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    Laboratory 1, 2Pharmacology

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    as c eore ca a a onPharmacology

    Pharmacology-the science that studies drugs, by drug understanding any substance o

    association that exerts certain effects, named therapeutic effects, by interacting with th

    Pharmacology-several parts, each of them with a certain focus:

    Pharmacokinetics-studies how the organism affects the drug from the administratexcretion; it practically describes all the processes and phenomena that a drug

    Pharmacodynamics-the effects of drugs on the body and their mechanisms of actbetween drug concentration and effect

    Clinical pharmacology-focuses on the application of pharmacological principles anthe clinical medicine

    Pharmacognosy-the physical, chemical, biochemical and biological properties of d

    Pharmacography describes the notion of prescribing a drug

    Pharmacotoxicology-adverse effects of a drug

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    Basic theoretical data onPharmacology

    Pharmacopoeia (pharmacopeiaorpharmacopoeia)-official book that contains the main compounds of the drugs, the pharmaceutictheir purity status; it also describes the general manufacture, control and storage dir

    -it is mainly addressed to pharmacists, but some of the chapters are useful for docto

    -there are national and international pharmacopoeias, all of them issued under the

    government, and their instructions have the force of law in their countries, excep

    United States, which was written by commissioners appointed by medical and p

    societies, and has no other authority, although generally accepted as the national te

    -the 1st Romanian pharmacopeia was written by Constantin Hepites, both in Roman

    in 1863

    -the latest-printed in 2008 (10thedition)

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    Pharmacopoeia-parts:

    1stpart:- monographs of simple substances, animal and vegetal products, pharm

    and officinal preparations

    -a monograph: the name in Romanian and Latin, chemical formula and na

    weight, chemical and physical properties, identity tests, purity conditions, methods

    measurement, storage stipulations, the dose for one administration and for 24 h2ndpart: general analysis methods for chemical, physical and biologic testing of p

    3rdpart: several tables; useful for practitioners-maximum doses

    VENENA chapter: extremely toxic preparations and drugs (ex. Opium, morphine)

    Basic theoretical data onPharmacology

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    Basic theoretical data onPharmacology

    SEPARADNA chapter: medicines with a low toxicity in usual doses, but extremely awith a high risk of toxicity if the maximum dose is exceeded

    The medicines from VENENA and SEPARANDA chapters are stored separately in ph

    special containers and lockers

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    Basic theoretical data onPharmacology

    Pharmacopoeia-measurement units: the following multiplicative prefixes, whdecimal multiples and submultiples of the SI units, are used in the International Ph

    giga (G) 109mega (M) 106kilo (k) 103centi (c) 10-2milli (m) 10-3

    micro () 10-6nano (n) 10-9pico (p) 10-12

    :

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    Basic theoretical data onPharmacologyPharmacopoeia-measurement units-Units of mass-all quantities are prescribed in

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

    kilogram (kg) 103ggram (g)milligram (mg) 10-3gmicrogram (g) 10-g

    nanogram (ng) 10-g

    litre (1) = 1 000 cm3

    millilitre (mL) = 1 cm3

    microlitre (l) = 0.001 cm3

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    Basic theoretical data onPharmacologyConcentrations

    Romanian Pharmacopoeia mentions the following types of noting the concentrati

    -% 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

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    Basic theoretical data onPharmacologyAproximate 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, therefoa 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

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    Basic theoretical data onPharmacologyFor 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

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    Basic theoretical data onPharmacologyNomenclature 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)-commoninternational name, recommended by WHO, and represents the main monograph t

    Latin or Romanian

    The officinal name, written in pharmacopoeia, which is known as official in a certa

    Ex. Dover powder-1 part opium powder, 1 part ipecac and 8 parts lactulose

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    Basic theoretical data onPharmacologyMedicines/preparations classification

    By the prescribing mode and their availability in pharmacies

    1. Magistral prescription-denoting a preparation, compounded in the pharmacy, aphysician's prescription. The receipt must specify the substances used and the qEx. Spasmolytic cachets

    2. Officinal preparations-fix formula, written in pharmacopoeia; they are written inofficinal name and are prepared in pharmacies. Ex. Dover powder cachets

    3. Commercial preparationsproduced industrially

    By composition:

    1. Simple-one active substance; ex. Acidum acetylsalicylicum troch-0.5g

    2. Composed-2 or more active substances; ex. Antacid powder

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    Basic theoretical data onPharmacology

    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

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    Pharmaceuticalforms/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, nasa(mouth), rectal solutions, urethral solutions, irrigation (vaginal) solutions, lotions, aromatic water, mucompresses, cataplasms, baths.

    -extractive: infusions, decoctions and maceration extractsb. 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 b

    3. Oil forms: solutions and extracts

    4. Emulsions

    5. Suspensions

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    Pharmaceuticalforms/preparationsB. Solid preparations

    1. Powders

    2. Troches

    3. Tablets

    4. Dragees

    5. Granulates

    6. Suppositories

    7. Capsules8. Pills

    9. Clods

    10. Medicinal pencil

    11. Drug delivery systems

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    Pharmaceuticalforms/preparationsC. Semi-solid preparations

    1. Ointments

    2. Cerates

    3. Medicinal soaps

    4. Plasters

    5. Liniments

    D. Gas forms

    1. Gases

    2. Aerosols

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    LIQUID FORMS/PREPARATION1.AQUEOUS FORMS

    1.1 Without sugar, non-extractive: obtained by diluting in water one or more activethe active substances are homogenous dispersed

    The quantity of active substance diluted in a certain quantity of solution=concentrformulated as g of active substance in 100g of solvent (mass concentration) or ml osubstance in 100ml solvent (volume concentration)

    The aqueous solutions must be clear; if the color, taste or smell is modified, then 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 prpharmaceutical forms

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    LIQUID FORMS/PREPARATION1.AQUEOUS FORMS-1.1 Without sugar, non-extractive

    a. Injectable solutions : liquid preparations that contain one or more chemical substances (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

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    LIQUID FORMS/PREPARATION1.AQUEOUS FORMS-1.1 Without sugar, non-extractive

    a. Injectable solutions

    Presenting forms:

    Ampoul/vial-glass recipient, usually cylindrical, hermetic closed, that contain one medicine

    Bottle-glass recipient, with various capacity, closed with a rubber bang; it can contmore doses of medicine, liquid or powder which will be solubilized when necessary

    Solutions for perfusion-iv >100ml

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    LIQUID FORMS/PREPARATION

    1.AQUEOUS FORMS-1.1 Without sugar, non-extractivea. 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 trtumors or for diagnostic purposes

    -intrathecal-when local and rapid effects of drugs on the meninges or cerebrospinal axis are desired, aanesthesia or treatment of acute CNS infections, drugs sometimes are injected directly into the spinal space. Brain tumors also may be treated by direct intraventricular drug administration.

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    LIQUID FORMS/PREPARATION

    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 stableclose to the lacrimal one (7.4-7.7)

    -they can be antibiotics, antiseptic, used for mydriasis, anti-inflammatory, local aes

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    LIQUID FORMS/PREPARATION1.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, glycepurgatives, 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 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 dsystem

    we avoid the phenomenon of first hepatic passage

    we can administrate different substances when the oral or parenteral routes are inapp

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    LIQUID FORMS/PREPARATION1.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 somalcohol, glycerin, ether

    -their fluidity allows rapid and uniform application over a wide skin surface

    -antiseptics, anti-mycosis..

    k. Compresses-externalapplications 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..

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    LIQUID FORMS/PREPARATION1.AQUEOUS FORMS-1.2 Without sugar, extractive

    -pharmaceutical preparations obtained by using the extractive action of watdifferent vegetable active substances

    -prepared exclusive in pharmacies

    a. Infusions

    -obtained by adding boiled water, for 5 minutes, over the fragile parts of a p

    (flowers, leaves)

    -when the plant does not contain toxic active substances, the ratio is 6g ofsubstance/100ml boiled water

    -if the plant contains toxic substances the ratio is 0.1-0.5g of substances/100

    Ex. Chamomile infusion 6g%, ipecac infusion 0.5g%, mint infusion..

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    LIQUID FORMS/PREPARATION1.AQUEOUS FORMS-1.2 Without sugar, extractive

    b. Decoctions

    -obtained by adding boiled water, for 30 minutes, over the woody parts of the plantsstools, 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, 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 tmeanwhile is shaken for 5-6 times

    -ex. Flax seeds maceration extract used as laxative

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    LIQUID FORMS/PREPARATION1.AQUEOUS FORMS-1.3 With sugar

    a. 5-10% sugara.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 dosea.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

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    LIQUID FORMS/PREPARATION2.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,95% ethanol-is used when on the recipe is not specified the concentration; diluted

    -alcoholic solutions are more stable compared to aqueous ones

    -they are prescribed as magistral, officinal or commercial preparations and are admthe 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 re

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    LIQUID FORMS/PREPARATION2.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 tinctureD. By the vehicle

    -alcohol

    -ether-alcohol

    ! All the tinctures are officinal preparations; mixture of tinctures can be prescribed mag

    ! Mostly, they are administered internal; 1g of tincture=56-67 drops 60 drops; some of skin

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    LIQUID FORMS/PREPARATION2.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 mof the active substances

    -ex. Borax glycerin for oral cavity

    2.3 Solutions using propylene glycol-mostly injections

    Ex. Phenobarbital

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    LIQUID FORMS/PREPARATION3.OILY FORMS

    3.1 Oily solutions-preparations using a vegetable (sunflower, olive, soya, castor oil),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

    3.2 Oily extarcts

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    LIQUID FORMS/PREPARATION4.EMULSIONS

    =preparations obtained from at least 2 liquid substances, not miscible, dispersed anemulsifying agents

    -emulsifying agents can be alkaline soaps, propylene glycol, gum Arabic, gelatin

    -opalescent aspect

    -administered shaken, external or oral, rarely injectable

    -magistral, officinal, commercial preparationsEx. KABIVEN-parenteral alimentation

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    LIQUID FORMS/PREPARATION5.SUSPENSIONS

    =preparations containing finely divided, undissolved drug particles dispersed throug(gum Arabic, propylene glycol, methocel)

    -depending on the concentration and size of undissolved suspended particles, suspdegree of opacity

    -the particles have a tendency to settle and form a sediment, but, after shaking thehomogenous dispersed

    ! They must be shaken before administration

    -can be prescribed as magistral, officinal, commercial preparations

    Ex.

    -Benzatin-penicillin-injectable

    -acetaminophen suspension for pediatric use