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Subject: Pharmacology Topic: Nature, Sources and Dosage Forms of Drugs Lecturer: Dr.

Deo Panganiban Date of Lecture: 06/17/2011 Transcriptionist: Group 21 Pages: 3

NATURE, SOURCES, & DOSAGE FORMS OF DRUGS

What are drugs:


o o o o Cure or arrest diseases Relieve symptoms Ease pain Vitamins and minerals to correct deficiency syndromes e.g: Vit C for scurvy

pharmacologic/chemical action when elaborated identified the chemical which can be used for pharmacology testing pharmacologic drug used approval (BFAD, FDA) marketing **we must know the generic name (chemical name of drug). o Testing y Safety: animal and human tests - (Clinical Trials) actual human use either sick or wellhealth. y Effectivity: Double blind tests (good basic tests) - Experimenter & experimentee both of them do not know which drug was given - Effects coming in monitor observe effects of drugs purpose: to eliminate bias Healthy and ill patients y Healthy subjects: to know what happens to the drug when given to a normal person with normal physiologic functions. y Ill patient: Will that person relieved the signs and symptoms? is the target disease cured? y Determines parameter of effectivity of the drug: How effective is a drug to an ill or to a healthy person? Approval (Food & Drug Administration) : y risks are weighed - It is approved for specific persons - i.e Precautions to pregnant & pediatric patients Marketing - Brand or trade name memorize the generic names universal, chemical name of the drug

Substances upon which a person may become dependent (there are classes of drugs which can cause dependency, when a person takes it and becomes tolerant and need more dose become more dependent, whether psychological or physical dependency) Mild stimulants (caffeine) Behavior or mood altering agents (anxiolytics) {may true form some persons, may cause stimulation or really mood altering ease anxiety (anxiolytics cause sedation}

Where drugs come from:


Originally, our ancestors used Herbalism o Herbalism (pharmacognosy)  Botanical e.g: sambong , diuretic (urinate some more); relieve UTI and lower Blood pressure.  Animals o Laboratory synthetic drugs come from y Chemical process e.g: penicillin - fungus from penicillium; was found out to heal the wounds of some soldiers in WWI DRUG DEVELOPMENT Drug Development: 3 phases Phase 1: get the lead compound Phase 2: Give to animals or non-animals (bacteria) Phase 3: The effects of drugs to small laboratories y Genetic engineering latest trend (pharmacobiotechnology)  to produce newer drugs;  drugs which are resistant to other fungi and bacteria (pharmacobiotechnology) i.e. Pfizer vs. Unilab

Drug Classification
o Specific Names: y General term y Brand name y Chemical name Generic terms: y Some of drugs can group together due to Chemical similarity: e.g: Calcium channel Blockers; Narcotics y Use: e.g: antidepressants (different drug groups but they have one use) y Biological effect: e.g: antipyretics(lower fever) -paracetamol, acetaminophen, aspirin

Developing and Marketing


o Molecular tincturing or elaboration Plant take anecdotes from people who used the plant effects of plant when taking up in raw elaborate chemicals from plant find out which part has

SY 2011-2012
1

Legal y Over-the-counter (OTC) you can buy it without the need for prescription y Prescription - need Rx of licensed Medical Doctor  Narcotics  CNS stimulants/depressants  Drugs causing serious complications: Steroids  Gluthathione: antioxidant

PHASE II METABOLITES y Products of these processes y May have chemical activities of their own Excretion y Inactive products of metabolism y Via the: Urine or feces (major route) Sweat/tears/saliva (minor route) Breathe (exhaled-minor route)

4 BASIC STAGES
o o Absorption y Main absorptive site: Small intestines (larger component which has larger absorption) y Biggest hurdle of a drug must overtake, especially if the drug taken orall. If Intravenous it has special parameter, it can directly go to the bloodstream. y ORAL drugs: take effect under special blood vessel leading from digestive tract to the liver (hepatic first pass effects) IV drugs: directly go to circulation; most of it doesn't go to liver for metabolism. y FIRST-PASS EFFECT: hepatic effect; metabolic enzymes in the liver destroy large amounts of the drug introduced (drugs taken orally) Distribution y circulation through bloodstream y Bloodstream (most often) distributes the drug throughout the body y S/E: occurs when drugs have an effect in an organ OTHER THAN the target organ  e.g: Sildenafil (Viagra) used for Hypertension but wasn't y ideal because of sudden decrease of BP y Influenced by many factors  Proteins Binded proteins: lesser effect than usual  Fat molecules Drugs destined for the CNS y Drugs destined for the CNS: (Brain and spinal cord) y Blood-brain barrier - impenetrable  Different barriers: Drugs: go directly to brain, intraspinal (get directly to CNS), intrathecal: to bypass the barrier Metabolism y Transformed to non toxic forms or active forms y Important Organ: Liver have effect y Drugs broken down y Diazepam - has a metabolite (methyldiazepam) - to make effect longer than parent drug for 6 hours or longer. y 2 steps in the LIVER: PHASE I ENZYMES y Break molecules into smaller ones y Link small molecules into long chains

NATURE OF DRUGS
First discovered in Modern technology 1880: Claude Bernard (French physiologist) y Discovered how CURARE works: plant extract that paralyzes muscle; used by South American Indians to poison arrow tips y NEUROTRANSMITTERS chemical messengers y AGONISTS - a molecule which triggers the response when encountering a cell e.g: Muscular contraction of hormone release y Instead of acetylcholine, curare occupies the receptor in postsynaptic surface

AGONIST-RECEPTOR INTERACTION
y Most medicines exert their effort by making physical contact with the receptors on the cell surface. A key fitting into lock (wrong key no reaction) RECEPTORS - critical role AGONISTS - open "cellular locks" -First step in communication between the outside of a cell and the inside. ANTAGONISTS o Drugs that act to COMPETE with natural agonists but act as decoys: freezing up receptors and preventing agonists' use of receptors. -Many drugs are ANTAGONISTS: blocks cell responses or designed to blunt over-active cellular response. i.e Calcium blockers jrise in blood pressure jIncrease in heart rate

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MOLECULAR SHAPE
The key to agonists fitting snugly into their receptors (does not occupy other receptors) o BROAD EFFECTS: Molecules FIT into receptors on MANY different kinds of cells o S/E: Can result from a drug encountering y receptors other than target site Major goal: reduce side effects y o

SOURCES OF DRUGS
y TERRESTIAL o Plants large percentage of drugs come from o Animals

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MARINE o Plants -Animals (seashells in the seashore) GENES OR CHEMISTRY Source of drugs: 60% (world pop) rely on plants for medicine Plants supply active ingredients for traditional medicine Leads: consistently successful ideas for new drugs natural products from plants & organism Lead Compounds = chemicals that have desirable properties in lab tests

DRUGS FROM ANIMALS


y y y y SNAKES/reptiles = anti-venoms you used the reptile venom to produce anti-venoms HORSES = equine vaccines cause allergies, anaphylaxis. PIGS = porcine hormones DUCK EMBRYO = vaccines

OCEAN MEDICINES
y Baldomero Olivera o Discovered PRAILT - from a cone snail found in the Phil jams nerve transmission in the SC and blocks certain pain signals from reaching the brain. y Conotoxins : exciting new leads more than 500 species of cone snails in the Philippines.

Bacteria
y Uncanny ability to protect or defend themselves against antibiotics; now a days, due to Modern Medicine bacteria seem to develop own natural defenses MDRs Multi Drug Resistant Pumps (MDRs) o Virtually all living things have MDRs o In humans: o Brain, GIT, liver & kidneys Bacterial ejection system pumps o Found in cell wall of the bacteria o monitors incoming chemicals o SPITS out chemicals that endanger the bacteria

CHEMISTRY & GENETICS


y COMBINATIONAL GENETICS: to custommake products that DO NOT even exists in nature.

Multi-drug Resistance Pumps(MDRs)


o o Virtually ALL living things have MDRs In humans : can frustrate efforts to get drug where they need to go: Chemotherapy drugs often kicked out of cancer cells by MDRs in the cell membranes MDRs in brain, digestive tract, liver and kidneys- perform important jobs in moving natural body molecules eg. Hormones, in and out of cells.

Chemists -turning plant and marine natural products, found in minute quantities, into useful medicines o 1 ton of caribbean sea sponge = 1 g of YONDELIS y Elias J. Corey - deciphered DNA to synthesize 1 g of Yondelis y Combinational Genetics: o To custom make products that DO NOT even exist in nature y Genetic instructions are REMOVED for entire metabolic pathways from certain microorganisms, ALTER the instructions, then PUT them back = generates NEW and different NATURAL products. y

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DRUGS FROM PLANTS


y EVOLUTION: plants produce chemicals that block bacterial MDR pumps. (plants are taken in and block bacterial compounds) Kim Lewis (Northeastern University in Boston) o Genetically knocked out MDR pump from S. aureus o Exposed the altered bacteria to a weak antibiotic: Berberine from barberry plants o Proved LETHAL for Staph. Aureus without the MDR pumps PERIWINKLE or CHICHIRICA= Vincristine anticancer drug WILLOW TREE (Bark) = Aspirin for pain, headache, active ingredient ACH CHINCHONA = Quinine used as antimalaria PACIFIC YEW = Taxol for breast Cancer found in pacific islands and in Phil, in mountainous region GUGGUL TREE = Guggulsterone steroidal FEVERFEW = Parthenolide POPPY PLANT = opium, Heroin main producer: Afghanistan MEADOW SAFFRON = Colchicine for gout

Then you will have success if you are careful to observe the decrees and laws that the LORD gave Moses for Israel. Be strong and courageous. Do not be afraid or discouraged.
1 Chronicles 22:13

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