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Neurology Pharmacology

  1. Glaucoma Drugs
    • Decrease IOP but decreasing amount of aqueous humor
    • -inhibit synthesis/secretion
    • -increase drainage

    • α-Agonists
    • -epinephrine
    • -Brimonidine

    • β-Blockers
    • -Timolol
    • -Betaxolol
    • -Carteolol

    • Diuretics
    • -Acetazolamide

    • Cholinomimetics
    • -Pilocarpine
    • -Carbachol
    • -Physostigmine
    • -Echothiophate

    • Prostaglandin
    • -Latanoprost
  2. Epinephrine
    • Mechanism:
    • -α-agonist
    • -decreased aqueous humor synthesis via vasoconstriction

    • Clinical Uses:
    • -glaucoma

    • Adverse Effects:
    • -mydriasis
    • -do not use in closed-angle glaucoma
  3. Brimonidine
    • Mechanism:
    • -α2 agonist
    • -decrease aqueous humor synthesis

    • Clinical Uses:
    • -glaucoma

    • Adverse Effects:
    • -blurry vision
    • -ocular hyperemia
    • -foreign body sensation
    • -ocular allergic reactions
    • -ocular pruritus
  4. β-Blockers
    • Timolol
    • Betaxolol
    • Carteolol

    • Mechanism:
    • -β antagonist
    • -decrease aqueous humor synthesis

    • Clinical Uses:
    • -glaucoma

    • Adverse Effects:
    • -no pupillary or vision changes
  5. Acetazolamide
    • Mechanism:
    • -diuretic
    • -decrease aqueous humor synthesis via inhibition of carbonic anhydrase

    • Clinical Uses:
    • -glaucoma

    • Adverse Effects:
    • -no pupillary or vision changes
  6. Cholinomimetics
    • Direct:
    • -Pilocarpine
    • -Carbachol

    • Indirect:
    • -Physostigmine
    • -Echothiophate
    • Mechanism:
    • - increase outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshwork

    • Clinical Uses:
    • -glaucoma
    • *use pilocarpine in emergencies: very effective at opening meshwork into canal of Schlemm

    • Adverse Effects:
    • -miosis
    • -cyclospasm (contraction of ciliary muscle)
  7. Latanoprost
    • Mechanism:
    • -prostaglandin analog (PGF2a)
    • -increase outflow of aqueous humor

    • Clinical Uses:
    • -glaucoma

    • Adverse Effects:
    • -darkens color of iris (browning)
  8. Opioid Analgesics
    • Morphine
    • Fentanyl
    • Codeine
    • Heroin
    • Methadone
    • Merperidine
    • Dextromethorphan
    • Diphenoxylate

    • Mechanism:
    • -agonists at opioid receptors
    • -mu → morphine
    • -delta → enkephalin
    • -kappa → dynorphin
    • -modulate synaptic transmission: opens K+ channels, closes Ca2+ channels
    • -decreases synaptic transmission
    • -inhibits release of ACh, NE, 5-HT, glutamate, substanceP

    • Clinical Use:
    • -pain
    • -cough suppression (dextromethorphan)
    • -diarrhea (loperamide and diphenoxylate)
    • -acute pulmonary edema
    • -maintenance programs for addicts (methadone)

    • Toxicity:
    • -addiction
    • -respiratory depression
    • -constipation
    • -miosis (pinpoint pupils)
    • -additive CNS depression with other drugs
    • -tolerance does not develop to miosis and constipation
    • -toxicity treated with naloxone or naltrexone (opioid receptor antagonist)
  9. Butorphanol
    • Mechanism:
    • -mu opioid receptor partial agonist and kappa opioid receptor agonist
    • -produces analgesia

    • Clinical Use:
    • -severe pain (migraine, labor etc)
    • -causes less respiratory depression than full opioid agonist

    • Toxicity:
    • -can cause opioid withdrawal symptoms if patient is also taking full opioid agonist (competition for opioid receptors)
    • -OD not easily reversed with naloxone
  10. Tramadol
    • Mechanism:
    • -very weak opioid agonist
    • -also inhibits serotonin and NE reuptake
    • "Works with multiple NTs: "tram it all" in with tramadol"

    • Clinical Use:
    • -chronic pain

    • Toxicity:
    • -similar to opioids
    • -decreases seizure threshold
  11. Epilepsy
    • Phenytoin
    • Carbamazepine
    • Lamotrigine
    • Gabapentine
    • Topiramate
    • Phenobarbital
    • Valproic Acid
    • Ethosuximide
    • Benzodiazepines
    • Tiagabine
    • Vigabatrin
    • Levetiracetam
  12. Phenytoin (Seizures)
    • Mechanism:
    • -increase Na+ channel inactivation

    • Clinical Use:
    • -simple partial seizures
    • -complex partial seizures
    • -First line for tonic-clonic seizures
    • -First line for prophylaxis of status epilepticus

    • Toxicity:
    • -nystagmus
    • -diplopia
    • -ataxia
    • -sedation
    • -gingival hyperplasia
    • -hirsutism
    • -megaloblastic anemia
    • -teratogenesis (fetal hydantoin syndrome)
    • -SLE-like syndrome
    • -induction of cytochrome P-450
    • -lymphadenopathy
    • -Stevens-Johnson Syndrome
    • -osteopenia

    • Notes:
    • -Fosphenytoin for parenteral use
  13. Carbamazepine
    • Mechanism:
    • -increase Na+ channel inactivation

    • Clinical Use:
    • -first line for simple partial seizures
    • -first line for complex partial seizures
    • -first line for tonic-clonic seizures
    • -first line for Trigeminal Neuralgia

    • Toxicity:
    • -diplopia
    • -ataxia
    • -blood dyscrasias (agranulocytosis, aplastic anemia)
    • -liver toxicity
    • -teratogenesis
    • -induction of cytochrome P-450
    • -SIADH
    • -Stevens-Johnson syndrome
  14. Lamotrigine
    • Mechanism:
    • -blocks voltage gated Na+ channels

    • Clinical Use:
    • -simple partial seizures
    • -simple complex seizures
    • -tonic-clonic seizures

    • Toxicity:
    • -Stevens-Johnson Syndrome
  15. Gabapentin
    • Mechanism:
    • -designed as a GABA analog
    • -primarily inhibits high voltage activated Ca2+ channels

    • Clinical Use:
    • -simple partial seizures
    • -simple complex seizures
    • -tonic-clonic seizures
    • -peripheral neuropathy
    • -postherpetic neuralgia
    • -migraine prophylaxis
    • -bipolar disorder

    • Toxicity:
    • -sedation
    • -ataxia
  16. Topiramate
    • Mechanism:
    • -blocks Na+ channels
    • -increases GABA action

    • Clinical Use:
    • -simple partial seizures
    • -complex partial seizures
    • -tonic-clonic seizures
    • -migraine prevention

    • Toxicity:
    • -sedation
    • -mental dulling
    • -kidney stones
    • -weight loss
  17. Phenobarbital
    • Mechanism:
    • -increase GABAA action

    • Clinical Use:
    • -simple partial seizures
    • -simple complex seizures
    • -tonic-clonic seizures
    • **first line in children

    • Toxicity:
    • -sedation
    • -tolerance
    • -dependence
    • -induction of cytochrome P-450
  18. Valproic Acid
    • Mechanism:
    • -increase Na+ channel inactivation
    • -increase GABA concentration

    • Clinical Use:
    • -simple partial seizures
    • -simple complex seizures
    • -first line for tonic-clonic seizures
    • -absence seizures
    • -myoclonic seizures

    • Toxicity:
    • -GI distress
    • -rare but fatal hepatotoxicity (measure LFTs)
    • -neural tube defects in fetus (spina bifida)
    • -tremor
    • -weight gain
    • -CI in pregnancy
  19. Ethosuximide
    • Mechanism:
    • -blocks thalamic T-type Ca2+ channels

    • Clinical Use:
    • -first line for absence seizures

    • Toxicity:
    • -GI distress
    • -fatigue
    • -headache
    • -urticaria
    • -Stevens-Johnson syndrome

    • EFGH
    • -Ethosuximide
    • -Fatigue
    • -GI
    • -Headache
  20. Benzodiazepines
    • Diazepam
    • Lorazepam

    • Mechanism:
    • -increase GABAA action

    • Clinical Use:
    • -first line for acute status epilepticus
    • -seizures of eclampsia (first line is MgSO4)

    • Toxicity:
    • -sedation
    • -tolerance
    • -dependence
  21. Tiagabine
    • Mechanism:
    • -inhibits GABA reuptake

    • Clinical Use:
    • -simple partial seizures
    • -simple complex seizures
  22. Vigabatrin
    • Mechanism:
    • -irreversibly binds GABA transaminase
    • -increases GABA

    • Clinical Use:
    • -simple partial seizures
    • -simple complex seizures
  23. Levetiracetam
    • Mechanism:
    • -unknown
    • -may modulate GABA and glutamate release

    • Clinical Use:
    • -simple partial seizures
    • -simple complex seizures
    • -tonic-clonic seizures
Author
jknell
ID
207908
Card Set
Neurology Pharmacology
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