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Table 1. Tetracycline Drug Tetracycline Characteristics Short acting (together with oxytetracycline) Broadspectrum, bacteriostatic antiobiotic MOA Pls refer above figure. Same MOA Pharmacokinetic Absorption 60-70% Impaired by: Food Formation of insoluble complexes with divalent (Ca2+, 2+ 2+ Mg , Fe ) and trivalent (Al3+) compounds Dairy products & Antacids (multivalent cations) Alkaline pH Pharmacokinetic Distribution Wide distribution to tissues & body fluids(except CSF) Cross the placenta & excreted in milk And therefore CONTRAINDICATED FOR PREGNANT WOMEN Pharmacokinetic Excretion EXCRETION: Bile : may exceed serum concentratio ns 10X => enterohepati c circulation Feces: 1040% Urine : 1050% via glomerular filtration Indication Prophylaxis for travellers diarrhea DOC 1. 2. 3. 4. 5. 6. 7. 8. 9. Adverse Effects Hypersensitvity uncommon Nausea, vomiting and diarrhea if tetracycline medication is discontinued Remedy 1. Food (ewan ko kung bakit kasi d ba impaired by food? Eh un nakasulat sa katzung eh hahaha) 2. CarboxymethylCellulose 3. Reducing drug dosage

Mycoplasma pneumonia Chlamydiae, including STD Rickettsiae, Some spirochetes Vibrio cholera (stops shedding) E. histolytica P. falciparum Chronic bronchitis Shigellosis

In combination regimens to treat gastric and duodenal ulcer disease of H. pylori Combination w. aminoglycoside 1. Plague 2. Tularemia 3. brucellosis Resistant Streptococcus Staphylococcus aureus (penicillinase-prod. strain) Pseudomonas

Modifies the normal flora of the intestine Hepatic impairment of function; >4g/day Renal: 1. Renal tubular acidosis Nitrogen retention 2. Fanconi-like syndrome Readily bound to calcium (Tetracycline-CalciumOrthophosphate ) and deposits to bone and teeth.

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aeruginosa Other clinical uses: Non-tuberculous mycobacteria Community-acquired pneumonia Leptospirosis Relapsing fever

o o o o

Bone growth is decreased Dysgenesis Staining Increased caries formation

If given during pregnancy, it can be deposited in the fetal teeth leading to fluorescence, discoloration and enamel dysplasia, bone deformity or growth inhibition Blood Interference with Vit. K synthesis Decreases Prothrombin activity

Doxycycline

Long-Acting

Same MOA

90-100% Same impairment as tetracycline EXCEPT food

half-life shortened (50%) by induction of hepatic enzymes with ingestion of: Carbamazepine Barbiturates Phenytoin Chronic alcohol intak High concentration in tears and saliva

Non-renal mechanism So no need for renal adjustment for patients with renal disease

1. Vaginal and abdominal hysterectomy 2. Bowel preparation for GIT 3. Pelvic Inflammatory Disease

If above 100mg/day Photosensitivity (UV/light) Dizziness Vertigo Nausea Vomiting

Minocycline

Long Acting

Same MOA

Same impairment as tetracycline EXCEPT food

o o

Eradication of meningococcal carrier state Acne

If above 200-400mg/day Photosensitivity Dizziness Vertigo Nausea Vomiting

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Demeclocycline

Intermediate acting (together with Methacycline)

Same MOA;

60-70%

Inhibits the action of ADH in renal tubule and has been used in the treatment of inappropriate secretion of ADH or similar peptides by certain tumors.

Photosensitivity

Chlortetracyline Tigecycline First glycylcycline Its spectrum is very broad

Same MOA Same MOA

30% Poorly absorbed orally and must be administered intravenously. Drug concentration in the urine is relatively low (thus not recommended as tx for UTI) Biliary; Non-renal mechanism Coagulase (-) staph and S. aureus, including MRSA, vancomycin-intermediate, and vanco-resistant strains; Streptococci, penicillinsusceptible and resistant; Enterococci, including vancomycin-resistant strains; Gram-positive rods; Enterobacteriaceae; MDR strains of Acinetobacter sp; Anaerobes, both gram-(+) & gram-(-); atypical agents, rickettsiae, Chlamydia, and Legionella; and rapidly growing mycobacteria all are susceptible. Skin and skin-structure infection and intra-abdominal infections. Resistants are: Proteus and P. aeruginosa

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Table 2. Quinolone

Characteristics 1st Generation Nalidixic acid

Pharmacokinetic-A

Pharmacokinetic-D

Pharmacokinetic-M

Pharmacokinetic-E Renal

Indication Enterobacteriaceae Narrow G ( - ) coverage Tx: Uncomplicated Urinary tract infections Not for use in systemic infections G ( - ) = Excellent activity G (+ ) = Good but limited activity Tx: Uncomplicated Urinary tract infections Not for use in systemic infections Prostatitis G ( - ) = Excellent activity

Adverse Effect

2nd Generation Class I Enoxacin, Lomefloxacin, Norfloxacin

Norfloxacin is the least active of the fluoroquinolones against both Gram (-) and gram (+) organisms, with minimum inhibitory concentrations (MICs) 4x-8x higher than those of ciprofloxacin.

T : 6-7 hrs Norfloxacin 3-4 hrs

Renal

2nd Generation Class II

group of similar agents possessing

1.

Good oral bioavailability

Wide distribution: a. Low protein

T1/2: 3-4 hrs

Renal (all)

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Ciprofloxacin, Ofloxacin:

excellent gram (-) (80-95%) activity and b. moderate Oral absorption: to good activity Impaired by diagainst gram-positive and trivalent bacteria. ions: o Take drugs 2-4 Levofloxacin, the L hours before any isomer of ofloxacin, antacids o Serum concentrations: similar for both drugs taken orally or administered IV

binding High lipid solubility

Ciprofloxacin 3-4 hrs

Oflo 70% G (+ ) = Moderate to good activity Coverage of atypical pathogens: Ciprofloxacin: Pseudomonas aeruginosa Levofloxacin (isomer of ofloxacin) has superior activity against gram-positive organisms, including Strep pneumoniae. Tx for Complicated urinary tract & catheter related infections Gastroenteriti s with severe diarrhea Prostatitis Nosocomial infections Sexually transmitted diseases G ( + ) : Improved activity S. pneumoniae & Staphylococci

3rd Generation Levofloxacin, Clinafloxacin, Sparfloxacin, Moxifloxacin

>12hrs; therefore once-daily dosing

Liver

Non-Renal clearance significant for: Sparfloxacin Trovafloxacin

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Gatifloxacin :

(Therefore should NOT to be used for tx of UTI) relatively contraindicated in hepatic failure patients

Coverage of atypical pathogens Clinafloxacin = best against G ( + ) cocci Not G ( - ) active Sparfloxacin = some anaerobic activity Tx for: nd Similar as for 2 Generation Communityacquired pneumonia in hospitalized pxs or if atypical pathogens Communityacquired pneumonia in non-hospitalized pxs with *risk factors for resistant pneumococcal infection Similar to 3rd Gen. G ( + ) : Enhanced activity Anaerobic bacteria : Good activity

4th Generation Trovafloxacin:

*Risk factors for PCNresistant pneumococcal infection: a. Age: < 5 yrs., > 65 yrs. b. Recent course of

Liver

Acute Hepatitis and hepatic failure

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antibiotics c. Co-morbid disease or alcohol abuse d. Immunodeficiency states/ HIV infection e. Day-care attendance, recent hospitalization & institutionalization

Tx: Consider for treatment of intraabdominal infections