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Advanced Pharmacology > Anesthesia Pharm > Flashcards

Anesthesia Pharm Flashcards

1
Q

Pharmacodynamics

A

The study of the intrinsic sensitivity or responsiveness of receptors to a drug and the mechanisms by which these effects occur.

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2
Q

Pharmacokinetics

A

The quantitative study of the absorption, distribution, metabolism, and excretion of injected and inhaled drugs and their metabolites.

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3
Q

Tachyphylaxis

A

Tolerance that develops acutely within only a few doses of a drug.
The most important factor in the development of tolerance to drugs is the neuronal adaptation, referred to as (1) cellular tolerance.
Other mechanisms of tolerance may include (2) enzyme induction and (3) depletion of neurotransmitters caused by sustained stimulation.

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4
Q

Synergistic Effect

A

Two drugs interact to produce an effect greater than the algebraic summation

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5
Q

VRG

A 
Vessel rich group 75% of Cardiac Output;
Heart = 5%
Brain = 10%
Lungs = 15%
Kidneys = 20%
Liver = 25%
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6
Q

Vessel Poor Group

A 
Muscle = 19%
Fat = 6%
Bone/cart/lig = <1%
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7
Q

Synonyms for Nonionized

A

Non polar, lipid soluble, hydrophobic, lipophilic; ACIDS

Active drugs.

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8
Q

Synonyms for Ionized

A

Non lipid soluble, Polar, hydrophilic, lipophobic; BASES

Facilitates excretion from renal tubules.

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9
Q

Henderson-Hasselbalch Equation

A

Relationship between the pKa of the drug and pH of the solution

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10
Q

Acid

A

Proton donor

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11
Q

Base

A

Proton acceptor

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12
Q

What does it mean if pH=pKa?

A

It means 50% of drug is ionized and 50% is unionized.

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13
Q

What do weak acids form from?

A

Weak acids form from salts with positive ions. Na+, K+, Ca2+, Mg2+

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14
Q

Weak acids: pKa>pH

A

then >50% nonionized, acid (lipophilic) Propofol

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15
Q

Weak base: pKa>pH

A

then >50% ionized, base (lipophobic)

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16
Q

What do weak bases form from?

Name some drugs.

A

Weak bases form from negative ions. Cl-, SO4-, PO4-

Local anesthetics, opioids, benzos, etomidate, ketamine

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17
Q

Clearance

A

Volume of plasma cleared of drug by renal excretion and or metabolism in the liver or other organs.

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18
Q

Hofmann Elimination

A

Clearance influenced by temp and pH. Temp/pH increases, so does elimination.
Atracurium & Cisatracurium

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19
Q

Ester Hydrolysis

A

Non organ Clearance of Succs and mivacurium

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20
Q

Zero-order kinetics

A

Constant amount of drug clearance per unit time. R/t concentration of drug exceeding available enzyme.
Straight line. Phase 2 (Conjugation).
Ex: EtOH, ASA, tylenol, Dilantin

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21
Q

Clearance Time Constants

A

Half-Life

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22
Q

Biotransformation

A

Conversion of pharmacologically active, lipid soluble drugs to water soluble and often inactive metabolites.

23
Q

First-order kinetics

A

A constant fraction of available drug is metabolized in a given time period.
Half-lives. Curves. Phase 1 (Red-ox reactions; Hydrolysis)

24
Q

Name 4 Phase 2 enzymes

A
  1. Glucuronosyltransferases
  2. Glutathione-S-transferases
  3. N-acetyl-transferases
  4. Sulfonotransferases
25
Q

Phase 1 needs what for it to work?

A

Oxygen (OIL RIG)

26
Q

Potency

A

Left shift of dose-response curve. Affected by absorption, distribution, metabolism, and affinity for receptor.

27
Q

First pass effect

A

Liver biotransforms the ingested drug before it reaches its site

28
Q

Slope of curve

A

Influenced by the number of receptors that must be occupied before a drug effect occurs; more receptors needing occupied = steep slope

29
Q

What does the plateau of the curve reflect?

A

The plateau is the efficacy or intrinsic activity of the drug. It is the maximal effect.

30
Q

Therapeutic Effect

A

The margin of safety. The ratio between the median lethal dose (LD50) and the median effective dose (ED50).
LD50/ED50

31
Q

What is G6PD

A

A genetic disorder in which certain drugs cause hemolysis

32
Q

Ligand gated ion channels, 3 types (although really two families)

A
  1. Cation selective and excitatory
  2. Anion selective and inhibitory
  3. Glutamate (excitatory in CNS).
33
Q

Cation-selective ligand gated ion channels

A

Excitatory,
nAChR
Serotonin receptors (5HT3)

34
Q

Anion-selective ligand gated ion channels

A

Inhibitory,
GABAa receptors
Glycine receptors

35
Q

Glutamate and its targets.

A 
the principal excitatory NT in the CNS;
Does not cross BBB, originates locally;
newer targets for pain management.
Binds to ligand gated ion channel receptors:
1. NMDA
2. AMPA
3. Kainate
36
Q

Kainate

A

A ligand-gated ion channel receptor that binds Glutamate.

37
Q

What drug(s) bind to nAChR?

A

Neuromuscular blockers.

38
Q

What drug(s) bind to GABA receptors?

A

Barbs, benzos, propofol, etomidate, VAs, EtOH

39
Q

What drug(s) bind to NMDA receptors?

40
Q

What are two main excitatory NT and what ion flows through their channels?

A

ACh and glutamate open Na+ channels

41
Q

What are two main inhibitory NT and what ion flows through their channels?

A

GABA and glycine open Cl- channels

42
Q

Two actions of GABA

A
  1. Increase agonist affinity for GABA receptors.

2. Prolongation of the Cl- conductance gated by these receptors

43
Q

What are the three types of transmembrane proteins?

A

Voltage gated ion channels
Ligand gated ion channels
Transmembrane receptors.

44
Q

Transmembrane receptors

A

Allow binding of Hydrophilic ligands.
Causing signal transduction
Involves G proteins

45
Q

What does activation of GABA receptors do.

A

GABA binds and Cl- enters cell, hyperpolarizing it, inhibiting neuronal activity, mainly in brain

46
Q

Glycine

A

an inhibitory receptor in the spinal cord.

47
Q

5HT receptors and their functions.

A

Excitatory;
cation permeable;
Antiemetic,
anxiolytic and analgesic

48
Q

How does concentration of receptors change in response to stimulation?

A

They can be decreased (down-regulated) or increased (up-regulated) in response to NT concentration.
Ex: Pheochromocytoma is an increase in [NE], resulting in down-regulation of receptors

49
Q

What NT(s) binds to NMDA receptors?

50
Q

What NT(s) binds to AMPA receptors?

51
Q

What NT(s) binds to Kainate receptors?

52
Q

Where does GABA mainly act?

53
Q

Where does glycine main act?

A

Spinal Cord

Advanced Pharmacology (7 decks)

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