Flashcards in Neurology Drug List Deck (60)
1
Typical D2 Antagonists
Chlorpromazine and Haloperidol
Haloperidol and the "azines"
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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.
3
Halperidol Side Effects (SE)
Extrapyramidal side effects (DA blockade), can cause tardive dyskinesias. Used to tx CNS stimulant psychosis.
4
Atypical D2/5HT Antagonists
Clozapine, Quetiapine, Olanpazine, Risperidone, Aripipazole. All cause weight gain.
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Clozapine SE
Agranulocytosis. Neuroleptic Malignancy. For pts who are refractive to other drugs.
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Quetiapine SE
Wt gain and Diabetes; decrease EPS
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SSRIs
Fluoxetine, Paroxetine, Escitralopam, Setraline, and Citalopram. Wide interpatient variations; wt gain, sexual dysfunction, cognitive blunting, and withdrawal sx.
8
Fluoxetine and Paroxetine
blocks serotonin transporter and P450 inhibitor. Withdrawal sx.
9
Escitralopam
SSRI
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NDRIs
Bupropion
11
Bupropion
Sedation, and potential for seizures at high doses. At high dose causes anxiety.
12
SNRIs
Venlafaxine
13
Venlafaxine
SNRIs. SE: HTN and anxiety, rapid withdrawal.
14
TCADs (Drugs and Uses)
Declining use; 2nd line agaents, antimuscarinic side effects, CV and seizures in overdose.
Amitriptyline.
15
Amitriptyline
TCADs; 2nd line agents for depression, has antimuscarinic SE. CV problems and seizures in overdose. Also has a sedative action.
16
MAOIs
Phenelzine
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Phenelzine
SE: postural hypotension, seizure, shock, hyperthermia in overdose, hypertensive crisis with foods high in tyramine, +SSRIs --> serotonin syndrome.
18
Antimanic Agents
Lithium Carbonate*, Carpamazepine, Valproate, Olanzapine, Fluoxetine
19
Lithium Carbonate
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.
20
Sedatives-Hypnotics-Anxiolytics
BDZs, Non-BDZ BDZ Agonists, Barbiturates, Melatonin Receptor Antagonist, Other (Diphenhydramine)
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BDZs
"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.
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Flumazenil
BDZ receptor antagonists; used in BDZ overdose to relieve CNS depression.
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Non-BDZ BDZ Agonists
Zolpidem, Eszopiclone, Zalepon, "Zzz drugs", only acts on a1 GABA receptors.
24
Zolpidem
"Ambien"; mild side effects and no hangover. Decrease sleep latency and nocturnal awakenings.
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Eszopiclone
Longer half life than zolpedam; next day psychomotor impairment with higher doses (FDA requires lower dose for initiation); used for sleep maintenance.
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Zalepon
Dizziness, HA, and somnolence. Decrease time for sleep onset.
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Barbiturates
Phenobarbital.Anticonvulsant effects without severe sedation or effects on mental or motor activity.
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Phenobarbital
Anticonvulsant effects without severe sedation or effects on mental or motor activity.
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Alprazopam
rapid po; acute management of anxiety
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Flurazepam
long half life --> result in daytime sedation.
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Diazepam
rapid po; acute management of anxiety
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Oxazepam
slow oral absorption; no P450 step, so metabolized to inactive glucuronides, short half life.
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Triazolam
anterograde amnesia; also very rapid --> rebound insomnia because short half life.
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Lorazepam
same as oxazepam, but rapid via IM
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Midazolam
status epilepticus
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Temazepam
intermediate half life; less anterograde amnesia than triazolam.
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Flumazenil
BDZ receptor antagonist in the case of overdose
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Melatonin Receptor Agonist
Ramelteon
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Ramelteon
MT1- induces sleepiness, MT2- regulation of circadian rhythms.
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Diphenhydramine
antihistamine and antimuscarinic; not recommended but is short term treatment for mild insomnia
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Buspirone
alternative as anxiolytic, 5HT partial agonist (no sedation); for CNS depressant withdrawal.
42
CNS Stimulants
Cocaine, Amphetamine, Methamphetamine --> interaction with catecholamine NT system; elevation of mood; SE: SNS overactivity. Increase tolerance and dependence; mild withdrawal sx.
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Tx for Withdrawal Symptoms from CNS stimulants
TCADs and bupropion (NDRI); both better with behavioral therapy. Topiramate (GABA inhibition in alcoholics)
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CNS Depressants
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.
45
Opiod Analgesics
Heroin: mu agonist; rush and euphoria (highly reinforcing because rapid), overdose (coma, respiratory distress, pinpoint pupils) = tx with naloxone. rapid tolerance and dependence.
46
Cannabinoids
endogenous CR1 receptor in the CNS; enhancement of sensory stimuli; tx with support therapy, little tolerance (if yes, goes away fast), 10% physical dependence
47
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.
48
Gaseous Anesthetics
Nitrous Oxide
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Nitrous Oxide
Common use for dental procedures; less soluble, exhibits more rapid increase in its partial pressure in blood. No surgical anesthesia.
50
Volatile Anesthetics
Halothane: substitute of cyclopropane; for surgical anesthesia. Can cause malignant hyperthermia.
51
Grand Mal (Tonic-Clonic Seizures)
Phenytoin, Carbamazepine, Valproate, Levetiracetam
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Phenytoin
Phenytoin- for partial and primary generalized tonic clonic, block VSSC (blockage use dependent)
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Carbamazepine
block VSSC (blockade use dependent)
54
Valproate
potentiation on GABA function; limits activity of T-type Ca2+ channel. hepatotoxicity, contraindicated in pregnancy; 1st line.
55
Levetiracetam
lower rate for fetal malformation, 1st line in tonic clonic. Also used for partial seizure.
56
Broad Spectrum Anti-Epileptics
Phenobarbital, Olazepam, Valproate, Divalproex (similar to valproate)
57
Phenobarbital
enhance GABA inhibition, antagonize glutamate excitation, P450 inducer
58
Absence Seizures Tx
Ethosuximide- supresses brain activity; metabolized by CYP34A; drug of choice. And valproate.
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Status Epilepticus
Diazepam, Lorazepam, Midazolam.
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