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DEPARTMENT OF PHARMACOLOGY
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
III. Synthetic sources of drugs
In searching for similar activity, many new drugs have been synthesized.
Semisynthetic drugs are based on natural ingredients:
Reserpine and synthetic antipsychotic agents
Morphine and synthetic analgesics
Curare and synthetic neuromuscular blockers
Adrenaline and amphetamines
Hormones, vitamins, antiepileptic drugs, synthetic antibiotics are only a small
part of the modern drugs, produced by synthesis.
Plant Species
Popular
name
Crude
Drug
Active ingredients
Pharmacological action
Drug
Atropa
Belladonna
Deadly
night shade
roots
Radix Belladonnae
anticholinergic: antispasmodic,antisecretory,
mydriatic, CNS-activity
Atropine
Scopolamine
Datura
stramonium
Jimson weed,
thorn apple
leaves
Folium Stramonii
anticholinergic: antispasmodic,antisecretory,
mydriatic, CNS-activity
Asthma cigarettes
Hyosciamus
Niger
leaves
Folium Hyosciami
opium dried
exudate of the incised
seed capsule
leaves
Folium Digitalis
leaves
Folium Digitalis
seeds
Semen Strophanthi
the overground part
Herba Adonidis
vernalis
roots
Radix Rauwolfiae
roots end rhizome
Radix et rhizoma
Valerianae
bark
Cortex Chinae
Asthma cigarettes
Henbane
alkaloids: atropine,
hyosciamine, hyoscine
(scopolamine)
alkaloids: atropine,
hyosciamine, hyoscine
(scopolamine)
alkaloids: atropine,
hyosciamine, hyoscine
(scopolamine)
alkaloids: morphine, codeine,
papaverine
cardiac glycosides
Morphine
Codeine Papaverine
cardiac glycosides
cardiotonics
Digitoxin
Digoxin
Strophanthin G and K
cardiac glycosides
cardiotonics
cardiac glycosides
mild cardiotonics
sedatives
hypotensive, antipsychotic
Papaverum
somniferrum
Opium poppy
Digitalis
Purpurea
Digitalis
Lanata
Strophanthus
Gratus et Kombe
Foxglove
Adonis
Vernalis
Rauwolfia
serpentine
Valeriana
officinalis
Pheasants eye
Cinchona
Grecian
Foxglove
Chandrika,
Patalagandhi
alkaloids: reserpine
Digitoxin
Adinorm
Reserpine
Valeriana
alkaloids: quinidine,
quinine, cinchonine
Quinine
Quinidine
buccal tablets
sublingual tablets
chewable tablets
effervescent tablets
sugar-coated tablets
film-coated tablets
enteric coated tablets
controlled-release tablets
2.2. Tablets for parenteral administration
tablets for solution
inserts
pellets (tablets for implantation)
3. Capsules
hard gelatin capsules
soft gelatin capsules
enteric-coated capsule
4.Granulae
5. Pills
6. Troches
dusting powders
CAPSULES
Capsules (capsula, -ae) are solid dosage forms in which the drug substance
is enclosed in either a hard or soft soluble container of suitable form of gelatin.
They are intended to mask the smell and taste of the drug substance.
Capsules are tasteless, easily administered and some patients prefer them to
the tablets.
1. Hard gelatin capsules (capsulae gelatinosae durae s. operculatae),
also referred to as dry-filled capsules (DFC), consist of two sections, one
slipping over the other, thus completely surrounding the drug formulation.
Commercially filled capsules have the conventional oblong shape.
2. Soft elastic capsules (SEC; capsulae gelatinosae molles s. elasticae)
are soft, globular, gelatin shells somewhat thicker than that of hard gelatin.
They may be round, oval, oblong, or tube-shaped and the contents may be
liquid, paste, or powder. Oil-soluble drugs, (e.g. vit A, E) can be
administered in SEC.
3. Enteric-coated capsules remain intact in the stomach, but dissolve and
release the contents of the capsule once it reaches the small intestine.
They delay the release of drugs which are inactivated by the stomach
contents or may irritate the gastric mucosa. Enteric coatings are prepared
of synthetic polymers.
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.
10
#
Rp./ Pulveris dermatici Topocini 5 g
(Pulv. derm. Topocini 5 g)
D. scat. 1.
S. For external application.
#
Rp/ Flac. Zinnati 125 mg/5 ml 60 ml
(Granulorum Zinnati 125 mg/5 ml 60 ml)
(Suspensionis Zinnati 125 mg/5 ml 60 ml)
Da. Signa. 2 ml every 12 hours (for baby with body mass 10 kg)
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
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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).
INFUSIONS AND DECOCTIONS
Infusion (infusum, -i, -a) is a dilute solution of the readily soluble
constituents of crude drugs (from the soft parts of plants). Fresh
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TYPES OF OINTMENTS:
1. OINTMENTS (UNGUENTUM, -I, -A) are prepared of solid active ingredients
(125%), finely powdered and then incorporated into the oleaginous base.
According to the way of administration they can be: ointments for skin
application (unguenta dermatica: 20100 g), eye ointments (unguenta
ophthalmica: 310 g), nose ointments (unguenta nasalia), etc.
2. PASTES (PASTA, -AE, -AE) contain powders dispersed in the vehicle in
quantity more than 25%. They are usually stiffer, less greasy and more
absorptive than ointments. Pastes adhere reasonably well to the skin and they
are suited for application on and around moist lesions. Pastes are less
macerating than ointments. They easily may be removed from the skin. They
are divided into pastes for application on the skin (pastae dermaticae) and
dental pastes (pastae dentifricae). An official paste is the Zinc Oxide paste.
3. CREAMS (CREME, -ORES) are similar to ointments but they contain a
water phase (water, aromatic water, etc.). They are classified as:
cold creams with roughly dispersed water phase and cooling properties
emollient creams with finely dispersed water phase, which soften the skin.
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
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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.
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 longterm 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
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the eye (plaques used in the treatment of glaucoma) or on the palate (plaques
with antifungal action).
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).
Aerosols are heterogeneous systems consisting of very finely subdivided
liquid or solid particles (optimum size 0,53 m) dispersed in a gas medium.
The pressurized aerosol packages contain different propellants (compressed
gases) driving the drug in the form of mist or foam. They can be inhaled
(nasally or orally) or applied topically to dispense a variety of agents for
treatment of systemic and topical diseases. Metered dose inhalers (with a
metering valve) contain multiple doses and they are intended for delivering
measured quantities of drug. Examples: Salbutamol, Salmeterol, Fenoterol,
etc.
Powders may be administered by mechanical devices that require manually
produced pressure and a deep inhalation by the patient (e.g., Cromolin
sodium).
Nebulizers are devices used for administration of solutions giving sufficiently
small droplets. Nebulised solutions may be breathed directly or by a plastic
face mask or a tent.
Advantages: rapid onset of action; bypass the hepatic circulation; avoidance of
degradation in the gastrointestinal tract; lower dosage that minimizes adverse
reactions; simple, convenient and acceptable therapy.
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.
#
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D. scat. 1 in supp.
S. Insert 1 suppository into rectum twice daily.
#
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.
2. Powder with caffeine for general refreshment
Rp./ Coffeini puri 0,05
Sacchari albi 0,2
M.
f. pulvis
D. t. d. 20
S. Take one powder each morning and at lunch-time.
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