DOSE

• Any amount of drug which modify cellular function of the body

• Types –

Therapeutic dose Minimal dose

Maximal dose Toxic dose

Lethal dose Fatal dose

Maintenance dose

Loading dose
 Dosage formulations

• It is the preparation of a drug for

administration into the body with the purpose
of diagnosis or treatment of a disease.

eg. Tablets, capsules, suppositories, syrups,

mixtures, aerosols
Therapeutic Index:
• It is a ratio of median lethal dose (LD50) or median toxic dose (TD50) and
median effective dose (ED50)

LD50 or TD50
TI =
ED50

• Median lethal dose –

It is the dose which produce lethal effect in 50% animal
• Median effective dose -
It is the dose which produce effective response in 50% animal
Importance of TI:

• Reflects the safety margin of a drug

• Evaluate therapeutic usefulness of a drug for an indication
• Describes the relationship between doses of a drug required to produce
desired and undesired effects. So predicts risk of toxicity
• More the TI more safer is the drug and vice versa
• For safer application of drug – TI must be >1
Drugs with high TI –
• Paracetamol
• Penicillin
• Atropine
• Diazepam

Drugs with low TI –

• Cardiac glycoside
• Warfarin
• Anesthetic agents
• Aminoglycosides
CALCULATION OF SAFETY MARGIN OF DRUG
• The gap between the therapeutic effects DRCs & the adverse
effects DRC defines the safety margin or the therapeutic index
of a drug.
• The therapeutic range is bounded by the dose which produces
minimal therapeutic effects & the dose which produces
maximal acceptable adverse effects.
The dose response curve (DRC) for different effects of a drug
may be different.

• The extent of separation of DRCs of a drug for different

effects is a measure of its selectivity eg: the DRCs for
bronchodilator & cardiac stimulation are quite similar in
case of isoprenaline but far apart in case of sulbutamal – So
sulbutamal is more selective drug.
Fig- Schematic diagram of the dose response relationship for the desired effects ( dose therapeutic response)& for
An an undesired adverse effects. The TI is the extent of displacement of 2 curves within the normal dose range.
 Fig – Log dose response curves of salbutamol for bronchodilatation (A) & cardiac stimulation (D) & Log dose response curves of isoprenal
-Ine for broncho dilatation (B) & cardiac stimulation (C)
 Terms related to drug receptor interaction
 AFFINITY: Tendency of a drug to combine with receptor to form a
complex and subsequently maintain it.

K1
D+R DR complex Response
K2

• Each drug have specific affinity constant for specific receptors

• Affinity may vary – insulin
• Example - Propranolol – B1= B2 receptor

Atenolol – B1 >>> B2

Salbutamol – B2 >>> B1
EFFICACY- Capacity
K1 of a drug to produce effect

K3
K2
D+R DR complex Response(K3 efficacy)

•Example – Amiloride - Low efficacy

Frusemide – High efficacy

Thiazide - Moderate efficacy

POTENCY- Quantity of a drug
required to achieve desired effect
or Potency is a comparative
measure refers to the different
doses of 2 drug that are needed to
produce desired effects.

• How to choose a drug ? - By

efficacy not by potency.
• Affinity :
Tendency of a drug to combine with receptor.

• Efficacy :
Capacity of a drug to produce effect. It depends on dissociation constant of a
drug.
• Potency :
Means biological activity per unit weight ( W / W). Potency are compared on
the basis of doses that produce same effects. Ex – chlorothiazide ( 1g ) & hydro
chlorothiazide ( 100 mg )- 10 times more potent.