Antimicrobial Library
v1.0 (alpha)
This library contains extensive information on antimicrobial drugs and is aimed at researching selection of drugs or drug combination, based on target protein or known interactions with human metabolism.
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Class | Drug | Mechanism/Target | Human Metabolic Interactions & Off-Target Effects | PBPs (cell wall synthesis) | β-(1,3)-D-glucan synthase | Lanosterol 14alpha-demethylase | Squalene epoxidase | Ergosterol binding/pore | 16S ribosomal subunit | 30S ribosomal subunit | 50S ribosomal subunit | DNA gyrase | Topoisomerase IV | RNA polymerase | Elongation factor G | 70S initiation complex | ATP synthase (myco) | β-tubulin | Glutamate-gated Cl- channel | DHFR | DHPS | PFOR | Mycolic-acid synthesis | Nitro / radical DNA damage | Membrane disruption | Heme detoxification block | Cytochrome bc1 | Nicotinic ACh receptor | FAS1 | Other | |||||
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1 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Benzimidazoles (Antiparasitic) | Albendazole | Binds to parasite β-tubulin, preventing microtubule polymerization; impairs glucose uptake and ATP production (vermicide). Broad anthelmintic (nematodes, cestodes) activity. | Prodrug rapidly hepatic metabolized to albendazole sulfoxide (active). CYP1A2 inducer with chronic use; metabolism inhibited by cimetidine (↑levels) and induced by phenytoin (↓levels). Take with fatty meal to enhance absorption. Off-target liver toxicity (monitor LFTs) and bone marrow suppression with prolonged high doses. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
2 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Aminoglycosides | Amikacin | 30S ribosome binding; resistant to many aminoglycoside-inactivating enzymes (for gentamicin-resistant bacteria). | Similar to gentamicin: renal elimination, significant oto- and nephrotoxicity risk. No CYP metabolism. Therapeutic drug monitoring required to avoid toxicity. | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
3 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Amoxicillin | Inhibits PBPs; broad-spectrum penicillin active vs Gram+ and some Gram- (bactericidal) | Oral absorption enhanced by food; renal excretion. Combined with clavulanate to overcome β-lactamases. Rash common in EBV infection. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
4 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Amoxicillin/Clavulanate | Amoxicillin inhibits PBPs; clavulanate irreversibly inhibits class A β-lactamases, extending spectrum. | Same as amoxicillin; clavulanate hepatically metabolised. Higher incidence of cholestatic hepatotoxicity. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
5 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Polyenes | Amphotericin B | Binds ergosterol in fungal membranes, forming pores and causing cell leakage (fungicidal). Broad spectrum: nearly all fungi (yeasts and molds). Also leishmanicidal (binds parasite ergosterol analogs). | IV only (deoxycholate or lipid formulations). No CYP metabolism. High affinity for cholesterol contributes to dose-limiting nephrotoxicity (off-target). Infusion reactions (fever, chills) common - cytokine release. Liposomal form reduces toxicity. | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
6 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Ampicillin | Same as penicillins - inhibits PBPs and cell wall cross-linking (especially Gram-positive and some Gram-negative). | Mostly renal excretion via OAT transporters. Can alter gut flora (diarrhea) and reduce oral contraceptive efficacy (gut flora effect). | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
7 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Echinocandins | Anidulafungin | Inhibits β-glucan synthase. Used for esophageal candidiasis and invasive Candida. | Undergoes slow chemical degradation in plasma (no significant hepatic metabolism). No clinically relevant drug interactions. Generally well tolerated; histamine release with rapid infusion. | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
8 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - Artemisinins | Artemether-Lumefantrine | Artemether (another artemisinin) plus lumefantrine (long-acting partner that inhibits heme detoxification). Combination kills initial parasites rapidly and clears residual parasites. | Artemether induces its metabolism (CYP3A4 inducer). Lumefantrine is metabolized by CYP3A4; absorption increases with food. QT prolongation can occur (lumefantrine effect). Few significant interactions aside from artemisinin induction effects. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 |
9 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - Artemisinins | Artesunate | Prodrug of dihydroartemisinin. Cleavage of endoperoxide bridge produces free radicals in presence of iron, damaging parasite proteins and membranes (rapidly cidal). Active against blood stages of Plasmodium, including falciparum. | Short half-life (~1 hour). Induces CYP2B6 and 3A4 via PXR/CAR activation - can reduce levels of itself and co-administered drugs over time. Generally well-tolerated; transient neutropenia possible. Not used alone (given in combination therapies to prevent resistance). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
10 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - ETC | Atovaquone/Proguanil | Atovaquone: inhibits parasite mitochondrial electron transport at cytochrome bc1 complex (collapses mitochondrial membrane potential). Proguanil: prodrug converted to cycloguanil, a dihydrofolate reductase inhibitor (enhances atovaquone effect). Used together (Malarone) for malaria. | Atovaquone: >99% protein-bound, excreted largely unchanged in feces. Inhibits no major CYPs (but rifampin reduces atovaquone levels ~50% by inducing clearance). Proguanil: metabolized by CYP2C19 to active cycloguanil (poor CYP2C19 metabolizers have reduced efficacy). Generally well tolerated; atovaquone can cause transient LFT elevations; proguanil can cause mouth ulcers/hair loss (rare). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 |
11 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Macrolides | Azithromycin | 50S ribosome binding; blocks bacterial protein elongation (similar to erythromycin). More acid-stable and broader Gram-negative coverage. | Minimal CYP3A4 inhibition (unlike erythro). Very high tissue penetration (long half-life). Off-target QT prolongation but lower risk than erythromycin. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
12 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Aztreonam (monobactam) | Inhibits PBPs of Gram-negative aerobes only (no activity vs Gram-positives). | Renal excretion. Little cross-allergenicity with other β-lactams. Negligible CYP involvement; generally well-tolerated. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
13 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antitubercular Diarylquinoline | Bedaquiline | Inhibits mycobacterial ATP synthase (diarylquinoline, c subunit), depleting energy stores. | CYP3A4 substrate; QT prolongation boxed warning; half‑life >5 months; avoid CYP3A4 inducers; co‑admin with rifampin contraindicated; hepatotoxic. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
14 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antiprotozoal Nitroimidazoles | Benznidazole | Nitroimidazole prodrug for Chagas disease; mechanism similar to nifurtimox - radical formation and DNA damage in T. cruzi. | Hepatic metabolism (CYP1A1 and possibly CYP3A4). Alcohol intolerance (disulfiram-like effect) possible. Off-target: rash, bone marrow suppression, peripheral neuropathy. Often better tolerated than nifurtimox. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
15 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Echinocandins | Caspofungin | Noncompetitively inhibits β-(1,3)-D-glucan synthase, weakening fungal cell wall (fungicidal against Candida). IV only. | Slow hepatic elimination (not via CYP450; degraded by peptide hydrolysis). Minimal drug interactions (does not inhibit P450 significantly). Histamine-like flushing with rapid infusion (off-target). | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
16 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Cefazolin (1st‑gen cephalosporin) | Binds PBPs; excellent Gram+ coverage, limited Gram‑ (e.g., PEcK). | Renal excretion. Used peri‑operatively. Disulfiram reaction rare; minimal CYP effects. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
17 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Cefepime (4th‑gen) | Inhibits PBPs; zwitterion penetrates Gram‑ outer membrane; broad incl. Pseudomonas. | Renal excretion; neurotoxicity (encephalopathy) in renal failure. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
18 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β‑Lactams (Siderophore Cephalosporin) | Cefiderocol | Siderophore cephalosporin; ferric‑iron uptake into Gram‑negative bacteria then PBP binding; stable to all carbapenemases. | Renal excretion unchanged; negligible CYP effects; monitor for Coombs positivity and possible QT prolongation. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
19 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Cefixime (3rd‑gen oral) | Inhibits PBPs; extended Gram‑ including some β‑lactamase producers. | Renal excretion; long half‑life allows once‑daily dosing. Minimal interactions. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
20 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Cefoxitin (2nd‑gen cephamycin) | Inhibits PBPs; active vs anaerobes incl. B. fragilis. | Renal elimination. Weak inducer of chromosomal AmpC in some Gram‑; minimal human CYP. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
21 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Ceftaroline (5th‑gen) | Binds PBP2a in MRSA and PBPs in Gram‑; only β‑lactam active vs MRSA. | Renal excretion; neutropenia with prolonged use; minimal CYP. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
22 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Ceftazidime (3rd‑gen) | Inhibits PBPs; strong activity vs P. aeruginosa. | Renal elimination. Can select for ESBLs; minimal CYP. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
23 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β‑Lactams + β‑lactamase inhibitor | Ceftazidime–Avibactam | 3rd‑gen cephalosporin plus diazabicyclooctane inhibitor of class A, C, some D β‑lactamases (incl. KPC, OXA‑48). | Renally cleared; adjust dose in renal impairment; minimal CYP; headache and C. difficile diarrhoea reported. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
24 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Ceftriaxone (3rd-gen cephalosporin) | Inhibits PBPs; stable against many β-lactamases; strong activity vs. Enterobacteriaceae and Streptococcus. | ~95% plasma protein-bound; biliary excretion (can cause biliary sludging). No significant CYP metabolism. Displaces bilirubin from albumin in neonates (risk of kernicterus - off-target effect). | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
25 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Cefuroxime (2nd‑gen cephalosporin) | Inhibits PBPs; improved Gram‑ coverage incl. H. influenzae, Enterobacter. | Renal excretion; crosses BBB only at high doses. Minimal CYP effects. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
26 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Cephalexin (1st‑gen) | Same as cefazolin; oral formulation. | Renal clearance. Minimal metabolism; can cause GI disturbance and rash. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
27 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Chloramphenicol | Chloramphenicol | Binds 50S ribosomal subunit and inhibits peptidyl transferase, blocking peptide bond formation (bacteriostatic). Broad spectrum (incl. anaerobes). | Glucuronidated in liver (UDP-glucuronyl transferase). In neonates, immature metabolism causes “Gray baby syndrome” (hypotension, cyanosis). Reversible dose-dependent bone marrow suppression; rare idiosyncratic aplastic anemia (off-target). Inhibits CYP2C19 and 3A4 (moderate). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
28 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - Quinoline | Chloroquine | Binds heme in Plasmodium food vacuole, preventing its polymerization to hemozoin; accumulation of free heme is toxic to parasite (blood schizonticide). Effective against P. vivax/ovale and sensitive P. falciparum. | Hepatic metabolism (CYP2C8/3A4). Inhibits P-gp and may raise levels of P-gp substrates. Off-target: retinal deposition (bull’s eye retinopathy) with long-term use; QT prolongation (caution with other QT drugs). In G6PD deficiency, risk of hemolysis. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 |
29 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Fluoroquinolones | Ciprofloxacin | Inhibits DNA gyrase (Gram-negatives) and topoisomerase IV (Gram-positives), blocking DNA replication (bactericidal). Broad Gram-negative activity. | Moderate inhibitor of CYP1A2 - can raise levels of theophylline, tizanidine. Oral absorption significantly reduced by divalent cations (avoid antacids). Off-target effects: QT prolongation, tendinopathy (risk of tendon rupture, especially in elderly). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
30 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Macrolides | Clarithromycin | 50S ribosome inhibitor, similar spectrum to erythromycin (adds H. pylori coverage). | Strong CYP3A4 inhibitor (and CYP2C9) - significant interactions (e.g. increases statin, theophylline levels). Metabolized in liver to active metabolite. Can cause QT prolongation and cholestatic hepatitis. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
31 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Lincosamide | Clindamycin | Binds 50S subunit, blocking peptide translocation (overlaps macrolide binding site; bacteriostatic). Good anaerobic and Gram+ coverage. | Hepatic metabolism (CYP3A4). High risk of C. difficile colitis due to gut flora disruption (off-target). No significant CYP inhibition. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
32 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Ansamycins | Clofazimine | Binds to mycobacterial DNA and interferes with replication; also generates intracellular ROS. Bactericidal against Mycobacterium leprae; used in leprosy. | Extremely long half-life (weeks) due to high lipid accumulation. No significant CYP interactions known. Off-target red-brown discoloration of skin and bodily fluids. GI upset common. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
33 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Polymyxins | Colistin (Polymyxin E) | Cationic lipopeptide binding LPS, disrupting Gram‑negative membranes; prodrug CMS hydrolysed in vivo. | Renal excretion; nephro & neurotoxicity; monitor CrCl; minimal CYP. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 |
34 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Oxazolidinones | Contezolid | 23S rRNA inhibitor similar to linezolid but weaker MAO inhibition; retains activity vs some linezolid‑resistant strains. | Metabolised by FMO5; low serotonin‑syndrome risk; mild transaminase rise; no significant CYP. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
35 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Glycopeptides | Dalbavancin | Lipoglycopeptide binding D‑Ala‑D‑Ala; depolarises membrane. | Extremely long half‑life (~8 days) allows single-dose regimens. No CYP effects. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 |
36 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Others | Dapsone | Competitive inhibitor of dihydropteroate synthase in bacteria and Pneumocystis jirovecii (like a sulfa drug). Bacteriostatic, used in leprosy and as second-line for Pneumocystis pneumonia. | Hepatic acetylation and hydroxylation (CYP2C9, 3A4). Moderate CYP2C9 inhibitor. Notable off-target: causes methemoglobinemia and hemolysis (especially in G6PD deficiency). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
37 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Lipopeptide | Daptomycin | Inserts into Gram-positive bacterial cell membranes, causing depolarization and potassium efflux (rapidly bactericidal). | Inactivated by pulmonary surfactant (ineffective in pneumonia). Muscle toxicity (CPK elevation) is off-target effect - monitor for rhabdomyolysis. Minimal CYP involvement. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 |
38 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Fluoroquinolones | Delafloxacin | Anionic fluoroquinolone inhibiting DNA gyrase and topoisomerase IV; retains activity in acidic infection sites. | 15 % CYP3A4 metabolism; chelation with divalent cations; less QT prolongation; tendinopathy still a risk. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
39 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antitubercular Nitroimidazole | Delamanid | Activated by F420‑nitroreductase; inhibits mycolic acid synthesis. | Albumin & CYP3A4 metabolism; QT prolongation; hypoalbuminemia increases exposure. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
40 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials – Artemisinin Combination | DHA–Piperaquine | Dihydroartemisinin free‑radical damage; piperaquine blocks heme detoxification; synergistic. | Piperaquine CYP3A4 substrate & inhibitor; QT prolongation; DHA glucuronidated; avoid with strong CYP3A4 modulators. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 |
41 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Dicloxacillin | Penicillinase‑resistant penicillin binding PBPs; active vs MSSA. | Hepatic metabolism; induces CYP3A4 mildly. GI upset and allergic reactions similar to other penicillins. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
42 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Diethylcarbamazine | Diethylcarbamazine (DEC) | Exact mechanism not fully understood - thought to sensitize filarial worms to host immune attack and disrupt arachidonic acid metabolism in microfilaria. Used for lymphatic filariasis. | Renal excretion (alkalinizing urine prolongs half-life). No known CYP interactions. Off-target: can cause intense reactions (Mazzotti-type) due to antigen release from dying microfilariae (fever, hypotension). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
43 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Doripenem | Carbapenem with enhanced anti‑Pseudomonas potency. | Renally cleared; similar to meropenem. No significant CYP. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
44 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Tetracyclines | Doxycycline | Binds 30S ribosomal subunit, preventing tRNA binding to the A-site (bacteriostatic). Broad-spectrum against bacteria and some protozoa. | Hepatic metabolism (doxycycline is non-renally eliminated). Strong chelation with Ca²⁺, Fe²⁺ - avoid co-administration with dairy, iron (reduces absorption). Binds developing teeth and bone (off-target; contraindicated in pregnancy & <8yrs). | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
45 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antitrypanosomal (African) | Eflornithine | Irreversible inhibitor of ornithine decarboxylase (prevents polyamine synthesis) - halts cell proliferation in Trypanosoma brucei gambiense. Also used topically to reduce unwanted hair (same target in follicles). | Renal clearance. No major CYP involvement. Bone marrow suppression and GI irritation are main off-target effects. Safer than melarsoprol, but not effective for T. b. rhodesiense. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
46 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Tetracyclines (Fluorocycline) | Eravacycline | Synthetic tetracycline with high 30S affinity; stable to most tetracycline resistance mechanisms. | CYP3A4 substrate; P‑gp interaction; nausea common; no significant QT effect. | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
47 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Ertapenem | Carbapenem binding PBPs; lacks Pseudomonas/Acinetobacter coverage. | High protein binding, once‑daily dosing. Renal excretion. Lower seizure risk. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
48 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Macrolides | Erythromycin | Binds 50S ribosomal subunit, blocking translocation of the peptidyl-tRNA from A to P site (bacteriostatic). Effective against respiratory pathogens, atypicals. | Potent inhibitor of CYP3A4 - elevates levels of drugs like carbamazepine, warfarin. Stimulates motilin receptors (off-target GI cramping). Causes QT prolongation (hERG K⁺ channel blockade). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
49 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Others | Ethambutol | Inhibits arabinosyl transferases (EmbB) blocking arabinogalactan synthesis in mycobacterial cell wall. | Renal excretion; optic neuritis (colour blindness) dose‑related; minimal CYP effects. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
50 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Macrocyclic Antibiotic | Fidaxomicin | Binds sigma‑dependent RNA polymerase subunit, blocking transcription; bactericidal against C. difficile with narrow spectrum. | Minimal systemic absorption; gut hydrolysis to OP‑1118; negligible CYP involvement; nausea common; preserves normal microbiota. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
51 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Azole Antifungals | Fluconazole | Inhibits fungal lanosterol 14α-demethylase (a CYP51A1) - blocks ergosterol synthesis in fungal cell membranes (fungistatic). Spectrum: Candida, Cryptococcus. | Strong inhibitor of CYP2C9 and moderate inhibitor of CYP3A4/2C19 - raises levels of warfarin, phenytoin, sulfonylureas. High oral bioavailability; primarily renal excretion. Off-target: reversible alopecia with long-term use; QT prolongation. | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
52 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimetabolite Antifungal | Flucytosine (5-FC) | Converted by fungal cytosine deaminase to 5-fluorouracil (5-FU), which then inhibits thymidylate synthase (DNA synthesis) and is incorporated into RNA (fungistatic). Active against Cryptococcus and Candida (used with amphotericin B). | Renal excretion of active drug. Narrow therapeutic window - bone marrow suppression (leukopenia, thrombocytopenia) and enterocolitis at high levels (5-FU toxicity, off-target). No direct CYP interactions. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
53 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Others | Fosfomycin | Inhibits MurA (enolpyruvyl transferase), blocking the first committed step of peptidoglycan synthesis (prevents formation of UDP-N-acetylmuramic acid). Bactericidal (especially urinary E. coli, Enterococcus). | Orally absorbed and excreted unchanged in urine (high urinary concentrations). No notable CYP interactions. Well tolerated; occasional headache or diarrhea. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
54 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitrofurans | Furazidin (Furagin) | Mechanism analogous to nitrofurantoin-reactive intermediates disrupt DNA and ribosomal proteins; used for UTIs in Eastern Europe. | Rapid renal excretion of inactive metabolites; dark yellow urine; contraindicated in G6PD deficiency; possible pulmonary hypersensitivity similar to nitrofurantoin. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
55 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitrofurans | Furazolidone | Nitrofuran reduced to radical intermediates that damage DNA; also weak monoamine oxidase inhibitor; active vs. Giardia, H. pylori, Vibrio cholerae. | Systemic absorption; MAO inhibition-hypertensive crisis with tyramine-rich foods; disulfiram-like reaction with alcohol; risk of hemolysis in G6PD deficiency; nausea/vomiting common. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
56 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Steroid Antibiotic | Fusidic Acid | Prevents turnover of elongation factor G on 70S ribosome, halting protein synthesis; strong activity vs staphylococci. | Hepatic metabolism; potent inhibitor of OATP1B1 and CYP3A4—contraindicated with statins (rhabdo risk); high protein binding. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
57 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Aminoglycosides | Gentamicin | Binds 30S ribosomal subunit; inhibits initiation complex and causes mRNA misreading (bactericidal). Oxygen-dependent uptake (ineffective against anaerobes). | Renal excretion; concentration accumulates in renal cortex and inner ear (off-target nephrotoxicity, ototoxicity). Minimal metabolism. Synergistic toxicity with loop diuretics (ear damage). | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
58 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Mitotic Inhibitor Antifungal | Griseofulvin | Binds fungal tubulin, disrupting microtubule function and mitosis (fungistatic). Deposits in keratin precursor cells (hair, skin, nails) to treat dermatophyte infections. | Induces CYP450 (1A2, 2C9, 3A4) - can reduce efficacy of warfarin, oral contraceptives. Best absorbed with fatty meal. Off-target: headache, confusion; teratogenic in animals (avoid in pregnancy). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
59 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - Quinoline | Halofantrine | Similar to mefloquine; disrupts heme detoxification. | CYP3A4 substrate; severe QT prolongation, hence rarely used. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 |
60 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Triterpenoid Antifungal | Ibrexafungerp | Oral β‑1,3‑D‑glucan synthase inhibitor; fungicidal vs Candida incl. azole‑resistant species. | CYP3A4 substrate; moderate P‑gp inhibitor; GI upset; avoid strong CYP3A4 inducers. | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
61 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Imipenem/Cilastatin | Imipenem inhibits PBPs; cilastatin inhibits renal dehydropeptidase‑I preventing drug degradation. | Seizure risk at high doses or renal dysfunction. Broadest β‑lactam spectrum. Minimal CYP. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
62 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β‑Lactams + β‑lactamase inhibitor | Imipenem–Cilastatin–Relebactam | Imipenem (PBP inhibitor) + cilastatin (DHP‑I blocker) + relebactam (class A/C β‑lactamase inhibitor). | Renal excretion; cilastatin prevents nephrotoxic metabolite; no CYP; CNS toxicity at high doses. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
63 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Azole Antifungals | Isavuconazole | Prodrug of isavuconazonium sulfate; inhibits 14α‑demethylase; active vs Mucorales. | Moderate CYP3A4 inhibitor & substrate; shortens QT (unique); avoids cardiotoxic prolongation. | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
64 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Triazole Antifungal | Isavuconazole | Prodrug isavuconazonium; inhibits lanosterol 14‑α‑demethylase; broad spectrum incl. Mucorales. | CYP3A4 substrate & moderate inhibitor; **shortens** QT interval (unique); contraindicated with strong CYP3A4 inducers/inhibitors. | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
65 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Others | Isoniazid | Inhibits mycobacterial mycolic acid synthesis (prodrug activated by KatG catalase-peroxidase in M. tuberculosis). Bactericidal to rapidly dividing TB. | Acetylated in liver (NAT2) - slow acetylators at risk of toxicity. Potent inhibitor of CYP2C19 and CYP3A4. Hepatotoxic (boxed warning) and causes vitamin B6 deficiency - can lead to peripheral neuropathy (off-target, prevent with pyridoxine). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
66 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Azole Antifungals | Itraconazole | Inhibits fungal lanosterol 14α‑demethylase; broad spectrum incl. Histoplasma, Blastomyces. | Strong CYP3A4 inhibitor; requires acidic pH for absorption (avoid PPIs); negative inotrope (contraindicated in heart failure). | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
67 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Avermectins (Macrocyclic lactones) | Ivermectin | Binds glutamate-gated chloride channels in invertebrate nerve/muscle, causing paralysis and death of parasite (nematodes, arthropods). Also potentiates GABAergic signals in parasites. | CYP3A4 substrate - extensively metabolized via hepatic CYP3A4 (and 3A5, 2C9). P-glycoprotein substrate - excluded from CNS; MDR1 mutations (in collies/humans) allow neurotoxicity (off-target CNS depression). Mild inhibitor of CYP2C9/2C19/2D6 (weak). Off-target effects: dizziness, pruritus (from parasite reactions). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
68 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Azole Antifungals | Ketoconazole | Inhibits 14α-demethylase (ergosterol synthesis). First oral azole (largely replaced by newer azoles due to toxicity). | Potent CYP3A4 inhibitor (and substrate) - causes many drug interactions. Inhibits adrenal and testicular steroid synthesis (off-target anti-androgenic effect causing gynecomastia, adrenal insufficiency). Hepatotoxic (boxed warning). | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
69 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Pleuromutilins | Lefamulin | Binds 50S peptidyl transferase centre (domain V 23S rRNA); blocks protein synthesis; active vs MRSA, atypicals. | CYP3A4 substrate & moderate inhibitor; QT prolongation; avoid strong CYP3A4 inducers/antiarrhythmics. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
70 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Fluoroquinolones | Levofloxacin | Inhibits DNA gyrase & topo IV (bactericidal). Enhanced Gram+ (including pneumococcus) compared to ciprofloxacin. | Less CYP inhibition than cipro (minimal). Primarily renal excretion. Prolongs QT interval. Associated with tendon damage and cartilage toxicity (avoid in pregnancy and children). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
71 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Oxazolidinones | Linezolid | Binds 50S ribosomal 23S rRNA, preventing formation of the 70S initiation complex (blocks protein synthesis initiation). Active against MRSA, VRE. | Partially metabolized by MAO; is a non-selective MAO inhibitor - risk of serotonin syndrome with SSRIs (off-target effect). No CYP450 induction/inhibition. Causes bone marrow suppression (especially thrombocytopenia) with prolonged use. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
72 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Benzimidazoles (Antiparasitic) | Mebendazole | Similar to albendazole - inhibits microtubules in parasites (broad-spectrum anthelmintic). | Poorly absorbed (mostly acts in gut). Metabolized by CYP3A4; induces CYP3A4 with repeated dosing. Low systemic exposure means few drug interactions. High doses can cause neutropenia, alopecia (off-target). Contraindicated in pregnancy (teratogenic in animals). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
73 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - Quinoline | Mefloquine | Probably disrupts parasite heme detoxification similar to chloroquine. Active against chloroquine-resistant P. falciparum (blood schizonticide). | Long half-life (~20 days). Metabolized by liver (CYP3A4). Minimal CYP inhibition. Off-target: vivid dreams, insomnia, and risk of severe neuropsychiatric effects (boxed warning). Contraindicated in epilepsy (seizures). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 |
74 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antitrypanosomal (African) | Melarsoprol | Arsenical compound that likely inactivates parasite enzymes (e.g. pyruvate kinase) by binding sulfhydryl groups. Used for late-stage CNS African trypanosomiasis. | Metabolized to an inactive arsenic-glucuronide. Extremely toxic (arsenic effects): causes reactive encephalopathy in ~10% (often fatal), peripheral neuropathy, nephrotoxicity. No known drug interactions (used as last resort). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
75 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Meropenem (carbapenem) | Binds PBPs with broad spectrum (Gram-positives, Gram-negatives, anaerobes). Resistant to most β-lactamases. | Primarily renal elimination (dehydropeptidase-I resistant, unlike imipenem). Lowers seizure threshold at high doses (imipenem > meropenem). Minimal CYP interaction. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
76 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β‑Lactams + β‑lactamase inhibitor | Meropenem–Vaborbactam | Carbapenem combined with cyclic boronate inhibitor targeting serine carbapenemases (KPC). | Renal elimination; no CYP; seizures rare; dose adjust for CrCl < 50 mL/min. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
77 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitroimidazoles | Metronidazole | Prodrug - in anaerobes and certain protozoa it’s reduced to reactive nitro radicals that damage DNA and other macromolecules (bactericidal). Effective against anaerobic bacteria and protozoa (Giardia, Entamoeba, Trichomonas). | Hepatic metabolism (via CYP2A6, 2C9) and renal excretion of metabolites. Inhibits aldehyde dehydrogenase - causes disulfiram-like reaction with alcohol (off-target). Inhibits CYP2C9 - potentiates warfarin (↑INR). Frequent side effects: headache, peripheral neuropathy with prolonged use. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
78 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Echinocandins | Micafungin | Inhibits β-1,3-glucan synthase (like caspofungin). Used for Candida (including prophylaxis in stem-cell transplant patients). | Metabolized by aryl sulfate transferase and COMT, not CYPs - few interactions. Increases levels of sirolimus and nifedipine (via unknown mechanism). Off-target: liver enzyme elevation. | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
79 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Alkylphosphocholine | Miltefosine | Disrupts parasite membrane lipid metabolism; cidal vs Leishmania, Naegleria fowleri. | Oral; long half‑life; teratogenic; GI upset; elevated creatinine; P‑gp substrate. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
80 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Avermectins (Macrocyclic lactones) | Moxidectin | Macrocyclic lactone with similar mechanism to ivermectin (paralyzes via glutamate-Cl⁻ channels). Used for river blindness. | Longer half-life than ivermectin. CYP3A4 metabolism. Inhibits P-gp less than ivermectin. Adverse effects mainly due to immune reaction to dying parasites (Mazotti reaction). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
81 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Fluoroquinolones | Moxifloxacin | Inhibits DNA gyrase & topo IV; stronger Gram+ & anaerobe activity. | Hepatic glucuronidation and sulfation; QT prolongation higher than cipro; no renal adjustment. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
82 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Topical RNA Synthetase Inhibitor | Mupirocin | Inhibits bacterial isoleucyl‑tRNA synthetase; potent vs MRSA when topical. | Minimal systemic absorption; hydrolysed to inactive monic acid; local burning/itching; no CYP concerns. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
83 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Nafcillin | Penicillinase‑resistant anti‑staph penicillin binding PBPs. | Hepatic metabolism, biliary excretion; potent inducer of CYP3A4, lowers warfarin/cyclosporine levels; risk of neutropenia. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
84 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Allylamines | Naftifine | Topical allylamine inhibiting squalene epoxidase. | Minimal systemic absorption; local irritation possible. | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
85 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | First‑Gen Quinolone | Nalidixic Acid | Inhibits DNA gyrase (topoisomerase II) in Gram‑negative bacilli; mainly urinary antiseptic. | Hepatic glucuronidation; inhibits CYP1A2 (↑warfarin, theophylline); phototoxicity and seizures at high concentrations. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
86 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Salicylanilide Anthelmintic | Niclosamide | Uncouples oxidative phosphorylation & inhibits glucose uptake in cestodes; cidal to tapeworms. | Very poor absorption; negligible CYP; mild GI upset; being repurposed for cancer & antiviral studies. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
87 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitrofurans | Nifuratel | Nitrofuran analogue producing reactive nitroso species; broad activity vs. Trichomonas, Candida, Giardia; also inhibits bacterial pyruvate ferredoxin oxidoreductase. | Oral; largely metabolised by hepatic reduction and conjugation; disulfiram-like reaction with ethanol; mild GI upset; limited CYP data-no major interactions reported. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
88 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitrofurans | Nifuroxazide | Nitrofuran acting on bacterial oxidoreductases; poor systemic absorption-stays in gut, inhibiting enteric pathogens. | Negligible systemic exposure; minimal CYP interaction; rare hepatic enzyme elevation in impaired gut barrier; hypersensitivity reactions uncommon. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
89 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antiprotozoal Nitroimidazoles | Nifurtimox | Yields reactive nitro anion radicals inside Trypanosoma cruzi (Chagas disease agent), causing DNA and macromolecule damage. Also used in combination for Trypanosoma brucei (African trypanosomiasis). | Metabolized in liver (multiple pathways, not well characterized). Causes oxidative stress in host cells too - common off-target effects: peripheral neuropathy and GI upset. No specific CYP interactions established, but its clearance may be induced by rifampin (by analogy to similar compounds). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
90 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Others | Nitazoxanide | Prodrug; active metabolite (tizoxanide) inhibits pyruvate:ferredoxin oxidoreductase in anaerobic energy metabolism of protozoa and some bacteria. Cidal against Cryptosporidium and Giardia. | Highly protein-bound, metabolized via glucuronidation. Colors urine yellow-green (off-target). Minimal CYP impact. Generally well tolerated; mild GI side effects. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
91 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitrofurans | Nitrofurantoin | Reduced inside bacteria generating reactive intermediates that damage ribosomal proteins, DNA; specific for urinary pathogens. | Rapid renal excretion; contraindicated in CrCl<30. Causes hemolysis in G6PD deficiency and pulmonary fibrosis with long use. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
92 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitrofurans | Nitrofurazone (Nitrofural) | Reduced by bacterial nitroreductases to reactive intermediates that damage DNA and inhibit ribosomal proteins; topical antibacterial for burns & skin grafts. | Minimal systemic absorption; rare hypersensitivity/contact dermatitis; prolonged topical use may cause systemic nitroso metabolites-avoid in pregnancy; negligible CYP involvement. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
93 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | 8‑Hydroxyquinoline | Nitroxoline | Chelates metal ions and inhibits bacterial DNA replication enzymes; potent anti‑biofilm activity vs Gram‑negatives, mycobacteria and Candida. | Rapid glucuronidation; >90 % excreted in urine (orange discoloration); minimal CYP; avoid in severe renal/hepatic impairment. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
94 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Polyenes | Nystatin | Topical polyene; same mechanism as amphotericin (binds ergosterol, pores). Used for Candida (skin, oral thrush). | Not absorbed orally (safe for GI Candida). No systemic metabolism when used topically. Bitter taste and mild GI upset if swallowed (off-target). | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
95 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Fluoroquinolones | Ofloxacin | Inhibits DNA gyrase/topo IV; racemic mixture (levofloxacin is L‑isomer). | Renal elimination; CNS stimulation risk; moderate CYP1A2 inhibition. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
96 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Orotomide Antifungal | Olorofim | Inhibits fungal dihydroorotate dehydrogenase; novel class active vs molds. | CYP3A4 substrate and mild inducer; reversible LFT rise; investigational use. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
97 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Tetracyclines (Aminomethylcycline) | Omadacycline | 30S ribosome inhibitor evading efflux and ribosomal protection; active vs MRSA, VRE, atypicals. | Not metabolised; chelation with Ca/Fe; avoid food 4 h pre‑dose; minimal CYP; transient ALT rise. | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
98 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Glycopeptides | Oritavancin | Lipoglycopeptide disrupting cell wall and membrane; inhibits transglycosylation & transpeptidation. | Weak inhibitor/inducer of multiple CYPs (2C9, 2C19, 3A). Interferes with coagulation tests (artifacts). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 |
99 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitroimidazoles | Ornidazole | Same as metronidazole; effective against anaerobes & protozoa. | Hepatic metabolism; longer t1/2; similar alcohol reaction. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
100 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Oxacillin (anti-staph penicillin) | Inhibits PBPs; resistant to staphylococcal β-lactamase (narrow spectrum against MSSA). | Hepatic metabolism (unlike most penicillins). Inducer of CYP3A4 (moderate) - can lower levels of drugs like warfarin. High protein binding; may cause hepatitis (off-target liver toxicity). | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
101 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Aminoglycosides | Paromomycin | 30S binding; luminal amebicide and IM option for visceral leishmaniasis. | Minimal absorption orally; IM route renally cleared; nephro/ototoxicity with parenteral use; no CYP. | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
102 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Penicillin G | Binds penicillin-binding proteins (PBPs) - D-Ala-D-Ala transpeptidase - inhibiting peptidoglycan cross-linking (bactericidal). | Primarily renally excreted unchanged; minimal CYP involvement. High doses may provoke seizures (GABA antagonism) in renal impairment. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
103 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Penicillin V | Binds PBPs, inhibits transpeptidase during cell wall synthesis (mainly Streptococcus spp.) | Acid-stable oral penicillin; renal tubular secretion (OAT). Minimal CYP involvement; may reduce efficacy of OCPs by altering gut flora. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
104 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antiprotozoal Diamidines | Pentamidine | Binds DNA in kinetoplasts and likely interferes with polyamine synthesis and topoisomerase in protozoa. Cidal for Trypanosoma brucei (hemolymphatic stage) and Pneumocystis jirovecii (alternate therapy). | IV/IM administration. Extensive tissue binding; eliminated via renal (slow). Hypotension and nephrotoxicity are notable off-target effects. No CYP metabolism. Can cause hypoglycemia (toxic to pancreatic islets) or hyperglycemia (later islet cell loss). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
105 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | β-Lactam Antibiotics | Piperacillin (+ tazobactam) | Inhibits PBPs; extended spectrum to Pseudomonas (given with β-lactamase inhibitor). | Primarily renal clearance. High sodium content (in formulations) - caution in cardiac patients (off-target electrolyte load). Minimal CYP effects. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
106 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Aminoglycosides | Plazomicin | Next‑gen aminoglycoside resistant to modifying enzymes; binds 16S rRNA; 30S misreading. | Renal elimination; black‑box nephro- and ototoxicity. Limited CYP. | 0 | 0 | 0 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
107 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Polypeptide | Polymyxin B | Binds to LPS and disrupts Gram-negative bacterial outer membrane; acts as cationic detergent (bactericidal). | Nephrotoxic and neurotoxic (off-target damage to host cell membranes). Primarily renal excretion. No significant CYP effects. P-glycoprotein substrate. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 |
108 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Azole Antifungals | Posaconazole | Inhibits 14α-demethylase. Broadest spectrum azole (incl. Mucorales, some protozoa). | Strong inhibitor of CYP3A4. Requires high-fat meal for absorption. Off-target: GI upset; can elevate liver enzymes. Investigational use in Chagas disease (Trypanosoma cruzi) due to cross-targeting parasite sterol enzyme. | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
109 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Isoquinoline Pyrazine | Praziquantel | Causes severe spasms and paralysis of worms’ musculature via Ca²⁺ influx; disrupts tegument of trematodes/cestodes, exposing antigens. Drug of choice for schistosomiasis and tapeworms. | Extensive first-pass metabolism via CYP3A4. Rifampin co-administration lowers praziquantel levels by ~90% (contraindicated). Dizziness and drowsiness common (avoid driving post-dose). Bitter taste (crushed tablets) can induce nausea. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
110 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antitubercular Nitroimidazooxazine | Pretomanid | Nitro‑prodrug releasing NO; blocks mycolic acid synthesis; active vs MDR/XDR TB. | CYP3A4 metabolism & induction; transaminase elevation; peripheral neuropathy with linezolid. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
111 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - Quinoline | Primaquine | Unknown exact target; believed to interfere with parasite electron transport in mitochondria. Kills liver hypnozoites of P. vivax/ovale and gametocytes (tissue schizonticide). | Rapid hepatic metabolism. Contraindicated in G6PD deficiency - causes severe hemolytic anemia (off-target oxidative damage to erythrocytes). No significant CYP interactions documented. Occasional GI upset; methemoglobinemia at high doses. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
112 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Depolarising Anthelmintic | Pyrantel Pamoate | Nicotinic acetylcholine receptor agonist causing spastic paralysis in nematodes. | Poor systemic absorption; cholinesterase inhibition rare; minimal drug interactions; transient GI cramps. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 |
113 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Others | Pyrazinamide | Prodrug converted to pyrazinoic acid; disrupts M. tuberculosis membrane energetics and inhibits fatty acid synthase I. | Hepatotoxicity major; hyperuricaemia via reduced renal urate excretion. Not CYP significant. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 1 | 0 |
114 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - ETC | Pyrimethamine (+ Sulfadiazine) | Pyrimethamine: selectively inhibits protozoal dihydrofolate reductase (similar to trimethoprim). Used with a sulfonamide for synergistic blockade of Toxoplasma gondii folate synthesis. | Hepatic metabolism (CYP2C9, 2C19). Inhibits CYP2C9 moderately. Long half-life (~4 days). Off-target: bone marrow suppression (leukopenia, thrombocytopenia) at high doses (folate depletion - often give folinic acid rescue). Sulfadiazine shares interactions/toxicities with sulfamethoxazole (see above). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
115 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials - Quinoline | Quinine | Interferes with heme detox in Plasmodium food vacuole; gametocidal for vivax. | CYP3A4 substrate; induces its own metabolism; causes cinchonism, hypoglycaemia; QT prolongation. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 |
116 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Streptogramins | Quinupristin/Dalfopristin | Synergistic streptogramin combination: dalfopristin binds 50S, inducing a conformational change that enhances quinupristin binding; together they inhibit peptide elongation and cause premature chain release (bactericidal in combination). | Potent inhibitor of CYP3A4 (due to quinupristin) - can raise levels of cyclosporine, midazolam, etc. Primarily hepatic elimination (bile). Arthralgia/myalgia common (off-target). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
117 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Topical Pleuromutilin | Retapamulin | Binds 50S peptidyl transferase center, blocking protein synthesis; used for impetigo. | Topical exposure minimal but metabolised by CYP3A4 if systemic; avoid in <9 months infants with CYP3A4 inhibitors; mild local irritation. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
118 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Echinocandin (2nd‑gen) | Rezafungin | Long‑acting β‑1,3‑D‑glucan synthase inhibitor; once‑weekly IV dosing. | Slow chemical degradation; no CYP; infusion reactions similar to other echinocandins. | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
119 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Rifamycins | Rifabutin | Rifamycin derivative with same RNA polymerase target as rifampin. Used in TB, MAC infections. | Milder CYP3A induction than rifampin (preferred in HIV patients on protease inhibitors). May cause uveitis at high doses (off-target). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
120 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Rifamycins | Rifampin | Binds β-subunit of bacterial DNA-dependent RNA polymerase, inhibiting RNA synthesis (bactericidal). Effective against Mycobacterium tuberculosis and certain Gram+ cocci. | Potent inducer of CYP3A4, 2C9, 2C19, 1A2 and P-gp - markedly reduces levels of many drugs (e.g. protease inhibitors, azoles, warfarin). Causes hepatotoxicity and turns body fluids orange (off-target pigment effect). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
121 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Rifamycins | Rifaximin | Non-absorbed rifamycin for GI use. Binds RNA polymerase in gut microbes (treats C. difficile, traveler’s diarrhea). | Minimal systemic absorption - actions confined to gut. Negligible CYP effect systemically. Off-target: can cause mild GI upset. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
122 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Aminoglycosides | Streptomycin | Binds 30S, inhibits initiation and causes misreading; first aminoglycoside. | Renal clearance; oto- and nephrotoxicity like others. Used in TB, plague. | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
123 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Sulfonamides & DHFR inhibitors | Sulfamethoxazole (+ Trimethoprim) | Sulfonamide: competitive inhibitor of dihydropteroate synthase (blocks folate precursor PABA incorporation); Trimethoprim: inhibitor of bacterial dihydrofolate reductase. Synergistic bacteriostatic combination (sequential folate synthesis blockade). | Sulfonamides: hepatically acetylated and renally excreted. Trimethoprim: renally excreted. CYP2C9 inhibitor - TMP-SMX raises warfarin levels (bleeding risk). Significant protein binding (sulfonamide can displace bilirubin in neonates - kernicterus risk). Common off-target effects: hypersensitivity (Stevens-Johnson syndrome) and bone marrow suppression (TMP-induced megaloblastic anemia). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
124 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antitrypanosomal (African) | Suramin | Exact target unknown; non-covalently binds many parasite proteins and enzymes (e.g. glycolytic enzymes) - broad trypanocidal effects in blood stream. Used for early-stage African trypanosomiasis (T. brucei rhodesiense). | Not metabolized, renal excretion. Long half-life (~50 days). Off-target toxicities are significant: kidney damage, adrenal cortical damage (hypotension), neuropathies. No CYP interactions (does not cross BBB or readily enter cells). | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
125 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Antimalarials – 8‑Aminoquinoline | Tafenoquine | Oxidative damage to Plasmodium hypnozoites & gametocytes; radical cure & prophylaxis. | CYP2D6 metabolism; contraindicated in G6PD deficiency; long half‑life; mild CYP3A4 inhibition. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
126 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Oxazolidinones | Tedizolid | Similar mechanism to linezolid (binds 50S to prevent initiation complex). More potent against staphylococci. | Not a significant MAOI at clinical doses (lower risk of serotonin syndrome). Primarily liver glucuronidation/sulfation. GI disturbances and reversible myelosuppression as off-target effects. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
127 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Glycopeptides | Teicoplanin | Binds D‑Ala‑D‑Ala like vancomycin; long half‑life. | Renal excretion. Less nephrotoxic than vancomycin. Minimal histamine release. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
128 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Allylamines | Terbinafine | Inhibits fungal squalene epoxidase, blocking ergosterol synthesis and accumulating toxic squalene (fungicidal). Effective for dermatophytes (skin/nail fungi). | Metabolized by CYP1A2, 2C9, 3A4 (moderate inhibitor of 2D6). Highly lipophilic (accumulates in skin, nails, fat). Off-target hepatotoxicity (rare but serious - monitor LFTs). Taste disturbances and headache are common side effects. | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
129 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Tetracyclines | Tigecycline (glycylcycline) | Binds 30S with higher affinity; evades tetracycline efflux pumps and ribosomal protection (effective against many TCN-resistant bacteria). | Mainly biliary excretion. Nausea/vomiting common (off-target GI effect). No major CYP interactions. May reduce oral contraceptive efficacy (like other antibiotics affecting gut flora). | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
130 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Nitroimidazoles | Tinidazole | Reduced to nitro radicals in anaerobes/protozoa damaging DNA; longer half‑life than metronidazole. | CYP3A4 substrate; disulfiram‑like with alcohol; metallic taste, less GI upset than metronidazole. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
131 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Aminoglycosides | Tobramycin | 30S binding; enhanced Pseudomonas activity. | Renal excretion; inhaled form for CF; similar toxicity profile. | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
132 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Benzimidazole (Flukicide) | Triclabendazole | Binds parasite β‑tubulin; highly effective against Fasciola spp. and Paragonimus. | CYP1A2 metabolism to sulfoxide/sulfone; elevated LFTs possible; bitter taste; contraindicated in pregnancy. | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
133 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Glycopeptides | Vancomycin | Binds D-Ala-D-Ala terminus of peptidoglycan precursors, blocking transglycosylation and transpeptidation (inhibits cell wall synthesis). | Not absorbed orally (given IV for systemic infections). Renal excretion - requires dose adjustment in renal dysfunction. No CYP metabolism. Off-target histamine release (“red man syndrome”) with rapid infusion. | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
134 | 3dghs | 13/05/2025 12:35 PM | 3dghs | 13/05/2025 12:35 PM | Azole Antifungals | Voriconazole | Inhibits 14α-demethylase (ergosterol biosynthesis). Broad spectrum: Candida, Aspergillus. Fungistatic/cidal (species-dependent). | Metabolized by CYP2C19, 2C9, 3A4; inhibits CYP3A4, 2C9, 2C19 - significant interactions (cyclosporine, tacrolimus require dose reduction). Nonlinear pharmacokinetics. Off-target: visual disturbances (reversible), hallucinations, QT prolongation. | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |