Spiramycin adipinate
Spiramycin adipinate Uses, Dosage, Side Effects, Food Interaction and all others data.
Spiramycin adipinate is a macrolide antibacterial that inhibits protein synthesis by irreversibly binding to the 50S subunit of the ribosomal subunit thus blocking the transpeptidation or translocation reactions of susceptible organisms resulting in stunted cell growth.
The absolute bioavailability of oral spiramycin is generally within the range of 30 to 40%. After a 1 g oral dose, the maximum serum drug concentration was found to be within the range 0.4 to 1.4 mg/L.
| Trade Name | Spiramycin adipinate |
| Generic | Spiramycin |
| Spiramycin Other Names | Demycarosylturimycin H, Foromacidin A, Foromacidine A, Spiramycin 1, Spiramycin A, Spiramycin I |
| Type | |
| Formula | C43H74N2O14 |
| Weight | Average: 843.065 Monoisotopic: 842.514005071 |
| Protein binding | Low level of protein binding (10-25%). |
| Groups | Approved |
| Therapeutic Class | Macrolides |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Acne vulgaris, Cryptosporidiosis, Protozoal infections, Susceptible infections, Toxoplasmosis
Spiramycin adipinate is also used to associated treatment for these conditions: Bacterial Infections
How Spiramycin adipinate works
The mechanism of action of macrolides has been a matter of controversy for some time. Spiramycin adipinate, a 16-membered macrolide, inhibits translocation by binding to bacterial 50S ribosomal subunits with an apparent 1 : 1 stoichiometry. This antibiotic is a potent inhibitor of the binding to the ribosome of both donor and acceptor substrates. The primary mechanism of action is done by stimulation of dissociation of peptidyl-tRNA from ribosomes during translocation.I
Dosage
Spiramycin adipinate dosage
Intravenous-
Toxoplasmosis, Cryptosporidiosis, Protozoal infections, Susceptible infections:
- Adult: 1.5 million units by slow infusion every 8 hr, may double the dose in severe infections.
Oral-Cryptosporidiosis, Protozoal infections, Susceptible infections, Toxoplasmosis:
- Adult: 6-9 million units/day in 2-3 divided doses, increased to 15 million units/day, given in divided doses for severe infections.
- Child and neonates: Chemoprophylaxis of congenital toxoplasmosis: 50 mg/kg bid.
May be taken with or without food.
Side Effects
Nausea, vomiting, abdominal pain, diarrhoea; urticaria, pruritus, macular rashes. Transient paraesthesia may occur.
Toxicity
Cardiac toxicity, specifically QT prolongation (irregular heartbeat; recurrent fainting).
Cholestatic hepatitis (abdominal pain; nausea; vomiting; yellow eyes or skin).
Gastrointestinal toxicity, specifically acute colitis (abdominal pain and tenderness; bloody stools; fever).
Intestinal injury (abdominal pain and tenderness).
Ulcerated esophagitis (chest pain; heartburn).
Precaution
Hepatic impairment; pregnancy and lactation. Monitor liver function. History of arrhythmias or predisposition to QT interval prolongation.
Interaction
Decreases carbidopa absorption and levodopa concentrations. Increased risk of ventricular arrhythmias when used with astemizole, cisapride and terfenadine. Risk of acute dystonia when used with fluphenazine
Food Interaction
- No food interactions are expected.
Volume of Distribution
The tissue distribution of spiramycin is extensive. The volume of distribution is in excess of 300 L, and concentrations achieved in bone, muscle, respiratory tract and saliva exceed those found in serum. Spiramycin adipinate showed high concentrations in tissues such as: lungs, bronchi, tonsils, and sinuses.
Elimination Route
The extent of absorption of Spiramycin adipinate was shown to be incomplete. Oral bioavailability ranges from 30-39%. Spiramycin adipinate has slower rate of absorption than Erythromycin. It has a high pKa (7.9) which could be a result of high degree of ionization in acidic medium of the stomach.
Half Life
Intravenous: Young persons (18 to 32 years of age): Approximately 4.5 to 6.2 hours. Elderly persons (73 to 85 years of age): Approximately 9.8 to 13.5 hours.
Oral: 5.5-8 hours, Rectal in children: 8 hours
Clearance
80% of the administered dose excreted in the bile, which makes the fecal-biliary route is the most important route of elimination. Enterohepatic recycling could also occur. Only 4 to 14% of an administered dose is eliminated through renal-urinary excretion route.
Elimination Route
Fecal-biliary route is the primary route of elimination. The secondary route is renal-urinary route.
Pregnancy & Breastfeeding use
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindication
Hypersensitivity.
Innovators Monograph
You find simplified version here Spiramycin adipinate
Spiramycin adipinate contains Spiramycin see full prescribing information from innovator Spiramycin adipinate Monograph, Spiramycin adipinate MSDS, Spiramycin adipinate FDA label
FAQ
What is Spiramycin adipinate used for?
Spiramycin adipinate is used to treat a wide variety of bacterial infections. This medication is known as a macrolide antibiotic.Spiramycin adipinate works by stopping the growth of bacteria. This antibiotic treats only bacterial infections.
How safe is Spiramycin adipinate?
Spiramycin adipinate 1.5 mg tablet is safe for kidney disease patients to use. No dosage change is recommended for the Spiramycin adipinate 1.5mg Tablet. Liver - Consult the physician Limited information on the use of the Spiramycin adipinate 1.5mg tablet in patients with liver disease is available.
What are the common side effects of Spiramycin adipinate?
Indigestion, nausea, vomiting, diarrhea or stomach ache may occur. If any of these effects continue or become bothersome, inform your doctor. In the unlikely event you have an allergic reaction to this drug, seek medical attention immediately.
Is Spiramycin adipinate safe during pregnancy?
Yes, Spiramycin adipinate is safe to use in pregnancy. Spiramycin adipinate is considered safe to use during pregnancy. Animal studies have shown little to no adverse effects on the developing baby; human studies, however, are minimal.
Is Spiramycin adipinate safe during pregnancy?
Spiramycin adipinate has less side effects and is recommended during breastfeeding period.
Is Spiramycin adipinate a penicillin?
Spiramycin adipinate proved to be equivalent to penicillin in the treatment of acute bacterial tonsillitis in adults.
Can I drive after taking Spiramycin adipinate?
Spiramycin adipinate normally does not affect your driving performance.
Does Spiramycin adipinate cross placenta?
Spiramycin adipinate is a macrolide antibiotic, which aims at the prevention of fetal infection. It does not cross the blood-placental barrier and, therefore, has no teratogenic effects to the fetus, or toxicity to the mother.
When is the best time to take Spiramycin adipinate?
Spiramycin adipinate is best taken on an empty stomach. To help clear up your infection completely, keep taking this medicine for the full time of treatment, even if you begin to feel better after a few days.
How to take Spiramycin adipinate?
Tell your doctor if you have ever had any unusual or allergic reaction to Spiramycin adipinate or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Is there any food or drink I need to avoid when taking Spiramycin adipinate?
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
How to proper use of Spiramycin adipinate?
Spiramycin adipinate is best taken on an empty stomach.To help clear up your infection completely, keep taking Spiramycin adipinate for the full time of treatment, even if you begin to feel better after a few days. If you stop taking Spiramycin adipinate too soon, your symptoms may return.
What happens if I miss a dose of Spiramycin adipinate?
If you miss a dose of Spiramycin adipinate, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
What happen if I overdose of Spiramycin adipinate?
Symptoms of overdose may include nausea, vomiting, and diarrhea.
Is Spiramycin adipinate an antibiotic?
Spiramycin adipinate is a macrolide antibiotic, first isolated from Streptomyces ambofaciens.
Is spiramycin broad spectrum?
Spiramycin adipinate is a broad-spectrum macrolide antibiotic effective against gram-negative and gram-positive bacteria as well as some Toxoplasma parasites. Spiramycin adipinate is a mixture of Spiramycin adipinate I, II, and III and has been used to study sepsis in mice.
