Neuro - Pharmacology (Anesthetics) Flashcards

Pg. 493-495 in First Aid 2014 Sections include: -Anesthetics - general principles -Inhaled anesthetics -Intravenous anesthetics -Local anesthetics

1
Q

CNS drugs must have either of what 2 properties?

A

CNS drugs must be lipid soluble (cross the blood-brain barrier) or be actively transported.

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2
Q

Which property of drugs lead to rapid induction? What other effect can this property have?

A

Drugs with decreased solubility in blood = rapid induction and recovery times

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3
Q

Which property of drugs causes increased potency? How does this potency relate to MAC?

A

Drugs with increased solubility in lipids = increase potency = 1/MAC

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4
Q

What is MAC?

A

MAC = Minimal Alveolar Concentration (of inhaled anesthetic) required to prevent 50% of subjects from moving in response to noxious stimulus (e.g., skin incision)

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5
Q

Give an example of a drug that has low blood and lipid solubility. What kind of induction and potency does it have?

A

N2O has low blood and lipid solubility, and thus fast induction and low potency

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6
Q

Give an example of a drug that has high blood and lipid solubility. What kind of induction and potency does it have?

A

Halothane, in contrast, has high lipid and blood solubility, and thus high potency and slow induction

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7
Q

What are 6 examples of inhaled anesthetics?

A

(1) Halothane (2) Enflurane (3) Isoflurane (4) Sevoflurane (5) Methoxyflurane (6) Nitrous oxide

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8
Q

What is the mechanism of inhaled anesthetics?

A

Mechanism unknown.

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9
Q

What are 4 effects of inhaled anesthetics?

A

(1) Myocardial depression (2) Respiratory depression (3) Nausea/Emesis (4) Increased cerebral blood flow (decreased cerebral metabolic demand)

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10
Q

What is the name and definition of the life-threatening toxicity that can be caused by inhaled anesthetics? What other drug can cause this? Which inhaled anesthetic does NOT cause this?

A

Can cause malignant hyperthermia - rare, life-threatening hereditary condition in which inhaled anesthetics (except nitrous oxide) and succinylcholine induce fever and severe muscle contractions

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11
Q

Again, what 2 substances can cause malignant hyperthermia? What is the treatment for malignant hyperthemia?

A

Inhaled anesthetics and succinylcholine; Treatment: Dantrolene

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12
Q

What kind of drug is halothane? What toxicity is associated with it?

A

Inhaled anesthetic; Hepatotoxicity (halothane)

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13
Q

What kind of drug is methoxyfurane? What toxicity is associated with it?

A

Inhaled anesthetic; Nephrotoxicity (Methoxyfurane)

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14
Q

What kind of drug is enflurane? What toxicity is associated with it?

A

Inhaled anesthetic; Proconvulsant (enflurane)

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15
Q

What kind of drug is nitrous oxide? What toxicity is associated with it?

A

Expansion of trapped gas in a body cavity (nitrous oxide)

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16
Q

What are 5 examples of intravenous anesthetics?

A

(1) Barbiturates (2) Benzodiazepines (3) Arylcyclohexylamines (Ketamine) (4) Opioids (5) Propofol; Think: “B. B. King on OPIOIDS PROPOses FOOLishly”

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17
Q

Which barbiturate is known as an intravenous anesthetic? What kind of potency, lipid solubility, and entry into the brain does it have?

A

Thiopental - high potency, high lipid solubility, rapid entry into brain.

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18
Q

What type of drug is thiopental? What are 2 clinical uses for Thiopental?

A

Barbiturates; Used for induction of anesthesia and short surgical procedures

19
Q

How is the effect of thiopental terminated?

A

Effect terminated by rapid redistribution into tissue (i.e., skeletal muscle) and fat

20
Q

What effect does thiopental have on cerebral blood flow?

A

Decreases cerebral blood flow

21
Q

What is the most common drug used for endoscopy? What kind of drug is this? With what is it used adjunctively?

A

Midazolam most common drug used for endoscopy; IV anesthetic, Benzodiazepines; Used adjunctively with gaseous anesthetics and narcotics.

22
Q

What are 3 side effects of Benzodiazepines used as IV anesthestics?

A

May cause severe severe postoperative respiratory depression, low BP (treat overdose with flumazenil), and anterograde amnesia

23
Q

What type of drugs are Arylcyclohexylamines (Ketamine), and what is their mechanism?

A

PCP analogs that act as dissociative anesthetics. Block NMDA receptors.

24
Q

What effect do Arycyclohexylamines have on the cardiovascular system?

A

Cardiovascular stimulants

25
Q

What are 3 side effects of Arylcyclohexylamines (Ketamine)?

A

Cause (1) disorientation, (2) hallucination, and (3) bad dreams

26
Q

What effect do Arylcyclohexylamines (Ketamine) have on cerebral blood flow?

A

Increased cerebral blood flow

27
Q

What are 2 examples of opioids? With what are they used clinically, and for what purpose?

A

Morphine, fentanyl used with other CNS depressants during anesthesia

28
Q

What are 3 clinical uses for propofol?

A

Used for sedation in ICU, rapid anesthesia induction, and short procedures

29
Q

How does propofol compare to thiopental?

A

Less postoperative nausea than thiopental

30
Q

What receptor does propofol act on, and how?

A

Potentiates GABAa

31
Q

What are 3 examples of local anesthetics that are esters?

A

Esters - (1) Procaine, (2) Cocaine, (3) Tetracaine

32
Q

What are 3 examples of local anesthetics that are amides?

A

Amides - (1) LIdocaIne, (2) mepIvacaIne, (3) bupIvacIne (amIdes have 2 I’s in name).

33
Q

What is the mechanism of local anesthetics? What do they bind preferentially, and what effect does this have?

A

Block Na+ channels by binding to specific receptors on inner portion of channel; Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons

34
Q

Describe the form of tertiary amine changes in penetration versus receptor binding.

A

Tertiary amines local anesthetics penetrate membrane in uncharged form, then bind to ion channels as charged form

35
Q

What are 2 clinical uses for local anesthetics?

A

(1) Minor surgical procedures (2) Spinal anesthesia

36
Q

What kind of local anesthetics are given if patient has an allergy to main kind? What is the main kind of local anesthetics?

A

If allergic to esters, give amides

37
Q

What are the 3 main toxicities of local anesthetics?

A

CNS excitation, Hypertension, Hypotension

38
Q

What type of drug is Bupivacaine? What is a toxicity associated with it?

A

Amide local anesthetics; Severe cardiovascular toxicity (bupivacaine)

39
Q

What type of drug is Cocaine? What is a toxicity associated with it?

A

Ester local anesthetics; Arrhythmias (cocaine)

40
Q

With what other drugs can local anesthetics be given? What effect(s) does (do) this have?

A

Can be given with vasoconstriction (usually epinephrine) to enhance local action - decreased bleeding, increased anesthesia by decreased systemic circulation

41
Q

What is the challenge of anesthetics in infected tissue, and why? What is the solution for this?

A

In infected (acidic) tissue, alkaline anesthetics are charged and cannot penetrate membrane effectively –> need more anesthetic.

42
Q

What is the order of the nerve blockade due to local anesthetics? Which factor predominates in determining this order?

A

Order of nerve blockade: small-diameter fibers > large diameter >. Myelinated fibers > unmyelinated fibers. Overall, size factor predominates over myelination such that small myelinated fibers > small unmyelinated fibers > large myelianted fibers > large unmyelianted fibers.

43
Q

What is the order of sensory loss upon use of local anesthetics?

A

Order of loss: (1) pain (2) temperature (3) touch (4) pressure

44
Q

A patient overdoses on Benzodiazepines and has a low BP as a result. How is this treated?

A

Treat overdose with flumazenil