CNS Agents Flashcards
__etine, __opram
SSRI Antidepressant
Prevent reuptake of Serotonin, potentiating its effects. Most common antidepressant type. Rx for depression, anxiety disorders, OCD, PDD, eating disorders. SE: sexual dysfunction, GI upset, loss of appetite, tremors.
DO NOT give SSRIs with MAOIs. Serotonin syndrome: mental status changes, muscle stiffness, hyperthermia.
Ex: Paroxetine, Fluoxetine (inhibit P-450), Dapoxetine, Escitalopram, Citalopram, Fluoxamine, Sertraline, Zimelidine.
__triptyline, __ipramine
Tricyclic Antidepressants
Serotonin/NE reuptake inhibitors. Less common use than SSRIs b/c also inhibit M, H, a-adrenergic receptors, leading to side effects.
Rx for major depression, panic disorders, enuresis, chronic pain. SE: sedation (H block), postural hypotension and arrhythmia (a block), cant see/pee/shit/spit (antiACh at M).
DO NOT give TCAs with MAOIs, seizures result. Overdose: EKG changes (widened QRS), arrhythmias, mental status changes, seizures.
Ex: Amitriptyline, Nortriptyline, Doxepin, Imipramine, Desipramine. Second generation: Amoxapine, Trazodone (Rx insomnia, cause priaprism), Buproprion (smoking cessation).
Nefazodone, Mirtazapine, Venlafaxine, Maprotiline
Heterocyclic Antidepressants
Block reuptake of NE/Serotonin. M: inhibits activation of a2-adrenergic and 5HT2 receptors, increasing release of NE/Serotonin
Rx of depressive disorders and GAD. SE: sedation, increased appetite and weight gain, HTN and increased HR.
Ex: Nefazodone, Mirtazapine, Venlafaxine, Maprotiline.
Tranylcypromine, Phenelzine, Isocarboxazid
MAOIs, Monoamine Oxidase Inhibitors.
Levels of NE, Serotonin, and DA increase because it wipes out Monoamine oxidase, which metabolizes them. Leak out into the synape and activate Serotonin and NE receptors.
Rx of atypical depression, phobias, panic disorder. SE: sedation, hypotension, blurred vision, weight gain. Can’t degrade tyramine in wine, cheese, and smoked meats. Leads to a hypertensive crisis (HA, arrhythmia, HTN) when builds up and stimulates release of EPI/NE.
Ex: Tranylcypromine, Phenelzine, Isocarboxazid.
Lithium
Antipsychotic
MOA not understood. May inhibit the phosphoinositol second messenger cascade and interfere with synthesis, storage, release, and reuptake of Serotonin/DA/NE.
Rx as a mood stabilizer for bipolar disorder. Combine with other Rx for schizoaffective disorder, schizophrenia, psychotic feature mood disorders. SE: fine hand tremor, hypothyroidism, ECG changes, nephrogenic diabetes insipidus (ADH antagonism - hypernatremia, polyuria, polydipsia). Risk of intoxication, monitor.
Dantrolene
Muscle relaxer. Rx of Neuroleptic Malignant Syndrome from antipsychotic drugs: muscle rigidity, altered mental status, hypothermia, autonomic instability. Or use DA agonist (Levodopa, Bromocriptine, Amantadine).
__operidol, Fluphenazine
Typical Antipsychotic Agents. High potency.
Blocks postsynaptic D2 receptors in limbic system, decreasing response to DA excitation. Some inhibition at H1, cholinergic, and a-adrenergic receptors, leads to side effects.
Rx positive symptoms of schizophrenia (delusions, hallucinations), Tourettes, delirium, agitation. SE: sedation (H), anticholinergic effects, orthostatic hypotension (a), extrapyramidal signs (dystonia, akinesia, akathisia, tardative dyskinesia) from DA blockade, increased prolactin (galactorrhea, amenorrhea) from lack of DA inhibition of pituitary.
Neuroleptic malignant syndrome: muscle rigidity, altered mental status, hypothermia, autonomic instability, Rx with Dantrolene or DA agonists.
Ex: Haloperidol, Fluphenazine.
__azine
Typical Antipsychotic Agents. Low potency.
Blocks postsynaptic D2 receptors in limbic system, decreasing response to DA excitation. Some inhibition at H1, cholinergic, and a-adrenergic receptors, leads to side effects.
Rx positive symptoms of schizophrenia (delusions, hallucinations), Tourettes, delirium, agitation. SE: sedation (H), anticholinergic effects, orthostatic hypotension (a), extrapyramidal signs (dystonia, akinesia, akathisia, tardative dyskinesia) from DA blockade, increased prolactin (galactorrhea, amenorrhea) from lack of DA inhibition of pituitary.
Neuroleptic malignant syndrome: muscle rigidity, altered mental status, hypothermia, autonomic instability, Rx with Dantrolene or DA agonists.
Ex: Chlorpromazine, Thioridazine.
__apine, __idone
Atypical Antipsychotic Agents.
Blocks Serotonin (5HT2) and DA receptors in limbic system, decreasing response to DA and Serotonin. Some inhibition in H1, Cholinergic, a-adrenergic receptors, but much less than the typicals.
Rx positive and negative symptoms of schizophrenia, bipolar, other psychotic disorders. O, R, Q Rx for delirium. SE: Drowsiness, mild weight gain, mild hypotension, Parkinsonism symptoms. Clozapine causes mild leukopenia and agranulocytosis. Fewer side effects than the typicals.
Ex: Clozapine, Risperidone, Olanzapine, Ziprasidone, Aripriprazole, Quetiapine.
__azepam, __zolam
Benzodiazepines. Sedative.
Bind adjacent to GABAa receptor and enhance activity, resulting in increased frequency of Cl- flow, leading to cell membrane hyperpolarization and ultimately decreased activity of the neurons of the limbic, thalamic, and hypothalamic regions of the CNS.
Rx anxiety, seizures, status epilepticus, muscle spasms, EtOH withdrawl, insomnia, panic disorder. Mida and Diaz also anesthetics. Dependence potential. SE: sedation, altered mental status, ataxia. Withdrawl: altered mental status, anxiety, tachycardia, vomiting. Overdose: cardiac and respiratory depression, Rx with Flumazenil (competitive antagonist at GABA).
Less dangerous than Barbiturates. Avoid in patients with liver disease, alcohol use, Barbituates, or other CNS depressants.
Ex: Short - Triazolam, Midazolam. Intermediate - Lorazepam, Temazepam, Oxazepam, Alprazolam. Long - Diazepam, Prazepam, Clonazepam, Flurazepam.
Flumazenil
CNS Agent.
Competative agonist for GABAa receptors.
Rx for Benzodiazepine overdose treatment along with supportive care. Benzo overdose: cardiac and respiratory depression.
__bartital
Bartiburates. Sedative.
Indirectly potentiate GABAa receptor activity in brain, increasing time Cl- open, leading to cell membrane hyperpolarization and decreased CNS neuronal activity.
Rx of anxiety, insomnia, anesthesia induction (Thio), seizure management and neonatal hyperbilirubinemia (Pheno). SE: Sedation, nausea, teratogen. Dependence potential. Withdrawal: nausea, anxiety, seizures, tachycardia. Overdose: cardiac and respiratory depression, Rx with ventilation, hemodialysis, alkalinization of urine.
More dangerous than Benzodiazepines. Avoid in liver disease, pregnancy, porphyria, alcohol, benzos, other CNS depressants. Induces P-450.
Ex: Phenobarbital, Thiopental, Secobarbital, Amobarbital, Pentobarbital.
Phenytoin
Anti-Epileptic
Decreases Na+ and Ca++ flow, leading in decreased depolarization of NS cells.
Rx for simple and complex partial seizures, grand maul seizures (generalized tonic-clonic), status epilepticus, trigeminal neuralgia, torsades de pointes.
SE: Nystagmus, diplopia, gait instability, gingival hyperplasia, hirsutism, neuropathy, megaloblastic anemia, rash, drug-induced lupus, teratogen (fetal hydantoin syndrome - prenatal growth deficiency, congenital cardiac and palate malformations). Induces P-450.
Lamotrigine
Anti-Epileptic
Inhibits Na+ channels and release of glutamate from nervous tissue.
Rx for simple and complex partial seizures, generalized tonic-clonic seizures. SE: severe rash, nausea, headache.
Valproic Acid
Anti-Epileptic
Increase GABA concentrations by inhibiting metabolizing enzymes and hyperpolarization of membrane via change in Na+/K+ conductance.
Rx in generalized tonic-clonic seizures, myocloni seizures, absence seizures, mania in bipolar, prevention of migraines. SE: hepatotoxicity, thrombocytopenia, teratogen (neural tube defects), GI upset, sedation, nausea, weight gain.
