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B 3.3 Strong Analgesics Compare the structures Morphine, codeine, heroine-semisynthetic Advantages/disadvantages Analgesics Opium Strong Analgesics • Relief of very severe pain, • include narcotics : heroin, codeine, morphine • Addictive • Controlled substances Strong Analgesics Morphine • Morphine is used intravenously, intramuscularly, subcutaneously, orally, intra articular Heroin Strong Analgesics • • • • The Opium alkaloids Narcotic / sleep inducing analgesics /pain relieving Morphine: alkaloid 10% by mass of raw opium • Codeine ~ 0.5 % by mass of raw opium • Heroin : synthetic / acetylation of morphine Meperidine Administration parenteral, oral fentanyl Demerol DEMEROL has been reported as being abused by crushing, chewing, snorting, or injecting the dissolved product. These practices will result in the uncontrolled delivery of the opioid and pose a significant risk to the abuser that could result in overdo Methadone /dolophine Blocks the euphoric high of heroin and is used in the treatment of heroin addicts in some countries /as a legal drug Advantages • • • • • Pharmacological effects on: Central nervous system The eye Gastrointestinal tract The prime medical uses of opiates: • Relief of severe pain caused by injury, cancer, surgery (before/afterward • Treatment of diarrhea by producing constipating effect • To relieve coughing by suppressing the cough center • Addictive nature of opiates/ it is replaced by synthetic non-narcotic drug Psychological effects of Opiates • Analgesia, drowsiness, mood changes and mental clouding • Anxiety, fear, lethargy, sedation, lack of concern, inability to concentrate, nausea and vomiting • Users feel a relief from emotional and psychological pain Tolerance and Dependence • Due to the induction of drug metabolizing enzymes in the liver • And adaptation of neurons in the brain to the presence of the drug • Tolerance to all other opiates Physical Dependence • Need to take drug to function properly • Withdrawal symptoms: restlessness, sweating, fever, chills, vomiting, Increase rate of respiration, unbearable aches / pains • Depends on dose • Frequency of drug administration • Duration of the drug dependence, the opiate used Opiates • • • • Extremely potent Capacity to induce euphoria Strong compulsion to misuse Induce profound tolerance, physiological dependence • Lead to crime Short term Effects • Sedation, stupor; relief from pain • Euphoria: impaired functioning and coordination • Reduced tension, worry, fear • Reduced coughing reflux • Occasional death from overdose Long term effects • • • • • Loss of appetite; malnutrition, constipation Sterility Withdrawal illness, loss of job, crime Diversion of $ and energy Risk of dangerous infections AIDS, due to shared needles Medical uses / Opiates • Strong analgesics / pain reliever in cancer, prior to and recovery from surgery • Heroin / 3 times as morphine • Codeine as 1/6th of morphine • In the treatment of diarrhea by producing constipation • To relieve coughing by suppressing the cough centers in brain Local anesthetics • Pain killers in localizes areas • Lidocaine and procaine (Novocain) • Used in dentistry Novocain • t is the first injectable local anesthetic to be synthesized, • commonly known as Novocain. • The German Chemist, Alfred Einhorn, developed it in 1904. • Procaine is the precursor to cocaine. • Procaine works to anesthetize a patient for about 15 minutes. To prolong anesthesia epinephrine is added as a vasoconstrictor. Procaine/Cocaine • Cocaine blocks Na+ passage through the axon cell membrane and • inhibits the reuptake of Dopamine and Serotonin • resulting in psycho-stimulation. Procaine • Procaine blocks nerve conductance via inhibiting Na+ at the membrane, • thus no psycho-stimulation. • Both reactions are brief. • Drug Interactions? • Procaine is thought to reduce the effects of sulfonamide antibiotics. • How is this medication administered? • Oral injection. Lidocaine General Anesthetics B9-447 SEROTONIN, happy neurotransmitter. • 5-hydoxytryptamine, is naturally produced in the pineal gland, which lies at the centre of our brain. • “It is essential to numerous body function including appetite control, sleep, memory and learning, temperature regulation, mood, behavior, cardiovascular function, muscle contraction, endocrine regulation and depression. DOPAMINE, • 4-(2-aminoethyl)benzene-1,2-idol, is produced in several areas of the brain including the substantia nigra. • It is central to movement coordination, cognitive functions (by mediating signal transduction in the frontal lobe thus affecting memory, attention, and problemsolving in particular), latent inhibition and creative drive. Dopamine • Its release is stimulated by naturally rewarding experiences • such as happy foods (bananas!), drugs,