Flashcards in Neurology Drug List Deck (60)
Typical D2 Antagonists
Chlorpromazine and Haloperidol
Haloperidol and the "azines"
Chlopromazine Side Effects (SE)
Dry mouth (antimuscarinic), orthostatic hypotension (a1 antagonist), and sedation (antimuscarinic and antihistamine). Low potency, but also weight gain and increased risk for diabetes.
Halperidol Side Effects (SE)
Extrapyramidal side effects (DA blockade), can cause tardive dyskinesias. Used to tx CNS stimulant psychosis.
Atypical D2/5HT Antagonists
Clozapine, Quetiapine, Olanpazine, Risperidone, Aripipazole. All cause weight gain.
Agranulocytosis. Neuroleptic Malignancy. For pts who are refractive to other drugs.
Wt gain and Diabetes; decrease EPS
Fluoxetine, Paroxetine, Escitralopam, Setraline, and Citalopram. Wide interpatient variations; wt gain, sexual dysfunction, cognitive blunting, and withdrawal sx.
Fluoxetine and Paroxetine
blocks serotonin transporter and P450 inhibitor. Withdrawal sx.
Sedation, and potential for seizures at high doses. At high dose causes anxiety.
SNRIs. SE: HTN and anxiety, rapid withdrawal.
TCADs (Drugs and Uses)
Declining use; 2nd line agaents, antimuscarinic side effects, CV and seizures in overdose.
TCADs; 2nd line agents for depression, has antimuscarinic SE. CV problems and seizures in overdose. Also has a sedative action.
SE: postural hypotension, seizure, shock, hyperthermia in overdose, hypertensive crisis with foods high in tyramine, +SSRIs --> serotonin syndrome.
Lithium Carbonate*, Carpamazepine, Valproate, Olanzapine, Fluoxetine
Interference with PIP recycling. Enhance 5HT action/ decrease NE and DA effect. Use dependent (greatest activity in most active cells); narrow therapeutic index. Diuretics and NSAIDs will increase lithium levels. Can also cuase hypothyroidism, poluuria, and polydipsia.
BDZs, Non-BDZ BDZ Agonists, Barbiturates, Melatonin Receptor Antagonist, Other (Diphenhydramine)
"Lams and Pams"; sedative (a1) and anxiolysis (a2/a5); need much greater dosage increments to achieve CNS depression, increase margin of safety than compared to BARBs.
BDZ receptor antagonists; used in BDZ overdose to relieve CNS depression.
Non-BDZ BDZ Agonists
Zolpidem, Eszopiclone, Zalepon, "Zzz drugs", only acts on a1 GABA receptors.
"Ambien"; mild side effects and no hangover. Decrease sleep latency and nocturnal awakenings.
Longer half life than zolpedam; next day psychomotor impairment with higher doses (FDA requires lower dose for initiation); used for sleep maintenance.
Dizziness, HA, and somnolence. Decrease time for sleep onset.
Phenobarbital.Anticonvulsant effects without severe sedation or effects on mental or motor activity.
Anticonvulsant effects without severe sedation or effects on mental or motor activity.
rapid po; acute management of anxiety
long half life --> result in daytime sedation.
rapid po; acute management of anxiety
slow oral absorption; no P450 step, so metabolized to inactive glucuronides, short half life.
anterograde amnesia; also very rapid --> rebound insomnia because short half life.
same as oxazepam, but rapid via IM
intermediate half life; less anterograde amnesia than triazolam.
BDZ receptor antagonist in the case of overdose
Melatonin Receptor Agonist
MT1- induces sleepiness, MT2- regulation of circadian rhythms.
antihistamine and antimuscarinic; not recommended but is short term treatment for mild insomnia
alternative as anxiolytic, 5HT partial agonist (no sedation); for CNS depressant withdrawal.
Cocaine, Amphetamine, Methamphetamine --> interaction with catecholamine NT system; elevation of mood; SE: SNS overactivity. Increase tolerance and dependence; mild withdrawal sx.
Tx for Withdrawal Symptoms from CNS stimulants
TCADs and bupropion (NDRI); both better with behavioral therapy. Topiramate (GABA inhibition in alcoholics)
Alcohol, Barbiturates, and Benzodiazepines; enhance GABA activity; euphoria and sedation --> coma and death. Tx overdose with supportive care or flumazenil (BDZ antagonist). Tolerance and dependence develop rapidly. Withdrawal= high morbidity and mortality.
Heroin: mu agonist; rush and euphoria (highly reinforcing because rapid), overdose (coma, respiratory distress, pinpoint pupils) = tx with naloxone. rapid tolerance and dependence.
endogenous CR1 receptor in the CNS; enhancement of sensory stimuli; tx with support therapy, little tolerance (if yes, goes away fast), 10% physical dependence
Drugs for Tx of Drugs of Abuse
- Methadone: tx opiod withdrawal
- Buprenorphine- tx opiod withdrawal
- Clonidine: tx opiod withdrawal
- Naltrexone: tx opiod withdrawal
- Disulfram: blocks aldehyde dehydrogenase --> reduce EtOH consumption.
Common use for dental procedures; less soluble, exhibits more rapid increase in its partial pressure in blood. No surgical anesthesia.
Halothane: substitute of cyclopropane; for surgical anesthesia. Can cause malignant hyperthermia.
Grand Mal (Tonic-Clonic Seizures)
Phenytoin, Carbamazepine, Valproate, Levetiracetam
Phenytoin- for partial and primary generalized tonic clonic, block VSSC (blockage use dependent)
block VSSC (blockade use dependent)
potentiation on GABA function; limits activity of T-type Ca2+ channel. hepatotoxicity, contraindicated in pregnancy; 1st line.
lower rate for fetal malformation, 1st line in tonic clonic. Also used for partial seizure.
Broad Spectrum Anti-Epileptics
Phenobarbital, Olazepam, Valproate, Divalproex (similar to valproate)
enhance GABA inhibition, antagonize glutamate excitation, P450 inducer
Absence Seizures Tx
Ethosuximide- supresses brain activity; metabolized by CYP34A; drug of choice. And valproate.
Diazepam, Lorazepam, Midazolam.