Classification of cephalosporins

These are chemically and in their mode of action similar to penicillin.

These are classified according to the generations:

First generation cephalosporins:
a. Cefacetrile,
b. Cefadroxil (R. E. Buck et al.) (Oral),
c. Cefalexin, (Oral)
d. Cefaloglycin,
e. Cefalonium,
f. Cefaloridine, (Parenteral)
g. Cefalothin, (Parenteral)
h. Cefapirin, (Parenteral)
i. Cefatrizine,
j. Cefazedone,
k. Cefazaflur,
l. Cefazolin, (Parenteral)
m. Cefradine, (Oral)
n. Cefroxadine,
o. Ceftezole

Second generation cephalosporins:
a. Cefaclor, (Oral)
b. Cefamandole, (Parenteral)
c. Cefmetazole, (Parenteral)
d. Cefminox,
e. Cefonicid, (Parenteral)
f. Ceforanide, (Parenteral)
g. Cefoxitin, (Parenteral)
h. Cefotiam,
i. Cefotetan, (Parenteral)
j. Cefprozil, (Parenteral)
k. Cefbuperazone,
l. Cefuroxime, (Parenteral)
m. Cefuzonam,
n. Loracarbef (Parenteral)

Third generation cephalosporins:
a. Cefcapene,
b. Cefdaloxime,
c. Cefdinir,
d. Cefditoren,
e. Cefetamet,
f. Cefixime, (Parenteral)
g. Cefmenoxime,
h. Cefodizime,
i. Cefoperazone, (Parenteral)
j. Cefotaxime, (Parenteral)
k. Cefpimizole,
l. Cefpiramide,
m. Cefpodoxime,
n. Cefsulodin,
o. Ceftazidime, (Parenteral)
p. Cefteram,
q. Ceftibuten,
r. Ceftiolene,
s. Ceftizoxime, (Parenteral)
t. Ceftriaxone, (Parenteral)
u. Flomoxef,
v. Latamoxef,
w. Moxalactam (Parenteral)

Fourth generation cephalosporins:
a. Cefepime,
b. Cefozopran,
c. Cefpirome,
d. Cefquinome

Fifth generation cephalosporins:
a. Ceftobiprole (Tatiana Bogdanovich et al.) (Andreas F. Widmer)
b. Ceftaroline (S Crofskey)

References:
Andreas F. Widmer, Division of Infectious Diseases and Hospital Epidemiology, University Hospital Basel, Switzerland. http://www.sld.cu/galerias/pdf/sitios/apua-cuba/v4-ceftobiprole._a_new_option_for_treatment_of_skin_and_soft-tissue_infections.pdf

R. E. Buck, K. E. Price. Cefadroxil, a new broad-spectrum cephalosporin. Infection (Journal), Volume 8, Supplement - 5, September, 1980, Pages S532-S537.

S. Crofskey. Ceftaroline a strong competitor in cSSSI. Inpharma weekly, October 14, 2006, Issue 1559, 7-8.

Tatiana Bogdanovich, Lois M. Ednie, Stuart Shapiro, Peter C. Appelbaum. Antistaphylococcal Activity of Ceftobiprole, a New Broad-Spectrum Cephalosporin. Antimicrobial agents and chemotherapy, October 2005, Volume 49, Number 10, Pages 4210-4219.

Further Reading:
The Goodman and Gilman Manual of Pharmacology and Therapeutics by Laurence Brunton, Donald blumenthal, Iain buxton and Keith Parker

AHFS Drug Information 2008 (Ahfs Drug Information) by American Society of Health-system

Lippincott's Illustrated Reviews: Pharmacology, 4th Edition (Lippincott's Illustrated Reviews Series) by Richard A. Harvey, Pamela C. Champe, Richard Finkel, Luigi Cubeddu and Michelle A. Clarke

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Classification of Macrolides

Macrolides include:

a. Azithromycin (J. Retsema et al.)
b. Clarithromycin (K. B. Waites et al.)
c. Erythromycin
d. Dirithromycin
e. Roxithromycin
f. Leucascandrolide A (Michele D. Ambrosio et al.)
g. Josamycin (T. Bergan et al.)
h. Kitasamycin
i. Midecamicine/midecamicine acetate
j. Oleandomycin
k. Spiramycin
l. Troleandomycin
m. Tylosin/tylocine
n. Carbomycin A
o. Miocamycin
p. Rokitamycin
q. Flurithromycin
r. Leucascandrolide B.
s. Maridomycin (Setsuo Harada et al.)
t. Kejanimicin (Rolf Hirsenkorn et al.)
u. Tetrocarcin (Rolf Hirsenkorn et al.)
v. Chlorothricin (Rolf Hirsenkorn et al.)

Ketolides:
a. Telithromycin
b. Cethromycin
c. Spiramycin
d. Ansamycin
e. Oleandomycin
f. Carbomycin
g. Tylocine

Structurally unrelated Macrolide:
a. Lincosamides
i. Clindamycin
ii. Lincomycin

b. Streptogrammins
i. Pristinamycin
ii. Quinopristin/dalfopristin

c. Sorangicin A

References:
J Retsema, A Girard, W Schelkly, M Manousos, M Anderson, G Bright, R Borovoy, L Brennan and R Mason. Spectrum and mode of action of azithromycin (CP-62,993), a new 15-membered-ring macrolide with improved potency against gram-negative organisms. Antimicrobial agents and chemotherapy. 1987 December; 31(12): Pages 1939-1947.

K. B. Waites, G H Cassell, K C Canupp and P B Fernandes. In vitro susceptibilities of mycoplasmas and ureaplasmas to new macrolides and aryl-fluoroquinolones. Antimicrobial agents and chemotherapy. 1988 October; 32(10): Pages 1500-1502.


Michele D'Ambrosio, Antonio Guerrieroa, Cécile Debitusb and Francesco Pietraa.
Leucascandrolide A, a New Type of Macrolide:the First Powerfully Bioactive Metabolite of Calcareous Sponges (Leucascandua caveolata, a New Genus from the Coral Sea). Separatum HELVETICA CHIMICA ACTA - Vol. 79 (1996)

Rolf Hirsenkorn, Richard R. Schmidt. Functionally substituted vinyl carbanions, 42. Synthesis of the top half of chlorothricolide. Liebigs Annalen der Chemie, Volume 1990 Issue 9, Pages 883 - 899.

Setsuo Harada, Masayuki Muroi, Masahiro Kondo, Kanji Tsuchiya, Tai Matsuzawa, Takeshi Fugono, Toyokazu Kishi and Jisaburo Ueyanagi. Chemical Modification of Maridomycin, a New Macrolide Antibiotic. Antimicrobial agents and chemotherapy. 1973 August; 4(2): Pages 140-148.

T. Bergan, B. Øydvin. Pharmacokinetics of Josamycin - A New Macrolide Antibiotic. International Journal of Experimental and clinical pharmacology, Volume 7, Number 1, 1972.

Further Reading:
The Goodman and Gilman Manual of Pharmacology and Therapeutics by Laurence Brunton, Donald blumenthal, Iain buxton and Keith Parker

AHFS Drug Information 2008 (Ahfs Drug Information) by American Society of Health-system

Lippincott's Illustrated Reviews: Pharmacology, 4th Edition (Lippincott's Illustrated Reviews Series) by Richard A. Harvey, Pamela C. Champe, Richard Finkel, Luigi Cubeddu and Michelle A. Clarke

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Arbekacin

(M. Kurebe et al.) Chemical name of Arbekacin is "1-N[(S)-4-amino-2-hydroxybutyl]-3',4'-dideoxykanamycin B".(Yusuke Tanigawara et al.) It is a derivative of "Dibekacin". (M. Inoue et al.)Arbekacin works good against methicillin resistant staphylococcus aureus (MRSA), which are even resistant to other types of good aminoglycosides. (M. Kurebe et al.)It is less toxic to ear than amikacin and dabekacin.

Dosage and administration:
(Yusuke Tanigawara et al.) Its usual dose for adults is 150-200 mg/day. It is administered IV or IM in divided doses.

Pharmacokinetics:

Elimination:
(Yusuke Tanigawara et al.) It is eliminated in the urine.

References:
M. Inoue, M. Nonoyama , R. Okamoto, T. Ida. Antimicrobial activity of arbekacin, a new aminoglycoside antibiotic, against methicillin-resistant Staphylococcus aureus. Drugs under experimental and clinical research, 1994, volume 20, number 6, pages 233-239.

M. Kurebe, M. Yokota, T. Niizato, F. Kai, T. Yoshida, R. Okamoto, S. Mitsuhashi. Antibacterial activity and ototoxicity in guinea pigs, and nephrotoxicity in rats of arbekacin. Arzneimittelforschung. 1986 Oct; Volume 36(10): Pages 1511-7.

Yusuke Tanigawara, Reiko Sato, Kunihiko Morita, Mitsuo Kaku, Naoki Aikawa, and Kihachiro Shimizu. Population Pharmacokinetics of Arbekacin in Patients Infected with Methicillin-Resistant Staphylococcus aureus. Antimicrobial Agents Chemotherapy. 2006 November; volume 50(11): Pages 3754–3762.

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Classification of Aminoglycosides

Aminoglycosides include:
1. Those that are derived from the genus of bacteria namely "Streptomyces". These aminoglycoside antibiotics end with "-mycin" and include:
a. Streptomycin ·
b. Neomycinc.
c. Kanamycin
d. Hygromycin B ·
e. Spectinomycin.

2. Those that are derived from the genus of bacteria namely "Micromonospora". These aminoglycoside antibiotics end with "-micin" and include:
a. Gentamicin
b. Verdamicin

3. Those that are derived from these antibiotics:
a. Arbekacin(1)
b. Framycetin
c. Amikacin
d. Paromomycin
e. Ribostamycin
f. Dibekacin
g. Tobramycin
h. Netilmicin
i. Sisomicin
j. Isepamicin(2)
k. Habekacin (N. Tanaka et al.)

Further reading:
Aminoglycoside Antibiotics: From Chemical Biology to Drug Discovery by Dey P. Arya.

References:
(1) Arti Kapil, Rashi Bali, B. K. Das, In vitro susceptibility of nosocomial isolates against a new aminoglycoside isepamicin. Indian Journal of Medical Research, Feb 2001.

(2) M. Inoue, M. Nonoyama , R. Okamoto, T. Ida. Antimicrobial activity of arbekacin, a new aminoglycoside antibiotic, against methicillin-resistant Staphylococcus aureus. Drugs under experimental and clinical research, 1994, volume 20, number 6, pages 233-239.

N. Tanaka, K. Matsunaga, A. Hirata, Y. Matsuhisa and T. Nishimura. Mechanism of action of habekacin, a novel amino acid-containing aminoglycoside antibiotic. Antimicrob Agents Chemother. 1983 November; 24(5): Pages 797–802.

Further Reading:
The Goodman and Gilman Manual of Pharmacology and Therapeutics by Laurence Brunton, Donald blumenthal, Iain buxton and Keith Parker

AHFS Drug Information 2008 (Ahfs Drug Information) by American Society of Health-system

Lippincott's Illustrated Reviews: Pharmacology, 4th Edition (Lippincott's Illustrated Reviews Series) by Richard A. Harvey, Pamela C. Champe, Richard Finkel, Luigi Cubeddu and Michelle A. Clarke

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Strychnine

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Cocaine

Cocaine is natural alkaloid and obtaine from Coca leaves. It is used topically as local anesthetic.

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Warfarin

Warfarin is an oral anti-coagulant.

P. Peterson et al. had found that anticoagulation therapy with warfarin to prevent thromboembolic complications is effective.
References:
Petersen P, Boysen G, Godtfredsen J, Andersen ED, Andersen B. Placebo-controlled, randomised trial of warfarin and aspirin for prevention of thromboembolic complications in chronic atrial fibrillation. The Copenhagen AFASAK study. Lancet. 1989 Jan 28;1(8631):Pages 175-9.

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