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Basics of Anesthesia > Basic Principle of Pharmacology > Flashcards

Basic Principle of Pharmacology Flashcards

1
Q

Similarities between facilitated diffusion and active transport

A

Carrier mediated
Specific
Saturable

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2
Q

Pharmacokinetics

A

Relationship between dose and resulting concentration in plasma/effect site

Description of the effect of the body on the drug

Quantitative study of absorption, distribution, metabolism and excretion of drug

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3
Q

Absorption

A

Process by which drug leaves its site of administration to enter bloodstream

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4
Q

Factors affecting speed of absorption

A

Drug Property (solubility, concentration, molecular size, ionization)
Local tissue condition
Area of absorbing surface
Blood flow to site of administration

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5
Q

Types of drug administration

A

Local

Systemic

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6
Q

Factors affecting choice of route

A 
Property of the drug
Site of desired action
Rate and extent of absorption
Effect of first pass metabolism
Desirable rapidity of response
Accuracy of dosage required
Condition of patient
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7
Q

Oral Administration

Absorption from the stomach

A

(+)
Non-ionized fraction of weak acid (barbiturates) is higher at low pH values

(-)
Small surface area,
Thick gastric mucosa
Rapid gastric emptying

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8
Q

Oral Administration

Small Intestine

A

(+)

Increases the non-ionized fraction of basic drugs such as (opioids)

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9
Q

First Pass Hepatic Effect

A

Passing of drugs that are absorbed from the GI tract into portal venous blood, and pass the liver before entering systemic circulation

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10
Q

Drug that undergoes extensive hepatic first pass extraction resulting in the inability to give this drug orally

A

Lidocaine

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11
Q

Concentration of Propranolol (Oral vs IV)

A

80-320 mg

0.4-3.0 mg

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12
Q

Hepatic effect on Sublingual administration

A

Passes directly into systemic circulation

Bypass the liver

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13
Q

Drugs properties suitable for Sublingual administration

A

Non-ionized

Highly lipid-soluble

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14
Q

Factors why Inhalational anesthetics is extremely rapid

A

Low molecular weight
High lipid solubility
Large total alveolar surface area
High alveolar blood flow

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15
Q

Rectal Administration

Proximal Rectum

A

Absorbed into superior hemorrhoidal veins

Transported to Liver

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16
Q

Rectal Administration

Lower Rectum

A

Bypass the liver

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17
Q

Drugs that can be used for Rectal Administration

A

Sedatives
Ketamine & Midazolam

Analgesic
Paracetamol suppository

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18
Q

Intrathecal administration

Advantage surguries

A

Lower abdominal
Inguinal
Rectal
Lower extremity surgery

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19
Q

Intrathecal administration

Disadvantages

A

Requires expertise

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20
Q

Epidural administration

Local anesthetics and opioid

A

Acute pain

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21
Q

Epidural administration

Steroids

A

Chronic pain

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22
Q

Determinants of degree of ionization

A 
Dissociation constant (pK )
pH of surrounding fluid
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23
Q

Dissociation constant (pK)

A

The pH where 50% of the drug is ionized and 50% is non-ionized

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24
Q

Ion Trapping

A

Build-up of a higher concentration of a chemical across a cell membrane due to the pKa value of the chemical and difference of pH across the cell membrane.

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25
Q

Fetal distress

A

Accumulation of LA in the fetus accentuated by the acidosis

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26
Q

Protein binding

A

Degree to which medications attach to proteins within the blood

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27
Q

Protein that most acidic drugs bind to

A

Albumin

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28
Q

Protein that most basic drugs bind to

A

Alpha1-acid glycoprotein

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29
Q

Bioavailability

A

Fraction of the administered dose of the unchanged drug that reaches the systemic circulation available to have an effect

30
Q

Factors that affect Bioavailability

A 
Dosage 
Dissolution and Absorption
Route
Stability of drug in GI
Extent of metabolism before systemic circulation
Presence of food/drugs in the GI
31
Q

Distribution

A

Movement of drug molecules through the bloodstream to the site of action

32
Q

Factors that affects Distribution

A

Blood flow
Concentration gradient
Drug properties
BBB

33
Q

Volume of distribution (Vd)

A

Mathematical expression in liters of distribution of a drug throughout plasma (central) and tissue (peripheral)

Vd = Dose of drug / plasma concentration before elimination

Apparent volume required to give a known concentration following a known initial dose

Proportion of drug in tissue space relative to plasma space

34
Q

Factors influencing Vd

A

Variations in tissue amount and blood flow

Drug physicochemical property (Lipid solubility, molecular size, PPB)

35
Q

Phase of distribution

Distribution/Alpha phase

A

Begins immediately after IV injection

Reflect distribution from central compartment to periphery

36
Q

Phase of distribution

Elimination/Beta phase

A

Gradual decline in drug plasma concentration as drug is redistributed back into the central compartment

Reflect elimination by renal and hepatic clearance

37
Q

Redistribution

A

Rapid entry and egress of lipophilic drugs from highly perfused organs

Reflects on rate of Recovery

38
Q

Placental drug transfer

Simple diffusion

A

Unbound drug
Lipid soluble
Low molecular weight

39
Q

Placental drug transfer

Do not readily cross the placenta

A

Water soluble
High molecular weight
Polar compounds

40
Q

Metabolism of drugs

A

Convert pharmacologically active, lipid soluble drugs into water soluble , often inactive metabolites

41
Q

Factors that affect Rate of metabolism

A

Concentration of drugs
Hepatic blood flow
Intrinsic rate of metabolism (genetics, enzyme induction)

42
Q

4 Basic pathways of Metabolism

A

Oxidation
Reduction
Hydrolysis
Conjugation

43
Q

Metabolism
Phase I reactions
How is it done?
Major reactions

A

Changing lipophilic compound into polar substance

Adding or altering a functional group by splitting the compound into two fragments

Oxidation
Reduction
Hydrolysis

44
Q

Metabolism

Phase II reactions

A

Conjugation of endogenous compounds (glucuronic acid, amino acid) to polar substance

Products are excretable, water soluble metabolites

45
Q

Enzyme responsible for metabolism of most drugs

A

Hepatic microsomal drug

46
Q

Other sites of drug metabolism

A

Plasma (Hofmann elimination, ester hydrolysis)
Lungs
Kidneys
GI

47
Q

Cytochrome P-450

A

Membrane bound heme proteins that catalyze metabolism of endogenous compounds

48
Q

Mixed function oxidase system (mono-oxygenase)

A

Other name of CP-450

Because it involves both oxidation and reduction steps

49
Q

Non Cytochrome P-450

A

Esters that catalyze reactions responsible for metabolism of drugs by conjugation, hydrolysis

50
Q

Enzyme inducing drugs

A

Enhance the production of liver enzymes that break down drugs

51
Q

Example of Enzyme inducing drugs

A 
Phenytoin
Phenobarbitone
Rifampin
Chronic alcohol take
Smoking
52
Q

Enzyme inhibiting drugs

A

Inhibit the enzymes which breakdown drugs

53
Q

Examples of Enzyme inhibiting drugs

A 
Erythromycin
Ciprofloxacin
Acute alcohol
CCB
Phenylbutazone
Sulfonamide
Isoniazid
54
Q

Elimination

A

All processes that remove drugs from the body

Metabolism + Excretion

55
Q

Excretion

A

Processes responsible for the removal of drug molecules and metabolites from the body usually in urine

56
Q

Primary organs involved with drug clearance

A

Liver
Kidney
Gall Bladder

57
Q

Clearance

A

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

58
Q

Hepatic Clearance

A

Product of hepatic blood flow and hepatic extraction ratio

59
Q

High hepatic extraction ratio

A

Drug clearance depends primarily on hepatic blood flow

60
Q

Low hepatic excretion ratio

A

Drug clearance depends primarily on enzymatic metabolism

61
Q

Process of Biliary excretion

A 
Metabolites of drugs or unchanged drug in liver
Excreted to bile 
Into GI
Circulation
Renal elimination
62
Q

Most important organ for elimination of unchanged drug or their metabolites

A

Kidney

63
Q

Factors affecting Renal drug elimination

A

Blood flow
GFR
Urine flow rate

64
Q

Renal clearance

Passive reabsorption

A

Lipophilic drug that easily cross the cell membrane of renal tubular epithelium

65
Q

Renal clearance

Active tubular secretion

A

Actively transport protein bound drugs across the tubular lumen

66
Q

Patient groups with altered renal function

A

Elderly
Neonates
Patients with renal impairment

67
Q

Elimination Half time

A

Time necessary for the plasma concentration of a drug to decrease to 50% during elimination phase

68
Q

Factors that affect Half life
Positively (Directly)
Negatively (Inversely)
Neutral (Independent)

A

(+) Vd
(-) drug clearance
(o) dosage

69
Q

Amount of elimination half time needed for near complete elimination of drug

A

5

70
Q

Recovery time

A

Amount of time that must elapse to allow plasma drug concentration to reach a level that allows patient awakening

71
Q

Major factors altering drug pharmacokinetics

A

Body weight and composition
Age
Organ function
Plasma Protein binding

Basics of Anesthesia (4 decks)

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