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Analgesics. Sandy Kulkarni. 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. Classification of Analgesics. Analgesics. Strong Analgesics.

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analgesics

Analgesics

Sandy Kulkarni

analgesics1
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
classification of analgesics
Classification of Analgesics

Analgesics

Strong

Analgesics

Mild

Analgesics

Opium

Aspirin

Ibuprofen

Heroin

Codeine

Acetaminophen

mild analgesics
Mild Analgesics
  • Mild Analgesics include over-the-counter pain relievers and fever depressants.
  • Examples of mild analgesics include Aspirin, acetaminophen, and ibuprofen
aspirin
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

aspirin1
Aspirin
  • 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
aspirin2
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.
aspirin3
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
side effects of aspirin
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 Reye’s syndrome
other mild analgesics
Other Mild Analgesics
  • Acetaminophen (Paracetamol)
    • Commonly sold as Tylenol
  • Ibuprofen
    • Commonly sold under the name Advil
acetaminophen
Acetaminophen
  • Acetaminophen is a pain reducer, such as Tylenol but does not reduce inflammation
  • When taken at recommended doses, it has negligible side effects
  • It’s low level side effects make it favorable to arthritis patients and children
  • Overuse and overdoses can lead to acute liver failure and kidney damage
ibuprofen
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
strong analgesics
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
morphine
Morphine
  • Naturally occurring in the poppy- Only needs to be isolated
  • Very strong pain reliever but also very addictive (2nd to Heroin)
  • Usually injected but can be smoked, sniffed or swallowed
  • Commonly used in hospitals
  • Large illegal street culture
codeine
Codeine
  • Most commonly used strong analgesic
  • Similar to Morphine except for the replacement of a (OH-) group for (OCH3) group
  • Commonly used with Tylenol as a more mild analgesic
  • 1/6 as strong as Morphine and less addictive
heroin
Heroin
  • Originally sold as cough suppressant and pain killer10 times stronger than Morphine
  • Incredibly addictive (many times, other strong analgesics are needed for withdrawal)
heroin1
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.
other synthetic strong analgesics
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
synthetic strong analgesics opioids
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.
demerol
Demerol
  • Demerol (Meperidine)
  • Used for moderate to severe pain and to stop muscle spasms.
  • Usually injected or taken orally.
methadone
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.
mechanism of strong analgesics
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.
mechanism of strong analgesics cont
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.
side effects of strong analgesics
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.
local anesthetics cocaine
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

history of cocaine
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)
cocaine
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
clinical action
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
effects of cocaine
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
derivatives of cocaine
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
procaine novacaine
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

lidocaine
Lidocaine
  • Sodium channel blocker
  • Administered parenterally for ventricular arrhythmias, subcutaneously for minor surgical procedures, and topically to mucosal surfaces prior to invasive procedures