Isepamicin: Difference between revisions

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__NOTOC__
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{{SK}} Isepamycin
{{SK}} Isepamycin


==Overview==
==Overview==


Isepamicin is an [[aminoglycoside]] [[antibiotic]].
Isepamicin is an [[aminoglycoside]] [[antibiotic]]. It has been used in the treatment of skin, upper respiratory tract, lower respiratory tract, and urinary tract infections caused by [[Gram-negative]] bacteria (including ''[[Pseudomonas aeruginosa]]'', Proteobacteria, and ''[[Escherichia coli]]'').


==Category==
==Category==
Line 12: Line 13:


==Brand Names==
==Brand Names==
EXACIN, ISEPACIN, ISEPACINE, ISEPALLINE
 
EXACIN<sup>®</sup>, ISEPACIN<sup>®</sup>, ISEPACINE<sup>®</sup>, ISEPALLINE<sup>®</sup> (not currently available in the U.S.)


==Prescribing Information==
==Prescribing Information==


''' [[XXXXX description|Description]]'''
====Clinical Pharmacology====
'''| [[XXXXX clinical pharmacology|Clinical Pharmacology]]'''
 
'''| [[XXXXX microbiology|Microbiology]]'''
General pharmacological properties of isepamicin sulfate (HAPA-B), a new aminoglycoside antibiotic, were studied in animals and the results obtained were summarized below. Intramuscular injections of HAPA-B at doses of 500 mg/kg inhibited the writing response induced by acetic acid, and at doses of 1,000 mg/kg, caused muscle relaxation, respiratory depression, suppression of spontaneous motor activity and prolongation of thiopental anesthesia. Anticonvulsive action and the effect on the rectal temperature were not observed.
'''| [[XXXXX indications and usage|Indications and Usage]]'''
 
'''| [[XXXXX contraindications|Contraindications]]'''
Intravenous Intravenous HAPA-B showed no significant effect on the general behavior and the function of the central nervous system at doses of 100 mg/kg. Intravenous injections of HAPA-B to anesthetized dogs resulted increases in the femoral arterial blood flow at doses of 12.5 mg/kg, decrease in the blood pressure and increase in the respiratory rate at doses of 25 mg/kg, and increase in the carotid arterial blood flow at doses of 50 mg/kg. Apparent changes were not recognized in the heart rate and electrocardiograms. In conscious rabbits, intravenous HAPA-B produced increases in the heart rate without significant changes of the blood pressure and electrocardiograms at doses of 100 mg/kg. Spontaneous beatings of isolated atria were depressed by HAPA-B in concentrations of 3 X 10(-4) to 10(-3) g/ml. The HAPA-B inhibited the gastric secretion at intramuscular doses of 500 mg/kg or intravenous doses of 100 mg/kg, and depressed charcoal transport through small intestine and the spontaneous movement of isolated ileum at intramuscular doses of 1,000 mg/kg and at concentrations of 3 X 10(-4) to 10(-3) g/ml, respectively. No irritative effect was found on the gastric mucous membrane. Intravenous HAPA-B inhibited the response of nictitating membrane to pre and post ganglionic stimulations of cervical sympathetic nerve at doses of 100 mg/kg. In in vitro test, HAPA-B inhibited nonspecifically the constrictive responses of trachea, aorta, stomach, ileum and vas deferens to various agonists in concentrations of 3 X 10(-4) to 10(-3) g/ml. Spontaneous movements of uteri of estrous or pregnant animals were depressed by HAPA-B at intravenous doses of 50 to 100 mg/kg and in in vitro at concentrations of 10(-4) to 3 X 10(-4) g/ml. Antidiuretic effect was also observed at intramuscular doses of 250 mg/kg. HAPA-B increased the length of the whole blood clotting time and raised the plasma glucose level at intramuscular doses of 1,000 mg/kg and inhibited the platelet aggregation induced by ADP in vitro at concentrations of 10(-3) g/ml.<ref name="www.tecolandcorp.com">{{Cite web  | last =  | first =  | title = http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | url = http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | publisher =  | date = | accessdate = }}</ref>
'''| [[XXXXX warnings and precautions|Warnings and Precautions]]'''
 
'''| [[XXXXX adverse reactions|Adverse Reactions]]'''
====Chemical Structure====
'''| [[XXXXX drug interactions|Drug Interactions]]'''
 
'''| [[XXXXX overdosage|Overdosage]]'''
{|
'''| [[XXXXX clinical studies|Clinical Studies]]'''
| [[File:Isepamycin01.jpg|400px|thumb]]
'''| [[XXXXX dosage and administration|Dosage and Administration]]'''
|}
'''| [[XXXXX how supplied|How Supplied]]'''
 
'''| [[XXXXX labels and packages|Labels and Packages]]'''
Molecular Formula: C<sub>22</sub>H<sub>45</sub>N<sub>5</sub>O<sub>16</sub>S<ref name="www.tecolandcorp.com">{{Cite web  | last =  | first =  | title =http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | url = http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | publisher =  | date =  |accessdate = }}</ref>
 
====Reported Use====
 
Treatment of susceptible bacterial infections<ref name="www.tecolandcorp.com">{{Cite web  | last =  | first =  | title =http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | url = http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | publisher =  | date =  |accessdate = }}</ref>
 
====Dosage====
 
* '''Adults''': I.M., I.V.: 8-15 mg/kg daily in 2 divided doses; maximum: 1.5 g/day<ref name="www.tecolandcorp.com">{{Cite web  | last =  | first =  | title =http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | url = http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | publisher =  | date =  |accessdate = }}</ref>
 
====Dosage Forms====
 
Injection, solution: 250 mg/mL (1 mL, 2 mL)<ref name="www.tecolandcorp.com">{{Cite web  | last =  | first =  | title =http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | url = http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm | publisher =  | date =  |accessdate = }}</ref>


==Mechanism of Action==
==Mechanism of Action==
Isepamicin is an aminoglycoside which inhibits bacterial [[protein synthesis]] by binding to [[30S]] and [[50S]] [[ribosomal]] subunits in susceptible micro-organisms.


==References==
==References==

Latest revision as of 17:42, 8 January 2014

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Synonyms and keywords: Isepamycin

Overview

Isepamicin is an aminoglycoside antibiotic. It has been used in the treatment of skin, upper respiratory tract, lower respiratory tract, and urinary tract infections caused by Gram-negative bacteria (including Pseudomonas aeruginosa, Proteobacteria, and Escherichia coli).

Category

Aminoglycoside

Brand Names

EXACIN®, ISEPACIN®, ISEPACINE®, ISEPALLINE® (not currently available in the U.S.)

Prescribing Information

Clinical Pharmacology

General pharmacological properties of isepamicin sulfate (HAPA-B), a new aminoglycoside antibiotic, were studied in animals and the results obtained were summarized below. Intramuscular injections of HAPA-B at doses of 500 mg/kg inhibited the writing response induced by acetic acid, and at doses of 1,000 mg/kg, caused muscle relaxation, respiratory depression, suppression of spontaneous motor activity and prolongation of thiopental anesthesia. Anticonvulsive action and the effect on the rectal temperature were not observed.

Intravenous Intravenous HAPA-B showed no significant effect on the general behavior and the function of the central nervous system at doses of 100 mg/kg. Intravenous injections of HAPA-B to anesthetized dogs resulted increases in the femoral arterial blood flow at doses of 12.5 mg/kg, decrease in the blood pressure and increase in the respiratory rate at doses of 25 mg/kg, and increase in the carotid arterial blood flow at doses of 50 mg/kg. Apparent changes were not recognized in the heart rate and electrocardiograms. In conscious rabbits, intravenous HAPA-B produced increases in the heart rate without significant changes of the blood pressure and electrocardiograms at doses of 100 mg/kg. Spontaneous beatings of isolated atria were depressed by HAPA-B in concentrations of 3 X 10(-4) to 10(-3) g/ml. The HAPA-B inhibited the gastric secretion at intramuscular doses of 500 mg/kg or intravenous doses of 100 mg/kg, and depressed charcoal transport through small intestine and the spontaneous movement of isolated ileum at intramuscular doses of 1,000 mg/kg and at concentrations of 3 X 10(-4) to 10(-3) g/ml, respectively. No irritative effect was found on the gastric mucous membrane. Intravenous HAPA-B inhibited the response of nictitating membrane to pre and post ganglionic stimulations of cervical sympathetic nerve at doses of 100 mg/kg. In in vitro test, HAPA-B inhibited nonspecifically the constrictive responses of trachea, aorta, stomach, ileum and vas deferens to various agonists in concentrations of 3 X 10(-4) to 10(-3) g/ml. Spontaneous movements of uteri of estrous or pregnant animals were depressed by HAPA-B at intravenous doses of 50 to 100 mg/kg and in in vitro at concentrations of 10(-4) to 3 X 10(-4) g/ml. Antidiuretic effect was also observed at intramuscular doses of 250 mg/kg. HAPA-B increased the length of the whole blood clotting time and raised the plasma glucose level at intramuscular doses of 1,000 mg/kg and inhibited the platelet aggregation induced by ADP in vitro at concentrations of 10(-3) g/ml.[1]

Chemical Structure

Molecular Formula: C22H45N5O16S[1]

Reported Use

Treatment of susceptible bacterial infections[1]

Dosage

  • Adults: I.M., I.V.: 8-15 mg/kg daily in 2 divided doses; maximum: 1.5 g/day[1]

Dosage Forms

Injection, solution: 250 mg/mL (1 mL, 2 mL)[1]

Mechanism of Action

Isepamicin is an aminoglycoside which inhibits bacterial protein synthesis by binding to 30S and 50S ribosomal subunits in susceptible micro-organisms.

References

  1. 1.0 1.1 1.2 1.3 1.4 "http://www.tecolandcorp.com/Product-Group-I/Isepamycin%20sulfate.htm". External link in |title= (help)

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