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INTRODUCTION TO PHARMACOLOGY

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Title: INTRODUCTION TO PHARMACOLOGY


1
INTRODUCTION TO PHARMACOLOGY
Lector prof. Posokhova K.A.
2
  • PHARMACOLOGY
  • (Greek Pharmacon drug, logos - teaching)
  • The science that studies the interaction of
    the chemical substances with live organisms,
    drugs administration for treatment and
    prophylaxis of various diseases and pathological
    processes

3
  • Pharmaceutical explosion
  • Nowadays there are over 350 thousand drugs in
    the world which are used for different diseases
  • In Ukraine nearly 16 thousand drugs are
    registered now and allowed for administration as
    curative agents

4
  • Ukraine 147 preparations of Diclofenac-sodium,
    60 Paracetamol
  • (Acetaminophen)
  • For each drug - only single international name
    and different trade names

5
Paracetamol (Ukraine)
  • Mono
  • ????????, ????????, ???????, ??????,
    ?????????, ???????, ????????, ???????, ???????,
    ??????????, ????????, ???????, ???????, ?????????
  • Combined
  • ?????????, ?????????, ???????, ??????? ???,
    ?????, ????????, ???????? ??????, ???????? ?????,
    ???????, ????????, ?????, ????? ????, ????????,
    ????-???, ????????, ???????? ??????,
  • ????????? ??????, ????? ???????, ?????????,
    ?????????, ??????????, ????????, ????????,
    ??????, ????????, ?????? ????, ???????, ????????,
    ????????, ??????? ????, ???????? ????, ???????,
    ?????????, ????-???, ????????, ???????, ????
    ????, ?????????, ????????, ???????????, ???????,
    ???????, ?????????, ??????, ???????, ??????????,
    ????????, ???????? ??????, ????? ???, ????????,
    ???????, ?????????, ???????, ???????,
    ??????????, ?????????, ?????????, ???????,
    ???????

6
Nadolol( ß1, ß 2 - adrenoblocker )
7
Becotide Beclometh(beclomethasone dipropionate)
8
  • Brand original drug which is defended by
    patent and may be produced during patent term
    only by this pharmaceutical firm
  • Generic when term of patent is discontinued
    the drug may be produced by different
    pharmaceutical companies under new product
    (trade) names but at the basis of original active
    substance (similar quantity, route of
    administration etc.)
  • All generics are much more cheaper compared
    to brands, that is the main reason why they are
    so popular among the patients

9
GENERICS
  • UK, Deutschland, French, Holland, Denmark the
    part of generics among all drugs is 50-75 (in
    Ukraine the majority of drugs)
  • Market volume of generics In Europe is over 10
    billion annually

10
SE (side effects) and complications of drugs
  • 200 000 people in U.S.A. die from side effects of
    drugs annually
  • 76,6 billion are spared in U.S.A. annually to
    treat complications attached to drugs usage

11
Side effects (SE) of drugs
  • Take 5th place among causes of mortality on the
    Earth after cardiac-vascular diseases, malignant
    tumors, lungs diseases, traumas
  • Among stationary patients frequency of SE after
    introduction of drugs makes 2-40

12
Medical mistakes in clinics
  • Doctors
  • - overdosing
  • - administration of drugs to patients with
    allergy
  • - mixing up names of the drugs
  • Medical nurses
  • - introduction of other drug by a mistake
  • - violation of drug introduction regime
  • - mistake in medical form
  • - mixing up names of the drugs

13
focomelia
Talidomide (katergan)
14
PHARMACOKINETICS
  • THE PART OF PHARMACOLOGY THAT CONCERNED WITH
    THE
  • ABSORBTION,
  • DISTRIBUTION,
  • METABOLISM (BIOTRANSFORMATION)
  • AND EXCRETION OF DRUGS
  • WHAT THE ORGANISM DOES TO THE DRUGS

15
PHARMACODYNAMICS
  • THE PART OF PHARMACOLOGY THAT CONCERNED WITH
    THE
  • BIOCEMICAL AND PHYSIOLOGICAL EFFECTS OF DRUGS AND
    THEIR MODE OF ACTION
  • IT INCLUDES THE DOSE-EFFECT RELATIONSHIP, FACTORS
    MODIFYING DRUG EFFECTS, DOSAGE, DRUG TOXICITY
  • WHAT DRUGS DO TO THE ORGANISM

16
PHARMACODYNAMICS
  • Pharmacological effect clinical manifestation
    of drug influence on the organism
  • Its basis is primary pharmacological reaction
    the result of drug influence on special
    structures of the organism
  • Pharmacological effects may be identical but
    caused by different pharmacological reactions
  • atropin and adrenalin dilates the pupils, 1st
    inhibits M-cholinoreceptos, 2nd activates
    adrenoreceptors
  • In contrary, different pharmacological effects
    may appear due to the same pharmacological
    reaction
  • anaprilinum causes ß-adrenoreceptors blockade
    that resulted in hypotension, antiarrhythmic
    action and antianginal effect

17
PHARMACOLOGICAL EFFECTS
  • Local action local anesthesia, astringent,
    covering, irritating, necrotizing, adsorbing
  • Reflex action as a result of local irritation
    (Sol. Ammonii caustici, Validolum, Charta
    Sinapis, expectorants of plant origin)
  • Resorbtive (systemic) action after drug
    absorption or its introduction to blood stream)
    1) direct (primary) and 2)
    indirect (secondary) cardiac glycosides 1 on
    heart, 2 diuretic effect
  • Selective action (salbutamol, celecoxyb,
    doxazosin)
  • Nonspecific action on all cells of the
    organism drugs for general anesthesia, salts of
    heavy metals
  • Basic (beneficial) action and adverse reaction
  • Reversible and irreversible

18
RECEPTOR THEORY OF DRUG ACTION
  • Receptors the places where drugs bind to
    tissues macromolecules, enzymes, channels,
    transport systems, genes
  • Agonists adrenalin, isadrine, morphine etc.
  • Antagonists atropin, anaprilin, dimedrol etc.
  • Agonist-antagonist
  • labetolol (?1, ?1-adreno-blocker, but
    activates ?2-adrenoreceptors),
  • pentazocin (agonist delta- and kappa-opiate
    receptors and mu-receptors antagonist)

19
NONSPECIFIC ACTION OF DRUGS
  • Due to their physical and chemical properties
  • Mannit increases osmotic pressure in kidneys
    canalicules and causes diuretic effect
  • Direct chemical interaction Antacides (MgO,
    NaHCO3) neutralize HCl, Trilon B (EDTA) binds
    salts of heavy metals, Na citrate binds Ca-ions
  • Physical-chemical interaction Protamine sulfate
    binds Heparin
  • Due to the same structure with metabolites of the
    organism drugs interferences with corresponding
    metabolic processes Sulfonamides (have the same
    structure to PABA), Mercaptopurin (to folic acid
    and purin)

20
  • Bioavailability
  • of drugs
  • complex of pharmacokinetic processes that
    maintenance active concentration of drug in the
    area of specific receptors (part of administered
    drug that reaches the systemic circulation and
    effects specific receptors)

21
PRESYSTEMIC ELIMINATION (first pass metabolism)
  • presystemic elimination extraction of the
    drug form blood circulatory system during its
    first passage through the liver it leads to
    decreasing of bioavailability (and therefore,
    decreasing of biological activity) of drugs
  • propranolol (anaprilin), labetolol, aminazin,
    acetylsalicylic acid, labetolol, hydralasin,
    isadrin, cortizone, lidokain, morphin,
    pentazocin, organic nitrates, reserpin

22
  • ONSET the period between the moment of drug
    introduction to the organism and the beginning of
    its action
  • DURATION OF DRUG ACTION the period then
    specific effects of the drug are maintained
  • WIDENESS of therapeutic action (therapeutic
    window) the distance between minimum
    therapeutic and minimum toxic doses of drug

23
Drugs effecting the afferent innervation
24
  • Substances which act in the area of afferent
    nerves endings
  • local anesthetics
  • astringent
  • covering
  • adsorbtive
  • irritative

25
  • Local anesthetics

26
  • Local anesthetics
  • Natural compound aether of benzoilekgonin -
    cocain
  • Synthetic neutrogen compounds
  • Aether compounds (derivatives from PABA)
  • a) easily dilluted in water novocain (procain),
    dicain (tetrakain)
  • b) badly dilluted in water anaesthesin
    (benzokain), orthokain
  • Amide compounds lidocain (xycain), trimecain,
    etydocain (duranest), prilocain (citanest),
    articain (ultracain), piromecain (bumekain),
    marcain (bupivacain)

27
STRUCTURE OF LOCAL ANESTHETICS
R
x
(CH2)n
N
R
I
II
III
I lipophilic aromatic group II intermediate
aliphatic chain III hydrophilic amine-group
28
  • Kinds of local anesthesia
  • terminal
  • conductive
  • infiltrative

29
  • Terminal (superficial) anesthesia - local
    anesthetic is spread over mucous membranes,
    wounds, ulcers, fresh granulations
  • For terminal anesthesia we often use anaesthesin,
    dicain, xycain, trimecain, very rarely
    novocain, because it badly penetrates through
    mucous membranes

30
  • Conductive (regional) anesthesia - is an
    introduction of anesthetic into area of nervous
    truncs, ganglia, sensitive roots of spinal cord.
  • Kinds of regional anesthesia truncal
    (conductive), plexal (anesthesia of nervous
    plexuses), paravertebral (anesthesia of nerovus
    ganglia), spinal-cord, peridural
  • For performing of this anesthesia novocain,
    xycain, trimecain, ultracain are used

31
  • Infiltrative anesthesia is a mixed kind of
    local anesthesia, in which nervous endings and
    fibres get turned off because of layer by layer
    infiltration of tissues with a solution of local
    anesthetic.
  • For infiltrative anesthesia novocain, xycain,
    trimecain, ultracain are used

32
  • Cocain (Cocainum) alcaloid, which is extracted
    from leaves of South-American plant Erythroxylon
    coca. Its local anesthetic action overwhelms
    local anesthetic activity of novocain in 3 times
    and toxicity is 3-5 times greater
  • It is used very rarely
  • only for superficial anesthesia
  • in stomatology, otholaryngology, urology in a
    form of 2-5 solutions

33
Erythroxylon coca
34
TOXICOLOGY OF COCAINAcute intoxication
short-time euforia, fear, tachicardia, exophtalm,
dizziness, delirium, loss of consciousness,
seizures, comatous condition, decreasing of
arterial pressure, stop of breathingChronic
intoxication cocainismpsychological and
physical addiction, mental degradation,
cretinism, atrophyc disorders, including
perforation of nasal septum, gangrene, heavy
cardiac arrythmias, cardiac arrest
35
  • Novocain (Novocainum) derivative of PABA
    (para-aminobenzoic acid)
  • usage
  • infiltrative anesthesia - 0,25-0,5 solutions
  • truncal anesthesia - 1-2 solutions
  • treatment blockades (paranephral,
    vagosympathetic) 0,25-0,5 solutions
  • spinal cord anesthesia - 2-3 ml of 5 solution
    (is introduced into subarachnoid space on the
    level higher than first lumbal vertebra)
  • At recent time novocain was used for depression
    of reflexes, central nervous system, heart, in
    patients with gastritis, ulcer disease,
    hypertonic disease, stenocardia, neurodermitis,
    spasms of peripheral vessels. In this case this
    drug was introduced intravenously or
    intramuscularly

36
  • Xycain (Lidocain)
  • it is 2 times stronger (activity regarding) than
    novocain with the same toxicity
  • usage
  • for all kinds of local anesthesia
  • infiltrative - 0,25-0,5 solutions
  • conductive 0,5-2 solutions
  • peridural 0,5 solution
  • spinal cord 5 solution
  • terminal 4-10 solutions

37
Xycain (Lidocain)
  • Xycain eliminates cardiac arrythmias of
    ventricular origin, i.e. extrasystolia,
    fibrillation of ventricules in acute miocardial
    infarction. In this cases xycain is administred
    intravenously, dropply, slowly, in a form of
  • 0,2 solution.
  • Xycain (lidocain) can be used in individuals,
    which are sensybilized towards novocain and other
    anesthetics of complexed aehters group (dicain,
    anesthesin)

38
Xycain (Lidocain)
39
XYCAIN (LIDOCAIN)
40
  • Trimecain
  • anesthetic avtivity and action duration are
    2 times greater, comparatively to novocain,
    toxicity is a bit higher
  • Usage


    infiltrative - 0,125 , 0,25 and
    0,5 solutions
  • truncal - 1 and 2 solutions peridural
    - 1 , 2 solutions
  • spinal cord - 5 solution
  • terminal - 2-5 solutions
  • as an antiarythmic drug in cardial arythmias of
    ventricular origin - intravenously, at the
    begging in a form of 2 solution very slowly
    after - dropply 0,2 soluiton

41
  • Bupivacain (marcain)
  • one of the most active anesthetics of prolonged
    action (onset 2-20 min, duration of action 7
    hours)
  • Usage
  • infiltrative, truncal, epidural anesthesia
  • considerable cardiotoxicity !

42
  • Articain (ultracain)
  • usage
  • infiltrative and conductive anesthesia
  • Analgetic action develops after 1-2 min. after
    introduction of the drug, lasts for 1-3,5 hours
  • in stomatology - combined drug, which consists
    of ultracain and adrenalini hydrochloridum
    (epinephrin)
  • - ultracain D-C

43
Acute poisoning with local anesthetics
  • Symptoms
  • decreasing of arterial pressure, of heart
    activity, cardiac arrest, depression of CNS and
    breathing, seizures
  • Treatment
  • vasoconstriction drugs (noradrenaline,
    adrenaline), cardiotonic (strophantin,
    corglycon), antiseizure drugs (sibazone,
    tiopental-sodium)
  • Prophilaxis
  • usage of least possible volume and most possible
    dillution of the local anesthetics

44
Astringent drugs
  • Organic, of plant origin
  • tannin, infusion of tea, herba Hyperici, flores
    Chamomillae, cortex Quercus
  • Nonorganic
  • Bismuthi subnitras, de-nol

45
Oak tree (bark) Quercus robur L.
46
T A N N I Nusagerinsing of mouth, pharynx,
larynx 1-2 solutiontreatment of burned
surfaces, cracks, bedsores 3-10
solutionsgastric lavage in case of poisoning
with salts of heavy metals and alcaloids 0,5
solutionNota bene! Tannin forms nonstable
compounds with morphine, phisostigmine, atropin,
nicotine, cocain
47
Saint-Johns-wort(Hypericum perforatum L.)
48
MatricaryChamomilla recutita L.
49
SageSalvia officinalis L.
50
Drugs, which stimulate nervous endingsIRRITATIVE
DRUGS
  • Ammonium solution
  • Menthol
  • Oleum Terpenthini purified
  • Mustard plaster
  • Camphor

51
Leaf MustardBrassica juncea
52
Ammonium solution 10 (ammoniac)
  • Usage
  • Unconsciousness (put a cotton ball moistured
    with ammonium solution to a nose)
  • In case of alcohol intoxication (orally
    5-10 drops of solution dilluted in half of
    a glass of water)
  • For washing of surgeons hands (rarely) (0,5
    solution)

53
  • Thanks for your attention!
  • Good-bye !
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