Anesthetics......
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Transcript of Anesthetics......
AnaestheticsPrepared by
Imran Ahammad Chowdhury
General Anesthetics
A drug that brings about a reversible loss of consciousness
Causes one or more of the following Pain relief Muscle relaxation Relaxation of reflexes Deep sleep
Commonly used during surgery
Pathway for general Anaesthetic
Stages of General Anesthesia
Stage I - Analgesia
Stage II - Disinhibition
Stage III - Surgical anesthesia
Stage IV - Medullary depression
Main Categories
Inhalation Anesthetics Gasses or Vapors Usually Halogenated
Intravenous Anesthetics Injections Anesthetics or induction agents
Inhalation Anesthetics
Inhaled – may be liquid or gas Nitrous oxide – gas Halothane – liquid
Several others that end with –ane
Inhaled drugs are used together with IV drugs to provide the best level of sedation for the patient & procedure = Balanced Anesthesia
Mechanisms of Action
o Activate K+ channels
o Block Na+ channels
o Disrupt membrane lipids
o In general, all general anesthetics increase
the cellular threshold for firing, thus
decreasing neuronal activity.
General Actions of Inhaled Anesthetics
Respiration Depressed respiration and response to CO2
Kidney Depression of renal blood flow and urine output
Muscle High enough concentrations will relax skeletal muscle
Cardiovascular System Generalized reduction in arterial pressure and peripheral vascular
resistance. Isoflurane maintains CO and coronary function better than other agents
Central Nervous System Increased cerebral blood flow and decreased cerebral metabolism
Intravenous Anaesthetics Commonly used IV induction agents
– Propofol– Thiopental sodium – Ketamine
Most exert their actions by potentiating GABAA receptor
GABAergic actions may be similar to those of volatile anesthetics, but act at different sites on receptor
Organ effects
Most decrease cerebral metabolism and intracranial pressure
Most cause respiratory depression
May cause apnea after induction of anesthesia
Barbiturates, benzodiazepines and propofol cause cardiovascular depression.
Thiopental sodium
rapid onset (20 sec) short-acting
Thiopental use i.v. for induction of anaesthesia, which is maintained with an inhalation agents.
Effect terminated not by metabolism but by redistribution
repeated administration or prolonged infusion approached equilibrium at redistribution sites
Propofol Short-acting agent used for the induction maintenance of GA and sedationThe onset of its action begins after 30 s. After a single dose patient recovers after 5 min with a clear headand no hangover.
Purpose
Overall purposes of intravenous general anaesthetic Opioid analgesic – pain relief (eg.Morphine) Benzodiazepine – amnesia (eg. Diazepam) Anticholinergic – decreases secretions Opioid analgesics – lighter pain relief Sedative/hypnotic – lighter amnesia/sedation
Toxicity and side effects Depression of respiratory drive
Decreased CO2 drive (medullary chemoreceptor's), Takes MORE CO2 to stimulate respiration
Depressed cardiovascular drive Gaseous space enlargement by NO Fluoride-ion toxicity from methoxyflurane
Metabolized in liver = release of Fluoride ions Decreased renal function allows fluoride to accumulate =
nephrotoxicity Malignant hyperthermia
Rapidly cool the individual and administer Dantrolene to block S.R. release of Calcium.
Local Anaesthetic
• Local Anaesthetics are drugs which reversibly prevent the transmission of pain stimuli locally at their site of administration.
• The clinical uses and responses of LA s
depend both on the drug selected and the site of administration.
Esters
NH2
O
O CH2 CH2 N
CH2
CH2
CH3
CH3
Amides
CH3
CH3
NH CH2 CH2 N
CH2 CH3
CH2 CH3
Procaine
Lidocaine
Mode of Action
Block ! Initiation & propagation of action potential (AP) by preventing voltage-gated Na+ channels.
Bind to specific sites on channel protein Prevent formation of open channel Inhibit influx of sodium ions into the neuron Reduce depolarization of membrane in response
to action potential Prevent propagation of action potential.
Choice of local Anaesthetic
Onset Duration Regional anesthetic technique Sensory vs. motor block Potential for toxicity
Local Anaesthetic major toxicity
Allergy CNS toxicity Cardiovascular toxicity. Excitation – anxiety, agitation, restlessness Convulsions Reduced myocardial contractility Vasodilatation
Thank You