Pcol

  1. Morphine
    Mu Receptor Agonist
  2. Codeine
    Mu Receptor Agonist
  3. Meperidine
    • Demerol
    • Mu Receptor Agonist
    • There is a metabolite called normeperidine
    • Normeperidine has a long half-life, and can cause seizures
    • Because this metabolite builds up, meperidine should not be used for more than 48 hours
  4. Hydrocodone w/ APAP
    • Vicodin
    • Mu Receptor Agonist
  5. Hydrocodone w homatropine
    • Hycodan
    • Mu Receptor Agonist
    • has anticholinergic effects
  6. Tramadol
    • Ultram
    • Mu Receptor Agonist
    • Can inhibit the reuptake of NE and 5-HT
    • Reduces levels of substance P and glutamate
    • may also be able to directly activate alpha-2 receptors, creating an analgesic effect
  7. Tapentadol
    • Nucynta
    • Mu Receptor Agonist
    • Block NE re-uptake
  8. Oxycodone CR
    • Oxycontin
    • Mu Receptor Agonist
  9. Oxycondone w/ APAP
    • Percocet
    • Mu Receptor Agonist
  10. Oxycodone w/ASA
    • Percodan
    • Mu Receptor Agonist
  11. Methadone
    • Mu Receptor Agonist
    • very long acting
  12. Hydromorphone
    • Dilaudid
    • Mu Receptor Agonist
    • Can cause hyperglycemia probably by reducing insulin release
  13. Oxymorphone
    Mu Receptor Agonist
  14. Levorphanol
    Mu Receptor Agonist
  15. Fentanyl
    • Duragesic, Actiq
    • Mu Receptor Agonist
  16. Diphenoxylate w/ atropine
    • Lomotil
    • Mu Receptor Agonist peripherally
  17. Loperamide
    • Imodium
    • Mu Receptor Agonist peripherally
  18. Paregoric
    Mu Receptor Agonist peripherally
  19. DTO (deodorized tincture of opium)
    Mu Receptor Agonist peripherally
  20. Naloxone
    • Narcan
    • Mu Receptor Antagonist
  21. Naltrexone
    Mu Receptor Antagonist
  22. Nalbuphine
    kappa agonist/ mu antagonist
  23. Butorphanol
    kappa agonist/ mu antagonist
  24. Pentazocine
    • Talwin
    • kappa agonist/ mu antagonist
  25. Pentazocine and Naloxone
    • Talwin NX
    • kappa agonist/ mu antagonist
  26. Buprenorphine
    • Subutex
    • Mu parital agonist/ kappa antagonist
  27. Buprenorphine w. naloxone
    • Suboxone
    • Mu parital agonist/ kappa antagonist
  28. Ziconotide
    • Prialt
    • Conotoxin
    • block N type calcium channels-Keep it more likely in the closed state
    • Ca cant enter channels, less NT released, Fewer impulses and less perception of pain(activation of the Mu receptors in dorsal horn decreases the release of NT) --> reducing activation of ascendingneuron
    • intrathecal injection Bc that is where the effect is
    • Doesn’t reach MOR in the brain (No respiratory depression, No euphoria.
    • Blocking these Ca channels give significant analgesia without the side effects fromactivating the Mu receptors in the brain
  29. BDZ therapeutic use
    • Anxiolytics
    • Treatment of insomnia
    • Treatment of alcohol withdrawal syndrome
    • Anticonvulsants: Agents with rapid onset of action is used in treatment of status epilepticus. Chronic treatment is associated with development of tolerance
    • Muscle relaxants: Reduce skeletal muscle spasticity by enhancing the activity of inhibitory neurotransmission in the spinal cord
  30. Midazolam
    • Versed
    • Short acting BDZ

    Pre-operative sedation, Anesthetic
  31. Triazolam
    • Halcion
    • Short Acting BDZ

    Insomnia: Fast-onset, decrease time to sleep
  32. Alpazolam
    • Xanax
    • Intermediate BDZ

    Anxiety disorders, phobias, withdrawal symptoms may be severe
  33. Estazolam
    • Prosom
    • Intermediate BDZ

    Insomnia
  34. Lorazepam
    • Ativan
    • Intermediate BDZ

    Anxiety disorders, IV general anesthetic, status epilepticus
  35. Oxazepam
    • Serax
    • Intermediate BDZ

    Anxiety
  36. Temazepam
    • Restoril
    • Intermediate BDZ

    Insomnia
  37. Chlordiazepoxide
    • Libirum
    • Long acting BDZ

    Anxiety disorders, alcohol withdrawal management, anesthetic premedication
  38. Clonazepam
    • Klonopin
    • Long acting BDZ

    Seizures, adjunctive in acute mania and movement disorders. Tolerance develops to anticonvulsant activity
  39. Clorazepate
    • Tranxene
    • Long acting BDZ

    Anxiety disorders, seizures
  40. Diazepam
    • Valium/ Diastat
    • Long acting BDZ

    Anxiety disorders, status epilepticus, muscle relaxants, alcohol withdrawal, anesthetic premedication
  41. Flurazepam
    • Dalmane
    • Long acting BDZ

    Insomnia; active metabolites accumulate with chronic use
  42. Quazepam
    • Doral
    • Long acting BDZ

    Insomnia; active metabolites accumulate with chronic use
  43. BDZ side effects
    • Lightheadedness, mental impairment, loss of motor function coordination, confusion, anterograde amnesia (additive effect with alcohol, other sedative/hypnotic drugs)
    • Paradoxical effects: anxiety, irritability, tachycardia, sweating, hallucinations
  44. BDZ mech of action
    BDZs work as positive allosteric GABAA modulator, enhancing GABA binding affinity and/or increased channel opening frequency
  45. Zolpidem
    • Ambien
    • BDZ related
  46. BDZ like drugs mech of action
    • Selective for α1GABAA. Binds to the same site as
    • Used in treatment of insomnia –Lack anticonvulsant, anxiolytic or
    • muscle-relaxant effects of BDZs
    • Side-effects: Amnesia, impairment of complex task performance similar to BDZs, may have similar abuse potential
  47. Zaleplon
    • Sonata
    • BDZ like
  48. Eszopiclone
    • Lunesta
    • BDZ like
  49. Flumazenil
    • Romazicon
    • BDZ antag

    Binds with high affinity to GABAA to competitively antagonize the binding and allosteric effects of BDZs

    BDZ OD antidote
  50. Barbiturates Mech of Action
    • Like BDZs, a positive GABAA allosteric receptor modulator increasing Cl- current
    • Site of binding to GABAA receptor is distinct from GABA and BDZs
    • Weak agonist activity at GABAA receptor (Direct opening of Cl- channel)
  51. Thiopental
    • Pentothal
    • Ultra short acting BDZ

    Anesthesia induction, short- term anesthesia maintenance, emergency seizure treatment, increased intracranial pressure
  52. Methohexital
    • Brevital
    • ultra short Barb

    Anesthesia induction, shortterm anesthesia
  53. Pentobrabital
    • Nembutal
    • Ultra short Barb

    Preoperative sedation, refractory status epilepticus, barbiturate coma
  54. Amobarbital
    • Amytal
    • Short acting Barb

    Hypnotic, sedative
  55. Butabrabital
    • Butisol
    • Short acting barb

    Anxiety, insomnia
  56. Butalbital
    • Fioricet, Fiorinal
    • short acting barb

    in combination with caffeine, acetaminophen Relief of the symptomatic complex of tension or muscle contraction headache
  57. Mephobarbital
    • Mebaral
    • Short acting barb

    Epilepsy, sedation
  58. Secobarbital
    • Seconal
    • Short acting barb

    Sedation
  59. Phenobarbital
    • Luminal
    • Long acting Barb

    Anticonvulsant, status epilepticus, preoperative sedation, hypnotic
  60. Barb Side effects
    • CNS depression, additive effects with other CNS depressants, e.g. BZDs and ethanol
    • Respiration: Depress respiratory drive and mechanisms for rhythmic control of respiration
    • Impaired motor skills, drowsiness
    • Generally, no significant effect on hemodynamics. In overdoses, blood pressure lowering and cardiac arrhythmia
    • Paradoxical excitement
  61. Ramelteon
    Rozerem

    • -MT1 and MT2 receptor agonist
    • -MT1 and MT2 are present within the suprachiasmic nucleus of the hypothalamus
    • Endogenous agonist is melatonin
    • -MT1 activation induces sleep, MT2 activation regulates circadian rhythm
    • -Ramelteon is more selective for MT1 compared to MT2
  62. Buspirone
    Buspar

    selective partial agonist at the 5-HT1a receptor
  63. Baclofen
    • Lioresal
    • GABA-b Receptor Agonist
    • Centrally acting muscle relaxant
  64. Tizanidine
    Clonidine
    • Zanaflex
    • α2 Receptor Agonists- decreases excitatory inputs to α motor neurons
    • Centrally acting muscle relaxant

    lower risk of hypertenion than clonidine
  65. Cyclobenzaprine
    • Flexeril
    • TCA like

    • -inhibits NET
    • -anticholingeric effects

    • -5-HT2 receptor antagonist at the spinal level
    • -Alpha motor neuronal activity is regulated by descending serotonergic neurons from medullary raphe
  66. Methocarbamol
    • Robaxin
    • Centrally acting muscle relaxant Msc
  67. Carisoprodol
    • Soma
    • Centrally acting muscle relaxant Msc
  68. Orphenadrine
    • Norflex
    • Centrally acting muscle relaxant Msc
  69. Gaba-b receptors
    • Metabotropic receptor (GPCR): Heterodimers composed of R1 and R2 subunits.
    • Endogenous agonist: GABA • Present pre-synaptically and post-synaptically
    • Pre-synapse: Inhibition of Ca2+ entry
    • Post-synapse: Stimulation of K+ efflux
  70. Phenytoin
    • Dilantin
    • seizures

    • • Binds to voltage-gated Na+ channel in the inactivated state
    • • Slows recovery of Na channel to the closed conformation
    • • Use-dependent channel antagonism
    • • non linear kinetics
  71. Fosphenytoin
    • Cerebyx
    • seizures

    • – Prodrug of phenytoin
    • – Metabolized by plasma esterases to phenytoin
    • – Similar side effects to phenytoin, less risk of hypotension
  72. Carbamazepine
    • Tegretol
    • seizures

    like phenytoin
  73. Oxcarbazepine
    • Trileptal
    • Seizures

    like carbamazepine
  74. Lamotrigine
    • Lamictal
    • seizures

    • • Na channel antagonist.
    • • Binds to the inactivated conformation and slows channel recovery
    • • Additional mechanism: inhibits neuronal glutamate release
  75. Ethosuximide
    • Zarontin
    • seizures

    • T-type Ca channel antagonist
    • –Reduces the extent of Ca entry through the channel without affecting rate of recovery of channel from inactivated state
  76. Zonisamide
    • Zonegran
    • seizures

    • • Inhibit T-type Ca channel through preferential binding to the inactivated state, prevents channel recovery
    • • Inhibit voltage-gated Sodium channel similar to phenytoin, carbamazepine
  77. Gabapentin
    • Neurontin
    • Seizures

    • Bind specific α2 δ subunit of voltage-gated calcium channel, reduces Ca influx mediated neurotransmitter release (Glu, NE, DA, substance P)
  78. Pregabalin
    • Lyrica
    • Seizures

    Bind specific α2 δ subunit of voltage-gated calcium channel, reduces Ca influx mediated neurotransmitter release (Glu, NE, DA, substance P)
  79. Tiagabine
    • Gabitril
    • Seizures

    Inhibits GAT-1 transporter
  80. Vigabatrin
    • Sabril
    • Seizures

    Irreversible inhibitor of GABA-T
  81. Valproic Acid
    • Depakote
    • Seizures

    • • Na channel antagonist (similar mechanism to phenytoin)
    • • T-type Ca channel antagonist
    • • Enhancing GABA transmission via increase in GABA neuronal content
  82. Levetiracetam
    • Keppra
    • Seizures

    • • Inhibition of High-voltage gated Ca channels
    • • Inhibition of excitatory neurotransmitter release
    • •Reversal of zinc-induced inhibition of GABAA receptors
  83. Topiramate
    Topamax

    • AMPA Receptor: Ligand-gated Na channel
    • AMPA Receptor antagonist: Topiramate
  84. Inhalation anesthetics MOA
    • Not clearly identified
    • Highly lipophilic
    • Thought to exert non-specific effect on plasma membrane of excitable neurons leading to stabilization of hyperpolarized state
    • GABAAstimulation and K+channel agonists
  85. Felbamate
    • NMDA Receptor: Ligand-gated Ca channel
    • –NMDA Receptor antagonist
  86. Isoflurane
    Inhalation anesthetics
  87. Enflurane
    Inhalation anesthetics
  88. Desflurane
    Inhalation anesthetics
  89. Sevoflurane
    Inhalation anesthetics
  90. Halothane
    Inhalation anesthetics
  91. Nitrous Oxide
    Inhalation anesthetics

    NMDA receptor antagonist effect
  92. Thiopental
    IV anesthetics
  93. Propofol
    • Diprivan
    • IV anesthetics

    • –Targets GABA-A receptors
    • –Voltage-gated Na+channel antagonist
  94. Etomidate
    • Amidate
    • IV anesthetics

    -Agonist at GABAAreceptor

    – Inhibits glucocorticoid and mineralocorticoid synthesis
  95. Ketamine
    • Ketalar
    • IV anesthetics

    • – NMDA Noncompetitive Receptor Antagonist
    • – α1and β1receptor agonist
    • – Prevents re-uptake of catecholamines

    causes emergence phenomenon
  96. MinimumAlveolarConcentratio
    Inhalational anesthetic %volume of inspired air at which 50% of patients do not respond to a surgical stimulus

    The lower the MAC, the higher the potency
  97. Malignant Hyperthermia
    Rare complication of inhalational general anesthetics, and depolarizing neuromuscular blockers

    • Increase cytoplasmic free Calcium in skeletal muscle cells (Rigidity, spasms)
    • – Increase body temperature
    • – Hypermetabolism: Increase oxygen consumption and CO2 production
    • – Muscle cell damage, sympathetic activation
  98. Dantrolene
    • antidote for malignant hyperthermia
    • Direct acting muscle relaxant

    Inhibits release of Ca2+ release from sarcoplasmic reticulum by binding to ryanodine receptor
  99. Abortive treatments for migraines
    • –Triptans
    • –Ergots
    • –NSAIDs, aspirin, acetaminophen (Treximet= sumatriptan+ naproxen)
    • –Fiorinalor Fioricet (Aspirin or acetaminophen, plus butalbital plus caffeine)
    • –Opiates
  100. Preventive treatments for migraines
    • –propranolol
    • –verapamil
    • –divalproex, topiramate
    • –ACE inhibitors, ARBs
    • –botulinumtoxin type A (Botox)
  101. Sumatriptan
    • Imitrex
    • triptans- migraines
  102. Almotriptan
    • Axert
    • triptans- migraines
  103. Zolmitriptan
    • Zomig
    • triptans- migraines
  104. Naratriptan
    • Amerge
    • triptans- migraines
  105. Rizatriptan
    • Maxalt
    • triptans- migraines
  106. Frovatriptan
    • Frova
    • triptans- migraines
  107. Eletriptan
    • Relpax
    • triptans- migraines
  108. Ergotamine
    ergots- migraines
  109. Dihydroergotamine
    ergots- migraines
  110. Methergine
    • methylergonovine
    • ergots- migraines
  111. Bromocriptine
    ergots- migraines
  112. Adderall
    Indirect-acting sympathomimetics, Amphetamines
  113. Dexedrine
    • dextroamphetamine
    • Indirect-acting sympathomimetics, Amphetamines
  114. Desoxyn
    • methamphetamine
    • Indirect-acting sympathomimetics, Amphetamines
  115. Vyvanse
    • lisdexamfetamine
    • Indirect-acting sympathomimetics, Amphetamines
  116. Ritalin
    Indirect-acting sympathomimetics, Methylphenidates
  117. Concerta
    Indirect-acting sympathomimetics, Methylphenidates
  118. Focalin
    • dexmethylphenidate
    • Indirect-acting sympathomimetics, Methylphenidate
  119. Benzphetamine
    • Didrex
    • Indirect-acting sympathomimetics, msc
  120. Diethylpropion
    Indirect-acting sympathomimetics, msc
  121. Phendimetrazine
    Indirect-acting sympathomimetics, msc
  122. fenfluramine(or dexfenfluramine) plus phentermine
    • Fen-phen
    • Indirect-acting sympathomimetics, msc
  123. Sibutramine
    • Meridia
    • Indirect-acting sympathomimetics, msc
  124. Modafinil
    • Provigil
    • Indirect-acting sympathomimetics, msc
  125. Armadafinil
    • Nuvigil
    • Indirect-acting sympathomimetics, msc
  126. ephedrine
    Indirect-acting sympathomimetics, msc
  127. Atomoxitene
    • Strattera
    • Indirect-acting sympathomimetics, msc
  128. Imipramine
    • TCA
    • antidepressants
  129. Desipramine
    • TCA
    • antidepressants
  130. Clomipramine
    • TCA
    • antidepressants
  131. Amitriptyline
    • Elavil
    • TCA
    • antidepressants
  132. Nortriptyline
    • TCA
    • antidepressants
  133. Doxepin
    • TCA
    • antidepressants
  134. Protriptyline
    • TCA
    • antidepressants
  135. Trimimpramine
    • TCA
    • antidepressants
  136. maprotiline
    • TCA
    • antidepressants
  137. Amoxapine
    • TCA
    • antidepressants
  138. Fluvoxamine
    SSRI antidepressants
  139. Sertraline
    • Zoloft
    • SSRI antidepressants
  140. Citalopram
    • Celexa
    • SSRI antidepressants
  141. Paroxetine
    • Paxil
    • SSRI antidepressants
  142. Escitalopram
    • Lexapro
    • SSRI antidepressants
  143. Fluoxetine
    • Prozac
    • SSRI antidepressants
  144. Venlafaxine
    • Effexor
    • SNRI antidepressants
  145. Desvenlafaxine
    • Pristiq
    • SNRI antidepressants
  146. Duloxetine
    • Cymbalta
    • SNRI antidepressants
  147. Milnacipran
    • Savella
    • SNRI antidepressants
  148. Phenelzine
    • Nardil
    • MAOi antidepressants
  149. Tranylcypromine
    MAOi antidepressants
  150. Bupropion
    • Wellbutrin
    • Atypical antidepressants
  151. Mirtazapine
    Atypical antidepressants
  152. Nefazodone
    Atypical antidepressants
  153. Trazodone
    Atypical antidepressants
  154. Lithium
    Bi-polar
Author
Anonymous
ID
71382
Card Set
Pcol
Description
exam 1/2 drugs
Updated