ROPIVACINELOCAL ANAESTHESIA

AMIDE GROUP

COMPARISON WITH BUPIVACINERopivacine Bupivacine

Duration of Action Upto 8 hrs Same

Cardio-toxicity Less More

CNS toxicity Less More

Affinity to Na Channel More (4.4 times) Less

Lipid Solublity Low High

Recovery Profile Rapid Slow

It was developed after bupivacaine when noted cardiac arrest particular in Pregnant women.

• Chemical Formula:C17H26N2O

• Molar Mass: 274.4 g/mol

• Route of administration : Parenteral

• Bioavailablity: 87%-98% (epidural)

• Biological half life: 1.6 to 6 hrs

• Greater Clearance

Fig Structure of Ropivacine

• Brand Name: Naropin,Naropin SDV, Naropin Novaplus

• Uses: Cesarean Section Labor Pain Local Anasthesia

Drug Class :Local Injectible anesthetics

New Anesthetic of Amino Amide Group Blocks Ad and C fibres more Completely So Blocks Pain transmission rather than motor Function Prolonged Use may delay uptake of drug into plasma and diminish clearance by liver

MECHANISM OF ACTION

PHARMACOKINETICS (VS BUPIVACINE)• 2-3 times more lipid Soluble (less penetration into A Fibres)

• 94% plasma protein Binding

• Cross Placental

• PH 7.4, Pka 8.07 (Bupivacine 8.1)

• Metabolism: Hepatic Cyt P450

• Excretion: 86% by Urine

PHARMACODYNAMICS

• Delayed motor block, for short duration

• Clinically Significant Vasoconstriction , not increased by addition of epinephrine

• Has advantage over lidocaine due to non-toxicity

Animals can tolerate higher level of Ropivacine than Bupivacine via Iv Route

INDICATION

• Local anaesthesia• Infiltration(during labour)• Nerve block (Surgery)• Epidural anaesthesia(acute pain management)• Intrathecal anaesthesia

DOSE CONC DURATION VOLUME/DOSEINFILTRATION 0.2-0.5°/o 2-4 hrs 200mgNERVE BLOCKminor

0.2-0.5°/o 4-7 hrs 10-100 mg I5-20 ml

NERVE BLOCKmajor

0.2-0.5°/o 6-12 hrs 250mg I30-50 ml

EPIDURAL 0.2-0.75% 3-6 hrs 250mg I15-30 ml

SPINAL hyperbaric 0.5-0.75% 90-200 mins 15-20 mg I

2-3 mlisobaric 0.5°/o 90-200 mins 3-4 ml

SIDE EFFECTS

• Drowsiness, dizziness or blurred vision• Abnormal Skin Sensations• Several allergic reactions

AVOID USING ROPIVACINE DURING PREGNANCY AND BREAST FEEDING

BENZOCAINELOCAL ANAESTHESIA

ESTER GROUP

Ethyl-p-aminobenzeneChemical Formula: C9H11NO2Low water solublityUsed primarily as a free esterApplied to damaged skin

In 1890 it was sold by the brand name Anasthesin

Fig Benzocaine

• Brand Name: Benzotic,Omedia,Oticaine,Pinnacaine• Use: topical• Used as topical pain remover or in Cough drops• Mixed in ear drops as well.• Onset of action: About 1 minute.

MOA

• Inhibits Voltage dependent Sodium Channel on neuron Membrane stopping Propagation of action potential.

DRUG INTERACTION

• Cholinesterase inhibitors (metabolism of an ester-derivative local anesthetic may be inhibited, leading to increased risk of systemic toxicity, when it is administered to a patient receiving a cholinesterase inhibitor)

• Sulfonamides (metabolites of PABA-derivative local anesthetics may antagonize antibacterial activity of sulfonamides)

APPLICATION

• Damaged skin,otic pain• Local anesthesia of Oral and Pharyngeal mucous membrane• Supress Vomiting as it blocks receptors in gastric mucosa

“It is slowly absorbed from site of application which provides more safely and longer

duration of action”

Bee Stings, Minor Burns, Sunburn, Insect Bites

Apply 5-20% to affected arearemove sting prior to application if a bee sting

Mouth and Gum Irritation Apply 10-20% solution (or other topical formulation) PRN

Sore Throat/Mouth Pain 2-3 drops with water every 2-3 hrs

Dental pain Use 2.5-20% solution (or other topical formulation)

Premature Ejaculation EjectDelay (7.5% gel): Apply small amount to the penis gland 15-20 min before sexual

DOSE

SIDE EFFECTS

• Produce allergic reactions • Cause methemoglobinemia• Seizures coma, irregular heart beat, respiratory depression (for high dose)• Increases risk of pulmonary aspiration.• Contact dermatitis and anaphylaxis.

Treatment for methemoglobinemia:Administering methylene blue (1 to 2 mg per kg of body weight, intravenously) and/or ascorbic

acid (100 to 200 mg orally).

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