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Basics of Anesthesia > Basic Principle of Pharmacology > Flashcards

Basic Principle of Pharmacology Flashcards

(71 cards)

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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
Fetal distress
Accumulation of LA in the fetus accentuated by the acidosis
26
Protein binding
Degree to which medications attach to proteins within the blood
27
Protein that most acidic drugs bind to
Albumin
28
Protein that most basic drugs bind to
Alpha1-acid glycoprotein
29
Bioavailability
Fraction of the administered dose of the unchanged drug that reaches the systemic circulation available to have an effect
30
Factors that affect Bioavailability
``` Dosage Dissolution and Absorption Route Stability of drug in GI Extent of metabolism before systemic circulation Presence of food/drugs in the GI ```
31
Distribution
Movement of drug molecules through the bloodstream to the site of action
32
Factors that affects Distribution
Blood flow Concentration gradient Drug properties BBB
33
Volume of distribution (Vd)
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
Factors influencing Vd
Variations in tissue amount and blood flow | Drug physicochemical property (Lipid solubility, molecular size, PPB)
35
Phase of distribution | Distribution/Alpha phase
Begins immediately after IV injection Reflect distribution from central compartment to periphery
36
Phase of distribution | Elimination/Beta phase
Gradual decline in drug plasma concentration as drug is redistributed back into the central compartment Reflect elimination by renal and hepatic clearance
37
Redistribution
Rapid entry and egress of lipophilic drugs from highly perfused organs Reflects on rate of Recovery
38
Placental drug transfer | Simple diffusion
Unbound drug Lipid soluble Low molecular weight
39
Placental drug transfer | Do not readily cross the placenta
Water soluble High molecular weight Polar compounds
40
Metabolism of drugs
Convert pharmacologically active, lipid soluble drugs into water soluble , often inactive metabolites
41
Factors that affect Rate of metabolism
Concentration of drugs Hepatic blood flow Intrinsic rate of metabolism (genetics, enzyme induction)
42
4 Basic pathways of Metabolism
Oxidation Reduction Hydrolysis Conjugation
43
Metabolism Phase I reactions How is it done? Major reactions
Changing lipophilic compound into polar substance Adding or altering a functional group by splitting the compound into two fragments Oxidation Reduction Hydrolysis
44
Metabolism | Phase II reactions
Conjugation of endogenous compounds (glucuronic acid, amino acid) to polar substance Products are excretable, water soluble metabolites
45
Enzyme responsible for metabolism of most drugs
Hepatic microsomal drug
46
Other sites of drug metabolism
Plasma (Hofmann elimination, ester hydrolysis) Lungs Kidneys GI
47
Cytochrome P-450
Membrane bound heme proteins that catalyze metabolism of endogenous compounds
48
Mixed function oxidase system (mono-oxygenase)
Other name of CP-450 | Because it involves both oxidation and reduction steps
49
Non Cytochrome P-450
Esters that catalyze reactions responsible for metabolism of drugs by conjugation, hydrolysis
50
Enzyme inducing drugs
Enhance the production of liver enzymes that break down drugs
51
Example of Enzyme inducing drugs
``` Phenytoin Phenobarbitone Rifampin Chronic alcohol take Smoking ```
52
Enzyme inhibiting drugs
Inhibit the enzymes which breakdown drugs
53
Examples of Enzyme inhibiting drugs
``` Erythromycin Ciprofloxacin Acute alcohol CCB Phenylbutazone Sulfonamide Isoniazid ```
54
Elimination
All processes that remove drugs from the body | Metabolism + Excretion
55
Excretion
Processes responsible for the removal of drug molecules and metabolites from the body usually in urine
56
Primary organs involved with drug clearance
Liver Kidney Gall Bladder
57
Clearance
Volume of plasma cleared of drug by renal excretion and/or metabolism in liver or other organs
58
Hepatic Clearance
Product of hepatic blood flow and hepatic extraction ratio
59
High hepatic extraction ratio
Drug clearance depends primarily on hepatic blood flow
60
Low hepatic excretion ratio
Drug clearance depends primarily on enzymatic metabolism
61
Process of Biliary excretion
``` Metabolites of drugs or unchanged drug in liver Excreted to bile Into GI Circulation Renal elimination ```
62
Most important organ for elimination of unchanged drug or their metabolites
Kidney
63
Factors affecting Renal drug elimination
Blood flow GFR Urine flow rate
64
Renal clearance | Passive reabsorption
Lipophilic drug that easily cross the cell membrane of renal tubular epithelium
65
Renal clearance | Active tubular secretion
Actively transport protein bound drugs across the tubular lumen
66
Patient groups with altered renal function
Elderly Neonates Patients with renal impairment
67
Elimination Half time
Time necessary for the plasma concentration of a drug to decrease to 50% during elimination phase
68
Factors that affect Half life Positively (Directly) Negatively (Inversely) Neutral (Independent)
(+) Vd (-) drug clearance (o) dosage
69
Amount of elimination half time needed for near complete elimination of drug
5
70
Recovery time
Amount of time that must elapse to allow plasma drug concentration to reach a level that allows patient awakening
71
Major factors altering drug pharmacokinetics
Body weight and composition Age Organ function Plasma Protein binding

Basics of Anesthesia (4 decks)

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