Pharm Flashcards
(135 cards)
1
Q
GABA role and system
A
inhibitory
role: regulator, sedation, sleep, pain, anxiety
system: inhibitory interneuron
2
Q
glutamate role and system
A
excitatory
role: excitatory and regulates Ca2+ influx; neuroplasticity, learning, pain, sensory regulation and perception
system: NMDA AMPA receptors throughout brain
3
Q
Ach role and system
A
role: movement
system: pontomesencephalo-tegmental, medial septal nucleus, basal nucleus of Meynert
4
Q
norepi role and system
A
role: alertness, attention, stress, fear, anxiety, SNS
system: locus ceruleus
5
Q
dopamine role and system
A
role: movement; reward, pleasure, motivation, focus, conditioning
system: nigrostriatal, mesocorticolimbic
6
Q
serotonin role and system
A
role: depression, anxiety, sleep, appetite, pain, aggression, impulse
system: raphe nuclei
7
Q
streptokinase
A
- Derived from bacteria so less expensive
- MOA: enhance conversion of plasminogen to plasmin to enhance fibrin degradation & subsequent clot
- AE: severe allergic reaction
8
Q
alteplase
A
- MOA: analogue of human tPA to enhance conversion of plasminogen to plasmin to enhance fibrin degradation & subsequent clot
- AE: severe bleeding (reverse w aminocaproic), wait 24 hrs to start ASA
9
Q
reverse severe bleeding via tPAs with __________
A
aminocaproic acid
10
Q
tenecteplase, reteplase
A
- Mutated longer acting forms tPA
- MOA: enhance conversion of plasminogen to plasmin to enhance fibrin degradation & subsequent clot
- AE: severe bleeding (reverse w aminocaproic), wait 24 hrs to start ASA
11
Q
aspirin (ASA)
A
- MOA: Irreversible COX Inhibitor that inactivates platelet COX-1 enzyme
- Long-duration decrease thromboxane (TXA2)
- Ideal preventative if patient can tolerate
- AE: bleeding, hemorrhage, allergic reaction (asthmatic), GI
12
Q
dipyridamole
A
- MOA: Phosphodiesterase inhibitor prolongs cAMP (plt agg inhibitor)
- Administered in prep w/ aspirin (ERDP/ASA)
- Increases serum adenosine (antiplatelet actions)
- Increases prostacyclin levels (counteracts TXA2 effects)
13
Q
clopidogrel
A
- MOA: Activated in liver to ADP receptor antagonist to inhibit clot formation (see cascade above)
- Alternative if can’t take aspirin
14
Q
warfarin
A
- MOA: competitively inhibits vitamin K epoxide reductase (VKOR) to decrease vit K regeneration (co-factor necessary for clotting)
- AE: major CYP inhibitor – drug interactions, bleeding (reverse with vit K)
- Slow onset – 5 days (not for emergencies)
- Indications: hx of thromboembolisms, afib, stroke prevention
15
Q
dabigatran
A
- MOA: competitive antagonist of thrombin=direct thrombin inhibitor
- Short-acting, rapid onset (benefits in early stroke treatment), orally available, Doesn’t block other clotting factors, Less drug interactions than warfarin
- AE: bleeding but has a short half-life so self-limiting
- Indications: active thrombosis, prevention of stroke in afib
16
Q
SSRI (fluoxdetine, escitalopram) MOA
A
selectively blocks the 5HT reuptake transporters (SERT) to increase 5HT
17
Q
SSRI adverse and blackbox
A
o Adverse
- Nausea, GI, sexual dysfunction, drug interactions (CYP2D6), weight changes, anxiety
o Black box
- Serotonin syndrome – OD can cause hyper -tension, -thermia, -reflexia, -stimuation (HR)
• Tx: cyproheptadine – 5HT receptor antagonist to block serotonin
- Suicidal ideation in pediatrics
18
Q
SNRI (venlafaxine, desvenlafaxine) MOA
A
Blocks SERT and NE reuptake transporters (NET) to increase 5HT and NE
19
Q
buproprion MOA
A
blocks dopamine reuptake transporters (DAT) and NET to increase DA and NE
for depression, SAD, quit smoking
20
Q
TCA MOA (-triptylines)
A
blocks NET and SERT with higher affinity for NET to increase 5HT and NE
21
Q
TCA adverse and OD
A
o Adverse
- Hypotension, constipation, urinary retention, blurry vision, dry mouth, tachycardia, weight gain, sedative, v-fib arrhythmia (due to fast Na+ channel myocyte block)
o Overdose
- Can be toxic, 3Cs – cardiac, convulsion and coma
• Tx: bicarbonate to direct drug away from heart via pH, saline for HoTN
22
Q
trazodone MOA
A
antagonist at SERT and 5HT2A to change 5HT auto-receptors over time
23
Q
mirtazapine MOA
A
a2 auto-receptor and 5HT2A receptor antagonist, also histamine antagonist
24
Q
trazodone adverse
A
priapism, weight gain, sedative
25
MAOi MOA (Phenelzine, selegiline)
inhibits MAO inhibits metabolism of NE and serotonin
| 3rd line antidepressant
26
MAOi adverse
- MAO inhibits metabolism of tyramine, which can build up and increase catecholamines
• Avoid tyramine rich foods (wine, cheese), can have dangerous CV and HTN effects
- High toxicity, HTN, serotonin syndrome, agitation, anxiety, stroke, seizures
- Avoid with sympathomimetics!
27
lithium MOA
uncompetitive inhibitor of inositol monophosphatase, an enzyme that regenerates inositol, so Li depletes free inositol (within 5 days) and stabilizes mood by slowing neurotransmitter receptors (5HT) coupled to PLC 2nd messenger system
28
lithium adverse
Weight gain, polydipsia and polyuria, hypothyroidism, tremor
Teratogen (Ebstein's anomaly), renal dysfunction, cardiac arrhythmias, nephrogenic DI, neurotoxicity
29
valproate MOA
potent anticonvulsant and mood stabilizer, exact MOA of mood stabilization unknown
VG Na+ C blocker, also blocks VG T-Type CC channels
• Maybe blocks VGNaC, enhances GABA, inhibits GSK3 and decreases PKC
30
valproate adverse
Hair loss, weight gain, hepatotoxic, pancreatitis
| 1st trimester teratogen= spina bifida, low IQ; also excreted in breast milk
31
lamotrigine adverse
SJS-TENS, dizzy, diplopia
32
lamotrigine MOA
anticonvulsant VGNaC, weak voltage-gated calcium channel (VGCC) inhibitor, reduces glutamate release
33
carbamazepine/oxcarbazepine MOA
potent VGNaC blocker anticonvulsants
34
benzodiazepines (diazepam, lorazepam, clonazepam) MOA
anxiolytic, sedative, muscle relaxant, anticonvulsant and amnestic effects via GABA, potent centrally acting
35
baclofen MOA
GABAb agonist that increases potassium conductance promotes hyperpolarization
- Enhances presynaptic inhibition and decreases release of excitatory NTs
36
gabapentin MOA
inhibits voltage-gated calcium channels (VGCC), reduces excessive glutamatergic activity, CNS depressant/ analgesic properties for pain
37
carisoprodol MOA
metabolized to meprobamate (barbiturate) to activate GABAa which leads to CNS depression
38
riluzole MOA
* Block Na channels and decrease Ca influx, reduces glutamatergic activity
* Used for neuroprotective properties in ALS
39
tizanidine MOA
a2 adrenergic agonist that reduces muscle spasms and pain
| for ALS, MS and stroke
40
cyclobenzaprine MOA
antimuscarinic
| TCA like
41
orphenadrine MOA
antimuscarinic and antihistamine
42
metaxalone MOA
CNS depressant that relaxes via central pathway but NT changes unknown
43
botox MOA
blocks Ach release to produce flaccid paralysis and reduces spasms
44
tizanidine adverse
dry mouth, drowsy, hypotension
45
L-Dopa MOA
• Gets converted to DA by dopa-decarboxylase in brain (3%) peripherally (97%)
• Anti-Parkinson effect is related to central D2 agonism on post-synaptic neurons
- If used alone, L-dopa mostly effect peripheral neurons which is not ideal
for parkinsons
46
Carbidopa
inhibits dopa-decarboxylase without crossing BBB
| • ↓peripheral conversion; lets more L-Dopa go to brain
47
bromocriptine MOA
ergot related non-selective but potent D2 receptor agonist
for parkinsons
48
apomorphine MOA
non-ergot non-selective DA agonist
for parkinsons
49
pramipexole MOA
D3 agonist
for parkinsons
50
ropinirole MOA
D2 agonist
for parkinsons
51
Selegiline and rasagiline MOA
MAO-B inhibitor that prolongs brain DA
52
Tolcapone, Entacapone MOA
COMT inhibitor that increase L-Dopa into brain
53
Amantadine MOA
antiviral that increase DA and is adenosine antagonist
54
Amantadine adverse
seizure, psychosis, restlessness, liver dysfx, edema, livdeo reticulari
55
Tolcapone, Entacapone adverse
dyskinesia, insomnia, nausea, orthostatic HoTN, vomiting, confusion, dizziness; tolcapone has block box for liver toxicity
56
benzotropine, trihexyphenidyl MOA
* Antagonist at muscarinic receptors to ↓unopposed Ach excitation from ↓DA
* Good adjunct with L-Dopa to control drooling and tremor
57
benzotropine, trihexyphenidyl adverse
* Dry mouth, constipation, blurred vision, urinary retention
* Can’t poop, can’t pee, can’t sweat, can’t see – cholinergic
58
Tetrabenzazine (and Deutetrabenzazine – slower onset
Reversible VMAT2 inhibitor that depletes DA and reduces hyperkinesia for Huntington's
59
donepezil MOA
reduce breakdown of central acetylcholine (Ach) = more Ach available to stimulate muscarinic receptors to improve memory & cognition in AD
long half life, 2D6 and 3A4
60
galantamine MOA
reduce breakdown of central acetylcholine (Ach) = more Ach available to stimulate muscarinic receptors to improve memory & cognition in AD
2D6 and 3A4
61
rivastigmine MOA
reduce breakdown of central acetylcholine (Ach) = more Ach available to stimulate muscarinic receptors to improve memory & cognition in AD
short half life
62
Ach esterase inhibitor adverse
GI (diarrhea, drooling), bradycardia, sweating, pulmonary, confusion if OD
63
memantine MOA
antagonizes NMDA receptor to block glutamate excitotoxicity
64
Local anesthesia effects sensory or motor fibers more
sensory
65
Local anesthesia effects delta or motor fibers more
delta
66
Local anesthesia effects myelinated or unmyelinated fibers more
myelinated
67
during inflammation, pH is more _____, so must inject _____ with anesthesia
acidic
| NaHCO3
68
Esters - anesthetic
long
short
surface
tetracine
procaine
benzocaine and cocaine
69
Amides- anesthetic
long
medium
short
bupivacaine, ropivacaine, etidocaine
lidocaine
articaine
mepvacaine - vasoconstricts
70
Naloxone
Mu antagonist for opioid overdose
71
morphine
Mu, Kappa and Delta agonist
hydrophilic
• Decrease immune function, constipation, miosis, itching, flushing, delirium
• Concern for asthmatics (histamine) and renal dysfunction
72
hydromorphone and oxymorphone
more potent than morphine with shorter duration and less histamine
73
fentanyl
full opioid agonist for severe pian
74
remifentanil metabolism
by plasma esterase in blood not in liver
75
methadone
Mu agonist and NMDA antagonist
| sub for heroin addicts
76
oxycodone and hydrocodone
less Mu agonist, but good oral availability
77
codeine
partial Mu agonist with tussive effects
| metabolized by 2D6
78
tramadol
partial Mu agonist with NET and SERT blocking
79
buprenorphine
Mu and Kappa agonist
less severe withdrawal
can't reverse OD with naloxone
80
meperidine
opioid agonist that also blocks SERT
| can cause seizures
81
nalbuphine
kappa agonist
mu antagonist
less addictive potential
82
pentazocine
kappa and mu agonist with less nausea but hallucinations
83
butorphanol
kappa and mu agonist that comes in nasal spray
84
triptan MOA
• 5HT agonist on intracranial blood vessels and sensory nerves to constrict cerebral vessels and decrease pain
1st line MH abortive
85
ergotamine, dihydroergotamine MOA
alpha1 adrenergic partial agonist with non-selective 5HT agonism on vessels
86
ergotamine, dihydroergotamine black box
gangrene and fatal ischemia if used with 3A4 inhibitor
87
lasmiditan
new neuronally active antimigraine agents (NAAMA)
5HT1F agonist that targets brainstem and trigeminal neurons to reduce release of CGRP and major peptide mediator without vasoconstriction
88
valproate and topiramate for MH
block VGNaC and augment GABA
89
benzodiazepams MOA
bind to ionotropic GABAa receptors and facilitate Cl influx when endogenous GABA activates GABAa to hyperpolarize membrane – allosteric!
90
benzodiazepams with no active metabolites
lorazepam
| oxazepam
91
benzodiazepam overdose
flumazenil
92
buspirone MOA
5HT1a auto-receptor partial agonist that has a non-BZD mechanism to alter serotonin firing, no rebound or withdrawal symptoms
93
SSRI approved for OCD
Fluvoxamine
94
Glatiramer MOA and for what
for MS
• Spares myelin basic protein by acting as a decoy to the immune system
• Induces and activates regulatory suppressor CD8+ T-cells specific for myelin antigen and increases anti-inflammatory IL-10
95
natalizumab MOA and for what
for MS
• Monoclonal antibody to a4 integrin chain on VLA4 – prevents VLA4 from binding VCAM1 so myelin-reactive T-cells can’t cross the BBB
96
ocrelizumab MOA and for what
for MS
| anti-CD20 monoclonal antibody that targets mature B-cells attacking the myelin sheaths of healthy neurons
97
fingolimod MOA and for what
forMS
| binds to sphingosine PO4 receptors and reduces CNS lymphocyte penetration
98
terflunomide
for MS
active metabolite of leflunomide
inhibits pyridimine synthesis --> immunosuppression
99
dimethyl fumartae
for MS
| activates NRF2 to immunomodulate
100
drugs of abuse increase _______ ______
mesocorticolimbic dopamine
101
```
drugs of abuse MOAs
EtOH
barbiturate
GHB
marijuana
```
EtOH - GABAa Cl influx and B-endorphin release
barbiturate - allosteric GABAa activator
GHB - GABAb agonist --> K+ influx
marijuana - binds cannabinoids
102
methamphetamine MOA
taken up by DAT, binds to VMAT and reduces vesicular packing of DA
promotes reverse transport
103
methamphetamine abuse signs
pruritis, bruxism, anorexia, aggression, anxiety, psychosis, seizures, paranoia
104
methylene dioxymethamphetamine (MDMA) ((Ecstasy)) MOA
taken up by SERT, NET & DAT and binds to VMAT and acts as reverse transporter
105
pharm tx for EtOH abuse
disulfiram
naltrexone
acamprosate
106
pharm tx for opioid abuse
methadone
| buprenorphine/naloxone
107
first generation antipsychotics
D2 antagonists
haloperidol, chlorpromazine
treats positive symptoms
has EPS adverse
108
atypical antipsychotics
5-HT2A antagonism, weaker D2 antagonists
aripiprazole, risperidone
less EPS adverse, more metabolic syndromes
109
clozapine
good for treatment resistant schizophrenia after 2 failures
minimal EPS risk
high agranulocytosis risk
110
valbenazine MOA
inhibits VMAT2 to release DA
| to reduce tardive dyskinesia
111
black boxes for antipsychotics
long QT
| increase mortality in elderly
112
caffeine MOA
* Competitive adenosine receptor antagonist that decreases blood flow to brain
* Also, a PDE inhibitor that blocks cAMP degradation, so increase cAMP
113
nicotine MOA
* Increases influx of Na+ and is excitatory by acting at cholinergic receptors
* Activates mesocorticolimbic dopamine
114
methylphenidate (Ritalin) MOA
blocks DAT & NET transporters; increases synaptic dopamine and norepinephrine
115
amphetamine (Adderall) MOA
increase monoamine release via reverse transport at DAT & NET transporter
reverse transporter
116
atomoxetine MOA
* Selective Inhibition of NET increases synaptic NE similar to TCA antidepressants
* Increased NE in reticular system should increase attention
117
acute relief of status epilepticus
lorazepam/diazepam
if no response -> IV fosphenytoin -> IV phenobarbital -> valproate or anesthesia
118
phenobarbital
GABA mimetic used as 2nd line anticonvulsant
119
phenytoin MOA
for epilepsy
| bind to inactivated state of voltage gated Na channels and prevent reopening and prolong inactivation of neurons
120
phenytoin kinetics
* 1st order kinetics at low dose
| * Zero order kinetics at saturation
121
phenytoin adverse
* Gingival hyperplasia, hepatotoxic, arrythmias, CV toxicity, HoTN
* Teratogen – Fetal Hydantoin Syndrome
122
carbamazepine adverse
for epilepsy
• Aplastic anemia, agranulocytosis, skin disorders
• Sign of toxicity – vestibular, diplopia, hematologic
123
levetiracetum MOA
for epilepsy
| binds presynaptic synaptic vesicular protein SV2A to increase GABA and reduce glutamate
124
ethosuximide MOA
for epilepsy
| “petit mal drug” that inhibits voltage gated T-Type Ca 2+ channel
125
gabapentin and pregabalin
for epilepsy
| bind to a2delta subunit of Ca channel
126
tiagabine MOA
inhibits GAT1 neuronal GAB reuptake site to increase synaptic GABA
127
cephalosporins that cross the blood brain barrier (5)
ceftazidime, ceftriaxone, cefotaxime, cefuroxime, cefepime
128
treatment for cocaine OD
BZDs
129
succinylcholine
depolarizing neuromuscular blocker that binds and blocks open gate; tetanic contraction followed by flaccid paralysis
130
what can tubocurarine / atracurium / rocuronium cause?
malignant hyperthermia
131
dantrolene
treat malignant hyperthermia by blocking RyR1 Ca influx
132
IV anesthetic examples (6)
```
thiopental
methohexital
propofol
etomidate
dexmedetomidine
ketamine
```
133
inhaled anesthetic examples (4)
halothane, isolurane, desflurane, methoxyfluarane
134
relationship of BGPC to induction of anesthesia
inverse
| such that lower BGPC has faster induction
135
relationship of MAAC to potency of anesthesia
inverse
| such that lower MAAC has greater potency
