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GENERAL PRINCIPLES http://crisbertcualteros.page.tl
GENERAL PRINCIPLES ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
PHARMACOKINETICS ,[object Object],[object Object],[object Object],[object Object]
FACTORS AFFECTING ABSORPTION ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
FACTORS AFFECTING ABSORPTION ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
DEGREE OF IONIZATION ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
FORMULA ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
EX OF WEAK ACID WITH PKA OF 8 ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
EXAMPLE OF A WEAK BASE WITH PKA OF 8 ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
ROUTES OF ADMINISTRATION ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
DISTRIBUTION OF DRUGS ,[object Object],[object Object],[object Object],[object Object],[object Object]
METABOLISM/ BIOTRANSFORMATION  OF DRUGS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
PHASE I METABOLISM ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
PHASE I METABOLISM ,[object Object],[object Object],[object Object],[object Object],[object Object]
PHASE II METABOLISM ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
DRUG METABOLISM ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
DRUG METABOLISM ,[object Object],[object Object],[object Object],[object Object],[object Object]
EXCRETION ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
QUANTITATIVE PHARMACOKINETICS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
DOSAGE REGIMEN ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
PHARMACODYNAMICS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
PHARMACODYNAMICS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
TARGET FOR DRUG ACTION ,[object Object],[object Object],[object Object],[object Object]
 
RECEPTORS Agonist Antagonist Beta adrenoreceptor Norepi- nephrine Propranolol Opiate (mu) Morphine Naloxone Dopamine (D2) Dopamine Bromocrip- tine Chlorpro- mazine Insulin insulin None known Estrogen receptors Ethinyl- estradiol Tamoxifen
ENZYMES INHIBITORS FALSE SUBSTRATE Cyclooxy- genase Aspirin Carbonic Anhydrase Acetazola- Mide Dihydrofolate reductase trimetoprin Monoamine oxidase B Selegiline Angiotensin convering enzymes Captopril
ION CHANNELS BLOCKERS MODULATORS Renal tubule Sodium channels Amiloride Aldosterone ATP sensitive K +  channels ATP Cromokalin sulfonylureas GABA gated chloride channels Picrotoxin Benzodiazepines Voltage gated Ca  ++ channels Divalent cations Beta-adrenoreceptor agonists
CARRIERS INHIBITORS FALSE SUBSTRATE Na + K + Cl co  transporter Loop diuretics Na  + K +   pump Cardiac glycosides Proton pump Omeprazole Weak acid carrier(renal tubule) Probenecid
OVERVIEW OF PRODUCT DEVELOPMENT Lead  Compound Efficacy Selectivity Mechanism Phase 1 Phase  2 Phase  3 Drug metabolism, safety assessment Phase  4 In vitro studies  Animal Studies Clinical Testing Marketing 0   2    4  8 – 9  20  YEARS
Thank You! ,[object Object],[object Object]

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General Principles in Pharmacology

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  • 25. RECEPTORS Agonist Antagonist Beta adrenoreceptor Norepi- nephrine Propranolol Opiate (mu) Morphine Naloxone Dopamine (D2) Dopamine Bromocrip- tine Chlorpro- mazine Insulin insulin None known Estrogen receptors Ethinyl- estradiol Tamoxifen
  • 26. ENZYMES INHIBITORS FALSE SUBSTRATE Cyclooxy- genase Aspirin Carbonic Anhydrase Acetazola- Mide Dihydrofolate reductase trimetoprin Monoamine oxidase B Selegiline Angiotensin convering enzymes Captopril
  • 27. ION CHANNELS BLOCKERS MODULATORS Renal tubule Sodium channels Amiloride Aldosterone ATP sensitive K + channels ATP Cromokalin sulfonylureas GABA gated chloride channels Picrotoxin Benzodiazepines Voltage gated Ca ++ channels Divalent cations Beta-adrenoreceptor agonists
  • 28. CARRIERS INHIBITORS FALSE SUBSTRATE Na + K + Cl co transporter Loop diuretics Na + K + pump Cardiac glycosides Proton pump Omeprazole Weak acid carrier(renal tubule) Probenecid
  • 29. OVERVIEW OF PRODUCT DEVELOPMENT Lead Compound Efficacy Selectivity Mechanism Phase 1 Phase 2 Phase 3 Drug metabolism, safety assessment Phase 4 In vitro studies Animal Studies Clinical Testing Marketing 0 2 4 8 – 9 20 YEARS
  • 30.