[1] PRELIMS | INTRODUCTION TO PHARMACOLOGY Flashcards
Basic Principles of Pharmacology
The science concerned with history, sources, physical, and chemical properties of drugs, in ways in which drugs affect biological systems
Pharmacology
Basic Principles of Pharmacology
Chemical entities, both endogenous and foreign, that are capable of reacting with biological systems
Drug
Basic Principles of Pharmacology
Are chemicals that are introduced to cause some sort of change
Drugs
Basic Principles of Pharmacology
Science of preparing, compounding, and dispensing medicines
Pharmacy
Basic Principles of Pharmacology
Identification and preparation of crude drugs from natural sources
Pharmacognosy
Basic Principles of Pharmacology
Study of poisonous aspects of drugs
Toxicology
‘Toxic’ = ‘Posionous’
Branch of Pharmacology
Also known as clinical pharmacology
Uses drugs to treat, prevent, and diagnose diseases
Pharmacotherapeutics
Concerns of Pharmacotherpeutics
How the drugs are affected by the biological system
Pharmacokinetics
What the body does to the drug
Concerns of Pharmacotherapeutics
Effects of drugs in a biological system
Pharmacodynamics
What the drug does to the body
Drug Names
Chemical structure of the drug
Chemical name
Drug Names
Official nonproprietary name of drugs, universally accepted
Generic name/Official name
Ex. Diphenhydramine
Drug Names
Proprietary name, chosen by drug company
Brand name/Trade
Ex. Benedryl (Diphenhydramine)
A drug may have one generic name but many brand names
Sources of Drugs
- P___ Source
- M___ Source
- A___ Source
- S___ drug Source
- M___ Source
- Plant Source
- Mineral Source
- Animal Source
- Synthetic drug Source
- Microorganism Source
Drug Development
Tests to see if the drug is safe and its pharmocokinetics
20-100 subjects
Clinical Testing | Phase 1
3rd Stage
Drug Development
Where biologic products and chemical synthesis and optimization creates a lead compound
In Vitro Studies
1st Stage
Drug Development
Testing of the efficacy selectivity mechanism of the drug
Animal Testing
2nd Stage
Drug Development
Tests to see how if the drug works/effective in patients
100-200 patients
Clinical Testing | Phase 2
3rd Stage
Drug Development
Tests to see if the drug works double blind
1000-6000 patients
Clinical Testing | Phase 3
3rd Stage
Drug Development
Postmarketing surveillance of the drug which lasts for 10-20 years
Drug can be released to the market
Clinical Testing | Phase 4
4th Stage (Marketing)
Drug Development
Generics become available only after ____ years as the patent expires
20 years
Classification of Drugs
Need to be prescribed before acquired
Prescription Drugs
Ex. Antibiotics
Classification of Drugs
Medications that can buy without a prescription
Over the Counter Drugs (OTC)
Classification of Drugs
Drugs that are not yet known and are under clinical trials
Investigational Drugs (ID)
Classification of Drugs
Prohibited substances and should not be sold to the public
Ilicit or Street Drugs
Process of Pharmacokinetics
The entry of a drug into the systemic circulation from the site of administration
Absorption
Physical factors are to be considered prior to absorption
Physico-chemical Considerations For Drug Passage Across Barriers
- ____ of plasma membrane
- Presence of ____
- ____ of extracellular environment
- ____ of drugs
- Selectively permeability of plasma membrane
- Presence of membrane proteins
- pH of extracellular environment
- Ionization of drugs
Absorption
Where drugs administered orally are first exposed to the liver and may be extensively metabolized before reaching the rest of the body
First Pass Hepatic Metabolism
GI Tract -> Portal Circulation -> Systemic Circulation
Clinical Relevance of First Pass Hepatic Metabolism
Drugs with high first pass metabolism should be given in ____ to ensure that enough active drug reaches the desired site of action
doses sufficient enough
Absorption
The measure of the fraction of a dose that reaches the systemic circulation
Bioavailability
Bioavailability
By definition, ____ doses have 100% bioavailability
intravascular (IV)
Common Routes of Administration
- Bioavailability: 100
- Most rapid onset
Intravenous (IV)
Common Routes of Administration
- Bioavailability: 75 to < or = 100
- Large volumes often feasible, may be painful
Intramuscular (IM)
Common Routes of Administration
- Bioavailability: 75 to < or = 100
- Smaller volumes than IM, may be painful
Subcutaneous (SC)
Common Routes of Administration
- Bioavailability: 5 to <100
- Most convenient; first-pass effect may be important
Oral (PO)
Common Routes of Administration
- Bioavailability: 30 to <100
- Less first-pass effect than oral
Rectal (PR)
Common Routes of Administration
- Bioavailability: 5 to <100
- Often very rapid onset
Inhalation
Common Routes of Administration
- Bioavailability: 80 to < or = 100
- Usually very slow absorption, used for lack of first pass effect, prolonged duration of action
Transdermal
Process of Pharmacokinetics
Wherein drug reversibly leaves the bloodstream and enters the target organ
Distribution
Factors that influence Distribution
- S____
- B____
- S____
- P____
- Size of the organ
- Blood flow
- Solubility
- Protein binding
Distribution
Drug from ____ to ____
systemic circulation to organ and tissue
Distribution
Under physiologic condition, protein-binding capacity is (1) ____ than the drug concentration and the free fraction is (2) ____
(1) greater
(2) constant
Distribution
Plenty of drugs bind to plasma protein, (1) ____, with a balance (2) ____
(1) albumin
(2) between bound and free molecule
Distribution
- [1] ____ (active, free) -> [2] ____ (inactive, bound)
[1] Drug + Protein
[2] Complex
Distribution
Sulfonamides and bilirubin in (1) ____
-> (2) ____ -> (3) ____
Sulfonamides should not be given to pregnant mothers and babies
(1) neonates
(2) Hyperbilirubinemia
(3) Kernicterus
Kernicterus causes cerebral palsy and hearing loss in neonates
Distribution
Warfarin and sulfonamides -> (1) ____ -> (2) ____
Warfarin (drug) is an anti-coagulant, it is bound to albumin (protein) which makes it inactive
(1) displacement of warfarin
(2) increase free Warfarin
Free Warfarin = Active Warfarin, resulting in increase risk of bleeding
Unique Barriers to Distribution
Most low molecular weight medicines cross this barrier
Placental Barrier
Criteria for Safe Drugs in Pregnancy
- W____
- L____
- H____
- Water-soluble
- Large molecule
- Highly protein-bound
These drugs will not cross the placental barrier, deeming it safe
Unique Barriers to Distribution
Permeable only to lipid soluble or low molecular weight drugs
Ex. Lithium, Ethanol, Levodopa, Dopamine
Blood Brain Barrier
Distribution
Drugs that can redistribute into fat tissue prior to elimination
Lipid-soluble Drugs
Redistributing into the fat tissue, the drug can go back once again into systemic circulation and increase the effect of the drug
Redistribution
CNS Drugs: The duration of action an initial dose may depend more in the ____
Ex. Thiopental
redistribution rate than on the half-life
Process of Pharmacokinetics
Is the metabolic converion of drug to more water soluble metabolites that are more easily excreted
Metabolism / Biotransformation
Fates of Drug Metabolism
- Active drug -> ____
- Active drug -> ____
- Prodrug -> ____
*Prodrug is an inactivated drug
(1) Inactive drug
(2) Less active metabolite
(3) Active drug
Phase I Metabolism
- R____
- O____
- H____
Goal: to make the drug more water-soluble but it is still active
- Reduction
- Oxidation
- Hydrolysis
Phase II Metabolism
- M____
- G____
- A____
- S____
Goal: to make the drug more water-soluble but it is now inactive
- Methylation
- Glucuronidation
- Acetylation
- Sulfation
Metabolism
Primary phase I enzyme system involved in the oxidative metabolism xenobiotics
Xenobiotics are foreign substances that are not in nature of the body
Cytochrome P450 System
Metabolism - Cytochrome P450 System
Responsible for metabolism and synthesis of ____ like ____
endogenous compounds like steroids and prostaglandins
Metabolism - CYP450 System
CYP 1A2 -> Substrate
- Theophylline
- Acetaminophen
Metabolism - CYP450 System
CYP 1A2 -> Inducers
- Aromatic hydrocarbons (smoke)
- Cruciferous vegetables
Metabolism - CYP450 System
CYP 1A2 -> Inhibitors
- Quinolone
- Macrolide
Metabolism - CYP450 System
CYP 1A2 -> Genetic Morphism
None
Metabolism - CYP450 System
CYP 2C9 -> Substrate
- Phenytoin
- Warfarin
Metabolism - CYP450 System
CYP 2C9 -> Inducers
General Inducers
Metabolism - CYP450 System
CYP 2C9 -> Inhibitors
None
Metabolism - CYP450 System
CYP 2C9 -> Genetic Morphism
Yes
Metabolism - CYP450 System
CYP 2D6 -> Substrate
Many CNS and CV Drugs
Metabolism - CYP450 System
CYP 2D6 -> Inducers
None known
Metabolism - CYP450 System
CYP 2D6 -> Inhibitors
- Haloperidol
- Quinidine
Metabolism - CYP450 System
CYP 2D6 -> Genetic Morphism
Yes
Metabolism - CYP450 System
CYP 3A4 -> Substrate
MOST ABUNDANT
60% of drugs
Metabolism - CYP450 System
CYP 3A4 -> Inducers
General Inducers
Metabolism - CYP450 System
CYP 3A4 -> Inhibitors
General Inhibitors
Metabolism
Decrease rate of metabolism -> More drug present
Enzyme Inhibitors
Metabolism
Increase rate of metabolism -> Less drug present
Enzyme Inducers
Metabolism
Type of enzyme inhibitors from grapefruit juice
Furocoumarins
Process of Pharmacokinetics
- Termination of drug
- Biotransformation to inactive metabolites
Elimination
Elimination
- Excretion via the (1) ____
- Excretion via other modes like (2) ____, ____, and ____
(1) kidney
(2) billary ducts, lungs, and skin
Elimination
The time to eliminate 50% of the given amount of drug or to decrease plasma level to 50% of the former drug level
Elimination Half-Life
Elimination
- The drug must have the conditions of being ____, ____, and ____ to be easily eliminated
polar, charged, and water-soluble
Elimination
- Drugs are eliminated either ____ or as ____
unchanged or as metabolites
Elimination
- ____ - for basic drugs
- ____ - for acidic drugs
- Acidification
- Alkalinization
Renal Elimination
- Filtration is (1) ____
- (2) ____ are filtered but ____ are not
(1) not saturable
(2) Ionized and nonionized / protein-bound drugs
Modes of Elimination
- Constant amount of the drug is being eliminated per unit of time
- Rate of elimination is independent of plasma concentration
- Fixed; No Half-Life
120mg -> 110mg -> 100mg -> 90mg
10mg is constantly being excreted
Zero Order Kinetics
Ex. Phenytoin, Ethanol, Aspirin
Modes of Elimination
- Constant fraction of the drug is eliminated per unit of time
- Most drugs are eliminated this way
- Half-Life is constant
120mg -> 60mg -> 30mg -> 15mg
First Order Kinetics
- Relates to drugs binding to their receptors and their effects
“What the drug does to the body”
Pharmacodynamics
Pharmacodynamics
Drug enters the plasma and lasts until it reaches the minimun effective concentration (MEC)
Onset of Action
Pharmacodynamics
Drug reaches its highest blood or plasma concentration
Peak Action
Pharmacodynamics
Length of time the drug has a pharmacologic effect
Duration of Action
Pharmacodynamics
The concentration level a drug must reach to exert its intended effect
Minimum Effective Concentration (MEC)
Pharmacodynamics
Ability of the drug to bind to the receptor
How good the drug and the receptor recognize each other
Affinity
Pharmacodynamics
The quantity of the drug to achieve a desired effect
Potency
Pharmacodynamics
Maximal effect an agonist can achieve at the highest practical concentrations
Efficacy
Pharmacodynamics
A drug binding to receptors will elicit a response
Agonist
Type of Agonist
Produce a maximal response (maximal efficacy)
Full Agonist
Type of Agonist
Less effective (incapable of eliciting maximal response)
Partial Agonist
Pharmacodynamics
A drug binding to a receptor will elicit no response and it prevents the agonist from binding to the receptor
Antagonist
Pharmacodynamics
- Fraction of the population that responds at each dose against the log of the dose administered
- At what specific dose will this drug be safe to give to the patient
Quantal Dose Response Curve
Quantal Dose Response Curve
Means 50% of the population that took the drug at a specific dose will be able to get an effect from the drug
Median Effective (ED50)
Quantal Dose Response Curve
Means 50% of the population that took the drug at a specific dose will have its toxic effects
Median Toxic (TD50)
Quantal Dose Response Curve
Means 50% of the population that took the drug at a specific dose will die
Median Lethal (LD50)
Quantal Dose Response Curve
- Reveals the range of ____
intersubject variability
Quantal Dose Response Curve
- (1) ____ required to produce a specified response is determined in each (2) ____
(1) Minimum dose
(2) member of a population
Pharmacodynamics
Measurment of drug safety
Therapeutic Index
Therapeutic Index
Dosage range that can safely and effectively treat disease
Therapeutic Window
Pharmacodynamics
Therapeutic Index = ____
TD50 / ED50
When the drug level exceed the therapeutic range, ____ are likely to occur
toxic effects
Toxic Effect of Drugs
Are physiologic effects of drugs not related to desired drug effects, may be desirable or undesirable
Side Effects
Toxic Effect of Drugs
Are a range of untoward effects of drugs that cause mild to severe side effects
Mostly negative effects
Adverse Reactions
Federal Drug Classifications / FDA Pregnancy Catergories
No evidence of risk
Category A
Federal Drug Classifications / FDA Pregnancy Catergories
Animal Studies have shown adverse effect, but adequate studies in pregnant women have not demonstrated a risk to the fetus
Category B
Federal Drug Classifications / FDA Pregnancy Catergories
There are no animal reproduction studies and adequate studies in human
Category C
Federal Drug Classifications / FDA Pregnancy Catergories
Evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women maybe acceptable
Category D
Federal Drug Classifications / FDA Pregnancy Catergories
Evidence of fetal risk and abnormalities
Category X
Toxic Effect of Drugs
Regardless of the designated category or presumed safety, no drug should be administered during ____ unless it is clearly needed
pregnancy
Bioethical and Legal Aspect
Self-determination
Autonomy
Bioethical and Legal Aspect
Trust through truth-telling
Veracity
Bioethical and Legal Aspect
Do no harm
Non-maleficence
Bioethical and Legal Aspect
Prevent harm, do good
Beneficence
Bioethical and Legal Aspect
Give to each person their right or due
Justice
Bioethical and Legal Aspect
Not to divulge information without consent
Confidentiality
Bioethical and Legal Aspect
An act to promote, require, and ensure the production of an adequate supply, distribution, use, and acceptance of drugs and medicines identified by their generic name
RA 6675 (Generics Act of 1988)
Bioethical and Legal Aspect
All prescriptions must contain the following information: Name of the prescriber, office address, license no., Professional Tax Receipt (PTR) No., patient’s name, age, sex, and date of prescription
RA 5921 (Pharmacy Act)
Bioethical and Legal Aspect
Act that identifies drugs that can harm the population through its illegal use
RA 6425 (Dangerous Drugs Act of 1972)
What to do if there are Unclear Orders
- Question the (1) ____
- Consult (2) ____ if the prescribing doctor is not available
- Ask the doctor to (3) ____
- Be familiar with the (4) ____
(1) prescribing doctor
(2) another doctor
(3) clearly write the drug order in a clearer way
(4) drug dosage
What to do if there are Telephone Orders
- Depends on (1) ____
- Write the (2) ____
- Ask the doctor to (3) ____
- (4) ____ back to the doctor
- Immediately write it to the (5) ____
- (6) ____
(1) hospital policies
(2) order (drug name, dosage, route, and frequency)
(3) repeat the order
(4) Read the order
(5) doctor’s orders sheet
(6) Document
Bioethical and Legal Aspects
- Clearly written (drug name, route, frequency)
- Specific circumstance for PRN (as needed) medication
- Do not accept unclear order if needed, if indicated as warranted
Standing Orders
Bioethical and Legal Aspects
- Verbal orders - emergency only!
Emergency/Verbal Orders
Key Points in Giving a Medication
- ____
- ____ the drug
- ____
- ____ the drug
- ____ while taking medication
- ____ of medication
- Name of drug
- Reason of taking the drug
- The dose
- Specific time to take the drug
- What specific things should or should not do while taking medication
- Possible side effect of medication
Checklist for Health Teaching in Drug Therapy
- Comprehensive ____
- ____ of drug therapy
- ____
- ____ and ____
- When to ____
- ____ and ____ interactions
- Required changes in ____
- Demonstration of ____
- ____ associated with ADLs as appropriate
- ____
- ____ to financial resources
- Developing ____
- ____
- Comprehensive drug and health history
- Reason for medication of drug therapy
- Expected results
- Side effects and adverse reactions
- When to notify physician, pharmacist, or HCP
- Drug-drug and drug-food interactions
- Required changes in activites of daily living
- Demonstration of learning
- Medication schedule associated with ADLs as appropriate
- Recording/Documentation
- Discussing and monitoring the disease to financial resources
- Developing back-up system
- Community resources
10 Rights in Drug Administration
- ® Client
- ® Drug
- ® Route
- ® Dose
- ® Time
- ® to Education
- ® Assessment
- ® Documentation
- ® Evaluation
- ® to Refuse
Nursing Responsibilites
- (1) ____
- (2) ____
- Intervening to make (3) ____
- Providing patient (4) ____
- Monitoring the overall patient care plan to ____
(1) Administering drugs
(2) Assessing drug effects
(3) drug regimen more tolerable
(4) teaching about drugs and drug regimen
(5) prevent medication errors