Bupizuva Heavy

Bupizuva Heavy Uses, Dosage, Side Effects, Food Interaction and all others data.

Bupivacaine injectioin is a preparation of bupivacaine, a long acting local anaesthetic agent that belongs to amide group. It blocks the generation and the conduction of nerve impulses, 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 voltage-gated sodium channels and blocks sodium influx into nerve cells, which prevents depolarization. Without depolarization, no initiation or conduction of a pain signal can occur.

The rate of systemic absorption of bupivacaine and other local anesthetics is dependent upon the 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 preparation.

Onset of action (route and dose-dependent): 1-17 minDuration of action (route and dose-dependent): 2-9 hrHalf life: neonates, 8.1 hr, adults: 2.7 hrTime to peak plasma concentration (for peripheral, epidural, or caudal block): 30-45 minProtein binding: about 95%Metabolism: hepaticExcretion: renal (6% unchanged)Bupivacaine is a widely used local anesthetic agent. Bupivacaine is often administered by spinal injection prior to total hip arthroplasty. It is also commonly injected into surgical wound sites to reduce pain for up to 20 hours after surgery. In comparison to other local anesthetics it has a long duration of action. It is also the most toxic to the heart when administered in large doses. This problem has led to the use of other long-acting local anaesthetics:ropivacaine and levobupivacaine. Levobupivacaine is a derivative, specifically an enantiomer, of bupivacaine. Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems. At blood concentrations achieved with therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal. However, toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block, ventricular arrhythmias and to cardiac arrest, sometimes resulting in fatalities. In addition, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure. Following systemic absorption, local anesthetics can produce central nervous system stimulation, depression or both.

Bupivacaine is a widely used local anesthetic agent. Bupivacaine is often administered by spinal injection prior to total hip arthroplasty. It is also commonly injected into surgical wound sites to reduce pain for up to 20 hours after surgery. In comparison to other local anesthetics it has a long duration of action. It is also the most toxic to the heart when administered in large doses. This problem has led to the use of other long-acting local anaesthetics:ropivacaine and levobupivacaine. Levobupivacaine is a derivative, specifically an enantiomer, of bupivacaine. Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems. At blood concentrations achieved with therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal. However, toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block, ventricular arrhythmias and to cardiac arrest, sometimes resulting in fatalities. In addition, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure. Following systemic absorption, local anesthetics can produce central nervous system stimulation, depression or both.

Dextrose is a monosaccharide that is used as a source of calories and water for hydration. It helps to reduce loss of body protein and nitrogen. It also promotes glycogen deposition in the liver. When used with insulin, it stimulates the uptake of potassium by cells, especially in muscle tissue, thus lowering serum potassium levels.

Blood glucose is an obligatory energy source in humans involved in various cellular activities, and it also acts as a signalling molecule for diverse glucose-sensing molecules and proteins. Glucose undergoes oxidation into carbon dioxide, water and yields energy molecules in the process of glycolysis and subsequent citric cycle and oxidative phosphorylation. Glucose is readily converted into fat in the body which can be used as a source of energy as required. Under a similar conversion into storage of energy, glucose is stored in the liver and muscles as glycogen. Glucose stores are mobilized in a regulated manner, depending on the tissues' metabolic demands. Oral glucose tablets or injections serve to increase the supply of glucose and oral glucose administration is more effective in stimulating insulin secretion because it stimulates the incretin hormones from the gut, which promotes insulin secretion.

Bupizuva Heavy
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Bupizuva Heavy
Generic	Dextrose + Bupivacaine
Weight	8%
Type	Injection
Therapeutic Class
Manufacturer	Abbott Healthcare Pvt Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Bupivacaine is used for the production of local or regional anaesthesia or analgesia for surgery, for oral surgery procedures, for diagnostic and therapeutic procedures, and for obstetrical procedures. The routes of administration and used Bupivacaine concentrations are:

Local infiltration: 0.25%
Peripheral nerve block: 0.25%, 0.5%
Sympathetic block: 0.25%
Lumbar epidural: 0.25%, 0.5% and 0.75% (non-obstetrical)
Caudal: 0.25%, 0.5%

Dextrose is administered as a parenteral nutrition solution in the treatment of carbohydrate depletion and hypoglycaemic coma. Because of its high dextrose content it is used in the treatment of cerebral edema, shock, circulatory collapse, unconsciousness and to correct hyperkalaemia with or without insulin.

Bupizuva Heavy is also used to associated treatment for these conditions: Acute Gouty Arthritis, Adrenal cortical hypofunctions, Alopecia Areata (AA), Ankylosing Spondylitis (AS), Berylliosis, Bullous dermatitis herpetiformis, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Dermatomyositis, Discoid Lupus Erythematosus (DLE), Edema of the cerebrum, Epicondylitis, Hemolytic Anemia, Keloid Scars, Leukemias, Mycosis Fungoides (MF), Necrobiosis lipoidica diabeticorum, Ocular Inflammation, Ophthalmia, Sympathetic, Osteoarthritis (OA), Pain, Labor, Polymyositis, Postoperative pain, Psoriatic Arthritis, Psoriatic plaque, Pure Red Cell Aplasia, Regional Enteritis, Rheumatoid Arthritis, Secondary thrombocytopenia, Stevens-Johnson Syndrome, Synovitis, Systemic Lupus Erythematosus (SLE), Temporal Arteritis, Trichinosis, Tuberculous Meningitis, Ulcerative Colitis, Uveitis, Acute Bursitis, Acute Idiopathic Nephrotic Syndrome, Acute Lupus Erythematosus, Acute Multiple sclerosis, Acute Rheumatic heart disease, unspecified, Acute nonspecific tenosynovitis, Cancer-associated hypercalcemia, Cystic tumors of aponeurosis, Cystic tumors of tendon, Disseminated Pulmonary Tuberculosis, Exfoliative erythroderma, Inflammatory lesions of granuloma annulare, Inflammatory lesions of lichen planus, Inflammatory lesions of lichen simplex, Non-suppurative Thyroiditis, Permphigus, Severe Allergic Reactions, General Anesthesia, Regional nerve block therapy, Local anesthesia therapyArrhythmia, 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 Bupizuva Heavy works

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 prevents depolarization by bindng to the intracellular portion of sodium channels and blocking sodium ion influx into neurons. 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.

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

Bupizuva Heavy dosage

Percutaneous infiltration anesthesia For prolonged action: 9 mg with adrenaline (1 in 200,000), may repeat 2-10 mins later if needed. Max: 90 mg per dental sitting.

Peripheral nerve block: 12.5 mg (as 0.25% solution) or 25 mg (as 0.5% solution). Max: 150 mg/dose.

Sympathetic nerve block: As 0.25% solution: 50-125 mg.

Retrobulbar block: As 0.75% solution: 15-30 mg.

Caudal block In surgery: 37.5-75 mg (as 0.25% solution) or 75-150 mg (as 0.5% solution). Lumbar epidural block In surgery: 25-50 mg (as 0.25% solution) and 50-100 mg (as 0.5% solution).

The volume and rate of infusion of dextrose solution will depend upon the requirements of the individual patient and the judgement of the physician.

The maximum rate at which dextrose can be infused without producing glycosuria is 0.5 gm/kg/hr.

The usual recommended flow rate for adult is 10-35 drops per minute infused intravenously.

Intravenous-

Hyperkalaemia:

Adult: 25-50 g combined with 10 units of regular insulin, administered over 30-60 minutes; may repeat if necessary. Alternatively, 25 g combined with 5-10 units of regular insulin infused over 5 minutes; may repeat if necessary.
Child and infants: 0.5-1 g/kg (using 25% or 50% solution) combined with regular insulin (1 unit for every 4-5 g dextrose given); infuse over 2 hr, may repeat if necessary.

Intravenous-

Hypoglycaemia:

Adult: 10-25 g (40-100 ml of 25% solution or 20-50 ml of 50% solution). Doses may be repeated in severe cases.
Child: ≤6 mth: 0.25-0.5 g/kg/dose; >6 mth: 0.5-1 g/kg/dose. Doses may be repeated in severe cases. Max: 25 g/dose.

Oral-

Hypoglycaemia:

Adult: 10-20 g as single dose; may repeat in 10 min if needed.
Child: >2 yr: 10-20 g as single dose; may repeat in 10 min if needed.

It should not be administered by SC or IM route. Dextrose should be infused through the largest available peripheral vein.

Side Effects

Central Nervous System and Neurological: Restlessness, excitement, nervousness, dizziness, tinnitus, blurred vision, miosis, nausea, vomiting, numbness of the tongue and perioral region, chills, tremors, muscle twitching, convulsions.

Cardiovascular System Reactions: Myocardial depression and peripheral vasodilatation resulting hypotension and bradycardia, ventricular arrhythmia, cardiac arrest.

Hypersensitivity: urticaria, pruritus, erythema, angioneurotic edema ,tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and possibly, anaphylactoid reactions.

Venous thrombosis, phlebitis, hypovolemia, hypervolemia, dehydration, oedema, fever, mental confusion, unconsciousness, hyperosmolar syndrome, hyperglycaemia, hypokalaemia, acidosis, hypophosphataemia, hypomagnesemia, polyuria, glycosuria, ketonuria, nausea, diarrhoea, polydipsia, vein irritation, tissue necrosis, pulmonary oedema, tachypnoea.

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.

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

Readiness for emergencies.The lowest dosage that gives effective anaesthesia should be used in order to avoid high plasma levels and serious systemic side effects. Injection of repeated doses of Bupivacaine Hydrocholoride may cause significant increase in blood levels with each additional dose, due to accumulation of the drug or its metabolites or due to slow metabolic degradation. Tolerance varies with the status of the patient. Debilitated, elderly patients and acutely ill patients should be given reduced doses commensurate with age and physical condition. Caution is advised in administration of repeat doses of Bupivacaine Hydrocholoride to patients with severe liver disease.Local anaesthetic procedures should be used with caution when there is inflammation and/or sepsis in the region of the proposed injection.

Concentrated dextrose solution should not be infused rapidly or for a long period. It may be hazardous in patients with impaired hepatic or renal function and severe sepsis.

Care should be taken to avoid circulatory overload, particularly in patients with cardiac insufficiency. Caution must be exercised in the administration of these injections to patients receiving corticosteroids or corticotropin. These injections should be used with caution in patients with overt or subclinical diabetes mellitus.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. Do not administer unless solution is clear and seal is intact.

Interaction

Bupivacaine should be used with caution in patients receiving other local anaesthetics or agents structurally related to amide‐type local anaesthetics, e.g. certain anti‐arrhythmics, such as lidocaine and mexiletine, since the systemic toxic effects are additive.Specific interaction studies with Bupivacaine and anti arrhythmic drugs class III (e.g. amiodarone) have not been performed, but caution should be advised.

There is no drug drug interaction and none well documented.

Volume of Distribution

The mean volume of distribution after intravenous infusion is 10.6L.

Elimination Route

Systemic absorption of local anesthetics is dose- and concentration-dependendent on the total drug administered. Other factors that affect the rate of systemic absorption include the route of administration, blood flow at the administration site, and the presence or absence of epinephrine in the anesthetic solution.

Bupivacaine formulated for instillation with meloxicam produced varied systemic measures following a single dose of varying strength. In patients undergoing bunionectomy, 60 mg of bupivacaine produced a C_max of 54 ± 33 ng/mL, a median T_max of 3 h, and an AUC_∞ of 1718 ± 1211 ng*h/mL. For a 300 mg dose used in herniorrhaphy, the corresponding values were 271 ± 147 ng/mL, 18 h, and 15,524 ± 8921 ng*h/mL. Lastly, a 400 mg dose used in total knee arthroplasty produced values of 695 ± 411 ng/mL, 21 h, and 38,173 ± 29,400 ng*h/mL.

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

2.7 hours in adults and 8.1 hours in neonates.

Bupivacaine applied together with meloxicam for postsurgical analgesia had a median half-life of 15-17 hours, depending on dose and application site.

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

Only 6% of bupivacaine is excreted unchanged in the urine.

Glucose can be renally excreted.

Pregnancy & Breastfeeding use

There are no adequate and well‐controlled studies in pregnant women of the effect of bupivacaine hydrochloride on the developing fetus. Bupivacaine should not therefore be given in early pregnancy only if the potential benefit justifies the potential risk to the fetus. Bupivacaine enters the mother's milk, but in such small quantities that there is no risk of affecting the child at therapeutic dose levels.

Pregnancy Category C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Contraindication

Hypersensitivity to Bupivacaine, other amide type local anaesthetics or other components of these preparations; Intravenous regional anaesthesia; obstetrical paracervical block anaesthesia.

Concentrated dextrose solution is contraindicated in patients with Glucose-Galactose Malabsorption Syndrome and severe hydration. The infusion of hypertonic dextrose injections is contraindicated in patients having intracranial or intraspinal hemorrhage, in patients who are severely dehydrated, in patients who are anuric, and in patients in hepatic coma. Solutions containing dextrose may be contraindicated in patients with known allergy to corn or corn products.

Special Warning

Paediatrics: For children a reduced dose based on body weight and surface area should be used. The dosage should be calculated for each patient individually and modified in accordance with the physician's experience and knowledge of the patient.

Geriatrics: A reduction in dosage may be necessary for elderly patients especially those with compromised cardiovascular and/or hepatic function. Where epidural administration is to be used, a small dose may provide sufficient anaesthesia.

Impaired hepatic function: Although bupivacaine is metabolised by the liver, dosage reduction is probably not warranted. However, caution should be exercised with repeated doses.

Impaired renal function: Impairment of renal function is unlikely to affect bupivacaine clearance in the short term (up to 24 hours). However, toxicity due to accumulation may develop with prolonged or repeated administration.