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
If a person has compromised liver function what is a concern for using LAs?
-Increased risk of systemic toxicity and complications
26
Where does prilocaine get metabolized?
- Liver | - Lungs
27
Where does Articaine get metabolized?
- Plasma | - Liver
28
What is a metabolite that is toxic of prilocaine?
-Orthotoludine
29
What is responsible for excretion and elimination of drugs?
-Kidneys
30
T/F Some LAs are excreted and eliminated completely unchanged
True
31
If a person has renal dysfunction what might LAs cause?
- Compromised excretion - Cause elevated blood levels - Increased potential for toxicity
32
If you stop action potentials in a nerve you stop them where as well and why?
-Heart because any anesthetic you use that will block a peripheral nerve will also act on the myocardium
33
What are four systemic actions of LAs?
- Reversibly blocks action potentials - Concentrates in highly perfused organs - CNS effects - Cardiovascular effects
34
What are some systemic actions of LAs on the CNS?
- Convulsions - Anti-convulsions - Analgesia (inability to feel pain) - Euphoria - Mood elevation
35
What is uncontrolled speaking a sign of?
-Intravascular injection of LAs
36
What are the systemic actions of LAs in the cardiovascular system?
- Decreased electrical excitability of myocardium - Decreased conduction rate - Decreased force of contraction
37
What is a health history of the malignant hyperthermia important for?
-Know that LAs can trigger the responses of malignant hyperthermia
38
What occurs when local anesthetics are injected intravascular
Local anesthetic leaves from site of injection into the blood stream and is carried throughout the body
39
What are the benefits of a vasocontrictor?
- Decreased tissue perfusion - Decreased cardiovascular absorption - Decreased potential for toxicity - Increased duration of actions - Increased hemostasis
40
What is the chemical structure of vasoconstrictors?
- Sympathomimetic - Catechols - Catecholamines (like epinephrine or norepinephrine)
41
What are the three modes of actions of sympathomimetic LAs?
- Direct - Indirect - Mixed
42
What are the two types of adrenergic receptors in the body?
- Alpha (vasoconstriction) | - Beta
43
Which alpha receptor is an excitatory post synaptic receptor?
-Alpha 1
44
Which alpha receptor is an inhibitory post synaptic receptor?
-Alpha 2
45
What are the beta receptors for?
-Relaxation of smooth muscle (vasodilations/bronchodilation and cardiac stimulation)
46
Where are beta 2 receptors found?
-Bronchi, vascular beds, and uterus
47
Where are beta 1 receptors found?
- Heart and small intestine
48
What concentration of LA do we use in dentistry?
-1/100,000 or .01 mg/ml
49
What do vasoconstrictors do to blood pressure?
Increase
50
What do vasoconstrictors do to the heart rate?
-Increase
51
What do vasoconstrictors do the the cardiac output?
-increase
52
What is the preservative added to epinephrine?
-Sodium metabisulfite
53
What are the benefits of adding epinephrine to LAs?
- Water solubility - Shelf life - Stability
54
What type of epinephrine receptors are found in the myocardium?
-Beta 1
55
What type of epinephrine receptors are found in pacemaker cells?
-Beta 1 receptors
56
Each carpule is about what volume of solution?
18 micrograms of anesthetic in a 1.8 mL carpule
57
At how many micrograms of anesthetic can you start seeing cardiac effects?
36 micrograms
58
How many carps can you give a compromised patient?
-2 carps (40 micrograms)
59
How many carps can you give a healthy patient?
-11 carps (200 micrograms)
60
What LA has a 1/200,000 carp?
Bupivicaine