Introduction To Pharmacology Flashcards
What are the divisions of Pharmacology
4PCNET
- Clinical Pharmacology
- Neuropharmacology
- Pharmacogenetics/-genomics
- Pharmacoepidemiology
- Toxicology
- Posology
- Pharmacognosy
- Environmental Pharmacology
Division that encompasses all aspects of the relationship between drugs and humans
Clinical Pharmacology
Division pf pharmacology under the discipline of neuroscience that aims to understand the actions of drugs on neurobiological processes in the mammalian nervous system
Neuropharmacology
Division that studies genetic causes of individual variations in drug response or simultaneous impact of multiple mutations in the genome that may determine the patient’s response to drug therapy.
Pharmacogenetics/Pharmacogenomics
Division that focuses on the utilization and effects of drugs in large numbers of people (usually as a part of post-marketing surveillance)
Pharmacoepidemiology
Division of pharmacology that studies the mechanisms by which drugs and chemicals in the environment produce unwanted effects (Toxic dose)
Toxicology
Division of pharmacology that is concerned with drug dosage, response, and toxicity
Posology
Division that studies drugs obtained from natural resources including plants, microbes, animal tissues, and minerals
Pharmacognosy
Division that focuses on the knowledge, study and the methods implemented for amalgamating the presence of pharmaceutical products and their metabolites in the environment
Environmental pharmacology
By this time, pharmacy is already an established profession where apothecaries mix and sell their own medicine to cater both medical practitioners and street costumers
17th century
These are substances that bring about change in biologic function through chemical actions. These are used in the prevention, diagnosis, mitigation, and treatment of diseases.
Drugs
Size variations of drugs according to molecular weight
MW 7 (Li) to MW 50,000 (thromolytic enzymes and proteins)
most drugs are between MW 100 - 1000
At what sizes of drugs can they be considered rarely selective or poorly absorbed by the body?
Rarely selective = less than 100
Poorly ABS and DIS = greater than 10000
Order of Drug Receptor Bonds according to strength from strongest to weakest
CIHV
- Covalent bond (irreversible)
- Ionic bond (electrostatic)
- Hydrogen
- Van der Waals
How are drugs named?
by Chemical, Generic, and Trade
Generic or nonproprietyary names follow conventions set by what institutions
INN USAN
- International Nonproprietary Names (INN)
- United States Adopted Name (USAN)
What are the classifications of drugs according to use?
FRDC
Functional Modifiers
Replenishers
Diagnostic Agents
Chemotherapeutic Agents
These drugs supplement endogenous substances that are lacking or deficient in the body.
**REPLENISHER DRUGS **
* Hormones (Insulin),
* Multivitamins,
* IV fluids, Electrolytes, Oral Rehydration Salts,
* Vit B12 (pernicious anemia)
These drugs alter or modulate body functions and processes
FUNCTION MODIFIER DRUGS
[Analgesics, Anti-pyretic, Anti-inflammatory, Anti-hypertensive]
These are agents used to determine any presence or absence of a condition or disease.
DIAGNOSTIC AGENTS
* Edrophonium (Tensilon),
* Histamine,
* Radiopharmaceuticals,
* Barium Sulfate (BaSO4),
* Dobutamine and Dipyridamole (Pharmacologic Stress Test for cardiac diseases)
Tensilon test is a diagnostic test used to evaluate what disease?
myasthenia gravis (muscle weakness)
These are agents that kill or inhibit growth of cells or nucleic acid considered as foreign to the body
Selective Toxicity considered
Chemotherapeutic Agents
* Anti-infectives
* Antineoplastics
Branch of pharmacology that studies the fate of drugs in the body or the effect the organism has on the drug
Pharmacokinetics
LADMERT
Branch of pharmacology that studies the action of the drug on the organism
Pharmacodynamics
This is the way in which the body handles the drug
how drugs enter/exit the body and how concentrations change over time
Drug disposition
pertains to the release of AI from the dosage form
Liberation
Disintegration & Dissolution
Factors influencing dissolution
SSSC
- Surface area
- Salt forms
- State of Hydration
- Crystal or Amorphous form
The rate and extent of drug entry into the systemic circulation
Absorption
What are the factors affecting absorption?
GFRET PADDDS
- size of dose administered
- degree of perfusion in the absorbing environment
- areas of absorbing surface
- pH of absorbing environment
- gastric emptying time
- dosage form
- drug solubility
- First pass effect
- enterohepatic recycling
- route of administration
- transport mechanisms
Aspirin is an acidic drug. In the stomach, will it exist mostly in ionized or non-ionized form?
Non-ionized. Aspirin is a weak acid and it tends to ionize (give up a H atom) in an aqueous medium at high pH. In a low pH environment like the stomach (pH =2), aspirin is predominantly unionized and crosses membranes into the blood vessels readily.
non-ionized = absorbed; aspirin is absorbed in the stomach
To increase the absorption of a basic drug…
To decrease the absorption of an acidic drug
alkanize the environment
To increase the absorption of a acidic drug…
To decrease the absorption of an basic drug
acidize the environment
What are the factors affecting the increase of gastric emptying time?
GLDSHH
Stress
Heavy exercise
Gastric ulcers
Hot Food
Lying on the left side
Drugs inhibiting gastric motility (Lopermide)
What are the factors that decrease the gastric emptying time
GDMCRE
- Gastrectomy
- Mild excercise
- Diabetes mellitus
- Cold food/drinks
- Lying on the right side
- Motility enhancing drugs (bisacodyl)
What type of dosage form undergoes liberation and what skips it?
solid dosage forms = liberates
solutions = direct to ABS
A phenomenon in which a drug gets metabolized at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the systemic circulation
First-pass Effect
This happens when some of the drugs that travel intact through the biliary tract after 1st ABS are reabsorbed into the bloodstream through the intestine
Enterohepatic recycling
These are the means of movement of drug molecule across cell membrane
Transport mechanism
What are the different modes or mechanisms of drug transport?
PCCVI
- Passive Diffusion
- Carrier-mediated Transport
- Convective Transport
- Vesicular Transport
- Ion-Pair Transport
molecules that can be transported through convective (pore) transport
- organic and inorganic electrolytes (150 - 400 MW)
- ions of opposite charge
- ionized sulfonamides
molecules that are transported through bulk or vesicular transport
- fats, glycerin, starch,
- parasite eggs and yeast cells
- plastic particles
- hairs
- Ferritin and insulin
molecules that are transported by ion-pair transport
QACs (+) and Mucin (-)
uncharged = easily absorbed through cell membrane
the process of transport of drug from the bloodstream to the site of action; drug passed into different tissues and fluid compartments of the body
Distribution
Parameters of Distribution
Vanilla Pumpkin Beer
Volume of Distribution
Protein Binding
Blood Brain and Placental Barrier
Physiocologic factors affecting Distribution
- Cardiac Output
- Regional Blood Flow
the* hypothetical* volume of body fluid required to dissolve a given amt of dose of drug to achieve conc = drug plasma conc
Volume of Distribution
Distribution of basic drugs vs acidic drugs
Acidic drugs (highly protein-bounded) = low VD
Basic drugs (extensively taken up by tissues) = high VD
A: chlorpropamide, tolbutamide
B: chloroquine, atropine, raloxifene
Phenomenon when drug combines with plasma, particularly albumin, or tissue protein to form a complex
Protein binding
Each protein binders bind to?
* albumin
* alpha acid glycoprotein
* lipoproteins
* globulin
* erythrocytes
- albumin = acidic drugs
- alpha acid glycoprotein = basic drugs
- lipoproteins = lipids and proteins
- globulin = hormones
- erythrocytes = exo/endogenous compounds
Types of hormones that bind to each type of globulin
* alpha 1
* alpha 2
* beta 1
* beta 2
* gamma
- alpha 1 = steroidal drugs
- alpha 2 (ceruloplasmin) = Vit ADEK
- beta 1 (transferrin) = ferrous ion
- beta 2 = carotinoid
- gamma = antigen
Factors affecting protein binding
- drug
- protein
- protein affinity to the drug
- drug interactions
- patient’s physiologic condition
What type of drugs can permeate the blood brain barrier?
Lipid-soluble drugs with very low molecular weight
pertains to the proportion of drug delivered to the site of action in the body
Bioavailability
Tuberculosis Tx; undergoes PhII first before PhI
Isoniazid
Why is metabolism important? give its purpose
- increase water solubility
- detoxify
- terminate pharmacological effect of the drug
the time required for any specified property (e.g. the concentration of a substance in the body) to* decrease by half*
Half Life
drugs that decrease metabolic activity of enzymes to increase pharmacologic action of co-administered drugs
Enzyme inhibitors
static as cement
Examples of Enzyme inhibitors
CKCDAG
- Isoniazid
- Cimetidine
- Ketoconazole
- Chloramphenicol
- Disulfiram
- Grapefruit Juice
- Acute Alcoholism
Drugs that increase metabolic activity of an enzyme, decreasing the pharmacologic action of co-administered drugs
CarbaPhenPhen SCARifamp
Enzyme Inducers
fast movers
Examples of enzyme inducers
CarbaPhenPhen SCARifamp
- Carbamazepine
- Phenobarbital
- Phenytoin
- Rifampicin
- Griseofulvin
- Chronic Alcoholism
- Smoking
Metabolism that polarizes drugs (more water soluble), and adds a chemically reactive functional group (-OH, -SH, -NH2) permitting conjugation in Phase 2;
Functionalization Rxn
Phase 1 Metabolism
Oxidation Reduction Hydrolysis
PH1 add oxygen or hydroxyl
ROH
oxidation
CYP450 - Iron
Non CYP 450 mediated kinemelins
Azo N=N
After phase 1, this is where an endogenous compound such as SO4)2, glucuronic acid, glycine, or glutamine, is added that increases polarity further
Conjugation Reactions
Phase 2 metabolism
Detoxification - GSH
Purposes of Phase 2 Metaolism
- Detoxification
- Terminate pharmacologic activity
- increase water solubility
phase 2 reactions that terminate pcol activity
Methylation and Acetylation
This is a detoxifying agent that combines itself to chemically reactive compounds to prevent damage to DNA, RNA, and proteins
Glutathione (GSH)
composed of glycine, cysteine, and glutamic acid
Glucuronidation
inability of newborns to conjugate bilirubin with glucuronic acid
neonatal hyper-bili-tubi-nemia
due to the inability to metabolize chloramphenicol of babies
Gray Baby Syndrome
Toxic metabolite of Paracetamol
NAPQI
N-acetyl-p-benzoquinone imine
disease due to inability to acetylize drugs
