Laboratory 1 Pharmacology

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Laboratory 1, 2

Pharmacology
Basic theoretical data on
Pharmacology
Pharmacology-the science that studies drugs, by drug understanding any substance or substances
association that exerts certain effects, named therapeutic effects, by interacting with the human organism
Pharmacology-several parts, each of them with a certain focus:
Pharmacokinetics-studies how the organism affects the drug from the administration, until its
excretion; it practically describes all the processes and phenomena that a drug is put through
Pharmacodynamics-the effects of drugs on the body and their mechanisms of action, relationship
between drug concentration and effect
Clinical pharmacology-focuses on the application of pharmacological principles and methods in
the clinical medicine
Pharmacognosy-the physical, chemical, biochemical and biological properties of drugs
Pharmacography describes the notion of prescribing a drug
Pharmacotoxicology-adverse effects of a drug


Basic theoretical data on
Pharmacology
Pharmacopoeia (pharmacopeia or pharmacopoeia)
-official book that contains the main compounds of the drugs, the pharmaceutical forms and
their purity status; it also describes the general manufacture, control and storage directions
-it is mainly addressed to pharmacists, but some of the chapters are useful for doctors
-there are national and international pharmacopoeias, all of them issued under the authority of
government, and their instructions have the force of law in their countries, except that of the
United States, which was written by commissioners appointed by medical and pharmaceutical
societies, and has no other authority, although generally accepted as the national textbook
-the 1
st
Romanian pharmacopeia was written by Constantin Hepites, both in Romanian and Latin,
in 1863
-the latest-printed in 2008 (10
th
edition)


Pharmacopoeia-parts:
1
st
part:- monographs of simple substances, animal and vegetal products, pharmaceutical forms
and officinal preparations
-a monograph: the name in Romanian and Latin, chemical formula and name, molecular
weight, chemical and physical properties, identity tests, purity conditions, methods of quantitative
measurement, storage stipulations, the dose for one administration and for 24 h
2
nd
part: general analysis methods for chemical, physical and biologic testing of preparations
3
rd
part: several tables; useful for practitioners-maximum doses
VENENA chapter: extremely toxic preparations and drugs (ex. Opium, morphine)


Basic theoretical data on
Pharmacology
Basic theoretical data on
Pharmacology

SEPARADNA chapter: medicines with a low toxicity in usual doses, but extremely active and
with a high risk of toxicity if the maximum dose is exceeded
The medicines from VENENA and SEPARANDA chapters are stored separately in pharmacies, in
special containers and lockers


Basic theoretical data on
Pharmacology
Pharmacopoeia-measurement units: the following multiplicative prefixes, which indicate
decimal multiples and submultiples of the SI units, are used in the International Pharmacopoeia

giga (G) 10
9

mega (M) 10
6

kilo (k) 10
3

centi (c) 10
-2

milli (m) 10
-3

micro () 10
-6

nano (n) 10
-9

pico (p) 10
-12

:

Basic theoretical data on
Pharmacology
Pharmacopoeia-measurement units-Units of mass-all quantities are prescribed in grams!




Pharmacopoeia-Units of volume (capacity)-all quantities are prescribed in ml!

kilogram (kg) 10
3
g
gram (g)
milligram (mg) 10-
3
g
microgram (g) 10-g
nanogram (ng) 10-g
litre (1) = 1 000 cm
3

millilitre (mL) = 1 cm
3

microlitre (l) = 0.001 cm
3

Basic theoretical data on
Pharmacology
Concentrations

Romanian Pharmacopoeia mentions the following types of noting the concentration:
-% g/g: the quantity of substance, in grams, contained in 100 grams of final product
-% g/v: the quantity of substance, in grams, contained in 100ml of final product
-% v/v: the volume of substance, in ml , contained in 100ml of final product
-% v/g: the volume of substance in ml, contained in 100 grams of final product
Basic theoretical data on
Pharmacology
Aproximate measurement units
For liquid preparations:
-1 spoon=15ml
-1 tea spoon=5ml
-1 dessert spoon=10ml
-1ml of alcoholic solution=50 drops
-1ml of hydrous solution=20 drops
Aqueous solutions- the density interferes with the approximate measurement, therefore, for ones with
a density close to 1, the mass values equal the capacity ones, for the rest:
1 tea spoon (5ml)=5g distilled water=6.5g syrup=4.5g oil
1 spoon (15ml)=15g distilled water=20g syrup=13.5g oil
Basic theoretical data on
Pharmacology
For substances conditioned as powder:
-1 tea spoon filled with powder=2.5-5g (depending of the substance)
-1 tea spoon medium filled=1.5-2.5g
-1 pinch of powder=0.5-1.5g

Other rarely used approximate measurement units:
-1 coffee cup=50ml
-1 glass for water=200ml
-1 glas for wine=100ml
Basic theoretical data on
Pharmacology
Nomenclature of medicines/preparations
Chemical name-describes the structural compounds and their relative positions
-ex. Acid 2-(7-methyl-naphtyl) propionic is the chemical name for naproxen
-ex. Magnesium sulphate, calcium carbonate etc.
DCI (Romanian abbreviation)= International Nonproprietary Name (INN)-common
international name, recommended by WHO, and represents the main monograph title, given in
Latin or Romanian
The officinal name, written in pharmacopoeia, which is known as official in a certain country
Ex. Dover powder-1 part opium powder, 1 part ipecac and 8 parts lactulose

Basic theoretical data on
Pharmacology
Medicines/preparations classification
By the prescribing mode and their availability in pharmacies
1. Magistral prescription-denoting a preparation, compounded in the pharmacy, according to a
physician's prescription. The receipt must specify the substances used and the quantity of each one;
Ex. Spasmolytic cachets
2. Officinal preparations-fix formula, written in pharmacopoeia; they are written in the receipt with the
officinal name and are prepared in pharmacies. Ex. Dover powder cachets
3. Commercial preparations produced industrially
By composition:
1. Simple-one active substance; ex. Acidum acetylsalicylicum troch-0.5g
2. Composed-2 or more active substances; ex. Antacid powder





Basic theoretical data on
Pharmacology

Medicines classification

By the route of administration:
1. Digestive (oral/intern; sublingual; in the rectum)
2. Injection (parenteral): intravenous, intramuscular, subcutaneous..
3. External-on skin and mucous membranes
4. Inhalation-gases, aerosol



Pharmaceutical
forms/preparations
By the state of aggregation:
A. Liquid preparations
1. Aqueous forms:
a. Without added sugar:
-non extractive: solutions for injections, collyrium (ophthalmic solutions), otic solutions, nasal solutions, oral solutions
(mouth), rectal solutions, urethral solutions, irrigation (vaginal) solutions, lotions, aromatic water, mucilage, glair substances,
compresses, cataplasms, baths.
-extractive: infusions, decoctions and maceration extracts
b. With added sugar: 5-10% sugar: tea, potion, lemonade
>60% sugar: syrup
2. Alcoholic forms: solutions, tincture/alcoholic extract, preparations with glycerin or propylene glycol base
3. Oil forms: solutions and extracts
4. Emulsions
5. Suspensions


Pharmaceutical
forms/preparations
B. Solid preparations
1. Powders
2. Troches
3. Tablets
4. Dragees
5. Granulates
6. Suppositories
7. Capsules
8. Pills
9. Clods
10. Medicinal pencil
11. Drug delivery systems



Pharmaceutical
forms/preparations
C. Semi-solid preparations
1. Ointments
2. Cerates
3. Medicinal soaps
4. Plasters
5. Liniments

D. Gas forms
1. Gases
2. Aerosols
LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS
1.1 Without sugar, non-extractive: obtained by diluting in water one or more active substances;
the active substances are homogenous dispersed
The quantity of active substance diluted in a certain quantity of solution=concentration; it is
formulated as g of active substance in 100g of solvent (mass concentration) or ml of active
substance in 100ml solvent (volume concentration)
The aqueous solutions must be clear; if the color, taste or smell is modified, then the solution
is no longer proper to use
By their composition, aqueous forms can be simple or complex
They can be used for administration (external, internal or parenteral use) or for preparing other
pharmaceutical forms
LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.1 Without sugar, non-extractive
a. Injectable solutions : liquid preparations that contain one or more chemical substances (solute/s), dissolved in a
solvent or mixture of solvents. Mainly, the solvent is represented by distilled water.
Other solvents: vegetable oils, water mixed with alcohol or propylene glycol
-the solvent must be clear, without taste or smell and with a proper viscosity
All injectable solutions must fulfil certain criteria:
-not contain mechanic impurities
-aseptic
-not to induce fever
-all the active solutes must be stable
-not painful
-an osmotic pressure similar to plasma
-a pH similar to plasma


LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.1 Without sugar, non-extractive
a. Injectable solutions
Presenting forms:
Ampoul/vial-glass recipient, usually cylindrical, hermetic closed, that contain one dose of
medicine
Bottle-glass recipient, with various capacity, closed with a rubber bang; it can contain one or
more doses of medicine, liquid or powder which will be solubilized when necessary
Solutions for perfusion-iv >100ml


LIQUID FORMS/PREPARATIONS

1.AQUEOUS FORMS-1.1 Without sugar, non-extractive
a. Injectable solutions
Administered:
-intramuscular (im)
-intravenous (iv)
-subcutaneous (sc)
-intradermic
-occasionally, intraarterial-in order to localize its effect in a particular tissue or organ, such as in the treatment of liver
tumors or for diagnostic purposes
-intrathecal-when local and rapid effects of drugs on the meninges or cerebrospinal axis are desired, as in spinal
anesthesia or treatment of acute CNS infections, drugs sometimes are injected directly into the spinal subarachnoid
space. Brain tumors also may be treated by direct intraventricular drug administration.

LIQUID FORMS/PREPARATIONS

1.AQUEOUS FORMS-1.1 Without sugar, non-extractive
a. Injectable solutions

! We never administer oily solutions iv

-Solutions for perfusion are administered with a special attachment,
drop by drop, with a rhythm specified by the doctor

LIQUID FORMS/PREPARATIONS

1.AQUEOUS FORMS-1.1 Without sugar, non-extractive
b. Ophthalmic solutions (collyrium)

-pure liquid forms, used for the diagnosis and treatment of ocular diseases
-they are administered in the conjunctiva sac
-must be: clear, osmotic balanced with the lacrimal secretion, pure, chemical stable, with a pH
close to the lacrimal one (7.4-7.7)
-they can be antibiotics, antiseptic, used for mydriasis, anti-inflammatory, local aesthetics
LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.1 Without sugar, non-extractive
c. Nasal solutions (nasal drops) : preparations intended for administration to the nasal cavities,
by instillation, to obtain a local effect
-antibiotics, antiseptic, vasoconstrictive substances, local anesthetics
-the pH must be 5.5-7.5, they must not interfere with the normal cilliary movement and non
irritating for the mucosa

d. Otic solutions: preparations used for treating otic diseases; they must be pure, clear, with a
pH between 5-7.5
-antiseptic, antibiotics, anti-inflammatory, local anesthetics, anti-mycosis..
LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.1 Without sugar, non-extractive

e. Enemas (rectal solutions) : liquid preparations used for rectal administration
e.1. Evacuate enemas: big volume (250-500ml) and contain emollient substances, glycerin, oil,
purgatives, boiled water;
-they determine the distension of the rectum and, by reflex action, its evacuation
e.2 Therapeutic enemas: small volume (100-150ml)-solutions of an active substance in water, that
will be absorbed in the rectum
- anesthetics, analgesics..
Advantages!
fast absorption in the inferior vena cava system-systemic effect
we can administrate substances that are gastric irritants or that are neutralized in the digestive
system
we avoid the phenomenon of first hepatic passage
we can administrate different substances when the oral or parenteral routes are inapproachable


LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.1 Without sugar, non-extractive

f.Aromatic water: clear, saturated solutions of volatile oils or other aromatic substances in water
-they are used for their therapeutic properties (ex. mint water) or to correct the smell or taste of
different preparations (ex. roses water)
g. Preparations used for gargle (oral/mouth solutions): liquid aqueous preparations used to clean
the oral cavity and the pharynx
-anesthetics, anti-inflammatory, antiseptic
h. Mucilage: solutions of mucilage vegetable substances or colloids in water
-used in enemas, in suspensions, as emulsion stabilizers
i. Substances used for anointment-glair solutions (colutoriu): to anoint/cover the oral cavity,
pharynx, gums
-antibiotics, antiseptics, local anesthetics
-a bigger amount of active substances compared to oral solutions
-ex. Glycerin with borax used for aphthaes


LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.1 Without sugar, non-extractive

j. Lotions-liquid preparations intended for external application to the skin
-suspensions or emulsions of dispersed solid or liquid materials mostly in water, but sometimes in
alcohol, glycerin, ether
-their fluidity allows rapid and uniform application over a wide skin surface
-antiseptics, anti-mycosis..
k. Compresses-external applications of different active substances on the skin,
using a fine muslin covered by polyethylene
l. Cataplasm-preparations (mostly vegetable) applied cold or hot on the skin,
used mostly for the treatment of abscesses
m. Urethral or vaginal solutions-used as antiseptics, emollients, to alkalize..
n. Therapeutic baths-calming, anti-inflammatory..


LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.2 Without sugar, extractive

-pharmaceutical preparations obtained by using the extractive action of water over
different vegetable active substances
-prepared exclusive in pharmacies
a. Infusions
-obtained by adding boiled water, for 5 minutes, over the fragile parts of a plant
(flowers, leaves)
-when the plant does not contain toxic active substances, the ratio is 6g of
substance/100ml boiled water
-if the plant contains toxic substances the ratio is 0.1-0.5g of substances/100ml water
Ex. Chamomile infusion 6g%, ipecac infusion 0.5g%, mint infusion..

LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.2 Without sugar, extractive

b. Decoctions
-obtained by adding boiled water, for 30 minutes, over the woody parts of the plants (roots,
stools, bulbs); ex. Valerian decoction
-They are prescribed for 24-48 hours because the decoction can ferment
c. Maceration extracts
-obtained by the extractive action of water, with a temperature similar to the room, over
vegetable preparations that contain mucilage substances
-the drug/water ratio is 5 %
-the mixture is kept in the room temperature for at least 30 minutes, depending of the drug, and
meanwhile is shaken for 5-6 times
-ex. Flax seeds maceration extract used as laxative

LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.3 With sugar
a. 5-10% sugar
a.1 Tea
- obtained by adding sugar in infusions or decoctions
-they can easily alter so we prepare them only for maximum 24 hours
-ex. Laxative tea, spasmolytic tea..
a.2 Potions
-complex liquid preparations with at least 2 active substances
-administered with a spoon or tea spoon and are prescribed as magistral preparations
-one spoon or tea spoon contains one therapeutic dose
a.3 Lemonades
-contain water, sugar 5-10% and a mineral, organic acid or a cell salt
-the route of administration is oral
-they can be kept for maximum 24-48 hours
-ex. anti-emetic lemonade

LIQUID FORMS/PREPARATIONS
1.AQUEOUS FORMS-1.3 With sugar

b. Over 60% sugar-syrup

-are officinal or commercial preparations
-the quantity of syrup is always prescribed in grams!
-the route of administration is oral, by spoon (20g) or tea spoon (6.5g)
Ex.
- Codeine syrup for cough
- Belladonna syrup for spasms

LIQUID FORMS/PREPARATIONS
2.ALCOHOLIC FORMS

2.1 Alcoholic forms using ethanol
a. Alcoholic solutions- obtained by diluting active substances in ethanol*
* In Romanian Pharmacopoeia are mentioned 2 forms of ethanol: officinal ethanol, concentrate, with
95% ethanol-is used when on the recipe is not specified the concentration; diluted ethanol-70%
-alcoholic solutions are more stable compared to aqueous ones
-they are prescribed as magistral, officinal or commercial preparations and are administered external on
the skin or internal
Ex. alcoholic solution of mint oil, camphor oil
oMedicinal wine-active substances dilute in wine (12-16% alcohol)
oMedicinal vinegar-the acetic acid concentration 6-9%; ex. Aromatic vinegar with revulsive action

LIQUID FORMS/PREPARATIONS
2.ALCOHOLIC FORMS

2.1 Alcoholic forms using ethanol
b. Alcoholic extracts (tinctures*)-hydro-alcoholic or ether-alcoholic preparations obtained by extracting
active priciples from vegetable or animal substances
*the term tincture comes from Latin word TINCTURI that means colourful
-most of the tinctures are dark brown and can be conserved for 1-2 years
Classification:
A. By the preparation manner:
-By maceration-orange peels tincture
-By percolation (extraction of a soluble substance using a solvent form a mixture)-belladonna tincture
-By diluting the fluid extracts or dissolving the dry ones

LIQUID FORMS/PREPARATIONS
2.ALCOHOLIC FORMS

2.1 Alcoholic forms using ethanol-b. Alcoholic extracts (tinctures)-classification

B. By composition:
-simple-one active substance-belladonna tincture
-complex-2 or more active substances
C. By toxicity:
-without toxicity; drug/liquid ratio=2/10; ex. valerian tincture
-with toxicity; drug/liquid ratio=1/10; ex.belladonna tincture
D. By the vehicle
-alcohol
-ether-alcohol
! All the tinctures are officinal preparations; mixture of tinctures can be prescribed magistral
! Mostly, they are administered internal; 1g of tincture=56-67 drops 60 drops; some of them external, on the
skin

LIQUID FORMS/PREPARATIONS
2.ALCOHOLIC FORMS

2.2 Alcoholic forms using glycerin
-glycerin is used as a solvent or mixed with water and ethanol in order to obtain a more efficient dilution
of the active substances
-ex. Borax glycerin for oral cavity

2.3 Solutions using propylene glycol
-mostly injections
Ex. Phenobarbital
LIQUID FORMS/PREPARATIONS
3.OILY FORMS
3.1 Oily solutions-preparations using a vegetable (sunflower, olive, soya, castor oil), animal (fish) or
mineral (paraffin) oil
-active principles are suspended or dissolved in oil
-administered internal, external or rarely injectable
They must fulfil certain criteria:
-must maintain liquid in room temperature
-must be clear
-must have a specific taste and smell
They need to be storage in hermetic closed containers, away from the light, in a dry, cool room

3.2 Oily extarcts


LIQUID FORMS/PREPARATIONS
4.EMULSIONS

=preparations obtained from at least 2 liquid substances, not miscible, dispersed and stabilized using
emulsifying agents
-emulsifying agents can be alkaline soaps, propylene glycol, gum Arabic, gelatin
-opalescent aspect
-administered shaken, external or oral, rarely injectable
-magistral, officinal, commercial preparations
Ex. KABIVEN-parenteral alimentation


LIQUID FORMS/PREPARATIONS
5.SUSPENSIONS

=preparations containing finely divided, undissolved drug particles dispersed throughout a liquid vehicle
(gum Arabic, propylene glycol, methocel)
-depending on the concentration and size of undissolved suspended particles, suspensions assume a
degree of opacity
-the particles have a tendency to settle and form a sediment, but, after shaking they must form a
homogenous dispersed
! They must be shaken before administration
-can be prescribed as magistral, officinal, commercial preparations
Ex.
-Benzatin-penicillin-injectable
-acetaminophen suspension for pediatric use

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