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Neuro 2 Mine > Pharmacology > Flashcards

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
Q

Local Anesthetic Toxicity

A
  • can block channels in all nerve and muscle tissue
  • convulsions
  • autonomic nervous system
  • cardiac arrhythmia
  • local anesthetic hypersensitivity
  • allergy
26
Q

Tetrodotoxin and Saxitoxin

A
  • block Na channels from outside of cell

- cause nerve block and paralysis

27
Q

Migraine Abortive Treatment

A
  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
Q

Migraine Prophylactic Treatment

A
  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
Q

Tension Headache Treatment

A

Abortive: aspirin, acetaminophen, NSAID (enc. pt not to overuse)
Prophylactic: tricyclic antidepressants, SSRIs, physical therapy, psychotherapy

30
Q

Cluster Headache Treatment

A
  • aggressive tx
  • abortive: O2, triptans inj, ergots
  • transitional: steroids, nerve blocks
  • preventive: CCB, lithium, antiepileptics
31
Q

Trigeminal Neuralgia Treatment

A
  • anti-epileptics

- surgery

32
Q

Giant Cell Arteritis Treatment

A

-glucocorticoids

33
Q

Target of NSAIDS (COX2 inhibitors) in Migraine Tx

A

-neuroinflammation

34
Q

Target of Triptan-Ergots Alkaloids in Migraine Tx

A

-5HT 1B-1D agonists

35
Q

Amide Drugs & Time Course

A
  • Lidocaine- faster, more local

- Bupivocaine- longer acting

36
Q

Opioid Analgesic Agonists

A
  • morphine
  • hydrocodone
  • oxycodone
  • codeine
  • tramadol
  • fentanyl
37
Q

Opioid Analgesic Combinations with NSAIDS

A
  • codeine-acetaminophen
  • codeine-aspirin
  • hydrocodone-acetaminophen
  • hydrocodone-ibuprofen
  • oxycodone-acetaminophen
38
Q

Opioid Analgesic Partial Agonists

A

-buprenorphine

39
Q

Opioid Analgesic Antagoinsts

A

-naloxone

40
Q

Non-Selective COX1/COX2 Inhibitors

A
  • naproxen (inc. risk bleeding)

- aspirin

41
Q

COX2 Selective Inhibitors

A

-Celecoxib (inc. risk clotting)

42
Q

COX2 Inhibitors (CNS)

A

-acetaminophen

43
Q

NMDA Receptor Antagonist & Function

A

-ketamine (blocks central sensitization)

44
Q

Antidepressants

A
  • tricyclics
  • SSRIs
  • SNRIs
45
Q

Anticonvulsants

A

-pregalin, gabapentin

46
Q

Tx for Dementia

A
  • cholinesterase inhibitors: donepezil

- NMDA-glutimate antagonists: memantine (Alzheimers tx)

47
Q

Wernicke’s Encephalopathy Tx

A

-Thiamine

48
Q

3 Classes of Opioid Receptors and Function

A
  • mu
  • delta
  • kappa
  • all are coupled to Gi/o G proteins
49
Q

Mu Opioid Receptor

  • pharm response
  • endogenous agonists
  • agonist drugs
A
  • pharm: analgesia (central), respiratory depression
  • endo agonists: b-endorphin
  • agonist drugs: morphine
50
Q

Delta Opioid Receptor

  • pharm response
  • endogenous agonists
  • agonist drugs
A
  • pharm: analgesia
  • endo angonists: met/Leu-enkephalin, b-endorphin
  • agonist drugs: no drugs in clinical use
51
Q

Kappa Opioid Receptor

  • pharm response
  • endogenous agonists
  • agonist drugs
A
  • pharm: spinal analgesia
  • endo agonists: dynorphin 1-17
  • agonist drugs: pentazocine
52
Q

Opioid Receptor Function

A
  • dec. neuronal excitability
  • inhibition of presynaptic VSCC
  • activation of K channels leading to membrane hyperpolarization
  • inhibition of cAMP synthesis
53
Q

Analgesic Actions of Opioids

A
  • inhibition of spinal cord/ascending pain pathway
  • activation of descending pain pathway
  • also reduce subjective response to pain
54
Q

Side Effects of Opioids

A
  • respiratory depression
  • nausea, vomiting
  • cough suppression
  • pupillary constriction
  • constipation
  • histamine release
55
Q

Fentanyl

A
  • opioid mu receptor agonist
  • short duration of action
  • requires mechanical ventilation
56
Q

Buprenoprhine

A

-partial mu agonist that can precipitate mild withdrawl

57
Q

Clonidine

A

-used to treat withdrawl sx caused by opioid addiction

58
Q

Opioid Mechanism of Action

A
  1. inhibiting asc. pain pathway
  2. activating dec. pain pathway (inhibits inhibitory gabaergic interuerons in PAG)
  3. modulate perception of pain
59
Q

Enkephalin

A

-endogenous opioid

60
Q

NMDA Receptor Role in Pain

A
  • 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
Q

Adjuvant

A
  • 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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