Pharmacology Midterm Flashcards

1
Q

Cardinal Signs of Inflammation

A

Dolor (pain)

Rubor (redness)

Calor (heat)

Tumor (swelling)

*5th sign is loss of function, added later

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2
Q

Inflammation Cell Types

A
  • Granulocytes
    • neutrophils
    • eosinophils
    • basophils
  • Monocytes
  • Mast cells
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3
Q

Which granulocyte is increased during allergic and parasitic reactions?

A

Eosinophils

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4
Q

Which granulocyte contains histamine?

A

Basophils

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5
Q

Types of Chemical Mediators

A
  • vasoactives
  • chemotactic factors
  • plasma proteases
  • reactive molecules
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6
Q

Phases in Inflammatory Response

A
  1. Vasodilation
  2. Chemotaxis
  3. Phagocytosis
  4. Resolution
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7
Q

Pharmacology for Inflammation

A
  • Steroids
  • NSAIDS
  • DMARDS
    • disease modifying anti-rheumatic drugs
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8
Q

Steroids used in Inflammation

A
  • Corticosteroids or glucocorticoids
    • induce calcium and lipocortins
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9
Q

Types of NSAIDS

A
  • salicylates (acetylated and non-acetylated)
  • selective COX-2 inhibitors
  • non-selective COX-2 inhibitors
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10
Q

Pharmacokinetic features of Anti-Inflammatories

A
  • weak acid
  • well absorbed in GI
  • highly protein bound
  • extensive liver metabolism
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11
Q

Non-Steroidal Anti-Inflammatory Drugs (NSAIDS)

A
  • COX inhibitors
    • COX catalyzes formation of prostanoids
  • Drugs:
    • acetylsalicyclic acid
    • ketorolac
    • Celecoxib
    • Meloxicam
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12
Q

Adverse Effects of NSAIDS

A
  • CNSH
    • headaches, tinnitus, and dizziness
  • Cadiovascular
    • fluid retention, hypertension, and edema
  • Gastrointestinal
    • abdominal pain, nausea, vomiting, ulcers, bleeding
  • Hematological
    • thrombocytopenia, neutropenia, aplastic anemia
  • Hepatic
    • abnormal LFT and rare liver failure
  • Pulmonary
    • airway hyper-reactivity
  • Integumentary
    • pruritis
  • Renal
    • insufficiency, failure, hyperkalemia, and proteinuria
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13
Q

Cyclooxygenase-1 (COX-1)

A
  • expressed gene
  • generates prostanoids for “housekeeping”
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14
Q

Cyclooxygenase-2 (COX-2)

A
  • inducible gene
  • major route by which prostanoids involved in inflammation are synthesized
  • selective NSAIDS target only COX-2
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15
Q

Non-Selective NSAIDS Drugs

A
  • Acetylsalicyclic acid
  • ketorolac
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16
Q

Selective NSAIDS Drugs

A
  • Celecoxib
  • Meloxicam
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17
Q

Acetylsalicylic Acid adverse effects

A
  • unwanted bleeding
  • gastric upset and ulcers
  • angioedema, hives, and rashes
  • nephrotoxicity, hepatotoxicity
  • airway hyperreactivity
  • salicylism
  • Reye’s syndrome
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18
Q

Salicylism

A

toxicity associated with high doses of aspirin

headache, vomiting, tinnitus, vertigo, fever, seizures, respiratory depressions

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19
Q

Reye’s Syndrome

A

Aspirin use in young children

vomiting, encephalopathy, hepatotoxicity

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20
Q

Ketorolac mechanism of action

A

reversible inhibitor of COX-1 and COX-2

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21
Q

Ketorolac duration of use

A

up to 5 consecutive days

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22
Q

Celecoxib Black Box Warning

A
  • risk of thrombosis, MI
  • contraindicated in CABG surgery
  • serious GI effects
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23
Q

Precautions of Steroidal Anti-Inflammatory Drugs

A
  • Children: growth retardation
  • elderly: osteoporosis
  • diabetes: increase blood glucose
  • psychosis: exacerbation
  • myasthenia gravis: muscle weakness
  • hypertension: sodium/water retention
  • systemic infections: immunosupression
  • pregnancy: catgeory C
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24
Q

Acetaminophen

A
  • COX-1, COX-2, and COX-3 inhibitor
  • analgesic and antipyretic
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25
Q

Meloxicam

(Mobic)

A
  • COX-2 inhibitor
  • arthritis
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26
Q

Cyclooxygenase (COX)

A

catalyzes formation of prostaglandins, thromboxane, and prostacyclin

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27
Q

Celecoxib

(celebrex)

A

selective COX-2 inhibitor

broad-spectrum anti-inflammatory

used off-label for prophylaxis of colorectal cancer

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28
Q

clinical characteristics of Asthma

A
  • shortness of breath
  • chest tightness
  • wheezing
  • coughing
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29
Q

pathological characteristics of asthma

A
  • hyper-responsive airways
    • inflammation, bronchoconstriction
  • vascular remodeling
    • collagen deposition, cellular hyperplasia
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30
Q

Model of Asthma

A
  • initial exposure produces IgE antibodies
  • IgE binds to FceRI receptors on mast cells
  • reexposure releases stored mediators of inflammation
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31
Q

Early asthmatic response

A
  • immediate airway constriction
  • histamine, prostaglandin, D2, leukotriene C4, tryptase, platelet activating factor (PAF)
  • immediate fall in FEV1
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32
Q

Late asthmatic response

A
  • elevated mucus production, edema, sustained bronchoconstriction
  • delayed fall in FEV1
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33
Q
A
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34
Q

Formoterol

(Foradil)

A

long-acting ß2-agonist (LABA)

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35
Q

Salmeterol

(Serevent)

A

long-acting ß2-agonist (LABA)

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36
Q

Theophylline

A

bronchodilation and antiinflammatory

  • increases intracellular cAMP
    • via phosphodiesterases
  • adenosine antagonist

*narrow therapeutic index

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37
Q

Ipratropium

A

COPD and asthma

structurally simila to atopine

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38
Q

Glucocorticoids for Asthma

A
  • Budesonide
  • Dexamethasone
  • Fluticasone
  • Mometasone
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39
Q

(7) ß2-agonist

A
  • Albuterol
  • Formoterol
  • Levalbuterol
  • Metaproterenol
  • Pirbuterol
  • Terbutaline
  • Salmeterol
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40
Q

Zileuton

(Zyflo CR)

A

asthma

reduces airway inflammation

Leukotriene synthesis (5-LOX) inhibitor

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41
Q

(2) Leukotriene receptor antagonists for Asthma

A

Montelukast (Singulir) and Zafirlukast (Accolate)

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42
Q
A

* Know where Zileuton and Montelkast/Zafirlukast

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43
Q

Omalizumab

(Xolair)

A

IgE antibody

treats asthma

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44
Q

Cromolyn

A

treats asthma

alters Cl- channels

  • inhibits mast cell degranulation
  • inhibits eosinophil responses
  • inhibits cough
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45
Q

Endogenous opioid peptides

A

produced in the human body

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46
Q

General mechanism of Opioids

A

Mu (u) agonist

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47
Q

General effects of Opioids

A
  • analgesia
  • cough suppression
  • hypotension
  • nausea
  • miosis
  • constipation
  • tolerance
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48
Q

General Indications for Opioids (5)

A
  • analgesia
  • cough suppression
  • diarrhea
  • shivering
  • acute pulmonary edema
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49
Q

Elimination of Opioids

A

mainly by the kidney

In kidney disease, Meperidine may cause seizures and Codeine may enchance opioid action

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50
Q

Morphine

A

full agonist

phenanthrenes

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51
Q

Methadone

A

Full opioid agonist

phenylheptylamine

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52
Q

Opioid Phenylpiperidines (3)

A
  • Fentanyl
  • Meperidine
  • Remifentanyl
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53
Q

Codeine

A

partial opioid agonist

phenanthrenes

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54
Q

Opioid Phenylpiperidines

(partial)

A

Diphenoxylate and Loperamide

treat diarrhea

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55
Q

Nalbuphine

(Nubain)

A

mixed opioid agonist

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56
Q

Absorption of Opioids

A

first-pass effect

interpatient variability

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57
Q

Which sedative drug has a linear relationship between dose and stage of anesthesia?

A

Barbituates

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58
Q

(5) Benzodiazepines for Sedation

A
  • Diazepam
  • Midazolam
  • Lorazepam
  • Temazepam
  • Triazolam
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59
Q

(4) Barbituates for Sedatin

A
  • Methohexital
  • Pentobarbital
  • Secobarbital
  • Thiopental (Pentothal)
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60
Q

Therapeutic Indications for Sedatives

A
  • anxiety
  • insomnia
  • epilepsy
  • nausea
  • control of ethanol withdrawal
  • spasticity
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61
Q
A
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62
Q

Schedule III Drug

A

barbituates

prescriptions with refills

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63
Q

Schedule IV Drug

A

chloral hydrate, zolpidem, zaleplon

prescriptions with refills

[less addicting than III]

64
Q

Schedule I Drug

A

No prescriptions

heroin, LSD

65
Q

Schedule II Drug

A

secobarbital

no refills on prescriptions

66
Q

Flumazenil

A

GABA antagonist

treats benzodiazepine overdose

67
Q
A
68
Q

Benzodiazepine-like Drugs for Insomnia

A

Zolpidem, Zaleplon, Eszopiclone

69
Q

Ramelteon

(Rozerem)

A

long-term treatment of insomnia

melatonin agonist

70
Q

OTC Sedatives

A
  • NyQuil
  • Tylenol PM
  • Unisom
  • Wal-Som
71
Q

Seizure

A

synchronous activity initiated by large depolarizations within a group of neurons (PDS)

  • heterogenous
72
Q

Epilepsy

A

disorder of the brain characterized by an enduring predisposition to generate seizures

73
Q

Phases of a Seizure

A

Aura, Ictal, Postictal

74
Q
A

Simple partial seizure

  • identifiable focus
    • conscious and memory are preserved
75
Q
A

Partial seizure secondarily generalized

  • localized onset that is extremely widespread
76
Q

Tonic-Clonic (grand mal) seizure

A

sustained contraction followed by rhythmic limb movements

77
Q

Status Epliepticus

A

life-threatening condition in which the brain is in a state of persistent seizure

78
Q
A

A - firing neuron

B - activated neuron

C - modulatory interneuron

D - activated neuron

79
Q
A

Glutamate

80
Q
A

GABA

81
Q

Phenytoin

(Dilantin)

A

treatment of seizures

blocks Na channels

82
Q

Carbamazepine

(Tegretol)

A

treats seizures

83
Q

Lamotrigine

(Lamictal)

A

treats seizures

84
Q

Anti-Seizure drug targets

A
  • Voltage-gated Na+ channels
  • Ca++ channels (HVA and T-type)
  • K+ channels
  • NMDA / AMPA receptors
  • GABAA Cl- channels
  • GABA transporters (GAT-1)
  • Synaptic vesicle proteins (SV2 A)
  • Glutamic acid decarboxylase
  • GABA transaminase
  • Collapsin-response mediator protein (CRMP-2)
85
Q

Valproate

A

treats seizures

86
Q

Which drug increases risk of Spina Bifida

A

Valproate

87
Q

Ethosuximide

(Zarontin)

A

treats seizures

T-type Ca channel blocker

88
Q

Levetiracetam

(Keppra)

A

treats seizures

binds to SV2A

89
Q

Benzodiazapine used for treatment in seizures and status epilepticus

A

Diazepam

90
Q

Barbiturates to treat seizures and status epileptics

A

Phenobarbital

91
Q
A
92
Q

Major Depressive Disorder (MDD)

A

recurrent depressive episodes without a history of mania

93
Q

Monoamine Hypothesis

A

depression results from decreased serotonin, norepinephrine, and/or dopamine

94
Q

Neurotrophic Hypothesis for Depression

A

loss of neurotrophic support leads to depression

(brain-derived neurotrophic factor)

95
Q

HPA axis dysregulation hypothesis for Depression

A

elevated levels of cortisol and CRH

96
Q

Pharmacotherapy for Depression

A
  • SSRI
  • SNRI
  • 5-HT2
  • MAO inhibitor
  • Atypical
97
Q

SSRI Drugs (6)

A
  • Citalopram (celexa)
  • Escitalopram (lexapro)
  • Fluoxetine (prozac)
  • Fluvoxamine (luvox)
  • Paroxetine (paxil)
  • Sertraline (zoloft)
98
Q

Selective Serotonin Reuptake Inhibitor (SSRI)

A

selectively inhibits the SERT glycoprotein

treatments for depression and anxiety

99
Q

SNRI Drugs (3)

A
  • Desvenlafaxine (pristiq)
  • Duloxetine (cymbalta)
  • Venlafaxine (effexor)
100
Q

Serotonin Norepinephrine Reuptake Inhibitor (SNRI)

A

mixed inhibitor effects on SERT and NET

treatment for depression and anxiety

101
Q

Tricyclic Antidepressants (TCA) drug

A

Imipramine

102
Q

5HT2 Antagonist

A

antidepressants

Ex: Trazodone (Desyrel)

103
Q

MAO Inhibitors

A

Increases level of NE, DA, and serotonin

Ex: Phenelzine (Nardil)

treatment for depression

104
Q

Tyramine toxicity

A

hypertensive crisis, headache, tachycardia, nausea, cardiac arrhythmias, stroke

105
Q

“Atypical” antidepressant drug

A

Bupropion (wellbutrin)

induces release of catecholamines

106
Q
A
107
Q

Serotonin Syndrome

A

hypertension, tachycardia, diaphoresis, delirium, tremor, and coma

caused by an interaction with MAO inhibitors

108
Q

Positive Symptoms of Schizophrenia

A

hallucinations, delusions, disorganized, speech, and catatonic behavior

109
Q

Negative symptoms of Schizophrenia

A

affective flattening, alogia, and avolition

110
Q

(2) Typical Anti-Psychotics

A

Chlorpromazine and Haloperidol

111
Q

(6) Atypical Anti-Psychotics

A
  • Aripiprazole
  • Clozapine
  • Olanzapine
  • Quetiapine
  • Risperidone
  • Ziprasidone
112
Q
A
113
Q

Nonselective Receptor Blockade in Anti-Psychotics

A
  • Dopamine receptor
  • Serotonin 5HT2A receptors
  • alpha adrenoceptors
  • Muscarinic receptors
  • Histamine H1 receptors
114
Q
A

Nigrostriatal - substantia nigra to striatum

115
Q
A
116
Q

Lithium - Mechanism of Action

A
  • enters through cation channels
  • disrupts IP3 and DAG
  • narrow therapeutic window

**Adjunct for MDD

** Prophylaxis of BPAD

117
Q

What monovalent cation is an adjunct for MDD?

A

Lithium

118
Q

Schizophrenia causes

A

excess Dopamine and/or serotonin signaing

119
Q
A
120
Q
A
121
Q

Class I : Opioids

A

morphine, heroin, codeine, oxycodone, meperidine

122
Q

Naloxone

(narcan)

A

short-acting opioid antagonist

123
Q

Naltrexone

(ReVia)

A

long-acting opioid antagonist

124
Q

Methadone

A

long-acting opioid agonist

used for opioid addiction

125
Q

Buprenorphine

(Buprenex)

A

mixed, long-acting opioid agonist

126
Q

Class I : Cannabinoids

A

Marijuana, dronabinol, nabilone, rimonabant

127
Q

Acamprosate

(campral)

A

treatment of alcoholism

GABAa agonist and NMDA antagonist

128
Q

Disulfiram

(antabuse)

A

treatment of alcoholism

inhibits aldehyde dehydrogenase

129
Q

Treatment of Cocaine withrdrawal

A

Buprenorphine and Bromocriptine

130
Q

5-HT3 Antagonist for Nausea

A

Ondansetron

131
Q

NK1 antagonist for nausea drug

A

Aprepitant

132
Q

H1 drug for Nausea

A

Diphenhydramine

133
Q

Anticholinergic for Nausea

A

Scopolamine

134
Q

Corticosteroid for nausea

A

Dexamethasone

135
Q

Dopamine antagonist for Nausea

A

Promethazine

136
Q
A
137
Q

Risk factors for Alzheimers

A
  • 1% of 65-69 year olds
    • risk doubles every 5 years afterwards
    • 40-50% over 95 years
  • Females > males
  • beta-amyloid precursor protein (APP), PS-1, and PS-2 genetic mutations
    • also APOE variant
138
Q

Pathological features of Alzheimers

A
  • loss of cortical and subcortical neurons
  • extracellular amyloid plaques
  • intracellular neurofibrillary tangles
139
Q

Pharmacotherapy Goals for Alzheimers

A
  • restore acetylcholine
    • centrally-acting acetylcholinesterase inhibitors
  • decrease glutamate-mediated excitotoxicity
    • NMDA antagonist
  • Improve cerebral blood flow
    • ergloid mesylates
140
Q
A
141
Q
A
142
Q

Donepezil

(aricept)

A

treats Alzheimers

reversible inhibitr of ACh E

143
Q

Ricastigmine

(exelon)

A

treats Alzheimers

irreversible inhibitor of ACh E

144
Q

Memantine

(namenda)

A

treats Alzheimers

uncompetitive NMDA antagonist

145
Q

Ergoloid Mesylates

A

cerebral vasodilator

may treat alzheimers

Combination of Dihydroergocornine, dihydroergocristine, and dihydroergocryptine

146
Q

Motor Symptoms of Parkinson’s

A
  • resting tremor
  • muscle rigidity
  • akinesia/bradykinesia
  • postural instability
147
Q

Pathological features of Parkinsons

A
  • loss of dopaminergic neurons
  • lewy bodies
148
Q

Risk factors for Parkinson’s

A
  • Age
    • 0.5-1.0% of individuals 65-69
    • 1-3% of people > 80 years
  • sex
    • males > females
  • genetic
    • alpha-synuclein
149
Q

Pharmacotherapy for Parkinsons

A
  1. dopamine precursor
  2. dopamine agonists
  3. inhibitors of dopamine metabolism
  4. antimuscarinic drug therapy
  5. amantadine
150
Q
A
151
Q

Dpamine precursor for Parkinsons

A

Levodopa and Carbidopa

152
Q

Dopamine agonist for Parkinsons

A

Pramipexole

(mirapex)

153
Q

inhibitors of dopamine metabolism for Parkinsons

A

MAO inhibitors - Selegiling (eldepryl)

COMT inhibitors - entacapone (comtan)

154
Q

Antimuscarinic treatment for Parkinsons

A

Benztropine

(cogentin)

155
Q
A
156
Q

Amantadine

(symmetrel)

A

treatment for Parkinsons