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PHARMACOLOGY 1


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[Front]


The study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes
[Back]


PHARMACOLOGY

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PHARMACOLOGY 1 - Details

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Two General Principles (PHARMACOLOGY)
1 All substances can under circumstances be toxic, and the chemicals in botanicals are no different from chemicals in manufactured drugs except for the proportion of impurities 2 All dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies
POWER PLANT:
1 Alkaloids 2 Glycosides 3 Gums 4 Resins 5 Oils
Animal Magnetism Drugs obtained from animal sources
1 hormones such as insulin 2 oils and fats (usually fixed) - cod liver oil 3 enzymes - pancreatin and pepsin 4 vaccines
Mineral Springs: __
• Iron • Iodine • Epsom salt
Routes of Administration
• buccal, sublingual, translingual • gastric • intradermal • intramuscular • intravenous • oral • rectal and vaginal • respiratory • subcutaneous • topical
The Physical Nature of Drugs
• Solid - Aspirin, Atropine • Liquid - Nicotine, Ethanol • Gaseous - Nitrous Oxide
Drug Size, SMALLEST and LARGEST
1 Smallest -- Lithium ion (MW 7) 2 Largest -- Alteplase (MW 59,050) 3 Most drugs -- MW 100-1000
Three major types of bonds
1 covalent, 2 electrostatic and 3 hydrophobic
Must undergo extensive animal studies
IND - Investigational New Drug
Exceptions to the Rule
1 Public health threat of disease like AIDS, COVID-19 2 Sponsors of drugs that reach phase II or III clinical trials can apply for FDA approval of treatment IND status
LADMERS
• Liberation of an active ingredient from the dosage form • Absorption into systemic circulation • Distribution • Metabolism in the body • Excretion of the drug from the body • Response
Factors influencing absorption
1 Effect of pH on drug absorption 2 Blood flow to the absorption site 3 Total surface area available for absorption 4 Contact time at the absorption surface
Factors Influencing Bioavailability
1 First-pass Hepatic Metabolism 2 Solubility of the drug 3 Chemical instability 4 Nature of the drug formulation
What are the Special Barriers to Distribution?
1 Placental (most small molecular weight drugs cross the placental barrier; fetal blood levels are usually lower than maternal) 2 Blood-brain (permeable only to lipid-soluble drugs or those of very low molecular weight)
Plasma concentration is a function of
– the rate of input of the drug (by absorption) into the plasma – the rate of distribution – and the rate of elimination
Pharmacokinetics TWO BASIC PARAMETERS
1 CLEARANCE 2 VOLUME OF DISTRIBUTION
The ratio of the amount of drug in the body to the drug concentration in the plasma or blood
Volume of distribution -Can be affected by liver and kidney disease
METABOLISM OF DRUGS Three major routes:
– Hepatic metabolism – Biliary metabolism – Urinary metabolism
Metabolism (Biotransformation) PHASES
1) Phase I (Functionalization) – Redox Reactions and hydrolysis. 2) Phase II (Conjugation) – Attacks certain drugs with existing functional groups and attaches conjugate molecules
Metabolism (Biotransformation) May be affected by
• Drug Interactions due to inducers, inhibitors, and substrates • Genetic factors • Disease states DRUG WITH INDUCER - FASTER DRUGS WITH INHIBITOR - SLOWER
EXCRETION; Renal elimination of drugs:
– Glomerular filtration – Proximal tubular secretion – Distal tubular reabsorption
Excretion process
1 Glomerular filtration of water and unbound drugs and metabolites 2 Active tubular secretion of acidic and basic drugs and metabolites 3 Active reabsorption of acidic and basic endogenous compounds and passive reabsorption of lipophilic drugs 4 Urinary excretion of drugs and metabolites that are filtered and or actively secreted and not reabsorbed
Controls Cl- channels
GABAA-receptor complex (CLASS 1)
G-proteins: __
1) Gs 2) Gi 3) Gq
CLASS III example
• Epidermal growth factor • Atrial natriuretic peptide • Insulin