CHAPTER 4 DOWNERS: OPIATES & OPIOIDS AND SEDATIVE-HYPNOTICS I. A. 1. 2. 3. 4.

General Classification Opiates & opioids Opiates are refined from the opium poppy Opioids (Demerol, Darvon, etc.) are manufactured synthetically Legally used to treat acute pain, diarrhea, coughs Illicitly used to produce euphoria, suppress pain, and avoid withdrawal symptoms

B. Sedative-hypnotics are synthesized drugs, devised to treat nervousness, pain, epilepsy, and insomnia C. Alcohol, produced by fermentation of plant sugars or starch, causes the most health problems worldwide D. Skeletal muscle relaxants are synthetically developed to depress areas of the brain responsible for muscle activity. They are used to treat muscle tension and pain. E. Antihistamines, synthetic drugs used to treat allergies, ulcers, shock, rashes, and motion sickness. One side effect is drowsiness. F. Over-the-counter sedatives are depressant drugs (Nytol, Sleep-Eze, Sominex) marketed as sleep aids or sedatives. They often contain scopolamine and antihistamines. II. A. Opiates & Opioids Classification. Opium is processed from the milky fluid of the unripe seed pod of the opium poppy (Papaver somniferum). Raw opium contains morphine -(4-20%); codeine - (1-5%) and thebaine (less than 1%). History of methods of use Sumerians, Egyptians, and Chinese record use before 2000 B.C. as a medicine, source of pleasure, and a poison

B. 1.

2.

Opium, taken orally, was used to induce drowsiness and to cure illnesses, but was bittertasting and slow acting. Smoking opium and later the refinement to morphine made the effects stronger and quicker, and increased the potential for addiction Hypodermic needle (1848) made morphine's effect even more potent and more addicting Heroin (diacetylmorphine) further increased potency and abuse potential. In the late 19th century, opiates were added to tonics and medications. In the 20th century, criminal organizations became widely involved in the opiate trade, including the Mafia and Chinese triads. Effects of opioids. Opioids deaden pain a. b. They block the release of substance "P" which transmits pain signals They mimic endorphins which are our endogenous pain killers.

3.

4. 5. 6. 7.

C. 1.

2. 3. 4.

Endorphins naturally activate dopamine neurons to trigger pleasure Opioids artificially activate the reward center to produce a state of euphoria. Because of tolerance, users might need 10 times an original dosage after a month of regular use. Cross tolerance, i.e. tolerance to all opiates and opioids, occurs Withdrawal occurs when someone stops using after 2-3 weeks of continuous use. It is not life threatening, but feels like a bad case of the flu. Short-acting drugs result in severe, short-acting withdrawal symptoms; long-acting drugs cause delayed, milder, and longer-acting symptoms. Relax muscles, cause dry skin and itching Suppress coughing, stimulate vomiting, cause constipation, constrict pupils

5. 6.

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8. 9.

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Neonatal effects a. Pregnant users have higher risk of miscarriage, placental separation, premature labor and still births. b. Opioids cross the placental barrier, causing addiction in the baby, even overdose or death

11.

Overdose occurs when high doses shut down the nervous system (blood pressure drops, heart beat slows, lungs fill with fluid). Principle Opioids Heroin (diacetylmorphine) use is a world-wide problem. a. Largest producer and exporter of illegal opium and heroin area is the Golden Triangle (Burma, Northern Thailand and Laos). India is the largest grower of opium for legal medical purposes. b. Types include "China White" and Persian brown". Since the 40's, Mexico has been largest supplier to U.S. of black tar" heroin which is often smoked.

C. 1.

2.

Codeine, not as strong as morphine, and generally used for relief of moderate pain or to control coughs. Morphine is refined from opium and is the standard for pain relief measurement. Other Opioids Methadone (Dolophine). A long-lasting opioid which is taken orally to reduce heroin craving and reduce withdrawal symptoms. Hydromorphone (Dilaudid). A semi-synthetic opioid refined from morphine. It is 8 times more potent than morphine. Oxycodone (Percodan). An oral pain reliever. Meperidine (Demerol) A short-acting opioid, usually injected Propoxyphene (Darvon) A prescribed for mild to moderate pain, especially by dentists. Fentanyl (Sublimaze). Most powerful opioid (50 to 100 times stronger than morphine). Designer heroin -- street versions of fentanyl, known as "China white," are made without controls and can be very dangerous.

3. D. 1.

2.

3. 4. 5. 6. 7.

8. 9. E. 1.

LAAM -- an opioid being tested for heroin replacement therapy Naloxone & Naltrexone -- opiate antagonists which block the effects of opiates. Problems with opiate use Dilution (street drugs can vary from 0 to 99% pure) & adulteration (cheap substitutes are used to cut or replace the drug). Dirty and shared needles can inject not only the drug, but other materials, bacteria, and viruses, including HIV virus that causes AIDS Cost of a heroin habit can range from $60 to $150/day. It is estimated that 60% of the cost is covered by prostitution and drug dealing and 40% by shoplifting and burglary. Sedative-hypnotics Classification This class of drugs is prescribed to control neurotic reactions in unstable patients, to control anxiety, hypertension, and epilepsy, and to induce sleep. The effects are similar to those of alcohol, though these drugs come in a more concentrated form than alcohol and withdrawal symptoms can be life-threatening General effects & metabolism Action of hypnotics and sedatives a. b. Hypnotics such as barbiturates work on the brain stem to induce sleep. Sedatives such as the benzodiazepines act at a number of brain sites and are used as sleeping aids or anti-anxiety agents

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3.

III. A. 1.

2.

B. 1.

2.

Tolerance to physical effects develops slower than tolerance to the mental effects, meaning accidental overdose can kill the user Withdrawal can be dangerous: seizures, delirium, rapid heart beat, and death Overdosing includes cold skin, weak pulse, shallow breathing and possibly death.

3. 4.

C. Barbiturates include 2,500 different compounds 1. Slow-acting, such as phenobarbital, last 12-24 hours; shorter-acting compounds such as Seconal last 4-6 hours 2. Some cause immediate unconsciousness; others, temporary stimulation and then sedating effects similar to alcohol 3. Dispositional tolerance results in the very efficient metabolization of the drug 4. Tissue dependence occurs when 8-10 times the normal dosage is taken daily for 30 days or more D. Benzodiazepines (Xanax, Valium, Halcion, etc.) 1. Most widely used sedative-hypnotics, developed in the '40's and 50's, including Librium and Valium Effects: used as anti-anxiety drugs, as sleep aids, as drugs to control seizures, as sedatives They interact with GABA receptors in the brain. Problems include long-lasting effects, addictiveness, and severe withdrawal a. Tolerance involves increasing amounts of drug needed to achieve the same effects and age-related tolerance (younger people tolerate more of the drug) Addiction develops if 10-20 times normal dosage is taken for several months. Withdrawal can be severe, sometimes involving seizures and convulsions and even death Overdose: symptoms include drowsiness, loss of consciousness, depressed breathing, coma, and death; persistence of the drug results in prolonged and cyclic withdrawal symptoms Prescribing practices require triplicate prescription forms

2. 3. 4.

b. c.

d.

e. E. 1.

Other sedative-hypnotics Quaaludes have been withdrawn from the legitimate market, though counterfeit versions are on the street

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Doriden is a short-acting non-barbiturate hypnotic used to treat insomnia and is abused in a polydrug combination with codeine Placidyl is an older sedative hypnotic, equivalent to Doriden in potency Miltown, popular in the '50's, was prescribed excessively (called Mother's little helper). Drug Interactions Drug synergism occurs when the combined effects of different drugs are greater than the sum of the parts. Drug synergism results in 4,000 deaths and 50,000 emergency room treatments per year Cross tolerance Tolerance to other drugs by continued exposure to a drug with similar chemistry. Probably occurs because many drugs are broken down by the same enzymes, and as use continues, the liver produces more and more enzymes Cross dependence Occurs when addiction to one drug supports addiction to other drugs Most often occurs with different drugs in the same chemical family

3. 4. IV. A.

B. 1. 2.

C. 1. 2.