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56 Cards in this Set

  • Front
  • Back

what kind of drugs can cross the BBB?

lipid-soluble

what kind of drugs can't cross the BBB?

protein bound and highly ionized drugs

what is tolerance?

decreased response occurring in the course of prolonged drug use

what is physical dependence?

state in which abrupt discontinuation of drug use will precipitate a withdrawal syndrome

give 2 examples that are excitatory NT (depolarization)

ACh and Glutamic Acid

binding of ACh to the post synaptic receptors causes the release of what?

Na+ ions

what is the excitatory pathway?

stimulation of excitatory neurons results in depolarization of the postsynaptic membrane

what is the inhibitory pathway?

stimulation of inhibitory neurons results in HYPERPOLARIZATION of the post synaptic membrane

name 2 inhibitory NT that causes hyperpolarization

GABA and Glycine

Binding of the inhibitory NT ______ or _______ causes entrance of ________ and ______ which makes it more hyperopolarizable.

GABA, Glycine, K+ and Cl-

What is Parkinson's disease?

d/o of EP system= dyskinesias

name the 3 main characteristics of Parkinson's

tremor at rest (supinate and pronate tremor), postural instability, and bradykinesia

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

what type of drugs are prescribed for Parkinson's?

1.Dopaminergic agents


2. anticholinergic agents (block ACh receptors)

what is the #1 drug for Parkinson's?

Levodopa-Carbidopa (Sinemet)

MOA of Levodopa

Levodopa is the precursor of dopamine. able to cross the BBB into CNS and convert to dopamine

why must Levodopa must be given with _______?

to decrease the SE; Carbidopa

SE of Levodopa

anorexia, N/V, tachycardia, HYPOTENSION, psychiatric problems (depression gets worse)

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)

what drug can have sedative effects and cause insomnia?

Levodopa-Carbidopa (Sinemet)

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)

SE of Ropinirole (Requip) and Pramipexole (Mirapex)

insomnia


nausea


auditory hallucinations


dizziness


constipation


ORTHOSTATIC HYPOTENSION

what else is Pramipexole used for?

Restless Leg Syndrome (RLS)

MOA of Amantadine

-increase dopamine release


-blocks cholinergic receptors


-inhibits NMDA glutamate recepetors

what was Amantadine originally used for?

bird flu



also effective for MS but not as effective as w/ Parkinson



SE of Amantadine

confusion, agitation, hallucinations



*once experiencing hallucinations, take the pt. off the drug immediately*

What drug is good to start early tx of Parkinson's? What drug is good for later tx?

1. Amantadine


2. Sinemet

what drug helps control mobility of Parkinson's?

Amantadine

what Parkinson's drugs are not anymore?

Congentin and Artane

what Parkinson drug is CI for cardiovascular issues?

Selegiline

If the patient forgot to take Sinemet and have acute, extreme ridigity, what drug is useful at this time?

Apomorphine (Apokyn)

patho of Alzheimer's

1. senile plaques (beta-amyloid accumulations)


2. neurofibrillary tangles


3. loss of cortical cholinergic

how do you diagnose Alzheimer's?

autopsy

What is the most commonly used drug to tx Alzheimer's?

Donepezil (Aricept)

MOA:


Donepezil (Aricept)


Galatamine (Razadyne)


Rivastigmine (Exelon)



acetylcholinesterase inhibitor= improve cholinergic transmission

which Alzheimer's drug has a long-acting patch for pts who forget to take their meds?

Rivastigmine (Exelon)

SE:


Donepezil (Aricept)


Galatamine (Razadyne)


Rivastigmine (Exelon)

-N/V/D


-anorexia


-MYALGIA


-BRADYCARDIA


-tremors

which Alzheimer drug is a NMDA receptor antagonist?

Memantine (Nemenda)



blocks NMDA receptor and limits Ca+ influx into the neuron

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

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)

MOA of Gilenya

alters lymphocyte migration



pill form

why should patients tell their PCP that they are on Gilenya?

VERY LOW WBC

MOA of Interferons

all help to diminish inflammatory response

Beta 1a (Avonex)

interferon- IM injecction qwk

what was the 1st MS drug on the market in 1993?

Interferon Beta 1b (Betaseron)


given subQ qod

MOA of Copaxone

synthetic polypeptide that resembles myelin protein and acts as a decoy for T cell to attack

how often is copaxone given?

daily SubQ injection

what is the #1 drug prescribed for MS?

Copaxone

what drug is the only category B for MS?

Copaxone

MOA of Aubagio

pyrimidine synthesis inhibitor that leads to lower concentration of active lymphocytes in CNS

what stage is Aubagio mainly used for?

secondary progressive- pill form

MOA of Tecfidera

alters cell response to oxidative stress to reduce disease progression

SE of Tecfidera

N/V


HEMATEMESIS→ reduce dosage

name the MS immunosuppressants

Natalizumab (Tysabri)


Mitoxantrone (Novantrone)

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

what drug do you not give to MS pts? why?

Novatrone. KILLS PEOPLE.