Neuro Exam #3

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pharmschool
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145341
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Neuro Exam #3
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2012-04-04 14:18:52
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Neuro
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Dr. Schiff
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  1. At least 5 genera of mushrooms of fungi – Psilocybe mexicana (Fam. Agaricaceae)
    Psilocybin Source
  2. Large amounts
    4-Hydroxydimethyltryptamine phosphate ester
    Ingestion results in hydrolysis of thephosphate ester -> psilocin (4-Hydroxydimethyltryptamine)
    Psilocybin Chemistry
  3. Actions of this compound are very similar to LSD:
    –Mydriasis
    –Blurred vision
    –Limpness
    –Dizziness
    –Difficulty in concentration
    –Hilarity
    –Auditory hallucinations
    Actions of Psilocybin
  4. "good" visual hallucinations, followed by:
    –Lassitude
    –Mental depression
    –Physical depression
    –Alteration of time and space perception
    Actions of Psilocybin
  5. The “dream-like state” becomes “reality”, resulting in great indifference to the surrounding

    Pleasant “reawakening” to reality with a lack of tiredness or “hangover”
    Actions of Psilocybin
  6. Occurs in the leaves of a plant of the Amazon – Prestonia amazonica (Benth.) Macbride (Fam. Apocynaceae)

    Actions are very similar to psilocybin
    N,N-dimethyltryptamine Source
  7. Lophophora williamsii (Lemaire) Coulter (Fam. Cactaceae)
    Small cactus
    Habitat: Northern Mexico and Southwestern United States
    Mescaline Source
  8. Mydriasis
    Tachycardia
    Hypertension
    Depressed deep tendon reflexes
    Hallucinations of “feeling”
    Visual hallucinations: Bright, colored lights, Geometric designs, Animals, People
    Auditory hallucinations
    Actions of Mescaline
  9. The period of intoxication may be divided into two periods:
    –One of extrasensitivity and contentment
    –One of artificial calm and muscular sluggishness during which time the individual pays less attention to the immediate environment and increases introspective mediation
    Actions of Mescaline
  10. There have been no known fatalities, even from massive overdosage
    Mescaline
  11. the historic prototype of all of the synthetic phenethylamines
    Methylenedioxyamphetamine (MDA)
  12. commonly referred to as“raves” or “rave drugs” or “club drugs”
    Methylenedioxyamphetamine (MDA) and Methylenedioxymethamphetamine (MMDA)
  13. Symptoms (within hours):
    – Euphoria
    – Agitation
    – Confusion
    – Bruxism (teeth grinding)

    Higher dosage:
    – Tachycardia and dysrhythmias
    – Vasoconstriction
    – Hypertensive crises
    – stroke/death
    Amphetamines
  14. Popular hallucinogen producingauditory and visual effects after oralingestion or inhalation
    Produces an overwhelming desire tobe/talk with others – “Love Drug”/”HugDrug” – strong empathy
    Mild visual hallucinations with actionsperceived within 30 min; peaking at 90min; lasting 8-12h
    3,4-Methylenedioxyamphetamine (MDA)
  15. Adrenergic/CNS effects:
    – Tachycardia
    – Tachypnea
    – Hypertension
    – Xerostomia
    – Mydriasis
    – Hyperthermia
    – Seizures
    3,4-Methylenedioxyamphetamine (MDA)
  16. Acute toxicity:
    –Hyperthermia with dehydration (may be fatal)
    –Serotonin syndrome
    3,4-Methylenedioxymethamphetamine (MDMA, XTC)
  17. Has been unequivocally demonstrated to destroy serotonin-producing neurons in animals

    Strong evidence in humans of permanent brain serotonin neuron neurotoxicity with resultant:
    –Performance deficits
    –Memory problems
    –Semantic recognition/verbal reasoning
    3,4-Methylenedioxymethamphetamine (MDMA, XTC)
  18. This alkaloid, which comes from Catha edulis (Fam. Celastraceae), possesses pharmacologicalactivities similar to those of (+)-amphetamine
    Cathinone
  19. 4-Methylcathinone

    AEs: Tachycardia, elevated blood pressure,seizures, high temperatures may occur

    “meow meow” or “MCAT”
    Mephedrone
  20. – A ring-group substituted compound(methylenedioxy group)
    – Similar to cocaine, amphetamine andMDMA in humans
    – Ring group substituted cathinones: Feelings of empathy, Stimulation + Euphoria, & Alertness + Awareness of Senses
    Methylenedioxypyrovalerone (MDPV) Pharmacodynamics
  21. Adverse Effects (≤ 5 mg):
    – Vasoconstriction
    – Tachycardia
    – Hypertension
    – Sweating
    – These effects continue a total of 6-8 hours
    – High doses: Intense, prolonged panic attacks; Bouts of psychosis with sleep deprivation
    Methylenedioxypyrovalerone (MDPV)
  22. naturally occurring kernel of the fruit of the evergreen tree Myristica fragrans Houtt. (Fam. Myristicaceae)
    Myristicin (Nutmeg)
  23. Effects include:
    – Distortions of time and space
    – Sleepless stupor
    – Hallucinations (uncommon)
    – Numerous others, appearing mainly to resemble adrenergic stimulation
    Myristicin (Nutmeg)
  24. Originally designed as an anesthetic(1960’s), but later discarded because ofpronounced postoperative delirium andhallucinations
  25. Minimal dosage (50 mcg/kg) produces:
    – Emotional withdrawal
    – Concrete thinking
    – Bizarre responses to projective testing
    – Catatonic posturing, resemblingschizophrenia
    – Hostile behavior (as dose increases) [Reaction to hallucinations]
    – Longlasting psychosis
    Phencyclidine (PCP)
  26. Increased dosage produces:
    – Stupor
    – Coma
    – Rhabdomyolysis
    – Hypertension
    – Hyperthermia

    Unlike LSD and other psychedelics in that it blocks NMDA (N-methyl-D-aspartic acid)-type glutamate receptors
    Phencyclidine (PCP)
  27. -H for -OH at position 3
    Decreases Activity
  28. -OCH3 for -OH at position 3
    Decreases Activity
  29. CH3CO-ester at position 3
    Decreases Activity
  30. Keto substitution for -OH at position 6
    Decreases Activity
  31. Keto sub for -OH at C-6 +7,8-dihydro substitution
    Increases Activity
  32. -H sub for -OH at C-6
    Increases Activity
  33. CH3CO-ester sub for -OH at C-6
    Increases Activity
  34. 7,8-dihydro substitution
    Increases activity
  35. 14B-OH substitution
    Increases activity
  36. NCH2CH2Phenyl for NCH3 substitution
    Increases activity
  37. NCH2CH=CH2 for NCH3
    Becomes a u antagonist
  38. 6-OH to 6-keto + 7,8-dihydro
    Hydromorphone
  39. 6-OH to 6-keto + 7,8-dihydro + 14B-OH
    Oxymorphone
  40. 3-OCH3 for -OH + 6-OH to 6-keto + 7,8-dihydro
    Hydrocodone
  41. 3-OCH3 for -OH + 6-OH to 6-keto + 7,8-dihydro + 14B-OH
    Oxycodone
  42. CH3CO-ester at 3,6
    Heroin (Diacetylmorphine)
  43. the air-dried milky exudate obtained by incision of the unripe capsules of Papaver somniferum L. or its var. album DeCandolle (Fam. Papaveraceae)
    Opium Source
  44. – Amphoteric morphinan alkaloid: Tertiary amine; Phenol
    – Commonly supplied as its sulfate salt
    Morphine
  45. – A morphinan alkaloid and tertiary amine
    – Most commonly furnished commercially as its water soluble sulfate salt, although the phosphate salt is also available
    -usually prepared via methylation of morphine with trimethylphenylammonium salt in xylene or xylene-methanol mixtures
    Codeine
  46. – Relief of mild to moderate pain
    – Relief of coughing induced by chemical ormechanical irritation of the respiratory system
    – Less potent than morphine
    – 2/3 as effective orally as morphine
    Codeine
  47. – In the relief of moderate to severe acute and chronic pain
    – In the preoperative sedation of a patient to allay apprehension
    – In the facilitation of the induction of anesthesia and to reduce anesthetic dosage
    – Less potent orally (15-33%) because of first-pass metabolism
    Morphine
  48. – Catalytic reduction of C-7/C-8 double bond in morphine to dihydromorphine
    – Oxidation of C-6 secondary alcohol to aketone
    – HCl salt is commercially available
    Hydromorphone Chemistry
  49. Relief of moderate to severe pain
    Hydromorphone
  50. – Demethylation of oxycodone
    – HCl salt is commercially available
    Oxymorphone Chemistry
  51. – Relief of moderate to severe pain
    – Obstetrical anesthesia
    – Support of anesthesia
    – Preoperative medication to allay apprehension
    – Relief of anxiety in patients with dyspnea-associated with acute left ventricular failure and pulmonary edema
    Oxymorphone
  52. – Hydrogenation of codeinone
    – Commercial availability as Bitartrate salt; Only marketed in combinations with other drugs (caffeine, others)
    Hydrocodone
  53. –Relief of moderate to severe pain
    - Frequently combined with acetaminophen or ASA, w/wo caffeine
    –Antitussive ---- Sometimes combined with anticholinergics, decongestants, and anthistamines
    Hydrocodone
  54. –Catalytic reduction of hydroxycodeinone
    –HCl and terephthalate salts are commercially available
    Oxycodone
  55. – In the relief of moderate to severe pain
    – Frequently combined with ASA oracetaminophen
    Oxycodone
  56. – Prepared via the acetylation of morphine
    Heroin (Diacetylmorphine)

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