The document discusses the relationship between drug dose and clinical response, known as the dose-response relationship. It notes that there are two components: the dose-plasma concentration relationship and the plasma concentration-response relationship. A typical curve showing the dose-response relationship is called a dose-response curve (DRC), which plots the intensity of response against increasing doses. The slope of the DRC provides information about a drug's potency, efficacy, and safety. A steep slope indicates a need for dose individualization while a flat slope means a standard dose can be given to most patients.
The document discusses the relationship between drug dose and clinical response, known as the dose-response relationship. It notes that there are two components: the dose-plasma concentration relationship and the plasma concentration-response relationship. A typical curve showing the dose-response relationship is called a dose-response curve (DRC), which plots the intensity of response against increasing doses. The slope of the DRC provides information about a drug's potency, efficacy, and safety. A steep slope indicates a need for dose individualization while a flat slope means a standard dose can be given to most patients.
The document discusses the relationship between drug dose and clinical response, known as the dose-response relationship. It notes that there are two components: the dose-plasma concentration relationship and the plasma concentration-response relationship. A typical curve showing the dose-response relationship is called a dose-response curve (DRC), which plots the intensity of response against increasing doses. The slope of the DRC provides information about a drug's potency, efficacy, and safety. A steep slope indicates a need for dose individualization while a flat slope means a standard dose can be given to most patients.
The document discusses the relationship between drug dose and clinical response, known as the dose-response relationship. It notes that there are two components: the dose-plasma concentration relationship and the plasma concentration-response relationship. A typical curve showing the dose-response relationship is called a dose-response curve (DRC), which plots the intensity of response against increasing doses. The slope of the DRC provides information about a drug's potency, efficacy, and safety. A steep slope indicates a need for dose individualization while a flat slope means a standard dose can be given to most patients.
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Relation Between
Drug Dose & Clinical Response Dose response curve ‘Dose’ is the amount of drug to administered to produce a certain degree of response in a patient. Dose–response relationship has two components: 1. Dose-plasma concentration relationship 2. Plasma concentration-response relationship
Response: The change in activity of the cell or tissue produce by the selected dose of the drug is called the response. o The dose and response is closely related to each other and this relationship is called as Dose response relationship. o There is direct relationship between dose intensity of response of the curve. i.e. the intensity of response increases with the increase in dose. A typical curve showing the dose response relationship is called dose response curve (DRC).
Fig. Dose response curve
Slope of Dose response curve (DRC)
Steep slope–moderate increase in dose
markedly increase the response (dose needs individualization)
Flat slope–little increase in response
occurs in wide range of doses (standard dose can be given to most patients)
Example: Hydralazine and
Hydrochlorothiazide DRC in Hypertension Dose-Effect Endpoints
Graded The graded dose-effect is measured on a continuous scale and
the intensity of the effect is proportional to the dose, such as measuring the change in blood pressure after administering an antihypertensive agent. Graded dose-effect relationships can be measured in a single biologic unit that is exposed to a range of doses. A graded dose-effect study relates the dose to the intensity of the effect.
Quantal Conversely a quantal effect is an all-or-none effect such as alive
or dead, asleep or awake, pain-free or in pain. Quantal dose- effect studies are performed in populations of subjects who are treated with a range of doses, and dose is related to the frequency of the all-or-none effect, such as the % of subjects who survived. Graded Dose-Effect Curve The DRC is useful to predict potency, efficacy & safety of drug.
1)Potency: The amount of drug required to produce a certain response.
Relative potency is more meaningful than absolute potency
Relative potency: comparing the dose of two agonists at which they elicit half maximal response (EC50) E.g: 10mg of Morphine is equivalent to 100mg of Pethidine to produce analgesia, hence morphine is 10 times more potent than Pethidine.
Potency for therapeutic effect should increase over the potency for adverse effects Potency of a drug is important to choose a dose Fig. log dose response curve for potency of drug A & B 2) Efficacy: Maximal response that can be elicited by the drug E.g: morphine produce analgesia not obtain with any dose of aspirin. Morphine is more efficacious than aspirin. Efficacy is an important factor in the choice of a drug Depending upon type of drug, both higher & lower efficacious drug is clinically prefered.
Fig. Log dose response curve for efficacy of drug A & B
3)Safety: The slop of the upper part of the curve is useful in assessing the relative safety of drug. eg. Most CNS depressants have steep slope which indicates a narrow margin of safety between the dose that produces sedation & the dose that produces coma. Dose individualization is required for use of such drug to avoid toxic effect. The drug with more shallow slope of curve produces little increase in response over a wide dose range & has greater margin of safety.
Fig. log dose response curve for safety of drug A & drug B Therapeutic Index: It is the ratio of the dose of drug that causes adverse effects at an incidence/severity not compatible with the targeted indication to the dose that leads to the desired pharmacological effect.
Therapeutic index is general index of the drug’s safety & some patients may display extreme sensitivity to certain drugs, eg. aspirin produces severe hypersensitivity reaction in some patient at the therapeutic doses.
Therapeutic window: It is the range of drug dosages which can treat disease effectively without having toxic effects. MTC = Minimum Toxic Concentration MEC = Minimum Effective concentration
Fig. Therapeutic Index & Therapeutic Window
Combined effects/response of drugs If two/more drugs given simultaneously, they may be either indifferent to each other or exhibit synergism/antagonism. Synergism: Action of one drug is facilitated or increased by the other • In a synergetic pair both drugs can have action in same direction or one may be inactive and enhancing the effect of other • Synergism is two types - Additive - Supraadditive/potentiation Additive: Effect of two drugs in same direction and simply adds up Effects of drugs A+B= effect of drug A+ effect of drug B Side effects do not add up Supraadditive: Effect of combination is greater than the individual effects.
Effects of drug A+B > effect of drug A+ effect of drug B
When one component given alone produces no effect, butenhances the effect of the other.
Antagonism: • One drug decreases or abolishes the action of the other Effects of A+B < effect of drug A+ effect of drug B • One drug is inactive and decreases the effect of the other. Three Types- 1. Physical 2. Chemical 3. Physiological antagonism 4. Receptor antagonism: Risk-benefit ratio
Judgment between estimated harm and the expected advantages.
• Estimated harms: o Adverse effects o Cost o Inconvenience
• Expected Benefits: Relief of symptoms Cure Reduction in complications/mortality Improvement in quality of life Thank you!!!!
