Product Information
Registration Status: ActiveSIN07977P
BEATHRICIN LOZENGES is approved to be sold in Singapore with effective from 1994-12-31. It is marketed by BEACONS PHARMACEUTICALS PTE LTD, with the registration number of SIN07977P.
This product contains Lignocaine 5mg, and Tyrothricin 1mg in the form of LOZENGE. It is approved for ORAL use.
This product is manufactured by BEACONS PHARMACEUTICALS PTE LTD in SINGAPORE.
It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacaine or prilocaine. [PubChem]
Indication
For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
Mechanism of Action
Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. Lidocaine alters signal conduction in neurons by blocking the fast voltage gated sodium (Na+) channels in the neuronal cell membrane that are responsible for signal propagation. With sufficient blockage the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential. This creates the anaesthetic effect by not merely preventing pain signals from propagating to the brain but by aborting their birth in the first place.
Pharmacokinetics
- Absorption
- Information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.
- Distribution
- * 0.7 to 2.7 L/kg [healthy volunteers]
- Metabolism
- Primarily hepatic.
- Elimination
Clearance
* 0.64 +/- 0.18 L/min
Toxicity
The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Active Ingredient/Synonyms
2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide | alpha-diethylamino-2,6-dimethylacetanilide | Lignocaine | α-diethylamino-2,6-dimethylacetanilide | Lidocaine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
Description
A polypeptide antibiotic mixture obtained from Bacillus brevis. It consists of a mixture of three tyrocidines (60%) and several gramicidins (20%) and is very toxic to blood, liver, kidneys, meninges, and the olfactory apparatus. It is used topically.
Indication
Tyrothricin is used as an over the counter topical antibiotic.
Mechanism of Action
Tyrocidines have a β-sheet structure containing both L and D amino acids [A32866]. These structural features contribute to the formation of a curved dimer in which most amino acid side chains are located on the convex surface. The dimer orients itself at the membrane-water interface on bacterial cells with the relatively hydrophilic back-bone on the concave side facing the external environment and the many hydrophobic side chains on the convex side facing into the cell's lipid bilayer. The tyrocidine dimer is able to disrupt the cell membrane producing leakage of cell contents but the exact mechanism of this permeabilization is unclear. Tyrocidines appear to act as reversible non-competitive inhibitors of acetylcholinesterase and β-galactosidase [A32867]. The relation of this to their antibacterial action is unknown. Gramcidins adopt similar β-sheet structures but are capable of forming β-helices [A32873]. They can either form a double helix, running either parallel or anti-parallel, or a helical dimer wherein the N-termini of each polypeptide meets in the middle of the lipid bilayer. The alternating L and D amino acid structure allows the hydrophobic side chains to point outwards into the lipid bilayer, leaving the more hydrophilic backbone to form the lumen of the pore. The carbonyl oxygen atoms aid in the transport of cations through the pore. In both double helix and helical dimer conformations, gramcidins are capable of transporting monovalent cations through the membrane. Divalent cations result in blockage of the pore or channel when bound. Loss of potassium ions through membrane permeabilization seems to inhibit bacterial growth. Gramcidin also appears to be able to insert into the mitochondial membrane and conduct hydrogen ions [A32874]. This results in an uncoupling of oxidative phosphorylation from ATP generation due to the loss of the hydrogen ion gradient necessary for H+ATPase function.
Pharmacokinetics
- Absorption
- The lack of water solubility prevents absorption of tyrothricin through the skin. It is not used through other routes due to toxicity concerns [A32843].
- Distribution
- Metabolism
- Elimination
Toxicity
The components of tyrothricin are capable of disrupting eukaryotic cell membranes at high concentrations resulting in toxicity [A32878]. This manifests as hemolysis in systemic administration. It is thought that the cholesterol present in eukaryotic cells affords some resistance to the toxic mechanisms of tyrothricin [A32877]. Loss of olfactory function has been noted and topical administration to the nasal mucous membranes is not recommended [A32843].
Active Ingredient/Synonyms
Bactratycin | Hydrotricine | Tirotricina | Tyrothricine | Tyrothricinum | Tyrothricin |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.