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deck code: nervouskey
"Note: DA=dopamine, BBB=blood brain barrier, PD=Parkinson's Dz, SE=side effect, pt or pts=patient(s), HA=headache"
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"Generally, what is the purpose of using Carbidopa/Levodopa?"
Increase domamine levels
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MOA of Carbidopa/Levodopa?
"inhibits decarboxylation of peripheral L-dopa, together they cross BBB where L-dopa is converted to DA"
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Indication of Carbidopa/Levodopa?
"Pt's suffering from PD >65 y/o, younger pt's may suffer worse side effects and drug may be less effective"
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Side effects of Carbidopa/Levodopa?
"drug-induced dyskinesias, ""on-off"" motor fluctuations, potentially compulsive behaviors (ie gamble, shop, binge eat)"
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Mechanism of action of Pramipexole and Ropinirole?
"they are DA receptor agonists, they directly stimulate DA receptors"
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Pluses and minuses with Pramipexole and Ropinidole over Carbidopa/Levodopa?
"Pluses: fewer side effects than L-dopa, minuses: less effective than L-dopa"
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Name two older agents that preceded Pramipexole and Ropinidole
Bromocriptine and pergolide- SE include cardiac valve regurgitaion
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Indication of Pramipexole and Ropinidole
monotherapy in PD patients <60yo w mild dz. adjunct therapy with L-DOpa in advanced PD
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SE of Pramipexole and Ropinidole
"dyskinesia and ""on-off"" motor problems (less than L-Dopa), postural hypotension, hallucination, somnolence esp in elderly"
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How is Pramipexole and Ropinidole administered?
Orally
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Apomorphine is a dopamine receptor agonist. How is it administered?
subcutaneously
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What is COMT?
"Catechol-O-methyltransferase is one of several enzymes that degrade catecholamines such as dopamine, epinephrine, and norepinephrine. (Wikipedia)"
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What type of drug is Entacapone and Tolcopone?
PD drug that acts to inhibit COMT
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MOA for entacapone and tolcopone?
inhibit plasma COMT enzyme thereby prolonging T1/2 of L-dopa
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Indication of entacapone and tolcopone?
used along with L-dopa in PD patients
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SIde effects of entacaopone and tolcopone?
elevated liver enzymes for tolcopone. GI sxs and dyskinesias in entacapone
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MOA of trihexiphenidyl?
antimuscarinic agent for patients with PD
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Indication of trihexiphenidyl?
young pts with PD w tremor and drooling
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SE's of trihexiphenidyl?
this is an anticholinergic agent so SEs include cognitive changes
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How is amantidine used in the nervous system?
"although anti-flu agent, also used in mild PD esp in younger pts with bradykinesia. MOA unknown"
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SIde effects of amantidine
confusion and ankle swelling
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MOA of selegine
inhibits catabolism of dopamine in brain
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indication of selegine
"used in early, mild PD"
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MOA for opioids
"agonists for mu, delta and kappa opioid receptors, work through Gi/Go proteins to hyperpolarize neurons and inhibit neurotrans release"
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Indication for for opioids?
"relief of moderate to severe pain, preop med, adjunct during anesthesia. sometimes used as antitussive and antidiarrheal agent"
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Why are opioids judiciously prescribed?
addiction liability
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SE of opioids (these are important to know for exams and for life)
constipation bc of decreased peristalsis
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How is an opiod OD characterized?
"coma, resp depression, pinpoint pupils, hypotension, decreased bowel sounds"
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How do you reverse opioid OD?
Give Naloxone. But risk in withdrawl
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MOA of local anesthetics?
"block Na channels, preventing generation and conduction of nerve impulses"
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Indication of local anesthetics
local and spinal anesthesia and nerve blocks
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SE of local anesthetics
seizures in high doses after intravascular injection or in young kids
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Name 4 examples of local anesthetics
"Lidocaine, procaine, bupivicaine, cocaine"
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Name the DOC for generalized tonic-clinic (grand mal) seizures
valproate or lamotrigine or levetiracetam
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"name the DOC for partial, secondary generalized seizures"
"carbamazepine, lamotriginem oxcarbazepinem, levetiracetam"
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name the DOC for absence seizures (petit mal)
ethosuximide or valproate
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Name the DOCs for atypical absence myoclonic and atonic seizures
"valproate, lamotrigine, levetiracetam"
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Which drug will worsen an absence seaizure?
phenytoin
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why is phenytoin no longer the DOC for generalized tonic-clonic or partial seizures?
"complicated pharmakokinetics, inferior adverse effect profile, frequent drug-drug interations"
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What is the indication of valproate (valproic acid and divalproex)?
anticonvulsant in tonic-clonic seizures as well as atypical absensem myoclonic and atonic seizures (also used as mood stablizer)
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What is the mode of action of valproate?
increases levels of GABA in the brain
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side effects of valproate?
"most common SE is nausea/vom, which can be limited by taking enteric coated form (depakote), or take w food or by slow titration. weight gain is relatively common. hepatotoxicity esp in <2yo"
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what is the indication for lamotrigine?
"anticonvulsant in most seizures except absence. monoRx in select adults, adjunct Rx in adults and kids >2. valproate decreases its clearance"
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SE of lamotrigine?
"rash- diffuse or severe (stevens-johnson synd, aka toxic epidermal necrolysis), often as a result of rapid administration or combo with valproate"
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What is the indication for levetiracetam?
"anticonvulsant: pt's >4 with partial seizures, pts >6 with primary generalized seizures, and pts >12 with myoclonic seizures"
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MOA of levetiracetam?
"binds selectively to synaptic vesicular protein SV2A, modifying release of glutamate and GABA"
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SE of levetiracetam?
"somnolence, dizziness, weakness and irritability. few drug interactions since not metab by CYP450"
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What is the indication for carbamazine?
anticonvulsant: Partial and secondary generalized seizures. also to treat trigeminal neuralgia and diabetic neuropathy
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MOA for carbamazine?
reduces polysynaptic responses and blocking post tetanic potentiation.
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SE for carbamazine?
"rashes, esp in high doses. high risk for Stevens Johnson synd (toxic epidermal necrolysis) for Asians. CNS sxs- HA, drowsiness and decreased cognitive function"
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"When treating absence seizures with carbamazine, SE may include..."
"mild leukopenia, hyponatremia and drug drug interaction"
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What is the indication for oxycarbamazine?
"like carbamazine, anticonvulsant: Partial and secondary generalized seizures. also to treat trigeminal neuralgia and diabetic neuropathy"
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What is the indication for ethosuximide?
anticonvulsant for absence (petit mal) seizures
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What are the side effects of ethosuximide?
"usually well tolerated although some nausea/vom, hiccups"
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What's the MOA for phenytoin?
"may block Na channels, stablizing threshold against hyperexitablility. may block Ca channels and enhance HABA"
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What's the former name of phenytoin?
dyphenylhydantoin
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Indication for phenytoin?
"no longer DOC for generalized tonic clonic seizures due to pharmacokinetic, adverse profile, drug interactions"
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SE of phenytoin?
"nystagmus, drowsiness, ataxia, diplopia, rash, gingival hyperplasia"
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Indication for gabapentin?
"used in combination therapy for convulsions, also used in pain syndromes and psych disorders"
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drug interactions for gabapentin?
few drug interaction
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Indication for topiramate?
"adjuvent therapy for seizures, prophylaxis for migraines, treat neuropathic pain"
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SEs for topiramate?
"parasthesias, cognitive impairment. metabolic acidosis and inc risk for renal calculi if used chronically"
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indication of diazepam?
"treat acute repetitive seizures, can be used as intermittent therapy with other drugs"
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mode of administration for doazepam?
rectal gel
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Ginkgo and ginseng....
i need more info
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