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56 Cards in this Set
- Front
- Back
what kind of drugs can cross the BBB? |
lipid-soluble |
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what kind of drugs can't cross the BBB? |
protein bound and highly ionized drugs |
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what is tolerance? |
decreased response occurring in the course of prolonged drug use |
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what is physical dependence? |
state in which abrupt discontinuation of drug use will precipitate a withdrawal syndrome |
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give 2 examples that are excitatory NT (depolarization) |
ACh and Glutamic Acid |
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binding of ACh to the post synaptic receptors causes the release of what? |
Na+ ions |
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what is the excitatory pathway? |
stimulation of excitatory neurons results in depolarization of the postsynaptic membrane |
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what is the inhibitory pathway? |
stimulation of inhibitory neurons results in HYPERPOLARIZATION of the post synaptic membrane |
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name 2 inhibitory NT that causes hyperpolarization |
GABA and Glycine |
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Binding of the inhibitory NT ______ or _______ causes entrance of ________ and ______ which makes it more hyperopolarizable. |
GABA, Glycine, K+ and Cl- |
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What is Parkinson's disease? |
d/o of EP system= dyskinesias |
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name the 3 main characteristics of Parkinson's |
tremor at rest (supinate and pronate tremor), postural instability, and bradykinesia |
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patho behind Parkinson's |
1. cell death in substantia nigra results in less dopamine release in the neostriatum 2. loss of inhibitory effect of dopamine results in more production of ACh, which triggers a chain of abnormal signaling leading to impaired mobility |
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what type of drugs are prescribed for Parkinson's? |
1.Dopaminergic agents 2. anticholinergic agents (block ACh receptors) |
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what is the #1 drug for Parkinson's? |
Levodopa-Carbidopa (Sinemet) |
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MOA of Levodopa |
Levodopa is the precursor of dopamine. able to cross the BBB into CNS and convert to dopamine |
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why must Levodopa must be given with _______? |
to decrease the SE; Carbidopa |
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SE of Levodopa |
anorexia, N/V, tachycardia, HYPOTENSION, psychiatric problems (depression gets worse) |
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what drug only works for about 5 years so that you might want to save it at a later time when the disease is more progressed? |
Levodopa-Carbidopa (Sinemet) |
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what drug can have sedative effects and cause insomnia? |
Levodopa-Carbidopa (Sinemet) |
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what is the On-Off phenomenon? what drug has the On-OFF phenomenon? |
chronic therapy which the drug can potentially lead to abrupt, unpredictable, and transient motor fluctuations (from mobility to immobility)
Levodopa/Carbidopa (Sinemet) |
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SE of Ropinirole (Requip) and Pramipexole (Mirapex) |
insomnia nausea auditory hallucinations dizziness constipation ORTHOSTATIC HYPOTENSION |
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what else is Pramipexole used for? |
Restless Leg Syndrome (RLS) |
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MOA of Amantadine |
-increase dopamine release -blocks cholinergic receptors -inhibits NMDA glutamate recepetors |
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what was Amantadine originally used for? |
bird flu
also effective for MS but not as effective as w/ Parkinson
|
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SE of Amantadine |
confusion, agitation, hallucinations
*once experiencing hallucinations, take the pt. off the drug immediately* |
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What drug is good to start early tx of Parkinson's? What drug is good for later tx? |
1. Amantadine 2. Sinemet |
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what drug helps control mobility of Parkinson's? |
Amantadine |
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what Parkinson's drugs are not anymore? |
Congentin and Artane |
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what Parkinson drug is CI for cardiovascular issues? |
Selegiline |
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If the patient forgot to take Sinemet and have acute, extreme ridigity, what drug is useful at this time? |
Apomorphine (Apokyn) |
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patho of Alzheimer's |
1. senile plaques (beta-amyloid accumulations) 2. neurofibrillary tangles 3. loss of cortical cholinergic |
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how do you diagnose Alzheimer's? |
autopsy |
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What is the most commonly used drug to tx Alzheimer's? |
Donepezil (Aricept) |
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MOA: Donepezil (Aricept) Galatamine (Razadyne) Rivastigmine (Exelon)
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acetylcholinesterase inhibitor= improve cholinergic transmission |
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which Alzheimer's drug has a long-acting patch for pts who forget to take their meds? |
Rivastigmine (Exelon) |
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SE: Donepezil (Aricept) Galatamine (Razadyne) Rivastigmine (Exelon) |
-N/V/D -anorexia -MYALGIA -BRADYCARDIA -tremors |
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which Alzheimer drug is a NMDA receptor antagonist? |
Memantine (Nemenda)
blocks NMDA receptor and limits Ca+ influx into the neuron |
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what do you start Alzheimer's patients with? what drug do you give later when the disease has progressed or the drug is no longer working? |
1. AChesterase inhibitor (Donepezil) 2. Namenda + Achesterase inhibitor |
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name the disease modifying drugs for MS |
1. Fingolimod (Gilenya) 2. Interferons- Beta 1a (Avonex) or Beta 1b (betaseron) 3. Glatiramer acetate (Copaxone) 4. Teriflunomide (Aubagio) 5. Dimetyl fumarate (Tecfidera) |
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MOA of Gilenya |
alters lymphocyte migration
pill form |
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why should patients tell their PCP that they are on Gilenya? |
VERY LOW WBC |
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MOA of Interferons |
all help to diminish inflammatory response |
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Beta 1a (Avonex) |
interferon- IM injecction qwk |
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what was the 1st MS drug on the market in 1993? |
Interferon Beta 1b (Betaseron) given subQ qod |
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MOA of Copaxone |
synthetic polypeptide that resembles myelin protein and acts as a decoy for T cell to attack |
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how often is copaxone given? |
daily SubQ injection |
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what is the #1 drug prescribed for MS? |
Copaxone |
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what drug is the only category B for MS? |
Copaxone |
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MOA of Aubagio |
pyrimidine synthesis inhibitor that leads to lower concentration of active lymphocytes in CNS |
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what stage is Aubagio mainly used for? |
secondary progressive- pill form |
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MOA of Tecfidera |
alters cell response to oxidative stress to reduce disease progression |
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SE of Tecfidera |
N/V HEMATEMESIS→ reduce dosage |
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name the MS immunosuppressants |
Natalizumab (Tysabri) Mitoxantrone (Novantrone) |
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Describe Tysabri. when do you give it? |
monoclonal antibody therapy NOT THE 1ST LINE OF TX IV DRUG ONCE A MONTH GIVEN WHEN PTS ARE NOT RESPONSIVE TO OTHER DRUGS OR FOR PROGRESSED PTS |
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what drug do you not give to MS pts? why? |
Novatrone. KILLS PEOPLE. |