Basic Pharmacology

What is a drug?
- any chemical agent which effects any biological process
Drugsthese are chemical substances used or intended to be used to modify or explore the physiological condition or pathological state for the benefit of the recipient. Drugs may be used for prevention, diagnosis and treatment. PreventionBCG vaccine, Anti-malarial drugs for malarial prophylaxis. DiagnosisBarium meal for Peptic ulcer diagnosis. TreatmentAnti-biotic, Anti-TB drugs.

What is pharmacology ?
- the

study of how drugs effect biological systems

Introduction

A. Physical Nature of Drugs Solid drugs -> oral route aspirin or atropine Liquid drugs -> oral route, IM, SC nicotine or ethanol Gaseous drugs -> inhalation nitrous oxide, halothane, amylnitrite

Many drugs are weak acids or bases pH differences in the body may alter the degree of ionization of drug

What is Pharmacology ?
Pharmacokinetics
What the body does to drug

Pharmacodynamics
What the drug does to body

Pharmacology
Pharmacotherapeutics
The study of the use of drugs

Pharmacocognosy
Identifying crude materials as drugs

Toxicology

Pharmacokinetics
What the body does to the drug - Absorption - Distribution - Metabolism (Biotransformation) - Excretion
Half-life (t1/2)
- the time required for the plasma concentration of a drug to be reduced by 50

Pharmacodynamics
What the drug does to the body - Drug receptors - Effects of drug - Responses to drugs - Toxicity and adverse effects of drugs

Sources of Drugs
Pharmacocognosy

Animals Plants Minerals Synthetic Microbes

Many of these old sources are still in use today

Foxglove

plant

Digitalis

comes from the foxglove plant and is used in the treatment of CHF is the drug of choice for treatment of gout is used today to treat diabetes and is derived from the pancreas of beef or pork or may be synthetically produced as

Meadow

flower Colchicum autumnale or pork pancreas

Colchicine

Beef

Insulin

Drugs Derived from Plants

Ephedrine

is present in the leaves of a bushy shrub (species name Ephedra), which, when burned were used by the ancient Chinese to treat respiratory ailments. Today, it is a bronchodilator. Many estrogen hormone replacement therapy drugs are derived from yams. The belladonna plant source of atropine, which is still used to dilate the pupils.

DRUG CLASSIFICATION
- Based on the chemical structure

- Based on the main effect (e.g. analgesics).

- Based on the therapeutic use (e.g. antipsychotic). -Based on mechanism of action (e.g. serotonin agonist).

Drug Nomenclature

Chemical name - *Generic name - Trade name

Chemical Name: 2-(4-isobutylphenyl)-propionic acid

Generic Name: ibuprofen

Trade Names: Advil, Aches-N-Pain, Brufen,

Emodin, Haltran, Medipren, Midol 200, Motrin, Nuprin, Rufen, Trendar, Wal-Profen
*preclinical nomenclature =
company abbrev-123456 (e.g. WAY-100635, MK-869)

Routes of Administration

Critical to efficacy
Rapidity

of onset Duration of effects Magnitude of effects

Systemic administration
Drug

into circulatory system via ... Enteral routes Parenteral routes Drug effects throughout body ~

Routes of Drug Administration

Enteral
within

or by way of the GI tract

Oral (PO), rectal, sublingual

Parenteral
Not

within the alimentary canal

Inhalation, IM, SC, IP, topical

Central

Into the brain or spinal cord Intrathecal, ICV

Routes of Drug Administration

common abbreviations
PO = per os = oral IV = intravenous = into the vein

IM = intramuscular = into the muscle

SC = subcutaneous = between the skin and muscle IP = intraperitoneal = within the peritoneal cavity icv = intracerebroventricular = directly into the ventricle of the brain

Oral

Per Os (PO)

by mouth

absorption

across membrane in GI most common most variable 1st pass metabolism

Cooperation required Can recall ~

Oral

Sublingual
Absorption:

mucous membrane salivary glands

e.g.,

nitroglycerin, buprenorphine across lining of

Chewing
absorbed

mouth ~

Injection

Intravenous (iv)
directly

into vein rapid onset of effects

Fastest ~ Intramuscular (im)

Location important
Deltoid

- rapid Thigh - moderate Buttocks - slowest Difference in blood

supply & distance

Routes of Drug Administration and Absorption.

Injecting (Intravenous):
Puts

drugs directly into a vein Put drugs into muscles or under skin
Intravenous (IV) Intramuscular (IM) Subcutaneous 15 30 seconds 3 5 minutes 3 5 minutes
4

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Injection

Subcutaneous (sc)
under

skin slow, steady absorption

Disadvantages
Variable

absorption limited volume skin irritations ~

Injection

Intrathecal
under

sheath of nerve fibers, cord, or brain

spinal

Mostly as local anesthesia

little

importance for most psychoactive drugs

Inhalation
Smoking Lungs

gases

or vapors densely lined with capillaries large surface area

Fast absorption
Similar

to iv ~

Routes of Drug Administration and Absorption.

Inhaling:
Allows

the vaporized drug to enter the lungs, the heart and then the brain in about 7-10 seconds (Most rapid)

Inhaling: 7 to 10 seconds
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(Pictures) Marijuana inhaling tent used by the Scythians, c. 500 B.C. Man in India smokes ganja (marijuana) in a chillum pipe.
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Other routes

Transdermal patches
absorbed

by skin slow continuous release

also liposomes: via injection

Suppositories - rectal or vaginal

absorption

incomplete & unpredictable

Pellets - Norplant Microcatheter & pump ~

Routes of Drug Administration and Absorption Contact or Transdermal

Absorption Absorption through the skin is the slowest method of drug use. It often takes 12 days for effects to begin and the absorption can continue for about 7 days. Nicotine, fentanyl, and heart medications can also be absorbed this way Skin creams & ointments absorbed through skin

Contact or Transdermal: 1 to 2 days

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Toxicity
Toxicity is the ability of a chemical to damage an organ system, to disrupt a biochemical process, or to disturb an enzyme system.

Drug Formulation
Dosage = the amount of drug to be administered
usually based on weight Example: mg/kg

Concentration = how the drug is formulated

Example: mg/ml

Injection Volume = a liquid measurement

based on weight Example: ml/kg

Factors Affecting Response to Drugs

Dosage Route of Administration
IV IH subling IM, SC IP PO topical

Rate of Absorption

Rate of Elimination
Physiochemical properties of the drug

age, sex, species, metabolism, etc

Drug-Receptor Interactions

Agonists activates or enhances cellular activity. triggers a series of biochemical events alteration in function second messengers: biochemicals that initiate these changes

Antagonists do not initiate a change in cellular function. prevent the binding and the action of agonists blockers

Drug-Receptor Interactions
Factors Governing Drug Action

1. Affinity: measure of the tightness that a drug binds to the receptor 2. Intrinsic activity: measure of the ability of a drug to generate an effect, producing a change in cellular activity

Binding of a drug

drug must interact with complementary surfaces on the receptor.

Antagonist

exhibit affinity for the receptor do not have intrinsic activity at the receptor competitive antagonist: binds to the receptor in a reversible mass-action manner -agonists given in high concentrations can displace the antagonist from the receptor
-agonist can then produce its effect