GENERAL PHARMACOLOGY

S.WASIM RAJA, M.Pharm.,

What is Pharmacology?
Pharmacology is the science that deals with drugs
Pharmacology can be defined as the study of the effects of drugs on the function of living systems. Pharmacology is the study of chemicalsdrugson living tissues and how those chemicals help diagnose, treat, cure, and prevent disease or correct the pathophysiology of living tissues. The term pharmacology is derived from two Greek words: pharmakon (drugs), and logos (science)

Development of Pharmacology

Pharmacology today with its various sub divisions

WHAT IS A DRUG?
The word Drug is derived from the French word Drogue,

a dry herb
A drug is defined as any substance used for the purpose of diagnosis, prevention, relief or cure of a disease in man or animals.

Drugs Vs Medicines
Drugs may be synthetic chemicals, chemicals obtained from plants or animals, or products of genetic engineering. To count as a drug, the substance must be administered as such, rather than released by physiological mechanisms. Many substances, such as insulin or thyroxine, are endogenous hormones but are also drugs when they are administered intentionally A medicine is a chemical

preparation, which usually but

not necessarily contains one or more drugs, administered with the intention of producing a

therapeutic effect
Medicines usually contain other substances (excipients, stabilisers, solvents, etc.)

besides the active drug, to

make them more convenient to use

The Source of Drugs

The origins are from one of four sources

Plants
Animals Minerals Synthetic/Chemical Derivatives Microorganisms

Genetic engineering
Hybridoma techniques

PLANTS
A number of plants have medicinal qualities and have been

used for centuries as natural remedies for injuries and

illnesses. Pharmaceutical firms harvest these plants and transform

them into drugs that have a specific purity and strength

sufficient to treat diseases. An example of a drug that comes from a plant is digitalis.

Digitalis is made from leaves of the foxglove plant and is

used to treat CHF and cardiac arrhythmias. Digitalis also strengthens the force of the contractions of the heart.

ANIMALS
Byproducts of animals, including humans, are a source for drugs because they contain hormones that can be reclaimed and given to patients who need increased hormonal levels to maintain homeostasis.

For example, Premiering is a drug that contains estrogen that is recovered from mare urine. This is used as hormonal therapy to manage menopausal symptoms.

MINERALS
Our body requires trace elements of minerals in order to maintain homeostasis. Minerals are inorganic crystal substances that are found naturally on earth. Patients lacking an adequate level of these materials may take specific mineral-based drugs to raise the level of minerals. Liquid paraffin, Magnesium sulfate, Magnesium trisilicate and kaolin

SYNTHETIC/CHEMICAL DERIVATIVES
Great strides in molecular biology and biochemistry

enable scientists to create manmade drugs referred to as

synthetic drugs. A synthetic drug is produced using chemical synthesis,

which rearranges chemical derivatives to form a new

compound. Sulfonamides are a common group of synthesized drugs

that are used to treat many infections including

bronchitis, pneumonia, and meningitis. Sulfonamides are designed to prevent the growth of bacteria

MICROORGANISMS
Bacteria and Fungi isolated from soil are important sources of antibacterials and other medicines

e.g.. Penicillin , Lactobacillus

GENETIC ENGINEERING
DNA Recombinant technology in which products like Insulin, growth hormones are produced

HYBRIDOMA TECHNIQUE
Monoclonal antibodies are prepared by this technique.

Drugs Name
Each drug has three names. The chemical name The generic name that is considered the official

name for the drug, and

The brand name, which is used by the manufacturer

to market the drug.

General classifications of drugs

There are two general classifications of drugs: prescription and over-the counter drugs. Prescription drugs are also known as legend drugs

and must be prescribed by an authorized healthcare

provider. Over-the-counter drugs can be purchased with or without a prescription.

Three effects of Drugs

Drugs have three effects: these are the therapeutic effect to fight or prevent a disease; a side effect that isnt harmful; and an adverse effect that is harmful to a varying degree. Some drugs can also cause an allergic response in some patients. Healthcare providers must know about these effects before

administering the medication to the patient. Furthermore,

the patient must be informed of these effects.

Dosage forms
Definition: Dosage forms are the means by which drug molecules are delivered to sites of action within the body. Classification: Dosage forms are classified based on Route of administration and Physical form,
Based on Route of Administration Oral Topical Rectal Parenteral Vaginal Inhaled Ophthalmic Otic Nasal Implants Based on Physical form Solid Semisolid Liquid Gaseous

Oral Dosage Forms

Tablet Buccal and sublingual tablet Effervescent tablet Chewable tablet Capsule hard-shelled capsules soft-shelled capsules Lozenge Pastilles Dental Cones Pills Granules Powder (Oral) Bulk Powders Divided Powders Powders for mixtures

Oral Dosage Forms (cont..)

Liquid preparations

Oral solution
Oral emulsion Oral suspension Syrup Elixir Linctuses Oral drops

Gargles
Mouthwashes

Topical dosage forms

Ointments Creams Oil In Water (O/W) creams Water in Oil (W/O) creams Gels (Jellies) Poultice Pastes Dusting powders Transdermal patch Plasters Liniments Lotions Collodion The flexible type Non-flexible Paints Pressurized dispensers (aerosol sprays)

Rectal dosage forms

Suppository Rectal suppository Vaginal suppository or pessaries Enema Evacuant enema Retention enema

Vaginal dosage forms

Pessaries Molded pessaries Compressed pessaries Vaginal capsules Vaginal ring Douche Intrauterine device (IUDs) inert and copper-based devices. hormonally-based devices that work by releasing a progesterone.

Parenteral dosage forms

An injection Intravenous injection

Intramuscular injection
Subcutaneous injection Intradermal injection Intraperitoneal injection Intracardiac injection Intraarticular injection Intraosseous infusion Inhaled dosage forms Inhaler Nebulizer or (atomizer)

Parenteral dosage forms

Ophthalmic dosage forms

Eye drops
Ophthalmic ointment & gel Otic dosage forms

Ear drops
Nasal dosage forms Nasal Drops and Sprays Implants Novel Dosage Forms (Multiphase Multi compartment dosage form)

Oral Dosage Forms

Tablet Buccal Sublingual Effervescent Chewable Capsule Hard shelled Soft shelled Lozenge Pastilles Dental Cones Pills Granules Powder (Oral) Powder (Mixtures) Oral Solution Oral Emulsion Oral Suspension Syrup Elixir Linctuses Oral Drops Gargles Mouthwashes

Oral Dosage Forms

Tablet
A tablet is a hard, compressed medication in round, oval or square shape.

The excipients include: Binders, glidants (flow aids) and lubricants

to ensure efficient tabletting. Disintegrants to ensure that the tablet breaks up in the digestive tract. Sweeteners or flavors to mask the taste of bad-tasting active ingredients. Pigments to make uncoated tablets visually attractive. A coating may be applied to: hide the taste of the tablet's components.

make the tablet smoother and easier to swallow .

make it more resistant to the environment. extending its shelf life.

Tablet
Buccal and sublingual tablet: Sublingual and buccal medications are administered by placing them in the mouth, either under the tongue (sublingual) or between the gum and the cheek (buccal).
- The medications dissolve rapidly and are absorbed through the mucous membranes of the mouth, where they enter into the bloodstream. - Avoid the acid and enzymatic environment of the stomach and the drug metabolizing enzymes of the liver. - Examples of drugs administered by this route: e.g. vasodilators, steroidal hormones.

Administration of Buccal Tablets

Administration of Sublingual Tablets

Tablet
Effervescent tablet : Effervescent tablets are uncoated tablets that generally contain acid substances (citric and tartaric acids) and carbonates or bicarbonates and which react rapidly in the presence of water by releasing carbon dioxide. They are intended to be dissolved or dispersed in water before use providing:

A- Very rapid tablet dispersion and dissolution.

B- pleasant tasting carbonated drink.

Effervescent tablet

Tablet
Chewable tablet: They are tablets that chewed prior to

swallowing.
They are designed for administration to children e.g. vitamin products.

Chewable tablet

Capsule
A capsule is a medication in a gelatin container.

Advantage: mask the unpleasant taste of its contents.

The two main types of capsules are: hard-shelled capsules, which are normally used for dry, powdered ingredients, soft-shelled capsules, primarily used for oils and for active ingredients that are dissolved or suspended in oil.

Soft-shelled capsules Hard-shelled capsules

Lozenge
It is a solid preparation consisting of sugar and gum,

the latter giving strength and cohesiveness to the

lozenge and facilitating slow release of the medicament.

It is used to medicate the mouth and throat for the

slow administration of indigestion or cough remedies.

Lozenge

Pastilles
They are solid medicated preparations designed to dissolve slowly in the mouth. They are softer than lozenges and their bases are either glycerol and gelatin, or acacia and sugar

Pastilles

Dental Cones
A tablet form intended to be placed in the empty socket following a

tooth extraction, for preventing the local multiplication of pathogenic

bacteria associated with tooth extractions. The cones may contain an antibiotic or antiseptic

Dental Cone a resorbable collagen wound dressing used for local

haemostasis of capillary, parenchymatous and seeping haemorrhages during dental surgeries. Its cylindrical shape is highly adaptable, plugs the extraction site and controls bleeding. It is rapidly and completely absorbed by the body, while the collagen promotes granulation and epithelialization.

Dental Cones Other similar products available in markets Dental Sponge Dental Film Dental Tape

Pills
Pills are oral dosage forms which consist of spherical masses

prepared from one or more medicaments incorporated with inert

excipients. Pills are now rarely used

Granules
They are consisting of solid, dry aggregates of powder particles often supplied in single-dose sachets. Some granules are placed on the tongue and swallowed with water, others are intended to be dissolved in water before taking. Effervescent granules evolve carbon dioxide when added to water.

Granules

Powder (Oral)
There are two kinds of powder intended for internal use. Bulk Powders are multidose preparations consisting of solid, loose, dry particles of varying degrees of fineness. They contain one or more active ingredients, with or without excipients and, if necessary, coloring matter and flavoring substances. usually contain non-potent medicaments such as antacids since the patient measures a dose by volume using a 5ml medicine spoon. The powder is then usually dispersed in water or, in the case of effervescent powders, dissolved before taking. Divided Powders are single-dose presentations of powder ( for example, a small sachet) that are intended to be issued to the patient as such, to be taken in or with water

Powder (Oral)

Powders for mixtures

The mixed powders may be stored in dry form and mixture prepared

by the pharmacist when required for dispensing, by suspending the

powders in the appropriate vehicle

Liquid preparations
Oral solution:

Oral solutions are clear Liquid preparations for oral use containing one or more active ingredients dissolved in a suitable vehicle.
Oral emulsion: Oral emulsions are stabilized oil-in-water dispersions, either or both phases of which may contain dissolved solids. Oral suspension: Oral suspensions are Liquid preparations for oral use containing one or more active ingredients suspended in a suitable vehicle. Oral suspensions may show a sediment which is readily dispersed on shaking to give a uniform suspension which remains sufficiently stable to enable the correct dose to be delivered.

Liquid preparations
Syrup:

It is a concentrated aqueous solution of a sugar, usually sucrose.

Flavored syrups are a convenient form of masking disagreeable tastes. Elixir: It is pleasantly flavored clear liquid oral preparation of potent or nauseous drugs. The vehicle may contain a high proportion of ethanol or sucrose together with antimicrobial preservatives which confers the stability of the preparation.

Liquid preparations
Linctuses:

Linctuses are viscous, liquid oral preparations that are usually prescribed for the relief of cough.
They usually contain a high proportion of syrup and glycerol which have a demulcent effect on the membranes of the throat.

The dose volume is small (5ml) and, to prolong the demulcent action, they should be taken undiluted.
Oral drops: Oral drops are Liquid preparations for oral use that are intended to be administered in small volumes with the aid of a suitable measuring device. They may be solutions, suspensions or emulsions.

Liquid preparations
Gargles

They are aqueous solutions used in the prevention or treatment

of throat infections. Usually they are prepared in a concentrated solution with directions for the patient to dilute with warm water before use. Mouthwashes These are similar to gargles but are used for oral hygiene and to treat infections of the mouth

Oral solution Oral emulsion

Oral suspension

Syrup

Elixir

Linctuses

Oral drops

Gargles

Mouthwashes

Topical dosage forms

Ointments
Ointments are semi-solid, greasy preparations for application to the skin, rectum or nasal mucosa. The base is usually anhydrous and immiscible with skin secretions. Ointments may be used as emollients or to apply suspended or dissolved medicaments to the skin.

Creams
Creams are semi-solid emulsions, that is mixtures of oil and water. They are divided into two types: Oil In Water (O/W) creams: which are composed of small droplets of oil dispersed in a continuous aqueous phase. Oil-in-water creams are more comfortable and cosmetically acceptable as they are less greasy and more easily washed off using water. Water in Oil (W/O) creams: which are composed of small droplets of water dispersed in a continuous oily phase. Water-in-oil creams are more difficult to handle but many drugs which are incorporated into creams are hydrophobic and will be released more readily from a water-in-oil cream than an oil-in-water cream. Water-in-oil creams are also more moisturizing as they provide an oily barrier which reduces water loss from the stratum corneum, the outermost layer of the skin.

Gels (Jellies)
Gels are semisolid system in which a liquid phase is constrained

within a 3-D polymeric matrix (consisting of natural or synthetic gum)

having a high degree of physical or chemical cross-linking. They are used for medication, lubrication and some

miscellaneous applications like carrier for spermicidal agents to

be used intra vaginally

Poultice
It is soft, viscous, pasty preparation for external use.

They are applied to skin while they are hot. Poultice must retain
heat for a considerable time because they are intended to supply warmth to inflamed parts of body.

E.g. Kaolin poultice (B.P.C.)

Pastes
Pastes are basically ointments into which a high percentage of insoluble solid has been added The extraordinary amount of particulate matter stiffens the system. Pastes are less penetrating and less macerating and less heating than ointment.

Pastes make particularly good protective barrier when placed on the skin, the solid they contain can absorb and thereby neutralize certain noxious chemicals before they ever reach the skin.
Like ointments, paste forms an unbroken relatively water impermeable film unlike ointments the film is opaque and therefore can be used as an effective sun block accordingly.

 Pastes are less greasy because of the absorption of the

fluid hydrocarbon fraction to the particulates. There are two types of paste: a) Fatty pastes (e.g: leaser's paste) . b) Non greasy pastes (e g: - bassorin paste).

Dusting powders
These are free flowing very fine powders for external use.

Not for use on open wounds unless the powders are sterilized.

Transdermal patch
A transdermal patch or skin patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream.

An advantage of a transdermal drug delivery route over other

types such as oral, topical, etc is that it provides a controlled release of the medicament into the patient. The first commercially available patch was scopolamine for motion sickness.

Transdermal patch

Plasters
Plasters are solid or semisolid masses adhere to the skin when spread upon cotton felt line or muslin as a backing material and they are mainly used to, Afford protection and mechanical support. Furnish an occlusive and macerating action. Bring medication into close contact with the surface of the skin.

Liniments
Liniments are fluid, semi-fluid or, occasionally,

semi-solid preparations intended for application

to the skin. They may be alcoholic or oily solutions or emulsions. Most are massaged into the skin (e.g. counter-irritant). Liniments should not be applied to broken

skin.

Lotions
These are fluid preparations (aqueous) for external application without friction. They are either dabbed on the skin or applied on a suitable dressing and covered with a waterproof dressing to reduce evaporation.

Collodion
Collodion is a flammable, syrupy solution of pyroxylin (a.k.a. "nitrocellulose", "cellulose nitrate", "flash paper", and "gun cotton") in

ether and alcohol.

There are two basic types; flexible and non-flexible. The flexible type is often used as a surgical dressing or to hold dressings in place. When painted on the skin, collodion dries to form a flexible cellulose film. While it is initially colorless, it discolors over time. Non-flexible collodion is often used in theatrical make-up Compound Wart Remover consists of acetic acid and salicylic acid in an acetone collodion base used in Treatment of warts by keratolysis.

Collodion

The flexible type as a surgical dressing

Non-flexible collodion theatrical make-up

Compound Wart Remover

Paints
Paints are liquids for application to the skin or mucous membranes.

Skin paints contain volatile solvent that evaporates quickly to leave a

dry resinous film of medicament. Throat paints are more viscous due to a high content of glycerol, designed to prolong contact of the medicament with the affected site.

Pressurized dispensers (aerosol sprays)

Several different types of pharmaceutical product may be packaged in pressurized dispensers, known as aerosols. Surface sprays produce droplets of 100 um diameter or greater. May be used as surface disinfectants, wound or burn dressing, relieve irritation of bites. Spray-on dusting powders are also available from pressurized containers.

Surface sprays

Spray-on dusting powders

Rectal dosage forms

Suppository
It is a small solid medicated mass, usually cone-shaped ,that is

inserted either into the rectum (rectal suppository), vagina (vaginal

suppository or pessaries) where it melts at body temperature

Enema
An enema is the procedure of introducing liquids into the rectum and

colon via the anus.

Types of enema: Evacuant enema: used as a bowel stimulant to treat constipation. E.g. soft soap enema & Mgso4 enema The volume of evacuant enemas may reach up to 2 liters. They should be warmed to body temperature before administration. Retention enema: Their volume does not exceed 100 ml. No warming needed.

Enema (cont..)
May exert:

Local effect: e.g. a barium enema is used as

a contrast substance in the radiological imaging of the bowel. Systemic effect: the administration of substances into the bloodstream. This may be done in situations where it is impossible to deliver a medication by mouth, such as

antiemetics.
e.g. nutrient enema which contains carbohydrates, vitamins & minerals.

Vaginal dosage forms

Pessaries
Pessaries are solid medicated preparations designed for insertion into the vagina where they melt or dissolve.

There are three types:

Molded pessaries: they are cone shaped and prepared in a similar way to molded suppositories. Compressed pessaries: made in a variety of shapes and are prepared by compression in a similar manner to oral tablets. Vaginal capsules: are similar to soft gelatin oral Capsules differing only in size and shape.

Vaginal ring
Vaginal rings are 'doughnut-shaped' polymeric drug delivery devices designed to provide controlled release of drugs to the vagina over extended periods of time. Several vaginal ring products are currently available, including: Femring : a low-dose estradiol-acetate releasing ring, manufactured from silicone elastomer, for the relief of hot flashes and vaginal atrophy associated with menopause. NuvaRing : a low-dose contraceptive vaginal ring, releasing progesterone and estrogen.

Douche
A douche is a device used to introduce a stream of water into the

body for medical or hygienic reasons

Intrauterine device
It is a birth control device placed in the uterus, also known as an IUD or a coil. The IUD is the world's most widely used method of reversible birth control. The device has to be fitted inside or removed from the uterus by a doctor . It remains in place the entire time pregnancy is not desired. Depending on the type, a single IUD is approved for 5 to 10 years use.

There are two broad categories of intrauterine contraceptive devices:

inert and copper-based devices. hormonally-based devices that work by releasing a progesterone.

Copper-T

Copper-T (Mirena)

Copper- 7

Saf- T Coil

Lippes Loop

Copper-T (Multi Load)

Cu Safe

Dana - Super

Parenteral dosage forms

An injection
An injection is an infusion method of putting liquid into the body, usually with a hollow needle and a syringe which is pierced through

the skin to a sufficient depth for the material to be forced into the
body. There are several methods of injection, including

Intravenous injection
Intramuscular injection Subcutaneous injection Intradermal injection Intraperitoneal injection Intracardiac injection Intraarticular injection Intraosseous infusion

Intravenous injection
It is a liquid administered directly into the bloodstream via a vein.

It is advantageous when a rapid onset of action is needed.

Intramuscular injection
It is the injection of a substance directly into a muscle.

Many vaccines are administered intramuscularly.

Depending on the chemical properties of the drug, the medication may either be absorbed fairly quickly or more gradually. Intramuscular injections are often given in the deltoid, vastus lateralis, ventrogluteal and dorsogluteal muscles. Injection fibrosis is a complication that may occur if the injections are delivered with great frequency or with improper technique.

Site of injection for IM

Subcutaneous injection
Subcutaneous injections are given by injecting a fluid into the

subcutis, the layer of skin directly below the dermis and epidermis.
Subcutaneous injections are highly effective in administering vaccines and such medications as insulin.

Intradermal injection
Intradermal injections are given by injecting a fluid into the dermis,
the layer of skin between epidermis and subcutaneous region

Inhaled dosage forms

Inhaler
Inhalers are solutions, suspensions or emulsion of drugs in a mixture of inert propellants held under pressure in an aerosol dispenser. Release of a dose of the medicament in the form of droplets of 50 um diameter or less from the container through a spring-loaded valve incorporating a metering device. The patient then inhales the released drug through a mouthpiece. In some types, the valve is actuated by finger pressure, in other types the valve is actuated by the patient breathing in through the mouthpiece. It is commonly used to treat asthma and other respiratory problems.

Inhaled dosage forms

Nebulizer or (atomizer)
A nebulizer is a device used to administer medication to people in forms of a liquid mist to the airways. It is commonly used in treating asthma, and other respiratory diseases. It pumps air or oxygen through a liquid medicine to turn it into a vapor, which is then inhaled by the patient.

Inhaler

Nebulizer or (atomizer)

Ophthalmic dosage forms

Eye drops
Eye drops are saline-containing drops used as a vehicle to administer medication in the eye. Depending on the condition being treated, they may contain steroids, antihistamines or topical anesthetics. Eye drops sometimes do not have medications in them and are only lubricating and tear-replacing solutions.

Ophthalmic ointment & gel

These are sterile semi-solid preparations intended for application to the conjunctiva or eyelid margin.

Eye drops

Ophthalmic ointment & gel

Otic dosage forms

Ear drops

Ear drops are solutions, suspensions or emulsions of drugs that

are instilled into the ear with a dropper. It is used to treat or prevent ear infections, especially infections of the outer ear and ear canal.

Nasal dosage forms

Nasal Drops and Sprays
Drugs in solution may be instilled into the nose from a dropper or from a plastic squeeze bottle. The drug may have a local effect, e.g. antihistamine, decongestant. Alternatively the drug may be absorbed through

the nasal mucosa to exert a systemic effect.

The use of oily nasal drops should be avoided because of possible damage to the cilia of the nasal mucosa.

Implants
Controlled drug delivery for over a long time (months/years)

Principle
Reservoir (Osmotic/diffusion) systems Matrix systems Non-biodegradable Biodegrable polymeric materials with dispersed drug Advantages largely overcomes problems with individual compliance

Disadvantages
mini-surgery is needed, uneasy to simply discontinue the therapy, local reactions Examples: hormones/contraception

Etonogestrel (Contraceptive- implants)

Implants

Thank You

Note: The images shown in this presentation is only to make the viewers to understand about the nature of the dosage forms and doesnt endorse anything about its quality or brand. All images are downloaded from various websites