Anti Bacterials *-too toxic for systemic use, just for mcqs/short answers etc.

Drug Type
Cell Wall Inhibs

Drug Name
Penicilins

Trade names

Uses
Strep, STIs, skin, boils, UTIs, influenza

Mechanism of Action
block crosslinking, bactericidal by blocking transpeptidases, loss of rigidity. same as above.

Pharmacokinetics
usually oral with food. cross BBB. Renal excretion, 80% in Tubules. Widely distributed. Exreted unchanged. 3rd generation cross BBB. Ideal for renal failure patients.

S/Es
Hypersensitivity in 10%, pain, GI disturbances

Resistance Issues
beta-lactamases, cleaves the beta lactam ring.

Cell Wall Inhibs

Cephalosporins

Cefadroxil Cefaclor

used in those allergic to penicillins. not effective against entercocci/mrsa 1st-e.coli,klebsiella. 2nde.coli,klebsiella, proteus. 3rd-n.menig, salmonella. gram negative-e.coli, Klebsiella, influenza, P.aeruginosa, enterobacter. broad spectrum, gram pos,+neg. Often given in hosp.

hypersensitivity 2-5%. Alcohol intolerance. Bleeding disorders. Can be nephotoxic when given with diuretics.

Cephalosporinases.

Cell wall Inhibs

Aztreonam

Azactam Cayston

same as above

parenteral administration.

Rash, GI disturbances

Highy lresistant to betalactamases.

Cell Wall inhibs

Carbapenems

Primaxin Invanz Azactam

same as above

IV, metabolised by dihydropeptidase nausea, GI, rashes, seizures in the kidney. Usually given with cysplatin. This stops nephrotoxic metabolites. Cross BBB. IV admin, not absorbed in GIT. Ototoxic with permanent auditory damage, nephrotoxic.

does not work with MRSA.

Cell Wall inhibs

Vancomycin

Vancocin

MRSA, gram pos.

Binds to growing peptidoglycan to prevent further growth and crosslinking, increased cell lysis. Disrupts cell membranes

reluctance to use, only in very serious cases for fear of resistance developing.

Cell membrance inhibs Tyrocidins*

gram pos.

used in creams, eye drops etc.

Extremely toxic in systems, Used as a topical treatment. Too toxic for systemic use. Neurotoxic/nephtoptosic. can have tetarogenic effects. Nephrotoxic, ototoxic-vertigo. Paralysis at high doses. GIT irritation, Vit B deficiency Bone deformity in neonates. Liver damage in pregnant women. Causes bone marrow suppression Pancytopenia/aplastic anaemia. GIT disturbance, rash, fever, jaundice resistance due to mutation at binding site. Growing resistance

Cell membrane inhibs Polymixins*

Polymyxin

gram neg. (LPS)

bind to LPS, disrupt membrane

topical, not absorbed in GIT.

Cell membrance inhibs Azoles* Protein Synth. Inhibs

Clotrimazole

gram pos. Anti fungals E.coli/sepsis, TB, used with Penicillin often, gram neg.

affects enzymes? interact with 30S ribosome unit which freezes the initation complex.

Topical IV/IM. Excreted in kidneys.

Aminoglycosides Gentamicin

Protein Synth Inhibs

Tetracyclines

Declemycin Vibramycin Minocycin

gram pos./neg., in the immune- binds to 30S unit, inhibiting protein compromised (HIV). synthesis.

oral/IV, wide distribution. excreted in bile and kidneys. liver metabolism (renal failure ok). topically, for conjuntivits.

resistance is common

Protein Synth Inhibs

Chloramphenicol loads

gram pos./neg.

binds to 50S unit,block peptidyltranferase, inhibit transcription. binds to 50S unit, inhibits translocation.

Protein Synth Inhibs

Macrolides

Erythromycin Tylosin

gram pos./some gram neg.

Nucleic Acid inhibs

Metronidazole

Flagyl (Pfizer)

used for oral infections, gram positive.

same as Azoles?

Oral drug, well absorbed. renal exrection, mainly unchanged.

Nausea, vomiting, rash, headache NO ALCOHOL,inhibits alcohol dehydrogendase.

resistance increasing due to prolific use in dentistry.

Nucleic Acid inhibs

Fluoroquinolones Ciprofloxacin

UTIs, Chlamydia N. gonorrhoeae. Anthrax ulcerative colitis

inhibit DNA gyrase, stop supercooling oral/IV, wide distribution in gram neg. also inhibits topoisomerase IV CYP450 metabolism. in gram pos. PABA, binds to dihydropteroate Synthetase, inhibits growth. competes with folates for enzyme dihydrofolate reductase, inhibit growth oral/IV/IM, crosses BBB Liver metabolism, kidney excretion

nausea, vomiting, GI pain, rash, staph resistance. Fever, inhibits theophylline causing Increased CV and breathing problems. nausea, vomiting, diarrhoea, headache, hepatitis, hypersensitivity, myelosuppression

Anti-Metabolites

Sulphonamides

Sulphonomide

Anti-Metabolites

Trimethropin

Proloprim

UTIs, resp tract infections Pneumocystis carinii (AIDS)

oral, well absorbed. Excreted in kidneys. Nausea, vomiting, rashes, folate deficiency.