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بسمميحرلا نمحرلا هللا جامعة كرري كلية الصيدلة Pharmaceutical Microbiology III 2021 Lecture (2)Part 1 Semi-synthetic

Dr.Eithar Karrar M.Pharm OIU2011

Karary university Dr. Eithar Karrar 2021 1 Objectives 1

• By the end of this part students should know regarding the following other types of penicillin’s:- • Their members. • Properties. • Spectrum of activity & therapeutic uses. • Side effects. • Drug drug interaction.

Karary university Dr. Eithar Karrar 2021 1. inhibitors-beta-lactam 1.penicillin 2.Penicllinase-resistant Penicillin characteristics members • They are active against • . Staphylococci that produce • . penicillinase. • Isoxazolyl penicillin. • These pencillin are not • . hydrolyzed by beta- • lactamase. . • • .

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 2.Penicllinase-resistant Penicillin Therapeutic Uses &spectrum of activity Pharmacokinetics • Penicillinase resistant • Nafcillin is excreted by liver. are used solely in • therefore may be useful in Staphylococcal infection treating Staphylococcal resulting from organisms infection in patient with that resist natural renal failure. penicillins.

• These agents are less

potent than natural penicillin.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 2.Penicllinase-resistant Penicillin Adverse effects Significant interactions

• Hypersensitivity reactions. • Probencid increase blood • Methicillin may cause levels of these penicillin and nepherotoxicity and may be given concurrently intestinal nepharitis. for this purpose . • Oxacillin may be hepatotoxic. • Cross-reaction exist among Penicillinase resistant penicillin.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 3.Aminopenicillin (Broad-spectrum penicillins)

Important properties Members • They are semi-synethetic 1. . agents. 2. Amoxycillin. • They have a wider 3. bacampicillins antibacterial spectrum. • therefore they are known as (broad-spectrum penicillins).

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 3.Aminopenicillin (Broad-spectrum penicillins)

Properties Spectrum of activity 1. They have a broader • Antimicrobial activity is spectrum of activity than extended to include gram- natural penicillins & negative organisms such as penicillinase resistant Hemophilus influenzae, penicillins. Escherichia coli and Proteus • They are easily destroyed mirabilis by Staphylococcal penicillinase.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 3.Aminopenicillin (Broad -spectrum penicillins) Therapeutic uses

• They are used to treat gonococcal• infections, upper respiratory infections, uncomplicated urinary tract infections and otitis media caused by susceptible organisms

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 3.Aminopenicillin (Broad-spectrum penicillins) combination with Beta-alactamase inhibitor

• penicillanic acid sulphone. • produced by gram-negative 1. organisms. • .having beta lactamase inhibition • Combined with Ampicillin

• Beta -lactamase inhibitor 2.Clavulanic • Combined with . acid

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 3.Aminopenicillin (Broad-spectrum penicillins) Precautions and Monitoring Ampicillin versus amoxicillin effects • Oral amoxicillin is better • Hypersensitivity reactions absorbed than ampicillin • Diarrhoea which is most and gives a higher blood levels. common with ampicillin. • Therefore amoxycillin is less effective than ampicillin in shigellosis. • For ampicillin to be readily absorbed, it should be taken either one hour before or two hours after meals

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 4. Extended spectrum penicillin(antipseudomonal penicillin)

Important properties Members • These agents have the widest • , antibacterial spectrum of all • carbenicillin penicillins 1.Carboxpenicillins indanyl, • their spectrum of activity is • . similar to that of aminopenicillin, but also effective against Klebsiella • Azolocillins, ,Enterocbacter species, some • , bacteroid fragilis organisms, 2.( • piperacillins indole positive Proteus & Pseudomonas organisms.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 4. Extended spectrum penicillin(antipseudomonal penicillin) 1.carboxpenicillin 1.4.1.Carbenicillin:- 1.4.2.Carbenicillin indantyl

• It is used in treatment of • It shows a good absorption Pseudomonal infections but from gastro-intestinal tract, other penicillin such as acid stable therefore ticarcillin or are suitable for oral usually preferred now. administration. • It isn't absorbed from gastro-intestinal tract and should be given by injection.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 4. Extended spectrum penicillin(antipseudomonal penicillin)

Enhanced activity of Ticarcillin 1.4.3Ticarcillin combination Ticarcillin • Is similar to carbenicillin but give combination higher blood levels. with an • It is 2-4 times as active as carbenicillin against Pseudomonas aminoglycosides aeruginosa. . • It is often used in conjunction with an aminoglycosides and is given by injection as sodium salt ,since it isn't absorbed from gastro-intestinal tract. with clavulanic • When combined with it has acid. enhanced activity against organisms that resist ticarcillin alone.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 4. Extended spectrum penicillin(antipseudomonal penicillin) 2.Ureidopenicillins

Members Characteristics 1. . • Azlocillin and Piperacillin are 2. Piperacillin. 10times as active as carbencillin against Pseudomonas organisms 3.(Piperacillin + & more active than carbenicillin combination):- against Streptococcal organisms. • is a beta-lactamase inhibitor • Mezlocillin and pipercillin are that expands the spectrum of more active than carbenicillin activity to include some against Klebsiella organisms. organisms not sensitive to • Mezlocillin has a similar piperacillin alone.(if resistant is antimicrobial action to pipercillin. due to beta-lactamase • It activity against Pseudomonas production). aeureginosa is less than that of azlocillin or pipericillin.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 4. Extended spectrum penicillin(antipseudomonal penicillin) Therapeutic uses

• They are used mainly to • Systemic Pseudomonas treat serious infections aeruginosa infections is caused by gram-negative best treated with organisms:- antipseudomonal penicillin • e.g. sepsis, pneumonia. + aminoglycoside or for synergistic • infections of abdomen effect. • bone and soft tissues.

Karary university Dr. Eithar Karrar 2021 1.Cell wall inhibitors 4. Extended spectrum penicillin(antipseudomonal penicillin)Precautions & monitoring effects of I. Hypersensitivity reaction may occur. II. Carbenicillin & Ticarcillin may cause hypokalaemia. III. The high sodium content of of carbenicillin and ticarcillin may pose a danger to patients with congestive heart failure. IV. All agents inhibit platelet aggregations which may result in bleeding except Mezlocillin.

Karary university Dr. Eithar Karrar 2021 Expected learning outcome

• By the end of this part students should know regarding the following other types of penicillin’s:- • Their members. • Properties. • Spectrum of activity & therapeutic uses. • Side effects. • Drug drug interaction.

Karary university Dr. Eithar Karrar 2021