Antibiotics

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*Penicillin*


#Formulations : tablet, Injection

#Brand_Names : BENZYL PENICILLIN 0.5, 1 MU INJ
PROCAINE PENICILLIN G 0.5,  1 MU DRY POWDER IN VIAL
FORTIFIED P.P. INJ 3+1 LAC U VIAL
BISTREPEN 6+4 LAC U/VIAL
PENIDURE-LA
LONGACILLIN, 0.6, 1.2, 2.4 MU AS DRY POWDER IN VIAL



#Pharmacological_Action : It is a narrow spectrum Antibiotic activity is limited primarily to gram positive bacteria few gram negative ones and anaerobes. Many bacteria are inherently insensitive to PnG because in them the target enzymes and PBPs are located deeper under lipoprotein barrier where PnG is unable to penetrate or have low affinity for PnG.  The primary mechanism of acquired resistance is production of penicillinase.
#Side_Effects : Local irritancy and direct toxicity, Hypersensitivity, Superinfections, Jarisch- Herxheimer reaction


#Therapeutic_Uses : used as antibiotics

*Amoxicillin*

#Formulations : Tablet, injection

#Dose : AMOXYLIN, NOVAMOX, SYNAMOX 250, 500MG CAP, 125 MG/5 ML DRY SYR. AMOXIL, MOX 250, 500 MG CAPS; 125 MG/5 ML DRY SYR; 250, 500 MG/VIAL INJ.   MOXYLONG: AMOXICILLIN 250MG + PROBENECID 500 MG TAB 

#Pharmacological_Action : It is a close congener of ampicillin similar to it in all aspects except:

• Oral absorption is better; food doesn't interfere with absorption higher and more sustained blood levels are produced. 

• Amoxicillin given 3 times a day is equivalent to ampicillin given 4 times a day. 

• Incidence of diarrhoea is lower. 

• It is less active against Shigella and H. influenzae. 

• It is more active against relatively penicillin resistant Strep. Pneumoniae. 

#Dose : 0.25-1 g TDS oral/i.m.; or slow i.v. injection, child 25-75mg/kg/day

#Therapeutic_Uses : used as Antibiotics

*Cloxacillin* 

#Formulations : Capsule, Injection.  

#Brand_Name: Ampiclox, Cloxin,Cloxa-A ,Bioclox ,Klox, Amclo 

#Pharmacological_Action : It has an isoxazolyl side chain and is highly penicillinase as well as acid resistant. Actively against PnG sensitive organism is weaker, and it should not be used as a substitute of PnG for any other infection. Activity against penicillinase producing Staph, is greater than that of methicillin, but not against MRSA. It is incompletely but dependably absorbed from oral route, especially if taken in empty stomach. It is >90% plasma protein bound. Elimination occurs primarily by kidney, also partly by liver. Plasma t½ is about 1 hour.

#Dose : 0.25-0.5 g orally every 6 hours ; for severe infection it may be injected i.m. or i.v. high bp are produced. 

#Therapeutic_Uses : used as Antibiotics

*Doxycycline*

₹Not for children and pregnant women

₹Never used alone always given in combination with quinone for treatment of CQ resistant malaria.


#Formulations :
Doxycycline Hydrochloride capsule IP
Doxycycline dispersible tablets IP
Doxycycline syrup.


#Brand_Names : Novadox, Tetradox, Monodox, Adoxa, Doxypal, Doxycip, Doxt, Peristat.



#Pharmacological_Action : slowly acting and weak erythrocytic schizontocidal action against all plasmodial species including Plasmodium falciparum resistant to CQ, MQ and S/P. The progeny schizonts of doxycycline exposed plasmodia die slowly. However, no clinically useful action is exerted on the pre erythrocytic stage. Gametocytes and vivax hypnozoites are also not killed.


#Therapeutic_Uses :
Acne, UTI, Intestinal infection, respiratory infection, Eye infection, periodontitis, gonococcal urethritis, in malaria.

*MINOCYCLIN*

#Formulations : 

MINOCYCLIN TABLET BP

MINOCYCLIN CAPSULES BP

MINOCYCLIN PROLONGED RELEASE CAPSULE BP

#Brand_Names : Arestin, Minocin, Dynacin, Amzeeq, Solodyn, Ximino

#Pharmacological_Action : It acts on both gram positive and gram negative bacteria.  Because of high lipophilicity this tetracycline penetrates into M.leprae and is active against them. A dose of 100mg/day produces peak blood levels that exceed MIC against M.leprae by 10-20 times. Antileprotic activity of minocyclin is less marked than that of rifampin, but greater than that of clarithromycin. In one trial monotherapy with minocyclin 100mg daily rendered all 8 patients of lepromatous leprosy negative for M.leprae after 8 weeks. A good clinical response in terms of releif of lepromatous  symptoms has also been reported. 

#Side_Effects : Vertigo due to long use

#Therapeutic_Uses : used as Antibiotics.

*Streptomycin*

#Formulations : 

Streptomycin tablet IP

Streptomycin injection IP

#Brand_Names : streptomac, AMBISTRYN-S, Chlorostrep, Enterostrop, Lykastrep, Cipstryn. 

#Pharmacological_Action : It is the first aminoglycosidic antibiotic obtained from Streptomyces griseus which was used extensively in the past, but is now practically restricted to treatment of tuberculosis. It is less potent (MICs are higher) than many other aminoglycosides.  The antimicrobial spectrum of streptomycin is relatively narrow primarily covers aerobic gram negative bacilli. Sensitive organisms are Haemophilus ducreyi, Brucella, Yersinia, pestis, Francisella tularensis, Nocardia, Calym granulomatis ,Malignant tuberculosis only few strains of Escherichia coli, Haemophilus influenzae, Vibrio cholerae, Shigella, Klebsiella, enterococci and some gram positive cocci are now inhibited that too at higher concentrations. All other organisms including Pseudomonas are unaffected.  

#Side_Effects : vestibular disturbances, auditory disturbances, neurotoxicity, rashes fever and exfoliative dermatitis 

#Therapeutic_Uses : tuberculosis, pneumoniae, influenzae, plague, mycobacterium avium complex, Endocarditis, Brucellosis, tubercular meningitis, cholecystitis and peritonitis

*ERYTHROMYCIN*

#Formulations : 

ERYTHROMYCIN TABLET

ERYTHROMYCIN INJECTION

ERYTHROMYCIN SOLUBLE POWDER

ERYTHROMYCIN ESTOLATE CAPSULE BP

ERYTHROMYCIN STEARATE TABLET BP, IP

#Brand_Names : Erythrocin , Althrocin, Erycin, Erysert, Acnederm, Acnelak. 

#Pharmacological_Action : Bacteriostatic at low concentrations but cidal at high concentration. Cidal action depends on the organism concerned and its rate of multiplication. Sensitive gram positive bacteria accumulate erythromycin intercellularly by active transport which is responsible for their high susceptibility to this antibiotic. Activity is enhanced several fold in alkaline medium because nonionized form of the drug is favoured at higher pH. It acts by inhibiting bacterial proteins synthesis. It works with translocation principle. 

#Side_Effects : Rashes, fever, GI, hearing impairment

#Dose : 250-500 mg 6 hourly 

Children; 30-60mg/kg/day

#Therapeutic_Uses : used as Antibiotics

*CHLORAMPHENICOL*

#Formulations : 

CHLORAMPHENICOL CAPSULE

CHLORAMPHENICOL EAR DROPS

CHLORAMPHENICOL EYE OINTMENT

CHLORAMPHENICOL INJECTION

CHLORAMPHENICOL PALMITATE SUSPENSION

#Brand_Names : Chloromycetin, Enteromycin, Fenicol, O- mycin

#Pharmacological_Action : It inhibits bacterial proteins synthesis by interfering with the transfer of the elongating peptide chain to the newly attached aminoacetyl - tRNA at the ribosome mRNA complex. It specifically attached to the 50S ribosome near the acceptor site and prevents peptide bond formation between the newly attached aminoacid and nascent peptide chain without interfering with the aminoacetyl tRNA attachment to the 30S ribosome. At high doses it can inhibit mammalian mitochondrial protein synthesis as well. Bone marrow cells are easily susceptible. 

#Side_Effects : bone marrow depression, hypersensitivity, gray baby syndrome, nausea, vomiting, diarrhoea

#Dose : oral :. 250- 500 mg 6 hourly (max. 100mg/kg/day)

#Therapeutic_Uses : used as Antibiotics