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01 Introduction To Pharmacology
01 Introduction To Pharmacology
LECTURE AUF-CON
PROCESSES
● A. Disintegration
○ Manual breakdown of tablets into smaller
pieces
○ Paano nadudurog
● B. Dissolution
FACTORS AFFECTING BODY’S RESPONSE TO ○ The process of dissolving smaller particles in
DRUGS the GIT before absorption
○ Liquefaction
● Three main factors that affects how the body
● Since solid particles cannot be absorbed by
responds to different chemicals or drugs exposed
the body (GIT), it needs to be liquified
to it
○ Paano natutunaw
○ DOSAGE: amount of medication administered
○ INJECTED MEDICATIONS
○ TIMING: frequency, intervals or timing of drug
● ‘Yung mga tinutusok sa swero, since diretso
administration
na sila sa circulation, there is no need for
○ ROUTE: route of medication administration
dissolution process
● Not following the prescribed DTR can lead to
toxicity, resistance, and superinfections
IMPORTANT TERMS
● Nursing Responsibility: provide and reiterate
health teachings about the appropriate use and Rate Limiting (RL) — ↓RATE LIMITING ↑ABSORPTION
●
intake of medications which includes the DTR
○ The time it takes a drug to disintegrate and
dissolve to become available for the body to
DIFFERENT PHASES absorb
○ Shorter rate limiting = faster absorption
● These are necessary for drugs to have a
● Excipients
therapeutic effect
○ Fillers and inert substances that take a
particular size and shape which enhances the
PHARMACEUTIC PHASE
dissolution phase (SHORTER RATE LIMITING)
● The first phase for orally-administered drugs ○ Binders and additives added into a drug to
○ Necessary for it to take effect have a shape and to liquify and dissolve rapidly
○ Oral medications are needed to be converted for faster absorption of the body
to a soluble liquid form to pass the ● Same drug, different size/shape
semipermeable layer ● Enteric Coated Medication
● Since it is needed to be absorbed by the GIT ○ Medications that are intended to be dissolved
system in the small intestine (an area that is less acidic
● Manual breaking down of medications into smaller compared to the stomach)
pieces ● Some medications possess a property that
○ Describes how solid forms of drugs disintegrate, causes them to be destroyed once exposed
becomes soluble and get absorbed into the to an area of high acidity (i.e. stomach)
bloodstream ○ Enteric coatings allow them to pass
● 💡 KEY IDEA: dinudurog at tinutunaw ang gamot through the gastric region and be
dissolved/absorbed in the small
para magka-effect sa katawan
intestine
● Not all tablets can be crushed, not all
capsules can be popped open
● Nursing Responsibility: not to crush or ○ Highly lipid-soluble drugs are absorbed more
open any enteric coated medication as it rapidly than drugs that have low lipid solubility
defeats the purpose of protective coating ○ Lipids and water do not mix
● Requires an emulsifying agent
PHARMACOKINETIC PHASE ○ Fat-Soluble vs Water-Soluble
● The GIT is lined with a phospholipid bilayer.
● The second phase which determines what the Hence, water-soluble medications do not
body does to the drug pass through the membrane easily,
● Determines how much of the administered dose affecting absorption
gets to its site of action ● Fat-soluble are absorbed faster than
○ 📌 KINETIC: how the drug moves inside the water-soluble as they easily pass through
body the bilayer
● Involves four different processes of drug movement ● pH Partitioning — NON-IONIZED = ↑ AB
to achieve the drug action (ADME) ○ Ionization has an important role in absorption
● 💡 KEY IDEA: ano’ng ginagawa ng katawan mo sa ● Kapag naiiba ‘yung drug (stand out), hindi
gamot kapag na-absorb na siya siya na-a-absorb nang mabilis
○ Non-ionized drugs are absorbed faster than
1. ABSORPTION ionized drugs
● Since same sila sa environment, mas
● Movement of drug from the site of administration to mabilis ‘yung absorption
the bloodstream ● Acidic medication + acidic environment =
faster absorption
FACTORS AFFECTING DRUG ABSORPTION
DIFFERENT MODES OF DRUG ABSORPTION
● Rate of Dissolution — ↓ RL = ↑ LIQ [RD] = ↑ AB
○ Prior to absorption, a drug must be dissolved ● Passive Absorption
first ○ Drug movement across the membrane that
○ Faster liquefaction, faster absorption does not require energy (e.g. diffusion)
● Surface Area — ↑ SA = ↑ AB ● Seen in lipid-soluble and non-ionized drugs
○ The larger the surface area, the faster the ○ Effortless movement
absorption ○ Depends on gradient differences
○ Intestinal villi (small intestine) and gastric ● Active Absorption
rugae (stomach) help with the faster ○ Drug movement that requires effort or a carrier
absorption of medications (ciliated projections (e.g. enzymes and different protein carriers) to
increases surface area) move the drug against a concentration
gradient
● Involves gated channels
○ Pinocytosis
● Cells carries the drug across membrane
barriers by phagocytizing/engulfing the
drug
● Bioavailability
○ A subcategory of absorption described as the
percentage of the administered drug dose that
reaches the systemic circulation (the
proportion of the drug that reaches its site of
● Blood Flow — ↑ BF = ↑ AB action)
○ Drugs are absorbed more rapidly in sites where ○ Drugs taken orally often have less than 100%
blood flow is high bioavailability while medications inserted
● RBCs and protein carry the medication intravenously/parentally have 100%
○ Subcutaneous vs Muscular ● Marami ‘yung pwedeng masira during the
● Mas mabilis ma-absorb sa muscular kasi pharmaceutic phase (orally-taken
mas marami ‘yung blood supply ro’n medications) before siya makaabot sa
● Lipid Solubility — LIPID-SOLUBLE = ↑ AB systemic circulation
○ Before it is distributed throughout the 2. Drug A, 500 mg, was administered to a client
body, it is screened in the liver and can complaining of fever. According to the manufacturer,
be metabolized there the drug has a T ½ = 2 hours. How much drug is left
○ Metabolism: napapawalang-bisa ang after 4 hours?
gamot na ininom mo; being converted A: 125 mg (500 mg * 0.25 [25% converted to decimal];
from an active to inactive particle get 25% of the drug)
○ EX.: Nitroglycerin has a high first pass
effect, which means that it is 3. A medication will be administered (1000 mg) to the
immediately converted into its inactive patient. How much drug will remain in your system
form after 9 hours if the half-life of the medication is 3
● 📌 REMEMBER: Drugs with high first pass hours?
effect should not be taken orally A: 125 mg (~12% of 1000; 1000/23 [8])
○ 💡 KEY IDEA: High first pass effect → faster
metabolism → lesser time for absorption in 4. A medication will be administered (1000 mg) to the
circulation (bioavailability) → lesser effect patient. How much drug will remain in your system
(useless) after 8 hours if the half-life of the medication is 2
● Half-life (t 1/2) hours?
○ The time it takes for half of the drug A: 62.5 mg (8 hours total time ta’s half life is 2 hours
concentration to be eliminated so 4 ang X then 1000/2 raised to 4 = 62.5)
○ This will determine the frequency of drug
administration for you will be able to determine 5. A medication will be administered (1000 mg) to the
or compute the time it takes to reach a steady patient. How much drug will remain in your system
state serum concentration of the drug after 5 hours if the half-life of the medication is 2
hours?
A: 187.5 mg
Sol.:
● After 2 hours, 500 mg of medication will be left;
after 4 hours, 250 mg will be left; after 6 hours,
125 mg will be left
● Between the 4th hour and the 6th hour, 125 mg
was reduced
● To get how much drug is reduced per hour
[after 4th hour is 5th hour], you will divide 125 by
2 = 62.5 and subtract it from 250 (4th hour)
● → [250 - 62.5 = 187.5])
● Prodrugs
○ Compounds that are pharmacologically
inactive when administered (no therapeutic
effect), however, it undergoes conversion to its
active form (increased therapeutic effect) via
metabolism
4. EXCRETION
PEAK OF ACTION
FORMULA: TI = TD50/ ED50 or ED50/ TD50 ● POTENCY: amount of drug needed for the
📌 REMEMBER: The closer the TI value is to 1, the higher medication to take effect
the chances of causing toxicity (narrow therapeutic
index/small margin of error; always monitor drug LOADING DOSE
serum concentration)
● A large or significantly higher initial dose of the drug
given to achieve a rapid minimum effective
concentration (onset of action) in the serum
concentration
● Used when immediate drug response is desired;
para maging potent kaagad
MAXIMAL EFFICIENCY
● Relationship between the minimal versus the 📌REMEMBER: All adverse effects are secondary, but
maximal amount of drug dose needed to produce not all secondary effects are adverse.
the desired drug response
● Physiologic response to changes in drug IDIOSYNCRATIC RESPONSES
concentration
● Unexpected responses