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Pharmacology Block 2 > General > Flashcards

General Flashcards

1
Q

Phenytoin

A
  • AE
  • Na blocker
  • long term pot hirtuism and osteoporosis
  • marked confusion (cognitive impairment), teratogen
  • cause gingival hyperplasia in 20%
  • hard to regulate
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2
Q

Tiagabine

A
  • AE
  • incr GABA– reuptake inh (prolong chanel open)
  • adjunct in partial seizures
  • short half life
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3
Q

Rufinamide

A
  • AE Na channel blocker

- add on for lenox-gastaut syndrome

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4
Q

Valporic acid

A

(divalporex) broad spectrum AE
- Treats all seizures- FIRST LINE
- teratogen, osteoporosis, weight gain, hair loss, hepatic and pancreatic injury
- cyp inducer
- also treats bipolar

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5
Q

Perampanel

A

AMPA antag AE

-partial seizures and tonic-clonic

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6
Q

Tonic-clonic seizure

A

Initial strong contraction of whole musculature; followed by series of violent jerks that gradually die out (2-4 min).

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7
Q

Which AE’s cause cognitive impairment?

A

Phenobarbital, phenytoin and topiramate

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8
Q

Lamotrigine

A
  • Broad spectrum AE (alt to valproic acid – less SE) prolong inact Na and inh glut
  • FIRST LINE general
  • tonic clonic seizures and lenox-gastaut
  • Rash when dose incr too rapidly
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9
Q

Vigabatrin

A

-AE
Irrev inh GABA-T (GABA aminotransferase)– degr enzyme
-patrial seizures
-RARELY used – vision loss

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10
Q

Ezogabine

A

-AE

enhance K channels (KCNQ family)

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11
Q

Which AEs cause osteoporosis

A

Phenytoin, phenobarbital, carbamazepine, oxcarbazepine and valproic acid.

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12
Q

Ethosuxamide

A
  • AE that decr Ca

- Absent seizures (FIRST LINE)

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13
Q

Felbamate

A
  • AE
  • Broad spectrum– multiple mechs (NMDA antag and enhance GABA)
  • aplastic anemia
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14
Q

Carbamazepine

A
  • AE Na channel blocker
  • modulate sustained high freq firing
  • Autoinduction (incr clearance with incr dose)
  • osteoporosis and teratogen
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15
Q

Which AEs are teratogenic?

A

Valproic acid & carbamazepine; barbiturates & phenytoin. Newer AEDs less teratogenic.

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16
Q

Leviteracetam

A
  • AE that binds to SV2A
  • Broad spectrum (modify release of GABA and glut)
  • not many SEs
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17
Q

Clonazepam

A
  • Long acting BZD— AE
  • incr GABA
  • sedation, memory impair, mood changes, addiction.
  • also used in anxiety and panic
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18
Q

Non-linear drug clearance

A

Either clearance decreases as dose increases or clearance increases with dose increase.
-with AEs

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19
Q

Topirimate

A
  • Broad spectrum AE

- memory impair, renal stones, glaucoma, weight loss

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20
Q

Gabapentin and pregabalin

A
  • AE that binds alpha-2-delta of Ca channel — decr glut
  • unsteadiness, weight gain, fatigue, dizzy
  • also for neuropathic pain, chronic pain, fibromyalgia
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21
Q

What is a seizure?

A

a group of cortical neurons that discharge abnormally

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22
Q

phenobarbital

A

-AE enhance GABA
-weak acid– elim by making urine alkaline
-similar to penytoin (preferred)
cognitive impair, osteoporosis, sedation
-not for absence

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23
Q

List 3 highly selective nonergot derivatives (dopamine agonist)

A
  1. Pramipexole
  2. Ropinirole
  3. Apomorphine
    Fewer side effects and are therefore preferred.
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24
Q

What are the 3 categories of partial seizures?

A

Simple
Complex
Secondarily Generalized

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25
Q

Most AED’s cause some CNS depression, therefore, what other drugs should be avoided?

A

Etoh, antihistamines, other AED’s, opioids.

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26
Q

How effective is Memantine?

A

Only modest benefit

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27
Q

How is preclinical AD diagnosed?

A

Completely on the basis of biomarkers

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28
Q

What is tegretol indicated for?

A

Like phenytoin, partial seizures and tonic-clonic seizures.

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29
Q

What is the first line drug class of choice for mild to moderate PD motor symptoms?

A

Dopamine agonists

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30
Q

What are the principal adverse effects of levodopa?

A

nausea, dyskinesia, hypotension, and psychosis.

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31
Q

If combined with levodopa, what drug will cause a hypertensive crisis?

A

MAOI

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32
Q

Which two AED’s have the highest risk of causing suicidality?

A

Topamax and Lamictal

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33
Q

What is the unique side effect caused by phenytoin in 20% of patients?

A

gingival hyperplasia

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34
Q

How can you minimize the risk to the fetus?

A

Use one drug at the lowest possible dose and avoid Depakote

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35
Q

What is the name of the enzyme that converts levodopa to dopamine?

A

decarboxylase

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36
Q

What is the primary pathology in PD?

A

Degeneration of neurons in the substantia nigra that supply dopamine to the striatum. The result is an imbalance between dopamine and acetylcholine.

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37
Q

Which COMT is safer and therefore preferred?

A

Entacapone

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38
Q

Name the 4 cholinesterase inhibitors that are approved for AD.

A
  1. Donepezil
  2. Galantamine
  3. Rivastigmine
  4. Tacrine
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39
Q

What is the gold standard for treatment of PD motor symptoms?

A

Levodopa + carbidopa

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40
Q

How are the motor symptoms of Parkinson’s Disease treated best?

A

Primarily with dopamine agonists. Anticholinergics can also be used.

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41
Q

Tegretol is often better tolerated than phenytoin, therefore, it is often preferred. True of False?

A

T

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42
Q

Rarely, phenytoin causes SJS or toxic epidermal necolysis (TEN). What may increase the risk?

A

HLA-B1501 gene variation, seen almost exclusively in pts of Asian descent.

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43
Q

What are the categories of generalized seizures?

A 
Tonic-Clonic (Grand Mal)
Absence (Petit Mal)
Atonic 
Myoclonic
Status Epiletpticus
Febrile
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44
Q

What role do NMDA receptors play?

A

learning and memory

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45
Q

How does carbidopa enhance the effects of levodopa in PD?

A

By preventing decarboxylation of levodopa in the intestine and peripheral tissues. (Can’t cross blood-brain barrier, so does not prevent conversion of levodopa to dopamine in the brain.)

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46
Q

What is a COMT drug and how do they work?

A

Catechol O-methyltransferase (COMT) inhibitors inhibit metabolism of levodopa in the periphery resulting in raised dopamine levels in treating PD.

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47
Q

How do you treat AD dementia?

A

Cholinesterase inhibitors or memantine (Namenda).

Benefit in most patients is marginal.

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48
Q

Dopamine agonists do have more serious side effects than levodopa. List some.

A

Hallucinations
Sleepiness
Postural hypotension
*Usually reserved for younger patients who can tolerate better.

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49
Q

What is the major known risk factor in developing AD?

A

Advancing age

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50
Q

What are the 2 major adverse reactions with Depakote?

A
  1. Potentially fatal liver injury (espec children
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51
Q

What is phenytoin indicated for?

A

Partial seizures and tonic-clonic seizures. NOT absence seizures.

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52
Q

What is the new class of drugs for AD?

A

NMDA receptor antagonists. Memantine (Namenda) is the first representative. Benefits are derived from modulating the effects of glutamate at NMDA receptors.

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53
Q

How does levodopa work to relieve motor symptoms in PD?

A

Levodopa relieves motor symptoms by converting to dopamine in surviving nerve terminals in the striatum and restores a proper balance between dopamine and AcH.

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54
Q

Depakote is a very broad spectrum AED. What are it’s indications?

A

ALL seizure types including most generalized seizures - tonic-clonic, absence, atonic, and myoclonic sz’s.

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55
Q

Dopamine agonists fall into two groups. What are they?

A
  1. Ergot derivatives

2. Nonergot derivatives

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56
Q

How long do you treat AD?

A

Indefinitely, or until the SE’s are intolerable or benefits are lost.

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57
Q

How do the MAO-B Inhibitors enhance responses to levodopa?

A

By inhibiting MAO-B, the brain enzyme that inactivates dopamine.

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58
Q

Only 1 cholinesterase inhibitor is approved for treating severe AD. Which one is it?

A

Donepezil

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59
Q

What is gabapentin used for?

A

Partial seizures, restless leg syndrome, phantom limb pain, and neurogenic pain.

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60
Q

What are the 2 MAO-B Inhibitors used with levodopa in treating PD?

A
  1. Selegiline

2. Rasagiline

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61
Q

What are the 2 COMT drugs?

A
  1. Entacapone

2. Tolcapone

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62
Q

What is the histology of Alzheimers (AD)?

A

Characterized by: 1. neuritic plaques 2. neurofibrillary tangles 3. degeneration of cholinergic neurons in the hippocampus and cerebral cortex.

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63
Q

How would you treat status epilepticus?

A

Initially, IV diazepam or lorazepam. Follow with Phenytoin if seizures do not stop. Move onto phenobarbital IV until stops.

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64
Q

When is the oral nonergot dopamine agonist, pramipexole indicated?

A

Alone in early PD for motor symptoms or with levodopa in advanced PD

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65
Q

What are the 3 phases of AD?

A
  1. An asymptomatic preclinical phase
  2. Two symptomatic clinical phases:
    a) . Mild cognitive impairment
    b) Dementia - both due to AD.
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66
Q

What is PD

A

A neurodegenerative disorder that produces characteristic motor symptoms: tremor at rest, rigidity, postural instability, and bradykinesia.

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67
Q

What are neuritic plaques?

A

Spherical, extracellular bodies that consist of a beta-amyloid core surrounded by remnants of axons and dendrites.

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68
Q

PD affects the ____

A

basal ganglia

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69
Q

What is the dopamine content of the substantia niagra in PD patients?

A

less than 10% of normal in PD patient brains postmortem

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70
Q

MPTP

A

is a compound used experimentally to study Parkinson’s disease; it impairs dopaminergic neurons

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71
Q

A molecule aspect of PD involves ______

A

Lewy bodies in various parts of the brain

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72
Q

Alpha synuclein

A

staining used to reveal Lewy bodies

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73
Q

Genetic forms of PD ____ and _______

A

PARK7 and PINK1

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74
Q

Main DE of LDOPA

A

Dyskinesias and a rapid fluctuation in clinical state

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75
Q

Acute side effects of LDOPA

A

Nausea, anorexia, hypotension

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76
Q

Bromocriptine

A

PD

-Primarily dopamine agonist; used most often in cases of hyperprolactinemia

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77
Q

Pergolide & cobergoline

A

PD

-dopamine agonist

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78
Q

Pramipexole and Ropinirole

A

-PD

D2/3 selective dopamine agonists, better tolerated; no fluctuations in efficacy

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79
Q

Rotigotine

A

Newer dopamine agonist, delivered as a transdermal patch

-PD

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80
Q

Apomorphine

A

-PD

Dopamine agonist with a powerful emetic action; must be combined with an antiemetic; LAST RESORT COMPOUND

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81
Q

Seligiline

A

-PD

MAO-B inhibitor (selective), used in combination with levodopa

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82
Q

Tolcapone and entacopone

A

Catechol-O-Methyltransferase inhibitors; used with L-DOPA and never alone

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83
Q

Deep brain stimulation

A

in PD

-electrode is placed into the subthalamic nucleus; used in cases where patients are intolerant to medication

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84
Q

Orphenadrine

A

Muscarinic receptor antagonist used for the parkinsonism caused by antipsychotic drugs

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85
Q

Amantadine

A

May enhance dopamine release

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86
Q

What is HD?

A

An inherited (autosomal dominant) disorder resulting in progressive brain degeneration

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87
Q

Trinucleotide repeat

A

in Huntington’s disease this expansion of the number of repeats of the CAG sequence coding for glutamine is over 50

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88
Q

Which drugs treat the invol movements of HD?

A

Tetrabenazine and chlorpromazine; baclofen

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89
Q

Baclofen

A

GABA agonist in HD

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90
Q

Tetrabenazine

A

-HD

Inhibitor of monoamine transporter 2 (VMAT2); decreases dopamine levels in addition to serotonin and norepi.

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91
Q

Amyloid cascade hypothesis

A

in AD
-Amyloid precursor protein accumulates following processing, aggregating to form plaques that are thought to damage the brain.

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92
Q

An allelic variant of apolipoprotein-E (APOE)-E4

A

Associated with 20 % of sporadic and familial AD; making it the single most important risk factor

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93
Q

Highly selective and reversible AChE inhibitor used in AD

A

Donepezil

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94
Q

Rivastigmine

A

-AD
Inhibits both AChE and butryylcholinesterase. Transdermal patch allows once a day administration and fewer GI side effects.

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95
Q

Galantamine

A

-AD
Reversible and competitive inhibitor of AChE and also an allosteric modulator binding to cholinergic nicotinic receptors.

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96
Q

Memantine

A

Noncompetitive glutamatergic receptor antagonist, blocking/regulating NMDA receptors

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97
Q

Cognitive reserve

A

Maximized by increasing social circle, maintaining a healthy weight, cognitively stimulating activities and strong literary skills

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98
Q

Pathophysio of AD

A

Acetylcholine in the diffuse cortex

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99
Q

Most prominent side effect of tricyclic antidepressants

A

anticholinergic

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100
Q

Tyrosine hydroxylase

A

Rate limiting enzyme in dopamine synthesis

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101
Q

Mertazapine

A

Atypical antidepressant with adverse effects of somnolence, increased appetite, weight gain, constipation and dizziness

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102
Q

Paroxetine

A

SSRI most assoc with constipation

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103
Q

Sertraline

A

SSRI most assoc with diarrhea

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104
Q

Buproprion

A

Atypical antidepressant used to treat depression and smoking cessation

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105
Q

These MAO-I potentially causes the most drug-food interactions

A

MAO-A selective

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106
Q

Serotonin syndrome

A

Due to high levels of serotonin; usually a drug interaction, and consists of hyperthermia, muscle rigidity, and fluctuations in vital signs and mental status

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107
Q

Phenelzine

A

Non-selective MAO inhibitor

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108
Q

Serotonin synthesis

A

Tryptophan, 5-hydroxytryptophan, 5-hydroxytriptamine

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109
Q

Buspirone

A

5-HT1A partial agonist

antidepressant (non BZD)

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110
Q

Venlafaxine, Duloxetine

A

SNRIs

111
Q

Side effects or problems with tricyclic antidepressants

A

Coma, convulsions, confusion in elderly, cardiotoxicity

112
Q

LSD

A

non-selective serotonin agonist

Binds to all serotonin receptors except 5-HT3 and 5-HT4

113
Q

selegiline

A

MAO-B inh

114
Q

Monoamine hypothesis of depression

A

Depression results from a decrease in serotonin and norepinephrine transmission

115
Q

Nortriptyline

A

TCA

116
Q

Modafanil, armodafanil

A

amphetamine

-depression

117
Q

dexmethylphenidate, methylphenidate

A

amphetamine

-depression

118
Q

lisdexamphetamine

A

amphetamine

-depression

119
Q

isocarboxazil, phenelzine

A

nonselective MAOI

-depression

120
Q

tranylcypromine

A

MAOI

depression

121
Q

Amitriptyline

A

TCA

-sedating can use for insomnia

122
Q

clomipramine

A

TCA

123
Q

Desipramine

A

TCA

124
Q

Doxapin

A

TCA

-low dose used for insomnia though H1

125
Q

Imipramine

A

TCA

126
Q

citalopram, escitalopram

A

SSRI

127
Q

fluvoxamine

A

SSRI

128
Q

Milnacipram

A

SNRI

129
Q

Trazodone

A

Atypical antidepressants

-sedating, can use for insomnia

130
Q

Mirtazapine

A

Atypical antidepressant

-sedating, can use for insomnia

131
Q

BDZ and hepatic induction

A

Benzodiazepines do not induce hepatic microsomal enzymes

132
Q

CBT

A

Often used in conjunction with SSRIs for anxiety

133
Q

BZD adverse effects

A

Sedation, tolerance, physical dependence, self-administration

134
Q

Clonazepam uses

A

Panic, anxiety, seizure

135
Q

PTSD first line treatment

A

SSRI, usually paroxetine or sertraline

136
Q

Flumazenil

A

BZD antagonist

137
Q

BZD toxicity

A

Impaired judgement, slurred speech, incoordination, stupor, respiratory depression, death

138
Q

Barbiturates

A

Bind to a distinct subunit combination on the GABA receptor and at high concentrations can open the channel on their own (without GABA).

139
Q

Sedating antidepressants

A

Trazodone, mirtazapine, amyitriptyline

140
Q

Which drugs are typically used for sleep?

A

Eszoiclone, hydroxyzine, zolpidem, zaleplon, ramelteon

141
Q

GABA binding site on GABA R

A

alpha-1 and beta-2 subunits

142
Q

Non-BZD GABA A agonists

A

Eszopiclone, zolpidem, zaleplon

hypnotics

143
Q

Doxepin

A

Tricyclic antidepressant, low dose mechanism for insomnia is histamine H1

144
Q

GABA shunt

A

Refers to alpha ketoglutarate from the Krebs Cycle, converted to glutamic acid by GABA-transaminase; then subsequently to GABA by glutamic acid decarboxylase (GAD). GABA is then metabolized to form succinic semialdehyde to succinic acid and returns to the Krebs Cycle.

145
Q

Alprazolam uses

A

panic, anxiety

short acting

146
Q

Diazepam uses

A

Anxiety, insomnia, pre-op, muscle relaxant, status epilepticus

147
Q

Flurazepam, Temazepam and Triazolam use

A

insomnia

BZDs

148
Q

Nonbenzodiazepine anxiolytic

A

Buspirone mechanism is serotoniergic 5-HT1A receptor partial agonist

149
Q

General anxiety disorder first line treatment

A

SSRI, usually venlafaxine, paroxetine or escitalopram

150
Q

Insomnia disorder

A

Insomnia complaint and significant daytime impairment

151
Q

Glutamine loop

A

Glutamine is formed as GABA is transaminated and converted to glutamine. The glutamine is reconverted to glutamate; then decarboxylated by neuronal GAD to GABA

152
Q

Zolpidem disadvantages

A

(Non BDZ GABA agonist)

4-6 hr effect, therefore not for middle of the night awakenings, associated with parasomnias

153
Q

BZD binding site on GABA A R

A

gamma-2 and alpha-1 subunits.

154
Q

Short acting BZDs

A

Alprazolam, triazolam, lorazepam, oxazepam

155
Q

Lorazepam uses

A

anxiety, alcohol related seizure, status epilepticis

156
Q

BDZ used for sleep

A

Estazolam, flurazepam, quazepam, temazepam, triazolam

157
Q

Long acting BZDs

A

Flurazepam, clorazepate, prazepam

158
Q

Traditional BZD disadvantages

A

Rebound insomnia, memory impairments, loss of coordination, abuse potential, not good for those with respiratory conditions

159
Q

Chlordiazepoxide use

A

alcohol detox

160
Q

Zolpidem advantages

A

Shorten sleep latency, improve duration, can be used as needed, no negative effect on sleep architecture

161
Q

Antipsychotics with CV effects

A

Chlorpromazine, Thioridazine, Ziprazidone, Asenapine

162
Q

Butyrophenones are:

A

Haloperidol, Droperidol

typicals

163
Q

All atypical antipsychotics:

A

D2 receptor antagonists and block 5-HT2

164
Q

Clozapine

A

Azepine atypical antipsychotic

-Associated with 1% risk of agranulocytosis, myocarditis

165
Q

Antipsychotic with the longest half-life:

A

Aripiprazole

166
Q

Classes of typical antipsychotics:

A

Phenothiazines, Thioxanthenes, and Butryophenones

167
Q

Patients taking clozapine must be monitored for

A

Agranulocytosis

168
Q

The phenothiazine class is:

A

typical antipsychotic (block D2)

169
Q

Antipsychotics and the tuberoinfundibular pathway

A

Typical antipsychotics blocking this dopaminergic pathway lead to prolactin secretion

170
Q

Aripiprazole

A

-Atypical antipsychotic, longest half life, in top 25 prescribed drugs
Is especially helpful for negative symptoms; is more activating than sedating

171
Q

Pos schizo symptoms

A

Delusions, hallucinations, thought disorder, aggressive behaviors, stereotyped movements

172
Q

Dopamine released from the hypothalamus blocks ______ via _______

A

prolactin via the tuberoinfundibular pathway

173
Q

Tardive dyskinesia

A

Develops after months or years, seen in 20-40% of patients on typical antipsychotics, often irreversible; consists of involuntary movements often of the face and tongue, trunk and limbs - severely disabling often

174
Q

Sedation with antipsychotics is caused likely by:

A

Histamine H1 receptor involvement

175
Q

Quetiapine

A

-atypical azepine antipsychotic

Known for association with lens changes; requires an eye examination at initiation and at 6-month intervals

176
Q

Mesolimbic tract

A

Ventral tegmentum to limbic area. First generation antipsychotics block D2 receptors, theory that this tract was involved.

177
Q

Serotonin theory of schizophrenia

A

Direct and indirect 5-HT agonists exacerbate the symptoms of schizophrenia

178
Q

Serotonin hyperactivity is assoc with:

A

Positive and negative symptoms of schizophrenia; second generation antispychotics (atypicals) block 5HT2 receptors in addition to D2 receptors

179
Q

Extrapyramidal motor disturbances (EPS):

A

-Antipsychotics
Are reversible, involve involuntary movements, occur in the first few weeks and diminish with time; are less with atypical drugs

180
Q

Glutamate theory of schizo

A

Observations that PCP induces acute psychotic, schizophrenia like symptoms

181
Q

Major SEs of typical antipsychotics

A

Extrapyramidal symptoms (Parkinsonism, dystonias, akathesia; tardive dyskinesia

182
Q

Mech of typical antipsychotics

A

D2 dopamine receptor antagonism

183
Q

Typical anti-psychotics antagonist what to cause their effects?

A

Noradrenergic alpha-1, histamine H1 and muscarinic M1 receptors

184
Q

Atypical antipsychotics got the name due to:

A

No or low extrapyramidal symptoms

185
Q

Olanzapine

A
  • Azepine atypical antipsychotic

- Weight gain

186
Q

Therapeutic effects of antipsychotics req:

A

80% occupancy of dopamine D2 receptors based on imaging studies

187
Q

Weight gain is seen with which types of antipsychotics?

A

Atypicals

188
Q

Risperidone

A

-Atypical antipsychotic

Demonstrates hyperprolactinemia even at low doses

189
Q

Sertindole

A

atypical antipsychotic

190
Q

sulpiride

A

atypical antipsychotic

191
Q

ziprasidone

A

atypical antipsychotic

-CV

192
Q

Molindone

A

atypical antipsychotic

193
Q

paliperidone

A

atypical antipsychotic

194
Q

zotepine

A

atypical antipsychotic azepine

195
Q

Lozapine

A

azepine atypical antipsychotic

196
Q

thiothixine

A

typical antipsychotic thioxanthene

197
Q

Zuclopentixol

A

typical antipsychotic thioxanthene

198
Q

Flupenthixol

A

typical antipsychotic thioxanthene

199
Q

Chlorprothixene

A

typical antipsychotic thioxanthene

200
Q

Trifluoperazine

A

typical antipsychotic phenothiazine

201
Q

Perphenazine

A

typical antipsychotic phenothiazine

202
Q

Mesoridazine

A

typical antipsychotic phenothiazine

203
Q

Thioridazine

A

typical antipsychotic phenothiazine

  • low potency
  • CV
204
Q

Fluphenazine

A

typical antipsychotic phenothiazine

205
Q

Chloralhydrate

A

barbiturate-like antidepressant

206
Q

Eczopiclone

A

non BDZ hypnotic GABA A agonist

207
Q

Zaleplon

A

non BDZ hypnotic GABA A agonist

-typically used for sleep

208
Q

Flurazepam

A

long acting BZD hypnotic

209
Q

Triazolam

A

short acting BZD hypnotic used for sleep

210
Q

Halothane

A

inhale anesthetic

-hepatitis

211
Q

Thiopental

A

iv anes

212
Q

Methohexital

A

iv anes

213
Q

propofol

A

iv anes

-can be used as aole (no muscle relaxant)

214
Q

ketamine

A

iv anes

  • dysphoria, low dose analgesia, CV stimulant
  • exception incr cerebral bl fl
215
Q

Fentanyl

A

iv anes

-analgesia

216
Q

novocaine

A

first inject LA (ester)

-metab in plasma

217
Q

tetracaine

A

LA (ester)
incr pka so slow onset, long duration
-topical

218
Q

2-chloropricaine

A

LA (ester)

219
Q

Benzocaine

A

first synthetic LA (ester)

-methemoglobinemia, low pka nonionized base

220
Q

Lidocaine

A

amide LA prototype

221
Q

mepivacaine

A

amide LA
similar to lidocaine but less vasodilation
-accumulation don’t use for long epidural

222
Q

Dibucaine

A

LA topical cream (amide)

223
Q

Bupivacaine

A

LA (amide)

  • long acting
  • cardiotoxic (fix with intralipid)
  • Freq dependent block
  • spinal
224
Q

Ropivacaine

A

LA AMide

-compare to Bupivavaine, lower cardiotox, lower potency, beter freq dependent block, long lasting but not as long.

225
Q

Prilocaine

A
  • LA amide
  • methemoglobinemia
  • most rapid metab
226
Q

Nitrous Oxide

A

anesthetic with highest MAC

227
Q

BZD and anesthesia

A

Sedatives only, not anesthetics; no analgesia; effects partially antagonized by flumazenil

228
Q

Opoids and anesthetics

A

Analgesics not anesthetics; can reduce the amount of anesthetic required; effects 100% reversible with naloxone

229
Q

Physical properties of LAs

A

Weak bases, poorly water soluble; synthetics derived from cocaine

230
Q

Unmyelinated nerve fibers and LA

A

Small (B and C) fibers appear more sensitive to local anesthetics

231
Q

Duration of action anesth

A

Directly proportional to protein binding; also relates to toxicity - high protein binding reduces amount of free drug

232
Q

Long acting LAs

A

Bupivacaine and Ropivacaine

233
Q

LA toxicity initial signs

A

Central nervous system: lightheadedness, peri-oral numbness, dizziness, visual and auditory disturbances, disorientation, drowsiness.

234
Q

LA peripheral toxic signs

A

Vasoconstriction (low doses); vasodilation (high doses); chest pain, shortness of breath, palpitations,
more

235
Q

Sufentanil

A
  • more potent than fentanyl
  • ultra short acting
  • respiratory depression
236
Q

Narcotic

A

Any psychoactive compound with sleep-inducing properties. Today means totally prohibited

237
Q

Relatively selective COX II

A

Celecoxib, diclofenac

238
Q

COX I selective drugs

A

Flurbiprofen

ketorolac

239
Q

Butorphenol

A

Kappa opioid receptor agonist and mu opioid receptor antagonist or partial agonist

240
Q

Non opoid Non NSAID drugs

A

Acetaminophen, Tramadol

241
Q

Heroin

A

Rapidly metabolized to morphine. Due to rapid brain penetration, heroin causes an intense euphoria. Not used clinically in U.S.

242
Q

Acetaminophen

A

Non opoid non NSAID

-Does not produce GI damage, ineffective in intense pain, narrow therapeutic index - liver damage

243
Q

Oxycodone

A

Semisynthetic weak opioid agonist used in combination with NSAIDs for analgesia.

244
Q

Non-selective COX inhs

A

Ketoprofen, aspirin, naproxen, ibuprofen, indomethacin, sulindac

245
Q

SE aspirin

A

GI upset; hypersensitivity-like reaction; Reye’s syndrome; anticoagulant

246
Q

Opoid agonist prototype

A

morphine

247
Q

Naloxone

A

NARCAN; pure opioid antagonist, most potent at the mu receptor

248
Q

COX 1

A

Constitutively active enzyme, involved in GI protection, platelet function, regulation of blood flow and kidney function

249
Q

Codeine

A

Weak mu opioid agonist used as antitussive and analgesic in mild pain. Prodrug for morphine

250
Q

COX II

A

Inducible enzyme, involved in inflammation, pain, fever and cardiovascular function

251
Q

Celecoxib

A

Osteoarthritis and rheumatoid arthritis in adult patients, acute pain an dysmenorrhea; increased risk of major cardiovascular problems (30%)

252
Q

Loperimide

A

IMODIUM, a mu opioid agonist that is poorly absorbed after oral administration; used as an antidiarrheal. Does not cross the blood brain barrier

253
Q

Mechanism of NSAID renal effects

A

Inhibit prostaglandin synthesis allowing vasoconstriction leading to acute renal failure

254
Q

Meperidine

A

Synthetic, weak mu opioid agonist used for analgesia during delivery.

255
Q

Methedone

A

Orally active long acting mu opioid receptor agonist. Does not cause significant euphoria. Cross tolerance with morphine or heroin and therefore useful with addicts

256
Q

Surgical treatment for chronic pain

A

Cut spinothalamic tract

257
Q

Morphine SEs

A

Euphoria, sedation, respiratory depression, nausea and vomiting, constipation, reduced release of hormones (GnRH and CRF) from hypothalamus

258
Q

A-delta fibers

A

Lightly myelinated axons, rapid condution of signal, mediate the fast, pricking or sharp quality of pain

259
Q

Nigro-striatal dopaminergic pathway

A

substantia niagra to striatum

260
Q

VTA

A

dopiminergic cell bodies

261
Q

Raphae nucleus

A

serotonin cell bodies

262
Q

Tuberoinfundibular pathway

A

Hypothalamus to anterior pituitary

263
Q

Nucleus basalis

A

Acetylcholine neuronal cell bodies

264
Q

Locus cereuleous

A

NE cell bodies

265
Q

PCP can produce

A

hallucinations (incr glut)

266
Q

Drugs of abuse produce their effects through:

A

Through G-protein coupled receptors, ionotropic receptors and monoamine transporters

267
Q

The mesolimbic pathway including the nucleus accumbens

A

Is responsible for the mood elevating euphoria and rewarding effects of cocaine and amphetamine

268
Q

Hallucinogens

A

Increase extracellular glutamate in the prefrontal cortex through stimulation of postsynaptic 5-HT2A receptors

269
Q

Varenicline

A

Partial agonist of nicotinic acetylcholine receptors used for smoking cessation

270
Q

Acamprosate

A

Antagonist of NMDA receptor used for treatment of alcoholism

271
Q

Types of tolerance

A

Pharmacokinetic, pharmacodynamics, behavioral, and inverse (sensitization)

272
Q

Anandamide

A

endogenous ligand for cannabinoids

273
Q

PCP mech of action

A

Noncompetitive NMDA calcium channel blocker

274
Q

Alcohol mech of action

A

Blocks NMDA receptor and enhances GABA receptor (through GABA-A)

Pharmacology Block 2 (4 decks)

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