Exam 1 Pharmacology Flashcards

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1
Q

What are Prostaglandins?

A

Lipids made at the site of tissue injury.

These increase pain sensitivity, inflammation, and blood flow

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2
Q

Acetaminophen (Tylenol) MOA

A

Inhibits synthesis of prostaglandins in the CNS and works peripherally to block pain impulse generation

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3
Q

Acetaminophen (Tylenol) info and affects

A

Good at lower body temp

1st line of use in OA

No anti-inflammatory effects

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4
Q

Acetaminophen (Tylenol) ADRs

A

Hepatic necrosis at high doses

Not to be used w/ alcohol

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5
Q

APAP (Tylenol) overdose & Treatment

A

too much dose causes exhausts glutathione stores in the level, which neutralize toxic metabolites

TREATMENT
NAC (for overdose) - replenishes glutathione

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6
Q

NSAIDs MOA and Clinical use

A

MOA
- COX-1/2 inhibitor, decrease prostaglandin precursors

Clinical use
- pain/inflammation
- commonly combined w/ opioids

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7
Q

NSAIDs SE/ADR and risk factors

A

SE/ADR
GI bleeding, perforation, and kidney disease

Risk of bleeding due to decreased platelet

Fluid retention

Risk factors
Avoid w/ kidney/hepatic disease
caution w/ elderly (bleeding/kidney damage)

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8
Q

Characteristics that distinguish NSAIDs to Narcotics (Opioids)

A
  • Antipyretic (reduce fever)
  • Anti-inflammatory
  • Ceiling affect to analgesia(pain)
  • DO NOT cause tolerance
  • DO NOT cause dependence
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9
Q

COX-1 ADR w/ inhibition

A

GI
Peptic ulcers
GI Bleeding

Kidney
- Na/Water retention
- HTN
- hemodynamic acute kidney injury

Cardiovascular
- Vasoconstriction
- platelet aggregation

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10
Q

COX-2 inhibition SE/ADR

A

Kidney
- Na/Water retention
- HTN
- hemodynamic acute kidney injury

Cardiovascular
- Increase vasodilation
- inhibit platelet aggregation
- Stroke
- MI

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11
Q

What is Naproxen and what is its advantage

A

NSAID

BID (twice/day)

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12
Q

What is Meloxicam and what is its advantage

A

NSAID

once/day dosing

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13
Q

What is Ketorolac (Toradol)?

A

1st NSAID in U.S.

limited to 5 days due to ADRs (GI bleeding)

caution w/ renal insufficient pts.

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14
Q

What is Diclofenac

A

NSAIDs

has multiple dosage forms/names

Oral and Topical

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15
Q

What is Indomethacin (Indocin)

A

NSAID

Used for gout

Higher risk for GI bleeding compared to other traditional NSAIDs

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16
Q

What are Propionic acids?

A

Most commonly seen OTC NSAIDs like Ibuprofen

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17
Q

What are the chronic ADRs of NSAIDs

A

GI bleeding

Kidney damage

Fluid retention

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18
Q

Selective COX 1 vs COX 2 inhibition differences in ADR

A

COX-1
- GI ADR (Peptic ulcers and GI bleeds)

COX-2
- Cardiovascular ADR (Stroke/MI)

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19
Q

What is the only COX-2 inhibitor left on the market?

A

Celecoxib (Celebrex)

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20
Q

What are Salicylates?

A

Aspirin (ASA)

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21
Q

What is the MOA for Aspirin (ASA)?

A

Inhibits Cyclooxygenase which decreases prostaglandins

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22
Q

What are the ADRs for Aspirin (ASA)?

A

Tinnitus (first sign of toxicity) - ringing on the ear

GI bleeding

must avoid in children under 12

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23
Q

What are adjuvants?

A

meds that are meant to treat conditions that are not directly pain.

Fibromyalgia / neuropathic pain

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24
Q

What is the MOA of Adjuvants?

A

Effect 5-HT and NE

often used w/ opioids for greater pain relief

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25
What are the 4 main types of adjuvants?
Antiepileptics SNRIs Local Anesthetics TCAs
26
What do you use to treat neuropathic pain?
Antidepressants: Focus on 5-HT+NE TCAs SNRI Antiepileptic drugs (AEDs) Local/topical anesthetics
27
What is the main ADR for TCAs
Anticholinergic effects
28
What are anticholinergic effects?
Urinary retention Increased HR Blurry vision Constipation
29
What are the two most common AEDs
Gabapentin and Pregabalin
30
What do Gabapentin and Pregabalin do?
Increase GABA inhibitory response Decrease seizures/epilepsy
31
What is a ADR of using a drug that increases NE
vasoconstriction and increased HR
32
What is the short-term treatment of anxiety?
Benzodiazepines
33
What are the long-term treatments of anxiety?
Buspirone SSRIs SNRIs TCA
34
What are the treatments for resistant anxiety?
Mood stabilizers and Beta blockers
35
What are Benzos MOA?
Bind to benzo receptors to enhance GABA. Rapid relief and very effective
36
What are the Disadvantages of Benzos?
Tolerance, addiction, need to taper and only treat symptoms not actual cause
37
What are Xanax?
BENZO intermediate onset w/ 12-15 hours t1/2
38
What are Klonopin?
BENZO intermediate onset w/ 24-40 hr t1/2
39
What is valium?
BENZO Rapid onset w/ 20-80 hr half life which makes it not good for the older pop.
40
What is Ativan?
BENZO intermediate onset w/ half life 10-20 hr
41
What is the MOA for Buspirone?
Mid brain modulator, effects NE, ACh, DA, 5-HT, and GABA basically affects all NTs
42
Adv and Disadv of Buspirone?
ADV - non sedating and no dependence DISADV - no buzz, multiple doses per day, 2-6 wks for affect.
43
What is the SSRI MOA
Blocks reuptake of serotonin in CNS (increases serotonin) *Inhibits the p450 system*
44
what are SSRIs
1st line of treatment for anxiety used to control mood (serotonin)
45
What are the risks and ADRs for SSRI
Risk of overstimulation INCREASES HR inhibits p450 System highly protein bound can increase suicide ideation sexual dysfunction 4-6 weeks for affect
46
What are Beta Blockers?
used for SITUATIONAL ANXIETY or PTSD EX. - Social anxiety - public speaking
47
What are the ADRs of Beta Blockers?
Hypotension, Drowsiness, nausea, and diarrhea
48
What is Propranolol?
Non-selective beta blocker that is PRN
49
What is the MOA of Propranolol?
Blunts effects of NE + Epinephrine (decreases adrenaline)
50
What are mood stabilizers?
Used if 1st line agents are unsuccessful but have nasty ADRs
51
What is the duration of treatment for anxiety?
4-6 wks but typically require lifelong treatment *NOT BENZOS need to get off ASAP but tamper*
52
What is a manic episode?
Irritable mood that last for at least 1 week has 3 of the following symptoms - inflated self esteem - decreased need for sleep - more talkative than usual - racing thoughts - distractibility - decreased judgement
53
What is the etiology of Bipolar disorder?
UNKNOWN
54
What is the patho of BPD?
Changes in the limbic system, basal ganglia + hypothalamus fluctuation in NE + DA and intracerebral Ca2+ lvls
55
What are the symptoms of BPD?
Overconfidence change in sleep patterns irrational decision making grandiosity increased activity pressured speech
56
How do you treat BPD?
There is NO CURE drug therapy is likely lifelong w/ the goals of controlling symptoms and reducing the frequency of cycles BZDs and antipsychotics are used or non-pharm treatment
57
What are the acute BPD treatment options?
Benzo (short-term), lithium, valproic acid, carbamazepine, antipsychotics
58
What are the maintenance BPD treatment options?
Monotherapy (one drug) but not likely lithium valproic acid lamotrigine
59
What are the treatment options for depressive BPD?
anti-depressants cautiously due to possible flip into mania
60
What is the MOA of lithium?
effects anion exchange and sodium transport in nerves which normalizes transmission of NE, 5-HT, and DA 100% renally eliminated
61
What are the ADRs of Lithium?
ACUTE Polyuria, polydipsia, tremor, and anthimeria LONG-TERM hypothyroidism, EKG changes, and increased WBC
62
What is lithium?
GOLD STANDARD of Mood Stabilizers takes 5-10 days for benefit but has a long t1/2
63
What is the MOA of Valproic acid?
Increase GABA onset in 3-5 days
64
What is valproic acid used for?
Good for rapid cyclers and mixed episodes but need baseline labs first to reduce ADRs
65
What is the MOA for Carbamazepine?
Increase the GABA system and block Na channels *Mood Stabilizer* Metabolized hepatically 1-2 wk onset
66
What is Lamotrigine?
Used as a last resort or add on therapy. *Mood Stabilizer*
67
What are atypical antipsychotics?
1st line agents for depression
68
What is the MOA for atypical antipsychotics?
DA antagonist, 5-HT partial agonist/antagonist
69
What is the biogenic amine hypothesis?
Depression is caused by reduction of multiple NTs (DA, 5-HT, and NE)
70
What parts of the brain and what NTs are involved w/ Depression?
Limbic system and hypothalamus most involved. NE, 5-HT, and DA
71
What are antidepressants?
Restore NT balance all work 60-70% of the time no matter the agent (generic or not) onset takes wks for benefit but quicker for ADRs
72
What are SSRIs used to treat?
Depression
73
What is the MOA of TCAs?
Inhibit reuptake of NE + 5-HT
74
What are the ADRs of TCAs?
Anticholinergic effects lowers threshold for seizures cardiovascular risks
75
What do TCAs put elderly people at a higher risk for?
Sedation and orthostatic hypotension all things to increase fall risk
76
TCAs
Antidepressant (1st generation SNRIs) used in combo w/ SSRIs to help sleep Fetal in overdose (20mg/kg)
77
What are monoamine Oxidase Inhibitors?
SUCK
78
What is the MOA of MAO?
impair degradation of NE, 5-HT, DA. These would increase NT concentration increases risk of HTN
79
What is the MOA of Desyrel?
inhibits serotonin reuptake (increase 5-HT)
80
What is the MOA of wellbutrin?
mild dopamine reuptake inhibitor only (no affect on other NTs)
81
ADRs of wellbutrin?
minimize alcohol use don't use w/ seizure pts no cardio, sexual, or anticholinergic effects weight loss, insomnia, headache, and nausea
82
What are the ADRs of Remeron?
sleepiness dizziness increased appetite increased cholesterol orthostatic hypotension *HALLUCINATIONS*
83
what is the MOA of SNRI
blocks reuptake of 5-HT and NE which means an increase in 5-HT and NE may cause BP risk in HTN pts.
84
What are the ADRs for fetzima?
serotonin syndrome increased BP hyponatremia
85
What is serotonin syndrome?
Too much serotonin which can cause peristalsis which will cause bad diarrhea
86
What is the definition of schizophrenia?
Heterogenous syndrome of disorganized and bizarre thoughts of delusions, hallucinations, disorganized speech/behavior, and impaired psychosocial function.
87
What are the structural changes that happen w/ schizophrenia?
Increased ventricular size reduction of medial temporal lobe and hippocampus
88
what is the patho of schizophrenia?
DA is hyperactive in limbic system and hypo functioning in prefrontal cortex
89
What are positive vs negative symptoms of schizophrenia?
Positive - things that schizophrenia pts have that normal people would not - easier to treat w/ drug therapy Negative - that that normal people have but pts w/ schizophrenia do not. - hard to treat w/ drug therapy
90
Examples of positive symptoms of schizophrenia?
hallucination delusion
91
Examples of negative symptoms of schizophrenia?
Alogia flattened affect avolition anhedonia attentional impairment
92
What is the MOA of schizophrenia treatment?
block DA receptors in mesolimbic area which will reduce hyperactivity D2 for antipsychotics D1 responsible for EPS symptoms
93
What are the classes of antipsychotics?
Typicals (1st class) Atypical 2nd class
94
What are the common ADRs w/ antipsychotics?
Weight gain and Type 2 diabetes
95
What happens when DA is affected?
relief of psychosis and can cause EPS
96
What happens when serotonin is affected?
suppresses DA and protects from EPS Can have weight gain
97
What happens when Alpha 1 is affected?
adrenaline orthostatic hypotension and dizziness
98
what happens when M1 is affected?
anticholinergic SE but may protect against EPS
99
What happens when H1 is affected
weight gain and drowsiness
100
What is the treatment algorithm for schizophrenia?
Atypical different atypical or typical clozapine add atypical or typical to clozapine
101
What is clozapine?
1st atypical and a mixed antagonist typically used only in pts who have failed other agents due to its strict monitoring of WBC affects that can lead to agranulocytosis
102
What are the ADRs for Clozapine?
NO EPS, NO Tardive dyskinesia (TD), NO effect on prolactin Hypersalivation weight gain hypotension sedation
103
What is Olanzapine?
Atypical and mixed antagonist worst anti-psychotic high metabolic impact weight gain orthostatic hypotension
104
What is Quetiapine?
atypical and mixed antagonist DOC for Parkinson's since it only blocks D2 receptors
105
What are the ADRs of Quetiapine?
low risk of EPS and TD sedation mild hypotension weight gain headache SE less severe than clozapine and Olanzopine
106
What is Risperidone
2nd atypical and SDA good if trying to stay away from Benzos
107
What are the ADRs of Risperidone?
not good for EPS low dose very sedating
108
What is Geodon (ziprasidone)?
Atypical and SDA has cardiac risk (prolonged QT interval)
109
What is invega (paliperidone)
Atypical and SDA active metabolite of risperidone
110
What are the ADRs of invega?
less risk of EPS more prolactin elevation sedation and orthostatic hypotension
111
What is lurasidone?
Atypical good but very expensive
112
What is ABILIFY?
Atypical and DA partial Agonist/ 5-HT Antagonist SHOULD BE FRONT LINE (used alot) Blocks D2 when DA is high and activates D2 when DA is Low VERY CLEAN (minimal ADRs)
113
What are the typical adverse effects of antipsychotics?
Extrapyramidal Symptoms BIGGEST W/ RISPERODONE
114
What does Benztropine (Cogentin) do?
Blocks ACh anticholinergic effects
115
What are Extrapyramidal effects?
Happen from all typicals and some atypicals related to blockage of D1 DA receptors Acute dystonia Pseudoparkinsonism Akathsia Tardive dyskinesia Metabolic changes w/ atypicals
116
What is Acute dystonia and how to treat?
Twisting repetitive motions Treated w/ benedryl and cogentin but will have anticholinergic effects these restore effects of DA and ACh
117
What is Pseudoparkinsonism and how to treat?
Presents w/ Parkinson's s/s DA blockage causes imbalance of DA and ACh treatment is to block ACh or to reverse blockage of DA
118
What is Akasthisia and how to treat?
Inner restlessness treated by decreasing dose of drug causing issues also by adding a beta blocker and/or BZDs (Ativan)
119
What is Tardive dyskinesia and how to treat?
This is the biggest limitation of typicals central movements (blinking, lip smacking, involuntary central movements) NO EFFECTIVE TREATMENT -cogentin makes worse w/ anticholinergic affects
120
What is Neuroleptic Malignant syndrome?
must have 5 of the following - change in mental status - incontinence - tachycardia - CPK elevation - Leukocytosis - tremor - tachypnea or hypoxia MUSCLE RIDGITY is the HALLMARK sign
121
How to treat NMS?
Atypicals w/in 7 days use muscle relaxors (Dantrium) and DA agonists fluid replacement temp reduction supportive care
122
What are the signs of Metabolic syndrome?
Any of the 3 - abdominal obesity - HTN - Impaired fasting glucose - Decreased HDL - Elevated Triglycerides
123
What is Bioavailability (BA or F)?
Total amount of drug that reaches circulation anything above 70% is considered good
124
What is bioequivalence?
same everything Generic band vs brand
125
What is Clinical/therapeutic equivalence?
Same drug outcome but doesn't have to get to the outcome the same way.
126
What is potency?
amount of med needed to achieve pharmacodynamic response used in toxicity ONLY SIGNIFICANT if fewer SE w/ more potent agent or admin less often
127
What does pharmacokinetics mean?
What the body does to the drug
128
What does Pharmacodynamics mean?
Effects of drug on the body
129
What is absorption?
Time required for dose to reach circulation bypassed by IV
130
What is distribution?
Time required for dose to arrive at desired site of action
131
What characteristics does a drug need to penetrate the BBB?
small molecule size low pH non-protein binding balance of fat solubility
132
What does protein binding have to do w/ drugs?
drugs bind to proteins in the blood low protein = more free drugs in circulation = ADRs
133
What is the normal Albumin levels?
3.5-4.5
134
What is biotransformation (metabolism)?
way of getting drug ready for elimination kidney or liver(99%) Source of a lot of drug interaction
135
What is the cyt p450 system?
system in liver responsible for most all metabolism major site of drug interaction
136
What is a metabolite?
Transformed molecule during metabolism aren't always less active can be more active than parent drug
137
What is a half life t1/2?
time required for 1/2 dose to be eliminated requires 6-7 t1/2 to be out of system
138
What is steady state?
amount of drug admin = amount of drug eliminated only time a pt can be objectively assessed requires 5-6 t1/2 to achieve ss
139
How is absorption affect in the elderly?
Delayed gastric emptying decrease splanchnic blood flow elevated gastric pH impaired intestinal motility
140
How is distribution affected in the elderly?
influenced by age increased t1/2 decreased protein binding = more free drug in circulation
141
How is renal excretion affected in the elderly?
50% decline by 70 y.o. BUN good predictor (5-25)
142
What drugs can be life-threatening if stopped cold turkey?
Benzos Opiates (Opioids) CNS stimulants Most psychoactive meds