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Analgesics

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

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  1. Analgesics Sandy Kulkarni

  2. 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

  3. Classification of Analgesics Analgesics Strong Analgesics Mild Analgesics Opium Aspirin Ibuprofen Heroin Codeine Acetaminophen

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

  5. 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

  6. 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

  7. 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.

  8. 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

  9. 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

  10. Other Mild Analgesics • Acetaminophen (Paracetamol) • Commonly sold as Tylenol • Ibuprofen • Commonly sold under the name Advil

  11. 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

  12. 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

  13. 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

  14. 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

  15. 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

  16. Heroin • Originally sold as cough suppressant and pain killer10 times stronger than Morphine • Incredibly addictive (many times, other strong analgesics are needed for withdrawal)

  17. 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.

  18. 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

  19. 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.

  20. Demerol • Demerol (Meperidine) • Used for moderate to severe pain and to stop muscle spasms. • Usually injected or taken orally.

  21. 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.

  22. 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.

  23. 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.

  24. 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.

  25. 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

  26. 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)

  27. 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

  28. 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

  29. 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

  30. 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

  31. 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

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

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