drugs

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dpaytons
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203102
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drugs
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2013-02-24 21:08:09
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drugs
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DRUGS
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  1. carbamezapine
    • targets sodium channels
    • This is a first choice for treating partial seizures and tonic-clonic seizures.  
    • The inactivated state of Na+ channels is prolonged, leading to decrease in repetitive action firing.
  2. Lamotragine
    • targets sodium channels
    • This is a first choice for treating partial seizures and tonic-clonic seizures.  
    • The inactivated state of Na+ channels is prolonged, leading to decrease in repetitive action firing.
  3. Pregablin
    • targets high voltage calcium channels
    • Used to treat partial seizures in those with impaired hepatic function (cleared by the kidneys).  
    • It is designed as a structural analog of GABA, and inhibits voltage-gated Ca+ channels.
  4. valproic acid
    • targets sodium channels, T-type calcium channels, and GABAergic signaling Targets sodium channels in the inactivated state and prolongs this to decrease rapid firing.
    • Targets T-type calcium channels by blocking them to stop absence seizures.
    • They target GABAergic signaling by increasing the levels of GABA.
  5. ethosuximide
    • targets T-type calcium channels
    • Blocks the T-type calcium channels that cause absence seizures.  
    • Ethosuximide is only effective in treating absence seizures.
  6. phenobarbital
    • targets GABAergic signaling
    • Used as an alternative treatment for partial and tonic-clonic seizures (is ineffective against absence seizures).  
    • Its anti-seizure properties are due to the action at the GABA-induced influx of chloride via GABA-A receptors.
    • Sometimes AMDPA receptors are blocked also.  Not all experience maximum effects at doses that also produce hypnosis—it needs to act only at GABA-A receptors.  Phenobarbital acts more like a general anesthetic, which targets the AMPA receptors.  It is also used in lethal injections because it profoundly depresses the CNS.
  7. clonazepam
    • targets GABAergic signaling
    • Clonazepam is a benzodiazepine.  It acts at the GABA-induced influx of chloride via the GABA-A receptor.  
    • It is useful in treating partial, tonic-clonic, and also absence seizures.  Clonazepam is also able to inhibit T-type calcium channels.  These are safer than barbiturates.  
    • They aid in returning surround inhibition.  Profound tolerance results from repeated administration.
  8. diazepam
    • targets GABAergic signaling
    • Diazepam is a benzodiazepine.  It acts at the GABA-induced influx of chloride via the GABA-A receptor.  It is useful in treating partial and tonic-clonic seizures.  
    • Diazepam is safer than barbiturates.  They aid in returning surround inhibition.  Profound tolerance results from repeated administration.
  9. rufinamide
    • targets Glutamatergic signaling
    • Rufinamide blocks the metabotropic glutamate receptors (mGluR5) and also prolongs Na+ channel activation.  
    • Glutamate underlies almost every signal in the brain, so need drugs that are selective for certain types of receptors and that have limited binding capabilities.
  10. morphine
    • prototypical opioid analgesic
    • poor oral bioavailability (25%)
  11. fentanyl
    • opioid full agonist
    • more lipophilic (faster acting)
    • transdermal application for chronic pain
  12. codeine
    • higher bioavailability than morphine following oral administration
    • analgesic prodrug
    • 1/10th affinity of morphine
    • 10% converted into morphine
    • effective antitussive
  13. tramadol
    • opioid full agonist
    • racemic mixture
    • one enatiomer is a prodrug of a weak opioid
    • another increases synaptic NE/50HT levels by inhibiting their reuptake and promiting release
    • serotonin syndrome
    • fewer morphine like side effects
  14. nalbuphine
    • opioid mixed partial agonist
    • agonist at kappa opioid receptors
    • antagonist at mu opioid receptors
    • still produces analgesia but not euphoria
  15. naltrexone
    • antagonist at mu opioid receptors
    • reverses full agonist adverse effects, such as respiratory depression
    • shorter half-life of most full agonists
  16. methylnaltrexone
    • antagonist of opioid receptors
    • incapable of penetrating the BBB
    • would not reverse any central mediated side effects, but still reduces peripheral side effects
  17. aspirin
    • eg sodium salicylate and acetylsalicylic acid
    • covalently modifies COX1 and 2 resulting in an irreversible inhibition of COX activity
    • more selective for COX1
  18. ibuprofen
    • propinoic acid derivative
    • less effective in reducing platelet aggregation
    • often used in place of chronic aspirin therapy in the treatment of inflammatory disorders
    • less likely to produce GI side effects compared to aspirin
  19. ketorolac
    • femanate
    • potent analgesic, poor anti-inflammatory effects
    • oral doses of ketorolac 10 mg more effective than aspirin 650 mg or acetaminophen 600 mg in reducing postoperative pain
    • moderate to severe pain
    • SIDE EFFECTS: acute renal failure
  20. rofecoxib
    • Vioxx
    • COX2 selective drug
    • effective against inflammation, pain, fever
    • 50-60% decrease in serious GI complications
    • can result in renal complications
    • increased cardiovascular risk
    • associated with higher incidence of thrombotic cardiovascular events than placebo
  21. acetaminophen
    • inhibition of central COX
    • lower levels of peroxide, COX3
    • does not inhibit inflammation or platelet aggregation
    • no GI side effects
    • adverse effects confined to acute overdose
  22. duloxetine
    • SNRI
    • inhibition of NE and serotonin uptake
    • treats depression and neuropathic pain
    • augment activity of descending pathways
  23. gabapentin
    • increases GABA levels
    • antiseizure agents
    • prolong the inactive state of voltage-dependent Na+ channels
  24. ketamine
    • NMDA R antagonist
    • inhibits central sensitization by decreasing calcium-mediated activation of kinase
    • can prevent phosphorylation of AMPA Rs
    • reduce chronic and postoperative pain
    • SIDE EFFECTS: psychtominmetric effects
  25. tricyclic antidepressants
    • they will block either NE transport alone (secondary amine) or 5-HT/NE transporter (tertiary amine)
    • Antidepressant
    • They block a lot of other things that you wouldn't get with an SNRI (muscarinic, histamine, and adrenergic receptors)
    • SIDE EFFECTS: nausea, vomiting, dry mouth, blurred vision, tachycardia, sedation, weight gain, orthostatic hypotension, drowsiness, dizziness
    • ACUTE TOXICITY: coma, respiratory depression, delirium, seizures, cardiac arrhythmias
    • POTENTIALLY FATAL
  26. selective serotonin reuptake inhibitors
    • antidepressant
    • selective blockade of serotonin (5-HT)
    • SIDE EFFECTS: nausea/vomiting, headaches, sexual dysfunction, insomnia, nonfatal acute toxicity)
    • DRUG INTERACTIONS: MAO inhibitors, serotonin syndrome, can occur weeks after SSRI administration due to half-life of active metabolites
  27. monoamine oxidase inhibtors
    • inhibition of monoamine oxidase A (5-HT and NE) and B
    • ADVERSE REACTIONS: sleep disturbances, weight gain, high risk of postural hypotension
    • ACUTE TOXICITY: agitation, hallucinations, convulsions, potentially fatal
    • acts in cytosol
  28. serotonin-norepinephrine reuptake inhibitors
    • blockade of NE and 5-HT transporters
    • SIDE EFFECTS: nausea, constipation, dry mouth, headache, insomnia, sweating, anxiety, sexual dysfunction
    • DRUG INTERACTIONS: MAO inhibitors, serotonin syndrome
  29. ketamine
    • NMDA receptor antagonist
    • immediate effects
  30. duloxetine
    SNRI
  31. venlafaxine
    SNRI
  32. phenelzine
    MAO inhibitor
  33. sertraline
    SSRI
  34. fluoxetine
    SSRI
  35. imipramine
    tricyclic antidepressant (tertiary)
  36. amoxapine
    tricyclic antidepressant (secondary)

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