Term
| Stimulation results in depolarization of postsynaptic membrane |
|
Definition
|
|
Term
| stimulation results in a hyperpolarization of the postsynaptic membrane |
|
Definition
|
|
Term
| The CNS contains more/less different types of neurotransmitters than the autonomic nervous system |
|
Definition
|
|
Term
| Neurotransmitters of the CNS types |
|
Definition
|
|
Term
|
Definition
| altering neurotransmission |
|
|
Term
| Drugs interfere what two ways |
|
Definition
| pre-synaptically or post-synaptically |
|
|
Term
| Information transmission requires.. |
|
Definition
release of neurotransmitters
(which bind post synaptic neuron receptors) |
|
|
Term
| How many neurotransmitters used |
|
Definition
|
|
Term
These neurons use neurotransmitters such as Glutamate, and Ach to open Na+ channels causing depolarization with generation of action potentials. |
|
Definition
| excitatory post synaptic potentials (EPSPs) |
|
|
Term
| these use GABA or glycine to allow K+ efflux or Cl- influx causing hyperpolarization with inhibiton of action potential generation |
|
Definition
| inhibitory post synaptic potentials (IPSPs) |
|
|
Term
| Types of neurotransmitters |
|
Definition
biogenic amines
amino acids
peptides
other |
|
|
Term
|
Definition
|
|
Term
|
Definition
serotonin (5HT)
catecholamines |
|
|
Term
|
Definition
|
|
Term
| Ach is excitatory/inhibitory? |
|
Definition
|
|
Term
Binds nicotinic and muscarinic receptors
involved in movement, balance, and cognition |
|
Definition
|
|
Term
| serotonin is excitatory/inhibitory? |
|
Definition
|
|
Term
| involved in mood regulation (anxiety and depression), psychosis, and eating disorders |
|
Definition
|
|
Term
| Types of norepinephrine neurotransmitters |
|
Definition
|
|
Term
excitatory
causes increase in sympathetic outflow |
|
Definition
|
|
Term
| alpha 1 is postsynaptic/presynaptic |
|
Definition
|
|
Term
inhibitory
causes inhibition of sympathetic outflow
involved in mood regulation (locus caeruleus) |
|
Definition
|
|
Term
| alpha 2 is presynaptic/postsynaptic |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| Dopamine plays large role in.. |
|
Definition
|
|
Term
|
Definition
|
|
Term
Excitatory to virtually ALL neurons
NMDA and non-NMDA receptors |
|
Definition
|
|
Term
inhibitory
mainly spinal cord |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
enkaphalins
endorphins
substance P, ect |
|
|
Term
|
Definition
|
|
Term
| Target areas for treatment |
|
Definition
receptor agonists or antagonists
reuptake inhibition
inhibited metabolism
presynaptic actions
neurotransmitter balance |
|
|
Term
|
Definition
SSRI
TCAs
(indirect agonists) |
|
|
Term
|
Definition
MAOI
Acetylcholinesterase
(indirect agonists) |
|
|
Term
|
Definition
production
storage
termination
receptors |
|
|
Term
Parkinson's disease is a progressive neurologic disorder of muscle movement characterized by:
|
|
Definition
tremors
muscular rigidity
bradykinesia
postural & gait abnormalities |
|
|
Term
| Death in parkinson's is due to.. |
|
Definition
complications related to immobility
(arteriosclerotic heart disease, bronchopneumonia, and cerebrovascular disease) |
|
|
Term
| Reduced activity of inhibitory dopaminergic neurons in substantia nigra & corpus striatum |
|
Definition
|
|
Term
| Parknson's Diease : Following viral encephalitis or multiple vascular lesions (infrequent), certain drug therapies - Haloperidol |
|
Definition
|
|
Term
| NOT primarily genetic, may increase susceptibility |
|
Definition
|
|
Term
| You treat parkinson's by replacing.. |
|
Definition
| dopamine and restoring balance |
|
|
Term
|
Definition
| excitatory cholinergic (M) neuron |
|
|
Term
| Loss of dopamine increases.... |
|
Definition
| basal neural tone to skeletal muscles decreasing voluntary action |
|
|
Term
| Clinical presentation of parkinson's disease |
|
Definition
tremor - pill-rolling involving thumb and index finger
rigidity-cogwheel or ratchet type movements
bradykinesia- spontaneous movement
postural diturbances - stooped posture |
|
|
Term
Drug induced
Dopamie Receptor blockers |
|
Definition
|
|
Term
| Focal points for treatment of parkinson's |
|
Definition
levadopa/carbidopa (Sinemet)
amantadine (Symmetrel)
MAO-B inhibitors
COMT inhibitors
Dopamine agonists
Antimuscarinic agents |
|
|
Term
|
Definition
|
|
Term
| DOPA Decarboxylase causes peripheral decarboxylation (97% lost) |
|
Definition
|
|
Term
| Levodopa with ______ (increases bioavailability) only 90% lost |
|
Definition
|
|
Term
| Patients normally respond favorably to levodopa for 3-5 years then the effects start to decline |
|
Definition
| honeymoon period of taking levodopa |
|
|
Term
| Take this drug on empty stomach |
|
Definition
|
|
Term
| No pyridoxine (vidamin B6) |
|
Definition
|
|
Term
| 1/2 life is short so frequent dosing (tid - qid) |
|
Definition
|
|
Term
| Does dopamine cross the BBB?? |
|
Definition
|
|
Term
| _____ is a dopamine precursor |
|
Definition
|
|
Term
| Interaction with antipsychotic (dopamine receptor blockers) and MAOI- A causes... |
|
Definition
|
|
Term
| Side effects of Levodopa/Carbidopa (Sinemet) |
|
Definition
hypotension
arrhythmias
glaucoma (mydriasis)
N/V, anorexia
psychosis
dyskinesias |
|
|
Term
On and off periods with long term therapy
sometimes works, sometimes it doesn't |
|
Definition
|
|
Term
Started with meal or snack to reduce GI discomfort
Motilium, Tigan, Zofran |
|
Definition
| given to help with N/V, anorexia effects of levodopa/carbidopa |
|
|
Term
| Concern with increase in gambling, binge eating, shopping, hyper-sexuality are side effects of.... |
|
Definition
|
|
Term
| Depression, agitation, insomnia, somnolence, confusion, hallucinations |
|
Definition
| psychosis side effects of levodopa/carbidopa |
|
|
Term
| inhibits MAO-B (metabolizes dopamine) |
|
Definition
|
|
Term
| MAO- B does not inhibit MAO-A (NE and Serotonin) except at high doses so it does NOT cause... |
|
Definition
|
|
Term
| However, high doses of _____ may cause severe HYPERtension |
|
Definition
|
|
Term
Last dose should be early afternoon to prevent insomnia
(metabolised to amphetamine) |
|
Definition
|
|
Term
Incorportate early in tx
(delay severe symptom onset by 50%) |
|
Definition
|
|
Term
| Decreases dosage of l-dopa needed |
|
Definition
|
|
Term
| Irreversibly inhibits MAO-B |
|
Definition
|
|
Term
| Used both as initial monotherapy as well as in combination with Levodopa |
|
Definition
|
|
Term
| May provide better neuroprotective effect than Selegiline as the later is metabolized to amphetamine derivatives that may be neurotoxic |
|
Definition
|
|
Term
| 2x as expensive a Selegiline |
|
Definition
|
|
Term
MOA: Prevents metabolism of levodopa to 3-O-MethylDOPA (competes with l-DOPA for BBB transport) therefore increases the amount of L-DOPA available. Use only as ‘add-on’ with l-dopa
|
|
Definition
|
|
Term
| Decreases on off phenomenon |
|
Definition
|
|
Term
AE: Similar to levodopa/carbidopa
Diarrhea, dyskinesias, nausea, postural hypotension, anorexia, and hallucinations |
|
Definition
|
|
Term
| Fatal hepatotoxicity - availabe in US/ not Canada- Limited use |
|
Definition
|
|
Term
| Combination LevoDopa + Carbidopa + Entacapone |
|
Definition
|
|
Term
| Act directly on postsynaptic dopamine receptors |
|
Definition
|
|
Term
| Dopamine agonist are less effective than ...... |
|
Definition
| levodopa for motor symptoms of PD |
|
|
Term
| Are effective for patients experiencing long-term problems with levodopa |
|
Definition
|
|
Term
|
Definition
|
|
Term
| D1 family dopamine receptors |
|
Definition
D1 and D5
uncertain action |
|
|
Term
|
Definition
D2, D3, and D4
stimulation of D2 family improves rigidity and bradykinesia |
|
|
Term
|
Definition
|
|
Term
| Selective Dopamine agonists |
|
Definition
|
|
Term
| Bromocriptine is classifed as... |
|
Definition
dopamine agonist
non- selective
ergot derivative |
|
|
Term
| Add on therapy with l-dopa/carbidopa |
|
Definition
|
|
Term
| 5HT mimetic so pulmonary and retroperitoneal fibrosis is a concern |
|
Definition
|
|
Term
| Abnormal pulmonary examination should trigger a chest x-ray |
|
Definition
bromocriptine
pulmonary and retroperitoneal fibrosis is a concern |
|
|
Term
Limited by poor side effect profile
CNS
GI
CV
Dyskinesias |
|
Definition
|
|
Term
| AE - CNS - hallucinations, confusion, delirium |
|
Definition
|
|
Term
| GI- N/V, GERD, ulcers - take with meals |
|
Definition
|
|
Term
| CV- orthostatic hypotension, MI, peripheral vasospasm, arrhythmias |
|
Definition
|
|
Term
Contraindications: Previous MI, peripheral vascular disease, uncontrolled HTN, HTN-pregnancy, potential for abortion, and ulcers. |
|
Definition
|
|
Term
| Dyskinesias are less common than with levodopa |
|
Definition
|
|
Term
| Non-ergoline compounds and bind specifically to the D2 receptor |
|
Definition
| Pramipexole, Ropinirole, Rotigotine |
|
|
Term
| Less effective than levodopa against motor- symptoms |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
| These are now the recommended first line monotherapy for most symptomatic patients for Parkinsons |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
| may delay need for levodopa for several years |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
| Rotigotine is what type of administration? |
|
Definition
|
|
Term
| Do not exacerbate peripheral vasospasm nor induce retroperitoneal fibrosis like bromocriptine |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
| less dyskinesia than with levadopa |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
| Adverse effects - N, vertigo, orthostatic hypotension, insomnia, somnolence |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
| increase in gambling binge eating, shopping, hyper-sexuality |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
do not use in patient with dementia
caution with CNS depressents |
|
Definition
| pramipexole, ropinirole, rotigotine |
|
|
Term
|
Renal dependent excretion, cimetidine (inhibits renal secretion of weak-bases) can greatly reduce renal excretion.
|
|
Definition
|
|
Term
|
Definition
|
|
Term
| Apomorphine is used for... |
|
Definition
| episodes of immobility "off-episodes" |
|
|
Term
| Apomorphine is classified as... |
|
Definition
| non-ergot dopamine agonist |
|
|
Term
Used for advanced parkinson disease
only IV |
|
Definition
|
|
Term
| to prevent apomorphine-induced emesis |
|
Definition
| Trimethobenzamide (Tigan-antihistamine) |
|
|
Term
| Can only use the antihistamine Tigan with the apomorphine NOT with |
|
Definition
5HT3 antagonists
because severe hypotension with loss of consciousness can result |
|
|
Term
| anti-viral used to treat influenze |
|
Definition
|
|
Term
| MOA - enhances synthesis, release, or re-uptake of dopamine from surviving neurons |
|
Definition
|
|
Term
| Amantadine is classified as |
|
Definition
| cholinergic receptor antagonist |
|
|
Term
|
Definition
| glutamate receptor antagonist |
|
|
Term
depends on surviving neurons
no effect if dopamine release at max |
|
Definition
|
|
Term
| Effectiveness: Rigidity, bradykinesia > tremor |
|
Definition
|
|
Term
| Not as affective for tremors as it is with bradykinesia |
|
Definition
|
|
Term
AE - CNS - restlessness, insomnia, agitation, confusion, hallucinations, psychosis
Peripheral complaints - orthostatic hypotension, urinary retention, dry mouth |
|
Definition
|
|
Term
| Amantadine adverse effects are consistent with the other... |
|
Definition
|
|
Term
|
Definition
Benztropine
Trihexyphenidyl
Biperiden |
|
|
Term
Effectiveness: tremor, drooling > bradykinesia
Adjuvant only << effective than l-dopa |
|
Definition
|
|
Term
| MOA: block excitatory muscarinic receptors to restore balance with dopamine |
|
Definition
|
|
Term
| only useful in mild disease, early on |
|
Definition
|
|
Term
| Adverse effects: pupil dilation, confusion, urinary retention, dry mouth & hallucinations |
|
Definition
|
|
Term
| avoid with glaucoma, BPH, & pyloric stenosis |
|
Definition
|
|
Term
| About ___ of patients with Parkinson's will have hallucinations |
|
Definition
|
|
Term
| Stop medications that may contribute to psychosis in the following order-- |
|
Definition
anticholinergics
amantadine
selegiline
dopamine agonists
levadopa/carbidopa |
|
|
Term
| Treat hallucinations with.. |
|
Definition
atypical antipsychotic/neuroleptic
seroquel NOT haloperidol (can cause drug-induced Parkinson's) |
|
|
Term
| Most effective treatment of Parkinson's disease |
|
Definition
|
|
Term
| Choice of treatment for Parkinson's |
|
Definition
levodopa/carbidopa
dopamine agonists (non-ergot preferred)
MAO-B
COMT inhibitor w/ l-dopa/carb
anticholinergics (rarely)
surgery |
|
|
Term
Neurodegenerative disorder
unknown cause
short term memory loss |
|
Definition
|
|
Term
| loss of cognitive, physical and behavioral control |
|
Definition
|
|
Term
|
Definition
|
|
Term
| Features of alzheimer disease |
|
Definition
accumulation of senile plaque (beta amyloid)
formation of neurofibrillary tangles
loss of cortical cholinergic neurons |
|
|
Term
| Acetylcholinesterase inhibitors treat... |
|
Definition
|
|
Term
| Acetylcholinesterase inhibitor drugs |
|
Definition
donezapril
galantamine
rivastigmine
tacrine |
|
|
Term
| All alzheimers drugs inhibit CYP 450 EXCEPT |
|
Definition
|
|
Term
Adverse Effects – bradycardia, nausea, diarrhea, vomiting, anorexia, tremors, and muscle cramps (know muscarinic and nicotinic and describe which is which) |
|
Definition
acetylcholinesterase inhibitors
alzheimers drugs |
|
|
Term
| NMDA receptor inhibitors are used to treat... |
|
Definition
|
|
Term
The first and only representative of a new class of alzheimer drugs
moderate affinity |
|
Definition
|
|
Term
| Excitotocity - gluatmate overstimulates... |
|
Definition
|
|
Term
Adverse effects : confusion, agitation, restlessness
Indistinguishable from Alzheimer disease |
|
Definition
|
|
Term
| Autoimmune, inflammatory, demylenating disease of CNS |
|
Definition
|
|
Term
| First line treatment for multiple sclerosis |
|
Definition
interferon beta
glatiramer acetate |
|
|
Term
|
Definition
|
|
Term
| Second-line therapies for multiple sclerosis |
|
Definition
anti-inflammatory MOA
corticosteroids, fingolmod, mitoxantrone, Natalizumba, Teriflunomide |
|
|
Term
| Metabolite of the pyrimidine synthesis inhibitor leflunomide |
|
Definition
|
|
Term
Amytrophic lateral sclerosis
(ALS) |
|
Definition
riluzole (NMDA-receptor antagonists)
may increase survival |
|
|
