PCOL 211 – Intro to Pharmacology 1 o Effect = Activates or Inhibits

Pharmacology body process

- Drugs are used in:
- Science of drugs and their effects on
o Prevention: ex. Vaccines; Oral
biological system
Contraceptive Pills (OCP)
Divisions of Pharmacology o Diagnosis: ex. Barium sulfate
(BaSO4) used as contrast
- Clinical Pharmacology medium in x-ray examination of
o Effects of drugs in humans GIT
o Patient care oriented o Mitigation: Reduction of
- Neuro Pharmacology severeness; Ex. Analgesics
o Effects of drugs in CNS and PNS o Treatment/Cure: Ex. Antibiotics
- Environmental Pharmacology
o Gene; Toxin; Drug-environment Nature of Drugs
interaction
1. Size and Molecular Weight
- Pharmacognosy
o MW < 100 = Rarely Selective
o Drugs of Biological and natural
o MW > 1000 = Poorly absorbed
origin (Plants)
and poorly distributed
- Posology
o Drug size varies from MW 7
o Associated with dosing of drugs
(Lithium) to over 50,000
o Affected by Race, Age, Weight …
(Thrombolytic enzymes and
- Toxicology
other proteins)
o Associated with Toxic and
▪ Majority of drugs have
Adverse effects
MW between 100-1000
- Pharmacoepidemiology
2. Drug-Receptor Bond
o Effects of drugs in large amount
▪ Stronger bond =
of people
irreversible effect
- Pharmacogenetics/Pharmacogenomics
o Covalent Bond = Strongest Bond
o Effects of drugs within Genetic
o Ionic Bond = Electrostatic Bond
variations (DNA)
o Hydrogen Bond
History o Van der Waals = Weakest Bond
3. How drugs are named
- De Materia Medica o Chemical name
o Precursor of Pharmacology ▪ Ex. 2-(p-isobutyphenyl)
o Written instructions for drug propionic acid
preparation and its effects o Generic/Nonproprietary name
o Written by Greek Physician ▪ Ex. Ibuprofen
Pedanius Dioscorides ▪ Guided and mandated
Drug by INN and/or USAN
▪ INN = International
- Any substance that brings change in Nonproprietary name
biologic function through its chemical ▪ USAN = United States
actions Adopted Name
- Drug –(Binds to Receptor)–> Effect
 o Trade Name/ Proprietary o H2 Blockers examples
Name/ Brand Name ▪ Cimetidine
▪ Ex. Motrin® ▪ Ranitidine
▪ Famotidine
Classification of Drugs according to use
▪ Nizatidine
- Functional modifiers - Diagnostic Agents
o Alters/Modulates normal o Agents used to determine
physiologic functions presence or absence of a
▪ Analgesics condition/disease
▪ Antipyretics o Edrophonium
▪ Anti-inflammatory ▪ Used in Tensilon’s Test
▪ Antihypertensive for Myasthenia Gravis
- Replenisher (Identified by severe
o Supplements endogenous muscle weakness)
substances lacking or deficient o Histamine
in the body ▪ Used in diagnosing
▪ Hormones = Insulin for allergic anaphylaxis
Type 1 DM o Radiopharmaceuticals
▪ IV Fluids/ Electrolytes/ ▪ Technetium 99m – for
Oral Rehydration salts ischemia diagnosis
for emesis and • Ischemia –
dehydration reduced blood
▪ Multivitamins flow and
o Pernicious Anemia oxygen
(Autoimmune disease) destroys ▪ Thallium 209 – for
parietal cells, infarction diagnosis
▪ Parietal cells are cells in • Infarction – no
the stomach that blood flow and
secretes HCl and oxygen
intrinsic factor o Barium sulfate
▪ Vitamin B12 ▪ Medium contrast for X-
(Cobalamin) should be ray GIT diagnosis
taken o Pharmacologic Stress Test
o Pernicious Anemia may be ▪ Electrocardiographic
caused by Proton Pump test of heart function
Inhibitors (PPI), Histamine 2 before, during, and
(H2) Blockers, and Fish Tape after controlled period
worms of increasing strenuous
o PPI examples exercise
▪ Omeprazole ▪ Dobutamine – B1
▪ Esomeprazole agonist, increases heart
▪ Lansoprazole contraction, heart rate
▪ Rabeprazole ▪ Dipyridamole – Anti-
▪ Pantoprazole platelet
 - Chemotherapeutic agents o Dissolution – Rate-limiting step
o Kill or inhibits growth of cells or in solid dosage form
nucleic acid considered foreign absorptions, dissolving of solid
to the body drug into medium
o Selective toxicity – specifically
Factors Affecting Dissolution Rate
targets selected
microorganisms - Surface area
▪ Anti-infectives o Higher S.A., Lower P.S., Higher
• Antibiotics D.R.
• Antiprotozoals - Salt form
• Antivirals o Dissolves readily compared to
▪ Antineoplastics drug in free form
• For cancer - State of Hydration
treatment and o Anhydrous form more soluble
prevention than hydrated form
o Ex., Ampicillin anhydrate >
2 Main areas of Pharmacology
Ampicillin trihydrate
- Pharmacokinetics - Crystal form or Amorphous form
o Study of the drugs movement o Ex. Chloramphenicol palmitate
and fate in the body inactive in crystalline form but
- Pharmacodynamics readily absorbed in GIT as
o Study of the body’s reaction to amorphous form
drugs o Short-acting Insulin (100%
amorphous)
Pharmacokinetics ▪ Semilente
- Study of the drugs movement and fate ▪ Rapid on-set; Short
in the body duration
- Drug disposition – way in which the o Intermediate Insulin (30%
body handles drugs Amorphous; 70% Crystalline)
- Process identified by LADMERT ▪ Lente
o Liberation o Long-acting Insulin (100%
o Absorption Crystalline)
o Distribution ▪ Ultralente
o Metabolism ▪ Short on-set; Long
o Excretion duration
o Response/Reabsorption Absorption
o Toxicology
- Rate and extent of drug entry into
Liberation systemic circulation
- Release of API from its dosage form; - Bioavailability – proportion of drug
usually identified in solid oral dosage delivered to site of action in the body
forms Factors Affecting Absorption
o Disintegration – breakdown into
smaller particles 1. Dose Size administered
 o Higher dose; Higher drug o Solid drug – dissolve/dissolution
absorption → Drug in solution –
2. Degree of Perfusion of the Absorbing Absorption
Environment 7. Drug solubility
o Perfusion = Blood supply o For a drug to be absorbed,
o Higher Perfusion; Greater solubility must correspond to
Absorption the characteristics of the
3. Areas of the absorbing surface absorption site
o Larger Area; Greater Absorption 8. First-pass effect
4. pH of the absorbing environment o Partial metabolism of drugs in
o Acidic drugs best absorbed in the liver or hepatic portal vein
acidic environments thus decreasing its
o Basic drugs best absorbed in concentration once entering the
basic environments system circulation
o Drugs in favorable environment o Lower concentration, lesser
produces non-ionized form absorption
which are uncharged and is o Routes that do not undergo
absorbed better than charged first-pass effect:
ionized forms ▪ Sublingual
o Ex. Aspirin, an acidic drug, is ▪ Buccal
absorbed better in the stomach. ▪ Rectal
In cases of Aspirin OD NaHCO3 ▪ Parenteral
is used to alkalinize and excrete ▪ Topical
aspirin. ▪ Inhalant
5. Gastric Emptying time ▪ Intranasal
o Time it takes for stomach to 9. Enterohepatic recycling
empty its contents o Drugs that travel through biliary
- Factors increasing gastric emptying time tract after initial absorption are
o Stress reabsorbed into the
o Heavy exercise bloodstream through the
o Gastric ulcers intestine instead of undergoing
o Hot food (Protein and Lipid rich excretion
foods) 10. Routes
o Lying on the Left side o Drug’s route of administration
o Drugs inhibiting gastric motility affects the rate and extent of
- Factors decreasing gastric emptying absorption
time o 100% Bioavailability =
o Mild exercise Intravenous route
o Gastrectomy o Enteral Route
o Cold food ▪ Oral; Sublingual; Buccal;
o Lying on the Right side ;Rectal
o Use of motility enhancing drugs o Parenteral Route
o Diabetes Mellitus ▪ IV; IM; SC; ID
6. Dosage form o Topical Route
 ▪ Skin; Transdermal; Eyes; o Exocytosis – releasing of
Ears; Nose; Lungs; molecules from the cell
Vaginal - Iron-pair Transport
o Enteral route; drug is absorbed o Pairing of a charged ion to
into the systemic circulation another ion with the opposite
through the oral or gastric charge to produce unionized
mucosa, small intestine, or form that is easily transported
rectum to the cell membrane
11. Transport Mechanism o Ex. Quaternary Ammonium
o The means of movement of Compound (+) and Mucin (-)
drug molecule across the cell
membrane

Modes of Drug Transportation

- Passive diffusion
o Most dominant and slowest
transportation mode
o Moves along the concentration
gradient
- Carrier-Mediated Transport
o Facilitated diffusion
▪ Passive movement of
molecules along the
concentration gradient
by means of a transport
protein
o Active transport
▪ Movement of
molecules against the
concentration gradient
by means of an energy
using transport protein
- Convective (Pore) Transport
o Transporting small molecules
between 150-400 MW with a
water filled pore channel called
Aquaporins
- Vesicular Transport
o Bulk transport of large
quantities of molecules through
a bubble-like structure called
Vesicles.
o Endocytosis – capturing of
molecules outside the cell