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Drugs Classification

Drugs Classification. Drugs Administration and Absorption. Ingestion Dissolve in the stomach & absorbed by intestine Absorbed thought stomach walls (e.g., alcohol) Absorption will depend on various factors: amount and type of food Injection Strong, fast, predictable

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Drugs Classification

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  1. Drugs Classification

  2. Drugs Administration and Absorption • Ingestion • Dissolve in the stomach & absorbed by intestine • Absorbed thought stomach walls (e.g., alcohol) • Absorption will depend on various factors: • amount and type of food • Injection • Strong, fast, predictable • Subcutaneous, intramuscular, intravenous • Inhalation • Difficult to regulate doses • Insufflation (snore) • Absorption through mucous membrane of: • nose, mouth, rectum, vagina

  3. Psychoactive/Psychotropic DrugsAction on Central Nervous System (CNS) • Analgesics • Anesthetics • Anxiolytics (anti-anxiety agents) • Antidepressants • Antipsychotics • Anticonvulsants • Mood stabilizers • Stimulants • Depressants • Hallucinogens

  4. Psychoactive Substances Usage • Analgesics (painkillers) • used to relive pain without producing anesthesia or loss of consciousness • Psychiatric medications • use in the treatment of psychiatric conditions • anxiolytics, antidepressants, antipsychotics, anticonvulsants, and mood stabilizers • Recreational drugs • used/abused for their mood and perception altering effects, including those with accepted uses in medicine and psychiatry • frequently used include narcotics, stimulants, depressants, hallucinogens • Entheogens • used for ritual and spiritual practice, such as the mescaline-containing peyote cactus or psilocybin-containing mushrooms

  5. Psychoactive DrugsClassification • Depressants • Stimulants • Narcotics • Hallucinogens

  6. CNSDepressants Slows down the central nervous system • Provide feeling of relaxation • Reduced inhibitions • Impair reflexes • Impair coordination • Reduce reaction time • Slurring speech, stumbling walk, and loss of balance • Hand-eye coordination is reduced • Thought and judgment impaired

  7. CNS Depressants • Sedative • Barbiturates • Benzodiazepines • Solvents-sedatives • Herbal sedatives • Nonbenzodiazepine • Uncategorized sedative-hypnotics • Narcotics (opiate derivatives) • Antihistamines (diphenhydramine)

  8. CNS DepresantsSedatives • Also known as sedative-hypnotic • Produces feelings of calmness, relaxation, sleepiness, slowed breathing, reduction of anxiety, and at higher doses slurred speech, staggering gait, poor judgment, and slowcertain reflexes. • Whenused to induce sleep tend to be higher doses than those used to relieve anxiety. • May be referred to as tranquilizers, depressants, anxiolytics, soporifics, and sleeping pills. • Can be abused to produce an overly-calming effect (alcohol being the most common sedating drug). • At high doses many of these drugs can cause unconsciousness and even death.

  9. CNS DepressantsBarbiturates • Effect range mild sedation to anesthesia. • Effective as anxiolytics, hypnotics and as anticonvulsants. • Widely used in surgical anesthesia. • Have addiction potential, both physical and psychological. • Dangerous in overdose. • Used for physician-assisted suicide (PAS), and in combination with a muscle relaxant for capital punishment by lethal injection. • Thiopental is an ultra-short acting barbiturate that is marketed under the name Sodium Pentothal is sometimes used as a "truth serum". When dissolved in water, it can be swallowed or administered by intravenous injection. The drug does not itself force people to tell the truth, but is thought to decrease inhibitions, making subjects more likely to be caught off guard when questioned.

  10. CNS DepressantsBarbiturates • amobarbital (Amytal) • pentobarbital (Nembutal) • secobarbital (Seconal) • Phenobarbitol (Luminal)

  11. CNS Depressants Benzodiazepines • Minor tranquilizers with varying properties. • Slow down the CNS. • Useful in treating anxiety, insomnia, agitation, seizures, muscle spasms, and alcohol withdrawal. • Also used before medical procedures such as endoscopies and dental work. • Recreational stimulant users often use benzodiazepines as a means of "coming down" • All have an addictive potential.

  12. CNS Depressants Benzodiazepines (minor tranquilizers) • alprazolam (Xanax) • bromazepam (Lexotan) • clonazepam (Klonopin) • diazepam (Valium) • estazolam (Prosom) • flunitrazepam (Rohypnol) • lorazepam (Ativan) • midazolam (Versed) • nitrazepam (Mogadon) • oxazepam (Serax) • triazolam (Halcion) • temazepam (Restoril, Normison, Planum, Tenox, and Temaze) • chlordiazepoxide (Librium)

  13. CNS DepressantsSolvents-Sedatives • chloral hydrate (Noctec) • diethyl ether (Ether) • ethyl alcohol (alcoholic beverage) • methyl trichloride (Chloroform)

  14. CNS DepressantsAlcohol • Among the most abused drugs in our society. • Can be as potent as many other illegal drugs. • Can cause severe damage to a developing fetus. • Reduces sensitivity to pain. • Long-term effectcan produce damage to liver, heart and pancreas. • Linked to gastro intestinal problems, malnutrition, high blood pressure, and lower resistance to disease. • Also linked to several types of cancer; including esophagus, stomach, liver, pancreas and colon. • People often do not realize that they are becoming dependent on alcohol.

  15. Other CNS Depressants • Herbal sedatives • kava • valerian • Nonbenzodiazepine sedatives • eszopiclone (Lunesta) • zaleplon (Sonata) • zolpidem (Ambien) • zopiclone (Imovane, Zimovane) • Uncategorized sedative-hypnotics • ethchlorvynol (Placidyl) • glutethimide (Doriden) • ketamine (Ketalar, Ketaset) • methaqualone (Sopor, Quaalude) • methyprylon (Noludar) • ramelteon (Rozerem)

  16. Narcotics • Refers to opium, opium derivatives, and their semi-synthetic or fully synthetic substitutes. • Most medical professionals prefer the more precise term “opioid”, which refers to natural, semi-synthetic and synthetic substances that behave pharmacologically like morphine, the primary active constituent of opium. • Main use: pain relief and cough suppressant.

  17. Four broad classes of Narcotics(opioids) • Endogenous Opioids • produced naturally in the body (endorphins) • Opium Alkaloids • morphine (the first alkaloid isolated from opium) • codeine • Semi-synthetic Opioids • heroin and oxycodone • Fully Synthetic Opioids • methadone and pethidine

  18. Clinical use of Narcotics(opioids) • Opioids have been used to treat acute pain • such as post-operative pain • Used in palliative care to alleviate • severe, chronic, disabling pain of terminal conditions such as cancer • In recent years there has been an increased use of opioids in • management chronic pain (transdermal patches)

  19. Clinical use of Narcotics(opioids) • Cough • (codeine and hydrocodone) • Diarrhea • (opium) • Anxiety due to shortness of breath (oxymorphone) • Detoxification • (methadone and buprenorphine )

  20. Narcotics Classification • Opium alkaloids • Phenanthrenes naturally occurring in opium: • Codeine • Morphine • Thebaine • Oripavine • Preparations of mixed opium alkaloids, including papaveretum, are still occasionally used. • Semisynthetic derivatives • Diacetylmorphine (heroin) • Dihydrocodeine • Hydrocodone • Hydromorphone • Nicomorphine • Oxycodone • Oxymorphone

  21. Examples of Narcotics Opium Codeine Morphine Heroin Methadone Oxycodone Demerol Dilaudid Percodan Lomotil

  22. CNS Stimulants • Stimulate central nervous system (CNS) • Increase alertness and wakefulness • Some produce a sense of euphoria • Can be used therapeutically • Narcolepsy - to counteract abnormal states that diminish alertness or consciousness • Used to boost endurance and productivity as well as to suppress appetite • Significant mood-altering effects • Controlled substances in many jurisdictions

  23. Common Stimulants • Amphetamines • Methylphenidate • Methamphetamine • Methcathinone • Cocaine • Ecstasy

  24. StimulantsAmphetamine • Also known as amfetamine, and benzedrine • brand name: Adderall • Prescription (Rx) stimulant used to treat • ADHD • Traumatic brain injury • Narcolepsy • Chronic fatigue syndrome • Initially used to control appetite • Also used illegally as • a recreational club drug • as a performance enhancer

  25. StimulantsMethylphenidate (MPH) • Amphetamine-like Rx stimulant • Used to treat • ADHD • Traumatic brain injury • Narcolepsy • Chronic fatigue syndrome • Brand names include • Ritalin (Ritalina, Rilatine) • Attenta, Concerta • Metadate, Methylin, Rubifen • Focalin (dextro-methylphenidate) • Daytrana (transdermal patch)

  26. StimulantsMethamphetamine • Also known as: Methyl amphetamine or desoxyephedrine • Rx for ADHD or narcolepsy under the brand name Desoxyn • Used illegally for recreational purposes • “crystal meth" refers to the crystalline (smokeable form) • It is prone to abuse and addiction • Rapidly enters the brain and triggers a cascading release of norepinephrine, dopamine and serotonin • Users may become obsessed or perform repetitive tasks such as cleaning, hand-washing, or assembling and disassembling objects • Withdrawal is characterized by excessive sleeping, eating and depression-like symptoms, often accompanied by anxiety • Users often take benzodiazepines as a means of "coming down"

  27. StimulantsMethcathinone • Potent CNS stimulant • Controlled substance • No clinical use at present • Used as antidepressant during 1930-40 • Snorted, smoked, injected, or ingested • Chronic abuse may result in acute mental confusion ranging from mild paranoia to psychosis

  28. StimulantsCocaine • Stimulant of CNS • Appetite suppressant • Produce euphoric feelings • Increased energy • Most often used recreationally • Used in medicine as a topical anesthetic: • eye, nose and throat surgeries

  29. History of Cocaine • In 1879 cocaine was used to treat morphine addiction • In 1884 cocaine is introduced as a local anesthetic • In 1885 Parke-Davis sold cocaine in various forms, including cigarettes, powder, and as a mixture that could be injected • Park-Davis promised that cocaine products would: “supply the place of food, make the coward brave, the silent eloquent and render the sufferer insensitive to pain” • In 1886 Coca-Cola included cocaine in its formula • In 1903 cocaine is eliminated from Coca-Cola • In 1914 the Harrison Narcotics Tax Act outlawed use of cocaine • This law incorrectly referred to cocaine as a narcotic • Cocaine is a stimulant, not a narcotic

  30. Forms of cocaine • Cocaine Sulfate • Produced by macerating coca leaves with water that has been acidulated with sulfuric acid, or a solvent, like kerosene or benzene. • Often accomplished by putting the ingredients into a vat and stamping on it, similar to the method for crushing grapes in wine production. • When water is evaporated will yield a pasty mass • Cocaine Sulfate is intermediate step to producing cocaine hydrochloride (salt form) • It is commonly sold in South America as a pasty mass • Also known as pasta,basuco,basa,pitillo,paco • Smoked along with tobacco

  31. Freebase Cocaine • Base form of cocaine • Cocaine base is insoluble in water and is therefore not suitable for drinking, snorting or injecting • Smoking freebase is preferred by many because cocaine is absorbed immediately into blood via the lungs, reaching the brain in about five seconds • Rush is more intense than sniffing the same amount of cocaine nasally • Peak of rush is over almost as soon as the user exhales • High typically lasts 5–10 minutes afterward

  32. Crack Cocaine • Another form, of freebase • Often called "crack" or "rocks“ • Created during early 1980s • Popular because it is cheap • Sodium bicarbonate (baking soda) is preferred in preparing the freebase • Commonly "cooked" the ratio of 50/50 to 40/60 % cocaine/bicarbonate • When the rock is heated, the water boils, making a crackling sound

  33. Chewed/eaten • Coca leaves typically are mixed with an alkaline substance (such as lime) and chewed in the same way as chewing tobacco • It is absorbed by the mucous membrane of the mouth and GI tract • Coca leaves can be infused in liquid and consumed like tea • Not readily absorbed when ingested alone • Need to be mixed with a highly alkaline substance (such as lime) to be absorbed through the stomach

  34. Coca Leaf InfusionsCoca Tea • Coca tea is used in coca-leaf producing countries much as any herbal medicinal tea. • The free and legal commercialization of dried coca leaves to be used as "coca tea" has been actively promoted by the governments of Peru and Bolivia for many years as a drink having medicinal powers. • Visitors to the city of Cuzco in Peru, and La Paz in Bolivia are greeted with the offering of coca leaf infusions (prepared in tea pots with whole coca leaves) purportedly to help the newly-arrived • The effects of drinking coca tea are a mild stimulation and mood lift • It does not produce any significant numbing of the mouth nor does it give a rush like snorting cocaine

  35. Insufflation“snorting," “sniffing," or "blowing" • Powder cocaine • The most common method of ingestion • Drug is absorbed through mucous membrane of sinuses • Absorption is approximately 30-60 % • Chronic use results in rhinitis and necrosis of the nasal membranes • Damage the inside of the nose since cocaine constricts blood vessel • Users report a burning sensation in the nostrils after cocaine's anesthetic effects wear off • Rolled up banknotes, hollowed-out pens, cut straws, and specialized spoons are often used to insufflate cocaine

  36. Injected Cocaine • The highest blood levels of drug in the shortest amount of time • Upon injection, cocaine reaches the brain in a matter of seconds • rush can be so intense that can induces uncontrollable vomit • Euphoria passes quickly • Aside from the toxic effects of cocaine, there is danger of • circulatory emboli from the substances used to cut the drug • risk of infection associated with use of contaminated needles • Speedball • Injected mixture of cocaine and heroin • Dangerous combination, as drugs complement each other

  37. StimulantsEcstasy/MDMA • Methylenedioxymethamphetamine • Often known as E, X, or XTC • Primary effect is inducing a general sense of openness, energy, euphoria, and well-being • Tactile sensations are enhanced, making physical contact with others more pleasurable • May produce aphrodisiac effects • A patent for MDMA was granted in 1914 to the German pharmaceutical company Merck • It was patented as an intermediate chemical used in the synthesis of a hydrastinine (a drug intended to control bleeding from wounds)

  38. Hallucinogens • Can cause subjective changes in perception, thought, emotion and consciousness • Induce experiences that are qualitatively different from those of ordinary consciousness • Three broad categories • Psychedelics • Dissociatives • Deliriants

  39. Hallucinogenous • Cannabissativa • Herbal form of the drug consists of dried mature leaves of pistillate ("female") plants • Hashish (resinous form) • Carefully produced and screened hashish is up to three times as potent as the highest quality herbal varieties • Active chemical compound in cannabis is: Δ9-tetrahydrocannabinol (THC)

  40. Psychedelic Any drug with perception-altering effects such as • Lysergic acid diethylamide (LSD), semisynthetic drug • synthesized from lysergic acid derived from ergot, a grain fungus that grows on rye • Psilocybin (psilocybine) • found in psilocybin mushroom • Mescaline occurs naturally in the • Peyote cactus, San Pedro cactus, Peruvian Torch cactus • Ayahuasca preparations (use for religious purposes) • Seeds of Morning Glory & Hawaiian Baby Woodrose

  41. Dissociatives Drugs • Reduce (or block) signals to the conscious mind from other parts of the brain, typically the physical senses • Such a state of sensory deprivation can produce hallucinations, and dreamlike states of mind • Some are • PCP (angel dust) • Ketamine (an anaesthetic) • DXM (dextromethorphan) active ingredient in many cough syrups • nitrous oxide (inhalant) • salvia divinorum (plant)

  42. Deliriants • Deliriants - effects similar to experience of delirious fevers • Considered to be true hallucinogens as users will • have conversations with people who aren't there • become angry with a 'person' mimicking their actions, not realizing it is their own reflection in a mirror • Included in this group are: • Plants such a: • deadly nightshade, mandrake, henbane and datura • Pharmaceutical drugs when taken in very high doses: • antihistamine diphenhydramine (Benadryl) • antiemetic dimenhydrinate (Dramamine or Gravol) • Native Americans can consumed large amounts of tobacco during religious ceremonies to experience deliriant effects. • Can be toxic, can cause death due to overdose.

  43. Metabolisms and Elimination • Elimination of most drugs by • enzymes synthesized by liver • Some are deactivates by being passed in: • urine, sweat, feces, mother's milk

  44. Drug Tolerance • Decreased sensitivity to a drug • Same doses has less effect • Need more drug to have same effect • Cross tolerance • Tolerance to the effect of one drug that develops as the result of exposure to another drug that act by same mechanism

  45. Drug ToleranceTwo type of changes • Metabolic Tolerance • results from a reduction in the amount of a drug getting to its sites of action • Functional Tolerance • results from a reduction in the reactivity of the nervous system (or other sites of action) to a drug • Tolerance to psychoactive drugs mainly fuctional

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