Drug Abuse/Overdose. By : Dr. Ragia M Hegazy, M.D. Assistant professor of Clinical Toxicology

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1 Drug Abuse/Overdose By : Dr. Ragia M Hegazy, M.D. Assistant professor of Clinical Toxicology

2 OPIATES DESIRED EFFECTS OF USE The Rush Sedation Euphoria Analgesia OPIUM COMES FROM THE POPPY PLANT PAPAVER SOMNIFERUM 2

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6 Papaver somniferum (opium poppy) After flowering, the petals drop in a few days leaving bulbous green capsules atop the stalks. These are the pods. 6

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8 Papaver somniferum Incisions are made in the pods and the milky fluid that oozes out is air dried. This must be done before the seeds are discharged. 8

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12 CONTENTS OF POPPY POD FLUID Active principle: opium BUT There are at least 20 other alkaloids (organic pharmacological agents) in the fluid it contains two group of active substances 3 CNS depressives: Morphine 4-21%, codiene1-25%, narcine 3 CNS stimutlatives: Narcotine, papaverine, thebaine

13 Classifications of opioids 1- pure agonists : Morphine Methadone & LAAM Pethidine Fentanyl Codeine, tramadol 2- partial agonists ( mixed- agonist- antagonist) Buprenorphine, pentazocine, nalbuphine & nalorphine. 3- pure antagonists : naloxone & naltroxone.

14 ACTION OF OPIUM Action: opium has 2 actions inhibitory and stimulatory Inhibitory: (-) Rs center central asphaxia (-) vasomoter center hypotension (-) CNS cortex sedation and analgesia (-) Intestinal motility constipation Stimulatory: (+) vagal n. bradycardia (+) acculomotor n. pin pointed miosis (+) CTZ vomiting (+) histamine release itching Cause of death: central asphaxia Heroin pupil 14

15 OPIATES MORPHINE a naturally occurring opiate HEROIN Heroin does not occur naturally, but is a semi - synthetic opiate HEROIN METABOLISM HEROIN (DIACETYLMORPHINE) HYDROLYZED MONOACETYL- MORPHINE (RESPONSIBLE FOR PHARMACOLOGIC EFFECTS) HYDROLYZED MORPHINE *see next slide for urine drug screen effects which result from heroin being made from morphine. 15

16 METHADONE Synthetic narcotic Used for treatment of narcotic addiction 16

17 METHADONE DRUG INTERACTIONS METHADONE LEVELS GO DOWN WITH USE OF: Carbamazepine Alcohol Phenobarbital Rifampin Methadone 10 mg METHADONE LEVELS GO UP WITH USE OF: Tagamet Ketoconazole Erthyromycin 17

18 LAAM L - Alpha - Acetylmethodol Acetate Long acting, orally active analog of Methadone ADVANTAGES OVER METHADONE Slower onset Longer duration of action Administer 3 times /week so diversion may be less likely times the patient s usual methadone dose DISADVANTAGES CARDIAC ARRHYTHMIAS ( TORSADES de POINTES) Manufacturing of this product has ceased. 18

19 BUPRENORPHINE PARTIAL OPIOID AGONIST Very high affinity for mu receptor Will displace Morphine, Methadone from the receptor, thus if given to someone maintained on Methadone or using opiates, it can cause significant withdrawal Desirable properties Low abuse potential Lower level of physical dependence Safety if ingested in overdose quantities Weak opioid effect as compared to Methadone 19

20 BUPRENORPHINE PHARMACOLOGIC USES Potent analgesic Available in many countries as a sublingual tablet ( mg) called Temgesic Available in the U.S. As an parenteral (IV, IM) form called Buprenex Poor oral bioavailability Sublingual with absorption through the oral mucosa Slow dissociation rate Prolonged therapeutic effect - so can be given every other or every third day Treatment of addictions* In the U.S. manufactured Subutex Suboxone 20

21 BUPRENORPHINE SUBUTEX 2 & 8 mg sublingual white tablets Schedule III under the Controlled Substance Act SUBOXONE Hexagonal orange sublingual tablets in 2 strengths 2 mg Buprenorphine with 0.5 mg Naloxone 8 mg Buprenorphine with 2 mg Naloxone Schedule III Use of Naloxone is to prevent IV use (diversion) Buprenorphine is absorbed sublingual and IV, but if used as a combination with Naloxone, the Naloxone IV can cause withdrawal. Naloxone is not absorbed sublingual. 21

22 HEROIN INTOXICATION MOST COMMON Miosis except Demerol (pupils dilate) Nodding Hypotension, Bradycardia Depressed respiration Euphoria, Floating feeling Pulmonary edema Seizures: Demerol, Darvon, Talwin Classic triad seen in overdose Miosis (small pupils) Coma Respiratory depression Heroin pupil 22

23 HEROIN WITHDRAWAL EARLY PHASE (8-12 after last dose of heroin): Lacrimation Rhinorrhea FLU LIKE SYMPTOMS Yawning (characteristic for opiate) Sweating Resembles severe influenza 23

24 HEROIN WITHDRAWAL - MIDDLE PHASE manifested Hs after last dose of heroin) Gooseflesh Hypothermia Restless sleep Dilated pupils Anorexia Irritability Tremor COLD TURKEY 24

25 HEROIN WITHDRAWAL - LATE PHASE (maximum in 2-3 days, disappear in 7-10 days): Increase in all previous signs and symptoms Increase in HR & Bl. P. Nausea, vomiting, &Diarrhea Abdominal cramps, Muscle spasm, Bone pain Depression Weakness 25

26 HEROIN WITHDRAWAL - TIME FRAME 1/2 life is 2-3 hours Onset after last dose is 8-12 hours Peak is 48 hours Duration is 7-10 days 26

27 PROTRACTED HEROIN WITHDRAWAL LASTS UP TO 9 MONTHS Weight gain Decrease in temperature Increase in RR, & Bl. P. Menstrual irregularities (secondary to increased prolactin) 27

28 HEROIN WITHDRAWAL TREATMENT INPATIENT POSSIBLE MEDICATIONS INCLUDE: Clonidine (catapress) 5µgm/kg oral with monitor of Bl. P. ethadone 10 mg Methadone (dolopine) (maintenance programs) it block the high euphoric effect of heroin Dose: 10 mg/4 Hs*1d oral then 40mg/d then gradual reduced by 5 mg daily. If withdrawal symptoms appear, reduction should proceed more slowly Naltrexone (trexan): competitive antagonist block the high euphoric effect of heroin but avoid in liver disease Dose: 50mg/d.*10 days then 100mg/3ds *another10 ds Buprenorphine (agonist antagonist:4-8mg prevent withdrawal) For agitation :Oxazepam (15-30 mg q 6 hours) or other BZD 28

29 OPIATE ACUTE OVERDOSE TREATMENT NARCAN (naloxone) Narcan is injected, usually initially IV for fastest action. Narcan after two minutes and last about minutes. Narcan reduce MR from overdose (caused by depressants of the CNS and respiratory system). Narcan may have to be repeated or the patient will lapse back into overdose symptoms Dose: 0.4 mg I.V., if no response repeat the dose every 2 min. till a total dose of 2mg. 29

30 OPIATES MANY OF THE COMPLICATIONS OF OPIATES ARE DUE TO THE ROUTE OF USE AND NOT THE DRUG Hepatitis or AIDs Neurologic Toxic amblyopia (toxic loss of sight) Mononeuropathy (one nerve involved) Polyneuropathy (several nerves involved) Meningitis Brain abscess Leukoencephalopathy (encephalopathy seen with smoking heroin) 30

31 OPIATES MANY OF THE COMPLICATIONS OF OPIATES ARE DUE TO THE ROUTE OF USE AND NOT THE DRUG Dermatologic Abscess Tracks Lymphangitis (inflammation of the lymph system) 31

32 OPIATES MANY OF THE COMPLICATIONS OF OPIATES ARE DUE TO THE ROUTE OF USE AND NOT THE DRUG Pulmonary Aspiration Pneumonia Lung abscess Pulmonary emboli (blood clot to the lung) Pulmonary fibrosis (thickening and scarring of connective tissue in the lung) Non-cardiogenic pulmonary edema Heroin lung case report!!!! due to central respiratory depression & hypoxia 32

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