Bupivacaine (HCl)

Drug #109

Bupivacaine (HCl) is amide local anesthetic and a homologue of mepivacaine, chemically related to lidocaine. It consists of an aromatic ring connected by an intermediate chain to an ionizable group, usually a tertiary amine. Bupivacaine (HCl) is more potent and has a longer duration of action than mepivacaine.

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Primary Characteristics

It is of Synthetic origin and belongs to Amide type.

It belongs to Na-Channel Local Anesthetic antagonist pharmacological group on the basis of mechanism of action.

Molecular Weight: 430.5 · pK_a: not relevant · Solubility in Water: 1 in 25 · Solubility in Alcohol: 1 in 8 · Non-proprietary name: Bupivacaine (HCl) · pH: 6.8 · Isotonic value: 5.38.

Molecular structure of Bupivacaine (HCl)

Pharmacokinetics

Absorption: Bupivacaine (HCl) has an oral bioavailability is 100%, pre-systemic (first-pass) metabolism accounts for 90%.

Distribution: Bupivacaine (HCl) has a volume of distribution is 73 litre. plasma protein binding is 86-90%.

Elimination: it is metabolised via hepatic, plasma half-life is 1-3 hr, renal excretion is 2%.

Indications

Bupivacaine (HCl) is primarily indicated in conditions like Epidural block, surgery, Heart failure, Labor, Local anaesthesia, Local infiltration, Peripheral nerve block, Supraventricular arrhythmias (particularly atrial fibrillation), Sympathetic block.

Contraindications

Bupivacaine (HCl) is contraindicated in conditions like Hypovolaemia, Intravenous regional anaesthesia, Hypersensitivity.

Dosage

Bupivacaine (HCl)'s dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
75 mg	75 mg	—	Intra Thecal	As Required
Paediatric Dosage (20kg)
1.25 mg/kg	1.25 mg/kg	—	Intra Thecal	As Required
Neonatal Dosage (3kg)
1.25 mg/kg	1.25 mg/kg	—	Intra Thecal	As Required

Drug Interactions

2 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Bupivacaine (HCl) produces potentially life-threatening effects which include Respiratory depression, Respiratory arrest. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Bupivacaine (HCl) are Metallic taste, Irrational behavior, Tinnitus , Circumoral numbness, Anxiety .

Bupivacaine (HCl) is known to cause more or less tolerable side effects which are usually transient. These include Anxiety, Circumoral numbness, Metallic taste, Shivering , Tinnitus.

Warnings / Precautions

Avoid Bupivacaine in patient with known hypersensitivity. It should be given with caution to the elderly, to debilitated, to children, patients with epilepsy, impaired cardiac conduction or respiratory function, shock or liver damage. It might be ototoxic and should not be instilled into the middle ear. The application of local anaesthatics to the skin for prolonged period or to the extensive area should be avoided.

Interference in Pathology

Bupivacaine (HCl) may interfere in the diagnosis of Interfere with the measurement of plasma cholinestrase enzyme in blood sample. .

Available Brands

Click on a strength to view available brands.

Single Ingredient

Inj

5 mg/ml 7.5 mg/ml

Inj CS

7.5 mg/ml

Multi-Ingredient Combinations

Inj

7.5 mg/ml

Storage Conditions

Bupivacaine (HCl) should be stored Inj.

Drug Classification

1.1.2 — Local anesthetics

Manufacturers

Manufacturers of Bupivacaine (HCl) in Pakistan:

Abbott Bosch Brookes Global LCPW Ophth-Pharma Surge