Local anesthetics

Local Anesthesia
• Local anesthetics block nerve conduction of
sensory impulses and in higher concentration
block motor impulses from periphery to CNS.
 Delivery techniques
• Topical administration
• Infiltration
• Spinal block
• Epidural block
Classification of drugs
Mechanism of action
Indications
Lidocaine
Side effects
 Complications of local anesthetics
• Pain on injection
• Burning on injection
• Failure to obtain anesthesias
• Soft tissue injury
• Hematoma
• Infections
 Toxicity
• CNS effects :
1. Lightheadedness
2. Sedation
3. Restlessness
4. Nystagmus
5. Tonic clonic convulsions
6. Severe convulsions followed by respiratory and
cardiovascular depression.
 Cardiovascular side effects
• With the exception of cocaine all causes
vasodilation(hypotension)
• Can convert heart disease into heart blocks
(arrythmias)
 Imp mcq
Which drug are cardiotoxic
1. Bupivacaine (both
hypotension and
arrythmias )
2. Ropivicaine
• Imp

Which Drug effects the hemoglobin in

blood ?
• Prolicaine is metabolized to by hepatic
enzymes into orthotoludine, an agent that
converts Hemoglobin into methemoglobin
 Management of toxicity (imp)
• Treatment is symptomatic
• No antidotes used
• Oxygen therapy to treat hyperventilation
• Convulsions are treated with IV diazepam
Alcohol
 Mechanism of action
• Enhance inhibitory action of GABA
• INHIBITS Activating effect on NMDA
Glutamate receptors
• Modify the activity of adenyl cyclase ,
phospholipase C and ion channels.
Ethanol
Effects of alcohol
 Dose related effects
Acute effects
1. 60_80 mg /dl:
• Impairment of driving in non tolerant person
• Slurring of speech
• Ataxia
• 120_130 mg/dl
Increase sedation
Decrease mental acuity
• Greater than 300 mg/dl
1. Loss of consciousness
2. Profound respiratory depression
3. Profound cardiovascular reaction
4. coma
• Greater than 500 mg /dl
Lethal
 Chronic effects
1. Liver disease
2. Peripheral neuropathy
3. Wernicke’s encephalopathy
4. Pancreatitis and gastritis
5. Heart disease
6. Fetal alcohol syndrome
 Fetal alcohol syndrome
• Ethanol used in pregnancy is associated with
teratogenic effects that includes
1. Mental retardness
2. Growth deficiencies
3. Microcephaly
4. Undevelopment of midface region.
 Acute alcohol intoxication(
Management)
1. Maintenance of vital signs and prevention of
aspiration after vomiting.
2. Thiamine administration to treat Wernicke’s
Korsakoff syndrome.
3. Correction of electrolyte imbalance.
Alcohol withdrawal syndrome
 Management of Alcohol withdrawal
Syndrome
• Correction of electrolyte imbalance
• Administration of thiamine
• Long acting bezodiazepene ( diazepam)
• If liver is not normal then give lorazepam.
 Treatment of alcoholism
• Opioid receptor antagonist Naltrexone
• Acamprosate an NMDA glutamate receptor
antagonist is FDA approved for treatment of
alcoholism.
• DISULFIRAM ( Alcohol dehydrogenase
inhibitor)
DISULFIRAM LIKE REACTION
Alcohol dehydrogenase inhibitor
Methanol poisoning
 Ethylene glycol poisoning
• Renal damage
• Severe acidosis
Skeleton muscle relaxant
Neuromuscular blocking agents

• Depolarizing Succinylcholine
Mechanism of action
 Pharmacokinetics
• Parental : Short duration of action (IV)
• Inactivated by plasma esterases
Adverse effects
 Imp mcq
• Which is most common
side effect of
succinylcholine ?
• Hyperkalemia
 Vimp point
• Which drug is used to treat
malignant hyperthermia ?
• Dantrolene
Non depolarizing Skeleton muscle
relaxant
Adverse effect
• Histamine
release
(mivacurium
and
tubocurarine)
Centrally acting skeleton
muscle relaxants
Hofmann elimination ( proff viva
question)
• Which drug is used for acute muscle
spasm?
Cyclobenzaprine ( act by interfering with
postsynaptic reflexes that maintain
skeleton muscle tone)
 Side effect of Cyclobenzaprine
• Confusion
• Visual hallucinations