Marcaine and Marcaine spinal heavy

El-Ezaby training department

Item Active ingredients Pharmacological action

Marcaine

Marcaine + adrenaline

Marcaine Spinal Heavy

Bupivacaine Bupivacaine (highest lipophilicity "longer duration") It is a homologue of mepivacaine and is chemically related to lidocaine. Local anesthetics block the generation and the conduction of nerve impulses. Marcaine is racemic mixture of (R,S enantiomers), Levobupivacaine (Chirocaine) is the S-enantiomer of Bupivacaine is equally effective of Bupivacaine but it has less cardiotoxic side effects Bupivacaine HCl + adrenaline Adrenaline: reduces the rate of systemic absorption and peak plasma concentration of Bupivacaine reduce systemic side effects, permitting the use of larger doses and prolonging the duration of action. Contain preservatives : - Multiple dose (methylparaben) - Single dose (sodium metabisulfite, monothioglycerol, and ascorbic acid) care for sulfite allergy 3.4-4.5 1.008

Additives

Bupivacaine only

Bupivacaine hydrochloride in dextrose injection "hyperbaric (high pressure) solution for subarachnoid injection (spinal block) ." Dextrose: increase density and adhesion (prolong duration of action) Does not contain any preservatives

pH Specific gravity (represents density)

4-6.5 1.010

4-6.5 1.035 (higher density)

Pharmacokinetics

Onset : very fast onset Duration: 2 hours (in 12 mg dose) with or without 0.2 mg epinephrine

Onset : within 1 min (maximum effect within 15 min) Duration: 3.5 hours without epinephrine 4.5 hours with 0.2 mg epinephrine

Indication

For the production of local or regional anesthesia or analgesia production of subarachnoid block (spinal anesthesia). for surgery, dental and oral surgery procedures, diagnostic and

therapeutic procedures, and for obstetrical procedures. A high protein binding capacity (95%) Has a low fetal/maternal ratio (0.2 to 0.4)- maximum dose in labor is 0.5 mg% Bupivacaine activity depends on degree of ionization, that become higher at lower pH 4-6 (local anesthetics are weak bases "pH 8-9")

Other features

References: Goodman & Gilman's Manual of Pharmacology and Therapeutics. Copyright 2008 by The McGraw-Hill Companies. Marcaine package insert. Wilson and Gisvold's-Textbook of organic, medicicnal and pharmaceutical chemistry. Copyright 2011 by Lippincott Williams & Wilkins.