Description

Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.Target: Sodium ChannelRopivacaine is a new long-acting local anesthetic, with vasoconstrictive properties. Ropivacaine given epidurally provided adequate sensory anesthesia and motor block for transurethral surgery. Addition of epinephrine did not provide any significant prolongation of the sensory or motor block, nor any influence upon the sympathetic block [1]. Ropivacaine was metabolized to 2',6'-pipecoloxylidide (PPX), 3'-hydroxyropivacaine (3'-OH Rop), and 4'-hydroxyropivacaine (4'-OH Rop) by hepatic microsomes from human and rat. Ropivacaine N-dealkylation and 3'-hydroxylation activities correlated well with the level of CYP3A4 and 1A2 in human hepatic microsomes, respectively [2].

Ropivacain is a potent sodium channel blocker and acts as a local anesthetic agent. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of regional anesthesia and neuropathic pain management[1].

Levobupivacaine Hcl is a local anaesthetic compound belonging to the amino amide group; long-acting local anesthetic.

Articaine Hydrochloride is a dental local anesthetic.Target: OthersArticaine Hydrochloride is a dental local anesthetic. Articaine: VAS (Visual Analogue Scale) scores (from 0 to 10 cm) by patients 4 to < 13 years of age are 0.5 for simple procedures and 1.1 for complex procedures, and average investigator scores are 0.4 and 0.6 for simple and complex procedures, respectively. No serious adverse events related to the articaine occurres, the only adverse event considered related to articaine is accidental lip injury in one patient [1]. Articaine results in success rate of 64.5% in electronic pulp testing in healthy adult volunteers injected with 4% articaine. Articaine infiltration produces significantly more episodes of no response to maximum stimulation in first molars than lidocaine. Mandibular buccal infiltration is more effective with 4% articaine with epinephrine compared to 2% lidocaine with epinephrine [2]. Articaine formulation results in successful pulpal anesthesia ranged from 75 to 92 percent and onset of pulpal anesthesia ranged from 4.2 to 4.7 minutes in healthy volunteer. For articaine, 4 percent (two of 56) of the subjects reported swelling and no subjects reported bruising. Ninety-eight percent (59 of 60) of the subjects had lip numbness with the articaine solution [3].

Lidocaine Hcl salt, an amide local anesthetic, has anti-inflammatory properties in vitro and in vivo, possibly due to an attenuation of pro-inflammatory cytokines, intracellular adhesion molecule-1 (ICAM-1), and reduction of neutrophils influx.Target: Lidocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery. Lidocaine, the first amino amide-type local anesthetic, was first synthesized under the name xylocaine by Swedish chemist Nils Lofgren in 1943. His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself.Lidocaine is approximately 95% metabolized (dealkylated) in the liver by CYP3A4 to the pharmacologically-active metabolites monoethylglycinexylidide (MEGX) and then subsequently to the inactive glycine xylidide. MEGX has a longer half life than lidocaine but also is a less potent sodium channel blocker. The elimination half-life of lidocaine is approximately 90-120 minutes in most patients. This may be prolonged in patients with hepatic impairment (average 343 minutes) or congestive heart failure (average 136 minutes).

Tetracaine is a topical local anesthetic for the eyes; works by interfering with entry of sodium ions into nerve cells.

Tetracaine HCl is a potent local anaesthetic and a channel function allosteric inhibitor.Target: Calcium ChannelTetracaine hydrochloride is a calcium channel protein inhibitor and blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum. Tetracaine is a potent local anesthetic of the ester group. It is mainly used topically in ophthalmology and as an antipruritic, and it has been used in spinal anesthesia. Tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. Tetracaine is an allosteric blocker of channel function. At low concentrations, tetracaine causes an initial inhibition of spontaneous calcium release events, while at high concentrations, tetracaine blocks release completely [1, 2].

Prilocaine hydrochloride is a local anesthetic of the amino amide type.Target: OthersPrilocaine is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils L?fgren. In its injectable form (trade name Citanest), it is often used in dentistry. It is also often combined with lidocaine as a preparation for dermal anesthesia, for treatment of conditions like paresthesia. As it has low cardiac toxicity, it is commonly used for intravenous regional anaesthesia (IVRA). In some patients, a metabolite of prilocaine may cause the unusual side effect of methemoglobinemia, which may be treated with methylene blue. Maximum dosage for dental use: 8.0 mg/kg (2.7 mg/lb), with a maximum dose of 500 mg.Eutectic Mixture of Local Anesthetics (EMLA) containing 5% lidocaine and prilocaine in a cream was found to give effective topical analgesia in normal and diseased skin, making it useful for superficial surgery and various other clinical procedures. To be effective, an adequate amount must be applied under occlusion and at the right time before the intervention.


Function

an amide local anesthetic. It is widely used in surface anesthesia, infiltration anesthesia, conduction anesthesia and epidural anesthesia.

 

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