Anesthesia Pharm

Question 1

Pharmacodynamics

Answer 1

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

Question 2

Pharmacokinetics

Answer 2

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

Question 3

Tachyphylaxis

Answer 3

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.

Question 4

Synergistic Effect

Answer 4

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

Question 5

VRG

Answer 5

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

Question 6

Vessel Poor Group

Answer 6

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

Question 7

Synonyms for Nonionized

Answer 7

Non polar, lipid soluble, hydrophobic, lipophilic; ACIDS

Active drugs.

Question 8

Synonyms for Ionized

Answer 8

Non lipid soluble, Polar, hydrophilic, lipophobic; BASES

Facilitates excretion from renal tubules.

Question 9

Henderson-Hasselbalch Equation

Answer 9

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

Question 10

Acid

Answer 10

Proton donor

Question 11

Base

Answer 11

Proton acceptor

Question 12

What does it mean if pH=pKa?

Answer 12

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

Question 13

What do weak acids form from?

Answer 13

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

Question 14

Weak acids: pKa>pH

Answer 14

then >50% nonionized, acid (lipophilic) Propofol

Question 15

Weak base: pKa>pH

Answer 15

then >50% ionized, base (lipophobic)

Question 16

What do weak bases form from?

Name some drugs.

Answer 16

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

Local anesthetics, opioids, benzos, etomidate, ketamine

Question 17

Clearance

Answer 17

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

Question 18

Hofmann Elimination

Answer 18

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

Question 19

Ester Hydrolysis

Answer 19

Non organ Clearance of Succs and mivacurium

Question 20

Zero-order kinetics

Answer 20

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

Question 21

Clearance Time Constants

Answer 21

Half-Life

Question 22

Biotransformation

Answer 22

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

Question 23

First-order kinetics

Answer 23

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

Question 24

Name 4 Phase 2 enzymes

Answer 24

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

Question 25

Phase 1 needs what for it to work?

Answer 25

Oxygen (OIL RIG)

Question 26

Potency

Answer 26

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

Question 27

First pass effect

Answer 27

Liver biotransforms the ingested drug before it reaches its site

Question 28

Slope of curve

Answer 28

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

Question 29

What does the plateau of the curve reflect?

Answer 29

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

Question 30

Therapeutic Effect

Answer 30

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

Question 31

What is G6PD

Answer 31

A genetic disorder in which certain drugs cause hemolysis

Question 32

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

Answer 32

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

Question 33

Cation-selective ligand gated ion channels

Answer 33

Excitatory, nAChR Serotonin receptors (5HT3)

Question 34

Anion-selective ligand gated ion channels

Answer 34

Inhibitory, GABAa receptors Glycine receptors

Question 35

Glutamate and its targets.

Answer 35

``` 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 ```

Question 36

Kainate

Answer 36

A ligand-gated ion channel receptor that binds Glutamate.

Question 37

What drug(s) bind to nAChR?

Answer 37

Neuromuscular blockers.

Question 38

What drug(s) bind to GABA receptors?

Answer 38

Barbs, benzos, propofol, etomidate, VAs, EtOH

Question 39

What drug(s) bind to NMDA receptors?

Answer 39

Ketamine

Question 40

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

Answer 40

ACh and glutamate open Na+ channels

Question 41

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

Answer 41

GABA and glycine open Cl- channels

Question 42

Two actions of GABA

Answer 42

1. Increase agonist affinity for GABA receptors. | 2. Prolongation of the Cl- conductance gated by these receptors

Question 43

What are the three types of transmembrane proteins?

Answer 43

Voltage gated ion channels Ligand gated ion channels Transmembrane receptors.

Question 44

Transmembrane receptors

Answer 44

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

Question 45

What does activation of GABA receptors do.

Answer 45

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

Question 46

Glycine

Answer 46

an inhibitory receptor in the spinal cord.

Question 47

5HT receptors and their functions.

Answer 47

Excitatory; cation permeable; *Antiemetic*, anxiolytic and analgesic

Question 48

How does concentration of receptors change in response to stimulation?

Answer 48

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

Question 49

What NT(s) binds to NMDA receptors?

Answer 49

Glutamate

Question 50

What NT(s) binds to AMPA receptors?

Answer 50

Glutamate

Question 51

What NT(s) binds to Kainate receptors?

Answer 51

Glutamate

Question 52

Where does GABA mainly act?

Answer 52

Brain

Question 53

Where does glycine main act?

Answer 53

Spinal Cord