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67 Cards in this Set

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carbamazine

Treat generalize & partial tonic-clonic seizure


MOA: Na+ channel blocker


ADR: ataxia, aplastic anemia, GI distress, cognitive impairment


DI: erythromycin, fluoxetine, chloramphenicol, isoniazid, verapamil, propoxyphene, valproate, phenytoin, felbamate

phenytoin

Treat generalize & partial tonic-clonic seizure


MOA: Na+ channel blocker


ADR: anemia secondary to folate deficiency, coarsening of facial features, hirsutism, peripheral neuropathy, gingival hyperplasia, dipoplia, ataxia, nystagmus, dec. bone density


DI: CYP3A4 inhibitors increase levels


CYP3A4 inducers decrease levels


Pregnancy category D

valproic acid

Treat generalize & partial tonic-clonic seizure


Treats generalized absence seizures


MOA: Blocks Na+ Channels, blocks T-type Ca++ channels, increases GABA, decreases glutamate


ADR: tremor, weight gain, thrombocytopenia, hepatotoxicity (esp in children)


DI: ASA, isoniazide and felbamate inc levels


carbamazine and phenytoin dec levels


Pregnancy category D

phenobarbital & primidone

Treat generalize & partial tonic-clonic seizure


MOA: Increases GABA, primidone blocks Na+ channels


ADR: ataxia, dizziness, cognitive impairment, folate, vit D & K deficiencies, hyperactivity in young children,


DI: valproate, phenytoin and isoniazid increase levels

ethosuxamide

Treats Generalized Absence seizures in children


MOA: inhibit T-type Ca++ channels in the thalamus


ADR: N/V, somnolence, dizziness, neutropenia


DI: valproate increases levels, haldol

felbamate

MOA: blocks glycine coactivation of NMDA recepters


ADR: FATAL APLASTIC ANEMIA (monitor weekly)


hepatic failure, weight loss


2nd line -- only used in refractory seizures

gabapentin

2nd line for seizures


MOA: increases GABA


ADR: ataxia, tremor, dizziness, drowsiness, nystagmus, hyperactivity in kids


DI: none

lamotrigine

MOA: blocks Na+ channels


ADR: rash, Stevens-Johnson syndrome, cerebellar dysfunction, headache,


CI: partial seizures in adults and children.


DI: Valproic acid inc levels

topiramate

MOA: Na+ channel blocker, inc GABA, dec glutamate


ADR: cerebellar dysfunction, drowsiness, weight loss, renal stones, glaucoma


CI: adjunct treatment for partial and generalized seizures

levitiracetam

MOA: increases GABA


ADR: brings out underlying psychiatric disorders, hallucinations, somnolence


CI: partial seizures in children


zonisamide

MOA: dec Na & Ca channel activity


ADR: Somnolens, kidney stones, dec sweating


CI: partial and generalized seizures (sulfa drug)

What is the treatment for status epilecticus?

1st: diazepam or lorazepam (IV) Q10-15 minutes


2nd: phenytoin

Non drug therapies for seizure disorders

ketogenic diet - 3:1 or 4:1 fat to protein/carb


1/3 of patients are seizure free, another 1/3 have 50% reduction


vagus nerve stimulator


Surgery: focal resection, hemispherectomy, corpus callostomy

Level A evidence migraine prevention

*

Antiepileptic drugs (AEDs): divalproex sodium, sodium valproate, topiramate


*

β-Blockers: metoprolol, propranolol, timolol


Triptans: frovatriptan for short-term MAMs prevention


*

INEFFECTIVE: LAMOTROGINE

Level B evidence migraine prevention

*

Antidepressants: amitriptyline, venlafaxine


*

β-Blockers: atenolol, nadolol


*

Triptans: naratriptan, zolmitriptan for short-term MAMs prevention


*

INEFFECTIVE: clomiperamine

Dementia treatment

cholinesterase inhibitors (donepezil, tacrine, galantamine)


neuropeptide modifying agent (memantine)

MOA of benzodiazepines

stimulate GABA



allosteric binding to GABA receptor-Cl channel, increase channel opening



inhibit reuptake of adenosine

Indications for benzodiazepines

acute anxiety


panic disorder (will cause sedation, SSRIs better)


phobic disorders (SSRIs better)


generalized anxiety disorder


PTSD (usually SSRI first)

Migraine headaches


- prevalence


- presentation

20% of population


prodrome -- 60% of patients -- mental changes, neurological changes, sluggishness, thirst anorexia, diarrhea or constipation


aura -- 20% of patients, minutes to 1 hour before headache -- visual disturbances, vertigo, aphasia, photofphobia

Migraine headaches


- headache phase

severe, throbbing


n/v in 90% of patients


photophobia


vertigo


diarrhea


tremor, chills, diaphoresis


Migraine headaches


- pathophysiology

Nerve fibers in CNS release vasoactive substances and trigger an inflammatory reaction around cerebral blood vessels


5-HT1 is serotonin receptor subtype that dec this inflammatory response and causes vasoconstriction


5-HT2 is excitatory and will worsen migraine symptoms when activated

What analgesic medication can result in toxicity with a relatively small dose and causes irreversible liver damage?

acetaminophen

Drugs used to abort a migraine headache are

ergot agents (ergotamine)


triptans (first - sumatriptan, additional -- naratriptan, rizatriptan, zolmitriptan, newest -- frovatriptan, almotriptan, eletriptan)

What migraine drug is contraindicated for patients with CAD

Ergot agents and triptans

Dose limitations for



-- ergotamines



-- triptans

ergotamine -- 8 treatment days/month



triptans -- 6 treatment days per months, 2 treatment days per week

Generalized seizures

originates in both hemispheres and involves loss of consciousness


includes absence & tonic-clonic

Partial (focal) seizures

originates in one hemisphere, no loss of consciousness


includes complex partial and simple partial

absence seizure

* Brief staring
* Eye blinking sometimes
* Can have several hundred per day
* Psychomotor slowing

Generalized tonic-clonic

* Stiffening, followed by rhythmic jerks of entire body
* Can begin with complex partial seizure and evolve into generalized, tonic clonic seizure

Complex partial seizure

* Variable presentationhand or mouth automatisms
* staring
* spinning around

Simple partial seizure

* Consciousness retainedRepetitive simple movement or sensation
* Can happen continuously (epilepsia partialis continua)

What are the cardinal signs of parkinsons?

Bradykinesia, resting tremor (pill rolling), rigidity, postural instability

What is the first agent used in the treatment of parkinsons?

levodopa-carbidopa

benzodiazepine pregnancy category

Pregnancy category D


Benzodiazepine antagonist

flumazenil

alprazolam drug interactions

fluoxetine and fluvoxamine inc levels

chlordiasepoxide and diazepam drug interactions

cimetidine and rifampin increase levels

lorazepam, oxazepam and temazepam drug interaction

cimetidine and rifampin increase levels

estazolam, flurazepam, triozalam

CI: Insomnia


triazolam banned in UK due to delirium -- short-acting


flurazepam -- long acting


DI: hypersensitivity, anaphylaxis, complex sleep behaviors


clonazepam clinical indications

panic disorder, seizure disorder

midazolam

IV only, anaesthetic

hypnotics for insomnia

zolpidem, zaleplon (Sonata), eszopiclone (lunesta)



Work at GABA receptor

ramelteon CI & MOA

insomnia


works at melatonin receptor, non sedating

list long-acting benzodiazepines (3)

chlordiazepoxide


diazepam


flurazepam



these have long lived metabolites

list short-acting benzodiazepines (4)

alprazolam


estazolam


midazolam


triazolam

benzodiazepins that bypass P1 oxidation and use only P2



short acting & safer (3)

oxazepam


temazepam


lorazepam

ceiling effect definition

benzodiazepines work only in the presence of GABA released by neurons, and therefore have a limited effect on sedation. They inc frequency that the channel opens.


barbituates work regardless of presence of GABA and keep channel open and can increase sedation without limit based on dose.

insomnia drugs w/MOA

zolpidem, zaleplon, escoplicone - selectively target GABA-A receptors. Shorter 1/2 life than benzos. Zaleplon has shortest 1/2 life of 1 hour.



benzodiazepines - bind to Cl channel and keep it open, increase GABA



ramelteon - melatonin receptors

benzodiazepine dependence

patient will experience withdrawal characterized by anxiety, insomnia, headache, irritability and muscle twitches.



Dosage should be gradually tapered over several weeks.

role of GABA and glutamate in seizure disorders

excessive activation by glutamate of N-methyl-D-aspartate (NMDA) displaces Mg++ ions and facilitates C++ entry into neurons



GABA (gamma-aminobutyric acid) neurotransmission is suppressed

Anti-epileptic drugs MOA

1) Block Na+ channels


2) Block T-type calcium channels


3) increase GABA activation or activate receptor or increase GABA release, or inhibit degradation


4) inhibit glutamate neurotransmission

First line agents for generalized tonic/clonic seizures (5)

* carbamazine -- Na+ channel blocker


* phenytoin -- Na+ channel blocker


* phenobarbital -- enhances GABA


* primidone -- degrades to phenobarbital & phenylethylmalonamide


* valproate - Na+ channel blocker, T-type calcium channel blocker, inc GABA, dec glutamate

first line agents for absence seizures (1 for kids, 1 for adults)

ethosuzamide - kids - inhibits T-type Ca++ channels


valproate -- adults

adjuvant agents for partial seizures (6)

felbamate


gabapentin


lamotrigine


topiramate


levetiracetam


zonisamide

First line agents for partial seizure

-------

etiology of parkinsons

degeneration of the dopaminergic neurons in the substantia nigra and development of Lewy bodies in the residual dopaminergic neurons

levodopa-carbidopa MOA & ADR

MOA - levodopa ^ dopamine levels & carbidopa ^ amount of levodopa that enters the brain


ADR - levodopa - N/V, which is reduced my co-administration with carbidopa; dyskinesias, psychosis

amantadine MOA & ADR

MOA - increases release of dopamine


ADR - sedation, restlessness, dreams, nausea, dry mouth, hypotension

selegiline MOA & ADR

MOA: inhibits MAO-B & thereby prevents the oxidation of dopamine


ADR: potential for food interactions, interactions with SSRIs and meperidine

tolcapone MOA & ADR

MOA: inhibits COMT, the enzyme that metabolizes levodopa


ADR: nausea, diarrhea which reduces over time; hepatotoxicity

Alzheimers Disease etiology & presentation

etiology: destruction of cholinergic and other neurons in the cortex and limbic structures of the brain, especially the amygdala, basal forebrain, and hippocampus


Presentation: dementia

donepezil

CI: Alzheimers


MOA: cholinesterase inhibitor


ADR: diarrhea, nausea, vomiting

rivastigmine

CI: Alzheimers


MOA: cholinesterase inhibitor


ADR:

galantamine

CI: Alzheimers


MOA: cholinesterase inhibitor

memantine

CI: Alzheimers


MOA: noncompetitive antagonist at NMDA receptor (attenuates the excitotoxic effects of glutamate)

ergot ADR

nausea, vomiting, diarrhea, muscle cramps, cold skin, paresthesias, vertigo


peripheral vasoconstriction -- contraindicated in persons with CAD or peripheral vascular disease


rebound headache

triptan ADR

chest tightness, weakness, somnolence, dizziness, paresthesias, coronary vasospasm



risk of serotonin syndrome with SSRIs