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Pharmacology

Local anesthetic selection

Local anesthetics are typically divided into 3 main categories:

short, intermediate and long acting local anesthetics.

Based on duration of the procedure and the duration of the individual agents

 

Infiltration

Nerve block

 

Pulpal

Soft tissue

Pulpal

Soft tissue

Short

30 min

2-3 hrs

45 min

2-3 hrs

Intermediate

60 min

2-3 hrs

75-90 min

3-4 hrs

Long

40 min

5-6 hrs

3-4 hrs

6-8 hrs

 

Short acting agents

1. Mepivacaine 3 %

2. Lidocaine 2%

Intermediate acting agents

1. Lidocaine 2% 1:100000 epi

2. Lidocaine 2% 1:50000 epi

3. Mepivacaine 2% 1:20000 neocobefrin

4. Prilocaine 4%

5. Articaine 4% 1:100000 epi

Long acting agents

1. Bupivacaine 0.5% 1:200000 epi

EPHEDRINE

It act indirectly and directly on α and β receptors. It increases blood pressure both by peripheral vasoconstriction and by increasing the cardiac output. Ephedrine also relaxes the bronchial smooth muscles.

Ephedrine stimulates CNS and produces restlessness, insomnia, anxiety and tremors.
Ephedrine produces mydriasis on local as well as systemic administration.
Ephedrine is useful for the treatment of chronic and moderate type of bronchial asthma, used as nasal decongestant and as a mydriatic without cycloplegia. It is also useful in preventing ventricular asystole in Stokes Adams syndrome.

Agonist, Antagonist, and Partial Agonists

Agonists:  molecules that activate receptors.  A drug that mimics the body's own regulatory processes.
Antagonists:  produce their effects by preventing receptors activation by endogenous regulatory molecules and drugs.  Block activation of receptors by agonists.
Noncompetive Antagonist:  Bind irreversibly to receptors, and reduce the maximal response that an agonist can elicit.
Competitive Antagonist:  Bind reversibly to receptors, competing with agonists for binding sites.
Partial Agonists:  Have moderate intrinsic activity, the maximal effect that a partial agonist can produce is lower than that of a full agonist.  Act as antagonists as well as agonists.
 

Needle selection

Nerve blocks:

Inferior alveolar- 25 G short (LLU technique)

PSA- 25 G short

Mental/Incisive- 25 G short

Palatal- 27/30 G short/ultrashort

Gow-Gates/Akinosi- 25 G long

Infraorbital- 25 G long

Field Block:

ASA 25/27 short

Infiltration:

Infiltration/SP 25/27 short

PDL/Intraosseous

PDL 27/30 short

Intraosseous 30 short/ultrashort

Example calculations of maximum local anesthetic doses for a 15-kg child

Articaine

5 mg/kg maximum dose × 15 kg = 75 mg

4% articaine = 40 mg/mL

75 mg/(40 mg/mL) = 1.88 mL

1 cartridge = 1.8 mL

Therefore, 1 cartridge is the maximum

Lidocaine

7 mg/kg × 15 kg = 105 mg

2% lidocaine = 20 mg/mL

105 mg/(20 mg/mL) = 5.25 mL

1 cartridge = 1.8 mL

Therefore, 2.9 cartridges is the maximum

Mepivacaine

6.6 mg/kg × 15 kg = 99 mg

3% mepivacaine = 30 mg/mL

99 mg/(30 mg/mL) = 3.3 mL

1 cartridge = 1.8 mL

Therefore, 1.8 cartridges is the maximum.

Prilocaine

8 mg/kg × 15 kg = 120 mg

4% prilocaine = 40 mg/mL

120 mg/(40 mg/mL) = 3 mL

1 cartridge = 1.8 mL

Therefore, 1.67 cartridges is the maximum

Clotrimazole: Clotrimazole is a potent, specific inhibitor of p450 enzymes.

It is used in some antifungal medications, and in the treatment of yeast infections.

Opiate Antagonists

Opiate antagonists have no agonist properties. They are utilized to reverse opiate induced respiratory depression and to prevent drug abuse.

A. Naloxone

 Pure opiate antagonist , Short duration of action,  Only 1/50th as potent orally as parenterally

B. Naltrexone

Pure opiate antagonist, Long duration of action, Better oral efficacy

 

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