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Pharmacology > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

What are the protein synthesis inhibitors

A

Acts on 30s ribosomal subunit = Aminoglycosides, Tetracycline
Acts on 50s ribosomal subunit = Chloramphenicol , Macrolides, Clindamycin , Linezolide

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2
Q

What are the macrolides?

A

Azithromycin
Erythromycin
Clarithromycin
Roxithromycin

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3
Q

Tetracycline

A

Tetracycline
Doxycycline
Minocycline

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4
Q

Aminogylocsides

A

Acc to route of administration
A)Oral = Neomycin , Kanamycin
B)Parenteral = Gentamicin Amikacin , Streptomycin

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5
Q

Why are they called macrolides? Give criteria of macrolides

A

They are called macrolides because they contain macrocyclic large lactone ring
Criteria = they contain macrocyclic large lactone ring
They are broad spectrum antibiotic
They are bacteriostatic
They act by protein synthesis inhibition

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6
Q

M/A of macrolides

A

Azithromycin ==> binds with 50s subunit of ribosome ==> (-) translocation ==>(-) protein synthesis ==> inhibition of bacterial growth

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7
Q

Clinical use of Azithromycin

A

Acute bacterial exacerbations of chronic obstructive pulmonary disorder
Acute bacterial sinusitis
Community acquired pneumonia
Pharyngitis
Tonsillitis
Sinusitis
Uncomplicated skin and skin structure infection
Toxoplasmosis
Granuloma inguinale
Diarrhoea
Pertussis
Urthetitis cervicitis
Typhoid
Gonorrhoea
Acne vulgaris

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8
Q

A/E of Azithromycin

A

Nausea
Abdominal pain
Diarrhoea , constipation
Rash , photosensitivity
Fever
Headache
Dizziness

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9
Q

Compare Azithromycin and erythromycin

A

Azithromycin. Erythromycin
Macrolides. Macrolides
Protein synthesis inhibitor. Psi
Bacteriostatic. Bacteriostatic
Rapid absorption. Slow absorption
Long duration of action. Short
Once daily dose. 4 times daily
Large volume of distribution. Low volume of distribution
Mostly effective in enteric fever , toxoplasmosis. Mostly effective in whooping cough , diphtheria

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10
Q

Indication of clindamycin

A

Infection of skin and soft tissue
Intra-abdominal sepsis
Infection of the respiratory tract
Dental infection
Infection of genital tract
Infection of bones and joints
Cardiovascular infection (endocarditis )
Anaerobic septicaemia
Osteomyelitis and septic arthritis
Acne vulgaris

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11
Q

A/E of clindamycin

A

Nausea
Vomitting
Abdominal pain Diarrhoea
Diarrhoea
Pseudomembranous colitis
Rash
Hepatotoxicity
Urticaria

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12
Q

Why called aminoglycosides

A

They are called aminoglycosides because they contain hexose ring with amino sugar side chain by glycosidic linkages

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13
Q

Common properties of aminoglycosides

A

Irreversible inhibitors of protein synthesis
Chemically composed of a hexose ring to which various amino sugars are attached by glycosidic linkage
They are water soluble , highly polar and stable in solution
More active in alkaline pH
Must be given parenterally to achieve adequate serum concentration
They can cross placental barrier but cannot pass the blood brain barrier
They are excreted unchanged in urine
Narrow therapeutic index
They accumulate in the renal cortex and endolymph and perilymph of the inner ear and causing nephrotoxicity and ototoxicity
Don’t reach to pharmacological sanctuary = CNS , prostrate , testes , joint cavity and ovary

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14
Q

M/ A of aminoglycosides

A

Gentamicin / Amikacin ==> Enter into bacteria ( through outer membrane by passive diffusion and across cell membrane into cytoplasm by active transport )===> binds with 30s subunit of microsomal ribosome ==> inhibition of bacterial protein synthesis ===> bacteriocidal action

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15
Q

M/ A of aminoglycosides

A

Gentamicin / Amikacin ==> Enter into bacteria ( through outer membrane by passive diffusion and across cell membrane into cytoplasm by active transport )===> binds with 30s subunit of microsomal ribosome ==> inhibition of bacterial protein synthesis ===> bacteriocidal action

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16
Q

Clinical uses of gentamycin

A

Pneumonia
Lung abscess
Abdominal and pelvic abscess
Bacterial endocarditis
Septiciemia
Plague / brucellosis
Conjunctival and ear infection ( tropical use )
Preoperative bowl preparation ( orally )
Tropical uses : ear eye skin burn and wound infection

17
Q

Clinical uses of streptomycin

A

Pneumonia
Lung abscess
Abdominal and pelvic abscess
Bacterial endocarditis
Septicemia
TB/ plaque / brucellosis

18
Q

A/E of streptomycin

A

Nephrotoxicity
Ototoxicity ( tinnitus , vertigo , dizziness )
Hypersensitivity
Chance of drug interactions

19
Q

Contraindications of aminoglycosides

A

Nephropathy
Neuropathy
Pregnancy
Respiratory failure

20
Q

Tetracycline is

A

Protein synthesis inhibitor (30s)

Broad spectrum
Bacteriostatic

21
Q

Classification of tetracycline

A

ACC TO SOURCE
NATURAL ==>chlortetracycline , oxytetracycline , tetracycline , demeclocyline
SEMISYNTHETIC ==> Doxycycline , Minocycline

ACC TO DURATION OF ACTION
SHORT ACTING ==> chlortetracycline , oxytetracycline , tetracycline

Intermediate acting => demecloclyine

Long acting ==> Doxycycline , Minocycline

22
Q

Clinical indications of tetracycline

A

1) Rickettsial infection => Rocky Mountain spotted fever , Q fever
2) Mycoplasma pneumonia
3)Cholera
4) Chlamydial infection ( lymphogranuloma venerum , PID, Trachoma)
5)Brucellosis
6) acne
7) Malaria
8) UTI
9) CAP

23
Q

A/E of tetracycline

A

Discolouration of skin
Growth deformity
Hepatotoxicity
Nephrotoxicity
Photosensitivity
Dizziness
Vertigo
Headache
Vaginal candiasis

24
Q

Contraindications of tetracycline

A

Pregnancy and lactation
Children less than 8 years
Renal failure
SLE
Any hypersensitivity reaction

25
Q

M/A of tetracycline

A

Tetracycline ===> enter into bacteria ( through outer membrane by passive diffusion and across cell membrane into cytoplasm by active transport ) ==> binds with 30s subunit of microsomal ribosome ==> inhibition of bacterial protein synthesis ===> bacteriocidal action

26
Q

Advantage of long acting tetracycline

A

More bioavailability
Chronic use of
Less dose frequency
More patients compliance

27
Q

Compare tetracycline and doxycycline

A

TETRACYCLINE DOZYCYCLINE
Natural. Semisynthetic
Low potent. High potent
T1/2 = 6=10 hrs. 18-24 hrs
Dosage schedule = 4 times daily. 2 times daily
Renal excretion. Faecal excretion
Can’t use in renal failure. Can
Low plasma binding drug High
Low photosensitivity. High photosensitivity

28
Q

Chloramphenicol

A

PSI 50S
Broad spectrum
Bacteriostatic
Bacteriocidal for Hinfluenxa , N meningitis

29
Q

Clinical uses of chloramphenicol

A

Bacterial conjunctivitis ( mostly use as an eye drop / ointment

30
Q

A/E of chloramphenicol

A

Superinfection
Bone marrow depression
Gray baby syndrome in neonates
Hypersensitivity reaction

31
Q

Contraindications of chloramphenicol

A

Neonates
Pregnancy
Lactating mother
Liver disease
Bleeding disorder

32
Q

Why chloramphenicol is not used first choice in enteric fever

A

Resistant to Salmonella Typhi
Bacteriostatic in nature
Relapse occur (10%)
Doesn’t cure carrier state
Short plasma half life so more dose needed
More toxic ( due to large dose/ so chance of bone marrow depression , aplastic anemia , typhoid shock syndrome )
Regular blood ( reticulocyte ) count needed for detecting BMD

Pharmacology (19 decks)

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