Pharmacology Nystatin and Daptomycin .pptx

Drugs that cause leakage of cell membrane of the bacteria

1. NYSTATIN JARRAH NABIL ,TURKI KHALED

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.

4. oral thrush

5. skin infections

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 LD 50  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.

11. Daptomycin(antimicrobial drug) Ziad khaldon , Hazem khaled

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.distribution 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 ❓❓

18. References 1-Gd3nh.com https://mn.kees.jra7.com/t/G07369 2-Wikipedia https://ar.wikipedia.org/w/index.php?go=Go&search=nystatin&title 3-Drug bank https://go.drugbank.com/drugs/DB00646