Neurologic Drugs (First Aid)

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DrMexito Plus on July 6, 2012

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Neurologic Drugs (First Aid)

morphine
opioid analgesic, can also be used as an IV anesthetic

agonist at mu receptor => open K+ channels, close Ca2+ channels => inhibit release of ACh, NE, 5-HT, glutamate and substance P
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morphine opioid analgesic, can also be used as an IV anesthetic

agonist at mu receptor => open K+ channels, close Ca2+ channels => inhibit release of ACh, NE, 5-HT, glutamate and substance P
fentanyl opioid analgesic, can also be used as an IV anesthetic (doesn't have histamine release like morphine)

agonist at mu receptor => open K+ channels, close Ca2+ channels => inhibit release of ACh, NE, 5-HT, glutamate and substance P
codeine opioid analgesic
methadone opiod analgesic

also used in maintenance programs for addicts
meperidine opioid analgesic
dextromethorphan opioid analgesic

used for cough suppression
tramadol very weak opioid agonist; also inhibits 5-HT and NE reuptake

SE: decreases seizure threshold
buprenorphine partial agonist at opioid mu and delta receptors

used in long-term replacement therapy for opioid dependency
butorphanol partial agonist at opioid mu and agonist at opioid kappa

less respiratory depression than full agonists
loperamide opioid used for diarrhea
diphenoxylae opioid used for diarrhea
phenytoin 1st line tx for tonic-clonic seizures (along w/ carbamazepine and valproic acid) and prophylaxis of status epilepticus; also used for both simple and complex seizures

MOA: inactivates Na+ channel

also a class IB antiarrhythmic
phenytoin side effects induces CYP450
drug-induced SLE
megaloblastic anemia (decreases folate)
nystagmus, diplopia, ataxia, peripheral neuropathy
sedation
teratogen (fetal hydantoin syndrome, similar to FAS)
gingival hyperplasia in kids
carbamazepine 1st line tx for tonic-clonic (along w/ phenytoin and valproic acid); also used for both simple and complex seizures

also used for trigeminal neuralgia and bipolar disorder

MOA: inactivates Na+ channel

SE: diplopia, ataxia, agranulocytosis, aplastic anemia, induces CYP450, SIADH, Stevens-Johnson syndrome
lamotrigine used for simple and complex partial seizures and tonic-clonic

MOA: blocks Na+ channel

SE: Stevens-Johnson syndrome (like carbamazepine and ethosuximide)
gabapentin used for simple and complex partial seizures and tonic-clonic

also used for neuropathic pain and bipolar disorder

MOA: GABA analog that blocks Ca2+ channels

SE: sedation, ataxia
topiramate used for simple and complex partial seizures and tonic-clonic

MOA: blocks Na+ channels, increases GABA action

SE: sedation, mental dulling, kidney stones, wt loss
valproic acid 1st line for tonic-clonic (along w/ phenytoin and carbamazepine), used for simple and complex partial seizures, absence seizures and myoclonic seizures

also used for bipolar disorder

MOA: blocks Na+ channels, increases GABA action

SE: GI distress, fatal hepatotoxicity NTD in fetus (decreased folate absorption), tremor, wt gain
ethosuximide 1st line tx for absence seizures

MOA: blocks thalamic T-type Ca2+ channels

SE: GI distress, fatigue, headache, urticaria, Stevens-Johnson syndrome
tiagabine used for simple and complex partial seizures

MOA: inhibits GABA uptake
phenobarbital (anti-epileptic) used for simple and complex partial seizures and tonic-clonic

1st line tx in pregnant women and children
benzodiazepines (anti-epileptic) 1st line tx for acute status epilepticus (prophylaxis is phenytoin)

also used for seizures assoc w/ ecclampsia (like Mg2+)
vigabatrin used for simple and complex partial seizures

MOA: inhibit GABA transaminase to increases [GABA]
levetiracetam used for simple and complex partial seizures and tonic-clonic

unknown MOA
phenobarbital barbituate, also used for seizures

MOA: increases duration of Cl- channel opening, decreasing neuronal firing

SE: respiratory or cardiovascular depression, induces CYP450

contraindicated in porphyria
pentobarbital barbituate

MOA: increases duration of Cl- channel opening, decreasing neuronal firing

SE: respiratory or cardiovascular depression, induces CYP450

contraindicated in porphyria
thiopental barbituate used as an IV anesthetic (used for induction)

high potency, high lipid solubility, rapid entry into brain

effect terminated by rapid redistribution into tissue and fat

SE: respiratory or cardiovascular depression, induces CYP450

contraindicated in porphyria
secobarbital barbituate

MOA: increases duration of Cl- channel opening, decreasing neuronal firing

SE: respiratory or cardiovascular depression, induces CYP450

contraindicated in porphyria
triazolam short acting benzodiazepine
oxazepam short acting benzodiazepine
midazolam short acting benzodiazepine

used as IV anesthetic (esp for endoscopy)
zolpidem used for insomnia

act at BDZ receptor but have lower dependence risk
zalepon used for insomnia

act at BDZ receptor but have lower dependence risk
eszopiclone used for insomnia

act at BDZ receptor but have lower dependence risk
halothane inhaled anesthetic, unknown MOA

highest potency of inhaleds

hepatotoxicity, can rarely cause malignant hyperthermia (tx dantrolene)
enflurane inhaled anesthetic, unknown MOA

proconvulsant, can rarely cause malignant hyperthermia (tx dantrolene)
isoflurane inhaled anesthetic, unknown MOA

can rarely cause malignant hyperthermia (tx dantrolene)
sevoflurane inhaled anesthetic, unknown MOA

can rarely cause malignant hyperthermia (tx dantrolene)
methoxyflurane inhaled anesthetic, unknown MOA

nephrotoxicity, can rarely cause malignant hyperthermia (tx dantrolene)
nitrous oxide inhaled anesthetic, unknown MOA

lowest potency of inhaled

expansion of trapped gas. can rarely cause malignant hyperthermia (tx dantrolene)
ketamine IV anesthetic

MOA: PCP analog that blocks NMDA receptor
propofol IV anesthetic used for rapid anesthesia induction and short procedures (like thiopental)

high TG content increases pancreatitis risk
procaine ester local anesthetic

MOA: blocks Na+ channels, esp activated ones, therefore most effective in rapidly firing neurons
cocaine ester local anesthetic

MOA: blocks Na+ channels, esp activated ones, therefore most effective in rapidly firing neurons
tetracaine ester local anesthetic

MOA: blocks Na+ channels, esp activated ones, therefore most effective in rapidly firing neurons
lidocaine amide local anesthetic

MOA: blocks Na+ channels, esp activated ones, therefore most effective in rapidly firing neurons

given if pt allergic to ester
mepivacaine amide local anesthetic

MOA: blocks Na+ channels, esp activated ones, therefore most effective in rapidly firing neurons

given if pt allergic to ester
bupivacaine amide local anesthetic

MOA: blocks Na+ channels, esp activated ones, therefore most effective in rapidly firing neurons

given if pt allergic to ester

cardiovascular toxicity
succinylcholine depolarizing neuromuscular blocking drug (works on motor nicotinic receptor)

used for muscle paralysis in sx or mechanical ventilation

SE: hypercalcemia and hyperkalemia due to prolonged muscle depolarization

reverse blockade w/ AChE inhibitors
tubocurarine nondepolarizing neuromuscular blocking drug

competes w/ ACh for receptor

reverse blockade w/ AChE inhibitors
atracurium nondepolarizing neuromuscular blocking drug

competes w/ ACh for receptor

reverse blockade w/ AChE inhibitors
mivacurium nondepolarizing neuromuscular blocking drug

competes w/ ACh for receptor

reverse blockade w/ AChE inhibitors
pancuronium nondepolarizing neuromuscular blocking drug

competes w/ ACh for receptor

reverse blockade w/ AChE inhibitors
vecuronium nondepolarizing neuromuscular blocking drug

competes w/ ACh for receptor

reverse blockade w/ AChE inhibitors
rocuronium nondepolarizing neuromuscular blocking drug

competes w/ ACh for receptor

reverse blockade w/ AChE inhibitors
dantrolene used to tx malignant hyperthermia and neuroleptic malignant syndrome (antipsychotic drugs)

MOA: prevents release of Ca from SR (blocks ryanodine receptor)
bromocriptine dopamine agonist (ergot) for Parkinson's
pergolide dopamine agonist (ergot) for Parkinson's
pramipexole dopamine agonist (non-ergot - preferred) for Parkinson's
ropinirole dopamine agonist (non-ergot - preferred) for Parkinson's
amantadine increase dopamine release for Parkinson's

also an antiviral agent (blocks viral penetration and uncoating)
L-dopa/carbidopa increase dopamine in brain for Parkinson's

L-dopa crosses BBB; carbidopa is a peripheral decarboxylase inhibitor and is given to increase the bioavailablitiy of the drug and limit peripheral side effects
selegiline selective MAO-B inhibitor (enzyme preferentially metabolizes dopamine over NE and 5-HT) for Parkinson's
entacapone COMT inhibitor for Parkinson's

prevents L-dopa degradation
tolcapone COMT inhibitor for Parkinson's

prevents L-dopa degradation
benztropine antimuscarinic agent used to control Parkinsonian tremors and rigidity
memantine NMDA receptor antagonist that helps prevent excitotoxicity in Alzeheimer's
donepezil AChE inhibitors used for Alzheimer's
galantamine AChE inhibitors used for Alzheimer's
rivastigmine AChE inhibitors used for Alzheimer's
sumatriptan 5-HT1B/1D agonist (anti-emetics are 5-HT antagonists)

used for migraine, cluster headache

tox: coronary vasospasm (contraindicated in CAD or Prinzmetal's angina); also contraindicated in pregnancy

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