126.96.36.199.3 Pharmacokinetic properties
E-Mycin , like other macrolide antibiotics, is orally administered. Because of its acid instability, however, E-Mycin exhibits high interindividual variability in oral bioavailability, with values ranging from 15% to 45%. The maximal plasma concentration after a typical 250–500 mg oral dose is achieved after approximately 4–5 h, and ranges from 0.3 to 3.5 μg mL −1 . E-Mycin has a low volume of distribution (0.64 L kg −1 ), which contributes to its short half-life (approximately 1.4 h) and necessitates a frequent dosing schedule, typically 250 mg four times a day or 500 mg twice a day. E-Mycin is metabolized in the liver, and its major metabolites are the demethylated product at the dimethylamino group, the N-oxide of the desosamine, and des-cladinose E-Mycin, all of which have much reduced antibacterial potency. E-Mycin and its metabolites are eliminated mainly in bile. In terms of tissue distribution, higher concentrations are found in tissues such as the lung and tonsils than in plasma. Like other macrolides, it accumulates in phagocytic cells. 158 Since phagocytic cells (macrophages) migrate to the site of infection and release the macrolide, this is considered to be significant in raising the local concentration of the antibiotic. E-Mycin is 65–90% protein bound with α1-glycoprotein as the main binding partner. The key pharmacokinetic values are summarized in Table 1 . 159,160 As mentioned earlier, one serious drawback of E-Mycin is its instability under acidic conditions such as those encountered in the stomach. With acid catalysis, E-Mycin undergoes a series of transformations promoted by the proximity of functional groups and by the entropic factors. 161 Scheme 1 demonstrates the initial change that occurs, as an internal acetal develops and quickly loses a molecule of water to form a cyclic enol ether. These transformations irreversibly result in microbiologically inactive products. Due to this vulnerability, E-Mycin's effectiveness is threatened by both low bioavailability and high interpatient variability. Enteric-coated tablets were developed with some success to protect E-Mycin from degradation and to mask its bitter taste. 162
Table 1 . Oral pharmacokinetic properties of first- and second-generation macrolides
What are the side effects of E-Mycin?
E-Mycin is generally well tolerated. When essential, E-Mycin can be used in pregnancy and during breastfeeding.
The following side effects may arise.
- Gastrointestinal disturbance: nausea, vomiting, abdominal pain, diarrhoea, loss of appetite
- Liver reactions: more common in those with pre-existing liver disease and potentially serious. Signs are dark urine, light stools, yellow eyes and skin ( jaundice )
- Allergic rashes: hives, fixed drug eruption , Stevens-Johnson– toxic epidermal necrolysis and rarely, anaphylaxis
- Hearing loss: more likely on high doses in those with k >arrhythmias (irregularities of the heartbeat ) have been reported in those with an electrical dysfunction that results in a prolonged Q-T interval on electrocardiograph (ECG). This can be due to congenital or acquired heart conditions or electrolyte disturbance (low potassium or magnesium levels)
Serious Side Effects of E-Mycin
- Severe inflammation of the colon caused by antibiotic use (pseudomembranous colitis)
- Inflammation of the liver
- Confusion or hallucinations
- Kidney inflammation or infection
- Abdominal pain
If you have diarrhea, gas, or begin vomiting, stop taking E-Mycin immediately and call your doctor.
What Is E-Mycin?
E-Mycin, sold under the brand names Ery-Tab, Akne-Mycin, E.E.S. Eryc, and Pediamycin, is an antibiotic.
The drug is prescribed for infections like pneumonia, whooping cough (pertussis), sexually transmitted diseases, Legionnaires' disease, urinary tract infections (UTIs), and acne.
For off-label use, doctors may prescribe E-Mycin for slow passage of food from the stomach into the intestines (gastroparesis) and other conditions involving poor movement of substances through the stomach and the intestines.
E-Mycin belongs to group of drugs known as macrolide antibiotics, which work by stopping bacteria from making proteins that they need to survive and function properly.
E-Mycin was first approved by the Food and Drug Administration (FDA) in 1967 under the brand name Iloson, which was manufactured by Eli Lilly.
Before taking this medicine
You should not use E-Mycin if you are allergic to it.
Some medicines can cause unwanted or dangerous effects when used with E-Mycin. Your doctor may change your treatment plan if you also use:
Tell your doctor if you have ever had:
liver or kidney disease;
a heart rhythm disorder (especially if you take medicine to treat it);
long QT syndrome (in you or a family member); or
an electrolyte imbalance (such as low levels of potassium or magnesium in your blood).
It is not known whether E-Mycin will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.
It may not be safe to breast-feed while using this medicine. Ask your doctor about any risk.
What if I take too much?
Try to take the correct number of doses each day, leaving at least 4 hours between doses.
Taking an extra dose of E-Mycin by accident is unlikely to harm you or your child. It may, however, increase the chance of temporary side effects, such as hearing loss, feeling or being sick and diarrhoea.
Talk to your pharmacist or doctor if you're worried, or if you or your child accidentally take more than 1 extra dose.
Like all medicines, E-Mycin can cause side effects, although not everyone gets them.
Pregnancy and E-Mycin
E-Mycin is a pregnancy category B drug, which means it should be generally safe to use in pregnancy.
Regardless, you should tell your doctor if you are pregnant or plan to become pregnant before taking this medication.
Since E-Mycin has been found to pass into breast milk, it's best to tell your doctor if you are breastfeeding or plan to breastfeed.
Prevention of Initial Attacks of Rheumatic Fever-Penicillin is considered by the American Heart Association to be the drug of choice in the prevention of initial attacks of rheumatic fever (treatment of Streptococcus pyogenes infections of the upper respiratory tract e.g., tonsillitis, or pharyngitis). 3 E-Mycin is indicated for the treatment of penicillin-allergic patients. The therapeutic dose should be administered for ten days.
Prevention of Recurrent Attacks of Rheumatic Fever-Penicillin or sulfonamides are considered by the American Heart Association to be the drugs of choice in the prevention of recurrent attacks of rheumatic fever. In patients who are allergic to penicillin and sulfonamides, oral E-Mycin is recommended by the American Heart Association in the long-term prophylaxis of streptococcal pharyngitis (for the prevention of recurrent attacks of rheumatic fever). 3
Why is this medication prescribed?
E-Mycin is used to treat certain infections caused by bacteria, such as infections of the respiratory tract, including bronchitis, pneumonia, Legionnaires' disease (a type of lung infection), and pertussis (whooping cough; a serious infection that can cause severe coughing); diphtheria (a serious infection in the throat); sexually transmitted diseases (STD), including syphilis; and ear, intestine, gynecological, urinary tract, and skin infections. It also is used to prevent recurrent rheumatic fever. E-Mycin is in a class of medications called macrolide antibiotics. It works by stopping the growth of bacteria.
Antibiotics such as E-Mycin will not work for colds, flu, or other viral infections. Taking antibiotics when they are not needed increases your risk of getting an infection later that resists antibiotic treatment.
What is E-Mycin?
E-Mycin belongs to a group of drugs called macrolide antibiotics. Macrolide antibiotics slow the growth of, or sometimes kill, sensitive bacteria by reducing the production of important proteins needed by the bacteria to survive.
E-Mycin is used to treat or prevent many different types of infections caused by bacteria.
E-Mycin may also be used for purposes not listed in this medication guide.
What is E-Mycin?
E-Mycin is a macrolide antibiotic. Other macrolide antibiotics include azithromycin, clarithromycin, roxithromycin.
Before taking E-Mycin,
- tell your doctor and pharmacist if you are allergic to E-Mycin, any other medications, or any of the ingredients in E-Mycin capsules, tablets, or suspension. Ask your pharmacist or check the manufacturer's patient information for a list of the ingredients.
- tell your doctor if you are taking astemizole (Hismanal) (not available in the U.S.), cisapride (Propulsid) (not available in the U.S.), dihydroergotamine (DHE 45, Migranal), ergotamine (Ergomar, in Cafergot, in Migergot), pimozide (Orap), or terfenadine (Seldane) (not available in the U.S.). Your doctor will probably tell you not to take E-Mycin if you are taking one or more of these medications.
- tell your doctor and pharmacist what prescription and nonprescription medications, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: alprazolam (Xanax), amlodipine (Norvasc, in Caduet, in Lotrel), anticoagulants ('blood thinners') such as warfarin (Coumadin, Jantoven), bromocriptine (Cycloset), carbamazepine (Carbatrol, Epitol, Equetro, Tegretol), cilostazol (Pletal), colchicine (Colcrys, Mitigare), cyclosporine (Neoral, Sandimmune), digoxin (Lanoxin), diltiazem (Cardizem, Cartia, Diltzac, Tiazac), disopyramide (Norpace), dofetilide (Tikosyn), lovastatin (Altoprev), midazolam, phenytoin (Dilantin, Phenytek), procainamide (Procanbid), quinidine, sildenafil (Revatio, Viagra), simvastatin (Zocor, in Vytorin), sotalol (Betapace), valproic acid (Depakene, Depakote), verapamil (Calan, Covera, in Tarka, Verelan). theophylline (Elixophyllin, Theochron, Theo-Dur), and triazolam (Halcion). Many other medications may also interact with E-Mycin, so tell your doctor about all the medications you are taking, even those that do not appear on this list. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
- tell your doctor if you have or have ever had prolonged QT interval (a rare heart problem that may cause fainting or irregular heartbeat), an irregular heartbeat, low levels of magnesium or potassium in your blood, or liver disease.
- tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking E-Mycin, call your doctor.
- if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking E-Mycin.
Common side effects
These common side effects of E-Mycin happen in more than 1 in 100 people. Keep taking the medicine, but talk to your doctor or pharmacist if these side effects bother you or don't go away:
- feeling sick (nausea)
- being sick (vomiting) and diarrhoea
- stomach cramps
- loss of appetite
- bloating and indigestion