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Pharmacology > Exam II > Flashcards

Exam II Flashcards

1
Q

Chlorpromazine

A
  • antagonist in decreasing order at: alpha1, H1, 5-HT2, D2, D1, M, alpha2.
  • typical antipsychotic.
  • low potency, low specificity.
  • use high doses.
    *
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2
Q

Imipramine

A
  • tertiatry amine TCA.
  • antagonist at alpha1, muscarinic and histaminergic H1 receptors.
  • inhibits NE and 5-HT reuptake pumps.
  • blocks fast-Na channels.
  • active metabolite = desipramine
  • use: bed-wetting.
  • side efects: dry mouth, constipation, blurred vision, orthostatic hypotension, difficulty urinating, sedation, confusion, weight gain, prolonged QT with cardiac toxicity in overdose.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
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3
Q

Buspirone

A
  • 5-HT1A partial agonist ⇒ anxiolytic
  • no hypnotic, anticonvulsant, or muscle relaxant effects.
  • takes 1-2 wks to work
  • no rebound anxiety or withdrawal symptoms
  • nonsedating, less psychomotor impairment, doesn’t impair driving.
  • minimal abuse potential
  • use: generalized anxiety disorder (GAD)
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4
Q

LSD

A
  • 5-HT2A partial agonist ⇒ hallucinogen
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5
Q

Ondansetron

A
  • 5-HT3 antagonist ⇒ antiemetic
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6
Q

Nefazadone

A
  • 5-HT2A antagonist ⇒ antidepressant
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7
Q

Risperidone

A
  • high potency atypical anti-psychotic
  • blocks 40-60% D2, 70-90 5-HT2A.
  • acute = tranquilizer.
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, some help with negative.
  • use: schizophrenia, psychosis with manic-drepressive/schizoaffective disorders or depression.
  • side effects: metabolic problems (weight gain)
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8
Q

Cocaine

A
  • inhibits DA reuptake in CNS.
  • rapidly penetrates BBB ⇒ elation and euphoria.
  • major drug of abuse.
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9
Q

Methylphenidate

A
  • inhibits DA reuptake in CNS.
  • slower BBB penetration ⇒ less elation or euphoria than cocaine.
  • use: ADHD
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10
Q

Amphetamine/Metamphetamine

A
  • induce release of NE and DA in CNS.
  • use: ADHD, narcolepsy
  • side effects: chronic abuse at high doses ⇒ paranoid psychosis after 2-3 wks.
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11
Q

Haloperidol

A
  • high potency typical antipsychotic.
  • inhibits D2 and other receptors.
  • acute = tranquilizing effects but still psychosis.
  • chronic = antipsychotic effects after 2-4 wks.
  • use: schizophrenia, particularly in emergencies and in pregnancy, Tourette’s syndrome, Huntington’s chorea.
  • side effects: tardive dyskinesia, parkinsonism, akathisia, acute dystonia, hyperprolactinemia.
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12
Q

Extrapyramidal Motor Symptoms

A
  • tremor, rigidity, bradykinesia, mask-like face, altered posture.
  • from dysfunction of basal ganglia (caudae nucleus, putamen, globus pallidus, subthalamic nucleus, substantia nigra).
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13
Q

L-DOPA

A
  • converted by DOPA-decarboxylase to DA.
  • ⇒ ↑ DA release by surviving neurons.
  • need higher dose as disease progresses
  • use: Parkinson’s Disease.
  • side effects: nausea, vomiting, ↑ risk dyskinesias, GI adverse effects, postural hypotension, depression, hallucination, anxiety, agitation.
  • 80% get dyskinesias with long term use.
  • may hasten disease progression.
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14
Q

Carbidopa

A
  • DOPA-decarboxylase inhibitor.
  • does not penetrate CNS.
  • prevents L-DOPA conversion to DA in periphery.
  • ↑ L-DOPA potency and ↓ nausea, vomiting, and adverse effects from peripheral generation of DA.
  • use: Parkinson’s Disease
  • side effects: ↑ risk dyskinesias, GI adverse effects, postural hypotension, depression, hallucinations, anxiety, agitation.
  • 80% develop dyskinesia with long term use.
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15
Q

SINMET

A
  • combination of L-DOPA and carbidopa.
  • use: Parkinson’s Disease
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16
Q

Bromocriptine

A
  • ergot DA receptor agonist
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • need careful dosing titration to avoid hypotension.
  • use: Parkinson’s Disease
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension.
  • dose related effects eventually outweight therapeutic effects.
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17
Q

Pergolide

A
  • ergot DA receptor agonist
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • need careful dosing titration to avoid hypotension.
  • use: Parkinson’s Disease
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension, risk of heart valve fibrosis from 5-HT2B activation
  • dose related effects eventually outweight therapeutic effects.
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18
Q

Pramipexole

A
  • non-ergot DA receptor agonist
    • preferred over ergots (faster and safer titration)
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • use: Parkinson’s Disease, restless-legs syndrome
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension, sudden onset daytime sleepiness
  • dose related effects eventually outweight therapeutic effects.
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19
Q

Ropinirole

A
  • non-ergot DA receptor agonist
    • preferred over ergots (faster and safer titration)
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • use: Parkinson’s Disease, restless-legs syndrome
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension, sudden onset daytime sleepiness
  • dose related effects eventually outweight therapeutic effects.
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20
Q

Apomorphine

A
  • potent non-ergot DA receptor agonist
  • given subQ for rapid, temporary relief of ‘off’ episodes, takes <10mins.
  • less motor recovery and more side effects than L-DOPA.
  • ↓ risk dyskinesias.
  • use: Parkinson’s Disease
  • side effects: nausea, vomiting, psychiatric rxns, postural hypotension.
  • dose related effects eventually outweight therapeutic effects.
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21
Q

Selegiline

A
  • MAO-B inhibitor.
  • enhances L-DOPA effects.
  • metabolites = aphetamine and methamphetamine ⇒ insomnia and anxiety.
  • use: add on for Parkinson’s Disease
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22
Q

Rasagline

A
  • MAO-B inhibitor.
  • enhances L-DOPA effects.
  • use: add on for Parkinson’s Disease
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23
Q

Entacapone

A
  • COMT inhibitor.
  • peripheral action only
  • enhances L-DOPA effects by blocking conversion to 3-O-methylDOPA.
  • use: add on for Parkinson’s Disease
  • side effects: from enhanced L-DOPA actions.
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24
Q

Tolcapone

A
  • COMT inhibitor.
  • enters CNS.
  • enhances L-DOPA effects by blocking conversion to 3-O-methylDOPA.
  • use: add on for Parkinson’s Disease
  • side effects: from enhanced L-DOPA actions, hepatotoxicity
  • need to monitor liver enzymes
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25
Q

Benztropine

A
  • antimuscarinic.
  • improves tremor and rigidity, little effect on bradykinesia.
  • use: add on for Parkinson’s Disease
  • side effects: sedation, dry mouth, etc. (anti-muscarinic effects)
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26
Q

Trihexiphenidyl

A
  • antimuscarinic.
  • improves tremor and rigidity, little effect on bradykinesia.
  • use: add on for Parkinson’s Disease
  • side effects: sedation, dry mouth, etc. (anti-muscarinic effects)
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27
Q

Diphenhydramine

A
  • antimuscarinic.
  • improves tremor and rigidity, little effect on bradykinesia.
  • use: add on for Parkinson’s Disease
  • side effects: sedation, dry mouth, etc. (anti-muscarinic effects)
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28
Q

Amantidine

A
  • enhances DA release
  • short-lived effects (wks to months)
  • use: add on for Parkinson’s Disease
  • side effects: CNS effects, peripheral edema, skin discoloration from vasodilation, toxic psychosis, convulsions from overdose.
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29
Q

Stalevo

A
  • combo pill of entacopone, carbidopa, and L-DOPA.
  • use: severe Parkinson’s Disease with on-off fluctuations.
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30
Q

Tacrine

A
  • AchE inhibitor
  • ⇒ modest improvement in mild to mod Alzheimer’s.
  • positive effects at low doses
  • use: Alzheimer’s Disease
  • side effects: cholinergic side effects
  • disease continues to progress
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31
Q

Donepezil

A
  • AchE inhibitor
  • ⇒ modest improvement in mild to mod Alzheimer’s.
  • positive effects at low doses
  • use: Alzheimer’s Disease
  • side effects: cholinergic side effects
    disease continues to progress
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32
Q

Rivastigmine

A
  • AchE inhibitor
  • ⇒ modest improvement in mild to mod Alzheimer’s.
  • positive effects at low doses
  • use: Alzheimer’s Disease
  • side effects: cholinergic side effects
  • disease continues to progress
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33
Q

Galantamine

A
  • AchE inhibitor
  • positive allosteric modulator of nicotinic Ach receptors
  • ⇒ modest improvement in mild to mod Alzheimer’s.
  • positive effects at low doses
  • use: Alzheimer’s Disease
  • side effects: cholinergic side effects
  • disease continues to progress
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34
Q

Memantine

A
  • NMDA receptor, negative allosteric modulator
  • use: mod to severe Alzheimer’s Disease
  • small benefit
  • disease still progresses
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35
Q

d-Tubocurarine

A
  • competitive NMJ blocking agent.
  • large and bulky
  • inhibits amplitue of endplate potentials so propagated action potential can’t develop
  • +++ histamine release
  • duration: hours
  • elimination: renal
  • use: muscle relaxant, anasthetic
  • side effects: blockade of nicotinic receptors in sympathetic ganglia. (↓ BP)
  • reversed by ACHEI and ↑ extracellular K+
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36
Q

Metocurine

A
  • competitive NMJ blocking agent.
  • large and bulky
  • 3x potency of d-tubocurarine.
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop
  • ++ histamine release
  • duration: hours
  • elimination: renal
  • use: muscle relaxant, anesthetic
  • side effects: autonomic
  • reversed by ACHEI and ↑ extracellular K+
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37
Q

Pancuronium

A
  • competitive NMJ blocking agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop
  • no histamine release
  • duration: hours
  • elimination: renal
  • use: muscle relaxant, anesthetic
  • side effects: blockade of nicotinic receptors in parasympathetic ganglia. (↑ HR, **↑ BP, **↑ AV conduction)
  • reversed by ACHEI and ↑ extracellular K+
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38
Q

Vecuronium

A
  • competitive NMJ blockingn agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop.
    • histamine release
  • duration: 30-40 mins
  • elimination: 85% bile, 15% renal
  • use: muscle relaxant, anesthetic
  • side effects: autonomic
  • reversed by ACHEI and ↑ extracellular K+
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39
Q

Rocuronium

A
  • competitive NMJ blockingn agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop.
    • histamine release
  • duration: 30-40 mins
  • elimination: 85% bile, 15% renal
  • use: muscle relaxant, anesthetic
  • side effects: autonomic
  • reversed by ACHEI and ↑ extracellular K+
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40
Q

Atracurium

A
  • competitive NMJ blocking agent
  • large and bulkly
  • inhibits amplitude of endplate potentials so propagated action potentials can’t develop
  • ++ histamine release
  • duration: 30-40 mins
  • elimination: spontaneous hydrolysis in plasma = Hofman elimination rxn.
  • use: muscle relaxant, anesthetic.
  • side effects: metabolite = Laudanoside is a CNS stimulator.
  • reversed by ACHEI and ↑ extracellular K+
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41
Q

Mivacurium

A
  • competitive NMJ blocking agent.
  • large and bulky
  • inhibits amplitude of endplate potentials so propagated action potential can’t develop
  • causes ++ histamine release
  • duration: 10-15 min
  • elimination: plasma pseudocholinesterase
  • use: muscle relaxant, anesthetic
  • side effects: autonomic
  • reversed by ACHEI and ↑ extracellular K+
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42
Q

Neostigmine

A
  • ACHEI
  • ⇒ ↑ Ach levels, competitively reverses block.
  • enhances depolarization block.
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43
Q

Edrophonium

A
  • ACHEI
  • ⇒ ↑ Ach levels, competitively reverses block.
  • enhances depolarization block.
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44
Q

Sugammedex

A
  • cyclodextrin molecule that encapsulates the blocker
  • ⇒ ↓ blocker.
  • mostly for steroids. (-oniums)
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45
Q

Succinylcholine

A
  • depolarization blocker.
  • flexible and narrow.
  • ⇒ sustained depolarization block of NMJ via nicotinic receptors.
  • muscle fasciculations at onset
  • phase 1 block = with single dose
  • phase 2 block = convert back to competitive block with repeated doses.
  • duration: 5-10 mins, short onset.
  • elimination: plasma pseudocholinesterase
  • use: endotracheal intubation.
  • side effects: activates nicotinic receptors in parasympathetic ganglion (↓ HR, ↓ BP)
  • enhanced by ACHEI and ↑ extracellular K+
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46
Q

Halothane

A
  • inhaled anesthetic
  • additive with competitive NMJ blockers
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47
Q

Diethyl Esterase

A
  • inhaled anesthetic
  • additive with competitive NMJ blockers
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48
Q

Isoflurane

A
  • inhaled anesthetic
  • additive with competitive NMJ blockers
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49
Q

Streptomycin

A
  • aminoglycoside antibiotic
  • synergistic with competitive blockers
  • blocks Ca reuptake presynaptically at NMJ.
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50
Q

Gentamycin

A
  • aminoglycoside antibiotic
  • synergistic with competitive blockers
    blocks Ca reuptake presynaptically at NMJ.
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51
Q

Tetracycline Antibiotics

A
  • synergistic with competitive blockers by chelating calcium
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52
Q

Mephenesin

A
  • centrally acting
  • depresses polysnaptic reflexes.
  • use: minor spasticity
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53
Q

Meprobamate

A
  • centrally acting
  • depresses polysnaptic reflexes.
  • use: minor spasticity
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54
Q

Carisoprodol

A
  • centrally acting
  • depresses polysnaptic reflexes.
  • use: minor spasticity
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55
Q

Diazepam

A
  • centrally acting benzodiazepine, halogen group
  • rapid acting, lipid soluble.
  • metabolite = **desmethyldiazepam **⇒ oxazepam ⇒ liver ⇒ urinary excretion
  • enhances GABA-A ⇒ ↑ inward Ca conduction post-synaptically
  • use: **minor spasticity, **relief of anxiety, insomnia, sedation and amnesia before procedures, status epilepticus (drug of choice), muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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56
Q

Baclofen

A
  • centrally acting
  • GABA-B receptor agonist ⇒ ↑ outward K+ conduction presynaptically
  • use: major spasticities (palsies)
  • side effects: renal toxicity
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57
Q

Dantrolene

A
  • direct acting
  • inhibits calcium release from sarcoplasmic reticulum
  • use: spastic condictions
  • side effects: hepatotoxicity
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58
Q

Chlordiazepoxide

A
  • benzodiazepine, halogen group
  • slow acting
  • metabolite = desmethylchlordiazepoxide ⇒ demoxepam ⇒ desmethyldiazepam ⇒ oxazepam ⇒ liver ⇒ urinary excretion
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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59
Q

Flurazepam

A
  • benzodiazepine, halogen group
  • rapid acting
  • metabolies:
    • **hydroxyethylflurazepam **⇒ liver ⇒ urinary excretion
    • **desalkylflurazepam **⇒ liver ⇒ urinary excretion
  • is a hypnotic (sedation)
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
  • side effects: daytime sedation
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60
Q

Desmethyldiazepam

A
  • benzodiazepine, halogen group
  • aka Nordiazepam
  • t1/2 > 40hrs
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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61
Q

Oxazepam

A
  • benzodiazepine, halogen group
  • slow acting, slow absorption
  • ⇒ liver ⇒ urinary excretion
  • no metabolites.
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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62
Q

Lorazepam

A
  • benzodiazepine, halogen group
  • ⇒ liver ⇒ urinary excretion
  • no active metabolites.
  • longer period of protection for status epilepticus than diazepam
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states (status epilepticus), muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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63
Q

Nitrazepam

A
  • benzodiazepine, halogen group
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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64
Q

Triazolam

A
  • benzodiazepine with triazole group
  • extremely rapid acting, short duration
  • metabolite: alpha-hydroxy metabolites ⇒ liver ⇒ urinary excretion
  • t1/2 = 3-5 hrs.
  • is a hypnotic (sedation)
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
  • side effects: rebound anxiety, next day amnesia, confusion.
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65
Q

Alprazolam

A
  • benzodiazepine with triazole group
  • rapid acting, rapid oral absorption
  • metabolite: alpha-hydroxy metabolites ⇒ liver ⇒ urinary excretion
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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66
Q

Clorazepate

A
  • inactive benzodiazepine. prodrug. hydrolyzed in stomach.
  • rapid acting. longest t1/2
  • metabolite = desmethyldiazepam ⇒ oxazepam ⇒ liver⇒ urinary excretion.
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, adjuvant for SPS and CPS, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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67
Q

Prazepam

A
  • benzodiazepine.
  • metabolite = desmethyldiazepam ⇒ oxazepam ⇒ liver ⇒ urinary excretion
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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68
Q

Temazepam

A
  • benzodiazepine.
  • ⇒ liver ⇒ urinary excretion
  • t1/2 is long
  • is a hypnotic (have sedation)
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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69
Q

Estazolam

A
  • benzodazepine
  • ⇒ liver ⇒ urinary excretion
  • t1/2 is long
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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70
Q

Quazepam

A
  • benzodiazepine
  • metabolite: desalkylflurazepam ⇒ liver ⇒ urinary excretion
  • t1/2 >75 hours
  • is a hypnotic
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
  • side effect: daytime sedation
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71
Q

Clonazepam

A
  • benzodiazepine
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, absence/myoclonic/akinetic seizures, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
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72
Q

Zolpidem

A
  • aka Ambien.
  • selective benzodiazepine receptor agonist.
  • t1/2 = 1.5-3.5 hours.
  • no active metabolites.
  • bind to BDZ1 receptors.
  • shorten sleep latency and ↑ total sleep
  • tolerance is rare.
  • use: hypnotics, prevent jet lag.
  • side effects: rebound insomnia when stopping, some sleepwalking.
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73
Q

Benzodiazepines (General Info)

A
  • works on BDZ1 and BDZ2 receptors.
  • enhances GABA when GABA is present.
  • needs GABA present to open chloride channel.
  • dangerous to give with barbitates or alcohol.
  • use: relief of anxiety, insomnia, sedation and amnesia before procedures, epilepsy and seizure states, muscle relaxation in neuromuscular disorders, ethanol/sedative-hypnotic withdrawal.
  • side effects: can be hypnotic (sedation), can have rebound anxiety, can have anterograde amnesia, confusion.
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74
Q

Barbiturates

A
  • work on the GABA-Benzo-Chloride receptor complex.
  • at high concentrations doesn’t need GABA to open chloride channel.
  • don’t give with benzodiazepines or alcohol.
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75
Q

Zaleplon

A
  • aka Sonata
  • selective benzodiazepine receptor agonist.
  • t1/2 = 1-2 hours.
  • metabolized via aldehyde dehydrogenase.
  • binds BDZ1 receptors.
  • shortens sleep latency and ↑ total sleep
  • tolerance is rare.
  • use: hypnotic (sedation), prevent jet lag
  • side effects: rebound insomnia when stoping.
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76
Q

Eszopiclone

A
  • aka Lunesta
  • selective benzodiazepine receptor agonist
  • t1/2 = 6 hours
  • minor active metabolites.
  • binds BDZ1 receptor
  • shortens sleep latency and ↑ total sleep
  • tolerance is rare.
  • use: hynotics (sedation), prevent jet lag.
  • side effects: rebound insomnia when stopping.
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77
Q

Flumazenil

A
  • nonspecific BDZ1/BDZ2 receptor antagonist.
  • blocks inverse agonist effects of beta carbolines.
  • given IV
  • t1/2 = 20 min
  • use: reverse benzo effects in anesthesia, benzo overdose.
  • side effects: rebound excitation and seizures.
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78
Q

Modafinil

A
  • aka Cephalon aka Provigil
  • wakefulness-promoting agent.
  • given orally
  • may ↑ NE or 5-HT in brain.
  • use: narcolepsy
79
Q

Pentobarbital

A
  • barbiturate
  • potentiate GABA at GABA-benzo-chloride channel.
  • short acting
  • metabolized in liver
  • induces CYTP450 metabolism of lipid-soluble drugs (oral BC, carbamazepine, phenytoin, warfarin)
  • chronic use ⇒ tolerance.
  • cross-tolerance btw benzo, barbiturates, ethanol.
  • use: NOT USED PORPHYRIAS
  • side effects: marked sedation, tolerance, respiratory depression
  • withdrawal: anxiety, agitation, life-threatening seizures
    • tx: supportive care, long acting benzo
80
Q

Secobarbital

A
  • barbiturate
  • potentiate GABA at GABA-benzo-chloride channel.
  • short acting
  • metabolized in liver
  • induces CYTP450 metabolism of lipid-soluble drugs (oral BC, carbamazepine, phenytoin, warfarin)
  • chronic use ⇒ tolerance.
  • cross-tolerance btw benzo, barbiturates, ethanol.
  • use: NOT USED PORPHYRIAS
  • side effects: marked sedation, tolerance, respiratory depression
  • withdrawal: anxiety, agitation, life-threatening seizures
    • tx: supportive care, long acting benzo
81
Q

Phenobarbital

A
  • barbiturate
  • potentiate GABA at GABA-benzo-chloride channel.
  • short acting
  • metabolized in liver
  • induces CYTP450 metabolism of lipid-soluble drugs (oral BC, carbamazepine, phenytoin, warfarin)
  • chronic use ⇒ tolerance.
  • cross-tolerance btw benzo, barbiturates, ethanol.
  • use: seizures
    • NOT USED IN PORPHYRIAS
  • side effects: marked sedation, tolerance, respiratory depression
  • withdrawal: anxiety, agitation, life-threatening seizures
    • tx: supportive care, long acting benzo
82
Q

Glutethimide

A
  • non-barbiturate mimic
83
Q

Meprobamate

A
  • non-barbiturate mimic
84
Q

Chloral Hydrate

A
  • non-barbiturate mimic
85
Q

Thiopental

A
  • barbiturate
  • potentiate GABA at GABA-benzo-chloride channel.
  • short acting
  • metabolized in liver
  • induces CYTP450 metabolism of lipid-soluble drugs (oral BC, carbamazepine, phenytoin, warfarin)
  • chronic use ⇒ tolerance.
  • cross-tolerance btw benzo, barbiturates, ethanol.
  • causes redistribution
  • use: induction of amnesia
    • NOT USED PORPHYRIAS
  • side effects: marked sedation, tolerance, respiratory depression
  • withdrawal: anxiety, agitation, life-threatening seizures
    • tx: supportive care, long acting benzo
86
Q

Remelteon

A
  • MT1 and MT2 receptor agonist for melatonin.
  • ⇒ ↓ sleep latency. no rebound insomnia
87
Q

Chlorpromazine

A
  • low potency typical antipsychotic.
  • blocks D2 at therapeutic doses.
  • also blocks M1, H1, and alpha-1.
  • takes a few weeks to take effect
  • helps with positive symptoms.
  • use: schizophrenia
  • side effects: block M1 ⇒ increased body temperature, cognitive impairment, constipation, urinary retention, closed-angle glaucoma, decreased seizure threshold, and cardiotoxicity (QT prolongation)
    • block H1 ⇒ weight gain and sedation, ↑ risk type 2 diabetes.
    • block alpha-1 ⇒orthostatic hypotension
    • block D2 ⇒ ↑ prolactin ⇒ galactorrhea, amenorrhea, infertility
    • tardive dyskinesia, parkinsonism.
88
Q

Thioridazine

A
  • low potency typical antipsychotic
  • blocks D2, M1, H1, and alpha-1.
  • takes a few weeks to take effect
  • helps with positive symptoms.
  • use: schizophrenia
  • _side effect_s: block M1 ⇒ ↑ body temp, cognitive impairment, constipation, urinary retention, closed-angle glaucoma, ↓ seizure threshold, cardiotoxicity (QT prolongation is really bad).
    • blocks H1 ⇒ weight gain, sedation, ↑ risk type 2 diabetes.
    • block alpha-1 ⇒ orthostatic hypontension.
    • block D2 ⇒ ↑ prolactin ⇒ galactorrhea, amenorrhea, infertility.
    • tardive dyskinesia, parkinsonism, irreversible retinal pigmentation.
    • can cause fatal arrhythmias with overdose or with TCAs.
89
Q

Fluphenazine

A
  • high potency typical antipsychotic.
  • blocks D2
  • use low doses, milder sedation
  • use: schizophrenia
  • side effects: tardive dyskinesia, akathisia, parkonsonism, acute dystonia, hyperprolactinemia.
90
Q

Thiothixene

A
  • high potency typical antipsychotic.
  • blocks D2
  • lower dosing, milder sedation.
  • use: schizophrenia
  • side effects: tardive dyskinesia, parkinsonism, akathisia, acute dystonia, hyperprolactinemia.
91
Q

Paliperidone

A
  • high potency atypical antipsychotic
  • blocks 40-60% D2, and 70-90% 5-HT2A.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good wtih positive symptoms, some help on negative.
  • use: schizophrenia, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: weight gain and sedation
92
Q

Clozapine

A
  • low potency atypical antipsychotic
  • blocks 40-60% D2, and 70-90% 5-HT2A.
    • blocks D2, D3, D4, 5-HT2, 5-HT3, 5-HT4.
  • acute = tranquilizer
  • chronic = antipsychotic takes a few wks.
  • good for positive symptoms, a little for negative.
  • use: refractory schizophrenia
  • side effects: 1% risk agranulocytosis, drooling, ↓ risk suicide, sedation, 2-5% risk of seizures from ↓ seizure threshold.
93
Q

Olanzapine

A
  • high potency atypical antipsychotic.
  • blocks 40-60% D2, and 70-90% 5-HT2A.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • use: schizophrenia, mood stabilizer, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: ↑ liver enzymes, drooling, sedation.
94
Q

Quetiapine

A
  • low potency atypical antipsychotic
  • blocks 40-60% D2, and 70-90% 5-HT2A.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • use: schizophrenia, psychosis with Parkinson’s disease, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: sedation, cataract and thyroid problems.
95
Q

Ziprasidone

A
  • medium potency atypical antipsychotic
  • blocks 40-60% D2, and 70-90% 5-HT2A.
    • some 5-HT1A agonist activity = antidepressant.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • use: schizophrenia, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: sedation, QT prolongation.
96
Q

Aripiprazole

A
  • high potency atypical antipsychotic.
  • blocks 40-60% D2, and 70-90% 5-HT2A.
  • acute = tranquilizer
  • chronic = antipsychotic after a few wks.
  • good for positive symptoms, a little for negative.
  • no weight gain! but less effective.
  • use: schizophrenia, depression, psychosis with manic-depressive/schizoaffective disorders or depression.
  • side effects: sedation, akathisia.
97
Q

Phencyclidine

A
  • noncompetitive NMDA receptor antagonist.
  • can induce psychotic state similar to schizophrenia.
98
Q

Reserpine

A
  • depletes DA in striatum.
  • use: Hungtington’s chorea
99
Q

Terabenazine

A
  • depletes DA in striatum.
  • use: Huntington’s chorea.
100
Q

Prochlorperazine

A
  • weak D2 blockade.
  • use: nausea and vomiting from chemotherapy
101
Q

Nitrazepam

A
  • use: infantile spasms
102
Q

Carbamazepine

A
  • prolongs inactivated Na channel.
  • induces CYP450 liver enzymes and has autoinduction of metabolism.
  • drug of choice for pt with depression and epilepsy.
  • use: partial seizures, complex partial seizures, tonic-clonic seizures, trigeminal neuralgia, depression, acute manic episodes and prophylaxis.
  • side effects: CNS depression, dilutional hyponatremia (intensifies ADH effects), Steven Johnson’s Syndrome (dermatitis), spina bifida (teratogenic), aplastic anemia, agranulocytosis, sedation, osteomalacia
103
Q

Phenytoin

A
  • prolongs inactivated Na channel.
  • metabolized in liver: para-hydroxylation of phenyl groups.
    • induce metabolism: phenobarbital, carbamazepine
    • cause ↑ levels: chloramphenicol, dicumarol, cimetidine, sulfonamides, isoniazid
  • narrow therapeutic window.
  • painful when given IV.
  • use: status epilepticus, simple partial seizures, complex partial seizures, tonic-clonic seizures.
  • toxicity: diplopia, ataxia, gingival hyperplasia, hirsutism, coarsening of facial features.
104
Q

Topiramate

A
  • prolongs inactivation of Na channel.
  • use: simple partial seizures, complex partial seizures, tonic-clonic seizures.
105
Q

Lamotrigine

A
  • prolongs inactivation of Na channel.
  • use: simple partial seizures, complex partial seizures, tonic-clonic seizures, acute manic episodes and prophylaxis.
106
Q

Valproate

A
  • aka sodium valproate, valproic acid, Depakote
  • prolongs inactivation of Na channel.
  • inhibits GABA-T and succinic semi-aldehyde dehydrogenase.
  • closes T type Ca channels
  • levels reduced by carbamazepine
  • use: absence seizures, partial seizures, clonic-tonic seizures, migraine prophylaxis, manic phase of bipolar disorder.
  • side effects: nausea, dizziness, sedation, vomiting, hepatotoxicity
107
Q

Zonisamide

A
  • prolongs inactivation of Na channel.
  • use: simple partial seizures, complex partial seizures.
108
Q

Ethosuximide

A
  • closes T type Ca channels
  • serum levels may be ↑ by valproic acid.
  • use: absence seizures (drug of choice)
  • side effects: dizziness, GI distress, drowsiness, nausea.
109
Q

Tiagabine

A
  • inhibits GAT-1, a GABA transporter.
  • use: simple partial seizures, complex partial seizures.
110
Q

Vigabratrin

A
  • inhibits GABA-T, a GABA transaminase ⇒ ↑ GABA.
111
Q

Oxcarbazepine

A
  • similar to carbamazepine but with a ketol group
  • reduced to an alcohol then a diol = fewer side effects than carbamazepine.
  • use: seizures.
  • side effects: CNS depression, megaloblastic and aplastic anemia, osteomalacia, Steven Johnson’s Syndrome, dilutional hyponatremia, teratogenic.
112
Q

Clorazepate

A
  • does NOT block Na channel.
  • use: simple partial seizures, complex partial seizures, anxiety disorders.
113
Q

Gabapentin

A
  • aka Neurontin
  • GABA mimetic, attempt to make GABA lipophilic.
  • does NOT bind GABA A receptor.
  • releases GABA from GABA-ergic neurons, indirect acting.
  • additive with other CNS depressants.
  • renal clearance, ↓ dose with renal impairment.
  • use: all partial seizures, chronic pain, migraine prophylaxis.
  • side effects: ataxia, dizziness, tremor, drowsiness, nystagmus.
114
Q

Pregabalin

A
  • similar to gabapentin
115
Q

Trimethadione

A
  • blocks T type Ca channels.
  • was previously used for absence seizures.
116
Q

Methsuximide

A
  • similar to ethosuximide but patients tolerate it better
117
Q

Phensuximide

A
  • similar to ethosuximide but patients tolerate it better.
118
Q

Phosphenytoin

A
  • phosphate derivative of phenytoin
  • soluble in water.
  • acts as both acute and loading dose for status epilepticus
  • use: status epilepticus
119
Q

Felbamate

A
  • blocks Na channels, enhances GABA, inhibits NMDA receptors
  • use: drug of last resort for epilepsy
  • side effects: hepatotoxicity, aplastic anemia, Steven Johnson’s Syndrome.
120
Q

Phenol

A
  • lipophilic solvent
  • affects ability to compartmentalize K+ and Na+ ⇒ nonpermanent neurolytic effect.
  • blocks Na channel by presence in membrane
  • use: erupting teeth
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death by respiratory failure.
121
Q

Lidocaine

A
  • amide local anesthetic.
  • weak base: pKa = 7.8
  • metabolized by microsomal hydrolases
  • blocks Na channels from inner aspect of membrane.
  • needs to be lipophilic to get into axoplasm
  • needs to be cationic to get to Na channel.
  • toxicity: CNS = depression of inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death by respiratory failure
122
Q

Procaine

A
  • ester local anesthetic
  • weak base, pKa 8.4
  • metabolized by plasma pseudocholinesterase
  • blocks Na channel from inner aspect of membrane.
  • needs to be lipophilic to get to axoplasm.
  • needs to be cationic to get to Na channel.
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death from respiratory failure
123
Q

Benzocaine

A
  • local anesthetic
  • very lipophilic, get into nerve membrane and block Na channel by its presence in the membrane.
  • use: sunburn creams
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death from respiratory failure.
124
Q

Benzyl Alcohol

A
  • local anesthetic
  • very lipophilic, blocks Na channel by presence in membrane.
  • use: eruping teeth.
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death by respiratory failure.
125
Q

Ethyl Alcohol

A
  • not really used
  • blocks Na channel by presence in membrane
  • toxicity**: **CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death by respiratory failure.
126
Q

Using Vasoconstrictor with Local Anesthetic

A
  • because local anesthetics block Na channels ⇒ vasodilation
  • ⇒ ↓ diffusion of drug from injection site ⇒ ↑ intensity and duration, prevents toxicity from too rapidly absorbing it.
  • usually use Epi
  • toxicity: cardiotoxicity, tissue necrosis at injection site
127
Q

Chloroprocaine

A
  • ester local anesthetic
  • metabolized by plasma pseudocholinesterase.
  • blocks Na channel from axoplasm.
  • toxicity: CNS = depression of inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death from respiratory failure
128
Q

Tetracaine

A
  • ester local anesthetic
  • metabolized by plasma pseudocholinesterase.
  • blocks Na channel from inside axoplasm.
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction
  • death from respiratory failure
129
Q

Bupivacaine

A
  • amide local anesthetic
  • metabolized by microsomal hydrolase
  • blocks Na channels from inside axoplasm
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • very little separation btw CNS and cardio side effects.
  • death by respiratory failure.
130
Q

Mepivacaine

A
  • amide local anesthetic.
  • metabolized by microsomal hydrolase
  • blocks Na channel from within axoplasm.
  • toxicity: CNS = depress inhibitory neurons ⇒ restlessness, tremor, convulsions.
    • cardio = vasodilation, hypotension, ↓ excitability of cardiac muscle, ↓ conduction velocity, ↓ force of contraction.
  • death by respiratory failure
131
Q

Spinal (Intrathecal) Anesthesia

A
  • long duration of action for these drugs.
  • ⇒ loss of rectal and bladder function, paralysis of lower extremities.
  • side effects:
    • hypotension from vasodilation.
      • prophylaxis = ephedrine (vasoconstrictor) or wrap the extremities, or adjust osmolarity of the solution.
    • post-dural puncture headache.
132
Q

Epidural Anesthesia

A
  • drug into tissues surrounding the dura.
  • could do segmental block.
  • may spare rectal and bladder function and paralsyis of lower extremities.
  • long delay of onset
  • large amounts must be used, could accidentally inject intrathecally.
133
Q

Bupropion

A
  • atypical antidepressant
  • selective NE reuptake inhibitor, a little DA reuptake inhibition.
  • activating agent, can cause hyperactivity.
  • no sexual side effects!
  • use: smoking cessation, depression
  • side effects: **psychosis and seizures in ppl with eating disorders, **GI discomfort, insomnia, tremor, acute anxiety.
134
Q

Desipramine

A
  • secondary amine TCA.
  • NE transporter inhibitor.
  • metabolite of imipramine.
  • alpha-2 autoreceptor desensitization with chronic use.
  • use: ADHD, cocaine withdrawal, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • side effects: ↑ body temp, cognitive impairment, constipation, urinary retention, closed-angle glaucoma, ↓ seizure threshold, cardiotoxicity, weight gain, sedation, orthostatic hypotension.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
135
Q

Mirtazapine

A
  • atypical antidepressant.
  • blocks alpha-2 and 5-HT2A.
  • no sexual side effects.
  • well tolerated by elderly.
  • does not ↑ seizure risk, safe from overdose
  • use: depression
  • side effect: 0.3% chance agranulocytosis, sedation, weight gain.
136
Q

Trazodone

A
  • antidepressant
  • blocks 5-HT2A.
  • H1 blockade.
  • block alpha-1 ⇒ reduce nightmares in PTSD.
  • active metabolite = m-chlorophenylpiperazine.
  • use: depression, sleep aide.
  • side effect: sedation, priapism
137
Q

Nefazodone

A
  • antidepressant
  • blocks 5-HT2A.
  • active metabolie = m-cholorphenylpiperazine
  • use: depression
  • side effect: sedation, hepatotoxicity.
138
Q

Amitriptyline

A
  • tertiary amine TCA.
  • metabolite = nortriptyline
  • blocks NE and 5-HT
  • use: depression, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • side effects: dry mouth, blurred vision, ↑ body temp, cognitive impairment, constipation, urinary retention, ↓ seizure threshold, cardiotoxicity, weight gain, orthostatic hypotension, sedation.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
139
Q

Nortriptyline

A
  • secondary amine TCA.
  • metabolite of amitriptyline.
  • narrow therapeutic window.
  • less side effects than amitriptyline.
  • use: depression, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
140
Q

Clomipramine

A
  • tertiary amine TCA.
  • selective 5-HT reuptake inhibitor.
  • use: OCD, depression, chronic neuropathic pain syndromes, fibromyalgia, stress incontinence.
  • side effects: dry mouth, blurred vision, ↑ body temp, cognitive impairment, constipation, urinary retention, ↓ seizure threshold, cardiotoxicity, weight gain, orthostatic hypotension, sedation.
  • overdose: agitation, delirium, seizure, coma, fatal cardiac arrhythmias
141
Q

Fluoxetine

A
  • SSRI, longest t1/2 = 72 hrs.
  • selective 5-HT reuptake inhibitor.
  • can inhibit metabolism of other drugs via CYP450.
  • minimal sedation, weight gain, autonomic effects.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, perimenopausal symptoms, pre-menstrual dysphoric disorder.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
142
Q

Fluvoxamine

A
  • SSRI, shortest t1/2 = 17 hrs.
  • selective 5-HT reuptake inhibitor.
  • worst drug interactions (inhibit metabolism of other drugs via CYP450)
  • minimal sedation, weight gain, or autonomic effects.
  • use: depression (1st line), OCD, GAD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
143
Q

Paroxetine

A
  • SSRI, 2nd shortest t1/2.
  • selective 5-HT reuptake inhibitor.
  • can inhibit metabolism of other drugs by CYP450.
  • most sedating SSRI, causes weight gain.
  • slightly anticholinergic.
  • activating agent, can cause hyperactivity.
  • can cause extrapyramidal symptoms in schizophrenic pts.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety, anisocoria
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
144
Q

Sertraline

A
  • SSRI.
  • selective 5-HT reuptake inhibitor.
  • minimal sedation, weight gain, or autonomic effects.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
145
Q

Citalopram

A
  • SSRI.
  • selective 5-HT reuptake inhibitor.
  • minimal sedation or autonomic effects.
  • NO WEIGHT GAIN, NO DRUG INTERACTIONS
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
146
Q

Escitalopram

A
  • best tolerated SSRI
  • isomer of citalopram
  • selective 5-HT reuptake inhibitor.
  • minimal sedation, minimal weight gain, minimal autonomic effects.
  • 2nd longest half life.
  • use: depression (1st line), GAD, OCD, phobias, bulimia, pre-menstrual dysphoric disorder, perimenopausal symptoms
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • discontinuation syndrome if stop suddenly = jittery, anxious, restless.
  • little chance of overdose.
147
Q

Venlafaxine

A
  • SNRI, short t1/2.
  • blocks NE and 5-HT reuptake.
  • use: depression, chronic pain disorders.
  • side effects: 6-13% develop HTN, GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
  • can get 5-HT discontinuation syndrome.
148
Q

Desvenlafaxine

A
  • SNRI.
  • blocks NE and 5-HT reuptake.
  • use: depression, chronic pain disorders.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
149
Q

Duloxetine

A
  • SNRI.
  • blocks NE and 5-HT reuptake.
  • activating agent.
  • use: depression and chronic pain disorders.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
150
Q

Milnacipran

A
  • SNRI.
  • blocks reuptake of NE and 5-HT.
  • use: depression, chronic pain syndromes.
  • side effects: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
151
Q

Phenelzine

A
  • MAOI
    • irreversibley inhibits MAO-A and MAO-B.
  • use: depression when can’t use other drugs from toxicity.
  • side effects: weight gain, postural hypertension, sexual dysfunction, altered sleep.
  • hypertensive crisis: if taking with foods containing tyramine or OTC decongestants (phenylephrine or pseudoephedrine).
  • serotonin syndrome = rigidity, hyperthermia, altered mental status, cardiovascular collapse.
    • if taking with SSRIs, meperidine, or dextromethorphan.
  • overdose: CNS intoxication (agitation, delirium, seizures, coma). can be fatal.
152
Q

Isocarboxazid

A
  • MAOI
    • irreversibly inhibits MAO-A and MAO-B.
  • use: depression when can’t take other drugs from toxicity.
  • side effects: weight gain, postural hypertension, sexual dysfunction, altered sleep.
  • hypertensive crisis: if take with foods containing tyramine or OTC decongestants (phenylephrine or pseudoephedrine)
  • serotonin syndrome = rigidity, hyperthermia, altered mental status, cardiovascular collapse.
    • if taking SSRIs, meperidine, or dextromethorphan.
  • overdose: CNS intoxication (agitation, delirium, seizures, coma). can be fatal.
153
Q

Tranylcypromine

A
  • MAOI
    • irreversibly inhibit MAO-A and MAO-B.
  • use: depression when can’t use other drugs from toxicity.
  • side effects: weight gain, postural hypertension, sexual dysfunction, altered sleep.
  • hypertensive crisis: if taken with foods with tyramine or OTC decongestants (phenylephrine, pseudoephedrine).
  • serotonin syndrome = rigidity, hyperthermia, altered mental status, cardiovascular collapse)
    • if taken with SSRIs, meperidine, or dextromethorphan.
  • overdose: CNS intoxication (agitation, delirium, seizures, coma). can be fatal.
154
Q

Tyramine

A
  • indirect sympathomimetic that provokes non-exocytotic release of NE.
155
Q

Atomoxetine

A
  • modern NE selective reuptake inhibitor.
  • use: ADHD.
  • side effects: some ↑ BP.
  • avoid in patients with cardiac abnormalities.
156
Q

Sibutramine

A
  • NE and 5-HT reuptake inhibitor.
  • use: weight loss.
  • side effects: ↑ CV risk.
  • removed from market.
157
Q

Lithium Carbonate

A
  • monovalent cation similar to Na.
  • impairs inositol recycling by inhibiting phosphatases
  • give orally, absorbed in 6-8 hrs.
  • plasma serum peaks in 30min to 2 hrs, t1/2 = 20 hrs..
  • excreted in urine, can be reabsorbed.
  • decrease dose if on thiazide or loop diuretic.
  • narrow therapeutic index (0.6-1.4).
  • use: bipolar disorder.
  • side effects: excessive thirst, polyuria, memory problems, tremor, weight gain, drowsiness, diarrhea.
  • toxicity: nausea, vomiting, diarrhea, ataxia, confusion, coma, convulsions, death. irreversible brain damage.
  • usually combine with atypical antipsychotic.
158
Q

Lurasidone

A
  • atypical antipsychotic.
  • blocks 5-HT2A, weakly blocks D2.
  • use: depression in bipolar disorder, schizophrenia.
  • few antimuscarinic or H1 effects, little weight gain.
159
Q

Morphine

A
  • opioid analgesic.
  • strong agonist of mu opioid receptors.
  • low bioavailability orally (25%). so give SC, IM, or IV.
    • rapid analgesia, duration = 4-5 hrs.
    • metabolized in liver to C3 or C6 glucuronic acid.
      • C6 is still analgesic and can accumulate with chronic use and slow clearance.
    • excreted in urine.
  • low lipophilicity so need high plasma concentration to cross BBB.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: IM or IV for mod to severe pain, orally for chronic therapy, MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: respiratory depression
160
Q

Methadone

A
  • synthetic opioid analgesic.
  • strong agonist of mu opioid receptors.
  • good oral bioavailability (slow hepatic metabolism)
  • easily penetrates BBB, duration = 4-6 hrs.
  • accumulates in tissues with chronic dosing from high protein binding.
  • can prevent drug craving or withdrawal.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: mod to severe pain, chronic maintenance of opioid addicts, MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: respiratory depression
161
Q

Meperidine

A
  • synthetic opioid analgesic.
  • strong agonist of mu opioid receptors.
  • extensive 1st pass metabolism
  • more lipophilic so crosses BBB, duration = 2-4 hrs.
  • ester hydrolysis ⇒ meperidinic acid (inactive and eliminated).
  • slower demethylation ⇒ normeperidine = toxic ⇒ delirium, seizures.
    • higher in pts with renal insufficiency or dehydration.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: mod to severe pain, childbirth, MI, acute dyspnea from heart failure, analgesia, anesthesia, post anesthesia shivering
  • side effects: respiratory depression
162
Q

Fentanyl

A
  • most potent opioid analgesic (100x morphine)
  • strong agonist of mu opioid receptors.
  • highly lipophilic, very fast across BBB.
  • IV lasts 15-30 min, SC or IM lasts 1-1.5 hrs, transdermal lasts 72 hrs.
  • ↑ risk overdose.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: mod to severe pain. conscious sedation with medazolam, **pain in opioid tolerant pts **(transdermal), MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: respiratory depression
163
Q

Oxycodone

A
  • opioid analgesic.
  • strong agonist of mu opioid receptors.
  • has 3-methoxy substitution.
  • 8x potent as codeine.
  • given low dose in combo with acetaminophen or aspirin.
  • dose limiting respiratory depression.
  • high potential for abuse/dependence.
  • use: mod to severe pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: respiratory depression
  • overdose: opioid toxicity with hepatotoxicity from acetaminophen.
164
Q

Codeine

A
  • opioid analgesic.
  • morphine with 3-methoxy = prodrug.
    • demethylated by CYP2D6 to morphine
  • mild to mod agonist of mu opioid receptors.
  • modest abuse potential.
  • use: mild to mod pain (short term use), MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: nausea, vomiting, histamine release.
  • use in combo with aspirin or acetaminophen.
165
Q

Hydrocodone

A
  • opioid analgesic.
  • mild to mod agonist of mu opioid receptors.
  • use: mild to mod pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
166
Q

Loperamide

A
  • synthetic opioid. related to meperidine.
  • mild to mod agonist of mu opioid receptors.
  • low aqueous solubility.
  • poorly absorbed orally, doesn’t cross BBB well.
  • works best in GI tract with no CNS effects.
  • no abuse potential.
  • use: diarrhea
167
Q

Pentazocine

A
  • opioid analgesic, mixed agonist-antagonist.
  • analgesia from agonist effects on kappa receptors.
  • mu antagonism evokes withdrawal in those addicted to strong opioid agonists.
  • use: mild to mod pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
168
Q

Nalbuphine

A
  • opioid analgesic, mixed agonist-antagonist.
  • analgesia from agonist effects on kappa receptors.
  • mu antagonism causes withdrawal in those addicted to strong opioid agonists.
  • use: mild to mod pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
169
Q

Buprenorphine

A
  • opioid analgesic, mixed agonist-antagonist.
  • antagonist at kappa receptors, partial agonist of mu receptors.
  • mu antagonism causes withdrawal from those addicted to strong opioid agonists.
  • duration = 24 hrs. slow dissociation from mu receptor.
    • may be resistant to naloxone since so slow.
  • IM for acute pain in opioid addicts.
    • sublingual for maintenance therapy
  • transdermal for chronic pain (lasts 7 days).
  • use: mild to mod pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
170
Q

Butorphanol

A
  • opioid analgesic, mixed agonist-antagonist.
  • analgesia from agonist effects on kappa receptors.
  • mu antagonism causes withdrawal in those addicted to strong opioid agonists.
  • use: mild to mod pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
171
Q

Naloxone

A
  • opioid antagonist.
  • antagonist at mu, kappa, and delta opioid receptors.
  • use: opioid overdose
172
Q

Naltrexone

A
  • opioid antagonist.
  • antagonist at mu, kappa, and delta opioid receptors.
  • use: prevent relapse in detoxified opioid addicts or alcoholics.
173
Q

Nalmefene

A
  • opioid antagonist.
  • antagonist at mu, kappa, and delta opioid receptors.
  • use: opioid overdose.
174
Q

Tramadol

A
  • weak mu agonist, inhibits reuptake of NE and 5-HT.
  • analgesia not fully blocked by naloxone.
  • low abuse potential
  • use: mild to mod pain, chronic pain, MI, acute dyspnea from heart failure, analgesia, anesthesia
  • side effects: modest respiratory depression, ↓ seizure threshold
175
Q

Met and Leu Enkephalins

A
  • opioid peptide from proenkephalin A gene.
  • likes mu and delta receptors.
176
Q

Beta-Endorphin

A
  • highest potency endogenous opioid peptide.
  • from POMC gene.
  • likes mu, kappa, and delta receptors.
177
Q

Dynorphin

A
  • opioid peptide from proenkephalin B gene.
  • selective for kappa opioid receptors.
178
Q

CNS Effects of Morphine

A
  • analgesia - better on continuous dull pain
  • euphoria
  • sedation - somnolence, can ⇒ coma
  • respiratory depression - primary cause of death
  • nausea and vomiting
  • miosis - ↑ cholinergic outflow through oculomotor
  • cough suppression - through medullary system
  • neuroendocrine effects - suppress LH and FSH.
    • morphine increases prolactin, GH, and ADH.
  • attenuation of CV reflexes - bradycardia, depress baroreceptor reflex.
  • ↑ tone thoracic muscles.
179
Q

Peripheral Side Effects of Morphine

A
  • constipation
  • histamine release from mast cells.
  • ↑ bladder tone and vesicle sphincter tone ⇒ sense of urinary urgency and difficulty urinating
180
Q

Dextromethorphan

A
  • use: cough suppression.
181
Q

Opioid Overdose

A
  • coma
  • pinpoint pupils
  • depressed respiration
182
Q

Midazolam

A
  • use: conscious sedation, pre-medication for monitored anesthesia
183
Q

Propofol

A
184
Q

Ketamine

A
  • use: dissociative anesthesia
185
Q

Droperidol

A
  • use: neuroleptanalgesia along with fentanyl, antiemetic
186
Q

Metoclopramide

A
  • promotes stomach emptying
187
Q

Halothane

A
  • halogenated inhaled anesthetic
188
Q

Isoflurane

A
189
Q

Nitrous Oxide

A
190
Q

Sevoflurane

A
191
Q

Methoxyflurane

A
192
Q

Dentrolene

A
193
Q

Etomidate

A
194
Q

Dexmedetomidine

A

Pharmacology (6 decks)

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