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PHAR 100 – Module 3 University of California, San Francisco
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low |doses |of |sedative-hypnotics |cause |- |answersanti-anxiety medium-low |doses |of |sedative |hypnotics |cause |- |answersrelieve |anxiety, |decrease |activity, |moderate | excitement, |calm Medium-high |doses |of |sedative |hypnotics |- |answershypnosis |(sleep) |- |drowsiness, |aid |in |onset |and | maintenance |of |sleep High |dose |of |sedative |hypnotics |- |answersgeneral |anesthesia |- |unconscious, |absence |of |pain How |do |depative-hypnotics |work? |- |answersBind |to |different |sites |than |GABA |on |the |chloride | channel, |enhancing |the |inhibitory |effect |of |GABA How |does |GABA |cause |inhibition? |- |answersBinds |to |chloride |channels |and |selectively |opens |them Causes |hyperpolarization |of |the |postsynaptic |membrane, |making |it |harder |for |the |postsynaptic | neurons |to |transmit |incoming |messages Depresses |CNS |neuronal |signalling Activation |of |the |benzodiazepine |receptor... |- |answersincreases |the |frequency |of |the |opening |of |the | chloride |channel What |is |the |most |common |drug |involved |in |overdose? |- |answersBenzodiazepines but |they |have |a |wide |margin |of |safety |so |deaths |are |rare |- |need |a |very |large |dose, |rapid |injection, |or |mixing |with |other |drugs What |is |the |antidote |to |benzodiazepines? |- |answersFlumazenil What |type |of |sleep |do |benzodiazepines |cause? |- |answersREM-type Short |term |effects |of |benzodiazepines |- |answersCNS: |relaxation, |calmness, |reduced |anxiert, | drowsiness, |fatigue, |impairment |of |thinking/memory Lungs: |respiratory |depression |following |rapid |intravenous |administration Motor |coordination: |moderate |doses |can |impair |motor |coordination |and |driving, |response | exaggerated |as |dose |is |increased Chronic |sedative-hypnotic |intoxication |- |answersimpaired |thinking, |poor |memory |and |judgement, | disorientation, |incoordination, |slurred |speech Benzodiazepines |and |pregnancy/breastfeeding |- |answersCan |cross |the |placenta If |administered |in |the |first |trimester |results |in |a |small |but |significant |risk |for |fetal |abnormalities
Are |secreted |into |breast |milk |which |can |lead |to |sedation |or |death |of |baby Abuse |and |dependence |of |benzodiazepines |often |in |combination |with |- |answersalcohol |to |enhance | depressant |effects Abuse |liability |of |benzodiazepines |is... |- |answerslow |since |they |have |weak |reinforcing |properties Inherent |harmfulness |of |benzodiazepines |is... |- |answerslow |(high |margin |of |safety) Does |not |depress |respiration |at |therapeutic |doses Often |does |not |lead |to |death |on |its |own Tolerance |can |develop |to |what | 3 |effects |of |benzodiazepines? |- |answersSedative |effects |and | impairment |of |coordination |(most |common) Anxiolytic |effects Euphoric |effects Why |is |there |a |high |degree |of |cross-tolerance |amount |the |sedative-hypnotics? |- |answersBecause |they |all |modulate |the |chloride |channel |in |the |CNS Risk |of |dependence |on |benzodiazepines |- |answerslow |for |short-term |use Can |withdrawal |occur |after |therapeutic |use |of |benzodiazepines? |- |answersYes anxiety, |headache, |insomnia, |tension, |difficulty |concentrating, |fatigue Can |addiction |occur |with |benzodiazepines? |- |answersCan |develop |in |some |users Zolpidem |- |answersBinds |to |a |subset |of |GABA |receptors |(agonist), |causing |sedation Have |more |sedative |effects |than |anxiolytic |effects Benefit |of |Zolpidem |over |benzodiazepines |- |answersDon't |disturb |REM |sleep |as |much Basic |structure |of |all |barbiturates |- |answersBarbituric |acid Activation |of |the |barbiturate |receptor |- |answersIncreases |the |duration |of |the |opening |of |the |chloride | channel How |are |barbiturates |classified? |- |answersLong |acting |(1-2h), |short |acting |(3-8h), |ultra |short |acting | (20 |min) What |are |the |uses |of |ultrashort |and |short-acting |barbituates? |- |answersInduce |anesthesia Therapeutic |use |of |barbiturates |- |answersantiepileptics Is |there |an |antidote |for |barbituate |overdose? |- |answersNo Lethality |from |barbituates |is |common, |especially |when |combined |with |- |answersAlcohol Therapeutic |index |of |barbiturates |- |answersLow
What |affects |the |absorption |rate |of |alcohol? |- |answersStomach |emptying |time/the |time |required |for | alcohol |to |reach |the |small |intestine Ethanol |concentration |in |GI |tract |and |presence |of |food Distribution |of |alcohol |- |answersdistributes |throughout |the |total |body |water, |readily |gains |access |to | the |brain, |readily |transfers |across |the |placenta |and |throughout |the |fetus Metabolism |of |alcohol |- |answersethanol |-> |acetaldehyde |-> |acetic |acid Describe |the |detailed |metabolism |of |alcohol |- |answers1. |ethanol |converted |to |acetaldehyde |by |ADH | (rate |controlling |step)
Irritate |the |lining |of |the |stomach, |causing |inflammation |and |erosion |(gastritis) |leading |to |vomiting, | abdominal |pain, |ulcers |can |be |aggravated |leading |to |gastrointestinal |bleeding Alcohol |binge |will |inhibit |glucose |production |by |the |liver, |in |association |with |fasting |can |lead |to | hypoglycemia |(low |blood |sugar) Alcoholic |dementia |- |answersdecrease |in |cognitive |functioning, |affecting |memory, |judgement |and | thinking, |alcohol |damages |axons |of |neurons |resulting |in |fewer |connections Alcoholic |cardiomyopathy |- |answersincreased |incidence |of |hypertension |and |stroke 3 |stages |of |alcoholic |liver |disease |- |answers1. |liver |cells |accumulate |fat, |liver |enlarges, |usually | asymptomatic |and |reversible |if |alchol |consumption |is |stopped
What |is |prescribed |to |prevent |nausea |and |vomiting |associated |with |anticancer |drugs? |Why? |- | answersSynthetic |THC |derivatives |because |they |are |generally |more |selective |than |cannabis |in |treating |nausea Medical |uses |of |cannabis |- |answersPrevent |nausea |and |vomiting |in |cancer |patients Stimulate |appetite |in |patients |on |anti-HIV |drugs Neuropathic |pain Epilepsy Glaucoma Spasticity Migranes Dependence |liability |of |cannabis |- |answersLow |to |moderate Inherent |harmfulness |of |cannabis |- |answerslow |especially |with |infrequent |use Risk |of |cannabis |addiction |is |more |evident |in |users |who |- |answersuse |cannabis |to |control | psychological |stress Tolerance |can |develop |to |what |effects |of |cannabis |- |answerspsychoactive |properties, |effects |on |the | cardiovascular |system, |impairment |of |performance |and |cognitive |function Cannabis |dependence |and |withdrawal |- |answerscan |occur |with |high-dose |use, |can |experience | withdrawal |symptoms Opiate |- |answersany |drug |derived |from |opium Opioid |- |answersany |natural |or |synthetic |substance |which |exerts |actions |on |the |body |similar |to |those | induced |by |morphine |and |that |are |antagonized |by |the |drug |naloxone Includes: |opiates, |synthetic |drugs, |endorphins 3 |families |of |endorphins |- |answersenkephalins, |dynorphins, |B-endorphins Neuromodulators |- |answerscan |act |on |other |neurons, |increasing |or |decreasing |the |effect |of | neurotransmitters, |but |does |not |itself |initiate |depolarization Where |are |opioid |receptors |located? |- |answersCNS, |GI |tract, |peripheral |nervous |system Where |are |MU |receptors? |- |answersBrain |and |spinal |cord Effects |of |MU |receptors |- |answersAnalgesia |(most |important |receptor |for |this) Responsible |for |morphine-mediated |depression |of |respiration |in |the |brain |stem Involved |in |the |compulsive |abuse |behaviour |demonstrated |by |opiate |users effects |of |kappa |receptors |- |answersanalgesia, |dysphoria |(state |of |dissatisfaction |or |unease), |miosis | (pin-point |pupils)
effects |of |delta |receptors |- |answersanalgesia |at |the |level |of |the |spinal |cord |and |brain May |modulate |emotional |response |to |opioids Heroin |- |answersproduced |from |morphine more |potent |but |not |more |efficacious |than |morphine rapidly |converted |to |morphine |in |the |body What |has |more |intense |sedation/hypnosis |effects, |CNS |depressants |or |opioids? |- |answersCNS | depressants Location |of |the |cough |centre |- |answersmedulla Respiratory |depression |due |to |opioids |- |answerssuppress |the |respiratory |center |in |the |brain |stem | response |to |respiratory |drive |by |CO2 |is |blunted |mediated |by |MU |and |delta |receptors Endocrine |effects |of |opioids |- |answersreduced |testosterone/estrogen/progesterone |release |from |the | hypothalamus Drop |in |libido Menstrual |irregularities Medical |uses |of |heroin |- |answersnone Medical |uses |of |morphine |- |answersRelief |of |severe |pain Treatment |of |diarrhea Cough |suppression Diphenoxylate |(Lomotil) |- |answersover |the |counter |antidiarrheal Opiate |that |is |not |an |analgesic, |does |not |produce |dependence Opioid |MOA |for |analgesia |- |answers1. |Reduce |presynaptic |release |of |chemical |transmitters |than |are | mobilized |by |pain |impulses
long |half-life lower |abuse |potential |than |morphine |and |heroin