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Submitted by:

Muhammad Ahmad Bashir (369)


Syed Ammar (304)
Abdurehman (388)
Kashif Khan (108)
Shahad kamal (102)
Section: 7th B
Group: F
Topic:
Difference in Pharmacokinetic parameters of three anesthetics with different
available dosage form

Submitted to:
Maam Mariyam Shabir

Anesthetic

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Any substance that produces a local or general loss of sensation, including pain. Anesthetic
achieve this effect by acting on brain or peripheral nervous system to suppress responses to
sensory stimulation. The unresponsive state thus induced is known as anesthesia.

Types of anesthetic:
There are four main categories of anesthesia used during surgery
1. General Anesthesia: General anesthesia or general anesthesia (see spelling differences)
is a medically induced coma with loss of protective reflexes, resulting from the
administration of one or more general anesthetic agents.
2. Regional Anesthesia: Regional anesthesia is a method of pain prevention for surgeries
and procedures. In regional anesthesia, only the area of the body that would feel pain is
numbed, allowing the patient to have the procedure while awake or while sedated but still
conscious. Spinal or epidural blocks are examples of regional anesthesia
3. Sedation (Sometimes Called "Monitored Anesthesia Care"): also called monitored
anesthesia care or MAC, is a type of anesthesia service during which a patient is typically
still aware, but very relaxed. The amount of sedation provided during MAC is determined
by the anesthesia professional (physician anesthesiologist or nurse anesthetist) providing
the care.
4. Local Anesthesia: Local anesthesia, in a strict sense, is anesthesia of a small part of the
body such as a tooth or an area of skin. Regional anesthesia is aimed at anesthetizing a
larger part of the body such as a leg or arm.
Example:
Examples include Ketamine, lidocaine, tetracaine etc.

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Comparison Pharmacokinetic Parameters of ketamine administered a single
dose of 2mg/kg BW Intravenously (IV) or intranasal (IN)
Pharmacokinetic Names Dosage Form 1 Dosage Form 2
Parameters IV IN (intranasal)

Brand Name KETALAR SPRAVATO


(50MG/ML)
Generic name Ketamine Esketamine

Cmax (ng/mL) Maximum / 1694.48±876.67


concentration
Tmax (h) Maximum time / 0.25±0.14

AUC0-4h (ng.h/mL) Area under curve 1415.78±338.40 1925.66±789.83

AUC0-∞ (ng.h/mL) Area under curve 1532.31±397.01 2199.27±773.23

Vd (mL/kg) Volume of 2869.08±570.03 2342.36±2086.60


distribution
Cl (mL/h/Kg) Clearance 1378.09±340.02 1008.68±333.27

T1/2 (h) Half life 1.47±0.24 1.50±0.97

F Bioavailability 93% 40%

Protein Binding 53.5% 43%

Reference:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/016812s039lbl.pdf

Ketalar Injection Sparavato

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Comparison Pharmacokinetic Parameters of Lidocaine topical cream 1.8%
and intravenous Lidocaine (0.7mg/Kg) IV.

Pharmacokinetic Names Dosage Form 1 Dosage Form 2


Parameters Topical Patch IV

Brand Name ZTLIDO XYLOCAINE

Generic name Lidocaine 1.8% Lidocaine


(10mg/ml)
Cmax (ng/mL) Maximum 75.5±25.53 1778.39±255
concentration
Tmax (h) Maximum time 14.0±9 0.13±0.1

AUC0-t (ng.h/mL) Area under curve 1160.3±394.5 1981.94

AUC0-∞ (ng.h/mL) Area under curve 1207.4 1998.56

Ke (h-1) Elimination rate 0.13 0.12


constant
T1/2 (h) Half life 5.6 2.92

F Bioavailability 5% 35%

Protein Binding 70% 70%

Vd (L/Kg) Volume of distribution 0.13-2.5 0.7-2.7

Reference:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207962s000lbl.pdf

Xylocaine IV Ztlido

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Comparison Pharmacokinetic Parameters of “Propofol”

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