Tetracyclines, Chloramphenicol, Aminoglycosides

rings.
Tetracyclines enter susceptible organisms via passive diffusion and also

by an energy-dependent transport.
The drugs bind reversibly to the 30S subunit of the bacterial ribosome. This action prevents binding of tRNA to the mRNA–ribosome complex, thereby inhibiting bacterial protein synthesis.
Type of action – bacteriostatic.

bacterium acnes, B. anthracis, V. cholerae, Yersinia, Campylobacter, Helicobacter pylori,

Brucella, Pasteurella multocida, Spirochetes (T. pallidum and Borrelia), F. tularensis, all rickettsiae (typhus, etc.), chlamydiae, Mycoplasma and Actinomyces. Protozoa (Entamoeba histolytica and Plasmodia) are inhibited at high concentrations.

fungi, Pseudomonas aeruginosa, Proteus, mycobacteria.
Tetracyclines are absorbed after oral ingestion.

They are concentrated well in the bile, liver, kidney, gingival fluid, and skin but do not pass BBB.
Tetracycline is primarily eliminated unchanged in the urine, doxycycline is primarily eliminated via the bile into the feces.

diseases (chlamydial nonspecific urethritis/endocervicitis); syphilis; gonorrhoea;
atypical pneumonia;
cholera; amoebiasis;

GIT infections;
brucellosis; plague; relapsing fever, leptospirosis; rickettsial infections (typhus); tetanus, anthrax, actinomycosis and listeria infections;
Conjunctivitis, acne vulgaris.

hypoplasia of teeth in children,
hepatotoxicity,
phototoxicity,
dysbiosis,
superinfection,
hypersensitivity (skin rashes,

urticaria, glossitis, pruritus ani and vulvae)

women or in children less than 8 years of age.

inhibits protein synthesis at the peptidyl transferase reaction.

and N. meningitidis, salmonella including S. typhi, B. pertussis, klebsiella,

anaerobes including Bact. Fragilis, rickettsiae, spirochetes, and anaerobes).
The drug is primarily bacteriostatic, but depending on the dose and organism, it may be bactericidal.
It is ineffective against Mycobacteria, Pseudomonas, many Proteus, viruses and fungi.

concentrations in the CSF.
It primarily undergoes hepatic metabolism to

an inactive glucuronide, which is secreted by the renal tubule and eliminated in the urine.

and others (wound infections, intraabdominal infections, pelvic abscess, and brain

abscess;
Intraocular infections;
Skin infections.

anaemia;
Dose and duration of therapy related myelosuppression.
Gray baby syndrome (hypotonia,

hypothermia, abdomen distended, irregular respiration, gray cyanosis of skin, cardiovascular collapse);
Hypersensitivity reactions (rashes, fever, angioedema);
Irritative effects (nausea, vomiting, diarrhoea);
Superinfections

two or more aminosugars.
1 gen.: Streptomycin, Kanamycin, Neomycin (Topical

aminoglycoside)
2 gen.: Gentamycin
3 gen: Amikacin, Sisomycin, Tobramycin
4 gen.:Netilmycin

organisms. These organisms also have an oxygen-dependent system that transports

the drug across the cytoplasmic membrane.
Inside the cell, they bind the 30S ribosomal subunit, where they interfere with ribosomal apparatus and cause the 30S subunit of the completed ribosome to misread the genetic code.
They also increase the permeability of the cytoplasmic membrane.
Type of action – bactericidal.

Enterobacter;
Cocci.
The causative agents of tularemia, plague, brucellosis.
Mycobacterium tuberculosis (streptomycin, kanamycin,

amikacin).
2 and 3 generations act on Pseudomonas aeruginosa.
Do not act on anaerobes, chlamydia, rickettsia, spirochetes, viruses, fungi, protozoa

only extracellularly. Relatively higher concentrations are present in endolymph and

renal cortex, which are responsible for ototoxicity and nephrotoxicity. Penetration in respiratory secretions is poor. Concentrations in CSF and aqueous humour are nontherapeutic even in the presence of inflammation.
Aminoglycosides are not metabolized in the body, and are excreted unchanged in urine

Septicaemias;
Pseudomonas, Proteus or Klebsiella infections: burns, urinary tract infection,

pneumonia;
lung abscesses, middle ear infection

pneumococcus, chlamydia, anaerobes.
It passes in bones, poorly through the BBB.
It

is used per os, IV, IM, locally (gel, vaginal cream).
Indications: diseases of ENT organs, bones, teeth, joints, abdominal organs, sepsis, peritonitis.
Side effects: pseudomembranous colitis, dysbacteriosis, allergy, hepatotoxicity, leukopenia

bacteria, including methicillin-resistant staphylococci.
Indications: severe staphylococcal and streptococcal infections (septicemia,

pneumonia, abscesses of brain or lungs, meningitis, peritonitis, osteomyelitis, endocarditis).
It is used IV or orally for pseudo membranous colitis (not absorbed from the gastrointestinal tract).
Side effects: phlebitis, hearing disorders, allergy, nephrotoxicity, rash, neutropenia.

cellular components and cell death.
Spectrum: P. aeruginosa, E. coli, K.

pneumoniae, Acinetobacter species, Enterobacter species, Proteus and Serratia.
Polymyxin B is available in otic, ophthalmic and topical preparations.

sodium, which is administered IV or inhaled via a nebulizer.
Adverse

effects: nephrotoxicity and neurotoxicity (for example, slurred speech, muscle weakness) when used systemically.
Uses: salvage therapy for patients with multidrug-resistant infections.

as low toxicity; are used routinely:
Isoniazid, Ethambutol, Pyrazinamide, Rifampin, Streptomycin;
Second

line: These drugs have either low antitubercular efficacy or higher toxicity or both; and are used as reserve drugs:
Ethionamide, Prothionamide, Cycloserine, Fluoroquinolones (Ofloxacin, Levofloxacin, Moxifloxacin, Ciprofloxacin), Kanamycin, Amikacin, Rifabutin, Para-aminosalicylic acid

most active drugs.
Combination of 2-3 drugs.
Long-term therapy for 6-8-12 months.

permeability of the cell membranes, facilitates the penetration of chemotherapeutic

substances into the Mycobacterium.
It disrupts the tissue respiration.
It acts bactericidal.
It is used orally, IV, into the cavities.
It is well absorbed, penetrates into all tissues, through BBB, into caseous foci, into cells. Isoniazid is acetylated slowly when it is combined with paraaminosalicylic acid

neuritis), euphoria, insomnia, psychosis, convulsions, epilepsy attacks, liver dysfunction. Development

of resistance.
Apply Vit. B1 and B6 for the prevention of neuritis .

M. leprae and many other gram-positive and gram-negative bacteria like

Staph. aureus, N. meningitidis, H.influenzae, E. coli, Klebsiella, Pseudomonas, Proteus and Legionella.
Rifampin interrupts RNA synthesis by binding to β subunit of mycobacterial DNA-dependent RNA polymerase.

the body: penetrates intracellularly, enters tubercular cavities, caseous masses and

placenta, passes BBB. It is metabolized in liver to an active metabolite which is excreted in bile, in urine.
Adverse effects:
Hepatitis;
Cutaneous syndrome (flushing, pruritus, rash, redness and watering of eyes);
Flu syndrome (chills, fever, headache, bone pains);
Abdominal syndrome (nausea, vomiting, abdominal cramps, diarrhoea);
Urine and secretions may become orangered.

violates the synthesis of the cell wall of M.
Resistance

to E develops slowly.
About 3/4 of an oral dose of E is absorbed. It is distributed widely, but penetrates meninges incompletely and is temporarily stored in RBCs.
Adverse effects: loss of visual acuity/colour vision, field defects due to optic neuritis; nausea, rashes, fever, rarely peripheral neuritis, hyperuricemia.

mycolic acid synthesis.
Type of action – weakly tuberculocidal.
Tolerance of

bacteria develops rapidly if it is used alone.
It penetrates through the BBB, into the caseous foci.
Adverse effects: dyspepsia, allergic reactions, arthralgia, gout exacerbation, liver dysfunction.

Jaypee Brothers Medical Publishers. The Health Sciences Publisher. -New Delhi.

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