Advanced Pharmacology

Med Reconciliation
-Improves drug history by 45-95%
-Reduces adverse drug events (ADEs) by 80%

Side Effect
A predictable effect from a drug
-Example: hypotension with an antihypertensive drug

Adverse Drug Reaction
An allergic or idiosyncratic reaction to a drug
-Not a predictable effect/reaction

Dispensing drug samples
Don’t do this!
-There are specific rules about dispensing samples

DOAP
Descriptor
Objective
Assessment
Plan

Pharmacokinetics
What the body does to the drug
-Absorption
-Distribution
-Metabolism
-Excretion

Enteral Routes of Administration
Oral, sublingual, eterostomy, buccal

Parenteral Routes of Administration
Intravenous, subcutaneous, intramuscular, transdermal, intra-arterial, intra-articular, intradermal, intrathecal

Other Routes of Administration
Skin, ear, eye, nose, lungs, vagina, rectum

Bioavailability
The extent to which the administered drug becomes available in the general circulation

Rate of Absorption
How fast does the drug become bioavailable
AUC = Area under the curve

Extent of Absorption
How much of the administered drug actually makes it to systemic circulation

First Pass Effect
Removal of a substatial amount of an enterally administered drug dose prior to the drug reaching the systemic circulation
-Gastrointestinal
-Hepatic

Distribution
Movement of the active drug from blood stream to site(s) of effect
-Involves crossing cell membranes

Membrane Penetration
Requires lipid solubility (lipophilicity)

Transport Proteins
ATP-Binding Cassette Superfamily (ABC)
Solute-Carrier Superfamily (SLC)

ATP-Binding Cassette Superfamily (ABC)
Active transport

Solute-Carrier Superfamily (SLC)
Facilitated transport

Volume of Distribution (Vd)
The volume the drug would have to distribute into so the concentration of the drug is equal throughout the blood stream
-NOT an anatomic volume!!

Small Vd occurs when
1. Lipid solubility is low
2. High degree of plasma protein binding
3. Low level of tissue binding

High Vd occurs when
1. Lipid solubility is high
2. Low degree of plasma protein binding
3. High level of tissue binding

Metabolism
Phase 1
-Hydrolysis, reduction, oxidation (CYP)
Phase 2
-Conjucation (UGT)

Pro-drug
A parent drug that has no clinical effect
-Example: Codeine

Excretion
Most common routes of drug excretion include Renal and Billiary

Clearance
The volume of a compartment, per unit of time that is cleared of a drug due to elimination

Half-life (t1/2)
Time for drug content to decrease by 50%
t1/2 = (Vd (0.693))/Cl

Steady State
When the amount of drug going out is equal to the amount of drug going in
-Usually takes 4-5 half lifes to reach steady state

Pharmacodynamics
What the drug does to the body

Efficacy
How effective is the drug at producing the desired effect
-Holds more clinical significance than potency

Potency
How much of the drug is required (dose) to produce the desired effect

Therapeutic Effect
The intended effect of a medication
-May be direct or indirect

Toxic Effect
The unintended effect of a medication
-Side effect (more predictable) Vs. Adverse drug reaction (less predictable)

Mechanisms of Action
Receptors
Enzymes
Non-selective (doesn’t work through receptors or enzymes)

Receptor Types
Ligand-gated ion channels
G protein-coupled receptors
Enzyme-linked receptors
Intracellular receptors

Drug Affinity
How much is the drug attracted to the receptor
-Higher affinity, stronger attraction—>requires less drug (potency)

Intrinsic Activity
Degree of receptor activation following drug binding
-“How much does it tickle the receptor?”
-Higher intrinsic activity—>more effective (efficacy)

Agonist
Drug that activates receptor; mimics physiologic actions
-Good affinity and high intrinsic activity

Antagonist
Drug that blocks receptor and physiologic actions
-Good affinity but NO intrinsic activity

Partial Agonist
Mimic physiologic actions to a lesser degree
-Some affinity but only moderate intrinsic activity
-Also referred to as “agonist-antagonist”

Pharmacogenetics
Study of the genetic variability between individuals that determine differences in drug response

Allele
One of several alternative forms of a gene at a specific chromosomal location that controls an alternative expression of a protein product

Variant Alleles
Single nucleotide plymorphisms (SNPs)
-May cause a drug not to work at all, or to become toxic very quickly.

CYP2D6
Responsible for metabolism of ~ 100 drugs
-Metabolizes codeine
-Ethiopians and Saudi Arabians have a high rate of incidence of overactive CYP2D6

Azathioprine
Can cause severe bone marrow depression
-Should NEVER be administered in the United States without first conducting an FDA-licensed test!

VKORC1
Specific test available to determine the appropriate dose for Warfarin to be therapeutic

Pharmacotherapeutics
Implementing and evaluating the best therapeutic plan for the patient based on the assessment

Pharmacotherapy in the elderly
Goal is to promote successful aging by maintaining functional independence, preventing disability and iatrogenic disease, and increasing the health-related quality of life

Pharmacokinetics in the elderly
-Drugs that undergo renal elimination need to be adjusted for renal function
-Significance of changes in drug distribution depends on drug properties

Pharmacodynamics in the elderly
Increased pharmacologic effect of several drugs due to:
-Altered pharmacokinetics
-Altered receptor sensitivity

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Non-catalytic Receptors Ligand or drug reversibly binds the receptor and elicits an effect; the ligand remains unaltered by the non-catalytic receptor Catalytic Receptors Ligans or drug reversibly binds the receptor and elicits an effect; the ligand is altered by the …

EC50 the drug concentration giving 50% maximal effect (not binding affinity – the magnitude of a drug effect is not proportional to the proportion of receptors occupied by that drug) a drug with a lower EC50 is more potent (half …

What does it mean that DR interactions are concentration dependent? It means that as the concentration of the drug increases the % of receptors bound increases What does it mean the DR interactions are saturable? At a certain concentration 100% …

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systemic dose relationship has two components: Dose – Plasma concentration relationship -Determined by pharmacokinetics parameters of drug (half life, clearance, volume of distribution) Plasma Concentration – Response relationship -Can be studied using in vitro studies How to Determine a Dose- …

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