pharm exam 1 Flashcards
1
Q
TCAs
antidepressant
A
Inhibit reuptake of NE and 5-HT
BUT also block alpha, histamine, and muscarinic receptors –> many SE
2
Q
TCAs, careful with
A
SI, potential for OVERDOSE
3
Q
TCAs are used minimally in depression, but also used for:
A
Chronic pain (TMJ)
Fibromyalgia
Enuresis (bedwetting)
4
Q
TCA toxicity
A
Histamine rec block: drowsy, fatigue, sedation
Cholinergic rec block: blurry vision, tachycardia, urinary retention, dry mouth, memory loss
alpha rec block: cardiac arrhythmia, hypotension, reflex tachycardia
5
Q
Other SE of TCA
A
Sexual dysfx
SIADH
Weight gain
6
Q
Can TCA be used in pregnancy?
A
YES, surprisingly
7
Q
Serious toxicity of TCA
A
Torsades de pointes!!!!!
prolonged QT
Met acidosis
Resp depression
Coma, shock
8
Q
Tx of OD on TCA
A
Cardiac monitor Lavage Charcoal Mg, Isoproterenol, Cardiac pacing for Torsades de pointe Lidocaine, Propranolol, Phenytoin
Na bicarb and KCl
9
Q
TCAs are either
A
Tertiary or Secondary amaines
Tertiary cause more seizures and are more sedating
10
Q
Tertiary amines (TCA)
A
Amitriptyline
Imapramine
block 5HT reuptake (seretonin)
11
Q
Secondary amines (TCA)
A
Nortriptyline
Desipramine
block NE reuptake
12
Q
SSRIs
A
Fluoxetine Sertraline Paroxetine Citalopram Escitalopram
13
Q
SSRIs
A
Depression (DOC) Panic disorder OCD Social anxiety Bulimia Alcoholism
Very safe therap window
14
Q
SSRIs mild SE
A
GI, nausea, weight cange, anxiety, insomnia
Sexual disinterest*
Photosensitivity (LIMIT SUN EXP)
15
Q
Fluoxetine
prototype SSRI
A
More drug intxns than other SSRIs
Impairs glucose levels, avoid in DIABETIC
16
Q
Fluoxetine and Sertraline (SSRI) spec have SE of
A
Anxiety, insomnia
17
Q
With SSRIs, be aware of what type of drug interaction?
A
Opoiods
- pain med will not work
- Serotonin synd
- Inc risk Seizures
18
Q
Avoid this SSRI if you are Diabetic
A
Fluoxetine (prozac)
19
Q
DOC for Depression
A
Citalopram (celexa)
20
Q
SNRI
Seretonin-NE reuptake inhibitor
A
Depression
Neuropathic pain*
Post menopause hot flashes
21
Q
SNRI
A
Inhibit NE and 5-HT but cleaner than TCAs
22
Q
SNRIs (2 drugs)
A
Venlafaxine
Duloxetine
23
Q
Venlafaxine (SNRI)
A
may increase BP
24
Q
Duloxetine (SNRI) bad SE
A
Hepatotoxicity
Glaucoma
25
MAOIs
Dirty drug
| LAST CHOICE
26
MAOIs
Avoid foods w Tyramine (HTN crisis)
With basically any other drug, SEROTONIN SYNDROME (high fever)
27
MAOIS
irrev inhibit MAO which break down NE, DA, and 5-HT
28
MAO-A
inhibit NE, DA, and 5HT in CNS AND Periphery
29
MAO-B
DA in CNS only
30
MAOIs (2 drugs)
Phenelzine
| Selegiline
31
Phenelzine (MAOI)
Use for depression that hasn't responded to other drugs
inhibits both MAO-A and MAO-B
**HTN CRISIS**
32
Selegiline (MAOI)
Depression and
Parkinsons (lower dose)
MAO-B only
33
Buproprion
Use if pts are having sexual dysfx w other Antidepressant meds
34
Buproprion
inhibit DA reuptake
35
SE of Buproprion
Seizure
Anxiety, insomnia, restless, tremor, psychosis
Tachycardic
36
Buproprion is CONTRA in
Seizure pts
37
Other uses for Buproprion
ADHD
Alcoholism
Smoking
38
Mirtazapine
Good if pts have Insomnia, Anxiety, AND depression
DROWSY EFFECT
39
Mirtazapine
block pre-syn a2 which usually inhibits NE and 5HT release
Result: increased amounts of NE and 5HT
40
Mirtazapine
No bad SE like anxiety, insomnia, sexual dysfx
| ONLY DROWSY
41
Atomoxetine
ADHD med
Increases memory/ attention
Good choice for addicts (no euphoria effect)
42
Atomoxetine
selective inhibitor of NE reuptake
SAFE and CLEAN drug
43
SE of Atomoxetine
GI distress
insomnia
Liver damage- but very rare
44
Trazadone
Sleep aid
Pain mgmt
NOT a good antidepressant
45
Trazadone
5HT2a receptor antagonist
46
Trazadone SE
| use rather for sleep and pain
sedating
dizzy
Priapism- rare but serious!!! persistent and painful erection
47
Priapism
persistent and painful erection
SE of Trazadone
48
Mesolimbic pathway
VTA to Limbic system
Emotion
D2 receptors
Positive sx
49
Mesocortical pathway
VTA to frontal Cortex
D4, Seretonin 4a receptors
Negative sx
50
Nigrostriatal pathway
SN to Striatum
| Motor control
51
Tuberofundibular pathway
Hypothalamus to pituitary
| Prolactin
52
Neuroleptic Malignant syndrome
SE of Antipsychotic drugs
Muscle rigidity
change in BP, HR
Block of D2 receptors in Striatum and Hypoth
Tx: Dantrolene (muscle relaxant)
53
"positive" sx of psychotic disorders
D2 pathway, emotion
Overactive DA in Limbic system
Catatonic behavior, disorganized speech and thinking
54
"negative" sx of psychotic disorders
Underactive DA pathways in frontal Cortex
| Depressed, withdrawing from activity
55
Chlorpromazine
"classical" antipsychotic
Use: Psychosis associated with Mania and Drugs of abuse
56
EPS
Extrapyramidal sx
| acute dyskinesias and dystonic reactions, neuroleptic malignant synd, etc
57
Classic antipsychotics run the risk of
EPS
58
Chlorpromazine
low incidence of EPS compared to other classics
59
Chlorpromazine SE
Seizures
Retinal deposits (browning vision)
Sedation, blurry vision
60
Fluphenazine
similar to Chlorpromazine, selective for D2
Less anticholinergic effects, thus more EPS potential (bad)
61
Haloperidol
injected
Classic antipsychotic
for ACUTE situations to pull someone out of psychotic episode
62
Haloperidol SE
injected
Potent D2 blocker
no anticholinergic activity, HIGH EPS POTENTIAL (bad)
63
The 3 types of Classic Antipsychotics we talk about are
Chlorpromazine
Fluphenazine
Haloperidol
64
Atypical Antipsychotic means:
Block 5HT2a receptors AND D2, D4
Alleviate pos and neg sx of psychosis
Lower incidence of EPS
65
Clozapine
Drug of LAST choice out of Atypicals d/t SE of AGRANULOCYTOSIS
```
seizures
hypersalivation
dizzy
tachy
wt gain
```
66
If you are on Clozapine, what do you need to monitor daily
Blood to check for Agranulocytosis
67
DO NOT STOP what Atypical Antipsychotic drug abruptly?
Clozapine bc effects do not persist
| unusual for antipsychotics
68
Olanzapine
A fairly safe Atypical Antipsychotic
| Also used for Bipolar (w Lithium)
69
Olanzapine SE
"Zyprexa Diabetes"
| caution of Hyperglycemia
70
Risperidone
DOC 1st choice for Schizophrenia
71
Risperidone
1st choice
| EPS is very very rare
72
Risperidone SE
Hypotension
Wt gain
Insomnia
Lengthen QT interval*
BUT, overall pretty safe. 1st choice for Schizo
73
Ziprasidone
Antidepressant use
and
Tourettes
Acute mania
74
Ziprasidone
Prolong QT interval
Sedation
Hyperprolactinemia
75
Ziprasidone CONTRA
Seizure hx
76
Quetiapine
VERY SEDATING
| Used to promote sleep
77
Good things about Quetiapine
No agranulocytosis
| Doesn't elevate prolactin
78
Aripiprazole unique trait
Dopamine system stabilizer
brings it back to natural levels
79
Aripiprazole SE
Hyperglycemia
Seizures
Sedation
Decreases esophogeal motility
80
Good things about Aripiprazole
no increase in prolactin
| no effect on QT
81
Lurasidone
Depression associated w Bipolar
don't know much about this drug, new
82
Lurasidone
new drug
hits 30 receptor subtypes
Monitor Blood for: Agranulocytosis and Neutropenia
83
Lithium
DOC for Bipolar
| calming manic state
84
Lithium
Small therapeutic window
85
Lithium SE
Extremely TOXIC in OD
Can lead to Diabetes Insipidus
Competes w Na for reabsorption (watch salt intake)
86
Lithium CONTRA
Hypothyroid
Pregnancy
with NSAIDs
87
Valproic acid
Use for Rapid Cycling manic/depressive episodes
88
Valproic acid
Bipolar pts who do not respond to Lithium
89
Valproic acid
Anticonvulsant
| mechanism unknown
90
Valproic acid SE
Surgical bleeding (dental)
GI, sedation, wt gain
91
Valproic Acid CONTRA
Pregnancy (remember, all anticonvulsants aren't safe in pregnancy)
92
Gabapentin
Also used for rapid cycling
minimal drug interactions
93
Carbamazepine
Use: Refractory Bipolar disorder
used w Lithium
94
Carbamazepine SE
Induce CYP450
| SJS/TEN risk!!!
95
Testing for human antigen required prior to using this to prevent SJS/TEN
Carbamazepine
96
Lamotrigine
prevention of Relapse following mania
Acute mania
97
Opioids work at the pre-syn and post-syn terminal
pre: decrease Ca, thus decrease neurotransmitter release (Glutamate and Substance P)
post: Mu agonist, hyperpolarize pain receptor and inhibiting the post-synaptic potential
98
Does neuropathic pain respond to opioids?
No
Gabapentin and Amitriptyline are better for neuropathic pain
99
What receptors are responsible for dysphoria? (bad)
Kappa
| Delta
100
What do pupils look like with Opioids?
Constricted
| may concert to dilation in comatose
101
Tolerance for Opioids develops after a few days, EXCEPT with
Miosis
Seizures
Constipation
tolerance never develops
102
Tolerance involves which parts of the nervous sytem
Thalamus
| Spinal cord
103
Addiction involves
reward pathway
104
Overdose Triad of Opioids
Respiratory depression
Pinpoint pupils
CNS depression
105
Tx of Opioid OD
ABCs
| Naloxone (Narcan)
106
MAOI and Opioids?
BAD NEWS BEARS
Seretonin Syndrome!!!
107
Drug intxns w Opioids
```
Meperidine
Dextromethorphan
MAOI
SSRI
Antipsychotic
Sedative hypnotics
```
108
CONTRA to opioid use
```
Partial agonist w full agonist
Pregnant
Head injury
Impaired lung, liver, or kidney fx
Some endocrine dz
```
109
Heroin and pregnancy
Can cross placental barrier
| Cause respiratory depression and dependence in baby
110
Morphine
SEVERE pain, strong agonist
Stimulates ALL receptors
best effective when injected (high first pass if given orally)
111
Morphine dosing
Standard dose is 10 mg SubQ or IM
all other drugs based off of this
112
Hydromorphone (Dilaudid)
Mod-Severe pain
| Good if pt has Renal dysfx
113
Hydromorphone (Dilaudid) is very similar to Morphine other than
Metabolites dont accumulate, less itching SE
114
Methadone (Dolophine)
Long term pain control
Maintenance tx of addicts
Low dose: prevent withdrawal
"Hard to treat" types of pain
115
Methadone (Dolophine
Mu agonist
| Block NMDA
116
GOOD effect of Methadone
pts less likely to become tolerant to this
117
Meperidine
"odd duck" drug
| Used in Obstetrics: less respiratory depression in babies
118
Meperidine
Mu agonist
119
Meperidine SE
Seizures
Tachycardia
Pupil dilation
*Seretonin synd if given w MAOI
120
Meperidine
Use in pregnancy!
121
Fentanyl (sublimaze)
Short surgical procedures
(with midazolam)
or
Longer surgeries
122
Fentanyl (Sublimaze)
Short duration! very lipid soluble
transdermal patch: slower release
123
Fentanyl (sublimaze) bad things/SE
Abuse potential is HIGH
Truncal rigidity
Drug intxns likely
124
In general, short acting drugs are
WORSE, higher risk for abuse potential
125
Hydrocodone (Vidocin)
Mod-severe pain
often combo w Acetaminophen
Does NOT work well w SSRI
126
"workhorse" opioid drugs
given often
Hydrocodone (vicodin)
| Oxycodone (oxycontin)
127
Oxycodone
mod-severe pain
| often combo w Acetaminophen (just like hydrocodone)
128
Oxycodone
huge drug of abuse
can be given in different forms to decrease abuse potential
129
Codeine
good cough suppressant (low dose)
mild-moderate pain
130
Codeine
converted to Morphine
131
Codeine CONTRA
children
132
Pentazoicne/Naloxene
moderate pain
Kappa agonist
Partial Mu agonist
133
Pentazocine/Naloxone
Dysphoria!!
| recovering addicts or those afraid for abuse use this bc it has LOW abuse potential
134
Buprepnorphine
Use: maintenance tx of addiction
decreases craving
(combine w Naloxone)
135
Buprenorphine
Mu partial agonist
does NOT cause euphoria
136
Buprenorphine and pentazocine/Naloxone
Low abuse potential
137
Tramadol
Mild-moderate pain
| Comb w Antidepressants to treat seizures
138
Tramadol
Weak Mu agonist
139
Tramadol SE
mild: dizzy, sedation, constipation, nausea
140
Tramadol CONTRA
with Antidepressants, can cause Serotonin syndrome and seizures
141
Dextromethorphan
Cough suppressant
Drug of abuse in teenagers
NOT a pain med
142
Dextromethorphan
blocks NMDA receptors
abuse potential
143
Anything with MAOIs
be cautious of Serotonin syndrome
144
Naloxone (Narcan)
DOC for Opioid overdose
now can be comb w some opioids to prevent abuse
145
Naloxone (Narcan)
Opioid antagonist
give until pupils dilate
146
How long is Naloxone (Narcan)'s duration?
Short! only 2 hours
Might have to give every couple hours until opioid wears off
Repeat dosing
147
Naltrexone
Another opioid antagonist
Tx of opioid addicts in Healthcare professionals
148
Naltrexone
Healthcare addicts
| Recovering alcoholics
149
Naltrexone
Orally effective
| 24 hour long drug (why its good for healthcare, can last their whole shift)
150
Naltrexone SE/ CONTRA
Liver toxicity w chronic use
CONTRA hx of liver dz
151
Parkinsons
death of DA neurons in Substantia Nigra
152
Lewy bodies
clumps of a-synuclein and other proteins in nerve cells, associated with Parkinson's
153
L dopa alone
end result: increase DA levels
Crosses BBB, then converted to DA
need high doses, only 1-3% gets into CNS
154
L dopa WITH Carbidopa
now 10% can get into CNS
bc Carbidopa inhibits dopa-decarboxylase, the enzyme that breaks L dopa down, inhibits SE also
155
SE of L-dopa/carbidopa
```
N/v
Dyskinesa
Hypotension
Arrhythmia
Depression, anxiety, agitation
```
Psychosis possible
156
Imp drug combo considerations with L-dopa/carbidopa
with MAOI: HTN crisis
| with Vit B6: decrease effectiveness of drug
157
CONTA to L-dopa/carbidopa
```
Psychosis
Closed glaucoma
Cardiac dz
active PUD
Malignant melanoma
```
158
Considerations w L-dopa/Carbidpoa
pt compliance
Has to take med 3-4x per day
"on off phenomenon"
159
On off phenomenon
Apomorphine used to treat
| D2 receptor agonist, pulls people out of the off phase
160
Selegiline
Parkinson tx
inhibits MAO-B in CNS (inhibits DA metabolsim)
161
Selegiline SE
Insomnia
| Severe HTN
162
Selegiline CONTRA
do NOT combo with Meperidine: Seretonin Syndrome
163
MAOB-I
Parkinson tx
Selegiline
Rasagiline
Safinamide
all inhibit MAO-B in the CNS only
which means does not affect DA in the periphery
164
COMT inhibitors
Tolcapone
| Entacapone
165
Tolcapone
inhibit DA and L-dopa metabolism in CNS and periphery
166
Tolcapone SE
Hepatic failure
167
Entacapone SE
Orange urine
confusion, hypotension, abd pain, insomnia
168
Stalevo
| combo
L-dopa, Carbidopa, Entacapone
169
Entacapone
inhibit DA and L-dopa metabolism in PERIPHERY only
170
COMT
usually metabolizes L-dopa and DA, that is why inhibitors of these drugs help tx Parkinson
171
DA receptor agonists
Bromocriptine
Ropinirole
Pramipexole
Rotigotine
continue to be effective as Parkinsons progresses bc act directly on receptors*
172
First line therapy for Parkinson
DA receptor agonists
Bromo
Ropinirole
Pramipex
Rotigot
173
Bromocriptine
can cause Erythromelalgia (vascular peripheral hand/feet spasm)
174
Ropinirole and
| Pramipexole
the "go to"
| Monotherapy in Mild parkinson, soothing response to L-dopa in Late parkinson
175
Ropinirole
DOC for restless leg syndrome (RLS)
176
Pramipexole
FDA warning: Heart Failure
177
Rotigotine
transdermal patch for Parkinson and Restless leg synd
178
Apomorphine
Tx temporary relief "rescue" for off period in pts on optimized L-dopa
179
Apomorphine SE
Nausea
| take anti-emetic b4, like trimethobenzamide
180
When giving anti-emetic with Apomorphine, avoid
targets to 5HT, like Ondansetron (can cause severe HTN, LOC)
blocks to D2 receptors, like Prochlorperazine
181
SE of DA agonist
Bromocriptine
ROpinirole
Pramipexole
Rotigotine
```
Anorexia, n/v
Postural hypotension (beg of tx)
Cardiac arrhytmias (DISCONTINUE if happens)
```
182
What causes erythromelalgia
Bromocriptine
183
Amantadine
increases DA neurotransmission
184
Amantadine
Antiviral for flu
| Early/mild Parkinson
185
Amantadine SE
Livedo reticularis - reddish blue spotting of skin
186
Amantadine overdose
Toxic psychosis
| Convulsions
187
Anticholinergics to treat Parkinson
Benztropine
Trihexyphenidyl
restores DA/Ach balance in striatum
188
Benztropine
| Trihexyphenidyl
modest anti-parkinson
Improve rigidity,t remor
Little effect on bradykinesia
189
Benztropine
| Trihexyph
usually used in addition to DA therapy
190
Pimavanserin
Atypical Antipsychotic
| For tx of psychosis and dellusions/hallucinations associated w Parkinson
191
Pimavanserin mechanism
inverse agonist/antagonist for 5HT receptors
192
Pimavanserin
NOT approved for tx of dementia assoc w Alzheimers, increases mortality
193
do NOT use Pimavanserin in
Alzheimers
194
B-amyloids and Tau proteins
plaques and tangles associated with Alzheimers
195
What causes Alzheimers
degeneration of Cholinergic neurons
Neuronal atrophy
196
Cholinesterase inhibitors for Alzheimers
Donepezil
Rivastigmine
Galnatamine
197
ACHe Inhibitors for ALzheimers
taken once/day
Inc brain activity and improve fx
may slow progression of dz
198
Memantine tx for Alzheimers
NMDA receptor antagonist,
reduces excitotoxic effect of glutamate and slow degeneration
199
Memantine CONTRA
do not give WITH Meperidine
200
Downfall of L-dopa for tx
Effectiveness goes down over time
Does not affect progression of dz; DA neurons continue to degenerate
201
SE of Cholinesterase inhibitors
GI most common
| n/v/d, stomach cramps
202
Amphetamines
Adderall
| Ritalin (methylphenidate)
203
Amphetamines
- adderal
- ritalin
increase release of DA, reverse DA transport thru the DAT
204
Bad things about Amphetamines (Adderall and Ritalin)
Increase BP
Pulmonary edema
Heart Failure
205
Amphetamines
```
Alertness
Euphoria
Excitement
Aggression
Paranoia
Delusions
```
206
Meth
| ICE, crystal meth
May produce Amphetamine psychosis
pale skin, body odor, hyperthermia, dental problems
"meth bugs"
"meth mouth"
207
More serious SE of Meth
seizures, organ damage, stroke, heart attack
208
Meth
| ICE, crystal meth
Rapid physical and psychological dependence
209
Chronic users of meth
Permanent damage to Noradrenergic and Serotonergic neurons, loss DA transport, Slow motor rxn, Memory loss, personality change
210
Cocaine
```
Alertnes
Euphoria
Anxiety
Hyperactivity
Tremor
Twitch
Pupil DILATION
```
211
Cocaine systemic effects
```
tachycardia
vasoconstriction
HTN
bronchodilation
hyperpyrexia
```
212
Medical use of cocaine
Local anesthetic
| Vasoconstrictor
213
Chronic use of cocaine
```
Reduce brain activity
Anxiety
Insomnia
Paranoia
Hallucinate
Repetitive behavior
Nasal congestion
Perforated nasal septum
```
214
Cocaine mechanism
inhibit DA reuptake
Physical and psychological dependence (severe withdrawal)
215
Cocaine overdose/toxicity
```
Ventricular tachy
V- Fib
Stroke
Cerebral hemorrhage
Seizure
```
216
Tx for Cocaine withdrawal
Bromocriptine (decreases craving)
217
Nicotine
Mild euphoria
Increased arousal
Appetite suppression
218
Nicotine mechanism
Increase 5HT and DA release
intense psychological and physical dependence
219
Nicotine withdrawal is so difficult partly because
Nicotinic receptors are in excess still 1 month after stopping
Normalize by 6-12 wks after
220
Tx for Nicotine withdrawal
Replacement therapy
Bupropion
Varenicline
Behavioral tx
221
NDMA "Ecstacy"
Feelings of peaceful
Empathy
Closeness
Trust, BUT
followed by: depression, confusion, anxiety, paranoi
222
NDMA "ecstasy"
inc Serotonin activity by blocking reuptake AND stimulating receptors
223
NDMA "ecstacy" SE
Hyperthermia
Dehydration
Kidney failure can --> DEATH
Memory loss
224
Long term use of NDMA "Ecstacy"
Decrease level of Serotonin in Cerebral cortex
225
Marijuana
```
Mild euphoria
Well being
Altered sense of time
Difficult to concentrate
Introspection
Tranquility
```
226
Marijuana SE
anxiety
dec memory
impaired reasoning
un-motivated
227
Marijuana SE
Hyperemesis
Cyclic vomiting
```
Bronchial irritaiton
risk of CA
Decreased ovulation
Decreased Testosterone
Low birth weight
FETAL malformations
```
228
Synthetic "cannabinoid" agonist
Psychoactive effects
Paranoid
hallucinate, mood swing, aggression, violent outburst, elevated HR and BP
not tested for human effects
229
Mary J pharmaco
Very lipophilic, long 1/2 life, quickly absorbed
no physical dependence
230
Mary J mechanism
Stimulate pre-syn CB1 receptors to inhibit Ach release
231
LSD/ Mescaline/ Psilocybin
Euphoria
Visual hallucinate
"bad trips" flashbacks
Increase BP, HR, flushing, dilated pupils
232
Synesthesia
LSD (and Mescaline/psilocybin)
Senses are all mixed up- colors are heard, sounds are seen
233
LSD
acts on serotinin receptors in brain
NO dependance, does NOT stimulate DA pathways
234
PCP (angel dust)
Developed as anesthetic
May cause analgesia WITH agression
often produces Psychosis
235
PCP (angel dust)
| Ketamine
NMDA antagonist
236
How to treat Psychosis caused by PCP (angel dust)?
Haloperidol
237
Ketamine and GHB
"date rape"
238
GHB mechanism
weak GABA agonist
239
Inhalants cause
toxicity in MANY organs
| Lesions in brain white matter!
240
Nitrous oxide
Peripheral neuropathy with chronic use
Frequently abused by DENTISTs
241
Nitrous oxide
rapid, short acting pleasure
OD can be fatal
242
Amyl/butyl nitrite
"poppers" "snappers"
Euphoria, light headed, blurry vision, HA, nausea, hypotension, tachycardia
Smooth muscle relaxant
243
Naltrexone CONTRA
treat alcoholism, pt doesn't even want it- curbs craving
Liver failure
causes hepatic damage
244
Acamprosate
treat alcoholism
analog of GABA
restores normal balance of GABA and glutamate
245
Disulfuram
treat alcoholism
acetaldehyde builds up, person feels awful BUT SE can be severe: vomiting, sweating, CP, hypotension, blurred vision, shock
246
Topiramate
treat alcoholism
Anticonvulsant
| mechanism not well understood
247
Barbiturates
works INDEPENDENT of GABA
No ceiling effect, dangerous bc levels can just keep rising
248
Barbiturates
| "phenobarbitol"
Bind to GABA, stimulate Cl influx
249
Barbiturates CONTRA
Porphyria (abnormal heme synthesis)
Pulmonary insufficiency
With other CNS drugs (supra-additive w alcohol)
250
Benzos
| "pam" mostly used for
Anxiety
| Insomnia
251
Benzos "pam" CONTRA
Pregnant
Sleep apnea
Elderly
252
Benzos "pam" are safer because
Have ceiling effect
| Dependent on GABA
253
Do not stop ____ abruptly
Benzos "pam"
254
Flurazepam and Temazepam
Insomnia
"hangover" drowsy effect
255
Diazepam and Lorazepam use:
Status Epilepticus
256
Midazopam
Short acting
| Given IV b4 short procedures
257
Flumazenil use
Hyperinsomnia (too much sleeping)
258
Flumazenil
Benzo "pam" ANTAGONIST
competes w benzos for GABA spot
259
Flumazenil (hyperinsomnia tx) CONTRA
Seizure hx
260
The Z drugs for insomnia
Zolpidem
Zaleplon
EsZopiclone
261
The Z drugs
bind to Benzo1 subtype of GABA
Strong and rapid sedative effects
High margin of safety; GOOD
262
Morning drowsy is unlikely with the Z drugs (except Eszopliclone) because
they have a short duration of action
besides EsZ
263
Suvorexant
| insomnia tx
Orexin antagonist
264
Caution w Suvorexant (insomnia tx)
Those w Depression, can worsen
265
Suvorexant (insomnia tx) CONTRA
Narcolepsy
266
Ramelteon mechanism
Melatonin analog
resets sleep/wake cycle
267
Chloral hydrate
Children sedation during dental procedures
268
Chloral hydrate
Children dental
nursing home
chronic care
269
Chloral hydrate
converted to Trichloroethanol which acts similar to barbs on GABA receptor
LOW margin of safety (just like Barb)
270
Chloral hydrate is dangerous d/t low margin of safety
Respiratory and vasomotor depression
Cardiac arrhythmia
Long term: liver damage, fatal intoxication
271
Buspirone use
Generalized anxiety
272
Buspirone
Relieves anxiety w/o causing sedation
Full agonist at 5HT1a presynaptic
Partial agonist at postsynaptic
273
Tiagabine
| anticonvulsant
block GABA reuptake
274
Vigabatrin
Refractory partial
| Infantile West spasm
275
Vigabatrin
Inhibit GABA-T metabolism (breakdown)
276
Vigabtrin SE
Visual field problems
Retinal damage
Agitate, confusion
277
Infantile West synd tx
Clonazepam
| Vigabatrin
278
Long duration Benzos "pam"
Diazepam
| Flurazepam
279
Intermediate duration Benzos "pam"
Alprozolam
Oxazepam
Lorazepam
280
Pregabalin (Lyrica)
Generalized anxiety disorder
Others:
Neuropathic pain
Fibromyalgia
Post op pain
281
Pregabalin
GABA analog, binds to Ca channels
CONTRA: pregnancy
282
Gabapentin (neurontin)
Adjunct partial and gen tonic-clonic seizure
Neuropathic pain
Bipolar (off label)
283
Gabapentin
Gaba analog- increase GABA release
CONTRA: pregnancy
284
Does Gabapentin have drug interactions?
NO
and Pregabalin has very little
285
Phenobarbitol
Stimulate GABAa receptor, prolong opening of Cl channel
partial seizures
gen tonic-clonic
286
Levetiracetam
Partial seizures
Myoclonic
Tonic clonic
287
Levetiracetam mechanism
SV2A, bind synaptic vesicular protein
Minimal drug intxns, SAFE to use w others
288
Phenytoin (dilantin)
Partial seizures
| Gen tonic-clonic
289
Phenytoin (dilantin) mechanism
prolongs inactivation of Na; decreases Glutamate activity
290
Phenytoin pharmaco
1st order at low doses
Zero order at therapeutic and HIGH doses; small change in dose can cause BIG change in plasma levels
(Caution)
291
Phenytoin (dilantin) SE
Gingival hyperplasia
Risk of SJS
CONTRA: pregnancy
292
Carbamazepine
DOC for Partial seizures
293
Carbamazepine other use (other than Partial seizures)
Trigeminal neuralgia
294
Carbamazepine mechanism
Block Na channel; decrease Glutamate activity
295
Carbamazepine SE
SJS risk, screen for HLAB1502 before use
Aplastic anemia and Agranulocytosis
CONTRA: pregnancy
296
Lamotrigine
Inactivate Na channels; decrease Glutamate activity
used for Partial seizures, but NOT DOC (Carbamazepine is)
297
Lamotrigine risk
SJS
| Pregnancy CONTRA
298
Topiratmate
Partial
Gen tonic-clonic
Migraine PREVENTION
299
Topiramate
Block Na channe; decrease Glutamate
300
Topiramate SE
Acute myopia
| Glaucoma
301
Levetiracetam
Minimal drug intxns
302
Ethosuximide
DOC for Abscence seizures
303
Ethosuximide mechanism
Inhibit low threshold Ca channels
304
Ethosuximide SE
Hiccups!
305
Ethosuximide's metabolism is inhibited by
Valproic acid
306
Valproic acid
Mixed seizures
| bc mechanism blocks Ca and Na channels, may enhance GABA
307
Valproic acid SE
Hepatotoxic (need to monitor LFTs)
| CONTRA pregnancy
308
Toxicity of all Anticonvulsants
Teratogenic; AVOID in pregnancy
Rebound seizures in withdrawal
OD CNS depression(rarely lethal, do NOT treat w CNS stimulant)
Suicidal thoughts
309
SJS risk, those that block Na channels
Phenytoin
Lamotrigine
Carbamezapine*
Valproic acid
310
Anticonvulstants cause what to be less effective
Birth control!
If pregnant, causes birth defects, congenital heart defects, neural tube defects
311
Esters
shorter duration of action, but
| increased TOXICITY
312
Mechanism of anesthetics
Block Na channels
inhibit neuron firing
313
Efficiency of anesthetic block is better in
Rapidly firing axons
314
Anesthetic block is enhanced in
Elevated K+ bc the membrane is already depolarized
315
Anesthetic block is diminished in
Elevated Ca++ bc the membrane is hyperpolarized
316
Lipid solubility does what to the duration of anesthetic action?
More lipid soluble = longer duration of action
317
Amides are metabolized in
Liver by CYP450
318
Esters are metabolized in
Plasma by butylcholinesterase
319
Have to caution with Liver damage with Amides or Esters?
Amides
met in the Liver
Toxicity is more likely in pt with Liver dz or Reduced Liver blood flow
320
Methemoglobinemia
Prilocaine metabolite
321
Allergic reactions are rare with Amides or Esters?
Rare with Amides
322
Procaine- short duration of action
Diagnostic infilration nerve block
metabolite product PABA; allergic rxn and inhibit sulfa
323
Tetracaine
Obhto (eye) use, retrobulbar procedure
and
Spinal anesthesia
324
Benzocaine
Very lipophilic
always in Non-ionized form
Topical only; sunburn
325
Cocaine
Reduce dental bleeding
CNS and CVD SE; caution
326
Lidocaine- prototype AMIDE
Infiltration block
Epidural anesthesia
NOT for spinal block (risk of TNS)
327
Prilocaine
Highes rate of clearance of Amides
328
Prilocaine SE
Risk of Methemoglobinemia
Too much methemoglobin in blood, SOB, fatigue, dizzy, coma, death
Tx; methylene blue
329
Prilocaine CONTRA
Cardiac or respiratory dz
330
Prilocaine use
LARGELY LIMITED to DENTISTRY
331
Bupivacaine
longer duration
post-op pain control
Spinal anesthesia, infiltration, epidural
GREATER cardiotoxicity than other amides
332
Bupivacaine use
Epidural during LABOR
sensory> motor block, important for delivery
333
Ropivacaine
S-enantiomer of Bupivacaine
less likely to have cardiac toxic SE, but still not DOC for birth bc has more effect on motor
334
Ropivacaine use
peripheral and
| epidural (not labor) nerve blocks
335
Etidocaine
Inverse differential block,
meaning motor> sensory block
336
Articaine
Widespread use in Dental medicine
337
Articaine rare SE
Persistent paresthesia
338
Dibucaine
test to measure butylcholinesterase activity
determines the ability to use Ester drugs
339
Centrally acting spasmolytics
Baclofen
Cyclobenazprine
Diazepam
Tizanidine
340
Direct acting spasmolytics
Dantrolene
| Botox
341
Diazepam affects all subtypes of GABA receptors
can be used as muscle relaxant, bu tproduces heavy sedation
342
Baclofen
GABA-b receptor
stimulates open K channels- hyperpolarize
inhibit Ca influx
343
Tizanidine
a2 agonist, inhibits BOTH pre and post synaptic spinal cord activity
chronic and acute muscle spasm
344
Dantrolene
inhibit Ca release from SR
RYR1 channel
345
Dantrolene use
Neuroleptic malignant syndrome
| Malignant hyperthermia
346
Botox
Small amts injected locally to control muscle spasm following Stroke or other neuro injury
347
Ach
Alzheimers
348
Dopamine (DA)
Parkinson's
| Schizophrenia
349
GABA
Major inhibitory
Relieves anxiety, promotes sedation
Cl- channels
350
Neuropeptide Y
food intake and fat storage
351
Genetic link to Alcoholism is related to
increase in release of B-endorphins in the Dopamine reward pathway
352
Genetic alcholism
B-endorphins
353
Alcohol metabolism
Acute vs Chronic pathways
Acute: Alcohol DH
| Chronic: MEOS and CYP2E1 now get activated as well
increases acetaminophen toxicity
354
Alcohol does what to CYP2E1?
induces CYP2E1, meaning they now metabolize it quicker, leading to increased tolerance
355
What happens to GABA and NMDA receptors in Alcoholics
Down regulate GABA
| Up regulate NMDA
356
An Alcoholic who is tolerant to Alcohol may also be tolerant to:
Benzos and Barbs
357
Alcohol mechanism
Bind to GABAa- increase Cl- influx and enhance GABA transmission
Increase DA in Limbic area
358
Alcohol leads to deficiencies in
Folate
| Thiamine
359
Wernicke Korsakoff syndrome
```
Paralysis of eye
Ataxia
Confusion
Coma
Death
```
All d/t THIAMINE deficiency
360
Korsakoff psychosis
Chronic disabling memory loss
361
Best tx for Acute Anxiety (short term, self limiting)
Benzos "pam"
362
Tx for Chronic/Generalized Anxiety
Buspirone
| Benzos "pam"
363
Kleine-Levin Syndrome
"sleeping beauty"
dissapears in teen years
sleeping for 24 hours at a time
364
DOC for Enuresis/ bed wetting
TCAs (Tricyclic Antidepressants)
365
Hydroxyzine
Antihistamine used as Anti-anxiety
1st gen Sedation
366
How is Barbiturate toxicity eventually cleared?
Diuresis and Alkalization of URINE
otherwise, just treat supportively
367
What is prescribed more for Anxiety/Insomnia?
Barbs or Benzos?
Benzos "pam"
368
Traits about Diazepam and Lorazepam
DOC: Status Epileptius
| Also, provide a tapered withdrawal (+ Chlordiazepoxide)
369
Benzos "pam" contra
Pregnant
Old
Sleep apnea
370
Barb contra
Porphyria
Pulm insufficiency
With other CNS depressants
371
What can be given to reverse the effects of Midalozam? (a short acting Benzo)
Flumenazil- a Benzo antagonist
372
Complex seizures are still <2 minutes
Altered or LOC
373
Partial with secondary Tonic Clonic
LOC
| muscle contraction w alternating contraction
374
Tonic clonic (grand mal) seizure
<2 minutes
Start rigid, then tremor, then clonic jerking
LOC
375
Absence seizure
10-30 seconda
| Not as aware, but STILL CONSCIOUS
376
Goal of seizure medicine in relation to GABA
Increase GABA
377
Goal of seizure medicine in relation to Glutamate (NMDA)
Decrease NMDA (glutamate)
378
Glutamate
Na and Ca channels
to treat seizure: inhibit these channels
379
Common SE of seizure meds
Teratogenic
| Hypersensitivity- SJS
380
Anytime you are prolonging the inactivation of Na and Ca channels, you are
decreasing Glutamate activity
381
Seizure meds affecting Na+ channels
Phenytoin
Carbamazepine
Lamotrigrine
Topiramate
382
Seizure meds affecting Ca++ channels
Ethosuximide
| Valproic acid
383
Seizure meds affecting GABA channels
```
Benzos
Barbs
Gabapentin
Pregabalin
Tiagabine
Vigabatrin
```
384
SV2A
Levetiracetam
385
Phenelzine
| Selegiline
MAOIs
386
Venlafaxine
| Duloxetine
SNRIs
387
Fluoxetine
Sertraline
Paroxetine
Citalopram
SSRIs
