Transcript of Sandy Kulkarni. Analgesics Analgesics are common pain relievers. Many analgesics also have...
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- Sandy Kulkarni
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- Analgesics Analgesics are common pain relievers. Many
analgesics also have antipyretic properties as well. They can be
used to reduce fever Some analgesics are also anti- inflammatory
drugs as well
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- Classification of Analgesics Aspirin Heroin Codeine Opium
Ibuprofen Acetaminophen Mild Analgesics Strong Analgesics
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- Mild Analgesics Mild Analgesics include over-the-counter pain
relievers and fever depressants. Examples of mild analgesics
include Aspirin, acetaminophen, and ibuprofen
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- Aspirin Aspirin is a derivative of salicyclic acid Salicyclic
acid was found in the bark of the willow tree and was used as a
pain reliever and as a way to relieve fever symptoms of malaria
Salicyclic Acid Aspirin
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- In 1899, Felix Hoffman, a chemist from the Bayer Company,
developed a low-cost process to synthesize an ethanoate ester of
salicyclic acid, called aspirin In the synthesis of Aspirin, the
ethanoic acid forms an ester with the alcohol group on the second
carbon
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- Aspirin Aspirin is believed to inhibit the enzyme,
Prostaglandin synthase which is formed at the site of an injury.
This inhibits the production of prostaglandins which produce fever
and swelling as well as transmitting pain signals to the
brain.
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- Aspirin Aspirin is able to reduce pain and fevers and dilate
blood vessels Aspirin enlarges blood vessels which helps prevent
blood clots. This vasodilation of the surface blood vessels also
allows an increase of heat released which lowers the temperature of
a fever Aspirin is also taken to prevent recurring heart attacks It
may also be effective in preventing prostrate cancer
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- Side Effects of Aspirin Aspirin can irritate the stomach lining
which may lead to ulcers If aspirin is used over long periods of
time, it may lead to problems with blood clotting An overdose on
aspirin, such as the case with some arthritis sufferers, may lead
to dizziness, ringing in the ears, gastrointestinal problems,
mental confusion, and bleeding. Some people are allergic to aspirin
leading to bronchial asthma In children under 12 Aspirin has been
linked to Reyes syndrome
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- Other Mild Analgesics Acetaminophen (Paracetamol) Commonly sold
as Tylenol Ibuprofen Commonly sold under the name Advil
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- Acetaminophen Acetaminophen is a pain reducer, such as Tylenol
but does not reduce inflammation When taken at recommended doses,
it has negligible side effects Its low level side effects make it
favorable to arthritis patients and children Overuse and overdoses
can lead to acute liver failure and kidney damage
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- Ibuprofen Ibuprofen is a more powerful pain reliever than
aspirin in high doses, but is inferior for anti-inflammation Side
effects include gastrointestinal bleeding and irritation Can
aggravate kidney problems
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- Strong Analgesics Only Available by prescription Used to
relieve severe pain associated with injuries, heart attacks, or
chronic diseases such as cancer Most strong analgesics are derived
from the opium poppy or synthetically produced Basically three
types: Natural, semi-synthetic, and synthetic
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- Morphine Naturally occurring in the poppy- Only needs to be
isolated Very strong pain reliever but also very addictive (2 nd to
Heroin) Usually injected but can be smoked, sniffed or swallowed
Commonly used in hospitals Large illegal street culture
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- Codeine Most commonly used strong analgesic Similar to Morphine
except for the replacement of a (OH-) group for (OCH 3 ) group
Commonly used with Tylenol as a more mild analgesic 1/6 as strong
as Morphine and less addictive
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- Heroin Originally sold as cough suppressant and pain killer10
times stronger than Morphine Incredibly addictive (many times,
other strong analgesics are needed for withdrawal)
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- Heroin Synthesized from morphine in a esterification reaction
with acetyl chloride It is absorbed by the brain very quickly
resulting in a potent high Many other problems are associated with
heroin addiction including as prostitution and AIDS.
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- Other Synthetic Strong Analgesics Vicodin Is solution of
acetaminophen and hydrocodone (the latter being the stronger)
Hydrocodone is addictive and can cause highs. Usually taken orally
Stronger than codeine but not as strong than Morphine
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- Synthetic Strong Analgesics (Opioids) The active area of
morphine has been identified and can be synthesized. This has
produced many synthetic analgesics and has allowed scientists to
eliminate some of the harmful side effects of more natural
analgesics.
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- Demerol Demerol (Meperidine) Used for moderate to severe pain
and to stop muscle spasms. Usually injected or taken orally.
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- Methadone Compared to most strong analgesics it is weaker. Has
been synthesized to not have euphoric properties and mild
withdrawal effects but is still addictive. Used as an analgesic but
most commonly to help in the withdrawal for Heroin addicts.
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- Mechanism of Strong Analgesics The human body contains natural
opiates in the brain called endorphins These are produced in the
body during extreme conditions such as running high and extreme
injuries. When these are absorbed by receptors in the brain the
body feels analgesia and the pain is reduced.
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- Mechanism of Strong Analgesics cont. Opiates derived from the
poppy act in the same way as endorphins but are not natural to the
human body. The high is produced because of the absorption of
opiates is quicker than endorphins Drugs such as naloxone act to
fill the receptors in the brain but are not analgesics and thus are
used to prevent overdoses on analgesics. Endorphins are not used as
analgesics because the cannot be stored and are unstable.
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- Side Effects of Strong Analgesics Short term Dulling of Pain
Euphoria Slow Nervous system Slowed heart rate Loss of cough reflex
Nausea Overdoses can lead to death Possibility of stroke Overall
slowdown of biological systems Long Term Addiction and very strong
withdrawal effects Constipation Loss of libido Disruptions in
menstruation Cross-tolerance Loss of appetite Problems associated
with buying street drugs i.e. sharing needles AIDS and
prostitution.
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- Local Anesthetics -- Cocaine Cocaine used in 1885 as a local
anesthetic. Extracted from the plant Erythoxylum coco
([1R-(exo,exo)]-3-(Benzoyloxy)-8-methyl-8-
azabicyclo[3.2.1]octane-2-carboxylic acid methyl ester
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- History of Cocaine Coca leaves have been chewed by South
American Indians for thousands of years. There were used to induce
feelings of euphoria Was banned by Spanish settlers in the 1500s
but the ban was repealed when it became apparent that slaves worked
harder while on it United States cocaine was used in soft drinks
until it was classified as narcotic in 1914 Clinically used as a
local anaesthetic for eye operations and in modified synthetic
forms for dental treatment (novocaine) and sore throats
(benzocaine)
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- Cocaine The leaves of the coca plant contain 0.6% - 1.8%
alkaloidal cocaine To extract, cocaine leaves are soaked in
kerosene and sulfuric acid HCl is added creating cocaine
hydrochloride, which can be extracted as powdery flakes or
rocks
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- Clinical Action Acts as a reuptake blocker for the monoamines
dopamine, norepinephrine and serotonin interacts with serotonin and
muscarinic acetylcholine receptors and the sodium channels
influence on the axonal voltage-gated sodium channels that provides
cocaine's local anaesthetic properties
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- Effects of Cocaine Subjective Euphoria Increased sociability
Increased energy Hyper vigilance Physiological Increased heart rate
Increased respiration rate Increased body temperature Increased
blood pressure Pupil dilation
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- Derivatives of Cocaine Cocaine is too addictive and in
appropriate for medicinal use Two derivatives of cocaine are widely
used as local anesthetics Procaine or Novacaine Lidocaine
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- Procaine (Novacaine) Principal use in dentistry for temporary
numbing of mouth area First synthesized in 1905 and was the first
injectable man-made local anesthetic Restricts blood vessels,
reducing bleeding Novacaine
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- Lidocaine Sodium channel blocker Administered parenterally for
ventricular arrhythmias, subcutaneously for minor surgical
procedures, and topically to mucosal surfaces prior to invasive
procedures