CNS Stimulants

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regill
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CNS Stimulants
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2015-02-17 11:18:58
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  1. Thereare four categories of drugs that are considered to have stimulant properties:
    • Analeptics
    • Methylxanthines
    • Central Sympathomimetic Agents (Psychomotor Stimulants)
    • Antidepressants
  2. a group of potent and relatively nonselective CNS stimulants.
    Analeptics
  3. obsolete, but still valuable in determine hownew drugs act.
    • Picrotoxinin
    • Pentylenetetrazole (BN)
  4. More selective and have use in narcolepsy and respiratory stimulant
    • Modafinil (BN)
    • Doxapram (BN)
  5. MOA: Intefere with the inhibitory effects of y-aminobutyric acid (GABA) at the level of the GABAa receptor's chloride channel.
    Drug is obsolete medically
    Picrotoxinin
  6. Used  in conjunction with the electroencephalograph to help locate epileptic foci. Used as a laboratory tool in determining potencies of potential anticonvulsant drugs in experimental animals
    Pentylenetetrazole (BN)
  7. Used in overall wakefulness-promoting properties similar to those of central sympathomimetics.Atypical a-norepinephrine (NE) receptor stimulant and is used to treat daytime sleepiness in narcolepsy patients.
    SE: nervousness, anxiety, andinsomnia.
    Route: Oral
    Modafinil (BN)
  8. Has an obscure molecular mechanismof action.
    MOA: Stimulates respiration by action on peripheral carotid chemoreceptors.
    Use: Respiratory stimulant post-anesthetically, after CNSdepressant drug overdose, in chronic obstructive pulmonary disease, and in the apneas.
    Route: IV; not given to neonates because of benzyl alcohol.
    Doxapram HCl (BN)
  9. Naturally occurring Methylxanthines are:
    • Caffeine
    • Theobromine
    • Theophylline
  10. is a widely used CNS stimulantit promotes an ability to concentrate on the task at hand, and lessens fatigue.may be used in treating poisoning from CNS-depressant drugs, although it is not a preferred drug.
    Caffeine (give the sources)
  11. A dosage of _ to _ mg of caffeine acts as a cortical stimulant and facilitates clear thinking and wakefulness.
    85 to 250
  12. Have valuable bronchodilating properties in asthma.
    Theophylline (give the source)
  13. Classified as a xanthine alkaloid
    Theobromine
  14. Theobromine is formerly known as:
    Xantheose
  15. Chemical formula of theobromine
    C7H8N4O2
  16. Theobromine is derived from :
    Theobroma, the name of the genus of the cacao tree.
  17. Psychomotor Stimulant or :
    Central Sympathomimetic agents
  18. -exert an anorexiant effect.
    -more resistant to metabolism, more non-polar.
    -able to cross the blood-brain barrier.
    -increase the ratio of central peripheral activity.
    CSA
  19. Chemical Name and Brand name of Amphetamine Sulfate
    • Amphetamine(±)-1-phenyl-2-aminopropane
    • (Benzedrine)
  20. The dextrorotatory isomer has the (S) configuration and fewer cardiovascular effects than the levorotatory (R)-isomer.MOA: Release of NE from the mobile pool of the nerve terminal.
    • Dextroamphetamine Sulfate and
    • Dextroamphetamine Phosphate (BN)

    NOTE:  The phosphate (more water-soluble salt); preferred if parenteral administration is required.
  21. N-methyl analog of dextroamphetamine.More marked central and less peripheral action than dextroamphetamine.
    Very high abuse potential. Its salts are known as “speed.”
    • Methamphetamine Hydrochloride (BN) or
    • 1-phenyl-2-methylaminopropane hydrochloride
  22. Compound is used as an appetite suppressant and is a schedule IV agent.
    -less abuse potential than dextroamphetamine.
    • Phentermine Ion-Exchange Resin and
    • Phentermine Hydrochloride
    • NOTE: Resin preparation (Ionamin)- slow release product; Hydrochloride (Wilpower)
  23. Has anorexiant properties
    Benzephetamine Hydrochloride (BN)
  24. -Fewer sympathomimetic, cardiovascular and CNS-stimulatory effects than amphetamine.
    -an anorexiant agent.
    -can be used for treatment of obesity in patients with hypertension and cardiovascular disease.
    Diethylpropion Hydrochloride
  25. (unique in this group of drugs)-tends to produce sedation rather than excitation.
    Fenfluramine Hydrochloride (BN)
  26. Considered an effective anorexiant that is less abuse prone than amphetamine.
    Phendimetrazine Tartrate (BN)
  27. -an uptake inhibitor of NE and 5-HT-An antidepressant and an anorexiant drug.
    Sibutramin (BN)
  28. Brand name of Methylphenidate Hydrochloride, a CSA.
    Ritalin
  29. The tricyclic antidepressants are structurally related to each other and possess related biological properties that can be summarized as characteristics of the group as:
    • DIMETHYL Compounds(sedative,Higher 5-HT to norepinephrine reuptake  block ratios, anticholinergic properties)
    • MONOMETHYL COMPOUNDS (Selective Norepinephrine reuptake,stimulatory)
  30. are extremely lipophilic and very highly tissue bound outside the CNS.  Because they have anticholinergic and noradrenergic effects, both  central and peripheral side effects are often unpleasant and sometimes dangerous.
    Tricyclic antidepressants
  31. Lead compound of TCA.Selective transport inhibitor to treat depression. Treatment of night time bed wetting in children. May improve your mood, sleep, appetite, and energy level and may help restore your interest in daily living.
    Imipramine Hydrochloride (BN?)
  32. Selective norepinephrine reuptake inhibitor.
    Desipramine Hydrochloride (BN?(2))
  33. Used in OCD (obsessive compulsive disorders)
    Clomipramine Hydrochloride (BN?)
  34. One of the most anticholinergic and sedative of the tricyclic antidepressants.
    Treat mental/mood problems such as depression.
    Amitriptyline Hydrochloride (BN?)
  35. BN of Trimipramine Maleate (TCA drug)
    Surmontil
  36. Norepinephrine and 5-HT reuptake blocker withsignificant anticholinergic and sedative properties
    Doxepin Hydrochloride (BN(2))
  37. “tetracyclic” depressant
    -SNERI
    Maprotiline Hydrochloride (BN?)
  38. 8-hydroxy metabolite is active as antidepressant and D2 receptor blocker
    Amoxapine (BN)
  39. differ from the tricyclics, in that the tricyclic system has been taken  apart in the center.  This abolishes the center ring, and one ring  is moved slightly forward from the tricyclic “all-in-a-row” arrangement
    SSRIs
  40. this diminishes unpleasant CNS effects and in- creases cardiovascular safety.
    SSRIs
  41. Therapy for 2 weeks or more is required for the anti-depressant effect. S-isomer moreselective for SERT.
    Fluoxetine (BN?)
  42. Anti-depressant and anxiolytic.
    Paroxetine (BN?)
  43. The Cl substituents also predict tropism for a5-HT system.
    Sertraline (BN?)
  44. A racemic mixture and is very SERT selective.
    Citalopram (BN?)
  45. SSRIs : (4)
    • Fluoxetine (BN)
    • Paroxetine (BN)
    • Setraline (BN)
    • Citalopram (BN)
  46. SNERIs: (1)
    It is claimed to be superior to fluoxetine in severe depression
    Reboxetine (RR & SS)
  47. NEWER (NONTRICYCLIC) NONSELECTIVE 5-HT AND NOREPINEPHRINE REUPTAKE INHIBITORS : (1)is an effective antidepressant. ___ is a serotonin–norepinephrine reuptakeinhibitor (SNRI).
    Venlafaxine
  48. SELECTIVE SEROTONINERGIC REUPTAKE INHIBITORS AND 5-HT2A ANTAGONISTS: (2)The structures of these two compounds derivefrom those of the fluorobutyrophenone antipsychotics.
    • Nefazodone (Serzone),
    • Trazadone (Desyrel)
  49. not as an antidepressant. A 100-mg dose can be used as a sedative–hypnotic.
    Trazadone (BN)
  50. produces better sleep hygiene than does trazodone, which is a rapid eye movement (REM)-suppressing compound.
    Nefazodone (BN)
  51. 5-HT₁ₐ AGONISTS AND PARTIAL AGONISTS: (1)
    has anxiolytic and antidepressant activities and is a partial 5-HT₁ₐ agonist. Its anxiolytic activity is reportedly caused by its ability to diminish 5-HT release (via 5-HT₁ₐ agonism).

    Buspirone (BN)
  52. α2 ANTAGONISTS: (1)
    Its parent, mianserin, was long known to be an
    antidepressant. It is reported to be faster acting and more potent than certain SSRIs
    Mirtazapine (BN))
  53. MISCELLANEOUS ANTIDEPRESSANTS : (2)
    • Bupropion (Wellbutrin)
    • Duloxetine (Cymbalta)
  54. It is considered complex and reportedly involves a block of DA re- uptake via the dopamine transporter (DAT), but the overall
    antidepressant action is noradrenergic
    Bupropion (BN)
  55. In Bupropion, reduction of the keto group also occurs, yielding _____ and ____ . Both of these metabolites are also active.
    • threohydrobupropion and
    • erythrohydrobupropion
  56. It is a newer antidepressant. It is largely like venlafaxine, which is a selective norepinephrine reuptake inhibitor. It is a treatment for depression, anxiety, muscle and bone aches.
    Duloxetine (BN)
  57. MISCELLANEOUS CNS-ACTING DRUGS:
    1ᵝ -Arylamino Hallucinogens
  58. A property of the 1B-arylamino hallucinogens.
    alteration of the perception of stimuli.
  59. can produce anxiety, fear, panic, frank hallucinations, and additional symptoms that may be found in a psychosis.
    • Accordingly, they are classed as hallucinogens
    • and psychotomimetics.
  60. 1ᵝ -Arylamino Hallucinogens can be subgrouped into:
    • those that possess an indolethylamine moiety,
    • those that possess a phenylethyl- amine moiety, and
    • those with both
  61. INDOLETHYLAMINES: (2)

    • Dimethyltryptamine
    • Psilocybin and Psilocin
  62. It is a very weak hallucinogen, active only by inhalation or injection, with a short duration of action. It possesses pronounced sympathomimetic (NE) side effects.
    Dimethyltryptamine
  63. is the phosphoric acid ester of psilocin and
    appears to be converted to psilocin as the active species in vivo.
    Psilocybin (occurs in: ____)
  64. Psilocybin occurs in
    Psilocybe mexicana.
  65. 2-PHENYLETHYLAMINES
    Mescaline (3,4,5-trimethoxyphenethylamine)
  66. It is a much- studied hallucinogen with many complex effects on the CNS. It occurs in the peyote cactus. The oral dose required for its hallucinogenic effects is very high, as much as 500 mg of the sulfate salt.
    Mescaline
  67. Mescaline occurs in :
    Peyote Cactus
  68. AN AGENT POSSESSING BOTH AN INDOLETHYLAMINE AND A PHENYLETHYLAMINE MOIETY (2)
    • (+)-Lysergic Acid Diethylamide
    • (DOM),(MDA), (DMDA; ECSTASY)
  69. It has marked effects on serotoninergic and
    dopaminergic neurons. Both an indolethylamine group and a phenylethylamine group
    (+)-Lysergic Acid Diethylamide
  70. (DMDA; Ecstasy).
    2,5-dimethyl-dicyanoquinonediimine
  71. DISSOCIATIVE AGENTS (1)
    Phencyclidine

  72. It was introduced as a dissociative anesthetic
    for animals.In humans, PCP produces a sense of intoxication, hallucinogenic experiences not unlike those produced by the anticholinergic hallucinogens, and often, amnesia.
    Phencyclidine

  73. EUPHORIANT-STIMULANT
    Cocaine
  74. is a euphoriant–stimulant, psychotomimetic, and drug of abuse. At low doses, it produces feelings of well-being, decreased
    fatigue, and increased alertness
    Cocaine
  75. DEPRESSANT-INTOXICANT
    ∆1-Tetrahydrocannabinol or ∆⁹-THC
  76. Two receptors for THC have been discovered.
    • The relevant receptor for CNS actions is CB1.
    • CB2 occurs in immune tissues
  77. involved in maintaining food intake and in other
    behaviors.
    Endocannabinoids (regulated by leptin)
  78. Other natural cannabinoids : (2)
    • arachidonic acid 2-glycerol ester and
    • 2-arachidonyl glycerol ether

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