Diverse classes of solutions and their activities Iain G. Jack 4 th February 2011Slide 2
Content of today\'s address How would we be able to order tranquilizes? How do drugs bring about their belongings? Particular receptors: bolt & key Non-particular impacts PharmacokineticsSlide 3
Introduction What is a medication? Any organically dynamic compound that does not happen actually in the human body that can influence living proceduresSlide 4
sixteenth century Egypt Ebers papyrus Poppy juniper berries beer lead swine teeth goose oil reptile\'s blood jackass hooves squashed valuable stones excreta from different creatures somewhat light historySlide 5
Where do drugs originate from now? Plants : Digoxin (foxglove) Belladonna (dangerous nightshade) Diamorphine (opium poppy) Animal tissue : Insulin, development hormone Synthetic fabricate : Most current medicationsSlide 6
Names of medications Chemical name: depicts the compound structure: acetyl-p-amino-phenol Generic name: a name that can be utilized by anybody: paracetamol Trade name: possessed by the manufacturer: CalpolSlide 7
Other approaches to sort drugs What sort of atom is it? What organ framework (or what infection) is it for? e.g., heart, psychotropic What parts of cells are influenced?Slide 8
What is the medication utilized for? To cure e.g., contaminations, growth To smother sicknesses or side effects without accomplishing a cure e.g., hypertension, diabetes, torment control To anticipate malady (prophylactic) e.g., inoculationSlide 9
How does the medication demonstration? Supplant an insufficiency , e.g., vitamins, minerals, hormones Interfere with cell work , e.g., square catalyst activity Kill/avert development of infections, microorganisms, organisms, protozoa, tumorSlide 10
Categories of medication Anti-incendiary Analgesic Antipyretic Vaccine Antihypertensive Vitamin supplement Antitussive Antiviral Antifungal Antibiotic Anesthetic Surfactant LaxativeSlide 11
Content of today\'s address How would we be able to sort drugs? How do drugs bring about their belongings? Particular receptors: bolt & key Non-particular impacts PharmacokineticsSlide 12
How do drugs work? Pharmacodynamics: investigation of how chemicals apply their belongings The functional significance of this is empowering the plan of new and better medicationsSlide 13
receptor Receptors are proteins on the phone surface or inside the phone. They tie the body\'s own particular substance courier chemicals Convert the coupling occasion to a flag that the phone can perceive and react to flagSlide 14
"Bolt & Key" Interaction between a receptor and its flag particle ( ligand) resembles "bolt & key". Consummate fit relies on upon correct 3D shape and size of both atoms.Slide 15
medicate receptor Receptors Drugs additionally convey data to cells by fitting into a similar receptor atoms. The medication picks the bolt and triggers a reaction by the cell .Slide 16
Cannabinoid receptor Where? Surface of mind cells and cells of stomach related framework and resistant framework What for? Ordinary cerebrum work and sound hunger So what? THC picks the bolt.Slide 17
Agonists and Antagonists Agonist: a medication that fits into a receptor and actuates a reaction e.g., morphine, nicotine Antagonist: a medication that fits into a receptor however obstructs the receptor and does not enact a reaction. ??? new against stoutness medicate: opponent to cannabinoid receptorSlide 18
Content of today\'s address How would we be able to classify drugs? How do drugs bring about their belongings? Particular receptors: bolt & key Non-particular impacts PharmacokineticsSlide 19
Non-particular impacts Acidic or basic properties Surfactant properties (amphotericin) Osmotic properties (intestinal medicines, diuretics) Interactions with film lipids (soporifics)Slide 20
Side-impacts and different impacts Not the "needed" impact e.g. headache medicine causes gastric ulcer Diphenhydramine has a helpful symptomSlide 21
Side-impacts and different impacts Hypersensitivity/sensitivity: overstated antagonistic response to medicate Toxic impacts e.g., Thalidomide: teratogenic Tolerance: expanding sums are expected to create a similar impactSlide 22
Content of today\'s address How would we be able to classify drugs? How do drugs bring about their belongings? Particular receptors: bolt & key Non-particular impacts PharmacokineticsSlide 23
Pharmacokinetics How the body manages the medication We have to consider: Dose Route of Administration Absorption and dispersion Metabolism and dischargeSlide 24
Dose: measure of medication taken at any one time Aim is to give the patient a dosage of medication that accomplishes the coveted impact without creating unsafe symptoms Therapeutic Index (TI) is the proportion of the restorative measurement to the poisonous measurement E.g\'s. of medications with low TI incorporate digoxin, lithium and methotrexateSlide 25
Administration Route of organization relies on upon: How simple it is to use for patient The substance make-up of the medication How rapidly a medication needs to achieve site of activity Where it needs to work in the bodySlide 26
Intravenous Routes of Administration Inhaled Oral Transdermal Subcutaneous or intramuscular infusion Topical RectalSlide 27
Oral Route Medications taken by mouth Formulated in either a strong or fluid frame Absorbed from the GI tract for the most part in the small digestive system which is specific for retention (extensive surface region because of villi and microvilli) .Slide 28
Disadvantages Onset of activity is moderately moderate Absorption might be sporadic Some medications wrecked by chemicals or different discharges found in GI tract Because blood from GI tract goes through liver it is liable to hepatic digestion system before achieving systemic flowSlide 29
Buccal Route Drug is detailed as a tablet or a splash and is consumed from the buccal cavity Sublingual retention quick onset of activity yet length is short Buccal assimilation speedy onset of activity that is of longer span than sublingual courseSlide 30
Rectal Route Drugs planned as fluids ,strong measurements and semi solids. The picked readiness is embedded into the rectum where it is discharged to give neighborhood impact or assimilated to give a systemic impactSlide 31
Disadvantages Absorption sporadic and capricious Less advantageous than oral course Low patient worthiness Rectal & Vaginal Route Advantages Can be utilized when oral course unacceptable Useful when medication causes GI bothering Can be utilized for nearby activitySlide 32
Advantages Drugs breathed in through the nose or mouth to create nearby or systemic impacts Drug measurements required to create coveted impact is much littler than oral course thusly decrease in symptoms Inhalation Route Used predominately in the treatment of asthma Drugs conveyed specifically to their site of activity ie lungsSlide 33
Topical Route Skin utilized as site of organization Lotions ,creams ,balms, powders Skin has characteristic obstruction work yet particular dose frames have been created that when connected they permit the medication to go through and deliver systemic impactSlide 34
Parenteral Route (tranquilizes that are given by infusion) IV course - drugs infused straightforwardly into the systemic flow (quick onset of activity) Subcutaneous course - drugs infused into the s/c layer of the skin (simplest and minimum difficult) Intramuscular course –drugs infused into muscle layersSlide 35
Examples in every classificationSlide 36
ADME A bsorption: the instrument by which a medication enters the body D istribution: the medication is transported all through the body M etabolism: the medication associates with, and is handled by, the body E limination: the medication is expelled from the bodySlide 37
Absorption Disintegration Dissolution Direct retention at site of activity, e.g., in the gutSlide 38
Steps in circulation Drug must spread all through blood volume Drug must escape the circulatory system between or through endothelial cells Drug must cross the phone film into cellsSlide 39
Factors a ffecting d istribution Binding to plasma proteins : if a medication is bound to vast plasma proteins , it will be not able get out as the proteins are too huge . Arggh! I can\'t fit through!Slide 40
Factors a ffecting d istribution Extent of blood supply. On the off chance that a tissue is very much perfused with blood , sedate s will arrive quicker. Advertisement ipose tissue has low bloo d perfusion so tranquilizes achieve it gradually .Slide 41
Factors a ffecting d istribution pH . A medication will go through layer s better in the event that it is not ionized Binding of medications to other tissue partsSlide 42
Lethal Dose Injected Dose Drug Concentration Therapeutic Range Oral Dose Sub-Therapeutic Time Metabolism: what happens to a medicationSlide 43
F irst pass impact A ll supplements and medications retained from the gut go in the blood specifically to the liver. The liver separates many medications so they are inactivated before they ever enter the systemic dissemination ! This can diminish medicate conveyance to target tissues But a few medications are initiated by the primary pass impactSlide 44
Elimination Mainly in the kidney. Likewise bile, gut, lung, bosom drain. End of a medication is generally connected to renal capacity.Slide 45
Individual variety Each individual is one of a kind how they react to a medication Age and sex (hormonal contrasts) Weight: a few medications are put away in fat so less successful and longer enduring in stout individuals Allergy Kidney & liver capacity: by what means will they influence disposal?
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