B 3.3 Strong Analgesics Compare the structures Morphine, codeine, heroine-semi- synthetic 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 parenteralAdministration 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 1/6 th 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 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 problem- solving in particular), latent inhibition and creative drive.

Dopamine Its release is stimulated by naturally rewarding experiences such as happy foods (bananas!), drugs,