Click to edit Master subtitle style Katie Chan

Medicines and Drugs

2/27/13

Click to edit Master subtitle style

Pharmaceutical Products

2/27/13

Natural Defense Systems of the Human Body

Human body can suffer breakdowns

through injury, genetics or environment, age, ect.

Attacking microorganisms = invaders Bodys responses = lines of defense Symptoms responses of the body to

invading organisms

Medicines work by supplementing our

natural healing processes

2/27/13

Non-specific Defense Mechanisms

Specific Defense Mechanisms

First line of defense: barriers to prevent entry skin mucous membranes closures and secretions of natural openings such as lips, eyelids, ear wax, ect.

Second line of defense: attack invaders

Third line of defense: Immune system

white blood cells white blood cells engulf produce specific invaders proteins (phagocytosis) (antibodies) to blood clotting to recognize and prevent blood destroy invaders loss and further memory cells invasions enable the body to inflammatory fight a repeat response invasion of the same 2/27/13 organism

Medicines vs. Drugs

Drug chemical that affects how the

body works
Medicine substance that improves

health
Can be natural or synthetic Synthetic medicines can contain non-

active ingredients that affect presentation of drug medicine

Therapeutic effect beneficial effect of

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Drug Effects on the Body

Alteration of the physiological state
Consciousness, activity level & coordination

Alteration of incoming sensory

sensations

Alteration of mood or emotions Most drugs have more than 1 effect,

which make them hard to classify

Target nervous system & brain; including

perception of stimuli ((analgesics, stimulants, depressants))

Target metabolic processes ((anatacids)) 2/27/13

Placebo Effect
Placebo effect patient receive

therapeutic & healing effects from pharmacologically inert medicines believe its the real drug
Brain scans show that patients who

believed they were taking pain meds release opiods/natural pain relief
1/3 of control group taking placebo

show some improvements

2/27/13

Administration of Drugs
Drug delivery depends on chemical

nature of drug, condition of patient & most effective way of getting drug to target organ
Ex. some chemicals (like insulin)

decompose by digestive enzymes in gut cannot be administered as pills, but injected directly into blood
2/27/13

Method of Administrating Drug Oral

Description

Example

Taken by mouth Tablets, capsules, pills, liquids Vapor breathed in; smoking Medications for respiratory conditions (ex. asthma); some drug abuses (nicotine & cocaine) Absorbed directly Some hormone from the skin into treatments, blood nicotine patch Inserted into the Treatment of 2/27/13 rectum digestive

Inhalation

Skin patches

Suppositories

Physiological Effects of Drugs

Are complex because the drug can

interact in many ways

Depend on dosage Therapeutic effect intended

physiological effect
Side effects - unintended physiological

effect
Vary between different drugs Vary between same drug & different people Can be beneficial or benign or cause 2/27/13

Physiological Effects (Cont)

Dosing regime amount of drug used

for each dose & frequency of administration

Variables: age, sex, weight of patient, diet,

environment, other drugs taken

Ideally, dosage should result in constant

levels of drug in blood (through continuous intravenous drip)

Therapeutic Window concentration in

bloodstream must be between therapeutic level & toxic level

Tolerance repeated dose of drug result

2/27/13 in smaller physiological effect

Research and Development

Goal: develop drugs to be more

effective & with fewer toxic side effects goes into drugs for obesity, depression, cancer, cardiovascular disease & ulcers b/c market can support cost 10-12 yrs

Very costly; large amount of research

Average development time for drugs:

2/27/13

Discovery Research (Yr 03)

Lead compounds compounds shown

to have biological activity; first stage in drug development is to identify and extract these
Often low levels of activity; often derived

from plants

Analogues - chemically related

compounds to lead compounds; next step: synthesis of analogues

combinatorial chemistry & high-

throughput screening enable production & testing vast medicines in 2/27/13

Development Research(Yr 39)

Phase 1: 50-100 healthy volunteers Phase 2: 200-400 patients Phase 3: 3000+ patients; half are

placebos

Year 11: launch product; post-marketing

monitoring: collect adverse drug reaction data

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Antacids

2/27/13

Acidity in the Stomach

Gastro-intestinal tract (gut) generates &

maintains different pH environments

Plays an important role in controlling the

activity of digestive enzymes

Stomach generates a pH as low as 1-2

by producing hydrochloric acid from

structure from gastric glands (lining of the walls)

Acid not only kills ingested bacteria

from food but also provides optimum environment for digestive enzymes
2/27/13

Acidity (Cont)
Excess acidity is potentially harmful Gastric juice acidic production
Excess production is caused by excess

alcohol, smoking, stress and some antiinflammatory drugs

Problems with gastric juice:

Acid indigestion feeling of discomfort from

too much acid in the stomach

Heartburn (acid reflux) acid from the

stomach rising into the oesophagus

Ulcer damage to the lining of stomach

wall, resulting loss of tissue and2/27/13

Antacids

Antacids excess acid

Drugs help combat antacids by neutralizing

the hydrochloric acid to relieve symptoms

Antacids are usually weak basic

compounds

Often metal oxides or hydroxides,

carbonates or hydrogen-carbonates
React with acid to produce salt and water Does not directly coat ulcers or induce

healing but they do allow stomach lining to mend

Because antacids can change2/27/13pH in the

Antacids (Cont)
Aluminum hydroxide Al(OH)3
Al(OH)3(s) + 3HCl(aq) AlCl3(aq) +

3H2O(l)
Dissolve more slowly and tend to provide

longer lasting relief (than magnesium)

Linked to development of Alzheimers

Magnesium hydroxide Mg(OH)2

Mg(OH)2(s) + 2HCl(aq) MgCl2(aq) +

2H2O(l)

Magnesium salts tend to be faster acting

2/27/13

Antacids (Cont)
Antacids with metal carbonates and

hydrogen carbonates react with acid to produce a salt, water and carbon dioxide bloating

Antifoaming agents are used to avert

Sodium hydrogen carbonate NaHCO3
NaHCO3(aq) + HCl(aq) NaCl(aq) + H2O(l)

+ CO2

Calcium carbonate CaCO3

CaCO3(s) + 2HCl(aq) CaCl2(aq) + H2O(l) 2/27/13

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Analgesics

2/27/13

General
Analgesics painkillers d drugs to

relieve pain
Pain receptors nerve messages of the

brain that detect pain as a sensation

Prostaglandins chemicals that

stimulate the pain receptors

Released from cells damaged by thermal,

mechanical or chemical energy

Inflammatory response cause dilation

(widening) of blood vessels near site of injury; can lead to swelling and increased pain 2/27/13

Mild Analgesics
Prevent stimulation of the nerve endings

at the site of pain

Release prostaglandins from the site of

injury; give relief to inflammation, fever & pain interfere with the functioning of the brain inflammatory drugs (NSAIDs) (ex. ibuprofen)

Non-narcotics analgesics that do not

Includes aspirin and non-steroidal anti-

Paracetamol (acetaminophen)
Reduces production of prostaglandins in the 2/27/13

Mild Analgesics Aspirin

Works by blocking the synthesis of

prostaglandins

Aspirin analgesic that was an ester

derived from salicylic acid

More tasty & less irritable in the stomach

than salicylic acid (which was proved to be effective for pain) & sore throats; reduces fever (antipyretic) & inflammation; provide relief from rheumatic pain & arthritis

Widely used to treat headaches, toothaches

Available in many formations w/ various

2/27/13 coatings & buffering components

Aspirin
Analgesic properties (painkiller) Antipyretic property (reduces fever) Reduces inflammation Side-effects Yes Yes Yes

Paracetamol
Yes Yes No

Stomach wall irritant, Does not irritate stomach blood anti-coagulant, can wall reduce colon cancer

Severe side-effects (over- Reyes syndrome (rare Serious kidney, liver & potentially fatal liver & brain brain damage dosage) disorder) in children Synergistic effect w/ alcohol Allergic reactions Recommended use for children Increased risk of stomach Toxic-side effects can be bleeding increased Relatively common Rare No; can cause Reyes Yes syndrome (although baby aspirin is available)

2/27/13

 Bind opioid receptors in the brain; which then

Strong Analgesics

blocks the transmission of pain signals between brain cells

Alters perception of pain Narcotics analgesics act on the brain and may

cause drowsiness & change in behavior/mood

Most effective painkillers for severe pain Side-effects: suppressing cough reflex,

constipation, constriction of pupil in eye, narcotic effects

Morphine heroin: etherification reaction; both OH

Codeine, morphine & heroin (diamorphine)

groups converted into ethanoate (ester) groups by 2/27/13 reaction w/ ethanoic acid CH3COOH; loss of 2 polar

Codeine Effective Increasing strength as analgesics ness Function Benzene ring, ether (2), alkene, alcohol al groups (1), tertiary amine Obtained Raw opium (0.5%) form
Preparation w/ a Therape non-narcotic drug utic uses (aspirin or

Morphine
Increasing narcotic effects

Diamorphine
Increasing side-effects

Benzene ring, ether, Benzene ring, ether, alkene, alcohol (2), alkene, ester-ethanoate tertiary amine (2), tertiary amine Raw opium (10%) Found in opium but usually obtained by reaction of morphine (semi-synthetic drug)

Used medically only in a few countries legally for relief of severe pain Most rapidly acting and paracetamol) in 2nd Habit forming can stage of pain most abused narcotic management ladder lead to dependence Initially produces Cough medications; use must be euphoric effects, but Short-term regulated by very high potential for treatment of diarrhea medical professional causing addiction & increasing tolerance Dependence leads to withdrawal symptoms & 2/27/13 many associated

Management of severe pain (& advanced cancer)

Narcotic Effects

Heroin induces feeling of euphoria, as it

causes a dulling of pain & a lessening of fear & tension constipation, reduced libido, loss of appetite & poor nutrition relatively quickly; cannot function properly w/o drug; suffer from withdrawal (sweating, anxiety); tolerance
2/27/13

Long-term regular use leads to

Heroin users show dependence

Drug taken by injection infections

Different analgesics work by blocking pain at different sites

Could be argued that
mild analgesics seek to eliminate pain at

the source

Strong analgesics only alter our ability to

perceive pain

Analgesic ladder pain management as

pain persists or increases

1. Use mild analgesics

2. Add a weak opioid (ex. codeine or

tramadol)
2/27/13 3. In severe intractable pain, use strong

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Depressants

2/27/13

General

Act on brain and spinal cord Neurotransmitters

concentration/activity of chemicals
Altered to change communication between

brain cells
Result: cause a depression or decrease in

brain activity that influences functions of Dosage Low High Extremely other body parts Moderate High Include drugs Slurred Dosage Calmness classified as Respiratory tranquilizers, sedatives & hypnotics effect Relief from speech depression anxiety Staggering Coma Very relaxed gait death 2/27/13 muscles Altered

Ethanol (C2H5OH) Uses

Has some antiseptic properties

Most widely used psychoactive drug

Used on skin before injection or to clean

small wounds

Effect of hardening on skin

Rubbed on feet to prevent blisters

Ethanol in alcoholic drinks

Low doses can create mild excitement;

users become more confident, talkative & relaxed

Low doses might have beneficial effect 2/27/13

Ethanol (C2H5OH) Abuses

Short-term
Change in behavior; more adverse as dose increases

Long-term effects
Dependence: alcoholism Liver disease (cirrhosis),

Loss of self-restraint;

effects

concentration, memory & insight are impaired

Loss of balance & judgment Violent behavior associated

liver cancer
Coronary heart disease High blood pressure Fetal alcohol syndrome Permanent brain damage

w/ domestic abuse & family breakdown

Dangerous risk-taking

behavior leading to many accidents involving motor vehicles & machinery

Dehydration caused by

increased urine output leading to hangover & loss

2/27/13

Ethanol (C2H5OH) Metabolism

Dissolvable in lipids b/c small organic

Polar OH group enables it to form hydrogen bonds w/ water readily soluble in aqueous solution

molecule

Can cross cell membrane easily Indigestion: C2H5OH passes quickly from

gut to blood & circulates to all tissues of the body

90% is broken down in the liver;

remainder eliminated by kidneys & lungs 2/27/13

Synergistic effect of ethanol

Synergy potential to increase activity

of other drugs when taken at the same time

Can lead to fatal results Examples
W/ aspirin stomach bleeding & risk of

ulcers
W/ depressants heavy sedation, possibly

coma
W/ tobacco cancers
2/27/13

Ethanol Detection

Ethanol analysis of breath

At body temp in lung, ethanol is dissolved in

the blood & is released into the air in exhaled breath

Breathalyzer - orange potassium

dichromate (VI) turns green chromium (III) Cr3+ as they oxidize the ethanol to ethanal & ethanoic acid; color change measured on photocell

Infrared spectroscopy; intoximeter

more accurate breath analysis

Different molecules have different

absorption bands in infrared part of 2/27/13 spectrum; cause vibrations

Ethanol Detection(Cont)
Fuel cell different version of

intoximeter

W/ catalyst, ethanol is oxidized in air first to

ethanoic acid and then to water & carbon dioxide

Fuel cell converts energy released when

oxidation occurs into detectable electrical voltage & measure concentration

Ethanol analysis in blood & urine: Gas-

liquid chromatography

Blood/urine is vaporized & injected into

stream of inert gas over surface of nonvolatile liquid 2/27/13

Other Depressants

Benzodiazepines Depresses activity in

part of the brain that controls emotion

used as tranquilizers in treatment of anxiety

disorders & related insomnia

Used as sleeping pills & muscle relaxants Dependence; mostly used for short term-

treatments
Contain benzene rings & diazepine structure

(7 membered heterocyclic ring w/ C & 2 N atoms); largely non-polar high lipid solubility cross blood-brain barrier

Anti-depressant fluoxetine

hydrochloride (Prozac)

2/27/13

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Stimulus

2/27/13

General

Affect nervous system Functions opposite to depressants

increase activity of brain & state of mental alertness

Prevent excessive drowsiness & allow

greater concentration
Physiological effects
Help facilitate breathing by relaxing air

passages; treatment of respiratory infections (ex. bronchitis)

May reduce appetite; treatment of obesity

2/27/13 May cause palpitations or tremors

Amphetamines
Adrenaline (epinephrine) hormone

released in times of stress & enables body to cope w/ sudden demands imposed by pain, shock, fear, cold, ect.
Increase heart rate & blood pressure Increase blood flow to brain & muscles Increase air flow to the lungs Increase mental awareness

Noradrenaline (norepinephrine) a

neurotransmitter responsible for communication in part of nervous system known as sympathetic nervous 2/27/13

Amphetamines (Cont)

Amphetamine stimulant that mimics

& enhances adrenaline & noradrenaline effects

Similar structure to adrenaline &

noradrenaline

Dervied from

CH2CH2NH3
ethyl amine

Phenyl

Sympathomimetic stimulating 2/27/13

Amphetamines
Side-effects
Dilation of pupils of they eyes Decreased appetite Possible blurred vision & dizziness Long-term: depression & reduced resistance

to infection

Regular use leads to tolerance &

dependence

Designer drugs modifications to the

amphetamine structure are very powerful & dangerous

2/27/13 Methamphetamine (crystal meth) & ecstasy

Nicotine

Most widespread & abused stimulant Obtained from tobacco plants; also

found in tomato, potato, green pepper & eggplant

Taken by inhalation (or chewing) of

smoke from cigarettes, cigars & pipe tobacco

Contain noxious components: tar & carbon

monoxide

Lipid soluble molecule can cross

blood-brain barrier & bring rapid effects on brain activity

2/27/13

Nicotine (Cont)
Short-term effects of Increases
Adverse effects on pregnancy and cancers of the lung, mouth & throat

Long-term effects of Nicotine High blood

Nicotine concentration Consumption Relieves tension and boredom

Helps counter

Consumption pressure heart disease (including angina)

Increases risk of

fatigue
Increases heart

Chronic lung

disease
Coronary 2/27/13

rate & blood

Caffeine

Worlds most widely used stimulant Present in coffee, tea, chocolate & colas Reduce physical fatigue & restore

mental alertness

Acts of small Effect as a respiratory stimulant Effect of large

increasing consumption rate of energy release within consumption cells Enhancement of Can cause anxiety, mental energy, irritability & insomnia Intensifies & prolongs effects of Can cause dependence alertness & ability to adrenaline Withdrawal: headaches concentrate Acts a diuretic, & nausea increasing volume of urine; can cause 2/27/13 dehydration

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Antibacterials

2/27/13

Penicillins - antibacterial agent Antibiotics chemicals that act against

General

other microorganisms; usually produced by microorganisms

Penicillin G

Inhibits development of cross-links in

bacterial cell walls, so weakening walls & causing bacteria to rupture & 2/27/13 die during

Antibiotic Resistance
Bacterial resistance major problem w/

use of penicillin; penicillin proved to be ineffective against some populations of bacteria resistant bacteria
render inactive

Penicillinase enzyme produced by

Can open pencillins 4-membered ring &

Arises by genetic mutation in bacteria

# of resistant organisms increases

dramatically w/ increased exposure to 2/27/13 antibiotic

Antibiotic Resistance (Cont)

Responses to challenge of antibiotic

resistance:

Developing different forms of penicillin, w/

modified side chains able to withstand action of penicillinase legislation to make them prescription-only drugs; encourage doctors not to overprescribe

Controlling & restricting use of antibiotics by

Patient Compliance: education &

encouragement of patience is important to complete the full course of treatment w/ antibiotic 2/27/13

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AntiVirals

2/27/13

Viruses
cells

Viruses take over functioning of other

Small & simple structure; no cellular structure Contain only protein & nucleic acid Only capable of reproducing inside another

living cell

Viral diseases: measles, meningitis, polio,

AIDS, avian flu

Treating viral infections is a challenge b/c

viruses live w/in cells & cannot be easily targeted

Cannot be attacked by antibiotics: lack 2/27/13

Viruses (Cont)

Antibodies vaccination for a virus

Helped w/ cholera, polio, measles, smallpox

Some antivirals work by altering the cells

DNA so virus cannot use it to multiply activity w/in host cell (prevents reproduction)

Antivirals could also block enzyme

Just because virus halted & relieved from

symptoms doesnt mean it hasnt completely eradicated from body

Amantadine antiviral that causes

changes in the cell membrane 2/27/13 that

AIDS: a viral pandemic

caused by virus HIV (human

AIDS (acquired immune deficiency

syndrome) failure in immune system

immunodeficiency virus)
Infection spreads at alarming rate through

global population

CD4+T cells vital white blood cells in

immune system HIV; primarily infects by binding to specific receptor proteins on surface & then penetrating the cell form of RNA rather than DNA (HIV is a 2/27/13 retrovirus)

Retrovirus having its genetic material in

AIDS (Cont)

HIV is a retrovirus, it releases its RNA in

the cell and enzyme reverse transcriptase

HIV DNA integrates into the cells own

DNA and replicates with it when the cell divides cell and are released in large numbers when cell dies

Viral particles are produced w/in the host

3 main reasons why its so hard to target:

Virus destroys T helper cells (cells in immune

system that defend the body against it)

2/27/13

AIDS (Cont)
fight HIV

Antiretroviral drugs drugs that help

Inhibits the enzyme reverse transcriptase so

virus does not affect host cell

Does not destroy HIV infection but delays

progression
Prevent mother to child transmission of HIV

during pregnancy
Block the binding of HIV to cell membranes or

to inhibit the assembly of new viral particles w/in cell

These also produce side effects

2/27/13