The Pharm of Old McDonald 6

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  1. ethosuximide
    • block thalamic T-type calcium channels. 1st line for absence seizures
    • GI, fatigue, headache, urticaria, SJS
    • ABC...EFGHIJ sorry I blanked. Sux to have absence seizures (Absence, Block Calcium, Ethosuximide, fatigue, GI, headache, itches, stevens-Johnson syndrome, absence seizures)
  2. diazepam
    • benzodiazipine
    • increase frequency of opening in GABA(A) channel, increasing Cl influx to decrease neuron firing. 1st line for acute status epilepticus and 2nd line for eclampsia (Mg is first line), anxiety, spasticity, alcohol DT, night terrors, sleepwalking (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, respiratory depression (less risk than barbiturates), treat overdose with flumazenil (GABA competitive antagonist), acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  3. lorazepam
    • benzodiazipine
    • increase GABA(A) channel, increasing Cl influx to decrease neuron firing. 1st line for acute status epilepticus and 2nd line for eclampsia (Mg is first line), anxiety, spasticity, alcohol DT, night terrors, sleepwalking (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, respiratory depression (less risk than barbiturates), treat overdose with flumazenil (GABA competitive antagonist), acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  4. midazolam
    • benzodiazipine
    • increase GABA(A) channel, increasing Cl influx to decrease neuron firing, short acting. adjuvant with inhaled anesthetics and narcotics for endoscopy1st line for acute status epilepticus and 2nd line for eclampsia (Mg is first line), anxiety, spasticity, alcohol DT, night terrors, sleepwalking (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, postoperative respiratory depression, hypotension (treat with flumazenil [GABA competitive antagonist]), anterograde amnesia, acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  5. phenobarbital
    • barbiturate
    • increase duration of GABA(A), increasing Cl ion influx, reducing neuron firing. 1st line in neonates for partial/generalized seizures (NOT absence), 2nd line for simple/complex partial (carbazepine 1st line for all partial), tonic-clonic, insomnia
    • sedation, tolerance, dependence, increases P-450, cardiorespiratory depression, CNS depression, overdose is supportive, contraindicated in porphyria for some reason
    • phirst in baby tal (1st line for neonatal seizures, phenobarbital)
    • barbidurate (barbiturates, duration of GABA(A))
  6. phenytoin
    • blocks Na channels. 1st line for tonic-clonic (w/ valproate), 1st line for status epilepticus prophylaxis, 2nd line for simple/complex partial (carbazepine 1st line for all partial), tonic-clonic
    • nystagmus, diplopia, ataxia, sedation, peripheral neuropathy, hirsutism, Stevens-Johnson syndrome, gingival hyperplasia, DRESS (drug reaction with eosinophilia and systemic symptoms [thrombocytopenia, lymphocytosis, fever, internal organ inflammation, death]), osteopenia, induced SLE, megaloblastic anemia, teratogen (fetal hydantoin), increases P-450
    • zero-order kinetics
    • zero order, 1st line, double vision, 3rd pair of teeth, CYP 450
  7. fosphenytoin
    • blocks Na channels. 1st line for tonic-clonic (w/ valproate), 1st line for status epilepticus prophylaxis, 2nd line for simple/complex partial (carbazepine 1st line for all partial), tonic-clonic
    • nystagmus, diplopia, ataxia, sedation, peripheral neuropathy, hirsutism, Stevens-Johnson syndrome, gingival hyperplasia, DRESS (drug reaction with eosinophilia and systemic symptoms [thrombocytopenia, lymphocytosis, fever, internal organ inflammation, death]), osteopenia, induced SLE, megaloblastic anemia, teratogen (fetal hydantoin), increases P-450
    • zero-order kinetics
    • zero order, 1st line, double vision, 3rd pair of teeth, CYP 450
  8. carbamazepine
    • blocks Na channels. 1st line for partial (complex and simple), line for trigeminal neuralgia, 2nd line tonic-clonic
    • diplopia, ataxia, agranulocytosis, aplastic anemia, hepatotoxic, teratogen, increases P-450, SIADH, Stevens-Johnson syndrome
    • simple and complex carbs are partially fizzytoin (1st line for partial seizures, carbamazepine, like phenytoin [Na block, side effects])
  9. valproic acid
    • activates Na channels, inhibits GABA transaminase to increase effect on GABA channel, increasing Cl influx to decrease neuron firing . 1st line (w/ phenytoin) for tonic-clonic, 2nd line for simple/complex partial, 2nd line for absence, also used for myoclonic seizures, bipolar disorder, migraine prophylaxis
    • GI distress, fatal hepatotoxicity (rare), pancreatitis, neural tube defects, tremor, weight gain
    • fight every evil with eval (many uses, many side effects)
  10. vigabatrin
    irreversible inhibition of GABA transaminase to increase GABA concentration, increasing Cl influx to decrease neuron firing. 2nd line for simple/complex partial
  11. gabapentin
    • primarily inhibits voltage-gated Ca channels. 2nd line for simple/complex partial, also peripheral neuropathy, postherpetic neuralgia
    • designed as GABA analog
    • sedation, ataxia
  12. topiramate
    • blocks Na channels, increases GABA action, increasing Cl influx to decrease neuron firing. 2nd line for simple/complex partial, 2nd line for tonic-clonic, alos for migraine prevention
    • sedation, mental dulling, kidney stones, weight loss
    • dopiramate (mental dulling)
    • less Na makes you thin (sodium channel blocker, weight loss)
  13. lamotrigine
    • blocks voltage-gated Na channels. 2nd line for simple/complex partial, 2nd line for tonic clonic and absence
    • stevens-johnson syndrome (titrate slowly)
    • lame otrigine (stevens johnson somehow)
  14. levitiracetam
    unknown (maybe GABA and glutamate). 2nd line for simple/complex partial, 2nd line for tonic clonic
  15. tiagabine
    inhibits GABA reuptake to increase GABA, increasing Cl influx to decrease neuron firing. 2nd line for simple/complex partial
  16. pentobarbital
    • barbiturate
    • increase duration of GABA(A), increasing Cl ion influx, reducing neuron firing. 1st line in neonates for partial/generalized seizures (NOT absence), 2nd line for simple/complex partial (carbazepine 1st line for all partial), tonic-clonic, insomnia, anxiety
    • sedation, tolerance, dependence, increases P-450, cardiorespiratory depression, CNS depression, overdose is supportive, contraindicated in porphyria for some reason
    • phirst in baby tal (1st line for neonatal seizures, phenobarbital)
    • barbidurate (barbiturates, duration of GABA(A))
  17. thiopental
    • barbiturate
    • increase duration of GABA(A), increasing Cl ion influx, reducing neuron firing. Rapid induction of anesthesia (very lipophilic, quickly redistributed to tissue/fat)
    • increases cerebral blood flow, sedation, tolerance, dependence, increases P-450, cardiorespiratory depression, CNS depression, overdose is supportive, contraindicated in porphyria for some reason
    • phirst in baby tal (1st line for neonatal seizures, phenobarbital)
    • barbidurate (barbiturates, duration of GABA(A))
  18. secobarbital
    • barbiturate
    • increase duration of GABA(A), increasing Cl ion influx, reducing neuron firing. 1st line in neonates for partial/generalized seizures (NOT absence), 2nd line for simple/complex partial (carbazepine 1st line for all partial), tonic-clonic, insomnia, anxiety
    • sedation, tolerance, dependence, increases P-450, cardiorespiratory depression, CNS depression, overdose is supportive, contraindicated in porphyria for some reason
    • phirst in baby tal (1st line for neonatal seizures, phenobarbital)
    • barbidurate (barbiturates, duration of GABA(A))
  19. triazolam
    • benzodiazipine
    • increase GABA(A) channel, increasing Cl influx to decrease neuron firing, short acting. Anxiety, spasticity, alcohol DT, night terrors, sleepwalking (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, respiratory depression (less risk than barbiturates), treat overdose with flumazenil (GABA competitive antagonist), acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  20. oxazepam
    • benzodiazipine
    • increase GABA(A) channel, increasing Cl influx to decrease neuron firing, short acting. Anxiety, spasticity, alcohol DT, night terrors, sleepwalking (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, respiratory depression (less risk than barbiturates), treat overdose with flumazenil (GABA competitive antagonist), acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  21. alprazolam
    • benzodiazipine
    • increase GABA(A) channel, increasing Cl influx to decrease neuron firing, short acting. Anxiety, spasticity, alcohol DT, night terrors, sleepwaling (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, respiratory depression (less risk than barbiturates), treat overdose with flumazenil (GABA competitive antagonist), acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  22. temazepam
    • benzodiazipine
    • increase GABA(A) channel, increasing Cl influx to decrease neuron firing. Anxiety, spasticity, alcohol DT, night terrors, sleepwaling (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, respiratory depression (less risk than barbiturates), treat overdose with flumazenil (GABA competitive antagonist), acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  23. chlordiazepoxide
    • benzodiazipine
    • increase GABA(A) channel, increasing Cl influx to decrease neuron firing. Anxiety, spasticity, alcohol DT, night terrors, sleepwaling (reduces REM sleep), general anesthesia, insomnia
    • sedation, tolerance, dependence, respiratory depression (less risk than barbiturates), treat overdose with flumazenil (GABA competitive antagonist), acute withdrawal precipitates seizures
    • frenzodiazipine (frequency of GABA(A), benzodiazipine)
    • Benzo O's last 0 seconds (-zOlams, and Oxazepam are short acting with no active metabolites)
  24. zaleplon
    • nonbenzodiazipine hypnotic
    • activate the GABA(BZ1) channel to increase Cl influx. Insomnia with less effect on REM sleep than benzodiazepines
    • ataxia, headaches, confusion, short-acting (only modest morning psychomotor/amnestic effects), and less dependency than benzodiazepines
    • ZZZs (Zaleplon, Zolpidem, esZopiclone)
    • ZaZolEs (order of increasing half-life, zaleplon, zolpidem, eszopiclone)
  25. zolpidem
    • nonbenzodiazipine hypnotic
    • activate the GABA(BZ1) channel to increase Cl influx. Insomnia with less effect on REM sleep than benzodiazepines
    • ataxia, headaches, confusion, short-acting (only modest morning psychomotor/amnestic effects), and less dependency than benzodiazepines
    • ZZZs (Zaleplon, Zolpidem, esZopiclone)
    • ZaZolEs (order of increasing half-life, zaleplon, zolpidem, eszopiclone)
  26. eszopiclone
    • nonbenzodiazipine hypnotic
    • activate the GABA(BZ1) channel to increase Cl influx. Insomnia with less effect on REM sleep than benzodiazepines
    • ataxia, headaches, confusion, short-acting (only modest morning psychomotor/amnestic effects), and less dependency than benzodiazepines
    • ZZZs (Zaleplon, Zolpidem, esZopiclone)
    • ZaZolEs (order of increasing half-life, zaleplon, zolpidem, eszopiclone)
  27. desflurane
    • inhaled anesthetic
    • unknown mechanism
    • malignant hypertension (fever, muscle contractions, AD inherited risk of voltage sensitive ryanodine receptors increase Ca release) (dantrolene [ryanodine receptor antagonist] reversal)
  28. halothane
    • inhaled anesthetic
    • unknown mechanism
    • malignant hypertension (fever, muscle contractions, AD inherited risk of voltage sensitive ryanodine receptors increase Ca release) (dantrolene [ryanodine receptor antagonist] reversal), liver toxicity
    • hepatothane (liver toxicity, halothane)
  29. enflurane
    • inhaled anesthetic
    • unknown mechanism
    • malignant hypertension (fever, muscle contractions, AD inherited risk of voltage sensitive ryanodine receptors increase Ca release) (dantrolene [ryanodine receptor antagonist] reversal), proconvulsant
    • encephlurane (proconvulsant, enflurane)
  30. isoflurane
    • inhaled anesthetic
    • unknown mechanism
    • malignant hypertension (fever, muscle contractions, AD inherited risk of voltage sensitive ryanodine receptors increase Ca release) (dantrolene [ryanodine receptor antagonist] reversal)
  31. sevoflurane
    • inhaled anesthetic
    • unknown mechanism
    • malignant hypertension (fever, muscle contractions, AD inherited risk of voltage sensitive ryanodine receptors increase Ca release) (dantrolene [ryanodine receptor antagonist] reversal)
  32. methoxyfulrane
    • inhaled anesthetic
    • unknown mechanism
    • malignant hypertension (fever, muscle contractions, AD inherited risk of voltage sensitive ryanodine receptors increase Ca release) (dantrolene [ryanodine receptor antagonist] reversal), nephrotoxicity
    • nephroxyflurane (nephrotoxic, methoxyflurane)
  33. N2O
    • nitrous oxide
    • inhaled anesthetic
    • unknown mechanism
    • malignant hypertension (fever, muscle contractions, AD inherited risk of voltage sensitive ryanodine receptors increase Ca release) (dantrolene [ryanodine receptor antagonist] reversal)
  34. ketamine
    • arylcyclohexylamine (PCP analog)
    • blocks NMDA receptor, causing dissociative anesthesia, disorientation, hallucination, bad dreams, cardiovascular stimulation
    • they're bad for the reasons they're good, and they cause increased cerebral blood flow
  35. propofol
    • potentiates GABA(A), rapid anesthesia induction. ICU sedation, short procedures
    • less postoperative nausea than thiopental
  36. esters
    • procaine, cocaine, tetracaine, benzocaine
    • local anesthetic
    • molecules that block Na channels by binding to receptors inside the channel, block nerves small to large and myelinated before unmyelinated (pain [small myelinated], temperature [small unmyelinated], touch [large myelinated], pressure [large unmyelinated]). Procedures, spinal anesthesia
    • action enhanced if given with vasoconstrictor (reduces systemic concentration)
    • ester allergy (give amides), higher dose needed in infected tissue[acidic tissue chargers alkaline anesthetics, inhibiting membrane passage], CNS excitation, hypertension, hypotension
  37. procaine (class/special?)
    • ester
    • local anesthetic
  38. cocaine (class/special?)
    • ester. local anesthetic. Also inhibits reuptake of sympathetics, causing vasoconstriction
    • arrhythmias
  39. tetracaine (class/special?)
    • ester
    • local anesthetic
  40. benzocaine (class/special?)
    • ester
    • local anesthetic
    • methemoglobinemia (cyanide sweet tooth Fe3+)
  41. amides
    • lidocaine, mepivacaine, bupivacaine
    • local anesthetic
    • molecules that block Na channels by binding to receptors inside the channel, block nerves small to large and myelinated before unmyelinated (pain [small myelinated], temperature [small unmyelinated], touch [large myelinated], pressure [large unmyelinated]). Procedures, spinal anesthesia (esp if ester allergy)
    • action enhanced if given with vasoconstrictor (reduces systemic concentration)
    • higher dose needed in infected tissue[acidic tissue chargers alkaline anesthetics, inhibiting membrane passage], CNS excitation, hypertension, hypotension
    • amIdes have Is (lIdocaine, mepIvicaine, bupIvacaine)
  42. lidocaine (class/special?)
    • amide
    • local anesthetic
    • amIdes have Is (lIdocaine, mepIvicaine, bupIvacaine)
  43. mepivacaine (class/special?)
    • amide
    • local anesthetic
    • amIdes have Is (lIdocaine, mepIvicaine, bupIvacaine)
  44. bupivacaine (class/special?)
    • amide
    • local anesthetic
    • severe cardiotoxicity
    • lub dub bupivacaine (cardiotoxic, bupivacaine)
    • amIdes have Is (lIdocaine, mepIvicaine, bupIvacaine)
  45. succinylcholine
    • depolarizing neuromuscular block
    • strong ACh agonist, keeping channels open, resulting in failure of channel (phase I), then closure of channels but desensitized (phase II)
    • phase I is irreversible
    • phase II reversed by acetylcholinesterase
    • hyperkalemia, hypercalcemia, hyperthermia
    • KCT(v5) sucks (hyperKalemia, hyperCalcemia, hyperThermia, succinylcholine)
  46. curares
    • tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium
    • competitive antagonism at ACh receptors. Nondepolarizing neuromuscular block
    • reversal with neostigmine (with atropine to prevent bradycardia), edrophonium, cholinesterase inhibitors
  47. flumazenil
    GABA competitive antagonist. Reverse effects of GABA agonists
  48. dantrolene
    inhibits ryanodine receptor from releasing Ca in skeletal muscles. Malignant hyperthermia, neuroleptic syndrome (toxicity of antipsychotics)
  49. baclofen
    activates GABA(B) receptors in the spinal cord, relaxing muscles. Muscle spams, low back pain
  50. cyclobenzaprine
    • blocks CNS serotonin, muscarinic, and histamine receptors. Central muscle relaxant for spasms
    • anticholinergic side effects
    • structure similar to TCAs
  51. bromocriptine
    • ergot dopamine agonist
    • direct agonism of dopamine receptors. Prolactinoma, parkinsonism (not preferred)
    • Dope! Bros romp an role in the pramapex hole
  52. pramipexole
    • non-ergot dopamine agonist (preferred over bromocriptine)
    • direct agonism of dopamine receptors. Parkinsonism
    • Dope! Bros romp an role in the pramapex hole
  53. ropinirole
    • non-ergot dopamine agonist (preferred over bromocriptine)
    • direct agonism of dopamine receptors. Parkinsonism
    • Dope! Bros romp an role in the pramapex hole
  54. amantadine
    • increases dopamine release and decreases dopamine reuptake. Parksonism
    • ataxia, livedo reticularis
  55. levodopa
    • L-DOPA converted to dopamine by DOPA decarboxylase and COMT. Parkinsonism
    • peripheral conversion to dopamine (nausea, vomiting, arrhythmias[increased catecholamines]) given with carbidopa to block peripheral conversion to dopamine, long term use->dyskinesia at dosing rapidly to akinesia
  56. carbidopa
    • inhibits DOPA decarboxylase peripherally, decreasing L-DOPA peripheral conversion, increasing L-DOPA concentration centrally (given with levodopa)
    • reduces perihperal dopamine effects of L-DOPA (nausea, vomiting, arrhythmias)
  57. entacapone
    • inhibits COMT peripherally, reducing degradation of L-DOPA to 3-O-methyldopa (3-OMD), increasing central L-DOPA concentration (given with levodopa)
    • entericapone (peripheral, entacapone)
  58. tolcapone
    • inhibits COMT peripherally and centrally(entacapone only acts peripherally), reducing degradation of L-DOPA to 3-methoxytyramine (3-OMD) peripherally, increasing central L-DOPA concentration, and decreasing degradation of dopamine to 3-MT centrally (given with levodopa)
    • topcapone (central (top) [and peripheral], tolcapone)
  59. selegiline
    • converted to active metabolite by MAO-B, irreversibly inhibits MAO-B, reducing dopamine degradation to DOPAC centrally (given with levodopa), can enhance adverse effects of levodopa (nausea, vomiting, arrhythmias). Also increases levels of amines(NE, 5-HT, dopamine), to increase their levels in the cleft. Atypical depression, anxiety
    • serotonin syndrome(contraindicated with SSRIs, TCAs, St. John's wort, meperidine, dextromethorphan, cheese, wine[tyramine][wait 2 weeks for clearance of MAOI]), CNS stimulation
    • savageline (backstabs MAO-B, selegiline)
    • that Mao is so carazy savage that he puts trannys in a funnel (MAOB, isocarboxazid, selegiline, tranylcypromine, phenelzine)
  60. rasagiline
    • converted to active metabolite by MAO-B, irreversibly inhibits MAO-B, reducing dopamine degradation to DOPAC centrally (given with levodopa), can enhance adverse effects of levodopa (nausea, vomiting, arrhythmias)
    • rasavagiline (backstabs MAO-B, rasagiline)
  61. memantine
    • NMDA antagonist, reducing glutamate release to prevent calcium mediated excitotoxicity. Slows progression of Alzheimers
    • dizziness, confusion, halucinations
  62. donepezil
    • AChE inhibitor
    • increases ACh levels. Reduces symptoms of Alzheimers
    • nausea, dizziness, insomnia
    • exacerbation of COPD, asthma, peptic ulcers
  63. galantamine
    • AChE inhibitor
    • increases ACh levels. Reduces symptoms of Alzheimers
    • nausea, dizziness, insomnia
    • exacerbation of COPD, asthma, peptic ulcers
  64. rivastigmine
    • AChE inhibitor
    • increases ACh levels. Reduces symptoms of Alzheimers
    • nausea, dizziness, insomnia
    • exacerbation of COPD, asthma, peptic ulcers
  65. tacrine
    • AChE inhibitor
    • increases ACh levels. Reduces symptoms of Alzheimers
    • nausea, dizziness, insomnia
    • exacerbation of COPD, asthma, peptic ulcers
  66. tetrabenazine
    inhibition of vesicular monamine transporter (VMAT), reducing dopamine entry into vesicles to reduce dopamine release. Huntington symptoms
  67. reserpine
    inhibition of vesicular monamine transporter (VMAT), reducing dopamine entry into vesicles to reduce dopamine release. Huntington symptoms
  68. riluzole
    • mechanism unclear, but reduces glutamate excitotoxicity. ALS increase in survival
    • relief for Lou's ol disease (ALS [Lou Gehrig], riluzole)
  69. sumatriptan
    • serotonin(1B/1D) agonist, inhibiting trigeminal nerve activation and vasoactive peptide release to cause vasoconstriction. Migraine buster, cluster headaches
    • coronary vasospasm, mild paresthesia

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countchocula58
ID:
318291
Filename:
The Pharm of Old McDonald 6
Updated:
2016-04-13 15:50:23
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tubberly tubblish pharm pharmacology step one
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Become a pharmacist!
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