Pharm Gen Concepts 1

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Pharm Gen Concepts 1
2012-07-20 14:15:08

Pharm Gen Concepts 1
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  1. Theophylline MOA
    • PDEase inhibitors; prevents breakdown of CAMP into 5'AMP
    • Antagonizes adenosine receptors
  2. Theophylline therapeutic uses
  3. Caffeine MOA
    • PDEase inhibitor, promotes wakefulness
    • antagonizes adenosine A1 and A2
  4. Caffeine effects
  5. Caffeine uses
  6. Sildenafil MOA
    inhibits phosphodiesterase type 5, enhancing effects of nitric oxide-activated increases in cGMP
  7. Sildenafil therapeutic uses
    • relaxes mm and inc BF to particular areas of the body (viagra)
    • ED
    • Revatio: rx pulm art hypertension and improve exercise capacity in men and women.
  8. Papaverine
    PDEase inhibitor
  9. Acetazolamide MOA
    carbonic anhydrase inhib (makes urine more basic to increase excretion of WA like aspirin)
  10. Acetazolamide uses
    CHF, altitude sickness, glaucoma, seizure disorders
  11. Ammonium chloride MOA
    makes urine more acidic to inc excretion of WB like amphetamine
  12. Acetylcholine
    cholinergic agonists
  13. methacholine
    cholinergic agonist
  14. carbachol (carbamycholine)
    cholinergic agonist
  15. bethanechol
    cholinergic agonist
  16. succinylcholine
    cholinergic agonist
  17. pilocarpine
    cholinergic agonist
  18. Phenobarbital
    • induces CYP1A2, 2C, 3A4 (when you induce CYP450 isozymes, then drug effect is diminished bc there is more metab of the drug and more plasma Cl due to more active CYP450)
    • pharmokinetic tolerance
  19. Furanocoumarin
    • inhibits CYP1A2, 3A4 (inc drug effect bc dec hepatic Cl)
    • drug toxicity
  20. Phenobarbital MOA
    alters sensory cortex, cerebellar, and motor activities; produces sedation, hypnosis, and anesthesia (barbiturate)
  21. Phenobarbital uses
    • sedative
    • treat/prevent seizures
    • short term insomnia rx
  22. Phenytoin
    stimulates synth of CYP450
  23. Ethanol
    stim synth of CYP450
  24. Dioxin
    stim synth of CYP450
  25. PCBs
    stim synth of CYP450
  26. Rifampin
    (TB rx) stim synth CYP450
  27. Carbamezpine
    stim synth CYP450
  28. cigarette smoke
    stim synth CYP450
  29. DDT
    stim synth CYP450
  30. Cimetidine
    inhib synth of CYP450
  31. Isoniazid
    (TB rx) inhib synth of CYP450
  32. Ethanol (acute)
    inhib synth of CYP450
  33. Ketoconazole
    (fungal rx) inhib synth CYP450
  34. Erythromycin
    inhib synth CYP450
  35. Hemicholinium
    blcoks choline uptake so that Ach synthesis is blocked
  36. Opiates
    inhibit Ach release in GI
  37. Serotonin
    Amplifies release of Ach in GI
  38. Botunlinim toxin MOA
    binds to surface proteins and its light chain shows protease activity to cleave proteins used in storage and therefore release Ach-->cholinergic nt will stop and result in mm paralysis
  39. Botulinim Uses
    • blephoraspasm
    • strabismus
    • cervical dystonia
    • laryngela dystonia
    • spasmodic torticollis
    • myofascial pain syndrome
    • hemifacial spasm
  40. Tetanus toxin MOA
    acts in conjunction w/ spinal cord to prevent release of inhib nt and results in spastic paralysis
  41. Black widow spider toxin (alpha latrotoxin)
    releases lots of Ach by binding to neurexins in PM
  42. Neogstigmine
    Inhibits Achase: slowly reversible carbamate inhibitor
  43. Malathion
    irreversible organophosphate inhib of Achase
  44. Carbachol
    agonist of nicotinic and muscarinic receptors
  45. Carbachol uses
    causes miosis after surgery in anterior chamber of the eye
  46. Methacholine 
    • provocholine
    • muscarinic agonist
  47. Methacholine uses
    proactive agent in dx of bronchial asthma
  48. Bethanechol
    • urecholine
    • muscarinic agonist w/ selective action on GI and GU
  49. Bethanechol Uses
    Rx bowel stasis, postoperative paralytic ileus, urinary retention
  50. Bethanechol CI
    CHF, hyperthyroidism, asthma, COPD, peptic ulcers
  51. Succinylcholine
    • cholinergic receptor agonist
    • IV: initial skel mm contraction then flaccid paralysis for 3-5min from constant depolarization of MEP (uses non competitive blocking of Ach)
  52. Succinylcholine Termination
    Determined by concentration of plasma cholinesterase before even at NMJ; diffusion away from NMJ determines true termination
  53. Pilocarpine
    • selective muscarinic agonist
    • Pilocar, Isopto Carpine
  54. Pilocarpine Uses
    rx of glaucoma, dry mouth from Sjorgren's
  55. Pilocarpine Terminatino
    Degraded by hepatic enz and not metabolized by Achase or pseudocholinesterase
  56. Cevimelline
    • Evoxac
    • synthetic muscarinic agonist
  57. Pilocarpine and Glaucoma MOA
    • muscarinic receptor agonist
    • contracts meridional fibers of ciliary mm-->increases iridocorneal angle and/or tone and alignment of slots-->more aqueous humor now flows through Schlemm
  58. Pilocarpine and glaucoma pharm effects
    • IOP decreases by 20% w/ persistent miosis that will give poor night vision
    • Contraction of ciliary mm gives fixation of lens for near vision so far vision impaired
  59. Betaxolol MOA
    • beta adrenoceptor antagonist 
    • Betaoptic
    • selectively blocks B1 receptors to decrease secretion of aqueous humor
  60. Betaxolol pharm effects
    • lowers IOP by 20-30%
    • bradycardia if any systemic absorption happens
  61. Betaxolol Uses
  62. Timolol MOA
    • Beta adrenoreceptor antagonist
    • timoptic
    • decreases secretion of aquesous humor since it blocks beta
  63. Timolol pharm effect
    • lowers IOP by 20-30%
    • bronchoconstriction and bradycardia if any systemic absorption happens
  64. Timolol uses
  65. Latanoprost MOA
    Analog of PGF2
  66. Latanoprost pharm effect
    • inc aqueous humor outflow
    • lowers IOP by 20-25%
  67. Latanoprost uses
  68. Bimatoprost Uses
  69. Bimatoprost MOA
    PGF2 analog, prolongs eye lash growth
  70. bimatoprost pharm effects
    inc length and thickness of eyelashes
  71. Epinepherin (glaucoma) MOA
    • glaucon, epitrate
    • <1% concentration: results in A2 stim-->dec synth of aq humor
    • >1% concentration: results in A1 stim--> inc normal outflow of aq humor
  72. Epinepherin Pharm effects
    either inc outflow of aq humor or dec its secretion; conc dependent

    causes mydriasis from stimulation of A1 in radial mm of iris
  73. Apraclonidine MOA
    stimulates A receptors
  74. Apraclonidine pharm effects
    reduces amt of aq humor to decrease IOP
  75. Apraclonidine Uses
    to decrease IOP after surgery
  76. Acetazolamide MOA
    • Diamox
    • carbonic anhydrase inhibitor on ciliary epithelium
  77. Acetazolamide pharm effect
    decreases production of aq humor
  78. Acetazolamide Uses
    to decrease IOP, glaucoma
  79. Dorzolamide MOA
    • Trusopt
    • carbonic anhydrase inhibitor on ciliary epithelium
  80. Dorzolamide pharm effect
    • dec IOP by 10-20%
    • decrease production of aq humor
  81. Dorzolamide Uses
    glaucoma, lower IOP
  82. Isofluophate (DFP) MOA
    Decreases amt of Ach available to contract meridional fibers of ciliary mm
  83. Isofluophate pharm effects
    lowers IOP
  84. Isofluophate uses
  85. Isofluophate AE
    toxicity and cataracts possible so only use on a pt if nothing else is working
  86. Echothiophate MOA
    binds irreversibly to Ach site on pseudoacetylcholinesterase (organophosphate cholinesterase inhibitor)
  87. Echothiophate uses
  88. Mannitol MOA
    • osmitrol
    • osmotic diuetic agent (elevates glomerular filtrate osmolarity)
  89. Mannitol Uses
    kidney failure (diuretic), dec IOP and brain P/swelling
  90. Mannitol pharm effects
    hyperosmolarity which leads to cellular dehydration and decreased IOP
  91. Mannitol uses
    angle-closure glaucomas
  92. Memantine MOA
    • Namenda
    • binds N-methyl-D-aspartate receptors, may slow Ca++ influx and nerve damage (NMDA receptor antagonist)
    • Note: prevents excitotoxicity and neuronal cell death (too much glutamate stimulation at NMDA receptors is bad but this prevents it)
  93. Memantine Uses
  94. Physostigmine MOA
    • Synapton
    • carbamate Achase inhibitor
  95. Physostigmine AE
  96. Physostigmine Uses
  97. Donepezil MOA
    • Aricept
    • carbamate Achase inhibitor
  98. Donepezil AE
    decreased apathy, hallucinations, anxiety, behavior prob, n/v, diarrhea, mm cramps, fatigue, peeing, bradycardia, anorexia, syncope, insomnia, vivid dreams
  99. Rivastigmine MOA
    • Exelon
    • carbamate Achase inhibitor
  100. Rivastigmine uses
  101. Galantamine
    • razadyne
    • carbamate Achase inhibitor
  102. Galantamine Uses
  103. Edrophonium MOA
    • tensilon
    • carbamate AChase inhibitor; only acts at NMJ via direct stimulation of cholinergic N2 receptors
  104. Edrophonium Uses
    • MG
    • distinguish btw MG and cholinergic crisis 
    • reverse mm paralysis from competive nm blocking agents (like D-tubocurarine)
  105. Neostigmine MOA
    • prostigmin
    • carbamate Achase inhibitor
    • Agonist at cholinergic N2 receptors (inhib Achase) at peripheral sites (results in increased Ach at N2 receptors of NMJ and muscarinics-heart, salivary)
  106. Neostigmine Uses
    • postoperative paralytic ileus
    • atony of GI/GU
    • MG
    • reversal of mm paralysis from competitive nm blocking stuff like D-tubocurarine
  107. Pyridostigmine
    • mestinon
    • carbamate Achase inhibitorAgonist at cholinergic N2 receptors (inhib Achase) at peripheral sites (results in increased Ach at N2 receptors of NMJ and muscarinics-heart, salivary)
  108. Pyridostigmine Uses
  109. Carbaryl MOA
    • sevin
    • irreversible organophosphate inhibitor of Ach (carbamate Achase inhibitor)
  110. Dimpylate MOA
    • diazinon
    • organophosphate Achase inhibitors
    • Active site of Achase is phosphorylated and rate of hydrolysis of enzyme is not really slow
  111. Parathion MOA
    organophosphate Achase inhibitor (phosphorylates AS to make enzyme slow)
  112. Parathion pharm effects
    converted to active metabolite paraoxon by CYP450
  113. Malathion MOA
    • organophosphate Achase inhibitor
    • As of Achase is phosphorylated and rate of hydrolysis of enzyme is now really slow
  114. Malathion uses
    • head lice
    • anti parasite 
  115. Malathion AE
    • Serious: burns
    • Common: skin irritations
  116. Pralaxidome MOA
    • protopam
    • accelerates hydrolysis of phosphate enzyme at NMJ (does not enter CNS)
  117. Pralidoxime uses
    antidote to insectide poisoning
  118. Atropine MOA
    muscarinic antagonist; tertiary
  119. Scopolamine MOA
    muscarinic receptor antagonist
  120. Scopolamine pharm effects
    • reverses block from D-tubocurarine
    • tranquilizer
  121. Scopolamine uses
    surgery, motion sickness, parkinsonism, spastic muscle states, irritable bowel syndrome, diverticulitis

    rx anteiror uveitis, keratitis, choroiditis (relaxes sphincter and ciliary mm to decrease pain)
  122. Cyclopentolate MOA
    muscarinic receptor antagonist; tertiary
  123. Cyclopentolate uses
    DOC for mydriasis in eye exam bc short duration
  124. Atropine uses
    rx anteiror uveitis, keratitis, choroiditis (relaxes sphincter and ciliary mm to decrease pain)
  125. Tropicamide MOA
    muscarinic receptor antagonist; tertiary

    inhibits response of sphincter and ciliary eye mm
  126. Tropicamide uses
    used in fundoscopic exam for mydriasis because shortest duration
  127. Benztropine MOA
    muscarinic receptor antagonist; tertiary
  128. Trihexyphenidyl MOA
    muscarinic receptor antagonist; tertiary
  129. Trihexyphenidyl
    treats mm stiffness as in Parkinson's
  130. Dicyclomine MOA
    • muscarinic receptor antagonist; tertiary
    • bentyl
  131. Dicyclomine Uses
    • relieves GI muscle spasms
    • rx IBS
  132. Hyoscyamine MOA
    • muscarininc receptor antagonist; tertiary
    • levsin
  133. Hyoscyamine Uses
    • relief from muscle spasms
    • reduces the fluid secretions of many organs and glands
    • including peptic ulcers, IBS
    • control mm spasms in the bladder, kidneys, GI, and to reduce stomach acid.
    • reduce tremors and rigid mm in Parkinson's
    • drying agent to control excessive salivation, runny nose, or excessive sweating
  134. Oxybutynin MOA
    • muscarinic receptor antagonist; tertiary
    • Ditropan XL
  135. Oxybutynin pharm effect
    blocks muscarinic receptors and gives antispasmodic effect on detrusor mm so that spontaneous contractions in the bladder are decreased and allows increased bladder storage and decreased frequency
  136. Oxybutynin Uses
    overactive bladder
  137. Tolterodine MOA
    • muscarininc receptor antagonist; tertiary
    • detrol
  138. Tolterodine AE
    somnolence, dry mouth, blurred vision, constipation
  139. Tolterodine usese
    overactive bladder
  140. Solifenacin MOA
    muscarinic receptor antagonist; tertiary
  141. Solifenacin uses
    overactive bladder
  142. Darifenacin MOA
    • selective muscarinic receptor antagonists; tertiary
    • enablex
  143. Darifenacin AE
    less dry mouth, nothing else really
  144. Diphenydramine MOA
    muscarinic receptor antagonists; tertiary
  145. Diphenydramine Uses
    aka benedryl
  146. N-methylatropine
    muscarinic receptor antagonist; quaternary
  147. Methscopolamine MOA
    muscarinic receptor antagonist; quaternary
  148. Methscopolamine AE
    impair your vision, thinking, or reactions
  149. methscopolamine uses
    reduce stomach acid secretions and rx peptic ulcers
  150. Tiotropium MOA
    muscarinic receptor antagonist; quaternary
  151. Tiotropium uses
    prevent bronchospasm in people with bronchitis, emphysema, or COPD
  152. Tiotropium pharm effects
  153. Ipratropium MOA
    muscarinic receptor antagonist; quaternary
  154. Ipratropium uses
    prevent bronchospasm in people with bronchitis, emphysema, or COPD
  155. Ipratropium pharm effects
  156. Glycopyrrolate MOA
    muscarinic receptor antagonist; quaternary
  157. Glycopyrrolate uses
    peptic ulcers and reduce drooling in kids
  158. Nicotine MOA
    • nicotinic receptor agonists; direct stimulation of peripheral N1/N2 cholinergics
    • In the CNS: stimulates N1 cholinergics to release NE and DA and increase/decrease Ach release
  159. Nicotine pharm effects
    acute CNS and cardio stuff (see notes)
  160. Trimethaphan MOA
    N1 receptor antagonist/ ganglionic blocking
  161. Epinepherine
    adrenergic agonist
  162. Dopamine
    adrenergic agonist
  163. dobutamine
    • adrenergic agonist; stimulates B1>B2
    • racemic mixture of entantiomers
  164. dobutamine uses
    short term rx for cardic decompensation
  165. isoproterenol MOA
    • adrenergic agonist
    • B1=B2
  166. Dobutamine pharm effects
    • Positive ionotropic: B1 receptor stimulation will increase SV
    • Arteriolar VD: B2 receptor stimulation lowers TPR so that DBP falls
    • Venodilation: B2 receptor stimulation will decrease VR and decrease cardiac filling P in pts w/ MI
  167. Isoproterenol pharm effects
    • + ionotropic and chronotropic effects in cardiac arrest
    • increase in AV conduction in AV block
  168. Salmeterol MOA
    • adrenergic agonist
    • serevent
    • B2>>B1
  169. Salmeterol Pharm effects
    relieves bronchoconstriction of asthma, COPD, bronchitis
  170. Salmeterol uses
    asthma, COPD, bronchitis
  171. Terbutaline MOA
    • adrenergic agonist
    • bricanyl, brethine
    • B2>>B1
  172. Terbutaline uses
    bronchospasms, asthma, bronchitis
  173. terbutaline pharm effects
    bronchodilator: relaxes mm in airway
  174. Albuterol MOA
    • adrenergic agonist
    • Ventolin, provetil
    • B2>>B1
  175. Albuterol uses
  176. Albuterol pharm effects
    bronchodilator to relax mm in airway to lungs
  177. Ritodrine MOA
    • adrenergic agonist
    • Yutopar
    • B2>>>>B1
  178. Ritodrine uses
    • delays birth
    • used to achieve external version of fetus from breach to vertex before birth
  179. Ritodrine pharm effects
    relaxes uterine sm mm
  180. Phenylephrine MOA
    • adrenergic agonist
    • A1 only 
    • neo-synephrine
  181. Phenylephrine pharm effects
    • systemic VC
    • constricts blood vessels in nasal mucosa (relieves congestion)
    • contracts radial mm (mydriasis)
  182. Ritodrine uses
    • fundoscopic exams (mydriasis via contracting radial mm)
    • relieves nasal congestion (constricts blood in nasal mucosa)
  183. Oxymetazoline MOA
    • adrenergic agonist
    • Afrin
    • A only
  184. Oxymetazoline uses
    nasal decongestant (better than phenylephrine)
  185. Tyramine MOA
    • adrenergic agonist
    • indirectly acting
  186. Tyramine pharm effects
    releases endogenous NE that has been stored until now; increases BP since releasing NE from sympathetic nerves that innervated blood vessels
  187. Tyramine uses
    in fermented food; must be taken IV because will be destroyed in gut if taken p.o.; cannot cross BBB so effects are confined to periphery
  188. Amphetamine MOA
    • adrenergic agonist
    • lipid soluble so can enter CNS and release NE from central AND peripheral  adrenergic neurons; blocks neuronal uptake of NE and will cause release of DA in NA
  189. Amphetamine pharm effects
    lipid soluble so can enter CNS and release NE from central AND peripheral  adrenergic neurons; blocks neuronal uptake of NE and will cause release of DA in NA
  190. Ephedrine MOA
    • adrenergic agonist; mixed
    • lipid soluble-->enters CNS to act at B1 and B2 directly
  191. Ephedrine pharm effects
    • Acts directly at both B1 and B2 via NE
    • Direct B: bronchodilation in asthma and increases AV conduction
    • Indirect A: mydriasis, increases BP, nasal decongestion
  192. Ephedrine uses
    asthma, mydriasis, nasal decongestant, reverses hypotension in anesthesia
  193. Pseudoephedrine MOA
    • adrenergic agonist
    • mixed, lipid soluble; goes into CNS
    • sudafed
  194. Pseudoephedrine uses
    nasal and sinus decongestant
  195. Pseudoephedrine AE
  196. Pseudoephedrine pharm effects
    since it is a stereoisomer of ephedrine; there is less CNS excitation and less BP/HR increases
  197. Phenoxybenzamine MOA
    • alpha adenoceptor antagonist
    • dibenzyline
    • non competitive receptor block results from covalent binding of receptor
    • A1>>A2
  198. Phenoxybenzamine uses
    reduce BP and sweating (pheochromocytoma ppl sweat a lot)
  199. Phentolamine MOA
    • A adrenoceptor antagonist
    • regitine
    • A1 = A2
  200. Phentolamine uses
    dental anesthesia reversal
  201. Prazosin, terazosin, doxazosin MOA
    • A adrenoceptor antagonist
    • minipress, hytrin, cardura respectively
  202. Tamsulosin MOA
    • A adrenoceptor antagonist
    • flomax
    • A1 only
  203. tamsulosin pharm effects
    Tamsulosin relaxes the muscles in the prostate and bladder neck, making it easier to urinate.
  204. Tamsulosin uses
    improve urination in benign prostatic hyperplasia
  205. Labetalol MOA
    • A adrenoceptor antagonist
    • trandate, normodyne
    • Blocks B1 and A1
  206. Labetalol uses
    hypertension treatment
  207. Yohimbine MOA
    • A adrenoceptor antagonist
    • A1<<<A2
    • yohimex, yocon
  208. Yohimbine pharm effects
    • CNS
    • Central A2 block in baroreflex arc will increase preganglionic sympathetic nerve activity to cause tachycardia, tremor, increase in BP
  209. Yohimbine AE
    restlessness, irritability, anxiety, no boners
  210. Ergotamine, dihydroergotamine MOA
  211. A adrenoceptor antagonist (partial agonist)
  212. Ergotamine and Dihydroergotamine pharm effects
    • constrict cerebral blood because partial A agonist
    • stimulates alpha adrenergic receptors, producing peripheral vasoconstriction and decreased blood flow; exhibits serotonin antagonistic properties
  213. Ergotamine and dihydroergotamine uses
    treat migraine like headaches (remember it constricts blood flow in brain!)
  214. Phentolamine MOA
    A adrenoceptor antagonist
  215. Phentolamine pharm effects
    reverses ischemia and tissue necrosis via extravation of DA from veins
  216. Phentolamine uses
    treats impotence
  217. Alprostadil MOA
    relaxes arterial smooth muscle, producing vasodilation; inhibits platelet aggregation (prostaglandin E1)
  218. Alprostadil uses
    treats impotence/ED (can be a topical use)
  219. Betaxolol
    • B adrenoceptor antagonist
    • Kerlone
    • cardio selective
  220. Betaxolol uses
    treats hypertension
  221. Atenolol MOA
    • B adrenoceptor antagonist
    • cardio selective
  222. Atenolol uses
    treat hypertension, treat/prevent heart attacks, treat angina
  223. Metoprolol MOA
    • B adrenoceptor antagonist 
    • lopressor, toprol
    • cardio selective
  224. Metoprolol uses
    angina, hypertension, heart attack
  225. Esmolol MOA
    • B adrenoceptor antagonist
    • breviblock
    • cardio selective
  226. Esmolol uses
    rapid control of ventricular rate
  227. Propranolol MOA
    • B adrenoceptor antagonist
    • not selective
    • Inderal
  228. Propranolol uses
    tremors, angina, hypertension,  heart rhythm disorders, treat or prevent heart attack, and to reduce the severity and frequency of migraine headaches
  229. Timolol MOA
    • B adrenergic antagonist
    • biocadren
    • non selective
  230. Timolol uses
  231. Labetalol MOA
    • B adrenoceptor antagonist
    • trandate
    • non selective
  232. Labetalol uses
  233. Alpha methyldopa MOA
    • sympathoyltic
    • Aldomet
    • Transported into central/peripheral noradrenergic via aromatic AA pump and is converted to alpha-methylNE; this will NOT be metab by MAO and will be stored in cytoplasm AND vesicles as a result
    • Also stored as nt in noradrenergic neurons and will be released by AP
    • See notes
  234. Alpha methyldopa pharm effects
    • VC (just as well as NE)
    • Blood: net balanced vasodilation
    • Heart: HR decreases, myocardial oxygen demand decreases
    • Pituitary: PL secretion increases
  235. Alpha methyldopa uses
    hypertension in kids and pregnant women
  236. Reserpine MOA
    • sympatholytic; alkaloid from plants
    • Seprasil
    • Destroys IC vesicles for nt in peripheral/central monoaminergics which results in depleted net stores
  237. Reserpine pharm effects
    • Small doses: deplete peripheral sympathetic monoaminergic stores only
    • Blood: decreases amount of NE released, net balanced VD
    • Heart: HR and CO little change
    • GI: increased motility and tone from unopposed PS
    • Pituitary: PL secretion increases because DA depleted
  238. reserpine uses
    hypertension, psychotic states?
  239. Guanethidine MOA
    • sympatholytic; adrenergic neuronal blocker
    • poor lipid solubility
    • directly inhibits NE release from peripheral sympathetic neurons
    • Ismelin
  240. Guanethidine uses
  241. Guanethedine pharm effects
    • Blood: net balanced VD
    • Heart: HR and CO unchanged
  242. Guanethidine AE
    orthostatic hypotension, sex dysfx, supersensitive to direct sympathomimetic amines (adrenoceptors are upregulated), unopposed PS activity
  243. Cocaine MOA
    • alkaloid
    • neuronal NE uptake 1 transporter
    • Local anesthesia via blocking Na channels in pain fibers-->non comp block monoamine uptake 1 in c/p neurons-->amp postj/s NE, DA, Epi, Serotonin effects
    • Increases peripheral sympathetic outflow
    • Increased DA stimulation in NA (euphoria)
  244. Cocaine Pharm effects
    • (See notes)
    • local anesthesia, CNS, dose related, indirect VC, local hemostasis
  245. cocaine AE
    see notes
  246. Cocaine uses
    anesthesia in eye and nose surgery
  247. Reserpine AE
    • (see notes)
    • Teratogenic
    • CNS 
    • orthostatic hypertension
    • sex dysfx
    • hyperprolactinemia
    • supersensitive to direct sympathomimetic amines
    • unopposed PS activity
  248. Alpha methyldopa AE
    sedation, dry mouth, congestion, edema, orthostatic intolerance, flu sx, + Coombs, HS rxn for hepatitis, hyperprolactinemia