Morphine tartrate

Morphine Tartrate 857.0 Strychnine Sulphate 1018 Erythromycin Stearate... 

Cyclimorph cyclizlne tartrate morphine tartrate, cyclizine [ban, inn) (cyclizIne hydrochloride (usan) cyclizlne tartrate BW 47-83 Valoid ) is one of the piperazine series of histamine H -receptor ANTAGONISTS, and a muscarinic CHOLINOCEPTOR antagonist with SEDATIVE actions. It can be used orally or systemically as an antiemetic in the treatment of nausea, vomiting, vertigo, motion sickness and disorders of the balance function of the inner ear. It is available in preparation together with morphine (e.g. Cyclimorph ). 

Thebaine, CjgHgiOgN. This base, which occurs in opium to the extent of 0-1 to 1 per cent., was first obtained by Pelletier and Thiboumery, who regarded it as isomeric with morphine, and named it paramorphine. It was examined by Kane, who first called it thebaine, and by Anderson, who described a method of isolation and provided the formula given above. It remains in the mother liquor after the removal of morphine and eodeine hydrochlorides in Gregory s process, and in Hesse s method of isolating it from this source is obtained as the acid tartrate. This is crystallised from hot water, and the alkaloid regenerated from it is reerystallised from dilute alcohol, from which it separates in leaflets, or from dry alcohol in prisms, m.p. 193°, — 218-6° (EtOH) or — 229-5°... 

Butorphanol tartrate is a weak partial p-receptor agonist, 3.5-5 times as potent as morphine. The incidence of psychotomimetic effects is relatively low. The recommended doses are 1-4 mg intramuscularly every 3-4 h or 0.5-2 mg intravenously. Respiratory depression produced by butorphanol 2 mg IV is similar to that of 10 mg morphine. However, there is a ceiling effect for respiratory depression, and near-maximum depression occurs after 4 mg in normal adults. In healthy volunteers, butorphanol 0.03-0.06 mg-kg-1 produces no significant cardiovascular changes. However, in patients with cardiac disease, progressive increases in cardiac index and pulmonary artery pressure occur, and butorphanol should be avoided in patients with recent myocardial infarction. Butorphanol is metabolised mainly in the liver to inactive metabolites. The terminal half-life is 2.5-3.5 h. 

L. Berczeller has shown that the presence of acids, chlorides, bromides, iodides, thiocyanates, and morphine accelerate the reaction while the presence of tartrates, sulphates, oxalates, carbonates, mercuric chloride, bromide, iodide, and cyanide, most alkaloids, colloids, proteins, etc., inhibit the reaction. Hydrocyanic acid, unlike other acids, also inhibits the reaction. A. Skrabal has shown that Landolt s reaction has a temp, coeff. greater than unity, so that the velocity of the reaction increases with a rise of temp. but if the system contains an excess of sodium sulphate, the temp, coeff. is less than unity, and the velocity of the reaction decreases with a rise of temp. 

In this synthetic derivative of codeine, a ketone group replaces the -OH of codeine at position 6 and two H atoms are added at positions 7 and 8. It thus bears the same relation to codeine as dihydromorphinone (Dilaudid ) does to morphine. It is marketed as the tartrate under the trade names Dicodid and Hycodan and is used chiefly for the relief of cough. 

The dextrorotatory isomer of 3-methoxy-A-methylmorphinan, a synthetic morphine derivative (Roinilar hydrobromide , Tusilan ) is employed exclusively as an antitussive agent. Its levorotary isomer (in the form of the 3-hydroxy tartrate) is described next. These compounds differ from morphine chemically in lacking the -O- bridge between carbons 4 and 5, the OH group at C6, and... 

The levorotatory isomer of 3-hydroxy-A-methylmorphinan tartrate dihydrate (Levo-dromoran tartrate ) is a more potent analgesic than morphine with an approximately equal margin of safety, but is longer acting and has a lesser constipating action. Contraindications to its use, including the danger of addiction, are similar to those of morphine. 

Piminodine (Alvodine ), ethyl-4-phenyl-l-(3-phenylaminopropyl)piperidine-4-carboxylate ethanesulfonate, is reputed to be equal to morphine in analgesic potency, but relatively free of the latter s narcotizing action. It is administered in doses of 25 to 50 mg orally every 4 to 6 h, or in doses of 10 to 20 mg subcutaneously or intramuscularly every 4 h as needed. Piminodine is habit forming, requires a narcotic prescription, and should be used with the same precautions as other members of this group. Levallorphan tartrate, nalorphine, naloxone, or naltrexone are antidotes to it. 

Butorphanol Tartrate With this drug, dependence, withdrawal, and interactions are similar to that of opioids. Butorphanol has less potential to produce dependence when compared with morphine, but it is a drug of abuse. Naloxone acts as an antagonist and can be used for the treatment of overdose.35... 

Subsequent animal tests indicated that butorphanol is about 4 times more potent than morphine as an analgesic and equivalent to nalorphine as an antagonist. Clinical evaluation shows that butorphanol is also an effective analgesic in man (approximately 5 times more potent than morphine), and the tartrate is now marketed as an injection (Stadol). In animals its PDC is low (less than that of pentazocine) as it is in man, and this fact and its ceiling rather than dose-related effect on respiration (see p. 414) are recommendations for clinical use of the drug.<5,64)... 

Dose. 5 to 20 mg of morphine hydrochloride, sulphate, or tartrate, by mouth or parenterally, every 4 hours. 

Ten days later, the same rabbit was again given subcutaneously 0.1 gram of morphine hydrochloride in water solution. This time the minimum rate of respiration was 18 per minute after five hours the rabbit was completely conscious and crawled around of its own accord and with no difficulty. The narcosis produced by the morphine was sensibly less in the absence of the sodium tartrate. 

Sodium thiocyanate therefore tends to antagonize morphine, as it should, and sodium tartrate tends to synergize it (the sodium tartrate did not appear to have any narcotic action in the absence of morphine), thus also falling into line. This then indicates something of what can be... 

Butorphanol tartrate (stadol) is better suited for the relief of acute than chronic pain. Because of its side effects on the heart, it is less useful than morphine or meperidine in patients with congestive heart failure or myocardial infarction. The usual dose is 1-4 mg of the tartrate given intramuscularly or 0.5-2 mg given intravenously every 3-4 hours. A nasal formulation (STADOLNS) is available and has proven to be effective. 

Morphine and related drugs possessing potent narcotic analgesic properties, are used in clinical practice. A few examples belonging to this class of compounds are morphine sulphate diamorphine hydrochloride codeine dihydrocodeine phosphate hydromorphone hydrochloride hydrocodone tartrate oxymorphone hydrochloride. 

Grewe (1946) introduced a vital alkylation reaction via a very specific stereo-selective (trans) synthesis followed by acid-catalyzed intramolecular, aromatic substitution, which caused the B/C-c/s CfD-trans ring fusions found to be common in either morphine or its natural congeners. This study has paved the way for an altogether new morphinan analogues known as benzomorphans . A few classical examples of this group of compoimds are listed below, viz., levorphanol tartrate dextromethorphan hydrobromide butorphanol tartrate ... 

Alkaloids are usually basic and combine with acids to form alkaloid salts, a property often exploited to extract them from their source. Other alkaloids occur naturally as salts of organic acids. Common salts include hydrochlorides, salicylates, sulphates, nitrates, acetates, and tartrates such as morphine acetate, cocaine hydrochloride, and strychnine nitrate. Water, alcohol, and ether solutions of alkaloids and their salts are often used to administer or carry the alkaloid, particularly for medicinal purposes. Nicotine preparations can include a variety of liquid and solid mixtures of nicotine (soluble in alcohol, chloroform, ether, and water), nicotine salts, and many other nicotine compounds (e.g., nicotine sulphate and nicotine tartrate). 

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