PHARMACOLOGY 1

FACULTY OF DENTISTRY 1
Pharmacology

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Pharmacokinetics

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A
D
M
E 3
Pharmacodynamics

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Introduction (Definitions and Sources of Drugs)

Pharmacokinetics

Pharmacodynamics
Course
Adverse Drug Effects Contents
Introduction to Autonomic Pharmacology

Cholinergic System, Cholinergic Agents

Anticholinergic Agents (Cholinergic Receptor Blockers)

Skeletal Muscle Relaxants

Adrenergic Agonists & Blockers

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Pharmacology is the science of drugs (Greek:
Pharmacon—drug; logos—discourse in).

it deals with the interaction of exogenously

administered chemical molecules (drugs )
with living systems.

In other words, any chemical substance that

can produce a biological response is a drug/
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• In the context of dental practice, a broad understanding of
pharmacology with emphasis on certain aspects is imperative
because:

✓ Dentists have to prescribe drugs, albeit from a limited range, for the
treatment of dental conditions.

✓Many dental patients concurrently suffer from other medical

conditions,
e.g., diabetes, hypertension, arthritis, etc.
for which they may be taking drugs that may have dental implications or
may interact with drugs prescribed by the dentist.

✓The dentist may have to deal with a medical emergency arising in the
dental office during a procedure.
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• For thousands of years most drugs were crude natural
products of unknown composition and limited efficacy.

• Over the past 150 years or so, drugs have been purified, and
chemically characterized and a vast variety of highly potent and
selective new drugs have been developed.

• The mechanism of action including the molecular target of

many drugs has been elucidated.

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The two main divisions
of pharmacology are:

Pharmacodynamics

Pharmacokinetics.
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 Pharmacodynamics

• Pharmacodynamics (Greek: dynamis—

power)—What the drug does to the body.
• This includes physiological and biochemical
effects of drugs and
• their mechanism of action at organ system/
subcellular/ macromolecular levels,
• e.g., Adrenaline

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 Pharmacokinetics

• Pharmacokinetics (Greek : Kinesis— movement) — What the body does to the drug.
• This refers to the movement of the drug in and alteration of the drug by the body; it
includes absorption, distribution, biotransformation, and excretion of the drug,

e.g., paracetamol :
• is rapidly absorbed orally attaining peak blood levels at 30- 60 min;
• 25% bound to plasma proteins, widely distributed in the body (volume of distribution ~
1 L/ kg);
• extensively metabolized in the liver, metabolites which are excreted in urine;
• has a plasma half-life (t½) of 2–3 hours and a clearance value of 5 ml/kg/min. 11
 Drug
• Drug (French: Drogue—a dry herb)
• It is the single active chemical entity present in medicine used for:
✓ Diagnosis,
✓Prevention,
✓ Treatment/cure of a disease.

• The WHO (1966) has given a more comprehensive definition—

“Drug is any substance or product that is used or is intended to be used to
modify or explore physiological systems or pathological states for the
benefit of the recipient.”
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Some other important aspect
Pharmacology :

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• Pharmacotherapeutics
• It is the application of pharmacological information and knowledge of the
disease for its prevention, modification, or cure.

✓Selection of the most appropriate drug,

✓Dosage,
✓Duration of treatment according to the specific features of a patient are a
part of pharmacotherapeutics

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Clinical pharmacology

• It is the scientific study of drugs (both new and old) in man.

• It includes pharmacodynamic and pharmacokinetic
investigation in healthy volunteers and inpatients;
• evaluation of efficacy and safety of drugs and comparative trials
with other treatment forms; surveillance of drug use patterns,
adverse effects, etc.

• Clinical pharmacology aims to generate data for the optimum

use of drugs and for the practice of medicine to be ‘evidence-
based’.

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 Chemotherapy

• It is the treatment of systemic infection/malignancy with specific drugs that have selective
toxicity for the infecting organism/malignant cell with no/ minimal effects on the host cells.

• Drugs, in general, can thus be divided into:

✓Pharmacodynamic agents
These are designed to have pharmacodynamic effects on the recipient

✓Chemotherapeutic agents
These are designed to inhibit/kill invading parasite malignant cells and have no/minimal
pharmacodynamic effects in the recipient.
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 Pharmacy
• It is the art and science of compounding and dispensing drugs or preparing suitable
dosage forms for administering drugs to man or animals.

• It includes:
✓ collection,
✓ identification,
✓ purification,
✓isolation,
✓synthesis,
✓standardization,
✓ quality control of medicinal substances.

• The large-scale manufacture of drugs is called Pharmaceutics. 17

 Toxicology

It is the study of the poisonous effect of drugs and other

chemicals (household, environmental pollutant, industrial,
agricultural, homicidal)
with emphasis on the detection, prevention, and treatment of
poisonings.

It also includes the study of adverse effects of drugs, since the

same substance can be a drug or a poison, depending on the
dose.

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Sources of Drugs

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• Drugs are obtained from a variety of sources:

1.Plants
Many plants contain biologically active substances and are the oldest source of
drugs.

• Chemically the active ingredients fall into several categories:

a. Alkaloids:
These are alkaline nitrogenous bases that have potent activity and are the most
important category of vegetable-origin drugs.
• Prominent examples are: morphine, atropine, ephedrine, nicotine,
ergotamine, reserpine, quinine, vincristine, etc.
They are mostly used as their water-soluble hydrochloride/ sulfate salts.

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 b. Glycosides:

• These compounds consist of a heterocyclic non-sugar moiety (aglycone)

linked to a sugar moiety through ether linkage.
• Cardiac glycosides (digoxin, ouabain) are the best-known glycosidic
drugs.
• Aminoglycosides (gentamicin, etc.) are antibiotics obtained from
microorganisms and have an amino-sugar in place of a sugar moiety

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c. Oils:
These are viscous, inflammable liquids, insoluble in
water.

• Fixed ( nonvolatile ) oils are calorie-yielding

triglycerides of higher fatty acids; mostly used for food
and as emollients,

e.g., groundnut oil, coconut oil, sesame oil, etc.

• Castor oil is a stimulant purgative.

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• Essential (volatile) oils,
mostly obtained from flowers or leaves are aromatic (fragrant) terpene
hydrocarbons that have no food value.

• They are used as:

➢ flavoring agents,
➢Carminatives
➢ counterirritants,
➢ astringents;

• examples are:
✓eucalyptus oil,
✓peppermint oil,
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• Clove oil is used to allay dental pain.

• Menthol, thymol, and camphor are volatile oils that

are solids at room temperature and are included in
mouthwashes, and toothpastes.
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• Mineral oils are not plant products but obtained from
petroleum; liquid paraffin is a lubricant laxative,
• and soft and hard paraffin are used as an emollient
and as ointment bases.
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 2. Animals
• Though animal parts have been used as a
cure since early times,
• it was an exploration of the activity of organ
extracts in the late 19th and early 20th century
that led to the introduction of animal products
into medicine,
• e.g., adrenaline, thyroxine, insulin, liver
extract (vit. B12).
• Antisera and a few vaccines are also
produced from animals.

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3. Microbes

Most antibiotics are obtained from fungi,

actinomycetes, and bacteria,

e.g., penicillin, gentamicin, tetracycline, erythromycin,

polymyxin B, and actinomycin D (anticancer).

Vaccines are produced using microbes.

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4. Minerals

• Few minerals, e.g.,

✓iron salts,
✓ calcium salts,
✓lithium carbonate,
✓ magnesium/aluminum hydroxide,
✓and iodine are used as medicinal
substances.

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5. Synthetic chemicals

• Synthetic chemistry made its debut in the 19th century and is now the
largest source of medicines.
• Not only diverse relatives of naturally obtained drugs
(atropine substitutes, adrenergic b2 agonists, synthetic
glucocorticoids/progestins/ cephalosporins)

have been introduced to achieve greater selectivity of action or even a novel

type of activity

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 Biotechnological products

• Several drugs, especially peptides and proteins are now

produced by recombinant DNA technology, e.g., human
growth hormone, human insulin, interferon, etc.

• Monoclonal antibodies, regulator peptides, erythropoietin,

and other growth factors are the newer drugs of
biotechnological origin.

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Dosage forms of
drugs

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• Dosage form is a product suitable for the administration of a drug to a
patient.

• Every active ingredient (drug) has to be formulated by adding

other substances:
✓ Excipients,
✓Diluents,
✓Preservatives,
✓Vehicles, )
• according to a specific recipe and packaged into a specific ‘dosage form
• ’ such as a tablet, elixir, ointment, injection vial, etc.
• which is then administered to the subject.

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The dosage form :

- Provides the body with the drug,

- Defines single doses,

- Protects the active ingredient(s),

- Makes it suitable for administration in various ways.

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Solid dosage forms

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1. Powders
The drug is in a dry and finely pulverized state.
• If the drug is for oral administration, each dose has to be
wrapped separately or packed in sachets; therefore, this
dosage form is inconvenient and unpopular except when the
quantity is several grams,
• e.g., oral rehydration salts.

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• Powders for topical application are supplied as bulk
powders.

• Effervescent powders contain granulated sod.

bicarbonate and citric or tartaric acid.
• They react when dissolved in water to liberate CO2
causing bubbling.

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2. Tablets
• The drug is powdered or granulated, mixed with binding agents, and
other excipients, and compressed/ molded into discoid, oblong, or
other shapes suitable for swallowing.
• The tablet may be:
✓ plain or
✓ sugar-coated/
✓film-coated/
✓enteric-coated, etc.

• Sustained-release tablets contain drug particles that are coated to

dissolve at different rates.
• In controlled-release tablets a semipermeable membrane controls
the release of the drug.
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3. Pills
• These are ancient dosage forms in which
the drug powder is mixed with honey/syrup
to make a sticky mass.

• This is then rolled into spherical/oval

bodies meant to be swallowed.
• The term is often loosely applied to tablets
as well.

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4. Capsules
• These are water-soluble cylindrical containers made of
gelatin which are filled with powdered or liquid medicament.
• The container dissolves on swallowing so that the drug is
released in the stomach.
• Enteric-coated capsules are designed to dissolve only on
reaching the ileum.

• Spansules are extended-release capsules that are packed

with granules of the drug having different coatings to dissolve
over a range of periods

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5. Lozenges

• These are tablet-like bodies of various shapes containing the drug along
with suitable gum, sweetening, and flavoring agents.

• They are to be retained in the mouth and allowed to dissolve slowly

providing the drug for local action in the mouth and throat.

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6. Suppositories
•These are conical bullet-shaped dosage forms
for insertion into the anal canal, in which the
drug is mixed with a modulable firm base that
melts at body temperature.
•Oval or suitably shaped bodies for vaginal
insertion are called ‘pessaries’, 43
Liquid dosage forms

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1. Aqueous solutions
They contain the drug dissolved in water; and may be meant for oral, topical,
or parenteral administration.

Oral drug solutions often contain sweetening and flavoring agents.

• Preservatives
• Have to be mostly added because the shelf-life of watery solutions is short.

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2. Suspensions are dispersion of insoluble drugs in water with the help of
a suspending agent.

• Emulsions are uniform mixtures of two immiscible liquids (mostly oil and
water) in which droplets of one (dispersed phase) are suspended in the
other (continuous phase) with the help of an amphiphilic emulsifying
agent.

• Milk is a naturally occurring emulsion.

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3. Elixirs are hydro-alcoholic solutions of drugs,
usually sweetened with syrup and flavored by fruit
extracts.

• Syrups have higher concentrations of sugar and are

thicker in consistency.

• Linctus is a viscous syrupy liquid meant to be licked

slowly to soothe the throat.
• It generally has menthol to impart a cooling
sensation and an antitussive.

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4. Drops
• These are relatively more concentrated solutions of
medicaments meant for oral ingestion or external
application to the eye, nose, or ear canal.

• Oral drops are the preferred dosage form for infants

and young children.

• Eye/nasal drops should be isotonic.

• Eye drops must also be sterilized.

• Drops are supplied in vials with a nozzle or along with a

dropper.

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5. Lotions
• These are solutions, suspensions, or emulsions meant for
external application to the skin without rubbing.

• They generally have soothing, protective, or emollient properties.

• Liniments are similar preparations that generally contain

counterirritants and are to be rubbed on the skin to relieve pain
and cause rubefaction.

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6. Injections
• These are sterile solutions or suspensions in the aqueous or oily medium
for subcutaneous or intramuscular administration,
• while only aqueous solutions (not suspensions) are suitable for
intravenous (i.v.) injection because particles in suspension and oils
injected i.v. can cause embolism.
• Injections are supplied in sealed glass ampoules or air-tight rubber-
capped vials.

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• Ampoules are broken just before injection and usually contain
a single dose.
Drug from the vial is sucked into a syringe by piercing the rubber
cap.

• Vials may be single or multi-dose.

Drugs that are unstable in solution are supplied as dry powder
vials.
Sterile solvent is injected in the vial just before it is to be
injected and the dissolved/suspended drug is then sucked out
into the syringe.

• Large volume i.v. infusions are marketed in

glass/polypropylene bottles. 51
Semisolid dosage
forms

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 1. Ointments

1. These are greasy semisolid preparations meant for external application to the skin,
eye, nasal mucosa, ear, or anal canal.
• The drug is incorporated in an oily base, such as soft or hard paraffin, wool fat, bee’s
wax, etc.

• Ointments are not suitable for oozing surfaces, because they do not allow evaporation
of water.
• Creams are like ointment, but the base is a water-in-oil emulsion

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2. Pastes
• These are nongreasy preparations of thick consistency containing hydrophilic
adhesive powders such as starch, prepared chalk, aluminum/magnesium hydroxide,
zinc oxide, carboxymethylcellulose, etc. which swell by absorbing water.

• Pastes may contain viscous nonoily liquids like glycerol or propylene glycol.
• Pastes can be applied to unbroken skin, oozing surfaces, and mucous membranes.
• Toothpaste is an item of personal hygiene, and medicated toothpaste is extensively
used in dentistry.

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3. Gels
• The medicament is incorporated in a viscous colloidal solution
of gelatin or similar material and is usually dispensed in
collapsible tubes.

• They are meant for external application to the skin or mucosa

and provide longer duration contact but are nongreasy and
washable with water.

• Gels are commonly applied to oral ulcers because they are better
retained than aqueous solutions.

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