BPS 2103

REPORT PHARMACEUTICAL
CHEMISTRY II

NAME : NURFATIHA NABILA BINTI KHAIRUL

AZMAN
MATRIC ID : 2061201001
COHORT :BPS 15
 SULPHADIZINE

Sulfadiazine is a sulfonamide with a relatively limited period of action. It is easily drained

from the Gastrointestinal tract and quickly excreted by the kidney. Because of the broad
variety of safer and more powerful alternative antibiotics, there are few clear warnings for
this sulfonamide, as there are for other sulfonamides. Furthermore, the advent of
sulfonamide resistance has made this drug class unsuitable for the treatment of many
infections that previously referred to them. Short-acting bacteriostatic sulfadiazine is a
synthetic pyrimidinyl sulfonamide analogue. By competing with para amino benzoic acid,
sulfadiazine prevents bacterial folic acid synthesis. It also used to treat toxoplasmosis in
adults with acquired immunodeficiency syndrome and newborns with congenital infections
when combined with pyrimethamine.

(Sulphadizine structure )

Mechanism of action Sulphadizine

Sulfadiazine is a dihydropteroate synthetase inhibitor that competes with other antibiotics.
This enzyme is required for the proper processing of PABA (para-aminobenzoic acid), which
is required for the synthesis of folic acid. In these species, the inhibited reaction is needed for
folic acid synthesis.

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Medical uses of Sulphadizine
In medical , Suplhadizine uses to eliminates bacteria that cause infections by stopping the
production of folate inside the bacterial cell. Other than that , Sulfadiazine is mainly used to
treat urinary tract infections and as an adjunct therapy for a few parasitic diseases. Although
sulfadiazine, like other sulfonamides, is generally well tolerated, its use has been linked to
side effects. One of the most common side effects of sulfadiazine is hypersensitivity reactions
and gastrointestinal upset. In combination, sulfadiazine and pyrimethamine can be used to
treat toxoplasmosis, the disease caused by Toxoplasma gondii. Toxoplasma gondii is a
protozoan parasite that infects most species of warm-blooded animals, including humans, and
causes the disease toxoplasmosis.

Toxoplasma gondii life cycle

Common side effect of Sulphadizine

The common of side effect Sulphadizine is nausea, vomiting, diarrhea, stomach pain, loss
of appetite. Other than that ,headache, and ringing in your ears. After that dizziness, spinning
sensation, loss of balance or coordination. Then ,numbness, tingling, or burning pain in your
hands or feet sleep problems (insomnia); or depressed mood. Make sure call your doctor for
medical advice about side effects.

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 METRONIDAZOLE

Metronidazole (flagyl) is a synthetic antiprotozoal and antibacterial agent,( l-β-

hydroxyethyl)-2-methyl-5-nitroimidazole, which has the following structural formula.
Metronidazole is an antibiotic and antiprotozoal drug sold under the trade names Flagyl and
others. It's used to treat pelvic inflammatory disease, endocarditis, and bacterial vaginosis,
either alone or in combination with other antibiotics. Dracunculiasis, giardiasis,
trichomoniasis, and amebiasis are all treated with it. If vancomycin or fidaxomicin aren't
available, it's an alternative for a first episode of mild-to-moderate Clostridium difficile
colitis. Metronidazole may be taken by mouth, used as a cream, or injected into a vein.

Mechanism Of Action Of Metronidazole

Metronidazole belongs to the nitroimidazole family of drugs. It prevents nucleic acid

synthesis by producing nitroso radicals, which disrupt microbial DNA. This mechanism is
only activated when metronidazole is partly reduced, and since this reduction typically occurs
only in anaerobic bacteria and protozoans, it has no effect on human cells or aerobic bacteria.

Medical Uses Of Metronidazole

Metronidazole is mainly used to treat the following conditions: bacterial vaginosis,
pelvic inflammatory disease (along with other antibacterials such as ceftriaxone),
pseudomembranous colitis, aspiration pneumonia, rosacea (topical), fungating wounds
(topical), intra-abdominal infections, lung abscess, periodontitis, amoebiasis, oral infections,
giardiasis , trichomoniasis, and infections caused by susceptible anaerobic organisms such as
Bacteroides, Fusobacterium, Clostridium, Peptostreptococcus, and Prevotella species. It is
also often used to eradicate Helicobacter pylori along with other drugs and to prevent
infection in people recovering from surgery.

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 Metronidazole and clindamycin are popular antibiotics used to treat bacterial
vaginosis. In nonpregnant patients, the medication of choice for bacterial vaginosis is
metronidazole oral twice daily for seven days, metronidazole gel intravaginally once daily for
five days, or clindamycin intravaginally at bedtime for seven days. Also , the 5-
nitroimidazole antibiotics (metronidazole and tinidazole) are the mainstay in therapy for
Trichomonas vaginalis infection. Treatment is prescribed for both the affected patient and the
patient's intimate companion, particularly though the patient is asymptomatic. Other than 5-
nitroimidazole medications, other therapies are available, but cure rates are much lower.
Then, oral metronidazole is a treatment choice for giardiasis; however, the rising prevalence
of nitroimidazole resistance is the the use of other compound groups. After that ,
Metronidazole, vancomycin, or fidaxomicin are used as first-line antibiotics for less serious
Clostridioides difficile infection colitis (pseudomembranous colitis). The IDSA proposed
vancomycin and fidaxomicin over metronidazole in 2017. Vancomycin used orally has been
found to be more effective in treating acute C. difficile colitis. Other than that ,
Metronidazole has since been used in women to avoid preterm delivery caused by bacterial
vaginosis, as well as other risk factors such as the involvement of cervicovaginal foetal
fibronectin (fFN). Metronidazole was unsuccessful in avoiding preterm delivery in high-risk
pregnant women (selected based on history and a positive fFN test), and the rate of preterm
delivery was shown to be higher in metronidazole-treated women.

Drug Interaction Of Metronidazole

The table shows of the drug interaction of Metronidazole. Since metronidazole has a similar
effect to disulfiram, it can cause nausea and vomiting if you drink alcohol while on it. It
enhances the anticoagulant activity of anticoagulants of the coumarin class. Cimetidine
decreases plasma clearance, while phenytoin and phenobarbitone can increase drug removal.

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Side Effect of Metronidazole
Side effect of Metronidazole is epigastric distress ,seisures ,metallic taste and darkening of
urine. Other than that ,peripheral neuropathy ,pancreatitis ,hepatitis and fever. Make sure
please call your doctor for medical advice about side effect.