Lecture 3 Flashcards

1
Q

What does ADME deal with?

A

-Pharmacokinetics

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2
Q

What is uptake of a drug?

A

-The drugs entry into the body

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3
Q

What are two types of enteral drugs?

A
  • GI

- Orally

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4
Q

What is a type of the parenteral drug?

A
  • IM
  • Intraoral
  • IV
  • Subcutaneous
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5
Q

Which local anesthetic is the most potent vasodilator and what is it used for?

A

-Procaine used to induce vasodialtion when peripheral blood flow has been compromised.

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6
Q

Are most Local anesthetics vasodialtors or vasocontrictors?

A

-Vasodilators

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7
Q

Do amides or esters produce potent vasodilation?

A

-Esters

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8
Q

Do amides or esters produce relative vasodilation?

A

-Amides

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9
Q

What can happen in an interarteriol injection of anesthetics and it enters the blood stream?

A
  • Slurred speech
  • Muscle twitching
  • CNS depression
  • Seizures
  • Headaches
  • Blurred vision
  • Dizzy
  • Increase BP and pulse
  • Drowsy
  • Ears ringing
  • Feeling numb
  • Unconsciousness
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10
Q

When do interarteriol injections tend to occur?

A

-When you do regional blocks such as PSA or IA blocks

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11
Q

What is the only anesthetic that causes vasoconstriction?

A

-Cocaine

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12
Q

What can occur as a secondary effect to cocaine use?

A

-Nasal septum perforation

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13
Q

Rate of absorption in bloodstream is dependent on what?

A

-Route of administration

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14
Q

T/F Once absorbed drug is distributed through body to all tissues

A

True

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15
Q

What is the most highly perfused tissues?

A

Skeletal muscle (most prone to overdose)

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16
Q

What are other highly perfused tissues?

A
  • Brain
  • Kidneys
  • Liver
  • Lungs
  • Spleen
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17
Q

What is the blood level amount of drug dependent on?

A
  • Rate of cardiovascular absorption
  • Rate of distribution into tissues
  • Elimination
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18
Q

What is the time necessary for a 50% reduction in drug level?

A

-Half life

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19
Q

T/F all local anesthetics cross the Blood brain barrier

A

True

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20
Q

Besides the BBB what is another barrier that local anesthetics readily cross?

A

-Fetal/placental blood barrier

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21
Q

What are the ester anesthetics metabolized into what?

A

-PABA

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22
Q

What are esters hydrolyzed in plasma by?

A

-Pseudocholinesterase

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23
Q

The longer (slower hydrolysis) it takes the drug to hydrolyze what occurs?

A

-It becomes more toxic

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24
Q

Amide LA go through a process of metabolism where does that primarily occur?

A

-Liver

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25
Q

If a person has compromised liver function what is a concern for using LAs?

A

-Increased risk of systemic toxicity and complications

26
Q

Where does prilocaine get metabolized?

A
  • Liver

- Lungs

27
Q

Where does Articaine get metabolized?

A
  • Plasma

- Liver

28
Q

What is a metabolite that is toxic of prilocaine?

A

-Orthotoludine

29
Q

What is responsible for excretion and elimination of drugs?

A

-Kidneys

30
Q

T/F Some LAs are excreted and eliminated completely unchanged

A

True

31
Q

If a person has renal dysfunction what might LAs cause?

A
  • Compromised excretion
  • Cause elevated blood levels
  • Increased potential for toxicity
32
Q

If you stop action potentials in a nerve you stop them where as well and why?

A

-Heart because any anesthetic you use that will block a peripheral nerve will also act on the myocardium

33
Q

What are four systemic actions of LAs?

A
  • Reversibly blocks action potentials
  • Concentrates in highly perfused organs
  • CNS effects
  • Cardiovascular effects
34
Q

What are some systemic actions of LAs on the CNS?

A
  • Convulsions
  • Anti-convulsions
  • Analgesia (inability to feel pain)
  • Euphoria
  • Mood elevation
35
Q

What is uncontrolled speaking a sign of?

A

-Intravascular injection of LAs

36
Q

What are the systemic actions of LAs in the cardiovascular system?

A
  • Decreased electrical excitability of myocardium
  • Decreased conduction rate
  • Decreased force of contraction
37
Q

What is a health history of the malignant hyperthermia important for?

A

-Know that LAs can trigger the responses of malignant hyperthermia

38
Q

What occurs when local anesthetics are injected intravascular

A

Local anesthetic leaves from site of injection into the blood stream and is carried throughout the body

39
Q

What are the benefits of a vasocontrictor?

A
  • Decreased tissue perfusion
  • Decreased cardiovascular absorption
  • Decreased potential for toxicity
  • Increased duration of actions
  • Increased hemostasis
40
Q

What is the chemical structure of vasoconstrictors?

A
  • Sympathomimetic
  • Catechols
  • Catecholamines (like epinephrine or norepinephrine)
41
Q

What are the three modes of actions of sympathomimetic LAs?

A
  • Direct
  • Indirect
  • Mixed
42
Q

What are the two types of adrenergic receptors in the body?

A
  • Alpha (vasoconstriction)

- Beta

43
Q

Which alpha receptor is an excitatory post synaptic receptor?

A

-Alpha 1

44
Q

Which alpha receptor is an inhibitory post synaptic receptor?

A

-Alpha 2

45
Q

What are the beta receptors for?

A

-Relaxation of smooth muscle (vasodilations/bronchodilation and cardiac stimulation)

46
Q

Where are beta 2 receptors found?

A

-Bronchi, vascular beds, and uterus

47
Q

Where are beta 1 receptors found?

A
  • Heart and small intestine
48
Q

What concentration of LA do we use in dentistry?

A

-1/100,000 or .01 mg/ml

49
Q

What do vasoconstrictors do to blood pressure?

A

Increase

50
Q

What do vasoconstrictors do to the heart rate?

A

-Increase

51
Q

What do vasoconstrictors do the the cardiac output?

A

-increase

52
Q

What is the preservative added to epinephrine?

A

-Sodium metabisulfite

53
Q

What are the benefits of adding epinephrine to LAs?

A
  • Water solubility
  • Shelf life
  • Stability
54
Q

What type of epinephrine receptors are found in the myocardium?

A

-Beta 1

55
Q

What type of epinephrine receptors are found in pacemaker cells?

A

-Beta 1 receptors

56
Q

Each carpule is about what volume of solution?

A

18 micrograms of anesthetic in a 1.8 mL carpule

57
Q

At how many micrograms of anesthetic can you start seeing cardiac effects?

A

36 micrograms

58
Q

How many carps can you give a compromised patient?

A

-2 carps (40 micrograms)

59
Q

How many carps can you give a healthy patient?

A

-11 carps (200 micrograms)

60
Q

What LA has a 1/200,000 carp?

A

Bupivicaine