THEME: General Anesthetics
THEME: General Anesthetics
ANESTHETICS
INTRAVENOUS ANESTHETIC AGENT
Rapid induction of anesthesia Must be injected slowly (IV). If given IM or intra-arterially, it will cause gangrene. Recovery from intravenous anesthetic is due to redistribution from sites other than CNS Drugs Barbiturate Thiopentone 1. Cheap, use long time ago (1915) Mechanism of action 1. Cause change in lipid metabolism (lipid theory) 2. Interfere with membrane permeability in the brain (membrane theory) 3. Interfere with ion channels in the brain, no action potentials Pharmacokinetics IV induction only! Slow metabolism relative to tissue redistribution Diffusion out of the brain occur rapidly due to redistribution to other body tissues such skeletal muscle and adipose tissue. Short duration of action due to decrease concentration in the brain High lipid solubility Fast onset <60s 7. Half-life 12 hours High lipid soluble After injection, it will overshoot to toxic level Not suitable for sedation. Extrahepatic and hepatic metabolism (fast metabolism) Do not cause toxicity if use repeatedly. Can give IV or IM, not toxic to muscle Suitable for children/ someone uncooperative Clinical indication Potent anesthetic but weak analgesic Adverse effects Toxic to body tissue Causes histamine release. Hypotension Bronchospasm Apnea Coughing
1. 2. 3. 4. 5. 6.
Phenol - Propofol
1. Cause change in lipid metabolism (lipid theory) 2. Interfere with membrane permeability in the brain (membrane theory) 3. Interfere with ion channels in the brain, no action potentials 1. Interacts with N-methyl-Daspartate receptor 2. Stimulates the central sympathetic outflow increase in HR, BP and cardiac output ( suitable for hypovolemic or cardiogenic shock or asthmatic patients)
Dissociative - Ketamine
1. Dissociate patient from environment 2. After injection, eyes still open 3. No pain, no sensation 4. Patient is unconscious but appear to be awake 5. Provides sedation,
ANESTHETICS
amnesia and immobility. 6. Maintain airway, good to be use during disaster. 5 effects: 1. 2. 3. 4. 5. 1. Rapid metabolism Sedation/ hypnosis Anti-anxiety (anxiolytic) Amnesia Muscle relaxation Anti-convulsive Steroids: Immune depression (even 1 dose)
Benzodiazepine Midazolam
Act on GABA receptor Clchannels open hyperpolarization inhibit brain function sedation
Steroids - Althesine
INHALED ANESTHETIC
Drugs Nitrous oxide Mechanism of action Inhaled anesthetic enhanced the binding of GABA to chloride channel opening of chloride channel more chloride enters the cells hyperpolarization reduce neural excitability Pharmacokinetics 1. 1.Poorly soluble in blood 2. and other tissue 3. Move rapidly in and out of the body 4. Decrease metabolism in the liver 5. Fast onset 1. Metabolized in the body to tissue-toxic hydrocarbons 2. Decrease metabolism in the liver 3. Fast onset Clinical indications Potent analgesic but weak general anesthetic Adverse effects Retard oxygen uptake during recovery, causing diffusion hypoxia.
Halothane
Methoxyfluorane Ether
1. Potent anesthetic, weakly analgesic. 2. Co-administered with nitrous oxide, opioids or local anesthetic. 3. Relaxes skeletal and uterine muscle Rarely used No longer used
1. 2. 3. 4. 5.
ANESTHETICS
Chloroform Desflurane Low volatility, delivered using special vaporizer 1. Suitable induction for children 2. Low solubility in blood 3. Rapidly taken up and excreted 4. Low pungency Popular anesthetic agent 1. Tissue toxicity is rare 2. Irritate the airway laryngospasm, coughing Nephrotoxic
Sevoflurane
ANESTHETICS
THEME: Local anesthetics
Drugs Esler - Cocaine Amide Lignocaine (safest) Amide - Bupivacaine Amide - Ropivacaine Mechanism of action Interacts with protein receptor of Na+ channel to inhibit its function 1. Pharmacokinetics Absorbed and metabolized in the liver Excreted by kidney Lignocaine fast onset Bupivacaine onset 23 hours Cocaine inject trans dermally Others should be given SC or give directly to nerve plexus. Clinical indications 1. Applied locally and block nerve conduction of sensory impulse from the periphery to CNS 2. Abolish sensation (in higher concentration, motor system as well) in a limited area of the body without producing unconsciousness. 1. 2. 3. 4. 5. Adverse effects Seizures CVS collapse Allergy Cardio toxicity (bupivacaine) Arrhythmias (cocaine)
2. 3. 4. 5. 6.