Local Anesthetics Flashcards

1
Q

Function of LA

A

Prevent transmission of nerve impulse in region to which its applied without affecting consciousness

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2
Q

Which are the topical LAs

A

Lignocaine
Prilocaine
Tetracaine
Benzocaine
Oxybuprocaine

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3
Q

Which are the injectable LAs

A

Bupivacaine
Levobupivicaine
Lignocaine
Mepivacaine
Ropivacine

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4
Q

MOA of LAs

A

block voltage gated Na channels and reduce infux of Na ions
=prevention of depolarisation of membrane by blocking AP

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5
Q

Steps in LA MOA

A

Unionised LA diffuses across CM
LA becomes ionised due to lower intracellular pH
Ionised LA blocks NA channel=prevent propagation of APs

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6
Q

Effects of infected tissue on LA

A

Infected tissue have decr. pH
therefore, fraction of ionised LA is reduced
=reduced effect
Infected tissue have incr. blood supply
= more LA removed from local area before it can have an effect

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7
Q

How does diameter influence LA

A

Smaller diameter nerve fibre= more blocade as compared to Larger diameter fibres

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8
Q

How does myelination affect LA

A

Myelinated fibres are more susceptible to blockade compared to unmyelinated fibres of same size

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9
Q

Order in Fibers blockade

A
  1. Sympathetic and pain
  2. Temperature
  3. Light touch and Proprioception
  4. Motor
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10
Q

Order in fiber recovery

A
  1. Motor
  2. Light touch and Proprioception
  3. Temperature
  4. Sympathetic and pain
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11
Q

DOA of LA depends on

A

-uptake into general circulation
-addiction of vasoconstrictor (AE/E, Levonodefrine)

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12
Q

Effects of adding vasoconstrictor to LA

A

Localise LA at desired site
Prolonged DOA
Reduced local hemorrhage
Reduce amount of LA absorbed into SC
Decrease toxcity

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13
Q

DI of Vasoconstrictor

A

TCAs: potentiate HT effect
Non-selective B-Blockers: incr. BP, reflex decr. HR, monitor BP
Cocaine, Methamphetamine abusers:
incr. risk HT crisis, stroke, MI
Digoxin: narrow TI=cardiac arrythmias

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14
Q

CI of Vasoconstrictors

A

Severe Heart disease
Uncontrolled Hyperthyroidism
Sulphite allergies
Asthmatics (corticosterioid-dependent)
Pheochromocytoma

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15
Q

Topical anaesthesia provide

A

Short term relief
High LA conc. in an oily vehicle slowly penetrate skin or mucous membrane

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16
Q

Infiltration anaesthesia provide

A

numbness faster than topical anesthesia.
LA is injected transdermally/subcutaneously by the area to be anaesthetised

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17
Q

Peripheral nerve block anesthesia provide

A

provide fields of anaesthesia distal to site of injection
Injection of LA around a nerve trunk

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18
Q

Which are the nerve block LAs

A

Bupivacaine
Lignocaine
Ropivacine
Mepivacaine

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19
Q

Central nerve block anaesthesia provide

A

produce anaesthesia above and below site of injection
LA is injected near the spinal cord

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20
Q

E.g of Central nerve block anaesthesia

A

Epidural anesthesia

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21
Q

Which are the Central nerve block LA

A

Bupivacaine
Lignocaine
Ropivacaine

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22
Q

IV regional anaesthesia allow for

A

Manipulation of fractures and minor surgical procedures
LA is injected into a limb after application of tourniquet

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23
Q

Which are the IV regional LA

A

Lignocaine

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24
Q

Which LAs are esters

A

Benzocaine
Oxybuprocaine
Tetracain

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25
Which LAs are amides
All have 2 'i's in them Bupivacaine Lignocaine Ropivacaine Mepivacaine Prilocaine Articaine
26
Metabolism of ester LA
Via Plasma cholinesterases
27
Metabolism of aminde LAs
Cytochrome P450
28
AEs of LAs
Psychogenic: alteration in BP, nausea, vomiting. hyperventilation, syncope Toxcity: CNS, CVS (bupivocaine) and respiratory distress Allergy: PABA, metabisulfate (with vasoconstrictors) Parasthesia: more common in Articaine Methaemoglobinaemia
29
LA toxicity results in
SAMS Slurred speech Altered CNS Muscle Twitching Seizures
30
CNS symptoms in LA toxicity
Slurred speech Tingling of lips Reduced level of consciousness Seizures
31
CVS symptoms in LA toxicity
Reduced myocardial contractility Arrythmias Hypotension: treated with vasodepressors Ventricular fibrillation caused by Bupivacaine: treated with Intralipid infusion
32
Indications of Bupivacaine
Local infiltration, nerve block, spinal, epidural Chiefly used for surgical anaesthesia Useful in providing several days of analgesia
33
Metabolism of Bupivacaine
Liver
34
Onset of action of Bupivacaine
Slow: 30 mins
35
DOA of Bupivacaine
3hrs Peripheral bloc: 2-24hrs
36
Bupivacaine is mostly used in
Labour and postoperatively Also capable of producing prolonged anesthesia: is potent
37
What is Levobupivacaine
is a S-enantiomer of bupivacaine Has a better CV safety profile than Bupivacaine
38
Indications of Lignocaine
Local/tropical Infiltration IV regional anaesthesia (biers block) Epidural anesthesia Eye blocks
39
Onset of action of Lignocaine
Rapid
40
DOA of lignocaine
Intermediate
41
CI of lignocaine
Heart block/conduction disturbances
42
DI of Lignocaine
Cimetidine/beta blockers NMB
43
Lignocaine is used as
Topical spray: larynx Jelly: urethral anesthesia and haemorrhoids Patch: (5%,S4) neuropathic pain relief (PHN)
44
DOA of Mepivacaine
Intermediate
45
Mepivacaine is used in
Dental practice
46
Indications of Mepivacaine
Infiltration Nerve blocks
47
Metabolism of Mepivacaine
Liver enzymes
48
DOA of Ropivacaine
Long
49
Indications of Ropivacaine
Epidural Local nerve block Infiltration Analgesia
50
Metabolism of Ropivacaine
Liver enzymes
51
Cautions in Ropivacaine
partial or complete heart block Elderly Liver dysfunction
52
Articaine is used in
Dental and Periodontal procedures
53
Indications of Articaine
Infiltration Nerve blocks
54
What is articaine: an ester or amide
Is an amide but contains a an ester side chain which is hydrolysed-plasma esterases
55
T1/2 of articaine
20-40mins
56
Onset of action Articaine
Rapid: 1-6mins
57
Commonly used formulation of Articaine
4% articaine with epinephrine
58
Prilocaine is used as
Topical anesthesia Patch: min app. time of 1hr Cream: Mucosa- apply and leave unoccluded for 10-15mins Intact skin: apply a thick layer and cover with an occlusive dressing for 1-2hrs (analgesia: apply +- 2hrs after removal of dressing)
59
Tetracaine is used for
Topical cream: pain relief in haemorrhoids and minor skin burns Eye drops: opthalmology in tonometry, foreign body removal, suture removal Oral gel: pain relief of mucous membranes of mouth, lips and gums
60
Benzocaine is used for
Topical gel: dentistry injection site-minimises sensation Lozenge: surface anaesthetic-pain relief of sore throats Throat spray Throat gargle
61
Oxybuprocaine is used for
Eye drops: opthalmology in tonometry, foreign body removal, suture removal
62
Oxybuprocaine has
an additive bactericidal activity