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Pharmacology Graphs - A Complete Guide
Pharmacology uses several types of graphs to describe how drugs behave in the body and at receptors. The major categories are: dose-response graphs, receptor binding graphs, agonist/antagonist graphs, and quantal dose-response / therapeutic index graphs.
1. Graded Dose-Response Curve
This is the most fundamental pharmacology graph. It plots the magnitude of a drug's effect (y-axis) against increasing drug concentration or dose (x-axis).
Figure: Panel A = linear plot; Panel B = semilogarithmic (sigmoidal) plot. The EC50 marks 50% of maximal effect.
Key features read from this graph:
| Parameter | Definition | What the graph shows |
|---|
| EC50 | Concentration producing 50% of maximal effect | Point on x-axis at 50% response - lower EC50 = more potent |
| Emax | Maximum effect a drug can produce | The plateau of the curve - indicates efficacy |
| Potency | Amount needed to produce an effect | Drug A (red) is more potent than Drug B because its EC50 is smaller |
| Efficacy | Magnitude of maximal response | Both drugs reach the same Emax here, so they have equal efficacy |
Why semilogarithmic (log scale)? Because the range of doses spans several orders of magnitude, plotting log dose converts the hyperbolic curve into a convenient S-shaped (sigmoidal) curve, making EC50 easy to read off the graph. - Lippincott Illustrated Reviews: Pharmacology, p. 95-96
Clinical example: Candesartan (dose range 4-32 mg) vs. irbesartan (75-300 mg) are both angiotensin receptor blockers - candesartan is more potent because it requires a lower dose to achieve the same effect, but both have equal efficacy for treating hypertension.
2. Potency vs. Efficacy Graph
This graph compares drugs with different potency AND efficacy simultaneously:
- A drug can be more potent but less efficacious (curve shifted left but lower plateau)
- A drug can be less potent but more efficacious (curve shifted right but higher plateau)
- Efficacy is clinically more important - morphine's greater efficacy makes it useful for severe cancer pain, where naproxen's identical efficacy to ibuprofen (just different potency) makes them therapeutically equivalent for headache.
3. Agonist Types on Dose-Response Curves
This graph shows three types of agonist behavior: - Lippincott Illustrated Reviews: Pharmacology, p. 101-103
| Drug Type | Curve Shape | Emax | Intrinsic Activity |
|---|
| Full agonist | Rises to 100% | Same as endogenous ligand | = 1 |
| Partial agonist | Rises but plateaus below full agonist | Less than full agonist, even at 100% receptor occupancy | 0 to 1 |
| Inverse agonist | Curve goes downward | Falls below baseline | < 0 (negative) |
| Competitive antagonist | Shifts full agonist curve to the right (same Emax) | Unchanged | = 0 |
| Non-competitive antagonist | Lowers the Emax plateau without shifting EC50 | Decreased | = 0 |
Partial agonist as a dual agent: A partial agonist can act as both agonist (when no full agonist is present) AND antagonist (competing with a full agonist, reducing its Emax to the partial agonist's ceiling). Aripiprazole exploits this in schizophrenia - it inhibits overactive dopamine pathways while stimulating underactive ones.
4. Effect of Antagonists - Rightward Shift
A very important graph pattern to recognize:
- Competitive (reversible) antagonist - dose-response curve shifts right in parallel (same shape, same Emax, higher EC50). The effect can be overcome by increasing the agonist dose.
- Non-competitive (irreversible) antagonist - curve is compressed downward (Emax falls, EC50 unchanged or altered). Cannot be reversed by adding more agonist.
5. Quantal Dose-Response Curve and Therapeutic Index
Unlike graded curves (individual responses), quantal curves show what fraction of a population responds to a given dose.
Figure: Green curve = desired therapeutic response; Red curve = toxic/adverse response. Yellow zone = therapeutic window.
Key parameters:
| Parameter | Definition |
|---|
| ED50 | Dose effective in 50% of the population |
| TD50 | Dose causing toxicity in 50% of the population |
| LD50 | Lethal dose in 50% of the population (used in animal studies) |
| Therapeutic Index (TI) | TI = TD50 / ED50 - larger value = safer drug |
Reading the graph:
- Warfarin (Panel A): The therapeutic (green) and toxic (red) curves are close together, meaning the therapeutic window is narrow. A small dose increase above the effective range causes bleeding. This demands careful monitoring.
- Penicillin (Panel B): The toxic curve is far to the right of the therapeutic curve - a very wide therapeutic window. You can give high doses without reaching toxic levels in most patients.
Drugs with low TI (digoxin, warfarin, lithium, aminoglycosides, theophylline) require therapeutic drug monitoring. - Lippincott Illustrated Reviews: Pharmacology, p. 108-110
6. Drug Concentration-Time Graph (Pharmacokinetics)
This graph plots plasma drug concentration (y-axis) vs. time after administration (x-axis):
Plasma Peak (Cmax)
Concentration ___
| / \
| / \___
| / \___
|______/ \___
|__________________________|___ Time
Tmax Half-life decay
Key features:
- Cmax - peak plasma concentration
- Tmax - time to peak concentration
- Half-life (t½) - time for plasma concentration to fall by 50%
- Area Under the Curve (AUC) - total drug exposure over time; used to calculate bioavailability
- On a log scale, first-order elimination appears as a straight line (exponential decay becomes linear)
- On a linear scale, elimination appears as a curve
Repeated dosing graph shows drug accumulating toward a steady state (typically reached after 4-5 half-lives) and then oscillating between a peak and trough concentration.
Summary Table of Graph Types
| Graph | X-axis | Y-axis | What it tells you |
|---|
| Graded dose-response (linear) | Drug concentration | % maximal effect | Potency (EC50), Efficacy (Emax) |
| Graded dose-response (log) | Log drug concentration | % maximal effect | Sigmoidal shape; easy comparison |
| Receptor binding | Drug concentration | Fraction receptors bound | Affinity (Kd) |
| Agonist comparison | Log concentration | Receptor activity | Full vs partial vs inverse agonist |
| Quantal | Log dose | % population responding | ED50, TD50, Therapeutic Index |
| Plasma concentration-time | Time | Drug concentration | t½, Cmax, AUC, bioavailability |
Source: Lippincott Illustrated Reviews: Pharmacology, 8th ed., Chapter 2 (Pharmacodynamics), pp. 95-110; Goodman & Gilman's The Pharmacological Basis of Therapeutics, Chapter 3 (Dose-Response)