Tismamisin
Tismamisin Uses, Dosage, Side Effects, Food Interaction and all others data.
Tismamisin is a lincosamide antibiotic first isolated from the soil bacterium Streptomyces lincolnensis in Lincoln, Nebraska. Clinical use of lincomycin has largely been superseded by its semisynthetic derivative clindamycin due to its higher efficacy and a wider range of susceptible organisms, though lincomycin remains in use.
Tismamisin was approved by the FDA on December 29, 1964.
Tismamisin is a lincosamide antibiotic derived as a natural fermentation product from Streptomyces lincolnensis. Like clindamycin, lincomycin is active against Gram-positive cocci and bacilli as well as Gram-negative cocci and some other organisms such as Haemophilus spp. It is also effective against anaerobic bacteria, though in this regard clindamycin is generally more potent. Prescribing information highlights that the range of clinically confirmed effectiveness is largely limited to Staphylococcus spp. and Streptococcus spp., with additional activity noted in vitro.
| Trade Name | Tismamisin |
| Availability | Prescription only |
| Generic | Lincomycin |
| Lincomycin Other Names | Cillimycin, Lincomicina, Lincomycin, Lincomycine, Lincomycinum |
| Related Drugs | amoxicillin, doxycycline, ciprofloxacin, ciprofloxacin ophthalmic, cephalexin, metronidazole, azithromycin, azithromycin ophthalmic, levofloxacin ophthalmic, erythromycin ophthalmic |
| Weight | 250mg, 500mg |
| Type | Capsule |
| Formula | C18H34N2O6S |
| Weight | Average: 406.54 Monoisotopic: 406.213757997 |
| Protein binding | Lincomycin serum protein binding varies greatly depending on the dose, ranging from 28 to 86% in one study, and generally decreases with increasing serum concentration suggesting saturable binding. It has been suggested that lincomycin, like clindamycin, is primarily bound to α1-acid glycoprotein, which is consistent with later studies in humans and animals. |
| Groups | Approved, Vet approved |
| Therapeutic Class | |
| Manufacturer | Metiska Farma |
| Available Country | Indonesia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tismamisin is an antibiotic indicated only for the treatment of serious infections and is typically reserved for use in cases of penicillin allergy or where penicillin is inappropriate.
Tismamisin is indicated for the treatment of serious bacterial infections by susceptible strains of streptococci, pneumococci, and staphylococci in patients who are allergic to penicillins or for situations in which a penicillin is deemed inappropriate. As with all antibacterial agents, lincomycin should only be used to treat infections proven or strongly suspected to be caused by susceptible bacteria.
Tismamisin is also used to associated treatment for these conditions: Serious Bacterial Infection
How Tismamisin works
Tismamisin contains the unusual amino acid moiety propyl hygric acid linked to the sugar moiety α-methylthiolincosamine (α-MTL) that, like other lincosamides, functions as a structural analogue of the 3' end of L-Pro-Met-tRNA and deacylated-tRNA to interact with the 23S rRNA of the 50S bacterial ribosomal subunit. Detailed investigations into the mechanism of the related lincosamide clindamycin suggested a two-phase binding, instantaneously to the A-site with a shift in equilibrium towards the P-site over several seconds. This shift appears to be due to rotation of the propyl hygric acid moiety, while the α-MTL remains relatively stationary. Recent crystal structures of lincomycin in complex with the 50S ribosomal subunit of Staphylococcus aureus show that the α-MTL moiety forms hydrogen bonds with C2611, A2058, G2505, A2059, and G2503 of the 23S rRNA while the propyl hygric acid moiety interacts only through van der Waals contacts, suggesting it may be free to rotate similar to clindamycin. This mechanism is supported by the observation that the most common resistance mechanism, which also affects macrolides and streptogramin B (MSLB resistance) involves methylation of A2058; other resistance mechanisms similarly target residues such as A2058, A2059, and C2611.
Toxicity
Toxicity information regarding lincomycin is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as gastrointestinal effects including colitis, secondary infections, and severe hypersensitivity reactions. Symptomatic and supportive measures are recommended. It is important to note that hemodialysis and peritoneal dialysis do not appreciably affect lincomycin serum concentrations.
Food Interaction
No interactions found.Tismamisin Drug Interaction
Unknown: arginine, arginine, levocarnitine, levocarnitine, cysteine, cysteine, lithium, lithium, acetaminophen, acetaminophen, valproic acid, valproic acid, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, cholecalciferol, cholecalciferol, phytonadione, phytonadione
Tismamisin Disease Interaction
Major: colitis, prematurityModerate: asthma, renal/liver disease
Volume of Distribution
Tismamisin administered intravenously to healthy adult males had a steady-state volume of distribution of 63.8 ± 23.8, 78.8 ± 17.0, and 105.1 ± 43.1 L for 600, 1200, and 2400 mg doses, respectively.
Elimination Route
A 600 mg dose of lincomycin administered over two hours intravenously results in an average Cmax of 15.9 μg/mL while the same dose given by intramuscular injection produces an average Cmax of 11.6 μg/mL after 60 minutes. Tismamisin administered intramuscularly to healthy adult male volunteers in doses between 600 and 1500 mg had an AUC0-∞ between 92.22 and 159.91 μg*h/mL. A similar study using intravenous infusion of 600-2400 mg lincomycin found AUC0-∞ values between 72.5 and 212.8 μg*h/mL. Overall, the AUC increases disproportionally to dose.
Half Life
Tismamisin has a biological half-life of 5.4 ± 1.0 hours following intramuscular or intravenous administration, which is prolonged in patients with impaired hepatic or renal function.
Clearance
Tismamisin administered intravenously to healthy adult males had a clearance of 9.9 ± 2.5, 10.0 ± 2.0, and 11.8 ± 2.4 L/h for 600, 1200, and 2400 mg doses, respectively.
Elimination Route
Following a 600 mg dose of lincomycin given either intramuscularly or intravenously, the urinary excretion ranges from 1.8-30.3% of the administered dose. Bile is also thought to be an important route of elimination. Dose adjustments are required in patients with either renal or hepatic impairment.
Innovators Monograph
You find simplified version here Tismamisin
FAQ
What is Tismamisin used for?
Tismamisin is an antibiotic that is used to treat severe bacterial infections in people who cannot use penicillin antibiotics. Tismamisin is used only for a severe infection.
How does Tismamisin work?
Tismamisin works by killing or stopping the growth of bacteria causing your infection.
What are the common side effects of Tismamisin?
Common side effects of Tismamisin are include:
- nausea,
- vomiting,
- swollen or painful tongue,
- vaginal itching or discharge,
- mild itching or skin rash,
- ringing in your ears,
- dizziness,
- spinning feeling,
- diarrhea,
- hives,
- anal itching, and
- hypersensitivity reactions (skin swelling, anaphylaxis).
Is Tismamisin safe during pregnancy?
There are no controlled data in human pregnancy; however, this Tismamisin has been used in various stages of human pregnancy without evidence of fetal harm.
Is Tismamisin safe during breastfeeding?
No adverse effects have been reported in nursing infants. A decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother.
Can I drink alcohol with Tismamisin?
Good idea to avoid alcohol until you finish your antibiotics and are feeling better. Ask your doctor before using Tismamisin with alcohol. Tismamisin and alcohol may lead to unpleasant side effects like fast heart beat, flushing, a tingly feeling, nausea, and vomiting.
Can Tismamisin be taken on empty stomach?
You should always take Tismamisin capsules on an empty stomach (1 hour before or 2 hours after meals) with plenty of water.
How long does Tismamisin take to work?
When injected into a vein, Tismamisin must be given slowly, and the infusion can take at least 1 hour to complete.
What is the half life of Tismamisin?
The biological half-life after intramuscular or intravenous administration is 5.4 ± 1.0 hours. The serum half-life of Tismamisin may be prolonged in patients with severe impairment of renal function compared to patients with normal renal function.
How often can I take Tismamisin?
Adults. Serious infections - 600 mg (2 mL) intramuscularly every 24 hours. More severe infections - 600 mg (2 mL) intramuscularly every 12 hours or more often.
Can I take Tismamisin for a long time?
Use this medicine for the full prescribed length of time, even if your symptoms quickly improve. Skipping doses can increase your risk of infection that is resistant to medication. Tismamisin will not treat a viral infection such as the flu or a common cold.
Who should not take Tismamisin?
You should not be treated with Tismamisin if you are allergic to Tismamisin. Before you receive Tismamisin , tell your doctor if you have a history of intestinal disorder such as ulcerative colitis. Tell your doctor if you have ever had: asthma; an intestinal disorder such as colitis; severe allergies; or liver or kidney disease.
What happens if I miss a dose?
Skipping doses can increase your risk of infection that is resistant to medication. Call your doctor for instructions if you miss a dose.
What happens if you overdose on Tismamisin?
If you take too much: You could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug can include: diarrhea. convulsions (sudden movements caused by tightening of the muscles).
