Product Information
Registration Status: ActiveSIN14273P
SURGICAINE INJECTION is approved to be sold in Singapore with effective from 2012-11-22. It is marketed by N.K. LUCK (S) PTE LTD, with the registration number of SIN14273P.
This product contains Bupivacaine 5mg, and Adrenaline 0.005mg in the form of INJECTION. It is approved for DENTAL use.
This product is manufactured by Novocol Pharmaceutical of Canada in CANADA.
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.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
A widely used local anesthetic agent. [PubChem]
Indication
For the production of local or regional anesthesia or analgesia for surgery, for oral surgery procedures, for diagnostic and therapeutic procedures, and for obstetrical procedures.
Mechanism of Action
Local anesthetics such as bupivacaine block the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. Bupivacaine binds to the intracellular portion of sodium channels and blocks sodium influx into nerve cells, which prevents depolarization. In general, the progression of anesthesia is related to the diameter, myelination and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone. The analgesic effects of Bupivicaine are thought to potentially be due to its binding to the prostaglandin E2 receptors, subtype EP1 (PGE2EP1), which inhibits the production of prostaglandins, thereby reducing fever, inflammation, and hyperalgesia.
Pharmacokinetics
- Absorption
- The rate of systemic absorption of local anesthetics is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic solution.
- Distribution
- Metabolism
- Amide-type local anesthetics such as bupivacaine are metabolized primarily in the liver via conjugation with glucuronic acid. The major metabolite of bupivacaine is 2,6-pipecoloxylidine, which is mainly catalyzed via cytochrome P450 3A4.
- Elimination
Toxicity
The mean seizure dosage of bupivacaine in rhesus monkeys was found to be 4.4 mg/kg with mean arterial plasma concentration of 4.5 mcg/mL. The intravenous and subcutaneous LD 50 in mice is 6 to 8 mg/kg and 38 to 54 mg/kg respectively. Recent clinical data from patients experiencing local anesthetic induced convulsions demonstrated rapid development of hypoxia, hypercarbia, and acidosis with bupivacaine within a minute of the onset of convulsions. These observations suggest that oxygen consumption and carbon dioxide production are greatly increased during local anesthetic convulsions and emphasize the importance of immediate and effective ventilation with oxygen which may avoid cardiac arrest.
Active Ingredient/Synonyms
(±)-bupivacaine | (RS)-bupivacaine | 1-Butyl-2',6'-pipecoloxylidide | 1-Butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide | Bupivacaina | Bupivacainum | dl-1-Butyl-2',6'-pipecoloxylidide | DL-Bupivacaine | racemic bupivacaine | Bupivacaine |
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
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.