General Flashcards
(274 cards)
1
Q
Phenytoin
A
- AE
- Na blocker
- long term pot hirtuism and osteoporosis
- marked confusion (cognitive impairment), teratogen
- cause gingival hyperplasia in 20%
- hard to regulate
2
Q
Tiagabine
A
- AE
- incr GABA– reuptake inh (prolong chanel open)
- adjunct in partial seizures
- short half life
3
Q
Rufinamide
A
- AE Na channel blocker
- add on for lenox-gastaut syndrome
4
Q
Valporic acid
A
(divalporex) broad spectrum AE
- Treats all seizures- FIRST LINE
- teratogen, osteoporosis, weight gain, hair loss, hepatic and pancreatic injury
- cyp inducer
- also treats bipolar
5
Q
Perampanel
A
AMPA antag AE
-partial seizures and tonic-clonic
6
Q
Tonic-clonic seizure
A
Initial strong contraction of whole musculature; followed by series of violent jerks that gradually die out (2-4 min).
7
Q
Which AE’s cause cognitive impairment?
A
Phenobarbital, phenytoin and topiramate
8
Q
Lamotrigine
A
- Broad spectrum AE (alt to valproic acid – less SE) prolong inact Na and inh glut
- FIRST LINE general
- tonic clonic seizures and lenox-gastaut
- Rash when dose incr too rapidly
9
Q
Vigabatrin
A
-AE
Irrev inh GABA-T (GABA aminotransferase)– degr enzyme
-patrial seizures
-RARELY used – vision loss
10
Q
Ezogabine
A
-AE
enhance K channels (KCNQ family)
11
Q
Which AEs cause osteoporosis
A
Phenytoin, phenobarbital, carbamazepine, oxcarbazepine and valproic acid.
12
Q
Ethosuxamide
A
- AE that decr Ca
- Absent seizures (FIRST LINE)
13
Q
Felbamate
A
- AE
- Broad spectrum– multiple mechs (NMDA antag and enhance GABA)
- aplastic anemia
14
Q
Carbamazepine
A
- AE Na channel blocker
- modulate sustained high freq firing
- Autoinduction (incr clearance with incr dose)
- osteoporosis and teratogen
15
Q
Which AEs are teratogenic?
A
Valproic acid & carbamazepine; barbiturates & phenytoin. Newer AEDs less teratogenic.
16
Q
Leviteracetam
A
- AE that binds to SV2A
- Broad spectrum (modify release of GABA and glut)
- not many SEs
17
Q
Clonazepam
A
- Long acting BZD— AE
- incr GABA
- sedation, memory impair, mood changes, addiction.
- also used in anxiety and panic
18
Q
Non-linear drug clearance
A
Either clearance decreases as dose increases or clearance increases with dose increase.
-with AEs
19
Q
Topirimate
A
- Broad spectrum AE
- memory impair, renal stones, glaucoma, weight loss
20
Q
Gabapentin and pregabalin
A
- AE that binds alpha-2-delta of Ca channel — decr glut
- unsteadiness, weight gain, fatigue, dizzy
- also for neuropathic pain, chronic pain, fibromyalgia
21
Q
What is a seizure?
A
a group of cortical neurons that discharge abnormally
22
Q
phenobarbital
A
-AE enhance GABA
-weak acid– elim by making urine alkaline
-similar to penytoin (preferred)
cognitive impair, osteoporosis, sedation
-not for absence
23
Q
List 3 highly selective nonergot derivatives (dopamine agonist)
A
- Pramipexole
- Ropinirole
- Apomorphine
Fewer side effects and are therefore preferred.
24
Q
What are the 3 categories of partial seizures?
A
Simple
Complex
Secondarily Generalized
25
Most AED's cause some CNS depression, therefore, what other drugs should be avoided?
Etoh, antihistamines, other AED's, opioids.
26
How effective is Memantine?
Only modest benefit
27
How is preclinical AD diagnosed?
Completely on the basis of biomarkers
28
What is tegretol indicated for?
Like phenytoin, partial seizures and tonic-clonic seizures.
29
What is the first line drug class of choice for mild to moderate PD motor symptoms?
Dopamine agonists
30
What are the principal adverse effects of levodopa?
nausea, dyskinesia, hypotension, and psychosis.
31
If combined with levodopa, what drug will cause a hypertensive crisis?
MAOI
32
Which two AED's have the highest risk of causing suicidality?
Topamax and Lamictal
33
What is the unique side effect caused by phenytoin in 20% of patients?
gingival hyperplasia
34
How can you minimize the risk to the fetus?
Use one drug at the lowest possible dose and avoid Depakote
35
What is the name of the enzyme that converts levodopa to dopamine?
decarboxylase
36
What is the primary pathology in PD?
Degeneration of neurons in the substantia nigra that supply dopamine to the striatum. The result is an imbalance between dopamine and acetylcholine.
37
Which COMT is safer and therefore preferred?
Entacapone
38
Name the 4 cholinesterase inhibitors that are approved for AD.
1. Donepezil
2. Galantamine
3. Rivastigmine
4. Tacrine
39
What is the gold standard for treatment of PD motor symptoms?
Levodopa + carbidopa
40
How are the motor symptoms of Parkinson's Disease treated best?
Primarily with dopamine agonists. Anticholinergics can also be used.
41
Tegretol is often better tolerated than phenytoin, therefore, it is often preferred. True of False?
T
42
Rarely, phenytoin causes SJS or toxic epidermal necolysis (TEN). What may increase the risk?
HLA-B1501 gene variation, seen almost exclusively in pts of Asian descent.
43
What are the categories of generalized seizures?
```
Tonic-Clonic (Grand Mal)
Absence (Petit Mal)
Atonic
Myoclonic
Status Epiletpticus
Febrile
```
44
What role do NMDA receptors play?
learning and memory
45
How does carbidopa enhance the effects of levodopa in PD?
By preventing decarboxylation of levodopa in the intestine and peripheral tissues. (Can't cross blood-brain barrier, so does not prevent conversion of levodopa to dopamine in the brain.)
46
What is a COMT drug and how do they work?
Catechol O-methyltransferase (COMT) inhibitors inhibit metabolism of levodopa in the periphery resulting in raised dopamine levels in treating PD.
47
How do you treat AD dementia?
Cholinesterase inhibitors or memantine (Namenda).
| Benefit in most patients is marginal.
48
Dopamine agonists do have more serious side effects than levodopa. List some.
Hallucinations
Sleepiness
Postural hypotension
*Usually reserved for younger patients who can tolerate better.
49
What is the major known risk factor in developing AD?
Advancing age
50
What are the 2 major adverse reactions with Depakote?
1. Potentially fatal liver injury (espec children
51
What is phenytoin indicated for?
Partial seizures and tonic-clonic seizures. NOT absence seizures.
52
What is the new class of drugs for AD?
NMDA receptor antagonists. Memantine (Namenda) is the first representative. Benefits are derived from modulating the effects of glutamate at NMDA receptors.
53
How does levodopa work to relieve motor symptoms in PD?
Levodopa relieves motor symptoms by converting to dopamine in surviving nerve terminals in the striatum and restores a proper balance between dopamine and AcH.
54
Depakote is a very broad spectrum AED. What are it's indications?
ALL seizure types including most generalized seizures - tonic-clonic, absence, atonic, and myoclonic sz's.
55
Dopamine agonists fall into two groups. What are they?
1. Ergot derivatives
| 2. Nonergot derivatives
56
How long do you treat AD?
Indefinitely, or until the SE's are intolerable or benefits are lost.
57
How do the MAO-B Inhibitors enhance responses to levodopa?
By inhibiting MAO-B, the brain enzyme that inactivates dopamine.
58
Only 1 cholinesterase inhibitor is approved for treating severe AD. Which one is it?
Donepezil
59
What is gabapentin used for?
Partial seizures, restless leg syndrome, phantom limb pain, and neurogenic pain.
60
What are the 2 MAO-B Inhibitors used with levodopa in treating PD?
1. Selegiline
| 2. Rasagiline
61
What are the 2 COMT drugs?
1. Entacapone
| 2. Tolcapone
62
What is the histology of Alzheimers (AD)?
Characterized by: 1. neuritic plaques 2. neurofibrillary tangles 3. degeneration of cholinergic neurons in the hippocampus and cerebral cortex.
63
How would you treat status epilepticus?
Initially, IV diazepam or lorazepam. Follow with Phenytoin if seizures do not stop. Move onto phenobarbital IV until stops.
64
When is the oral nonergot dopamine agonist, pramipexole indicated?
Alone in early PD for motor symptoms or with levodopa in advanced PD
65
What are the 3 phases of AD?
1. An asymptomatic preclinical phase
2. Two symptomatic clinical phases:
a) . Mild cognitive impairment
b) Dementia - both due to AD.
66
What is PD
A neurodegenerative disorder that produces characteristic motor symptoms: tremor at rest, rigidity, postural instability, and bradykinesia.
67
What are neuritic plaques?
Spherical, extracellular bodies that consist of a beta-amyloid core surrounded by remnants of axons and dendrites.
68
PD affects the ____
basal ganglia
69
What is the dopamine content of the substantia niagra in PD patients?
less than 10% of normal in PD patient brains postmortem
70
MPTP
is a compound used experimentally to study Parkinson's disease; it impairs dopaminergic neurons
71
A molecule aspect of PD involves ______
Lewy bodies in various parts of the brain
72
Alpha synuclein
staining used to reveal Lewy bodies
73
Genetic forms of PD ____ and _______
PARK7 and PINK1
74
Main DE of LDOPA
Dyskinesias and a rapid fluctuation in clinical state
75
Acute side effects of LDOPA
Nausea, anorexia, hypotension
76
Bromocriptine
PD
| -Primarily dopamine agonist; used most often in cases of hyperprolactinemia
77
Pergolide & cobergoline
PD
| -dopamine agonist
78
Pramipexole and Ropinirole
-PD
| D2/3 selective dopamine agonists, better tolerated; no fluctuations in efficacy
79
Rotigotine
Newer dopamine agonist, delivered as a transdermal patch
| -PD
80
Apomorphine
-PD
| Dopamine agonist with a powerful emetic action; must be combined with an antiemetic; LAST RESORT COMPOUND
81
Seligiline
-PD
| MAO-B inhibitor (selective), used in combination with levodopa
82
Tolcapone and entacopone
Catechol-O-Methyltransferase inhibitors; used with L-DOPA and never alone
83
Deep brain stimulation
in PD
| -electrode is placed into the subthalamic nucleus; used in cases where patients are intolerant to medication
84
Orphenadrine
Muscarinic receptor antagonist used for the parkinsonism caused by antipsychotic drugs
85
Amantadine
May enhance dopamine release
86
What is HD?
An inherited (autosomal dominant) disorder resulting in progressive brain degeneration
87
Trinucleotide repeat
in Huntington's disease this expansion of the number of repeats of the CAG sequence coding for glutamine is over 50
88
Which drugs treat the invol movements of HD?
Tetrabenazine and chlorpromazine; baclofen
89
Baclofen
GABA agonist in HD
90
Tetrabenazine
-HD
| Inhibitor of monoamine transporter 2 (VMAT2); decreases dopamine levels in addition to serotonin and norepi.
91
Amyloid cascade hypothesis
in AD
-Amyloid precursor protein accumulates following processing, aggregating to form plaques that are thought to damage the brain.
92
An allelic variant of apolipoprotein-E (APOE)-E4
Associated with 20 % of sporadic and familial AD; making it the single most important risk factor
93
Highly selective and reversible AChE inhibitor used in AD
Donepezil
94
Rivastigmine
-AD
Inhibits both AChE and butryylcholinesterase. Transdermal patch allows once a day administration and fewer GI side effects.
95
Galantamine
-AD
Reversible and competitive inhibitor of AChE and also an allosteric modulator binding to cholinergic nicotinic receptors.
96
Memantine
Noncompetitive glutamatergic receptor antagonist, blocking/regulating NMDA receptors
97
Cognitive reserve
Maximized by increasing social circle, maintaining a healthy weight, cognitively stimulating activities and strong literary skills
98
Pathophysio of AD
Acetylcholine in the diffuse cortex
99
Most prominent side effect of tricyclic antidepressants
anticholinergic
100
Tyrosine hydroxylase
Rate limiting enzyme in dopamine synthesis
101
Mertazapine
Atypical antidepressant with adverse effects of somnolence, increased appetite, weight gain, constipation and dizziness
102
Paroxetine
SSRI most assoc with constipation
103
Sertraline
SSRI most assoc with diarrhea
104
Buproprion
Atypical antidepressant used to treat depression and smoking cessation
105
These MAO-I potentially causes the most drug-food interactions
MAO-A selective
106
Serotonin syndrome
Due to high levels of serotonin; usually a drug interaction, and consists of hyperthermia, muscle rigidity, and fluctuations in vital signs and mental status
107
Phenelzine
Non-selective MAO inhibitor
108
Serotonin synthesis
Tryptophan, 5-hydroxytryptophan, 5-hydroxytriptamine
109
Buspirone
5-HT1A partial agonist
| antidepressant (non BZD)
110
Venlafaxine, Duloxetine
SNRIs
111
Side effects or problems with tricyclic antidepressants
Coma, convulsions, confusion in elderly, cardiotoxicity
112
LSD
non-selective serotonin agonist
| Binds to all serotonin receptors except 5-HT3 and 5-HT4
113
selegiline
MAO-B inh
114
Monoamine hypothesis of depression
Depression results from a decrease in serotonin and norepinephrine transmission
115
Nortriptyline
TCA
116
Modafanil, armodafanil
amphetamine
| -depression
117
dexmethylphenidate, methylphenidate
amphetamine
| -depression
118
lisdexamphetamine
amphetamine
| -depression
119
isocarboxazil, phenelzine
nonselective MAOI
| -depression
120
tranylcypromine
MAOI
| depression
121
Amitriptyline
TCA
| -sedating can use for insomnia
122
clomipramine
TCA
123
Desipramine
TCA
124
Doxapin
TCA
| -low dose used for insomnia though H1
125
Imipramine
TCA
126
citalopram, escitalopram
SSRI
127
fluvoxamine
SSRI
128
Milnacipram
SNRI
129
Trazodone
Atypical antidepressants
| -sedating, can use for insomnia
130
Mirtazapine
Atypical antidepressant
| -sedating, can use for insomnia
131
BDZ and hepatic induction
Benzodiazepines do not induce hepatic microsomal enzymes
132
CBT
Often used in conjunction with SSRIs for anxiety
133
BZD adverse effects
Sedation, tolerance, physical dependence, self-administration
134
Clonazepam uses
Panic, anxiety, seizure
135
PTSD first line treatment
SSRI, usually paroxetine or sertraline
136
Flumazenil
BZD antagonist
137
BZD toxicity
Impaired judgement, slurred speech, incoordination, stupor, respiratory depression, death
138
Barbiturates
Bind to a distinct subunit combination on the GABA receptor and at high concentrations can open the channel on their own (without GABA).
139
Sedating antidepressants
Trazodone, mirtazapine, amyitriptyline
140
Which drugs are typically used for sleep?
Eszoiclone, hydroxyzine, zolpidem, zaleplon, ramelteon
141
GABA binding site on GABA R
alpha-1 and beta-2 subunits
142
Non-BZD GABA A agonists
Eszopiclone, zolpidem, zaleplon
| hypnotics
143
Doxepin
Tricyclic antidepressant, low dose mechanism for insomnia is histamine H1
144
GABA shunt
Refers to alpha ketoglutarate from the Krebs Cycle, converted to glutamic acid by GABA-transaminase; then subsequently to GABA by glutamic acid decarboxylase (GAD). GABA is then metabolized to form succinic semialdehyde to succinic acid and returns to the Krebs Cycle.
145
Alprazolam uses
panic, anxiety
| short acting
146
Diazepam uses
Anxiety, insomnia, pre-op, muscle relaxant, status epilepticus
147
Flurazepam, Temazepam and Triazolam use
insomnia
| BZDs
148
Nonbenzodiazepine anxiolytic
Buspirone mechanism is serotoniergic 5-HT1A receptor partial agonist
149
General anxiety disorder first line treatment
SSRI, usually venlafaxine, paroxetine or escitalopram
150
Insomnia disorder
Insomnia complaint and significant daytime impairment
151
Glutamine loop
Glutamine is formed as GABA is transaminated and converted to glutamine. The glutamine is reconverted to glutamate; then decarboxylated by neuronal GAD to GABA
152
Zolpidem disadvantages
(Non BDZ GABA agonist)
| 4-6 hr effect, therefore not for middle of the night awakenings, associated with parasomnias
153
BZD binding site on GABA A R
gamma-2 and alpha-1 subunits.
154
Short acting BZDs
Alprazolam, triazolam, lorazepam, oxazepam
155
Lorazepam uses
anxiety, alcohol related seizure, status epilepticis
156
BDZ used for sleep
Estazolam, flurazepam, quazepam, temazepam, triazolam
157
Long acting BZDs
Flurazepam, clorazepate, prazepam
158
Traditional BZD disadvantages
Rebound insomnia, memory impairments, loss of coordination, abuse potential, not good for those with respiratory conditions
159
Chlordiazepoxide use
alcohol detox
160
Zolpidem advantages
Shorten sleep latency, improve duration, can be used as needed, no negative effect on sleep architecture
161
Antipsychotics with CV effects
Chlorpromazine, Thioridazine, Ziprazidone, Asenapine
162
Butyrophenones are:
Haloperidol, Droperidol
| typicals
163
All atypical antipsychotics:
D2 receptor antagonists and block 5-HT2
164
Clozapine
Azepine atypical antipsychotic
| -Associated with 1% risk of agranulocytosis, myocarditis
165
Antipsychotic with the longest half-life:
Aripiprazole
166
Classes of typical antipsychotics:
Phenothiazines, Thioxanthenes, and Butryophenones
167
Patients taking clozapine must be monitored for
Agranulocytosis
168
The phenothiazine class is:
typical antipsychotic (block D2)
169
Antipsychotics and the tuberoinfundibular pathway
Typical antipsychotics blocking this dopaminergic pathway lead to prolactin secretion
170
Aripiprazole
-Atypical antipsychotic, longest half life, in top 25 prescribed drugs
Is especially helpful for negative symptoms; is more activating than sedating
171
Pos schizo symptoms
Delusions, hallucinations, thought disorder, aggressive behaviors, stereotyped movements
172
Dopamine released from the hypothalamus blocks ______ via _______
prolactin via the tuberoinfundibular pathway
173
Tardive dyskinesia
Develops after months or years, seen in 20-40% of patients on typical antipsychotics, often irreversible; consists of involuntary movements often of the face and tongue, trunk and limbs - severely disabling often
174
Sedation with antipsychotics is caused likely by:
Histamine H1 receptor involvement
175
Quetiapine
-atypical azepine antipsychotic
| Known for association with lens changes; requires an eye examination at initiation and at 6-month intervals
176
Mesolimbic tract
Ventral tegmentum to limbic area. First generation antipsychotics block D2 receptors, theory that this tract was involved.
177
Serotonin theory of schizophrenia
Direct and indirect 5-HT agonists exacerbate the symptoms of schizophrenia
178
Serotonin hyperactivity is assoc with:
Positive and negative symptoms of schizophrenia; second generation antispychotics (atypicals) block 5HT2 receptors in addition to D2 receptors
179
Extrapyramidal motor disturbances (EPS):
-Antipsychotics
Are reversible, involve involuntary movements, occur in the first few weeks and diminish with time; are less with atypical drugs
180
Glutamate theory of schizo
Observations that PCP induces acute psychotic, schizophrenia like symptoms
181
Major SEs of typical antipsychotics
Extrapyramidal symptoms (Parkinsonism, dystonias, akathesia; tardive dyskinesia
182
Mech of typical antipsychotics
D2 dopamine receptor antagonism
183
Typical anti-psychotics antagonist what to cause their effects?
Noradrenergic alpha-1, histamine H1 and muscarinic M1 receptors
184
Atypical antipsychotics got the name due to:
No or low extrapyramidal symptoms
185
Olanzapine
- Azepine atypical antipsychotic
| - Weight gain
186
Therapeutic effects of antipsychotics req:
80% occupancy of dopamine D2 receptors based on imaging studies
187
Weight gain is seen with which types of antipsychotics?
Atypicals
188
Risperidone
-Atypical antipsychotic
| Demonstrates hyperprolactinemia even at low doses
189
Sertindole
atypical antipsychotic
190
sulpiride
atypical antipsychotic
191
ziprasidone
atypical antipsychotic
| -CV
192
Molindone
atypical antipsychotic
193
paliperidone
atypical antipsychotic
194
zotepine
atypical antipsychotic azepine
195
Lozapine
azepine atypical antipsychotic
196
thiothixine
typical antipsychotic thioxanthene
197
Zuclopentixol
typical antipsychotic thioxanthene
198
Flupenthixol
typical antipsychotic thioxanthene
199
Chlorprothixene
typical antipsychotic thioxanthene
200
Trifluoperazine
typical antipsychotic phenothiazine
201
Perphenazine
typical antipsychotic phenothiazine
202
Mesoridazine
typical antipsychotic phenothiazine
203
Thioridazine
typical antipsychotic phenothiazine
- low potency
- CV
204
Fluphenazine
typical antipsychotic phenothiazine
205
Chloralhydrate
barbiturate-like antidepressant
206
Eczopiclone
non BDZ hypnotic GABA A agonist
207
Zaleplon
non BDZ hypnotic GABA A agonist
| -typically used for sleep
208
Flurazepam
long acting BZD hypnotic
209
Triazolam
short acting BZD hypnotic used for sleep
210
Halothane
inhale anesthetic
| -hepatitis
211
Thiopental
iv anes
212
Methohexital
iv anes
213
propofol
iv anes
| -can be used as aole (no muscle relaxant)
214
ketamine
iv anes
- dysphoria, low dose analgesia, CV stimulant
* exception incr cerebral bl fl
215
Fentanyl
iv anes
| -analgesia
216
novocaine
first inject LA (ester)
| -metab in plasma
217
tetracaine
LA (ester)
incr pka so slow onset, long duration
-topical
218
2-chloropricaine
LA (ester)
219
Benzocaine
first synthetic LA (ester)
| -methemoglobinemia, low pka nonionized base
220
Lidocaine
amide LA prototype
221
mepivacaine
amide LA
similar to lidocaine but less vasodilation
-accumulation don't use for long epidural
222
Dibucaine
LA topical cream (amide)
223
Bupivacaine
LA (amide)
- long acting
- cardiotoxic (fix with intralipid)
- Freq dependent block
- spinal
224
Ropivacaine
LA AMide
| -compare to Bupivavaine, lower cardiotox, lower potency, beter freq dependent block, long lasting but not as long.
225
Prilocaine
- LA amide
- methemoglobinemia
- most rapid metab
226
Nitrous Oxide
anesthetic with highest MAC
227
BZD and anesthesia
Sedatives only, not anesthetics; no analgesia; effects partially antagonized by flumazenil
228
Opoids and anesthetics
Analgesics not anesthetics; can reduce the amount of anesthetic required; effects 100% reversible with naloxone
229
Physical properties of LAs
Weak bases, poorly water soluble; synthetics derived from cocaine
230
Unmyelinated nerve fibers and LA
Small (B and C) fibers appear more sensitive to local anesthetics
231
Duration of action anesth
Directly proportional to protein binding; also relates to toxicity - high protein binding reduces amount of free drug
232
Long acting LAs
Bupivacaine and Ropivacaine
233
LA toxicity initial signs
Central nervous system: lightheadedness, peri-oral numbness, dizziness, visual and auditory disturbances, disorientation, drowsiness.
234
LA peripheral toxic signs
Vasoconstriction (low doses); vasodilation (high doses); chest pain, shortness of breath, palpitations,
more
235
Sufentanil
- more potent than fentanyl
- ultra short acting
- respiratory depression
236
Narcotic
Any psychoactive compound with sleep-inducing properties. Today means totally prohibited
237
Relatively selective COX II
Celecoxib, diclofenac
238
COX I selective drugs
Flurbiprofen
| ketorolac
239
Butorphenol
Kappa opioid receptor agonist and mu opioid receptor antagonist or partial agonist
240
Non opoid Non NSAID drugs
Acetaminophen, Tramadol
241
Heroin
Rapidly metabolized to morphine. Due to rapid brain penetration, heroin causes an intense euphoria. Not used clinically in U.S.
242
Acetaminophen
Non opoid non NSAID
| -Does not produce GI damage, ineffective in intense pain, narrow therapeutic index - liver damage
243
Oxycodone
Semisynthetic weak opioid agonist used in combination with NSAIDs for analgesia.
244
Non-selective COX inhs
Ketoprofen, aspirin, naproxen, ibuprofen, indomethacin, sulindac
245
SE aspirin
GI upset; hypersensitivity-like reaction; Reye's syndrome; anticoagulant
246
Opoid agonist prototype
morphine
247
Naloxone
NARCAN; pure opioid antagonist, most potent at the mu receptor
248
COX 1
Constitutively active enzyme, involved in GI protection, platelet function, regulation of blood flow and kidney function
249
Codeine
Weak mu opioid agonist used as antitussive and analgesic in mild pain. Prodrug for morphine
250
COX II
Inducible enzyme, involved in inflammation, pain, fever and cardiovascular function
251
Celecoxib
Osteoarthritis and rheumatoid arthritis in adult patients, acute pain an dysmenorrhea; increased risk of major cardiovascular problems (30%)
252
Loperimide
IMODIUM, a mu opioid agonist that is poorly absorbed after oral administration; used as an antidiarrheal. Does not cross the blood brain barrier
253
Mechanism of NSAID renal effects
Inhibit prostaglandin synthesis allowing vasoconstriction leading to acute renal failure
254
Meperidine
Synthetic, weak mu opioid agonist used for analgesia during delivery.
255
Methedone
Orally active long acting mu opioid receptor agonist. Does not cause significant euphoria. Cross tolerance with morphine or heroin and therefore useful with addicts
256
Surgical treatment for chronic pain
Cut spinothalamic tract
257
Morphine SEs
Euphoria, sedation, respiratory depression, nausea and vomiting, constipation, reduced release of hormones (GnRH and CRF) from hypothalamus
258
A-delta fibers
Lightly myelinated axons, rapid condution of signal, mediate the fast, pricking or sharp quality of pain
259
Nigro-striatal dopaminergic pathway
substantia niagra to striatum
260
VTA
dopiminergic cell bodies
261
Raphae nucleus
serotonin cell bodies
262
Tuberoinfundibular pathway
Hypothalamus to anterior pituitary
263
Nucleus basalis
Acetylcholine neuronal cell bodies
264
Locus cereuleous
NE cell bodies
265
PCP can produce
hallucinations (incr glut)
266
Drugs of abuse produce their effects through:
Through G-protein coupled receptors, ionotropic receptors and monoamine transporters
267
The mesolimbic pathway including the nucleus accumbens
Is responsible for the mood elevating euphoria and rewarding effects of cocaine and amphetamine
268
Hallucinogens
Increase extracellular glutamate in the prefrontal cortex through stimulation of postsynaptic 5-HT2A receptors
269
Varenicline
Partial agonist of nicotinic acetylcholine receptors used for smoking cessation
270
Acamprosate
Antagonist of NMDA receptor used for treatment of alcoholism
271
Types of tolerance
Pharmacokinetic, pharmacodynamics, behavioral, and inverse (sensitization)
272
Anandamide
endogenous ligand for cannabinoids
273
PCP mech of action
Noncompetitive NMDA calcium channel blocker
274
Alcohol mech of action
Blocks NMDA receptor and enhances GABA receptor (through GABA-A)
