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111 Cards in this Set

  • Front
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Amino-penicillin's uses
HELPs……..
Infections caused by the following organisms:
Haemophilius influenzae
E.coli
Listeria monocytogenes
Proteous mirabilis
Salmonella typhi

Ampicillin
Active against gram +ve and gram - ve organisams
Side effect of Ampicillin
Diarrhea is a side effect
Antipseudomonal penicillins are used to treat
pneumonias associated with cystic fibrosis…..DOC (Fluroquinolone e.g. Ciprofloxacin also DOC)

Mechanical ventilation……..For prophylaxis of pseudomonal inf.
----> DOC
UTI (if…..caused by E.coli, Pseudomonas, proteus, Kebsiella)
It has good activity against Pseudomonas aeruginosa

High dose cause bleeding by interfering with platelet function.
DOC for pneumonia associated with cystic fibrosis
Anti pseudomonal PC
(Fluroquinolone e.g. Ciprofloxacin also DOC.)
Beta-lactamase/Penicillinase inhibitors:
Clavulanic acid
Sulbactum
Tazobactum
what formulations combine a beta-lactam antibiotic with a beta-lactamase inhibitor (beta-lactam antibiotic + beta-lactamase inhibitors)
Ampicillin-Sulbactam
Ticarcillin-Clavulanic acid
Piperacillin- Tazobactam
Amoxicillin–Clavulanic acid
route of admin. for beta lactamase inhi. and what is the exception?
All of the beta-lactamase inhibitor combinations except amoxicillin-clavulanic acid are parenteral formulations.
Penicillins….in Pregnancy
Ampicillin
Penicillin G
penicillin V
safe for pregnant women.
What is the major antigenic determinent of Pc hypersensitivity?
The major antigenic determinent of Pc hypersensitivity is its metabolite, penicilloic acid, which reacts with proteins and serve as a hapten to cause an immune reaction.
Jarisch Herxheimer Reaction
in the treatment of Syphilis……. Penicillin injected in a secondary syphilitic patient produce fever, exacerbation of lesions and vascular collapse.
Type of hypersensitivity RXN
1.IgE mediated- Rapid onset, Anaphylaxis,Angioedema,Laryngospasm.

2.IgM and IgG antibodies fixed to the cells
-Vasculitis,Neutropenia, Positive Coombs test.

3.Immune Complex formation- Vasculitis, serum sickness, Interstitial nephritis.

4.T-Cell Mediated---Urticarial and Maculopapular rashes, Stevens-Johnson Syndrome
Coombs' test
The Coombs' test looks for antibodies that may bind to red blood cells and cause premature red blood cell destruction (hemolysis).

Positive Coombs' test means pt have antibodies that act
against red blood cells.
Positive Coombs' test may be due to:
Autoimmune hemolytic anemia
CLL
Drug-induced hemolytic anemia
Erythroblastosis fetalis (hemolytic disease of the newborn)
Infectious mononucleosis
Mycoplasmal infection
Systemic lupus erythematosus
Transfusion reaction
1st generation cephalosporin uses?
Acts as Pc G substitutes
Activity includes Gram positive cocci(not MRSA), E.coli,Klebsiella pneumoniae and some proteus species (PEcK).

Common use in Surgical prophylaxis.
None enter CNS.
what is cefazolin and what is it DOC for?
Cefazolin …DOC for surgical prophylaxis, good penetration into bone.
3rd generation cephalosporin uses?
3rd generation Cephalosporins are important in empiric management of Meningitis and Sepsis. since they enter CNS.
Ceftizoxime uses? family?
Ceftriaxone(IM) and Cefixime (PO) used in single dose for Gonorrhea.

Cefotaxime-active against most bacteria causing Meningitis.

Ceftizoxime is active against B.fragilis.

3rd generation ceph.
The treatment of choice for gonorrhea in Pc/Cephalosporin -allergic patients.
Ofloxacin or ciprofloxacin is the treatment of choice for gonorrhea in Pc/Cephalosporin -allergic patients.
Organisms NOT covered by
Cephalosporins?
Organisms NOT covered by
Cephalosporins are “LAME”.
Listeria monocytogenes
Atypicals(Chlamydia,Mycoplasma)
MRSA(Methicillin Resistant Staphylococcus aureus)
Enterococci.
Cephalosporins side effects?
Most authorities recommend avoiding cephalosporins in patients allergic to penicillins.
Cefotetan,Cefoperazone,Cefamandole, cause hypoprothrombinemia (anti-vitamin K effect)---- cause bleeding and also disulfiram like interactions with ethanol
IV injections-Phlebitis (inflammation of a vein)
IM injections-Pain.
Meningitis DOC?
if meningitis caused by Listeria DOC?
Meningitis….. Ceftriaxone is DOC (if meningitis caused by Listeria DOC…ampicillin and st. pneumoniae …Pc G)
Gonorrhea…… DOC?
Ceftriaxone(IM) and Cefixime (PO) used in single dose for Gonorrhea…… DOC
Typhoid fever – DOC?
Typhoid fever – Ceftriaxone (azythromycin, fluroquinolone..also DOC)
Gonococcal Urethritis DOC? In case of allergies to this group of drugs?
Ceftriaxone
Ofloxacin or ciprofloxacin is the treatment of choice for gonococcal urethritis in Pc/Cephalosporin -allergic patients.
Non-gonococcal urethritis DOC?
azithromycin or doxycycline. 
(a single dose of azithromycin or a 7-day course of doxycycline.  Rates of success with either regimen are around 90%)
Carbapenams (imipenam and meropenam) USES
Wide spectrum that includes:
Gram positive cocci
Gram negative rods(Enterobacter,Pseudomonas species)
Anaerobes (nocardia and actinomyces)

●Important in hospital agents for empiric use in severe life threatening infections.


Imipenam is given with Cilastatin
(Imipenam +Cilastatin),which inhibits its rapid
metabolism by renal dihydropeptidases.
Carbapenams Adverse Effects
GI distress…..nausea, vomiting, diarrhea
Drug fever(partial cross-allergenicity with penicillins)
CNS effects,including seizures
Renal dysfunction.
Eosinophilia, Neutropenia, Neurotoxicity
VANCOMYCIN use
Gram positive cocci including MRSA(DOC) and
enterococci and
Clostridium difficile……DOC
antibiotic associated colitis/pseudomembranous colitis TX?
One of the DOC……in antibiotic associated colitis due to clostridium difficile or staphylococci

(antibiotic associated colitis/pseudomembranous colitis… ……ampicillin, Tc, clindamicin
RX…..Vancomycin…may be 1st choice but it is reserve drug.
Metronidazole…1st choice)
Vanco. enters all tissue except?
CNS, and bone
Vanco. Adverse effects
Ototoxicity (usually permanent)
Hypotension/Shock (due to histamine release)
diffuse hyperemia(“Red man syndrome”/Red neck syndrome)…… due to histamine release---if given too rapidly IV
nephrotoxicity
hypersensitivity reactions.
Monobactam
Monobactam---------Aztreonam:

Mode of Action:
Monobactam inhibitor of early step in cell wall synthesis.

It is a novel beta lactam antibiotic which is not fused to other ring.

It inhibits enterobacteriacea and gram –ve rods, e.g Pseudomonas
Has no activity against gram +ve and anaerobes.
Resistant to Beta-Lactamases.

Use:
IV drug mainly used in Hospital acquired infections.
No cross allergenicity with penicillins or cephalosporins.
Fosfomycin
AKA Phosphomycin and phosphonomycin
Inhibits initial steps in the bacterial wall synthesis
Active against both gram +ve and gram –ve
Orally used for UTI
Safe in pregnancy
Protein synthesis inhibitors
MCAT

Macrolides (50S)
Aminoglycosides (30 S)
Chloramphenicol (50S)
Tetracyclines (30S)
MOA of Aminoglycosides
(30S)
Interfere with initiation codon functions-block association of 50S ribosomal subunit with mRNA-30S(static);misreading of code- incorporation of wrong AA(cidal).
Tetracyclines
(30S)
2.Amino acid incorporation
Block the attachment of aminoacyl tRNA to acceptor site,(static)
ChloramPhenicol (50S)
3.Formation of Peptide bond
Inhibit the activity of peptidyl transferase,(static)
Macrolides and Clindamycin
(50S)
4.Translocation
Inhibit translocation of peptidyl t RNA from acceptor to donor site,(static).
Macrolides
Use as an alternative to Pc in individuals who are allergic to beta-lactam antibiotics.

Antibiotics in this group include:
Erythromycin
Clarithromycin
Azithromycin
Oleandomycin
Dirithromycin (semisynthetic derivative of erythromycin ) -----is no longer available in the United States
Uses of Macrolides
is used for the infections caused by
Gram positive cocci (not MRSA)
Atypical organisms (chlamydia, Mycoplasma and Ureaplasma species)
Legionella pnemophilia
Campylobacter jejuni.
Syphilis (if allergic to Pc)
Corynebacterium diptheriae

Use as an alternative to Pc in individuals who are allergic to beta-lactam antibiotics.
Azithromycin
similar spectrum but it is less effective against streptococci and staphylococci than erythromycin, is far more active, especially organisms associated with sinusitis or otitis media (H.influenza, M.catarrhalis)
Erythromycin and azithromycin are excreted primarily in active form in bile, with only low levels found in urine.

Mycobacterium avium intracellulare (MAC)
Carithromycin:
Carithromycin has more activity for MAC and H.pylori.
DOC…for MAC(mycobacterium avium intracellular)

Clarithromycin is eliminated largely by the kidney
Erythromycin Vs. Azithromycin side effects
rythromycin causes GI distress (via stimulation of motilin receptors)

The estolate form (of erythromycin) is associated with cholestasis and not recommended in Pregnancy or the Elderly.

Inhibits P450 drug metabolism(potential drug interactions)

Auditory dysfunction at High I.V doses

IV administration of erythromycin is associated with high incidence of thrombophlebitis.

Azithromycin:
Azithromycin is safer in Pregnancy and does not inhibit P450 Drug metabolism.
Clarithromycin side effects?
Clarithromycin causes less GI distress than erythromycin.
It also inhibits P450 drug metabolism (potential drug interactions)
Causes Reversible Deafness at high doses
Animal studies have shown Teratogenic effects.
Clindamycin
Gram positive cocci(not MRSA) and
anaerobes including B.fragilis.

Has also been used in Toxoplasmosis…..DOC
osteomyelitis due to Gram positive cocci.

First known drug to cause Pseudomembranous colitis (S/A..ampicillin, Tc, clindamycin)
(Rx…Vancomicin, Metronidazole)
Pseudomembranous colitis TX?
Vancomicin,
Metronidazole
AMAs avoided in Pregnancy
Aminoglycosides
Erythromycin estolate
Clarithromycin
Fluroquinolones
Tetracyclines
Sulfonamides
Why anaerobes are resistant to amino-glycosides?
Aminoglycosides are bactericidal, accumulated intracellularly in microorganisms via an O2-dependent uptake.
Thus Anaerobes are innately resistant.
NAme the amino glycosides?
Streptomycin
Neomycin
Kanamycin
Gentamicin
Tobramycin
Amikacin
Netilmicin
clinical uses of amino glycosides?
Infection due to Pseudomonas
Chronic UTI
Tularemia
Pneumonia caused by …….E.coli,Klebsiella


Aminoglycosides are often used in combinations.
Synergistic actions occur for infections caused by enterococci (with penicillin G or ampicillin) and P.aeroginosa (with an extended spectrum penicillin).
Streptomycin is used for?
Streptomycin is used in Tuberculosis

Bacterial endocarditis

Tularemia…..AKA rabbit fever, deer fly fever (Francisella tularensis, gram-negative coccobacillus)

Plague (Yersinia pestis, Gram negative ……usually resulting from the bite of an infected flea. The fleas are often found on rodents, such as rats and mice )

Brucellosis
One of the DOC for (Bubonic) Plague and Tularemia.
Neomycin systemic or tpical use?
Too toxic for systemic use, is used topically.
Tularemia TX?
Streptomycin or gentamicin……… IV
Tetracycline class ( doxycycline) or Fluoroquinolone class (ciprofloxacin) of antibiotics are taken orally.
Streptomycin….DOC
Dosage of Streptomycin for renal dysfunction?
Renal elimination is proportional to GFR, and major dose reduction is needed in Renal dysfunction.
adverse effect of streptomycin?
Nephrotoxicity includes Proteinuria,Hypokalemia,Acidosis,and Acute tubular necrosis(ATN)……..usually reversible.

Ototoxicity from Hair cell damage; includes Deafness and Vestibular dysfunction……which are not readily reversible.

Ototoxicity……may be enhanced by Loop Diuretics.

Neuromuscular blockade: may enhance the effects of Skeletal muscle relaxants.

Contact dermatitis: By Neomycin
CHLORAMPHENICOL
Is active against a wide range of Gram +ve and Gram
–ve organisms, but because of its toxicity, its use is
restricted to life-threatening infections in which there
are no alternatives.
clinical use of chloramphenicol?
Bacteriostatic with a wide spectrum of activity but
currently a back up drug for infections due to…….
Salmonella typhi
B.fragilis, Rickettsia
Bacterial meningitis.

▪Orally effective, with good tissue distribution,including
CSF.
because of its toxicity, its use is
restricted to life-threatening infections in which there
are no alternatives
metabolization and does consideration for chloramphenicol
Metabolized by Hepatic glucuronidation
So…..
dose reductions are needed in Liver dysfunction and in Neonates.
Side effects of chloramphenicol
Dose-dependent bone marrow suppression is common.
Aplastic anaemia
“Gray Baby Syndrome” in neonates (Due to decreased Glucuronysyl transferase).
Optic neuritis in children.
Inhibits CyP450----->Inhibits metabolism of Phenytoin, Sulfonylureas,and Warfarin
--->thus elevating their concentration and potentiating their effects.
NAme Bacteriostatic drugs,actively taken up by susceptible bacteria?
MOA?
MOA: Block the attachment of aminoacyl tRNA to acceptor site.
Tetracycline
Chlortetracycline
Oxytetracycline
Demeclocycline….may cause diabetes incipdus
Methacycline
Doxycycline….can be used in renal failure
Minocycline
tetracyclines display broad-spectrum activity and are Effective against?
both gram-positive and gram-negative
bacteria, including atypical microorganisms….
Rickettsia
Coxiella
Mycoplasma
Tc.. are also effective in the treatment of
brucellosis
tularemia
infections caused by Pasteurella and Mycoplasma spp.
Tetracyclines are still the drugs of choice for treatment of ?
Tetracyclines are still the drugs of choice for treatment of
Cholera
diseases caused by Rickettsia, Coxiella
chlamydial diseases (trachoma, lymphogranulomavenereum, and psittacosis )
Nonspecific urethritis
--->DOC: Atypical microorganisms
Tetracyclines are clinically effective in acne because of?
their antioxidant effect on the degranulated neutrophils in the comedone acidic contents (in which long-term low-dose therapy is popular).
which tetracycline is a popular choice for patients with preexisting renal disease or those who are at risk for developing renal insufficiency? why?
Doxycyclin
The lack of nephrotoxicity is related mainly to biliary excretion, which is the primary route of doxycycline elimination. (S/A…erythromycin and azithromycin)
Doxycyclin is DOC for?
Doxycycline is DOC… anthrax (Bacillus anthracis) after exposure.

Doxycycline is DOC…primary stage of Lyme disease in adults and children older than 8 years.

DOC..for chronic/acute Prostatitis because it reaches high levels in prostatic fluid
Minocycline appears where?
what is the usage?
in Saliva at high concentrations and is used in the Meningococcal Carrier State (alternative to rifampin).
which tetracycline is the most lipid soluble?
Doxycycline
Demeclocycline use?
Demeclocycline is used in Syndrome of inapproriate secretion of ADH (SIADH ….excessive release of ADH)---> Demeclocycline blocks
-> ADH actions in the collecting ducts.
Tetracycline's side effects?
GI distress (this can be avoided if the drug is taken with food other than dairy products ,e.g milk, yogurt)

Superinfections leading to Candidiasis or Colitis.

Tooth enamel dysplasia and possible decreased bone growth in children (avoided in Children).

Renal dysfunction (Fanconi syndrome)

Photo toxicity with Demeclocycline and Doxycycline.

Have caused Liver dysfunction during Pregnancy at very high doses(Contraindicated in Pregnancy)

Vestibular dysfunction by Minocycline and Doxycycline.

Pseudotumor cerebri : benign ICH characterized by headache, and blurred vision
C/I of Tetracyclines
Pregnant or breast feeding women
Children under 8 yrs of age
Renal impairment
RX for Lyme disease( B. burgdorferi )
Rx :
Doxycycline ---->DOC
If pt is pregnant/age <8 yrs…..then Pc (amoxycillin)………..DOC
If allergic to Pc--> erythromycin



If pt has= skin rash+7th CN palsy+ arthritis----> doxycycline or amoxycillin
If pt has=CVS+CNS symptoms…then--> Ceftriaxone or PcG inj.
Quinupristin and Dalfopristin
Quinupristin and Dalfopristin are Streptogramins that act in concert via several mechanisms.- via 50S
Protein synthesis Inhibitors.
Quinupristin and Dalfopristin uses?
parenterally in severe infections caused by Vancomycin Resistant Staphylococci(VRSA) and Enterococci(VRE) as well as other Drug resistant Gram positive cocci
Quinupristin and Dalfopristin adverse effects?
Toxic potential remains to be established.
Resistance has been reported via the formation of inactivating enzymes and increased efflux mechanisms.
activity and clinical use of Linezolid
Linezolid is an oxazoli-di-none that inhibits the formation of the initiation complex in bacterial translation systems by preventing formation of the N-formyl-methionyl-t-RNA-ribosome-mRNA ternary complex
Linezolid use and side effect?
A new drug available in oral and parenteral
formulations for treatment of VRSA,
VRE(vancomycin-resistant enterococci ) and
Drug resistant Pneumococci.


Adverse effects:
Headache and
GI distress
Folic acid inhibitors, how they fxn?
Folic acid coenzymes are required
---- for the synthesis of purines and pyrimidines (precursors of RNA and DNA) and other compunds are required for cellular growth and replication.

In absence of folic acid, cells can not grow or divide. Sulfa drugs are inhibitors of folic acid synthesis.
Antifolate Drugs?
1. Inhibitors of dihydropteroate synthetase: Sulfonamides
2. Inhibitors of dihydrofolate reductase: Trimethoprim
Pyrimethamine
3. Inhibitors of dihydropteroate synthetase and dihydrofolate reductase: Co-trimoxazole
MOA of Sulfonamides?
All sulfonamides are synthetic strustural analogs of p-aminobenzoic acid (PABA)

Compete with PABA, causing inhibition of Dihydropteroate synthase and formation of non functional folic acid.
Sulfonamides are used against which bacteria?
Sulfonamides inhibit both gram positive and gram-negative bacteria, nocardia, Chlamydia trachomatis, and some protozoa.
Some enteric bacteria, such as E coli, klebsiella, salmonella, shigella, and enterobacter, are inhibited
Clinical use of Sulfonamides? and are DOC for?
Nocardial infections……DOC

Simple Urinary Tract Infections (UTI)…….Sulfisoxazole

Ulcerative Colitis….Sulfasalazine..DOC

Trachoma….Sulfacetamide,topical

Burns……Silver Sulfadiazine, topical

Toxoplasmosis-Sulfadiazine+Pyrimethamine…DOC
(S/A. Clindamycin)
Biodisposition and elimination of Sulfonamides?
Effective orally and eliminated via Hepatic metabolism (acetylation) and renally as unchanged drug.

Less water soluble metabolites of the drug……… may cause Crystalluria.

Sulfonamides bind to plasma proteins…..increased drug interactions including increased effects of Methotrexate,Phenytoin and Warfarin.
Adverse effects of Sulfanamides
Hypersensitivity, mostly Rashes,which can be Severe (Stevens-Johnson Syndrome….S/A Pc).

cross allergenicity between Sulfonamides and possibly with Sulfonylurea hypoglycemics.

GI distress (NVD),Phototoxicity

Haemolysis in G6PD deficiency are common.

Avoid in third trimester because they cross placental barrier and may displace bilirubin from the plasma proteins in Neonates-------Kernicterus

Crystalluria…nephrotoxicity (RX..adequate hydration, alkalinization of urine)
Dihydrofolate reductase
inhibitors
Name
MOA
Trimethoprim
Pyrimethamine
inhibits bacterial dihydrofolic acid reductase (dihydrofolate reductase).
Use in combination with sulfonamide drugs


1st combination :
Trimethoprim +Sulfamethoxazole combination ----called Co-trimoxazole

2nd combination :
Pyrimethamine + Sulfadiazie
Trimethoprim
Pyrimethamine
are used as combination with what drugs and why?
When Trimethoprim is used with Sulfamethoxazole (TMP-SMX),there is synergism and decreased emergence of resistance resulting from the sequential blockade of Folic acid synthesis.
the combination used usually is Bactericidal.


2nd combination :
Pyrimethamine inhibits Dihydrofolate Reductase in Toxoplasma gondii and is used with Sulfadiazine in prophylaxis and treatment of Toxoplasmosis.
Pyrimethamine + Sulfadiazine ………prophylaxis and treatment of Toxoplasmosis.
Co-trimoxazole…clinical uses ?
Possible co-DOC in complicated UTI and in Respiratory,Ear and Sinus infections associated with H.influenzae, M.catarrhalis.

Backup drug for L.monocytogenes, Proteus mirabilis, S.typhi, MRSA, and Vibrios.

DOC for prophylaxis and treatment of Pneumocystis carinii Pneumonia (PCP)
Trimethoprim may cause what adverse effects?
Megaloblastic anaemia
Leukopenia (Rx…Leucovorin)
Thrombocytopenia
Haematotoxicity, Drug fever,Rashes and severe GI distress are problematic in patients with AIDS.
Inhibitors of nucleic acid metabolism?
The quinolones/FQ classified into:
1st generations: older
Nalidixic acid
Cinoxacin

FLUOROQUINOLONES
2nd generations:
Norfloxacin
Ciprofloxacin, Ofloxacin
Enoxacin, Lomefloxacin
3rd generations:
Levofloxacin
Sparfloxacin
Gatifloxacin;

4th generations:
Trovafloxacin
Moxifloxacin.

Several of the newer quinolones have been recently removed from the market as a result of QT prolongation
Fluoroquinolones MOA?
The Fluoroquinolones are Bactericidal

They interfere with Bacterial DNA synthesis.

They inhibit Topoisomerase 2 (DNA gyrase), blocking the relaxation of supercoiled DNA, required for replication.
Also inhibit Topoisomerase 4, responsible for separation of replicated DNA during cell division.
Fluoroquinolones clinical use?
Wide spectrum that includes
Gram positive
Gram negative Cocci, Gram negative rods (E.coli,S.typhi, Shigella,Serratia etc.)
some anaerobes (C.jejuni)
Mycobacteria.

Active when administered orally (inhibited by Antacids) and have a wide tissue distribution including Bone.

FQs may have enhanced activity against
resistant Pneumococci …..Sparfloxacin
resistant Chlamydia……Ofloxacin
Fluroquinolones are DOC for?
Ciprofloxacin and Ofloxacin are co-DOC for Gonorrhea(single doses) but Ceftriaxone….DOC 1st choice.

DOC for…complicated/recurrent UTI (3rd gen cephalosporin can be used after having C/S report)
(for uncomplicated/simple UTI..Sulfonamides or
Amoxicillin or 1st gen cephalosporin)
C/I to Fluroquinolones
GI distress(NVD), Rash, Phototoxicity (especially sparfloxacin).

CNS effects usually mild (insomnia,dizziness and headache),but seizures occur in overdose and in susceptible patients.

Contraindicated in Pregnancy and Children, based on animal studies showing effects on collagen metabolism and cartilage development;tendonitis(and tendon rupture) has occurred in adults.
Drug specific toxicity of Sparfloxacin?
Increases Q-T interval
Drug specific toxicity of Trovafloxacin?
Hepatotoxicity
The primary/1st line drugs in combination
regimens for TB treatment are :
Isoniazid (INH)..most potent anti-TB drug, bacteriostatic
Rifampicin…..bactericidal
Ethambutol
Pyrazinamide


Regimens may include two to four of these drugs, but in the case of highly resistant organisms, other agents may also be required.
Backup/2nd line drugs for treatment of TB include:
Backup/2nd line drugs include:
FAACCE
Aminoglycosides (streptomycin, amikacin, kanamycin)
Aminosalicylic acid : competitive inhibitor for PABA
Fluroquinolones
Capreomycin (marked hearing loss)
Cycloserine (Neurotoxic)
Ehtionamide : analog of INH
Drugs For prophylaxis of TB?
For prophylaxis of TB:
Usually INH, But Rifampicin if intolerant to
INH.

In suspected drug resistance, both drugs may be used in combination.
Prophylaxis and RX of Mycobacterium Avium Intracellulare (MAC)
For Prophylaxis:
Azithromycin
or
Clarithromycin
For Rx:
Clarithromycin+Ethambutol+Rifabutin (an analog of Rifampicin)
Isoniazid
MOA
Inhibits mycolic acid synthesis;

high level of resistance…
deletion in cat K gene (codes for catalase).
Isoniazid
Adverse effects
Hepatitis,
Peripheral neuritis (use Vit B6), Haemolysis in G6PDdeficiency,
SLE in Slow acetylators.
Rifampicin use
Also used for Leprosy, prophylactically household members exposed to meningitis caused by for meningococci, H.influenzae
Rifampicin MOA
Inhibits DNA dependent RNA polymerase.
Rifampicin adverse effect
Proteinuria,
Hepatitis,
“Flu like Syndrome”
Induction of P 450,
Thrombocytopenia,
Red orange metabolites.
Ethambutol MOA
Inhibits synthesis of arabinogalactan (cell wall component)
Ethambutol adverse effects
Dose dependent Retrobulbar neuritis--->decreased visual acuity and Red –Green discrimination
Pyrazinamide adverse effects
Polyarthralgia,Myalgia, Hepatitis,Rash,
Hyperuricemia(#1 side effect)
Phototoxicity, increased porphyrin synthesis.
Streptomycin adverse effects and MOA
Deafness(*)
Vestibular dysfunction
Nephrotoxicity(*)
MOA: Protein syn.Inhibition
define:
Multi-drug-resistant tuberculosis (MDR-TB)
Extensively drug-resistant TB (XDR-TB)
Multi-drug-resistant tuberculosis (MDR-TB):
is defined as resistance to the two most effective first-line TB drugs: rifampicin and isoniazid.

Extensively drug-resistant TB (XDR-TB) :
is also resistant to three or more of the six classes of second-line drugs.
Chemotherapy for leprosy?
Triple drug regimen:
Dapsone
Clofazimine
Rifampicin/Rifampin
Dapsone is used for?
S/E are?
Dapsone: structrually related to sulfonamides.

Use Rx: Leprosy, PCP
S/E: hemolysis in pt with G6PD deficiency, methemoglobinemia, peripheral neuropathy.
Clofazimine use?
Clofazimine is indicated in the treatment of lepromatous leprosy, including dapsone-resistant lepromatous leprosy and lepromatous leprosy complicated by erythema nodosum leprosum.