Product Information
Registration Status: ActiveXYLOCAINE 2% WITH ADRENALINE 1:80,000 INJECTION is approved to be sold in Singapore with effective from 1991-08-04. It is marketed by DENTSPLY (SINGAPORE) PTE LTD, with the registration number of SIN05752P.
This product contains Adrenaline 0.0125mg/ml, and Lignocaine 20mg/ml in the form of INJECTION. It is approved for DENTAL use.
This product is manufactured by Showa Yakuhin Kako Co. in JAPAN.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
The active sympathomimetic hormone from the adrenal medulla in most species. It stimulates both the alpha- and beta- adrenergic systems, causes systemic vasoconstriction and gastrointestinal relaxation, stimulates the heart, and dilates bronchi and cerebral vessels. It is used in asthma and cardiac failure and to delay absorption of local anesthetics. [PubChem]
Indication
Used to treat anaphylaxis and sepsis. Also one of the body's main adrenergic neurotransmitters.
Mechanism of Action
Epinephrine works via the stimulation of alpha and beta-1 adrenergic receptors, and a moderate activity at beta-2 adrenergic receptors.
Pharmacokinetics
- Absorption
- Usually this vasodilator effect of the drug on the circulation predominates so that the modest rise in systolic pressure which follows slow injection or absorption is mainly the result of direct cardiac stimulation and increase in cardiac output.
- Distribution
- Metabolism
- Epinephrine is rapidly inactivated in the body and is degraded by enzymes in the liver and other tissues. The larger portion of injected doses is excreted in the urine as inactivated compounds and the remainder either partly unchanged or conjugated. The drug becomes fixed in the tissues and is inactivated chiefly by enzymatic transformation to metanephrine or normetanephrine either of which is subsequently conjugated and excreted in the urine in the form of sulfates and glucuronides. Either sequence results in the formation of 3-methoxy-4-hydroxy-mandelic acid which also is detectable in the urine. Main metabolic enzymes include MAO and COMT
- Elimination
Toxicity
Skin, LD50 = 62 mg/kg (rat)
Active Ingredient/Synonyms
(-)-(R)-Epinephrine | (-)-3,4-Dihydroxy-alpha-((methylamino)methyl)benzyl alcohol | (-)-Adrenaline | (−)-adrenaline | (R)-(-)-Adnephrine | (R)-(-)-Adrenaline | (R)-(-)-Epinephrine | (R)-(-)-Epirenamine | (R)-(−)-adrenaline | 4-[(1R)-1-Hydroxy-2-(methylamino)ethyl]-1,2-benzenediol | Adrenaline | Epinefrin | Epinefrina | Epinephrin | Epinephrine | Epinephrinum | L-Adrenaline | levoepinephrine | Epinephrine |
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 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.