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59 Cards in this Set
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Bromocriptine
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MECH: agonize dopamine receptors
USE: Parkinson's Disease, hyperprolactinemia TOX: nausea, somnolence, hallucinations, orthostatic hypotension |
PD
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Pramipexole
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MECH: agonize dopamine receptors
USE: Parkinson's Disease TOX: nausea, somnolence, hallucinations, orthostatic hypotension |
PD
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Ropinirole
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MECH: agonize dopamine receptors
USE: Parkinson's Disease TOX: nausea, somnolence, hallucinations, orthostatic hypotension |
PD
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Amantadine
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MECH: increase dopamine release
USE: Parkinson's Disease |
PD
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L-dopa (levodopa)
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MECH: crosses BBB, converted by dopa decarboxylase → ↑dopamine levels
USE: Parkinsonism TOX: arrhythmias, long term use → dyskinesia following admin and akinesa btw doses |
PD
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Carbidopa
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MECH: peripheral decarboxylase inhibitor → ↑ L-dopa bioavialability and ↓ side effects
USE: Parkinsonism in conjunction with L-dopa |
PD
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Selegiline
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MECH: selectively inhibits MAO type B → ↑ dopamine availability
USE: adjunctive agent to L-dopa to treat PD TOX: may enhance adverse effects of L-dopa |
PD
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Entacapone
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MECH: selectively inhibits COMT (catechol-O-methyl transferase) → ↑ dopamine availability
USE: adjunctive agent to L-dopa to treat PD TOX: may enhance adverse effects of L-dopa |
PD
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Tolcapone
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MECH: selectively inhibits COMT → ↑ dopamine availability
USE: adjunctive agent to L-dopa to treat PD TOX: may enhance adverse effects of L-dopa |
PD
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Benzotropine
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MECH: antimuscarinic
USE: improves tremor and rigidity of PD TOX: antimuscarinic side effects (impaired cognition, dry mouth, urinary retention) |
PD
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Sumatriptan
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MECH: 5HT-1D agonist → vasoconstriction
USE: acute migraine, cluster headache attacks TOX: coronary vasospasm, mild tingling (contraindicated with CAD or Prinzmetal's) |
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Phenytoin
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MECH: ↑ Na+ channel inactivation (use-dependent) → ↓ glutamate release from excitatory presynaptic neurons
USE: tonic-clonic seizures; antiarrhythmic TOX: nystagmus, ataxia, diplopia, sedation, SLE-like syndrome, ↑cytochrome P450 chronic use → gingival hyperplasia in children, peripheral neuropathy, hirsutism, ↓ folate absorption → megaloblastic anemia, malignant hyperthermia teratogenic |
Epilepsy
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Carbamazepine
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MECH: ↑ Na+ channel inactivation (use-dependent) → ↓ glutamate release from excitatory presynaptic neurons
USE: tonic-clonic seizures; trigeminal neuralgia; acute mania and mania/depression prophylaxis TOX: ataxia, diplopia, hepatotox, blood dyscrasias, ↑cytochrome P450; teratogenic |
Epilepsy, Mood stabilizer
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Valproic Acid
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MECH: ↑ Na+ channel inactivation; ↑ GABA concentration
USE: Absence seizures, myoclonic seizures; acute mania TOX: GI, hepatotox (measure LFTs), neural tube defects in fetus, tremor, weight gain |
Anticonvulsant, Mood stabilizer
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Lamotrigine
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MECH: blocks voltage-gated Na+ channels
USE: anti-epileptic; acute mania and mania/depression prophylaxis TOX: Stevens-Johnson syndrome |
Anticonvulsant, mood stabilizer
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Gabapentin
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MECH: ↑ GABA release
USE: anti-epileptic, peripheral neuropathy TOX: sedation, ataxia |
Epilepsy
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Topiramate
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MECH: blocks Na+ channels; ↑ GABA actions
USE: anti-epileptic TOX: sedation, mental dulling, kidney stones, weight loss |
Epilepsy
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Phenobarbital
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Barbiturate
MECH: facilitate GABA-A action by ↑ Cl- channel open duration → ↓ neuron firing USE: sedative (anxiety), seizures, insomnia TOX: dependence, additive CNS depression effects with alcohol, resp/CV depression, ↑ cytochrome P450 → interactions; treat overdose with symptom management (assist resp, ↑ BP) |
Epilepsy
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Pentobarbital
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Barbiturate
MECH: facilitate GABA-A action by ↑ Cl- channel open duration → ↓ neuron firing USE: sedative (anxiety), seizures, insomnia TOX: dependence, additive CNS depression effects with alcohol, resp/CV depression, ↑ cytochrome P450 → interactions; treat overdose with symptom management (assist resp, ↑ BP) |
Epilepsy
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Thiopental
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Barbiturate
MECH: facilitate GABA-A action by ↑ Cl- channel open duration → ↓ neuron firing USE: sedative (anxiety), seizures, insomnia, *anesthesia induction TOX: dependence, additive CNS depression effects with alcohol, resp/CV depression, ↑ cytochrome P450 → interactions; treat overdose with symptom management (assist resp, ↑ BP) |
Epilepsy
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Secobarbital
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Barbiturate
MECH: facilitate GABA-A action by ↑ Cl- channel open duration → ↓ neuron firing USE: sedative (anxiety), seizures, insomnia TOX: dependence, additive CNS depression effects with alcohol, resp/CV depression, ↑ cytochrome P450 → interactions; treat overdose with symptom management (assist resp, ↑ BP) |
Epilepsy
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Ethosuximide
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MECH: Blocks thalamic T-type Ca++ channels
USE: absence seizures TOX: GI, lethargy, HA, urticaria, Stevens-Johnson |
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Benzodiazepines (diazepam, lorazepam, temazepam, chlordiazepoxide, alprazolam)
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MECH: facilitate GABA-A action by ↑ freq of Cl- channel opening
USE: anxiety, spasticity, *status epilepticus, detox (alcohol withdrawal), night terrors, sleepwalking TOX: sedation, tolerance, dependence, additive with alcohol; treat overdose with flumazenil (GABA antagonist) |
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Benzodiazepines (triazolam, oxazepam, midazolam)
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Short acting
MECH: facilitate GABA-A action by ↑ freq of Cl- channel opening USE: anxiety, spasticity, detox (alcohol withdrawal), night terrors, sleepwalking, (midazolam for endoscopy anesthesia) TOX: sedation, tolerance, dependence, additive with alcohol |
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Lithium
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MECH: inhibits phosphoinositol cascade (not established)
USE: mood stabilizer (prophylaxis and treatment of acute mania and depression) TOX: tremor, hypothyroidism*(check thyroid regularly), polyuria (ADH antagonist → nephrogenic DI), teratogenic; narrow therapeutic window (monitor serum levels) |
Mood stabilizer
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Buspirone (BuSpar)
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MECH: stimulates 5HT-1A receptors
USE: anxiolysis for generalized anxiety disorder TOX: unlike benzo - does not cause sedation, addiction, alcohol interactions |
Anti-anxiety
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Thioridazine
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Neuroleptic
MECH: block D2 receptors (dopamine) USE: schizophrenia, psychosis, acute mania, Tourette syndrome TOX: Extrapyramidal - dystonia (extended spasm), akinesia, akathisia (restlessness), *Tardive dyskinesia (stereotypic oral/facial movements, often irreversible) Hypothalimic/Endocrine - hyperprolactinemia Muscarinic antagonism - dry mouth, constipation Alpha antagonism - hypotension Histamine antagonism - sedation *Neuroleptic Malignant Syndrome - rigidity, myoglobinuria, autonomic instability, hyperpyrexia; treat with dantrolene and dopamine agonists |
Antipsychotic
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Haloperidol
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Neuroleptic
MECH: block D2 receptors (dopamine) USE: schizophrenia, psychosis, acute mania, Tourette syndrome TOX: Extrapyramidal - dystonia (extended spasm), akinesia, akathisia (restlessness), *Tardive dyskinesia (stereotypic oral/facial movements, often irreversible) Hypothalimic/Endocrine - hyperprolactinemia Muscarinic antagonism - dry mouth, constipation Alpha antagonism - hypotension Histamine antagonism - sedation *Neuroleptic Malignant Syndrome - rigidity, myoglobinuria, autonomic instability, hyperpyrexia; treat with dantrolene and dopamine agonists |
Antipsychotic
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Fluphenazine
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Neuroleptic
MECH: block D2 receptors (dopamine) USE: schizophrenia, psychosis, acute mania, Tourette syndrome TOX: Extrapyramidal - dystonia (extended spasm), akinesia, akathisia (restlessness), *Tardive dyskinesia (stereotypic oral/facial movements, often irreversible) Hypothalimic/Endocrine - hyperprolactinemia Muscarinic antagonism - dry mouth, constipation Alpha antagonism - hypotension Histamine antagonism - sedation *Neuroleptic Malignant Syndrome - rigidity, myoglobinuria, autonomic instability, hyperpyrexia; treat with dantrolene and dopamine agonists |
Antipsychotic
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Chlorpromazine
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Neuroleptic
MECH: block D2 receptors (dopamine) USE: schizophrenia, psychosis, acute mania, Tourette syndrome TOX: Extrapyramidal - dystonia (extended spasm), akinesia, akathisia (restlessness), *Tardive dyskinesia (stereotypic oral/facial movements, often irreversible) Hypothalimic/Endocrine - hyperprolactinemia Muscarinic antagonism - dry mouth, constipation Alpha antagonism - hypotension Histamine antagonism - sedation *Neuroleptic Malignant Syndrome - rigidity, myoglobinuria, autonomic instability, hyperpyrexia; treat with dantrolene and dopamine agonists |
Antipsychotic
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Clozapine
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Atypical Antipsychotic
MECH: Block 5HT-2 and D4 receptors USE: schizophrenia (positive and negative symptoms) TOX: agranulocytosis (weekly WBC monitoring); fewer extrapyramidal and anticholinergic side fx than neuroleptics |
Antipsychotic
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Olanzapime
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Atypical Antipsychotic
MECH: Block 5HT-2 and D4 receptors USE: schizophrenia (positive and negative symptoms); OCD, anxiety disorder, depression, mania, Tourette syndrome TOX: fewer extrapyramidal and anticholinergic side fx than neuroleptics |
Antipsychotic
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Risperidone
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Atypical Antipsychotic
MECH: Block 5HT-2 and D4 receptors USE: schizophrenia (positive and negative symptoms) TOX: fewer extrapyramidal and anticholinergic side fx than neuroleptics |
Antipsychotic
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Fluoxetine (Prozac)
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SSRI
MECH: serotonin-specific reuptake inhibitor USE: endogenous depression, OCD TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse) |
Antidepressants
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Sertraline (Zoloft)
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SSRI
MECH: serotonin-specific reuptake inhibitor USE: endogenous depression, OCD TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse) |
Antidepressants
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Paroxetine (Paxil)
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SSRI
MECH: serotonin-specific reuptake inhibitor USE: endogenous depression, OCD TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse) |
Antidepressants
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Citalopram (Celexa)
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SSRI
MECH: serotonin-specific reuptake inhibitor USE: endogenous depression, OCD TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse) |
Antidepressants
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Imipramine
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Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT USE: major depression, bed wetting TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects (acute angle-closure glaucoma) |
Antidepressants
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Clomipramine
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Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT USE: major depression, OCD TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects |
Antidepressants
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Amytriptyline
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Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT USE: major depression TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects |
Antidepressants
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Desipramine
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Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT USE: major depression TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects |
Antidepressants
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Nortriptyline
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Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT USE: major depression (especially in elderly) TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects |
Antidepressants
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Doxepim
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Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT USE: major depression TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects |
Antidepressants
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Bupropion
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MECH: not understood
USE: depression, smoking cessation TOX: stimulant effects, HA, seizure in bulimics; does not cause sexual side fx |
Antidepressant
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Venlafaxine
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MECH: inhibits 5HT, NE, and DA reuptake
USE: depression, generalized anxiety disorder TOX: stimulant effects, sedation, nausea, constipation, HTN |
Antidepressant
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Mirtazapine
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MECH: 5HT-2 and 5HT-3 antagonist; alpha2 antagonist
USE: depression TOX: sedation, ↑ appetite, weight gain, ↑ serum cholesterol, dry mouth |
Antidepressant
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Maprotiline
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MECH: blocks NE reuptake
USE: depression TOX: sedation, orthostatic hypotension |
Antidepressant
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Trazodone
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MECH: inhibits serotonin reuptake
USE: depression TOX: sedation, nausea, priapism, postural hypotension |
Antidepressant
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Phenelzine
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MAOI
MECH: nonselective monoamine oxidase inhibition → ↑ levels of amine neurotransmitters (NE, DA, 5HT) USE: atypical depression (w/ psychotic or phobic features), anxiety, hypochondriasis TOX: hypertensive crisis with tyramine ingestion and meperidine; CNS stimulation. Contraindicated with SSRI or beta-agonists to prevent serotonin syndrome |
Antidepressant
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Tranylcypromine
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MAOI
MECH: nonselective monoamine oxidase inhibition → ↑ levels of amine neurotransmitters (NE, DA, 5HT) USE: atypical depression (w/ psychotic or phobic features), anxiety, hypochondriasis TOX: hypertensive crisis with tyramine ingestion and meperidine; CNS stimulation. Contraindicated with SSRI or beta-agonists to prevent serotonin syndrome |
Antidepressant
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Enflurane, isoflurane, sevoflurane, methoxyflurane
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Inhaled Anesthetic
MECH: unknown, probably GABA agonist USE: surgical anesthesia; causes mycardial and resp depression, N/V, ↑ cerebral blood flow TOX: Malignant hyperthermia, nephrotox (methoxy-), proconvulsant (en-) |
Anesthetic
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Halothane
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Inhaled Anesthetic
MECH: unknown, probably GABA agonist USE: surgical anesthesia; causes mycardial and resp depression, N/V, ↑ cerebral blood flow TOX: Malignant hyperthermia, hepatotox |
Anesthetic
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Nitrous oxide
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Inhaled Anesthetic
MECH: unknown, probably GABA agonist USE: incomplete anesthesia with rapid onset and recovery; causes myocardial and resp depression, N/V, ↑ cerebral blood flow TOX: Malignant hyperthermia |
Anesthetic
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Ketamine
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MECH: PCP analog
USE: dissociative anesthetic → disorientation, hallucination, bad dreams; ↑ cerebral blood flow |
Anesthetic
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Procaine, cocaine, tetracaine
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Local anesthetic - Esters
MECH: block Na+ channel by binding to receptors on inner portion of channel USE: minor surgical procedures, spinal anesthesia TOX: CNS excitation, hypertension, hypotension, arrhythmias |
Anesthetic
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Lidocaine, mepivacaine, bupivacaine
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Local anesthetic - Amides
MECH: block Na+ channel by binding to receptors on inner portion of channel USE: minor surgical procedures, spinal anesthesia TOX: CNS excitation, hypertension, hypotension, CV tox |
Anesthetic
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Flumazenil
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MECH: GABA antagonist
USE: benzo overdose |
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Propofol
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IV anesthetic
MECH: binds GABA-a USE: short procedures (rapid induction) TOX: less N/V than thiopental |
Anesthetic
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Etomidate
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IV anesthetic
MECH: enhancing inhibitory synaptic transmission at the GABA-a USE: anesthesia in unstable patients (no CV fx) TOX: inhibits 11-beta hydroxylase activity → ↓ cortisol |
Anesthetic
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