MED Chem Quiz 4

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ljohnstad
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201344
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MED Chem Quiz 4
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2013-02-18 16:58:40
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MED CHEM III
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Med Chem III Quiz 4
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  1. Dopamine
    • To much-Psychoses, Schizophrenia
    • Chloropromazine-Thorazine
    • Too Little- Parkinsons
    • Levodopa
  2. GABA
    • too little- Seizures anxiety
    • Diaxepam-Valium
    • Clonazepam-Klonopin
  3. Norepinephrine
    • Too-little- Depression, ADHA, Harcolepsy
    • TCS- Doxepin-Sinequan, Reuptake inhibition
  4. Seortonin-5HT
    • Too little- Depression
    • SSRIS- Fluoxetine-Prozac, Sertraline-Zoloft
    • Too Much-Emesis
    • Ondansetron-Zofran
  5. CNS= Central Vervouse System
    • Brain Spinal chord
    • Parallels Autonomic Nervouse System
    • Not jsut Norepinenphrine & Acetylcholine
  6. PNS=Peripheral Nervouse sysstme
    • Autonomic- involuntary (cardiac & smooth muscle)
    • Sympathetic-Fight or flight
    • Parasympathetic
    • Somatic-Voluntary
    • Pain & touch
  7. Monoamines(Catecholamines)
    • Norepinephrine-sympathetic transmitter
    • Dopamine
    • 5-hydroxytryptamine (5-HT or Serotonin)
    • Adrenergice: Referes to neurons that use catecholamine as neurotransmitters at teh synaps when a nerve mplus passes sympathetic fibers
  8. Acetylcholine-para
    parasympathetic transmitter
  9. Gamma-amino butyric acid (GABA)
    inhibitory
  10. Excitatory amino acids (EAA)
    Glutamate
  11. Opioid activity
    caused by actually by peptides
  12. Norepinephrine- Sympathetic transmitter
    • 1. L-Tyrosine is converted to L-dopa which is then hydroxylated to Dopamine ( Presynaptic)
    • 2. B-hydroxylase converts dopamine to norepinephrine (Presynaptic)
    • 3)Norepi relase- Ca2+
    • 4. Receptor binding
    • 5-7
    • 8. Catechol Omethyl transferase degrades catecholamines COMT (Post synaptic)
    • 9. Reuptake into presynaptic neuron
    • 10. Repackagin
    • 11. Degraded by mitnochondrial MAO
    • 12. Path for indirect sympathomimetics
  13. Dopamin
    Dopaminergic Receptors
  14. Seortonin-5-HT
    • Tryptophan is hydroxylated and decarbosylated to form 5-HT
    • Stored in vesicles, released, taken up by pre-synaptic neurons, recycled or metaolized
    • 5-HT is realsed by inhibitiory neurons
  15. Acetylcholine
    • 1. Choline acetyltransferase catalyzes formation of acetylcholine from choline and acetyl CoA
    • 2. Storage in vesicles
    • 3. CA2+ stimulated release
    • 4.Receptor binding
  16. Acetylcholine
    MUSCARINIC-CNS

    • 1. Choline acetyltransferase catalyzes formation of acetylcholine from choline and acetyl CoA
    • 2. Storage in vesicles
    • 3. Ca2+ sitmulated release
    • 4. REceptor binding
    • Nicotinic
    • Muscarinic-CNS
    • REuptake and hydrolysis by acetylcholine esterase
    • 10. Breakdown products recycled
  17. Acetylcholine
    • Cholinergic antagonists used primary to treat parkinsons
    • imbalnace produced by degradatio nof dopaminergic nerves
  18. GABA - y-Amino butyric acid
    • Inhibitory amino acid
    • synthesized from glutamate
    • Binds to GABA-A or Gaba-B receptors
    • Clorid ion channel
    • Stimulate influx of clorid
    • Hyperpolarizes the neuron
    • Benzodiazepine-Enhance GABA-A receptors ONLY
  19. GABA enhancers (Benzodiazepines, Barbiturates) used:
    • Anxiety
    • Seizures
    • Act as sedatives or muscle relaxants
  20. HIstamine
    • Role as CNS neurotransmitter is being extensivel explored
    • Receptor subtyprs known: H1-4
  21. Rituzole-Rilutek
    Target decrease in glutamate toxicty
  22. Excitatory Amino Acis-EAA
    • Glutamate and others
    • Stimulation of EAA receptors increased cation conductance
    • Important in learning, memory
  23. Glutamate-induced toxicity
    • Alzheimers
    • Huntingtons
    • Stroke
    • Epilepsy
    • Amyotrophic Lateral Schlerosis (ALS)
  24. Opiates & Opiods
    Opiate receptors located along the periaquiductal gray matter

    Morphine and related compounds act on opiate receptors to relieve pain

    In tiems of stress & pain endogenous peptides act on opiate receptors
  25. Opiate receptor Agonists
    • PEPTIDES
    • Endorphins
    • Enkephalins
    • Dynaorphins
  26. Schedule I
    • High abuse risk, NO safe accepted medical use in the United STates
    • Heroin, LSD, PCP, crack cocaine
  27. Schedule II
    Drugs with a high abuse risk, but also have safe/accepted medical uses in the United States.  Can Cause sever psychological or physical dependence

    Morphine, cocaine, oxycodone(Percodan) methylphenidate (Ritalin)  dextroamphetamien (Dexedrine), THC for N/V
  28. Schedule III-IV
    Drugs categorized as prescription drugs.  Potential abuse goes down with each level
  29. Paracellular squaous pathway
    (extremly rare)
    Water-soluble agents
  30. Transcellular lipophillic pathway
    Lipid-soluble agents
  31. Transport proteins
    • Glucose
    • Levadopa
    • amino acids
    • nucleosides
  32. Receptor-mediated trancytosis
    • Insulin,
    • transferrin
  33. Adsorptive transcytosis
    Albumin, other plasma proteins
  34. CNS active agents
    stimulants and simililar agents
  35. Caffeine: Nodoz tablet
    Cafcit: injectible
    Analeptic agent
    A methylxathine

    MOA: non-selectrive antagonist of adenosine receptors increased cAMP via phosphodiaseterase inhibition

    REcuces the rate of bronchopulmonary dysplasi in infants with very low birth weight

    Treatmetn excited or comatose alcoholic patients, postprandial hypotension
  36. Analeptics
    a drug used to stimulate the CNS that can induce convulsions in a dose-dependent manner
  37. Doxapram HCL-Dopram
    Analeptic
    PNS STIMULANT
    IND: Post-anesthesis drug induced respiratory depression apnea due to drugs othe rthan muscle relaxamant, stimulation of drug induced CNS depression, COPD associated with acute hypercapnia, apnea of prematurity

    MOA: Stimulates Peripheral carotid chemorecpetors- increase tital voludm, and respiration rate,
  38. Modafinil-Provigal
    Racimic
    Analeptics
    • Ind: Narcolepsy
    • MOA: Unknown,   wakefulness-promoting effects similar to sympathomimetic agents,
    • RACEMIC DRUG HAS different half lives- R-enantiomer has 3X the lifetime of the S-enantiomenr, 60% protein bound, deamidation & hepatic metabolism and glucornidation followed by predominately urinary excretion, p-glycoprotein substrate, coderate CYP induction, CYP2C19 inhibitor
  39. Armodafinil-Nuvigil
    R-enantiomenr
    Analeptic
    • IND: Narcolepsy
    • MOA: UNKNOWN, Promots wakefulness-promoting effects

    RACEMIC DRUG HAS different half lives- R-enantiomer has 3X the lifetime of the S-enantiomenr, 60% protein bound, deamidation & hepatic metabolism and glucornidation followed by predominately urinary excretion, p-glycoprotein substrate, coderate CYP induction, CYP2C19 inhibitor
  40. Amphetamines
    A CNS Stimulant
  41. Racemic Amphetamine Sulfate
    Adderall
    Adderall XR
    Dextroamphetamine Sulfate-Dexedrine
    1-phenyl-2 aminopropane-simplest

    Various salts- Adderall
  42. Methamphetamine HCL- Desoxyn
    • Racemic
    • Amphetamine
    • Also has been used as an anorexiant
  43. Lisdexamfetamine dimesylate- Vyvanse
    Amphetamine
    • A pro drug:  Provides for once a day dosing with less abuse potential:  Plasma protease will NOT hydrolyze the amide bond to release the drug
    • Only GI protease is capable of this transformation
    • LESS IV drug USE

  44. Amphetamines-A CNS stimulatn
    • MOA: enhance release and hinder dopamine reuptake
    • indirect agonist

    IND: ADHD, Narcolepsy
  45. Amphetamines- A CNS stimulant
    • No longer indicated for obestity, or antidepressant
    • ADR: Addition tolerance, toxic psychosis, hypertention, angina hyperthyroidism
    • CNS effects : increase arousal, wakefulness, increased confidence, ability to concentrate, exhilaration, anorexia, insomnia
    • CV: contraindicated in abnormality

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