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Pharm407 > Lecture 1 part 2: pharmaceutical aspects of infections drug therapy > Flashcards

Lecture 1 part 2: pharmaceutical aspects of infections drug therapy Flashcards

1
Q

What infection characteristics influence drug delivery? (8 points)

A
  • site of infection
  • patient condition
  • acute vs. chronic infection
  • required dosage schedule
  • multi drug therapy
  • drug and dosage form availability
  • orphan drugs for rare diseases
  • drug resistance
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2
Q

Which two infection characteristics that influence drug delivery dictate the choice of administration?

A
  1. site of infection

2. patient condition

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3
Q

What causes super bugs?

A

-antibiotic resistance due to insufficient/excessive use

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4
Q

What are the possible causes of superbugs? (6 points)

A
  • self medication
  • uncontrolled availability of antibiotics
  • in appropriate prescribing
  • incomplete therapy (education, cost)
  • international travel (hard to control)
  • lower R&D investment -> few new antibiotics
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5
Q

What are the different formulation requirements for antibiotics that should be considered? (7 points)

A
  • short/long term therapy
  • systemic/targeted delivery
  • route of administration
  • patient acceptability
  • side effects
  • dose requirements
  • physicochemical characteristics of the active compound
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6
Q

What are the differences between benzylpenicillin, phenoxymethyl penicillin and procaine penicillin?

A
  1. benzyl = administered IV due to instability in GIT
  2. phenoxymethyl = can be adminsitered orally, but only achieves low blood concentrations. Not enough for systemic use, so used for local infections in stomach.
  3. Procaine= salt form of benzylpenicillin. Given IM to avoid pain at site of injection. Also provides SR release. Used for veterinary purposes.
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7
Q

What is OPAT?

A

outpatient parenteral antimicrobial therapy.

-parenteral antimicrobial therapy conducted in the community

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8
Q

What are the advantages of OPAT? (3 points)

A
  • reduces costs associated with in-patient stay
  • empowers patients
  • decreases morbidity
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9
Q

What is special about the formulation of antimicrobials used in OPAT?

A

They are extemporaneously compounded and placed in infusors. These are self administered by the patient.

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10
Q

What antibiotics are commonly used in OPAT? (7 points)

A
  • amoxicillin
  • vancomycin
  • ceftriaxone
  • flucloxacillin
  • benzylpenicillin
  • cefazolin
  • meropenem
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11
Q

what is amoxicillin?

A

-broad spectrum bacterialcidic beta lactam antibtiotic

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12
Q

How can amoxicillin be administered?

A
  • in bolus doses or as a continuous infusion

- pharmaceutical companies recommend administering as multiple bolus doses throughout the day

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13
Q

How do patients with severe infections achieve better outcomes with amoxicillin?

A

-if it is given as a continuous infusion

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14
Q

What is the stability data on amoxicillin like?

A

There is a lack of data on formulations packed in infusors

-some references say there is a significant concentration dependent degradation after 7 days

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15
Q

What are examples of novel drug deliver systems? (6 points)

A
  • micelles
  • vesicles
  • multifunctional dendritic polymers
  • nanospheres
  • nanocapsules
  • liquid crystals
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16
Q

What is Atrigel?

A
  • Patented drug delivery technology which enables site-specific and systemic drug delivery
  • consists of biodegradeable polymers dissolved in biocompatible carriers
  • forms solid implant upon contact with aqueous bodily fluids
17
Q

WHat is Atridox?

A
  • a sustained release formulation of doxycyline hyclate 10% using Atrigel delivery system
  • used to treat peridontal disease
  • available as 2 separate solutions of drug and polymer which are mixed before injection
  • liquid flows around infected tooth area and adapts to local morphology, hardening to waxy substance
  • Slow release of doxycycline up to 21 days
18
Q

What is Vitrasert?

A
  • Polymer based intravitreal implant formulation containing ganciclovir
  • for patients with AIDS related cytomegalovirus retinitis.
  • Consists of tablet coated with poly vinyl alcohol and ethylene vinyl acetate polymer
  • adminstration, removal or replacement requires surgery
  • releases drug over 5-8 months in slow release fashion.
19
Q

What is amphotericin B?

A
  • antifungal antibiotic that is administered by IV
  • pure drug is yellow/orange powder insoluble in water
  • initial formulations marketed as powder for injection
  • may cause nephrotoxicity
20
Q

What is Abelcet?

A
  • Amphotericin B liquid complex
  • has lipid conjugates ranging from 500-5000nm with 33% drug loading
  • ribbon like particles
  • uses DMPG and DMPC as carrier lipids
21
Q

What is Amphotec?

A
  • Amphtericon B formulated as sulfate complex colloidal dispersion.
  • carrier lipids include cholestryl sulfate
  • particles are disk shaped
  • approx 125nm in size with 50% drug loading.
22
Q

What is Ambisome?

A
  • liposomal amphotericin B formulation
  • various carrier lipids.
  • 100nm diameter spheres
  • liposomes hold drug in bilayer membrane
  • lower levels of side effects
  • offers highest plasma concentration and low clearance rates.
23
Q

What are examples of future novel formulations?

A
  • Aciclovir available as 200, 400, and 800mg dispersible tablets have complex dosing regimen
  • associated with GIT side effects such as nausea
  • poorly absorbed from the GIT
24
Q

What is Amikacin?

A
  • water soluble aminoglycoside
  • ribosomal protein synthesis inhibitor
  • used to treat pulmonary infections like CF
25
Q

What is Arikace?

A

-Developed to treat lung infections in patients with limited options e.g. CF, non-tuberculosis mycobacteria lung disease.

26
Q

What is special about Arikace?

A
  • enables assess to bacteria in infected tissues and macrophages
  • neutral charge in core allows it to travel through mucous and biofilm (which is negatively charged)
  • enters bacteria.
  • Bacteria may secrete agents which disrupt liposomal encapsulation thus releasing the drug.
27
Q

What are novel core-shell capsules?

A
  • encapsulated drug delivery system for recalcitrant UTI
  • uses gentamicin in PMSQ carrier
  • biocompatible and non toxic with high drug loading capacity
  • effectively penetrates bladder cells
  • provides SR of antibiotic
28
Q

What are charge switching polymeric nanoparticles?

A
  • formulations for targeted bacterial cell wall delivery of antibiotics
  • due to change in environment, ionisation etc. may change surface charge allowing it to enter the bacterium to exert its effect.

Pharm407 (5 decks)

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