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The Art of Compounding Drugs From Various Substances Is Known as

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Introduction to pharmacology 1

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Slides are prepared as per INC Syllabus Unit Vii Miscellaneous drugs and it is about benefited for B sc Nursing students and faculty of the field of study

Slides are prepared as per INC Syllabus Unit VII Miscellaneous drugs and information technology is nearly benefited for B sc Nursing students and faculty of the discipline

  1. i. Introduction to Pharmacology Mr. Dipti Y. Sorte Chapter 2-1Mr.Dipti Southward.08/23/eighteen
  2. two. Syllabus – (Unit I: Introduction to Pharmacology) • Definitions: Terminology use. • Pharmacognosy: Sources • Types: Classification • Pharmaco-dynamics: Actions, therapeutic Adverse, toxic effect. • Pharmacokinetics: Absorption, distribution, metabolism, interaction, excretion 208/23/18
  3. iii. • Review: Routes and principles of administration of drugs • Indian pharmacopoeia: Legal bug, Storage of various drugs. • Calculation of drug dosage. • Rational use of drugs. • Pharmacotherapeutics: Principles of therapeutics. 08/23/18 Mr.Dipti South. Chapter 2-iii
  4. 4. Introduction to Pharmacology History, Types of pharmacology, sources of Drug information etc. 08/23/18 Mr.Dipti S. Chapter 2-iv
  5. 5. INTRODUCTION TO PHARMACOLOGY • Pharma=Drugs, Logos = Cognition (Pharmacology = The study or science of drugs) • Pharmacology: It is the science of drugs derived from 2 Greek words: Pharmakon (Greek give-and-take for drugs) and logos (the Greek word for science). It is the study of the actions of drugs on living arrangement. • It includes physical and chemical backdrop, biochemical and physiological effects, mechanism of activeness, therapeutic uses and adverse effects of drugs.
  6. 6. Drug • Any chemical that affects the processes of a living organism Affiliate 2-6Mr.Dipti Due south.08/23/eighteen
  7. 7. Pharma=Drugs, Logos = Knowledge Pharmacology • The study or science of drugs Chapter two-7Mr.Dipti South.08/23/18
  8. eight. History of Pharmacology 08/23/18 Mr.Dipti Due south. Chapter ii-eight
  9. 9. HISTORY OF PHARMACOLOGY • Knowledge of drugs and their uses in diseases are as old equally history of mankind. • Primitive men gather the cognition of healing and medicines past observing the nature, noticing the animals while ill and personal feel after consuming plants and herbs as remedies. • Ancient civilizations discovered that extracts from plants, animals, and minerals had medicinal effects on body tissue. These discoveries became the foundation of pharmacology.
  10. 10. Pharmacology in the present form is relatively recent branch nigh hundred years quondam. Historical developments in Pharmacology •PEN PSAO (2700 BC) It was the great herbal materia medica written in communist china. •Kahun Papyrus (2000 BC) is an oldest Egyptian document containing information about veterinary medicines and uterine diseases of women. •Ebers papyrus (1550 BC) also an Egyptian certificate containing data about number of diseases and 829 prescription where castor oil, opium like drug are being used.08/23/18 Mr.Dipti S. Affiliate 2-10
  11. 11. Historical developments in Pharmacology • Hippocrates (460-375 BC) A greek physician consider "father of Medicine". He was the commencement person who recognize disease as abnormal reaction of body. He introduce use of metallic salts for the treatment of disease. • Theophrastus (380-287 BC) a not bad philosopher called begetter of Pharmacognosy. He classified medicinal plants on the base of medicinal characteristics.
  12. 12. Historical developments in Pharmacology • Dioscorides (AD 57) a greek, produced i of the outset materia medica of approximately 500 plants and remedies. • Claudius Galen (AD 129–200) first attempted to consider the theoretical groundwork of pharmacology. • Paracelsus (1493–1541) a Swiss scholar and alchemist, ofttimes considered the "grandfather of pharmacology". He introduces the use of chemicals for treatment of disease. • Valerius Cordus (1514-1544) He compiled the offset pharmacopeia where he described techniques for the grooming of drugs.
  13. 13. MODERN PHARMACOLOGY • Conversion of quondam medicines into the modern pharmacology kickoff taking shape following the introduction of animal experimentation and isolation of agile ingredients from plants. • Francois Megendie (1783-1855) a first pharmacologist established the foundation of modernistic pharmacology. He developed experiment to elucidate the physiological processes and activeness of drugs on the body. • Rudolph Buchheim (1820–1879) High german pharmacologist a key figure in the development of pharmacology, a who at the University of Dorpat, created the first pharmacological plant.
  14. 14. Modern PHARMACOLOGY • Frederich Sertürner, German pharmacist's assistant, isolated morphine—the commencement pure drug—in 1805 • Claude Bernard (1813-1878) considered Male parent of experimental Medicine. He identifies the site of action of curare (arrow Poisoning). 08/23/18 Mr.Dipti Due south. Affiliate 2-14
  15. xv. MODERN PHARMACOLOGY • Oswald Schmiedeberg (1838–1921) "Male parent of Pharmacology" established pharmacology every bit an independent discipline. He kickoff pedagogy Pharmacology in University of Strasbourg (France). • John Jacob Abel (1857-1938) founded first department of pharmacology in U.s. in the University of Michigan in 1893. In 1897 he established pharmacology section at Johns Hopkins University. Abel also co- founded the Periodical of Pharmacology and Experimental Therapeutics in 1909.
  16. 16. Modern PHARMACOLOGY • 50. mayer Jones (1912-2002) regarded as father of modernistic veterinary pharmacology. He authored first book of veterinarian pharmacology therapeutics in 1954. SCOPE OF PHARMACOLOGY • It provides the rational footing for the therapeutic use of the drug. Before the establishment of this discipline, even though many remedies were used, but doctors were reluctant to apply scientific principles to therapeutics. • In 1920s, many constructed chemicals were first introduced and the modern pharmaceutical companies began to develop.
  17. 17. Scope OF PHARMACOLOGY • Scientific agreement of drugs enables usa to predict the pharmacological result of a new chemical that will produce a specified therapeutic effect. • The telescopic of pharmacology has expanded profoundly over the final decade to incorporate many new approaches such as estimator-assisted drug pattern, genetic screens, protein engineering and use of novel drug commitment vehicles including viruses and artificial cells. • Our society needs pharmacologists who sympathize the basis of modern therapeutics for careers within academic, pharmaceutical and governmental laboratories to written report and develop tomorrow'south drugs.
  18. 18. Sources of Drug information • The sources of drug information is received by pharmacopeia, that is a volume which contains a list of established and officially approved drug with description of their physical and chemical characteristics and tests for their identification, purity, methods of storage etc. some of the pharmacopeia's are: • Indian Pharmacopeia.(I.P.) • British Pharmacopeia (B.P.) • European Pharmacopeia.(East.P) • The states Pharmacopeia.(U.S.P).08/23/eighteen Mr.Dipti Due south. Affiliate 2-18
  19. 19. contd • Other sources of drug data are • National formulary (NF), Martindale – The extra Pharmacopeia, • Physician desk Reference (PDR), • American Medical Association drug Evaluation, • Textbook & Periodical of pharmacology and therapeutics, Drug bulletins, information bases similar drug Micromedex, Medline, Cochrane library etc. • Sources of drug data is as well present in Formulary which provides information about available drugs – their use, dosage, adverse effect, contraindications, precautions, warnings and guidance on selecting right drugs for a range of conditions. 08/23/18 Mr.Dipti S. Chapter 2-19
  20. 20. Definitions: Terminology uses. 08/23/18 Mr.Dipti S. Chapter ii-xx
  21. 21. Definitions Pharmacology Pharmacognosy Chemist's Detailed study of drugs Science of identification of drug Scientific discipline of identification,selection, preservation, standardization, compounding and dispensing of medical substances Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg ii
  22. 22. Definitions Therapeutics Toxicology Branch of medicine concerned With cure of disease or relief of Symptoms and includes drug Treatment Science of poisons. # Measurement / detections of poisons # Handling of poisoning Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg ii (Contd)
  23. 23. Definitions Chemotherapy Pharmacopoeia Event of drugs upon micro- organisms and parasites, living and multiplying in a living organism An official code containing a selected list of the established drugs and medicinal preparations with clarification of their concrete properties and tests for their identity, purity and dominance Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg 2 (Contd)
  24. 24. Drug – WHO scientific group definition Any substance or product that is used/ intended to be used to modify or explore physiological systems or pathological systems or pathological states for the benefit of the recipient Whatsoever substance or product that is used/ intended to be used to modify or explore physiological systems or pathological systems or pathological states for the do good of the recipient
  25. 25. Drug Attachment • Medication chemically binds to specific sites called "receptor sites" – Agonist-chemical fits at receptor site well – Adversary- a chemical blocks some other chemical from getting to a receptor – Fractional agonist - attach to the receptor but only produce a small effect Pharmacology AY 2013-2014 25
  26. 26. Basics of Drug Action • Desired action – the expected response of a medication • Side effects –known and oft experienced, expected reaction to drug. • Adverse reaction –unexpected, unpredictable reactions that are non related as well usual effects of a normal dose of the drug. 26
  27. 27. Drug Interaction • Takes place when 1 drug alters the action of some other drug. • Some are helpful but frequently produce agin effects. 27
  28. 28. Common Drug Interactions 28 PharmacologyAY2013-2014 • Additive effect- takes place when 2 drugs are given together & double the effect is produced. Alcohol + aspirin= Pain relief
  29. 29. • Antagonist- a chemical blocks another chemical from getting to a receptor • Combative effect- takes place when 1 drug interferes with the action of some other drug. • Eg. Protamine sulpha to counteract heparin toxicity 29 Common Drug Interactions
  30. xxx. • Displacement consequence - takes place when 1 drug replaces another at the drug receptor site, increasing the outcome of the 1st drug. xxx Common Drug Interactions
  31. 31. • Incompatibility –occurs when two drugs mixed together in a syringe produce a chemical reaction so they cannot be given. e.grand. Protamine sulfate & vitamin K 31 Mutual Drug Interactions
  32. 32. 32 PharmacologyAY2013-2014 • Interference- occurs when 1 drug promotes the rapid excretion of another, thus reducing the activity of the 1st . • Synergistic issue takes identify when the effect of 2 drugs taken at the same time is greater than the sum of each drug given solitary. E.yard. combining diuretics & adrenergic blockers to lower the BP Mutual Drug Interactions
  33. 33. Pharmacognosy: Sources of Drugs 08/23/eighteen Mr.Dipti Southward. Chapter 2-33
  34. 34. Pharmacognosy • The study of natural (found and animal) drug sources Chapter 2-34Mr.Dipti Due south.08/23/18
  35. 35. Sources of Drugs • The dissimilar sources of drugs are: • Plants: • Alkaloids: eg. Morphine, Atropine, Quinine, reserpine, ephedrine. • Glycosides: eg. Digoxin, Digitoxin. • Animals: Insulin, Heparin. • Minerals: ferrous sulphate, Magnesium sulphate. • Microorganisms: Penicillins, Streptomycin, Grisiofulvin. • Semisynthetic: Hydromorphone, Hydrocodone. • Synthetic: Virtually of the drugs used today are synthetic. Eg. Aspirin, paracetamol. 08/23/eighteen Mr.Dipti S. Chapter 2-35
  36. 36. contd • Drugs are besides produced by genetic engineering (Deoxyribonucleic acid recombinant technology) eg. Human insulin, Man growth hormone and Hepatitis B Vaccine. 08/23/18 Mr.Dipti Due south. Affiliate 2-36
  37. 37. Types: Classification of Pharmacology. 08/23/18 Mr.Dipti S. Chapter 2-37
  38. 38. Classification - Pharmacology 08/23/eighteen Mr.Dipti Due south. Chapter ii-38
  39. 39. PHARMACOLOGY, Link to other biomedical principles
  40. 40. Types of Pharmacology 1. Experimental Pharmacology: Done in the laboratory on experimental animals such equally rodents and non rodents. 2. Clinical Pharmacology: On human subjects normal or deceased Chapter 2-40Mr.Dipti Southward.08/23/18
  41. 41. Nomenclature OF DRUGS one. Chemic Nature 2. Source 3. Target organ/Site of Activity 4. Way of Action 5. Therapeutic Uses 6. Physiological system 7. Physical Effects
  42. 42. 1. Classification BASED ON CHEMICAL NATURE • Chemical Nature of drug is discussed by a Chemist and based on chemical nature we divide drugs into • INORGANIC DRUGS Metals and their Salts (Ferrous Sulphate, Zinc Sulphate, Magnesium Sulphate. Non Metals Includes Sulphur. • ORGANIC DRUGS • Alkaloids (atropine, Morphine, Strychnine) • Glycosides (Digitoxin, Digoxin). • Proteins(Insuline, Oxytocin) • Esters, Amide, Alcohol, Glycerides.
  43. 43. 2. Classification BASED ON SOURCE Natural Source • Plants (Morphine, Atropine, Digitoxin) • Animals (Insuline, eCG) • Micro organism (Penicillin) • Mineral (Sodium Chloride) Constructed Source • (Sulphonamide, Procaine). Semi-synthetic Source Amoxicillin, Ampicillin, Doxycycline Bios-ynthetic Source Recombinant Homo erythropiotin, Recombinant bovine somattotropine Sources of drugs are discussed by a Pharmacologist and Pharmacist
  44. 44. three. CLASSIFICATION BASED ON TARGET ORGAN • Drugs acting on CNS (Diazepam, Phenobarbitone). • Drugs acting on Respiratory Organisation (Bromhexaine). • Drugs acting on CVS (Digitoxin, Digoxin). • Drugs acting on GIT (Omeprazole, Kaoline, Sulphadimidine). • Drugs acting on Urinary System (Magnesium Sulphate, Lasix • Drugs acting on reproductive organisation (Oxytocin, Estrogen) Classification based on target organs are done by the Physicians.
  45. 45. 4. Classification BASED ON Mode OF ACTION • Inhibitor of bacterial cell wall synthesis (penicillin) • Inhibitor of bacterial protein synthesis (Tetracycline) • Calcium Aqueduct blocker (Verapamil, nifedipine) Classification based on mode of action is done by Physicians & Pharmacologists.
  46. 46. 5. CLASSIFICATION BASED ON THERAPEUTIC USE Nomenclature based on mode of action is done by Physicians & Pharmacologists. • Antimicrobials/Antibacterials (Penicillin, Streptomycin, Quinolones, Macrolides). • Antihypertensive (Clonidine, hydralazine, Enalpril). • Antidiarrheal (Lopramide, Kaoline). • Antiemetics (Domperidone, Meclizine and Metoclopramide). 08/23/eighteen Mr.Dipti S. Affiliate 2-46
  47. 47. 6. CLASSIFICATION BASED ON PHYSIOLOGICAL Arrangement • Sympathomimetics (Adrenaline, Noradrenaline). • Parasympathomimetics (Carbachol, Pilocarpine, Neostigmine). • Neuromuscular blockers Suxamethonium, Gallamine). vii. CLASSIFICATION BASED ON Physical Furnishings • Emollients (Lanolin, Vaseline) • Caustics (Silverish nitrate) • Demulcents (Zinc Oxide, Tannic Acrid).
  48. 48. –Vioxx would autumn into the class chosen Musculo-Skeletal and Joint Diseases – MIMS sets out these classes – Utilize MIMS to notice your drug'due south nomenclature This is another fashion of classifying drugs according to the system of the trunk on which information technology acts Site/Blazon of Activity
  49. 49. Drug Nomenclature Naming of drugs (Drug Nomenclature) Three Names # The Chemical Name - technical description of the bodily molecule due east.g. Cozaar is ii-Butyl, 4 Chloro- tetrazol, five Phenylbenzylimidazole, 5 Methanol sodium # The Generic Proper name - The official medical proper name Cozaar's generic name is Losartan # The Brand or Propriety Name - The name under which the product is marketed i.eastward. Cozaar Naming of drugs (Drug Nomenclature) Three Names # The Chemical Name - technical description of the actual molecule e.k. Cozaar is 2-Butyl, 4 Chloro- tetrazol, 5 Phenylbenzylimidazole, 5 Methanol sodium # The Generic Proper name - The official medical proper noun Cozaar'due south generic name is Losartan # The Brand or Propriety Name - The name under which the product is marketed i.e. Cozaar
  50. 50. Pharmaco-dynamics: Actions, therapeutic Adverse, toxic. 08/23/18 Mr.Dipti S. Chapter 2-50
  51. 51. Pharmacotherapeutics: Types of Therapies • Acute therapy • Maintenance therapy • Supplemental therapy • Palliative therapy • Supportive therapy • Prophylactic therapy Chapter 2-51Mr.Dipti Southward.08/23/18
  52. 52. Pharmacotherapeutics: Monitoring • The effectiveness of the drug therapy must be evaluated. • One must be familiar with the drug's • intended therapeutic activeness (benign) • and the drug's unintended but potential side effects (predictable, agin drug reactions). Chapter 2-52Mr.Dipti S.08/23/18
  53. 53. Pharmacotherapeutics: Monitoring • Therapeutic index • Drug concentration • Patient's status • Tolerance and dependence • Interactions • Side effects/agin drug effects Chapter ii-53Mr.Dipti South.08/23/eighteen
  54. 54. Pharmacotherapeutics: Monitoring Therapeutic Index • The ratio between a drug's therapeutic benefits and its toxic effects Chapter 2-54Mr.Dipti S.08/23/18
  55. 55. Pharmacotherapeutics: Monitoring Tolerance • A decreasing response to repetitive drug doses Dependence • A physiologic or psychological demand for a drug Chapter ii-55Mr.Dipti S.08/23/18
  56. 56. Pharmacotherapeutics: Monitoring Interactions may occur with other drugs or food • Drug interactions: the alteration of activity of a drug by: – Other prescribed drugs – Over-the-counter medications – Herbal therapies Affiliate 2-56Mr.Dipti S.08/23/18
  57. 57. Pharmacotherapeutics: Monitoring Interactions • Additive effect • Synergistic consequence • Combative effect • Incompatibility Chapter 2-57Mr.Dipti South.08/23/18
  58. 58. Pharmacotherapeutics: Monitoring Medication Misadventures Adverse drug events • ALL are preventable • Medication errors that outcome in patient damage Agin drug reactions • Inherent, not preventable event occurring in the normal therapeutic utilise of a drug • Any reaction that is unexpected, undesirable, and occurs at doses normally used Chapter 2-58Mr.Dipti S.08/23/18
  59. 59. Pharmacotherapeutics: Monitoring Some adverse drug reactions are classified as side effects. • Expected, well-known reactions that result in little or no change in patient management • Predictable frequency • The effect'due south intensity and occurrence is related to the size of the dose Chapter 2-59Mr.Dipti Southward.08/23/18
  60. 60. Pharmacotherapeutics: Monitoring Adverse Drug Reaction An undesirable response to drug therapy • Idiosyncratic • Hypersensitivity reactions • Drug interactions Affiliate 2-60Mr.Dipti S.08/23/18
  61. 61. Pharmacotherapeutics: Monitoring Iatrogenic Responses Unintentional adverse furnishings that are treatment-induced • Dermatologic • Renal damage • Blood dyscrasias • Hepatic toxicity Chapter ii-61Mr.Dipti S.08/23/18
  62. 62. Pharmacotherapeutics: Monitoring Other Drug-Related Effects • Teratogenic • Mutagenic • Carcinogenic Affiliate ii-62Mr.Dipti S.08/23/xviii
  63. 63. Pharmacokinetics: Assimilation, distribution, metabolism, interaction, excretion. 08/23/eighteen Mr.Dipti Due south. Affiliate 2-63
  64. 64. Pharmacokinetics # AAbsorption # D# Distribution # Grand# Metabolism # E# Excretion # Bioavailability# Bioavailability
  65. 65. Factors influencing the efficacy of a drug are: – The route of Administration – The rate of Absorption – The distribution of the drug to the required site – The charge per unit of biotransformation or metabolism – The presence of active metabolites – The charge per unit of excretion – The route of Assistants – The charge per unit of Absorption – The distribution of the drug to the required site – The rate of biotransformation or metabolism – The presence of agile metabolites – The rate of excretion
  66. 66. Absorption # To be effective a drug must be absorbed - except for topical and Four # This ways drugs have to cross cell membranes # The ability of the drug to cantankerous the cell membrane is influenced by its solubility in water or fat, its size and shape
  67. 67. Drug Absorption of Various Oral Preparations Liquids, elixirs, syrups Fastest Pause solutions  Powders  Capsules  Tablets  Coated tablets  Enteric-coated tablets Slowest Chapter 2-67Mr.Dipti South.08/23/eighteen
  68. 68. Absorption • Drugs cross membranes past: – Filtration - simply modest h2o-soluble molecules which flow through the hydrophilic pores – Passive Transport - Diffusion i.east. from loftier concentrations to low concentrations – Active Transport - Energy and carriers are required to movement non-fat soluble substances beyond the jail cell membrane east.g confronting concentration gradient • Drugs cantankerous membranes by: – Filtration - only small water-soluble molecules which flow through the hydrophilic pores – Passive Transport - Diffusion i.eastward. from loftier concentrations to low concentrations – Active Transport - Energy and carriers are required to movement not-fat soluble substances across the cell membrane due east.1000 against concentration gradient
  69. 69. Absorption # IV injection# IV injection # delivered directly to bloodstream # rapid action # delivered straight to bloodstream # rapid activeness # All other routes# All other routes # demand to be absorbed from site of assistants # speed of action depends on assimilation rate (ka) # need to be captivated from site of administration # speed of action depends on absorption rate (ka)
  70. 70. Absorption Factors affecting the absorption rate (ka) #Route of administration # Blood supply to the site of absorption # Conception of the drug # Gut transit time # pH in the gut # Solubility of the product Factors affecting the absorption rate (ka) #Route of administration # Blood supply to the site of absorption # Formulation of the drug # Gut transit fourth dimension # pH in the gut # Solubility of the production
  71. 71. Distribution # Key compartment -(major organs & claret vessels) – depression lipid solubility (hydrophilic) – low book of distribution (depression Vd) # Peripheral compartment • (peel & fat stores) – high lipid solubility (lipophilic) – high book of distribution (loftier Vd) # Central compartment -(major organs & blood vessels) – depression lipid solubility (hydrophilic) – low volume of distribution (low Vd) # Peripheral compartment • (skin & fat stores) – high lipid solubility (lipophilic) – loftier book of distribution (loftier Vd) Drug in bloodstream is distributed to body:
  72. 72. Plasma protein binding: #Only 'free fraction' can motion to target site (e.g. fourscore% bound / twenty% gratuitous) #Dynamic process i.e. as free drug moves into tissues, protein-bound drug is released into plasma to maintain ratio (ratio of 'complimentary fraction' : 'plasma protein bound' remains constant) #Drugs vary in the degree to which they are plasma poly peptide bound (< 99.9%) Distribution
  73. 73. Metabolism Major organ of metabolism - LIVER Enzyme Pathways Unchanged drug Metabolites Inactive Metabolites Active Metabolites DRUG
  74. 74. Metabolism Major organ of metabolism - LIVER • Active metabolites : Clinical or side furnishings • Inactive metabolites N.B. Patients with hepatic impairment may require: - higher doses (where metabolism active metabolites) - lower doses (where metabolism inactive metabolites)
  75. 75. Metabolism # Genetic factors # Other drugs e.g. Cimetidine / Ciproxen # Smoking #Enzyme consecration/inhibition(CYP450/others) # Some foods #Liver illness #Age # Genetic factors # Other drugs e.yard. Cimetidine / Ciproxen # Smoking #Enzyme consecration/inhibition(CYP450/others) # Some foods #Liver disease #Age Factors affecting metabolism (i.east. compete for enzyme pathways in the liver)
  76. 76. Showtime-Laissez passer Effect The metabolism of a drug and its passage from the liver into the apportionment. •A drug given via the oral route may exist extensively metabolized by the liver before reaching the systemic circulation (loftier beginning-pass effect). •The aforementioned drug—given 4—bypasses the liver, preventing the first-pass effect from taking place, and more drug reaches the circulation. Chapter 2-76Mr.Dipti S.08/23/18
  77. 77. Metabolism Gut Liver Body # the breakdown of a drug in the liver before it reaches the site of action #oral dose may need to be college than parenteral dose # Prodrug First pass metabolism (Portal vein) (Full general circulation)
  78. 78. First Pass (Presystemic)First Laissez passer (Presystemic) MetabolismMetabolism # Metabolism of orally administered drugs in a single# Metabolism of orally administered drugs in a single passage thru the gut wall and (principally) the liver.passage thru the gut wall and (principally) the liver. # Drugs for which presystemic elimination is# Drugs for which presystemic elimination is pregnant – Isosorbide dinitrate, Propranolol etc.significant – Isosorbide dinitrate, Propranolol etc. # First pass elimination is reduced in severe hepatic# First pass elimination is reduced in severe hepatic cirrhosiscirrhosis Clinical Pharmacology, Laurence,, 1997, p92
  79. 79. Starting time-Laissez passer Effect • Routes that bypass the liver: –Sublingual Transdermal –Buccal Vaginal –Rectal Intramuscular –Intravenous Subcutaneous –Intranasal Inhalation *Rectal route undergoes a college degree of first-pass effects than the other routes listed. Chapter 2-79Mr.Dipti S.08/23/18
  80. 80. Elimination EliminationElimination = ++ Metabolism Excretion
  81. 81. Excretion #The process past which drug is removed from the body. Main # via the kidneys (in urine) likewise # via the gut (faeces), the pare (sweat), the lungs (jiff), saliva # North.B. Patients with renal disease or dysfunction (elderly/centre disease) may crave lower doses equally the drug volition be retained for longer than in 'normal' patients
  82. 82. Bioavailability • It is defined every bit the extent to which active ingredients are absorbed and transported to sites of activeness. • Factors 1. Drug solubility 2. Pharmaceutical conception iii. pH 4. Food 82
  83. 83. Dose regimes • Factors determining Dosage : –Half Life –Age –Sex –Torso Weight and Area –Tolerance –Specific disease
  84. 84. Dose regimes • OD(mane / nocte) • BD (12 hourly) • TDS (8 hourly) • QDS (6 hourly) • PRN (as required) • Depot (weekly / monthly / quarterly) • Stat (immediately) • OD(mane / nocte) • BD (12 hourly) • TDS (eight hourly) • QDS (6 hourly) • PRN (as required) • Depot (weekly / monthly / quarterly) • Stat (immediately)
  85. 85. Plasma profiles • Single dose plasma profile absorption elimination concentration time
  86. 86. Plasma levels • Abiding plasma levels merely with constant I.V. infusion. • Peaks & troughs in plasma levels with all other routes of administration (due to absorption & elimination) • Dose regimes are calculated to maintain therapeutic plasma levels • Abiding plasma levels only with abiding I.V. infusion. • Peaks & troughs in plasma levels with all other routes of administration (due to assimilation & elimination) • Dose regimes are calculated to maintain therapeutic plasma levels
  87. 87. Plasma profiles Dose plasma contour concentration time DRUG A DRUG B
  88. 88. One-half-lifeHalf-life • Refers to the fourth dimension required for the trunk to eliminate fifty% of the drug. – It is important in planning the frequency of dosing. • Short half-life (2-iv hours) : needs to be given frequently • Long one-half life: (21-24 hours): requires less frequent dosing Annotation: It takes 5 to half-dozen one-half lives to eliminate approximately 98% of a drug from the torso 88
  89. 89. • Liver and kidney disease patients may accept bug of excreting a drug. • Difficulty in excreting a drug increases the half-life and increases the risk of toxicity. • Implication: may require frequent diagnostic tests and measuring renal and hepatic function. 89 One-half-lifeHalf-life
  90. ninety. One-half Life = ½ # Fourth dimension in which a mensurate (concentration furnishings) declines by i one-half # Measured in 3 ways : - 1) Plasma half life ii) Biological effect one-half life 3) Biological half life
  91. 91. Plasma – Half Life # Time in which the plasma concentration falls by one half # Influenced by diverse factor – tissue improvidence, protein binding , renal excretion
  92. 92. Biological consequence half life # Fourth dimension in which a the pharmacological upshot of the drug, and of any of the active metabolites, has declined by one one-half # Eg. For antibiotics, varies with each infection
  93. 93. Biological half life # Time in which a the total amount of drug in the torso after equilibrium of plasma with other compartments (fat, muscle) is halved # Measured using radioisotopes, rates of excretion
  94. 94. Plasma profiles Multiple dose plasma contour steady statesteady state assimilation = elimination (avg plasma level is abiding) absorption = elimination (avg plasma level is abiding) concentration time
  95. 95. Steady state concentration # Plateau concentration # Charge per unit of input of drug to the trunk is matched by charge per unit of elimination # Has to exist in therapeutic range to maintain effect # Affected by half life of drug
  96. 96. Therapeutic Index/Ratio # Devised by Ehrlich # Maximum tolerated dose / minimum curative dose # Gives indication of safety # Particularly applicable to antibiotics # Defines safe in relation to efficacy
  97. 97. Review: Routes and principles of administration of drugs 08/23/18 Mr.Dipti S. Chapter 2-97
  98. 98. Routes of Assistants # To be effective a drug must : – Be present in an active grade – At the correct site – At the right concentration – For the right duration of time # The conception of the product for each delivery road is vital to ensure optimal activity and consistent delivery # Thus choose the right Route of Administration and Formulation
  99. 99. Route of Administration & Formulation (Dosage forms) OralOral ParenteralParenteral Sub-lingual / buccalSub-lingual / buccal InhaledInhaled Tablets / Capsules / Elixirs / Syrups / Suspensions /Granules / Powders / Caplets / Drops Tablets / Capsules / Elixirs / Syrups / Suspensions /Granules / Powders / Caplets / Drops Intra-dermal / Subcutaneous / Intra-muscular / Intra-venous / Intra-thecal / Epidural / Spinal / Depot Intra-dermal / Subcutaneous / Intra-muscular / Intra-venous / Intra-thecal / Epidural / Spinal / Depot Tablets / SpraysTablets / Sprays Aerosol inhalers / Dry pulverisation inhalers / Nebuliser solutions / Spacers Aerosol inhalers / Dry powder inhalers / Nebuliser solutions / Spacers
  100. 100. Road of Administration & Formulation (Dosage forms) Road of Administration & Conception (Dosage forms) Rectal (PR) Vaginal (PV) Transdermal Topical Suppositories / Enemas Pessaries / Creams / Vaginal tablets Creams / Gels / Patches Creams / Lotions / Gels / Nasal sprays / Shampoos / Suppositories / Peccaries
  101. 101. Oral RouteOral Road # Absorption hampered by nutrient# Absorption hampered by nutrient # Drug may exist destroyed (insulin)# Drug may be destroyed (insulin) # Drug may not be absorbed# Drug may not be absorbed (Streptomycin)(Streptomycin) # First pass metabolism# First pass metabolism
  102. 102. Sublingual routeSublingual route # Arable claret supply# Abundant claret supply # Quick event# Quick effect # No degradation by digestive juices# No deposition by digestive juices # No first pass metabolism# No first pass metabolism # Irritation of mucous membranes# Irritation of mucous membranes
  103. 103. Rectal RouteRectal Road # Rich blood supply# Rich blood supply # No irritation of GIT# No irritation of GIT # Useful in patients who# Useful in patients who cannot swallow/airsickness /cannot consume/vomiting / uncooperative patientuncooperative patient
  104. 104. Effects of Protein BindingEffects of Protein Bounden on Drugson Drugs ## Assists oral absorption of a drugAssists oral absorption of a drug # Delays metabolic degradation# Delays metabolic deposition # Delays excretion# Delays excretion # Diminishes penetration into the CNS# Diminishes penetration into the CNS Significance – acts every bit reservoir and thereby prolongsSignificance – acts as reservoir and thereby prolongs action of drugaction of drug Pharmaclogy & Pharmacotherapeutics, Satokar, 1997, p14
  105. 105. Enteric CoatingEnteric Coating Pills or tablets are coated with substances whichPills or tablets are coated with substances which resist the acid juice of the stomach only permitresist the acrid juice of the stomach but permit disintegration in intestinal juices.disintegration in abdominal juices. # To foreclose gastric irritation & alteration of drug in stomach# To prevent gastric irritation & alteration of drug in stomach # To get desired concentration of the drug in pocket-size intestine# To go desired concentration of the drug in small intestine # To retard the assimilation of the drug.# To retard the absorption of the drug. Pharmaclogy & Pharmacotherapeutics, Satokar, 1997, p5
  106. 106. SR PreparationsSR Preparations SR = TR = XLSR = TR = XL Sustained release or time release preparationsSustained release or time release preparations for oral usefor oral employ # Release the active drug over an extended# Release the active drug over an extended catamenia of time.menses of time. # Particles of drug covered with coatings# Particles of drug covered with coatings which deliquesce at different time intervals.which dissolve at different time intervals. Pharmacology & Pharmacotherapeutics, Satokar, 1997, p5
  107. 107. Basic pharmacology - Agenda #Classification of Drugs #Routes of administration & drug formulations #A.D.Thousand.Due east. #Dose regimes & plasma levels #Package insert information #Scheduling of drugs #Pharmacodynamics #Drug uses & ADR #Clinical pharmacology
  108. 108. Indian pharmacopoeia: Legal issues, Storage of various drugs 08/23/18 Mr.Dipti South. Chapter 2-108
  109. 109. Indian Pharmacopeia • The central drug potency is based in Nirman bhavan, New Delhi. • It is the body which is controlled past the govt. for manufacturing, auction, import and export of drugs. • The drug dominance of state is mostly based on their capitals. • The central drug authorisation formulate the policies and authorisation of land follows and implement the policies. 08/23/18 Mr.Dipti S. Chapter two-109
  110. 110. Implementation is under the control of drug controller. 1. Informational Bureau: Information technology include Drug technical advisory board (DTAB) and drug consultative committee (DCC). They frames and modify rules regarding drugs. 2. Belittling Agency: Information technology includes central drug laboratory (situated at Kolkata) and drug laboratories in respective state, these laboratories examination, analyse the sample of drugs and cosmetics. 08/23/xviii Mr.Dipti S. Chapter two-110
  111. 111. 3. Executive Agency: Authorities which grants license to various organizations for manufacturing, storing, recapping, selling, importing and exporting drugs. 08/23/eighteen Mr.Dipti South. Affiliate 2-111
  112. 112. Scheduling of medicines • Scheduling based on potential effects on the trunk :the molecule, and it'due south concentration Expressed with an 'S' and a number 7 schedule classes. • Unscheduled - tin can be sold through any outlet. • S2 upwards only in pharmacies • S1 and S2 - do not require a prescription • S3 upwardly must be sold with a prescription by a pharmacist or doctor • S5 upwards is highly controlled • Schedule 6 &seven are kept under lock and cardinal, the prescription cannot be repeated • Schedules viii and 9 - banned substances
  113. 113. Scheduling of drugs • S1 –Miscellaneous • S2 –Analgesics, Flu preparations, Antihistamines, Anticholinergics • S3 –Non-steroidal anti-inflammatories, Anti- hypertensives, Topical steroid preparations, Anti-diabetic medicine, The Pill • S4 –Antibiotics, Hormones, Steroid anti- inflammatory medicines, statins
  114. 114. Scheduling of drugs • S5 –Psychotropic drugs, e.g anti-depressants, sleeping tablets, tranquilisers • S6 –Anorexigenics, Short-acting barbiturates, Opoid drugs • S7 –Opoid drugs • S8,S9 –Prohibited except for research due east.m. heroin, LSD, cannabis (dagga)
  115. 115. Storage and Maintenance of Drugs
  116. 116. • The Drugs which are supplied to ward are stored in drug cupboards to provide a uniform supply of drugs to the patients. • The drugs are stocked in containers, such equally boxes and on flexible racks and shelves etc. • Information technology must be ensure that drugs which are stored remain preserved during their storage. • There should not be any damage due to high temperature or exposure to sunlight. • The drugs are to exist stored as per the prescribed weather of their storage. Introduction
  117. 117. • The drugs stored in a drug store exist arranged in such a fashion that they are easily traceable as and when required. one.According to pharmacological activeness 2.Alphabetically Introduction - contd
  118. 118. Drug Storage 1. Proper drug storage ii. Storage Environment 3. Organisation of drugs on shelves iv. The storeroom five. The dispensary
  119. 119. Drugs are stored in a particularly designed secure area or space of a building in order to: • Avoid contamination or deterioration, • Avoid disfiguration of labels, • Maintain integrity of packaging and so guarantee quality and say-so of drugs during shelf life, • Prevent or reduce pilferage, theft or losses, • Prevent infestation of pests and vermin. i. Proper drug storage
  120. 120. • The storage should non hinder the cleaning and should have sufficient space for movement of stocks and handling. • Products are to be stored in a manner that prevents impairment due to excessive vertical stacking heights and not to exceed eight stacks. • Store the products as per production storage status (Equally per label) to prevent deterioration of finished product on storage. • Monitor and record the temperature of storage expanse on daily basis.
  121. 121. The storage environment should possess the post-obit: • Adequate temperature, • Sufficient lighting, • Make clean atmospheric condition, • Humidity control, • Cold storage facilities, • Adequate shelving to ensure integrity of the stored drugs. two. Storage Surroundings
  122. 122. • Drugs to exist stored under condition that prevent contamination & every bit far as possible, deterioration. • "Well closed container" precautions to be taken in relation to the effects of the atmosphere, moisture, heat &light. • "Protected from moisture" means that the product is to be "stored in air tight container" Storage and Maintenance
  123. 123. • "Protected from light" the product is to be stored either in a container fabricated of cloth that absorbs actinic light sufficiently to protect the contents from alter induced by such light. Protected from low-cal
  124. 124. • In a deep freeze (-xv°C) • In a refrigerator 2°C -8°C • Cold or cool 8°C-fifteen°C • Room temperature15°C-25°C Temperature
  125. 125. • The Storage area must be free from unsanitary conditions(Ex Rodents, insects, Birds, litter etc). • The flooring of the warehouse should be fabricated of difficult flooring (Concrete /Kota/Epoxy) and must exist in a good land of repair and appearance at all times. • The floors are kept make clean and free of trash, dirt, sippage h2o, drain water etc. • The expanse must be kept clean and gratuitous of turn down. Storage Premises
  126. 126. • The area used for storage of Four fluids should take adequate space and to forbid exposure to direct sunlight. • Secured surface area availability for damaged, rejected and expired goods. • Ensure adequate pest control program in identify and shall exist carried out at a minimum frequency of a year. • The Pest control shall cover treatment for Termite and Rodents. Storage Premises
  127. 127. • Shelves should be made of steel or treated wood. • Shelves should be strong. • Drugs are bundled in alphabetical order of generic names. • Each dosage form of drug is arranged in separate and distinct areas. • Sufficient empty space should demarcate one drug or dosage form from another. 127 three. Arrangement of drugs on shelves
  128. 128. • Virtually recently received drugs are placed behind old stock on the shelf except where new drugs have shorter expiration dates. • Always put lids properly on tins e'er and at the close of the day.
  129. 129. • Put drugs in a dry place protected from light and heat. • Store liquids on a pallet on the floor or on the lowest shelf. • The store must be cleaned daily and mopped at to the lowest degree once a calendar week.
  130. 130. • A well-arranged shop enables easy identification of drugs and saves time when picking a drug from the shelves. • This helps remove drugs quickly and makes for easy inventory command. iv. The store-room
  131. 131. • The rule of Start IN FIRST OUT (FIFO) should be practical always. • Then, drugs that were received kickoff should be used first, except where the new stock has shorter expiration dates than the old stock. • In this regard, the principle of Beginning TO EXPIRE Outset OUT (FEFO) should apply. • To accept admission to drugs with shorter expiration dates offset, put these in front of the shelves. • Those with longer expiration dates should be placed behind those with shorter dates.
  132. 132. five. The dispensary • Make clean afterward each use tablet counters and place inside easy reach on the table. • Avoid dispensing wrong drugs by arranging drugs on the table in alphabetical guild so that the drug being dispensed is not dislocated with some other. • E'er shut drug containers from which drugs are not being dispensed to prevent spillage or dispensing the wrong drug.
  133. 133. • Shelf life- the time where a given product stored under reasonable condition, is expected to remain stable (>ninety%authorization) • Essential drugs- drugs that satisfy the health care needs of the majority of the population. • Essential drugs should there fore available at all times in adequate amounts & in appropriate dosage forms. Drug death
  134. 134. • Medications must not exist administered, and products and equipment must non be used beyond their decease dates. • All medical equipment, dressings and solutions used during invasive procedures must be sterile. • Single-use devices are meant for single use merely and must not be re-used. Expiry dates
  135. 135. • All drugs, including samples, should exist maintained carve up from non-medications in a locked chiffonier which is sufficiently secure to deny access to unauthorized persons. • Key should be available only to authorized personnel who are assigned medication-related responsibilities. • Store medications that are "for external employ only" dissever from medications intended for internal apply. Storage, Maintenance & Security
  136. 136. • Store expect-alike and sound-alike drugs separately. • Maintain temperature between 59 caste and 86 degrees Fahrenheit for not-refrigerated medications. • Where refrigeration is necessary use a "Medications Just" refrigerator and maintain temperature between 36 degrees and 46 degrees Fahrenheit. Storage, Maintenance & Security
  137. 137. • On daily basis check, verify and certificate the proper temperature. • All multiple-dose injectable medications should be initialed and accept the date of commencement entry recorded on the characterization. • Rotate medication stock monthly employing a "FIFO" (first in/offset out) process. Storage, Maintenance & Security
  138. 138. • Double Locked Container Controlled Drug Regulations
  139. 139. • 2 licensed personnel count (or verify whatsoever discrepancies) every shift (8 hours) • Witness to all discards • Record on Control Substance Sheet all administrations and wastes. Controlled Drug Regulations
  140. 140. All details must be completed in the Doctors own handwriting, like: • Name of drug • Dose of drug • Number of doses or length of class • Signature of prescribing dr. and date Controlled Drugs
  141. 141. Storage of Controlled Drugs • They must be kept in a locked cabinet or cupboard • The keys to the chiffonier must be in the possession of an authorised person • Authorised person, refers to Ward Managing director or deputy who must be a Trained Nurse or Midwife • Students should not exist responsible for the controlled drug cupboard keys
  142. 142. • Records in the form of CONTROLLED DRUG REGISTERS must be kept • Each drug must have its ain specified page which is Headed with the Drugs name and Strength • The Number of Ampoules of a drug must exist entered and updated with every use. Recording of Controlled Drug Utilize
  143. 143. • Must record: – Date – Time – Dose of every administration – Proper noun of receiving patient/customer – Number of ampoules at get-go and finish of assistants Entry must be signed by 2 people one of who must be registered No alterations must be fabricated to the entry All entries must be in Blackness Ink Recording of Controlled Drug Use
  144. 144. Rational employ of drugs & Adding of drug dosage 08/23/18 Mr.Dipti Due south. Chapter 2-144
  145. 145. Rational apply of drugs • Any drug is made with help of combination or mixture of the chemicals which some times harm to the other parts of body. • Rational use: Eg. Patient is having hypertension then the goal is to reduce blood pressure to the normal level in order to forbid prolonged hypertension, thus creating complication. • Once identifying the person suffering from specific disease, the dr. or nurse should discover out other factors contribution the sick result of the prescribed drug.08/23/18 Mr.Dipti S. Chapter 2-145
  146. 146. • Any drug required good renal or hepatic organisation to pass drug and to be drain out or metabolize in the body. • The choice of drug has to exist make wisely by the doctor or nurse to avoid side effects, drug interaction, contraindication. • Nurse should follow the 6 Rights of drug assistants to avert incorrect administration of drug. • Utilise of combination drug tin exist one option in treatment, eg. Ibufen (Brufen+Paracetamol) 08/23/18 Mr.Dipti South. Chapter two-146
  147. 147. Conclusion Rational use of drugs requires that the patients receiving medications appropriate to their clinical needs, in does that meet their own requirement of an acceptable period for time and at everyman cost to them and their community. 08/23/xviii Mr.Dipti S. Chapter two-147
  148. 148. Drug Calculations (Ref. Another slide) 08/23/eighteen Mr.Dipti Southward. Chapter two-148
  149. 149. Pharmacotherapeutics: Principles of therapeutics 08/23/xviii Mr.Dipti S. Chapter 2-149
  150. 150. Drug – WHO scientific group definition Any substance or production that is used/ intended to exist used to alter or explore physiological systems or pathological systems or pathological states for the benefit of the recipient Whatsoever substance or product that is used/ intended to exist used to modify or explore physiological systems or pathological systems or pathological states for the benefit of the recipient
  151. 151. Pharmacology PharmacodynamicsPharmacodynamics - Biological and therapeutic effects of drugs pharmacokinetics - Absorption, Distribution, Metabolism & Excretion of drugs
  152. 152. The Relationship between Pharmacokinetic and Pharmacodynamic processes Pharmaco kineticsDrug is excreted Drug is excreted Drug is taken Drug is absorbed into the blood Stream & is available for apportionment Drug is absorbed into the blood Stream & is bachelor for circulation Drug is metabolised Drug is metabolised Drug is concentrated at the site of action Drug is concentrated at the site of activeness Pharmacological effectPharmacological event Clinical responseClinical response EfficacyEfficacySide effectsSide furnishings Pharmaco dynamics
  153. 153. Drug – and – patient related factors. • Drug and patient related factors determined the option of routes for drug administration. These are: • Characteristics of the drug. • Emergency/ Routine use. • Condition of the patient ( Unconscious, Vomiting and Diarrhoea) • Age of patient. • Associated disease. • Patients/ Doctors choice (Sometimes) 08/23/eighteen Mr.Dipti S. Affiliate 2-153
  154. 154. 08/23/18 Pharmacology Unit 1 Course Session 1Pharmacology 154
  155. 155. Pharmacokinetics # AAbsorption # DDistribution # MMetabolism # EExcretion # AAbsorption # DDistribution # MMetabolism # EExcretion
  156. 156. Basic pharmacology - Agenda • Definitions • Classification of Drugs • Routes of administration & drug formulations • Dose regimes & plasma levels • Package insert information • Scheduling of drugs • Pharmacodynamics
  157. 157. Bundle insert information (Literature) • Composition (drug/dose per tablet) • Schedule • Pharmacological classification • Pharmacological action • Indications • Contra-indications • Dosage & directions for use • Side effects & special precautions • Known symptoms of overdose & particulars of its treatment • Identification (physical description of tablet) • Presentation (package details) • Storage instructions • Registration number • Name of applicant
  158. 158. Pharmacodynamics: Mechanisms of Action The ways past which drugs tin produce therapeutic effects: • One time the drug is at the site of action, it can modify the rate (increase or decrease) at which the cells or tissues function. • A drug cannot make a cell or tissue perform a function it was not designed to perform. Chapter two-158Mr.Dipti S.08/23/18
  159. 159. Pharmacodynamics • The effect the drug has on the body • Based on either: – Non-specific action – Binding with a receptor –Enzyme interaction • The effect the drug has on the torso • Based on either: – Non-specific action – Binding with a receptor –Enzyme interaction
  160. 160. Pharmacodynamics # Non-specific activeness depends on the drug'southward accumulation in jail cell membranes # Specific deportment result from the drug becoming affixed to the receptor i.eastward. binding to receptors # Drugs can simply increase or decrease jail cell role - they cannot totally alter the action of the specific cell # Non-specific action depends on the drug'due south accumulation in cell membranes # Specific actions result from the drug becoming affixed to the receptor i.e. binding to receptors # Drugs can only increase or decrease cell function - they cannot totally change the action of the specific prison cell
  161. 161. Mechanism of Action Mechanism of action Cell membranceCell membrance Clinical Pharmacology,Laurence;1997: pg 7812 Metabolic processes Within the cells Metabolic processes Inside the cells Outside the cellOutside the cell
  162. 162. Prison cell Membrance # Specific receptors-agonists and antagonists on adrenoceptors # Interference with selective passage of ions across membracnes eg: Calcium channel blockers # Specific receptors-agonists and antagonists on adrenoceptors # Interference with selective passage of ions across membracnes eg: Calcium channel blockers
  163. 163. Outside the prison cell # Direct chemical interaction eg: chelating agents, antacids # Osmosis with diuretics similar mannitol # Direct chemical interaction eg: chelating agents, antacids # Osmosis with diuretics like mannitol
  164. 164. Receptor # Protein macromolecules # Agonist to receptor proteins alter induces changes within cell response to drug # Agonists : activate receptors # Antagonists : blockers of receptors # Protein macromolecules # Agonist to receptor proteins change induces changes inside cell response to drug # Agonists : activate receptors # Antagonists : blockers of receptors Clinical Oharmacology, Laurence; 1997, pg:78
  165. 165. Condiment Effect When the full pharmacological action of 2 or more drugs administered together Is equivalent to the summation of their Indicidual pharmacological deportment Eg: ephedrine + aminophylline in handling of bronchial asthma When the total pharmacological activeness of Two or more drugs administered together Is equivalent to the summation of their Indicidual pharmacological actions Eg: ephedrine + aminophylline in treatment of bronchial asthma Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg 45 1 + 1 = 2
  166. 166. Synergistic effect When the full pharmacological activeness of Ii or more drugs administered together Is more the summation of their individual pharmacological actions Eg: cotrimoxazole(sulphamthoxazole +pyrimethamine) Septran When the total pharmacological action of Two or more than drugs administered together Is more than than the summation of their individual pharmacological deportment Eg: cotrimoxazole(sulphamthoxazole +pyrimethamine) Septran Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg 45 1 + ane=10 (>ii)
  167. 167. Terminology # Bioavailability –the extent of the drug which is delivered to the circulation (expressed as %) # Bioequivalence –the rate and extent of absorption of two products is equivalent - 'no pregnant departure' # Bioavailability –the extent of the drug which is delivered to the circulation (expressed equally %) # Bioequivalence –the rate and extent of absorption of ii products is equivalent - 'no meaning difference'
  168. 168. Drug uses # Curative, as primary therapy (bacterial / parasitic infections), or auxilary therapy (anaesthetics, ergometrine and oxytocin in obstetrics) # Suppressive of disease/symptoms, used continuely or intermittently to maintain health with out attaining cure as in hypertension, diabetes, epilepsy, asthama/ to control symptoms such as pain and coughing, while awaiting recovery from crusade # Preventive (prophylactic), as when a not- allowed person enters a malarial area or contraception
  169. 169. Using more than than one drug simultaneously Possible responses: – The drugs have no effect on each other – Animosity - the combination results in a lower response than when either is given on its own – Potentiation - the response rate of the 2 drugs when combined is more than than the sum of their independent response rates – Synergy - the combination offers greater effect than the sum of the ii products given individually I.e. one+i=3 or more – Globally there is a move away from polypharmacy Possible responses: – The drugs take no effect on each other – Antagonism - the combination results in a lower response than when either is given on its own – Potentiation - the response rate of the two drugs when combined is more than the sum of their independent response rates – Synergy - the combination offers greater effect than the sum of the ii products given individually I.e. i+i=3 or more – Globally there is a motion away from polypharmacy
  170. 170. Adverse Drug Reaction (ADR) An adverse reaction is a harmful or seriously unpleasant effect acquired by a drug at doses intended for therapeutic outcome/prophylaxis/ diagnosis which warrants reduction of dose/ withdrawal of the drug and/or foretells hazard from future administration
  171. 171. Degrees of certainty of (ADR) Definite : time from taking drug is reasonable result corresponds to what is known of drug event ceases on stopping drug even returns on restarting drug Likely: time sequence reasonable corresponds to what is known of drug ceases on stopping drug non reasonably explanined past patient'southward disease
  172. 172. Degrees of certainty of (ADR) Possible : time sequence reasonable corresponds to what is known of drug could be due to disease / other therapy Conditional : time sequence reasonable corresponds not to what is known of drug cannot be explained by patients disease Doubtful : event not meeting above criteria
  173. 173. Anaphylaxis Systemic reaction in a sensitized human bailiwick following repeat injection of a drug like penicillin characterized by laryngeal edema, severe bronchospasm leading to asphyxia, or circulatory plummet. Eg: Penicillin Pharmacology & Pharmacotherapeutics, Satoskar;1997: pg 35
  174. 174. Clinical Pharmacology # Scientific study of drug in human being # Provides facts for – - Improving treatment of patients - Understanding drugs - Agreement furnishings of drugs in different historic period groups
  175. 175. Clinical Pharmacology #Stage I(pharmacokinetic, dose, safety) #Phase II(safety & efficacy in Small population) #Phase 3 (safety & efficacy in big population) #Phase IV (Mail service-marketing Study, safety in special population & new indication)
  176. 176. Clinical Pharmacology Clinical Trial # Randomized # Non randomized # Controlled # Open # Cross over
  177. 177. Placebo # Latin – "I will delight" # Placebo are used for two purposes : - Equally a control in scientific evaluation of drugs - To benefit or delight a patient not by any pharmacological actions, but by psychological ways
  178. 178. Therapeutic evaluations Whether a drug is of value and how information technology may Best exist used : a) formal therapeutic trials b) surveillance studies for both efficacy and adverse effects
  179. 179. Patient Compliance # Patient takes prescribed drug # Failure due to : one) Non comprehension of instructions a) Inadequacy of doctor b) Inadequacy of patient 2) Comprehension, but failure to behave out instructions
  180. 180. Factors for Noncompliance Disease – Regimen – Source of Medicine – Doctor / Patient Relation – Patient - # Psychiatric diagnosis # Complexity # Long elapsing # Time wasting # Inconvenient clinics # Inadequate supervision # Patient dissatisfaction # Inappropriate health beliefs
  181. 181. References 1. Dr. P.K. Panwar, Essentials of pharmacology for nurses, AITBS pub. 2017, India, Pg no. 1 – 9. 2. Dr. Suresh grand sharma, Textbook of pharmacology, pathology & genetics for nurses, Jaypee pub. 2016 Bharat Pg no 5 – 22. iii. Tara v. Shanbhag, Smita shenoy, Pharmacology preparation transmission for undergraduate, Elsevier pub. 2014. Pg no. 1 – 45. 4. Marilyn Herbert – Ashton, Nancy Clarkson, Pharmacology, Jones & Barlet pub 2010 India, Pg no 1-two. five. Madhuri Inamdar, Pharmacology in nursing, Vora medical pub. 2006 India 1st edition, Pg no i – 13.
  182. 182. Thanks 08/23/xviii Mr.Dipti S. Chapter ii-182
  183. 183. Drugs " Poisons in small doses are the best medicines; and useful medicines simply in besides large doses they are poisonous" Willam Withering (1741 – 1799) MD, FRS

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