General & Local Anesthetics Flashcards

1
Q

What are the General anesthetics drugs?

A

Inhalational anesthetics: sevoflurane, isoflurane, nitrous oxide

Intravenous anesthetics:
- propofol
- Barbiturates: thiopental

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2
Q

What are the Local anesthetics drugs?

A
  • lidocaine, bupivacaine
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3
Q

What is the General anesthesia?

A

is a REVERSIBLE state of central nervous system (CNS) depression

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4
Q

What are the 5 important benefits of General anesthesia?

A
  1. Analgesia – surgical incision
  2. Hypnosis and sedation – loss of consciousness
  3. Amnesia – loss of memory
  4. Skeletal muscle relaxation
  5. Suppression of undesirable reflexes
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5
Q

What are the commonly used drugs for Inhalational general anesthetics?

A
  • sevoflurane, isoflurane, nitrous oxide, …….
  • Sedation – loss of consciousness
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6
Q

What are the commonly used drugs for Intravenous general anesthetics?

A
  • Propofol: sedation
  • Thiopental (barbiturate): sedation
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7
Q

What are the commonly used Adjunctive drugs?

A

several categories of drugs are used in combination with anesthetics:
- Benzodiazepines
- Narcotics (opioids)
- Neuromuscular blockers

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8
Q

What are the 3 steps of anesthesia?

A

a) Induction

b) Maintenance

c) Termination or Recovery

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9
Q

Step 1 of Anesthesia:

A

Induction:
- Induced by intravenous anesthetics (e.g. propofol, thiopental): Unconsciousness 30-45 seconds
- Adjunctive drugs

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10
Q

Step 2 of Anesthesia:

A
  • Maintained with inhalation anesthetics (sevoflurane…..
  • Adjunctive drugs
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11
Q

Step 3 of Anesthesia:

A

Termination or Recovery:
- Withdraw anesthetic admixture
- Monitor patients for consciousness; respiration, blood pressure, heart rate, intact reflexes….
- May give cholinesterase inhibitors, analgesics
- DETERMINED BY REDISTRIBUTION FROM SITES OF ACTION IN CNS, NOT BY METABOLISM OF THE ANESTHETICS

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12
Q

What are Inhalational anesthetics?

A

are nonflammable and nonexplosive
- gas (nitrous oxide),
- volatile and halogenated hydrocarbons (i.e. sevoflurane, isoflurane).

Maintenance of anesthesia after administration of an IV agent.

Depth of anesthesia can be rapidly altered.

Delivered in a recirculation system.

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13
Q

What are the Pharmacokinetics of Inhalation anesthetics?

A

Factors affect onset of action and elimination:

Onset of action:
- Blood/gas partition coefficient: Low coefficient = fast onset of action (=rapid rate of induction, rapid rate of recovery)

Elimination:
- drug effect is not terminated by metabolism of the drug

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14
Q

What are the Pharmacodynamics of Inhalation anesthetics?

A

Potency:
- minimal alveolar concentration (MAC) of anesthetic gas req. to abolish the response to surgical incision in 50% of pt’s
- MAC/potency relationship (HIGH MAC, LOW potency)
- Factors affecting MAC (lipophilicity) (HIGH potency, LOW MAC)

Action sites:
- Not fully understood

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15
Q

What are the ex’s of Inhalation anesthetics?

A

Nitrous oxide:
- It is not flammable; Non-irritating; “Laughing gas”

Sevoflurane:
- It is not flammable; volatile halogenated hydrocarbon; has
pungent odor.

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16
Q

What are the Pharmacokinetics (PK) of Inhalation anesthetics (Nitrous Oxide (N2O) vs Sevoflurane)?

A

Nitrous oxide:
- Blood/gas partition coefficient is low → low blood solubility → uptake rapidly
Sevoflurane:

  • Blood/gas partition coefficient is higher than nitrous oxide

BOTH ARE NOT METABOLIZED — ARE NOT TOXIC TO LIVER & KIDNEYS

17
Q

What are the Pharmacodynamics (PD) of Inhalation anesthetics (Nitrous Oxide (N2O) vs Sevoflurane)?

A

Potency; MAC

Nitrous oxide:
- MAC is high → Low potency, a weak general anesthetic.
- Does not depress respiration, not used alone for anesthesia
- MAY CAUSE DIFFUSION HYPOXIA

Sevoflurane:
- MAC is lower than nitrous oxide: it is more potent as an anesthetic than nitrous oxide
- Induces respiratory depression.

18
Q

What is the clinical use of Inhalation anesthetics (Nitrous Oxide (N2O) vs Sevoflurane)?

A

Nitrous oxide
- 30-50% nitrous oxide and 20% oxygen – dental surgery
- Nitrous oxide has analgesic effects.

Sevoflurane
- Widely used inhalation anesthetic
- maintain a state of general anesthesia

19
Q

What are ex’s of the Intravenous anesthetics?

A

Propofol & thiopental

20
Q

What are the Intravenous anesthetics in general?

A
  • Intravenous injection
  • Thiopental – it is an ultra-short acting barbiturate
  • Propofol – not barbiturate
21
Q

What are the Pharmacokinetics (PK) of the Intravenous anesthetics (Propofol vs thiopental)?

A

Propofol / thiopental: High lipophilicity, rapid transfer across the blood-brain barrier – rapid action – induction of anesthesia is fast (30-45 seconds)

Propofol:
- Rapidly metabolized. NO CUMULATIVE EFFECT, LESS HANGOVER THAN THIOPENTAL

Thiopental:
- Slowly metabolized, accumulates in body fat, cause hang- over

22
Q

What are the Pharmacodynamics (PD) of the Intravenous anesthetics (Propofol vs thiopental)?

A
  • Enhance GABA-A receptor activation
  • Directly activate GABA-A receptor
  • Increases chloride channel-opening events →
    hyperpolarization
  • Act as CNS depressants
23
Q

What is the clinical uses of the Intravenous anesthetics (Propofol vs thiopental)?

A

For induction of anesthesia

24
Q

What is Propofol’s clinical use?

A
  • First choice for induction of anesthesia
  • Useful for day case surgery
25
Q

What is the concept of Local anesthetics?

A

refers to loss of sensation in a limited region of the body

CONSCIOUSNESS IS MAINTAINED

26
Q

What is the classification of Local anesthetics?

A
  • Esters: procaine, chloroprocaine, cocaine……….
  • Amides: lidocaine, bupivacaine, mepivacaine……….
27
Q

What are the Pharmacokinetics of Local anesthetics?

A

Systemic absorption, distribution and metabolism
- Play a lesser role than with systemic therapeutics
- Serve only to diminish or terminate their effect.
- Critical to the potential development of adverse reactions
- METABOLISM (BIOTRANSFORMATIONS):
- AMIDES: primarily in liver
- ESTERS: plasma cholinesterases

28
Q

What are the Pharmacodynamics: Action sites of Local anesthetics?

A

1) BLOCK VOLTAGE-GATED SODIUM ION CHANNEL
- Inhibit neuron depolarization - Inhibit neuron activity

2) OTHER SITE: inhibit α- adrenergic receptor → vasodilation

29
Q

What are the Clinical use of Local Anesthesia?

A

dental surgery, finger stitches, and surgery in the pelvis and legs.

Delivery techniques:
- Topical administration
- Infiltration
- Ring blocks
- Peripheral nerve blocks
- Neuraxial (spinal, epidural or caudal) blocks

MAY BE USED WITH A VASOCONSTRICTOR (EPINEPHRINE)
- Lower blood flow to injection site
- Decrease diffusion and absorption
- Increase duration of action
- Minimize systemic toxicity