Morphine tablets

In other indications such as hypertension, the OROS technology (oral osmotic system developed by ALZA) has already proven its value, and therefore it seemed appropriate to use this technology with its typical, virtually constant, release rate (zero-order kinetics) for once-daily opioid tablets. Such a morphine tablet is already available, but is not yet on the market, and a hydromorphone OROS is currently being clinically developed by Knoll. 

New Zealand seized 25 litres of acetic anhydride in 2006. Small amounts of the substance were also found in four laboratories in Australia manufacturing on a small scale home-made heroin from morphine tablets. 

Moriarty M, McDonald CJ, Miller AJ. A randomised crossover comparison of controlled release hydromorphone tablets with controlled release morphine tablets in patients with cancer pain. J Qin Res 1999 2 1-8. 

Hanks GW, Twycross RG, Bliss JM. Controlled release morphine tablets a double-blind trial in patients with advanced cancer. Anaesthesia 1987 42(8) 840-4. 

Drake J, Kirkpatrick CT, Aliyar CA, Crawford FE, Gibson P, Horth CE. Effect of food on the comparative pharmacokinetics of modified-release morphine tablet formulations Oramorph SR and MST Continus. BrJ Clin Pharmacol (1996) 41, 417-20,... 

In clinical practice various oral dosage forms are also used for rectal administration. There is often little scientific support for such use, nevertheless it may be effective. Evidence exists for rectal administration of an oral controlled release morphine tablet (MS-Contin ) [2, 3]. Rectal use of temazepam oral capsules is not effective. There is a broad variation in time to reach the maximum plasma concentration and in the biological availability. Better outcomes are obtained with temazepam dissolved in glycofuroFethanol water = 5 1 4 and given rectally as an enema [4]. 

Walsh D, Tropiano PS (2002) Long-term rectal administration of high-dose sustained-release morphine tablets. Support Care Cancer 10 653-655... 

Holgado MA, I mine A, Alvarez-Puentes J, Fernandez-Arevalo M. Development and in vitro evaluation of controlled release formulation to produce wide dose interval morphine tablets. Eur J Pharm Biopharm 2008 70(2) 544-549. 

Salem and Galan have developed a new method for determining the amount of morphine hydrochloride in tablets. Results, in milligrams, for several tablets containing different nominal dosages follow... 

OxyContin is a controlled-released form of oxycodone and indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time OxyContin is not intended for use as a PRN analgesic The patient may experience fewer adverse reactions with oxycodone tlian morphine, and the drug is effective and safe for the elderly. The tablets are to be swallowed whole and are not to be broken, chewed, or crushed. 

Opioids maybe administered in a variety of routes including oral (tablet and liquid), sublingual, rectal, transdermal, transmucosal, intravenous, subcutaneous, and intraspinal. While the oral and transdermal routes are most common, the method of administration is based on patient needs (severity of pain) and characteristics (swallowing difficulty and preference). Oral opioids have an onset of effect of 45 minutes, so intravenous or subcutaneous administration maybe preferred if more rapid relief is desired. Intramuscular injections are not recommended because of pain at the injection site and wide fluctuations in drug absorption and peak plasma concentrations achieved. More invasive routes of administration such as PCA and intraspinal (epidural and intrathecal) are primarily used postoperatively, but may also be used in refractory chronic pain situations. PCA delivers a self-administered dose via an infusion pump with a preprogrammed dose, minimum dosing interval, and maximum hourly dose. Morphine, fentanyl, and hydromorphone are commonly administered via PCA pumps by the intravenous route, but less frequently by the subcutaneous or epidural route. 

The MS Contin 200 mg tablet is for use only in opioid-tolerant patients requiring daily morphine-equivalent dosages of 400 mg or more. Reserve this strength for patients who have already been titrated to a stable analgesic regimen using lower... 

Tablets-A patient s daily morphine requirement is established using IR oral morphine (dosing every 4 to 6 hours). The patient is then converted to morphine ER in either of 2 ways ... 

With either method, dose and dosing interval is then adjusted as needed. The 15 mg ER tablet should be used for initial conversion for patient s total daily requirement is expected to be less than 60 mg. Morphine ER tablets of 30 mg strength are recommended for patients with a daily morphine requirement of 60 to 120 mg. When the total daily dose is expected to be greater than 120 mg, the appropriate tablet strength should be employed. 

Conversion from parenteral morphine or other opioids (parenteral or oral) to CR/ER/SR doseforms- Exercise particular care in the conversion process. Because of uncertainty about, and intersubject variation in, relative estimates of opioid potency and cross-tolerance, initial dosing regimens should be conservative that is, an underestimation of the 24-hour oral morphine requirement is preferred to an overestimate. To this end, estimate initial individual doses conservatively. In patients whose daily morphine requirements are expected to be 120 mg/day or less, the 30 mg tablet strength is recommended for the initial titration period. Once a stable dose regimen is reached, the patient can be converted to the 60 or 100 mg tablet strength, or appropriate combination of tablet strengths, if desired. Conversion from CR/ER/SR oral morphine to parenteral opioids - It is best to assume that the parenteral-to-oral potency is high. For example, to estimate the required 24-hour dose of morphine for IM use, one could employ a conversion of 1 mg morphine IM for every 6 mg of morphine... 

CR/ER/SR tablets/capsules Swallow whole do not break, chew, crush, or dissolve because of the risk of acute overdose. Ingesting chewed or crushed beads or pellets will lead to the rapid release and absorption of a potentially toxic dose of morphine. 

Depending on the type, opioids can be injected, smoked, snorted, or taken orally. Smoking heroin is termed chasing the dragon. ControIIed-release oral tablets of morphine (MS-Contin ) or of oxycodone (OxyContin ) should never be crushed or chewed, as the entire dose of opioid released at once may be toxic. 

It was felt that a trial period was indicated on an alternative oral substitute medication, namely morphine sulphate tablets, with Alan s girlfriend involved in overseeing his daily... 

More than half (57 %) of all seizure cases involved cannabis (herb, resin, oil, plants and seeds). Opiates (opium, morphine, heroin, synthetic opiates and poppy seeds), accounted for 17 per cent, with heroin alone accounting for 14 per cent of the total. This is followed by seizures of the amphetamine-type stimulants (12 %). About half of these seizures (or 5.5 % of the total) is accounted for by methamphetamine, followed by amphetamine (2.5 %) and ecstasy (2%) the rest (2 %) includes Captagon tablets (Near East) and Maxiton Forte (Egypt), ephedrone (methcathinone) and various undefined amphetamines. Coca products account for 9 percent of global seizure cases the bulk of coca related seizure cases concern cocaine (8 % of total). 

The success of prolonged-release morphine prompted the development of prolonged-release formulations for other opioids, for example the matrix made of hydrophobic and hydrophilic matrix formers, for example on hydrocodeine (DHC retard with cetostearyl alcohol and hydroxyethyl-cellulose), oxycodone (oxygesic with stearyl alcohol and polyacrylate) and tramadol (tramundin with cetostearyl alcohol and ethylcellulose). By virtue of the oblong shape of hydrocodeine and tramadol tablets the prolonged-release tablets can be divided, whereby compared with whole tablets release from the divided tablets is slightly accelerated. The difference with these forms is that with increasing dose the release slows down. 

In Great Britain tramadol is available as once-daily tablets made up of granules in a purely fatty matrix (Zydol XL), as described above for morphine, which again reduces the release rate compared with the granules. 

Buprenorphine is derived from thebaine. It is a partial mu agonist with kappa antagonist activity. Buprenorphine has 25 to 50 times the potency of morphine. It is used to produce a longer-lasting analgesia than morphine. Effects of buprenorphine last longer because it is released more slowly from mu receptors than morphine. It is available as an injectable for intramuscular (IM) or intravenous administration in a 1-ml solution containing 0.3 mg buprenorphine (as buprenorphine HC1) for the relief of moderate to severe pain. It is also available to treat opioid dependence in the formulation of a tablet,51 alone or in combination with naloxone, in 2- or 8-mg... 

Anlar, S., Capan, Y., Guven, O., et al. Formulation and in vitro-in vivo evaluation of buccoadhesive morphine sulfate tablets. Pharm. Res. 11(2) 231—236, 1994. 

Apomorphine hydrochloride (Figure 44.2), an alkaloid obtained in the laboratory by rearrangements within the morphine molecule, is a grayish-white, glistening, light-sensitive, and air-sensitive crystalline powder, soluble in both water and alcohol in the proportions of about 1 50 it is available in small amounts in bulk and more easily as 5 mg (1/12 grain) tablets. 

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