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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
**Benztropine**
* **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)
26
**Trihexiphenidyl**
* **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**)
27
**Diphenhydramine**
* **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**)
28
**Amantidine**
* **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.
29
**Stalevo**
* combo pill of **entacopone, carbidopa, and L-DOPA.** * _use_: **severe Parkinson's Disease with on-off fluctuations**.
30
**Tacrine**
* **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
31
**Donepezil**
* **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
32
**Rivastigmine**
* **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
33
**Galantamine**
* **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
34
**Memantine**
* **NMDA receptor, negative allosteric modulator** * _use_: **mod to severe Alzheimer's Disease** * small benefit * disease still progresses
35
**d-Tubocurarine**
* **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+**
36
**Metocurine**
* **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+**
37
**Pancuronium**
* **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+**
38
**Vecuronium**
* **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+**
39
**Rocuronium**
* **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+**
40
**Atracurium**
* **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+**
41
**Mivacurium**
* **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+**
42
**Neostigmine**
* **ACHEI** * **⇒ ↑ Ach levels, competitively reverses block.** * **enhances depolarization block.**
43
**Edrophonium**
* **ACHEI** * **⇒ ↑ Ach levels, competitively reverses block.** * **enhances depolarization block.**
44
**Sugammedex**
* **cyclodextrin molecule that encapsulates the blocker** * ⇒ ↓ blocker. * mostly for **steroids**. (-oniums)
45
**Succinylcholine**
* **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+**
46
**Halothane**
* inhaled anesthetic * additive with competitive NMJ blockers
47
**Diethyl Esterase**
* inhaled anesthetic * additive with competitive NMJ blockers
48
**Isoflurane**
* inhaled anesthetic * additive with competitive NMJ blockers
49
**Streptomycin**
* aminoglycoside antibiotic * synergistic with competitive blockers * blocks Ca reuptake presynaptically at NMJ.
50
**Gentamycin**
* aminoglycoside antibiotic * synergistic with competitive blockers blocks Ca reuptake presynaptically at NMJ.
51
**Tetracycline Antibiotics**
* synergistic with competitive blockers by chelating calcium
52
**Mephenesin**
* centrally acting * depresses polysnaptic reflexes. * _use_: **minor spasticity**
53
**Meprobamate**
* centrally acting * depresses polysnaptic reflexes. * _use_: **minor spasticity**
54
**Carisoprodol**
* centrally acting * depresses polysnaptic reflexes. * _use_: **minor spasticity**
55
**Diazepam**
* 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.
56
**Baclofen**
* centrally acting * **GABA-B receptor agonist** ⇒ **↑ outward K+ conduction presynaptically** * _use_: **major spasticities** (palsies) * _side effects_: **renal toxicity**
57
**Dantrolene**
* direct acting * **inhibits calcium release from sarcoplasmic reticulum** * _use_: **spastic condictions** * _side effects_: **hepatotoxicity**
58
**Chlordiazepoxide**
* **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.
59
**Flurazepam**
* **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**
60
**Desmethyldiazepam**
* **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.
61
**Oxazepam**
* **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.
62
**Lorazepam**
* **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.
63
**Nitrazepam**
* **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.
64
**Triazolam**
* **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**.
65
**Alprazolam**
* **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.
66
**Clorazepate**
* 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.
67
**Prazepam**
* **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.
68
**Temazepam**
* **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.
69
**Estazolam**
* **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.
70
**Quazepam**
* **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**
71
**Clonazepam**
* **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.
72
**Zolpidem**
* 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**.
73
**Benzodiazepines (General Info)**
* 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.**
74
**Barbiturates**
* 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.
75
**Zaleplon**
* 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.
76
**Eszopiclone**
* 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.
77
**Flumazenil**
* **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.**
78
**Modafinil**
* aka Cephalon aka Provigil * **wakefulness-promoting agent**. * given orally * may **↑ NE or 5-HT in brain**. * _use_: **narcolepsy**
79
**Pentobarbital**
* **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
**Secobarbital**
* **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
**Phenobarbital**
* **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
**Glutethimide**
* **non-barbiturate mimic**
83
**Meprobamate**
* **non-barbiturate mimic**
84
**Chloral Hydrate**
* **non-barbiturate mimic**
85
**Thiopental**
* **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
**Remelteon**
* **MT1 and MT2 receptor agonist** for melatonin. * ⇒ **↓ sleep latency**. no rebound insomnia
87
**Chlorpromazine**
* **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
**Thioridazine**
* **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
**Fluphenazine**
* **high potency typical antipsychotic**. * blocks **D2** * use low doses, **milder sedation** * _use_: **schizophrenia** * _side effects_: **tardive dyskinesia, akathisia, parkonsonism, acute dystonia, hyperprolactinemia**.
90
**Thiothixene**
* **high potency typical antipsychotic**. * blocks **D2** * lower dosing, **milder sedation**. * _use_: **schizophrenia** * _side effects_: **tardive dyskinesia, parkinsonism, akathisia, acute dystonia, hyperprolactinemia**.
91
**Paliperidone**
* **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
**Clozapine**
* **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
**Olanzapine**
* **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
**Quetiapine**
* **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
**Ziprasidone**
* **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
**Aripiprazole**
* **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
**Phencyclidine**
* **noncompetitive NMDA receptor antagonist**. * can **induce psychotic state** similar to schizophrenia.
98
**Reserpine**
* depletes DA in striatum. * _use_: **Hungtington's chorea**
99
**Terabenazine**
* depletes DA in striatum. * _use_: **Huntington's chorea**.
100
**Prochlorperazine**
* weak D2 blockade. * _use_: **nausea and vomiting from chemotherapy**
101
**Nitrazepam**
* _use_: **infantile spasms**
102
**Carbamazepine**
* 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
**Phenytoin**
* **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
**Topiramate**
* prolongs **inactivation of Na channel**. * _use_: **simple partial seizures, complex partial seizures, tonic-clonic seizures**.
105
**Lamotrigine**
* prolongs **inactivation of Na channel**. * _use_: **simple partial seizures, complex partial seizures, tonic-clonic seizures, acute manic episodes and prophylaxis.**
106
**Valproate**
* 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
**Zonisamide**
* prolongs **inactivation of Na channel**. * _use_: **simple partial seizures, complex partial seizures.**
108
**Ethosuximide**
* **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
**Tiagabine**
* **inhibits GAT-1**, a GABA transporter. * _use_: **simple partial seizures, complex partial seizures**.
110
**Vigabratrin**
* **inhibits GABA-T**, a GABA transaminase ⇒ ↑ GABA.
111
**Oxcarbazepine**
* 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
**Clorazepate**
* does NOT block Na channel. * _use_: simple partial seizures, complex partial seizures, **anxiety disorders**.
113
**Gabapentin**
* 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
**Pregabalin**
* similar to gabapentin
115
**Trimethadione**
* blocks T type Ca channels. * was previously used for absence seizures.
116
**Methsuximide**
* similar to ethosuximide but patients tolerate it better
117
**Phensuximide**
* similar to ethosuximide but patients tolerate it better.
118
**Phosphenytoin**
* **phosphate derivative of phenytoin** * soluble in water. * acts as both acute and loading dose for status epilepticus * _use_: **status epilepticus**
119
**Felbamate**
* **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
**Phenol**
* **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
**Lidocaine**
* **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
**Procaine**
* **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
**Benzocaine**
* **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
**Benzyl Alcohol**
* **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
**Ethyl Alcohol**
* 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
**Using Vasoconstrictor with Local Anesthetic**
* 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
**Chloroprocaine**
* **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
**Tetracaine**
* **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
**Bupivacaine**
* **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
**Mepivacaine**
* **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
**Spinal (Intrathecal) Anesthesia**
* 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
**Epidural Anesthesia**
* 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
**Bupropion**
* **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
**Desipramine**
* **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
**Mirtazapine**
* **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
**Trazodone**
* **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
**Nefazodone**
* **antidepressant** * **blocks 5-HT2A**. * active metabolie = **m-cholorphenylpiperazine** * _use_: **depression** * _side effect_: sedation, **hepatotoxicity**.
138
**Amitriptyline**
* **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
**Nortriptyline**
* **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
**Clomipramine**
* **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
**Fluoxetine**
* **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
**Fluvoxamine**
* **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
**Paroxetine**
* **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
**Sertraline**
* **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
**Citalopram**
* **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
**Escitalopram**
* 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
**Venlafaxine**
* **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
**Desvenlafaxine**
* **SNRI**. * **blocks NE and 5-HT reuptake**. * _use_: **depression, chronic pain disorders**. * _side effects_: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
149
**Duloxetine**
* **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
**Milnacipran**
* **SNRI**. * **blocks reuptake of NE and 5-HT**. * _use_: **depression, chronic pain syndromes**. * _side effects_: GI discomfort, sexual dysfunction, insomnia, tremor, acute anxiety.
151
**Phenelzine**
* **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
**Isocarboxazid**
* **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
**Tranylcypromine**
* **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
**Tyramine**
* indirect sympathomimetic that **provokes non-exocytotic release of NE.**
155
**Atomoxetine**
* modern **NE selective reuptake inhibitor**. * _use_: **ADHD**. * _side effects_: some **↑ BP**. * avoid in patients with cardiac abnormalities.
156
**Sibutramine**
* **NE and 5-HT reuptake inhibitor**. * _use_: **weight loss**. * _side effects_: **↑ CV risk**. * removed from market.
157
**Lithium Carbonate**
* **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
**Lurasidone**
* **atypical antipsychotic**. * blocks **5-HT2A, weakly blocks D2**. * _use_: **depression in bipolar disorder**, schizophrenia. * few antimuscarinic or H1 effects, little weight gain.
159
**Morphine**
* 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
**Methadone**
* 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
**Meperidine**
* 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
**Fentanyl**
* 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
**Oxycodone**
* 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
**Codeine**
* 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
**Hydrocodone**
* opioid analgesic. * **mild to mod agonist of mu opioid receptors**. * _use_: **mild to mod pain, MI, acute dyspnea from heart failure, analgesia, anesthesia**
166
**Loperamide**
* 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
**Pentazocine**
* 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
**Nalbuphine**
* 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
**Buprenorphine**
* 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
**Butorphanol**
* 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
**Naloxone**
* **opioid antagonist**. * antagonist at **mu, kappa, and delta opioid receptors**. * _use_: **opioid overdose**
172
**Naltrexone**
* **opioid antagonist**. * antagonist at **mu, kappa, and delta opioid receptors**. * _use_: **prevent relapse in detoxified opioid addicts or alcoholics**.
173
**Nalmefene**
* **opioid antagonist**. * antagonist at **mu, kappa, and delta opioid receptors**. * _use_: **opioid overdose**.
174
**Tramadol**
* **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**
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**Met and Leu Enkephalins**
* **opioid peptide** from **proenkephalin A gene**. * likes mu and delta receptors.
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**Beta-Endorphin**
* **highest potency endogenous opioid peptide**. * from **POMC gene**. * likes mu, kappa, and delta receptors.
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**Dynorphin**
* **opioid peptide** from **proenkephalin B gene**. * selective for kappa opioid receptors.
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**CNS Effects of Morphine**
* **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**.
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**Peripheral Side Effects of Morphine**
* **constipation** * **histamine release** from mast cells. * ↑ bladder tone and vesicle sphincter tone ⇒ **sense of urinary urgency and difficulty urinating**
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**Dextromethorphan**
* _use_: **cough suppression**.
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**Opioid Overdose**
* **coma** * **pinpoint pupils** * **depressed respiration**
182
**Midazolam**
* use: conscious sedation, pre-medication for monitored anesthesia
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**Propofol**
184
**Ketamine**
* use: dissociative anesthesia
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**Droperidol**
* use: neuroleptanalgesia along with fentanyl, antiemetic
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**Metoclopramide**
* promotes stomach emptying
187
**Halothane**
* halogenated inhaled anesthetic
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**Isoflurane**
189
**Nitrous Oxide**
190
**Sevoflurane**
191
**Methoxyflurane**
192
**Dentrolene**
193
**Etomidate**
194
**Dexmedetomidine**

Pharmacology (6 decks)

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