Term
| Weak base or weak acid drugs result in what state? |
|
Definition
| Ionized= with a net electrical charge |
|
|
Term
| How do you facilitate absorption of ionized drugs? |
|
Definition
| Administer as a salt= as anion and cation |
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|
Term
| Which form of charged drug is more lipid soluble? |
|
Definition
| non-ionized= more lipid soluble |
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|
Term
| Aspirin is in a.. form, therfore more active in the...pH |
|
Definition
| Ionized form, but less ionized in an acid medium like the stomach around pH 3.0 |
|
|
Term
| The most rapid onset route of drug administration is.. |
|
Definition
| Intravenous injection- which also allows for more intense effects |
|
|
Term
| Latin name for oral administration |
|
Definition
|
|
Term
| IV drugs must be in _____form or in a _____ |
|
Definition
| Solution, or an aqeous vehicle |
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|
Term
| Another method of administration quicker than PO, is ____ as it is supplied well with blood vessels |
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Definition
|
|
Term
| The ____ administration route prevents first-pass elimination |
|
Definition
|
|
Term
Injection into fatty tissue is called___
and is used for more___ absorption |
|
Definition
subcutaneous (SC) drug injection
Slower and more even absorption |
|
|
Term
| Route used for drugs destroyed in the stomach |
|
Definition
| Sublingual or buccal admin |
|
|
Term
| Methods used to bypass the BBB |
|
Definition
Intrathecal ( subdural space injection)
Intracerebroventricular injection into brain ventricles |
|
|
Term
| Methods of controlled release are |
|
Definition
| couple drug to specific transport molecule, as pro-drugs for internal activation |
|
|
Term
| transdermal admin is limited by |
|
Definition
| charged or large molecules that cannot pass through the skin |
|
|
Term
| Feature of the BBB preventing free diffusion |
|
Definition
| Tight junctions at capillary bases |
|
|
Term
| Brain capillaries are joined tightly to long processes___ of ___cell |
|
Definition
| Extension processes or glial cells called astrocytes |
|
|
Term
| Sheath surrounding brain capillaries |
|
Definition
| glial feet forming lipid sheath from astrocytes |
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|
Term
| Transport mechanism using energy |
|
Definition
|
|
Term
|
Definition
| nutritive, but non-lipid soluble substances |
|
|
Term
| Drugs that act on CNS neurons must be |
|
Definition
| Lipid-soluble, or compatible with membrane transporter systems |
|
|
Term
|
Definition
| top of the brain stem- and is exposed to the blood to detect poisons |
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|
Term
| Single most important variable in drug admin for the effect |
|
Definition
|
|
Term
| Discussing drugg's effects |
|
Definition
|
|
Term
| How to dose-response study |
|
Definition
| Take gorup of population, administer different doeses, and record degree of effect specified effects of drug |
|
|
Term
|
Definition
| Placebo, vehicle solution for delivery, or active placebo |
|
|
Term
|
Definition
| mimics physiological characteristics of drug of interest without neuronal effects of interest |
|
|
Term
|
Definition
Magnitude of the effect of a drug, expressed in terms of maximal drug effect
Best to use efficacy as effects at organismal level |
|
|
Term
|
Definition
| the dose at which an effect occurs |
|
|
Term
|
Definition
| ED50(effective dose 50% of maximal effect) |
|
|
Term
| Potency is related to ED50 how? |
|
Definition
|
|
Term
| Dose-response curves y-axis |
|
Definition
|
|
Term
|
Definition
|
|
Term
| Typical dose-response shape |
|
Definition
|
|
Term
|
Definition
| minimal dose for detectable effects |
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|
Term
|
Definition
| ED50 compared to LD50, Divide LD50 by ED50 |
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|
Term
|
Definition
| Repetitive , ritualistic, compulsive behaviours |
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|
Term
| Major metabolic processes for drugs |
|
Definition
| Cleavage, oxidation,conjugation, reduction |
|
|
Term
|
Definition
| metabolism in the liver by the hepatic microsomal enzyme system |
|
|
Term
|
Definition
| drugs metabolism is log proportional to plasma concentration |
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|
Term
| Liver tolerance can build by |
|
Definition
| upregulation of CYp450 synthesis genes |
|
|
Term
|
Definition
| increasing metabolism and excretion of drugs based on pH and excreted medium pH |
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|
Term
| alcohol is metabolized by what enzyme? |
|
Definition
| ADH Alcohol dehydrogenase |
|
|
Term
|
Definition
| differences in behavioural effects of alcohol based on the rising or falling phase of intoxication at the SAME BAC |
|
|
Term
|
Definition
| Acetaldehyde and then acetate then water and CO2 |
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|
Term
|
Definition
| CYP450-2E1, Catalase-H2O2. and ADH |
|
|
Term
|
Definition
| make membranes more fluid |
|
|
Term
|
Definition
| inhibition of Na+ and K+ inhibiting action potentials |
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|
Term
| Neurotrasmitter responsible for Alcohol rewards |
|
Definition
|
|
Term
| Receptors relevant to ETOH tolerance, dependence and chronic use |
|
Definition
|
|
Term
GABAa activation allows what
NMDA activation allows what |
|
Definition
GABAa= Cl- influx and hyperpolarization
NMDA= Ca2+ influx and depolarization |
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|
Term
| Ethanol effects on receptors? |
|
Definition
| Enhances GABAa, inhibits NMDA |
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|
Term
| Individuals at risk display what preactivation curve characteristics |
|
Definition
| Greater stimulant like on ascending, and lesser sedative like on descending |
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|
Term
| Wernickes'-Korsakoffs is usually a result of? |
|
Definition
| Malnutition, and Thiamine deficiencies |
|
|
Term
| Abstinence syndrome consists of |
|
Definition
| EEG disturbances during sleep, high degree of arousal tremors, weakness, and increase Bp and resp R. |
|
|
Term
| Visual hallucinations, fever, nausea in alcoholic withdrawal is called |
|
Definition
|
|
Term
| Kindling process in alcoholism is |
|
Definition
| each episode of withdrawal leads to more intense withdrawal responses |
|
|
Term
|
Definition
| require high soocial reward dependence, display guilt when drinking, abstain for longer periods, and then binge, do not seek thrill |
|
|
Term
|
Definition
| rarely binge, chronic drink, thrill-seekers, anti-social, no guilt when drinking, and rarely require social rewards |
|
|
Term
|
Definition
| providing anti-craving NMDA receptor antagonism |
|
|
Term
| Naltrexone and Nalmefene work by |
|
Definition
| blocking endorphine receptors, preventing euphoric feelings and damped next-drink craving |
|
|
Term
|
Definition
| increasing abstinence periods in early-onset alcoholics |
|
|
Term
|
Definition
| the GABAa receptor as allosteric agonists to increase GABA release and Cl- influx for hyperpolarization |
|
|
Term
|
Definition
| a atypical anxiolytic, reduces emotional problems of anxiety |
|
|
Term
|
Definition
| acting to downregulate 5-HT, as a 5_HT1A partial agonist |
|
|
Term
| opiates influence and work on |
|
Definition
inhibiting NE and stimulates DA release indirectly
stimulate endorphin systems stimulating opiate receptors |
|
|
Term
| primary analgesia pathwaysa |
|
Definition
| thalamus, periaqueductal grey, spinal cord, locus coeruleus, VTA, and NA |
|
|
Term
|
Definition
| endorphine, enkaphalin, dynorphin |
|
|
Term
|
Definition
|
|
Term
| endogenous opiods primarily target |
|
Definition
|
|
Term
| exogenous opiod agonists target |
|
Definition
|
|
Term
| activation of opioid receptors causes? |
|
Definition
| inhibiting of GABA leading to facilitate DA release |
|
|
Term
|
Definition
| analgesia, cough suppression, heroin addiction |
|
|
Term
|
Definition
| g-protein coupled metabotropic |
|
|
Term
| Mu opioid agonists are responsible for |
|
Definition
| euphoria, analgesic effects, respiratory depression, GI motility slowing and sedation |
|
|
Term
| Delta receptors are ____selective and responsible for |
|
Definition
| enkephalin selective, spinal analgesia |
|
|
Term
|
Definition
| cause aversive psychosis like effects and drugs are aversive and do not cause drug seeking behaviours |
|
|
Term
|
Definition
| hyperalgesia, and blocks morphine effects |
|
|
Term
| heroine compared to morphine |
|
Definition
| modified morphine, crosses BBB quicker and accumulates in brain quicker, thereby mroe fast-acting but similar potency |
|
|
Term
| Methadone compared to heroin and morphine |
|
Definition
same potency as morphine and half potency of heroin for analgesia
Suppress opiate withdrawl symptoms 2X comapred to heroin, and $x for morphine
Lasts longer than either as well |
|
|
Term
| One of most potent non endogenous opiods |
|
Definition
|
|
Term
|
Definition
| work best to reduce dull pain- for chronic pain conditions post-op= not effective during surgery |
|
|
Term
| opiate rushes are localized in what nucleus? |
|
Definition
|
|
Term
| opiate receptor activation on presynaptic terminals induces? |
|
Definition
| Ca2+ inlfux inhibition, enhances K+ efflux hyperpolarizing membranes |
|
|
Term
| opioid receptors belong to the family of? |
|
Definition
| inhibitory g-protein coupled receptors |
|
|
Term
| naltrexone is effective for opiates by |
|
Definition
| blocking opiate actions for3 days and not inducing physical dependence or dysphoria |
|
|
Term
| Drug discrimination paradigm |
|
Definition
| animals are rewarded upon detecting specific subjective effects of drug vs. non-drug administrations= used to determine subjective effects of varying compounds |
|
|
Term
| MA pph's induce similarity to what kinds of effects of drugs? |
|
Definition
| Amphetamine (MDA) to LSD like (Psilocybin, mescaline) |
|
|
Term
|
Definition
| psychostimulant, sympathomimetic, pupilarry dilation...etc.. |
|
|
Term
| LSD acts on what systems? |
|
Definition
inhibiting serotonergic systems
activates 5-HT autoreceptors and some post-synaptic receptors |
|
|
Term
|
Definition
| partial agonist on 5-HT2A enhancing asynchronous release of GLU due to low Ca2+ levels remaining in terminals following initial influx, stimulating hallucinations |
|
|
Term
| MDMA as a PPH exerts effects through |
|
Definition
| the serotonergic system as a reuptake inhibiter and releaser of 5-HT, DA, NA and Ach |
|
|
Term
|
Definition
| LSD like and amphetamine like without LSD hallucinations |
|
|
Term
| potential damage by short-term MDMA exposure? |
|
Definition
| neurotoxic effects on serotonergic systems, depleting 5-ht levels, and causing nerve degeneration |
|
|
Term
|
Definition
| the self-adjustment of dosage by individuals self-administering a drug in order to achieve the desired affects |
|
|
Term
| how does tHC have sedative effects without aenesthetic properties? |
|
Definition
| by fluidizing membranes nonspecofically |
|
|
Term
| The L-THC isomer is _____active than the D-isomer? |
|
Definition
|
|
Term
| THC exerts effects at ___ and ___ receptors |
|
Definition
|
|
Term
| THC receptors are located where? |
|
Definition
|
|
Term
| THC receptors__ act on ____systems to ___them |
|
Definition
| CB1, secondary messenger to inhibit them |
|
|
Term
| Two other compounds in marijuana besides THC |
|
Definition
| Cannibinol, and Cannabidiol |
|
|
Term
| Endogenous cannabinoids ____ and ___ |
|
Definition
|
|
Term
|
Definition
|
|
Term
| Cannabinoids act as ____ Nt's |
|
Definition
| Retrograde by inhibiting GABA release, and GLU |
|
|
Term
| Lack of cannabin receptors in the ___ |
|
Definition
|
|
Term
| Low doses of stimulants increase ____ and ___ behaviours |
|
Definition
| locomotion and exploratory |
|
|
Term
| Higher doses of stimulants reduce ___ and increase____ |
|
Definition
|
|
Term
| DA depletion in NA causes_____ |
|
Definition
| supressed locomotor activity only |
|
|
Term
| DA depletion in NEostriatum cases___ |
|
Definition
| reduced sterotypy but not locomotor |
|
|
Term
| caffeine exerts effects by___ |
|
Definition
| antagonizing adenosine A1 receptors, activating pre-synaptic NT release by inhibiting adenosine |
|
|
Term
| cigarrette smokers have ___ levels of plasma caffiene while smoking compered to abstinence |
|
Definition
|
|
Term
| Headaches from caffiene withdrawal are likely due to |
|
Definition
| rebound of vasoconstrictive properties |
|
|
Term
|
Definition
|
|
Term
| Nicotine can cause mild ___ effects |
|
Definition
| psychostimulant, enchanced vigilance comparable to caffiene doeses |
|
|
Term
| Nicotine shifts EEG patterns towards those associated with ____ |
|
Definition
|
|
Term
| Nicotine is ____to simpale tasks but apepars ___ to more complex tasks |
|
Definition
| beneficial to simple, detrimental to complex |
|
|
Term
| in the PNS Nach activation causes _____ due to NAchR presence on ____ releasing ___? |
|
Definition
| sympathomimetic stimulation (activation), presence on adrenal glands releasing NE but are also present on parasympathomime neurons |
|
|
Term
| Nicotine smoke affects MAO by ______ |
|
Definition
| inhibiting them, increasing DA presence in synapses |
|
|
Term
| Chronic exposure to nicotine causes Narc _____, but causes Narcs to ______ |
|
Definition
| upregulation, but desensitize an dinactivate |
|
|
Term
| Nicotine has ____ as well as ____ reinforcing properties |
|
Definition
|
|
Term
| More potent isomer of Amphetamine |
|
Definition
|
|
Term
| Amphet is more used in low doses to ______control, and high doses _____ performance |
|
Definition
| enhance muscle coordination and control, and interferes with performance |
|
|
Term
| subjective increases in effects to amphetamine after the third admin indicates ____? |
|
Definition
|
|
Term
| subjective decreases in ratings of liking to amphetamine after thirds admin indicates ___? |
|
Definition
|
|
Term
| Amphetamine neurodegeneration can be attributed to their ability to _____? |
|
Definition
| inhibit MAO and allow MA's to oxidize into neurotoxic compounds |
|
|
Term
| Formication and snow light are what associations to which drug? |
|
Definition
| bugs on skin and distorted lights, with cocaine |
|
|
Term
| Cocaine effects for ___mins, amphetamine for ____ mins |
|
Definition
|
|
Term
| snortin cocaine allows ____ rapid onset, and ____ duration than smoking |
|
Definition
| slower absorption, longer duration than smoking |
|
|
Term
|
Definition
| cocaine vasoconstrictiion |
|
|
Term
| free-base cocaine is used for |
|
Definition
| crack, to smoke, as hydrochloride is degraded whem volatalized |
|
|
Term
| Tolerance to cocaine can develop by |
|
Definition
| autoreceptor activation, or depletion of MA's, or down-regulation of MA receptors |
|
|
Term
| subconvulsive doses of cocaine can ____threshold |
|
Definition
| lower seizure threshold - kindling |
|
|
Term
| cocaine withdrawl follows a ____ model? |
|
Definition
|
|
Term
| effects of heavy amphetamine use? |
|
Definition
| psychosis, irritability, paranois, eating and sleeping disturbances |
|
|
Term
| effects of heavy cocaine use? |
|
Definition
| psychosis, irritability, anorexia, focus on cocaine, and precipitate panic attacks |
|
|
Term
|
Definition
| myocardial infarction, seizure, haemorrhaging, arrhythmias |
|
|
Term
|
Definition
| teratogenic, impedes fetal blood supply, dysfunction of DA receptors and signalling, abnormal dendritic patterns |
|
|
