3 Principles of Drug Actions and Interactions

Pharmacodynamics and Pharmacokinetics

LEARNING OBJECTIVES
1. Identify five basic principle of drug action
2. Explain potential problems associated with absorption of medications
3. Apply appropriate nursing concepts and actions holistically and comprehensively.
4. Discuss the pharmacodynamics of specific drugs.
5. Explain the pharmacokinetics of given drugs.
6. Analyze the factors affecting responses to drugs.
7. Identify the meaning and significance to the nurse of the half-life when used in relation to drug
therapy.

Therapeutic Methods
• Drug therapy – treatment with drugs
• Diet therapy – treatment by diet, such as a low-salt diet for CVD patients or Kidney Failure
• Physiotherapy – treatment with natural physical forces such as water, light and heat.
• Psychological therapy – identification of stressors and methods to reduce or eliminate stress
and/or the use of drugs.

Effects of Drug
a. Local or Systemic
b. Desired or Adverse
C. Indications and Side effects

Nontherapeutic Drug Actions/Effects
a. Side Effects
b. Adverse Reactions
c. Toxic Effects
d. Drug Allergy
e. Idiosyncratic Reaction
f. Drug Tolerance

Toxic Effects of Drugs
a. Teratogenic
b. Idiosyncrasy
c. Paradoxical/Paradoximal
d. Tolerance
e. Dependency
f. Hypersensitivity

Pharmacologic Process - important factors in determining the response of a drug at its site of action

*Branches of Pharmacology
1. Pharmacokinetics: What Body does to Drugs?
1. Study the FATE of drugs once ingested and the variability of drug response in varying
patient population
2. The relationship between the dose of a drug and the drug’s concentration in biological
fluids
3. Includes (LADME) liberation, absorption, distribution, metabolism, and excretion of
drugs
2. Pharmacodynamics: What Drugs do to the Body?

1. Study the mechanisms by which Drugs act?
2. The relationship between

a. The concentration of drug at the site of action and

b. The biochemical and

c. Physiological effect

3. Pharmacotherapeutics: Use of drugs for prevention and cure of diseases
3. Clinical management of diseases

*Pharmacodynamics
1. Therapeutic Index and Drug Safety
2. Graded Dose Response
3. Potency and Efficacy
4. Cellular Receptors and Drug Action
5. Types of Drug Receptor Interactions

*Pharmacokinetics (LADME)
1. Liberation
2. Absorption
3. Distribution
4. Metabolism (Biotransformation)
5. Excretion

Factors Influencing Responses to Drugs (Factors that may alter Drug actions)
1. Client Factors Influencing Drug Action
2. Client’s age, sex , weight and diet
3. Renal and liver function
4. Genetic factors
5. Amount of body fat
6. Psychological state

Drug Preparations and Administration

*Choices of Routes of Drugs
 Drugs may be acidic, basic, or neutral and come in a variety of chemical forms such as small
organic molecules, large polymers such as proteins, carbohydrates and other compounds with
complex chemistries
 Physical and chemical properties of drug – solid/gas/liquid or solubility, pH etc.
 Site of desired action – localized or generalized
 Effect of digestive juices and first pass metabolism of drug
 Accuracy of dosage required
 Condition of the patient – unconscious, vomiting etc

A. Local Routes
Topical – External application of the drug to the surface for localized action, e.g. lotion,
ointment, cream, powder, paints, and spray etc.
Deeper tissues – Certain deep areas can be approached by syringe and needle, e.g. intra-articular,
intra-medullarly, intra-lesional injection, intrathecal and infiltration
Arterial supply – Closed intra arterial injection, e.g. angiography and anticancer drugs.

1. Enema
 Application of medicaments into rectum
 Two types:
 Evacuant enema: Mainly liquid form for local action e.g., soap water enema
 Quantity of fluid 600 ml
 Retention enema: Mainly solid form meant for systemic action e.g., prednisolone enema

B. Systemic Routes
a. Oral (enteral)
ADVANTAGES:
 Self medication possible – no assistance required
 Vast area of absorption
 Simplicity of procedure – no extra cost
 Slow in action and hence safe with some risky drugs
 Both solid and liquid dosage forms can be given

DISADVANTAGES:
 Onset of action is tardy
 Irritant and unpalatable drugs cannot be administered
 Absorption is irregular with some drugs e.g. aminoglycosdes
 May induce nausea and vomiting
 Not useful in presence of vomiting and diarrhoea
 Can be destroyed by gastric juice – penicillin G, insulin
 Cannot be used in unconscious and uncooperative patient.

1. Enteric coated: with acetate-pthalate, glutean and anionic polymers of methacrylic acid and
its esters.
 To prevent gastric irritation and alteration of drug in stomach.
 To achieve desired concentration of drug in small intestine
 To retard the absorption of drug

2. Controlled release (CR): Timsules/Spansules
 To provide uniform medication for prolonged period

b. Sublingual
 Kept under the tongue or crushed and spread over the buccal mucosa
Advantages:
 rapid absorption – action in 1 minute
 liver is bypassed – directly in systemic circulation
 can spit out the drug
 Unconscious patients

Disadvantages:
 Only lipid soluble drugs
 Uncooperative patients
 Irritation of mucosa
 Drugs: GTN (Glyceryl trinitrate), Buprenorphine (Nifedepine)

c. Rectal
 Irritant and unpleasant drugs as suppositories or retention enema
 Can be used in presence of vomiting and unconsciousness
 Absorbed by external hemorrhoid veins – bypasses liver
 Drugs – Diazepam, Indomethacin and Aminophylline etc.

d. Inhalation
 Very rapid absorption due to vast surface area of lungs
 General anesthetics – gases and liquids
 Pressurized metered dose aerosols - MDI
 Dry powder inhalation - Rotahalers

e. Nasal
 Absorbed by mucous membrane of the nose
 Hepatic first pass metabolism and gastric juices are bypassed
 (GnRH agonists like Leuprolide, dDAVP and calcitonin)

C. Parenteral (Par – beyond, enteral – intestine)
Advantages:
 Unconscious and uncooperative patient
 In presence of vomiting and diarrhea
 Irritant drugs
 By pass alimentary juice and 1st pass metabolism
 Rapid action and accuracy of dose

Disadvantages:
 Costly and painful
 Self medication is difficult
 Less safe and chance of infection
 Injury to nerves and arteries
 Risky
 Intradermal
 Subcutaneous
 Intramuscular
 Intravenous
 Intrathecal
 Intraperitoneal

a. Intradermal and Subcutaneous
 Intradermal: BCG and sensitivity Tests
 Subcutaneous: Non-irritant substances
 Small amount as less vascular
 Self injection is possible
 Avoid in shock
 Repository depot preparations
– aqueous suspensions
 Best example – Insulin
 Hypodermoclysis

b. Intramuscular
 Soluble substances, mild irritants, suspensions and colloids
 Sites of Injection – buttock, deltoid muscle
 No IM injection to child before walking

D. Intravenous route
Advantages
 Quick action – ideal for emergency
 Desired concentration can be obtained
 No hepatic first pass metabolism
 Can be used in unconscious and uncooperative patients

Disadvantages
 Costly – special apparatus required
 Thrombophlebitis and local irritation
 Self medication not possible
 Action cannot be halted
 Extravasation may cause severe irritation
 Aseptic and antiseptic measures to be maintained

E. Transcutaneous Routes
 Innunction: Nitroglycerin in angina pectoris
 Iontophoresis: Galvanic current is for penetration of drugs to deeper tissues – anode and
cathode iontophoresis e.g., salicylates
 Jet injection: Painless injection – high velocity jet produced through a microfine orifice
 Transdermal therapeutic system (Novel drug delivery): Examples – GTN, Nicotine and
Estrdiol
i. Scopolamine patch
 Implants: Biodegradable and non-biodegradable. Example - Norplants

F. Transcutaneous images Transdermal Inunction Dermojet
Special Drug Delivery System
 Ocusert: Pilocarpine, progestsert
 Prodrug: Examples
i. levodopa to dopamine
ii. Chloramphenicol palmitate
 Targeted delivery: Monoclonal antibodies
 Liposomes: daunorubicin, doxorubicin nd amphotericin B etc

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Pharmacodynamics and Pharmacokinetics

2. Pharmacodynamics: What Drugs do to the Body?

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