PCL201H1 Lecture Notes - Lecture 1: Timolol, Large Intestine, Reuptake

37 views36 pages
11 Jan 2018
School
Course

For unlimited access to Class Notes, a Class+ subscription is required.

Introduction
Digitalis
Foxglove plant
Digitoxin and Digoxin
Treat cardiac arrhythmias
Morphine
Opium Poppy
Analgesic
Precursor to semi and synthetic opiates
Salicin
Willow bark
Headache, pain, fever
Salicylic acid later purified (active metabolite)
19th century
Rudolf Buchheim: first professor of Pharmacology
Schwmiedeberg: founder of modern pharmacology
20th century
Langley and Ehrlich proposed receptor theory
Clark introduced model
Ach, oxytocin, histamine, penicillin, insulin, streptomycin all isolated
Insulin: Banting and Best, 1922, Toronto
1200 new drugs approved between 1950-2008
Industry
1000 prescription drugs marketed
4 billion prescriptions/year US
100$ billion in research, 643$ billion spent on drugs
Drugs
Chemical substance exerting biochemical or physiological effect
Defined by USE, change pathway of some sort
Natural (morphine)
Plants, animal sources (islet cells, fish venom)
Semi-synthetic (hydromorphone)
Chemically modify pure compounds, improve parameters
Paclitaxel (Taxol): Yew tree, used semi-synthetic production
Synthetic (fentanyl)
Most drugs
Reduce cost, improve design
Barbital, phenobarbital (sedatives)
Biologics
Antibodies, proteins, vaccines
Extracted from tissues or produced by DNA tech
Expensive, complex
Can be therapeutic or not
Toxin (botulinum toxin) or toxicant (fentanyl)
find more resources at oneclass.com
find more resources at oneclass.com
Unlock document

This preview shows pages 1-3 of the document.
Unlock all 36 pages and 3 million more documents.

Already have an account? Log in
High dose ascorbic acid for treatment (drug) vs. orange juice (not drug)
Insulin administered as replacement (drug) vs. insulin from own pancreas (not drug)
Regulated by TPD or FDA
Drug Names
Generations
Generic Name is generally used (acetominophen, ibuprofen)
Trade name is brand name (tylenol, advil)
First generic has 180 days market exclusivity!
find more resources at oneclass.com
find more resources at oneclass.com
Unlock document

This preview shows pages 1-3 of the document.
Unlock all 36 pages and 3 million more documents.

Already have an account? Log in
Pharmacokinetics
Determine time course for drug after administration
Linked to PD by plasma concentration
Pharmacodynamics
Interaction with target
Reversible via weak chemical bonds
Irreversible require new synthesis of target
Concentration range (saturable at high, no response at low)
Desired specificity, chemical specificity (twice dose in racemic mixture)
Can be inhibited
Response is relative to drug concentration, intrinsic activity and number of receptors
activated
Changes in signaling
Receptors participate in intracellular communication via chemical signals
Drugs are like ligands
Effectors are activated by signaling cascade
Adenylyl cyclase: increases cAMP
Physiological effect
Dose-response curve (acute response dissipates over time)
Saturates
Semi-logarithmic: expands conc. scale at low, compresses at high
Efficacy: ability to give effect
Emax: maximal response
EC50: drug conc. at 50% of max response (POTENCY)
ED *effective dose
Classification
Agonist
Mimic or enhance action of endogenous compound
Full
Binds at same site, full response
Salbutamol: mimics epinephrine at B2 activating GPCR
Partial
Pindolol: at B1, treat hypertension by blunting signalling
Positive Allosteric Modulator
Distinct site
Shift curve LEFT
Diazepam: PAM of GABA receptor that decreases neuronal activity
Antagonist
Pharmacological: Blocks ability of receptor-drug interaction by another ligand
Chemical: chelation, effect lost
Physiological: opposing effects
Zero efficacy on its own
Competitive
Binds same site
find more resources at oneclass.com
find more resources at oneclass.com
Unlock document

This preview shows pages 1-3 of the document.
Unlock all 36 pages and 3 million more documents.

Already have an account? Log in

Get access

Grade+
$10 USD/m
Billed $120 USD annually
Homework Help
Class Notes
Textbook Notes
40 Verified Answers
Study Guides
1 Booster Class
Class+
$8 USD/m
Billed $96 USD annually
Homework Help
Class Notes
Textbook Notes
30 Verified Answers
Study Guides
1 Booster Class