What does lidocaine dissolve in?

Lidocaine is practically insoluble in water and very soluble in alcohol; it dissolves in oils. It can be mixed with prilocaine to form a eutectic with a lower melting point than that of either of the ingredients, and the eutectic can be incorporated into topical dosage forms.

How does pH affect lidocaine?

The uncharged lidocaine base B is lipophilic and easily diffuses through the lipid bilayer of a cell membrane. The higher the pH of a lidocaine solution, the greater is the proportion of uncharged lidocaine base, and the more rapidly the lidocaine will enter a neuron’s axoplasm.

Why is lidocaine mixed with HCL?

This pH is so far below the drug’s pKa that essentially all the drug is present in the more stable, charged, water-soluble form. Hydrochloric acid is added to lignocaine solutions to achieve this low pH.

Why is lidocaine soluble in water?

Lidocaine is an Anesthetic (local); antiarrhythmic (class IB). Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic….137-58-6.

Is lidocaine water soluble?

Lidocaine hydrochloride is very soluble in water (1:0.7) and in alcohol (1:1.5). It is available in both anhydrous and monohydrate forms. Approximately 1.16 g of lidocaine hydrochloride is equivalent to 1 g of lidocaine.

How is lidocaine metabolized?

Lidocaine is metabolized in the liver by the P450 3A4 isoenzyme, a member of the subfamily of P450 isoenzymes. This isoenzyme, the most abundant of the human P450 enzymes, is responsible for the metabolism of more drugs than any other hepatic enzyme.

What is the pH of lidocaine?

Plain 1\% lidocaine had a pH of 6.09±0.16, and plain 2\% lidocaine had a pH of 6.00±0.27.

Is lidocaine polar or non polar?

At that pH, there are two species of lidocaine molecules: one is the charged or polar molecule, and the other is the uncharged or nonpolar molecule. There is a predominance of the charged molecule: about 10 times as much charged/polar lidocaine ion as uncharged/nonpolar lidocaine.

Is lidocaine HCL soluble in water?

What metabolizes lidocaine?

Lidocaine is metabolized in the liver by the P450 3A4 isoenzyme, a member of the subfamily of P450 isoenzymes.

What is the MOA of lidocaine?

The principal mechanism of action of lidocaine as a local anaesthetic is through blockade of voltage-gated sodium channels (VGSCs) leading to a reversible block of action potential propagation.

Is lidocaine an acid?

Lidocaine with epinephrine is very acidic compared with subcutaneous tissue. The addition of 8.4\% bicarbonate at a volume ratio of 1 mL:10 mL neutralizes the acidity of 1\% lidocaine with 1:100,000 epinephrine. Neutralizing the pH of lidocaine has been previously shown to decrease the pain of injection.

What is the dissociation constant of lidocaine?

As lidocaine is a weak base with a dissociation constant (pKa) of 7.7,[2] approximately 25\% of molecules will be un-ionized at a physiological pH of 7.4 and will be available to translocate inside the nerve cells, meaning that lidocaine has a more rapid onset of action than other local anesthetics with higher pKa values.

What is the structure of lidocaine?

Lidocaine is 65\% protein-bound to albumin and alpha1-acid glycoprotein in the plasma, giving it a medium duration of action compared to other local anesthetic agents. It is less lipid soluble than other agents, limiting its overall potency.

What is the maximum amount of lidocaine in a single application?

A single application should not exceed 5 g of Lidocaine Ointment USP, 5\% containing 250 mg of lidocaine base (equivalent chemically to approximately 300 mg of lidocaine hydrochloride). This is roughly equivalent to squeezing a six (6) inch length of ointment from the tube.

What happens when lidocaine is charged or uncharged?

An uncharged lidocaine molecule diffuses across a neuron cell membrane more rapidly than a charged molecule. The Henderson-Hasselbalch equation for bases states the following: where B is concentration of nonionized base, and B H + is concentration of a positively charged ionized base.