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59 Cards in this Set

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Bromocriptine
MECH: agonize dopamine receptors
USE: Parkinson's Disease, hyperprolactinemia
TOX: nausea, somnolence, hallucinations, orthostatic hypotension
PD
Pramipexole
MECH: agonize dopamine receptors
USE: Parkinson's Disease
TOX: nausea, somnolence, hallucinations, orthostatic hypotension
PD
Ropinirole
MECH: agonize dopamine receptors
USE: Parkinson's Disease
TOX: nausea, somnolence, hallucinations, orthostatic hypotension
PD
Amantadine
MECH: increase dopamine release
USE: Parkinson's Disease
PD
L-dopa (levodopa)
MECH: crosses BBB, converted by dopa decarboxylase → ↑dopamine levels
USE: Parkinsonism
TOX: arrhythmias, long term use → dyskinesia following admin and akinesa btw doses
PD
Carbidopa
MECH: peripheral decarboxylase inhibitor → ↑ L-dopa bioavialability and ↓ side effects
USE: Parkinsonism in conjunction with L-dopa
PD
Selegiline
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
Entacapone
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
Tolcapone
MECH: selectively inhibits COMT → ↑ dopamine availability
USE: adjunctive agent to L-dopa to treat PD
TOX: may enhance adverse effects of L-dopa
PD
Benzotropine
MECH: antimuscarinic
USE: improves tremor and rigidity of PD
TOX: antimuscarinic side effects (impaired cognition, dry mouth, urinary retention)
PD
Sumatriptan
MECH: 5HT-1D agonist → vasoconstriction
USE: acute migraine, cluster headache attacks
TOX: coronary vasospasm, mild tingling (contraindicated with CAD or Prinzmetal's)
Phenytoin
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
Carbamazepine
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
Valproic Acid
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
Lamotrigine
MECH: blocks voltage-gated Na+ channels
USE: anti-epileptic; acute mania and mania/depression prophylaxis
TOX: Stevens-Johnson syndrome
Anticonvulsant, mood stabilizer
Gabapentin
MECH: ↑ GABA release
USE: anti-epileptic, peripheral neuropathy
TOX: sedation, ataxia
Epilepsy
Topiramate
MECH: blocks Na+ channels; ↑ GABA actions
USE: anti-epileptic
TOX: sedation, mental dulling, kidney stones, weight loss
Epilepsy
Phenobarbital
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
Pentobarbital
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
Thiopental
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
Secobarbital
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
Ethosuximide
MECH: Blocks thalamic T-type Ca++ channels
USE: absence seizures
TOX: GI, lethargy, HA, urticaria, Stevens-Johnson
Benzodiazepines (diazepam, lorazepam, temazepam, chlordiazepoxide, alprazolam)
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)
Benzodiazepines (triazolam, oxazepam, midazolam)
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
Lithium
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
Buspirone (BuSpar)
MECH: stimulates 5HT-1A receptors
USE: anxiolysis for generalized anxiety disorder
TOX: unlike benzo - does not cause sedation, addiction, alcohol interactions
Anti-anxiety
Thioridazine
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
Haloperidol
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
Fluphenazine
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
Chlorpromazine
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
Clozapine
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
Olanzapime
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
Risperidone
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
Fluoxetine (Prozac)
SSRI
MECH: serotonin-specific reuptake inhibitor
USE: endogenous depression, OCD
TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse)
Antidepressants
Sertraline (Zoloft)
SSRI
MECH: serotonin-specific reuptake inhibitor
USE: endogenous depression, OCD
TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse)
Antidepressants
Paroxetine (Paxil)
SSRI
MECH: serotonin-specific reuptake inhibitor
USE: endogenous depression, OCD
TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse)
Antidepressants
Citalopram (Celexa)
SSRI
MECH: serotonin-specific reuptake inhibitor
USE: endogenous depression, OCD
TOX: GI, sexual dysfunction (anorgasmia), Serotonin Syndrome (hyperthermia, muscle rigidity, CV collapse)
Antidepressants
Imipramine
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
Clomipramine
Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT
USE: major depression, OCD
TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects
Antidepressants
Amytriptyline
Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT
USE: major depression
TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects
Antidepressants
Desipramine
Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT
USE: major depression
TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects
Antidepressants
Nortriptyline
Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT
USE: major depression (especially in elderly)
TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects
Antidepressants
Doxepim
Tricyclic Antidepressant
MECH: Block reuptake of norepi and 5HT
USE: major depression
TOX: Convulsions, Coma, Cardiotoxicity, sedation, alpha-blocking effects, anticholinergic effects
Antidepressants
Bupropion
MECH: not understood
USE: depression, smoking cessation
TOX: stimulant effects, HA, seizure in bulimics; does not cause sexual side fx
Antidepressant
Venlafaxine
MECH: inhibits 5HT, NE, and DA reuptake
USE: depression, generalized anxiety disorder
TOX: stimulant effects, sedation, nausea, constipation, HTN
Antidepressant
Mirtazapine
MECH: 5HT-2 and 5HT-3 antagonist; alpha2 antagonist
USE: depression
TOX: sedation, ↑ appetite, weight gain, ↑ serum cholesterol, dry mouth
Antidepressant
Maprotiline
MECH: blocks NE reuptake
USE: depression
TOX: sedation, orthostatic hypotension
Antidepressant
Trazodone
MECH: inhibits serotonin reuptake
USE: depression
TOX: sedation, nausea, priapism, postural hypotension
Antidepressant
Phenelzine
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
Tranylcypromine
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
Enflurane, isoflurane, sevoflurane, methoxyflurane
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
Halothane
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
Nitrous oxide
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
Ketamine
MECH: PCP analog
USE: dissociative anesthetic → disorientation, hallucination, bad dreams; ↑ cerebral blood flow
Anesthetic
Procaine, cocaine, tetracaine
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
Lidocaine, mepivacaine, bupivacaine
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
Flumazenil
MECH: GABA antagonist
USE: benzo overdose
Propofol
IV anesthetic
MECH: binds GABA-a
USE: short procedures (rapid induction)
TOX: less N/V than thiopental
Anesthetic
Etomidate
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