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Anesthesia Pharmacology > Pharmacodynamics/kinetics > Flashcards

Pharmacodynamics/kinetics Flashcards

Test 1

1
Q

What are the 4 ways a drug binds to a receptor? How do they work?

A

Ion: one atom transfers in electron

Hydrogen: attracted to nearby electronegative atoms

Van der Waals: weak fluctuating bonds

Covalent: shared electrons

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2
Q

What is another name for ion bonding?

A

Electrocovalent

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3
Q

Competitive antagonists shift the dose curve to the ______

A

Right

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4
Q

What is an inverse agonist? Give examples

A

A drug that competes for the same site as an agonist but produces the opposite effect.

Propranolol
Metoprolol
Cetirizine
Loratadine
Prazosin
Naloxone

“Pro met sneezing cat named Lora, who praised Nala”

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5
Q

Inverse agonist were once called _______

A

Antagonist

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6
Q

T/F: the amount of receptors that we have can increase or decrease depend, depending on comorbidities and drug therapies

A

T

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7
Q

How are receptors classified?

A

By location

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8
Q

What are the three types of receptors? What do they consist of?

A
  1. Lipid bilayer: opioids benzos, beta blockers, catecholamines, NMBD
  2. Intracellular proteins: insulin, steroids, Milrinone
  3. Circulating proteins: anticoagulant (warfarin)
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9
Q

What are your vessel rich groups?

A

Parts of the body that have a high cardiac output; in a 1 compartment model, blood flows here after the aorta

Heart
lungs
liver
kidney
brain

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10
Q

What is the more realistic model?

A

2 compartmet model

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11
Q

What type of drugs are able to leave the central compartment and go to the peripheral compartment?

A

Fat soluble drugs (lipid solube)

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12
Q

Which drugs have a larger volume of distribution, fat/lipid soluble, or water soluble?

A

Fat soluble

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13
Q

Where do water soluble drugs normal stay?

A

Plasma

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14
Q

Can narcotics cross the bilayer?

A

Yes

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15
Q

What are the 2 things that affect volume of distribution?

A
  1. changes in blood volume
  2. # of carrier proteins
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16
Q

Almost all drugs we give are bound to ________

A

plasma proteins

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17
Q

What type of protein do acidic drugs primarily bind to? Alkalotic drugs?

A

Acidic drugs: albumin

Alkalotic drugs: A-1 acid glycoprotein

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18
Q

What are conditions that decrease albumin? Would affect does this have on anesthesia?

A

Malnutrition
Burns
Liver failure
Acidosis

This increases the free drug which can cross into membranes and increase concentration/potency.

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19
Q

What can cause decreased plasma proteins in general?

A

Pregnancy
Age
Hepatic disease
Renal failure

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20
Q

What does it mean when a drug has poor protein binding and is lipophilic? What are some examples?

A

This drug is free and can cross lipid bilayers

This drug will have a big volume of distribution

ex) Thiopental, Diazepam

21
Q

Highly protein bound to plasma, protein drugs have a _________ volume of distribution. What are some examples?

A

Small

Ex) warfarin

22
Q

What drugs have active metabolites?

A

Diazepam
Propranolol
Morphine (has 2)
Prodrugs like codeine

23
Q

What happens during metabolism?

A

Convert active, lipid, soluble drugs to inactive drugs that are able to be excreted

24
Q

What are the ways that drugs are metabolized?

A
  1. CYP450 enzyme in the liver (liver main way)
  2. Kidney
  3. Tissue esterase (GI, Placenta)
25
Q

What is phase 1 of metabolism consist of?

A

Oxidation

Reduction

Hydrolysis

** all drugs and bonds are getting ready to be water soluble**

26
Q

What is phase 2 of metabolism consist of?

A

Conjugation

** covalently links, a highly polar molecule to become water soluble**

27
Q

Describe CYP450

A

-Large family with 10 isoforms
-Membrane bound
-contains a heme cofactor
-involves oxidation and reduction

28
Q

What is the most common Phase 1 enzyme for anesthesia drugs?

A

CYP3A4

29
Q

What is the difference between something that induces and inhibits the CYP450 enzyme?

A

Induces: increases the amount of enzyme –> increases metabolism
ex) phenobarbital

Inhibits: decreases amount of enzyme –> increases concentration of drug
ex) grapefruit juice

30
Q

T/F: Hepatic aesthetic drugs clearance is constant

A

T

31
Q

Differentiate between flow llimited and capacity limited hepatic clearance

A

Flow limited: rate is proportional to concentration

Capacity limited: metabolism is exceeded since liver capability is not unlimited

32
Q

What is Context Sensitive Half-Time?

A

Time to a 50% decrease after an infusion at a constant concentration is discontinued

33
Q

What does it mean when the PK in the pH are identical?

A

50% of the drug is ionized and 50% of the drug is non-ionized

34
Q

What’s the main difference between ionized drugs, and non-ionized drugs?

A

Drugs that are ionized are more likely to stay water soluble and not cross barriers

35
Q

Most drugs are ______ acids & bases

A

weak

ex) acids: barbs
bases: LA; opioids

36
Q

Elderly populations have _________ cardiac output and __________ protein binding

A

Decreased

Decreased

37
Q

Define efficacy versus potency

A

Efficacy: the ability of a drug to produce a clinical effect

Potency: less drug with more affect. Concentration versus response.

38
Q

T/F: plasma is a site of effect for anesthetic drugs

A

F

CNS

39
Q

What is lag time?

A

Time between administration and effect in the CNS

40
Q

The therapeutic index =

A

Lethal dose 50% / effective dose 50%

41
Q

What are enantiomers?

A

Structures that are chemically identical & are mirror images

42
Q

What are chiral compounds?

A

Molecules with asymmetric centers

43
Q

What are optical isomers?

A

Enantiomers

44
Q

Describe rotation of light in optical isomers

A

rotates light in solution

If right: Dextrorotatory

left: levorotatory

45
Q

Describe molecule sequence in optical is isomers

A

R: rectus

S: sinister

46
Q

Describe Racemic mixtures

A

50/50 mixtures of 2 optical isomers/enantiomers

1 enantiomer is active
the other is inactive of has adverse side effects

47
Q

The enantiomer for Albuterol is ______

A

Xopenex

48
Q

_______ is the enantiomer for Atracurium. What does it do?

A

Nimbex

Lacks histamine effects

Anesthesia Pharmacology (4 decks)

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