MT1 - Review - Important Concepts Flashcards
Pharmacology is derived from what two words?
What do they mean?
Pharmakon - magical substance, treatment or poison
logos - word, discourse, or bodies of knowledge
Provide the biological functioning classification of drugs.
1 - Drugs with selective toxicity (penicillin)
2 - Drugs used to replace inadequacies or naturally occuring substances (insulin)
3 - Drugs that change regulation (birth control)
4 - Drugs that alter mood or behaviour (alcohol)
Provide the clinical purpose classification of drugs.
1 - Curing illnesses (penicillin)
2 - Preventing diseases (vaccine)
3 - Improving health/quality of life (sleeping pills)
What are common routes of administration?
Oral ingestion, injection
What are the factors to consider when choosing a route of administration?
Molecular properties of the drug Physiological nature of the route Patient compliance Onset of action Condition being treated Systemic or local effect Metabolism
What are the different parenteral routes of administration?
IV - to vein
IM - to muscle
SC - to fat or CT
IO - to bone marrow
What are the other administration routes?
Sublingual, transdermal, rectal, topical, pulmonary
Dosage forms of enteral administration
Tablet, capsule, elixir, solution, syrup
Advantages of enteral administration
safest
most convenient
most economical
Disadvantages of enteral administration
Limited absorption for lipid soluble drugs
Certain drugs cause emesis (irritation)
Destruction of the drug due to low pH, food or other drugs
What is the dosage form of parenteral administration?
injections
Advantages of parenteral administration
Rapid, extensive and predictable
Effective dose can be delivered efficiently during emergency
Drug delivered in active form
Disadvantages of parenteral route
Pain
Asepsis must be maintained
Training required
Dosage form of sublingual
Orodisperable or orally disintegrating tablets
Transdermal dosage form
Cream, past, controlled-release patches
Rectal dosage form
Suppository
Pulmonary dosage form
Volatile liquids, aerosols, gases
Difference between topical and transdermal?
Topical - local - site of administration is the site of action
Transdermal - systemic - site of administration is not the site of action
Provide the route of administration and effective time in order of increasing time
IV, IO > endotracheal, inhalation > sublingual > IM > SC > rectal > ingestion > [transdermal] (Variable)
Factors affecting the strength of an acid
Any factor stabilizing the conjugate base will make a stronger acid:
- resonance and induction stabilization
- reduction of electron density on the atom
Factors affecting the strength of a base
Availability of lone pair electrons
Improving the formulation of a biological compound that dissolves poorly can be accomplished by?
- create/form a salt
- decrease particle size
- find and use a better solvent
What are the immiscible solvents used to determine the P-value?
What phases do they represent?
water - aqueous phase
n-octanol - organic phase
What is Lipinski’s rule of 5?
For all orally administered drugs: - No more than 5 hydrogen bond donors - No more than 10 hydrogen bond acceptors - MW less than 500 Da - log P less than 5 (no more than 7 rotatable bonds)
Isomers will differ from one another in what way?
Potency, duration, side effects/desirable effects
What are the different causes of non-compliance?
Frequency/time of administration multiple drugs age Patient conditions ease of administration
What routes/rates is pharmacokinetics concerned with?
Route of administration
Rate and extent of absorption
Rate of distribution (particularly to site of action)
Rate of elimination
Absorption is not needed for what route of administration?
IV
What are the different capillary types?
Continuous
Fenestrated
Discontinuous/sinusoid
Where are continuous capillaries located?
NS, Muscle, Fat
Where are continuous capillaries with many transport vesicles located?
Finger, gonad, skeletal muscle, skin
Where are continuous capillaries with few vesicles located?
CNS - part of the BBB
What is the route of administration for continuous capillaries with many transport vesicles?
IM, topical
What is the route of administration for continuous capillaries with few transport vesicles?
epidural lumbar injection
What is the location of fenestrated capillaries?
Intestinal villi, pancreas, endocrine gland, kidney glomeruli
What is the route of administration for fenestrated capillaries?
Enteral
What is the administration route for discontinuous capillaries?
intraosseus injection
What is the administration route for discontinuous capillaries?
intraosseus injection
What types of drugs use active transport?
Drugs that have similar structures to cellular metabolites
What types of drugs use ion-pair transport?
Drugs as organic anions or cations
What types of drugs use vesicle formations?
Hormone-related drugs
Compare passive and active transport
Passive
- No ATP hydrolysis
- Follows Fick’s Law
Active
- ATP hydrolysis
- Against concentration gradient
- Requires carrier/transporter
Factors affecting drug absorption
Drug properties: - pKa - P-value Other factors: - blood flow - surface area - contact time
Factors affecting enteral absorption
Presence of food, other drugs
Plasma protein binding
What are the excreting organs related to reabsorption?
Kidney, mammary gland, LI, gallbladder
What are the two factors of distribution?
Perfusion
Permeability
Describe interactions of drugs with plasma proteins
Reversible
intermolecular interactions
Surface
High capacity, low affinity
What are the factors that affect drug distribition
Human Body: - Blood perfusion - membrane permeability - Biomolecules Drug properties: - pKa - P-value -affinity for macromolecules/serum proteins
Drugs falling under pattern 1 of drug distribution are located where?
In the blood
Drugs falling under pattern 2 of drug distribution are located where?
Total body of water
Drugs falling under pattern 3 of drug distribution are located where?
Specific organs or tissues
Drugs falling under pattern 4 of drug distribution are located where?
Various organs
Describe type one drugs.
Large drugs - high MW
- highly charged
- high affinity for plasma proteins
Describe type two drugs
Small drugs with low MW
follow the distribution of water molecules
Describe type 3 drugs
Drugs with affinity for special proteins/biomolecules of a specific organs
Describe type 4 drugs
Combination of patterns 1 and 2
Most drug’s distribution pattern
Non-uniformly distribute through the body’s compartments
Describe the rule of 60:40:20
60% - Total body water 40% - intracellular fluid 20% - extracelluar fluid 16% - interstitial fluid 4% - plasma
The rate of distribution is determined by what factors?
Perfusion
permeability
The extent of distribution is determined by what factors?
pH-pKa
P-value
Plasma protein binding
intracellular binding