Beruflich Dokumente
Kultur Dokumente
DEPARTMENT OF PHARMACOLOGY
Modern drugs, available for use today, are obtained from many sources:
50% of total prescriptions are composed of synthetic or semisynthetic (based
on natural active ingredients) chemical agents
25% contain higher plant principles
12% are microbial-derived products
7% are mineral in character
6% are animal-derived
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1. Higher plants
Plants are biosynthetic laboratory for a multitude of chemical compounds:
glycosides, alkaloids, steroids. The active ingredients might be found in any
part (or all parts) of the plant: leaves, root, bark, seeds, fruits, flowers, etc.
2. Microorganisms
Microbial metabolites used as drugs, especially the antibiotics and
antineoplastic agents are produced by fermentation.
a strain of mold Penicillium chrysogenicum produces Penicillin G
Clavulanic acid is a product of fungus Streptomyces clavuligerus
Microorganism from sea water, identified as Cefalosporium
acremonium, gives material for the production of semisynthetic
cephalosporins
Streptomycine was isolated from a strain of Streptomyces griseus
Gentamicin is produced by Micromonospora purpurea, an
actinomycete
3. Minerals
Precipitated sulfur is a very fine powder for external use, acting as
parasiticide, which is used in the treatment of skin disorders
Purified sulfur is used internally only, as a laxative
Talc powder is an absorbent, etc.
4. Animals
Animal organs, tissues, fluids and other animal derivatives can be used to
obtain active ingredients:
Beef and pork pancreas are the source of the natural insulin sold
today
Exogenous thyroxine can be obtained from the thyroid glands of
animals, usually pigs
Most commercial preparations of Corticotrophin are obtained from
either hog or sheep pituitary glands
Vesicular extracts from sheep and bulls are used to yield
prostaglandins
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Plant Species Popular Crude Active ingredients Pharmacological action Drug
name Drug
Atropa Deadly roots alkaloids: atropine, anticholinergic: antispasmodic,antisecretory, Atropine
Belladonna night shade Radix Belladonnae hyosciamine, hyoscine mydriatic, CNS-activity Scopolamine
(scopolamine)
Datura Jimson weed, leaves alkaloids: atropine, anticholinergic: antispasmodic,antisecretory, Asthma cigarettes
stramonium thorn apple Folium Stramonii hyosciamine, hyoscine mydriatic, CNS-activity
(scopolamine)
Hyosciamus alkaloids: atropine, anticholinergic: antispasmodic, antisecretory, Asthma cigarettes
Niger Henbane leaves hyosciamine, hyoscine mydriatic,CNS-activity
Folium Hyosciami (scopolamine)
Papaverum opium – dried centrally acting analgesics, Morphine
somniferrum Opium poppy exudate of the incised alkaloids: morphine, codeine, antitussives, Codeine Papaverine
seed capsule papaverine smooth muscle relaxant (papaverine)
Digitalis Foxglove leaves cardiac glycosides cardiotonics Digitoxin
Purpurea Folium Digitalis
Digitalis Grecian leaves cardiac glycosides cardiotonics Digitoxin
Lanata Foxglove Folium Digitalis Digoxin
Strophanthus seeds Strophanthin G and K
Gratus et Kombe Semen Strophanthi cardiac glycosides cardiotonics
the overground part
Adonis Pheasant’s eye Herba Adonidis cardiac glycosides mild cardiotonics Adinorm
Vernalis vernalis sedatives
Rauwolfia Chandrika, roots alkaloids: reserpine hypotensive, antipsychotic Reserpine
serpentine Patalagandhi Radix Rauwolfiae
Valeriana roots end rhizome volatile oil, valerenic acid and
officinalis Radix et rhizoma valepotriates sedatives Valeriana
Valerianae
Cinchona bark alkaloids: quinidine, antiarrhythmic, antimalarial, antipyretic Quinine
Cortex Chinae quinine, cinchonine Quinidine
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GALENIC PREPARATIONS (PHYTOMEDICINALS)
The term “Galenic preparations” is related to classes of natural drug products
obtained from plants by using simplified pharmaceutical procedures. Such
preparations (known as tinctures, extracts, syrups, spirits, aromatic
waters, etc.) popularly have been called galenicals, after Galen, the 2 nd
century Greek physician. They are relatively impure products intended only for
oral or external use, which consist of active ingredients in the same proportion
as they are in the crude drug.
III. Syrups (Sirupus, -i, -i) – syrups are concentrated solutions of sugar in
water. Types:
1. Simple syrups – contain sugar and water
1. Medicated syrups – contain some added medicinal substances
1. Flavored syrup contains aromatic substances or concentrated fruit
juices (raspberry, cherry, strawberry). Simple and flavored syrups are
useful for preparing liquid oral dosage forms (as Remedium corrigens).
Examples: Sirupus Codeini (antitussiva), Sirupus Rubi idaei (cherry syrup)
POWDERS
Historically, powders represent one of the oldest dosage forms.
They posses some advantages: flexibility in compounding and
relatively good chemical stability. The main disadvantages are their
unsuitability for dispensing unpleasant tasting or hygroscopic drugs
and inaccuracy of dose (for bulk powders).
Classification of powders:
1. According to the division into prescribed doses:
bulk powders (Pulveres nondivisi) – all doses are given
inseparably (as a bulk). They may be classified as:
oral powders – e.g., antacid and laxative powders
dentifrices
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dusting powders – locally applied nontoxic preparations.
Commercial dusting powders are available in sifter-top
containers and pressure aerosols.
insufflations – finely divided powders introduced into body
cavities (ears, nose, throat) with a powder blower (insufflator).
Specialized equipment has been developed for the
administration of micronized powders of relatively potent drugs
(e.g., pressure aerosols)
divided powders (Pulveres divisi) are divided into the
prescribed number of doses and are given orally. Each individual
dose (0.1–1.0 g) should be transferred to a powder paper.
2. According to the composition:
simplex powders (Pulveres simpliciti) consist of one active
ingredient and suitable inert substances (constituents)
complex powders (Pulveres compositti) are mixtures of more
than one active ingredient and constituents.
TABLETS
Tablets (tabuletta, -ae) are solid dosage forms containing drug substance
with or without suitable diluents, and prepared by compression. This is the
most frequently used dosage form of administering a drug. They are
swallowed, chewed, or held sublingually. Scoring of some tablets into halves
or quadrants facilitates breaking them if a smaller dose is needed. A tablet’s
color or shape can help identify it. Advantages: simplicity and economy,
stability and convenience in packaging, accuracy of dosage, compactness,
portability, and ease of administration.
PILLS
Pills (pilula, -ae) are small, round dosage forms for oral administration which
are prepared by the pharmacist. They are rarely prescribed today. The
powdered ingredients are mixed together with binding agents and solid
extracts (excipiens, -entis) and made into a plastic mass (massa pilularum).
The pill mass is rolled into spheres and coated with talc, gelatin, or sugar.
TROCHES
Troches (lozenges or pastilles) are discoid-shaped oral forms containing a
drug substance in a flavored base. They are placed in the mouth where they
slowly dissolve, liberating the active ingredient. The drug involved can be
antiseptic, local anesthetic, antibiotic, antitussive, or decongestant.
GRANULES
Granules (granulae) are dosage forms related to powders. They are
particularly suitable for the preparation of solutions or mixtures of drugs, such
as antibiotics, that are unstable in the presence of water.
Effervescent granules contain sodium bicarbonate and citric acid or tartaric
acid in addition to the active ingredients. On solution in water, carbon dioxide
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is released. These forms mask the unpleasant taste and ensure better
absorption of the medications.
PRESCRIPTION WRITING
SOLUTIONS
Solutions (solutio, -onis, -ones) are homogeneous mixtures that are
prepared by dissolving a solid, liquid, or gas in another liquid. The molecules
of the dissolved substance are dispersed among those of the solvent. Many
pharmaceuticals are simply solutions of a medicament in water, alcohol, ether,
glycerin, oils, or some other solvent. Various aromatic waters (e.g., chloroform
or peppermint water) may also be used as solvents. Solutions are intended for
internal, external, and parenteral administration.
1. Aqueous solutions include those pharmaceutical forms that are prepared
with purified water (aqua destillata – deionized, demineralized water) or
aromatic water as a solvent. Simple solutions for oral administration, douches,
enemas, gargles, mouthwashes, nasal and otic solutions are assigned to this
category.
2. Nonaqueous solutions are the alcoholic and hydroalcoholic solutions,
ethereal solutions, glycerin solutions, etc.
Solutions may be prepared in bulk or as single-use packages, and they are
usually bottled automatically (few of them can be prepared extemporally).
EMULSIONS
Emulsions (emulsio, -onis, -ones) are two-phase systems in which one
liquid is dispersed throughout another liquid in the form of small droplets. They
are classified as:
oil-in-water (O/W) emulsion – oil is the dispersed phase and an aqueous
solution is the continuous phase
water-in-oil (W/O) emulsion – an aqueous solution is the dispersed phase
and oil is the continuous phase
These forms can be administered orally, topically, or parenterally
(intramuscularly). Specialized uses include emulsions for intravenous feeding
of lipid nutrients (Intralipid). Other radiopaque emulsions are used as
diagnostic agents for X-ray examinations.
Emulsions are thermodynamically unstable. They appear white and tend to
separate on standing. In order to prepare suitable emulsions and to have them
remain stable for a suitable period of time, a number of emulsifying agents
are used in their preparation. They can be natural substances (acacia or
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Gumma arabicum, tragacanth, pectin, gelatin, egg yolk, lecithin, etc.), finely
divided solids, or synthetic agents.
SUSPENSIONS
Suspensions (suspensio, -onis, -ones) are two-phase systems
consisting of a finely divided solids dispersed in liquids. If the drug
is insoluble or poorly soluble, a suspension may be the most
suitable dosage form. The taste of drugs can be improved if they
are supplied in suspension form rather than solutions. Suspensions
may be formulated for oral, parenteral (intramuscular or
intraarticular) or topical administration. Antibiotic granules are
generally used for preparation of suspensions in pediatric practice.
Well formulated suspensions should posses certain basic
properties. The dispersed phase should settle slowly, if at all
possible, and be dispersed readily on shaking.
The main ingredients in a suspension are:
a drug
natural viscosity agents (natural gums and cellulose derivatives)
an external medium – it is usually water for oral preparations; or
other polar liquids (glycerin, alcohol)
MUCILAGES
Mucilages (mucilago, -inis, -ines) are thick, viscid, adhesive
liquids, produced by dispersing gum in water, or by extracting the
mucilaginous principles from plant substances with water (Gumma
arabicum, Radix althaeae, etc.). They are unstable and should
never be made in quantities larger than those that can be used
immediately, unless a preservative is added.
Mucilages are used primarily to prevent immediate sedimentation
of insoluble substances in liquids. They can prevent mucous
irritation caused by some drug substances (e.g., Chlorali hydras).
DROPS
Drops (guttae, -arum) are solutions, tinctures, or mixtures of high-
potent drug substances. These forms are intended to be
administered internally or externally (as eye drops or collyrium,
nasal, and otic drops). Drops are prescribed in small quantity (10 –
30 g). For officinal forms, the right number of drops per 1 ml of
liquid have to be labeled.
MIXTURES
Mixtures (mixtura, -ae, -ae) are multicomponent liquid containing
two or more active ingredients, dissolved, suspended, or dispersed
in a suitable liquid base (water, alcohol, glycerin, aromatic water, or
infusions and decoctions). Some mixtures may contain tinctures.
Suspended solids may separate slowly on standing, but are easily
redispersed on shaking (shake mixtures – mixturae
agitandae).Syrups are added as Remedium corrigens, in quantity of
20% of the total volume (30% for children). Mixtures are unstable
dosage forms with short duration and they are subject to
contamination by microorganisms during the period of their use.
STERILE DOSAGE FORMS FOR INJECTION
Sterile dosage forms for injection differ from all other drug dosage forms
because of their unique use for injection directly into body tissue through the
primary protective systems of the human body, the skin and mucous
membranes. Therefore, they must be exceptionally pure and free from
contaminants.
Injections may be classified in several categories:
1. Solutions ready for injection
2. Dry, soluble products ready to be combined with a solvent just prior to
administration (ex tempore)
3. Suspensions ready for injections
4. Emulsions
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5. Liquid concentrates ready for dilution prior to administration
These injections may be administered by such routes as intravenous,
subcutaneous, intradermal, intramuscular, intraarticular, and intrathecal. The
nature of the product will determine the route of administration. Suspensions
would not be administered directly into the blood stream because of the
danger of insoluble particles blocking capillaries. Unstable emulsions, if
injected intravenously may cause lipid embolism (excluding some forms with
special characteristics). Hypertonic solutions are administered only
intravenously. When compared with other dosage forms, injections possess
certain advantages:
1. They provide drugs for immediate action
2. The therapeutic dose is adjusted more accurately and readily
3. Drugs can be administered parenterally in cases of unconscious or
uncooperative state of the patient, or because of lack of absorption from the
GIT.
Among the disadvantages are requirement of asepsis, pain factor, risk of local
irritation, difficulty in correcting the error.
Parenteral products are packaged in ampoules, vials, bottles, plastic bags,
and prefilled disposable syringes. Containers for injections can be made of
glass or thermoplastic polymers. They may range in size from 1000 ml bottles
to 1 ml or less ampoules, vials, or syringes. Each vial is sealed with a rubber
closure held in place by an aluminum cap.
The most widely used solvent for parenteral preparations is sterile water for
injection (aqua redestillata or bidestillata – pyrified water rendered sterile and
pyrogen-free by repeated distillation). Other common solvents include sodium
chloride injection, peach oil (for water-insoluble drugs), etc.
PRESCRIPTION WRITING
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3. Emulsion bases: most commonly used type of ointment bases. The oil
phase is typically made up of Vaselinum and/or liquid petrolatum (Paraffinum
liqidum).
4. Water-soluble bases – they are generally prepared of polyethylene glycol.
TYPES OF OINTMENTS:
4. GELS or jellies (gel, -i) are semisolid dosage forms with high degree of
clarity, ease of application and ease of removal and use. The active
ingredients are incorporated into water-soluble bases. The gels often provide a
faster release of drug substance as compared to creams and ointments. Gel
formulations include ophthalmic preparations of pilocarpine, carbachol; topical
preparations for burn therapy; anti-inflammatory treatment; treatment of acne,
etc. Depending on their ingredients some gels may function as protective
coatings. Gels are prepared in adhesive forms in order to increase the contact
time of the active ingredients, e.g., topical dosage forms for aphthous
stomatitis.
LINIMENTS
Liniments (linimentum, -i, -a) are thick, viscid liquids, emulsions,
suspensions, etc. They are intended for external application. They usually are
applied with friction and rubbing onto the affected area. The oily liniments are
milder in their action but are more useful when massage is required.
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SUPPOSITORIES
Suppositories (suppositorium, -i, -a) are solid dosage forms of various
weights and shapes for insertion into the rectum, vagina, or the urethra. After
insertion, suppositories soften, melt, and dissolve in the cavity fluids.
Suppository vehicles (bases) can be classified into two types: fatty (e.g.,
Cocoa butter) and water soluble (e.g., polyethylene glycol). Cocoa butter is a
naturally occurring triglyceride, being solid at room temperature and melting
quickly at body temperature.
Types: (1) Rectal suppositories (suppositoria rectalia) are administered
rectally either to treat local conditions such as hemorrhoids or to achieve
systemic absorption (sedatives, tranquilizers, and analgesics).
Rectal suppositories can be used when the patient is enable to take
medication by mouth, or when the patient is unconscious. The lower, middle
and upper hemorrhoidal veins surround the rectum. Only the upper vein
conveys blood into the portal system, thus drugs absorbed into the lower and
middle hemorrhoidal veins will bypass the liver. Disadvantages to the use of
rectal suppositories include possible uncertain, local irritation and possible
accidental loss of the medication.
(2) Vaginal suppositories are applied vaginally for a local effect.
Following intravaginal administration, some drug absorbtion from the intact
vaginal mucosa is likely.
(3) Urethral suppositories (suppositoria urethralia) are cylindrical
dosage forms, administered urethrally to treat local conditions. They are
unusual dosage forms.
PLASTERS
Plasters (emplastrum, -i, -a) are substances intended for external application
made of such materials and of such consistency as to adhere to the skin. They
are intended to protection and support and/or to bring medication into close
contact with the skin.
adhesive plasters
medicated plasters are used for local or regional drug delivery
transdermal delivery (or therapeutic) systems (TTS) are used for long-
term systemic delivery of therapeutic agents through the skin (e.g.,
antihypertensive, antianginal, analgesic, steroidal and contraceptive drugs).
Examples: Nitroderm TTS, Estraderm TTS, Durogesic, etc.
PLAQUES
Plaques are special devices for local controlled, prolonged drug therapy,
which are intended for application under the eyelid or in the conjunctival sac of
the eye (plaques used in the treatment of glaucoma) or on the palate (plaques
with antifungal action).
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AEROSOLS (SPRAY)
These drugs are designed to carry the drug into the respiratory tree of the
patient or on the skin and mucous (nasal, etc.). According to the chemical
characteristics, they are categorized in three groups: gases (nitrous oxide,
oxygen), vapors of volatile liquids (ether, halothane, chloroform), and
aerosols (sprays).
PRESCRIPTION WRITING
1. Ointments
Rp./ Acidi borici 1,0
Vaselini albi ad 20,0
Msce fiat unguentum.
D. S. Apply twice daily to the affected skin. Not for children under 3 years.
#
Rp./ Unguenti dermatici Acidi borici 5% 18,0
D. tub. № 1.
S. Apply twice daily to the affected skin. Not for children under 3 years.
#
Rp./ Ung. derm. Gentamycini 0,1% 15,0
D. tub. № 1.
S. Apply twice daily to affected skin.
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#
Rp./ Unguenti ophthalmici Gentamycini 0,3% 5,0
(Ung. Ophth.) Gentamycini 0,3% 5,0
D. tub. № 1.
S. Apply in the lower conjunctival sac of the affected eye twice daily.
#
Rp./ Ultraproct 15,0
(Ultraproct 15 g)
D. tub. № 1.
S. Apply rectally in the evening.
2. Pastes
Rp./ Acidi salicylici 2,0
Zinci oxydi 25,0
Vaselini 48,0
M. f. pasta.
D. S. Apply externally to the burned area once daily.
#
Rp./ Pastae Zinci 25,0
D. tub. № 1.
S. Apply externally to the burned areas once daily.
3. Gels
Rp./ Geli Troxevasini 2 % 40,0
D. tub. № 1
S. Apply twice daily to the affected area (for treatment of varices).
4. Creams
Rp./ Creme Clotrimazoli 1% 20,0
D. tub. № 1.
S. Apply externally to the affected area.
5. Liniments
Rp./ Olei Lini
Aquae Calcis aa 50,0
M. f. linimentum.
D. S. Apply to the burned area.
6. Suppositories
Rp./ Paracetamoli 150 mg
(Paracetamoli 0,150)
D. scat. № 1 in supp.
S. Insert 1 suppository into rectum twice daily.
#
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Rp./ Morphini hydrochlorici 0,01
Butyri Cacao q. s.
M. f. supp.
D. t. d. № 3.
S. Insert 1 supp. into rectum in case of pain.
#
Rp./ Doloproct
D. scat. № 1 in supp.
S. Insert 1 supp. into rectum in the evening.
7. Plasters
Rp./ Nitrodermi TTS 25 mg
D. scat. № 1
S. Stick 1 plaster daily on the precordial area.
8. Aerosols
Rp./ Ventolini inhaler 0,1 mg
D. t. d. № 1 in flac.
S. For inhalation in case of asthma attack.
#
Rp./ Bicromati 20,0
D. scat. №1 in caps.
S. Inhale 2 capsules every 12 hours, with spinhaler.
EXTEMPORANEOUS PRESCRIPTIONS
1. Antacid powder with anaesthesine (benzocaine)
Rp./ Anaesthesini
Bismuthi subnitratis aa 3,0
Magnesiae oxydi 40,0
M. f. pulvis.
D.S. Half a teaspoon to be taken with meal.
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