Local Anaesthesia Flashcards

1
Q

What is a local anaesthetic ?

A

a drug or agent which reversibly blocks neuronal transmission in the applied region causing a temporary loss of sensation/pain, without affecting consciousness

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2
Q

What is a general anaesthetic?

A

a drug or agent which produces a loss of response to painful stimulation (analgesia) and a loss of reflexes (motor and autonomic) with a reversible loss of consciousness

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3
Q

What is an analgesic?

A

a drug or agent which relieves and prevents pain without a loss of consciousness

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4
Q

What is a sedative?

A

a drug or agent which reduces irritability, excitement or nervousness

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5
Q

Where is LA injected?

A

Near nerve branches innervating the small, specific area of the body near the surgical site

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6
Q

Briefly state some reasons why LA is clinically useful

A

temporary and rapid in action, completely reversible
sufficient potency to provide complete anaesthesia
sufficient in duration to complete procedure comfortably
not irritating to tissues
does not produce allergic reaction (hypoallergenic)
not addictive
low degree of systemic toxicity
high therapeutic ratio

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7
Q

What was the first naturally occurring local anaesthetic

A

cocaine
Found in coca leaves

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8
Q

Who was the first clinician to inject cocaine to perform a peripheral nerve block? When did this take place?

A

William Halsted (1884)

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9
Q

What does a low therapeutic index refer to ?

A

This is when there is a small difference between the therapeutic and toxic doses of a drug

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10
Q

Give an example of a toxic effect of cocaine

A

respiratory depression

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11
Q

There is a potential for abuse an addiction when using cocaine. Briefly state why this is the case

A

CNS stimulant, psychological dependence
crave drugs euphoric and stimulatory effects

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12
Q

What are the short term CNS effects of cocaine?

A

Mydriasis (dilated pupils)
headache
nausea
vomiting
muscle tremors
twitching
pseudohallucinations (cocaine bugs)

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13
Q

What are the long term CNS effects of cocaine?

A

Generalised seizures
hallucinations
gross muscle tremors and twitching
decreased responsiveness to stimuli
increased deep tendon reflexes
incontinence

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14
Q

What are effects of a cocaine overdose on the CNS?

A

Generalised convulsions
cerebral infarction and haemorrhage
pupils fixed and dilated
flaccid paralysis
loss of vital support functions
CNS depression
coma

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15
Q

What are the short term cardiovascular system effect of cocaine?

A

vasoconstriction
hypertension
tachycardia
pallor

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16
Q

What are the long term cardiovascular effects of cocaine?

A

cardiac dysrhythmias
hypertension
tachycardia
peripheral cyanosis

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17
Q

What is cyanosis?

A

blue/grey lips or skin; happens when there is not enough blood supply to these areas

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18
Q

What are effects of a cocaine overdose on the cardiovascular system?

A

aortic dissection
MI
cardial arrest

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19
Q

What are short term respiratory effects of cocaine?

A

increase in breathing rate and depth

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20
Q

What are long term respiratory effects of cocaine?

A

abnormally rapid breathing (tachypnoea)
shortness of breath/gasping (dypnoea)
irregular breathing pattern

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21
Q

What are the effects on a cocaine overdose of the respiratory system?

A

respiratory depression
respiratory failure
cyanosis (lack of oxygen)
gross pulmonary oedema
paralysis of respiration

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22
Q

What are the short term effect of cocaine on the body temperature?

A

elevation

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23
Q

What are the long term effects of cocaine on the body temperature?

A

sever hyperthermia

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24
Q

What is the effect of a cocaine overdose on the body temperature?

A

Severe hyperthermia

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25
Q

What are the short term behaviour effect of cocaine?

A

euphoria
elation
excitation
restlessness (increased motor activity)
Garrulousness (excessively talkative)
alert
energetic
strong
paranoia

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26
Q

What are the short term behaviour effect of cocaine?

A

social maladjustment
paranoia
depression
agitation
difficulties with emotion regulation and impulse control
violent or suicidal tendencies

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27
Q

What is the effect of a cocaine overdose on behaviour?

A

death

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28
Q

Synthetic local anaesthetics are broadly split into ________ and _______.

A

Esters
Amide

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29
Q

State a method that can be used to identify ester and amide local anaesthetics

A

Amides have an “i” in the prefix before the “caine” whilst esters do not

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30
Q

Name some examples of ester LA

A

Cocaine
Procaine
Tetracaine
Benzocaine

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31
Q

Give some examples of amide LA

A

Bupivacaine
Lidocaine (lignocaine)
Articaine (has an ester side-chain)
Prilocaine

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32
Q

Regarding the structure of amides and esters; they both contain an ________

A

aromatic ring

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33
Q

Ester LAs are metabolised by …

A

plasma esterases

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34
Q

Amide LAs are metabolised by…

A

hepatic enzymes

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35
Q

What does pharmacokinetics refer to ?

A

what the body does to the drug
ADME

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36
Q

What does pharmacodynamics refer to?

A

what the drug does to the body

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37
Q

Local anaesthetic drugs are classified as …

A

Weak bases
BH+ <—-> B + H+
B exists as the unionised form

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38
Q

At the physiological pH of 7.4, all local anaesthetics will exist in what form ?

A

more will be in the ionised form as opposed to the unionised from

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39
Q

What affects the proportions of ionised V unionised forms of LA at physiological pH 7.4?

A

The pKa
How much exist in ionised form
How much exist in unionised form

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40
Q

What percentage of lidocaine exists in the unionised form?

A

25%

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41
Q

What percentage of bupivacaine exists in the unionised form?

A

15%

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42
Q

Between lidocaine and bupivacaine, which one of these would reach their target site more quickly and why?

A

lidocaine reaches the target site more quickly and has a faster onset of action because more of it exists in the unionised form and thus can cross the membrane and reach the target site much quicker

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43
Q

Why would LA delivery be less effective in a patient with irreversible pulptitis?

A

“Hot tooth” will have infected/inflamed tissue; infected environments tend to have a lower (acidic) pH; this means that a greater proportion of LA will exist in the ionised form (BH+)
the ionised form is unable to penetrate the cell membrane and therefore is less effective

Areas of inflammation also have an increased body supply due to vasodilation and thus this might increase “wash-out” before it can reach the site of action on the neurone

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44
Q

What are the 4 principles of local anaesthetics?

A

Lipid solubility
Dissociation constant
Chemical linkage
Protein binding

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45
Q

Lipid solubility correlates to the _______ of LA

A

potency

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46
Q

The dissociation constant (pKa) correlates to the ___________.

A

time of onset

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47
Q

The chemical linkage correlates to the ___________ of LA

A

metabolism

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48
Q

Protein binding correlated to the ___________ of LA

A

duration

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49
Q

Briefly state why the potency (lipid solubility) of LA is important

A

greater lipid solubility enhances diffusion through neuronal coverings (myelin sheath) and the cell membrane, thus allowing lower milligram dosage

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50
Q

What is the importance of the pKa of LA

A

It determines the portion of an administered dose that exists in the lipid soluble, unionised form at given pH

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51
Q

LA with a lower pKa have a _________ proportion in the unionised form. What is the benefit of this

A

Greater proportion in unionised form
this leads to a quicker onset

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52
Q

Ester LAs are hydrolysed by …

A

plasma cholinesterases

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53
Q

The duration of action of LA is dependent on _________

A

Protein binding at the receptor site (Na channels)
A higher affinity for proteins means that the LA remains at the site of action for longer period of time

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54
Q

The affinity of LA for proteins at the receptor site (with sodium channels) corresponds to…

A

Their affinity for plasma proteins
if they bind tightly to plasma proteins then they will do the same at the receptor site

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55
Q

What is the effect of local anaesthetic on neurones?

A

They disrupt the ion channel function within the neuronal cell membrane.
Thus preventing the transmission of the neuronal action potential

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56
Q

What is the MOA of local anaesthetics?

A

Once the unionise form has diffused into the neuron
The ionised form then blocks the voltage gated Na+ channels via the open gate from the intracellular side of the membrane

It acts as a physical plug which repels positively charged Na+ (the ionised form is also positively charged)

Therefore blocks initiation and propagation of action potentials

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57
Q

When do LAs gain access to the voltage gated Na+ channel? What is the consequence of this on the depth of the block observed?

A

In its open state
Therefore, the depth of the block increasease with action potential firing
Use dependence

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58
Q

What is use dependence?

A

This is the selective inhibition of hyper active neurons while minimising the effects on normal neuronal activity

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59
Q

LA differentially blocks neurons. Nerve fibres associated with what sensory modality are blocked first?

A

Nerve fibres associated with pain are blocked before other sensory modalities such as touch, pressure and proprioception.

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60
Q

What nerve fibres are blocked first?

A

Adelta and fibres (nociception, temperature, touch)
blocked before Abeta fibres (touch, pressure and proprioception)

61
Q

What other types of nerve fibres are blocked quicker?

A

myelinated nerve fibres are blocked unmyelinated
smal diameter nerve fibres are blocked before large diameter nerve fibres
- large diameter motor axons are relatively resistant

62
Q

During dental treatment, what is the order of sensation loss?

A

pain, temperatue, touch, proprioception (pressure), skeletal muscle tone (motor)
This is the reason why you may still feel touch but not pain during dental treatment

63
Q

When considering the site of injection, what should you take into account?

A

whether it is an area of high vascularity
an area of high vascularity will result in a greater uptake and high blood concentrations of the LA
consider systemic toxicity

64
Q

What is the uptake of local anaesthetic from greatest to lowest

A

IV>tracheal>intercostal>caudal>paracervical>epidural>bracial>sciatic>subcutaneous

65
Q

The peak blood concentrations of LA corresponds proportionally to …

A

the total dose administered

66
Q

What doe of LA should be used for a planned treatment?

A

the lowest dosage that results in effective anaesthesia for that planned treatment

67
Q

How can the maximum safe dose of LA be calculated ?

A

By multiplying the patients weight by the dosage factor

68
Q

What does a higher dosage factor mean?

A

A higher dosage factor means a higher maximum safe dose

69
Q

What is the maximum dosage of 2% lidocaine (dosage factor: 0.22) for a 57kg adult?

A

0.22ml/kg x 57kg= 12.54ml
1 cartridge= 2.2ml
12.54/2.2= 5.7 cartridges

Therefore; maximum number of safe cartridges for 2% lidocaine is 6 cartridges

70
Q

What is the maximum dosage of 2% lidocaine (dosage factor 0.22kg/ml) for a 20kg child?

A

0.22ml/kg x 20kg= 4.4ml
4.4/2.2= 2
2 cartridges

71
Q

What is the purpose of the addition of a vasoconstrictor to LA?

A

Most LAs have a direct vasodilator action
This increases the rate of absorption into systemic circulation which increases their potential toxicity
This reduces their LA action

vasoconstrictor keeps the LA at the site of action and limits their potential toxicity
Increasing their LA action

72
Q

Give examples of vasoconstrictors used in LA

A

Adrenaline
Felypressin

73
Q

What is the “gold standard” LA used in most dental procedures?

A

2% lidocaine 1: 80 000 epinephrine

74
Q

Individual local anaesthetics exhibit different rates of absorption. Give an example of this

A

at the brachial plexus blockade lidocaine is absorbed faster than prilocaine

75
Q

What kind of LA is absorbed at a slower rate ?

A

LA that is highly tissue bound are absorbed at a slower rate

76
Q

Absorption of individual LAs is dependent on…

A

their intrinsic ability to cause vasodilation

77
Q

Where are higher concentrations of local anaesthetics found during distribution?

A

In highly perfused organs such as kidneys, brain and heart

78
Q

What tissue has the highest level of distribution of LA after absorption and why?

A

skeletal muscle
it has the largest mass of tissue in the body

79
Q

Weak acids such as warfarin bind to what plasma protein?

A

Albumin

80
Q

Weak bases such as lidocaine bind to which plasma proteins?

A

acidic glycoproteins

81
Q

What is the advantage of drugs that have a higher affinity for plasma proteins?

A

they have a longer duration of action as only the free drug is available for metabolism

82
Q

Patients with a pseudocholinesterase deficiency may experience ____________ due to __________

A

LA toxicity
due to slower metabolism of ester drugs

83
Q

Some ester LA can be hydrolysed into _________. Give examples of LA that can be hydrolysed into this compound.

A

Paraaminobenzoic acid (PABA)
Procaine
Benzocaine

84
Q

PABA is associated with _____________. What is the implication of this?

A

allergic reactions
Can become a medical emergency

85
Q

What is an advantage of amide LA over ester LA?

A

They rarely cause allergic reactions

86
Q

What is a contraindication for amide LA use?

A

liver dysfunction
this means that amide LAs will be slowly metabolised and this can lead to LA toxicity

87
Q

Large doses of prilocaine can cause a condition known as _____________.

A

methhaemoglobinaemia
the metabolite of prilocaine causes methaemoglobin to be produced (oxygen delivery affected)

88
Q

What are some signs/symptoms of methaemoglobinaemia?

A

Dyspnoea (shortness of breath)
Cyanosis (purple lips or extremeties?); due to lack of oxygen in these areas

89
Q

PABA interferes with…

A

the antibacterial effect of sulphonamides

90
Q

A hypersensitivity reaction to PABA can present as…

A

swelling of the tongue, throat and face

91
Q

What is the onset of a PABA hypersensitivity reaction?

A

within 5 minutes
may be delayed for up to 40 minutes

92
Q

What are the symptoms associated with 3-15% methaemoglobin levels?

A

slight discoloration (pale, grey) of the skin

93
Q

What are the symptoms associated with 15-20% methaemoglobin levels?

A

cyanosis (patients are ususally asymptomatic)

94
Q

What are the symptoms associated with 25-50% methaemoglobin levels?

A

headache
light headedness
weakness
confusion
palpitations
chest pain

95
Q

What are the symptoms associated with 50-70% methaemoglobin levels?

A

abnormal cardiac rhythms
altered mental status
delirium
seizures
coma
profound acidosis

96
Q

What are the symptoms associated with 70% methaemoglobin levels?

A

death

97
Q

What forms/preparations are LAs available as?

A

solution for injection
sprays
creams
hel

98
Q

LAs are prepared as ___________ for LA base to be stable in solution

A

hydrochloride salt

99
Q

Give examples of topical anaesthesia

A

Lignocaine 5% gel, 10% spray
benzocaine 20% gel
EMLA (eutetic mixture of 2.5% lidocaine and 2.5% prilocaine)

100
Q

What preservatives are found in LA?

A

0.1% sodium meta-bisulphite with or without a fungicide
multidose vials contain 1mg/ml of methyl para-hydroxybenzoate

101
Q

What is an additive/adjuvant ?

A

increases the efficacy or potency of other drugs when given concurrently (at the same time)

102
Q

What are the benefits of using adrenaline as a vasoconstrictor?

A

-reduces traumatic blood loss from the site via same mechanism
-minimise vasodilator action of LA
-decrease the rate at which the drug is removed from the site of action by absorption into systemic circulation

103
Q

What is the purpose of the addition of bicarbonate to LA ?

A

more of the drug is present in the unionised for and thus this speeds up the onset of action

104
Q

The addition of too much bicarbonate to LA can lead to ____________

A

the precipitation of the LA

105
Q

The unionised form of LA is ______ soluble in water than the hydrochloride salt

A

less

106
Q

When is lidocaine (xylocaine) use contraindicated?

A

when there is an amide allergy or increased adrenaline may be hazardous (heart conditions?)

107
Q

What LA can be administered without a vasoconstrictor and why?

A

Mepivacaine (scandonest)
This is because it has less vasodilation effects

108
Q

What LA is widely used because of the long duration of action?

A

Bupivacaine (marcaine)

109
Q

What is the duration of plain lidocaine (without adrenaline) and lidocaine with adrenaline ?

A

10 minutes
1-2 hours

110
Q

When is prilocaine (citanest) use indicated?

A

when adrenaline needs to be avoided
- pt may have severe hypertension or unstable cardiac rhythm

-prilocaine with or without felypressin

111
Q

Why does articaine (septanest) have a short duration of action?

A

the chemical structure contains an amide linkage and an ester side chain; hydrolysis of the side chain in the plasma inactivates the drug

112
Q

Which type of tissue is blocked by LA first, pulp or soft tissue ?

A

soft tissue is blocked first

113
Q

Systemic toxicity of LA is ______ dependent

A

dose

114
Q

What are some unwanted CNS effect of LA ?

A

Light-headedness
drowsiness
numbness of tongue
restlessness
parasthesia
dizziness
blurred vision
tinnitus
headache
nausea
vomiting
convulsions
muscle twitching
tremors
respiratory failure
unconsciousness
coma

115
Q

What are some unwanted CVS effects of LA?

A

myocardial depression
peripheral vasodilation
hypotension
bradycardia
arrhythmias and cardiac arrest

116
Q

What LA has a tendency for cardiotoxicity?

A

Bupivacaine

117
Q

What LA has less of a tendency to cause CNS effects?

A

lidocaine

118
Q

What are some potential LA complications ?

A

-Ischaemic necrosis of tissues and nerve damage may follow injections of LA
-vascular damage
-drug error
-needle breakage and dental cartridge failure
-no anaesthetic block; block failure

119
Q

What can cause ischaemic necrosis of tissues and nerve damage following injections of LA?

A

irritating nature of solution
pressure from large volumes
constriction of vasculature by adrenaline

120
Q

Give an example of vascular damage caused by LA

A

haematoma

121
Q

Give another use of lidocaine drug (aside from anaesthetic agent)

A

used as an anti-arrhythmic at high doses in combination with other LA may cause myocardial depression or increase the risk of ventricular arrhythmias

122
Q

There is an increased risk of methaemoglobinaemia with prilocaine is a patient is concomitant _____________

A

sulphonamide e.g. co-trimoxazole

123
Q

There is an increased risk of ___________ if high doses of lidocaine are administered with antipsychotics that prolong the QT interval

A

ventricular arrhythmias

124
Q

What effects do antivirals have on lidocaine ? Give examples of these antivirals

A

they increase plasma concentration of lidocaine and potentially increase cardiotoxicity
Fosamprenavir
Darunavir
Atazanavir
Lipinavir
Saquinavir

125
Q

Lidocaine clearance is reduced by which beta-blockers?

A

propanolol
Possibly nadolol

126
Q

Lidocaine in combination with beta-blockers can cause …

A

myocardial depression

127
Q

What potential interaction can occur if diuretics such as acetazolamide is concurrently taken with lidocaine?

A

Acetazolamide causes hypokalemia (increased secretion of K+) which antagonised action of lidocaine
Hypokalemia antagonises action of lidocaine

128
Q

Sedative, midazolam has been reported to cause a modest reduction in serum _________ levels but not _________ levels

A

lidocaine
mepivacaine

129
Q

What LA uses felypressin vasoconstrictor?

A

prilocaine

130
Q

What LA considerations must you make for patients who abuse cocaine?

A

avoid using LA containing adrenaline in patients who abuse cocaine unless certain they have not used in >24 hours

131
Q

Cocaine and adrenaline have sympathomimetic effects. What does this mean?

A

combined use increases these effects and the risk of arrhythmias

132
Q

What is the name of the new long-acting LA ?

A

Ropivacaine
an effective alternative to bupivacaine

133
Q

Ropivacaine is an isomer of ____________ and is used mainly for _________ blocks

A

levobupivacaine
Mandibular nerve blocks

134
Q

What are the advantages of ropivacaine ?

A

lowe cariovascular toxicity
no need for adrenaline to achieve prolonged duration
lowers the need of postoperative analgesics

135
Q

What is the disadvantage of ropivacaine?

A

not available as dental cartridges

136
Q

What is Opaqix ?

A

EMLA (eutectic mixture of 2.5 % lidocaine and 2.5% prilocaine)

137
Q

What is the purpose of thermosetting agents in Opaqix ?

A

enables dispension as a liquid and change (in body tem) in periodontal pocket to a gel

138
Q

What is the benefit of Opaqix having a pH of 7.5-8.0?

A

it is effective in inflamed and infected tissue

139
Q

Contraindications for opaqix use include …

A

allergy to lidocaine, prilocaine or similar LA
congenital or idiopathic methaemoglobinaemia

140
Q

Intranasal administration is suitable for what kinds of patients ?

A

patients anxious of needles

141
Q

Give an example of LA administered intranasally

A

kovacaine mist nasal spray

142
Q

What is phentolamine mesylate (OraVerse) ?

A

an injection which is the first and only local dental anaesthesia reversal agent

143
Q

What is the function (use) of OraVerse?

A

reversal of soft tissue anaesthesia post dental procedure (e.g. numb lip or tongue)
this can help prevent injuries/symptoms associated with soft tissue parasthesia -self-inflicted injuries, uncontrolled drooling, perceied sense of altered appearance

144
Q

What is the MOA of phentolamine mesylate?

A

increase diameter of blood vessels in the area
increase blood flow removes extra LA which can be metabolised and excreted by liver and kidneys

145
Q

OraVerse is no suitable in what situations?

A

post-oral surgery where pain is anticipated

146
Q

Briefly state correct administration techniques for OraVerse (phentolamine mesylate)

A

same injection site and technique as LA
1:1 cartridge ratio to LA

147
Q

What is the maximum dose of OraVerse for adults?

A

2 cartiridges

148
Q

What is the maximum dose of OraVerse for children?

A

<1 cartridge