Tetracyclines Alcohol

Alcohol, amiodarone, didanosine, 1-asparaginase, piroxicam, stavudine, tamoxifen, tetracycline derivatives, valproic acid, and zidovudine... 

Didanosine (ddl) NRTT1 Tablets, 400 mg daily,3 adjusted for weight. 30 min before or 2 h after meals. Separate dosing from fluoroquinolones and tetracyclines by 2 h Peripheral neuropathy, pancreatitis, diarrhea, nausea, hyperuricemia. Possible increase in myocardial infarction Avoid concurrent neuropathic drugs (eg, stavudine, zalcitabine, isoniazid), ribavirin, and alcohol. Do not administer with tenofovir... 

The JACS paper describes the total synthesis of the more highly oxygenated (-)-tetracycline 16. To this end, the alcohol S was carried on to the enone 10. Opening of the cyclobutane 11 to the o-quinone methide followed by Diels-Alder cycloaddition to 10 delivered the endo adduct 12. 

Tetracycline antibiotics are closely related derivatives of the polycyclic naphtha-cenecarboxamide. They are amphoteric compounds with characteristic dissociation constants corresponding to the acidic hydroxyl group at position 3 (pK about 3.3), die dimethylamino group at position 4 (pK, about 7.5), and the hydroxyl group at position 12 (pK about 9.4). In aqueous solutions of pH 4-7, tetracyclines exist as dipolar ions, but as the pH increases to 8-9 marked dissociation of the dimethylamine cation occurs. They are soluble in acids, bases, and alcohols but are quite insoluble in organic solvents such as chloroform. Their ultraviolet spectra show strong absorption at around 270 and 360 nm in neutral and acidic solutions. Tetracyclines are readily transformed into fluorescent products in the presence of metal ions or under alkaline conditions. 

This is the accumulation of triglycerides in hepatocytes, and there are a number of mechanisms underlying this response as is discussed below (see the sect. "Mechanisms of Toxicity"). The liver has an important role in lipid metabolism, and triglyceride synthesis occurs particularly in zone 3. Consequently, fatty liver is a common response to toxicity, often the result of interference with protein synthesis, and may be the only response as after exposure to hydrazine, ethionine, and tetracycline, or it may occur in combination with necrosis as with carbon tetrachloride. It is normally a reversible response, which does not usually lead to cell death, although it can be very serious as is the case with tetracycline-induced fatty liver in humans. Repeated exposure to compounds, which cause fatty liver, such as alcohol, may lead to cirrhosis. 

To 18.3 g of L-lysine hydrochloride dissolved in 100 ml of water is added 10 ml of 37% aqueous solution of formaldehyde. To the resultant mixture is added 44.0 g of anhydrous tetracycline dissolved in 500 ml of tetrahydrofuran. After thorough mixing the product forms over a period of about 15 min as an oily layer which after separation from the aqueous phase is added dropwise to 3 L of stirred isopropyl alcohol. The product after recovery by filtration, is reslurried with acetone, filtered and dried at 65°C at reduced pressure. 

Aminophylline Aminophylline should not be mixed with acidic drugs, as it becomes precipitated if the pH of the final solution falls below pH 8. Mixture with glucose may increase the pH above 10 where proteins, such as insulin and erythromycin, are unstable. Some drugs that are incompatible with aminophylline include amiodarone, benzylpenicillin potassium, cisatracurium, ceftazidime, ceftriaxone, dobutamine, tetracycline hydrochloride, verapamil hydrochloride, warfarin sodium, and vitamin B and C injection. Alcohol-free theophylline should be stored in amber-colored containers maximum care must be taken to protect it against exposure to light.92-94... 

ALCOHOL TETRACYCLINE Likely 1 efficacy of antibiotic Uncertain Be aware... 

Plots of Po/w or vs. plate counts for benzene and 2-ethylanthraquinone eluted with micellar SDS, in the presence of several alkanols and alkane diols, show an initial steep increase in efficiency, after which an approximately constant value is reached (Fig. 3). Among the alcohols, maximal efficiency for benzene and 2-ethylanthraquinone is obtained with the butanols and the pen-tanols, with enhancement factors of 2.5 and 25 (compared to pure SDS), respectively. However, final efficiencies for the latter compound are much lower compared to that for benzene. Dipolar aprotic modifiers (acetonitrile or dimethylsulfoxide) appear to be somewhat more effective in enhancing efficiencies than alcohols with comparable Pq/w- Some recent work has shown the advantage of using acetonitrile as additive in MLC for the analysis of sulfonamides, tetracyclines, and the most polar steroids. 

Rolitetracydlne, U5P. Rolitetracyclinc. Af-(pyrrolidi-nomcthyDtctracycline (Syntetrin) was introduced for u.sc by intramuscular nr intravenous injection. This derivative is made by condensing tetracycline with pyrrolidine and formaldehyde in the presence of rerr-butyl alcohol. It is very soluble in water (I g dissolves in about I mL) and provides a means of injecting the antibiotic in a small volume of... 

Several agents have been associated with producing acute pancreatitis or inflammation of the pancreas. The main causes are alcohol and a disturbance of the bile duct, which account for 50% of cases. Drugs with a clear association include sulfonamides, thiazide diuretics, tetracycline, azathioprine, estrogens, and valproic acid. The mechanism for the underlying injury is not well understood. Possible associations have been reported with other medications including methyldopa, procainamide, and 1-asparaginase. A relationship between cortico-steriods has not been established. 

Psychoactive activity is potentiated when tetracycline, propanolol, or alcohol is used with either cinnamon (Cinnamomum zeylanicum) (in excess... 

Calcium absorption is reduced by high pH complex-ing agents such as oxalate, phytate, free fatty acids, and phosphate and shortened transit times. These factors are probably of clinical importance only when associated with vitamin D deficiency, marginal calcium intake, or malabsorption disorders. Absorption is also reduced by increased intake of protein, fat, and plant fiber increasing age stress chronic alcoholism immobilization (e.g., prolonged hospitalization) and drugs such as tetracycline, thyroid extract, diuretics, and aluminum-containing antacids. 

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