CONTROLLED DRUGS

Controlled Substance Act Comprehensive Drug Abuse Prevention and Control Act Controlled Substance Act 1970 Drug Enforcement Administration DEA ENFORCE GATHER INFORMATION TRAIN AND CONDUCT RESEARCHES SCHEDULE I DRUG High potential for abuse No current accepted medical use Lack of accepted safety for use under medical supervision Marijuana, Peyote, Heroin, Hashish

SCHEDULE III DRUG High potential for abuse but less so than drugs in schedules I and II A current accepted medical use An abuse potential that may lead to moderate or low physical and severe psychological dependence Lortab, Florinal, Tylenol with codeine

SCHEDULE IV DRUG Low potential for abuse compared with those in schedule III A current accepted medical use An abuse potential that may lead to limited psychological or physical dependence, compared with drugs in schedule III Phenobarbital, Diazepam, Flurazepam SCHEDULE II DRUG High potential for abuse A current accepted medical use An abuse potential that may lead to severe psychological and physical dependence Amphetamines, Morphines, Secobarbital

SCHEDULE V DRUG Low potential for abuse compared with those in schedule IV A current accpeted medical use An abuse potential that may lead to limited psychological or physical dependence liability, compared with drugs in schedule IV, because abuse potential is low prescription may not be required Lomotil, Robitussin A-C

REPRESENTATIVE AGENTS CAPABLE OF PRODUCING DEPENDENCE

Register biannually with the DEA Manufacturer Physician Nurse practitioner physician assistant Dentist Pharmacy Prescription Health providers name address DEA registration number Signature Patients name and address Date of issue Pharmacist cannot refill w/o approval of health care provider Ward stock Ordered in special hospital forms to maintain inventory and dispersion control record Nurse must enter in controlled substance record Name of patient Date of administration Drug administered Drug dose Possession of these drug is a crime Conditions that allow nurses to have possession of these drugs Under the direction of the physician or dentist licensed to prescribed these meds/giving them to patient under doctors order The nurse is the patient him/herself The nurse is the custodian of the limited supply of these substances in the ward or hospital Controlled substances ordered but not used should be returned to the source DRUG ABUSE Inappropriate and usually excessive, self-administration of a drug for non-medical purposes. Abused drugs exert their effects in the CNS. Compulsive drug-seeking behavior. Preoccupation with the procurement and use of the drug may be so demanding as to decrease the users productivity. Prolonged abuse may cause chronic toxicity. Psychological Dependence Motivational component: great subjective need, compulsion, drive to get the drug. Will take drug periodically. Although physical dependence for a drug may not occur, drug-seeking behavior is present. Habituation; Just "like" the drug; Drug effects serve as positive reinforcers. No tolerance increase.

DRUG DEPENDENCE Repetitive use of substances that produce an optimal state of well being because of their positive reinforcing effects in the CNS. Psychological dependence Physical dependence

Physiological Dependence The body needs the drug for normal physiological function. Tend to increase dose because of tolerance. Withdrawal Symptoms/Absence Syndrome (negative reinforcement). Predictable group of signs and symptoms resulting from abrupt removal of a drug. Psychological dependence is also present. DRUGS PRODUCING ILLUSIONS, DELUSIONS AND HALLUCINATIONS

CROSS-DEPENDENCE When a drug is administered to achieve the same outcome as that of another drug. i.e. heroin methadone. In a heroin user, methadone can be substituted for heroin in preventing the withdrawal syndrome. CROSS-TOLERANCE When an individual has become tolerant to a drug and requires higher than normal doses of a second drug to have its effects. i.e. Barbiturates BDZ. Amphetamine cocaine. BARBs or BDZs Anesthetics. In general there is cross-dependence and crosstolerance between drugs of the same class, but not between drugs in different classes. Exceptions: Sedative-hypnotics and volatile intoxicants. LSD and phenylethylamines, but not with other hallucinogens. CO-ADMINISTRATION/CO-ABUSE Many of these drugs are used in combination with other drugs from one or more categories. Alcohol and Heroin Nicotine and Alcohol Speed balls cocaine + heroin Cocaine + BDZs Heroin and BARBs Be aware of the possibility of combination of drugs when treating withdrawal or overdose, each drug will require a specific treatment. Because of the diverse character of these drugs, there is no single reason for their use, nor is there an addictive personality". IT IS NOT NECESSARY TO HAVE A PREEXISTING EMOTIONAL OR PSYCHIATRIC PROBLEM TO BECOME DRUG DEPENDENT!!! TOXICOLOGY Tissue and organ toxicity Acute use Respiratory depression --- narcotics, inhalants, barbiturates. Cardiovascular effects and seizures --- cocaine, amphetamines. Arrhythmias --- volatile intoxicants. Lack of motor coordination Accidents (car

DRUG ADDICTION The drug-use and drug-seeking behavior of dependent individuals is maintained by the reinforcing central activity of the drug despite its negative social, psychological and physical consequences. Physiological and psychological dependence is present. Physiological changes have occurred. Symptoms of withdrawal, will be involved. High tendency to relapse. DRUG TOLERANCE After chronic use, the same amount of drug is insufficient to cause the desired effect and thus, more drug is used. A compensatory response. Innate Tolerance 1. Sensitivity 2. Insensitivity Acquired Tolerance 1. Pharmacokinetic or metabolic 2. Pharmacodynamic or functional 3. Learned or behavioral Tachyphylaxis Rapid development of tolerance to the drug after a few doses or a single administration.

accidents, big machinery accidents) death --alcohol, narcotics, stimulants, PCP, marihuana, hallucinogens, CNS depressants. Chronic use Abnormal neuronal activity --- ALL Liver damage --- alcohol. Increase incidence of lung, breast, gastrointestinal and rectal cancer, and cardiovascular diseases --- tobacco. Pregnancy complications and babies born dependent --- narcotics.

Psychic toxicity Acute use Bad trips, flashbacks --- hallucinogens, CNS stimulants. Mood liability --- marihuana, hallucinogens, PCP. Panic attacks --- cocaine, amphetamines, marihuana, hallucinogens, PCP. Chronic use Reality distortion --- alcohol, hallucinogens, stimulants .

Behavioral toxicity Acute use Lack of motivation. Lack of judgment. Loss of concentration. Violence death. Chronic use Amotivational syndrome Loss of productivity. Decrease hygiene. Decrease health. Alcohol, narcotics, stimulants, PCP, marihuana, hallucinogens, CNS depressants. Associated Diseases Infections AIDS Venereal diseases Others Tobacco-related fires. Toxicity due to bad batches of drug can produce permanent damage such as Parkinson-like disorders --- heroin (MPTP). AMPHETAMINES d, l-Amphetamine, Methylphenidate (Ritalin, use to treat attention deficit and hyperactivity disorders in children), Phenmetrazine (used to treat obesity), Methamphetamine (crystal, speed, ICE). methylendioxyamphetamine, (MDA). methylenedioxymetamphetamine, (MDMA, ecstasy, XTC). Pharmacology: Used as nasal decongestants (benzedrine, replaced by propylhexedrine). Used as antidepressants and to treat obesity (anorectic) => can cause dependence. Used to stay awake. Present clinical therapeutic use, only in narcolepsy. Amphetamine and methamphetamine -HCl (speed), Amphetamine or methamphetamine => I.V. D-methamphetamine (ice) => smoked like cocaine but has a much longer duration of action.

Subjective CNS effects Drowsiness Difficulty concentrating Apathy Decreased physical activity Lethargy Extremities feel heavy and the body feels warm Undesirable Effects Dysphoria Dizziness Nausea Vomiting Constipation* Biliary tract spasm Urinary retention Acute Toxicity/Overdose 1. Disruption of central control of peripheral sympathetic activity. o Brainstem Respiratory depression o o o o 2.

DEATH Circulatory depression dec.BP

Pupils constricted (miosis), (may be dilated with meperidine or severe hypoxia) Nausea and Vomiting Pulmonary edema Reflexes dec.

CNS depression o Drowsiness

Sedation Coma

3.

CNS abnormal neuronal activity o Convulsions -- with propoxyphene or meperidine

CNS STIMULANTS Cocaine, Crack (free base or hydrochloride). Amphetamines. Khat: Cathinone, methcathinone. Methylxanthines: caffeine, theophyline, theobromide. Nicotine Cocaine Pharmacology Cocaine and the amphetamines have very similar effects on mood, patterns of abuse, the type of dependence produced, and their toxic effects. Differences are mainly in the pharmacokinetics (t of cocaine is shorter (50-90min) vs longer (5-10hrs) t for amphetamines). Cocaine-HCl is injected I.V. => rush or flash => euphoria. Rate of absorption is limited by local vasoconstriction. Cocaine free base (crack, rock) is smoked => delivered directly to pulmonary circulation, left heart and brain. Acute effects Causes an initial but temporary euphoria, rush. Causes craving within 30 minutes of taking the drug. Increase alertness, feeling of elation and well being, increased energy, feelings of competence, increased sexuality. The user becomes more talkative, restless and often more irritable. Consciousness is clear, but delusions may occur as well as visual, tactile (formication) and auditory hallucinations. These drugs are sympathomimetic, thus, they cause HR, BP, skeletal muscle tension, but musculature of the bronchi and intestines relax. Cocaine Given unlimited access to the drugs, animals will self-administer these drug until they die.

Psychological Dependence Similar to Cocaine May cause hallucinations OPIOIDS or NARCOTICS Morphine Codeine Meperidine Methadone Acute effects 1. Positive Effects Desirable Subjective 2. Negative Effects Undesirable

MDA, DOM, MDMA

Desirable Effects Euphoria Sedation Relief of anxiety and various other forms of distress. Analgesia. Depression of cough reflex*

Acute toxicity/Overdose Runs Uninterrupted sequences of stimulant abuse to maintain a continuous state of intoxication, to extend the pleasurable feeling, and to postpone the postintoxication crash than ensues as the drug effects subside.

Phenobarbital Pentobarbital Secobarbital Amobarbital

Street Names purple hearts yellow jackets red devils blue angels

Benzodiazepines: Used as anxiolytics and hypnotics. Flurazepam => sleeping pills. Flunitrazepam => date rape drug. Diazepam (Valium) => tranquilizer. Chlordiazepoxide (Librium) => tranquilizer. Clonazepam => anticonvulsant. They all cause sedation and muscle relaxation. Induce sleep (hypnosis). Abuse may cause "BDZ-induced aggression". Methaqualone (Quaalude) => "Downer", works as Valium, seriously abused, very addictive. Synthesized as part of an Indian program looking for antimalarial drugs. In 1965 it was approved for prescription use and placed in Schedule V. In 1984 methaqualone was transferred to Schedule I of the CSA.

Cocaine Acute tolerance may occur in such people, particularly in those taking the drug I.V., resulting in the need of increasingly larger doses. This spiral of tolerance and dose increases continues until the drug is depleted or the person collapses from exhaustion. Drug taking and drug seeking take a compulsive character. Stimulant overdose results in excessive activation of the sympathetic nervous system and cardiac toxicity. tachycardia and hypertension myocardial infarction cerebrovascular hemorrhage Cocaine can cause coronary vasospasms and cardiac dysrhythmias. CNS symptoms include anxiety feelings of paranoia and impending doom, and restlessness. Users exhibit unpredictable behavior and may become violent. Treatment of overdose Beta blockers => for autonomic hyperactivity. o -

Acute toxicity/Overdose Acute Intoxication Pupils are normal; BP and respiration are depressed; nystagmus on lateral gaze; tendon reflexes depressed; ataxia; slurred speech; confusion; coma; shock => Risk of Death, particularly with BARBs. Treatment of overdose Treatment of overdose w/BDZs: flumazenil (BDZ receptor blocker). No treatment for Barbiturates.

1 blockade (Atenolol, metoprolol, esmolol and

non-selective : labetolol). This treatment is controversial: Problems with

Withdrawal Minor: tremors; insomnia (REM rebound); high fever; clonic blink. Anxiety and dysphoria. Sleep disturbances. 12-16hrs: minor symptoms plus abdominal cramps; nausea and vomiting, o. hypotension; deep tendon reflexes, hyperreflexia. 24hrs: pronounced weakness, course tremors (the shakes), hyperactive reflexes, early illusions and hallucinations. Hyperpyrexia. 48-72hrs: convulsive seizures (rum fits); vivid auditory and visual hallucinations (the horrors), formication, agitation, disorientation, delirium, paranoid delusions. Drugs causing hallucinations and delusions Psychedelics and hallucinogens Indolamines: Lysergic acid diethylamide (LSD), morning glory seed (LSM), psilocybin, psilocin, ibogaine, dimethyltryptamine (DMT). Phenyethylamines: mescaline, bufotenin, dimethoxymethyl-amphetamine (DOM). Cannabis. Marihuana, delta-9-THC. Dissociative anesthetics. Ketamine, Phencyclidine (PCP). Anticholinergics. Mandrake root, jimson weed, atropine, scopolamine.

using non-selective blockers may lead to unopposed effects => BP Nitroglycerine or other nitrites/nitrates for angina. Calcium channel blockers (verapamil, diltiazem) for hypertension. Ice baths for high fever. Acidify urine to hasten excretion. After the acute toxic effects are handled: Antidepressants for depression Haloperidol Alprazolam

for psychosis. for panic attacks.

SEDATIVE HYPNOTICS Barbiturates Used clinically as anticonvulsant, anti-anxiety drugs or preanesthetics.

Hallucinogens Pharmacology These four classes of drugs are usually considered together because of their prominent feature of intoxication (hallucinations, delusions, illusions), but

they differ in almost every aspect: chemical structure, mechanism of action, CNS receptor involved, picture of intoxication, type and seriousness of their toxic effects. They occur naturally in plants, mushrooms and in some frogs

Acute Effects At low doses: Euphoria; Changes in affect (mood): anxiety, tension, labile mood; Thought and feeling disorders: perceptual changes (distortion), depersonalization, illusions visual hallucinations, time and visual distortions, synesthesias; nausea, pupils are dilated,

HR, BP, temperature, reflexes, tremors.

Panic, paranoia. At high doses: Dangerous behavior may cause accidents. For the amphetamines: Visual hallucinations => convulsions, coma. Subjective reason for taking these drugs: Allows insight into oneself and new ways of looking at the world. Cross-tolerance between LSD and mescaline. Usually polydrug users. Acute toxicity/Overdose Depends on the individual drug. Tissue toxicity. Some are neurotoxic. Psychic toxicity. Acute transient psychosis. Flash backs. Behavioral toxicity. Distorted behavior, aggressive, violent. Withdrawal These drugs do not cause physical dependence, but they have tremendous abuse potential (psychological dependence). Use is occasional. MARIHUANA (CANNABIS) Pharmacology From the Indian hemp plant, or Cannabis sativa. Medicinal powers => Egyptians. Probably originated in Central Asia. Delta-9-tetrahydrocannabinol (THC) is the active ingredient. Marihuana, marijuana, bhang, ganja, hashish or charas, sinsemilla, red oil. High lipid solubility but does not dissolve well in water so if taken orally they are absorbed through the digestive system rather slowly. Smoking causes 50% of cannabinoids to enter the lungs. Holding the smoke in the lungs maximizes absorption. Mechanism of Action In 1990 the THC receptor was cloned and in 1992 the endogenous cannabimimetic was discovered. They named it anandamide (nanda, in Sanskrit = bliss). Anandamide is the ethanolamine of arachidonic acid. Cannabinoids as well as anandamide inhibit Adenylate Cyclase (which produces cAMP) both in brain and periphery, via G protein-coupled cannabinoid receptors. They also inhibit the N-type calcium channel current, which may affect regulation of neurotransmitter release.

Cannabinoids have effects not related to receptor function, including activation of PLA2 and intracellular calcium mobilization. THC causes the release of serotonin, causes an elevation of ACh and inhibits the synthesis of prostaglandins. They have also been known to influence levels of NE, DA and GABA. THC concentrates in the limbic system, particularly in hippocampus and amygdala and sensory centers for hearing. A new peripheral cannabinoid receptor, with only 44% homology to the brain receptor, has been found in spleen, lymph nodes and leukocytes. Thus, they appear confined to the immune system. Cannabinol, a compound also found in marihuana but with less psychotropic effects seems to have preference for this receptor. Dronabinol. Medicinal grade cannabinol. Approved as an antiemetic.

PCP Phencyclidine, Angel Dust, Hog Pharmacology It is a synthetic phenylcyclohexylamine derivative. Initially introduced in 1957 as a dissociative anesthetic, which caused no loss of consciousness. It was removed from the market for use in humans, but it was used in veterinary practice. It is the most commonly used hallucinogenic agent. It may be snorted, taken orally, smoked with tobacco, or injected IV. Usually gives bad trips. Behavior under the influence of the drug may be unpredictable, bizarre and violent.

Acute toxicity /Overdose Intoxication may last 4 to 6 hrs. Usually not lethal. Treatment of Intoxication/Overdose No treatment Physical dependence is not clear.