mouth
Mitazapine
MoA: blocks NE reuptake
Use: atypical antidepressant
ADRs: sedation, orthostatic hypotension
Maprotiline
MoA: inhibits serotonin reuptake
Use: insomnia (antidepressent Fx = v. high dose)
ADRs: sedation, nausea, priapism, postural hypotension
Trazodone
MoA: 5-HT2-R antagonist)
Use: Serotonin Syndrome
Cyproheptadine
modafinil (CNS stimulant thought to inc DA signalling; effective, well tolerated, low abuse potential)
DOC for narcolepsy
propranolol (beta-blockers)
DOC for essential tremor
