Exercise No.

15

Anti-Infectives

1. Antibacterial

Antibacterials Generic Name Use Dose Toxicity Treatment

1.Aminoglycosides Gentamicin, treatment of -1.5–2.0 mg/kg altering phospholipid a class of antibiotics

amikacin, aerobic gram- -5.0–7.5 metabolism used to treat serious
tobramycin, negative bacilli mg/kg. infections caused by
neomycin, and infections -15–30 bacteria that are
streptomycin. mcg/mL difficult to treat.
2. Beta-lactams ampicillin / used in the 150 mg/kg to neurotoxic, treatment of various
sulbactam management 450 mg/kg nephrotoxic, genotoxic infections caused by
and treatment and some are susceptible strains
of bacterial reproductive toxic. of bacteria, such as
infections. lower respiratory
infections, urinary
tract infections, skin
infections, and bone
and joint infections.
3. Macrolides azithromycin use to manage 100 mg / Severe toxicity is very They are also
and treat 250mg / rarely observed with used in
various 500mg / macrolides. uncomplicated
bacterial 600mg – oral skin infections and
infections tablets otitis media in
pediatric patients.
4. Quinolones and Ciprofloxacin, in human and 500 mg PO nausea, diarrhea, and The
fluoroquinolones norfloxacin and veterinary q12hr or 400 vomiting fluoroquinolones
ofloxacin medicine to mg IV q12hr are indicated for
treat bacterial for 10 days treatment of
infections, as several bacterial
well as in infections,
animal including bacterial
bronchitis,
husbandry,
pneumonia,
specifically
sinusitis, urinary
poultry tract infections and
production. etc.

5. Trimethoprim Bactrim, Bactrim to treat 800 milligrams Nausea/vomiting. It is an

and DS, Septra, infections (mg) of Dizziness. Headache antimicrobial
sulfamethoxazole Septra DS, including sulfamethoxazole used to treat and
Cotrim, urinary tract and 160 mg of prevent many
Cotrimoxazole, infections, trimethoprim bacterial
Sulfatrim. middle ear once a day infections.
 infections
(otitis media),
bronchitis,
traveler's
diarrhea, and
shigellosis
(bacillary
dysentery).
6. Leprostatic thalidomide to treat acne 100 mg per Blood disorders Substances that
drugs vulgaris, day include anemia, suppress
Hansen's methemoglobinemia, Mycobacterium
disease, and sulfhemoglobinemia, leprae, ameliorate
dermatitis hemolysis the clinical
herpetiformis. manifestations of
leprosy, and/or
reduce the
incidence and
severity of leprous
reactions.
7. Anti- rifampin, to treat 5 mg/kg (300 hepatotoxicity The most common
tuberculosis drugs isoniazid, Mycobacteriu mg). 15 mg/kg associated with treatment for
pyrazinamide, m tuberculosis (900 mg). 15 isoniazid, rifampicin active TB
and ethambutol infections. mg/kg (900 mg) and pyrazinamide is isoniazid INH in
combination with
three other drugs
—rifampin,
pyrazinamide and
ethambutol

2. Antifungals

Antifungals Method Toxicity Treatment

1. The polyene These drugs interact with sterols in An antifungal agent is nystatin, natamycin,
antifungal drugs cell membranes (ergosterol in a drug that and amphotericin B
fungal cells; cholesterol in human selectively eliminates
cells) to form channels through the fungal pathogens
membrane, causing the cells to from a host with
become leaky minimal toxicity to
the host
2. The Flucystosine Flucytosine enters the fungal significant toxicity for used to treat serious
cell via cytosine permease; thus, the bone marrow, fungal infections in
flucytosine is metabolized to 5- liver, and the body.
fluorouracil within fungal gastrointestinal tract.
 organisms.
3. Imidazoles multicomponent approach. low acute toxicity as A topical antifungal
indicated by the used to treat a variety
LD 50 of 970 mg/kg of dermatophyte
infections.

3. Antiparasitic

Antiparasitic Toxic Effect Dose

1. 4-Aminoquinolones Toxicity 4- liver damage and Dosages ranging
(chloroquine hydroxychloroquine Aminoquinolines have agranulocytosis from 3.5 to 4.0
and amodiaquine) been shown to mg/kg per day for
accumulate selectively chloroquine and 6.0
in melanin structures of to 6.5 mg/kg per day
fetal eyes for
hydroxychloroquine
are clinically safe.
2. 8-aminoquinolones Primaquine may cause effective against the 120 or 240 mg
(primaquine) hemolytic anemia in intrahepatic
patients with these permanent forms
conditions. of Plasmodium
vivax and
Plasmodium ovale.
3. Cinchona alkaloids (quinine) toxic features effective when 325 mg to 1 g as
(cinchonism) in patients combined with the sulfate salt.
with excessive intake, clindamycin to treat
but only quinine babesiosis.
produces blindness.
4. Dihydrofolate reductase bone marrow dysmorphic facial dosage of 25
inhibitors (Proguanil and suppression, features, skull and mg/week
pyrimethanine) limb abnormalities,
and growth
deficiency.
5. Dihydrofolate reductase Sulfadoxine targets differently act on folic dose of 25 plus 1.25
inhibitors plus a sulfonamide or Plasmodium acid synthesis. mg/kg.
sulfone (pyrine thiamine plus dihydropteroate
sulfadoxin and plus dapsone) synthase
and dihydrofolate
reductase
6. Antibiotics (tetracycline and The incidence of gastrointestinal 333 milligrams (mg)
erythromycin) undesirable side effects irritation, diarrhea, every 8 hours or 500
associated with the use phototoxic mg every 12 hours
of erythromycin is low. dermatitis, and
vestibular damage
7. Quinolone methanol anxiety, panic attacks, insomnia, anxiety, 20-25 mg/kg split
(mefloquine) paranoia, persecutory vivid dreams, and into 2-3 doses 6-8
delusions, dissociative visual disturbances hourly.
psychosis, and
anterograde amnesia

4. Case Analysis

Antibacterial Dose Dose Ingested Toxic effect Treatment

Ciprofloxacin 200mg/20mL ; 500 milligrams have idiosyncratic treat urinary

oral suspension. (mg) 2 times a hypersensitivity tract infections,
day, taken reactions in the sexually
every 12 hours form of liver transmitted
for 60 days. injury or life infections
(gonorrhea and
chancroid),
skin, bone, joint
infections

Questions to answer:

1. What are the risk factors for aminoglycoside?

 Prolonged duration of therapy.

 Advanced age.
 Comorbid disease
 Reduced effective arterial volume.
 Sepsis.
 Concomitant medications.
 Elevated plasma drug concentrations.
 Type of aminoglycoside.

2. What organs are usually affected in anti-infective poisoning?

  The liver and kidney are particularly susceptible to organ toxicity as they are the sites of
toxin filtration and toxin metabolic breakdown

3. What is the effect of concomitant use of griseofulvin with alcohol?

 Griseofulvin may increase the effects of alcohol. If taken with alcohol it may also cause
fast heartbeat, flushing, increased sweating, or redness of the face

4. What should be given to patients who have ingested more than 5g of chloroquine with a BP less
than 80 mmHg?
 Chloroquine is currently administered orally when used as a prophylaxis for malaria and the
treatment of chronic autoimmune diseases. [7] For malaria prophylaxis, 500 mg is typically
administered orally two weeks before, during, and up to 8 weeks after exposure to an endemic
area, taken as a weekly dose.

5. Which drug is used as the gold standard in antifungal therapy?

 Amphotericin B. Still the 'gold standard' for antifungal therapy.