Pharmacology Exam 2 Flashcards
1
Q
Liraglutide: Indication and distribution
A
Primarily - DM2
Also used as an anorexiant
highly bound to protein
2
Q
Anorexiant MOA
A
Sympathomimetic amines → stimulate the satiety centers in the hypothalamus and limbic regions
- noradrenergic, dopaminergic, or serotonergic pathways
3
Q
Anorexiants: Contraindications
- General
- Liraglutide
- Lorcaserin
A
DM - can cause hypoglycemia
Liraglutide - Pregnancy: due to wt loss
Lorcaserin -
- Pregnancy due to category X
- other drugs that increase serotonin
- <18 yo
4
Q
Anorexiants: ADRs
- General
A
Hypoglycemia - decreaed intake
CNS overstimulation and agitation, confusion, insomnia, dizziness, hypertension, headache, palpitations, arrhythmias, dry mouth, mydriasis, dysuria, constipation, vomiting, diarrhea, and impotence
5
Q
ADRs
Liraglutide
A
N/V/D
- Hypoglycemia
- Suicidal Ideation
- Slowed gastric emptying – may alter other drug’s absorption
6
Q
ADRs
Lorcaserin
A
Suicidal ideation
stimulate ADRs
euphoria/hallucinations
priapism/prolactin
CBC changes
hypoglycemia
7
Q
Anticonvulsants (AEDs): Precautions
A
- Increased risk for suicidal thoughts
- Monitor seizure activity
- associated with fetal defects
- suicidal ideation
- lactation
8
Q
Anticonvulsants: Topiramate MOA
A
Inhibition of carbonic anhydrase → may lead to increased renal bicarb LOSS → metabolic acidosis
Inhibition of carbonic anhydrase can also lead to increased ammonia levels
9
Q
Phenytoin (Hydantoin)
- MOA
- Blackbox Warning
- Common Hypersensitivity
- Newborn who have been exposed
A
- blocks Na+ - decreased potential
- IV < 50mg/min in adults and 1-3mg/kg in peds
- Phenytoin-induced hepatitis is a common hypersensitivity
- Newborns need Vit K
10
Q
Phenytoin (Hydantoin): Common Drug Interaction
A
IBUPROFEN – increases dilantin lvls
11
Q
Phenytoin monitoring
A
LFTs,CBC with diff, UA
Drug levels
Assess for phenytoin hypersensitivity syndrome → fever, rash, lymphadenopathy → typically weeks 3-8
12
Q
Phenytoin (Hydantoin): Education
A
Good oral hygiene – tenderness
Urine may look pink, red, or reddish brown
DM - inhibits glucose stimulated insulin release - hyperglycemia
13
Q
Phenytoin indication
A
Seizures, status epilepticus
14
Q
Carbamazepine indications
A
epilepsy, bipolar disorder, trigeminal neuralgia, aggressive behavior
15
Q
Carbamazepine: MOA - including additional
A
Decreases the amount of Na+ going into cortical neurons → decreases action potential → decreased seizure activity from interrupting the abnormal neuronal discharge
Alos: anticholinergic, antidiuretic, antidysrhythmic, and antidepressant activity
16
Q
Carbamazepine: Metabolism
A
Self-induced – therapeutic ranges may fall
17
Q
Carbamazepine: Precautions
-include Black Box Warning
A
Intraoccular pressure – due to anticholinergic affects
grapefruit juice increases drug levels
Decrease TSH
Black Box Warning: SJS - Screen asian patients for HLA-B*1202 gene
Black Box Warning: May cause blood dyskrasias – leukopenia, thrombocytopenia, agranulocytosis, and aplastic anemia
18
Q
Carbamazepine: screening
A
SJS and toxic epidermal necrolysis → particularly among asians
Screen asian patients for HLA-B*1202 gene
19
Q
Carbamazepine: Contraindications
A
pregnancy: CATEGORY D
Hypersensitivity to Carbamazpines or TCAs,
hx of bone marrow suppression,
concurrent administration with MAOs
20
Q
Carbamazepine can decrease levels of the following drugs:
A
Beta blockers, warfarin
21
Q
Carbamazepine: Monitor
A
Baseline CBC, chemistry, LFT, Renal function, CMP, TSH/ T4 → then frequently → then every 3-4 mo if nrml
Carbamazepine → drug levels
22
Q
Lamotrigine: Indications
A
seizure, bipolar disorder, mood
23
Q
Lamotrigine: MOA
A
decraese sodium channels and inhibits the presynaptic release of glutamate and aspartate in the neuron
24
Q
Carbamazepine: Side Effects
A
N/V, dizzy, drowsy, DRY MOUTH, feels like swollen tongue
25
Lamotrigine: Precautions
- includingn Black Box Warning
Multi-organ failure - DIC → begin as fever or lymphadenopathy
BLACK BOX WARNING
Life-threatening rashes: SJS, TEN, and rash-related death → more likely in peds
Coadmininstration with valproate may increase risk of rash
26
Lamotrigine: Drug interactions
Many → due to CYP450
Estrogen → decrease Lamictal
Rifampin → decreases Lamictal
Valproate → increased chance of life threatening skin rash
27
Succinimides [ethosuximide (Zarontin)]:
- Indication
- Pregnancy
Indication: Seizures
Appears safe in pregnancy
Birth control → succinomides may decrease effectiveness of birthcontrol
28
Zosinamide:
- Indication
- Drug Interactions
Seizures
Used with other carbonic anhydrase inhibitors (topiramate, acetazolamide, dichlorphenamide) → may increase risk of metabolic acidosis
29
Zosinamide: Distribution
extensively bound to erythrocytes
- 40% bound to proteins
30
Topiramate: Indication
Gabapentin: Indication
T - Seizures, migraine prophylaxis
G- Seizures, migraine prophylaxis
31
Gabapentin and Topiramate: Metabolism
G: Not metabolized -- excreted unchanged in kidney
T: Isn't metabolized a lot
32
Gabapentin : Side Effects
aggression/hostility
suicidal ideation (all AEDs)
33
Topiramate: Adverse effects
vision problems
oligohydramnios and hyperthermia
inhibition of carbonic anhydrase → may lead to increased renal bicarb LOSS → metabolic acidosis
Inhibition of carbonic anhydrase can also lead to increased ammonia levels
dizziness, drowsiness, fatigue
impaired concentration/memory
nervousness, speech problems
nausea, weight loss
ataxia
photosensitivity
behavioral problems, mood problems
anorexia
34
Topiramate: Monitoring
electrolytes (esp bicarbonate)
intraocular pressure
body temp/sweating
35
Perampanel:
- Indication
- MOA
- SE
Indication: Seizurs
MOA: AMPA antagonist
SE: Hosility, aggression, agitation, anger, homicidal
Dizziness and gait disturbances
36
Levetiracetam:
- Indication
- Metabolism
- SE
Indication: Seizures
Metabolism:
Less than 10% protein bound
Doesn't use CYP450
SE: Alopecia --> reversible
37
What are the cardiac effects of TCA antidepressants?
- tachycardia d2 inhibition of norepinephrine uptake and anticholinergic effects when TCAs block acetylcholine
- slowing of depolarization contributes to a prolonged QRS and subsequent QT interval.
38
Which malignant neoplasm is carbidopa-levodopa known to activate?
Melanoma
39
How do you dc lorazepam (Ativan)?
- Decrease the dose by 0.5 mg per week, then by 0.25 mg for the last few weeks.
- Switching to a shorter-acting benzodiazepine, not a long-acting agent.
40
Benzodiazepines increase the levels of what two drugs?
TCAs and digitalis
41
TCA: adverse reactions
- Histamine: drowsiness and weight gain
- Tachycardia due to decreased norepinephrine reuptake and anticholinergic
- Prolongation of QRS and PR/QT intervals
- Anticholinergic adverse effects are common and can include dry mouth, constipation, urinary hesitancy or retention, blurred vision, sedation, orthostatic hypotension, weight gain, nausea and vomiting, gynecomastia, and changes in libido
- older adults: anticholinergic and norepinephrine effects→ confusion, orthostatic hypotension, and falls
42
Why shouldn't you use MAOIs when you are on TCAs?
can cause hyperpyrexia
43
TCA contraindications
- Cardiac disorders: alpha-adrenergic blocking effect and quinidine-like effect on the myocardium
- MAOIs → hyperpyrexia
- High risk of suicide
44
TCA precautions
- Overdose can be fatal - makes them less safe to use in patients who are a high risk for suicide
- Glaucoma, prostatic hypertrophy, & urinary incontinence: d2 anticholinergic effects
- Older adults: anticholinergic and norepinephrine effects→ confusion, orthostatic hypotension, and falls
- Be alert for an energizing effect that precedes depressive symptom remission because this may contribute to sufficient neurocognitive activation to follow through with a suicidal plan
45
TCAs MOA
- Inhibit reuptake of serotonin and norepinephrine
- Histamine
- Anticholinergic effects
46
Common TCAs
Amitriptyline (Elavil)
Doxepin (Sinequan)
Imipramine (Tofranil)
nortriptyline (Pamelor, Aventyl)
trazodone
47
4 MAOIs
Phenelzine (Nardil),
isocarboxazid (Marplan), tranylcypromine (Parnate), and selegiline (Emsam)
48
MAOI MOA
Irreversibly inactivating the enzymes (MAOs) that metabolize norepinephrine, serotonin, and dopamine, thereby increasing the bioavailability of these neurotransmitters
Prevent breakdown of tyramine
49
MAOI food resctrictions
No food with tyramine → cured foods, fermented foods, citrus
50
Which SSRI is pregnancy category D?
paroxetine
51
SSRI meds
fluoxetine
sertraline
paroxetine
fluvoxemine
citalopram
escitalopram
52
Titrating off SSRIs
When stopping → titrate down → 5 half-lives per dose change
Fluoxetine does not need to taper down because very long half life.
A single dose of fluoxetine as the last step in tapering off other SSRIs is helpful in avoiding withdrawal symptoms
53
Why is there an increased risk of suicide during the first 6-8 weeks of taking an SSRI?
Lag time in receiving the full therapeutic effect, while there is an increase in neurocognitive activation early in initiation of the drug.
Therefore, patients have greater energy to act on suicidal thoughts.
54
SSRI adverse effects
Most common are nausea and sometimes vomiting, headache, light-headedness, dizziness, dry mouth, increased sweating, weight gain or loss, exacerbation of anxiety, and agitation. Sexual side effects
55
SSRI drug interactions
1. MOAIs - serotonin syndrome
2. Lithium-Increased lithium levels, increased serotonergic effect
3. Antipsychotics-Increased EPSEs
4. Benzodiazepines -Increased benzodiazepine half-life
5. TCAs -Increased TCA serum levels → toxicity -Displacement of TCAs from serum proteins → increased cardiac effects
6. St. Johns wort → serotonin syndrome
7. Betablockers → bradycardiaa, syncope, increased levels fo SSRI
56
Bupropion (Wellbutrin) MOA
Norepinephrine and dopamine reuptake inhibitor
57
Mirtazapine (Remeron) MOA
Central pre-synaptic alpha-2 antagonist.
Antagonist of 5HT2 and 5HT3 receptors.
Inhibitor of histamine H1 receptors and alpha 1 and muscarinic receptors.
58
Bupoprion (Wellbutrin) contraindications
Mirtazapine (Remeron) contraindications
W: seizures or risk of developing seizures
M: 14 days of taking MAOIs
59
Bupoprion (Wellbutrin) adverse effects
insomnia (up to 40%), headache, agitation, dizziness, diaphoresis, nausea and vomiting, xerostomia, and constipation. Tachycardia and cardiac arrhythmias may occur
60
Mirtazapine (Remeron) adverse effects
sedation, dry mouth, increased appetite, constipation
61
Antipsychotic drugs:
Haloperidol, Thioridazine, Chlorpromazine
62
Typical antipsychotics MOA
block dopamine D2 receptors
inhibit histamine, cholinergic, and alpha adrenergic receptors
63
Typical Antipsychotics adverse effects
EPS- akathesia, dystonic reactions, parkinsonism;
Hyperprolactinemia;
sedation; weight gain; anticholinergic side effects; orthostatic hypertension;
decreased seizure threshold (low potency); sexual dysfunction;
photosensitivity.
64
Dopamanerigics Indication and MOA
Parkinsons
Increases dopamine or dopamine like activity
65
Atypical antipsychotic drugs
Aripiprazole (Abilify), cariprazine (Vraylar), lurasidone (Latuda),
olanzapine (Zyprexa, Zyprexa Zydis IM), quetiapine (Seroquel),
risperidone (Risperdal, Risperdal M-Tabs, Risperdal Consta)
66
Atypical antipsychotics: MOA
Block serotonin receptors in the cortex, which blocks the usual ability of serotonin to inhibit the release of dopamine. Thus, more dopamine is released to the prefrontal cortex, which reduces the negative symptoms of schizophrenia
Block D2 receptors → less so than typical antipsychotics
Variously affect adrenergic, histaminic, and cholinergic receptors
67
Cloazapine:
- Drug class
- Used for
- Major SE
- Monitor
Antipsychotic - severe granulocytosis → reserved for severe refractory schizophrenia
Falling WBC count (fever, lethargy, bruising, sore throat, flu-like symptoms) → can be fatal within 24 to 72 hours → IDENTIFY EARLY
weekly CBC before 1 weeks worth of meds are picked up
68
Atypical antipsychotics: adverse effects
Weight gain → metabolic syndrome
Seizures, dry mouth, weight gain, diabetes,
hyperprolactinemia, dizziness, orthostatic hypotension, tachycardia, sleep disturbance, constipation, and rhinitis
Less risk of developing EPS, TD, and NMS compared to typical antipsychotics
69
Dopamanergics: Amantadine
Contraindicated: Kidney issues → bc excreted unchanged in the kidney
70
5 Basic Pathogen Types
Gram+ Cocci: SSE
Gram- Cocci: H flu, Neisseria, Moraxella
Gram- Bacilli: EKP, ESP, Salmonella, and Shigella
Pseudomonas Aeruginosa
Anaerobes - Bacteriodes
71
5 Basic Pathogen Types AND their clinical associations
Gram+ Cocci: SSE
Infection --> skin, soft tissue, respiratory, GI/GU
Gram- Cocci: H flu, Neisseria, Moraxella
Infection --> AOM, sinusitis, bronchitis, Neisseria--meningitis, GU
Gram- Bacilli: EKP, ESP, Salmonella, and Shigella
Infection --> EKP--UTI and GI, ESP, Salmonella, and Shigella--GI
Pseudomonas Aeruginosa
Infection --> pneumonia, skin, various
Anaerobes - Bacteriodes
Infection --> GI, aspiration pneumonia
72
Gram+ Cocci: SSE
- associated with what infections
skin, soft tissue, respiratory, GI/GU
73
Gram- Cocci: H flu, Neisseria, Moraxella
- associated with what infections
AOM, sinusitis, bronchitis, Neisseria--meningitis, GU
74
Gram- Bacilli: EKP, ESP, Salmonella, and Shigella
- associated with what infections
EKP--UTI and GI, ESP, Salmonella, and Shigella--GI
75
Pseudomonas Aeruginosa
- associated with what infections
pneumonia, skin, various
76
Anaerobes - Bacteriodes
- associated with what infections
GI, aspiration pneumonia
77
PCNs cover what types of bacteria?
Gram+ (SSE) (Skin, soft tissue, resp)
78
PCNs extended spectrum cover what types of bacteria?
Less Gram +, More Gram - EKP, ESP (GU/GI)
B lactamase Gram+ (skin, soft tissue, Resp)
79
Tetracyclines cover what types of bacteria?
Gram- (SKIN, GU/GI)
Atypicals - chlamydiae, mycoplasma, protozoan parasites;
MRSA
Gram+ step pneumonia
80
Sulfonamides cover what types of bacteria?
Gram- EKP (GU)
Gram+ MRSA (SKIN)
81
Which antibiotics attack the cell wall of bacteria?
B-lactams
- PCNs
- Cephalosporins
- Monobactams
- Carbapenems
Glycopeptides
- Vacomycin
Bacitracin
82
Which antibiotics attack DNA or RNA synthesis?
Fluoroquinolons
- Cipro
- Levoflaxacin
- Moxifloxacin
Rifamycins
- Rifampin
83
Which antibiotics attack bacterial plasma membrane?
Polymyxins
Lipopeptide
84
Which antibiotics attack the ribosomes of bacteria?
- Aminoglycosides
- Tetracyclines
- Macrolides
- lincosamides
85
Which antibiotics attack the folic acid pathway?
- Sufonamides
- trimethoprim
86
Which antibiotics attack Mycolic acid synthesis?
Izoniazid
87
1st Generation cephalosporins
- Drug Names
- Bacteria Type
Cefazolin (Ancef),
cephalexin (Keflex), cefadroxil
Bacteria: Gram+ (SSE)
very little Gram-
88
2nd Generation cephalosporins
- Drug Names
- Bacteria Type
Cefotetan (Cefoten), cefoxitin (Mefoxin)
Cefaclor (Ceclor), cefprozil, cefuroxime (Ceftin)
Bacteria: Gram+ (SSE)
weak Gram-
89
3rd Generation cephalosporins
- Drug Names
- Bacteria Type
Cefotaxime (Claforan), ceftazidime (Fortaz) , ceftriaxone (Cipro)
cefdinir (Omnicef), cefditoren (Scpectracef), cefpodoxime proxetil (Vantin), ceftibuten (Cedax), cefixime (Suprax)
Bacteria: Weak gram+, Strong Gram -
EKP, ESP, H flu, Neisseria, some enterobacteriacceae
B-lactamase
90
4th Generation cephalosporins
- Drug Names
- Bacteria Type
cefepime (Maxipime)
Bacteria: Enhanced Gram-, polymicrobial,
ESP, EKP, SSE, H flu, Neisseria, P. Aueroginosa
91
5th Generation cephalosporins
- Drug Names
- Bacteria Type
Ceftaroline (Teflaro)
Bacteria: Gram+, Gram-
MRSA, DRSP
92
Cephalosporin + B lactamase inhibitor
Ceftazidime - avibactam
Ceftolozane-tazobactam
93
Gram+ Cocci:
- bacteria
- location of infections
SSE
Skin, soft tissue, respiratory, GI/GU
94
Gram- Cocci:
- bacteria
- location of infections
H flu, Neisseria, Moraxella
AOM, Sinusitis, bronch
Neisseria - meningitis, GU
95
Gram- Bacilli:
- bacteria
- location of infections
EKP, ESP, Salmonella, and Shigella
Infection --> EKP--UTI and GI, ESP,
Salmonella, and Shigella--GI
96
Pseudomonas Aeruginosa: Location
Infection --> pneumonia, skin, various
97
Anaerobes - Bacteroides: Location
Infection --> GI, aspiration pneumonia
98
What treats SSE?
Gram+
PCNs, carbapenenms, macrolides, clindamycin, cephalosporins, fluoroquinolones
99
What treats H. Influenzae, Neisseria, Moraxella
Gram-
Macrolides, carbapenems, fluoroquinolones, Ceph 3&4
100
EKP
ESP
Salmonella
Shigella
Gram-
Ceph 2, 3, & 4
TMP-SMX &Fluoroquinolones
Stronger Gram-
carbapenems, fluroquinolones, Aminoglycosides
101
Pseudomonas: which meds treat
Fluoroquinolones, aminoglycosides
102
Bacteroides: which meds treat
Carbapenems, Clindamycin, Tetracyclines
103
Carbapenems: which bacteria
Listeria
Gram+ → many
Gram- → most
Anaerobic bacteria → most
104
Carbapenems: adverse reactions
n/v/d, rash, drug fever
SEIZURES
105
Vacomycin:
- MOA
- Which bacteria
Large molecule → can’t use porins
Prevent cell wall synthesis
Binds to d-alanyl-dalanine portin of the peptide side chain precursor or peptidoglycan subunits → units can’t access PBPs
Bacteria:
Gram+ due to molecule size --> can't use porins of Gram-
MRSA,VRSA
Cdiff
106
Vancomycin: Toxicity and Adverse Reaction
Toxicity
Nephrotoxicity and hearing loss
Adverse
Red man’s syndrome → red, itchy, rash → slow down infusion
107
Daptomycin:
MOA
Bacteria
Adverse
MOA
Binds to bacterial cytoplasmic membrane → effects enzymes needed for cell wall synthesis
Gram+
MRSA, PCN resistant S. Pneumoniae,VRE
POOR in lungs → not for pneumonia
Adverse
Reversible myopathy
Phlebitis, rash, eosinophilic pneumonia, GI upset
108
Colistin
MOA
Bacteria
Adverse
MOA
Cationic → + charge allows drug to bind to negatively charged lipopolysaccharide molecules in the outer membrane → displaces Ca++ and Mg++ → increased permeability of cell wall
Gram-
P aeruginosa
E coli, Klebsiella
H flu
Toxicity
Associate with nephrotoxicity and neurotoxicity
109
Rifampin:
Important
MOA
Bacteria
Adverse
Usually use in a combo
Or prophylaxis of Neisseria and H Flu
NOT MONOTHERAPY because easy to develop resistance
MOA
Inhibit RNA polymerase
Gram
Mycobacteria and staphylococci
Adverse
CYP450 inducers
GI
Causes orange/red color of tears, urine, and other body fluids
110
Tetracyclines mainly used to treat:
Atypical: rickettsiae, chlamydiae, and mycoplasmas
Tetracyclines are broad spectrum: Gram+/-, anaerobic and aerobic
