2022 PHARMA TRANS Recording

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NRS 2109-7 Pharmacology

Prof. Glenn L. Rianzares

U – Umiwas (Preventive)
Contents
• Basic Pharmacology Concepts T – Tukuyin ang sanhi (Diagnosis)
• Introduction to Pharmacology
• Pharmacokinetics Pharmacokinetics
• Pharmacodynamics
• Different factors affecting pk and pd
parameters A – Absorption
D – Distribution
Pharmacology
M – Metabolism
Pharmacology – the study of drug use in the
prevention, diagnosis, and treatment of the E – Elimination/Excretion
disease. (General definition) Empirical doses
• Study of drugs in prevention: could be • How is the drug being distributed
vitamins, prophylactic drugs (prep drugs), • Ex: In drugs for neuro, we have blood brain
polio vaccine, chloroquine (to prevent barrier that prevents the entrance of other
malaria) molecules. So, when we have infections in
• Study of drugs in diagnosis: th brain, we need higher dosage (1,500 ml)
radiopaque/radioisotopes agents (used for • Being given by the experience
visualization during x-rays), aspirin, PPD • Nursing responsibility: Monitor the toxic
(purified protein derivative) used to effects of that medication to our patients.
diagnose TB, Flourecein
Absorption
• Study of drugs in treatment: Anti-biotic,
anti-inflammatory, etc. Absorption – uptake into the circulations, how it
• PK – Pharmacokinetics can reach the circulation. (Kung gano karami yung
• PD – Pharmacodynamics gamit na nar-reach nya yung circulation mo)
Pharmacokinetics bioavailability
• What the body does to the drugs • Bioavailability is the rate and extent of
• How the body process the drug systemic absorption. (Kung gano kadami at
Pharmacodynamics gaano katagal tumatagal yung absorption
into the systemic circulations.)
• What the drugs does to the body o Absolute – given na yung absorption
• Power of the drug o Relative – another way para maging
• Effect of the drug to the body bioavailable yung medication (water
soluble, fat soluble) needs certain
Gamut mnemonics (PD)
precursor to be available
G – Ginhawa (Symptomatic)
A – Alisin ang sanhi (Curative) Bioequivalent drugs
M – Ibalik sa normal (Restorative)
NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

Bioequivalence – biochemical similarity of two or Fillers


more drugs that share the same active ingredients
• Tablets are not 100% is not all drugs.
and desired outcomes for the patient.
• Inserted into substance to prepare the
• Differences in your bioavailability of the drugs.
drugs that are not statistically significant. • Used in drug preparation
• Magkakaibang drugs na medyo may • For the drug to achieve a particular size or
kamukha but not stat significant. shape
• May mga gamut kasi nan add-decrease and
Determination of Absorption absorption sa GI Tract
• For better absorption
• Disintegration • Enhances dissolution process
• Dissolution • Additives: sodium and potassium salt (ex.
Penicillin)
• Diffusion
• 80% of drugs are taken orally
Drugs in liquid form
o First phase of Drug Action
• GI Tract → medication taken orally will
pass in the GI Tract • Drugs in liquid form are more rapidly
available for GI absorptions since they will
Disintegration, Dissolution, & not undergo the disintegration and
diffusion dissolution process.
• Drugs dissolved more faster in an acidic
fluid
Disintegration – breakdown of tablets in a smaller o Ph 1-2 – Acidic
particle o Normal Ph in blood: 7.4 (perfect
normal)
Dissolution – drugs will be dissolved in a smaller
particle into the GI fluid before the drugs will be
absorbed
Considerations

Drugs that are in liquid form are already solution.


• Young and elders have different
Rate Limiting metabolism.
o Lesser gastric production for them
for better absorption.
Rate Limiting – the time you take the drugs to o Gastric Irritant – needs food +
disintegrate and dissolve for it to have availability causes gastric irritation that will lead
in your body to be absorbed. to ulcer
• Azithromax – suspension (needs to be
• Time it takes to disintegrate and to be
shaken) mas better na iniinom na walang
dissolved.
NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

laman ang tyan bcs nababawasan ng 50% • Diet, presence of different pathological
(ang acidic environment) pag kumakain process such as cancer into the intestine,
• Most pain relievers are gastric irritant. infections, can decrease mucosal villi =
• Enteric coated tablets/capsule - has lesser absorption
specific coating • Manner of giving the drugs could be
o to prevent the drugs to be disoluted changed because of certain pathologica
o Magkakaroon ng dissolutions into condition either change the dose or change
alkaline environment (small the route
intestine) • Surgery – removal portions of the intestine
o Delayed in onset then you also removes mucosal villi which
o Should not be crushed! decreases absorption

Passive absorption
Pharmacokinetics

• Promotes drug safety • Happens without any requirement of


• Maximize the therapeutic effect and lessen energy
the harm • Diffusion of the drug (no energy)
• Steroids are highly gastric irritant • No atp, lacks oxygen and glucose
• Cell stabilizer to prevent intercranial • Pyruvate is produced then to lactate then
pressure to the patient but induces gastric lactic acid
ulcer
Active absorption
Considerations in pharmacokinetic
factors
• Requires drug to move across to your body
• Minimize harm • With the aid of glucose and oxygen
• Avoids unnecessary effects of the drug into consumption to produce atp
our patient • Requires movement
• Knows how to select the most effective • Pinocytosis – cell drinking
route of the drugs, including its dosage and o Engulf drug particles
time of administration o Cells can absorb by means of
• Reduces drug error drinking

Pathological conditions that affect


absorption

• Absorption happens from the GI tract to


small intestine
NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

Week 2 - Contents I. Pharmaceutical Type


a. Type of drug
i. Dose formulation (form nung
drugs)
ii. Route of administration
b. Physiochemical properties of the
drugs
i. Lipid solubility
ii. Particle size
c. Excipients and container – inactive
GI membrane substance that actually serves to the
drug for medium of vehicles. (Ex.
It is made up of:
Preservative of the drugs, coloring,
o Fats & CHON (proteins) → fillers)
embedded into the lipid bilayer II. Physiological Type
o 2 phospholipid molecules a. Blood flow/Circulation
• There are drugs that are lipid soluble that i. Ex. Hypertensive drugs which
can pass rapidly to the membrane. Drugs is the captopril – taken in the
that pass rapidly to the membrane are sublingual. Must be cautious
called lipophilic type drugs. in giving this medication to
• Water soluble drugs – it requires or needs those that suffers
energy or enzymes and protein and uses It hypertensive crisis.
as a vehicle. (180/100)
• Non ionized drugs or particles – drugs that ii. temperature
can easily pass through the lining very b. Gastric emptying time and
rapidly. Intestinal motility
o Needs acidic environment for better i. Metabolic state of the body
absorptions like antifungal drugs c. pH level
o Ca CO5 - needs an acidic d. Area of absorption surface
environment for better absorptions. e. Microbial flora – tries to convert
o Give food to stimulate acid using enzymes for absorption of
production in the stomach. certain drugs.
• Some drugs need lesser acidic environment f. Drug concentration – increase in
like aspirin. concentrations of the drugs causes
• HCL Acid – can destroy certain drugs. increase in the absorption of the
o Ex. Penicillin, penicillin-based drugs drug.
o Remedy: Higher dose to upset the
Stomach vs. small intestine
partial losses.

Factors affecting absorptions


NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

o 3 to 5x a day
o Larger doses in comparison to IV
Absorption is better on the small intestine than the
doses
stomach.
o High hepatic first pass = high hepatic
Stomach Small Intestine toxicity
Total
1 m^2 200m^2
Absorption Factors affecting bioavailability
Blood flow 150 ml/min 1 liter/min
• Drug form (Capsule, tablet, etc.)
Permeability Low High • Route of administrations
• GI mucosa and motility
Factors affecting absorptions • Food and other drugs
• Liver metabolism
• Patient History is very important! o Once the liver is dysfunctional, the
III. Pathological Type haptic blood flow decreases.
IV. Pharmacological Type Drugs are primarily being metabolized by the liver.
a. Drug interaction
b. Effect of drug ↓
Hepatic first pass – stomach → intestinal lumen → Liver disease = less hepatic blood flow
portal vein → liver. In the liver, drugs can be ↓
metabolized into inactive form.
Decrease hepatic blood flow = less drug
• Warfarin Na metabolism
o Morphine – cannot be used when
there is an increase in intra-orbital ↓
pressure or intra-cranial pressure. Less drug metabolism = less conversion into
o NGT (Nasogastric Tubing) inactive from of drugs
Extensive 1st pass - Drugs that are not given orally ↓
• Lidocaine – not given orally, through Less conversion = higher bioavailability
patches

Bioavailability – a subcategory of absorptions. The
High bioavailability = high drug concentration
percent of the administered drug that reaches the
systemic circulations. ↓
• Oral route – bioavailability occurs after High drug concentration = high drug accumulation
absorption and the hepatic drug

metabolism
o Less than 100% -- 20% - 40% (hindi Drug toxicity → death
sya 100% available)
NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

Absorption
• Metabolism
↑ Rapid absorption of drugs = ↑ drug • Excretion
concentration
Factors affecting drug metabolism
↑ drug concentration = ↑ drug toxicity
↓ slow absorption = ↓ bioavailabilty • Age
↓ bioavailability = ↓ serum drug concentration • Genetic factors
• Change in metabolic rate
Slower absorption of drugs, higher drug dose by o Enzyme induction - facilitates
the doctor. o Enzyme inhibition – inhibits
• Most common dangerous drug that causes Factors affecting excretion
toxicity lever = digitalis drugs (digoxin (ex.
Lanoxin))
• Lanoxin – slows that heartbeat, is given OD • Renal functions
• Drug interactions
distribution o Nephrotoxic (bad to kidney)
o Renal blood flow
Distribution – is a reversible process between the o Change in pH
drug and the protein carrier.
Summary
• Bound and unbound form
Drugs can be distributed by: Drugs
• Receptor sites (produce effect) ↓
• Tissue depot (storage)
• Liver (metabolism) Absorption
• Kidney (excretions) ↓
Factors affecting distribution Distribution
Metabolic Receptor
site site
• Protein (CHON) bound/binding
• Circulations Plasma
• Capillary permeability Free drugs – Bound drugs

Elimination excretion Tissue


site depot

Elimination – irreversible loss of drug in the body.


NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

carbidopa and
levodopa for the
Paano magkaroon ng epekto ang
treatment of
gamot? Parkinson’s disease
and its syndrome.
For the drugs to have an effect, it needs a receptor 3. Interactions with DNA & RNA – Inhibits
site. DNA replications and functions
a. Folic acid Analog (In the form of
Drug + receptor = Intrinsic activity (Agonist)
methotrexate – which is a drug that
Drug + receptor = No intrinsic activity (Antagonist) inhibits ditropholic reductase)
b. Purine analogs – in the form of
• Idiosyncrasy – certain response to the
aguanine, that antagonize the
drugs which are unusual
purine synthesis.
• Tolerance – High dose is given for the drugs c. Pyrimidine analogs – 5FU which
to produce effect inhibits the pyrimidine synthesis.
Therapeutic Index – measurement of the drugs in Used in cancer drugs.
line with safety, including the loading dose - Free radical drugs – drugs that inhibit the
topoisomerase of your cells which are toxin
• Potency – it is the concurrent to produce to your cells. It damages your DNA and
effect. Is also related to the dose and destroys your RNA. (such as bleomycin –
concentration of the drugs. antibiotic for cancer)
• Efficacy – maximal response 4. Inhibition to CHON synthesis – inhibits
protein synthesis.
Mechanisms of Drug Action a. Tetracycline
b. chloramphenicol (for typhoid fever))
c. erythromycin
1. Interaction with the receptors – without
d. aminoglycoside
the receptors, the drugs will have no
5. Interaction with cell membrane
efficacy.
a. Digitalis glycoside – inhibit sodium
2. Interactions with an enzyme
and potassium pump
a. Induction
b. Local anesthesia – interferes with
b. Inhibition
the membrane permeability to
i. ACE (Angiotensin Converting
sodium and potassium in the form
Enzymes) inhibitors – inhibits
of lidocaine.
the
c. Omeprazole, lansoprazole, etc.
conversion of Angiotensin II
(proton pump ihibitors) – inhibits
which is the most powerful
HCL and potassium (H/K) pump in
vasoconstrictor.
the parietal cells in the stomach.
ii. Carbidopa – in a form of
i. Very active H/K pump is
Sinemet
prone to multiple gastric
1. Sinemet – is a
ulcers.
combination of drugs
NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

ii. Aspirin, steroid drugs are c. Phase 3 – “How well does it work?”
highly ulcerogenic “More positive or negative effect?”
medications causing gastric i. Ex. Doxycycline –
irritant. prophylactic drugs for
1. Always give proton leptospirosis which has
pump inhibitors in positive effects but more
giving it. negative effects in the body.
d. Phase 4 – Post marketing studies.
Net effect of the drug therapy Still studying its effects and develops
it on the safer side.

• The net effect of the drug therapy is the The information needed on the drugs
sum of the pharmacological effects of the
drug and the nonspecific placebo effect is
• Description of the drugs
associated with the therapeutic effort.
• Clinical pharmacology
• Placebo effect – effect of the drugs that is
o Indication and use of the drugs or
actually not in the drugs.
approved us (talaga bang para diyan
o Ex. You were given an antibiotic for
siya?)
your infection and fever, as a
o Contraindications – when not to use
placebo effect of the drugs, you
the drugs
think that your headache is also
▪ Teratogenic –
healed by the drugs (even though
contraindicated for pregnant
antibiotics weren’t for headaches)
woman
o Warning and precautions
Pharmacodynamic interactions o Dosage and administrations
o How is it being supplied (oral form,
• Addition 1+1 = 2 effects to the budy iv form, etc.)
▪ Ex. Anticoagulants durgs
• Synergism 1+1 = 3 or more effects in the
body • Warfarin – oral form
• Potentiation 0+1 = 2 or more effects in the • Heparin – iv form
body
Elements of rational drug use
• Antagonism 1 + 1 = 0 effects in the body

New drug activity • Safe


• Affordability
o Generic act law – make the drugs
1. Pre-clinical stage – studying the affordable and safe to use
compositions of the drug
• Needed
2. Clinical stage – testing stage
• Effectiveness
a. Phase 1 – “is the drug safe?”
• Quality
b. Phase 2 – “does the drug work?”
NRS 2109-7 Pharmacology
Prof. Glenn L. Rianzares

• Colloids – esteryl,
Role of the nurse albumin
• According to studies,
• Preparations (example: diluting the iv taking 4 colloids gets
drugs) the kidney
o Role: Ensure the exact dosing and compromised.
sterility of the drugs • Crystalloids – mas
• Administration mabilis sa katawan
o Is it intended for IM, SubQ, or maalis
others?
o Role: Must have a concrete • Knowledge – knowledge on pharmacology
knowledge on how to administer the
drugs and your responsibility while Legislations & Standards
administering the drugs
o Role: Read the drug insert • Federal
o Ex. LMWH – Low molecular weight • State
heparin in subq. Do not aspirate. • Policy and guidelines of health care
Aspirating will create hematoma constitutions
• Medication regulations and nursing practice
• Health teaching
o Ex. If taking steroids, it must be Dosage of your administration and
consumed after you eat and must be schedule
consumed with proton pump
inhibitors since steroids are very
highly gastric irritant. • ac – before meals
o There are medications you cannot • bid – twice a day
stop abruptly like anti-seizure drugs • HS – hours of sleep (At bedtime)
(status epilepticus).
• Qam – Every morning
• Evaluation
• prn - As needed
o Evaluate the effects of the
• RTC – round the clock
medication to the patient
• TID – three times a day
o Immediate and the long terms
• QID – four times a day
evaluations
• Stat - immediately
o Ex. A patient having a shock because
of blood loss, we give plasma
expanders to support the
circulation. In giving that, you need
to evaluate the effects to the patient
long term.
▪ In the form of esteryl:

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