- blocks dopamine reuptake and also increase release of dopamine in presynaptic - primarily used to tx dyskinesia associated w/ peak-dose of carbidopa/levodopa warning: somnolence (including falling asleep w/out warning during activities of daily living, psychosis! SE: hypotension, dizziness... also livedo reticularis (reddish skin mottling!)

neurological condtions Flashcards by Krupa Bhakta

Pathophysiology of Parkinson’s

less dopamine-> less instructions to the brain -> movement problems (called TRAP major symptoms)

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TRAP

Tremor: when resting
Rigidity: in legs, arms, trunk, and face (mask-like face)
Akinesia/bradykinesia: lack of/slow start in movement
Postural instability: imbalance, falls

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dopamine-blocking drugs that can worsen PD

Phenothiazines (prochlorperazine) used for psychosis, nausea, agitation
Butyrophenones (haloperidol, droperidol) used for psychosis and behavior disorder or nausea
first and second gen antipsych (risperidone at higher dose, paliperidone); lowest risk is quetiapine
metoclopramide, a renally-cleared drug that can accumulate in elderly pt

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PD pt also depresssion

Depression common in PD pts
concerns w/ SSRI and SNRI but TCAs (secondary os desipramine and nortriptyline), and dopamine agonists like pramipexole provide antidepressants effects

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quetiapine in PD

quetiapine is preferred in psychosis PD pts
low risk of movement disorders but can cause metabolic complications

clozapine has a low risk of worsening movement disorders but has a high risk of seizures and agranulocytosis

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hallucinations and delusions in PD

pimavanserin (Nuplazid)

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rapid withdrawal of levodopa or dopamine agonists

can lead to neuroleptic malignant syndrome (NMMS)… tapper off slowly

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levodopa
carbidopa

levodopa- prodrug of dopamine, is the most effective agent
carbidopa: prevents peripheral metabolism of levodopa - to work 70-100 dose

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PD primary tx

primary tx: replace dopamine
- give a precursor to dopamine that becomes dopamine in the brain (that’s levodopa in Sinemet)
- give dopamine agonist that act like dopamine
- give other drugs for specific symptoms (benztropine for resting tremor)

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tremor-predominants disease in younger pts

can be tx w/centrally-acting anticholinergic (e.g. benztropine)

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carbidopa/levodopa

Sinemet
- contra w/non-selective MOA (14 day washout)
70-100 mg of carbidopa required
- coombs test: positive d/c (hemodialysis risk)

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COMT inhibitors

increase the duration of action of levodopa by inhibiting the enzyme COMT (catechol-O-methyltransferase) to prevent peripheral conversation of levodopa.

COMT should only be sued w/ levodopa

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entacapone

+ carbidopa/levodopa

Comtan

Stalevo

COMT inhibitor

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Pramipexole

Mirapex
warning: somnolence (including sudden daytime sleep attacks)
impulsive disorder…
postural deformity
- dopamine agonist

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Ropinirole

Requip XL
- dopamine agonist

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Rotigotine

Neupro
patch!
- dopamine agonist

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apomorphine

apokyn
- contra: w/ 5Ht-3 agonist (ondansetron) due to severe hypotension
- QT prolongation
severe nausea/vomiting
for emesis prevention give trimethobenzamide (Tigan)

dopamine agonist use as a “rescue” movement drug for “off” periods

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Amantadine

blocks dopamine reuptake and also increase release of dopamine in presynaptic
primarily used to tx dyskinesia associated w/ peak-dose of carbidopa/levodopa

warning: somnolence (including falling asleep w/out warning during activities of daily living, psychosis!

SE: hypotension, dizziness… also livedo reticularis (reddish skin mottling!)

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selective MAO-B inhibitors

block the breakdown of dopamine, primarily used as adjunctive tx to carbidopa/levodopa; rasagiline has a indication for monotherapy

selegiline (capsule genetic)
- Zelapar- ODT
- Emsam- patch only indicated for depression

rasagiline (azilect)
Safinamide (Xadago)

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benzatropine

Cogentin
centrally acting anticholinergic: have anticholinergic and antihistamine effects: primarily used for tremors

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natural products for memory-related lol

viatmine E (2,000 IU dialy)
ginkgo

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MMSE

mini-mental state exam, max 30 and less than 24 is a memory disorder

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key drugs that can worsen dementia

antiemetics (e.g. promethazine)
antihistamine (e.g. diphenhydramine, doxylamine)
antipsychotics (e.g. chlorpromazine, aripiprazole)
barbiturates (e.g. phenobarbital, butalbital)
benzodiazepines (e.g. alprazolam, clonazepam)
centrally acting anticholinergic (e.g. benztropine)
peripheral anticholinergics (including incontinence and IBS drugs)
Skeletal muscle relaxants (e.g. baclofen)
Other CNS depressants (e.g. opioids, sedative-hypnotics)

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mild-moderate Alzheimer’s disease

donepezil, rivastigmine, galantamine
(acetylcholinesterase inhibitor)

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moderate-severe

donepezil, rivastigmine, galantamine (acetylcholinesterase inhibitor) and/or memantine

donepezil + memantine

aricept Namzaric QHS to decrease nausea if stable on 10mg donepezil, can switch to namzaric - acetylcholinesterase inhibitor

Rivastigmine

exelon - patch form has less nausea! does not contain metal so do not have to remove for MRI - acetylcholinesterase inhibitor

memantine

Namenda ER capsules and numeric can be sprinkled on apple sauce after the opened - blocks NMDA receptor, which inhibits glutamate from binding and decreases abnormal neuron activation

key drugs that can lower seizure threshold

- bupropion - clozapine - theophylline - varenicline - carbapenems (esp. imipenem)* - lithium* - meperidine* - quinolones* - tramadol* *High doses and renal impairment

diastat acudial dispensing

- Each package contains two rectal syringes and prefilled w/ diazepam rectal gel syringes MUST be dialed to the right dose and locked BEFORE DISPENSING. Syringes come in 2.5, 10, and 20mg

Pharmacist instructions for locking diastat acudial

1. Hold the barrel of the syringe in one hand w/ the cap facing down and some window visible. Do not remove cap 2. Use the other hand to grab the cap firmly and turn to adjust the dose 3. confirm the correct dose in the window, hold the locking ring at the bottom of the syringe barrel and push upward to lock both sides of the ring 4. Repeat these steps w/ he second syringe in the case once locked, the green band should say "READY"

benzo AED mechanism of action

increase GABA AED= antiepileptic drugs

Valproic acid AED mechanism of action

increase GABA

phenobarbital AED mechanism of action

enhance/potentiate GABA efects

levetiracetam AED mechanism of action

Ca channel blocker and increase GABA

ethosuximide AED mechanism of action

t-type Ca channel blocker

pregaba/ gaba AED mechanism of action

Ca channel blocker

oxcarbazepine AED mechanism of action

Na and Ca channel blocker

carbamazepine AED mechanism of action

Na channel blocker

lamotrigine AED mechanism of action

Na channel blocker

phenytoin/fosphenytoin AED mechanism of action

Na channel blocker

topiramate

Na channel blocker

carbamazepine, oxcarbazepine, eslicarbazepine AED cousins SE

hyponatremia, rash, enzyme induction

gaba and pregaba AED cousins SE

- weight gain, peripheral edema, mild euphoria - used primarily for neuropathic pain

phenobarbital and primidone AED cousins SE

primidone (prodrug of phenobarbital) - sedation, dependence/tolerance/overdose risk, enzyme induction

topiramate and zonisamide AED cousins SE

- weight loss, metabolic acidosis - nephrolithiasis and oligohidrosis/hyperthermia (in children)

supplement w/ AEDs

- all AEDs: Ca and Vitamin D - women of childbearing age: folate - Valproic acid: possibly carnitine - lamotrigine and valproic acid: if alopecia develops, supplement w/ selenium and zinc

lamotrigine

lamictal - SJS/TEN severe

levetiracetam

Keppra Warning: psychiatric reactions, including psychotic symptoms, somnolence, fatigue

topiramate

topamax - metabolic acidosis, oligohidrosis (reduced perspiration), nephrolititasis (kideny stones) , fetal harm, visual problem - also used for migraine proplyaxis

valproic acid divalproex

depakote, ER and sprinkle form - hepatic failure, fetal harm - hyperammonemia (tx w/carnitine only in adults) also used for bipolar and migraine prophylaxis

carbamazepine

tegretol equetro for bipolar also used for trigeminal neuraliga - HLA-B testing.. especially if Asian descent contra: myelosuppression, hypersensitive to TCAs, use of MAO in past 14 days - autoinducer

lacosamide

vimpat - prolonged PR interval and increased risk of arrhythmias

oxcarbazepine

trileptal - HLA-B considers for Asian pts - not an autoinducer

phenobarbital

severe hepatic impairment contra... habit forming, respiratory depression, fetal harm....

phenytoin

Dilantin IV rate should not exceed 50mg/min

fosphenytoin

cerebyx fosphenytoin IV rate should not exceed 150mg PE/min dosed in PE, phenytoin equivalents. 1mg PE= 1 mg of phenytoin 1.5mg of fosphenytoin= 1 PE

IV phenytoin admin...

- do not exceed 50mh/ min (slow infusion) - Monitor BP, respiratory function and ECG - requires filter - Dilute in NS, stable for 4 hrs, do not refrigerate

NG-tube phenytoin admin

- eternal feedings (e.g. tube feeds) decrease phenytoin absorption - Hold feeding 1-2 hrs before and after admin

IV fosphenytoin admin

- Do not exceed 150mg PE/min - monitoring same as above - lower risk of purple glove syndrome than phenytoin

ethosuximide

zarontin

pregabalin

lyrica

gabapentin

neurontin

vigabatrin

sabril, igadrone - permanent vision loss >30% of pt....

primidone

mysoline prodrug of phenobarbital

phenytoin correction

total phenytoin measured/ [(0.2xalbumin)+0.1]

AEDs enzyme inducers

carbamazepine oxcarbamazepine phenytoin fosphenytoin phenobarbital primidone

AED enzyme inhibitors

valproic acid (increases lamotrigine dose so remember when dosing lamotrigine)