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ANTIMICROBIALS

Prepared by
DR/ MOHAMMAD ABDUL BASET BADR
• 1- Gram +ve
1- Cocci ( Staphylococcus spp. – Streptococcus spp. )
2- Baccilli ( lactobacillus spp. - Bacillus spp. – Clostridium spp.)

• 2- Gram –ve
1- Cocci ( Neisseria )
2- Bacilli ( E.Coli – Salmonella – Pseudomonas – H.Pylori )

• 3- Atypical
( Chlamydia – Mycoplasma )

• 4- Mycobacteria
( Mycobacterium liprae – Mycobacterium t.B )
Types of antibiotics :
A- Cell wall synthesis inhibitors
• 1- Beta lactams:
• 1- Penicillins
• 2- Cephalosporins
• 3- Monobactams
• 4- Carbapenems

• 2- Non beta lactams :


• 1- Vancomycin
• 2- Fosofomycin
• 3- Bacitracin
• To calculate antibiotic dose we need 3 items:
• 1- Weight

• 2- Dose of antibiotic

• 3- Conc. Of antibiotic
A- CELL WALL SYNTHESIS INHIBITORS
• 1 – Penicillins :
- Penicillin G : the first antibiotic discovered. Not effective orally.

- Benzathine penicillin as Retarpen .

- Amino penicillins : ( Amoxicillin – Ampicillin )


- Amoxicillin as Amoxil – Hymox – Remox.
- Ampicillin as Epicocillin vial
- Dose of Amoxicillin:
- Adults : 500mg every 8 hours
Pediatrics : 25-50 mg/kg/day in 3 divided doses
Ampicillin every 6 hours.
Ampiciilin absorption affected by food

- Amoxicillin + Clavulenic acid as Augmentin – Klavox


Dose :
Adults : 1gm every 12 hours or 625mg every 8 hours
Pediatrics 20-50 mg/kg/day diveded in 2 or 3 doses.
It may cause diarrhea in infants younger than 8 months
- Ampicillin + Sulbactam
- Dose :
- AdultS : 1.5-3 gm every 6 hours
- Childs : 200mg/kg/day
- Sultamicillin ( oral )

- Amoxicillin + Clavulenic is the first line in treatment of otitis media &


UTI in pregnancy.
• In high amoxycillin conc. Products ( every 12 hours ).
• In low amoxycillin conc. Products ( every 8 hours ).

• Amoxycillin clavulenic conc.


4 : 1 as in 156 – 312 – 625 mg every 8 hours.
7 : 1 as in 228 – 457 – 1000 mg every 12 hour.
14: 1 as in 642 mg used every 12 hour.
• Dose of 228 or 457
• If less than 15 kg give 228
• Total daily dose of 228 = body weight

• If more than 15 kg give 457


• Total daily dose of 457 = ½ body weight
• Side effects of penicillins:
• 1- Hypersensetivity reactions : ( anaphylactic shock )
• Hypersensetivity test must be applied at everytime of injection.
• Signs :
• Severe bronchospasm
Severe hypotension
Skin allergy
• Treatment:
• 1- Epinephrine is physiological antidote I.M or S.C ( 1mg/1ml)
• Dose : 0.1 – 0.5 mg every 15 minute.
• 2- Hydrocortisone ( Solu cortef )
• 3- Chloropheniramine ( Avil )

• 2- Pseudomembranous colitis : ( Diarrhea )


• Super infection by C.Difficle treated by probiotics ( CROSS SELLING )

• 3- Oral fungal infection


2 – CEPHALOSPORINS :
• First generation as
- Cephalexin as Keflex
Dose : Adult 500mg every 12 hours
Child 25-50 mg/kg/day in 3 divided doses

- Cephradine as Ceframid
Dose : Adult 500mg every 12 hours
Child 25-50 mg/kg/day in 2 divided doses

- Cefadroxil as Roxil
Dose : Adult 500-1000 mg every 12 hours
Child 30 mg/kg/day in 2 divided doses
SECOND GENERATION :
- Cefaclor as Ceclor the best flavour antibiotic
Dose : Adult 250-500 mg every 8hours
Child 20-40 mg/kg/day divided in 3 doses

- Cefuroxime as Zinnat – Zinoximor – Daroxime.


- It is the most bad taste antibiotic ( need to shaking for long time to
decrease the bad taste ).
Dose : Adult 250-500 mg every 12 hours.
Child 30 mg/kg/day divided in 2 doses.
• THIRD GENERATION:
I – Oral :
- Cefixime as Suprax – Magnacef – cefix.
* It is one of the best antibiotics act on GIT bacteria
Dose : Adult 400 mg once daily
Child 8 mg/kg/day once daily
Total daily dose = body weight × 0.4
- Cefdinir as Omnicef – Sefarix
- Dose : adult 300mg every 12 hours
- Child 14 mg/kg/day in 2 divided doses
- Total daily dose = body weight/2 + 1
• THIRD GENERATION:
II – Parentral :
- Ceftriaxone as Triaxone
Dose : Adult 1-2 gm once daily
Child 50-75 mg/kg/day single daily dose
* Do not mix with calcium containig products as ringer solution
• Not used in premature neonates or hyperbilirubinemic neonates

- Cefotaxime as Cefotax
- Dose : Adult 1-2 gm every 12 hours
Child 50-100 mg/kg/day in 2 divided doses.
• FOURTH GENERATION :
- Cefepime as Maxipime
Dose : Adult 1-2 gm every 12 hours.
Child 50 mg/kg every 12 hours.
CEPHALOSPORINS SPECTRUM
• Fosfomycin
• Act on gm +ve and gm –ve bacteria
• Very good in UTI
• Dose : 3gm
• Single dose in UTI
• Once daily for 3 days in prostatitis
B – PROTEIN SYNTHESIS INHIBITORS
I- Tetracyclines :
as Tetracyclin – Doxycycline - Minocycline.

- Tetracycline as tetracyclin ( rarely used now ).


- Doxycyline as Vibramycin – Tabocin – Doxycin.
- Minocycline as Vulga xr.

Doxycyline and Minocycline are very good in treat Propionibacterium


acnes.
• Side effects :
1- GIT discomfort ( local irritation ) that may be minimized by coadministration with
food ( except tetracycline ) or fluids with standing up

2- Discoloration and hypoplasia of teeth and effect on the bone growth in children
less than 8 years and fetus during pregnancy ( Category D )

3- Photosensetivity : severe sunburn may occur so use sunblock ( cross selling )

4- Vestibular disturbance : dizziness and tinnitus ( Minocycline )


• Dairy products and other foods as well as supplements high in
calcium or iron can prevent absorption.

• Don’t consume dairy products or take calcium or iron supplements


within 1 hour before or 2 hours after taking tetracyclines .

• For Acne,
• Dose of doxycycline is 50 mg twice daily or 100 mg once daily.
• Dose of minocycline : 0.9 – 1.1 mg/kg/day
• Uses of tetracyclines :
• Treat infections such as
• Acne
• Chest infections
• Skin infections
• Rosacea
• Sexually transmitted infections (STIs)
• Cholera
Patient counseling :
1- taken with food ( except tetracycline ) with large amount of water
and remain upright

2- Do not take with calcium rich foods as milk&milk products

3- Do not take with other drug specially ca,iron and antacids

4- Avoid sun exposure and use sunscreen

5- Do not use for children less than 8 years and pregnancy

6- Check for expiry date


II - AMINOGLYCOSIDES
- As Streptomycin – Neomycin – Amikacin – Gentamicin – Tobramycin .
- All ( except neomycin due to severe nephrotoxicity ) must be given
parentrally .
- Neomycin can be used orally for hepatic encephalopathy or hepatic coma
( act locally in ammonia producing bacteria )
- Act mainly in gm –ve bacteria .
Side effects :
1- Nephrotoxicity : increased by use some drugs as nsaid.
2- Ototoxicity : increased by use some drugs as furosemide.
3- Neuromascular paralysis : increased by use some drugs as NMB (
neuromascular blockers ) .
III- MACROLIDES :
As Erythromycin – Clarithromycin – Azithromycin

- Erythromycin as Omathrocin 250 mg tablet.

- Clarythromycin as Klaccid – Claritt.

- Azithromycin as Zithromax – Zimax – Azi once.


• Erythromycin dose : Adult 250-500 mg every 6hours
Child 40-50 mg/kg/day divided in 4 doses

• Clarithromycin dose : Adult


Immediate release 250-500 mg every 12 hours
Extended release 1000 mg ( two 500 mg tabs once daily )
Children 15 mg/kg/day divided in 2doses.
• Azithromycin dose : /4
- For Genital ulcer disease and Gonorrhaea
- 1gm once as single dose .

- For Tonsillitis :
- Adults 500 mg once daily for 3 days .
child 10 mg/kg/day once

• For Acne :
• Azithromycin 500 mg once daily for 3 days per week for 12 weeks
• Erythromycin and Azithromycin capsules should be taken 1 hour
before or 2 hours after meals . ( tab not affected )

• Azithromycin has tissue conc. Exceeding serum conc. By 10-100 fold


( tissue half life 2-4 days ).

• Side effects of macrolides :


1- Git discomfort ( especially with erythromycin is prokinetic agent ).
2- QT interval prolongation .
3- Azithromycin may cause taste/smell loss .
Exercise
IV – LINEZOLID :
- LINDEC 600 mg film-coated tablet ( 1706.4 SR ) .
- Act on resistant gm +ve bacteria as MRSA – VRSA .
- Bioavailability 100% .
- No dose adjustment in renal or hepatic dysfunction .
- Used in children and pregnancy ( category c ).
- Dose :
Adult 300 mg every 12 hours for 10-14 days
Child 10 mg/kg every 12 hours .
- Side effects :
1- Reversible and mild bone marrow depression .
2- Serotonin syndrome ( MAOIs Action ) so not use with MAOI and serotonergic
drugs ( SSRIs ).
V – LINCOSAMIDES :
Clindamycin as dalacin
- Good action in anaerobs so used in teeth infections .
- High conc. In bone and teeth .

Dose : 150-300 mg every 6 hours.

Side effects :
Diarrhea
Nausea & vomiting
C- NUCLEIC ACID INHIBITORS
I – Quinolones and fluoroquinolones :
- 1st generation as Nalidixic acid ( not used now ).
- 2nd generation : as
Ciprofloxacin ( Ciprobay – Cipromax – Ciproxen )
Ofloxacin ( Tarivid )
- 3rd generation : as
Levofloxacin ( Tavanic – Levox )
- 4th generation : as
Moxifloxacin ( Avelox – Maxim )
Gemifloxacin ( Factive )
• Oral fluoroquinolones should be taken 2 hours before or 4 hours after
any products contain calcium – iron – zinc .
• Concentrate in in bone , urine and prostate .
• Lowest urine concentration Moxifloxacin – Gemifloxacin (not used in UTIs )
• Highest urine concentration levofloxacin .
• Most FQ excreted renally except Moxifloxacin by liver ( good for patient
with kidney disease ).
• Levofloxacin , Moxifloxacin , Gemifloxacin used once daily.
• Doses :
• Ciprofloxacin 500-750 mg every 12 hours.
• Levofloxacin 500-750 once daily .
• Moxifloxacin 400mg once daily .
• Gemifloxacin 320mg once daily .
• Side effects of FQ :
1- CNS : headache – insomnia – hallucination and rarely seizures . contraindicated
with epilepsy. Especially CIPROFLOXACIN.

2- CVS : QT interval prolongation . especially LEVO , GEMI , MOXI.

3- Dermatologic : photo sensetivity and severe sunburn may occur ( avoided by


sunscreen ). CROSS SELLING

4- Articular cartilage erosion ( arthropathy ) and not used in children younger than
18 years.
II – ANTIFOLATES ANTIBIOTICS :
• Co-trimoxazole ( Trimethoprim/sulfamethoxazole ) as Septrin – Bactrim .

- it is synergestic combination and decrease bacterial resistance.

- Used in UTI , RTI , GI infections.

- Conc. Of TMP/SMX comes in fixed ratio 1:5 of the two components.

- Dose :
- Adult : 160/800 mg 1 tab every 12 hours.
- Child : 40/200 mg 8-10 mg of TMP/kg/day divided in 2 doses.
• Side effects :
1- Rash which is severe in eldery.
2- Steven Johnson syndrome may occur but rare. (What else ?)
3- Hemolytic anemia may occur in G6PD patient. (What else ?)
4- Renal : crystalluria, so should taken with large amount of water.
5- Kernictrus in newborns .

• Contraindications :
1- Hypersensetivity to sulfa .
2- Age less than 2 months.
3- Crcl. Less than 15 ml/min.
4- Favism.
5- Pregnancy and breast feeding mothers.
URINARY TRACT ANTISEPTICS
• Nitrofurantoin : as Uvamin retard
- Nitrofurantoin is metabolized and secreted rapidly ( no systemic antibacterial
action ).
- Dose :
- 100mg BID for 7days or for 3 days after obtaining sterlie urine.
Take with food to improve absorption and decrease GI discomfort.
- Pregnancy category B ( except at 38-42 weeks of gestation is contraindicated ).
- Contraindicated in Favism.
- Urine colour : may turn urine to dark yellow or a brownish colour
SPECTRUM OF ANTIBIOTICS
Urinary tract infections treatment
Urinary tract infections treatment

•CROSS SELLING
• 1- Mannose

• 2- Cranberry
Bacterial tonsilitis treatment
• Common symptoms include:
• Sore or scratchy throat
• Pain or difficulty swallowing
• Red, swollen tonsils and throat
• Whitish spots on the tonsils .
• Fever
•Causes of tonsillitis :
• Viral tonsillitis: Most cases (up to 70 percent) of tonsillitis
• Bacterial tonsillitis (strep throat) .
• Treatment of Bacterial tonsillitis :
• Penicillins
• Clindamycin
• Cephalosporins
• Macrolides
VAGINAL INFECTIONS
• Vaginal infections can be caused by bacteria, fungi, parasites or
viruses growing in and around vagina and vulva.
• A normal, healthy vagina contains bacteria and sometimes yeast
without necessarily having an infection. But certain things can change
the environment in the vagina, enabling bacterial or yeast overgrowth
and causing symptoms. These include:
• 1- Recurrent douching, or rinsing the vagina .
• 2- Female hormone level changes
• 3- Taking antibiotics
• 4- Vaginal intercourse
• 5- Pregnancy and breastfeeding
• Symptoms of common vaginal infections
• Unusual discharge from vagina, which can be thick and white like
cottage cheese, or thinner, white/grey, green or yellow .
• Itchiness or soreness in or around the vagina
• Pain when having sex
• pain with urination
• pain in the lower abdomen or pelvis
• bleeding between periods or after having sex
Causes symptoms treatment Cross selling

Candida Thick, white Clotrimazole 2% cream daily for 3 days Vaginal douch
FUNGAL
Discharge Miconazole 2% cream daily for 7 days Topical
albicans
Vaginal itching Miconazole 400 mg vaginalsuppository, one for 3 days corticosteroid
Redness of the vulva Miconazole 1,200 mg vaginal suppository, one dose Cream
Fluconazole 150 mg orally in a single dose Dicoflor vag cap

Thin gray or white Metronidazole 500 mg pills twice a day for 7 days Vaginal douch
BACTERIAL lactobacilli
Discharge Tinidazole 2g orally once Topical
Fishy-smelling odor Metronidazole vaginal supp once a day for 5 days corticosteroid
Burning sensation Clindamycin vaginal cream 2% once a day for 7 days Cream
while urinating Dicoflor vag cap
itching of the vulva
Yellow or white, treat both parteners
PARASITIC Trichomonas
Frothy discharge one dose of metronidazole (2gm) or tinidazole ( 2gm )
vaginalis
Foul-smelling metronidazole twice a day, for 5 to 7 days.
DOSES OF COMMON ANTIMICROBIALS IN CHILDREN
• Amoxicillin – amoxicillin clavuleniec 20-50 MG/KG/DAY
• 1st and 2nd gen. cephalosporin 30MG/KG/DAY
• Ceftriaxone 50-75 MG/KG/DAY
• Cefotaxime 50-100 MG/KG/DAY
• Cefixime 8 MG/KG/DAY
• Co-trimoxazole 8-10 MG TMP/KG/DAY
• Azithromycin 10 MG/KG/DAY
• CEFDINIR 14MG/KG/DAY
• Clarithromycin 15 MG/KG/DAY
• Metronidazole 35-50 MG/KG/DAY

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