“Anesthesia and GENERAL ANESTHETICS”

What is Anesthesia?

Anesthesia is a medical procedure that induces a temporary and controlled state of loss of sensation or awareness,
enabling medical procedures to be performed without causing pain or distress to the patient. The main types of
anesthesia include:1. General Anesthesia: Causes a reversible loss of consciousness and sensation over the entire
body. It is typically used for major surgeries.2. Regional Anesthesia: Blocks sensation in a larger area of the body,
such as an entire limb or the lower half of the body (e.g., epidural anesthesia used during childbirth).3. Local
Anesthesia: Numbs a small, specific area of the body, typically used for minor surgical procedures.

What are Anesthetics?

Anesthetics are drugs used to induce anesthesia. They can be broadly classified into:1. General Anesthetics: These
drugs cause a loss of consciousness and sensation.2. Local Anesthetics: These drugs cause a loss of sensation in a
specific area without affecting consciousness.

Stages of General Anesthesia

General anesthesia can be divided into four stages:

1. Stage I (Analgesia Stage): - Begins with the administration of the anesthetic agent. - The patient experiences
analgesia without amnesia initially but progresses to both analgesia and amnesia. - Consciousness is maintained,
but the sensation of pain is diminished.

2. Stage II (Excitement Stage): - Characterized by delirium and violent, combative behavior. - The patient may
experience irregular breathing, increased heart rate, and blood pressure. - This stage is typically brief due to rapid
progression to the next stage.

3. Stage III (Surgical Anesthesia Stage): - Divided into four planes (light to deep surgical anesthesia). - The patient
becomes unconscious with regular breathing and progressive muscle relaxation. - This stage is ideal for surgical
procedures as it provides adequate depth of anesthesia.

4. Stage IV (Medullary Depression): - Occurs if there is an overdose of anesthetic agents. - Characterized by severe
depression of the respiratory and cardiovascular systems. - Without immediate intervention, it can lead to
respiratory arrest, circulatory collapse, and death.
Mechanism of General Anesthetics

Inhalational Anesthetics:

Gas

1. Nitrous Oxide: A colorless, odorless gas used for its analgesic and anesthetic effects. It works by inhibiting NMDA
(N-methyl-D-aspartate) receptors and modulating the release of neurotransmitters such as dopamine and
norepinephrine. Often used in combination with other anesthetics for balanced anesthesia. -

Adverse Effects: Hypoxia, nausea, vomiting, dizziness, and potential for abuse. -

Contraindications: Vitamin B12 deficiency, pneumothorax, middle ear disease, and during the first trimester of
pregnancy.

Volatile Liquids

1. Halothane, Enflurane, Isoflurane, Desflurane, Sevoflurane, Methoxyflurane: These agents are administered as
vapors and work by enhancing the effect of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) at
GABA-A receptors and modulating other ion channels like potassium channels. They reduce neuronal excitability
and induce a state of unconsciousness. Each has unique properties: -

Halothane: Potent but with significant side effects. -

Adverse Effects: Hepatotoxicity, arrhythmias, hypotension, respiratory depression, and malignant hyperthermia. -
Contraindications: History of halothane-induced hepatitis, susceptibility to malignant hyperthermia.

- Enflurane: Less commonly used due to risk of seizures.

- Adverse Effects: Seizures, hypotension, respiratory depression, nausea, and vomiting.

- Contraindications: Epilepsy, increased intracranial pressure.

- Isoflurane: Commonly used with a favorable safety profile.

- Adverse Effects: Hypotension, respiratory depression, arrhythmias, nausea, and postoperative shivering.

- Contraindications: Susceptibility to malignant hyperthermia.

- Desflurane: Rapid onset and recovery but can cause airway irritation.

- Adverse Effects: Coughing, breath-holding, laryngospasm, hypotension, and tachycardia. -

Contraindications: Severe respiratory diseases, susceptibility to malignant hyperthermia.

- Sevoflurane: Rapid onset and recovery, commonly used for induction in pediatric anesthesia.

- Adverse Effects: Nephrotoxicity, hypotension, respiratory depression, nausea, and vomiting. -

Contraindications: Susceptibility to malignant hyperthermia, renal impairment. -

Methoxyflurane: Potent but limited by nephrotoxicity. -

Adverse Effects: Nephrotoxicity, hepatotoxicity, respiratory depression, hypotension, and nausea. -

Contraindications: Renal disease, susceptibility to malignant hyperthermia.

Intravenous Anesthetics

Inducing Agents

1. Thiopentone, Methohexitone, Propofol, Etomidate, Dexmedetomidine: These agents induce anesthesia quickly,
primarily by enhancing GABAergic activity, increasing chloride ion influx into neurons, leading to hyperpolarization
and decreased neuronal excitability. -

Thiopentone and Methohexitone: Barbiturates that induce rapid unconsciousness, primarily used for induction and
short procedures.

- Adverse Effects: Respiratory depression, hypotension, myocardial depression, allergic reactions, and prolonged
recovery.
- Contraindications: Porphyria, severe cardiovascular diseases.

- Propofol: A widely used agent known for its rapid onset and short duration of action, with antiemetic properties.

- Adverse Effects: Hypotension, respiratory depression, bradycardia, pain on injection, and hypertriglyceridemia.

- Contraindications: Allergies to eggs or soy products, lipid metabolism disorders.

- Etomidate: Known for cardiovascular stability, suitable for patients with heart disease.

- Adverse Effects: Myoclonus, adrenal suppression, nausea, vomiting, and pain on injection. -

Contraindications: Adrenal insufficiency, severe sepsis. -

Dexmedetomidine: An alpha-2 adrenergic agonist providing sedation, analgesia, and anxiolysis without respiratory
depression.

- Adverse Effects: Hypotension, bradycardia, dry mouth, nausea, and prolonged sedation.

- Contraindications: Advanced heart block, severe ventricular dysfunction.

Slower Acting

1. Fentanyl: An opioid used for its potent analgesic properties. It binds to opioid receptors, particularly the mu-
receptor, reducing pain perception and response. -

Adverse Effects: Respiratory depression, bradycardia, constipation, nausea, and sedation.

- Contraindications: Severe respiratory depression, acute asthma, gastrointestinal obstruction.

2.Diazepam, Lorazepam, Midazolam: These drugs enhance the effect of GABA, leading to sedation, muscle
relaxation, and anxiolysis.

- Adverse Effects: Drowsiness, respiratory depression, hypotension, amnesia, and dependency. -

Contraindications: Severe respiratory insufficiency, sleep apnea, myasthenia gravis.

Dissociative Anesthesia

1. Ketamine: A dissociative anesthetic that works by blocking NMDA receptors, leading to analgesia and a trance-
like state without complete loss of consciousness.

- Adverse Effects: Hallucinations, increased intracranial pressure, hypertension, tachycardia, and nausea. -

Contraindications: Severe hypertension, increased intracranial pressure, psychosis.

“LOCAL ANESTHETICS”

Local Anesthetics: Detailed Mechanism, Adverse Effects, Drug Interactions, and Contraindications

Mechanism of Action:

Local anesthetics block sodium channels in neuronal cell membranes, preventing the initiation and
propagation of action potentials. This blockade inhibits the transmission of nerve impulses, leading to
a reversible loss of sensation in the area where the anesthetic is applied. Local anesthetics are
classified into two main types based on their chemical structure: esters and amides.

Injectable Anesthetics:

Low Potency, Short Duration:

1. Procaine

• Mechanism:

Procaine is an ester-type local anesthetic. It blocks voltage-gated sodium channels on the neuronal
cell membrane, reducing the influx of sodium ions, which in turn inhibits the depolarization of the
neuron. This prevents the propagation of nerve impulses, leading to loss of sensation in the targeted
area.

• Adverse Effects:

• Allergic reactions (due to the metabolite para-aminobenzoic acid (PABA))

• Hypotension

• Bradycardia

• Central nervous system (CNS) toxicity, including dizziness, confusion, and seizures

• Methemoglobinemia (rare)

• Drug Interactions (DI):

• Sulfonamide antibiotics: PABA, a metabolite of procaine, can inhibit the antibacterial action of
sulfonamides.

• Other ester anesthetics: Increased risk of systemic toxicity when combined.

• Contraindications:

• Known hypersensitivity to ester-type local anesthetics or PABA

• Severe cardiovascular disease

 • Myasthenia gravis

2. Chloroprocaine

• Mechanism:

Chloroprocaine is another ester-type local anesthetic with a similar mechanism of action to procaine,
blocking voltage-gated sodium channels and preventing nerve impulse transmission.

• Adverse Effects:

• CNS toxicity, including restlessness, tremors, and seizures

• Hypotension

• Cardiac arrhythmias

• Allergic reactions (less common than with procaine)

• Respiratory depression (high doses)

• Drug Interactions (DI):

• Similar to procaine, interactions with sulfonamide antibiotics and other ester anesthetics can
increase systemic toxicity.

• Contraindications:

• Similar to procaine, including hypersensitivity to ester-type anesthetics and severe

cardiovascular conditions.

Intermediate Potency and Duration:

1. Lidocaine (Lignocaine)

• Mechanism:

Lidocaine is an amide-type local anesthetic. It binds to and inhibits voltage-gated sodium channels on
the neuronal cell membrane, blocking the initiation and propagation of action potentials.

• Adverse Effects:

• CNS toxicity: Symptoms include dizziness, tinnitus, tremors, and seizures.

• Cardiovascular effects: Hypotension, bradycardia, and, in severe cases, cardiac arrest.

• Allergic reactions: Rare but possible, often related to preservatives used in multi-dose vials.
 • Methemoglobinemia (rare)

• Peripheral nerve damage (prolonged use)

• Drug Interactions (DI):

• Beta-blockers: Can increase lidocaine levels, increasing the risk of toxicity.

• Antiarrhythmic drugs (e.g., amiodarone): Additive effects can lead to severe cardiac depression.

• Other local anesthetics: Combined use increases the risk of systemic toxicity.

• Contraindications:

• Severe liver disease (lidocaine is metabolized in the liver)

• Known hypersensitivity to amide-type local anesthetics

• Complete heart block (without a pacemaker)

2. Prilocaine

• Mechanism:

Prilocaine is an amide-type local anesthetic similar to lidocaine, blocking sodium channels and
preventing nerve impulse transmission.

• Adverse Effects:

• Methemoglobinemia: Prilocaine can cause elevated levels of methemoglobin, reducing the

oxygen-carrying capacity of blood.

• CNS toxicity: Symptoms include drowsiness, dizziness, and seizures.

• Cardiovascular effects: Hypotension, bradycardia.

• Allergic reactions: Rare.

• Drug Interactions (DI):

• Nitrites and sulfonamides: Can increase the risk of methemoglobinemia.

• Beta-blockers: Can increase prilocaine levels and toxicity.

• Other local anesthetics: Combined use increases the risk of systemic toxicity.

• Contraindications:
 • Severe liver disease

• Known hypersensitivity to amide-type local anesthetics

• Congenital or idiopathic methemoglobinemia

High Potency, Long Duration:

1. Tetracaine

• Mechanism:

Tetracaine is an ester-type local anesthetic. It blocks voltage-gated sodium channels on the neuronal
cell membrane, preventing the propagation of nerve impulses.

• Adverse Effects:

• CNS toxicity: Symptoms include nervousness, tremors, and seizures.

• Cardiovascular effects: Hypotension, bradycardia, cardiac arrest.

• Allergic reactions: More common due to ester structure.

• Methemoglobinemia (rare)

• Drug Interactions (DI):

• Sulfonamide antibiotics: PABA, a metabolite of tetracaine, can inhibit the action of sulfonamides.

• Other ester anesthetics: Combined use increases the risk of systemic toxicity.

• Contraindications:

• Known hypersensitivity to ester-type anesthetics or PABA

• Severe cardiovascular disease

• Myasthenia gravis

2. Bupivacaine

• Mechanism:

Bupivacaine is an amide-type local anesthetic. It blocks sodium channels on the neuronal cell
membrane, preventing the initiation and propagation of nerve impulses.

• Adverse Effects:
 • CNS toxicity: Symptoms include dizziness, tinnitus, seizures, and coma.

• Cardiovascular effects: Hypotension, bradycardia, arrhythmias, cardiac arrest (more cardiotoxic

than lidocaine).

• Allergic reactions: Rare.

• Peripheral nerve damage (prolonged use)

• Drug Interactions (DI):

• Beta-blockers: Can increase bupivacaine levels, increasing the risk of toxicity.

• Antiarrhythmic drugs: Additive effects can lead to severe cardiac depression.

• Other local anesthetics: Combined use increases the risk of systemic toxicity.

• Contraindications:

• Severe liver disease

• Known hypersensitivity to amide-type local anesthetics

• Complete heart block (without a pacemaker)

3. Ropivacaine

• Mechanism:

Ropivacaine is an amide-type local anesthetic. It works by blocking voltage-gated sodium channels,

inhibiting the propagation of nerve impulses.

• Adverse Effects:

• CNS toxicity: Symptoms include dizziness, seizures, and confusion.

• Cardiovascular effects: Hypotension, bradycardia, arrhythmias (less cardiotoxic than

bupivacaine).

• Allergic reactions: Rare.

• Peripheral nerve damage (prolonged use)

• Drug Interactions (DI):

• Beta-blockers: Can increase ropivacaine levels, increasing the risk of toxicity.

• Antiarrhythmic drugs: Additive effects can lead to severe cardiac depression.

 • Other local anesthetics: Combined use increases the risk of systemic toxicity.

• Contraindications:

• Severe liver disease

• Known hypersensitivity to amide-type local anesthetics

• Complete heart block (without a pacemaker)

4. Levobupivacaine:

• Mechanism:

Levobupivacaine is an amide-type local anesthetic. It blocks sodium channels, inhibiting nerve

impulse transmission.

• Adverse Effects:

• CNS toxicity: Symptoms include dizziness, seizures, and confusion.

• Cardiovascular effects: Hypotension, bradycardia, arrhythmias (less cardiotoxic than

bupivacaine).

• Allergic reactions: Rare.

• Peripheral nerve damage (prolonged use)

• Drug Interactions (DI):

• Beta-blockers: Can increase levobupivacaine levels, increasing the risk of toxicity.

• Antiarrhythmic drugs: Additive effects can lead to severe cardiac depression.

• Other local anesthetics: Combined use increases the risk of systemic toxicity.

• Contraindications:

• Severe liver disease

• Known hypersensitivity to amide-type local anesthetics

• Complete heart block (without a pacemaker)

Surface Aesthetics

Soluble:
 1. Cocaine

• Mechanism:

Cocaine is an ester-type local anesthetic. It blocks sodium channels and also inhibits the reuptake of
norepinephrine, leading to vasoconstriction.

• Adverse Effects:

• CNS toxicity: Excitement, restlessness, seizures.

• Cardiovascular effects: Hypertension, tachycardia, arrhythmias.

• Vasoconstriction: Can cause tissue necrosis.

• Addiction and abuse potential.

Lidocaine, Tetracaine, Proparacaine

1. Lidocaine:

• Mechanism:

• Blocks voltage-gated sodium channels in nerve cells, preventing the propagation of action
potentials and resulting in loss of sensation.

• Adverse Effects:

• CNS: Drowsiness, confusion, seizures.

• Cardiovascular: Hypotension, arrhythmias.

• Allergic reactions: Rare but possible.

• Drug Interactions:

• May interact with other antiarrhythmics (e.g., quinidine, procainamide) increasing the risk of
cardiac side effects.

• Caution with other CNS depressants.

• Contraindications:

• Severe heart block.

• Known hypersensitivity to lidocaine or other local anesthetics.

2. Tetracaine:

• Mechanism:

• Blocks sodium channels in nerve fibers, similar to lidocaine but with a longer duration of action.

• Adverse Effects:

• CNS: Drowsiness, confusion, seizures.

• Cardiovascular: Hypotension, bradycardia.

• Allergic reactions: Possible but rare.

• Drug Interactions:

• May enhance effects of other CNS depressants.

• Caution with antiarrhythmics and other local anesthetics.

• Contraindications:

• Severe cardiovascular disease.

• Hypersensitivity to tetracaine or similar anesthetics.

3. Proparacaine:

• Mechanism:

• Blocks sodium channels in sensory nerves, leading to localized numbing with a rapid onset and
short duration.

• Adverse Effects:

• Ocular irritation, redness, and discomfort.

• Rare systemic effects if absorbed: dizziness, headache.

• Drug Interactions:

• Minimal systemic interactions due to its topical use.

• Caution when used with other ocular medications.

 • Contraindications:

• Known hypersensitivity to proparacaine.

• Avoid in patients with eye infections where corneal damage could occur.

Insoluble Anesthetics:

1. Benzocaine:

• Mechanism:

• Blocks sodium channels on nerve endings, leading to localized numbness.

• Adverse Effects:

• Methemoglobinemia (particularly in children and with large doses).

• Allergic reactions: rash, itching.

• Drug Interactions:

• Rarely interacts with other drugs but caution with other local anesthetics.

• Contraindications:

• Known hypersensitivity to benzocaine.

• Use with caution in patients with methemoglobinemia or anemia.

2. Oxetazene:

• Mechanism:

• Similar to other local anesthetics, blocks sodium channels to prevent nerve signal propagation.

• Adverse Effects:

• Allergic reactions: itching, rash.

• Systemic toxicity: rare but may include CNS symptoms.

• Drug Interactions:

• Caution with other local anesthetics and CNS depressants.

 • Contraindications:

• Hypersensitivity to oxetazene.

• Not recommended in patients with significant cardiovascular or hepatic disease.

3. Benzylaminobenzoate:

• Mechanism:

• Local anesthetic action through sodium channel blockade.

• Adverse Effects:

• Allergic reactions: skin irritation, rash.

• Systemic toxicity: rare, but possible CNS symptoms with overdose.

• Drug Interactions:

• Minimal interactions with other drugs due to local application.

• Contraindications:

• Hypersensitivity to the compound.

• Use with caution in patients with compromised skin integrity.

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