Anti Folate Drugs Flashcards

1
Q

3 classes of anti folate drugs

A

Sulphonamides
Trimathoprim
Contrimoxazole

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2
Q

Absorption of Sulphonamides

A

Completely absorbed except Sulphosalazine…

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3
Q

Adv. Of poor absorption of Sulphosalazine.

A

It can be used for inflammatory bowel and ulcerative colitis diseases..

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4
Q

Sulphosalazine splits into and their effects

A

Sulpha pyridine, — poor abs. Accumulation – toxic effects
5 amino salicylate — anti inflammatory effect

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5
Q

Sulphonamides used in burn infections

A

Sulphadiazine Mafenide…

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6
Q

Distribution of sulphonamides

A

BBB, CSF, BREAST MILK,
ACETYLATED BY liver and precipitate at acidic PH… Can cause stone formation…….

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7
Q

MOA of sulphonamides
Enzyme used for conversion…

A

Dihydropteroate synthetase

PABA - Dihydro folic acid - Tetra hydro folic acid ..

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8
Q

2 Drugs in Co-trimoxazole…

A

Sulphamethaxazole and Trimathoprim…

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9
Q

Why sulphonamides don’t effect humans

A

PABA isn’t a precursor of folic…

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10
Q

Spectrum of Sulphonamides

A

Entero bacteria in UTI infections and Nocardial infections

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11
Q

Treatment of toxoplasmosis

A

Sulphadiazine with pyrimethamine

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12
Q

Resistance of sulphonamides

A

Altered pathway, Alteration in target site and decreased uptake

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13
Q

4 ADRs of Sulphonamides

A

Crystalluria
Hypersensitivity Reactions
Hemolytic disorders
Kernicterus

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14
Q

What is crystalluria

A

Nephrotoxicity

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15
Q

Kernicterus

A

Displacement of Bilirubin

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16
Q

Pharmacokinetics of Trimathoprim

A

Well absorbed in body fluids acidic vaginal, cross BBB, 60-70% of drug is eliminated without change

17
Q

MOA of Trimathoprim

A

Inhibition of formation of tetrahydrofolic acid ..

18
Q

Spectrum of Trimathoprim

A

Bacteriostatic
UTI
prostatitis

19
Q

Resistance of Trimathoprim

A

Decrease permeability
Increase efflux
Alternative pathway..

20
Q

Most common ADRs of Trimathoprim

A

Megaloblastic anemia
Leukopenia and hemolytic disorders

21
Q

Contrimoxazole is combination of

A

Sulphamethaxazole and Trimathoprim
So greater anti bacterial activity

22
Q

MOA Co-trimoxazole

A

Conversation of PABA into terta hydrofolic acid..

23
Q

Spectrum of Co-trimoxazole

A

UTI, Respiratory tract infections, ampicillin and chloramphenicol resistance salmonella
Skin and soft tissue infections

24
Q

Treatment of listeriosis

A

Septicemia and meningitis caused by listeria

25
Q

Major ADRs of Co trimoxazole

A

Prolongation of thrombin time, thrombocytopenia