Drugs (ALL) Flashcards
1
Q
Disulfiram
A
used for substance abuse with alcohol
causes unpleasant run if alcohol is consumed
but no s/s if no alcohol is not consumed
2
Q
Naltrexone
A
used in substance abuse with alcohol
used as a opiod antagonist = blocks euphoria!
in both cases = blocks the measurable effects of the substances
3
Q
Acamprosate
A
pharm for maintaining abstinence with alcohol
reduces some of the unpleasant feelings with abstinence
4
Q
Nicotine replacement therapy
A
we want to substitute cigarettes with a pharmaceutical source nd then you gradually withdraw the nicotine
similar to how methadone used for heoin addicts
5
Q
bupropion
A
dealing with smoking abstinence
atypical antidepressants and is structurally different to amphetamine
helps by reducing cravings
DO NOT USE with MAOI
6
Q
Varenicline
A
smoking abstinence
partial nicotine agonist
most effective aid in smoking cessation
promotes the release of DA so it is pleasurable
7
Q
Methadone
A
opioid agonist
opioid abuse treatment/ abstinence
longer 1/2 life with less euphoria
8
Q
Buprenorphine
A
opioid agonist/ antagonist
partial mu agonist ad kappa antagonist which helps alleviate the cravings
can be used for abstinence treatment
9
Q
Flumazenil
A
this is the antidote for Benzos
dealing with benzo. and the pharm of abstinence maintenance
you taper off the drug slowly over. few months
10
Q
FGA
A
first generation conventional antipsychotics
these are cheaper
more extrapyramidal side effects (tar dive dyskensias) = Parkinson like symptoms (because think about how the mechanism of this drug is to block dopamine)
NO to Parkinson’s patients on these drugs
11
Q
neuroleptics
A
AKA FGA
a type of first generation anti psychotic
12
Q
SGA
A
second generation antipsychotic (atypical)
more expensive
more metabolic effects seen –> weight gain etc.
risk for CV events and premature death
NO to alziemers patients taking
13
Q
Chlorpromazine
A
first generation antipsychotic that is low potency
AE = sedation, orthostatic hypotension, anticholinergic side effects
Occasionally causes photosensitivity reactions & neuroendocrine effects
Prolongs QT interval
14
Q
Haloperidol
A
H = HIGH
high potency FGA
**** Generally preferred for initial therapy EPS symptoms earlier in txn Lower frequency of all other AE Prolongs QT interval Cheaper
15
Q
Selective serotonin reuptake inhibitors (SSRIs)
A
MOA = blocks the reuptake of 5 - HT and thus increases the concentration in the synapses
since only blocks 5 - HT there less side effects
AE:
Nausea
Agitation/insomnia
Sexual dysfunction
Weight gain
Decreased platelet aggregation (still low risk)
Serotonin syndrome (usually in 1st 3 days of tx)
Withdrawal syndrome w/ abrupt d/c (taper)
In late pregnancy: withdrawal & pHTN in the newborn
16
Q
Fluoxetine
A
a type of SSRI that is the prototype
17
Q
Serotonin and Norepinephrine Reuptake Inhibitors (SNRIs)
A
similar mechanism as SSRI
not as safe as SSRI
MAIN AE = dose related hypertension
18
Q
venlafaxine
A
SNRI prototype
19
Q
Tricyclic Antidepressants (TCAs)
A
both a 5-HT and NE reuptake inhibitor
Not very selective!
Also can impact histamine/H receptors, ACh/M receptors, and various others
AE (d/t H & M receptors): Orthostatic hypotensio Anticholinergic effects Sedation **cardiac toxicity** Seizure risk Suicide risk Toxicity = dysrhythmias, heart block
20
Q
Amitriptyline
A
TCA
21
Q
Monoamine Oxidase Inhibitors (MAOIs)
A
Mechanism: inhibition of MAO (liver/intestine)
- -> Decreased breakdown of NE, 5-HT, DA
- -> MAO also breaks down tyramine
22
Q
Nonselective MAOI
A
deals with both MAOI - A and MAOI - B
leads to =
Increase in 5-HT, NE, DA
Breaks down tyramine
23
Q
MAOI B (selective MAOI)
A
leads to an increase in DA
- -> Selegiline
- -> Rasagiline
Parkinson treatment as well
24
Q
Bupropion
A
atypical antidepressant
Mechanism unclear, may be d/t DA/NE reuptake block
-No effect on ACh, 5-HT, or H
Adverse:
- Agitation, tremor, insomnia; seizures in high doses
- Weight loss
- Agitation
- GI upset, constipation
**No weight gain or sexual dysfunction issues! ***
25
Lithium
mood stabilizer connected to bipolar disorder
MOA: unclear
PK: PO. Short ½ life (rapid renal excretion)
Must be administered multiple times per day
Caution in renal disease
Renal excretion is affected by [Na+]
VERY LOW THERAPEUTIC INDEX!!!!
MUST MONITOR DRUG LEVELS
Goal range = 0.4-1mEq/L
ideally 0.6-0.8mEq/L).
no treatment for overdose!
26
Valproate (bipolar considerations:)
traditional antiseizure medication
undersand can be used to help with modo stabilizing as well
Valproate has largely replaced lithium as drug of choice
Faster onset & greater margin of safety
Lithium is better at reducing suicide risk & relapses
27
carbamazepine (bipolar considerations)
a traditional antiseizure medication
can also be used as a mood stabilizer for bipolar
28
Benzodiazepines
Mechanism: potentiation of GABA (ceiling effect exists)
PK: highly lipid soluble (easy BBB crossing)
Hepatic metabolism w/ active metabolites (most)
```
Adverse:
CNS depression
Anterograde amnesia
Can have paradoxical effects
PO dosing: minimal resp depression, minimal CV effects
Teratogenic (avoid in pregnancy)
```
can be used for INSOMNIA!!!!
29
Zolpidem
Benzo like drugs -->
All act as agonists at GABA receptor
All are schedule IV
30
Ramelteon
melatonin agonist
The only sleep aid that isn’t a controlled substance!!!
Rapid onset, short DOA = helpful for falling asleep, not staying asleep
15x more potent at melatonin receptor than melatonin itself
Melatonin usually secreted along w/ circadian rhythm (darkness/environmental light)
AE: no notable. No physical dependence/abuse
31
Suvorexant
Orexin antagonist -->
Orexin = promotes wakefulness
Used for sleep onset & sleep maintenance issues
```
AE:
somnolence, dizziness
HA
Dry mouth, cough
Physical dependence/tolerance (schedule IV)
```
Caution with OSA/COPD
32
Barbiturates
Mechanism: agonize GABA receptor directly
NO CEILING EFFECT TO SEDATION/RESP DEPRESSION
```
AE:
Respiratory depression death
Sedation general anesthesia
Minimal CV effects at hypnotic doses
CYP450 induction
Tolerance & physical dependence (schedule III)
```
33
buspirone
anxiety treatment
Mechanism: not well established
Binds 5-HT receptors, less so to DA receptors
No GABA effects
As effective as benzos, but no abuse potential/CNS depressant interactions
Anxiolysis develops slowly (weeks)
PK: PO, hepatic metabolism (CYP450), renal elimination
Caution w/ CYP450 inducers/inhibitors (+grapefruit juice)
AE: minimal even in large doses. Dizziness, nausea, HA
34
CNS Stimulation
Different from antidepressants in that they cannot elevate mood w/ CNS excitation
At high enough doses, all can cause seizures
35
Amphetamines
CNS stimulation for ADHD
think this is adder all
Cause release of NE & DA, partially inhibit their reuptake
-Actions CNS & PNS
Adverse:
-CNS: insomnia, restlessness, euphoria, talkativeness, appetite suppression
-CV: tachycardia, increased contractility, vasoconstriction à dysrhythmias, HTN
-Psychosis w/ excessive use
36
Methylxanthines
CNS stimulation for ADHD
| think this is caffeine
37
Modafinil
CNS stimulant for ADHD
38
MMR vaccine
Live virus
39
L- Dopa
thinking about Parkinson's and the want to increase dopamine
* directly activates DA receptors
* SO this is a prodrug that needs to be converted to DA in the CNS BUT in order to do this we need to avoid three things (see below)
40
carbidopa
Decarboxylase inhibitors needed to go with the L- Dopa
| needed in order for L dopa to directly activates DA receptors
41
entacapone
COMT inhibitors
| need in order to allow L dopa to work
42
MAO-B inhibitors
in normal states = MAO B will break down dopamine
so in those with Parkinson's who want to inhibit MAO B in order to have more circulating dopamine
we use this drug in mild to moderate cases
43
Selegiline
MAO B inhibitor
44
rasagiline
MAO B inhibitor
45
Amantadine
Parkinsons and dopamine agonist
| *promotes DA release and inhibits reuptake
46
Dopamine agonists
*NON ergot alkaloid = SELECTIVE DA receptor
Act like dopamine
Less effective then L-Dopa BUT less risk of dyskinesia
47
Pramipexole
dopamine agonist
| less effective then L Dopa but less risk of tarditive dyskinesia
48
Ropinirole
dopamine agonist
| less effective then L Dopa but less risk of tarditive dyskinesia
49
Rotigotine
dopamine agonist
| less effective then L Dopa but less risk of tarditive dyskinesia
50
apomorphine
dopamine agonist
| less effective then L Dopa but less risk of tarditive dyskinesia
51
benzotropine
anticholinergic drug for Parkinson's
Second line drug for tremor
Less effective than L-dopa or DA agonists
Better tolerated
AE
CNS (sedation, confusion, hallucinations)
Peripheral (anticholinergic effects)
52
Cholinesterase inhibitors (AChE inhibitors)
in alziemers patients, ACH is 90% less then in normal patients so want to inhibit the break down
- Donepezil
- Galantamine
- rivastigmine
53
Donepezil
AChE inhibitor
| a reversible drug that is highly protein bound and CNS selective
54
Galantamine
AChE inhibitor
| a reversible drug
55
Rivastigmine
used for AChE in alziembers
| this drug is irreversible and has PNS effects
56
memantine
NMDA antagonist
Can slow cognitive decline due to allowing for normal signaling
We tolerated and minimal AE
57
Immunomodulators: interferon beta
MS
* preferred choice when looking at these two options to stop the progression of the autoimmune
* can stimulate antibody production against drug itself
* special handling
58
Immunosuppressants: mitoxantrone
MS
*inhibits DNA synthesis and repair
*decreased immune cell proliferation
Decreased myelin sheath destructions
59
dalfampridine
Treat distressing or harmful symptoms
helps with the gait issues in a patient with MS
60
Phenytoin
```
traditional seizure medication
prototype
Na+ selective blocker
high toxicity risk
due to metabolizing the liver quickly can become maxed out and leads to high toxicity issue
```
61
Carbamazepine
```
a traditional anti-seizure medication
CNS depression
Bone marrow suppression
Increase in ADH suppression
Derm rashes/ hypersensitive
```
62
Valoprate
traditional seizure medication
Enhances GABA transmission and blocks Na+ like phenytoin
do not use in pregnant women
63
Ethosuximide
Suppression of Ca++ channel in the thalamus
Absence of seizure usage
minimum AE
64
Phenobarbital
Traditional Anti seizure medication
| Potentiates effects of GABA used in anesthesia!!
65
Albuterol
short acting B2 agonist that is used as a bronchodilator
inhaled so less risk of adverse effects!
Immediate onset, peak 30mins, DOA 3-5hrs
Taken PRN to abort acute attacks
If need to take >2x/week, additional drug should be added
66
salmeterol
inhaled long acting bronchodilator = LABAS
Fixed dosing schedule (not PRN)
**** Preferred in COPD
When used as sole therapy in asthma → increased incidence of asthma-associated death (use with a glucocorticoid)
67
formoterol
inhaled long acting bronchodilator = LABAS
Fixed dosing schedule (not PRN)
**** Preferred in COPD
When used as sole therapy in asthma → increased incidence of asthma-associated death (use with a glucocorticoid)
68
terbutaline
bronchodilator = PO beta 2 agonist
PO B2 agonists: only for long term control, not first line
-Dosing is 3-4x/day
69
theophylline
Methylxanthines
broncho dilators
MOA: Block adenosine receptors → relaxation of bronchial smooth m (probably)
Index = 10 -20 (minter blood levels!!!).
20-25 = N/V, diarrhea, restlessness, insomnia
>30 = risk for death d/t cardioresp collapse due to cardio decline
CYP450 inducers → subtherapeutic theophylline levels
CYP450 inhibitors → supratherapeutic (even toxic) theophylline levels
70
ipratropium
```
short acting anticholinergic
MOA:
Block muscarinic (M) receptors in bronchi = decreased bronchoconstriction
USAGE:
Approved for COPD
Also used as alternative therapy for asthma
Inhalation administration to avoid AE
AE:
nhaled drugs really minimal effect
Nasopharyngitis
URIs
```
71
tiotropium
```
long acting anticholinergic
MOA:
Block muscarinic (M) receptors in bronchi = decreased bronchoconstriction
USAGE:
Approved for COPD
Also used as alternative therapy for asthma
Inhalation administration to avoid AE
AE:
nhaled drugs really minimal effect
Nasopharyngitis
URIs
```
72
Beclomethasone
inhaled glucocorticoid
| minimal AE when in haled and can prevent by thrush by washing mouth out
73
Budesonide
inhaled glucocorticoid
| minimal AE when in haled and can prevent by thrush by washing mouth out
74
Fluticasone
inhaled glucocorticoid
| minimal AE when in haled and can prevent by thrush by washing mouth out
75
Leukotriene receptor antagonists
Mechanism: suppression of leukotriene effects
Leukotrienes effects to understand :
Smooth m constriction
Increased blood vessel permeability
Increased inflammatory responses (directly & through recruitment of eosinophils)
Used for maintenance and second line if the person cannot tolerate glucocorticoids
76
Montelukast
Leukotriene receptor antagonists
Rapid absorption
-Peak 3-4hrs
-Highly PB (99%)
```
Liver metabolism
Biliary excretion
AE:
-minimal!
-Rare neuropsych effects
-No CYP450 inhibition or liver injury
```
77
Zileuton
Blocks leukotriene SYNTHESIS
Rapid absorption
-Peak 2-3hrs
Liver metabolism
Renal excretion
AE:
- Liver injury (monitor LFTs)
- Neuropsych effects
- CYP450 inhibition
78
Cromolyn
Mechanism: stabilizes membrane of mast cells = decreased histamine/mediator release decreased inflammation
Does not cause bronchodilation
SAFEST of all the anti-asthma drugs (very rare AE).
Also used for exercise induced asthma (neb) & allergic rhinitis (intranasal)
79
omalizumab
IgE Antibody Antagonist
Mechanism: forms complex w/ IgE that prevents it’s binding with receptors on mast cells
Decreased inflammatory mediator release
AE: viral infections, injection site rxns hypersensitivity reactions
PK: peak 7-8 days, liver metabolism, ½ life 26 days. Takes approx. 1yr for IgE to return to pre-tx levels
80
IL-5 receptor antagonists
monoclonal antibododies --> antiinflammation goal
Mechanism: inhibit IL-5
IL-5 = differentiation/maturation eosinophils
IL-5 inhibition = decreased eosinophils
AE: HA, pharyngitis, fatigue, hypersensitivity rxns
Resilzumab has black box warning d/t anaphylaxis events (0.3%)
81
IL-4 receptor alpha antagonist
monoclonal antibodies used for reducing inflammation
Mechanism: inhibit IL-4
IL-4 = inflammatory cytokine expressed on many immune cell types
Inhibition = decreased cytokine-induced inflammation
AE: injection site rxn, oral herpes, conjunctivitis, antibody development against the drug
82
roflumilast
PDE4 inhibitor = used for reducing inflammation
Used for severe bronchitis primary COPD (not first line)
Mechanism: inhibits PDE4 (enzyme that breaks down cAMP)
PK: PO, peak 1hr, ½ life 17hrs d/t high PB. CYP450 metabolism, urinary excretion
AE: diarrhea, anorexia, HA, back pain, insomnia.
Avoid in pregnancy
Psych rxns can occur that can be as severe as SI
83
Symbicort
glucocorticoid + LABA
84
Advair
glucocorticoid + LABA
85
Combivent
anticholinergic + SABA
86
Phenylephrine
drug for allergic rhinitis
Sympathomimetics
ONLY to relieve congestion
a1 agonism = vasoconstriction, decreased vascular permeability
87
pseudoephedrine
drug for allergic rhinitis
Sympathomimetics
ONLY to relieve congestion
a1 agonism = vasoconstriction, decreased vascular permeability
88
Antitussives
```
drugs for cough
some act in CNS, some peripherally
Helpful for chronic nonproductive cough
Codeine, hydrocodone
Both act in CNS to elevate cough threshold
```
89
timolol
drugs used to treat glaucoma
| beta blockers
90
latanoprost
Increases outflow of AH by relaxing ciliary muscle
AE: ocular hyperemia (engorged vessels)
prostaglandin analogues
91
brimonidine
a2 agonist
Decrease production of AH
AE: dry mouth, ocular hyperemia
92
dorzolamide
Decrease production of AH
Less effective, used as adjunct
Carbonic anhydrase inhibitors
93
azelastine
H1 receptor blocker
| Drugs for allergic conjunctivitis
94
phenylephrine
Drugs for allergic conjunctivitis
Ocular decongestants
can also be used for allergic rhinitis because it is a sympathomimetic and is used to help with congestion only
95
bevicizumab
Macular Degeneration
Blurring of central vision d/t macular injury
Painless, gradual
Leading cause of blindness in older adults
Tx: angiogenesis inhibitors (VEGf inhibitors)
96
salicylic acid
Keratolytic: used for overgrowth/thickening; dandruff, psoriasis, warts, corns
AE: rarely, toxicity with long-term, high-dose use
97
cortisone creams
Glucocorticoids: used for rash/itching
Vary in potency
AE: local reactions, thinning of skin with long-term use (increased with higher potency, dressing, large area)
98
benzo peroxide
acne
First-line tx
AE: peeling, drying
99
azelaic acid
acne treatment
Keratolytic
Suppresses P. acnes
AE: itching, burning, pigment reduction
100
tretenoin
acne txn = retinoid
Vitamin A derivatives
Hyperproliferation of epithelial cells
AE: peeling, drying
101
tacrolimus
topical immunosuppresents for eczema
AE: erythema, pruritis
No systemic absorption
Possible increase in skin cancer risk; avoid direct sunlight
102
psoriasis treatment
Chronic autoimmune disorder
Main sx: plaque formation
Treatment goal: control/minimize symptoms
Topical: glucocorticoids, salicylic acid, coal tar: suppress DNA synthesis, inhibits keratinocytes
Systemic: methotrexate, biologics, TNF agonists
103
Topical minoxidil
Androgenetic alopecia (male pattern baldness)
Other types of alopecia=typically different treatments
MOA: direct vasodilator, MOA unknown, possibly d/t increased blood flow
AE: local allergic reactions
104
acetic acid
outer ear infection
105
amoxicillin
Otitis media: infection, fluid, inflammation of middle ear; outward bulging of TM
Often develops after URI
Observation for 48-72 hours with supportive tx
Abx: high-dose amoxicillin for infants <6m, 6m-2y with confirmed dx, >2y with dx and severe sx
