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Pharmacology
study of medicines
Pharmacotherapeutics
utilization of medicines to heal or manage patient care
Naturally sourced drugs (5)
1. aspriin (willow tree bark)
2. Penicillin (molds)
3. Digoxin (digitalis plant)
4. Taxol -> yew tree bark
5. morphine -> poppy milk
Canadian Pharmaceutical Association
publishes the CPS (Compendium of pharmaceuticals and specialties) + collaborates with health canada
Drug approval process (5)
1. Laboratory (testing on non-humans; 3-5 years)
2. CTA (clinical trials application to health canada) -> 3 phases
3. NDS (new drug submission) to health canada; 10% approval)
4. NOC (Notice of compliance) + DIN (Drug ID) assigned
5. Drug monitoring via MHDP (marketed health product directorate; monitor adverse cases)
Clinical trial phases (3)
phase I -> small sample (100 volunteers)
phase II -> up to 300 volunteers (with disease/ailment)
phase III -> up to 3000 (10% of drugs make it here)
Placebo (3)
substance "said" to have an effect, which may lead to an actual effect
2. not used as standard
3. not used as comparative subsances
categories of drugs (3)
1. drug/medication
2. biologic
3. natural health product NHP
drug/medication
chemical agent, synthetically produced
Biologic
from endogenous substance of animal cells
i.e. antibodies, blood products, hormones, etc.
Natural health product (NHP), examples and differentation (3)
from nature
i.e. vitamins, minerals, herbs, etc.
2. less regulated
3. effects vary
therapy
anything that benefits the patient
Generic drug name (2)
1. Describes drug without proprietary affiliation
2. 1 generic name per drug and same throughout the world
Brand/trade drug name (3)
1. From manufacturing company
2. Often the 1st drug to the market and patent protected for 20 years prior to other manufacturers.
3. Many trade names per one generic drug
Chemical drug name
name is chemical composition. Assigned by IUPAC
i.e. potassium chloride
If a drug has a generic name will it have a different chemical name
no, they will be the same
What are the brand and generic names for reactine
reactine -> brand name
Cetrizine hydrochloric acid -> generic
Brand vs Generic drug (3)
1. Cost:
- generic -> cheaper; covered by insurance companies
- brand -> expensive; sometimes no covered by insurance
- i.e. Tylenol vs acetaminophen
2. Prescribing -> may sub generic name if trade not available
3. Bioequivelence (amount of drug in circulation)
prototype drug (2)
1. single drug from drug class to serve as a reference drug within a particular class
2. Usually the original drug of the kind, and not necessarily the most utilized drug
Therapeutic drug class nomenclature and example
the name specifies a treatment/therapy of a particular disease/disorder; more broad
i.e. antihypertensive
Pharmacological drug class nomenclature and example
describes molecular/receptor activity; more specific, defines exact mechanism of action
i.e. calcium channel blocker
Schedule I (3)
1. prescription and dispensed by pharmacist
2. all prescription drugs and controlled drugs (potential for abuse)
3. Prescription can be granted to specific health care professionals
Schedule II (2)
1. only from a pharmacist, must be retained in an area with no public access
2. need to talk to a pharmacist but no prescription
Schedule III
open access in a pharmacy or pharmacy area
Unscheduled
sold in any store without professional supervision
examples of unscheduled drugs
advil, ibuprofen, tylenol
Pharmacotherapy in implementation
assessment -> alterations to physiology?
implementation -> enhance or suppress normal physiology
evaluation -> assessment of drug action
Pros of prescribed meds (4)
1. continous therpatutic level maintained
2. prevent complications, safer
3. predictable
4. long term
Cons of prescribed meds (2)
1. strict adherence to timing
2. less flexibility
Pros of unscheduled meds (3)
1. symptom specific
2. flexible dosing
3. patient centered control
Cons of unscheduled meds
risk of under or over use
Pharmocotherapeutics in pediatrics
measured by weight (per kilogram) until exceeds adult weight
What weight measurment should be sued for dose
Kgs
Prophylaxis
giving something before it happens
Example of prophylaxis
if drug causes nausea -> give patient something to treat nausea before it happens
What is serum synonymous with
blood and plasma
diligence in drug administration (3)
1. understand therapeutic goal
2. specific monitoring requirements
3. monitoring for effect and adverse effects
drug formulation
ingredients are prepared to be administered in a specific form (solid, liquid, injectable)
Drug route of administration definition and specification (2)
1. way the drug is taken into the body
2. specified by drug formulation.
Drug route of administration is dependent on what (3)
Dependent on medical situation
2. drug kinetics
3. formulation availability
4. setting
Oral (PO) what and what kind of effects (2)
1. mouth -> liquid (syrup, elixir); tablets/pills (chewable, gel); powder (mixed with food, drink)
2. leads to systemic effects
What is another name for Oral (PO) drugs
Classified as enteral (passes through GI tract)
Oral drug kinetics challenges (3)
1. Acidic environment
2. peristalsis depended
3. enters portal circulation (liver first).
What does it mean when a drug has to enter portal circulation first
1st pass metabolism
Why is PO not advisable (6)
1. GI obstruction
2. need for rapid drug action
3. Gi surgery
4. inability to swalow
5. malabosprtion disorders
6. stomach acid
Why is PO the hardest route (7)
1. must survive stomach acid and enzymes
2. first pass metabolism
3. absorption affected by food, pH, motility
4. slow onset
5. variable
6. GI effects
7. unpredictability
Sublingual (SL) (location, MOA, systemic?) (3)
1. under the tongue
2. capillary absorption into blood stream, bypassing GI system and 1st pass metabolism, faster than PO
3. systemic effect
Intranasal (insufflation) (location and MOA 2)
1. nasal cavity
2. capillary absorption, transport along cranial nerve network, BBB
is intranasal systemic or local? examples (4)
localized or systemic effects (based on drug)
- local (nasal mucosa) -> Rhinocort spray
- systemic effect -> flu vaccine
- CNS effect -> cocaine
Inhalation (location and MOA 2)
1. inhaled into lungs
2. pulmonary capillary network (rapid effects)
is inhalation systemic or local and examples (3)
localized or systemic effect (drug dependent)
- local -> asthma drugs
- systemic -> general anesthesia
Endotracheal (ET) (3)
1. lungs
2. ER/ICU situations
3. Tube inserted into an airway through the nose
endotracheal systemic localied? what kind of durg
1. systemic
2. few drugs only (i.e. epinephrine)
Topical (2)
1. applied directly to surface (creams, ointments)
2. many molecules too large to penetrate skin layers
topical prescence (local, systemic)
local effect
minimal systemic presence
how is molecule size expressed
- expressed in daltons (molecular weight)
What is the size range for a molecule to penetrate the capillary networj
500 daltons
caution with topical
systemic presence % can be contraindicated
Example of topical systemic and local
retinoid creams local effect -> collagen fiber repair and synthesis
systemic -> low but contraindicated in pregnancy
Transdermal definition, absorption, attributes and effect (4)
1. patch
2. dermal capillary absorption -> small enough molecules to penetrate skin layers
3. systemic effect desired
5. long acting -> slow and steady release and absorption
Example of transdermal (3)
1. nitroglycerine patch
2. nicotine patch
3. morphine patch
Rectal
1. inserted into rectum
Rectal drug effect (3)
1. local and systemic effect
2. 50-75% bypasses 1st pass metabolism
- systemic effect unreliable, many factors affecting it
Where are rectal drugs absorbed
intestine
rectal drug examples for each effect (2)
- local (glycerine suppository)
- systemic (morphine suppository)
Parenteral administration
not enteral, requires an injection
Intravenous (IV) location and attributes (3)
1. needle-catheter into a vein
2. immediate absorption, fast onset of action
3. dose given = dose circulating to receptors
Intravenous effect (1) and cons (2)
1. systemic effect, common in hospital settings
2. expensive
3. nfection risk
intramuscular (IM)
1. needle injection into muscle tissue
2. capillary bed absorption into bloodstream
Aqueous IM
faster effect
depot preperation of IM
slower effect
Intramuscular effect
systemic
Intramuscular injection sites (3)
1. deltoid site
2. ventrogluteal site
3. Rectus femoris
Subcutaneous (SC) (2) location and how is it absorbed
1. Injection into adipose tissue of hypodermis
2. absorption via capillary bed
Subcutaneous effect and example (2)
1. systemic efect -> faster or slower onset
2. i.e. insulin
recommended sites of subcutaneous (4)
1. abdomen
2. outer thighs
3. outer arms
4. above buttoks
Implanted ports considerations (4)
1. what type of port
2. A&P
3. which drugs can be administered
4. how to maintain potency
Pharmacokinetics (2)
1. movement across cell membranes via lipid bilayer
2. 4 phases: ADME
Factors of molecular kinetics (2)
1. Molecular characteristics
2. Membrane transport
Molecular characteristics (3)
1. charge (ionization)
2. lipophillicity vs hydrophilicity
3. size
Size affecting molecular characteristics
1. large is hard
2. small is easier
Membrane transport (2)
1. passive (not ATP) -> diffusion, osmosis, facilitated diffusion
2. active (ATP) -> electrolyte pumps (sodium, potassium)
ADME general rule (2)
1. lipophilic, non-ionized, small = easy absorption and distribution
2. hydrophilic, ionized = easy excretion
Absorption is
time for drug to reach systemic circulation
Factors affecting absorption (2)
- administration route
- molecular characteristics
Which route has a higher plasma concentration
IV route
Bioavailability
systemic circulation concentration
How to measure bioavailability
measurable via blood (plasma) tests (rarely: urine)
First pass metabolism (orally) (2)
1. less then 100% bioavailability
2. drug through lumen of GI tract -> liver (hepatic portal) -> metabolizes -> less effect
Some drugs that pass through gastric mucosa (5)
1. ETOH
2. Caffeine
3. ASA
4. Warfarin
5. Dilantin
What bioavailability do intravenous routes have
100% bioavailability
Drug dosage based of oral or not (2)
orally -> large dosage because first pass
others -> not enough produced
IV drug examples (6)
1. Nitroglycerine
2. Lidocaine
3. Midazaolam
4. Diazepam
5. Meperidine
6. THC
Therapeutic range and loading dose (4)
1. achieve peak plasma level quickly
2. repeated doses or higher 1st dose of drug given
3. regular recommended doses given after, to keep the drug 4. within therapeutic range, commonly IV, PO
recommended therapeutic dose symbol (2)
ED 50 -> median therapeutic dose
range is recommended
In pediatrics what metric should be used
kg
Avoiding toxic range or dose use what symbol
TD 50 -> median toxicity dose
therapeutic index calculation
TD50/ED50 or TD50:ED50
TD 50 is derived from
LD 50 lab data
Is a larger or smaller TI safer
larger because TD:ED shows difference and how many more times a dose has to be to become toxic