407 flashcards.txt

  1. Acetylcholine
    Cholinergic agonist; ester
  2. Methacholine
    Cholinergic agonist; ester
  3. Carbachol
    direct muscarinic agonist
  4. Bethanechol
    muscaranic selective (b methyl)
  5. Nicotine
    Cholinergic agonist; alkaloid
  6. Pilocarpine
    muscarinic; glaucoma
  7. Varenicline tartrate (Chantix)
    Nicotinic PARTIAL agonist; dampens withdrawal sx
  8. Tetraalkylammonium ions
    Reversible AChE inhibitor
  9. Endrophonium
    [indirect parasympathomimetic] Reversible AChE inhibitor; Quaternary ammonium; MG dx
  10. Neostigmine
    Reversible covalent AChE inhib; carbamate
  11. Pyridostigmine
    Reversible covalent AChE inhib; carbamate
  12. Physostigmine
    Reversible covalent AChE inhib; carbamate
  13. Isofluorophate
    [indirect parasympathomimetic] Irreversible AChE inhib; organophosphate; glaucoma
  14. Echothiophate
    [indirect parasympathomimetic] Irreversible AChE inhib; organophosphate; glaucoma
  15. Sarin
    Irreversible AChE inhib; organophosphate; nerve gas
  16. Soman
    Irreversible AChE inhib; organophosphate; nerve gas
  17. Malathion
    Irreversible AChE inhib; organophosphate; insecticide
  18. Diazinon
    Irreversible AChE inhib; organophosphate; insecticide
  19. Pralidoxime Chloride (2-PAM)
    Antidote for AChE poisoning
  20. Tacrine
    Reversible AChE inhib; Alzheimers (DOES NOT SLOW DISEASE PROGRESSION)
  21. Donepezil
    Reversible AchE inhib; alzheimers
  22. Parasympathomimetic drugs� CONTRAINDICATIONS
    1. Asthma 2. COPD 3. ulcer 4. GI/urinary tract obstruction
  23. Cholinergic SE
    SLUD, inc sweating, dec HR, pupil constriction, CNS activation
  24. Tx for cholinergic SE
    Atropine (cholinergic antagonist)
  25. Rivastigmine
    Reversible carbamate AchE inhib; alzheimers (loses effectiveness)
  26. Eptastigmine
    Longer acting than rivastigmine; alzheimers
  27. Reminyl
  28. Memantine (Namenda)
    NMDA antagonist; alzheimers (MAY SLOW PROGRESSION)
  29. Atropine
    [parasympatholytic] antidote, VERY LONG HALF LIFE; tachycardia, dec GI motility
  30. Homatropine HBr
    Less toxic and shorter duration than atropine
  31. Homatropine methyl Br
    QUATERNARY (cant cross BBB); GI spasm and ulcer
  32. Clidinium Br
    If lacking quaternary, this would be �BZ� (the chemical warfare agent)
  33. Ipratropium Br
    COPD but no quaternary so would enter CNS
  34. Tropicamide
    VERY SHORT DURATION; mydriasis
  35. Tolterodine (Detrol)
    Dec frequency of urinary bladder contractions
  36. Diphemanil
    Antispasmodic with double bond instead of an ester
  37. Diphenhydramine (Benadryl)
    Antihistamine and strong sedative
  38. Imipramine
    TCA with anticholinergic effects
  39. Solifenacin (Vesicare)
    Muscarinic antagonist for incontinence
  40. Darifenacin (Enablex)
    M3 antagonist for incontinence
  41. Propantheline Br
  42. Benztropine (Cogentin)
    Parkinsons; sedation
  43. Procyclidine
  44. Trimethaphan camphorsulfonate
    MINUTE TO MINUTE CONTROL; controls intracranial bleeding during surgery
  45. Mecamylamine
    Smoking cessation; bad b/c of orthostatic hypotension
  46. d-tubocurarine
    parenteral ONLY, neuromuscular blocker
  47. metocurine
    neuromuscular blocker with WORST CV effects
  48. Succinyl choline
    Only depolarizing neuromuscular blocker used therapeutically; perfect poison
  49. Norepinephrine CV effect
    a1 (inc BP), b1 (dec HR)
  50. Epinephrine CV effect
    a1 and b2 (no BP change), b1 (inc HR)
  51. isoproterenol CV effect
    b2 (dec BP), b1 (inc HR)
  52. l-Norepinephrine (Levophed)
    a, b1, pressor
  53. epinephrine
    a, b1, b2; for anaphylaxis (EPIPENS) and glaucoma
  54. Phenylephrine
    full a1, nasal decongestant, glaucoma
  55. Naphazoline
    Partial a agonist; decongestant; TACHYPHYLAXIS
  56. Tetrahydrozoline (Visine)
    Partial a agonist; ophthalmic decongestant; TACHYPHYLAXIS
  57. Oxymetazoline (Afrin, Visine)
    Partial a agonist; decongestant; TACHYPHYLAXIS
  58. alpha 1 agonist contraindication
  59. Clonidine
    a2, for HTN or opiate withdrawal
  60. Guanbenz
    a2; Open ring imidazoline; HTN
  61. guanfacine
    a2; Open ring imidazoline; HTN
  62. methyldopa
    a2; PRODRUG; HTN
  63. Apraclonidine
    a2; glaucoma
  64. tizanidine
    a2, muscle relaxer
  65. a2 agonists most important indications
    antihypertensives, alcohol withdrawal but cause withdrawal themselves
  66. a2 agonist SE
    sedation, NA/water retention, dry mouth, withdrawal syndrome
  67. Isoproterenol
    b agonist (nonselective); asthma, COPD, SE: inc HR and BP
  68. b2 agonist structure characteristic
    large bulky group on N
  69. metaproterenol
    b2, asthma, COPD; resorcinol
  70. terbutaline
    b2, asthma, COPD, tocolytic; resorcinol
  71. albuterol
    b2, asthma COPD
  72. salmeterol
    b2, asthma, COPD
  73. salmeterol
    b2, slow onset/long duration, long term asthma, COPD
  74. formoterol
    b2, slow onset/long duration, long term asthma, COPD
  75. ritodrine
    b2, tocolytic
  76. zosins
    a1 antagonist for HTN (dec BP), but reflex tachycardia
  77. b agonist SE
    tachycardia, CNS stimulation at high doses, caution in CAD pts
  78. dobutamine
    mixed agonist; racemic; POSITIVE IONOTROPIC WITH LITTLE CHRONOTROPIC EFFECT for cardiac failure
  79. phenoxybenzamine
    a antagonist (nonselective), IRREVERSIBLE; pheochromacytoma
  80. phentolamine
    a antagonist (nonselective); vasodilator but reflex tachycardia
  81. prazosin
    a1 antagonist, smooth muscle relaxation in BPH, 1st dose effect
  82. terazosin
    a1 antagonist, smooth muscle relaxation in BPH, 1st dose effect
  83. doxazosin
    a1 antagonist, smooth muscle relaxation in BPH, 1st dose effect
  84. yohimbine
    a2 antagonist; indole alkaloid (aphrodesiac), inc BP and HRs
  85. propranolol
    b blocker (nonselective); HTN but contraindicated in COPD and asthma
  86. beta antagonist SE
    bradycardia, bronchostriction, WITHDRAWAL (ALL Can be used for glaucoma)
  87. therapeutic uses for b blockers
    HTN, angina, arrhythmias, migraine, stage fright, thyrotoxicosis, CHF
  88. Nadolol
    B blocker (nonselective); less lipophilic than propranolol
  89. Timolol (timoptic)
    B blocker (nonselective); glaucoma
  90. Pindolol
    B blocker (nonselective); PARTIAL � ISA
  91. Carteolol
    B blocker (nonselective); PARTIAL � ISA
  92. Metoprolol
    b1, for almost all cardiac conditions
  93. bisoprolol
    b1, for almost all cardiac conditions
  94. atenolol
    b1, PERFECT B BLOCKER (cardioselective, low lipophilicity, long duration); HTN and angina
  95. esmolol
    b1, cleared quickly b/c of ester group (IV infusion used in emergency to stop heart)
  96. B blocker SE
    1. bradycardia 2. AV block 3. Sedation 4. Masked hypoglycemia sx 5. Withdrawal
  97. B blocker (nonselective) contraindications
    Asthma, COPD, late stage CHF
  98. Labetalol
    B blocker (nonselective), a1 antagonist; racemic mix prevents reflex tachy (BETTER THAN PRAZOSIN)
  99. Carvedilol
    B blocker (nonselective), a1 antagonist; racemic (no reflex tachy)
  100. Metyrosine
    Blocks tyrosine hydroxylase; no NE, DA, Epi produced
  101. Reserpine
    indole alkaloid; Blocks vesicular storage of DA, NE, 5HT; sympatholytic, causes Parkinsons sx and depression
  102. Bretylium
    Blocks NE release; antiarrhythmic
  103. Renin
    Angiotensin � ang I � ang II � vasoconstriction/aldosterone (inc Na and water reabsorp)
  104. Hindbrain
    Medulla and pons (cerebellum)
  105. Medulla
    Respiration, cardiac, vasomotor
  106. Cerebellum
  107. Forebrain
    Higher struc (thalamus, hypothalamus, basal ganglia, limbic)
  108. Thalamus
    Relay station to and from cortex
  109. Hypothalamus
  110. Basal ganglia
    Voluntary motor
  111. Limbic
    Hippocampus, amygdala (Emotions, memory)
  112. EPS sx
    Dystonia, pseudoparkinsonism, tremor, akathisia
  113. EPS tx
    Benztropine, artane, anticholinergics, antihistamines, DA releasing agents
  114. Tardive dyskinesia sx
    IRREVERSIBLE; mouth movements, choreiform, athetoid, to and fro movements
  115. Neuroleptic malignant syndrome
    Serious. Rapid. Fatal.
  116. Chlorpromazine
    FIRST 1st gen antipsychotic; phenothiazine
  117. Promethazine
    1st gen antipsychotic; antiemetic
  118. Thioridazine
    1st gen antipsychotic; MANY MANY SE
  119. Fluphenazine
    1st gen antipsychotic; EPS
  120. Proclorperazine
    1st gen antipsychotic; antiemetic
  121. Perphenazine
    1st gen antipsychotic; CATIE equal efficacy but tardive dyskinesia
  122. Thiothixene
    1st gen antipsychotic; modest EPS
  123. Haloperidol
    1st gen antipsychotic; EPS
  124. Molindone
    1st gen antipsychotic; moderate EPS
  125. Pimozide
    1st gen antipsychotic; tourette�s
  126. Clozapine
    2nd gen antipsychotic; agranulocytosis
  127. Olanzapine
    2nd gen antipsychotic; (clozapine bioisostere) wt gain and diabetes
  128. Quetiapine (Seroquel)
    2nd gen antipsychotic; metabolite w/antidepressant property
  129. Risperidone
    2nd gen antipsychotic; designed to be 5HT2 AND D2 antagonist
  130. Ziprasidone
    2nd gen antipsychotic; prolongs QT interval
  131. Lurasidone
    2nd gen antipsychotic; low doses similar effectiveness as high (fast onset; days without titration)
  132. Aripiprazole (abilify)
    2nd gen antipsychotic; D2 partial agonist, 5HT1A (anxiety)
  133. Phenelzine
    Nonselective MAO inhibitor; depression
  134. Selegiline
    MAO-B; antidepressant and parkinsons
  135. Moclobemide
    MAO-A; antidepressant; REVERSIBLE so no cheese syndrome
  136. MAO inhibitors SE
    Hypertensive crisis, avoid tyramine, lots of interactions an SE
  137. TCA indications
    Depression, panic, chronic pain, enuresis BUT CAUTION SUICIDE
  138. Imipramine
    TCA (enuresis and ADHD)
  139. Amitriptyline
  140. Clomipramine
    TCA, OCD
  141. TCA moa
    NET/SERT blockers
  142. Desipramine
    TCA secondary amine from imipramine
  143. Nortriptyline
    TCA secondary amine from amitriptyline
  144. TCA SE
    LESS everything but pts may be suicidal
  145. SSRI uses
    MANY b/c of modest SE
  146. SSRI SE
    SERT blocker; no antimuscarinic but ANXIETY, SEXUAL SE, insomnia, tremor
  147. Vilazodone
    (antidepressants) SSRI and 5ht1a partial agonist (REDUCED SEXUAL SE)
  148. Maprotiline
    Tetracyclic NET inhibitor (antidepressants)
  149. Amoxapine
    (antidepressants) tetracyclic NET inhibitor; D2 antagonist
  150. Mirtazapine
    (antidepressants) targets a bunch of RECEPTORS; tetracyclic
  151. Bupropion
    (antidepressants) unicyclic; GAD
  152. Trazodone
    (antidepressants) 5ht2 antagonist
  153. Venlafaxine
    (antidepressants) SNRI; GAD and panic
  154. Desvenlafaxine
    (antidepressants) SNRI
  155. Duloxetine (Cymbalta)
    (antidepressants) SNRI; GAD and peripheral neuropathy
  156. Milnacipran
    (antidepressants) SNRI; fibromyalgia
  157. Atomoxetine
    (antidepressants) NSRI; ADHD; NOT APPROVED for depression
  158. Lithium
    MANIA; Gq; small TI with dose related SE and toxicity; lag time
  159. Psychostimulant uses
    Appetite suppressant; narcolepsy; ADHD
  160. Psychostimulant pharmacophore
    • Adderall
    • [psychostimulants] Mixture of + salts and racemic amphetamine; ADHD; longacting
  161. Amphetamine MOA
    Monoamine releasing agent
  162. Cocaine
    [psychostimulants] Esterases cleave so not given orally; block reuptake of DA, 5HT, NE
  163. Methylphenidate (Ritalin, concerta)
    [psychostimulants] narcolepsy, ADHD; DAT and NET
  164. Straterra (Atomoxetine)
    [psychostimulants] but NOT a stimulant; ADHD; NET
  165. Modafinil
    [psychostimulants] narcolepsy, little euphoria low addiction but $$$
  166. R-modfainil (Nuvigil)
    [psychostimulants] narcolepsy; cheaper
  167. Vyvanse (lisdexamfetamine)
    [psychostimulants] PRODRUG; only orally active
  168. Intuniv
    [psychostimulants] a2 agonist for pts who cant tolerate psychostimulant; long acting form of ganfacine
  169. Phentermine
    [psychostimulants] appetite control
  170. Phenmetrazine
    [psychostimulants] appetite control
  171. Benzphetamine
    [psychostimulants] appetite control
  172. Diethylpropion
    [psychostimulants] appetite control drug of choice
  173. Trimethylxantine
    [psychostimulants] Caffeine
  174. Dimethylxanthines
    [psychostimulants] Theophylline and thebromine
  175. Cathinone
    [psychostimulants] bath salts
  176. L-dopa (levodopa)
    [parkinsons] gold standard
  177. Carbidopa
    [parkinsons] peripheral acting decarboxylase inhibitor
  178. Sinemet
    [parkinsons] Carbidopa and L-DOPA; requires functional dopamine synthesis
  179. Entacapone (comtan)
    [parkinsons] only COMT inhibitor avail; given when pt begins experiencing end-of-dose wearing off
  180. Stalevo
    [parkinsons] levodopa + sinemet + comtan; inc �on time�
  181. Apomorphine
    [parkinsons] mixed D1 D2 partial agonist
  182. Pramipexole
    [parkinsons] D2/D3 agonist
  183. Ropinirole
    [parkinsons] D2/D3 agonist, N/V; also for restless legs
  184. Rotigotine NeuroPro
    [parkinsons] D2/D3 agonist, N/V; transdermal
  185. Bromocriptine
    [parkinson] ergoline, D2
  186. Pergolide
    [parkinsons] ergoline, D2
  187. Dihydrexidine
    [parkinsons] d1 agonist; NICHOLS DRUG
  188. MPTP
    Activated by MAO-B to MPP and induces parkinsonism
  189. Deprenyl (selegiline)
    [parkinsons] MAO B inhibitor; SLOWS progression, neuroprotectives
  190. Rasagiline mesylate
    [parkinsons] MAO B inhibitor; SLOWS progression, neuroprotectives
  191. psyhadelics
    5HT2A agonists, tachycardia, extreme tolerance but no DA inc so no abuse
  192. Psilocin
    [psychadelics] tryptamine; mushroom
  193. Psilocybin
    [psychadelics] tryptamine; mushroom
  194. DMT
    [psychadelics] tryptamine; natural plant alkaloid smoked or injected
  195. LSD
    [psychadelics] Lysergic acid diethylamide; ergoline
  196. Phenethylamine psychadelics
    Substituted amphetamines developed from mescaline
  197. Phenethylamine psychedelic pharmacology
    Activate 5ht2a; low toxicity; nonaddicting; rapid tolerance
  198. Ecstasy (MDMA)
    [psychadelics] not a hallucinogen; 5HT (serotonin syndrome-death) and DA(abuse) release; several deaths
  199. THC
    [psychadelics] CB1/2 agonist; not an alkaloid; GPCR
  200. THC medical uses
    AIDS wasting, glaucoma, nausea from chemo, multiple sclerosis
  201. THC SE
    Impaired short term memory, panic or anxiety from potent marijuana, cannabis dependence in 1/9, bronchitis, psychosis
  202. PCP (phencyclidine)
    [psychadelics] toxic psycotomimetic that causes schizo-like effects
  203. Ketamine
    [psychadelics] less dangerous than PCP but still dissociative; dependence and addiction
  204. �Spice�
    Synthetic cannabinoids
  205. Fomepizole
    [alcohol] inhibits ADH and used for ethylene glycol/methanol poison
  206. Disulfuram
    [alcohol] inhibits ALDH; makes you sick if you use alcohol
  207. Naltrexone
    [alcohol] alcoholism tx; opioid antagonist that dec cravings
  208. Acomprosate
    [alcohol] alcoholism tx; NMDA antagonist that reduces withdrawal sx
  209. Sedative defn
    Calms anxiety; dec excitement and activity; does NOT produce drowsiness or impair performance
  210. Hypnotic defn
    Induces natural SLEEP
  211. Anxiolytic defn
    Relieves anxiety WITHOUT sleep or sedations; not all anxiolytics are sedatives
  212. Narcotic defn
    Literally SLEEP PRODUCING; opioids/illegal drugs
  213. Factors that regulate sleep
    Age, sleep hx, drug ingestion, circadian rhythm
  214. GABA-a/BZD ligands at BZD site
    BZDs (PAM), non-BZDs like zolpidem, BZD antagoniss, inverse agonists (NAM)
  215. GABA-a/BZD ligands at other sites
    Bbts, alcohol, GABA antagonists, GABA agonists, etomidate and propofol
  216. BZD 1 position
    Active source of metabolits
  217. BZD 5 position
    Decreased activity if substituted
  218. BZD 7 position
    Inc affinity if group is electronegative
  219. BZD 1-2 position
    Electron rich ring = high affinity but dec half life
  220. Slow elimating BZDs
    Chlordiazepoxide, Diazepam, Flurazepam, Clorazepate, Quazepam, Prazepam
  221. Chlordiazepoxide
    [sedative-hypnotics] slow; anxiolytic and alcohol withdrawal
  222. Diazepam (Valium)
    [sedative-hypnotics] slow; anxiolytic, alcohol withdrawal (DOC), convulsive disorders
  223. Flurazepam
    [sedative-hypnotics] slow; hypnotic
  224. Clorazepate
    [sedative-hypnotics] slow; anxiolytic, alcohol withdrawal;, convulsive disorders
  225. Quazepam
    [sedative-hypnotics] slow; hypnotic
  226. Prazepam
    [sedative-hypnotics] slow; anxiolytic
  227. Intermediate eliminating BZDs
    Alprazolam, Lorazepam, Clonazepam, Oxazepam, Temazepam, Estrazolam
  228. Alprazolam
    [sedative-hypnotics] intermediate; anxiolytic and anesthetic
  229. Lorazepam
    [sedative-hypnotics] intermediate anxiolytic, hypnotic
  230. Clonazepam
    [sedative-hypnotics]; intermediate; anticonvulsant
  231. Oxazepam
    [sedative-hypnotics] intermediate; anxiolytic and alcohol withdrawal
  232. Temazepam
    [sedative-hypnotics] intermediate; hypnotic
  233. Estrazolam
    [sedative-hypnotics] intermediate; DC�ed
  234. Rapid eliminating BZDs
    Midazolam, triazolam
  235. Midazolam
    [sedative-hypnotics]; rapid; anesthesia
  236. Triazolam
    [sedative-hypnotics]; rapid; hypnotic
  237. Slow eliminating BZD characteristics
    Accumulation, active metabolites, sedation, useful in pts who wake up in the middle of the night
  238. Intermediate to rapid eliminating BZDs characteristics
    Preferred in hepatic problems and elderly, alter liver enzymes, rapid tolerance, rebound insomnia
  239. BZD indications
    Anxiolytic, hypnotic, epilepsy, alcohol withdrawal, muscle relaxant, anesthetic
  240. BZD SE
    Sedation, weakness, HA, nausea, vertigo, paradoxical effects, but LOW abuse potential
  241. Flumazenil
    [sedative-hypnotics] BZD and Z hypnotic overdose; neutral antagonist (Safe)
  242. Flumazenil SE
    [sedative-hypnotics] induce convulsions and panic attacks
  243. Zolpidem
    [sedative-hypnotics] non BZD Z-hynpnotic; short term insomnia tx; sometimes abused
  244. Zaleplon
    [sedative-hypnotics] non BZD Z hypnotic; BZ1; short term insomnia tx; rapid acting
  245. Eszopiclone (Lunesta)
    [sedative-hypnotics] nonBZD Z hypnotic; LONG TERM insomnia tx; allows you to sleep through the night
  246. Z hypnotics
    [sedative-hypnotics] PAMS, more selective than BZDs; cause less neg effects on sleep than BZDs
  247. Z hypnotics SE
    Daytime drowsiness, sleep-activities
  248. Flunitrazepam
    [sedative-hypnotics] BZD; ROOFIES; anterograde amnesia
  249. Phenobarbital
    [sedative-hypnotics] barbiturate, anticonvulsant, long acting
  250. Barbiturate pharmacology
    [sedative-hypnotics] More dangerous (CV and resp depression) but sleep effects similar to BZDs
  251. GABA-B receptor
    Metabotropic; Gi/o; heterodimer
  252. Baclofen
    [sedative-hypnotics] GABA-b agonist; muscle relaxant; alcoholism tx
  253. GABA-B antagonists
    Phaclogen, saclofen, 2-hydroxysaclofen
  254. Xyrem (GHB)
    [sedative-hypnotics] DATE RAPE DRUG; dual classified; special administration procedures; used for sleep disorders
  255. Gamma-hydroxybutyric acid (GHB)
    [sedative-hypnotics] illicit drug; loss of consciousness
  256. Ramelteon (Rozerem)
    [sedative-hypnotics] Melatonin agonist; faster sleep onset (insomnia); NO ABUSE, WITHDRAWAL, DEPENDENCY
  257. Antihistamines used as sleep aids
    [sedative-hypnotics] Diphenhydramine, doxylamine, pyrilamine
  258. Sedative hypnotic abuse
    Similar effects to etOH; euphoria; dependence (except rozerem)
  259. Types of anxiety
    GAD, panic, OCD, social, PTSD, anxiety from medical issues
  260. Anxiolytic BZDs
    Alprazolam, chlordiazepoxide, clonazepam, clorazepate, diazepam, lorazepam, oxazepam
  261. Buspirone
    [anxiolytics] partial 5HT1A agonist; longer onset than BZD but less abuse; NOT GOOD FOR PANIC
  262. Buspirone advantages
    little/no sedation, no CNS depression, no muscle relaxation, little abuse tolerance or withdrawal
  263. Buspirone disadvatanges
    Slow onset, not for severe or panic, best in BZD-naive pts
  264. SSRI anxiolytic use
    OCD and panic 1st line
  265. SSRI anxiolytics
    Fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram
  266. Clomipramine [anxiolytics]
    TCA; 2nd line for OCD
  267. Venlafaxine [anxiolytics]
    SNRI for GAD, social, panic
  268. Duloxetine [anxiolytics]
    SNRI for GAD
  269. Propranolol [anxiolytics]
    Social and PTSD (nightmares)
  270. Hydroxyzine [anxiolytics]
    Histamine h1 antagonist
  271. Clonidine [anxiolytics]
    a2 agonist; panic and anxiety from withdrawal
  272. factors triggering seizure
    stress/fatigue, blood gas and ph, hypoglycemia, light/sound/touch, alcohol withdrawal
  273. Maximal electricshock (MES) model
    [anticonvulsant] tonic-clonic (TC), complex partial
  274. Metazole model
    [anticonvulsant] GABA-A NAM; drug-induced and absence
  275. Kindled-limbic
    [anticonvulsant] repeated electrical stimulation; complex and tests effectiveness
  276. Phenytoin
    [anticonvulsant] Na channels; partial, TC
  277. Phenytoin SE
    [anticonvulsant] nystagmus, chronic stuff like hirsutism, SJS
  278. Phenytoin interactions
    [anticonvulsant] Induces p450, CBZ enhances and gets enhanced
  279. Fosphenytoin
    [anticonvulsant] prodrug, metabolized by phosphatases
  280. Ethotoin
    [anticonvulsant] TC, psychomotor seizures
  281. x-mephenytoin
    [anticonvulsant] d/c
  282. carbamazepine (CBZ)
    [anticonvulsant] Na channel, all except absence, neuralgias, DOC for partial
  283. CBZ SE
    [anticonvulsant] HEPATIC and blood
  284. CBZ interactions
    [anticonvulsant] autoinducer; clearance inhibited by valproic acid
  285. Oxcarbamazepine
    [anticonvulsant] Na channel; partial
  286. Phenobarbital [anticonvulsant]
    Partial and TC (infants)
  287. Phenobarbital SE
    [anticonvulsant] sedation, dependence, and paradoxical in kids
  288. Phenobarb interactions
    [anticonvulsant] CBZ, valproate, lamotrigine, tiagabine, zonisamide
  289. Primidone
    [anticonvulsant] TC, simple, complex, adjunct
  290. Mephobarbital
    [anticonvulsant] not really used
  291. BZDs as anticonvulsants
    Diazepam, lorazepam, midazolam, chlorazapate, clonazepam
  292. BZDs as anticonvulsants indication
    Status epilepticus
  293. Gabapentin
    [anticonvulsant] partial, neuropathic pain, migraine
  294. Gabapentin MOA
    [anticonvulsant] inc GABA, modulates Ca
  295. Pregabalin
    [anticonvulsant] neuropathy (diabetic and post herpetic), anxiety
  296. Vigabatrin
    [anticonvulsant] irreversible GABA transaminase inhib; use in refractory
  297. Tiagabine
    [anticonvulsant] GAT inhibitor; partial; TC
  298. Lacosamide
    [anticonvulsant] Na channels; CRMP-2
  299. Rufinamide
    [anticonvulsant] triazole deriv w/little similarity to others; partial and Lennox Gastaut
  300. Lamotrigine
    [anticonvulsant] Na channel; partial and absence adjunct
  301. Zonisamide
    [anticonvulsant] partial in pts >12
  302. Levetiracetam
    [anticonvulsant] GABA, Ca channel; partial adjunct
  303. Ionotropic excitatory amino acid receptors [anticonvulsant]
    NMDA, AMPA, kainite
  304. NMDA activation
    [anticonvulsant] Glu binding, Glycine, Mg removal from cell depolarization
  305. Felbamate
    [anticonvulsant] NMDA antagonist; 3rd line bc of APLASTIC ANEMIA and HEPATOTOXIC
  306. Topiramate receptor effects
    [anticonvulsant] kainite/AMPA antagonist; Na channels; GABA-a
  307. Topiramate use
    [anticonvulsant] partial onset, TC, has CNS SE
  308. Ethosuximide
    [anticonvulsant] Ca channels; ABSENCE ONLY
  309. Phensuximide
    [anticonvulsant] ethosuximide deriv
  310. Methsuximide
    [anticonvulsant] ethosuximide deriv
  311. Valproic acid
    [anticonvulsant] generalized and absence
  312. Dilvaproex sodium
    [anticonvulsant] valproic acid deriv; ABSENCE and generalized; monitor liver fct
  313. Grand mal/TC drugs of choice
    CBZ, phenytoin, valproate
  314. General absence DOC
  315. Partial DOC
    CBZ/oxCBZ, phenytoin, valproate
  316. Atypical DOC
  317. Myoclonic DOC
  318. Atonic DOC
  319. Status epilepticus DOC
    Diazepam, lorazepam
  320. Diazepam [muscle relaxants]
    SPASMOLYTIC; GABA A, CNS and spinal cord, sedation
  321. Baclofen [muscle relaxants]
    SPASMOLYTIC; GABA B, CNS and spinal cord, less sedation than BZDs, WARNING for withdrawal syndrome from intrathecal use
  322. Tizanidine [muscle relaxants]
    SPASMOLYTIC; a2 agonist; clonidine congener
  323. cyclobenzaprine (flexeril)
    [muscle relaxants] SPASMOLYTIC; tricyclic; sedation; ACUTE
  324. Chlorzoxazone
    [muscle relaxants] SPASMOLYTIC; similar to flexeril
  325. Orphenadrine
    [muscle relaxants] SPASMOLYTIC; similar to flexeril
  326. Carisprodol
    [muscle relaxants] SPASMOLYTIC; similar to flexeril; drug seekers
  327. Dantrolene sodium
    [muscle relaxants] SPASMOLYTIC; ONLY ONE TO WORK AT MUSCLE; blocks contractions
  328. Dantrolene sodium indications
    [muscle relaxants] cerebral palsy, MS, MALIGNANT HYPERTHERMIA
  329. Spasmolytic indications
    CHRONIC neurological diseases and ACUTE injury
  330. Short acting neuromuscular blockers
    [muscle relaxants] succinylcholine, mivacurium
  331. Intermediate acting neuromusc blocker
    [muscle relaxants] atracurium, vecuronium, rocuronium
  332. Long acting neuromusc blocker
    [muscle relaxants] pancuronium
  333. Neuromusc blocker indications
    Musc relaxation during surgery, endotracheal intub, controlled ventilation
  334. Ether
    [anesthetics] inhaled; EXPLOSIVE, irritant, N/V
  335. Nitrous oxide
    [anesthetics] inhaled; good analgesia and good for short procedures (rapid)
  336. Halothane (Fluothane)
    [anesthetics] inhaled; less analgesia and musc relaxation, hepatoxic, INC MYOCARDIUM SENSITIVITY
  337. Enflurane
    [anesthetics] inhaled; similar to but less toxicity than halothane
  338. Isoflurane
    [anesthetics] inhaled; dec mean arterial pressure
  343. LOW solubility effect on induction
    FAST induction
  344. HIGH solubility effect on induction
    SLOW induction
  345. MAC
    Minimum conc in alveoli to eliminate pain response in 50% of pts
  346. Inhalation anesthetics SE
    Dec brain metabolic rate and inc intracranial pressure; MALIGNANT HYPERTHERMIA
  347. Malignant hyperthermia
    Massive Ca release; tachy, HTN, hyperkalemia, muscle rigidity, hyperthermia; genetics
  348. Ketamine [anesthetics]
    IV; dissociative; blocks Glu receptors
  349. Etomidate
    [anesthetics] IV; non-bbt, high N/V
  350. Propofol
    [anesthetics] IV; similar to etOH; antiemetic; rapid onset and recovery
  351. Thiopental
    [anesthetics] IV; short acting Bbt
  352. Midazolam [anesthetics]
    IV, BZD, very short acting
  353. IV Anesthetics
    Most do not have good analgesia
  354. Local anesthetics MOA
    Block sensory transmission to brain; block Na channels (CAINES)
  355. Local anesthetics SAR
    Esters or amides; weak bases; lipid sol = potency = onset rate
  356. Cocaine [anesthetics]
    Local ester; medium duration
  357. Procaine
    [anesthetics] local ester; short duration
  358. Tetracaine
    [anesthetics] local ester; long duration
  359. Benzocaine
    [anesthetics] local ester; topical only
  360. Lidocaine
    [anesthetics] local amide; medium duration
  361. Mepivacaine
    [anesthetics] local amide; medium dur
  362. Bupivacaine
    [anesthetics] local amide; long dur
  363. Local anesthetic toxicities
    CNS (sedation, restlessness, nystagmus, convulsions), CV (arrhythmias, vasodilation, block), Allergic
  364. m (Mu) opioid receptor
    analgesia; euphoria; resp depression, miosis, constipation, tolerance, withdrawal
  365. K (kappa) opioid receptor
    Analgesia, SEDATION, DYSPHORIA but less miosis, resp depression and dependence
  366. d (delta) opioid receptor
  367. orphanin opioid receptor like subtype 1 (ORL1)
    ANTAGONIZE for analgesia, Gi/o
  368. Phenanthrene SAR 3 position
    [Opioids] substitution = dec potency - codeine
  369. Phenanthrene SAR 6 position
    [Opioid] inc activity � hydromorphone, oxycodone
  370. Phenanthrene SAR 14 position
    [Opioid] inc acitivity � oxycodone
  371. Phenanthrene SAR N-allyl
    Antagonist � naloxone/ naltrexone
  372. Codeine
    [Opioid] weak analgesia, good antitussive, CYP2d6 converts to morphine
  373. Morphine
    [Opioid] severe, acute, chronic pain
  374. Hydromorphone (Dilaudid)
    [Opioid] severe
  375. Oxymorphone
    [Opioid] severe
  376. Levorphanol
    [Opioid] severe
  377. Apomorphine
    [Opioid] emetic; parkinsons
  378. Hydrocodone (Vicondin, Lortab)
    [Opioid] moderate
  379. Oxycodone/aspirin
    [Opioid] mod to severe
  380. Oxycontin
    [Opioid] controlled release oxycodone. Hillbilly heroin abuse
  381. Dextromethorphan (DXM)
    [Opioid] antitussive only
  382. Heroin (diacetylmorphine)
    [Opioid] low m affinity, high lipophilicity, metabolized to 6acetylmorphine
  383. Meperidine (Demerol)
    [Opioid] M agonist, no antitussive, less SE than phenanthrenes
  384. Methadone
    [Opioid] M agonist, treats pain and ADDICTION (long duration)
  385. Tramadol (Ultram)
    [Opioid] Weak m, inhibits 5HT and NE reuptake; non addicting, no resp depression, no constipation
  386. Ketorolac
    [Opioid] NSAID for severe; short term use only
  387. Tapentadol
    [Opioid] weak m agonist and inhibit NET; lower SE profile
  388. Methotrimeprazine
  389. Fentanyl injection
    [Opioid] anesthetics; m agonist, MORE POTENT THAN MORPHINE
  390. Sufentanil
    [Opioid] anesthetics, m agonist, fentanyl bioisostere; SUPER POTENT
  391. Alfentanil
    [Opioid] anesthetics, m agonist, MORE POTENT THAN MORPHINE. Ultra short acting
  392. Remifentanil
    [Opioid] anesthetic. Selective m; similar to alfentanil
  393. Diphenoxylate with atrophine (Lomotil)
    [Opioid] antidiarrheal
  394. Difenoxin with atropine (Motofen)
    [Opioid] antidiarrheal; active metabolite of diphenoxylate
  395. Loperamide (Imodium)
    [Opioid] OTC antidiarrheal; travelers diarrheal; caplet or liquid
  396. Buprenorphine
    [Opioid] mixed activity; treats opioid withdrawal and addiction
  397. Butorphanol
    [Opioid] mixed; morphinan struc;
  398. Nalbuphine
    [Opioid] mixed; phenanthrene; k agonist, m antagonist (produces withdrawal)
  399. Pentazocine
    [Opioid] benzomorphan struc; k agonist, m antagonist
  400. Dezocine
    [Opioid] partial m, postop and cancer pain
  401. Pentazocine and naloxone combination (Talwin)
    [Opioid] orally = naloxone not bioavail. Injected = naloxone blocks opioid action of pentazocine
  402. Naloxone
    [Opioid] m antagonist; IV; no antitussive; for opioid overdose
  403. Naltrexone
    [Opioid] oral; blocks heroin effects, etOH dependence
  404. Nalmefene
    [Opioid] longer acting version of naloxone
  405. Drugs for mild pain
    Aspirin, APAP, Ibu, NSAIDs, Cox2
  406. Drugs for moderate pain
    Codeine, Darvocet, tylox, Percocet
  407. Drugs for severe pain
    Morphine, hydromorphone, meperidine, pentazocine
  408. Therapeutic use of opioids
    Cough, constipating effect, pulm edema, sedative, anesthesia, addiction
  409. Agonist maintenance for long term tx of opioid addiction
    Methadone maintenance � stabilize, cross tolerance to heroin, tolerance to sedation
  410. Partial agonist therapy for long term tx of opioid addiction
    Buprenorphine � cross tolerance, blocks effect, long acting and low tol
  411. Antagonist maintenance for long term tx of opioid addiction
    Naltrexone � does not alleviate cravings
  412. negative log P
    hydrophilic; electronegative groups like O, N
  413. positive log P
    hydrophobic; phenyl rings, Br, I (large groups)
  414. positive sigma value
    electron withdrawing; NO2 > SO2NH2 > esters, amides
  415. negative sigma value
    electron donating; NH2 > OCH3, OH
  416. parasymp control of eye
    M3: lacrimation, miosis dec IOP
  417. symp control of eye
    a1: mydriasis, dec IOP / b: inc IOP
  418. parasymp control of heart
    M3: slows
  419. symp control of heart
    B1: inc HR and force
  420. parasymp control of lung
    M3: bronchostriction
  421. symp control of lung
    B2: bronchodilation
  422. parasymp control of GI
    M3: SLUD
  423. symp control of GI
    a1: bladder constrictions (holding your pee) so a1 antagonists good for BPH
  424. symp control of blood vessels
    a1: HTN
  425. symp control of kidney
    b1: inc renin, inc BP, D1 DA activation
  426. a methyl groups on ACh
    Nicotinic selective
  427. b methyl groups on ACh
    muscarinic selective
  428. direct parasympathomimetics indications
    glaucoma, miosis
  429. direct parasympathomimetics contraindications
    asthma COPD
  430. direct parasympathomimetics SE
    SLUD, confusion
  431. Varenicline
    special direct parasympathomimetic bc it acts on NICOTINIC receptors
  432. use atropine for overdose of these indirect parasympathomimetics
    stigmines, memantine
  433. scopolamine
    parasympatholytic for sea sickness
  434. what to use as anti-GI spasms
    quaternary amines (stays in gut, cant reach brain)
  435. parasympatholytic SE
    sedation, dry mouth, blurry eyes, coma, death, tachycardia (block M2 in heart)
  436. ganglionic blocker structure
    n= 5 or 6
  437. neuromuscular blocker structure
    n = 7 or greater
  438. ganglionic nicotinic blocker indication
    controlled surgical hypotension
  439. neuromuscular nicotinic blockers
    succinylcholine, Curiums, caution DEATH by resp paralysis
  440. NET and DAT
    uptake 1; presynaptic
  441. uptake 2
    cationic; postsynaptic
  442. VMA
    from MAO and COMT; too much in urine = pheochromacytoma
  443. a1 receptors
    vessels; inc BP, dec aq humor, mydriasis
  444. a2 receptors
    brain; presynaptic; dec BP and HR
  445. b1 receptors
    heart, kidney, inc HR and force and BP (renin)
  446. b2 receptors
    lungs, inc bronchodilation, inc aq humor
  447. psychostimulant indications
    ADHD, narcolepsy
  448. droperidol
    typical antispychotic for antiemesis
  449. typical antipsychotics
    D2 so EPS that may progress to TARDIVE DYS (permanent)
  450. atypical antipsychotics
    5HT2A, less EPS and TD but weight gain and diabetes; treat negative sx better
  451. MAOIs
    irreversible; cheese syndrome (inc tyramine = inc BP, HR)
Card Set
407 flashcards.txt
407 final flashcards updated