Flashcards in Pharm Deck (115):
Drugs for Parkinson?
What worsens Parkinsons?
increasing Ach, decreasing Dopamine
What is the goal of Parkinson pts?
Parkinson-What is the last resort drug?
issue b/c if used early on, there is no tx for long term
Parkinson - BBB issue?
Dopamine itself does NOT pass the BBB - drugs must pass the BBB and THEN convert to dopamine
What drugs for rigidity and akinesia?
What drug helps w/ tremors?
What does GABA do?
slows neurological movement down
Parkinson - What happens to GABA?
There is no dopamine so there is a GREAT increase of Ach --> hypokinesia
What is Benztropine doing to GABA?
blocks Ach so it can decrease Ach --> improve movement (tremor and drooling)
Is Benztropine better or Levodopa?
Benztropine is not as effective as Levodopa BUT "start low and slow" (Levodopa is NOT first line)
mostly anticholinergic (dec Ach) but may also incr dopamine
helps w/ tremors NOT rigdity and akinesia
DO NOT USE IN ELDERLY (cognitive probs - over 70yo) - use Levodopa instead
"mad as a hatter"
"blind as a bat"
"dry as bone"
"red as a beet"
Benztropine - how to dec ADRs?
titration is needed "start low and slow"
Benztropine - who do you avoid?
Benztropine - DI?
anything w/ anticholinergic effect (benadryl)
-helps promote Dopamine from the synapse and inhibits reuptake
-increasing Dopamine and decreasing Dopamine that is reabsorbed
-helps w/ Parkinson sx
-can be used w/ Levodopa (helps w/the fluctuation of the half life)
-pts can build a tolerance --> drug holiday (bursts of the drug)
-MUST taper off (esp during the drug holiday)- do not stop abruptly
What is the point of using Benztropine and Amantadine?
to delay the use of Levodopa
Monoamine Oxidase inhibitors?
-can increase dopamine levels
-prevent free radicals
MAO - B inhibitors ADR?
CNS irritation (sleepiness, depression)
Apomorphine, Bromocriptine, cabergoline?
-bind to dopamine receptors
-can be used alone or supplemental (use less Levodopa if used together)
-helps w/ fluctuations of levodopa
Dopamine agonist -ADR?
CNS issues (hallucination, confusion, fainting, syncope)
peripheral edema (thiazide)
drink w/ water
RLS if removed abruptly
prodrug (not active until metabolized)
metabolized in GI
given w/ carbidopa
How does Levodopa and Carbidopa work together?
Levodopa - 1-3% to the brain
+ Carbidopa - 10% to the brain
motor skills are impaired
intitaion of therapy is individualized
GI issues (N&V) - can take w/ food but efficacy goes down
behavioral effects (depression, anxiety)
resistance of the drug
Levodopa half life?
wearing off (efficacy goes away) --> "on and off" motor fluctuations
can give together w/ MAO B inhibitor
honey moon (no sx) - 3 yrs
wearing off - 3-5 yrs
on - off dyskinesia -5-10yrs
*drug holidays does not help-DO NOT DO
dopamine agonist can worsen ADR
MAO I used for depression
increases dopamine in the brain
increases Levodopa to the brain
prevents breakdown of dopamine in the brain
helps fluctuations of Levodopa
COMT inhibitors - labs?
watch liver enzymes
Tension headache - sx?
upper back and neck
base of head
ears, above ears
above the eyes
What to keep in mind when tx HA and drugs?
episodic HA can turn into chronic headache - d/t meds (rebound)
can be drug withdrawal headache
earlier the better
OTC: excedrin extra strength - first line
triptan (sumatriptan, rizatriptan) - "second line" but first line w/ migraine is severe
abortive NOT prophylactic
faster the better
selective 5HT 1D and 2B agonist --> interrupts the pain signal through the trigeminal nerve)
first triptan, cheapest
not as effective as Rizatriptan
more lipophilic than sumatriptan, more effective
Sumatriptan and Rizatriptan ADR?
vasoconstrictor: coronary artery spasm, MI, CVA
Sumatriptan and Rizatriptan DI?
skip the GI absorption, etc --> sublingual, nasal
vasoconstricts - decreased blood flow to extremities and decreases pulsatile headache
like triptan but not as effective
add caffeine to increase efficacy
Ergot Alkaloids ADR?
toxicity (Nausea, diarrhea, constipation, etc)
do not use in pregnancy
Ergo alkaloid forms?
Migraine prophylactic management criteria?
migraine is so bad that it disrupts daily activities
more than 2x/mo
Migraine prophylactic goal?
Migraine prophylactic management - is it working?
Migraine prophylactic drugs?
Cluster HA - tx?
abortive - triptans, erogtamines
100% if avail
Prophylactic cluster HA drugs?
Prevention of recurrent stroke?
Tx RF: HTN, diabetes, lipids
antiplatelet therapy (ASA)
Ischemic stroke - tx?
tPA - if able to use
TIA - tx?
do not jump to tPA - unless you can prove to be a stroke
ASA! - long term
Common cx of bacterial meningitis?
1) Neisseria Meningitidis (places w/ mold and high humidity) - multiply in nasal mucous
Population of the bacterial meningitis?
Polio - sx?
variable (some people are asymptomatic)
two doses are reommended
now is inactive vaccine (live vaccine is out)
total of 4 doses
Neuropathic pain - cx?
inflammation of infxn
not like regular pain
can cause damage to nerves
Neurological pain - tx?
mitigate the pain, not completely tx (tolerable pain)
start low and slow
ibuprofen, acetaminophen, et do not work
TCAs, SNRIs, topical lidocaine, opioids, NA ch blockers, anticonvulsants - Gabapentin* and Pregabalin*
neuropathic pain - esp postherpetic neuralgia and polyneuropathies
relieve atypical pain
insomnia (can help w/ comorbidities)
Gabapentin and Pregabalin ADR?
used for diabetics
insomnia and anxiety (helps w/ comorbidities)
tPA is good until?
neuropathetic pain -tx?
NOT NSAID, acetaminophen
Low Ach levels?
Parkinson AND dementia?
parkinson - give anticholinergic (brings down Ach)
BUT dementia too? (you want to increase Ach)
teeter totter - balance!
Antiepileptic drugs used for?
prevent epilepsy (unprovoked)
1st seizure? Then 2nd one will occur..?
within the next 2 yrs
Goal of epilepsy?
tx underlying trigger and avoid
well used in peds
Most effective anticonvulsants?
Valproic acid but not well tolerated
Well tolerated anticonvulsants?
Lamatrigine but not as effective as valproic acid
What to keep in mind for pts taking anticonvulsants?
depresses CNS so suicide rate goes up
diazepam and lorazepam
How does anticonvulsant work?
enhancing GABA abilities
opens up Cl channels --> slows down the signaling (inhibitory) --> enhances GABA effects
Drug classification foor Diazepam and Lorazepam?
Does benzodiazepine increase GABA?
no, just enhances the effectiveness of GABA
How does benzodiazepine work?
anxiety - small dose
sedation - little more
loss of consciousness/hypnosis - heavy dose
Benzodiazepine - ADR?
CNS depression - sedation, drowsiness
dependence: NOT GOOD FOR LONG TERM; ONLY FOR SHORT TERM
CARDIOPULM pts - respiratory/cardio depression
Benzodiazepine - DI?
other CNS depressants
CYP 450 - liver
anticonvulsant - first gen
inhibits repetitive firing by blocking Na channels
Carbamazepine - important labs to check?
check HLA in asians
Carbamazepine - what kind of characteristics does it have?
Carbamezpine - ADR?
bone marrow depression
Carbamazepine - DI?
CYP450 and inducer (speeds up metabolism) - CHECK OTHER DRUGS
do not stop abruptly
used for partial seizures
serum levels - CBCs, LFTs (liver toxicity) HLA
Phenytoin - ADR?
Phenytoin - DI
CYP 450 and inducer
Valproate (Valporic acid) - drug use?
first generation anticonvulsant
Valproate - labs?
serum levels - LFT CBC
Valproate - ADR?
do not chew meds
hyperammonemia (encephalopathy can occur)
anticonvulsant second generation
prophylactic for cluster HA
Na channel blocker
*glutamiate (opp of GABA - excitatory part of the brain) inhibitor
Topiramate - ADR?
loss of appetite
Topiramate - DI?
CYP 450 inducer
hypersensitivity (esp if they're young and HD)
Lamotrigine - DI?
decrease in Ach
Alzheimer dz drugs?
acetyl cholinesterease inhibitor
Donezepil -drug use?
reversible acetyl cholinesterase inhibitor
Donezepil - when to take? what to monitor?
HR and BP
Donezepil - ADR?
GI - diarrhea, loss of appetite
HTN --> AV block, seizures, syncope
Donezepil - DI?
used for severe Alzheimer
Glutimate inhibitor - blocks the excitatory part of the brain
helps w/ memory fxn
balance and coordination
can be addictive