Intravenous anaesthetics Flashcards
1
Q
IV induction of anaesthesia?
A
- Dependent on cardiac output
- LOC in one arm brain circulation about 30-45 secs
- Action on ligand-gated ion channels - GABA-A and also potassium channels (Neural activity)
2
Q
GABA-A receptors?
A
- Ligand-gated ion channels consisting of 5 subunits
- Three isoforms which determine its; Agonist affinity, ion channel opening and conductance
- In humans - 2-alpha, 2-Beta and 1-gamma
- Forms a chloride anion channel.
- Targeted by Benzodiazepines, barbiturates, propofol, etomidate and volatile agents
- Activation leads to post-synaptic hyperpolarisation of cell membrane, inhibition of post-synaptic currents and ultimately inhibition of neural activity.
3
Q
Two-pore domain potassium channels?
A
- Contains 15 potassium ion channels
- They are voltage independent
- They are not inactivated by action potential
- They are responsible for leak currents determining the resting membrane potential
- Present in CNS & modeulated by GA
- They are present pre & post-synaptically
- Competitive inhibition of post-synaptic ion channel receptor sites.
4
Q
Standard ATP-dependent potassium channels?
A
They are activated and inactivated by every action potential
5
Q
Other mechanisms of action ?
A
- Potassium channels
- Extrasynaptic receptors
3.
6
Q
Extrasynaptic receptors?
A
- Includes alpha-5 and delta-subunit containing GABA-A receptors expressed in the hippocampus
- Their activation inhibits long-term potentiation and memory
7
Q
Presentation of anaesthetic agents?
A
- Presentation
- Uses
- Effects (Dynamics)
- Kinetics
- Toxicity / contraindications
8
Q
Thiopentone?
A
- It is based on a barbiturate ring
- Hygroscopic pale yellow powder
- Contains 500mg of thio and 6% sodium carbonate in an inert atmosphere of nitrogen
- Its a 2.5% solution when mixed with water
- It has a pH of 10.8
- It is alkaline, bacteriostatic and safe to keep for 48 hours.
- Dose is 4-5mg/kg
9
Q
Uses of Thiopentone?
A
- Induction of GA
2. Status epilepticus
10
Q
Dynamics (effects) of Thiopentone?
A
- Dose is 4-5mg/kg
- Depresses cardiac contractility, reducing CO & BP
- Decrease of venous tone and pooling of blood in the peripheral veins
- Respiratory depression
- Airway reflexes are preserved (LMA not appropriate)
- Histamine release may occur
11
Q
Dynamics (effects) of Thiopentone on CNS?
A
- Reduces CBF, CMR and oxygen demand
- Anticonvulsant properties
- Reduces intracranial pressure
12
Q
Kinetics of Thiopentone?
A
- The pKa = 7.6
- About 60% unionized at pH=7.4
- Its about 65-85% protein bound. Only 12% immediately available.
- It is highly lipid soluble
- Rapid emergence due to redistribution and not metabolism
- Metabolism occurs in the liver and excretion in the kidney
- Metabolism follows zero order kinetics - Constant amount of drug is being eliminated per unit time irrespective of plasma concentration
13
Q
Porphyrias?
A
- Characterised by the over over-production and excretion of porphyrins (intermediate compounds produced during haemoprotein synthesis).
- Attacks may be caused by drugs, stress, infection, alcohol, pregnancy and starvation.
- Caused by thiopentone due to hepatic enzyme induction
14
Q
Etomidate?
A
- Its an imidazole ester
- Liquid emulsion or clear solution
- Contains propylene glycol at a conc. of 2mg/ml
15
Q
Uses of Etomidate?
A
- Induction - 0.3mg/kg
- Induction may mimic seizure activity
- It can be used in CV compromised & elderly patients.