Prelim Chapter 1 Introduction Flashcards
According to book:
The study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes.
PHARMACOLOGY
Simplify:
Is the study of drugs
Pharmacology
From the greek word Pharmakon means—- and logos means——-
Pharmakom means drug
Logos means study
Pharmacology is the study of drug
Simplify:
For you what is pharmacology?
Pharmacology is the study of drugs, when we say we are studying about the drug, we are studying “EVERYTHING ABOUT THE DRUG” so it includes its mechanism of action, how are body respond when we take the drug and also its toxic effect!
The science of substances used to prevent, diagnose and treat disease.
Medical Pharmacology
The branch of pharmacology that deals with the undesirable effects of chemicals on living systems, from individual cells to humans to complex ecosystems.
TOXICOLOGY
Its the study of toxic
TOXICOLOGY
The science of drug preparation and the medical use of drugs – the precursor of pharmacology
Materia Medica
Precursor of Pharmacology
Materia Medica
Two General Principles: understand the concept first!
1.All substances can under certain circumstances be toxic, and the chemicals in botanicals (herbs and plant extracts) are no different from chemicals in manufactured drugs except for the proportion of impurities
- All dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies.
Answer the missing: All substances can under certain circumstances be toxic, and the chemicals in——— (herbs and plant extracts) are no different from chemicals in manufactured drugs except for the——————
All substances can under certain circumstances be toxic, and the chemicals in botanicals (herbs and plant extracts) are no different from chemicals in manufactured drugs except for the proportion of impurities
Answer the missing: All dietary supplements and all therapies promoted as health—————should meet the same standards of—— and ——- as ———- drugs and medical therapies.
All dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies.
Also known as Pharmacogenetics
Pharmacogenomics
The study of the genetic variations that cause differences in drug response among individuals or populations.
Pharmacogenomics
What do you understand by when i say Pharmacodynamics and Pharmacokinetic?
Pharmacodynamic what the drug does to the body
Pharmacokinetic what the body does to the body
What the drug does to the body
Pharmacodynamics
Keywords to remember: mechanisms of drug actions
What the body does to the drug
Pharmacokinetic
Keywords to remember: absorption, distribution, metabolism, and excretion of a drug
the biochemical and physical effects of drugs and the mechanisms of drug actions
Pharmacodynamics
the absorption, distribution, metabolism, and excretion of a drug
Pharmacokinetics
the use of drugs to prevent and treat disease.
Pharmacotherapeutics
a scientific name that precisely describes its atomic and molecular structure.
Chemical Name
•Nonproprietary name
•Abbreviation of the chemical name
Generic Name
•Brand name/ Proprietary name
•Selected by the drug company selling the product
•Protected by copyright
Trade Name
Identify if Chemical Name/Generic Name/Trade name
Paracetamol
Generic name
It is on how we classifing drug or group to study
Thru
…..Family Ties
Identify if Chemical Name/Generic Name/Trade name
APAP
Generic name
Identify if Chemical Name/Generic Name/Trade name
Acetyl-para-aminophenol
Chemical name
It is also known as APAP
N-Acetyl-para-aminophenol
This type of Class
They
Share mechanism of action
Share same structure
Pharmacologic Class
Group drugs by therapeutic use
Therapeutic class
What class if i say Beta Blocker, NSAID’s , Penicillins
Pharmacologic Class
What class when i say Antihypertensive like, beta Blocker, diuretics, ACE’s?
Therapeutic Class
Beta Blocker also known as
Beta-Adrenergic blocker
Beta-Adrenergic blocker drugs end with “—“
Olol
What does “Beta-Adrenergic blocker” block receptor?
Beta blocker receptor
Beta blocker are usually ———— drugs
Anti hypertensive drugs
Metropolol, propanolol, timolol,carvedolol and atenolol is an example of what pharmacologic class?
Beta Blockers
What does NSAID’s means
Non-Steroidal Antiinflamatory Drugs
NSAID’s are usually ———- drugs
Antiinflammatory drugs
Is paracetamol considered as antiinflammatory?
No its analgesic which is a Pain Reliever!
Diclofenac, ibuprofen, celecoxib, etoricoxib,naproxen is an example of what pharamacologic class?
Non-steroidal AntiInflammatory Drugs
This type of drug came from fungus and it can kill other microorganism
Antibacterial Antibiotic
What do you called if the antibacterial were not came from Fungus?
Sythetic AntiBacterial Agents
ARBs means
Angiotensin Receptor Blocker
CCBs means
Calcium Channel Blocker
Calcium Channel Blocker, drugs end with “———-“
Calcium Channel Blocker, drugs end with “Dipine”
If Calcium Channel Blocker, drugs end with “Dipine”, what are the two drugs that is Exempted that dont end with “Dipine” but still a CCBs?
Verapamil
Diltiazem
When Diagnose first time with hypertension,
What is the First line of drugs for hypertention?
Diuretic
Explanation: Diagnose first time with Hypertension, to Get rid of water inside the body, lower the blood volume, para di mahirapan sa Flow!
ACEs means
Angiotensin Convertig Enzyme
Angiotensin Convertig Enzyme drugs usually end with “——“
Angiotensin Convertig Enzyme drugs usually end with “Pril”
Alpha blocker drugs usually ends with “———“
Alpha blocker drugs usually ends with “sozin”
Who discover Penicillin?
Alexander Fleming
Penicillin was discover from what bacteria?
Not Bacteria! Its from Fungus
Penicillin was discover from what fungus?
Penicillium notatum
What are the three source of our Drugs?
Plants
Animals
Minerals
Morphine, codeine,antropine, from what source of drugs that it came from?
Plants
What drug/hormone do we extract from pig before, but now its not due to adverst effect
Insulin
Scientic name of plant source Morphine
Opium poppy
Scientic name of plant source codeine
Papaver somniferum
Scientic name of plant source Digoxin
Digitalis lanata
Scientic name of plant source Atropine
Atropa belladonna
Aluminum hydroxide is from what source of drug
Minerals
What is the old style or old Fashioned METHOD called?
Concoction or in bisaya “ ginapabukalan”
Old Fashioned Medinces
The earlies drug concoctions from plants used “everything” including….
Leaves
Roots
Bulb,stems
Seeds
Buds
And blossoms
Refers to a plant that is a source of medicinal powern or therapeutic properties
Power Plant
Most active component of the plants
Component of our plants with nitrogen in their structure and they are the most active in term of pharamcologic use
Alkaloids
Alkaloids components drugs usually ends with “ine” ……familiar?
Antropine, nicotine, morphine
Its the transfer of the drug from one site of administration to the blood circulation
Absorption
Amoxicillin
Therapeutic Class:
Pharmacologic Class:
Amoxicillin
Therapeutic Class: Antibacterial Antibiotic
Pharmacologic Class: Penicillin
Chemical Name : APAP or —————-
Generic Name:
Brand name:
Chemical Name : APAP or N-acetyl-para-aminophenol
Generic Name: Paracetamol or Acetaminophen
Brand name: Biogesic
Inactive the drug then transfer it into secretable form
Metabolism
In phamacokinetic,
Blood is the responsible, it circulate in the body
Distribution
Excretion of the drugs thru?
Urine, stool, sweat, Milk
“——“ is a Component of plants, found sugar in their structure
Also active component of plant
And give one example:…..
Glycosides
Digoxin
This type of drugs fron plant use to increase the force of heart contraction
Digoxin
Compenent of Plant “not active ingredient”
Give products ability to attract and hold water
Gums
Use as suspensing agent or emulsifying agent to make dosage form
Ex. Seaweed extraction
Gums
Component of plants that causes local irritants or laxative
Ex. Pinetree sap
Resins
thick and sometimes greasy liquids, are classified as volatile or fixed
Oils
Two types of Oil
Volatile Oils-(Perfume Making) peppermint
Fixed Oil-Olive Oil, Coconut oil
Animal Magnetism
Hormones
Oils and fats
Enzymes
Vaccines
In Animal Magnetism such as Insulin
Hormones
Animal Magnetism such as pancreatin and pepsin
Enzymes
Animal Magnetism such as cod liver oil
Oils and fats
Animal Magnetism such as suspension or killed, modified or attenuated microorganism
Vaccines
Iron, iodine and epsom salt is and example of
Mineral spring
In DNA, Drug produce in Laboratory such as….
Antivenoms
Insulin
Route of Administration:
Buccal
Sublingual
Translingual
Gastric
Intradermal
Intramuscular
Intravenous
Oral
Rectal and viginal
Respiratory
Subcutaneous
Topical
…
Also knowns as Rectal or Vaginal in route of administration
Suppository
What about “ilalum sa dila”
Sublingual
What about “taas sa dila”
Translingual
Motivation sa ta….
“Just as you wouldn’t settle for low-quality drugs that fail to deliver the expected therapeutic effects, consider yourselves as the product you’ll be offering in the future din. Strive for excellence to ensure na you can provide the best service possible. Your commitment to quality reflects your dedication to delivering effective solutions and services para sa future. Always think of your future patients as one of your loved ones, diba you wouldn’t want to do anything that would compromise their health? So do better. Be better. Remember, striving for excellence is not just for the sake of others but also for your own advancement.”
-Medida C. , 2024
Any SUBSTANCE that brings about a change in boilogical function through its chemical actions
Drug
Drug use to prevent, mitigate, treat, cure and diagnose
….
Two Type of drugs:
Agonist
Antagonist
In your own word what do you mean by
Agonist: (One word)
Antagonist( one word)
Agonist : ACTIVATOR
Antagonist: INHIBITOR
Any molecule that is found in our body that can play a regulatory role of our biologic function and also it is where the drug interact
Receptor
Has Affinity Only
Antagonist
- kaya niya mag bind sa receptor pero dili niya kaya mag activate sa receptor
It has Affinity to receptor and Intrinsict Activity
Agonist
Bind then activate
Drugs that dont need the receptor for it to have an effect inside the body
Chemical Antagonist- may interact directly with other drugs
Example of a chemical Antagonist?🤔
Antacid-Acid = neutralization. Why is it consider as chemical antagonist?
Antacid-Acid= neutralization
Direct na siya, no receptor involved :3
Drugs may be synthesized in the body (kita mismo ang naga buhat sa body)
Example:
Hormones- insulin
——-means chemically not synthesized in the body
Xenobiotic
Xenos- means Stranger
It is also a drug
Drug that have almost exclusively harmful effect
Poisons
No good effect, but only harmful effect
Ex. Cyanide
Who said that “ the dose makes the poison”
Paracelsus
Which means the poison of biologic origin (synthesize by plants and animals)
Toxins
In contrast to Inorganic Poisons such as lead and arsenic
Poisons
Three physical nature of drug
Solid- aspirin, antropine
Liquid- nicotine, ethanol
Gaseous- nitrous oxide
Used to dilate pupils
Atropine
Is a Nicotine a Solid, liquid or Gaseous?
Liquid
Most widely abused recreational drug
Ethanol
Long term side effect of ethanol in the body
Accumulation of fat in the tummy
Also knowns as laughting gas and general anesthetic
Nitrous Oxide
Drug size
Smallest- lithium ions(MW7)
Largest -alteplase (MW 59,050)
Most drugs( mw 100 - 1000
Drugs for Bipolar
Lithium
Alteplase is drug act as
Anticouagulant (Heart Attack , Stroke)
Three major types of bond in drug reactivity and drug-receptor bonds
Covalent
Electrostatic
Hydrophobic
Very strong and not reversible under biologic condition
Ex.
Aspirin with cycloxygenase enzyme
DNA alkylating agents used in cancer chemotherapy
Covalent bond
Very from relatively strong linkages between permanently charges ionic molecules to weaker hydrogen bond and very weak induce dipole interations such as van der waals forces
Electrostatic bonding
Drug that are lipid soluble para maka cross siya sa lipid bilayer na mga cells with the internal walls of receptor (pocket)
Hydrophobic bonds
What to remember in Bonding:
Covalent bond- very strong bond
Electrostatic bonding- weaker than covalent, generally strong bond
Hydrophobic bonds- usually Quite weak
Depends on the chirality (sterioisomerism) of the drug chemical structure
Drug shape
Implies the ability to predict the appropriate molecular structure of a drug on the basis of information about its biological Receptor
Rational Drug Design
Rational Drug Design is made by —- and —- in Research and Development of Drugs design
Pharmacist and chemist
In New Drug Development
IND means
Investigational New Drug
Most undergo extensive animal studies or also known as
Pre clinical trial
If sa tao na ang tawag kay Clinical Trial
Phases of New Drug Development
And what to remember during this Phase
Phase 1- Efficacy
Phase 2- safety and Efficacy
Phase 3 - Infrequent or rare adverst effect
Phase 4- Post market surveillance
The drug is tested on healthy volunteers.
Phase 1
involves trials with people who have the disease for which the drug is thought to be effective.
Phase 2
-large number of patients in medical reasearch centers receive the drug.
- provides information about infrequent or rare adverse effects
- FDA will approve a new drug application if phase III studies are satisfactory
Phase 3
voluntary and involves postmarket surveillance of the drug’s therapeutic effects at the completion of phase III.
Phase 4
Exception to the Rule of Phases
Public Health Threats like Covid, Aids
Sponsors of drug that reach phase 2 or 3 clinical trial can apply FDA Approval or treatment IND status
What are the two Drug-Body Interaction in pharmacology
Pharmacodynamic and Pharmacokinetic
Major site of absorption
Small intestine
-Villi and microvilli
Terms in Concentration Means
Along:
Against:
Along- higher to lower concentration
Againt- lower to Higher concentraion
Action of drug on the body
Pharmacodynamics
Action of Body on the drug
Pharmacokinetics
The transfer of a drug from one site of administration to the bloodstream
Absorption
Route of Administration that excempted from Absorption
IV
Mechanisms of absorption of drugs
Passive Diffusion
Fick’s Law of Diffusion
Facilitated Diffusion
Active Transport
Endocytosis & Exocytosis
- the drug moves from a region of high concentration to one of lower concentration
– does not involve a carrier and not saturable
– movement is along the concentration gradient
Passive Diffusion
Diffentiate Osmosis and Diffusion
Osmosis- movement of Water
Diffusion- movement of substance
•directly proportional to the concentrations, surface area and permeability coefficient
•inversely proportional to the thickness of the membrane
Fick’s Law of Diffusion
- drugs enter the cell through specialized transmembrane carrier proteins that facilitate the passage of large molecules
– movement is along concentration gradient
– does not require energy & can be saturated
– may be inhibited by compounds that compete for the carrier
Facilitated Diffusion
Active transport
- involves specific carrier proteins that span the membrane
– energy-dependent & saturable
– movement is against the concentration gradient
– selective and may be competitively inhibited by other cotransported substances
- used to transport drugs of exceptionally large size across the cell membrane
Endocytosis & Exocytosis
- engulfment of a drug by the cell membrane and transport into the cell by pinching off the drug-filled vessicle
Endocytosis
- reverse of endocytosis
Exocytosis
Cell eating
Phagocytosis
Cell drinking
Pinocytosis
Factors influencing absorption
•Effect of pH on drug absorption - A drug passes through membranes more readily if it is uncharged.
•Blood flow to the absorption site
•Total surface area available for absorption
•Contact time at the absorption surface
•Expression of P-glycoprotein -
…
The more time sa stomach, the more ma absorbed and drug, under the contact time at the absorption time, what drugs symptoms has exception of this
Diarrhea (high Motility)
2 loperamide at a time first intake in order to absorbed the drug
- responsible for transporting various molecules, including drugs, across cell membranes
– “pumps” drugs out of the cells
– associated with multi-drug resistance
•Expression of P-glycoprotein
Responsible for MultiDrug Resistance
Expression of P-glycoprotein
•is the rate and extent to which an administered drug reaches the systemic circulation
•determined by comparing plasma levels of drugs after a particular route of administration with levels achieved by IV administration
Bioavailability
It has a 100% Bioavailability
IV
Major site of Metabolism
Liver
Factors Influencing Bioavailability
•First-pass Hepatic Metabolism
•Solubility of the drug
•Chemical instability
•Nature of the drug formulation
- when a drug is absorbed from the GI tract, it enters the portal circulation before entering the systemic circulation
First-pass Hepatic Metabolism
Two drug are bioequivalent if they show comparable bioavailability and similar times to achieve peak blood concentrations.
BIOEQUIVALENCE
•Two drugs are therapeutically equivalent if they are pharmaceutically equivalent with similar chemical and safety profiles.
THERAPEUTIC EQUIVALENCE
If the Drug
-same Dosage Form
-contain same active ingredient
-same ROUTE OF ADMINISTRATION
Pharmaceutical Equivalence
the process by which a drug reversibly leaves the bloodstream and enters the instertitium (extracellular fluid) and the tissues.
DRUG DISTRIBUTION
Responsible for DRUG DISTRIBUTION
Blood!
III. METABOLISM OF DRUGS
•Three major routes of elimination(Excretable):
– Hepatic metabolism
– Biliary metabolism
– Urinary metabolism
Two purpose of Metabolism
Activation and Inactivation of Drug
•an inactive precursor chemical that is readily absorbed and distributed and then converted to the active drug by biologic processes inside the body
Prodrug
They are inactive and they need the help of liver para ma activate ang drug
Prodrug
Example of Prodrug
ACE’s that end with “Pril” except Captopril(already active)
Prodrugs ACEs end with “pril” except
Captopril (already active)
Inactive:Enalapril
Active:
Inactive:Enalapril
Active: Enalaprilat
Inactive: Quinapil
Active:
Inactive: Quinapil
Active: Quinaprilat
Inactive:captopril
Active:
X
Active na siya daan😂🫣🤡
All ACEs end with “pril” is a prodrug except: Captopril
Major site of Excretion
Kidney
Filtering unit of kidney
Nephron
IV. EXCRETION
•A. Renal elimination of drugs
– Glomerular filtration
– Proximal tubular secretion
– Distal tubular reabsorption
…..
Excretion can be secreted as
Stool
Milk of mother
Sweat
Urine
Antidote for Paracetamol Poisoning
Fluimucil
