Pharm Flashcards
What worsens Parkinsons?
meds (antinauseua)
increasing Ach, decreasing Dopamine
Drugs for Parkinson?
Benztropine
Levodopa/Carbidopa
What is the goal of Parkinson pts?
Increasing Dopamine
Decreasing Ach
Parkinson-What is the last resort drug?
Levodopa/Carbidopa
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?
Amontadine
What drug helps w/ tremors?
Anticholingeric (Benztropine)
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)
Benztropine MOA?
mostly anticholinergic (dec Ach) but may also incr dopamine helps w/ tremors NOT rigdity and akinesia
Benztropine ADR?
DO NOT USE IN ELDERLY (cognitive probs - over 70yo) - use Levodopa instead orthostasis delirium constipation "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?
Alzheimer’s
Dementia
Cognitive issues
Elderly
Benztropine - DI?
ADR duplication
anything w/ anticholinergic effect (benadryl)
Amantdaine?
- antiviral
- helps promote Dopamine from the synapse and inhibits reuptake
- increasing Dopamine and decreasing Dopamine that is reabsorbed
- neuroprotective benefits
- helps w/ Parkinson sx
- can be used w/ Levodopa (helps w/the fluctuation of the half life)
Amantadine ADR?
- 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?
- parkinson
- can increase dopamine levels
- prevent free radicals
MAO - B inhibitors ADR?
CNS irritation (sleepiness, depression)
N&V&D
Constipation
syncope
Apomorphine, Bromocriptine, cabergoline?
- bind to dopamine receptors
- dopamine agonist
- metabolized differently
- can be used alone or supplemental (use less Levodopa if used together)
- young pts
- helps w/ fluctuations of levodopa
Dopamine agonist -ADR?
CNS issues (hallucination, confusion, fainting, syncope) constipation, diarrhea peripheral edema (thiazide) drink w/ water RLS if removed abruptly
Levodopa/Carbidopa?
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
Levodopa/Carbidopa population?
cognitive impairment
elderly
motor skills are impaired
intitaion of therapy is individualized
Levodopa ADR?
GI issues (N&V) - can take w/ food but efficacy goes down postural hypotension irreversible dyskinesias behavioral effects (depression, anxiety) resistance of the drug
Levodopa half life?
90 min
wearing off (efficacy goes away) –> “on and off” motor fluctuations
can give together w/ MAO B inhibitor
Levodopa timeline?
honey moon (no sx) - 3 yrs
wearing off - 3-5 yrs
on - off dyskinesia -5-10yrs
*drug holidays does not help-DO NOT DO
Levodopa DI?
dopamine agonist can worsen ADR
ADR duplication
MAO I used for depression
COMT inhibitors?
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 jaw above the eyes
What to keep in mind when tx HA and drugs?
episodic HA can turn into chronic headache - d/t meds (rebound)
HA -cx?
DRUGS!
can be drug withdrawal headache
Acetaminophen ADR?
alcohol
hypersensitivity
Migraine tx?
earlier the better
OTC: excedrin extra strength - first line
triptan (sumatriptan, rizatriptan) - “second line” but first line w/ migraine is severe
Sumatriptan ADR?
N&V
Triptan MOA?
abortive NOT prophylactic
faster the better
selective 5HT 1D and 2B agonist –> interrupts the pain signal through the trigeminal nerve)
Sumatriptan MOA?
first triptan, cheapest
not as effective as Rizatriptan
Rizatriptan MOA?
more lipophilic than sumatriptan, more effective
Sumatriptan and Rizatriptan ADR?
bad taste GI upset dizziness vasoconstrictor: coronary artery spasm, MI, CVA seizure blindness hypersensitivity
Sumatriptan and Rizatriptan DI?
ADR duplication
Triptan forms?
oral (cheapest)
skip the GI absorption, etc –> sublingual, nasal
Ergot alkaloids?
abortive vasoconstricts - decreased blood flow to extremities and decreases pulsatile headache like triptan but not as effective faster, better add caffeine to increase efficacy
Ergot Alkaloids ADR?
rebound HA
toxicity (Nausea, diarrhea, constipation, etc)
do not use in pregnancy