Pharmacology for anaesthesia Flashcards

(40 cards)

1
Q

Define pharmacokinetics.

A

The relationship between drug dose, concentration in bodily fluids and tissues, and time

What the body will do with a given drug

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2
Q

Give 4 routes of drug administration.

A

Oral, sublingual, rectal, inhalational, transdermal, transmucosal, subcutaneous, intramuscular, and intravenous

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2
Q

Which 4 processes make up pharmacokinetics?

A

Absorption
Distribution
Metabolism
Excretion

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2
Q

Define absorption.

A

The processes by which a drug moves from the site of administration to the bloodstream.

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2
Q

Give 3 factors that affect volume distribution.

A

Lipid solubility

Protein binding

Ion binding- electrical charge

Molecular weight- smaller easy to cross membrane

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2
Q

Define Volume of distribution.

A

Apparent volume into which a drug has mixed-distributed throughout the body.

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2
Q

Give 2 factors that affect absorption.

A
  • Physical properties of drug- Solubility, Diluent, Binders, Formulations
  • Dose
  • Site/Route.
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3
Q

How do you calculate volume of distribution?

A

VD = Total quantity of drug / Plasma concentration in steady state

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4
Q

Define terminal half life.

A

Time required for the plasma concentration to decrease by 50% during the terminal phase of decline

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5
Q

Define clearance.

A

Represents the volume of blood or plasma from which the drug is completely eliminated in unit time (ml/min)

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6
Q

What is pharmacokinetic modeling used for?

A

Used to analyze drug distribution and elimination as well as complex patient situations to describe and predict drug behavior.

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7
Q

What is the one compartment model?

A

The rate of drug elimination is assumed to be proportional to the amount of drug in the body (X) at any time (t), it decreases exponentially with time and is consistent with first-order kinetics (dX/dt = k X)

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8
Q

What is two compartment model?

A

Each phase follows exponential first-order processes

A-rapid distribution
B- elimination of the drug

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9
Q

Which compartment model is most important in anaesthesia?

A

Three compartment model

It divides the body into three compartments: a central compartment (usually representing plasma) and two peripheral compartments representing tissues that are either highly or scarcely perfused by blood.

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10
Q

What is zero order elimination?

A

A constant amount of drug is eliminated per time unit (Thiopentone, Phenytoin, Salicylates, Theophyllin, alcohol)

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11
Q

Define pharmacodynamics.

A

Relationship between a drug’s mechanism of action and the biochemical and physiologic response produced in the body.

What does the drug do to the body.

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12
Q

What is Minimal Alveolar Concentration (MAC)?

A

The concentration at which 50% of subjects do not produce a reaction to a standard stimulus.

13
Q

What does the anesthesia triad include?

A

Hypnosis—-Analgesia—Paralysis

14
Q

What are intravenous anaesthetics used for?

A

Hypnosis- During Induction & maintenance.

15
Q

What are the properties of an ideal IV anaesthetic agent? (4)

A
  • Rapid onset + rapid recovery
  • Storability: Long shelf-life at room temperature
  • Pleasant effect during the induction phase
  • Safety following extravasation or inadvertent intra-arterial injection
  • Analgesic at sub-anaesthetic concentrations
  • Minimal cardiovascular and respiratory depression
16
Q

Give 4 examples of IV anaesthetic drugs.

A

Barbiturates (thiopental, methohexitone)

Non-barbiturates (propofol, ketamine, etomidate)

17
Q

What properties should an ideal IV anaesthetic agent not have? (4)

A
  • toxic effects
  • emetic effects
  • pain on injection
  • histamine release or hypersensitivity reaction
  • interference with other drugs
  • stimulation of porphyria
  • unpleasant experiences in the peri-operative phase
18
Q

Name the 3 IV anaesthetic drugs most commonly used in Malawi.

A

Thiopentone

Ketamine

Propofol

19
Q

What are the key pharmacological properties and cautions of Thiopentone?

A

Class: Barbiturate

MOA: Prolongs GABA-dependent Cl⁻ channel opening

Onset: Rapid (one arm-brain circulation time)

Duration: Short (due to redistribution)

Effects: Antiepileptic, mild muscle relaxation, causes hypotension, histamine release

Cautions: Unsafe in porphyria

Formulation: Alkaline solution (pH ~10.5)

Note: Long half-life with repeated doses or infusion

20
What are the key pharmacological features and routes of administration for Ketamine?
Class: Phencyclidine derivative MOA: NMDA receptor antagonist Metabolism: Hepatic P450 → active metabolite norketamine Effects: Stimulates sympathetic nervous system → ↑ adrenaline & noradrenaline Doses & Routes: IV: 1–2 mg/kg (onset 10–20 sec, duration 10–30 min) IM: 4–10 mg/kg (onset 1–5 min, duration 45–60 min) Rectal: 5–10 mg/kg (onset 5–10 min, duration 2–3 hrs) Analgesia: 0.2–0.5 mg/kg Note: Oral/inhalational use is mostly recreational
21
What kind of state does ketamine cause?
Dissociative state
22
Give 4 effects of ketamine.
- Analgesia (acute, chronic, Complex reginal pain syndrom) - Anaesthesia - Hallucinations - Increased blood pressure - Bronchodilatation - Dissociative anaesthesia - Antidepressive - Airway reflexes are maintained
22
What are the key formulation and pharmacological properties of Propofol?
Structure: 2,6-diisopropylphenol MOA: Acts on GABA chloride channels Solubility: Highly lipid soluble Form: Oil-in-water emulsion Concentration: 10 mg/mL Additives: Soybean oil, glycerol, egg lecithin pKa: 11 Solution pH: 7–8.5
23
When is propofol used? (3)
Induction & maintenance of general anaesthesia Sedation in ICU Sedation for other procedures
24
Give 4 side effects of propofol.
Reduces laryngeal reflexes Dose dependent fall in SVR, no reflex tachycardia, slight fall in CO Considerable fall in BP (cave hypovolaemia) Pain on injection Spontaneous excitatory movements (misinterpretation can happen) Crosses placenta (not used in obstetrics)
25
Name 3 inhalation anaesthetic drugs (volatiles).
Halothane Isoflurane (Enflurane) Sevoflurane (standard in rich countries) Desflurane Xenon
26
What is oil: gas partition coefficient
Measure of the lipid solubility
27
What is the Meyer-Overton Hypothesis?
The Meyer–Overton hypothesis is the theory of anaesthetic action which proposes that the potency of an anaesthetic agent is related to its lipid solubility
28
Table on MAC values
Slide 43
29
What are the key properties and effects of Halothane as an inhalational anesthetic?
Colorless liquid with pleasant smell Light-sensitive; stabilized with thymol Hepatic metabolism: 20–25% → risk of hepatotoxicity Cardiovascular: Dysrhythmias, ↓ contractility, HR, CO, BP CNS: ↑ cerebral blood flow & ICP Respiratory: ↓ tidal volume, ↑ RR & PaCO₂, ↓ laryngeal reflexes & airway resistance Uterine: Causes relaxation → caution in obstetrics
29
What are the key characteristics and physiological effects of Isoflurane?
Class: Halogenated methyl ethyl ether Properties: Colourless volatile liquid with irritant smell; expensive Pharmacokinetics: Lower blood-gas solubility than Halothane → rapid onset & recovery Safety: Low hepatic and renal toxicity CNS: ↑ cerebral blood flow & ICP (less than Halothane) Cardiovascular: No arrhythmias; minimal effect on contractility; ↓ BP due to ↓ SVR Respiratory: ↓ tidal volume, ↑ respiratory rate
29
Name a depolarizing muscle relaxant.
Suxamethonium
30
Give 3 side effects of suxamethonium.
Mild to severe muscle fasciculation which can lead to increased CO, BP, ICP Myalgia Hyperkalemia (burns, neurological conditions, peripheral nerve injuries, renal failure, acidosis) which can lead to cardiac arrest Dual block Increased intraocular pressure Malignant hyperpyrexia Parasympathetic effects
31
Give 4 examples of non-depolarizing muscle relaxants.
Steroids: Vecuronium, Rocuronium, Pancuronium Esters: Atracurium
32
What drug is used to reverse the effects of Vecuronium?
Neostigmine ( + atropine)