Methadone Barbiturates

Examples narcotics such as meperidine, methadone, morphine, oxycodone amphetamines and barbiturates... 

Ibrahim RB, Wilson JG, Thorsby ME, et al Effect of buprenorphine on CYP3Aactivity in rat and human liver microsomes. Life Sci 66 1293—1298, 2000 Iguchi MY, Handelsman L, Bickel WK, et al Benzodiazepine and sedative use/abuse by methadone maintenance clients. Drug Alcohol Depend 32 257—266, 1993 Isbell H Manifestations and treatment of addiction to narcotic drugs and barbiturates. Med Clin North Am 34 423 38, 1950... 

Depressants alcohol, barbiturates Opioids heroin, morphine, methadone... 

Deaths, cardiac and resp have been reported during initiation and conversion of pain pts to methadone Tx from Tx w/ other opioids Uses Severe pain detox w/ maint of narcotic addiction Action Narcotic analgesic Dose Adults. 2.5-10 mg IM q3-8h or 5-15 mg PO q8h titrate as needed Feds. 0.7 mg/kg/24 h PO or IM -s- q8h T slowly to avoid resp depression X in renal impair Caution [B/D (prolonged use/high doses at term), + (w/ doses =/> 20 mg/24 h)], severe liver Dz Disp Tabs, inj SE Resp depression, sedation, constipation, urinary retention, T QT interval, arrhythmias Interactions T Effects W/ cimetidine, CNS depressants, protease inhibitors EtOH T effects OF anticoagulants, antihistamines, barbiturates, glutethimide, methocarbamol ... 

Opiates Methadone Amphetamines Barbiturates Cocaine Benzodiazepines... 

T effects OF amiodarone, astemizole, atorvastadn, barbiturates, bepridil, bupropion, cerivastatin, cisapride, clorazepate, clozapine, clarithromycin, desipramine, diazepam, encainide, ergot alkaloids, estazolam, flecainide, flurazepam, indinavir, ketoconazole, lovastatin, meperidine, midazolam, nelfinavir, phenytoin, pimozide, piroxicam, propafenone, propoxyphene, quinidine, rifabutin, saquinavir, sildenafil, simvastatin, SSRIs, TCAs, terfenadine, triazolam, troleandomycin, zolpidem X effects W/ barbiturates, carbamazepine, phenytoin, rifabutin, rifampin, St. John s wort, tobacco X effects OF didanosine, hypnotics, methadone, OCPs, sedatives, theophylline, warfarin EMS T Effects of amiodarone, diazepam, midazolam and BBs, may need X- doses concurrent use of Viagra-type drugs can lead to hypotension X- effects of warfarin concurrent EtOH use can T adverse effects T glucose ODs May cause an extension of adverse SEs symptomatic and supportive Rivasrigmine (Exelon) [Cholinesterase Inhibitor/Anri ... 

Naloxone (Narcan) and naltrexone hydrochloride (Trexan) reverse the respiratory depressant action of narcotics related to morphine, meperidine, and methadone. They differ from other narcotic analgesics in several respects. Naloxone does not cause respiratory depression, pupillary constriction, sedation, or analgesia. However, it does antagonize the actions of pentazocine. Naloxone neither antagonizes the respiratory depressant effects of barbiturates and other hypnotics nor aggravates their depressant effects on respiration. Similar to nalorphine, naloxone precipitates an abstinence syndrome when administered to patients addicted to opiate-like drugs. 

A4 Acetaminophen, alfentanil, amiodarone, astemizole, cocaine, cortisol, cyclosporine, dapsone, diazepam, dihydroergotamine, dihydropyridines, diltiazem, ethinyl estradiol, gestodene, indinavir, lidocaine, lovastatin, macrolides, methadone, miconazole, midazolam, mifepristone (RU 486), paclitaxel, progesterone, quinidine, rapamycin, ritonavir, saquinavir, spironolactone, sulfamethoxazole, sufentanil, tacrolimus, tamoxifen, terfenadine, testosterone, tetrahydro-cannabinol, triazolam, troleandomycin, verapamil Barbiturates, carbamazepine, macrolides, glucocorticoids, pioglitazone, phenytoin, rifampin Erythromycin, 613-hydroxy cortisol... 

Cross-tolerance occurs between all opiates that act primarily via the mu receptors. This is the basis of the methadone substitution therapy which is commonly used to withdraw people who are dependent on heroin or morphine methadone is used because of its relatively long half-life (about 12 hours) and its ease of administration in an oral form. Cross-tolerance does not occur between the opiates and other classes of dependence-producing drugs such as the barbiturates, alcohol or the amphetamines, which act through different mechanisms. 

SCHEDULE II Certain barbiturates, cocaine, codeine, codeine + acetaminophen (depends on dose and formulation), fentanyl (depends on dose), hydrocodone, hydromorphone, meperidine, methadone, morphine (depends on combination with other pain relievers), oxycodone, propoxyphene... 

B. Widdop. Screening for Drugs of Abuse (II) Cannabinoids, Lysergic Acid Diethylamide, Buprenorphine, Methadone, Barbiturates, Benzodiazepines and Other Drugs. Annals of Clinical Biochemistry 34 (5) (1997) 460-510 Shannon, M. Toxicology Reviews Physostigmine. Pediatric Emergency Care 14 (3) (1998) 224-226. 

All compounds that behave as narcotic analgesics characterized by the usual criteria contain a basic nitrogen center that either forms parts of an alicyclic ring system, as in morphine and pethidine, or terminates an acyclic chain, as in methadone, etonitazene, and the enkephalins. Nonbasic compounds of high activity in antinociceptive tests invariably fail to satisfy criteria for narcotic analgesics, such as reversal of effects by naloxone or nalorphine or evidence of binding to opioid receptors recent examples are the barbiturate... 

BARBITURATES ANALGESICS - OPIOIDS 1. Barbiturates t sedative effects of opioids 2.1 efficacy of fentanyl and methadone with phenobarbital and primidone 1. Additive sedative effect. 2. t hepatic metabolism of fentanyl and methadone 1. Monitor respiratory rate and conscious levels 2. Be aware that the dose of fentanyl and methadone may need to t... 

OPIOIDS ANTIEPILEPTICS 1. Barbiturates T sedative effects of opioids 2.1 efficacy of fentanyl and methadone with carbamazepine, phenobarbital, phenytoin or primidone 3. Carbamazepine l tramadol levels 4. Risk of pethidine toxicity 1. Additive sedative effect 2. t hepatic metabolism of fentanyl and methadone, and possibly an effect at the opioid receptor 3. Carbamazepine T metabolism of tramadol 4. Phenytoin induces metabolism of pethidine, which causes T level of a neurotoxic metabolite 1. Monitor respiratoiy rate and conscious levels 2. Be aware that the dose of fentanyl and methadone may need to be t 3. Watch for poor effect of tramadol. Consider using an alternative opioid 4. Co administer with caution the effect may be i by administering pethidine intravenously... 

Clinically important, potentially hazardous interactions with alcohol, amprenavir, barbiturates, buprenorphine, chlorpheniramine, clarithromycin, CNS depressants, efavirenz, esomeprazole, eucalyptus, fluoroquinolones, imatinib, indinavir, ivermectin, macrolide antibiotics, MAO inhibitors, methadone, mianserin, nalbuphine, narcotics, nelfinavir, nilutamide, phenothiazines, ritonavir, SSRIs... 

Special arrangements apply to the prescribing of drugs of dependence in the UK under the provisions of the Misuse of Drugs Act 1971. Drugs controlled include cocaine, dipipanone, diamorphine (heroin), methadone, morphine, opium, pethidine, phencyclidine, lysergjde (LSD), amphetamines, barbiturates, cannabis, codeine, pholcodine, and certain drugs related to the amphetamines, such as chlorphentermine and diethylpropion. 

Barbiturates Opiates Pentobarbital tolerance test initial detoxification at upper limit of tolerance test decrease dosage by 100 mg every 2-3 days Methadone 20-80 mg orally daily taper by 5-10 mg daily or clonidine 2 mcg/kg three times a day x 7 days taper over additional 3 days... 

Prescription regulations for most CNS drugs are based on their abuse liability. The potent opioid analgesics (e.g., morphine, methadone, meperidine, fentanyl) are judged to have the highest potential for abuse, along with CNS stimulants (e.g., amphetamine, cocaine) and short-acting barbiturate (e g., secobarbital). No refills or telephone prescriptions are permissible. 

Table IV-1-10 summarizes the properties of drugs of abuse. These include the CNS stimulants (cocaine j and amphetamines), the CNS depressants (benzodiazepines, barbiturates, and ethanol), the opioids j (morphine, heroin, methadone, fentanyl, and others), the hallucinogens (marijuana and other j...

Rifampin induces the activity of the hepatic microsomal enzyme, metabolizing numerous drugs including acetaminophen, anticoagulants, barbiturates, benzodiazepines, beta-blockers, chloramphenicol, clofibrate, contraceptives, corticosteroids, cyclosporine, digitoxin, disopyramide, estrogens, hydantoins, methadone, mexiletine, quinidine, sulfones, sul-fonylureas, theophyllines, tocainide, and verapamil. The plasma levels and effectiveness of these agents may be decreased. 

Noninterfering aprobarbital, barbituric acid, ethinamate, ethosuximide, gentamicin, li-docaine, mebutemate, meprobamate, methadone, methyprylon, nirvanol, phenobarbital, procainamide, propox5q>hene, thioamyl, thioridazine, trifluoperazine, triflupromazine, ty-bamate, vinbarbital... 

W-Allylnormorphine does not antagonize the respiratory depression or the general central depression from the barbiturates. It is a specific antidote for morphine, meperidine, and methadone poisoning (Eckenhoff et al., 88). 

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