BIOM 3090 Study Guide - Winter 2018, Comprehensive Midterm Notes - Agonist, Cell Surface Receptor, Vasodilation
12 Oct 2018
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BIOM 3090
MIDTERM EXAM
STUDY GUIDE
Fall 2018
BIOM 3090 CLASS NOTES
Dispensing medicines: drug schedules
- drugs are categorized (scheduled) based on
o safety concerns
o abuse potentials: drugs with recreational value have increased
potential
o ability of a lay person to understand and execute directions for their
use
- scheduling of drugs/products dictates
o how drug is ordered/prescribed by physician for dispensing from a
pharmacy
o how the drug is obtained by the patient
o schedules may be found at the Natural association of Pharmacy
Regulatory authorities
- Drug schedules
o NAPRA I: prescription needed for sale by Pharmacist; includes
prescription drugs (Pr), narcotics (N) (ex. morphine), controlled
substances (C1, C2, C3) and targeted substances (TS) (ex. Xanax,
steroids)
o NAPRA II: prescription not required; however must be dispensed by
the pharmacist behind the counter: Ex. For insulin you don’t need a
prescription but you have the ask the pharmacist for it and they will
decide whether to give it to you or not
o NAPRA III: client may obtain at the pharmacy without the need of the
pharmacist; all the drugs behind the shelf
o Unscheduled: client may obtain at retail stores as well as pharmacy:
Advil, Tylenol
Nature of drugs
- a drug (aka ligand) is any substance that brings about a change in biological
function through its chemical actions
o the actions of drugs on the body is termed PHARMACODYNAMICS
o the actions of the body on drugs is termed PHARMACOKINETICS
- useful drugs must have properties enabling transport from the site of
administration to the target site (aka biophase)
- useful drugs should be inactivated and excreted from the body at a
reasonable rate to avoid duration of action concerns
- at room temperature..
o most drugs are solids (ex. aspirin): even powdered drugs that cane be
mixed with a liquid and ingested are also solid drugs
o some are liquids ex. ethanol, nicotine, inhalant anaesthetics
o few are gases ex. nitrous oxide
Drug receptor interactions: Overview
find more resources at oneclass.com
find more resources at oneclass.com
- most drugs are small organic molecules that produce effects by
interacting with macromolecular components of the organism called
receptors
- proteins represent the most important type of receptor for drugs
o some are hormones (ex. insulin, growth factors, neurotransmitters)
o enzymes for metabolic pathways
o transporters (ex. Na+, K + ATPase)
o structural proteins (ex. tubulin and nucleic acids)
- most drugs exert their effects by binding to regulatory proteins in the plasma
membrane of cells.. i.e. physiological receptors
o physiological receptors normally respond to endogenous regulatory
ligands
- the receptor, its cellular target and any intermediary molecules are referred
to as the signal transduction pathway
- there are some drugs that DO NOT act as receptors
o antacids directly neutralize HCl in stomach
o osmotic diuretics ex. mannitol promote increased urine formation by
osmotic forces in the lumen of renal tubules (in kidney)
- how can metoprolol act selectively on adrenergic beta-1 receptors?
o ANS: because of the structure and chemical properties of the drug and
receptor
o drug = metoprolol and receptor = beta-1 receptor
o drugs that are highly selective are always the best
o adrenergic beta-1 receptor I also found on the myocardium of heart
and increases the force of contraction
- most drug receptors are proteins
o proteins consist of a sequence of aa’s determined by DNA code:
primary structure
o proteins aa’s begin to interact with nearby aa’s on the same protein:
secondary structure
▪ hydrogen bonds mainly
▪ -helix, - barrel and -pleated sheets
o tertiary structure: results from interactions of more distant aa’s
along the protein molecule
▪ hydrogen, ionic and covalent (disulphide) bonds
o quaternary structure: multiple polypeptides can interact to form
more complex structures
- the receptor binding site has unique properties enabling the drug, with its
unique properties to interact and bind
o favourability of a drug-receptor binding interaction is called affinity
- in order for drugs to interact selectively with receptor binding sites, they
need to posses adequate shape and atomic composition, charge and size
o Size (100-1000 MW)
▪ Lower limit (100 MW): minimum size needed to impart
specificity of action and allow binding to select receptors
find more resources at oneclass.com
find more resources at oneclass.com
Document Summary
Drug schedules: napra i: prescription needed for sale by pharmacist; includes prescription drugs (pr), narcotics (n) (ex. morphine), controlled substances (c1, c2, c3) and targeted substances (ts) (ex. Xanax, steroids: napra ii: prescription not required; however must be dispensed by the pharmacist behind the counter: ex. Useful drugs must have properties enabling transport from the site of administration to the target site (aka biophase) Useful drugs should be inactivated and excreted from the body at a reasonable rate to avoid duration of action concerns. Most drugs are small organic molecules that produce effects by interacting with macromolecular components of the organism called receptors. Proteins represent the most important type of receptor for drugs: some are hormones (ex. insulin, growth factors, neurotransmitters, enzymes for metabolic pathways, transporters (ex. Na+, k + atpase: structural proteins (ex. tubulin and nucleic acids) Intermolecular interactions: sum total of forces imparts high affinity of the drug for receptor.
