Ultracaine Heavy 0.5%+8% Intraspinal Injection
Ultracaine Heavy 0.5%+8% Intraspinal Injection Uses, Dosage, Side Effects, Food Interaction and all others data.
Each 4 ml injection contains- Bupivacaine Hydrochloride USP 20 mg Dextrose Anhydrous USP 320 mg| Trade Name | Ultracaine Heavy 0.5%+8% Intraspinal Injection |
| Generic | Bupivacaine Hydrochloride + Dextrose |
| Weight | 0.5%+8% |
| Type | Intraspinal Injection |
| Therapeutic Class | Regional anesthesia |
| Manufacturer | Jayson Pharmaceuticals Ltd. |
| Available Country | Bangladesh |
| Last Updated: | September 24, 2024 at 5:38 am |
Uses
Bupivacaine Hydrochloride & Dextrose is indicated for- Bupivacaine is indicated for lower abdominal surgery (including Caesarean section), urological and lower limb, including hip surgery, lasting 1.5 to 3 hours. Bupivacaine are indicated for intrathecal (subarachnoid, spinal) anesthesia for surgical and obstetrical procedures. ... Read moreUltracaine Heavy 0.5%+8% Intraspinal Injection is also used to associated treatment for these conditions: Arrhythmia, Caloric Deficit, Edema of the cerebrum, Metabolic Alkalosis, Hypoglycemic reaction, Blood Specimen Collection, Electrolyte replacement, Nutritional supplementation, Parenteral Nutrition, Parenteral rehydration therapy, Plasmapheresis, Positive cardiac inotropic effect, Total parenteral nutrition therapy, Urine alkalinization therapy, Fluid and electrolyte maintenance therapy
How Ultracaine Heavy 0.5%+8% Intraspinal Injection works
Glucose supplies most of the energy to all tissues by generating energy molecules ATP and NADH during a series of metabolism reactions called glycolysis. Glycolysis can be divided into 2 main phases where the preparatory phase is initiated by the phosphorylation of glucose by a hexokinase to form glucose 6-phosphate. The addition of the high-energy phosphate group activates glucose for subsequent breakdown in later steps of glycolysis and is the rate-limiting step. Products end up as substrates for following reactions, to ultimately convert C6 glucose molecule into two C3 sugar molecules. These products enter the energy-releasing phase where total of 4ATP and 2NADH molecules are generated per one glucose molecule. The total aerobic metabolism of glucose can produce up to 36 ATP molecules. This energy-producing reactions of glucose is limited to D-glucose as L-glucose cannot be phosphorlyated by hexokinase. Glucose can act as precursors to generate other biomolecules such as vitamin C. It plays a role as a signaling molecule to control glucose and energy homeostasis. Glucose can regulate gene transcription, enzyme activity, hormone secretion, and the activity of glucoregulatory neurons. The types, number and kinetics of glucose transporters expressed depends on the tissues and fine-tunes glucose uptake, metabolism, and signal generation in order to preserve cellular and whole body metabolic integrity .
Dosage
Ultracaine Heavy 0.5%+8% Intraspinal Injection dosage
The following dosage recommendations should be regarded as a guide for use in the average adult: Spinal anesthesia for surgery: 2-4 ml (10-20 mg Bupivacaine hydrochloride) The patient's physical status and concomitant medication should be considered when deciding the dose, and the lowest dose required for adequate anesthesia should be used. Duration varies with dose, while segmental spread may be difficult to predict, especially with the isobaric (plain) solution. The dose should be reduced in the elderly and in patients in the late stages of pregnancy.Pediatrics: Bupivacaine may be used in children. One of the differences between small children and adults is a relatively high CSF volume in infants and neonates, requiring a relatively larger dose/kg to produce the same level of block as compared to adults. <5 kg: 0.40-0.50 mg/kg 5 to 15 kg: 0.30-0.40 mg/kg 15 to 40 kg: 0.25-0.30 mg/kgIt should not be administered by SC or IM route. Dextrose should be infused through the largest available peripheral vein.
Side Effects
The adverse reaction profile for Bupivacaine is similar to those for other long acting local anesthetics administered intrathecally. Adverse reactions caused by the drug per se are difficult to distinguish from the physiological effects of the nerve block (e.g. decrease in blood pressure, bradycardia, temporary urinary retention), events caused directly (e.g. nerve trauma) or indirectly (e.g. epidural abscess) by the needle puncture or events associated to cerebrospinal leakage.Toxicity
Oral LD50 value in rats is 25800mg/kg. The administration of glucose infusions can cause fluid and/or solute overloading resulting in dilution of the serum electrolyte concentrations, over-hydration, congested states, or pulmonary oedema. Hypersensitivity reactions may also occur including anaphylactic/anaphylactoid reactions from oral tablets and intravenous infusions.
Precaution
Local anesthetics react with certain metals and cause the release of their respective ions which, if injected, may cause severe local irritation. The ampoules are designed for single use only; any unused portions of solutions should be discarded. The solution should be used immediately after opening the ampoule. Solutions showing discoloration should not be used.Interaction
Bupivacaine should be used with care in patients receiving antiarrhythmic drugs with local anaesthetic activity, as their toxic effects may be additive. Phenothiazines and Butyrophenones may reduce or reverse the pressor effect of epinephrine.Volume of Distribution
The mean volume of distribution after intravenous infusion is 10.6L.
Elimination Route
Polysaccharides can be broken down into smaller units by pancreatic and intestinal glycosidases or intestinal flora. Sodium-dependent glucose transporter SGLT1 and GLUT2 (SLC2A2) play predominant roles in intestinal transport of glucose into the circulation. SGLT1 is located in the apical membrane of the intestinal wall while GLUT2 is located in the basolateral membrane, but it was proposed that GLUT2 can be recruited into the apical membrane after a high luminal glucose bolus allowing bulk absorption of glucose by facilitated diffusion . Oral preparation of glucose reaches the peak concentration within 40 minutes and the intravenous infusions display 100% bioavailability.
Half Life
The approximate half-life is 14.3 minutes following intravenous infusion. Gut glucose half-life was markedly higher in females (79 ± 2 min) than in males (65 ± 3 min, P < 0.0001) and negatively related to body height (r = -0.481; P < 0.0001).
Clearance
The mean metabolic clearance rate of glucose (MCR) for the 10 subjects studied at the higher insulin level was 2.27 ± 0.37 ml/kg/min at euglycemia and fell to 1.51±0.21 ml/kg/ at hyperglycemia. The mean MCR for the six subjects studied at the lower insulin level was 1.91 ± 0.31 ml/kg/min at euglyglycemia.
Elimination Route
Glucose can be renally excreted.
Pregnancy & Breastfeeding use
It is reasonable to assume that a large number of pregnant women and women of child-bearing age have been given Bupivacaine. No specific disturbances to the reproductive process have so far been reported, e.g. no increased incidence of malformations. It should be noted that the dose should be reduced in patients in the late stages of pregnancy. With recommended doses, Bupivacaine enters breast milk in such small quantities that there is generally no risk of affecting the breast-fed child. At maternal serum levels of up to 0.45 g/mL produced by the epidural use of Bupivacaine for vaginal delivery, Bupivacaine could not be detected in breast milk during the first 24 hours after delivery (detection limit 0.02 g/mL).Contraindication
General contraindications related to intrathecal anesthesia should be taken into account absolute Allergy or hypersensitivity to amide type local anesthetics. Detection of suspected sensitivity by skin testing is of limited value. Acute active diseases of the cerebrospinal system such as meningitis, tumours (primary or secondary), and poliomyelitis, subacute combined degeneration of the spinal cord, cranial haemorrhage, demyelinating disease and raised intracranial pressure. Spinal stenosis and active disease or recent trauma in the vertebral column. Relative: Arthritis and other diseases of the vertebral column are relative contraindications due to technical difficulties in performing a spinal injection.Special Warning
Use in Children: Administration to children under 12 years of age is not recommended until further experience is gained in this group.Acute Overdose
Acute emergencies associated with the use of local anesthetics are generally related to high plasma levels. Since the dose required for spinal anesthesia is so small (20% or less than that required for epidural anesthesia), acute systemic toxicity is extremely unlikely and has not been reported. With accidental intravascular injections of local anesthetics, the toxic effects will be obvious within 1-3 minutes. With over dosage, peak plasma concentrations may not be reached for 20-30 minutes, depending on the site of injection and toxic signs will be delayed. Toxic reactions mainly involve the central nervous and cardiovascular systems.Storage Condition
Store at temperature not exceeding 30ºC in a dry place. Protect from light.Innovators Monograph
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