DOCSLIB.ORG

Glutethimide Market in the United States of America Because of (S 116) and Methyprylon (S 117) Have Been Marketed Serious Side-Effects

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Glutethimide Market in the United States of America Because of (S 116) and Methyprylon (S 117) Have Been Marketed Serious Side-Effects 44 H. ISBELL & T. L. CHRUSCIEL 184. Swanson, L. A. & Okada, T. (1963) J. Amer. med. 186. Wilson, J. C. (1963) Amer. J. Psychiat., 120, 600-601 Ass., 184, 780 (Death after withdrawal of mepro- (Status epilepticus associated with withdrawal bamate) from deprol (meprobamate and benactyzine)) 185. Taddei, J. & Parmi, E. (1959) Boll. Soc. ital. Biol. 187. Veress, F., Major, V., Fink, M. & Freedman, A. M. sper., 35, 211-214 (Pharmacological observation (1969) J. clin. Pharmacol., 9, 232-238 (High dose on the meprobamate habit) tybamate therapy of heroin dependence) PIPERIDINEDIONE DERIVATIVES Of the seven drugs listed (Table VII), glutethimide market in the United States of America because of (S 116) and methyprylon (S 117) have been marketed serious side-effects. for the longest time. Originally, both glutethimide and methyprylon were advertised as being " non- REFERENCES barbiturate" hypnotics. Actually both drugs are pharmacologically quite similar to barbiturates and 188. Berger, H. (1961) J. Amer. med. Ass.. 177, 63 glutethimide is more toxic than barbiturates when (Addiction to methyprylon) taken in large doses. Shortly after both glutethimide 189. Horn, M. H. (1968) Fortschr. Neurol. Psychiat.. 36, and methyprylon became available, case reports 310-316 (Einige Aspekte der Methyprylonsucht) began to appear in the literature indicating that the 190. Jensen, R. (1960) N. Z. med. J., 59, 431 (Addiction two drugs caused dependence of the barbiturate- to Nodular. A report of 2 cases) 191. Johnson, F. A. & VanBuren, H. C. (1962) J. Amer. alcohol type in man.1881l95 Glutethimide has been med. Ass., 180, 1024 (Abstinence syndrome shown to induce dependence in dogs and monkeys following glutethimide intoxication) and to suppress abstinence from barbital in physically 192. Lloyd, E. A. & Clark, L. D. (1959) Dis. nerr. Syst., dependent dogs and monkeys. Accordingly, glute- 20, 1 (Convulsions and delirium incident to thimide must be judged to have dependence potential glutethimide (Doriden) withdrawal) of high degree equal to that of the barbiturate 193. Luby, E. D. & Domino, E. F. (1962) J. Amer. med. hypnotics. Although less well documented, methy- Ass., 181, 46 (Additional evidence of addiction prylon must be rated as having moderate or high liability of glutethimide) 194. Ossenfort, W. F. (1957) Dallas med. J., 43. 229 abuse liability. The potential for dependence of (Drug addictions) aminoglutethimide (S 112), and cinperene (S 113) 195. Sadwin, A. & Glen, R. S. (1958) Amer. J. Psychiat., may, by chemical and pharmacological analogy, be 115, 469 (Addiction to glutethimide-Doriden) assessed as being equal to that of methyprylon. 196. World Health Organization (1966) Drug Informa- Aminoglutethimide has been withdrawn from the tion No. 56, Geneva (unpublished document) Un a) C 'C > U a)EC1 C a)a)) x co w 0) EZ(CZ 0) ) a) CC z CDa w0 c CL Q o 0 CO IF C z o 0 *30= w 0C a. M 0 ._ 00 CZ. C E ) a)*z¢t Ca a)-M C0a( .0 0 4a)a)CC C E a) a a) C C.)o 0 oc co - s E .- " z.'Z.' Z: C - o ° 0 0~~~~~~~~~~~~~~ U(1 Da. o o o- o N° 0 .x CL Ua)D 0._ co c -c U a) 0". .0 ~.r0 N~~~~~~~~ -Ca > C E E E .C a) a a)co_ a)0Q a) - IZ >CC~~~~~~~~~~~~~~~~~~~~~~~~~C = M tn.-a4 -)zq0 .°- 0~ aasc)o U, o.0 Ca)C) Co (D Ca .0 a).e 3 ~~ E a)a) ~~~~~~~3 U_ (U a) a) a) 0 .0'al C--O.CO)t II CD~~~~~~~~~~~~~~ B ~~~~~~~~~EE .Cao° CCa0 0°c o) E .xo 0-. c .- E ~4c (n Oa) )n a 4D 03 z (n cn w Oto0 a o4 a) a. 04 E w C,)a z 4a) it w a) znj- o (- 0 >" c o .0 1 cn Ca- °cm D 0.7 I 0 E ao s "0 a) E) 0 Cq I 0 a)E.C~ ~ Z-I "Ua)0Q0> z 0 Q) -J -a ._ CIL -Z co@ 0=0) 0= C Q r aE ° a U z C~ ._ 0'-a LLJ a)E _w E H= C- z II E -0mE N E a5 C. ct 0CL I .3 00U 0_ Q 0 OVQ r- w 0. ._ -J ('4 C.) r mco m- ,_ 0) I)V. :5 I, = WU) U) L~ C 45 0 U) 0 0C) 0 C C) - 0 U) LU a 0- aLU 0 0~~~~~~~~~~~~~ z 0 a LU a ic~~~~~~~~~~~~~~~~~~~~~a. z 00~~~ C0 0~~~~~~-.C .0C 0.oE 0 0~~ .O0.CC 0 0..C-0 4.00 0 0 0CCCC C-0C C .0.0 0. _ 02 0 C. ~~~~~~~>00 0 . !o 30I. 0 0'.- co C C 0c 00 :E 0 $--0 ~ ~ ~ UC0 E ~ E O.0 0 0 0"- LU 0 CD IL 0 0 ~ ~ ~ ~ ~ ~ ~ ~ ~~00 co Z5 ZC0 o 0 00= oc tL 0 0 ~~~~~~~~~~~~~~~~00 0 0 0- 0 z z az C * LU) a LU) 0) LU 0 0 LU E2 C In 0 0 in ._ Ct m C E 0 .0 000 ._ 0 x x >% LU) coX I-Z O 3r 0 E y= \ O=X ,a a :2,IQ Z Q QL -) I I - 0= Z-I I t 0 011 00= 0 Co) U t 0 0o EM 0.b. / - 0 ICl)IC,) f C I I In O h- U I- ., 00U a) 6 Ct CL 0I z U- C. E U) U)- U)~~~~~~~~~V -46.
Load more

Recommended publications
  • Definition of Controlled Substance Schedules
    UPDATED MARCH 2018 DEFINITION OF CONTROLLED SUBSTANCE SCHEDULES Drugs and other substances that are considered controlled substances under the Controlled Substances Act (CSA) are divided into five schedules. An updated and complete list of the schedules is published annually in Title 21 Code of Federal Regulations (C.F.R.) §§ 1308.11 through 1308.15. Substances are placed in their respective schedules based on whether they have a currently accepted medical use in treatment in the U.S., their relative abuse potential, and likelihood of causing dependence when abused. Examples of the drugs in each schedule are listed below. Schedule I Controlled Substances Substances in this schedule have no currently accepted medical use in the United States, a lack of accepted safety for use under medical supervision, and a high potential for abuse. Some examples of substances listed in Schedule I are: heroin, lysergic acid diethylamide (LSD), marijuana (cannabis), peyote, methaqualone, and 3,4- methylenedioxymethamphetamine ("Ecstasy"). Schedule II/IIN Controlled Substances (2/2N) Substances in this schedule have a high potential for abuse which may lead to severe psychological or physical dependence. Examples of Schedule II narcotics include: hydromorphone (Dilaudid®), methadone (Dolophine®), meperidine (Demerol®), oxycodone (OxyContin®, Percocet®), and fentanyl (Sublimaze®, Duragesic®). Other Schedule II narcotics include: morphine, opium, codeine, and hydrocodone. Examples of Schedule IIN stimulants include: amphetamine (Dexedrine®, Adderall®), methamphetamine (Desoxyn®), and methylphenidate (Ritalin®). Other Schedule II substances include: amobarbital, glutethimide, and pentobarbital. 1 Schedule III/IIIN Controlled Substances (3/3N) Substances in this schedule have a potential for abuse less than substances in Schedules I or II and abuse may lead to moderate or low physical dependence or high psychological dependence.
    [Show full text]
  • Drug-Facilitated Sexual Assault Panel, Blood
    DRUG-FACILITATED SEXUAL ASSAULT PANEL, BLOOD Blood Specimens (Order Code 70500) Alcohols Analgesics, cont. Anticonvulsants, cont. Antihistamines, cont. Ethanol Phenylbutazone Phenytoin Cyclizine Amphetamines Piroxicam Pregabalin Diphenhydramine Amphetamine Salicylic Acid* Primidone Doxylamine BDB Sulindac* Topiramate Fexofenadine Benzphetamine Tapentadol Zonisamide Guaifenesin Ephedrine Tizanidine Antidepressants Hydroxyzine MDA Tolmetin Amitriptyline Loratadine MDMA Tramadol Amoxapine Oxymetazoline* Mescaline* Anesthetics Bupropion Pyrilamine Methcathinone Benzocaine Citalopram Tetrahydrozoline Methamphetamine Bupivacaine Clomipramine Triprolidine Phentermine Etomidate Desipramine Antipsychotics PMA Ketamine Desmethylclomipramine 9-hydroxyrisperidone Phenylpropanolamine Lidocaine Dosulepin Aripiprazole Pseudoephedrine Mepivacaine Doxepin Buspirone Analgesics Methoxetamine Duloxetine Chlorpromazine Acetaminophen Midazolam Fluoxetine Clozapine Baclofen Norketamine Fluvoxamine Fluphenazine Buprenorphine Pramoxine* Imipramine Haloperidol Carisoprodol Procaine 1,3-chlorophenylpiperazine (mCPP) Mesoridazine Cyclobenzaprine Rocuronium Mianserin* Norclozapine Diclofenac Ropivacaine Mirtazapine Olanzapine Etodolac Antibiotics Nefazodone Perphenazine Fenoprofen Azithromycin* Nordoxepin Pimozide Hydroxychloroquine Chloramphenicol* Norfluoxetine Prochlorperazine Ibuprofen Ciprofloxacin* Norsertraline Quetiapine Ketoprofen Clindamycin* Nortriptyline Risperidone Ketorolac Erythromycin* Norvenlafaxine Thioridazine Meclofenamic Acid* Levofloxacin* Paroxetine
    [Show full text]
  • House Bill No.11 (2019)
    LEGISLATURE OF THE STATE OF IDAHO Sixty-fifth Legislature First Regular Session - 2019 IN THE HOUSE OF REPRESENTATIVES HOUSE BILL NO. 11 BY HEALTH AND WELFARE COMMITTEE 1 AN ACT 2 RELATING TO CONTROLLED SUBSTANCES; AMENDING SECTION 37-2705, IDAHO CODE, TO 3 REVISE THE LIST OF SCHEDULE I CONTROLLED SUBSTANCES; AMENDING SECTION 4 37-2709, IDAHO CODE, TO PROVIDE AN EXCLUSION AND TO MAKE A TECHNICAL 5 CORRECTION; AMENDING SECTION 37-2713, IDAHO CODE, TO REVISE THE LIST OF 6 SCHEDULE V DRUGS AND SUBSTANCES; AND DECLARING AN EMERGENCY. 7 Be It Enacted by the Legislature of the State of Idaho: 8 SECTION 1. That Section 37-2705, Idaho Code, be, and the same is hereby 9 amended to read as follows: 10 37-2705. SCHEDULE I. (a) The controlled substances listed in this sec- 11 tion are included in schedule I. 12 (b) Any of the following opiates, including their isomers, esters, 13 ethers, salts, and salts of isomers, esters, and ethers, unless specifically 14 excepted, whenever the existence of these isomers, esters, ethers and salts 15 is possible within the specific chemical designation: 16 (1) Acetyl-alpha-methylfentanyl (N-[1-(1-methyl-2-phenethyl)-4-pip- 17 eridinyl]-N-phenylacetamide); 18 (2) Acetylmethadol; 19 (3) Acetyl fentanyl (N-(1-phenethylpiperidin-4-yl)-N-phenylac- 20 etamide); 21 (4) Allylprodine; 22 (5) Alphacetylmethadol (except levo-alphacetylmethadol also known as 23 levo-alpha-acetylmethadol, levomethadyl acetate or LAAM); 24 (6) Alphameprodine; 25 (7) Alphamethadol; 26 (8) Alpha-methylfentanyl; 27 (9) Alpha-methylthiofentanyl
    [Show full text]
  • Pharmaceuticals As Environmental Contaminants
    PharmaceuticalsPharmaceuticals asas EnvironmentalEnvironmental Contaminants:Contaminants: anan OverviewOverview ofof thethe ScienceScience Christian G. Daughton, Ph.D. Chief, Environmental Chemistry Branch Environmental Sciences Division National Exposure Research Laboratory Office of Research and Development Environmental Protection Agency Las Vegas, Nevada 89119 [email protected] Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada Why and how do drugs contaminate the environment? What might it all mean? How do we prevent it? Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada This talk presents only a cursory overview of some of the many science issues surrounding the topic of pharmaceuticals as environmental contaminants Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada A Clarification We sometimes loosely (but incorrectly) refer to drugs, medicines, medications, or pharmaceuticals as being the substances that contaminant the environment. The actual environmental contaminants, however, are the active pharmaceutical ingredients – APIs. These terms are all often used interchangeably Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada Office of Research and Development Available: http://www.epa.gov/nerlesd1/chemistry/pharma/image/drawing.pdfNational
    [Show full text]
  • Commonly Abused Prescription and Otc Medications
    C OMMONLY A BUSED P RESCRIPTION AND OTC MEDIcaTIONS Substance Examples of Commercial and Street Names DEPRESSANTS barbiturates Amytal, Nembutal, Seconal, Phenobarbital; barbs, reds, red birds, phennies, tooies, yellows, yellow jackets Benzodiazepines Ativan, Halcion, Librium, Valium, Xanax; candy, downers, sleeping (other than flunitrazepam) pills, tranks Flunitrazepam Rohypnol; forget-me pill, Mexican Valium, R2, Roche, roofies, (associated with sexual assaults; roofinol, rope, rophies not sold in US, but may be brought in) OPIOIDS AND MORPHINE DERIVATIVES codeine Empirin with Codeine, Fiorinal with Codeine, Robitussin A-C, Tylenol with Codeine; Captain Cody, Cody, schoolboy; (with glutethimide) doors & fours, loads, pancakes and syrup fentanyl and fentanyl analogs Actiq (oral), Duragesic (patch), Sublimaze; Apache, China girl, China white, dance fever, goodfella, jackpot, murder 8, TNT, Tango & Cash morphine Roxanol, Duramorph; M, Miss Emma, monkey, white stuff oxycodone HCL Oxycontin; Oxy, O.C., killer hydrocodone bitartrate, acetaminophen Vicodin; vike, Watson-387 STIMULANTS amphetamine Biphetamine, Dexedrine, Adderall; bennies, black beauties, crosses, hearts, LA turnaround, speed, truck drivers, uppers methylphenidate Ritalin; JIF, MPH, R-ball, Skippy, the smart drug, vitamin R (safe & effective for treatment of ADHD) OVER-THE-COUNTER (OTC) MEDICATION Dextromethorphan (DXM) Found in any cold medicine with “DM” or “Tuss” in the title or name; Orange Crush, Triple C’s, C-C-C, Red Devils, Skittles, Dex, Vitamin D, Robo, Robo-trippin’,
    [Show full text]
  • Chloral Hydrate: Summary Report
    Chloral Hydrate: Summary Report Item Type Report Authors Yuen, Melissa V.; Gianturco, Stephanie L.; Pavlech, Laura L.; Storm, Kathena D.; Yoon, SeJeong; Mattingly, Ashlee N. Publication Date 2020-02 Keywords Compounding; Food, Drug, and Cosmetic Act, Section 503B; Food and Drug Administration; Outsourcing facility; Drug compounding; Legislation, Drug; United States Food and Drug Administration; Chloral Hydrate Rights Attribution-NoDerivatives 4.0 International Download date 26/09/2021 09:06:16 Item License http://creativecommons.org/licenses/by-nd/4.0/ Link to Item http://hdl.handle.net/10713/12087 Summary Report Chloral Hydrate Prepared for: Food and Drug Administration Clinical use of bulk drug substances nominated for inclusion on the 503B Bulks List Grant number: 2U01FD005946 Prepared by: University of Maryland Center of Excellence in Regulatory Science and Innovation (M-CERSI) University of Maryland School of Pharmacy February 2020 This report was supported by the Food and Drug Administration (FDA) of the U.S. Department of Health and Human Services (HHS) as part of a financial assistance award (U01FD005946) totaling $2,342,364, with 100 percent funded by the FDA/HHS. The contents are those of the authors and do not necessarily represent the official views of, nor an endorsement by, the FDA/HHS or the U.S. Government. 1 Table of Contents REVIEW OF NOMINATION ..................................................................................................... 4 METHODOLOGY ...................................................................................................................
    [Show full text]
  • Flunitrazepam Elisa Kit Instructions Product #109519 & 109516 Forensic Use Only
    Neogen Corporation 944 Nandino Blvd., Lexington KY 40511 USA 800/477-8201 USA/Canada | 859/254-1221 Fax: 859/255-5532 | E-mail: [email protected] | Web: www.neogen.com/Toxicology FLUNITRAZEPAM ELISA KIT INSTRUCTIONS PRODUCT #109519 & 109516 FORENSIC USE ONLY INTENDED USE: For the determination of trace quantities of Flunitrazepam and/or other metabolites in human urine, blood, oral fluid. DESCRIPTION Neogen Corporation’s Flunitrazepam ELISA (Enzyme-Linked ImmunoSorbent Assay) test kit is a qualitative one-step kit designed for use as a screening device for the detection of drugs and/or their metabolites. The kit was designed for screening purposes and is intended for forensic use only. It is recommended that all suspect samples be confirmed by a quantitative method such as gas chromatography/mass spectrometry (GC/MS). ASSAY PRINCIPLES Neogen Corporation’s test kit operates on the basis of competition between the drug or its metabolite in the sample and the drug-enzyme conjugate for a limited number of antibody binding sites. First, the sample or control is added to the microplate. Next, the diluted drug-enzyme conjugate is added and the mixture is incubated at room temperature. During this incubation, the drug in the sample or the drug-enzyme conjugate binds to antibody immobilized in the microplate wells. After incubation, the plate is washed 3 times to remove any unbound sample or drug-enzyme conjugate. The presence of bound drug-enzyme conjugate is recognized by the addition of K-Blue® Substrate (TMB). After a 30 minute substrate incubation, the reaction is halted with the addition of Red Stop Solution.
    [Show full text]
  • Drug Interactions and Lethal Drug Combinations
    J Clin Pathol: first published as 10.1136/jcp.s3-9.1.94 on 1 January 1975. Downloaded from J. clin. Path., 28, Suppl. (Roy. Coll. Path.), 9, 94-98 The drug dilemma-benefits and hazards Drug interactions and lethal drug combinations ALAN RICHENS From the Department of Clinical Pharmacology, St Bartholomew's Hospital, London Although the development of drugs of greater example, aspirin can displace oral anticoagulants potency and efficacy confers on the physician from their plasma-protein-binding sites, and in- increasing power to treat serious diseases, it also directly acting sympathomimetics contained in cough increases the number and seriousness of potential mixtures can cause a hypertensive crisis in patients adverse effects and drug interactions which can on monoamine oxidase inhibitors. Self-medication is occur. Most hospital patients receive more than one common, and often involves drugs obtained on drug at a time, the average number often being prescription for a previous illness. greater than five (Smith, Seidl, and Cluff, 1966). The 4 When several clinics or doctors are involved in incidence of drug reactions rises with the number of the care of a patient, one doctor may not be aware of drugs prescribed simultaneously. In patients pre- what another has prescribed. scribed one to five drugs the incidence of reactions is 5 When preparations which contain more than 18-6%, while in patients prescribed six or more one ingredient are prescribed by their trade names. it rises to 814 % (Hurwitz and Wade, 1969). There are a number of ways in which drugs may The Boston Collaborative Drug Surveillance interact.
    [Show full text]
  • Clinical Practice Guideline for the Pharmacologic Treatment of Chronic Insomnia in Adults: an American Academy of Sleep Medicine Clinical Practice Guideline Michael J
    pii: jc-00382-16 http://dx.doi.org/10.5664/jcsm.6470 SPECIAL ARTICLES Clinical Practice Guideline for the Pharmacologic Treatment of Chronic Insomnia in Adults: An American Academy of Sleep Medicine Clinical Practice Guideline Michael J. Sateia, MD1; Daniel J. Buysse, MD2; Andrew D. Krystal, MD, MS3; David N. Neubauer, MD4; Jonathan L. Heald, MA5 1Geisel School of Medicine at Dartmouth, Hanover, NH; 2University of Pittsburgh School of Medicine, Pittsburgh, PA; 3University of California, San Francisco, San Francisco, CA; 4Johns Hopkins University School of Medicine, Baltimore, MD; 5American Academy of Sleep Medicine, Darien, IL Introduction: The purpose of this guideline is to establish clinical practice recommendations for the pharmacologic treatment of chronic insomnia in adults, when such treatment is clinically indicated. Unlike previous meta-analyses, which focused on broad classes of drugs, this guideline focuses on individual drugs commonly used to treat insomnia. It includes drugs that are FDA-approved for the treatment of insomnia, as well as several drugs commonly used to treat insomnia without an FDA indication for this condition. This guideline should be used in conjunction with other AASM guidelines on the evaluation and treatment of chronic insomnia in adults. Methods: The American Academy of Sleep Medicine commissioned a task force of four experts in sleep medicine. A systematic review was conducted to identify randomized controlled trials, and the Grading of Recommendations Assessment, Development, and Evaluation (GRADE) process was used to assess the evidence. The task force developed recommendations and assigned strengths based on the quality of evidence, the balance of benefits and harms, and patient values and preferences.
    [Show full text]
  • 483 Administrative Records, Texas Department of Criminal Justice
    Consistent with the terms of the Court’s May 22, 2017 scheduling order, the record has been redacted for all information that plaintiff, Texas Department of Criminal Justice (Texas), has identified as confidential. In addition, Defendants have also redacted information that the drug’s supplier and broker have separately advised the agency they consider confidential and private, as well as information the agency itself generally treats as confidential. This information has been redacted pending final FDA’s review of confidentiality claims, and our filing of the record with these redactions does not necessarily reflect our agreement with all of the claims of confidentiality Defendants have received. Defendants explicitly reserve the right to make an independent determination regarding the proper scope of redactions at a later time. Should we identify any of Texas’s redactions that are over-broad or otherwise improper, we will work with Texas’s counsel to revise the redactions in the record. Exhibit 14 FDA 095 Case 1:11-cv-00289-RJL Document 13-3 Filed 04/20/11 Page 1 of 74 CERTJFICATE Pursuant to the provisions ofRule 44 ofthe Federal Rules ofCivil Procedure, I hereby certifY that John Verbeten, Director ofthe Operations and Policy Branch, Division of Import Operations and Policy, Office ofRegional Operations, Office ofRegulatory Affairs, United States Food and Drug Administration, whose declaration is attached, has custody ofofficial records ofthe United States Food and Drug Administration. In witness whereof, I have, pursuant to the provision ofTitle 42, United States Code, Section 3505, and FDA StaffManual Guide 1410.23, hereto set my hand and caused the seal ofthe Department ofHealth and Human Services to be affixed th.is ~oi{.
    [Show full text]
  • Jack Deruiter, Principles of Drug Action 2, Fall 2003 1
    Jack DeRuiter, Principles of Drug Action 2, Fall 2003 BARBITURATE ANALOGUES AND OTHER SEDATIVE-HYPNOTICS I. Primidone (Mysoline) O CH2CH3 O CH2CH3 R H N N H ON O N O H H H Phenobarbital Primidone ("2-deoxyphenobarbital") Structure, Chemistry and Actions: The 2-deoxy analogue of phenobarbital. Primidone is similar to phenobarbital in its chemical properties, except that it is not acidic (not an imide!). It is metabolized by oxidation to phenobarbital and phenylethylmalonamide (PEMA), both of which have anticonvulsant activity (tonic/clonic and partial seizures) and may express their actions by a mechanism similar to the barbiturates (GABA actions). Thus primidone could be considered to be a prodrug: O CH2CH3 H N O CH2CH3 O N O H O CH2CH3 CYP H N H Phenobarbital H CYP N N O H HO H N O O CH CH H 2 3 Primidone H (2-deoxyphenobarbital) H2N Oxidation Intermediate H2N O PEMA Absorption/Distribution: Primidone is readily absorbed from the GI tract yielding peak serum concentrations occur in 3 hours. Peak serum concentrations of PEMA occur after 7 to 8 hours. Phenobarbital appears in plasma after several days of continuous therapy. Protein binding of primidone and PEMA is negligible; phenobarbital is about 50% protein bound. Monitoring of primidone therapy should include plasma level determinations of primidone and phenobarbital. Metabolism/Execretion: PEMA is the major metabolite and is less active than primidone. Phenobarbital formation ranges from 15% to 25%. The plasma half-life of primidone is 5-15 hours. PEMA and phenobarbital have longer half-lives (10-18 hours and 53-140 hours, respectively) and accumulate with chronic use.
    [Show full text]
  • Drug/Substance Trade Name(S)
    A B C D E F G H I J K 1 Drug/Substance Trade Name(s) Drug Class Existing Penalty Class Special Notation T1:Doping/Endangerment Level T2: Mismanagement Level Comments Methylenedioxypyrovalerone is a stimulant of the cathinone class which acts as a 3,4-methylenedioxypyprovaleroneMDPV, “bath salts” norepinephrine-dopamine reuptake inhibitor. It was first developed in the 1960s by a team at 1 A Yes A A 2 Boehringer Ingelheim. No 3 Alfentanil Alfenta Narcotic used to control pain and keep patients asleep during surgery. 1 A Yes A No A Aminoxafen, Aminorex is a weight loss stimulant drug. It was withdrawn from the market after it was found Aminorex Aminoxaphen, Apiquel, to cause pulmonary hypertension. 1 A Yes A A 4 McN-742, Menocil No Amphetamine is a potent central nervous system stimulant that is used in the treatment of Amphetamine Speed, Upper 1 A Yes A A 5 attention deficit hyperactivity disorder, narcolepsy, and obesity. No Anileridine is a synthetic analgesic drug and is a member of the piperidine class of analgesic Anileridine Leritine 1 A Yes A A 6 agents developed by Merck & Co. in the 1950s. No Dopamine promoter used to treat loss of muscle movement control caused by Parkinson's Apomorphine Apokyn, Ixense 1 A Yes A A 7 disease. No Recreational drug with euphoriant and stimulant properties. The effects produced by BZP are comparable to those produced by amphetamine. It is often claimed that BZP was originally Benzylpiperazine BZP 1 A Yes A A synthesized as a potential antihelminthic (anti-parasitic) agent for use in farm animals.
    [Show full text]