Nystatin is an antifungal medication used to treat fungal infections like oral thrush and skin infections. It works by killing fungi and preventing further infections. Nystatin is applied topically as a cream, ointment, or liquid and is not absorbed systemically. It acts by disrupting the fungal cell membrane. Common side effects are limited to gastrointestinal issues in high doses. Resistance is rare and develops slowly against most fungi.
2. Objectives
Upon completion of this presentation you will know:
1-what is nystatin.
2-pharmacodynamics of nystatin:
-site of action.
-mood of action.
3-pharmacokinetics of nystatin:
-absorption.
-metabolism.
-distribution.
-clearance.
4-Resistance.
5-Toxicity and sideffects.
3. Nystatin
Nystatin is an antifungal medicine. It's used to treat or prevent infections
caused by a fungus (or yeast). These include:
1-oral thrush.
2-skin infections.
-Nystatin kills the fungus and gets rid of the infection.
-It can also be used to stop you getting an infection.
-Nystatin is only available on prescription.
-It comes as a liquid (suspension) that you swirl around your mouth and
then swallow.
- It also comes mixed with steroids, antiseptics or antibacterials as a
cream or ointment.
6. Pharmacodynamic
Nystatin is an antifungal that is both fungistatic and fungicidal in
vitro against a wide variety of yeasts and yeast-like fungi.
Nystatin carries no significant activity against bacteria,
protozoa, or viruses. It carries significant systemic toxicity
and is currently unavailable in a formula appropriate for
systemic use - its efficacy is currently restricted, therefore, to
topical, oral, and gastrointestinal infections.
7. Mechanism of action
Nystatin is a channel-forming ionophore, meaning it exerts its
therapeutic effect via formation of a membrane-spanning pore in
the fungal plasma membrane. The formation of this pore results in
a change in membrane permeability that allows for leakage of
intracellular contents and the subsequent disruption of
electrochemical gradients necessary for proper cell function.
Selectivity for fungal cells over mammalian cells is due to
nystatin’s greater binding affinity for ergosterol, a key sterol found
in fungal cell walls, as opposed to its mammalian counterpart,
cholesterol.
8. pharmacokinetics
Absorption:
Systemic absorption of nystatin is minimal following oral administration , and
no detectable plasma concentrations are attained following topical or vaginal
administration.
Volume of distribution:
Nystatin is not absorbed into the systemic circulation and thus does not
undergo distribution.
Protein binding:
Nystatin is not absorbed into the systemic circulation and is therefore not
subject to plasma protein binding.
Metabolism:
Because nystatin undergoes little-to-no systemic absorption it is not
metabolized to any appreciable extent.
Route of elimination:
The majority of orally administered nystatin is eliminated unchanged in the
feces.
Clearance:
Not Available
9. Resistance
Resistance to nystatin is minimal in Candida albicans, but tends to develop
in other species of Candida such as C. tropicalis, can develop resistance to
nystatin, but resistance is rarely observed clinically.
10. Toxicity and sideffects
The oral LD50 in rats is 10 g/kg. There have been no reports of
serious toxic effects following overdosage of nystatin - doses in
excess of five million units daily have resulted in nausea and
gastrointestinal upset with no other associated effects.
12. introduction
Daptomycin is a cyclic lipopeptide
antibiotic used to treat complicated
skin and skin structure infections
by susceptible Gram-positive
bacteria and bacteremia due to
Staphylococcus aureus
13. pharmacodynamic
1.Mode of action
the proposed mechanism involves insertion of the
lipophilic daptomycin tail into the bacterial cell
membrane, causing rapid membrane depolarization
and a potassium ion efflux. This is followed by arrest
of DNA, RNA and protein synthesis resulting in
bacterial cell death
14. pharmacodynamic
2.Side effect
Like other antibacterial agents, daptomycin carries a
risk of severe hypersensitivity reactions, including
Drug Reaction with Eosinophilia and Systemic
Symptoms. There have been reports of myopathy,
rhabdomyolysis, and increased creatine
phosphokinase (CPK) levels in patients taking
daptomycin, which increased when daptomycin was
given more than once per day. Patients should be
monitored for CPK levels
15. pharmacokinetic
1.distributio
n
Daptomycin has a very small volume of distribution,
averaging ~0.1 L/kg in healthy adult subjects
independent of dose .he volume of distribution tends to
increase with decreasing renal function, being estimated
at ~0.2 L/kg in patients with severe renal impairment
16. pharmacokinetic
2.Absorbtion
No absorbtion / tacken intervens
3.Metabolism
studies using human hepatocytes suggest that daptomycin
effectively does not interact at all with the various CYP450
enzymes present in the liver.
4.Excretion
#Daptomycin is excreted primarily by the kidneys.
17. Drug resistance
1.Daptomycin hase concentration dependent
bactericidal activity against most gram-positive
pathogens, including those with multidrug resistance
It is not active against gram-negative organisms
because of its inability to penetrate the outer
membrane of the bacteria.
*Don't use daptomycin with s.pneomniae or other lunge
infections, why ❓❓