4. Neuropharmacology Flashcards

1
Q

Most important CNS neurotransmitters?

A

Glutamic acid, GABA, ACh, DA, NE, 5HT, opioid peptides

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2
Q

Action of glutamic acid?

A

Direct coupling and G-protein linked on NMDA -> influx of cation -> excitatory

Potential target for ketamine and PCP

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3
Q

Mechanism of ACh?

A

Excitatory and inhibitory on muscarinic receptors by decreasing/increasing K+ efflux by coupling DAG and cAMP

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4
Q

Mechanism of GABA?

A

Increase K+ influx by direct coupling -> inhibitory

Potential target for anticonvulsant, sedatives, hypnotics, some muscle relaxants

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5
Q

What drugs act on GABA?

A
Barbiturates (duration of Cl- ion channel)
Benzos (frequency of Cl- ion channel)
Propofol (GABA-A)
Baclofen (GABA-B)
Valproic acid (high concentration)
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6
Q

Mechanism of flumazenil?

A

Benzo antagonist (decreases frequency)

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7
Q

What nonbenzo drug binds to benzo receptor?

A

Zolpidem (sleep)

Less tolerance and dependence

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8
Q

Name a nonbenzo anxiolytic

A

Buspirone (partial 5HT1A receptor)

No dependence or withdrawal

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9
Q

Side effects of benzos

A

Sedative, amnestic, anxiolytic, antidepressant, muscle relaxant

Not for T1 preg
May result in hypotension/resp depression if with opioids

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10
Q

Benzo withdrawal syndrome

A

Hypertension, tachycardia, muscle twitching, tremulous, diaphoresis, confusion, dysphoria, seizures

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11
Q

Pharm strategy in Parkinson

A

Increase DA activity and decrease ACh at muscarinic in striatum

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12
Q

Midazolam (1-2mg IV): onset and duration

A

Rapid and shortest

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13
Q

Diazepam (2-10mg BID-QID): onset and duration

A

Rapid and longest

aka Valium

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14
Q

Alprazolam (0.25-0.5 mg TID)

A

Intermediate/Intermediate (Antidepressant effect)

aka Xanax

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15
Q

Chlordiazepoxide (5-10mg TID)

A

Intermediate/Long

aka Librium

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16
Q

Lorazepam (1mg TID)

A

Intermediate/Intermediate (liver ok)

aka Ativan

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17
Q

Temazepam (15-30mg)

A

Intermediate/intermediate (liver ok)

aka Resteril

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18
Q

What 3 benzos are not metabolized in the liver?

A

Alprazolam
Temazepam
Oxazepam

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19
Q

What drug increases dopamine function?

A

Levodopa to dopamine by dopa-decarboxylase

Carbidopa blocks peripheral decarboxylation

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20
Q

Tolcapone and entacapone?

A

COMT inhibitor

Enhances CNS uptake of L-dopa; reduces on-off effects

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21
Q

Dopamine receptor agonists (2)

A

Bromocriptine (hallucinations, confusion, psychosis)

Pramipexole/Ropinirole

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22
Q

MAO B inhibitor

A

Selegiline

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23
Q

What drugs decrease ACh function?

A

Benztropine and trihexyphenidyl (M receptor blockers)

Reduce tremor/rigidity, EPS syndrome, but exacerbates tardive dyskinesia and cause atropine-like effects

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24
Q

Why do antipsych drugs cause atropine-like effects, postural hypotension, sexual dysfunction?

A

Block D2 receptors, muscarinic, alpha receptors

25
Side effects of DR antagonists?
Akathisia, acute dystonic rxn, extrapyramidal dysfunction, prolactinemia
26
Chronic dopaminergic receptor bockage?
Akathisia and tardive dyskinesia months later
27
Neuroleptic malignant syndrome?
Hyperthermia, cardiovascular instability, rigidity, altered MS due to enhanced sensitivity of DR to blocking agents
28
Tx of NMS?
Bromocriptine and dantrolene
29
Mechanism of TCA
Block reuptake of NE and 5HT | Also block muscarinic/alpha receptors (sedation, decrease seizure threshold, cardiotoxicity)
30
Mechanism of SSRI
5HT reuptake blocker | Can cause anxiety, agitation, bruxism, sexual dysfunction, seizure, transitory weight loss
31
Serotonin syndrome?
Excess seratonergic activity in CNS | Diaphoresis, rigidity, myoclonus, hyperthermia, instability of autonomic NS, seizures
32
Drug of choice for GTC
Valproic acid, phenytoin, carbamazepine - prevent Na+ influx through fast Na channel
33
First-line drug for complex partial seizure
Carbamazepine
34
Absence seizure tx
Ethosuximide (presynaptic calcium influx through type T channels in thalamic neurons)
35
Common side effects of phenytoin
Sedation, ataxia, diplopia, acne, gingival overgrowth
36
Common side effects of valproic acid
Pancreatitis, hepatotoxicity, thrombocytopenia
37
Meds that lower seizure threshold
1) Antidepressants (baclofen) 2) Analgesics (meperidine, fentanyl, tramadol) 3) Anesthetics (methohexital, enflurane) 4) Benzodiazepines 5) Barbiturates and withdrawal of antiepileptic 6) Antibiotics: Cefazolin, imipenem, metronidazole 7) Radiographic contrast materials
38
Propofol infusion syndrome
High dose/long-term use of propofol Metabolic acidosis, cardiac failure, rhabdo, hypotension, death Using >5mg/kg/h
39
Intrathecal baclofen pump overdose
Hallucinations, seizures, confusion, psych, resp depression, hypotension, coma
40
Time course for intrathecal baclofen withdrawal
Over 1-3 day | Tx: restoration of baclofen
41
Toxic doses of acetaminophen
>10g/d (lower if liver dx, and taking cytochrome p450 enzyme-inducing drugs)
42
Prescribing NSAIDS
Do not create dependence misoprostol may reduce side effects ASA is irreversible - inhibits platelet function for 8-10 days. All can cause water and sodium retention and potential nephrotoxicity
43
Ketorolac (Toradol)
Only parenteral. Useful if sensitive to narcotics. | 30 mgIV or IM q6h; maximum 120 mg/d
44
Celecoxib
COX-2 inhibitor; 200mg 2x daily
45
Most common antispasmodics in spine surgery
Little evidence Cyclobenzaprine, methocarbamol, carisoprodol Diazepam for muscle spasms
46
1/2 life of cortisone
90 min
47
Normal physiologic replacement of steroids (under no stress)
Prednisone 5mg qAM and 2.5mg qPM (or hydrocortisone 10mg qAM and 5mg qPM)
48
Which doses of steroids unlikely to cause HPA axis suppression
<1w | Axis suppression with 40-60mg after 2w
49
Equivalent corticosteroid doses
``` Dexamethasone 0.75mg Methylprednisolone 4mg Prednisone 5mg Hydrocortisone 20mg Cortisone 25mg ```
50
Neurologic side effects of steroids
Mental agitation "steroid psychosis", spinal epidural lipomatosis, multifocal leukoencephalopathy, pseudotumor cerebri
51
Weak opioids, doses and delivery time
Codeine 30-60 mg IM/PO q3 PRN Propoxyphene 1-2 tablets PO q4-6h Tramadol 50-100mg PO q4-6 PRN
52
Antidote for morphine
Naloxone
53
Dexmedetomidine - indication?
Anxiety Opioid sparing analgesia/sedation without resp depression Allows brain mapping without interfering with electrophysiologic monitoring
54
Dexmedotomidine on traumatic spinal cord injury
Decreases inflammation.
55
Two types of antiemetics
Phenothiazine (promethazine, prochlorperazine) - lower seizure threshold Trimethobenzamide - for nausea 2/2 posterior fossa surgery Metoclopramide - can cause EPS Ondansetron - n/v post chemo and surgery
56
Why use acid inhibitors in nsu px?
Stress ulcers from brain/spinal injury, tumors, ICH, SIADH
57
Acid inhibitors use in NSU patients
Ranitidine 150mg PO BID or 50 mg IV Q8 Famotidine 40mg PO (thrombocytopenia) Omeprazole 20-40mg BID Sucralfate 1g PO QID
58
Ondansetron mechanism of action
5HT3 receptor in area postrema and peripheral sensory/enteric nerves.