Analgesic and antipyretic drug

Overview of these drug. About Pain & Fever and Mechanisms of Action with Binding Receptor. Also have Pain scale, Choice of Drug and Their Side Effect, Adverse Effect. About Misuse of These Drug & Management

1. Analgesic and Antipyretic Drug UNIVERSITY OF DEVELOPMENT ALTERNATIVE

2. Presented By – Name Std ID 01 M.M. Maidul Islam (Group leader) 031151039 02 Nasrin Akhter Shova 031151029 03 Md. Asaduzzaman 032121047 04 Ipsita Nag 031151015 05 Md. Kamruzzaman 031151004 06 Faozia Abida Islam 031151047 07 Sumaiya Alam 031151047 08 Shahbaz Hossain Pranto 031151012

3. First, we should know about Pain and Fever Pain: Pain is a symptom of inflammation. Fever: When temperature is above of 98.6 F. We know, when temperature is 100.4 F , it is called fever. Analgesic: A drug that selectively relieves pain by acting on CNS or on peripheral pain mechanisms without significantly altering consciousness. It is a pain relive drug. Antipyretic: A drug that reduces fever by lowering the body temperature (Some analgesic drugs have antipyretic activity).

4. TYPES OF PAIN

5. PAIN S CALE 1 3 4 6 7 10 Mild Moderate Severe Non opioid analgesics are mostly used for mild to moderate pain. Opioid analgesic are used for severe pain.

6. PAIN RECEPTOR Pain receptor in our bodies are nerves that transmit pain. These are free nerve endings located in various body tissues that respond to thermal, mechanical, & chemical stimuli. When tissue becomes injured, they release chemicals called prostaglandins and leukotrienes that make the pain receptor more sensitive and these causing pain.

7. PHYSIOLOGY of PAIN

8. BASIC ANATOMY of NOCICEPTION

9. CENTRAL ANALGESICS Opioids : Morphine & morphine like drugs Non- Opoid : NSAIDs Acetaminophen/PCM Flupirtine Ziconotide

10. DIFFERENCE : OPIOID ANALGESICS NON OPIOID ANALGESICS(ANTIPYRETIC): Act centrally Act peripherally Cause addiction Do not cause addiction Produce CNS depression Do not produce CNS depression Do not produce gastric irritation Produce gastric irritation Show no anti inflammatory effect Show anti inflammatory effect. Reduce body temperature. e g . Morphine, Tramadol , Pethidine etc. Diclofenac , Ibuprofen, Aspirin etc.

11. OPIOID ANALGESIC “Opium” is a Greek word meaning “juice,” or the exudates from the poppy. Opium is extracted from poppy seeds ( Paper somniforum ) “ Opioid ” is a natural or synthetic drug that binds to opioid receptors producing agonist effects. Which are present in the central and peripheral nervous system, can cause numbness and induce a state of unconsciousness.

12. MECHANISM of ACTION All opioid receptors are G-protein coupled receptors and inhibit adenylate cyclase . They are also involved in Postsynaptic hyperpolarization (increasing K+ efflux) Reducing presynaptic Ca ++ influx Thus inhibits neuronal activity. OPIOID RECEPTOR: All opioid receptors are linked through G-proteins to inhibition of adenylate cyclase . They also facilitate opening of potassium channels (causing hyperpolarisation ) and inhibit opening of calcium channels (inhibiting transmitter release). They are of 4 types: μ receptor σ receptor δ receptor Κ receptor

13. RECEPTOR BINDING of MORPHINE Morphine exerts a narcotic action manifested by analgesia, drowsiness, changes in mood, and mental clouding. The major medical action of morphine sought in the CNS is analgesia. Opiates suppress the "cough center" which is also located in the brainstem, the medulla. Such an action is thought to underlie the use of opiate narcotics as cough suppressants.

14. RECEPTOR BINDING of MORPHINE Morphine activates analgesic receptors in the CNS. Which leads to a reduction in the transmission of pain signal to the brain. There are 3 main types of analgesic or o opioid receptor activated by morphine. Called the mu, kappa, delta receptors. Which are g-protein coupled receptor. Morphine acts a agonist at all three receptors and activation leads to : Opening of potassium ion channel Closing of calcium ion channels Reduces the pain signal Inhibition of Neurotransmitter release Morphine has high affinity for mu receptor. Activation of the mu receptor results in sedation, which is the strongest analgesic effect. But activation of this receptor also leads to depression, euphoria, and addiction.

15. PHARMACOLOGICAL ACTIONS Analgesia Respiratory depression Cough suppression Vagal stimulation ( bradycardia ) Sedation & hypnosis Hypothermia Itching Physical & pshycological dependence Euphoria Histamine release , hypotension….etc.

16. ADVERSE EFFECTS Morphine can produce a wide range of adverse effects like nausea , vomiting , dizziness , mental clouding , respiratory depression , constipation , dysphoria , urinary retention , & hypotension, allergic reactions . Tolerance - Repeated administration of morphine results in the development of tolerance to some of its effects including respiratory depression, analgesia, sedation, etc . Dependence - Opium has been a drug of addiction for many centuries. Its ability to produce euphoria makes it a drug of addiction. Opioids produce both physiological & pshycological dependence. Manifestations are lacrimination , sweating, yawning, anxiety, restlessness..etc.

17. Non- Opoid Analgesics (NSAID’s)-as Antipyretic Drug Non steroidal anti- inflamatory drugs are aspirine -type or non- opioid analgesics. In addition, they have anti- inflamatory , anti pyretic & uricosuric properties without addiction liability. The active principle is salicin , that is converted into salicylic acid in body. Drugs for antipyretic Aspirin Paracetamol / Acetaminophen

18. CLASSIFICATION

19. MECHANISM of ACTION Activities of antipyretic: Used to treat fever. Inhibits the enzyme COX. Fever  release of endogenous pyrogens ( e.g ., interleukin-1) released from leucocytes  acts directly on the thermoregulatory centers in hypothalamus  increase body T°. This is assoc with increase in brain PGs ( pyrogenic ). Aspirin prevents the T°-rising effects of interleukin-1 by preventing the increase in brain PGs.

20. MECHANISM of ACTION Arachidonic acid COX-1 COX-2 Leukotrienes \Prostaglandins Prostaglandins Primarily support platelet function Primarily protect GI-tract mucosa Primarily mediate inflamation , fever, pain NSAIDs COX-2 inhibitors

21. ADVERSE EFFECT Analgesics doses are usually well tolerated but anti-inflammatory doses are usually associated with adverse effects whed used for a long period. A. G.I tract:- Epigastric distress, nausea, vomiting, erosive gastritis, peptic ulcer, increase occult blood loss in stools are common B. Allergic reactions are not common and may be manifested as rashes, photo sensitivity..etc C. Haemolysis D. Nephrotoxicity E. Reye’s syndrome F. Salicylism G. Acute salicylate intoxication

22. SIDE EFFECTS of ANALGESICS & ANTIPYRETIC DRUG Risk of experiencing side effects depends on the type of analgesic what we take, and how long we take it. Side effects of analgesics may include: Constipation Drowsiness Dizziness Upset stomach Ringing in your ears Skin itching or rash Dry mouth

23. OVERVIEW Some of analgesic and antipyretic drugs are also called OTC drugs. OTC drugs are those drugs which are not prescribed by physician, like paracetamal , aspirin, diclophenac sodium, ibuprofen etc. These drugs are helpful for those person who are not capable for going to physician. So, they can treat their usual problem. But these drugs are also have some harmful. These drugs are sometimes abused. Many people are used these drugs as dope because they are addicted by these drugs. Actually these drugs are not so costly.but some drugs are costly like cocaine,morphine,heroine,pathedine etc.These drugs are created addiction.So government should take proper step for these and people should concern about these.

24. MANAGEMENT OF ANALGESIC ABUSE AND DEPENDENCE Crisis intervention: Directed at immediate survival by reversing the potentially lethal effects of overdose with an opioid antagonist. Harm reduction: Intended to reduce morbidity and mortality associated with use of dirty needles and overdose. Detoxification/withdrawal: Aims to remove the opioid of abuse from the patient's body, either through gradual taper and substitution of a long-acting opioid or through ultra-rapid opioid detoxification. Maintenance treatment or opioid (agonist) replacement therapy. Abstinence-oriented therapy: Treatment directed at cure. The patient is tapered off of short-acting opioids during the detoxification/withdrawal process and may be placed on an opioid antagonist with the goal of minimizing relapse. All treatment approaches share the common goal of improving health outcomes and reducing drug-related criminality and public

25. References The Pharmacological Basis of Therapeutics, Goodman & Gillman 12 th ed Ch 18 Pg 481 Foy’s Principles of Medicinal Chemistry 6 th ed http://en.wikipedia.org/wiki/Morphine nawrot.psych.ndsu.nodak.edu/courses/.../morphine/Page2WP.htm www.rxmed.com/.../MORPHINE%20SULFATE%20INJECTION%20BP.html depression.about.com/od/ glossaryt /g/toxicity.htm medical-dictionary.thefreedictionary.com/ morphine+poisoning www.drugbank.ca/drugs/DB00295 http://www.answers.com/Q/What_is_the_antidote_for_morphine www.optionsbehavioralhealthsystem.com/.../heroin/effects-signs-symptoms http:// www.drugs.com/drug-class/narcotic-analgesics.htm Slideshare.com/net

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