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Pharmacology > Analgesia (Final) > Flashcards

Analgesia (Final) Flashcards

1
Q

What are the four steps of nociception, and where do they each take place?

A
  • transduction (peripheral tissue)
  • transmission (via peripheral nerves)
  • modulation (in spinal cord)
  • perception (in the brain)
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2
Q

Local Anesthetics

  • main action
  • chemical structure
A
  • cause reversible blockade of transmission in peripheral nerves or spinal cord (stops pain signals)
  • consist of an aromatic group joined to a tertiary amine group by either an amide or ester
  • all weak bases
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3
Q

Describe the MOA of local anesthetics

A
  • block propagation of an action potential by inhibiting influx of Na through voltage-gated Na channels
  • must be non-ionized to enter cell, but inside, the ionized form interacts with the Na receptor
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4
Q

Describe the metabolism of local anesthetics

A
  • ester LAs are rapidly broken down by plasma esterases
  • amide LAs are mainly metabolized in the liver
  • metabolites are excreted in the urine
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5
Q

What are the clinical uses of local anesthetics?

A
  • regional anesthesia (minor procedures, lameness localization)
  • pre and post-operative analgesia (nerve blocks, epidurals)
  • operative analgesia (with sedation)
  • treatment of ventricular arrhythmias
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6
Q

What are adverse affects of local anesthetics?

A
  • local irritation
  • CNS stimulation (muscle twitch, tremors, seizures)
  • CNS depression (unconsciousness, respiratory arrest)
  • cardiovascular depression (bradycardia, vasodilation, hypotension)
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7
Q

Lidocaine

  • type of drug
  • onset/duration
  • which animals are more sensitive?
  • contraindication?
A
  • amide local anesthetic
  • rapid onset, medium duration
  • cats more sensitive than dogs
  • sheep more sensitive that other livestock
  • banned in food animals
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8
Q

Systemic use of Lidocaine

A
  • class 1B antiarrhythmic used to control ventricular arrhythmias
  • CRI as adjunctive analgeisa (MLK drips)
  • CRI as a GI prokinetic/anti-inflammatory
  • prevention of reperfusion injury/endotoxemia
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9
Q

Local use of Lidocaine

- formulations

A
  • solution for injection
  • may contain epinephrine
  • some mixed with sodium bicarbonate to reduce pain
  • used topically
  • EMLA cream
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10
Q

Bupivacaine

  • type of drug
  • onset/duration
  • caution
A
  • amide local anesthetic
  • slow onset and duration
  • most cardiotoxic of LAs
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11
Q

Mepivacaine

  • type of drug
  • use
  • duration
A
  • amide local anesthetic
  • used for diagnostic nerve blocks in horses
  • duration longer than lidocaine
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12
Q

Procaine

  • type of drug
  • use
  • caution
A
  • ester local anesthetic
  • won’t use as an LA, but is in some penicillin G preparations
  • toxic, can cause CNS stimulation, don’t give IV
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13
Q

Proparacaine

  • type of drug
  • use
  • onset/duration
A
  • ester local anesthetic
  • used topically, ophthalamic
  • allows for corneal and conjunctival manipulation
  • rapid onset, short duration
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14
Q

What is the function of TXA2, and why do we block it?

A
  • promotes platelet aggregation

- block to prevent thromboembolism from certain diseases

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15
Q

Describe the actions of PGE1

A
  • involved with GI mucosal maintenance and vasodilation in kidney, in response to decreased blood flow
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16
Q

What is produced by COX-1?

By COX-2?

A

COX-1: prostaglandins important for homeostasis

COX-1: prostaglandins produced during inflammation

17
Q

What are the types of NSAIDs?

4

A
  • COX-1 selective inhibitors
  • non-specific COX inhibitors
  • COX-2 preferential inhibitors
  • COX-2 selective inhibitors
18
Q

Describe the anti-inflammatory effects of NSAIDs

A
  • inhibit synthesis of eiconsanoids (thromboxane, prostacyclin, prostaglandins)
  • not as potent as glucocorticoids
  • do not delay wound healing or lead to immunosuppression
  • greater effect on acute inflammation than chronic
19
Q

Describe the analgesic effects of NSAIDs

A
  • provide analgesia whether there is inflammation or not
  • decreases PG sensitization of neurons
  • central
20
Q

Piroxicam

  • type of drug
  • use
A
  • NSAID

- used to block COX-2, resulting in anti-neoplastic effects

21
Q

What are some adverse effects of NSAIDs

A
  • GI irritation/ulceration (PGs involved in maintenance of GI homeostasis)
  • renal damage (PGs control vasodilation of renal vascular beds)
  • hepatotoxicity
  • increased bleeding time
  • bone marrow suppression
22
Q

Flunixin Meglumine

  • type of drug
  • administration
  • cautions
A
  • large animal NSAID
  • given PO, IV, IM
  • labeled only for IV use in cattle and IM in swine
  • do not use IM in equines
  • intracarotid injection can cause seizures/CNS stimulation
  • caution with GI, renal, hepatic, or hematologic diseases
  • do not use in small animals, avoid in birds
23
Q

Phenylbutazone

  • type of drug
  • animals
  • use
  • administration
  • cautions
A
  • NSAID
  • used in horses, banned in dairy cattle
  • used for musculoskeletal pain
  • PO, labeled for IV
  • do not give IM/SC (very irritating)
  • caution with GI, renal, hepatic, or hematologic disease
  • can mask lameness
24
Q

Carprofen

  • type of drug
  • use
  • administration
A
  • COX-2 preferential NSAID
  • used in small animals as analgesic and anti-inflammatory agents
  • oral and injectible
25
Q

Firocoxib

  • type of drug
  • administration
A
  • COX-2 selective NSAID
  • oral paste for horses
  • chewable tablets for dogs
26
Q

Robenacoxib

- type of drug

A

COX-2 selective NSAID

- approved for multiple doses in cats

27
Q

Explain the washout periods for switching between NSAIDs and steroids

A

NSAID to steroid: sufficient washout period, 1-2 weeks
Steroid to NSAID: wean the steroid, then have at least 1 week washout period
NSAID to another NSAID: washout based on half-life or use at least 1 week

28
Q

Which drug is the only NSAID labeled for cattle, and what is it used for?

A
  • Flunixin meglumine

- control of pyrexia associated with bovine respiratory disease, endotoxemia, and mastitis

29
Q

Grapiprant

- type of drug

A
  • non-COX inhibiting NSAID

- antagonist at prostaglandin E2 EP4 receptor

Pharmacology (14 decks)

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