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Drugs : Organization by Pharmacology. Narcotic Drugs  Pharmacologically classified as an analgesic  Central Nervous System Depressants  Popular drugs.

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Presentation on theme: "Drugs : Organization by Pharmacology. Narcotic Drugs  Pharmacologically classified as an analgesic  Central Nervous System Depressants  Popular drugs."— Presentation transcript:

1 Drugs : Organization by Pharmacology

2 Narcotic Drugs  Pharmacologically classified as an analgesic  Central Nervous System Depressants  Popular drugs – heroin, morphine, codeine, methadone and propoxyphene  Pharmacologically classified as an analgesic  Central Nervous System Depressants  Popular drugs – heroin, morphine, codeine, methadone and propoxyphene

3 Hallucinogens  Marijuana  Derived from the plant Cannabis  Hashish – concentrated  Sinsemilla – unfertilized flowering tops of the female Cannabis plant  Active ingredient is THC  Potency is normally 4-5%  Simsemilla averages 6-12%  Liquid hashish averages 8- 22%  Potential medical uses  Marijuana  Derived from the plant Cannabis  Hashish – concentrated  Sinsemilla – unfertilized flowering tops of the female Cannabis plant  Active ingredient is THC  Potency is normally 4-5%  Simsemilla averages 6-12%  Liquid hashish averages 8- 22%  Potential medical uses

4 Hallucinogens  LSD – derived from ergot, a fungus of certain grains and grasses  Powerful drug  Visual hallucinations, changes in moods, anxiety, tension, etc  Flashbacks possible  Phencyclidine – PCP  Human response unpredictable  Dangerous drug – paranoia and violence possible  Schizophrenic behavior possible days after use  Methylenedioxymethamphetamine (aka MDMA or ecstasy)  Originally patented as appetite suppressant  Severe adverse reactions, including fatal side effects  LSD – derived from ergot, a fungus of certain grains and grasses  Powerful drug  Visual hallucinations, changes in moods, anxiety, tension, etc  Flashbacks possible  Phencyclidine – PCP  Human response unpredictable  Dangerous drug – paranoia and violence possible  Schizophrenic behavior possible days after use  Methylenedioxymethamphetamine (aka MDMA or ecstasy)  Originally patented as appetite suppressant  Severe adverse reactions, including fatal side effects

5 Depressants  Alcohol (aka ethanol, ethyl alcohol, booze, etc.)  Central nervous system depressant  Legalized and most widely used drug  A common effect is impairment  Legal blood alcohol level in Oklahoma  is 0.10%, or 100 mg/dL  Barbiturates  All are derivatives of barbituric acid  Big 5: amobarbital, secobarbital, phenobarbital, pentobarbital and butalbital  Methaqualon . Tranquilizers  Major players: reserpine, chlorpromazine, meprobamate, chlordiazepoxide, diazepam  Inhalants  Volatile organic solvents – toluene, naphtha, gasoline among others  Initial exhilaration and euphoria followed by impaired judgment, drowsiness and stupor  Danger of liver, heart and brain damage  Alcohol (aka ethanol, ethyl alcohol, booze, etc.)  Central nervous system depressant  Legalized and most widely used drug  A common effect is impairment  Legal blood alcohol level in Oklahoma  is 0.10%, or 100 mg/dL  Barbiturates  All are derivatives of barbituric acid  Big 5: amobarbital, secobarbital, phenobarbital, pentobarbital and butalbital  Methaqualon . Tranquilizers  Major players: reserpine, chlorpromazine, meprobamate, chlordiazepoxide, diazepam  Inhalants  Volatile organic solvents – toluene, naphtha, gasoline among others  Initial exhilaration and euphoria followed by impaired judgment, drowsiness and stupor  Danger of liver, heart and brain damage

6 Stimulants  Amphetamines  Initial feeling of well-being and alertness followed by fatigue and a loss of appetite  Amphetamine, methamphetamine and “ice” (crystal meth) are favorites  Phenmetrazine and phendimetrazine have similar properties  Cocaine  First used medically by Freud in Europe  Medical use is now limited  Extracted from the leaves of coca plant (Erythroxylon coca)  “Crack” cocaine is the drug of choice  Cocaine produces the strongest psychological compulsions for continued use  Amphetamines  Initial feeling of well-being and alertness followed by fatigue and a loss of appetite  Amphetamine, methamphetamine and “ice” (crystal meth) are favorites  Phenmetrazine and phendimetrazine have similar properties  Cocaine  First used medically by Freud in Europe  Medical use is now limited  Extracted from the leaves of coca plant (Erythroxylon coca)  “Crack” cocaine is the drug of choice  Cocaine produces the strongest psychological compulsions for continued use

7 Drugs: Organized by Control Laws  Federal law restricting the manufacture and distribution of dangerous substances  The U.S. Attorney General has the authority to change the schedules  The criminal penalties associated with this law are greatest with schedules I and II.  Federal law restricting the manufacture and distribution of dangerous substances  The U.S. Attorney General has the authority to change the schedules  The criminal penalties associated with this law are greatest with schedules I and II.

8 Controlled Substances Act  Schedule I  No medical use  High potential for abuse  Heroin, LSD, methaqualone and marijuana High potential for abuse  Cocaine, opiates, PCP, amphetamines, methadone and fast-acting barbiturates  Schedule II  Accepted medical use  Potential for psychological or physical dependence  Cocaine, opiates, PCP, amphetamines, methadone and fast-acting barbiturates  Schedule III  Less potential for abuse than schedules I and II  Currently accepted medical use  Potential for low or moderate physical dependence or high psychological dependence  Anabolic steroids, some codeine preparations and some barbiturate preparations (phenobarbital not included)  Schedule I  No medical use  High potential for abuse  Heroin, LSD, methaqualone and marijuana High potential for abuse  Cocaine, opiates, PCP, amphetamines, methadone and fast-acting barbiturates  Schedule II  Accepted medical use  Potential for psychological or physical dependence  Cocaine, opiates, PCP, amphetamines, methadone and fast-acting barbiturates  Schedule III  Less potential for abuse than schedules I and II  Currently accepted medical use  Potential for low or moderate physical dependence or high psychological dependence  Anabolic steroids, some codeine preparations and some barbiturate preparations (phenobarbital not included)

9 Controlled Substances Act  Schedule IV  Low potential for abuse relative to schedule III drugs  Currently accepted medical use  Relatively low limited dependence risk  Propoxyphene, phenobarbital, meprobamate, diazepam and chlordiazepoxide  Schedule V  Low abuse potential  Medical use  Less potential for producing dependency  Certain opiate drug mixtures that contain non-narcotic medicinal ingredients  Designer drugs  Can be placed under schedule I  Fentanyl analogues  Control of chemical precursors  Example – precursors to amphetamine, methamphetamine and PCP are controlled as schedule II substances  Schedule IV  Low potential for abuse relative to schedule III drugs  Currently accepted medical use  Relatively low limited dependence risk  Propoxyphene, phenobarbital, meprobamate, diazepam and chlordiazepoxide  Schedule V  Low abuse potential  Medical use  Less potential for producing dependency  Certain opiate drug mixtures that contain non-narcotic medicinal ingredients  Designer drugs  Can be placed under schedule I  Fentanyl analogues  Control of chemical precursors  Example – precursors to amphetamine, methamphetamine and PCP are controlled as schedule II substances

10  Extraction, Separation and isolation  Liquid-Liquid  TLC  HPLC  Characterization  Color tests - often termed presumptive tests  Marquis – purple color in presence of opiates and orange- brown in presence of amphetamines  Dillie-Koppanyi – violet-blue color in presence of barbiturates  Duquenois-Levine – purple color in presence of marijuana  Van Urk – blue-purple color in presence of LSD  Scott – blue color in presence of cocaine  Characterization  UV and IR Spectroscopy  GC-MS  Extraction, Separation and isolation  Liquid-Liquid  TLC  HPLC  Characterization  Color tests - often termed presumptive tests  Marquis – purple color in presence of opiates and orange- brown in presence of amphetamines  Dillie-Koppanyi – violet-blue color in presence of barbiturates  Duquenois-Levine – purple color in presence of marijuana  Van Urk – blue-purple color in presence of LSD  Scott – blue color in presence of cocaine  Characterization  UV and IR Spectroscopy  GC-MS Drugs: Organized by Chemistry

11  Note that the neutral classification includes thosedrugs that have no ionizable center and those which are amphoteric  Alkaloids are generally derived from plants ehile the nonalkaloids are syhtthetic or semisynthetic

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13 Methyl Salicylate - Aspirin pKa = 3.5 Morphine amphoteric Dia(acetyl)morphine - opiod, active ingredient in heroin pKa = 8

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23 HPLC Separation of Methamphetamines Column: C8, 4.6 x 150 mm Mobile Phase: 85% 25 mM phosphate buffer 15% ACN Flow Rate: 1.0 mL/min Temperature: 35°C Detection: 254 nm Sample: AmphetaminespKa 1. Phenylpropanolamine Ephedrine9.6 3.Amphetamine Methamphetamine Phenteramine10.1

24 5. Aspirin (acetylsalicylic acid) has a of 3.5. The pH of the stomach is approximately 1, while the pH of the intestines is approximately 6. Calculate the fraction of aspirin that is ionized in each area (show your work), and use the results to predict where the drug is preferentially absorbed. 6. Repeat the calculation in Question 5 for caffeine, a weak base with a of Diazepam tablets are supplied in 2-, 5-, and 10-mg increments. Suppose several tablets are received in a laboratory as evidence and, using the Physician’s Desk Reference, an analyst was able to tentatively identify them as Valium®, 10 mg. Suppose further that you learn that the tablets also contain anhydrous lactose, starches, dyes, and calcium stearate. Describe a method for isolating the active ingredient from fillers, using a LLE scheme. Justify and explain each step of the method. 8. Quinine is a dibasic molecule with of 5.1 and 9.7. It is encountered as a diluent (cutting agent) for heroin. To extract quinine from an aqueous solution, what pH should be used and why? 9. Devise a solvent extraction method that could be used to separate a mixture of powdered sugar, cornstarch, cocaine, and amphetamine. Justify each step and separation. Problems; Bell page 128


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