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76 Cards in this Set
- Front
- Back
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many anti-psychotics such as phenothiazines and TCAs have
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anticholinergic compoenents
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Ach in alzheimer's dx is important in
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learning and memory
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irreversible Ach inhibitors
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isofluorphate
organophosphate insecticide compounds |
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Ach reactivators
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atropine
2-PAM |
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reversib le ache-esterase inhibitors
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physostigmeine
tacrine donepezil (QD and has excellent bioavaility!) |
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NE exists at significant levels in
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the hypothalamus
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DA is highly concentrated in
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the caudate nucleus (extrapyradmial system)
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D1 receptors
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stimulate the synthesis of cAMP
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D2 receptors
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inhibits cAMP
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dopamine
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predominant neurotransmitter of the extrapyramidal system
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serotonin exists in high levels in
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hypothalamus, medulla, midbrain
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5HT1, 5HT2, 5HT4-7 are
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g-protein-coupled receptors
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5HT3 are
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ligand-gated ion channels
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melatonin
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principle indolamine in the pineal gland
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bufotenine
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alkaloid
found in schizophrenic patients derivative of serotonin |
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H1 agonist
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allergic response
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H2 agonist
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gastric secretion
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GABAa
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chloride channel
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GABAb
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GPCR
K+ channel |
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precursor of GHB
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succinic acid
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precursor of GABA
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L-glutamic acid
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glycine & GABA
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inhibitory nuerotransmitters
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strychnine
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convulsant
blocks postsynaptic glycine receptor |
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receptors activated by glutamic acid
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kainic acid
quisqualic acid N-methyl-D-aspartic acid (NMDA) |
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NDMA receptor is involved in
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epileptic discharge and hypoxic damage
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Kainic acid
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glutamic acid agonist
neuronal toxin |
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D-APV5
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selective NMDA agonist
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PCP
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angel dust
noncompetitive NMDA receptor antagonist |
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memantine
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Namenda
new MAO for tx of Alzeimers 1st open channel blocker of NMDA receptors works better w/aricept |
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Dx with over-activity of NMDA receptor
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neuropathic pain
stroke amyotrphic lateral scelrosis huntington's dx |
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Stimulants
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analeptics
methylxanthines B-phenethylamine analogs antidepressants psychedelics |
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analeptics
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picrotoxin
pentylenetetrazole nikethamide doxapram |
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methylxanthines
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caffeine
theophillin theobromine |
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B-phenethylamine analogs
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amphetamine-like drugs
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antidepressants
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TCAs
MOA inhibitors SSRI SNRI |
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psychedelics
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LSD
cocaine PCP |
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amphetamine-like drugs have effects
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similar to those of sympathetic nervous system
CNS stimulants anorexia addiction high abuse potential |
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b-phenethylamine functional groups:
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alpha-alkyl to retard MAO
N subsituents (not larger than methyl) increase acitivity halogenation of aromatic ring increases acitivity |
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produce methamphetamine
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1) hydrogenate pseudoephedrine
2) methylamine + P2P and reduction |
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mazinodol
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sanorex
amphetamine-like inhibits NE & DA uptake enol preferred |
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methlyphenidate
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amphetamine-like
blocks NE & DA uptake only 4% reaches BBB concerta is CR |
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atomoxetine
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Strattera
amphetamine-like 1st nonstimulant for ADHD slow reuptake of NE |
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Vyvanse
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lisdexamfetamine
amphetamine-like prodrug only QD prodrug stimulant to tx adults w/ADHD conjugates amphetamine w/lysine (not as toxic) |
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modafinil
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provigil
nonamphetamine drug to tx narcolepsy no dopamine activity (less side effects) |
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analgesia
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loss of pain
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hypnosis
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loss of consciousness
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general anesthetics are
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drugs that produce analgesia, hypnosis, amnesia, and muscle relaxation by depressing reversibly the CNS
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Volatile (gas) anesthetics:
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N2O
halogenated hydrocarbons cyclopropane |
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fixed (IV/ING) anesthetics:
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barbituates, BZD, ehtomidate, ketamine, certain opoid anagesics
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Anesthetics the bind to GabaA
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BZDs
propofol halogenated volatiles barbiturates |
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anesthetics that are glutamic acid receptor inhibitors
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ketamine, N2O, cyclopropane, xenon
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MAC
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minimum alveolar concentration in umol/L required to prevent movement of 50% of patients in response to a surgical stimulus
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methoxyflurane is an anesthetic that causes
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renal damage!
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halothane is a volatile anesthetic that causes
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liver necrosis via trifluoroacetylated protein
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problems with barbiturates
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high toxicity
abuse and addiction potential inferior at producing sleep respiratory problems |
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BZDs
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parenteral anesthetics
anesthetic adjuncts, used for sedation |
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midazolam
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Versed
most frequently used BZD high P value |
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flumazenil
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BZP - receptor antagonist
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Ketamine
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fixed IV anesthetics
blocks NMDA receptor dissassociate anesthsia |
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etomidate
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fixed IV anesthetics
ultra short acting GABA-like MAO IDEAL for patients w/hypotentsion! |
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propofol
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most popular parenteral iv anesthetic
binds to GABAa receptor ultra short acting water soluble IV ONLY |
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GabaA receptor
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ligand gated Cl- channel
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DMCM
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inverse agonist of Gaba receptor
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BZD are metabolized extensively
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by CYP34A & CYP2C9 to 3-glucuronides
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inhibitors of CYP34A
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erythromycin
ritonavir ketoconazole grape fruit juice |
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DMD
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active metabolite of many BZPs
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drugs that are dopamine receptor agonists tend to have
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EPS side effects
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anxiolytic
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preventing or reducing anxiety
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5 criteria for nuerotransmitters:
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produced & found in nueron
must be released by nueron upon sitmulation have a post-synaptic receptor cause a biological effect chemical must be inactivated once released effect of chemical = effect of stimulating presynaptic pathway |
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PPA
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banned due to CV AE
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which isomer of methlyphenidate is more active agaisnt ADHD?
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R-ISOMER
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Vyvanse
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amphetamine prodrug
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the higher the partition coefficient
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the lower the MAC
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major urinary metabolite of buspirone
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1-PP
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addition of OH to BZP
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makes drug more susceptible to phase 2 metabolism:
glucornidation |
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increase acitivity of BZPs
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e- withdrawing group on position 7
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