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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
**Meloxicam** | (Mobic)
* COX-2 inhibitor * arthritis
26
Cyclooxygenase (COX)
catalyzes formation of prostaglandins, thromboxane, and prostacyclin
27
**Celecoxib** | (celebrex)
selective COX-2 inhibitor broad-spectrum anti-inflammatory used off-label for prophylaxis of colorectal cancer
28
clinical characteristics of Asthma
* shortness of breath * chest tightness * wheezing * coughing
29
pathological characteristics of asthma
* hyper-responsive airways * inflammation, bronchoconstriction * vascular remodeling * collagen deposition, cellular hyperplasia
30
Model of Asthma
* initial exposure produces IgE antibodies * IgE binds to FceRI receptors on mast cells * reexposure releases stored mediators of inflammation
31
Early asthmatic response
* immediate airway constriction * histamine, prostaglandin, D2, leukotriene C4, tryptase, platelet activating factor (PAF) * immediate fall in FEV1
32
Late asthmatic response
* elevated mucus production, edema, sustained bronchoconstriction * delayed fall in FEV1
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34
**Formoterol** | (Foradil)
long-acting ß2-agonist (LABA)
35
**Salmeterol** | (Serevent)
long-acting ß2-agonist (LABA)
36
Theophylline
bronchodilation and antiinflammatory * increases intracellular cAMP * via phosphodiesterases * adenosine antagonist \*narrow therapeutic index
37
Ipratropium
COPD and asthma structurally simila to atopine
38
Glucocorticoids for Asthma
* Budesonide * Dexamethasone * Fluticasone * Mometasone
39
(7) ß2-agonist
* Albuterol * Formoterol * Levalbuterol * Metaproterenol * Pirbuterol * Terbutaline * Salmeterol
40
**Zileuton** | (Zyflo CR)
asthma ## Footnote reduces airway inflammation Leukotriene synthesis (5-LOX) inhibitor
41
(2) Leukotriene receptor antagonists for Asthma
Montelukast (Singulir) and Zafirlukast (Accolate)
42
\* Know where Zileuton and Montelkast/Zafirlukast
43
**Omalizumab** | (Xolair)
IgE antibody treats asthma
44
Cromolyn
treats asthma alters Cl- channels * inhibits mast cell degranulation * inhibits eosinophil responses * inhibits cough
45
Endogenous opioid peptides
produced in the human body
46
General mechanism of Opioids
Mu (u) agonist
47
General effects of Opioids
* analgesia * cough suppression * hypotension * nausea * miosis * constipation * tolerance
48
General Indications for Opioids (5)
* analgesia * cough suppression * diarrhea * shivering * acute pulmonary edema
49
Elimination of Opioids
mainly by the kidney ## Footnote In kidney disease, Meperidine may cause seizures and Codeine may enchance opioid action
50
Morphine
full agonist phenanthrenes
51
Methadone
Full opioid agonist phenylheptylamine
52
Opioid Phenylpiperidines (3)
* Fentanyl * Meperidine * Remifentanyl
53
Codeine
partial opioid agonist phenanthrenes
54
Opioid Phenylpiperidines | (partial)
Diphenoxylate and Loperamide treat diarrhea
55
**Nalbuphine** | (Nubain)
mixed opioid agonist
56
Absorption of Opioids
first-pass effect interpatient variability
57
Which sedative drug has a linear relationship between dose and stage of anesthesia?
Barbituates
58
(5) Benzodiazepines for Sedation
* Diazepam * Midazolam * Lorazepam * Temazepam * Triazolam
59
(4) Barbituates for Sedatin
* Methohexital * Pentobarbital * Secobarbital * Thiopental (Pentothal)
60
Therapeutic Indications for Sedatives
* anxiety * insomnia * epilepsy * nausea * control of ethanol withdrawal * spasticity
61
62
Schedule III Drug
barbituates prescriptions with refills
63
Schedule IV Drug
chloral hydrate, zolpidem, zaleplon prescriptions with refills [less addicting than III]
64
Schedule I Drug
No prescriptions heroin, LSD
65
Schedule II Drug
secobarbital no refills on prescriptions
66
Flumazenil
GABA antagonist treats benzodiazepine overdose
67
68
Benzodiazepine-like Drugs for Insomnia
Zolpidem, Zaleplon, Eszopiclone
69
**Ramelteon** | (Rozerem)
long-term treatment of insomnia melatonin agonist
70
OTC Sedatives
* NyQuil * Tylenol PM * Unisom * Wal-Som
71
Seizure
synchronous activity initiated by large depolarizations within a group of neurons (PDS) * heterogenous
72
Epilepsy
disorder of the brain characterized by an enduring predisposition to generate seizures
73
Phases of a Seizure
Aura, Ictal, Postictal
74
Simple partial seizure * identifiable focus * conscious and memory are preserved
75
Partial seizure secondarily generalized * localized onset that is extremely widespread
76
Tonic-Clonic (grand mal) seizure
sustained contraction followed by rhythmic limb movements
77
Status Epliepticus
life-threatening condition in which the brain is in a state of persistent seizure
78
A - firing neuron B - activated neuron C - modulatory interneuron D - activated neuron
79
Glutamate
80
GABA
81
**Phenytoin** | (Dilantin)
treatment of seizures blocks Na channels
82
**Carbamazepine** | (Tegretol)
treats seizures
83
**Lamotrigine** | (Lamictal)
treats seizures
84
Anti-Seizure drug targets
* 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
Valproate
treats seizures
86
Which drug increases risk of Spina Bifida
Valproate
87
**Ethosuximide** | (Zarontin)
treats seizures T-type Ca channel blocker
88
**Levetiracetam** | (Keppra)
treats seizures binds to SV2A
89
Benzodiazapine used for treatment in seizures and status epilepticus
Diazepam
90
Barbiturates to treat seizures and status epileptics
Phenobarbital
91
92
Major Depressive Disorder (MDD)
recurrent depressive episodes without a history of mania
93
Monoamine Hypothesis
depression results from decreased serotonin, norepinephrine, and/or dopamine
94
Neurotrophic Hypothesis for Depression
loss of neurotrophic support leads to depression (brain-derived neurotrophic factor)
95
HPA axis dysregulation hypothesis for Depression
elevated levels of cortisol and CRH
96
Pharmacotherapy for Depression
* SSRI * SNRI * 5-HT2 * MAO inhibitor * Atypical
97
SSRI Drugs (6)
* Citalopram (celexa) * Escitalopram (lexapro) * Fluoxetine (prozac) * Fluvoxamine (luvox) * Paroxetine (paxil) * Sertraline (zoloft)
98
Selective Serotonin Reuptake Inhibitor (SSRI)
selectively inhibits the SERT glycoprotein treatments for depression and anxiety
99
SNRI Drugs (3)
* Desvenlafaxine (pristiq) * Duloxetine (cymbalta) * Venlafaxine (effexor)
100
Serotonin Norepinephrine Reuptake Inhibitor (SNRI)
mixed inhibitor effects on SERT and NET treatment for depression and anxiety
101
Tricyclic Antidepressants (TCA) drug
Imipramine
102
5HT2 Antagonist
antidepressants ## Footnote Ex: Trazodone (Desyrel)
103
MAO Inhibitors
Increases level of NE, DA, and serotonin Ex: Phenelzine (Nardil) treatment for depression
104
Tyramine toxicity
hypertensive crisis, headache, tachycardia, nausea, cardiac arrhythmias, stroke
105
"Atypical" antidepressant drug
Bupropion (wellbutrin) induces release of catecholamines
106
107
Serotonin Syndrome
hypertension, tachycardia, diaphoresis, delirium, tremor, and coma caused by an interaction with MAO inhibitors
108
Positive Symptoms of Schizophrenia
hallucinations, delusions, disorganized, speech, and catatonic behavior
109
Negative symptoms of Schizophrenia
affective flattening, alogia, and avolition
110
(2) Typical Anti-Psychotics
Chlorpromazine and Haloperidol
111
(6) Atypical Anti-Psychotics
* Aripiprazole * Clozapine * Olanzapine * Quetiapine * Risperidone * Ziprasidone
112
113
Nonselective Receptor Blockade in Anti-Psychotics
* Dopamine receptor * Serotonin 5HT2A receptors * alpha adrenoceptors * Muscarinic receptors * Histamine H1 receptors
114
Nigrostriatal - substantia nigra to striatum
115
116
Lithium - Mechanism of Action
* enters through cation channels * disrupts IP3 and DAG * narrow therapeutic window \*\*Adjunct for MDD \*\* Prophylaxis of BPAD
117
What monovalent cation is an adjunct for MDD?
Lithium
118
Schizophrenia causes
excess Dopamine and/or serotonin signaing
119
120
121
Class I : Opioids
morphine, heroin, codeine, oxycodone, meperidine
122
**Naloxone** | (narcan)
short-acting opioid antagonist
123
Naltrexone | (ReVia)
long-acting opioid antagonist
124
Methadone
long-acting opioid agonist used for opioid addiction
125
**Buprenorphine** | (Buprenex)
mixed, long-acting opioid agonist
126
Class I : Cannabinoids
Marijuana, dronabinol, nabilone, rimonabant
127
**Acamprosate** | (campral)
treatment of alcoholism GABAa agonist and NMDA antagonist
128
**Disulfiram** | (antabuse)
treatment of alcoholism inhibits aldehyde dehydrogenase
129
Treatment of Cocaine withrdrawal
Buprenorphine and Bromocriptine
130
5-HT3 Antagonist for Nausea
Ondansetron
131
NK1 antagonist for nausea drug
Aprepitant
132
H1 drug for Nausea
Diphenhydramine
133
Anticholinergic for Nausea
Scopolamine
134
Corticosteroid for nausea
Dexamethasone
135
Dopamine antagonist for Nausea
Promethazine
136
137
Risk factors for Alzheimers
* 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
Pathological features of Alzheimers
* loss of cortical and subcortical neurons * extracellular amyloid plaques * intracellular neurofibrillary tangles
139
Pharmacotherapy Goals for Alzheimers
* restore acetylcholine * centrally-acting acetylcholinesterase inhibitors * decrease glutamate-mediated excitotoxicity * NMDA antagonist * Improve cerebral blood flow * ergloid mesylates
140
141
142
**Donepezil** | (aricept)
treats Alzheimers reversible inhibitr of ACh E
143
**Ricastigmine** | (exelon)
treats Alzheimers irreversible inhibitor of ACh E
144
**Memantine** | (namenda)
treats Alzheimers uncompetitive NMDA antagonist
145
Ergoloid Mesylates
cerebral vasodilator may treat alzheimers Combination of Dihydroergocornine, dihydroergocristine, and dihydroergocryptine
146
Motor Symptoms of Parkinson's
* resting tremor * muscle rigidity * akinesia/bradykinesia * postural instability
147
Pathological features of Parkinsons
* loss of dopaminergic neurons * lewy bodies
148
Risk factors for Parkinson's
* Age * 0.5-1.0% of individuals 65-69 * 1-3% of people \> 80 years * sex * males \> females * genetic * alpha-synuclein
149
Pharmacotherapy for Parkinsons
1. dopamine precursor 2. dopamine agonists 3. inhibitors of dopamine metabolism 4. antimuscarinic drug therapy 5. amantadine
150
151
Dpamine precursor for Parkinsons
Levodopa and Carbidopa
152
Dopamine agonist for Parkinsons
Pramipexole | (mirapex)
153
inhibitors of dopamine metabolism for Parkinsons
MAO inhibitors - Selegiling (eldepryl) COMT inhibitors - entacapone (comtan)
154
Antimuscarinic treatment for Parkinsons
Benztropine | (cogentin)
155
156
**Amantadine** | (symmetrel)
treatment for Parkinsons

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