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1. Different classes of Malaria - Correct Answer: 1. Tissue Schizonticides: Drugs
that eliminate developing or dormant liver forms
2. Blood schizonticides: act on erythrocytic parasites
3. Gametocides: kill sexual stages and prevent transmission to mosquitoes
2. Treatment of Malaria - Correct Answer: Use of chloroquine for
chemoprophylaxis in areas infested by only chloroquine-sensitive malaria
(Hispaniola & Central America west of Panama Canal), Malarone, Mefloquine, or
Doxycycline for most other areas. Alternative chemophrophylactic drugs:
Primaquine & Tafenoquine
3. Sulfonamides - Correct Answer: 1. Characteristics: oily liquids or crystalline
solids that are almost always prepared by the reaction of a sulfonyl chloride with
ammonia or an amine, most commonly in the presence of caustic alkali.
2. MOA: Inhibit dihydropteroate synthase and folate production
3. Meds: PO Absorbable: Trimethoprim-sulfamethoxazole, Sulfadiazine +
pyrimethamine (treats toxoplasmosis), Sulfadoxine (second line to treat malaria);
PO Nonabsorbable: Sulfasalazine (salicylazosulfapyridine (treats IBS)); Topical:
Sulfacetamide (second line to treat bacterial conjunctivitis), Mafenide acetate
(absorbed from burn sites), Silver sulfasiazine (prevention of infection of burn
wounds)
,4.Adverse Reactions:
Common: fever, skin rashes, exfoliative dermatitis, photosensitivity, urticaria,
N/V/D & difficulties with urinary tract (crystalluria, hematuria, or obstruction)
Serious: Steven-Johnson syndrome
Others: stomatitis, conjunctivitis, arthritis, hematopoietic disturbances (hemolytic
or aplastic anemia, granulocytopenia, thrombocytopenia or leukemoid reaction),
hepatitis
Rarely: polyarteritis nodoas & psychosis
4. Fluoroquinolones - Correct Answer: 1. Characteristics: high oral
bioavailability, large volume of distribution, and broad-spectrum antimicrobial
activity.
2. MOA: block bacterial DNA synthesis by inhibiting bacterial topoisomerase II
(DNA gyrase) and topoisomerase IV
3. Meds: Ciprofloxacin, Delafloxacin, Gemifloxacin, Levofloxacin, Moxifloxacin,
Norfloxacin, Olfloxacin, Gatifloxacin (not for sale in US), Enoxacin, Lomefloxacin
4. Adverse Reactions:
Common: N/V/D, HA, dizziness, insomnia, skin rash, or abnormal liver function.
- Lomefloxacin & Pefloxacin: Photosensitivity
- Gatifloxacin, Levofloxacin, Gemifloxacin, & Moxifloxacin: Prolongation of QT
interval
- Avoid or use with caution in pts with QT interval prolongation or uncorrected
hypokalemia
- Gatifloxacin: Hyperglycemia in DM pts
- May damage growing cartilage, cause arthropathy (not recommended in pts
under 18yrs)
,Serious: Tendinitis
Rarely: Aortic dissection or rupture
Others: peripheral neuropathy, central neurotoxicities - agitation, impaired
memory/attention
5. Macrolides - Correct Answer: - Characteristics: macrocyclic lactone ring
(usually containing 14 or 16 atoms) to which deoxy sugars are attached.
- MOA: Inhibition of protein synthesis by binding to 50S ribosomal RNA
1. Erythromycin (EES)
-Clinical Use: Treats corynebbacterial infections (diphtheria, corynebacterial
sepsis, erythrasma), resp, neonatal, ocular, or genital chlamydial infections.Treats
Staphylococci & Streptococci.PCN substitute
2. Clarithromycin
- Clinical Use: Active against Mycobacterium leprae, Toxopladma gondii, & H.
influenzae. Lower incidence of GI intolerance and less frequent dosing then EES.
Treats Staphylococci & Streptococci.
- Metabolized in liver and partially eliminated in urine
3. Azithromycin
- 15-atom lactone macrolide ring compound, derived from EES by addition of
methylated nitrogen into the lactone ring.
- Clinical Use: active against M avium complex & T gondii. Slightly less active
against Staphylococci & Streptococci. Slightly more active against H. Influenzae.
Highly active against Chlamydia
4. Fidaxomicin
- Clinical Use: Treat Clostridioides difficile infections
5. Ketolides
, - Semisynthetic, 14-membered ring macrolides, differ from EES by substitution of
a 3-keto group for neutral sugar L-Cladinose
- Meds: Telithromycin (bacterial PNA -not in US), Solithromycin (not FDA
approved)
SIDE EFFECTS: Common: Anorexia, N/V/D
Acute cholestatic hepatitis (fever, jaundice, imparied liver function) -recover from
but hepatitis recurs is readmin.
Other: fever, eosinophilia, rash
EES inhibit CYP P450 enzymes - increase serum concentration including:
theophylline, Warfarin, Cyclosporine, & Methylpresnisoline, PO Digoxin
Prolong QT interval d/t effect on potassium channels → leads to rosades de
pointes arrhythmia
Azithromycin - increased risk of cardiac death
6. Beta Lactams: Penicillins - Correct Answer: - Characteristics: A thiazolidine
ring is attached to a B-lactam ring that carries a secondary amino group. Structural
integrity of the 6-aminopenicillanic acid nucleus is essential for biologic activity of
the compunds.
1. PCN (PCN G) - Greatest activity against gram-positive organisms, gram-negative
cocci, & non-B-lactamase-producing anaerobes
- Clinical Use: Except for Amoxicillin, PO PCNS should be given 1-2 hrs before or
after food. PCN G - drug of choice for infections caused by streptococci,
meningococci, some enterococci, penicillin-susceptible pneumococci,
staphylococci, Treponema pallidum, Clostridium species, Actinomyces. PCN V -
only in minor infections. Benzathine PCN & Procaine PCN G - B-hemolytic
streptococcal pharyngitis: single dose