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Pharmacology Flashcards

1
Q

Morphine

A
  • produces analgesia

- activates opioid receptors on periaqueductal grey (PAG)

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2
Q

Naloxone

A
  • antagonist
  • blocks effects of morphine
  • blocks placebo effect
  • competitive antagonist
  • short duration of action
  • no oral availability
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3
Q

Cocaine

A

-blocks catecholamine reuptake

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4
Q

What confers most of key properties of local anesthetics?

A

-chemical structure

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5
Q

Local anesthetics are weak _______.

A

Bases

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6
Q

The intermediate chain of a local anesthetic is determinant for:

A
  • onset speed
  • duration
  • potency
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7
Q

Aromatic Moiety of Local Anesthetic

A
  • lipophilic

- allows cross of nerve cell membrane

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8
Q

Amino Group of Local Anesthetic

A
  • hydrophlic

- can be protinated

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9
Q

Intermediate Chain of a Local Anesthetic can be either:

A
  • an ester
  • or an amide
  • drugs with two “i”s are amides
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10
Q

Equation to determine ratio between cationic and neutral forms of local anesthetic:

A

neutral/cationic = 10^(pH-pKa)

-higher pKas and lower pHs cause dec. in fraction of neutral local anesthetic

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11
Q

Local Anesthetic MOA

A
  • block Na channels-> thereby blocking action potentials
  • LA passes through nerve cell membrane into nerve before blocking Na channel from inside
  • LAs are use dependent
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12
Q

LAs preferentially block:

A
  • pain sensation
  • block small diameter neurons with less myelination
  • ex. C fibers that modulate pain and temp
  • LAs don’t block CNS
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13
Q

Faster onest, more potent, and longer lasting LAs have:

A
  • lower pKa
  • higher lipid solubility
  • inc. protein binding (protects LA)
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14
Q

Ester Local Anesthetics

A
  • hydrolyzed in plasma and in liver

- typically shorter duration

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15
Q

Amides Local Anesthetics

A
  • metabolized only in liver

- longer duration

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16
Q

a1-acid-glycoprotein

A
  • binds LAs and buffers them

- affected by age, contraceptive use, and smoking

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17
Q

Local Anesthetic Excretion

A

-via kidney

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18
Q

Topical Anesthesia

A
  • tetracaine, lidocaine, cocaine
  • EMLA cream
  • benzocaine
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19
Q

Infiltration Anesthesia

A
  • lidocaine
  • procaine
  • bupivacaine
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20
Q

Nerve Block Anesthesia

A
  • lidocaine

- bupivacaine

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21
Q

IV Regional Anesthesia (Bier’s Block)

A

lidocaine

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22
Q

Spinal Anesthesia

A
  • lidocaine
  • bupivacaine
  • tetracine
  • injection into CSF bathing lumbar spinal cord
  • loss toxicity and loss to plasma
  • internal to dura placement
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23
Q

Epidural Anesthesia

A
  • lidocaine
  • bupivacaine
  • injection just outside dural enclosed spinal canal
  • can catheterize
  • higher loss in plasma
  • good for longer surgery
  • external dura placement
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24
Q

Epinephrine

A
  • coapplication of epi with LAs causes vasoconstriction and helps retain LA near injection site
  • inc. duration of LA
  • dec. peak plasma levels of LA
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25
Local Anesthetic Toxicity
- can block channels in all nerve and muscle tissue - convulsions - autonomic nervous system - cardiac arrhythmia - local anesthetic hypersensitivity - allergy
26
Tetrodotoxin and Saxitoxin
- block Na channels from outside of cell | - cause nerve block and paralysis
27
Migraine Abortive Treatment
1. aspirin, acetaminophen, NSAIDs 2. combo: ibuprofen/caffeine, aspirin, or similar 3. triptans (sumatriptan) (5HT 1B/1D agonists) 4. ergotamine derivative (dihydroergoatmine) (nonselective 5HT agonists)(also agonizes alpha1 receptors and causes vasoconstriction)
28
Migraine Prophylactic Treatment
1. beta blockers (propanolol, metoprolol) (most efficacious) 2. Ca channel blockers (verapamil) (do not give if already on beta blockers) 3. ACE inhibitors (lisinopril) 4. antidepressants (SSRIs and tricyclic) 5. anti-convulsants (gabapentin) 6. botox injections for chronic migraine
29
Tension Headache Treatment
Abortive: aspirin, acetaminophen, NSAID (enc. pt not to overuse) Prophylactic: tricyclic antidepressants, SSRIs, physical therapy, psychotherapy
30
Cluster Headache Treatment
- aggressive tx - abortive: O2, triptans inj, ergots - transitional: steroids, nerve blocks - preventive: CCB, lithium, antiepileptics
31
Trigeminal Neuralgia Treatment
- anti-epileptics | - surgery
32
Giant Cell Arteritis Treatment
-glucocorticoids
33
Target of NSAIDS (COX2 inhibitors) in Migraine Tx
-neuroinflammation
34
Target of Triptan-Ergots Alkaloids in Migraine Tx
-5HT 1B-1D agonists
35
Amide Drugs & Time Course
- Lidocaine- faster, more local | - Bupivocaine- longer acting
36
Opioid Analgesic Agonists
- morphine - hydrocodone - oxycodone - codeine - tramadol - fentanyl
37
Opioid Analgesic Combinations with NSAIDS
- codeine-acetaminophen - codeine-aspirin - hydrocodone-acetaminophen - hydrocodone-ibuprofen - oxycodone-acetaminophen
38
Opioid Analgesic Partial Agonists
-buprenorphine
39
Opioid Analgesic Antagoinsts
-naloxone
40
Non-Selective COX1/COX2 Inhibitors
- naproxen (inc. risk bleeding) | - aspirin
41
COX2 Selective Inhibitors
-Celecoxib (inc. risk clotting)
42
COX2 Inhibitors (CNS)
-acetaminophen
43
NMDA Receptor Antagonist & Function
-ketamine (blocks central sensitization)
44
Antidepressants
- tricyclics - SSRIs - SNRIs
45
Anticonvulsants
-pregalin, gabapentin
46
Tx for Dementia
- cholinesterase inhibitors: donepezil | - NMDA-glutimate antagonists: memantine (Alzheimers tx)
47
Wernicke's Encephalopathy Tx
-Thiamine
48
3 Classes of Opioid Receptors and Function
- mu - delta - kappa - all are coupled to Gi/o G proteins
49
Mu Opioid Receptor - pharm response - endogenous agonists - agonist drugs
- pharm: analgesia (central), respiratory depression - endo agonists: b-endorphin - agonist drugs: morphine
50
Delta Opioid Receptor - pharm response - endogenous agonists - agonist drugs
- pharm: analgesia - endo angonists: met/Leu-enkephalin, b-endorphin - agonist drugs: no drugs in clinical use
51
Kappa Opioid Receptor - pharm response - endogenous agonists - agonist drugs
- pharm: spinal analgesia - endo agonists: dynorphin 1-17 - agonist drugs: pentazocine
52
Opioid Receptor Function
- dec. neuronal excitability - inhibition of presynaptic VSCC - activation of K channels leading to membrane hyperpolarization - inhibition of cAMP synthesis
53
Analgesic Actions of Opioids
- inhibition of spinal cord/ascending pain pathway - activation of descending pain pathway - also reduce subjective response to pain
54
Side Effects of Opioids
- respiratory depression - nausea, vomiting - cough suppression - pupillary constriction - constipation - histamine release
55
Fentanyl
- opioid mu receptor agonist - short duration of action - requires mechanical ventilation
56
Buprenoprhine
-partial mu agonist that can precipitate mild withdrawl
57
Clonidine
-used to treat withdrawl sx caused by opioid addiction
58
Opioid Mechanism of Action
1. inhibiting asc. pain pathway 2. activating dec. pain pathway (inhibits inhibitory gabaergic interuerons in PAG) 3. modulate perception of pain
59
Enkephalin
-endogenous opioid
60
NMDA Receptor Role in Pain
- glutimate binds to AMPA and NMDA receptors - ions that go through AMPA receptor - NMDA must bind glutimate and require depolarization to open and allow Ca to enter cell - Ca causes hyperphosphorylation of NMDA receptor to act like AMPA receptor making the cell depolarize more quickly
61
Adjuvant
- drug that was not intended to prevent pain but is added to tx neuropathic pain - not combined with opioids

Neuro 2 Mine (9 decks)

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