CLINDAMYCIN Brand names Dosage forms Mechanism of action Clindamycin may prolong the effects of neuromuscular-blocking drugs, such

as succinylcholine and vecuronium. Its similarity to the mechanism of action of macrolides and chloramphenicol means they should not be given simultaneously, as this causes antagonism and possible cross-resistance. indictaions It is usually used to treat infections with anaerobic bacteria but can also be used to treat some protozoal diseases, such as malaria. It is a common topical treatment for acne and can be useful against some methicillinresistant Staphylococcus aureus (MRSA) infections.

Cleocin, Dalacin C , Cleocin Pediatric, Cleocin Phosphate Cleocin T, Cleocin Vaginal Ovules, Clinda-Derm Clindagel, ClindaMax, Clindets, Acne-aid
Anerocin, Clindal, Inprosyn-HP, Klindex,.

Oral Parenteral topical dermatologic solution for acne vaginal preparation

FLUCONAZOLE Brand name Diflucan Trican Dyzolor Exomax Fleozol Flucandia Flucol Fluzocan Fukole Flucaz Funzela Odaft Syscan Zoleshot Dosage form Tablet IV suspension Mechanism of action
Like other imidazoleand triazole-class antifungals, fluconazole inhibits the fungal cytochrome P450 enzyme 14-demethylase. Mammalian demethylase activity is much less sensitive to fluconazole than fungal demethylase. This inhibition prevents the conversion of lanosterol to ergosterol, an essential component of the fungal cytoplasmic membrane, and subsequent accumulation of 14-methyl sterols. Fluconazole is primarily fungistatic; however, it may be fungicidal against certain organisms in a dose-dependent manner, specifically Cryptococcus. It is interesting to note, when fluconazole was in development at Pfizer, it was decided early in the process to avoid producing any chiral centers in the drug so subsequent synthesis and purification would not encounter difficulties with enantiomer separation and associated variations in biological effect. A number of related compounds were found to be extremely potent teratogens, and were subsequently discarded.

indication Used in the treatment and prevention of superficial and systemic fungal infections. In a bulk powder form, it appears as a white crystalline powder, and it is very slightly soluble in water and soluble in alcohol.

ACYCLOVIR Brand names Aciherpin Biraxin Ciclox Clover Cloviron Covelay Cyclostad Hapivir Herpex Klozivex Virest Zealor Zolteran Zovirax Dosage forms Tablets Topical cream IV inj. Opthalmic ointment Mechanism of action
Acyclovir differs from previous nucleoside analogues in containing only a partial nucleoside structure: the sugar ring is replaced with an open-chain structure. It is selectively converted into acyclo-guanosine monophosphate (acyclo-GMP) by viral thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase. Subsequently, the monophosphate form is further phosphorylated into the active triphosphate form, acyclo-guanosine triphosphate (acyclo-GTP), by cellular kinases. Acyclo-GTP has approximately 100 times greater affinity for viral than cellular polymerase. As a substrate, acycloGTP is incorporated into viral DNA, resulting in premature chain termination. Although acyclovir resembles a nucleotide, it has no 3' end. Therefore, after its incorporation into a growing DNA strand, no further nucleotides can be added to this strand. It has also been shown that viral enzymes cannot remove acycloGTP from the chain, which results in inhibition of further activity of DNA polymerase. Acyclo-GTP is fairly rapidly metabolised within the cell, possibly by cellular phosphatases. In sum, aciclovir can be considered a prodrug: it is administered in an inactive (or less active) form and is metabolised into a more active species after administration.

indication

It is primarily used for the treatment of herpes simplex virus infections, as well as in the treatment of varicella zoster (chickenpox) and herpes zoster (shingles).

METRONIDAZOLE Brand names Aldazole Altozol Ameryl Amizol Dosage form Tablet IV inj. Mechanism of action
Metronidazole, taken up by diffusion, is selectively absorbed by anaerobic bacteria and sensitive protozoa. Once taken up by anaerobes, it is non-enzymatically reduced

Indication Used particularly for anaerobic bacteria and protozoa. Metronidazole is an

Anerobizol Bacimes Biogyl Clovizole Dazomet Flacel Flagyl Flagystatin Flamibazid Foramebex Medgyl Metrinox Metroxid Neopenotran Nortene Nozol Panazole Patryl Protozole Rodazid Servizol Trichomar Tricomycin Tridel Winthrop Zol

by reacting with reduced ferredoxin, which is generated by pyruvate oxido-reductase. Many of the reduced nitroso intermediates will form sulfinamides and thioether linkages with cysteine-bearing enzymes, thereby deactivating these critical enzymes. As many as 150 separate enzymes are affected. In addition or alternatively, the metronidazole metabolites are taken up into bacterial DNA, and form unstable molecules. This function only occurs when metronidazole is partially reduced, and because this reduction usually happens only in anaerobic cells, it has relatively little effect upon human cells or aerobic bacteria.

antibiotic, amebicide, and antiprotozoal. It is the drug of choice for first episodes of mildto-moderate Clostridium difficile infection.

DIGOXIN Brand names

Cardioxin Lanox Lanoxin Metildigoxin

Dosage forms
Tablet IV inj. Drops

Mechanism of action
The mechanism of action is not completely understood; however the current hypothesis is outlined below. Digoxin binds to a site on the extracellular + + aspect of the -subunit of the Na /K ATPase pump in the membranes of heart cells (myocytes) and decreases its function. This causes an increase in the level of sodium ions in the myocytes, which leads to a rise in the level of intracellular calcium ions. This occurs because the sodium/calcium exchanger on the plasma membrane depends on a constant inward sodium gradient to pump out calcium. Digoxin decreases sodium concentration gradient and the subsequent calcium outflow, thus raising the calcium concentration in

Indication
Used in the treatment of various heart conditions, namely atrial fibrillation, atrial flutter and sometimes heart failure that cannot be controlled by other medication.

myocardiocytes and pacemaker cells. Increased intracellular calcium lengthens Phase 4 and Phase 0 of the cardiac action potential, which leads to a decrease in heart [16] 2+ rate. Increased amounts of Ca also leads to increased storage of calcium in the sarcoplasmic reticulum, causing a corresponding increase in the release of calcium during each action potential. This leads to increased contractility, the force of contraction, of the heart. There is also evidence that digoxin increases vagal activity, thereby decreasing heart rate by slowing depolarization of pacemaker cells in [17] the AV node. This negative chronotropic effect would therefore be synergistic with the direct effect on cardiac pacemaker cells. Digoxin is used widely in the treatment of various arrhythmias.